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Sample records for activated duloxetine hydrochloride

  1. Study on fluorescence characteristics of duloxetine hydrochloride

    NASA Astrophysics Data System (ADS)

    Liu, Xiangping; Du, Yingxiang; Wu, Xiulan

    2008-12-01

    The fluorescence characteristics of duloxetine hydrochloride are studied in this paper. The fluorescence emission spectra of duloxetine demonstrate that intramolecular charge-transfer takes place between thiophene ring and napthalenyloxy group upon irradiation. The effects of excitation light, solvent system, variation of solution pH value, metal ions and vitamin C on the fluorescence spectra of duloxetine hydrochloride are elucidated, respectively. A spectrofluorometric method of quantitative determination of duloxetine in dosage form is reported for the first time, the linear range is 7.14 × 10 -8 mol/L to 1.43 × 10 -5 mol/L, the linear correlation coefficient r is equal to 0.9997, and the detection limit is 3.5 × 10 -8 mol/L. The accuracy and the precision are satisfactory.

  2. The Combination of Antidepressant Duloxetine with Piracetam in Mice does not Produce Enhancement of Nootropic Activity.

    PubMed

    Kale, Pravin Popatrao; Addepalli, Veeranjaneyulu; Sarkar, Amrita; Patel, Sonam; Savai, Jay

    2014-09-01

    There is a strong association between depression and memory impairment. The present study aims to assess the nootropic activity of duloxetine and piracetam combination. Male Swiss Albino mice were divided randomly into 4 groups. Treatment of normal saline (10 ml/kg), duloxetine (10 mg/kg), piracetam (100 mg/kg), and duloxetine (5 mg/kg) plus piracetam (50 mg/kg) were given through intra-peritoneal route to group I-IV, respectively. Transfer latency in elevated plus maze (EPM) and time spent in target quadrant in Morris water maze (MWM) were recorded. Estimation of brain monoamines in hippocampus, cerebral cortex, and whole brain were done using HPLC with fluorescence detector. Piracetam treated group showed significant decrease in transfer latency in EPM and increase in time spent in target quadrant recorded in MWM. Combination treated group failed to produce statistically significant nootropic effect in both EPM and MWM. Combination treated group failed to increase brain monoamine levels when compared against duloxetine and piracetam treated groups, separately. But there was exception of significant increase in norepinephrine levels in hippocampi when compared against duloxetine treated group. Results indicate no cognitive benefits with piracetam plus duloxetine combination. These findings can be further probed with the aim of understanding the interaction between duloxetine and piracetam as a future endeavor.

  3. Analysis of duloxetine hydrochloride and its related compounds in pharmaceutical dosage forms and in vitro dissolution studies by stability indicating UPLC.

    PubMed

    Rao, Dantu Durga; Sait, Shakil S; Reddy, A Malleswara; Chakole, Dinesh; Reddy, Y Ramakoti; Mukkanti, K

    2010-11-01

    A reproducible gradient reversed-phase ultra-performance liquid chromatographic method is developed for quantitative determination of duloxetine hydrochloride in pharmaceutical dosage forms. The method is also applicable for analysis of related substances and for study of in vitro dissolution profiles. Chromatographic separation is achieved on a 50 mm × 4.6 mm, 1.8 μm C-18 column. Mobile phase A contains a mixture of 0.01 M KH(2)PO(4) (pH 4.0) buffer, tetrahydro furan, and methanol in the ratio 67:23:10 (v/v/v), respectively, and mobile phase B contains a mixture of 0.01 M KH(2)PO(4), (pH 4.0) buffer, and acetonitrile in the ratio 60:40 (v/v), respectively. The flow rate is 0.6 mL/min, and the detection wavelength is monitored at 236 nm. Resolution of duloxetine hydrochloride and three potential impurities is greater than 2.0 for all pairs of components. The drug was subjected to ICH prescribed hydrolytic, oxidative, photolytic, and thermal stress conditions. Method is validated for linearity, specificity, accuracy, precision, ruggedness, and robustness.

  4. Clinical study of duloxetine hydrochloride combined with doxazosin for the treatment of pain disorder in chronic prostatitis/chronic pelvic pain syndrome: An observational study.

    PubMed

    Zhang, Mingxin; Li, Hanzhong; Ji, Zhigang; Dong, Dexin; Yan, Su

    2017-03-01

    To explore the safety and efficacy of the selective 5-serotonin and norepinephrine reuptake inhibitor duloxetine hydrochloride and alpha-adrenergic receptor blocker (alpha-blocker) doxazosin mesylate-controlled tablets in the treatment of pain disorder in chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS).In all, 150 patients were enrolled and 126 patients completed the study (41 patients in the doxazosin group, 41 patients in the sertraline group, and 44 patients in the duloxetine group). This was an open randomized 6-month study. CP/CPPS patients who met the diagnostic criteria were randomized into 3 groups. The patients in the duloxetine group received doxazosin 4 mg + duloxetine 30 mg once a day, and the dosage of duloxetine was increased to 60 mg after a week. The patients in the doxazosin group received doxazosin 4 mg once a day. The patients in the sertraline group received doxazosin 4 mg + sertraline 50 mg once a day. National Institutes of Health Chronic Prostatitis Symptom Index (NIH-CPSI) score, the short-form McGill Pain questionnaire (SF-MPQ), and the hospital anxiety and depression scale (HAD) were applied for evaluations during follow-up of 1, 3, and 6 months after treatment.There were slight positive significant correlations between NIH-CPSI scores and HAD scores, moderate positive significant correlations between the quality of life (QOL) and SF-MPQ, and slight positive significant correlations between HAD and QOL. The effective rate in the doxazosin group was 4.88%, 19.51%, and 56.10% after 1, 3, and 6 months, respectively (P < 0.05). The SF-MPQ score in the doxazosin group decreased to 1.80 ± 1.29, 2.66 ± 1.57, and 3.24 ± 1.67 after 1, 3, and 6 months, respectively (P < 0.05). The HAD score in the doxazosin group decreased to 2.24 ± 2.17, 4 ± 2.11, and 4.90 ± 2.62 after 1, 3, and 6 months, respectively (P < 0.05). The effective rate in the sertraline group was 9.76%, 36.59%, and 63

  5. Clinical study of duloxetine hydrochloride combined with doxazosin for the treatment of pain disorder in chronic prostatitis/chronic pelvic pain syndrome

    PubMed Central

    Zhang, Mingxin; Li, Hanzhong; Ji, Zhigang; Dong, Dexin; Yan, Su

    2017-01-01

    Abstract To explore the safety and efficacy of the selective 5-serotonin and norepinephrine reuptake inhibitor duloxetine hydrochloride and alpha-adrenergic receptor blocker (alpha-blocker) doxazosin mesylate-controlled tablets in the treatment of pain disorder in chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS). In all, 150 patients were enrolled and 126 patients completed the study (41 patients in the doxazosin group, 41 patients in the sertraline group, and 44 patients in the duloxetine group). This was an open randomized 6-month study. CP/CPPS patients who met the diagnostic criteria were randomized into 3 groups. The patients in the duloxetine group received doxazosin 4 mg + duloxetine 30 mg once a day, and the dosage of duloxetine was increased to 60 mg after a week. The patients in the doxazosin group received doxazosin 4 mg once a day. The patients in the sertraline group received doxazosin 4 mg + sertraline 50 mg once a day. National Institutes of Health Chronic Prostatitis Symptom Index (NIH-CPSI) score, the short-form McGill Pain questionnaire (SF-MPQ), and the hospital anxiety and depression scale (HAD) were applied for evaluations during follow-up of 1, 3, and 6 months after treatment.There were slight positive significant correlations between NIH-CPSI scores and HAD scores, moderate positive significant correlations between the quality of life (QOL) and SF-MPQ, and slight positive significant correlations between HAD and QOL. The effective rate in the doxazosin group was 4.88%, 19.51%, and 56.10% after 1, 3, and 6 months, respectively (P < 0.05). The SF-MPQ score in the doxazosin group decreased to 1.80 ± 1.29, 2.66 ± 1.57, and 3.24 ± 1.67 after 1, 3, and 6 months, respectively (P < 0.05). The HAD score in the doxazosin group decreased to 2.24 ± 2.17, 4 ± 2.11, and 4.90 ± 2.62 after 1, 3, and 6 months, respectively (P < 0.05). The effective rate in the sertraline group was 9.76%, 36

  6. Determination of duloxetine hydrochloride in the presence of process and degradation impurities by a validated stability-indicating RP-LC method.

    PubMed

    Raman, N V V S S; Harikrishna, K A; Prasad, A V S S; Reddy, K Ratnakar; Ramakrishna, K

    2010-03-11

    A stability-indicating gradient reverse phase liquid chromatographic purity and assay method for duloxetine hydrochloride (DUH) was developed and validated. DUH was subjected to the stress conditions and it is sensitive towards oxidative, acid and hydrolytic degradation. Successful separation of DUH from its two process impurities and one degradation impurity formed under stress conditions was achieved on a Symmetry C18, 250x4.6mm, 5microm column using a gradient mixture of solvent A (0.01M potassium dihydrogen orthophosphate having 0.2% triethyl amine, pH adjusted to 2.5 with orthophosphoric acid) and solvent B (20:80 v/v mixture of acetonitrile and methanol). The flow rate is 1ml/min and the detection wavelength is 230nm. The mass balance was found to be in the range of 99.2-99.7% in all the stressed conditions.

  7. Characterization of stress degradation products of duloxetine hydrochloride employing LC-UV/PDA and LC-MS/TOF studies.

    PubMed

    Chadha, Renu; Bali, Alka; Bansal, Gulshan

    2016-03-20

    Duloxetine HCl was subjected to forced degradation under conditions of hydrolysis (neutral, acidic and alkaline), oxidation, photolysis and thermal stress, as suggested in the ICH guideline Q1A(R2). The drug showed significant degradation under acidic, alkaline and aqueous hydrolytic as well as photolytic conditions. The drug remained stable under thermal and oxidative stress conditions. In total, seventeen degradation products (I-XVII) were formed under varied conditions, which could be separated by chromatography of respective degraded solutions on C18 (250 mm×4.6 mm; 5 μ, Nulceodur) column using isocratic elution method. Detection wavelength was selected as 290 nm. MS/TOF accurate mass studies were carried out to establish the complete fragmentation pathway of the drug and degradation products, which, in turn, was utilized in characterization of the products. The degradation pathway of the drug leading to generation of fifteen products I-X, XII-XIII, XV-XVII was postulated and this has not been reported so far.

  8. Effects of duloxetine on norepinephrine and serotonin transporter activity in healthy subjects.

    PubMed

    Chappell, Jill C; Eisenhofer, Graeme; Owens, Michael J; Haber, Harry; Lachno, D Richard; Dean, Robert A; Knadler, Mary Pat; Nemeroff, Charles B; Mitchell, Malcolm I; Detke, Michael J; Iyengar, Smriti; Pangallo, Beth; Lobo, Evelyn D

    2014-02-01

    Duloxetine selectively inhibits the serotonin (5-HT) and norepinephrine (NE) transporters (5-HTT and NET, respectively), as demonstrated in vitro and in preclinical studies; however, transporter inhibition has not been fully assessed in vivo at the approved dose of 60 mg/d. Here, the in vivo effects of dosing with duloxetine 60 mg once daily for 11 days in healthy subjects were assessed in 2 studies: (1) centrally (n = 11), by measuring concentrations of 5-hydroxyindoleacetic acid, 3,4-dihydroxyphenylglycol (DHPG), and NE in cerebrospinal fluid, and (2) versus escitalopram 20 mg/d (n = 32) in a 2-period crossover study by assessing the ΔDHPG/ΔNE ratio in plasma during orthostatic testing and by pharmacokinetic/pharmacodynamic modeling of reuptake inhibition using subjects' serum in cell lines expressing cloned human 5-HTT or NET. At steady state, duloxetine significantly reduced concentrations of DHPG and 5-hydroxyindoleacetic acid (P < 0.05), but not NE, in cerebrospinal fluid; DHPG was also decreased in plasma and urine. The ΔDHPG/ΔNE ratio in plasma decreased significantly more with duloxetine than escitalopram (65% and 21%, respectively; P < 0.0001). Ex vivo reuptake inhibition of 5-HTT was comparable (EC50 = 44.5 nM) for duloxetine and escitalopram, but duloxetine inhibited NET more potently (EC50 = 116 nM and 1044 nM, respectively). Maximal predicted reuptake inhibition for 5-HTT was 84% for duloxetine and 80% for escitalopram, and that for NET was 67% and 14%, respectively. In summary, duloxetine significantly affected 5-HT and NE turnover in the central nervous system and periphery; these effects presumably occurred via inhibition of reuptake by the 5-HTT and NET, as indicated by effects on functional reuptake inhibition ex vivo.

  9. Evaluation of anti-obesity activity of duloxetine in comparison with sibutramine along with its anti-depressant activity: an experimental study in obese rats.

    PubMed

    Chudasama, H P; Bhatt, P A

    2009-11-01

    5-HT and noradrenaline are important neurotransmitters that control increase in body mass and are involved in the pathophysiology of obesity and depression. Sibutramine, an established anti-obesity agent, and duloxetine, an anti-depressant agent, are serotonin noradrenaline reuptake inhibitors (SNRIs). The objective of the present study was to compare the anti-obesity effect of duloxetine with sibutramine along with its effect on blood pressure and depression in obese rats. The secondary objective of the study was to determine if a relationship exists between obesity and depression. Obesity was induced by high-fat diet (HFD) in healthy male Sprague-Dawley rats. After 5 weeks of feeding HFD, animals were overweight (17.57%) with high food intake (57.15%) in comparison with normal animals. These obese animals were treated with duloxetine (30 mg x kg(-1), p.o.) and sibutramine (5 mg x kg(-1), p.o.) for 4 weeks. Control animals were treated with duloxetine alone (30 mg x kg(-1), p.o.). Our results depict that duloxetine was as effective as sibutramine in reducing food intake, body mass, and relative adiposity, and increasing rectal temperature with an added advantage of decreasing blood pressure, which sibutramine failed to do. Besides reduction in body mass, unlike sibutramine, duloxetine improved depressive state as evaluated by despair swimming test, tail suspension test, and open field test, speculating its use as an anti-obesity agent in obese-depressive animals. Since obese control animals reflected decreased locomotor activity, a positive relationship can be speculated to exist between obesity and depression. Further studies on various antidepressant models are required to confirm this relationship.

  10. Duloxetine versus other anti-depressive agents for depression

    PubMed Central

    Cipriani, Andrea; Koesters, Markus; Furukawa, Toshi A; Nosè, Michela; Purgato, Marianna; Omori, Ichiro M; Trespidi, Carlotta; Barbui, Corrado

    2014-01-01

    Background Although pharmacological and psychological interventions are both effective for major depression, in primary and secondary care settings antidepressant drugs remain the mainstay of treatment. Amongst antidepressants many different agents are available. Duloxetine hydrochloride is a dual reuptake inhibitor of serotonin and norepinephrine and has been licensed by the Food and Drug Administration in the US for major depressive disorder (MDD), generalised anxiety disorder, diabetic peripheral neuropathic pain, fibromyalgia and chronic musculoskeletal pain. Objectives To assess the evidence for the efficacy, acceptability and tolerability of duloxetine in comparison with all other antidepressant agents in the acute-phase treatment of major depression. Search methods MEDLINE (1966 to 2012), EMBASE (1974 to 2012), the Cochrane Collaboration Depression, Anxiety and Neurosis Controlled Trials Register and the Cochrane Central Register of Controlled Trials up to March 2012. No language restriction was applied. Reference lists of relevant papers and previous systematic reviews were hand-searched. Pharmaceutical company marketing duloxetine and experts in this field were contacted for supplemental data. Selection criteria Randomised controlled trials allocating patients with major depression to duloxetine versus any other antidepressive agent. Data collection and analysis Two review authors independently extracted data and a double-entry procedure was employed. Information extracted included study characteristics, participant characteristics, intervention details and outcome measures in terms of efficacy, acceptability and tolerability. Main results A total of 16 randomised controlled trials (overall 5735 participants) were included in this systematic review. Of these, three trials were unpublished. We found 11 studies (overall 3304 participants) comparing duloxetine with one selective serotonin reuptake inhibitor (SSRI) (six studies versus paroxetine, three studies

  11. Maintaining efficacy in the treatment of diabetic peripheral neuropathic pain: role of duloxetine

    PubMed Central

    Zilliox, Lindsay; Russell, James W

    2010-01-01

    Introduction Neuropathy is one of the most frequent complications of diabetes. Of all the symptoms associated with diabetic neuropathy, pain has the largest impact on sleep and quality of life. In the past few years further medications have been added to the available therapies for neuropathic pain. One of these medications, duloxetine hydrochloride (duloxetine), is a balanced and potent selective serotonin and norepinephrine reuptake inhibitor. Methods Medline was searched from January 2005 to September 2009 using the key words duloxetine and peripheral neuropathy for clinical trials limited to human research published in English and duloxetine and pharmacology in the nervous system. Results Duloxetine has been shown to effectively reduce diabetic peripheral neuropathic pain compared to placebo at doses of 60 mg/day and 120 mg/day with minimal to moderate side effects. This effect is seen with minimal effects on glycemic control and without any clinically relevant effects on lipid control, or cardiovascular parameters. In addition, its efficacy and tolerability is comparable to other medications commonly used in the management of neuropathic pain. Furthermore, duloxetine performs favorably both in terms of quality of life and in cost utility analyses. Discussion and conclusion This article reviewed the issues related to management of diabetic peripheral neuropathic pain, the pharmacology and rationale for use of duloxetine, efficacy studies, and the safety and tolerability of treatment with duloxetine. Duloxetine is an acceptable initial or alternative treatment for patients with diabetic neuropathic pain. PMID:21437071

  12. Comparative antibacterial activities of temafloxacin hydrochloride (A-62254) and two reference fluoroquinolones.

    PubMed Central

    Hardy, D J; Swanson, R N; Hensey, D M; Ramer, N R; Bower, R R; Hanson, C W; Chu, D T; Fernandes, P B

    1987-01-01

    The in vitro and in vivo properties of a new 1-difluorophenyl-6-fluoroquinolone, temafloxacin hydrochloride (A-62254), were compared with those of difloxacin and ciprofloxacin. Temafloxacin hydrochloride was as active as ciprofloxacin and difloxacin against staphylococci and as active as ciprofloxacin and 2 twofold dilutions more active than difloxacin against streptococci. Against gram-negative enteric bacteria and Pseudomonas aeruginosa, temafloxacin hydrochloride was 2 twofold dilutions more active than difloxacin but 2 to 4 twofold dilutions less active than ciprofloxacin. The MICs of temafloxacin hydrochloride and difloxacin were increased by 2 to 5 twofold dilutions in urine at pH 6.5 compared with 4 to 5 twofold-dilution increases in the MICs of ciprofloxacin. The MICs of temafloxacin hydrochloride, difloxacin, and ciprofloxacin were increased by 1 to 3 twofold dilutions in serum. The MICs of temafloxacin hydrochloride, difloxacin, and ciprofloxacin were the same or within 1 to 2 twofold dilutions at pHs 6.5, 7.2, and 8.0. When administered orally in mouse protection tests, temafloxacin hydrochloride was as active as difloxacin and 5 to 10 times more active than ciprofloxacin against infections with Staphylococcus aureus and streptococci. Against infections with gram-negative enteric bacteria and P. aeruginosa, temafloxacin hydrochloride was as active as difloxacin and ciprofloxacin. Temafloxacin hydrochloride was three times less active than difloxacin but was five times more active than ciprofloxacin against infections with Salmonella typhimurium. Temafloxacin hydrochloride was as active as difloxacin and ciprofloxacin against P. aeruginosa and Proteus mirabilis pyelonephritis in mice. The peak serum concentration and serum half-life of temafloxacin hydrochloride in mice were approximately one-half and one-sixth, respectively, that of difloxacin after oral administration. The peak serum concentration of temafloxacin hydrochloride in mice after oral

  13. Duloxetine: a review of its use in the treatment of generalized anxiety disorder.

    PubMed

    Carter, Natalie J; McCormack, Paul L

    2009-01-01

    numerous metabolites, which are inactive, are mainly excreted in the urine. The mean elimination half-life of duloxetine is approximately 12 hours. Duloxetine is a substrate for CYP1A2 and CYP2D6 and a moderate inhibitor of CYP2D6. Concomitant use of duloxetine and potent CYP1A2 inhibitors should be avoided and duloxetine should be used with caution in patients receiving drugs that are extensively metabolized by CYP2D6, particularly those with a narrow therapeutic index. Duloxetine was effective in the short-term treatment of patients with primary GAD of at least moderate severity. In four randomized, double-blind, placebo-controlled, multicentre, phase III trials, duloxetine 60-120 mg once daily for 9 or 10 weeks was significantly more effective than placebo with regard to the primary endpoint of mean change in Hamilton Anxiety Rating Scale (HAM-A) total score from baseline to study endpoint. In addition, all other endpoints were generally improved from baseline to a greater extent with duloxetine 60-120 mg once daily than with placebo. Duloxetine also improved patient role functioning (assessed using Sheehan Disability Scale global impairment functioning scores), health-related quality of life and patient well-being compared with placebo. Duloxetine was effective in patients with GAD who were aged >/=65 years. Pooled results of data from the two short-term efficacy trials that also included an active comparator arm showed that the mean change in HAM-A scores with duloxetine relative to placebo were of the same magnitude as those with venlafaxine extended release versus placebo. Duloxetine 60-120 mg once daily was also more effective than placebo in preventing or delaying relapse in responders to duloxetine in a longer-term study. In this study, patients with GAD received duloxetine during a 26-week, open-label, acute treatment phase and responders were then randomized to continue on duloxetine or receive placebo during a 26-week, double-blind, continuation phase. Time to

  14. Duloxetine-related panic attacks.

    PubMed

    Sabljić, Vladimir; Rakun, Radmir; Ružić, Klementina; Grahovac, Tanja

    2011-03-01

    Side-effects arising on the grounds of antidepressant administration pose as a substantial obstacle hindering successful depressive disorder treatment. Side-effects, especially those severe or those manifested through dramatic clinical presentations such as panic attacks, make the treatment far more difficult and shake patients' trust in both the treatment and the treating physician. This case report deals with a patient experiencing a moderately severe depressive episode, who responded to duloxetine treatment administered in the initial dose of 30 mg per day with as many as three panic attacks in two days. Upon duloxetine withdrawal, these panic attacks ceased as well. The patient continued tianeptine and alprazolam treatment during which no significant side-effects had been seen, so that she gradually recovered. Some of the available literature sources have suggested the possibility of duloxetine administration to the end of generalised anxiety disorder and panic attack treatment. However, they are outnumbered by the contributions reporting about duloxetine-related anxiety, aggressiveness and panic attacks. In line with the foregoing, further monitoring of each and every duloxetine-administered patient group needs to be pursued so as to be able to evaluate treatment benefits and weigh them against risks of anxiety or panic attack onset.

  15. Duloxetine: a review of its use in the management of major depressive disorder in older adults.

    PubMed

    Dhillon, Sohita

    2013-01-01

    Duloxetine (Cymbalta(®)) is a selective serotonin norepinephrine reuptake inhibitor indicated for the treatment of major depressive disorder (MDD). This article reviews the therapeutic efficacy and tolerability of duloxetine in older adults with MDD and summarizes its pharmacological properties. Treatment with duloxetine significantly improved several measures of cognition, depression, anxiety, pain and health-related quality-of-life (HR-QOL) in older adults with MDD in two 8-week, double-blind, placebo-controlled trials. However, no significant improvements in measures of depression were observed at week 12 (primary endpoint) of a 24-week, double-blind trial, although symptoms of depression did improve significantly at earlier timepoints. Benefit of treatment was also observed during continued therapy in the 24-week study (i.e. after the 12-week primary endpoint) and in an open-label, 52-week study, with improvements being observed in some measures of depression, pain and HR-QOL. Duloxetine was generally well tolerated in these studies, with nausea, dizziness and adverse events reflecting noradrenergic activity (e.g. dry mouth, constipation) being the most common treatment-emergent adverse events during treatment for up to 52 weeks. Duloxetine therapy had little effect on cardiovascular parameters and bodyweight. Although further well designed and long-term studies in this patient population are required to confirm the efficacy of duloxetine and to compare it with that of other antidepressants, current evidence suggests that treatment with duloxetine may be beneficial in older adults with MDD.

  16. Photoacoustic imaging to detect rat brain activation after cocaine hydrochloride injection

    NASA Astrophysics Data System (ADS)

    Jo, Janggun; Yang, Xinmai

    2011-03-01

    Photoacoustic imaging (PAI) was employed to detect small animal brain activation after the administration of cocaine hydrochloride. Sprague Dawley rats were injected with different concentrations (2.5, 3.0, and 5.0 mg per kg body) of cocaine hydrochloride in saline solution through tail veins. The brain functional response to the injection was monitored by photoacoustic tomography (PAT) system with horizontal scanning of cerebral cortex of rat brain. Photoacoustic microscopy (PAM) was also used for coronal view images. The modified PAT system used multiple ultrasonic detectors to reduce the scanning time and maintain a good signal-to-noise ratio (SNR). The measured photoacoustic signal changes confirmed that cocaine hydrochloride injection excited high blood volume in brain. This result shows PAI can be used to monitor drug abuse-induced brain activation.

  17. Duloxetine for the treatment of fibromyalgia.

    PubMed

    Wright, Cheryl L; Mist, Scott D; Ross, Rebecca L; Jones, Kim D

    2010-09-01

    This article presents a brief review of the physiologic abnormalities seen in fibromyalgia, current theories of widespread pain, and treatment options, including emerging therapeutics, with a focus on the use of duloxetine to manage fibromyalgia symptoms. Major clinical trials that examine the efficacy and effectiveness of duloxetine to date are reviewed, and safety issues are discussed.

  18. Synergistic spermicidal activity of neem seed extract, reetha saponins and quinine hydrochloride.

    PubMed

    Garg, S; Doncel, G; Chabra, S; Upadhyay, S N; Talwar, G P

    1994-08-01

    In order to identify potent spermicidal agents which are free from the side effects of currently available agents, spermicidal activity of purified neem seeds extract (Praneem), reetha saponins and quinine hydrochloride was studied individually and in combination. Sander-Cramer test was used to assess the activity on human sperm. Under the test conditions, minimum effective spermicidal concentrations for Praneem, reetha saponins and quinine hydrochloride were 25%, 0.05% and 0.346%, respectively. At these concentrations, 100% of the sperm were immobilised within 20 seconds. A positive synergistic effect in the spermicidal activity of these components, if used in combination, was observed which implies the use of reduced concentrations of each to bring about the desired action. The selected combination formulated into a suitable dosage form is likely to offer dual benefit of a potent contraceptive and an antimicrobial preparation.

  19. Berberine hydrochloride attenuates lipopolysaccharide-induced endometritis in mice by suppressing activation of NF-κB signal pathway.

    PubMed

    Fu, Kaiqiang; Lv, Xiaopei; Li, Weishi; Wang, Yu; Li, Huatao; Tian, Wenru; Cao, Rongfeng

    2015-01-01

    Endometritis is a common disease in animal production and influences breeding all over the world. Berberine is one of the main alkaloids isolated from Rhizoma coptidis. Previous reports showed that berberine has anti-inflammatory potential. However, there have been a limited number of published reports on the anti-inflammatory effect of berberine hydrochloride on LPS-induced endometritis. The purpose of the present study was to investigate the effects of berberine hydrochloride on LPS-induced mouse endometritis. Berberine hydrochloride was administered intraperitoneally at 1h before and 12h after LPS induction. Then, a biopsy was performed, and uterine myeloperoxidase (MPO) and nitric oxide (NO) concentrations were determined. Tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) levels in the uterus homogenate were measured by ELISA. The extent of IκB-α and P65 phosphorylation was detected by Western blot. The results showed that berberine hydrochloride significantly attenuated neutrophil infiltration, suppressed myeloperoxidase activity and decreased NO, TNF-αand IL-1βproduction. Furthermore, berberine hydrochloride inhibited the phosphorylation of the NF-κB p65 subunit and the degradation of its inhibitor, IκBα. These findings suggest that berberine hydrochloride exerts potent anti-inflammatory effects on LPS-induced mouse endometritis and might be a potential therapeutic agent for endometritis.

  20. Effect of duloxetine, a norepinephrine and serotonin reuptake inhibitor, on sneeze-induced urethral continence reflex in rats.

    PubMed

    Miyazato, Minoru; Kaiho, Yasuhiro; Kamo, Izumi; Chancellor, Michael B; Sugaya, Kimio; de Groat, William C; Yoshimura, Naoki

    2008-07-01

    We investigated the effect of duloxetine, a norepinephrine (NE) and serotonin (5-HT) reuptake inhibitor, on the neurally evoked urethral continence reflex induced by sneezing in rats. To clarify the role of noradrenergic and serotonergic mechanisms in preventing stress urinary incontinence (SUI) during sneezing, we examined the effect of duloxetine followed by intrathecal (it) methiothepin maleate (5-HT receptor and alpha1-adrenoceptor antagonist) or terazosin or idazoxan (selective alpha1- and alpha2-adrenoceptor antagonists, respectively). Amplitude of urethral pressure responses during sneezing (A-URS), urethral baseline pressure (UBP) at the midurethra, and sneeze-induced leak point pressure (S-LPP) were measured in normal adult female rats and rats with SUI induced by vaginal distension (VD). In normal and VD rats, intravenous application of duloxetine (1 mg/kg) increased A-URS by 35% and 34% and UBP by 21% and 34%, respectively. Sneezing-induced fluid leakage from the urethral orifice was observed in VD rats but not in normal rats. S-LPP was increased from 39.1 to 92.2 cmH2O by intravenous duloxetine in incontinent VD rats. Duloxetine-mediated enhancement of A-URS was inhibited by terazosin but not methiothepin maleate (it). In addition, simultaneous intrathecal application of methiothepin and terazosin induced a reduction in A-URS during sneezing, which was not increased by intravenous duloxetine. However, the reduced A-URS after intrathecal application of methiothepin and terazosin returned to the control level when duloxetine (iv) was applied after intrathecal idazoxan administration. These results indicate that duloxetine can prevent SUI by facilitating noradrenergic and serotonergic systems in the spinal cord to enhance the sneeze-induced active urethral closure mechanism.

  1. Glucosamine hydrochloride

    MedlinePlus

    ... or it can be made in the laboratory. Glucosamine hydrochloride is one of several forms of glucosamine. It ... as supplements. These products may contain glucosamine sulfate, glucosamine hydrochloride, or N-acetyl-glucosamine. These different chemicals have ...

  2. Duloxetine

    MedlinePlus

    ... can develop in people who have diabetes) and fibromyalgia (a long-lasting condition that may cause pain, ... generalized anxiety disorder, the pain of diabetic neuropathy, fibromyalgia, or ongoing bone or muscle pain, it is ...

  3. Controlled release and antibacterial activity of tetracycline hydrochloride-loaded bacterial cellulose composite membranes.

    PubMed

    Shao, Wei; Liu, Hui; Wang, Shuxia; Wu, Jimin; Huang, Min; Min, Huihua; Liu, Xiufeng

    2016-07-10

    Bacterial cellulose (BC) is widely used in biomedical applications. In this study, we prepared an antibiotic drug tetracycline hydrochloride (TCH)-loaded bacterial cellulose (BC) composite membranes, and evaluated the drug release, antibacterial activity and biocompatibility. The structure and morphology of the fabricated BC-TCH composite membranes were characterized using scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR). The TCH release results show that the incorporation of BC matrix to load TCH is able to control the release. In vitro antibacterial assay demonstrate that the developed BC-TCH composites displayed excellent antibacterial activity solely associated with the loaded TCH drug. More importantly, the BC-TCH composite membranes display good biocompatibility. These characteristics of BC-TCH composite membranes indicate that they may successfully serve as wound dressings and other medical biomaterials.

  4. Is there a place for duloxetine?

    PubMed

    2007-04-01

    Duloxetine, a combined serotonin and norepinephrine reuptake inhibitor, is licensed in the UK under two brand names for a total of three different indications. It is available as Cymbalta (jointly promoted by Boehringer Ingelheim and Lilly) for the treatment of patients with major depression, or with diabetic peripheral neuropathic pain; and as Yentreve (Lilly) for the treatment of women with "moderate to severe" stress urinary incontinence. Here we consider whether duloxetine has a role in the treatment of patients with any of these conditions.

  5. Validated spectrophotometric method for the determination, spectroscopic characterization and thermal structural analysis of duloxetine with 1,2-naphthoquinone-4-sulphonate

    NASA Astrophysics Data System (ADS)

    Ulu, Sevgi Tatar; Elmali, Fikriye Tuncel

    2012-03-01

    A novel, selective, sensitive and simple spectrophotometric method was developed and validated for the determination of the antidepressant duloxetine hydrochloride in pharmaceutical preparation. The method was based on the reaction of duloxetine hydrochloride with 1,2-naphthoquinone-4-sulphonate (NQS) in alkaline media to yield orange colored product. The formation of this complex was also confirmed by UV-visible, FTIR, 1H NMR, Mass spectra techniques and thermal analysis. This method was validated for various parameters according to ICH guidelines. Beer's law is obeyed in a range of 5.0-60 μg/mL at the maximum absorption wavelength of 480 nm. The detection limit is 0.99 μg/mL and the recovery rate is in a range of 98.10-99.57%. The proposed methods was validated and applied to the determination of duloxetine hydrochloride in pharmaceutical preparation. The results were statistically analyzed and compared to those of a reference UV spectrophotometric method.

  6. Vortioxetine, but not escitalopram or duloxetine, reverses memory impairment induced by central 5-HT depletion in rats: evidence for direct 5-HT receptor modulation.

    PubMed

    Jensen, Jesper Bornø; du Jardin, Kristian Gaarn; Song, Dekun; Budac, David; Smagin, Gennady; Sanchez, Connie; Pehrson, Alan Lars

    2014-01-01

    Depressed patients suffer from cognitive dysfunction, including memory deficits. Acute serotonin (5-HT) depletion impairs memory and mood in vulnerable patients. The investigational multimodal acting antidepressant vortioxetine is a 5-HT3, 5-HT7 and 5-HT1D receptor antagonist, 5-HT1B receptor partial agonist, 5-HT1A receptor agonist and 5-HT transporter (SERT) inhibitor that enhances memory in normal rats in novel object recognition (NOR) and conditioned fear (Mørk et al., 2013). We hypothesized that vortioxetine's 5-HT receptor mechanisms are involved in its memory effects, and therefore investigated these effects in 5-HT depleted rats. Four injections of the irreversible tryptophan hydroxylase inhibitor 4-chloro-dl-phenylalanine methyl ester hydrochloride (PCPA, 86mg/kg, s.c.) induced 5-HT depletion, as measured in hippocampal homogenate and microdialysate. The effects of acute challenge with vortioxetine or the 5-HT releaser fenfluramine on extracellular 5-HT were measured in PCPA-treated and control rats. PCPA's effects on NOR and spontaneous alternation (SA) performance were assessed along with the effects of acute treatment with 5-hydroxy-l-tryptophan (5-HTP), vortioxetine, the selective 5-HT reuptake inhibitor escitalopram, or the 5-HT norepinephrine reuptake inhibitor duloxetine. SERT occupancies were estimated by ex vivo autoradiography. PCPA depleted central 5-HT by >90% in tissue and microdialysate, and impaired NOR and SA performance. Restoring central 5-HT with 5-HTP reversed these deficits. At similar SERT occupancies (>90%) vortioxetine, but not escitalopram or duloxetine, restored memory performance. Acute fenfluramine significantly increased extracellular 5-HT in control and PCPA-treated rats, while vortioxetine did so only in control rats. Thus, vortioxetine restores 5-HT depletion impaired memory performance in rats through one or more of its receptor activities.

  7. Functional photoacoustic imaging to observe regional brain activation induced by cocaine hydrochloride

    NASA Astrophysics Data System (ADS)

    Jo, Janggun; Yang, Xinmai

    2011-09-01

    Photoacoustic microscopy (PAM) was used to detect small animal brain activation in response to drug abuse. Cocaine hydrochloride in saline solution was injected into the blood stream of Sprague Dawley rats through tail veins. The rat brain functional change in response to the injection of drug was then monitored by the PAM technique. Images in the coronal view of the rat brain at the locations of 1.2 and 3.4 mm posterior to bregma were obtained. The resulted photoacoustic (PA) images showed the regional changes in the blood volume. Additionally, the regional changes in blood oxygenation were also presented. The results demonstrated that PA imaging is capable of monitoring regional hemodynamic changes induced by drug abuse.

  8. Associated with intrathecal baclofen treatment and duloxetine in patients with multiple sclerosis.

    PubMed

    Ranieri, M; Putignano, P; Fiore, P; Santamato, A; Megna, G; Bellomo, R G; Cristella, G; Saggini, R; Megna, M

    2012-01-01

    Baclofen is now used in treatment of patients with severe spasticity secondary to neurological diseases through the direct infusion of the drug into the subarachnoid space with an implanted programmable pump. Among patients whose quality of life improved after the use of intrathecal systems, a very important role belongs to people with multiple sclerosis (MS): a disease that due to a great variety of symptoms and signs, seriously affects the activities of daily living. Among the clinical manifestations of MS are also found mental health problems including depression mood. The drugs most commonly offered, for treatment of depression in patients with MS, are selective serotonin reuptake inhibitors (SSRIs), reuptake inhibitors of serotonin and norepinephrine (SNRIs) and tricyclic antidepressants (TCA). Duloxetine presents a high affinity for transporters reuptake of serotonin and noradrenalin, and exerts its activity on both molecules. In addiction, Duloxetine has demonstrated very effective in treatment of depressive disorders of mood as demonstrated by scientific evidences about the utility of Duloxetine in the modulation of painful physical symptoms associated with depression and in treatment of pain associated with diabetic neuropathy. The purpose of our study is to evaluate the effects of antidepressant therapy with duloxetine, 60 mg/day in 7 patients with multiple sclerosis treated with intrathecal baclofen for spastic modulation of tone. The experience we gained, according to data from several multicenter trials confirmed the efficacy of Baclofen intrathecally administered, especially with regards to modulation of spasticity. Our study also showed, although the limitations of a small sample size still, a good clinical response to combined treatment Baclofen intrathecal/duloxetine 60 mg/day.

  9. Duloxetine Inhibits Microglial P2X4 Receptor Function and Alleviates Neuropathic Pain after Peripheral Nerve Injury

    PubMed Central

    Yamashita, Tomohiro; Yamamoto, Shota; Zhang, Jiaming; Kometani, Miho; Tomiyama, Daisuke; Kohno, Keita; Tozaki-Saitoh, Hidetoshi; Inoue, Kazuhide; Tsuda, Makoto

    2016-01-01

    P2X4 receptors (P2X4R) are a family of ATP-gated non-selective cation channels. We previously demonstrated that activation of P2X4R in spinal microglia is crucial for neuropathic pain, a highly debilitating chronic pain condition, suggesting that P2X4R is a potential therapeutic target for treating neuropathic pain. Thus, the identification of a compound that has a potent inhibitory effect on P2X4R is an important clinical challenge. In the present study, we screened a chemical library of clinically approved drugs and show for the first time that duloxetine, a serotonin and noradrenaline reuptake inhibitor, has an inhibitory effect on rodent and human P2X4R. In primary cultured microglial cells, duloxetine also inhibited P2X4R-, but not P2X7R-, mediated responses. Moreover, intrathecal administration of duloxetine in a model of neuropathic pain produced a reversal of nerve injury-induced mechanical allodynia, a cardinal symptom of neuropathic pain. In rats that were pretreated with a serotonin-depleting agent and a noradrenaline neurotoxin, the antiallodynic effect of duloxetine was reduced, but still remained. Based on these results, we suggest that, in addition to duloxetine’s primary inhibitory action on serotonin and noradrenaline transporters, an inhibitory effect on P2X4R may be involved at least in part in an antiallodynic effect of intrathecal duloxetine in a model of neuropathic pain. PMID:27768754

  10. Novel glucosamine hydrochloride-rectorite nanocomposites with antioxidant and anti-ultraviolet activity

    NASA Astrophysics Data System (ADS)

    Wang, Xiaoying; Liu, Bo; Li, Xiang; Sun, Runcang

    2012-12-01

    In this study, an attempt was made to prepare novel D-glucosamine hydrochloride-rectorite (DGH-REC) nanocomposites with improved antioxidant and anti-ultraviolet activity via the solution-intercalation method. The structure and morphology of DGH-REC nanocomposites were characterized by XRD, TEM, 13C CP/MAS NMR, FT-IR, XPS and SEM. The results showed that the interlayer distance of REC was enlarged after intercalation of DGH; the largest value reached 11.76 nm, and in this case exfoliation of the REC layer was observed. Moreover, most strong crystals of DGH were greatly disrupted while two other weak crystals of DGH were stronger after intercalation of DGH into REC. More importantly, it was found that DGH-REC nanocomposites showed pronounced antioxidant activity, in contrast with DGH, and the nanocomposites had anti-ultraviolet capacity, which was not observed in DGH. Furthermore, the nanocomposites did not show apparent cytotoxicity. Therefore, DGH-REC nanocomposites have great potential in health or functional food application as compared to DGH.

  11. Synthesis and characterization of pharmaceutical surfactant templated mesoporous silica: Its application to controlled delivery of duloxetine

    SciTech Connect

    Mani, Ganesh; Pushparaj, Hemalatha; Peng, Mei Mei; Muthiahpillai, Palanichamy; Udhumansha, Ubaidulla; Jang, Hyun Tae

    2014-03-01

    Graphical abstract: - Highlights: • Usefulness of dual pharmaceutical surfactants in silica synthesis was evaluated. • Effects of concentration of secondary template (Tween-40) were studied. • Effects of fixed solvothermal condition on mesostructure formation were studied. • Duloxetine drug loading capability was studied. • Sustained release of duloxetine was evaluated. - Abstract: A new group of mesoporous silica nanoparticles (MSNs) were synthesized using combination pharmaceutical surfactants, Triton X-100 and Tween-40 as template and loaded with duloxetine hydrochloride (DX), for improving the sustained release of DX and patterns with high drug loading. Agglomerated spherical silica MSNs were synthesized by sol–gel and solvothermal methods. The calcined and drug loaded MSNs were characterized using X-ray diffraction (XRD), Braunner–Emmett–Teller (BET), thermogravimetric analysis (TGA), Fourier-transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), diffuse reflectance ultraviolet–visible (DRS-UV–vis) spectroscopy. MSNs with high surface area and pore volume were selected and studied for their DX loading and release. The selected MSNs can accommodate a maximum of 34% DX within it. About 90% was released at 200 h and hence, the synthesized MSNs were capable of engulfing DX and sustain its release. Further form the Ritger and Peppas, Higuchi model for mechanism drug release from all the MSN matrices follows anomalous transport or Non-Fickian diffusion with the ‘r’ and ‘n’ value 0.9 and 0.45 < n < 1, respectively. So, from this study it could be concluded that the MSNs synthesized using pharmaceutical templates were better choice of reservoir for the controlled delivery of drug which requires sustained release.

  12. Spectrofluorimetric determination of 3-methylflavone-8-carboxylic acid, the main active metabolite of flavoxate hydrochloride in human urine

    NASA Astrophysics Data System (ADS)

    Zaazaa, Hala E.; Mohamed, Afaf O.; Hawwam, Maha A.; Abdelkawy, Mohamed

    2015-01-01

    A simple, sensitive and selective spectrofluorimetric method has been developed for the determination of 3-methylflavone-8-carboxylic acid as the main active metabolite of flavoxate hydrochloride in human urine. The proposed method was based on the measurement of the native fluorescence of the metabolite in methanol at an emission wavelength 390 nm, upon excitation at 338 nm. Moreover, the urinary excretion pattern has been calculated using the proposed method. Taking the advantage that 3-methylflavone-8-carboxylic acid is also the alkaline degradate, the proposed method was applied to in vitro determination of flavoxate hydrochloride in tablets dosage form via the measurement of its corresponding degradate. The method was validated in accordance with the ICH requirements and statistically compared to the official method with no significant difference in performance.

  13. Spectrofluorimetric determination of 3-methylflavone-8-carboxylic acid, the main active metabolite of flavoxate hydrochloride in human urine.

    PubMed

    Zaazaa, Hala E; Mohamed, Afaf O; Hawwam, Maha A; Abdelkawy, Mohamed

    2015-01-05

    A simple, sensitive and selective spectrofluorimetric method has been developed for the determination of 3-methylflavone-8-carboxylic acid as the main active metabolite of flavoxate hydrochloride in human urine. The proposed method was based on the measurement of the native fluorescence of the metabolite in methanol at an emission wavelength 390 nm, upon excitation at 338 nm. Moreover, the urinary excretion pattern has been calculated using the proposed method. Taking the advantage that 3-methylflavone-8-carboxylic acid is also the alkaline degradate, the proposed method was applied to in vitro determination of flavoxate hydrochloride in tablets dosage form via the measurement of its corresponding degradate. The method was validated in accordance with the ICH requirements and statistically compared to the official method with no significant difference in performance.

  14. Development of topical hydrogels of terbinafine hydrochloride and evaluation of their antifungal activity.

    PubMed

    Çelebi, Nevin; Ermiş, Seda; Özkan, Semiha

    2015-04-01

    The purpose of this study was to prepare hydrogels and microemulsion (ME)-based gel formulations containing 1% terbinafine hydrochloride (TER-HCL) and to evaluate the use of these formulations for the antifungal treatment of fungal infections. Three different hydrogel formulations were prepared using chitosan, Carbopol® 974 and Natrosol® 250 polymers. A pseudo-ternary phase diagram was constructed, and starting from ME formulation, a ME gel form containing 1% Carbopol 974 was prepared. We also examined the characteristic properties of the prepared hyrogels. The physical stability of hydrogels and the ME -based gels were evaluated after storage at different temperatures for a period of 3 months. The release of TER-HCL from the gels and the commercial product (Lamisil®) was carried out by using a standard dialysis membrane in phosphate buffer (pH 5.2) at 32 °C. The results of the in vitro release study showed that the Natrosol gel released the highest amount of drug, followed by Carbopol gel, chitosan gel, commercial product, and the microoemulsion-based gel in that order. In vitro examination of antifungal activity revealed that all the prepared and commercial products were effective against Candida parapsilosis, Penicillium, Aspergillus niger and Microsporum. These results indicate that the Natrosol®-based hydrogel is a good candidate for the topical delivery of TER-HCL.

  15. Duloxetine in the management of diabetic peripheral neuropathic pain

    PubMed Central

    Ormseth, Michelle J; Scholz, Beth A; Boomershine, Chad S

    2011-01-01

    Diabetic neuropathy affects up to 70% of diabetics, and diabetic peripheral neuropathic pain (DPNP) is the most common and debilitating of the diabetic neuropathies. DPNP significantly reduces quality of life and increases management costs in affected patients. Despite the impact of DPNP, management is poor with one-quarter of patients receiving no treatment and many treated with medications having little or no efficacy in managing DPNP. Duloxetine is one of two drugs approved by the United States Food and Drug Administration for DPNP management. Duloxetine is a serotonin and norepinephrine reuptake inhibitor (SNRI) proven safe, effective, and cost-saving in reducing DPNP symptoms at a dose of 60 mg/day. Duloxetine doses greater than 60 mg/day for DPNP management are not recommended since they are no more efficacious and associated with more side effects; addition of pregabalin or gabapentin for these patients may be beneficial. Side effects of duloxetine are generally mild and typical for the SNRI class including nausea, dizziness, somnolence, fatigue, sweating, dry mouth, constipation, and diarrhea. Given its other indications, duloxetine is a particularly good choice for DPNP treatment in patients with coexisting depression, anxiety, fibromyalgia, or chronic musculoskeletal pain. Duloxetine treatment had no clinically significant effect on glycemic control and did not increase the risk of cardiovascular events in diabetes patients. However, duloxetine use should be avoided in patients with hepatic disease or severe renal impairment. Given its safety, efficacy, and tolerability, duloxetine is an excellent choice for DPNP treatment in many patients. PMID:21845034

  16. LASSBio-1829 Hydrochloride: Development of a New Orally Active N-Acylhydrazone IKK2 Inhibitor with Anti-inflammatory Properties.

    PubMed

    Guedes, Isabella A; Freitas, Rosana H C N; Cordeiro, Natália M; do Nascimento, Thaís S; Valerio, Tayna S; Fernandes, Patrícia D; Dardenne, Laurent E; Fraga, Carlos A M

    2016-01-19

    Inhibitor of nuclear factor κB kinase 2 (IKK2) is suggested to be a potential target for the development of novel anti-inflammatory and anticancer drugs. In this work, we applied structure-based drug design to improve the potency of the inhibitor (E)-N'-(4-nitrobenzylidene)-2-naphthohydrazide (LASSBio-1524, 1 a: IC50 =20 μm). The molecular model built for IKK2 together with the docking methodology employed were able to provide important and consistent information with respect to the structural and chemical inhibitor characteristics that may confer potency to IKK2 inhibitors, providing important guidelines for the development of a new N-acylhydrazone (NAH) derivative. (E)-N'-(4-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzylidene)-2-naphthohydrazide hydrochloride (LASSBio-1829 hydrochloride, 10) is a 7-azaindole NAH able to inhibit IKK2 with an IC50 value of 3.8 μm. LASSBio-1829 hydrochloride was found to be active in several pharmacological inflammation tests in vivo, showing its potential as an anti-inflammatory prototype.

  17. Duloxetine in the treatment of generalized anxiety disorder.

    PubMed

    Norman, Trevor R; Olver, James S

    2008-12-01

    Duloxetine, a medication with effects on both serotonin and noradrenaline transporter molecules, has recently been approved for the treatment of generalized anxiety disorder. The evidence for its efficacy lies in a limited number of double blind, placebo controlled comparisons. Statistically significant improvements in the Hamilton Anxiety Rating Scale from baseline were demonstrated in all studies at doses of 60 to 120 mg per day. The significance of such changes in terms of clinical improvements compared to placebo is less certain, particularly when the effect size of the change is calculated. In comparative trials with venlafaxine, duloxetine was as effective in providing relief of anxiety symptoms. In addition to improvements in clinical symptoms duloxetine has also been associated with restitution of role function as measured by disability scales. Duloxetine use is associated with nausea, dizziness, dry mouth, constipation, insomnia, somnolence, hyperhidrosis, decreased libido and vomiting. These treatment emergent side effects were generally of mild to moderate severity and were tolerated over time. Using a tapered withdrawal schedule over two weeks in the clinical trials, duloxetine was associated with only a mild withdrawal syndrome in up to about 30% of patients compared to about 17% in placebo treated patients. Duloxetine in doses of up to 200 mg twice daily did not prolong the QTc interval in healthy volunteers. Like other agents with dual neurotransmitter actions duloxetine reduces the symptoms of generalized anxiety disorder in short term treatments. Further evidence for its efficacy and safety in long term treatment is required.

  18. Comparison of neurogenic effects of fluoxetine, duloxetine and running in mice

    PubMed Central

    Marlatt, Michael W.; Lucassen, Paul J.; van Praag, Henriette

    2010-01-01

    Hippocampal neurogenesis can be regulated by extrinsic factors, such as exercise and antidepressants. While there is evidence that the serotonin re-uptake inhibitor (SSRI) fluoxetine (Prozac) enhances neurogenesis, the new dual serotonin/noradrenaline reuptake inhibitor (SNRI) duloxetine has not been evaluated in this context. In addition, it is unclear whether effects of antidepressants and running on cell genesis and behavior are of similar magnitude in mice. Here,we assessed neurogenesis and open field behavior in 2 month old female C57Bl/6 mice after 28 days of treatment with either fluoxetine (18 mg/kg), duloxetine (2, 6 or 18 mg/kg) or exercise. New cell survival, as measured by 5-bromo-2´-deoxyuridine (BrdU) labeled cells, was enhanced by 200% in the running group only. Both running and fluoxetine, but not duloxetine, increased the percentage of new cells that became neurons. In the open field test, animals treated with either drug spent less time in the center than controls and runners. In addition, fluoxetine treatment resulted in reduced locomotor activity. Together, these data not only show that the neurogenic response to exercise is much stronger than to antidepressants, but also imply a low likelihood that reported effects of these two drugs on anxiety are mediated by adult neurogenesis in C57Bl/6 mice. PMID:20381469

  19. Parkinsonism secondary to duloxetine use: a case report

    PubMed Central

    Bayrak, Arzu; Cetin, Bugra; Meteris, Handan; Kesebir, Sermin

    2015-01-01

    In literature, there are more than hundred cases of extrapyramidal symptoms (EPS) associated with selective serotonin reuptake intibitors (SSRI) whereas EPS case reports associated with serotonin noradrenaline reuptake inhibitors (SNRI) are in a relatively small number. A SNRI group drug duloxetine that is used for indication of major depression since 2004 is a double acting antidepressant that acts by blocking serotonin and noradrenaline reuptake. Side effects of duloxetine on extrapyramidal system are not expected due to low affinity to D2 receptors. In this case, report manifestations of parkinsonism developed in a patient who used duloxetine for major depression are presented. Since any duloxetine induced EPS case has not reported so far, we have thought that this case can contribute to the literature. PMID:28058376

  20. A case of retrobulbar optic neuritis caused by duloxetine.

    PubMed

    Bicer, Tolga; Kosker, Mustafa; Celikay, Osman; Gurdal, Canan

    2016-09-01

    Psychotropic medications may cause many ocular adverse effects including toxic optic neuropathy. We present a unique case of a 44-year-old woman using duloxetine who presented with unilateral visual loss due to retrobulbar neuritis. Physicians and patients should be alerted to this potential side effect. To the best of our knowledge, this is the first case of developing retrobulbar neuritis related to duloxetine usage.

  1. The safety of duloxetine during pregnancy and lactation.

    PubMed

    Andrade, Chittaranjan

    2014-12-01

    Depression is common in women, especially during pregnancy and the postpartum period. Untreated depression is associated with many adverse gestational outcomes. It is therefore important to know about the safety of different antidepressant drugs during pregnancy and lactation so that informed decisions can be made regarding treatment. This article summarizes published literature on the subject with regard to duloxetine, an antidepressant with serotonin-norepinephrine reuptake inhibition properties. In general, it appears that the use of duloxetine during pregnancy is associated with an increase in the risk of spontaneous abortion, but no increase in other adverse outcomes, such as major fetal malformations. Late-pregnancy exposure to duloxetine may be associated with poor neonatal adaptation syndrome, but the magnitude of this risk is not known. Infant exposure to duloxetine in breast milk is less than 1% of the maternal weight-adjusted dose, suggesting that duloxetine can be safely administered to a woman who is breastfeeding her infant. In general, the very limited data available on the subject do not uncover a signal that the use of duloxetine during pregnancy or lactation increases the risk of adverse outcomes.

  2. Implications of Pain in Generalized Anxiety Disorder: Efficacy of Duloxetine

    PubMed Central

    Hartford, James T.; Endicott, Jean; Kornstein, Susan G.; Allgulander, Christer; Wohlreich, Madelaine M.; Russell, James M.; Perahia, David G. S.; Erickson, Janelle S.

    2008-01-01

    Objective: To conduct a post hoc evaluation of the prevalence of clinically significant pain and the efficacy of duloxetine in patients with generalized anxiety disorder (GAD) and concurrent pain. Method: Data from two 9- to 10-week double-blind, placebo-controlled, randomized clinical trials of duloxetine (60 to 120 mg) in DSM-IV–defined GAD were analyzed (study 1 was conducted from July 2004 to September 2005; study 2 was conducted from August 2004 to June 2005). Efficacy was assessed with the Hamilton Rating Scale for Anxiety (HAM-A), visual analog scales (VAS) for pain, the Hospital Anxiety Depression Scale (HADS), the Clinical Global Impressions-Improvement of Illness (CGI-I) scale, the Patient Global Impressions-Improvement (PGI-I) scale, and the Sheehan Disability Scale (SDS) global functional impairment scale. Results: Of 840 patients randomly assigned to treatment, 61.3% (302 duloxetine, 213 placebo) had VAS scores ≥ 30 mm on at least 1 of the pain scales, indicating clinically significant pain. Among those patients with concurrent pain at baseline, change from baseline to endpoint in the HAM-A total score (42.9% change in mean scores for duloxetine, 31.4% for placebo), HADS anxiety scale (40.3% vs. 22.8%), HADS depression scale (36.1% vs. 20.5%), HAM-A psychic factor (45.9% vs. 29.9%), and SDS global functional improvement score (45.5% vs. 22.1%) was significantly (all p's < .001) greater for duloxetine compared with placebo. Improvement on the CGI-I (p = .003) and PGI-I (p < .001) was also significantly greater for duloxetine. Response (HAM-A total score decrease ≥ 50%) (49% vs. 29%) and remission (HAM-A total score ≤ 7 at endpoint) (29% vs. 18%) rates were significantly greater for duloxetine compared with placebo (p < .001 and p = .041, respectively). Duloxetine demonstrated statistically significantly greater reduction in pain on all 6 VAS pain scales (all p's < .001 except headaches with p < .002) (for duloxetine, percent change in means from

  3. Effects of benidipine hydrochloride on autonomic nervous activity in hypertensive patients with high- and low-salt diets.

    PubMed

    Nomura, Masahiro; Nakaya, Yutaka; Uemura, Eiko; Sawa, Yuko; Iga, Akiko; Kageyama, Norihito; Nakayama, Toru; Kusunoki, Kanji; Kawano, Tomohito; Katoh, Kansei; Okamoto, Hiroshi; Nishikado, Akiyoshi; Saito, Ken; Ito, Susumu

    2003-01-01

    The effects of benidipine hydrochloride (CAS 91559-74-5, Coniel) on autonomic nervous activity in hypertensive patients with high- and low-salt diets were investigated. Six patients having a urinary sodium excretion of 80 mEq/day or less (low salt group) and 6 patients having a urinary sodium excretion of 200 mEq/day or more (high salt group) were orally given benidipine hydrochloride (4 mg). Before and four weeks after the treatment with benidipine, 24-h circadian variation in blood pressure and 24-h Holter electrocardiogram (ECG) were recorded. The low frequency power spectrum of heart rate (LF power; 0.04-0.15 Hz), high frequency power spectrum of heart rate (HF power; 0.15-0.40 Hz), and the ratio of LF to HF (LF/HF) were calculated, and these parameters were averaged every hour in every subject. HF power was significantly lower and LF/HF ratio was significantly higher in the high-salt group than in the low-salt group before the treatment. However, the benidipine treatment significantly increased the HF power in both groups, particularly in the high-salt group, and significantly decreased the LF/HF ratio in both groups. Moreover, there was no significant difference in the antihypertensive effect of benidipine between the high- and low-salt intake groups. These results suggest that benidipine favourably influences blood pressure and autonomic nervous activity in hypertensive patients with a high-salt intake. It is concluded that benidipine may be useful for improving the development of salt-induced hypertension and its accompanying haemodynamic responses.

  4. Early effects of duloxetine on emotion recognition in healthy volunteers

    PubMed Central

    Bamford, Susan; Penton-Voak, Ian; Pinkney, Verity; Baldwin, David S; Munafò, Marcus R; Garner, Matthew

    2015-01-01

    The serotonin-noradrenaline reuptake inhibitor (SNRI) duloxetine is an effective treatment for major depression and generalised anxiety disorder. Neuropsychological models of antidepressant drug action suggest therapeutic effects might be mediated by the early correction of maladaptive biases in emotion processing, including the recognition of emotional expressions. Sub-chronic administration of duloxetine (for two weeks) produces adaptive changes in neural circuitry implicated in emotion processing; however, its effects on emotional expression recognition are unknown. Forty healthy participants were randomised to receive either 14 days of duloxetine (60 mg/day, titrated from 30 mg after three days) or matched placebo (with sham titration) in a double-blind, between-groups, repeated-measures design. On day 0 and day 14 participants completed a computerised emotional expression recognition task that measured sensitivity to the six primary emotions. Thirty-eight participants (19 per group) completed their course of tablets and were included in the analysis. Results provide evidence that duloxetine, compared to placebo, may reduce the accurate recognition of sadness. Drug effects were driven by changes in participants’ ability to correctly detect subtle expressions of sadness, with greater change observed in the placebo relative to the duloxetine group. These effects occurred in the absence of changes in mood. Our preliminary findings require replication, but complement recent evidence that sadness recognition is a therapeutic target in major depression, and a mechanism through which SNRIs could resolve negative biases in emotion processing to achieve therapeutic effects. PMID:25759400

  5. Impact of Pretreatment With Antidepressants on the Efficacy of Duloxetine in Terms of Mood Symptoms and Functioning: An Analysis of 15 Pooled Major Depressive Disorder Studies

    PubMed Central

    Barros, Bruno R.; Schacht, Alexander; Happich, Michael; Televantou, Foula; Berggren, Lovisa; Walker, Daniel J.

    2014-01-01

    Objective: This post hoc analysis aimed to determine whether patients with major depressive disorder (MDD) in duloxetine trials who were antidepressant naive or who were previously exposed to antidepressants exhibited differences in efficacy and functioning. Method: Data were pooled from 15 double-blind, placebo- and/or active-controlled duloxetine trials of adult patients with MDD conducted by Eli Lilly and Company. The individual studies took place between March 2000 and November 2009. Data were analyzed using 4 pretreatment subgroups: first-episode never treated, multiple-episode never treated, treated previously only with selective serotonin reuptake inhibitors (SSRIs), and previously treated with antidepressants other than just SSRIs. Measures included the 17-item Hamilton Depression Rating Scale (HDRS-17) total and somatic symptom subscale scores, Montgomery-Asberg Depression Rating Scale (MADRS) total score, and Sheehan Disability Scale total score. Response rates (50% and 30%) were based on the HDRS-17 total score and remission rates on either the HDRS-17 or MADRS total score. Results: Response and remission rates were significantly greater (P < .05 in 11 of 12 comparisons) for duloxetine versus placebo in the 4 subgroups. A trend of greater response and remission occurred for first-episode versus multiple-episode patients; both groups were generally higher than the antidepressant-treated groups. Mean changes in efficacy measures were mostly significantly greater (P < .05 in 13 of 16 comparisons) for duloxetine versus placebo within each pretreatment subgroup, with some (P < .05 in 2 of 24 comparisons) significant interaction effects between subgroups on HDRS-17 total and somatic symptoms scores. Conclusions: Duloxetine was generally superior to placebo on response and remission rates and in mean change on efficacy measures. Response and remission rates were numerically greater for first-episode versus multiple-episode and drug-treated patients. Mean change

  6. Study on the sonodynamic activity and mechanism of promethazine hydrochloride by multi-spectroscopic techniques

    NASA Astrophysics Data System (ADS)

    He, Ling-Ling; Wang, Xin; Liu, Bin; Wang, Jun; Sun, Ya-Guang; Xu, Shu-Kun

    2011-10-01

    In this paper, the bovine serum albumin (BSA) was selected as a target molecule, the sonodynamic damage to protein in the presence of promethazine hydrochloride (PMT) and its mechanism were studied by the means of absorption, fluorescence and circular dichroism (CD) spectra. The results of hyperchromic effect of absorption spectra and quenching of intrinsic fluorescence spectra indicate that the ultrasound-induced BSA molecules damage is enhanced by PMT. The damage degree of BSA molecules increases with the increase of ultrasonic irradiation time and PMT concentration. The results of synchronous fluorescence, three-dimensional fluorescence and CD spectra confirmed that the synergistic effects of ultrasound and PMT induced the damage of BSA molecules. The results of oxidation-extraction photometry with several reactive oxygen species (ROS) scavengers indicate that the damage of BSA molecules could be mainly due to the generation of ROS and both 1O 2 and rad OH are the important mediators of the ultrasound-induced BSA molecules damage in the presence of PMT.

  7. Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells.

    PubMed

    Lin, Xian-Bin; Jiang, Lei; Ding, Mao-Hua; Chen, Zhen-Hua; Bao, Yi; Chen, Yi; Sun, Wei; Zhang, Chen-Ran; Hu, Hong-Kang; Cai, Zhen; Lu, Cheng-Yin; Zhou, Jue-Yu; Qian, Jun; Wu, Xiao-Jun; Jin, Wei-Lin; Hu, Guo-Han

    2016-03-01

    Phenoxybenzamine hydrochloride (PHEN) is a selective antagonist of both α-adrenoceptor and calmodulin that exhibits anticancer properties. The aim of this study was to explore the anti-tumor function of PHEN in glioma. Cell proliferation assay was used to assess glioma cell growth. Migration and invasion capacity of glioma cells was monitored by wound-healing and transwell assay, respectively. Neurosphere formation test was adopted for the tumorigenesis of glioma cells, which was also confirmed by soft agar cloning formation test in vitro and a nude mouse model in vivo. Finally, we explored the potential pathway utilized by PHEN using Western blot and immunofluoresce staining. PHEN exhibited a significant inhibitory effect on the proliferation of both U251 and U87MG glioma cell lines in a positive dose-dependent manner. PHEN apparently attenuated the malignancy of glioma in terms of migration and invasion and also suppressed the tumorigenic capacity both in vitro and in vivo. Mechanism study showed that PHEN promoted tumor suppression by inhibiting the TrkB-Akt pathway. The results of the present study demonstrated that PHEN suppressed the proliferation, migration, invasion, and tumorigenesis of glioma cells, induced LINGO-1 expression, and inhibited the TrkB-Akt pathway, which may prove to be the mechanisms underlying the anti-tumor effect of PHEN on glioma cells.

  8. Structure activity studies of an analgesic drug tapentadol hydrochloride by spectroscopic and quantum chemical methods

    NASA Astrophysics Data System (ADS)

    Arjunan, V.; Santhanam, R.; Marchewka, M. K.; Mohan, S.; Yang, Haifeng

    2015-11-01

    Tapentadol is a novel opioid pain reliever drug with a dual mechanism of action, having potency between morphine and tramadol. Quantum chemical calculations have been carried out for tapentadol hydrochloride (TAP.Cl) to determine the properties. The geometry is optimised and the structural properties of the compound were determined from the optimised geometry by B3LYP method using 6-311++G(d,p), 6-31G(d,p) and cc-pVDZ basis sets. FT-IR and FT-Raman spectra are recorded in the solid phase in the region of 4000-400 and 4000-100 cm-1, respectively. Frontier molecular orbital energies, LUMO-HOMO energy gap, ionisation potential, electron affinity, electronegativity, hardness and chemical potential are also calculated. The stability of the molecule arising from hyperconjugative interactions and charge delocalisation has been analysed using NBO analysis. The 1H and 13C nuclear magnetic resonance chemical shifts of the molecule are analysed.

  9. Evaluation of toxicological impact of cartap hydrochloride on some physiological activities of a non-heterocystous cyanobacterium Leptolyngbya foveolarum.

    PubMed

    Singh, D P; Khattar, J I S; Gupta, Meenu; Kaur, Gurdeep

    2014-03-01

    The present study was aimed to the evaluation of toxicological impact of insecticide cartap hydrochloride on photosynthesis and nitrogen assimilation of a non-heterocystous cyanoprokaryote Leptolyngbya foveolarum isolated from paddy fields of Punjab, India. The microorganism tolerated commercial grade insecticide up to 80 ppm. Lower concentration (20 ppm) of cartap supported good growth with high dry weight of biomass, total protein content, photosynthetic pigments, photosynthesis and respiration compared to untreated control cultures while higher concentrations (40 and 60 ppm) inhibited these parameters in a dose dependent manner. Treatment of the microorganism with 60 ppm cartap lowered the content of photosynthetic pigments with maximum inhibitory effect on phycoerythrin (70% decrease) followed by allophycocyanin (66% decrease). Rates of photosynthesis and respiration were inhibited by 63% and 45%, respectively, while PS-I, II and whole chain activity were decreased by 45%, 67% and 40% respectively, compared to untreated control cultures. Cartap at 60 ppm decreased nitrate and nitrite uptake by 31% and 61%, respectively, whereas uptake of ammonium was slightly increased (18%) in cartap (60 ppm) treated cells. Nitrate and nitrite reductase, and glutamine synthetase activities of the microorganism decreased by 36-50% in 60 ppm cartap. The low levels of growth, photosynthetic pigments and activities of nitrogen assimilating enzymes in cells grown in nitrogen depleted medium supplement with insecticide indicated that insecticide may be used by the organism as a nitrogen source.

  10. Antimicrobial activities of polyhexamethylene guanidine hydrochloride-based disinfectant against fungi isolated from cocoa beans and reference strains of bacteria.

    PubMed

    Mathurin, Yao K; Koffi-Nevry, Rose; Guéhi, Simplice T; Tano, Kablan; Oulé, Mathias K

    2012-06-01

    This study was conducted to assess the antibacterial and the antifungal activity of a polyhexamethylene guanidine hydrochloride (PHMGH)-based disinfectant and to determine if it could be used as a disinfectant for the treatment of cocoa beans. The activity of PHMGH was tested in vitro for efficacy against five reference strains of pathogenic bacteria and six strains of fungi isolated from cocoa beans. All the strains tested were sensitive to the disinfectant. The MICs reported were between 0.01 and 1.9 mg/ml and equal to the MBC or minimum fungicidal concentration (MFC) regardless of the strains of those microorganisms. The bacteria were more sensitive to PHMGH than were the fungi. Enterobacter cloacae was the most sensitive bacterium with a MIC and MBC of 0.01 mg/ml, whereas the genus Aspergillus was the least susceptible of the microorganisms tested, with a MIC and MFC from 1.0 to 1.9 mg/ml. The time required for the activity of PHMGH varies from 2 min for Enterobacter cloacae to 12 min for Aspergillus tamarii and generally increases with the MBC or the MFC. Through this in vitro study, the PHMGH has been proved to be bactericidal and fungicidal on the strains studied. Hence, it could probably serve as a fungicidal disinfectant for the treatment of cocoa beans after harvesting.

  11. Effects of milnacipran, duloxetine and indomethacin, in polyarthritic rats using the Randall-Selitto model.

    PubMed

    Mico, Juan Antonio; Berrocoso, Esther; Vitton, Olivier; Ladure, Philippe; Newman-Tancredi, Adrian; Bardin, Laurent; Depoortère, Ronan

    2011-09-01

    Milnacipran, a serotonin and noradrenalin reuptake inhibitor (SNRI), is efficacious in rodents in various models of acute or chronic pain (traumatic, neuropathic, inflammatory, visceral). However, its activity against arthritic pain has never been explored. Here, we assessed the activity of acute treatment with milnacipran in a polyarthritic rat model. Rats were injected in the tail base with complete Freund's adjuvant to induce a state of polyarthritis. Analgesic effects of acute treatment with intraperitoneal administration of milnacipran were then evaluated, using the Randall-Selitto model, against two levels of pressure applied to both hind paws (a lower one, addressing mechanical allodynia and a higher one, addressing mechanical hyperalgesia). The other SNRI duloxetine and the nonsteroidal anti-inflammatory drug indomethacin were tested as positive controls. Milnacipran was significantly and dose dependently active against the decrease of paw withdrawal threshold produced by complete Freund's adjuvant for low (minimum effective dose=5 mg/kg, range tested: 2.5-10 mg/kg) and high (minimum effective dose=10 mg/kg, range tested: 5-20 mg/kg)-pressure levels. Duloxetine (20 mg/kg, intraperitoneally) was significantly active against low pressure only. Indomethacin (3 mg/kg per os) was efficacious against both pressure levels. These rodent data suggest that milnacipran should be efficacious in painful conditions associated with chronic inflammatory states, such as arthritis.

  12. Multimodal antidepressant vortioxetine increases frontal cortical oscillations unlike escitalopram and duloxetine – a quantitative EEG study in rats

    PubMed Central

    Leiser, S C; Pehrson, A L; Robichaud, P J; Sanchez, C

    2014-01-01

    Background and Purpose EEG studies show that 5-HT is involved in regulation of sleep–wake state and modulates cortical oscillations. Vortioxetine is a 5-HT3, 5-HT7, and 5-HT1D receptor antagonist, 5-HT1B partial agonist, 5-HT1A agonist, and 5-HT transporter inhibitor. Preclinical (animal) and clinical studies with vortioxetine show positive impact on cognitive metrics involving cortical function. Here we assess vortioxetine's effect on cortical neuronal oscillations in actively awake rats. Experimental Approach Telemetric EEG recordings were obtained with the following treatments (mg·kg−1, s.c.): vehicle, vortioxetine (0.1, 1.0, 3.0, 10), 5-HT1A agonist flesinoxan (2.5), 5-HT3 antagonist ondansetron (0.30), 5-HT7 antagonist SB-269970-A (10), escitalopram (2.0), duloxetine (10) and vortioxetine plus flesinoxan. Target occupancies were determined by ex vivo autoradiography. Key Results Vortioxetine dose-dependently increased wakefulness. Flesinoxan, duloxetine, ondansetron, but not escitalopram or SB-269970-A increased wakefulness. Quantitative spectral analyses showed vortioxetine alone and with flesinoxan increased θ (4–8 Hz), α (8–12 Hz) and γ (30–50 Hz) power. Duloxetine had no effect on θ and γ, but decreased α power, while escitalopram produced no changes. Ondansetron and SB-269970 (≈31–35% occupancy) increased θ power. Flesinoxan (≈41% occupancy) increased θ and γ power. Conclusions and Implications Vortioxetine increased wakefulness and increased frontal cortical activity, most likely because of its 5-HT7 and 5-HT3 antagonism and 5-HT1A agonism. Vortioxetine differs from escitalopram and duloxetine by increasing cortical θ, α and γ oscillations. These preclinical findings suggest a role of vortioxetine in modulating cortical circuits known to be recruited during cognitive behaviours and warrant further investigation as to their clinical impact. PMID:24846338

  13. Agomelatine and duloxetine synergistically modulates apoptotic pathway by inhibiting oxidative stress triggered intracellular calcium entry in neuronal PC12 cells: role of TRPM2 and voltage-gated calcium channels.

    PubMed

    Akpinar, Abdullah; Uğuz, Abdülhadi Cihangir; Nazıroğlu, Mustafa

    2014-05-01

    Calcium ion (Ca(2+)) is one of the universal second messengers, which acts in a wide range of cellular processes. Results of recent studies indicated that ROS generated by depression leads to loss of endoplasmic reticulum-Ca(2+) homeostasis, oxidative stress, and apoptosis. Agomelatine and duloxetine are novel antidepressant and antioxidant drugs and may reduce oxidative stress, apoptosis, and Ca(2+) entry through TRPM2 and voltage-gated calcium channels. We tested the effects of agomelatine, duloxetine, and their combination on oxidative stress, Ca(2+) influx, mitochondrial depolarization, apoptosis, and caspase values in the PC-12 neuronal cells. PC-12 neuronal cells were exposed in cell culture and exposed to appropriate non-toxic concentrations and incubation times for agomelatine were determined in the neurons by assessing cell viability. Then PC-12 cells were incubated with agomelatine and duloxetine for 24 h. Treatment of cultured PC-12 cells with agomelatine, duloxetine, and their combination results in a protection on apoptosis, caspase-3, caspase-9, mitochondrial membrane depolarization, cytosolic ROS production, glutathione peroxidase, reduced glutathione, and lipid peroxidation, values. Ca(2+) entry through non-specific TRPM2 channel blocker (2-APB) and voltage-gated Ca(2+) channel blockers (verapamil and diltiazem) was modulated by agomelatine and duloxetine. However, effects of duloxetine on the Ca(2+) entry through TRPM2 channels were higher than in agomelatine. Results of current study suggest that the agomelatine and duloxetine are useful against apoptotic cell death and oxidative stress in PC-12 cells, which seem to be dependent on mitochondrial damage and increased levels of intracellular Ca(2+) through activation of TRPM2 and voltage-gated Ca(2+) channels.

  14. Improvement with Duloxetine in an Adult ADHD Patient

    ERIC Educational Resources Information Center

    Tourjman, Smadar Valerie; Bilodeau, Mathieu

    2009-01-01

    Introduction: Attention-deficit/hyperactivity disorder (ADHD) is a common and disabling disorder among adults and is treated with stimulant and non stimulant medication. Objective: To report the case of a patient with ADHD showing good clinical response to duloxetine, a selective serotonin and norepinephrine reuptake inhibitor (SSNRI). Case…

  15. Duloxetine in the treatment of major depressive disorder.

    PubMed

    Goldstein, David J

    2007-04-01

    Since depression impacts all body systems, antidepressant treatments should relieve both the emotional and physical symptoms of depression. Duloxetine demonstrated antidepressant efficacy at a dose of 60 mg qd in two placebo-controlled, randomized, double-blind studies and significantly improved remission rates compared with placebo. Duloxetine-treated patients had significant reduction in severity of the symptoms of depression as assessed by the HAM-D(17), anxious symptoms as measured by the HAM-A and quality of life measures compared to placebo. Duloxetine also improved somatic symptoms, particularly painful symptoms which may have contributed to significantly improved remission rates compared to placebo. Approximately 10% of the 1139 patients with major depressive disorder in placebo-controlled trials discontinued treatment due to an adverse event, compared to 4% of the 777 patients receiving placebo. In addition to nausea (1.4% incidence), which was the most common reason for discontinuation, dizziness, somnolence, and fatigue were the most common AEs reported as reasons for discontinuation and all were considered drug-related. Duloxetine treatment lacks effects on ECG, increases heart rate, and has little effect on blood pressure or weight.

  16. Cartap Hydrochloride Poisoning.

    PubMed

    Kalyaniwala, Kimmin; Abhilash, Kpp; Victor, Peter John

    2016-08-01

    Cartap hydrochloride is a moderately hazardous nereistoxin insecticide that is increasingly used for deliberate self-harm in India. It can cause neuromuscular weakness resulting in respiratory failure. We report a patient with 4% Cartap hydrochloride poisoning who required mechanical ventilation for 36-hours. He recovered without any neurological deficits. We also review literature on Cartap hydrochloride poisoning.

  17. DNA breaking activity of the carbon-centered radical generated from 2,2'-azobis(2-amidinopropane) hydrochloride (AAPH).

    PubMed

    Hiramoto, K; Johkoh, H; Sako, K; Kikugawa, K

    1993-01-01

    When supercoiled plasmid DNA was incubated with 2,2'-azobis (2-amidinopropane)hydrochloride (AAPH) at pH 7.4 in the presence and absence of oxygen, the DNA single strands were effectively cleaved. The breaking in the presence of oxygen was not inhibited by superoxide dismutase and catalase, but inhibited by mannitol, ethanol, butyl hydroxyanisole, thiol compounds, tertiary amines and spin trapping agents N-tert-butyl-alpha-phenylnitrone (PBN) and 5,5-dimethyl-1-pyrroline N-oxide (DMPO). The breaking in the absence of oxygen was inhibited by ethanol, a tertiary amine and PBN. By electron spin resonance spin-trapping with PBN, the carbon-centered radical was detected both in the presence and the absence of oxygen. Hydroxyl radical was detected by use of DMPO only in the presence of oxygen. The DNA breaking activity of AAPH was found to be due primarily to the aliphatic carbon-centered radical. While the reactivity of carbon-centered radicals have received little attention, the aliphatic carbon-centered radical generated from AAPH was found to be highly reactive to break the DNA strands.

  18. The short- and long-term effect of duloxetine on painful physical symptoms in patients with generalized anxiety disorder: results from three clinical trials.

    PubMed

    Beesdo, Katja; Hartford, James; Russell, James; Spann, Melissa; Ball, Susan; Wittchen, Hans-Ulrich

    2009-12-01

    Generalized anxiety disorder (GAD) is associated with painful physical symptoms (PPS). These post hoc analyses of previous trial data assessed PPS and their response to duloxetine treatment in GAD patients. Studies 1 and 2 (n=840) were 9- to 10-week efficacy trials; study 3 (n=887) was a relapse prevention trial comprising a 26-week open-label treatment phase and a 26-week double-blind, placebo-controlled treatment continuation phase. Mean baseline visual analog scale scores (VAS, 0-100; n=1727) ranged from 26 to 37 for overall pain, headache, back pain, shoulder pain, interference with daily activities, and time in pain while awake. In studies 1 and 2, improvement on all VAS scores was greater in duloxetine-treated than in placebo-treated patients (pduloxetine (pduloxetine was efficacious in the short- and long-term treatment of PPS, which are common in GAD patients.

  19. Comprehensive quantum chemical and spectroscopic (FTIR, FT-Raman, 1H, 13C NMR) investigations of O-desmethyltramadol hydrochloride an active metabolite in tramadol - An analgesic drug

    NASA Astrophysics Data System (ADS)

    Arjunan, V.; Santhanam, R.; Marchewka, M. K.; Mohan, S.

    2014-03-01

    O-desmethyltramadol is one of the main metabolites of tramadol widely used clinically and has analgesic activity. The FTIR and FT-Raman spectra of O-desmethyl tramadol hydrochloride are recorded in the solid phase in the regions 4000-400 cm-1 and 4000-100 cm-1, respectively. The observed fundamentals are assigned to different normal modes of vibration. Theoretical studies have been performed as its hydrochloride salt. The structure of the compound has been optimised with B3LYP method using 6-31G** and cc-pVDZ basis sets. The optimised bond length and bond angles are correlated with the X-ray data. The experimental wavenumbers were compared with the scaled vibrational frequencies determined by DFT methods. The IR and Raman intensities are determined with B3LYP method using cc-pVDZ and 6-31G(d,p) basic sets. The total electron density and molecular electrostatic potential surfaces of the molecule are constructed by using B3LYP/cc-pVDZ method to display electrostatic potential (electron + nuclei) distribution. The electronic properties HOMO and LUMO energies were measured. Natural bond orbital analysis of O-desmethyltramadol hydrochloride has been performed to indicate the presence of intramolecular charge transfer. The 1H and 13C NMR chemical shifts of the molecule have been anlysed.

  20. Considering benefits and harms of duloxetine for treatment of stress urinary incontinence: a meta-analysis of clinical study reports

    PubMed Central

    Maund, Emma; Guski, Louise Schow; Gøtzsche, Peter C.

    2017-01-01

    BACKGROUND: The European Medicines Agency makes clinical study reports publicly available and publishes reasons for not approving applications for marketing authorization. Duloxetine has been approved in Europe for the treatment of stress urinary incontinence in women. The reported adverse effects of duloxetine include mental health problems and suicidality. We obtained clinical study reports from the European Medicines Agency concerning use of this drug for stress urinary incontinence. METHODS: We performed a meta-analysis of 4 randomized placebo-controlled trials of duloxetine (involving a total of 1913 patients) submitted to the European Medicines Agency for marketing approval for the indication of stress urinary incontinence in women. We used data from the clinical study reports (totalling 6870 pages and including individual patient data) to assess benefits (including frequency of incontinence and changes in quality-of-life scores, such as Patient Global Impression of Improvement rating) and harms (both general harms, including discontinuation because of adverse events, and harms related to suicidality, violent behaviour and their potential precursors, such as akathisia and activation [stimulating effects such as insomnia, anxiety and agitation]). RESULTS: Duloxetine was significantly better than placebo in terms of percentage change in weekly incontinence episodes (mean difference −13.56%, 95% confidence interval [CI] −21.59% to −5.53%) and change in Incontinence Quality of Life total score (mean difference 3.24, 95% CI 2.00 to 4.48). However, the effect sizes were small, and a sensitivity analysis (with removal of one trial) showed that the number needed to treat for a Patient Global Impression of Improvement rating of “much better or very much better” was 8 (95% CI 6 to 13). The numbers needed to harm were 7 (95% CI 6 to 8) for discontinuing because of an adverse event and 7 (95% CI 6 to 9) for experiencing an activation event. No suicidality

  1. The Use of Duloxetine in Chronic Bulimia Nervosa

    PubMed Central

    Averbuch, Robert N.

    2009-01-01

    Selective serotonin reuptake inhibitors are routinely prescribed as off-label treatments for bulimia nervosa. There is, however, a paucity of literature addressing the efficacy of the serotonin norepinephrine reuptake inhibitors in the pharmacologic management of this disorder. This article describes a clinical situation in which duloxetine, a serotonin norepinephrine reuptake inhibitor, effectively treated a patient with long-standing bulimia nervosa, purging type, and comorbid generalized anxiety disorder. PMID:19763204

  2. Facile synthesis of Cu(II) impregnated biochar with enhanced adsorption activity for the removal of doxycycline hydrochloride from water.

    PubMed

    Liu, Su; Xu, Wei-Hua; Liu, Yun-Guo; Tan, Xiao-Fei; Zeng, Guang-Ming; Li, Xin; Liang, Jie; Zhou, Zan; Yan, Zhi-Li; Cai, Xiao-Xi

    2017-03-16

    In this study, the effect factors and mechanisms of doxycycline hydrochloride (DOX) adsorption on copper nitrate modified biochar (Cu-BC) was investigated. Cu-BC absorbent was synthesized through calcination of peanut shells biomass at 450°C and then impregnation with copper nitrate. The Cu-BC has exhibited excellent sorption efficiency about 93.22% of doxycycline hydrochloride from aqueous solution, which was double higher than that of the unmodified biochar. The experimental results suggest that the adsorption efficiency of DOX on the Cu-BC is dominated by the strong complexation, electrostatic interactions between DOX molecules and the Cu-BC samples. Comprehensively considering the cost, efficiency and the application to realistic water, the Cu-BC hold the significant potential for enhancing the effectiveness to remove DOX from water.

  3. Ion-activated in situ gelling systems for sustained ophthalmic delivery of ciprofloxacin hydrochloride.

    PubMed

    Balasubramaniam, J; Pandit, J K

    2003-01-01

    The poor bioavailability and therapeutic response exhibited by the conventional ophthalmic solutions due to precorneal elimination of the drug may be overcome by the use of in situ gel forming systems that are instilled as drops into the eye and undergo a sol-gel transition in the cul-de-sac. Our present work describes the formulation and evaluation of an ophthalmic delivery system of an antibacterial agent, CPH, based on the concept of ion-activated in situ gelation. Gelrite gellan gum, a novel ophthalmic vehicle that gels in the presence of mono or divalent cations, present in the lacrimal fluid was used alone and in combinations with sodium alginate as the gelling agent. The developed formulations were therapeutically efficacious and provided sustained release of the drug over an 8-hr period in vitro.

  4. Effects of chronic and acute methylphenidate hydrochloride (Ritalin) administration on locomotor activity, ultrasonic vocalizations, and neuromotor development in 3- to 11-day-old CD-1 mouse pups.

    PubMed

    Penner, M R; McFadyen, M P; Carrey, N; Brown, R E

    2001-11-01

    The present study examined the effects of chronic and acute treatment with methylphenidate hydrochloride (Ritalin) on isolation-induced ultrasonic vocalizations, spontaneous locomotor activity, and neuromotor coordination in 3- to 11-day-old CD-1 mouse pups. In Experiment 1, 3- to 11-day-old pups received daily injections of saline, 5 mg/kg or 20 mg/kg of methylphenidate hydrochloride, or no injection and were tested on postnatal Days 3, 5, 7, 9, and 11. Both doses of methylphenidate resulted in significant increases in locomotor activity at all ages, but had no significant effect on body weight, neuromotor development, or emission of ultrasonic vocalizations. In Experiment 2, pups were given a single dose of methylphenidate (5 or 20 mg/kg), saline, or no injection on one of postnatal Days 5, 7, 9, or 11. This acute methylphenidate treatment increased locomotor activity, but had no significant effects on ultrasonic vocalizations or neuromotor coordination. These results indicate that short-term, chronic methylphenidate treatment elevates locomotor responses, but has no immediate effects on anxietylike responses or on the development of neuromotor behavior of CD-1 mice in the first 11 days of life.

  5. Netupitant and Palonosetron Hydrochloride

    Cancer.gov

    This page contains brief information about netupitant and palonosetron hydrochloride and a collection of links to more information about the use of this combination drug, research results, and ongoing clinical trials.

  6. Trifluridine and Tipiracil Hydrochloride

    Cancer.gov

    This page contains brief information about trifluridine and tipiracil hydrochloride and a collection of links to more information about the use of this combination drug, research results, and ongoing clinical trials.

  7. Duloxetine and 8-OH-DPAT, but not fluoxetine, reduce depression-like behaviour in an animal model of chronic neuropathic pain.

    PubMed

    Hu, Bing; Doods, Henri; Treede, Rolf-Detlef; Ceci, Angelo

    2016-04-21

    The current study assessed whether antidepressant and/or antinociceptive drugs, duloxetine, fluoxetine as well as (±)-8-hydroxy-2-[di-n-propylamino] tetralin (8-OH-DPAT), are able to reverse depression-like behaviour in animals with chronic neuropathic pain. Chronic constriction injury (CCI) of the sciatic nerve in rats was selected as neuropathic pain model. Mechanical hypersensitivity and depression-like behaviour were evaluated 4 weeks after surgery by "electronic algometer" and forced swimming test (FST), which measured the time of immobility, and active behaviours climbing and swimming. The selective noradrenergic and serotonergic uptake blocker duloxetine (20mg/kg) and the selective 5-HT1A agonist 8-OH-DPAT (0.5mg/kg) significantly reversed both mechanical hypersensitivity and depression-like behaviour in CCI animals. Duloxetine significantly reversed depression-like behaviour in CCI rats by increasing the time of climbing and swimming, while 8-OH-DPAT attenuated depression-like behaviour mainly by increasing the time of swimming. However, the selective serotonergic uptake blocker fluoxetine (20mg/kg) failed to attenuate mechanical hypersensitivity and depression-like behaviour, possibly due to confounding pro-nociceptive actions at 5-HT3 receptors. These data suggest to target noradrenergic and 5-HT1A receptors for treatment of chronic pain and its comorbidity depression.

  8. Investigation on the enantioseparation of duloxetine by capillary electrophoresis, NMR, and mass spectrometry.

    PubMed

    Sánchez-López, Elena; Salgado, Antonio; Crego, Antonio L; Marina, María Luisa

    2014-10-01

    The enantiomeric separation of the antidepressant drug duloxetine was investigated by CE using 15 neutral CDs as chiral selectors. Among them, (2-hydroxypropyl)-β-CD and methyl-γ-CD gave rise to the highest enantioresolution. The enantiomer migration order for duloxetine was found to be reversed depending on the CD employed: R-duloxetine was the first-migrating enantiomer for (2-hydroxypropyl)-β-CD while it was the second-migrating enantiomer for methyl-γ-CD. NMR and MS experiments were performed in order to justify this behavior. Although the elucidation of the structure of the enantiomer-CD complexes was not possible, their averaged stoichiometry was studied and their apparent and averaged equilibrium constants were calculated. The results obtained showed that the chiral separation of duloxetine by CE depends not only on the thermodynamic stability of the enantiomer-chiral selector complexes but also on their electrophoretic mobility.

  9. A Randomized Placebo-Controlled Trial of Duloxetine for Central Pain in Multiple Sclerosis

    PubMed Central

    Slee, April

    2015-01-01

    Background: Pain is common in multiple sclerosis (MS). Duloxetine has a potential therapeutic role in treating MS-related pain. Methods: Thirty-eight MS patients were randomized 1:1 to receive duloxetine (n = 18) or matched placebo (n = 20). The dosing regimen was 30 mg daily for 1 week, then 60 mg daily for 5 weeks. The primary outcome measure was change in worst pain for week 6 relative to baseline recorded on a daily pain diary. Results: Of 38 randomized patients, 14 (78%) patients randomized to duloxetine and 18 (90%) randomized to placebo completed treatment per protocol. These participants had an average age of 55.5 years, 25% were male, and 66% had relapsing-remitting MS (RRMS). Baseline characteristics were similar. Discontinuations were due primarily to drug intolerance. Among those who completed treatment, worst pain at 6 weeks was reduced by 29% (±20%) for duloxetine versus 12% (±18%) for placebo (P = .016). Average daily pain at 6 weeks was reduced by 39% (±29%) in the duloxetine group compared to 10% (±18.8%) in the placebo group (P = .002). There were no significant changes (week 6 vs. baseline) or between-group differences for subject global impression, Beck Depression Inventory, 36-item Short Form Health Status Survey (SF-36), or sleep quality score. Conclusions: Fewer patients could tolerate duloxetine compared to placebo. Among patients who completed 6 weeks of treatment, there were significant reductions in average and worst daily pain scores with duloxetine compared to placebo. This study suggests that duloxetine has a direct pain-relieving effect in MS. PMID:25892978

  10. Augmentation of antidepressant effects of duloxetine and bupropion by caffeine in mice.

    PubMed

    Kale, Pravin Popatrao; Addepalli, Veeranjaneyulu

    2014-09-01

    There is an unmet need in the treatment of depression suggesting requirement of new therapeutic approaches having better efficacy and safety profile. Patients receiving antidepressant therapy generally consume caffeine in the form of tea or coffee. The objective of the present study was to evaluate the augmentation of antidepressant effects of duloxetine and/or bupropion with caffeine. Male Swiss Albino mice received treatment of normal saline (10 ml/kg), 'caffeine alone' (10mg/kg), 'duloxetine alone' (10mg/kg), 'bupropion alone' (10mg/kg), caffeine+duloxetine (5mg/kg, each), bupropion+caffeine (5mg/kg, each), and bupropion+duloxetine (5mg/kg, each) through the intra-peritoneal route. The immobility period was analyzed 30 min after the treatment in forced swim and tail suspension tests. Norepinephrine, dopamine, and serotonin levels were analyzed in hippocampus, cerebral cortex and whole brain using HPLC with fluorescence detector. Euthanasia was performed 1h after treatment. Comparison between vehicle treated group and other groups showed significant decrease in immobility in all drug treated groups in both antidepressant models. Caffeine plus duloxetine treated group was better among the combination treated groups in terms of decrease in immobility and increase in norepinephrine, dopamine, and serotonin levels in hippocampi, cerebral cortices, and whole brain when compared to their respective monotherapy treated groups. These combination approaches may help in reducing the dose of duloxetine/bupropion, and consequently lower the associated side/adverse effects.

  11. Prescribing patterns of duloxetine in France: a prescription assessment study in real-world conditions.

    PubMed

    Augendre-Ferrante, Beatrice; Picard, Hernan; Evans, David; Arkoub, Hafida; Pamulapati, Sireesha; Perrot, Serge; Valensi, Paul; Rouillon, Frederic

    2014-01-01

    Duloxetine is a serotonin and norepinephrine reuptake inhibitor approved in the European Union for the treatment of major depressive disorder, generalized anxiety disorder, and diabetic peripheral neuropathic pain in adults. This study aimed to assess the real-world conditions of duloxetine use in France. Between April 2009 and January 2010, 290 dispensing pharmacies, randomly selected from a nationally representative list, included 1,104 patients who presented a duloxetine prescription and consented to the study. Demographic, clinical, and prescription data were extracted from pharmacy records and requested from prescribing physicians. Of the 294 patients with full data available, the mean age (standard deviation) was 54.5 (13.5) years; 74.1% were female; and 86.7% presented with a renewal prescription. 73.5% of patients had major depressive disorder; 3.4% generalized anxiety disorder; and 3.4% diabetic peripheral neuropathic pain. Overall, 78.2% (95% CI: 73.1; 82.8) of patients received duloxetine for an EU-approved indication; 95.2% (95% CI: 92.1; 97.4) of patients had no contra-indication to duloxetine; and 99.0% (95% CI: 97.0; 99.8) received an approved dose. Combining these three criteria, the overall approved use of duloxetine was 73.7% (95% CI: 68.3; 78.7). The strengths and limitations of the study design are discussed.

  12. Enhancement of nootropic effect of duloxetine and bupropion by caffeine in mice

    PubMed Central

    Kale, Pravin Popatrao; Addepalli, Veeranjaneyulu

    2015-01-01

    Objective: The existing evidence suggests an association between depression and memory impairment. The objective of present study was to assess the effect of low dose caffeine with duloxetine and bupropion on memory. Materials and Methods: Mice were divided randomly into seven groups. Intra-peritoneal treatment of normal saline (10 ml/kg), caffeine (10 mg/kg), duloxetine (10 mg/kg), bupropion alone (10 mg/kg), caffeine + duloxetine (5 mg/kg, each), caffeine + bupropion (5 mg/kg, each), and bupropion + duloxetine (5 mg/kg, each) were given to groups I-VII, respectively. Elevated plus maze was used to evaluate transfer latency (TL) and Morris water maze was used to estimate the time spent in target quadrant. Results: Caffeine with duloxetine treated group was better than other combination treated groups in terms of a significant decrease in TL and increase in the time spent in target quadrant recorded. Conclusion: Combining lower dose of caffeine with duloxetine may enhance cognitive benefits than respective monotherapies. PMID:25878382

  13. Corneal critical barrier against the penetration of dexamethasone and lomefloxacin hydrochloride: evaluation by the activation energy for drug partition and diffusion in cornea.

    PubMed

    Yasueda, Shin-ichi; Higashiyama, Masayo; Yamaguchi, Masazumi; Isowaki, Akiharu; Ohtori, Akira

    2007-08-01

    The cornea is a solid barrier against drug permeation. We searched the critical barrier of corneal drug permeation using a hydrophobic drug, dexamethasone (DM), and a hydrophilic drug, lomefloxacin hydrochloride (LFLX). The activation energies for permeability of DM and LFLX across the intact cornea were 88.0 and 42.1 kJ/mol, respectively. Their activation energies for permeability across the cornea without epithelium decreased to 33.1 and 16.6 kJ/mol, respectively. The results show that epithelium is the critical barrier on the cornea against the permeation of a hydrophobic drug of DM as well as a hydrophilic drug of LFLX. The activation energy of partition for DM (66.8 kJ/mol) was approximately 3-fold larger than that of diffusion (21.2 kJ/mol). The results indicate that the partition for the hydrophobic drug of DM to the corneal epithelium is the primary barrier. Thermodynamic evaluation of activation energy for the drug permeation parameters is a good approach to investigate the mechanism of drug permeability.

  14. Protective effect of 3-(naphthalen-2-yl(propoxy)methyl)azetidine hydrochloride on hypoxia-induced toxicity by suppressing microglial activation in BV-2 cells

    PubMed Central

    Kim, Jiae; Kim, Su-Min; Na, Jung-Min; Hahn, Hoh-Gyu; Cho, Sung-Woo; Yang, Seung-Ju

    2016-01-01

    We recently reported the anti-inflammatory effects of 3-(naphthalen-2-yl(propoxy)methyl)azetidine hydrochloride (KHG26792) on the ATP-induced activation of the NFAT and MAPK pathways through the P2X7 receptor in microglia. To further investigate the underlying mechanism of KHG26792, we studied its protective effects on hypoxia-induced toxicity in microglia. The administration of KHG26792 significantly reduced the hypoxia-induced expression and activity of caspase-3 in BV-2 microglial cells. KHG26792 also reduced hypoxia-induced inducible nitric oxide synthase protein expression, which correlated with reduced nitric oxide accumulation. In addition, KHG26792 attenuated hypoxia-induced protein nitration, reactive oxygen species production, and NADPH oxidase activity. These effects were accompanied by the suppression of hypoxia-induced protein expression of hypoxia-inducible factor 1-alpha and NADPH oxidase-2. Although the clinical relevance of our findings remains to be determined, these data results suggest that KHG26792 prevents hypoxia-induced toxicity by suppressing microglial activation. PMID:27756444

  15. Synergistic analgesia of duloxetine and celecoxib in the mouse formalin test: a combination analysis.

    PubMed

    Sun, Yong-Hai; Dong, Yu-Lin; Wang, Yu-Tong; Zhao, Guo-Li; Lu, Gui-Jun; Yang, Jing; Wu, Sheng-Xi; Gu, Ze-Xu; Wang, Wen

    2013-01-01

    Duloxetine, a serotonin and noradrenaline reuptake inhibitor, and celecoxib, a non-steroidal anti-inflammatory drug, are commonly used analgesics for persistent pain, however with moderate gastrointestinal side effects or analgesia tolerance. One promising analgesic strategy is to give a combined prescription, allowing the maximal or equal efficacy with fewer side effects. In the current study, the efficacy and side effects of combined administration of duloxetine and celecoxib were tested in the mouse formalin pain model. The subcutaneous (s.c.) injection of formalin into the left hindpaw induced significant somatic and emotional pain evaluated by the biphasic spontaneous flinching of the injected hindpaw and interphase ultrasonic vocalizations (USVs) during the 1 h after formalin injection, respectively. Pretreatment with intraperitoneal (i.p.) injection of duloxetine or celecoxib at 1 h before formalin injection induced the dose-dependent inhibition on the second but not first phase pain responses. Combined administration of duloxetine and celecoxib showed significant analgesia for the second phase pain responses. Combination analgesia on the first phase was observed only with higher dose combination. A statistical difference between the theoretical and experimental ED50 for the second phase pain responses was observed, which indicated synergistic interaction of the two drugs. Concerning the emotional pain responses revealed with USVs, we assumed that the antinociceptive effects were almost completely derived from duloxetine, since celecoxib was ineffective when administered alone or reduced the dosage of duloxetine when given in combination. Based on the above findings, acute concomitant administration of duloxetine and celecoxib showed synergism on the somatic pain behavior but not emotional pain behaviors.

  16. Synergistic Analgesia of Duloxetine and Celecoxib in the Mouse Formalin Test: A Combination Analysis

    PubMed Central

    Zhao, Guo-Li; Lu, Gui-Jun; Yang, Jing; Wu, Sheng-Xi; Gu, Ze-Xu; Wang, Wen

    2013-01-01

    Duloxetine, a serotonin and noradrenaline reuptake inhibitor, and celecoxib, a non-steroidal anti-inflammatory drug, are commonly used analgesics for persistent pain, however with moderate gastrointestinal side effects or analgesia tolerance. One promising analgesic strategy is to give a combined prescription, allowing the maximal or equal efficacy with fewer side effects. In the current study, the efficacy and side effects of combined administration of duloxetine and celecoxib were tested in the mouse formalin pain model. The subcutaneous (s.c.) injection of formalin into the left hindpaw induced significant somatic and emotional pain evaluated by the biphasic spontaneous flinching of the injected hindpaw and interphase ultrasonic vocalizations (USVs) during the 1 h after formalin injection, respectively. Pretreatment with intraperitoneal (i.p.) injection of duloxetine or celecoxib at 1 h before formalin injection induced the dose-dependent inhibition on the second but not first phase pain responses. Combined administration of duloxetine and celecoxib showed significant analgesia for the second phase pain responses. Combination analgesia on the first phase was observed only with higher dose combination. A statistical difference between the theoretical and experimental ED50 for the second phase pain responses was observed, which indicated synergistic interaction of the two drugs. Concerning the emotional pain responses revealed with USVs, we assumed that the antinociceptive effects were almost completely derived from duloxetine, since celecoxib was ineffective when administered alone or reduced the dosage of duloxetine when given in combination. Based on the above findings, acute concomitant administration of duloxetine and celecoxib showed synergism on the somatic pain behavior but not emotional pain behaviors. PMID:24116126

  17. Efficacy of Duloxetine for the Treatment of Generalized Anxiety Disorder: Implications for Primary Care Physicians

    PubMed Central

    Koponen, Hannu; Allgulander, Christer; Erickson, Janelle; Dunayevich, Eduardo; Pritchett, Yili; Detke, Michael J.; Ball, Susan G.; Russell, James M.

    2007-01-01

    Objective: This study examined the efficacy and tolerability of duloxetine, a dual reuptake inhibitor of serotonin and norepinephrine, for the treatment of patients with generalized anxiety disorder (GAD). Method: Patients were ≥ 18 years old and recruited from 5 European countries, the United States, and South Africa. The study had a 9-week, multicenter, randomized, double-blind, fixed-dose, placebo-controlled, parallel-group design. A total of 513 patients (mean age = 43.8 years; 67.8% female) with a DSM-IV–defined GAD diagnosis received treatment with duloxetine 60 mg/day (N = 168), duloxetine 120 mg/day (N = 170), or placebo (N = 175). The primary efficacy measure was the Hamilton Rating Scale for Anxiety (HAM-A) total score. Secondary measures included the Sheehan Disability Scale, HAM-A psychic and somatic anxiety factor scores, and HAM-A response, remission, and sustained improvement rates. The study was conducted from July 2004 to September 2005. Results: Both groups of duloxetine-treated patients demonstrated significantly greater improvements in anxiety symptom severity compared with placebo-treated patients as measured by HAM-A total score and HAM-A psychic and somatic anxiety factor scores (p values ranged from ≤ .01 to ≤ .001). Duloxetine-treated patients had greater functional improvements in Sheehan Disability Scale global and specific domain scores (p ≤ .001) than placebo-treated patients. Both duloxetine doses also resulted in significantly greater HAM-A response, remission, and sustained improvement rates compared with placebo (p values ranged from ≤ .01 to ≤ .001). The rate of study discontinuation due to adverse events was 11.3% for duloxetine 60 mg and 15.3% for duloxetine 120 mg versus 2.3% for placebo (p ≤ .001). Conclusion: The results of this study demonstrate that duloxetine 60 mg/day and 120 mg/day were efficacious and well tolerated and thus may provide primary care physicians with a useful pharmacologic intervention for

  18. Combination of pregabalin with duloxetine for fibromyalgia: a randomized controlled trial.

    PubMed

    Gilron, Ian; Chaparro, Luis E; Tu, Dongsheng; Holden, Ronald R; Milev, Roumen; Towheed, Tanveer; DuMerton-Shore, Deborah; Walker, Sarah

    2016-07-01

    Fibromyalgia is a syndrome characterized by chronic widespread pain and associated with sleep disturbance, depression, fatigue, and cognitive dysfunction. Polypharmacy is commonly used, but supportive evidence is limited. Most fibromyalgia trials focus primarily on pain reduction with monotherapy. This trial compares a pregabalin-duloxetine combination to each monotherapy. Using a randomized, double-blind, 4-period crossover design, participants received maximally tolerated doses of placebo, pregabalin, duloxetine, and pregabalin-duloxetine combination-for 6 weeks. Primary outcome was daily pain (0-10); secondary outcomes included global pain relief, Fibromyalgia Impact Questionnaire, SF-36 survey, Medical Outcomes Study Sleep Scale, Beck Depression Inventory (BDI-II), adverse events, and other measures. Of 41 participants randomized, 39 completed ≥2 treatments. Daily pain during placebo, pregabalin, duloxetine, and combination was 5.1, 5.0, 4.1, and 3.7, respectively (P < 0.05 only for combination vs placebo, and pregabalin). Participants (%) reporting ≥moderate global pain relief were 18%, 39%, 42%, and 68%, respectively (P < 0.05 for combination vs placebo, pregabalin, and duloxetine). Fibromyalgia Impact Questionnaire scores were 42.9, 37.4, 36.0, and 29.8, respectively (P < 0.05 for combination vs placebo, pregabalin, and duloxetine). SF-36 scores were 50.2, 55.7, 56.0, and 61.2, respectively (P < 0.05 for combination vs placebo, pregabalin, and duloxetine). Medical Outcomes Study Sleep Scale scores were 48.9, 35.2, 46.1, and 32.1, respectively (P < 0.05 only for combination vs placebo, and duloxetine). BDI-II scores were 11.9, 9.9, 10.7, and 8.9, respectively (P < 0.05 only for combination vs placebo). Moderate-severe drowsiness was more frequent during combination vs placebo. Combining pregabalin and duloxetine for fibromyalgia improves multiple clinical outcomes vs monotherapy. Continued research should compare this and other combinations to monotherapy

  19. Self-Limited Kleptomania Symptoms as a Side Effect of Duloxetine

    PubMed Central

    Gallagher, Keith E.

    2016-01-01

    Introduction. Impulse control disorders (ICDs) have been described as a side effect of dopamine agonists, frequently used in neurodegenerative conditions affecting the nigrostriatal pathway. Serotonin-norepinephrine reuptake inhibitors (e.g., duloxetine) have dose-dependent differential affinity for monoaminergic transporters, inhibiting the dopamine transporter at higher doses, thus increasing availability of synaptic dopamine, with the potential for similar impulse control side effects. Case Presentation. A 19-year-old Asian-American female with a history of depression developed new-onset stealing behaviors after an increase in her dose of duloxetine from 60 mg to 90 mg; she described these actions as “compulsive” and irresistible, later experiencing either relief or guilt, features compatible with an ICD. Her symptoms eventually subsided with continued use of 90 mg of duloxetine. Discussion. To the knowledge of the authors, this is the first report of a patient developing new-onset ICD behaviors after being placed on a higher dose of duloxetine, which can inhibit the dopamine transporter and cause difficulty with impulse control. The self-resolving nature of the symptoms may result from compensatory upregulation of dopamine transporters, increasing reuptake of dopamine. Asian populations may be at a higher risk due to the frequent occurrence of CYP2D6 polymorphisms, which decrease the conversion of duloxetine to its inactive metabolites. PMID:28018697

  20. Thermoanalytical Investigation of Terazosin Hydrochloride

    PubMed Central

    Attia, Ali Kamal; Mohamed Abdel-Moety, Mona

    2013-01-01

    Purpose: Thermal analysis (TGA, DTG and DTA) and differential scanning calorimetry (DSC) have been used to study the thermal behavior of terazosin hydrochloride (TER). Methods: Thermogravimetric analysis (TGA/DTG), differential thermal analysis (DTA) and differential scanning calorimetry (DSC) were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*), enthalpy (∆H*), entropy (∆S*) and Gibbs free energy change of the decomposition (∆G*) were calculated using different kinetic models. Results: The purity of the used drug was determined by differential scanning calorimetry (99.97%) and specialized official method (99.85%) indicating to satisfactory values of the degree of purity. Thermal analysis technique gave satisfactory results to obtain quality control parameters such as melting point (273 ºC), water content (7.49%) and ash content (zero) in comparison to what were obtained using official method: (272 ºC), (8.0%) and (0.02%) for melting point, water content and ash content, respectively. Conclusion: Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs. DSC data indicated that the degree of purity of terazosin hydrochloride is similar to that found by official method. PMID:24312828

  1. Delirium associated with concomitant use of duloxetine and bupropion in an elderly patient.

    PubMed

    Ma, Szu-Pin; Tsai, Chia-Jui; Chang, Cheng-Chen; Hsu, Wen-Yu

    2017-03-01

    Delirium is common in daily practice. Drug-induced delirium constitutes approximately one-third of all cases of delirium. In cases characterized by the limited efficacy of a single antidepressant, a combination of two antidepressants is required, which may induce a complex drug-drug interaction. We reviewed a case of duloxetine- and bupropion-related delirium in an elderly male patient in our clinical practice. The patient was diagnosed with major depressive disorder and was treated with duloxetine. However, he developed delirium 10 days after bupropion was added to his treatment regimen. Three days after the cessation of bupropion, his delirious condition gradually improved. Duloxetine and bupropion are both cytochrome P450 2D6 inhibitors that may result in a higher level of hydroxybupropion. An increased level of hydroxybupropion may cause the elevation of dopamine and a risk of subsequent delirium. We should be aware of the risk of delirium induced by drug-drug interactions.

  2. Duloxetine in the treatment of burning mouth syndrome refractory to conventional treatment: A case report.

    PubMed

    Kim, Yeon-Dong; Lee, Ji-Hye; Shim, Jee-Hoon

    2014-06-01

    Patients with burning mouth syndrome (BMS) report burning sensation and pain involving the tongue and oral mucosa without any apparent medical or dental cause. The pathogenesis of this syndrome remains unclear and there is currently no standard treatment. BMS is, therefore, often misdiagnosed and its management is complex. This lack of clinical expertise may result in decreased health-related quality of life and increased psychological distress among patients with BMS. The present case report involves a 77-year-old female patient with BMS refractory to conventional treatment with nerve block and medication, who was successfully treated with duloxetine. Duloxetine may become a new therapeutic option in the management of BMS.

  3. Predictors of duloxetine response in patients with oxaliplatin-induced painful chemotherapy-induced peripheral neuropathy (CIPN): a secondary analysis of randomised controlled trial - CALGB/alliance 170601.

    PubMed

    Smith, E M L; Pang, H; Ye, C; Cirrincione, C; Fleishman, S; Paskett, E D; Ahles, T; Bressler, L R; Le-Lindqwister, N; Fadul, C E; Loprinzi, C; Shapiro, C L

    2017-03-01

    Duloxetine is an effective treatment for oxaliplatin-induced painful chemotherapy-induced peripheral neuropathy (CIPN). However, predictors of duloxetine response have not been adequately explored. The objective of this secondary and exploratory analysis was to identify predictors of duloxetine response in patients with painful oxaliplatin-induced CIPN. Patients (N = 106) with oxaliplatin-induced painful CIPN were randomised to receive duloxetine or placebo. Eligible patients had chronic CIPN pain and an average neuropathic pain score ≥4/10. Duloxetine/placebo dose was 30 mg/day for 7 days, then 60 mg/day for 4 weeks. The Brief Pain Inventory-Short Form and the EORTC QLQ-C30 were used to assess pain and quality of life, respectively. Univariate and multiple logistic regression analyses were performed to identify demographic, physiologic and psychological predictors of duloxetine response. Higher baseline emotional functioning predicted duloxetine response (≥30% reduction in pain; OR 4.036; 95% CI 0.999-16.308; p = 0.050). Based on the results from a multiple logistic regression using patient data from both the duloxetine and placebo treatment arms, duloxetine-treated patients with high emotional functioning are more likely to experience pain reduction (p = 0.026). In patients with painful, oxaliplatin-induced CIPN, emotional functioning may also predict duloxetine response. ClinicalTrials.gov, Identifier NCT00489411.

  4. Organic Anion Transporting Polypeptide (OATP)2B1 Contributes to Gastrointestinal Toxicity of Anticancer Drug SN-38, Active Metabolite of Irinotecan Hydrochloride.

    PubMed

    Fujita, Daichi; Saito, Yoshimasa; Nakanishi, Takeo; Tamai, Ikumi

    2016-01-01

    Gastrointestinal toxicity, such as late-onset diarrhea, is a significant concern in irinotecan hydrochloride (CPT-11)-containing regimens. Prophylaxis of late-onset diarrhea has been reported with use of Japanese traditional (Kampo) medicine containing baicalin and with the antibiotic cefixime, and this has been explained in terms of inhibition of bacterial deconjugation of SN-38-glucuronide since unconjugated SN-38 (active metabolite of CPT-11) is responsible for the gastrointestinal toxicity. It is also prerequisite for SN-38 to be accumulated in intestinal tissues to exert toxicity. Based on the fact that liver-specific organic anion transporting polypeptide (OATP)1B1, a member of the same family as OATP2B1, is known to be involved in hepatic transport of SN-38, we hypothesized that intestinal transporter OATP2B1 contributes to the accumulation of SN-38 in gastrointestinal tissues, and its inhibition would help prevent associated toxicity. We found that uptake of SN-38 by OATP2B1-expressing Xenopus oocytes was significantly higher than that by control oocytes. OATP2B1-mediated uptake of SN-38 was saturable, pH dependent, and decreased in the presence of baicalin, cefixime, or fruit juices such as apple juice. In vivo gastrointestinal toxicity of SN-38 in mice caused by oral administration for consecutive 5 days was prevented by coingestion of apple juice. Thus, OATP2B1 contributes to the uptake of SN-38 by intestinal tissues, triggering gastrointestinal toxicity. So, in addition to the reported inhibition of bacterial β-glucuronidase by cefixime or baicalin, inhibition of OATP2B1 may also contribute to prevention of gastrointestinal toxicity. Apple juice may be helpful for prophylaxis of late-onset diarrhea observed in CPT-11 therapy without disturbance of the intestinal microflora.

  5. Syndrome of inappropriate antidiuretic hormone secretion: a story of duloxetine-induced hyponatraemia.

    PubMed

    Amoako, Adae Opoku; Brown, Carina; Riley, Timothy

    2015-04-24

    Hyponatraemia is the most commonly encountered electrolyte abnormality in clinical practice. Syndrome of inappropriate antidiuretic hormone secretion (SIADH) accounts for nearly 60% of all hyponatraemias. Selective serotonin reuptake inhibitors (SSRIs) are well known to have side effects of SIADH. There have been few reported cases of serotonin norepinephrine reuptake inhibitors (SNRIs) causing SIADH-induced hyponatraemia. Duloxetine is one type of SNRI used to treat several conditions, including depression and diabetic neuropathy. We present a case of a 76-year-old woman with a history of fibromyalgia who had recently been prescribed duloxetine for her condition. On admission to the hospital, her sodium decreased to a low of 118 mmol/L. Evaluation for other causes of hyponatraemia yielded negative results. Duloxetine was discontinued and after 3 days the patient's sodium increased to 130 mmol/L. The purpose of this case report is to highlight the importance of having suspicion for rare but real side effects of medications such as duloxetine.

  6. The Effect of Initial Duloxetine Dosing Strategy on Nausea in Korean Patients with Major Depressive Disorder

    PubMed Central

    Lee, Min-Soo; Ahn, Yong Min; Chung, Seockhoon; Walton, Richard; Kim, Mun Sung

    2012-01-01

    Objective To assess the relative severity of nausea in patients from Korea with major depressive disorder (MDD) who were treated with duloxetine at low (30 mg) or high (60 mg) doses, with or without food, for the first week of an 8 week treatment. Methods Adult patients (n=249), with MDD and a 17-item Hamilton Rating Scale for Depression (HAMD17) score of ≥15, received open-label once daily duloxetine. At Week 0, patients were randomized to 4 groups: 30 mg with food (n=63), 60 mg with food (n=59), 30 mg without food (n=64), and 60 mg without food (n=63). At Week 1, all patients switched to duloxetine 60 mg for 7 weeks. The primary outcome measure was item 112 (nausea) of the Association for Methodology and Documentation in Psychiatry adverse event scale. Effectiveness was assessed by change in HAMD17 total score. Results Overall, 94.4% (235/249) of patients completed Week 1 and 55.0% (137/249) of patients completed the study. For Week 1, nausea was significantly less severe for patients who received 30 mg compared with 60 mg duloxetine (p=0.003), regardless of food intake. In all groups, nausea severity was highest at Week 1 and declined throughout the study. HAMD17 score was reduced in all groups and the most common adverse event reported was nausea (145/249; 58.2%). Conclusion To minimize nausea, Korean patients with MDD who require duloxetine treatment could be given 30 mg once daily, regardless of food, for the first week followed by 60 mg once daily for the course of therapy. PMID:23251205

  7. Differential inhibition of cardiac and neuronal Na(+) channels by the selective serotonin-norepinephrine reuptake inhibitors duloxetine and venlafaxine.

    PubMed

    Stoetzer, Carsten; Papenberg, Bastian; Doll, Thorben; Völker, Marc; Heineke, Joerg; Stoetzer, Marcus; Wegner, Florian; Leffler, Andreas

    2016-07-15

    Duloxetine and venlafaxine are selective serotonin-norepinephrine-reuptake-inhibitors used as antidepressants and co-analgesics. While venlafaxine rather than duloxetine induce cardiovascular side-effects, neither of the substances are regarded cardiotoxic. Inhibition of cardiac Na(+)-channels can be associated with cardiotoxicity, and duloxetine was demonstrated to block neuronal Na(+)-channels. The aim of this study was to investigate if the non-life threatening cardiotoxicities of duloxetine and venlafaxine correlate with a weak inhibition of cardiac Na(+)-channels. Effects of duloxetine, venlafaxine and amitriptyline were examined on endogenous Na(+)-channels in neuroblastoma ND7/23 cells and on the α-subunits Nav1.5, Nav1.7 and Nav1.8 with whole-cell patch clamp recordings. Tonic block of the cardiac Na(+)-channel Nav1.5 and rat-cardiomyocytes (CM) revealed a higher potency for duloxetine (Nav 1.5 IC50 14±1µM, CM IC50 27±3µM) as compared to venlafaxine (Nav 1.5 IC50 671±26µM, CM IC50 452±34µM). Duloxetine was as potent as the cardiotoxic antidepressant amitriptyline (IC50 13±1µM). While venlafaxine almost failed to induce use-dependent block on Nav1.5 and cardiomyocytes, low concentrations of duloxetine (1, 10µM) induced prominent use-dependent block similar to amitriptyline. Duloxetine, but not venlafaxine stabilized fast and slow inactivation and delayed recovery from inactivation. Duloxetine induced an unselective inhibition of neuronal Na(+)-channels (IC50 ND7/23 23±1µM, Nav1.7 19±2µM, Nav1.8 29±2). Duloxetine, but not venlafaxine inhibits cardiac Na(+)-channels with a potency similar to amitriptyline. These data indicate that an inhibition of Na(+)-channels does not predict a clinically relevant cardiotoxicity.

  8. Effects of duloxetine on microRNA expression profile in frontal lobe and hippocampus in a mouse model of depression.

    PubMed

    Pan, Bing; Liu, Yamei

    2015-01-01

    Depression is a major mood disorder affecting people worldwide. The posttranscriptional gene regulation mediated by microRNAs (miRNAs) which may have critical roles in the pathogenesis of depression. However, to date, little is known about the effects of the antidepressant drug duloxetine on miRNA expression profile in chronic unpredictable mild stress (CUMS)-induced depression model in mice. Healthy adult male Kunming mice were randomly divided into three groups: control group, model group and duloxetine group. Sucrose preference test and open field test were used to represent the behavioral change. MiRNAs levels in frontal lobe and hippocampus of mice were analyzed using miRNA microarrays assay. We observed that long-term treatment with duloxetine significantly ameliorated the CUMS procedure-induced sucrose preference decreases and mice treated with duloxetine demonstrated a reversal of the number of crossings, and rearings reduced by CUMS. A significant upregulation of miR-132 and miR-18a in hippocampus in the duloxetine treatment group compared with model group, whereas the levels of miR-134 and miR-124a were significantly downregulated. Furthermore, miR-18a showed significant upregulation in frontal lobe in the duloxetine treatment group relative to model group. Our data showed that miRNA expression profile in frontal lobe and hippocampus was affected by duloxetine in mice model of depression. The effect was especially pronounced in the hippocampus, suggesting that hippocampus might be the action site of duloxetine, which presumably worked by regulating the expression of miRNA levels.

  9. A six-month double-blind, placebo-controlled, randomized clinical trial of duloxetine for the treatment of fibromyalgia

    PubMed Central

    Chappell, Amy S; Bradley, Laurence A; Wiltse, Curtis; Detke, Michael J; D’Souza, Deborah N; Spaeth, Michael

    2008-01-01

    Objective: Assess the efficacy of duloxetine 60/120 mg (N = 162) once daily compared with placebo (N = 168) in the treatment of patients with fibromyalgia, during six months of treatment. Methods: This was a phase-III, randomized, double-blind, placebo-controlled, parallel-group study assessing the efficacy and safety of duloxetine. Results: There were no significant differences between treatment groups on the co-primary efficacy outcome measures, change in the Brief Pain Inventory (BPI) average pain severity from baseline to endpoint (P = 0.053) and the Patient’s Global Impressions of Improvement (PGI-I) at endpoint (P = 0.073). Duloxetine-treated patients improved significantly more than placebo-treated patients on the Fibromyalgia Impact Questionnaire pain score, BPI least pain score and average interference score, Clinical Global Impressions of Severity scale, area under the curve of pain relief, Multidimensional Fatigue Inventory mental fatigue dimension, Beck Depression Inventory-II total score, and 36-item Short Form Health Survey mental component summary and mental health score. Nausea was the most common treatment-emergent adverse event in the duloxetine group. Overall discontinuation rates were similar between groups. Conclusions: Although duloxetine 60/120 mg/day failed to demonstrate significant improvement over placebo on the co-primary outcome measures, in this supportive study, duloxetine demonstrated significant improvement compared with placebo on numerous secondary measures. PMID:20428412

  10. An open treatment trial of duloxetine in elderly patients with dysthymic disorder

    PubMed Central

    Kerner, Nancy; D’Antonio, Kristina; Pelton, Gregory H; Salcedo, Elianny; Ferrar, Jennifer; Roose, Steven P

    2014-01-01

    Objective: We evaluated the efficacy and side effects of the selective serotonin and norepinephrine reuptake inhibitor antidepressant duloxetine in older adults with dysthymic disorder. Methods: Patients ≥ 60 years old with dysthymic disorder received flexible dose duloxetine 20–120 mg daily in an open-label 12-week trial. The main outcomes were change from baseline to 12 weeks in 24-item Hamilton Depression Rating Scale scores and Treatment Emergent Symptoms Scale scores. Response required ≥ 50% decline in Hamilton Depression Rating Scale scores with a Clinical Global Impression of much improved or better, and remission required final Hamilton Depression Rating Scale ≤ 6. Intent-to-treat analyses were conducted with the last observation carried forward. Results: In 30 patients, the mean age was 70.7 (standard deviation (SD) = 7.6) years and 56.7% were female. In intent-to-treat analyses, there were 16 responders (53.3%) and 10 remitters (33.3%). Of these, 19 patients completed the trial. The mean maximum dose was 76.3 mg (SD = 38.5) in the total sample and 101 mg (SD = 17.9) in completers. In the total sample, the mean final dose was 51 mg (SD = 27.2) and correlated significantly with decline in Hamilton Depression Rating Scale (p < .03); decline in Hamilton Depression Rating Scale correlated significantly with decline in Treatment Emergent Symptoms Scale (p < .001). Daily doses above 60 mg were associated with greater improvement and well tolerated. This result was partly confounded by early dropouts having received low doses. Demographic and medical comorbidities, including cardiac disease and hypertension, were not related to response. Somatic side effects were common prior to duloxetine treatment and improved rather than worsened with duloxetine. There were no serious adverse events. Conclusion: Duloxetine at relatively high doses showed moderate efficacy in elderly patients with dysthymic disorder and was well tolerated in successful completers

  11. Validated Colorimetric Assay of Clonidine Hydrochloride from Pharmaceutical Preparations.

    PubMed

    Corciova, Andreia

    2016-01-01

    Clonidine hydrochloride is an antihypertensive agent used for migraine prophylaxis, attention deficit hyperactivity disorder, menopausal flushing and Tourette syndrome. The quantity of the active substance in pharmaceutical preparations must be within specific limits, in agreement with the respective label claim. Therefore, the aim of this study was to establish the conditions for two spectrophotometric methods for clonidine determination, based on the formation of the ion pair complex between clonidine hydrochloride and thymol blue/bromophenol blue. A Jasco UV-Vis 530 spectrophotometer was used for the analysis and the maxim absorbance was measured at 418 nm/448 nm against blank solution. After validation, the methods were used for quantification of clonidine hydrochloride in two commercial samples (tablets). The recovery of active substance varies between 98.06 and 100.13 % without interferences from the excipients.

  12. Validated Colorimetric Assay of Clonidine Hydrochloride from Pharmaceutical Preparations

    PubMed Central

    Corciova, Andreia

    2016-01-01

    Clonidine hydrochloride is an antihypertensive agent used for migraine prophylaxis, attention deficit hyperactivity disorder, menopausal flushing and Tourette syndrome. The quantity of the active substance in pharmaceutical preparations must be within specific limits, in agreement with the respective label claim. Therefore, the aim of this study was to establish the conditions for two spectrophotometric methods for clonidine determination, based on the formation of the ion pair complex between clonidine hydrochloride and thymol blue/bromophenol blue. A Jasco UV-Vis 530 spectrophotometer was used for the analysis and the maxim absorbance was measured at 418 nm/448 nm against blank solution. After validation, the methods were used for quantification of clonidine hydrochloride in two commercial samples (tablets). The recovery of active substance varies between 98.06 and 100.13 % without interferences from the excipients. PMID:27610155

  13. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section 522.1222b Food and Drugs FOOD AND... hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. (a) Chemical name... hydrochloride, 10- phenothiazine monohydrochloride, and aminopentamide hydrogen sulfate. (b) Specifications....

  14. Iontophoretic transdermal delivery of buspirone hydrochloride in hairless mouse skin.

    PubMed

    Al-Khalili, Mohammad; Meidan, Victor M; Michniak, Bozena B

    2003-01-01

    The transdermal delivery of buspirone hydrochloride across hairless mouse skin and the combined effect of iontophoresis and terpene enhancers were evaluated in vitro using Franz diffusion cells. Iontophoretic delivery was optimized by evaluating the effect of drug concentration, current density, and pH of the vehicle solution. Increasing the current density from 0.05 to 0.1 mA/cm2 resulted in doubling of the iontophoretic flux of buspirone hydrochloride, while increasing drug concentration from 1% to 2% had no effect on flux. Using phosphate buffer to adjust the pH of the drug solution decreased the buspirone hydrochloride iontophoretic flux relative to water solutions. Incorporating buspirone hydrochloride into ethanol:water (50:50 vol/vol) based gel formulations using carboxymethylcellulose and hydroxypropylmethylcellulose had no effect on iontophoretic delivery. Incorporation of three terpene enhancers (menthol, cineole, and terpineol) into the gel resulted in a synergistic effect when combined with iontophoresis. Menthol was the most active enhancer, and when combined with iontophoresis it was possible to deliver 10 mg/cm2/day of buspirone hydrochloride.

  15. Probing the Interaction between Acotiamide Hydrochloride and Pepsin by Multispectral Methods, Electrochemical Measurements, and Docking Studies.

    PubMed

    He, Jiawei; Ma, Xianglin; Wang, Qing; Huang, Yanmei; Li, Hui

    2016-07-01

    The interaction between acotiamide hydrochloride and pepsin was systematically characterized by fluorescence and electrochemical approaches. Fluorescence lifetime measurements showed that acotiamide hydrochloride quenched the intrinsic fluorescence of pepsin with a new complex formation via static mode, which was reconfirmed by cyclic voltammetry results. Both of the binding number and binding constants were calculated from differential pulse voltammetry analysis and fluorescence spectroscopy. The values obtained from the above two methods displayed a relatively high degree of consistency. Thermodynamic parameters suggested that acotiamide hydrochloride interacted with pepsin spontaneously by hydrogen bonding and van der Waals interactions. These results were consistent with the results obtained from molecular docking analysis. As revealed by synchronous fluorescence, three-dimensional fluorescence, Fourier transform infrared spectrometry, and circular dichroism spectra, acotiamide hydrochloride could affect the microenvironment and slightly change the secondary structure of pepsin. Furthermore, acotiamide hydrochloride can inhibit pepsin activity in vitro, as explained by the molecular docking.

  16. Real-world comparison of health care utilization between duloxetine and pregabalin initiators with fibromyalgia

    PubMed Central

    Peng, X; Sun, P; Novick, D; Andrews, J; Sun, S

    2014-01-01

    Objectives To compare health care utilization of duloxetine initiators and pregabalin initiators among fibromyalgia patients in a real-world setting. Methods A retrospective cohort study was conducted based on a US national commercial health claims database (2006–2009). Fibromyalgia patients who initiated duloxetine or pregabalin in 2008, aged 18–64 years, and who maintained continuous health insurance coverage 1 year before and 1 year after initiation were assigned to duloxetine or pregabalin cohorts on the basis of their initiated agent. Patients who had pill coverage of the agents over the course of 90 days preceding the initiation were excluded. The two comparative cohorts were constructed using propensity score greedy match methods. Descriptive analysis and paired t-test were performed to compare health care utilization rates in the postinitiation year and the changes of these rates from the preinitiation year to the postinitiation year. Results Both matched cohorts (n=1,265 pairs) had a similar mean initiation age (49–50 years), percentage of women (87%–88%), and prevalence of baseline comorbid conditions (neuropathic pain other than diabetic peripheral neuropathic pain, low back pain, cardiovascular disease, hypertension, headache or migraine, and osteoarthritis). In the preinitiation year, both cohorts had similar inpatient, outpatient, and medication utilization rates (inpatient, 15.7%–16.1%; outpatient, 100.0%; medication, 97.9%–98.7%). The utilization rates diverged in the postinitiation year, with the pregabalin cohort using more fibromyalgia-related inpatient care (3.2% versus 2.2%; P<0.05), any inpatient care (19.3% versus 16.8%; P<0.05), and fibromyalgia-related outpatient care (62.1% versus 51.8%; P<0.05). From the preinitiation period to the postinitiation period, the duloxetine cohort experienced decreases in certain utilization rates, whereas the pregabalin cohort had increases (percentage of patients with a fibromyalgia

  17. Safety and tolerability of duloxetine in the treatment of patients with fibromyalgia: pooled analysis of data from five clinical trials.

    PubMed

    Choy, Ernest H S; Mease, Philip J; Kajdasz, Daniel K; Wohlreich, Madelaine M; Crits-Christoph, Paul; Walker, Daniel J; Chappell, Amy S

    2009-09-01

    The purpose of this report is to describe the overall safety profile of both short- and longer-term duloxetine treatment of fibromyalgia. Data from four double-blind, randomized, placebo-controlled studies (two with 6-month open-label extension phases) and a 1-year, open-label safety study were included. Safety measures included treatment-emergent adverse events (TEAEs), adverse events leading to discontinuation, serious adverse events (SAEs), clinical laboratory tests, vital signs, and electrocardiograms. The most common TEAEs for short-term treatment with duloxetine were nausea (29.3%), headache (20.0%), dry mouth (18.2%), insomnia (14.5%), fatigue (13.5%), constipation (14.5%), diarrhea (11.6%), and dizziness (11.0%; all p < 0.05 vs. placebo). Most TEAEs emerged early and were mild to moderate in severity. The profile of adverse events in patients enrolled at least 6 months, and for patients in the 1-year study, was similar to that found in the short-term treatment studies, with no new adverse events emerging at a notable rate. About 20% of patients discontinued due to adverse events in the short-term treatment studies and in the 1-year study. SAEs were uncommon, and none occurred at a significantly higher frequency for duloxetine compared with placebo. Mean changes in vital signs and weight were small. Rates of treatment-emergent potentially clinically significant (PCS) vital sign, laboratory, and electrocardiogram measures were low, with only PCS rates of alanine aminotransferase being significantly higher for duloxetine compared with placebo in the placebo-controlled treatment studies. In the 1-year study, four patients (1.1%) had suicide-related behavior. The data provided here summarize short- and long-term safety from five clinical studies in patients treated with duloxetine for fibromyalgia. In addition, postmarketing surveillance continues for adverse events reported with duloxetine in fibromyalgia, as in other indications.

  18. Compatibility of cholecalciferol, haloperidol, imipramine hydrochloride, levodopa/carbidopa, lorazepam, minocycline hydrochloride, tacrolimus monohydrate, terbinafine, tramadol hydrochloride and valsartan in SyrSpend SF PH4 oral suspensions.

    PubMed

    Polonini, H C; Silva, S L; Cunha, C N; Brandão, M A F; Ferreira, A O

    2016-04-01

    A challenge with compounding oral liquid formulations is the limited availability of data to support the physical, chemical and microbiological stability of the formulation. This poses a patient safety concern and a risk for medication errors. The objective of this study was to evaluate the compatibility of the following active pharmaceutical ingredients (APIs) in 10 oral suspensions, using SyrSpend SF PH4 (liquid) as the suspending vehicle: cholecalciferol 50,000 IU/mL, haloperidol 0.5 mg/mL, imipramine hydrochloride 5.0 mg/mL, levodopa/carbidopa 5.0/1.25 mg/mL, lorazepam 1.0 mg/mL, minocycline hydrochloride 10.0 mg/mL, tacrolimus monohydrate 1.0 mg/mL, terbinafine 25.0 mg/mL, tramadol hydrochloride 10.0 mg/mL and valsartan 4.0 mg/mL. The suspensions were stored both refrigerated (2 - 8 degrees C) and at controlled room temperature (20 - 25 degrees C). This is the first stability study for these APIs in SyrSpend SF PH4 (liquid). Further, the stability of haloperidol,ilmipramine hydrochloride, minocycline, and valsartan in oral suspension has not been previously reported in the literature. Compatibility was assessed by measuring percent recovery at varying time points throughout a 90 days period. Quantification of the APIs was performed by high performance liquid chromatography (HPLC-UV). Given the percentage of recovery of the APIs within the suspensions, the beyond-use date of the final preparations was found to be at least 90 days for most suspensions both refrigerated and at room temperature. Exceptions were: Minocycline hydrochloride at both storage temperatures (60 days), levodopa/carbidopa at room temperature (30 days), and lorazepam at room temperature (60 days). This suggests that compounded suspensions of APIs from different pharmacological classes in SyrSpend SF PH4 (liquid) are stable.

  19. Duloxetine in OsteoArthritis (DOA) study: study protocol of a pragmatic open-label randomised controlled trial assessing the effect of preoperative pain treatment on postoperative outcome after total hip or knee arthroplasty

    PubMed Central

    Blikman, T; Rienstra, W; van Raaij, T M; ten Hagen, A J; Dijkstra, B; Zijlstra, W P; Bulstra, S K; van den Akker-Scheek, I; Stevens, M

    2016-01-01

    Introduction Residual pain is a major factor in patient dissatisfaction following total hip arthroplasty or total knee arthroplasty (THA/TKA). The proportion of patients with unfavourable long-term residual pain is high, ranging from 7% to 34%. There are studies indicating that a preoperative degree of central sensitisation (CS) is associated with poorer postoperative outcomes and residual pain. It is thus hypothesised that preoperative treatment of CS could enhance postoperative outcomes. Duloxetine has been shown to be effective for several chronic pain syndromes, including knee osteoarthritis (OA), in which CS is most likely one of the underlying pain mechanisms. This study aims to evaluate the postoperative effects of preoperative screening and targeted duloxetine treatment of CS on residual pain compared with care-as-usual. Methods and analysis This multicentre, pragmatic, prospective, open-label, randomised controlled trial includes patients with idiopathic hip/knee OA who are on a waiting list for primary THA/TKA. Patients at risk for CS will be randomly allocated to the preoperative duloxetine treatment programme group or the care-as-usual control group. The primary end point is the degree of postoperative pain 6 months after THA/TKA. Secondary end points at multiple time points up to 12 months postoperatively are: pain, neuropathic pain-like symptoms, (pain) sensitisation, pain catastrophising, joint-associated problems, physical activity, health-related quality of life, depressive and anxiety symptoms, and perceived improvement. Data will be analysed on an intention-to-treat basis. Ethics and dissemination The study is approved by the local Medical Ethics Committee (METc 2014/087) and will be conducted according to the principles of the Declaration of Helsinki (64th, 2013) and the Good Clinical Practice standard (GCP), and in compliance with the Medical Research Involving Human Subjects Act (WMO). Trial registration number 2013-004313-41; Pre

  20. Predictors of duloxetine response in patients with oxaliplatin-induced painful chemotherapy-induced peripheral neuropathy (CIPN): a secondary analysis of randomised controlled trial – CALGB/alliance 170601

    PubMed Central

    SMITH, E.M.L.; PANG, H.; YE, C.; CIRRINCIONE, C.; FLEISHMAN, S.; PASKETT, E.D.; AHLES, T.; BRESSLER, L.R.; LE-LINDQWISTER, N.; FADUL, C.E.; LOPRINZI, C.; SHAPIRO, C.L.

    2016-01-01

    Duloxetine is an effective treatment for oxaliplatin-induced painful chemotherapy-induced peripheral neuropathy (CIPN). However, predictors of duloxetine response have not been adequately explored. The objective of this secondary and exploratory analysis was to identify predictors of duloxetine response in patients with painful oxaliplatin-induced CIPN. Patients (N = 106) with oxaliplatin-induced painful CIPN were randomised to receive duloxetine or placebo. Eligible patients had chronic CIPN pain and an average neuropathic pain score ≥4/10. Duloxetine/placebo dose was 30 mg/day for 7 days, then 60 mg/day for 4 weeks. The Brief Pain Inventory-Short Form and the EORTC QLQ-C30 were used to assess pain and quality of life, respectively. Univariate and multiple logistic regression analyses were performed to identify demographic, physiologic and psychological predictors of duloxetine response. Higher baseline emotional functioning predicted duloxetine response (≥30% reduction in pain; OR 4.036; 95% CI 0.999–16.308; p = 0.050). Based on the results from a multiple logistic regression using patient data from both the duloxetine and placebo treatment arms, duloxetine-treated patients with high emotional functioning are more likely to experience pain reduction (p = 0.026). In patients with painful, oxaliplatin-induced CIPN, emotional functioning may also predict duloxetine response. ClinicalTrials.gov, Identifier NCT00489411 PMID:26603828

  1. [Neuropharmacological studies on tolperisone hydrochloride (author's transl)].

    PubMed

    Fujii, Y; Ishii, Y; Suzuki, T; Murayama, S

    1979-10-01

    Neuropharmacological properties of tolperisone hydrochloride (2,4'-dimethyl-3-piperidinopropiophenone hydrochloride) were investigated in mice, rats and cats. Tolperisone inhibited the spontaneous movement and methamphetamine-induced hyperactivity in mice and the ED50 was approx. 50 mg/kg, s.c. At this dose, tolperisone did not prolong the pentobarbital-induced sleeping time. Tolperisone inhibited convulsions induced by pentylenetetrazol, nicotine and maximum electric shock, but did not affect convulsions induced by strychnine and picrotoxin. Tolperisone induced muscle relaxation in mice and rats in several pharmacological tests, but did not affect neuro-muscular transmission. Tolperisone did not affect conditioned avoidance response in rats and methamphetamine-induced rotational behaviour in nigro-lesioned rats. Tolperisone reduced decerebrated rigidity in cats with i.v. administration of 5 approximately 10 mg/kg and intraduodenal administration of 50 approximately 100 mg/kg. Tolperisone elicited a slight drowsy pattern in the spontaneous EEG of cats at 5 approximately 10 mg/kg, i.v., and inhibited the EEG arousal response and pressor response to stimulation of mesencephalic reticular formation or posterior hypothalamic area. These results suggest that inhibition of the activity in the gamma pathway descending from the mesencephalic reticular formation may be involved in the mechanism of muscle relaxant action of tolperisone.

  2. Neuroprotective effect of penehyclidine hydrochloride on focal cerebral ischemia-reperfusion injury★

    PubMed Central

    Yu, Cuicui; Wang, Junke

    2013-01-01

    Penehyclidine hydrochloride can promote microcirculation and reduce vascular permeability. However, the role of penehyclidine hydrochloride in cerebral ischemia-reperfusion injury remains unclear. In this study, in vivo middle cerebral artery occlusion models were established in experimental rats, and penehyclidine hydrochloride pretreatment was given via intravenous injection prior to model establishment. Tetrazolium chloride, terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate-biotin nick end labeling and immunohistochemical staining showed that, penehyclidine hydrochloride pretreatment markedly attenuated neuronal histopathological changes in the cortex, hippocampus and striatum, reduced infarction size, increased the expression level of Bcl-2, decreased the expression level of caspase-3, and inhibited neuronal apoptosis in rats with cerebral ischemia-reperfusion injury. Xanthine oxidase and thiobarbituric acid chromogenic results showed that penehyclidine hydrochloride upregulated the activity of superoxide dismutase and downregulated the concentration of malondialdehyde in the ischemic cerebral cortex and hippocampus, as well as reduced the concentration of extracellular excitatory amino acids in rats with cerebral ischemia-reperfusion injury. In addition, penehyclidine hydrochloride inhibited the expression level of the NR1 subunit in hippocampal nerve cells in vitro following oxygen-glucose deprivation, as detected by PCR. Experimental findings indicate that penehyclidine hydrochloride attenuates neuronal apoptosis and oxidative stress injury after focal cerebral ischemia-reperfusion, thus exerting a neuroprotective effect. PMID:25206707

  3. Action of tilidine hydrochloride and morphine hydrochloride on ventilatory control in normal subjects.

    PubMed

    Maranetra, N; Pain, M C

    1976-03-20

    The action of tilidine hydrochloride and morphine hydrochloride on the ventilatory response to inhaled carbon dioxide has been assessed in 10 normal volunteers. In doses of 50 mg and 100 mg given intravenously, tilidine hydrochloride induced less respiratory depression than 10 mg of morphine given intravenously. Side effects were not different or troublesome with either drug. Depending on its relative pain-relieving property, tilidine hydrochloride may have advantages over morphine as an analgesic.

  4. Isolation and identification of two unknown impurities from the raw material of clindamycin hydrochloride.

    PubMed

    Sun, Qiushi; Li, Yue; Qin, Li

    2014-10-01

    Clindamycin hydrochloride belongs to the antibiotic family of lincomycin. It has the same antibacterial spectrum as lincomycin, but the antibacterial activity is four to eight times stronger than that of lincomycin. There have been some adverse reactions in clinical use of clindamycin hydrochloride and its finished drug products. The impurities in drugs are directly related to their safety. In this study, two unknown impurities were isolated from the raw material of clindamycin hydrochloride through various chromatographic methods. Their structures were identified as clindamycin isomer (impurity 1) and dehydroclindamycin (impurity 2) by mass spectrometry and NMR spectroscopy. Both of them were found for the first time. The two impurities exhibit a similar but lower antibacterial activity compared with clindamycin hydrochloride.

  5. Rapid onset of syndrome of inappropriate antidiuretic hormone secretion induced by duloxetine in an elderly type 2 diabetic patient with painful diabetic neuropathy.

    PubMed

    Kamei, Shinji; Kaneto, Hideaki; Tanabe, Akihito; Irie, Shintaro; Hirata, Yurie; Shimoda, Masashi; Kohara, Kenji; Mune, Tomoatsu; Kaku, Kohei

    2015-05-01

    Diabetic neuropathy is the most common diabetic complication. Duloxetine, a serotonin noradrenaline reuptake inhibitor (SNRI), is widely used for the treatment of diabetic painful neuropathy (DPN) because of the efficacy and safety profile. Syndrome of inappropriate antidiuretic hormone secretion, which is strongly associated duloxetine, is a rare but occasionally life-threatening adverse effect. Here, we report a case of syndrome of inappropriate antidiuretic hormone secretion that rapidly developed after starting duloxetine in an elderly Japanese female type 2 diabetes mellitus patient. Furthermore, we discuss the possible relationship between the onset of syndrome of inappropriate antidiuretic hormone secretion and the gene polymorphism of cytochrome P450 isoform 1A2 and 2D6, both of which are responsible for duloxetine metabolism.

  6. Biowaiver monographs for immediate release solid oral dosage forms: ciprofloxacin hydrochloride.

    PubMed

    Olivera, M E; Manzo, R H; Junginger, H E; Midha, K K; Shah, V P; Stavchansky, S; Dressman, J B; Barends, D M

    2011-01-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of new multisource and reformulated immediate release (IR) solid oral dosage forms containing ciprofloxacin hydrochloride as the only active pharmaceutical ingredient (API) are reviewed. Ciprofloxacin hydrochloride's solubility and permeability, its therapeutic use and index, pharmacokinetics, excipient interactions and reported BE/bioavailability (BA) problems were taken into consideration. Solubility and BA data indicate that ciprofloxacin hydrochloride is a BCS Class IV drug. Therefore, a biowaiver based approval of ciprofloxacin hydrochloride containing IR solid oral dosage forms cannot be recommended for either new multisource drug products or for major scale-up and postapproval changes (variations) to existing drug products.

  7. Desipramine hydrochloride overdose

    MedlinePlus

    ... measure and monitor the patient's vital signs, including temperature, pulse, breathing rate, and blood pressure. Tests may be done to check the person's heart function. Symptoms will be treated. The person may receive: Activated charcoal Breathing support, including a tube through the mouth ...

  8. Efficacy of Duloxetine in the Early Management of Urinary Continence after Radical Prostatectomy

    PubMed Central

    Alan, Cabir; Eren, Ali E.; Ersay, Ahmet R.; Kocoglu, Hasan; Basturk, Gokhan; Demirci, Emrah

    2015-01-01

    Aim To evaluate the efficacy of early duloxetine therapy in stress urinary incontinence occurring after radical prostatectomy (RP). Material and Method Patients that had RP were randomly divided into 2 groups following the removal of the urinary catheter. Group A patients (n = 28) had pelvic floor exercise and duloxetine therapy. Group B patients (n = 30) had only pelvic floor exercise. The incontinence status of the patients and number of pads were recorded and 1-hour pad test and Turkish validation of International Consultation on Incontinence Questionnaire-Short Form test were applied to the patients at the follow-up. Results When the dry state of the patients was evaluated, 5, 17, 3, and 2 of 28 Group A patients stated that they were completely dry in the 3rd, 6th, 9th and 12th month respectively and pad use was stopped. There was no continence in 30 Group B in the first 3 months. Twelve, 6, and 8 patients stated that they were completely dry in the 6th, 9th and 12th month, respectively. But 3 of 4 patients in whom dryness could not be provided were using a mean of 7.6 pads in the first day and a mean of 1.3 pads after 1 year. When pad use of the patients was evaluated, the mean monthly number of pad use was determined to be 6.2 (4-8) in the initial evaluation, 2.7 (0-5) in the in 3rd month, 2 (0-3) in the 6th month and 1.6 (0-2) pad/d in the 9th month in the group taking medicine. The mean monthly number of pads used was determined to be 5.8 (4-8) in the initial evaluation, 4.3 (3-8) in the 3rd month, 3 (0-6) in the 6th month and 1.6 (0-6) pad/d in the 9th month in the group not taking medicine. Conclusion According to the results, early duloxetine therapy in stress urinary incontinence that occurred after RP provided early continence. PMID:26195963

  9. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... milliliter of etorphine hydrochloride injection, veterinary, contains 1 mg of etorphine hydrochloride in... use the drug unless diprenorphine hydrochloride injection, veterinary, as provided for in § 522.723, is available for use in reversing the effects of etorphine hydrochloride injection, veterinary....

  10. 21 CFR 522.1462 - Naloxone hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Naloxone hydrochloride injection. 522.1462 Section... § 522.1462 Naloxone hydrochloride injection. (a) Specifications. Naloxone hydrochloride injection is an aqueous sterile solution containing 0.4 milligram of naloxone hydrochloride per milliliter. (b)...

  11. 21 CFR 522.1462 - Naloxone hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Naloxone hydrochloride injection. 522.1462 Section... § 522.1462 Naloxone hydrochloride injection. (a) Specifications. Naloxone hydrochloride injection is an aqueous sterile solution containing 0.4 milligram of naloxone hydrochloride per milliliter. (b)...

  12. Development and validation of chemometrics-assisted spectrophotometry and liquid chromatography methods for the simultaneous determination of the active ingredients in two multicomponent mixtures containing chlorpheniramine maleate and phenylpropanolamine hydrochloride.

    PubMed

    Hadad, Ghada M; El-Gindy, Alaa; Mahmoud, Waleed M M

    2007-01-01

    Multivariate spectrophotometric calibration and liquid chromatography (LC) methods were used for the simultaneous determination of the active ingredients in 2 multicomponent mixtures containing chlorpheniramine maleate and phenylpropanolamine hydrochloride with ibuprofen and caffeine (mixture 1) or with propyphenazone (mixture 2). For the multivariate spectrophotometric calibration methods, principal component regression (PCR) and partial least squares (PLS-1), a calibration set of the mixtures consisting of the components of each mixture was prepared in distilled water. A leave-1-out cross-validation procedure was used to find the optimum numbers of latent variables. Analytical parameters such as sensitivity, selectivity, analytical sensitivity, limit of quantitation, and limit of detection were determined for both PLS-1 and PCR. The LC method depends on the use of a cyanopropyl column with the mobile phase acetonitrile-12 mM ammonium acetate, pH 5.0 (25 + 75, v/v), for mixture 1 or acetonitrile-10 mM potassium dihydrogen phosphate, pH 4.7 (45 + 55, v/v), for mixture 2; the UV detector was set at 212 nm. In spite of the presence of a high degree of spectral overlap of these components, they were rapidly and simultaneously determined with high accuracy and precision, with no interference from the matrix excipients. The proposed methods were successfully applied to the analysis of pharmaceutical formulations and laboratory-prepared mixtures containing the 2 multicomponent combinations.

  13. Functioning in patients with major depression treated with duloxetine or a selective serotonin reuptake inhibitor in East Asia

    PubMed Central

    Novick, Diego; Montgomery, William; Haro, Josep Maria; Moneta, Maria Victoria; Zhu, Gang; Yue, Li; Hong, Jihyung; Dueñas, Héctor; Brugnoli, Roberto

    2016-01-01

    Purpose To assess and compare the levels of functioning in patients with major depressive disorder treated with either duloxetine with a daily dose of ≤60 mg or a selective serotonin reuptake inhibitor (SSRI) as monotherapy for up to 6 months in a naturalistic setting in East Asia. In addition, this study examined the impact of painful physical symptoms (PPS) on the effects of these treatments. Patients and methods Data for this post hoc analysis were taken from a 6-month prospective observational study involving 1,549 patients with major depressive disorder without sexual dysfunction. The present analysis focused on a subgroup of patients from East Asia (n=587). Functioning was measured using the Sheehan Disability Scale (SDS). Depression severity was assessed using the 16-item Quick Inventory of Depressive Symptomatology-Self Report. PPS were rated using the modified Somatic Symptom Inventory. A mixed model with repeated measures was fitted to compare the levels of functioning between duloxetine-treated (n=227) and SSRI-treated (n=225) patients, adjusting for baseline patient characteristics. Results The mean SDS total score was similar between the two treatment cohorts (15.46 [standard deviation =6.11] in the duloxetine cohort and 16.36 [standard deviation =6.53] in the SSRI cohort, P=0.077) at baseline. Both descriptive and regression analyses confirmed improvement in functioning in both groups during follow-up, but duloxetine-treated patients achieved better functioning. At 24 weeks, the estimated mean SDS total score was 4.48 (standard error =0.80) in the duloxetine cohort, which was statistically significantly lower (ie, better functioning) than that of 6.76 (standard error =0.77) in the SSRI cohort (P<0.001). This treatment difference was more apparent in the subgroup of patients with PPS at baseline. Similar patterns were also observed for SDS subscores (work, social life, and family life). Conclusion Depressed patients treated with duloxetine achieved

  14. Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation.

    PubMed

    Eassa, Bayoumy I; El-Shazly, Mohamed A

    2013-01-01

    Premature ejaculation (PE) is the most common sexual disorder. It affects 20%-30% of adult men; the aetiology of this condition has not yet been elucidated. The aim of this study is to evaluate the efficacy, safety, tolerability, undesirable effects and improved satisfaction with sexual intercourse with tramadol hydrochloride at different dosages for the treatment of PE. A total of 300 patients who presented with lifelong (primary) PE were included in this study. The study was performed for 28 weeks, in which placebo (starch tablet) was given for 4 weeks, and active ingredient (tramadol hydrochloride) was administered at different therapeutic dosages for 24 weeks. Patients were divided into three equal groups, each consisting of 100 patients. The first group (A) was given tramadol hydrochloride capsule 25 mg. The second group (B) was given tramadol hydrochloride capsule 50 mg. The third group (C) was given tramadol hydrochloride capsule 100 mg. All of the 300 participants included completed the study voluntarily. The age of the patients varied from 25 to 50 years. After the treatment period, the recorded data were collected for each group and analysed. The results showed a highly significant increase in the mean intravaginal ejaculatory latency time (IELT) in all groups compared to baseline data (P<0.0001). We concluded that using tramadol hydrochloride at different doses on demand for the treatment of PE is effective, safe and tolerable, with minimal undesirable effects, and approval for this indication should be sought.

  15. Using crystal structure prediction to rationalize the hydration propensities of substituted adamantane hydrochloride salts.

    PubMed

    Mohamed, Sharmarke; Karothu, Durga Prasad; Naumov, Panče

    2016-08-01

    The crystal energy landscapes of the salts of two rigid pharmaceutically active molecules reveal that the experimental structure of amantadine hydrochloride is the most stable structure with the majority of low-energy structures adopting a chain hydrogen-bond motif and packings that do not have solvent accessible voids. By contrast, memantine hydrochloride which differs in the substitution of two methyl groups on the adamantane ring has a crystal energy landscape where all structures within 10 kJ mol(-1) of the global minimum have solvent-accessible voids ranging from 3 to 14% of the unit-cell volume including the lattice energy minimum that was calculated after removing water from the hydrated memantine hydrochloride salt structure. The success in using crystal structure prediction (CSP) to rationalize the different hydration propensities of these substituted adamantane hydrochloride salts allowed us to extend the model to predict under blind test conditions the experimental crystal structures of the previously uncharacterized 1-(methylamino)adamantane base and its corresponding hydrochloride salt. Although the crystal structure of 1-(methylamino)adamantane was correctly predicted as the second ranked structure on the static lattice energy landscape, the crystallization of a Z' = 3 structure of 1-(methylamino)adamantane hydrochloride reveals the limits of applying CSP when the contents of the crystallographic asymmetric unit are unknown.

  16. Temperature and concentration dependences of density and refraction of aqueous duloxetine solutions

    NASA Astrophysics Data System (ADS)

    Deosarkar, S. D.; Deoraye, S. M.; Kalyankar, T. M.

    2014-07-01

    Present paper reports the measured densities (ρ) and refractive indices ( n D) of aqueous solutions of Duloxetine drug in wide range of molal concentrations ( m = 0.0101-0.1031 mol kg-1) and at different temperatures (297.15, 302.15, and 307.15 K). Apparent molar volumes (φv) of drug were calculated from density data and fitted to Masson's relation and partial molar volumes (φ{v/0}) were evaluated at different temperatures. Concentration dependence of refractive index ( n D = Kc + n {D/0}) at experimental temperature has been studied. Density and refractive index data has been used for the calculation of specific refractions ( R D). Experimental (ρ and n D) and calculated (φv, φ{v/0}, and R D) properties have been interpreted in terms of concentration and temperature effects on structural fittings and drug-water interactions.

  17. Modified Synthesis of Erlotinib Hydrochloride

    PubMed Central

    Barghi, Leila; Aghanejad, Ayuob; Valizadeh, Hadi; Barar, Jaleh; Asgari, Davoud

    2012-01-01

    Purpose: An improved and economical method has been described for the synthesis of erlotinib hydrochloride, as a useful drug in treatment of non-small-cell lung cancer. Method: Erlotinib hydrochloride was synthesized in seven steps starting from 3, 4-dihydroxy benzoic acid. In this study, we were able to modify one of the key steps which involved the reduction of the 6-nitrobenzoic acid derivative to 6-aminobenzoic acid derivative. An inexpensive reagent such as ammonium formate was used as an in situ hydrogen donor in the presence of palladium/charcoal (Pd/C) instead of hydrogen gas at high pressure. Result: This proposed method proceeded with 92% yield at room temperature. Synthesis of erlotinib was completed in 7 steps with overall yield of 44%. Conclusion: From the results obtained it can be concluded that the modified method eliminated the potential danger associated with the use of hydrogen gas in the presence of flammable catalysts. It should be mentioned that the catalyst was recovered after the reaction and could be used again. PMID:24312780

  18. Evaluation of genetic models for response in a randomized clinical trial of duloxetine in major depressive disorder.

    PubMed

    Houston, John P; Zou, Wei; Aris, Virginie; Fijal, Bonnie; Chen, Peining; Heinloth, Alexandra N; Martinez, James

    2012-11-30

    In self-identified white patients with major depressive disorder (N=126) treated with open-label duloxetine (60-120 mg/d), a significant association of (P=0.020) of a composite risk score (based on SLC6A2 rs5569 [G1287A] AA, HTR1A rs6295 [C(-1019)G] GG, and COMT rs174697 AA/AG) with 17-item Hamilton Depression Rating Scale total score change from baseline to 12 weeks was observed.

  19. Immobilization of porcupines with tiletamine hydrochloride and zolazepam hydrochloride (Telazol).

    PubMed

    Hale, M B; Griesemer, S J; Fuller, T K

    1994-07-01

    Immobilization of North American porcupines (Erethizon dorsatum) with tiletamine hydrochloride (HCl) and zolazepam HCl (Telazol) was evaluated in central Massachusetts (USA) during 1991 and 1992. Doses between 9 and 11 mg/kg resulted in a mean (+/- SD) induction time of 3.2 +/- 1.3 min and a mean (+/- SD) immobilization time of 44.2 +/- 19.5 min. Induction time did not differ by dose, sex, capture method, or porcupine weight. Immobilization time differed by dose and porcupine weight but not by sex or capture method. Tiletamine HCl and zolazepam HCl seems to be an effective combination of drugs for immobilizing porcupines as long as sufficient time is allowed for recovery.

  20. Immobilization of swift foxes with ketamine hydrochloride-xylazine hydrochloride

    USGS Publications Warehouse

    Telesco, R.L.; Sovada, M.A.

    2002-01-01

    There is an increasing need to develop field immobilization techniques that allow researchers to handle safely swift foxes (Vulpes velox) with minimal risk of stress or injury. We immobilized captive swift foxes to determine the safety and effectiveness of ketamine hydrochloride and xylazine hydrochloride at different dosages. We attempted to determine appropriate dosages to immobilize swift foxes for an adequate field-handling period based on three anesthesia intervals (induction period, immobilization period, and recovery period) and physiologic responses (rectal temperature, respiration rate, and heart rate). Between October 1998-July 1999, we conducted four trials, evaluating three different dosage ratios of ketamine and xylazine (2.27:1.2, 5.68:1.2, and 11.4:1.2 mg/kg ketamine:mg/kg xylazine, respectively), followed by a fourth trial with a higher dosage at the median ratio (11.4 mg/kg ketamine:2.4 mg/kg xylazine). We found little difference in induction and recovery periods among trials 1-3, but immobilization time increased with increasing dosage (P<0.08). Both the immobilization period and recovery period increased in trial 4 compared with trials 1-3 (P???0.03). There was a high variation in responses of individual foxes across trials, making it difficult to identify an appropriate dosage for field handling. Heart rate and respiration rates were depressed but all physiologic measures remained within normal parameters established for domestic canids. We recommend a dosage ratio of 10 mg/kg ketamine to 1 mg/kg xylazine to immobilize swift foxes for field handling.

  1. Evaluation of the effect of duloxetine treatment on functioning as measured by the Sheehan disability scale: pooled analysis of data from six randomized, double-blind, placebo-controlled clinical studies.

    PubMed

    Mancini, Michele; Sheehan, David V; Demyttenaere, Koen; Amore, Mario; Deberdt, Walter; Quail, Deborah; Sagman, Doron

    2012-11-01

    The purpose of this work is to describe the effect of duloxetine on functioning as measured by the Sheehan disability scale (SDS) compared with placebo in patients with major depressive disorder (MDD). Pooled data from six randomized, parallel, double-blind, placebo-controlled duloxetine studies in adult MDD patients were analyzed at the short-term (7-13 weeks) and the long-term (>24 weeks) endpoint. The primary variable was the SDS total score. Secondary variables included functional remission (SDS total ≤ 6) rates, Hamilton rating scale for depression total score, and pain visual analog scale. Analysis of covariance and logistic regression methods were used to assess differences in treatment and identify prognostic baseline factors. In total, 2496 patients (1424 duloxetine; 1072 placebo) were included. The between-treatment difference of -2.52 between duloxetine and placebo in the SDS total score at the short-term endpoint was statistically significant in favor of duloxetine vs. placebo (95% confidence interval: -3.17, -1.87; P < 0.001). The endpoint functional remission rates were 39.5% with duloxetine and 28.7% with placebo. Time since first depression episode, antidepressant pretreatment (yes/no), baseline visual analog scale pain (≤30 / >30 mm), and sex were significant prognostic factors. The effect of duloxetine was maintained at the long-term endpoint. Duloxetine is effective in improving MDD patients' functioning. Further antidepressant studies focusing on functioning would be helpful.

  2. A novel asymmetric synthesis of cinacalcet hydrochloride

    PubMed Central

    Gorentla, Laxminarasimhulu; Dubey, Pramod K

    2012-01-01

    Summary A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described. PMID:23019473

  3. Protein stabilization by urea and guanidine hydrochloride.

    PubMed

    Bhuyan, Abani K

    2002-11-12

    The urea, guanidine hydrochloride, salt, and temperature dependence of the rate of dissociation of CO from a nonequilibrium state of CO-bound native ferrocytochrome c has been studied at pH 7. The heme iron of ferrocytochrome c in the presence of denaturing concentrations of guanidine hydrochloride (GdnHCl) and urea prepared in 0.1 M phosphate, pH 7, binds CO. When the unfolded protein solution is diluted 101-fold into CO-free folding buffer, the protein chain refolds completely, leaving the CO molecule bonded to the heme iron. Subsequently, slow thermal dissociation of the CO molecule yields to the heme coordination of the native M80 ligand. Thus, the reaction monitors the rate of thermal conversion of the CO-liganded native ferrocytochrome c to the M80-liganded native protein. The rate of this reaction, k(diss), shows a characteristic dependence on the presence of nondenaturing concentrations of the denaturants in the reaction medium. The rate decreases by approximately 1.9-3-fold as the concentration of GdnHCl in the refolding medium increases from nearly 0 to approximately 2.1 M. Similarly, the rate decreases by 1.8-fold as the urea concentration is raised from 0.l to approximately 5 M. At still higher concentrations of the denaturants the denaturing effect sets in, the protein is destabilized, and hence the CO dissociation rate increases sharply. The activation energy of the reaction, E(a), increases when the denaturant concentration in the reaction medium is raised: from 24.1 to 28.3 kcal mol(-1) for a 0.05-2.1 M rise in GdnHCl and from 25.2 to 26.9 kcal mol(-1) for a 0.1-26.9 M increase in urea. Corresponding to these increases in denaturant concentrations are also increases in the activation entropy, S(diss)/R, where R is the gas constant of the reaction. The denaturant dependence of these kinetic and thermodynamic parameters of the CO dissociation reaction suggests that binding interactions with GdnHCl and urea can increase the structural and energetic

  4. Randomized, Double-blind, Placebo-controlled Phase III Trial of Duloxetine Monotherapy in Japanese Patients With Chronic Low Back Pain

    PubMed Central

    Konno, Shinichi; Oda, Natsuko; Ochiai, Toshimitsu; Alev, Levent

    2016-01-01

    Study Design. A 14-week, randomized, double-blind, multicenter, placebo-controlled study of Japanese patients with chronic low back pain (CLBP) who were randomized to either duloxetine 60 mg once daily or placebo. Objective. This study aimed to assess the efficacy and safety of duloxetine monotherapy in Japanese patients with CLBP. Summary of Background Data. In Japan, duloxetine is approved for the treatment of depression, diabetic neuropathic pain, and pain associated with fibromyalgia; however, no clinical study of duloxetine has been conducted for CLBP. Methods. The primary efficacy measure was the change in the Brief Pain Inventory (BPI) average pain score from baseline to Week 14. Secondary efficacy measures included BPI pain (worst pain, least pain, pain right now), Patient's Global Impression of Improvement, Clinical Global Impressions of Severity, and Roland-Morris Disability Questionnaire, among other measures, and safety and tolerability. Results. In total, 458 patients were randomized to receive either duloxetine (n = 232) or placebo (n = 226). The BPI average pain score improved significantly in the duloxetine group compared with that in the placebo group at Week 14 [−2.43 ± 0.11 vs. −1.96 ± 0.11, respectively; between-group difference (95% confidence interval), − 0.46 [−0.77 to−0.16]; P = 0.0026]. The duloxetine group showed significant improvement in many secondary measures compared with the placebo group, including BPI pain (least pain, pain right now) (between-group difference: −1.69 ± 0.10, P = 0.0009; −2.42 ± 0.12, P P = 0.0230, respectively), Patient's Global Impression of Improvement (2.46 ± 0.07, P = 0.0026), Clinical Global Impressions of Severity (−1.46 ± 0.06, P = 0.0019), and Roland-Morris Disability Questionnaire (−3.86 ± 0.22, P = 0.0439). Adverse events occurring at a significantly higher incidence in the duloxetine group were somnolence

  5. Biowaiver monographs for immediate release solid oral dosage forms based on biopharmaceutics classification system (BCS) literature data: verapamil hydrochloride, propranolol hydrochloride, and atenolol.

    PubMed

    Vogelpoel, H; Welink, J; Amidon, G L; Junginger, H E; Midha, K K; Möller, H; Olling, M; Shah, V P; Barends, D M

    2004-08-01

    Literature data related to the Biopharmaceutics Classification System (BCS) are presented on verapamil hydrochloride, propranolol hydrochloride, and atenolol in the form of BCS-monographs. Data on the qualitative composition of immediate release (IR) tablets containing these active substances with a Marketing Authorization (MA) in the Netherlands (NL) are also provided; in view of these MA's the assumption was made that these tablets were bioequivalent to the innovator product. The development of a database with BCS-related data is announced by the International Pharmaceutical Federation (FIP).

  6. Antinociceptive Effects of the Serotonin and Noradrenaline Reuptake Inhibitors Milnacipran and Duloxetine on Vincristine-Induced Neuropathic Pain Model in Mice.

    PubMed

    Katsuyama, Soh; Aso, Hiromu; Otowa, Akira; Yagi, Tomomi; Kishikawa, Yukinaga; Komatsu, Takaaki; Sakurada, Tsukasa; Nakamura, Hitoshi

    2014-01-01

    Vincristine is an anticancer drug used to treat a variety of cancer types, but it frequently causes peripheral neuropathy. Neuropathic pain is often associated with the appearance of abnormal sensory signs, such as allodynia. Milnacipran and duloxetine, serotonin/noradrenaline reuptake inhibitors, have shown efficacy against several chronic pain syndromes. In this study, we investigated the attenuation of vincristine-induced mechanical allodynia in mice by milnacipran and duloxetine. To induce peripheral neuropathy, vincristine was administered once per day (0.1 mg/kg, intraperitoneally (i.p.)) for 7 days. Mechanical allodynia was evaluated by measuring the withdrawal response to stimulation with a von Frey filament. In vincristine-treated mice, mechanical allodynia was observed on days 3-28 of vincristine administration. A single administration of milnacipran (40 mg/kg, i.p.) or duloxetine (20 mg/kg, i.p.) had no effect on vincristine-induced mechanical allodynia. However, repeated administration of milnacipran (20 or 40 mg/kg, once per day, i.p.) or duloxetine (5, 10, or 20 mg/kg, once per day, i.p.) for 7 days significantly reduced vincristine-induced mechanical allodynia. These results suggest that chronic vincristine administration induces mechanical allodynia, and that repeated milnacipran and duloxetine administration may be an effective approach for the treatment of neuropathic pain caused by vincristine treatment for cancer.

  7. Chromatographic Determination of Aminoacridine Hydrochloride, Lidocaine Hydrochloride and Lidocaine Toxic Impurity in Oral Gel.

    PubMed

    Bebawy, Lories I; Elghobashy, Mohamed R; Abbas, Samah S; Shokry, Rafeek F

    2016-04-01

    Two sensitive and selective analytical methods were developed for simultaneous determination of aminoacridine hydrochloride and lidocaine hydrochloride in bulk powder and pharmaceutical formulation. Method A was based on HPLC separation of the cited drugs with determination of the toxic lidocaine-related impurity 2,6-dimethylaniline. The separation was achieved using reversed-phase column C18, 250 × 4.6 mm, 5 µm particle size and mobile phase consisting of 0.05 M disodium hydrogen phosphate dihydrate (pH 6.0 ± 0.2 adjusted with phosphoric acid) and acetonitrile (55 : 45, v/v). Quantitation was achieved with UV detection at 240 nm. Linear calibration curve was in the range of 1.00-10.00, 13.20-132.00 and 1.32-13.20 µg mL(-1) for aminoacridine hydrochloride, lidocaine hydrochloride and 2,6-dimethylaniline, respectively. Method B was based on TLC separation of the cited drugs followed by densitometric measurement at 365 nm on the fluorescent mode for aminoacridine hydrochloride and 220 nm on the absorption mode for lidocaine hydrochloride. The separation was carried out using ethyl acetate-methanol-acetic acid (65 : 30 : 5 by volume) as a developing system. The calibration curve was in the range of 25.00-250.00 ng spot(-1) and 0.99-9.90 µg spot(-1) for aminoacridine hydrochloride and lidocaine hydrochloride, respectively. The results obtained were statistically analyzed and compared with those obtained by applying the manufacturer's method.

  8. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... recommended dose from 15 to 20 milligrams ketamine base per pound of body weight, depending on the effect... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section 522.1222b Food and Drugs FOOD...

  9. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... recommended dose from 15 to 20 milligrams ketamine base per pound of body weight, depending on the effect... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section 522.1222b Food and Drugs FOOD...

  10. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... recommended dose from 15 to 20 milligrams ketamine base per pound of body weight, depending on the effect... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section 522.1222b Food and Drugs FOOD...

  11. The effects of Dalmane /flurazepam hydrochloride/ on human EEG characteristics.

    NASA Technical Reports Server (NTRS)

    Frost, J. D., Jr.; Carrie, J. R. G.; Borda, R. P.; Kellaway, P.

    1973-01-01

    Evaluation of the changes in the waking EEGs of six healthy male subjects who received 30 mg daily oral doses of flurazepam hydrochloride for two weeks. A placebo was then substituted for flurazepam for another two weeks. An increase in beta activity with a maximum in fronto-central leads was observed during the test period. A small increase in the mean wavelength of the alpha and theta activities in the central-occipital derivations was also apparent in the subjects during the period.

  12. Pregabalin, the lidocaine plaster and duloxetine in patients with refractory neuropathic pain: a systematic review

    PubMed Central

    2010-01-01

    Background Patients frequently fail to receive adequate pain relief from, or are intolerant of, first-line therapies prescribed for neuropathic pain (NeP). This refractory chronic pain causes psychological distress and impacts patient quality of life. Published literature for treatment in refractory patients is sparse and often published as conference abstracts only. The aim of this study was to identify published data for three pharmacological treatments: pregabalin, lidocaine plaster, and duloxetine, which are typically used at 2nd line or later in UK patients with neuropathic pain. Methods A systematic review of the literature databases MEDLINE, EMBASE and CCTR was carried out and supplemented with extensive conference and grey literature searching. Studies of any design (except single patient case studies) that enrolled adult patients with refractory NeP were included in the review and qualitatively assessed. Results Seventeen studies were included in the review: nine of pregabalin, seven of the lidocaine plaster, and one of duloxetine. No head-to-head studies of these treatments were identified. Only six studies included treatments within UK licensed indications and dose ranges. Reported efficacy outcomes were not consistent between studies. Pain scores were most commonly assessed in studies including pregabalin; trials of pregabalin and the lidocaine plaster reported the proportion of responders. Significant improvements in the total, sensory and affective scores of the Short-form McGill Pain Questionnaire, and in function interference, sleep interference and pain associated distress, were associated with pregabalin treatment; limited or no quality of life data were available for the other two interventions. Limitations to the review are the small number of included studies, which are generally small, of poor quality and heterogeneous in patient population and study design. Conclusions Little evidence is available relevant to the treatment of refractory

  13. Comparative efficacy and tolerability of duloxetine, pregabalin, and milnacipran for the treatment of fibromyalgia: a Bayesian network meta-analysis of randomized controlled trials.

    PubMed

    Lee, Young Ho; Song, Gwan Gyu

    2016-05-01

    The aim of this study was to assess the relative efficacy and tolerability of duloxetine, pregabalin, and milnacipran at the recommended doses in patients with fibromyalgia. Randomized controlled trials (RCTs) examining the efficacy and safety of duloxetine 60 mg, pregabalin 300 mg, pregabalin 150 mg, milnacipran 200 mg, and milnacipran 100 mg compared to placebo in patients with fibromyalgia were included in this Bayesian network meta-analysis. Nine RCTs including 5140 patients met the inclusion criteria. The proportion of patients with >30 % improvement from baseline in pain was significantly higher in the duloxetine 60 mg, pregabalin 300 mg, milnacipran 100 mg, and milnacipran 200 mg groups than in the placebo group [pairwise odds ratio (OR) 2.33, 95 % credible interval (CrI) 1.50-3.67; OR 1.68, 95 % CrI 1.25-2.28; OR 1.62, 95 % CrI 1.16-2.25; and OR 1.61; 95 % CrI 1.15-2.24, respectively]. Ranking probability based on the surface under the cumulative ranking curve (SUCRA) indicated that duloxetine 60 mg had the highest probability of being the best treatment for achieving the response level (SUCRA = 0.9431), followed by pregabalin 300 mg (SUCRA = 0.6300), milnacipran 100 mg (SUCRA = 0.5680), milnacipran 200 mg (SUCRA = 0.5617), pregabalin 150 mg (SUCRA = 0.2392), and placebo (SUCRA = 0.0580). The risk of withdrawal due to adverse events was lower in the placebo group than in the pregabalin 300 mg, duloxetine 60 mg, milnacipran 100 mg, and milnacipran 200 mg groups. However, there was no significant difference in the efficacy and tolerability between the medications at the recommended doses. Duloxetine 60 mg, pregabalin 300 mg, milnacipran 100 mg, and milnacipran 200 mg were more efficacious than placebo. However, there was no significant difference in the efficacy and tolerability between the medications at the recommended doses.

  14. Chromatographic Determination of Cyclopentolate Hydrochloride and Phenylephrine Hydrochloride in the Presence of Their Potential Degradation Products.

    PubMed

    Rezk, Mamdouh R; Fayed, Ahmed S; Marzouk, Hoda M; Abbas, Samah S

    2017-03-01

    Two sensitive, selective, and precise stability-indicating methods have been developed for the simultaneous determination of the active pharmaceutical ingredients cyclopentolate hydrochloride (CLO) and phenylephrine hydrochloride (PHE) in their pure forms and in the presence of their degradation products. The methods were applied for the determination of CLO and PHE in a pharmaceutical formulation. Method A was based on isocratic elution HPLC determination. Separation was achieved using a Waters Spherisorb ODS2 C18 analytical column (5 μm particle size) and a mobile phase of 0.1% heptane-1-sulphonic acid sodium salt in methanol-water (80 + 20, v/v). The flow rate was 1.0 mL/min and detection was performed at 210 nm. Method B was an HPTLC- densitometric method using HPTLC silica gel 60 F254 plates and an optimized mobile phase of ethyl acetate-methanol-ammonia (8 + 2 + 0.1, v/v/v). The separated spots were densitometrically scanned at 210 nm. Polynomial equations were used for regression. The developed methods are suitable for the determination of CLO and PHE in their binary mixture and in the presence of their corresponding degradation products. The two methods were validated in compliance with International Conference on Harmonization guidelines and successfully applied for the determination of CLO and PHE as synthetically prepared in laboratory mixtures and in the presence of their possible degradation products. CLO alkaline degradation products were stated as potential impurities in British Pharmacopoeia. The degradation products were separated and identified by mass spectra. Postulation of a PHE oxidative degradation pathway was suggested. The obtained results were statistically analyzed and compared with those obtained by applying the official methods for both drugs.

  15. pH-Responsive chimaeric pepsomes based on asymmetric poly(ethylene glycol)-b-poly(l-leucine)-b-poly(l-glutamic acid) triblock copolymer for efficient loading and active intracellular delivery of doxorubicin hydrochloride.

    PubMed

    Chen, Peipei; Qiu, Min; Deng, Chao; Meng, Fenghua; Zhang, Jian; Cheng, Ru; Zhong, Zhiyuan

    2015-04-13

    pH-Responsive chimaeric polypeptide-based polymersomes (refer to as pepsomes) were designed and developed from asymmetric poly(ethylene glycol)-b-poly(l-leucine)-b-poly(l-glutamic acid) (PEG-PLeu-PGA, PEG is longer than PGA) triblock copolymers for efficient encapsulation and triggered intracellular delivery of doxorubicin hydrochloride (DOX·HCl). PEG-PLeu-PGA was conveniently prepared by sequential ring-opening polymerization of l-leucine N-carboxyanhydride and γ-benzyl-l-glutamate N-carboxyanhydride using PEG-NH2 as an initiator followed by deprotection. Pepsomes formed from PEG-PLeu-PGA had unimodal distribution and small sizes of 64-71 nm depending on PLeu block lengths. Interestingly, these chimaeric pepsomes while stable at pH 7.4 were quickly disrupted at pH 5.0, likely due to alternation of ionization state of the carboxylic groups in PGA that shifts PGA blocks from hydrophilic and random coil structure into hydrophobic and α-helical structure. DOX·HCl could be actively loaded into the watery core of pepsomes with a high loading efficiency. Remarkably, the in vitro release studies revealed that release of DOX·HCl was highly dependent on pH, in which about 24.0% and 75.7% of drug was released at pH 7.4 and 5.0, respectively, at 37 °C in 24 h. MTT assays demonstrated that DOX·HCl-loaded pepsomes exhibited high antitumor activity, similar to free DOX·HCl in RAW 264.7 cells. Moreover, they were also potent toward drug-resistant MCF-7 cancer cells (MCF-7/ADR). Confocal microscopy studies showed that DOX·HCl-loaded pepsomes delivered and released drug into the cell nuclei of MCF-7/ADR cells in 4 h, while little DOX·HCl fluorescence was observed in MCF-7/ADR cells treated with free drug under otherwise the same conditions. These chimaeric pepsomes with facile synthesis, efficient drug loading, and pH-triggered drug release behavior are an attractive alternative to liposomes for targeted cancer chemotherapy.

  16. 40 CFR 721.10687 - Fatty acid amide hydrochlorides (generic).

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 40 Protection of Environment 31 2014-07-01 2014-07-01 false Fatty acid amide hydrochlorides... Specific Chemical Substances § 721.10687 Fatty acid amide hydrochlorides (generic). (a) Chemical substance... fatty acid amide hydrochlorides (PMNs P-13-201, P-13-203, P-13-204, P-13-205, P-13-206, P-13-207,...

  17. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  18. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  19. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Glutamic acid hydrochloride. 182.1047 Section 182...) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Multiple Purpose GRAS Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride. (b) (c) Limitations, restrictions, or explanation....

  20. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  1. Synthesis, spectral, and anti-microbial studies of thioiminium iodides and amine hydrochlorides.

    PubMed

    Britto, Sebastian; Renaud, Philippe; Nallu, Maruthai

    2014-01-01

    To avoid the undesired deprotonation during the addition of organolithium and organomagnesium reagents to ketones, the thioiminium salts, easily prepared from lactams and amides are converted into 2,2-disubstituted and 2-monosubstituted amines by reaction with simple nucleophiles such as organocerium and organocopper reagents. The reaction of thioiminium iodides with organocerium reagents derived by transmetalation of corresponding lithium reagents with anhydrous cerium(III) chloride has been investigated. These thioiminium iodides act as good electrophiles and accept alkylceriums towards bisaddition. The newly synthesized amines have been characterized by 1H and 13C NMR, IR and mass spectra. The amines have been converted into their hydrochlorides and characterized by COSY. These hydrochlorides have been subjected to antimicrobial screening with clinically isolated microorganisms, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella typhi and Candida albicans. The hydrochlorides show quite good activity against these bacteria and fungus.

  2. Biowaiver monographs for immediate release solid oral dosage forms: amitriptyline hydrochloride.

    PubMed

    Manzo, R H; Olivera, M E; Amidon, G L; Shah, V P; Dressman, J B; Barends, D M

    2006-05-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing amitriptyline hydrochloride are reviewed. Its therapeutic uses, its pharmacokinetic properties, the possibility of excipient interactions and reported BE/bioavailability (BA) problems are also taken into consideration. Literature data indicates that amitriptyline hydrochloride is a highly permeable active pharmaceutical ingredient (API). Data on the solubility according to the current Biopharmaceutics Classification System (BCS) were not fully available and consequently amitriptyline hydrochloride could not be definitively assigned to either BCS Class I or BCS Class II. But all evidence taken together, a biowaiver can currently be recommended provided that IR tablets are formulated with excipients used in existing approved products and that the dissolution meets the criteria defined in the Guidances.

  3. Does early improvement in depressive symptoms predict subsequent remission in patients with depression who are treated with duloxetine?

    PubMed Central

    Sueki, Akitsugu; Suzuki, Eriko; Takahashi, Hitoshi; Ishigooka, Jun

    2016-01-01

    Purpose In this prospective study, we examined whether early reduction in depressive symptoms predicts later remission to duloxetine in the treatment of depression, as monitored using the Montgomery–Asberg Depression Rating Scale (MADRS). Patients and methods Among the 106 patients who were enrolled in this study, 67 were included in the statistical analysis. A clinical evaluation using the MADRS was performed at weeks 0, 4, 8, 12, and 16 after commencing treatment. For each time point, the MADRS total score was separated into three components: dysphoria, retardation, and vegetative scores. Results Remission was defined as an MADRS total score of ≤10 at end point. From our univariate logistic regression analysis, we found that improvements in both the MADRS total score and the dysphoria score at week 4 had a significant interaction with subsequent remission. Furthermore, age and sex were significant predictors of remission. There was an increase of approximately 4% in the odds of remission for each unit increase in age, and female sex had an odds of remission of 0.318 times that of male sex (remission rate for men was 73.1% [19/26] and for women 46.3% [19/41]). However, in the multivariate model using the change from baseline in the total MADRS, dysphoria, retardation, and vegetative scores at week 4, in which age and sex were included as covariates, only sex retained significance, except for an improvement in the dysphoria score. Conclusion No significant interaction was found between early response to duloxetine and eventual remission in this study. Sex difference was found to be a predictor of subsequent remission in patients with depression who were treated with duloxetine, with the male sex having greater odds of remission. PMID:27307739

  4. Human serum paraoxonase-1 (hPON1): in vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium.

    PubMed

    Türkeş, Cüneyt; Söyüt, Hakan; Beydemir, Şükrü

    2015-01-01

    In this study, we investigated the effects of antibacterial drugs (moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium) on human serum paraoxonase-1 (hPON1) enzyme activity from human serum in vitro conditions. For this purpose, hPON1 enzyme was purified from human serum using simple chromatographic methods. The antibacterial drugs exhibited inhibitory effects on hPON1 at low concentrations. Ki constants were calculated to be 2.641 ± 0.040 mM, 5.525 ± 0.817 mM, 35.092 ± 1.093 mM, 252.762 ± 5.749 mM and 499.244 ± 10.149 mM, respectively. The inhibition mechanism of moxifloxacin hydrochloride was competitive, whereas levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium were noncompetitive inhibitors.

  5. Fate and transport of the ß-adrenergic agonist ractopamine hydrochloride in soil-water systems

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The feed additive ractopamine hydrochloride was fortified at four concentrations into batch vials containing soils that differed in both biological activity and organic matter (OM). Sampling of the liquid layer for 14 d demonstrated that ractopamine rapidly dissipated from the liquid layer. Less t...

  6. Pharmacodynamics of norepinephrine reuptake inhibition: Modeling the peripheral and central effects of atomoxetine, duloxetine, and edivoxetine on the biomarker 3,4-dihydroxyphenylglycol in humans.

    PubMed

    Kielbasa, William; Lobo, Evelyn

    2015-12-01

    Norepinephrine, a neurotransmitter in the autonomic sympathetic nervous system, is deaminated by monoamine oxidase to 3,4-dihydroxyphenylglycol (DHPG). Inhibition of the NE transporter (NET) using DHPG as a biomarker was evaluated using atomoxetine, duloxetine, and edivoxetine as probe NET inhibitors. Pharmacokinetic and pharmacodynamic data were obtained from healthy subjects (n = 160) from 5 clinical trials. An indirect response model was used to describe the relationship between drug plasma concentration and DHPG concentration in plasma and cerebrospinal fluid (CSF). The baseline plasma DHPG concentration (1130-1240 ng/mL) and Imax (33%-37%) were similar for the 3 drugs. The unbound plasma drug IC50 (IC50U ) based on plasma DHPG was 0.973 nM for duloxetine, 0.136 nM for atomoxetine, and 0.041 nM for edivoxetine. The baseline CSF DHPG concentration (1850-2260 ng/mL) was similar for the 3 drugs, but unlike plasma DHPG, the Imax for DHPG was 38% for duloxetine, 53% for atomoxetine, and75% for edivoxetine. The IC50U based on CSF DHPG was 2.72 nM for atomoxetine, 1.22 nM for duloxetine, and 0.794 nM for edivoxetine. These modeling results provide insights into the pharmacology of NET inhibitors and the use of DHPG as a biomarker.

  7. Duloxetine Reduces Oxidative Stress, Apoptosis, and Ca(2+) Entry Through Modulation of TRPM2 and TRPV1 Channels in the Hippocampus and Dorsal Root Ganglion of Rats.

    PubMed

    Demirdaş, Arif; Nazıroğlu, Mustafa; Övey, İshak Suat

    2016-07-21

    Overload of Ca(2+) entry and excessive oxidative stress in neurons are the two main causes of depression. Activation of transient receptor potential (TRP) vanilloid type 1 (TRPV1) and TRP melastatin 2 (TRPM2) during oxidative stress has been linked to neuronal survival. Duloxetine (DULOX) in neurons reduced the effects of Ca(2+) entry and reactive oxygen species (ROS) through glutamate receptors, and this reduction of effects may also occur through TRPM2 and TRPV1 channels. In order to better characterize the actions of DULOX in peripheral pain and hippocampal oxidative injury through modulation of TRPM2 and TRPV1, we tested the effects of DULOX on apoptosis and oxidative stress in the hippocampal and dorsal root ganglion (DRG) neurons of rats. Freshly isolated hippocampal and DRG neurons were incubated for 24 h with DULOX. In whole-cell patch-clamp and intracellular-free calcium ([Ca(2+)]) concentration (Fura-2) experiments, cumene hydroperoxide and ADP-ribose-induced TRPM2 currents in the neurons were inhibited by N-(p-amylcinnamoyl) anthranilic acid (ACA) and capsaicin-induced TRPV1 currents were inhibited by capsazepine (CPZ) incubations. TRPM2 and TRPV1 channel current densities, [Ca(2+)] concentration, apoptosis, caspase 3, caspase 9, mitochondrial depolarization, and intracellular ROS production values in the neurons were lower in the DULOX group than in controls. In addition, the above values were further decreased by DULOX + CPZ and DULOX + ACA treatments. In conclusion, TRPM2 and TRPV1 channels are involved in Ca(2+) entry-induced neuronal death and modulation of the activity of these channels by DULOX treatment may account for their neuroprotective activity against apoptosis, excessive ROS production, and Ca(2+) entry.

  8. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients...

  9. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients...

  10. The respiratory effects of tilidine hydrochloride.

    PubMed

    Moyes, D G; Kingston, H G

    1975-07-26

    A standard 50-mg dose of tilidine hydrochloride (Valoron) was administered to 20 patients in the postoperative phase of open-heart surgery. No significant change in respiratory status, as measured by arterial blood gas analysis, was demonstrated with this dosage.

  11. Cartap hydrochloride poisoning: A clinical experience

    PubMed Central

    Boorugu, Hari K.; Chrispal, Anugrah

    2012-01-01

    Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular toxicity resulting in respiratory failure. It is hypothesized that the primary effect of Cartap hydrochloride is through inhibition of the [3H]-ryanodine binding to the Ca2+ release channel in the sarcoplasmic reticulum in a dose-dependent manner and promotion of extracellular Ca2+ influx and induction of internal Ca2+ release. This results in tonic diaphragmatic contraction rather than paralysis. This is the basis of the clinical presentation of acute Cartap poisoning as well as the treatment with chelators namely British Anti Lewisite and sodium dimercaptopropane sulfonate. PMID:22557838

  12. Cartap hydrochloride poisoning: A clinical experience.

    PubMed

    Boorugu, Hari K; Chrispal, Anugrah

    2012-01-01

    Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular toxicity resulting in respiratory failure. It is hypothesized that the primary effect of Cartap hydrochloride is through inhibition of the [(3)H]-ryanodine binding to the Ca(2+) release channel in the sarcoplasmic reticulum in a dose-dependent manner and promotion of extracellular Ca(2+) influx and induction of internal Ca(2+) release. This results in tonic diaphragmatic contraction rather than paralysis. This is the basis of the clinical presentation of acute Cartap poisoning as well as the treatment with chelators namely British Anti Lewisite and sodium dimercaptopropane sulfonate.

  13. A clinical evaluation of benzydamine hydrochloride.

    PubMed

    Hunter, K M

    1978-04-01

    A double-blind clinical trial of the effects of the use of benzydamine hydrochloride for patients undergoing the surgical removal of impacted lower third molar teeth showed no significant effects on swelling and trismus between control and experimental groups, although a significant reduction in the post-operative consumption of analgesics was noted.

  14. 21 CFR 522.1077 - Gonadorelin hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Gonadorelin hydrochloride. 522.1077 Section 522.1077 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS §...

  15. 21 CFR 522.1077 - Gonadorelin hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Gonadorelin hydrochloride. 522.1077 Section 522.1077 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS §...

  16. Butaclamol hydrochloride in newly admitted schizophrenics.

    PubMed

    Hollister, L E; Davis, K L; Berger, P A

    1975-01-01

    Butaclamol hydrochloride, a new type of antipsychotic drug, was evaluated by an uncontrolled study of 13 newly admitted schizophrenic patients. The drug had antipsychotic effects as well as a strong propensity for evoking extrapyramidal side effects. With the maximal daily doses of 30 mg used in this study, therapeutic results obtained were probably somewhat less than optimal.

  17. Altruism, personal benefit, and anxieties: a phenomenological study of healthy volunteers' experiences in a placebo‐controlled trial of duloxetine

    PubMed Central

    Kwakye, Isaac N.; Garner, Matthew; Baldwin, David S.; Bamford, Susan; Pinkney, Verity

    2016-01-01

    Objective The objective of this study was to develop an in‐depth understanding of healthy volunteers' experiences of mental health trials. Methods A qualitative study was nested within a healthy volunteer placebo‐controlled trial of duloxetine, a psychotropic drug used for treating patients with major depression and generalized anxiety disorder. Eight participants were interviewed, and data were analyzed using interpretative phenomenological analysis. Results Interviewees described volunteering for the trial because they were interested in research, wanted the monetary incentive, wanted to help researchers, and wanted to be part of something. On entering the trial, participants considered the possible risks and described feeling anxious, excited, and determined; they had some clear expectations and some loosely held hopes about what would happen. During the trial, participants were curious about whether they were taking duloxetine or placebo, self‐monitored their bodies' reactions, and guessed which treatment they received. On being un‐blinded to treatment allocation after completing the trial, some participants' guesses were confirmed, but others were surprised, and a few were disappointed. Conclusions Small changes to advertising/consent materials to reflect volunteers' motivations could improve recruitment rates to similar trials; “active” placebos might be particularly useful for maintaining blinding in healthy volunteer trials; and sensitive procedures are needed for un‐blinding participants to treatment allocation. © 2016 The Authors. Human Psychopharmacology: Clinical and Experimental published by John Wiley & Sons, Ltd. PMID:27378326

  18. A subtle grey-matter increase in first-episode, drug-naive major depressive disorder with panic disorder after 6 weeks' duloxetine therapy.

    PubMed

    Lai, Chien-Han; Hsu, Yuan-Yu

    2011-03-01

    We designed this study to investigate the modulating effects of duloxetine on symptoms and grey matter of patients with major depressive disorder combined with panic disorder. We also aimed to discover if there was any persistence of grey-matter deficits after remission and to find 'trait markers' for this comorbidity. High-resolution magnetic resonance imaging and voxel-based morphometric measurements were performed on 15 patients at baseline and remitted status (week 6) compared to 15 healthy control subjects who were scanned twice within 6 wk. The rating scales of depressive and panic symptoms improved with statistical significance (corrected p<0.001). A widespread pattern of grey-matter deficits in infero-frontal, limbic, occipital, temporo-parietal, cerebellar areas (trait marker regions) in drug-naive patients were observed compared to controls at baseline (family-wise error corrected p<0.0002). There were no significant changes of grey matter in healthy controls over the 6-wk period. Duloxetine-induced increases of grey matter were very subtle in left infero-frontal cortex, right fusiform gyrus, and right cerebellum VIIIa areas (state marker regions) after 6-wk therapy (uncorrected p<0.0005). Duloxetine did not increase grey matter to the level of control subjects and grey-matter deficits in patients appear largely unaffected by duloxetine. We suggest that short-term duloxetine therapy improved the clinical symptoms of patients with major depressive disorder combined with panic disorder. These improvements might be related to a modest increase of grey matter in state marker regions of the brain. The deficits of trait marker regions were more evident and are likely to be important for pathogenesis.

  19. Dispersive liquid-liquid microextraction based on solidification of floating organic droplets followed by high performance liquid chromatography for the determination of duloxetine in human plasma.

    PubMed

    Suh, Joon Hyuk; Lee, Yun Young; Lee, Hee Joo; Kang, Myunghee; Hur, Yeoun; Lee, Sun Neo; Yang, Dong-Hyug; Han, Sang Beom

    2013-03-05

    A novel dispersive liquid-liquid microextraction method based on solidification of floating organic droplets (DLLME-SFO) technique was developed for the determination of duloxetine in human plasma samples by high performance liquid chromatography with fluorescence detection (HPLC-FLD). During the extraction procedure, plasma protein was precipitated by using a mixture of zinc sulfate solution and acetonitrile. After the protein precipitation step, duloxetine in an alkaline sample solution was quickly extracted by DLLME-SFO with 50 μL of 1-undecanol (extractant). Disperser was unnecessary because the small amount of remaining acetonitrile, which acts as a protein precipitating reagent, was also employed as a disperser; therefore, organic solvent consumption was reduced as much as possible. The emulsion was centrifuged and then fine droplets were floated to the top of the sample solution. The floated droplets were solidified in an ice bath and easily transferred. Various DLLME-SFO parameters such as extractant type, extractant amount, ionic strength, pH and extraction time were optimized. The chromatographic separation of duloxetine was carried out using ethanol as mobile phase. Validation of the method was performed with respect to linearity, intra- and inter-day accuracy and precision, limit of quantification (LOQ), and recovery. Calibration curves for duloxetine showed good linearity with correlation coefficients (r²) higher than 0.99. The method showed good precision and accuracy, with intra- and inter-assay coefficients of variation less than 15% (LOQ: less than 20%) at all concentrations. The recovery was carried out following the standard addition procedure with yields ranging from 59.6 to 65.5%. A newly developed environmentally friendly method was successfully applied to the pharmacokinetic study of duloxetine in human plasma and was shown to be an alternative green approach compared with the conventional solid-phase microextraction (SPME) and dispersive

  20. Antinociceptive effects of AS1069562, the (+)-isomer of indeloxazine, on spinal hypersensitivity induced by intrathecal injection of prostaglandin in mice: comparison with duloxetine and amitriptyline.

    PubMed

    Murai, Nobuhito; Tsukamoto, Mina; Tamura, Seiji; Aoki, Toshiaki; Matsuoka, Nobuya

    2014-06-15

    The (+)-isomer of indeloxazine AS1069562 exerts multiple pharmacological actions including the inhibition of serotonin (5-HT) and norepinephrine reuptake and analgesia in experimental animal pain models. Here, we evaluated the antinociceptive effects of AS1069562 and the antidepressants duloxetine and amitriptyline in mouse models of prostaglandin-induced spinal hypersensitivity. Prostaglandin E2 (PGE2) and F2α (PGF2α) were intrathecally administered to induce spinal hypersensitivity, causing tactile allodynia in mice. Allodynia induced by PGF2α but not by PGE2 was suppressed by desensitization of C-fibers with systemic pretreatment with resiniferatoxin. C-fiber hyperexcitability might therefore play a role in allodynia induced by PGF2α but not PGE2. In the PGE2-induced allodynia model, AS1069562 and duloxetine significantly suppressed allodynia, whereas amitriptyline did not. In the PGF2α-induced allodynia model, AS1069562 and amitriptyline significantly ameliorated allodynia, whereas duloxetine did not. To demonstrate the broad effects of AS1069562 compared to duloxetine, additional studies were conducted to elucidate other target mechanisms of AS1069562 beyond 5-HT and norepinephrine reuptake inhibition. AS1069562 exhibited affinity for both 5-HT1A and 5-HT3 receptors, and the analgesic effect of AS1069562 on PGF2α-induced allodynia was significantly blocked by the 5-HT1A receptor antagonist (S)-WAY100135 and the 5-HT3 receptor agonist SR57227. Taken together, these results indicate that AS1069562 inhibits both C-fiber- and non-C-fiber-dependent prostaglandin-induced allodynia, while duloxetine inhibits only non-C-fiber-triggered allodynia, and amitriptyline inhibits only C-fiber-triggered allodynia. These broad antinociceptive effects of AS1069562 may be due not only to 5-HT and norepinephrine reuptake inhibition but also to its effects on 5-HT receptors such as 5-HT1A and 5-HT3 receptors.

  1. Is duloxetine's effect on painful physical symptoms in depression an indirect result of improvement of depressive symptoms? Pooled analyses of three randomized controlled trials.

    PubMed

    Harada, Eiji; Tokuoka, Hirofumi; Fujikoshi, Shinji; Funai, Jumpei; Wohlreich, Madelaine M; Ossipov, Michael H; Iwata, Nakao

    2016-03-01

    In treating Major Depressive Disorder with associated painful physical symptoms (PPS), the effect of duloxetine on PPS has been shown to decompose into a direct effect on PPS and an indirect effect on PPS via depressive symptoms (DS) improvement. To evaluate the changes in relative contributions of the direct and indirect effects over time, we analyzed pooled data from 3 randomized double-blind studies comparing duloxetine 60 mg/d with placebo in patients with major depressive disorder and PPS. Changes from baseline in Montgomery-Åsberg Depression Rating Scale total and Brief Pain Inventory-Short Form average pain score were assessed over 8 weeks. Path analysis examined the (1) direct effect of treatment on PPS and/or indirect effect on PPS via DS improvement and (2) direct effect of treatment on DS and/or indirect effect on DS via PPS improvement. At week 1, the direct effect of duloxetine on PPS (75.3%) was greater than the indirect effect through DS improvement (24.7%) but became less (22.6%) than the indirect effect (77.4%) by week 8. Initially, the direct effect of duloxetine on PPS was markedly greater than its indirect effect, whereas later the indirect effect predominated. Conversely, at week 1, the direct effect of treatment on DS (46.4%) was less than the indirect effect (53.6%), and by week 8 it superseded (62.6%) the indirect effect (37.4%). Thus, duloxetine would relieve PPS directly in the initial phase and indirectly via improving DS in the later phase.

  2. Influence of insecticidal derivative (cartap hydrochloride) from the marine polycheate on certain enzyme systems of the fresh water fish Oreochromis mossambicus.

    PubMed

    Palanivelu, V; Vijayavel, K; Balasubramanian, S Ezhilarasi; Balasubramanian, M P

    2005-04-01

    The activities of phosphatases and transaminases were studied in muscle and liver of the fresh water fish, Oreochromis mossambicus on exposure to different sublethal concentrations (0.25, 0.5, 0.75 and 1 mgl(-1)) of cartap hydrochloride (insecticidal derivative from marine polycheate) for 96 h. There was an overall decrease in phosphatases and transaminases activity in muscle and liver of the fish subjected to cartap hydrochloride.

  3. Treatment of allergic conjunctivitis with olopatadine hydrochloride eye drops

    PubMed Central

    Uchio, Eiichi

    2008-01-01

    Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H1 receptor antagonist action, chemical mediator suppressive action, and eosinophil infiltration suppressive action. Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol®) was introduced to the market in Japan in October 2006. In a conjunctival allergen challenge (CAC) test, olopatadine hydrochloride 0.1% ophthalmic solution significantly suppressed ocular itching and hyperemia compared with levocabastine hydrochloride 0.05% ophthalmic solution, and the number of patients who complained of ocular discomfort was lower in the olopatadine group than in the levocabastine group. Conjunctival cell membrane disruption was observed in vitro in the ketotifen fumarate group, epinastine hydrochloride group, and azelastine hydrochloride group, but not in the olopatadine hydrochloride 0.1% ophthalmic solution group, which may potentially explain the lower discomfort felt by patients on instillation. Many other studies in humans have revealed the superiority of olopatadine 0.1% hydrochloride eye drops to several other anti-allergic eye drops. Overseas, olopatadine hydrochloride 0.2% ophthalmic solution for a once-daily regimen has been marketed under the brand name of Pataday®. It is expected that olopatadine hydrochloride ophthalmic solutions may be used in patients with a more severe spectrum of allergic conjunctival diseases, such as vernal keratoconjunctivitis or atopic keratoconjunctivitis, in the near future. PMID:19668750

  4. Solid Lipid Nanoparticles of a Water Soluble Drug, Ciprofloxacin Hydrochloride

    PubMed Central

    Shah, M.; Agrawal, Y. K.; Garala, K.; Ramkishan, A.

    2012-01-01

    The aim of this study was to understand and investigate the relationship between experimental factors and their responses in the preparation of ciprofloxacin hydrochloride based solid lipid nanoparticles. A quadratic relationship was studied by developing central composite rotatable design. Amount of lipid and drug, stirring speed and stirring time were selected as experimental factors while particle size, zeta potential and drug entrapment were used as responses. Prior to the experimental design, a qualitative prescreening study was performed to check the effect of various solid lipids and their combinations. Results showed that changing the amount of lipid, stirring speed and stirring time had a noticeable influence on the entrapment efficiencies and particle size of the prepared solid lipid nanoparticles. The particle size of a solid lipid nanoparticle was in the range of 159-246 nm and drug encapsulation efficiencies were marginally improved by choosing a binary mixture of physically incompatible solid lipids. Release of ciprofloxacin hydrochloride from solid lipid nanoparticle was considerably slow, and it shows Higuchi matrix model as the best fitted model. Study of solid lipid nanoparticle suggested that the lipid based carrier system could potentially be exploited as a delivery system with improved drug entrapment efficiency and controlled drug release for water soluble actives. PMID:23716872

  5. Coding of adverse events of suicidality in clinical study reports of duloxetine for the treatment of major depressive disorder: descriptive study

    PubMed Central

    Tendal, Britta; Hróbjartsson, Asbjørn; Lundh, Andreas; Gøtzsche, Peter C

    2014-01-01

    Objective To assess the effects of coding and coding conventions on summaries and tabulations of adverse events data on suicidality within clinical study reports. Design Systematic electronic search for adverse events of suicidality in tables, narratives, and listings of adverse events in individual patients within clinical study reports. Where possible, for each event we extracted the original term reported by the investigator, the term as coded by the medical coding dictionary, medical coding dictionary used, and the patient’s trial identification number. Using the patient’s trial identification number, we attempted to reconcile data on the same event between the different formats for presenting data on adverse events within the clinical study report. Setting 9 randomised placebo controlled trials of duloxetine for major depressive disorder submitted to the European Medicines Agency for marketing approval. Data sources Clinical study reports obtained from the EMA in 2011. Results Six trials used the medical coding dictionary COSTART (Coding Symbols for a Thesaurus of Adverse Reaction Terms) and three used MedDRA (Medical Dictionary for Regulatory Activities). Suicides were clearly identifiable in all formats of adverse event data in clinical study reports. Suicide attempts presented in tables included both definitive and provisional diagnoses. Suicidal ideation and preparatory behaviour were obscured in some tables owing to the lack of specificity of the medical coding dictionary, especially COSTART. Furthermore, we found one event of suicidal ideation described in narrative text that was absent from tables and adverse event listings of individual patients. The reason for this is unclear, but may be due to the coding conventions used. Conclusion Data on adverse events in tables in clinical study reports may not accurately represent the underlying patient data because of the medical dictionaries and coding conventions used. In clinical study reports, the

  6. Application of physiologically based pharmacokinetic modeling in predicting drug–drug interactions for sarpogrelate hydrochloride in humans

    PubMed Central

    Min, Jee Sun; Kim, Doyun; Park, Jung Bae; Heo, Hyunjin; Bae, Soo Hyeon; Seo, Jae Hong; Oh, Euichaul; Bae, Soo Kyung

    2016-01-01

    Background Evaluating the potential risk of metabolic drug–drug interactions (DDIs) is clinically important. Objective To develop a physiologically based pharmacokinetic (PBPK) model for sarpogrelate hydrochloride and its active metabolite, (R,S)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol (M-1), in order to predict DDIs between sarpogrelate and the clinically relevant cytochrome P450 (CYP) 2D6 substrates, metoprolol, desipramine, dextromethorphan, imipramine, and tolterodine. Methods The PBPK model was developed, incorporating the physicochemical and pharmacokinetic properties of sarpogrelate hydrochloride, and M-1 based on the findings from in vitro and in vivo studies. Subsequently, the model was verified by comparing the predicted concentration-time profiles and pharmacokinetic parameters of sarpogrelate and M-1 to the observed clinical data. Finally, the verified model was used to simulate clinical DDIs between sarpogrelate hydrochloride and sensitive CYP2D6 substrates. The predictive performance of the model was assessed by comparing predicted results to observed data after coadministering sarpogrelate hydrochloride and metoprolol. Results The developed PBPK model accurately predicted sarpogrelate and M-1 plasma concentration profiles after single or multiple doses of sarpogrelate hydrochloride. The simulated ratios of area under the curve and maximum plasma concentration of metoprolol in the presence of sarpogrelate hydrochloride to baseline were in good agreement with the observed ratios. The predicted fold-increases in the area under the curve ratios of metoprolol, desipramine, imipramine, dextromethorphan, and tolterodine following single and multiple sarpogrelate hydrochloride oral doses were within the range of ≥1.25, but <2-fold, indicating that sarpogrelate hydrochloride is a weak inhibitor of CYP2D6 in vivo. Collectively, the predicted low DDIs suggest that sarpogrelate hydrochloride has limited potential for causing

  7. Biowaiver monographs for immediate release solid oral dosage forms: mefloquine hydrochloride.

    PubMed

    Strauch, S; Jantratid, E; Dressman, J B; Junginger, H E; Kopp, S; Midha, K K; Shah, V P; Stavchansky, S; Barends, D M

    2011-01-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release solid oral dosage forms containing mefloquine hydrochloride as the only active pharmaceutical ingredient (API) are reviewed. The solubility and permeability data of mefloquine hydrochloride as well as its therapeutic use and therapeutic index, its pharmacokinetic properties, data related to the possibility of excipient interactions and reported BE/bioavailability studies were taken into consideration. Mefloquine hydrochloride is not a highly soluble API. Since no data on permeability are available, it cannot be classified according to the Biopharmaceutics Classification System with certainty. Additionally, several studies in the literature failed to demonstrate BE of existing products. For these reasons, the biowaiver cannot be justified for the approval of new multisource drug products containing mefloquine hydrochloride. However, scale-up and postapproval changes (HHS-FDA SUPAC) levels 1 and 2 and most EU type I variations may be approvable without in vivo BE, using the dissolution tests described in these regulatory documents.

  8. Quantitative HPLC Analysis of a Psychotherapeutic Medication: Simultaneous Determination of Amitriptyline Hydrochloride and Perphenazine

    NASA Astrophysics Data System (ADS)

    Ferguson, Glenda K.

    1998-12-01

    A quantitative high-performance liquid chromatography (HPLC) laboratory experiment which entails the isocratic separation and simultaneous determination of the two active components of a commercial antipsychotic tablet has been developed. The prescription formulation used in this experiment contains amitriptyline hydrochloride (a tricyclic antidepressant) and perphenazine (a tranquilizer). Our experiment makes use of a straightforward HPLC separation on a cyanopropyl-packed column with an acetonitrile:methanol:aqueous monopotassium phosphate mobile phase pumped at a flow rate of 2.0 mL/min. Analytes are detected by UV absorbance at 215 nm. These conditions yield highly symmetrical and well-resolved peaks in less than 5 min after the injection of a mixture. In the experiment, students are given amitriptyline hydrochloride-perphenazine tablets without the manufacturer's labeled composition claim and a stock solution mixture with known concentrations of amitriptyline hydrochloride and perphenazine. They prepare four standards and a pharmaceutical sample of unknown concentration, assay each solution in quadruplicate, and plot average peak areas of the concentrations of the known solutions in the construction of a standard curve. From the mathematical relationships that result, the average masses of amitriptyline hydrochloride and perphenazine in the prescription tablet are determined. Finally, the standard deviations of the mean masses are calculated. The entire laboratory procedure and statistical data analysis can be completed in a single 3-hour period.

  9. 40 CFR 721.10682 - Fatty acid amide hydrochlorides (generic).

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 40 Protection of Environment 31 2014-07-01 2014-07-01 false Fatty acid amide hydrochlorides... Specific Chemical Substances § 721.10682 Fatty acid amide hydrochlorides (generic). (a) Chemical substances... fatty acid amide hydrochlorides (PMNs P-13-63, P-13-64, P-13-65, P-13-69, P-13-70, P-13-71, P-13-72,...

  10. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  11. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  12. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  13. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  14. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... organisms sensitive to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law...

  15. The efficacy of duloxetine, non-steroidal anti-inflammatory drugs, and opioids in osteoarthritis: a systematic literature review and meta-analysis

    PubMed Central

    2014-01-01

    Background This meta-analysis assessed the efficacy of duloxetine versus other oral treatments used after failure of acetaminophen for management of patients with osteoarthritis. Methods A systematic literature review of English language articles was performed in PUBMED, EMBASE, MedLine In-Process, Cochrane Library, and ClinicalTrials.gov between January 1985 and March 2013. Randomized controlled trials of duloxetine and all oral non-steroidal anti-inflammatory drugs and opioids were included if treatment was ≥12 weeks and the Western Ontario and McMaster Universities Index (WOMAC) total score was available. Studies were assessed for quality using the assessment tool from the National Institute for Health and Clinical Excellence guidelines for single technology appraisal submissions. WOMAC baseline and change from baseline total scores were extracted and standardized. A frequentist meta-analysis, meta-regression, and indirect comparison were performed using the DerSimonian-Laird and Bucher methods. Bayesian analyses with and without adjustment for study-level covariates were performed using noninformative priors. Results Thirty-two publications reported 34 trials (2 publications each reported 2 trials) that met inclusion criteria. The analyses found all treatments except oxycodone (frequentist) and hydromorphone (frequentist and Bayesian) to be more effective than placebo. Indirect comparisons to duloxetine found no significant differences for most of the compounds. Some analyses showed evidence of a difference with duloxetine for etoricoxib (better), tramadol and oxycodone (worse), but without consistent results between analyses. Forest plots revealed positive trends in overall efficacy improvement with baseline scores. Adjusting for baseline, the probability duloxetine is superior to other treatments ranges between 15% to 100%. Limitations of this study include the low number of studies included in the analyses, the inclusion of only English language

  16. Nalfurafine hydrochloride to treat pruritus: a review

    PubMed Central

    Inui, Shigeki

    2015-01-01

    Uremic pruritus has a great negative influence on quality of life in hemodialysis (HD) patients and, importantly, negatively affects mortality risk. Recently, nalfurafine hydrochloride, an opioid κ-selective agonist, has been officially approved for resistant pruritus in HD patients on the basis of a well-evidenced clinical trial in Japan. From clinical observation, it has been suggested that the upper neuron system plays a role in its pathogenesis. According to previous experimental results, using mice injected with opioids, dynorphin suppresses itch through binding κ-opioid receptors, suggesting that κ-opioid opioid receptor agonists act as potential therapeutic reagents for pruritus in HD patients. In Japan, a large-scale placebo-controlled study was performed to examine the efficacy and safety of oral nalfurafine hydrochloride for intractable pruritus in 337 HD patients. Two daily doses of 2.5 or 5 μg nalfurafine or placebo were orally administered for 2 weeks, and clinical responses were analyzed. The results showed that the mean decrease in the visual analog scale for pruritus from baseline was 22 mm in the 5 μg nalfurafine hydrochloride group (n=114) and 23 mm in the 2.5 μg group (n=112). These reductions were statistically significant compared with 13 mm, which is the mean decrease of visual analog scale in the placebo group (n=111), demonstrating that nalfurafine is an effective and safe drug for uremic pruritus in HD patients. Moreover, another open-label trial (n=145) examining the long-term effect of 5 μg oral nalfurafine revealed the maintenance of the antipruritic effect of nalfurafine for 52 weeks. In addition, on the basis of recent data showing κ-opioid receptor expression in the epidermis of atopic dermatitis and psoriasis, nalfurafine hydrochloride also can be potentially used for these two skin diseases. PMID:26005355

  17. Sinomenine hydrochloride protects against polymicrobial sepsis via autophagy.

    PubMed

    Jiang, Yu; Gao, Min; Wang, Wenmei; Lang, Yuejiao; Tong, Zhongyi; Wang, Kangkai; Zhang, Huali; Chen, Guangwen; Liu, Meidong; Yao, Yongming; Xiao, Xianzhong

    2015-01-23

    Sepsis, a systemic inflammatory response to infection, is the major cause of death in intensive care units (ICUs). The mortality rate of sepsis remains high even though the treatment and understanding of sepsis both continue to improve. Sinomenine (SIN) is a natural alkaloid extracted from Chinese medicinal plant Sinomenium acutum, and its hydrochloride salt (Sinomenine hydrochloride, SIN-HCl) is widely used to treat rheumatoid arthritis (RA). However, its role in sepsis remains unclear. In the present study, we investigated the role of SIN-HCl in sepsis induced by cecal ligation and puncture (CLP) in BALB/c mice and the corresponding mechanism. SIN-HCl treatment improved the survival of BALB/c mice that were subjected to CLP and reduced multiple organ dysfunction and the release of systemic inflammatory mediators. Autophagy activities were examined using Western blotting. The results showed that CLP-induced autophagy was elevated, and SIN-HCl treatment further strengthened the autophagy activity. Autophagy blocker 3-methyladenine (3-MA) was used to investigate the mechanism of SIN-HCl in vitro. Autophagy activities were determined by examining the autophagosome formation, which was shown as microtubule-associated protein light chain 3 (LC3) puncta with green immunofluorescence. SIN-HCl reduced lipopolysaccharide (LPS)-induced inflammatory cytokine release and increased autophagy in peritoneal macrophages (PM). 3-MA significantly decreased autophagosome formation induced by LPS and SIN-HCl. The decrease of inflammatory cytokines caused by SIN-HCl was partially aggravated by 3-MA treatment. Taken together, our results indicated that SIN-HCl could improve survival, reduce organ damage, and attenuate the release of inflammatory cytokines induced by CLP, at least in part through regulating autophagy activities.

  18. Sinomenine Hydrochloride Protects against Polymicrobial Sepsis via Autophagy

    PubMed Central

    Jiang, Yu; Gao, Min; Wang, Wenmei; Lang, Yuejiao; Tong, Zhongyi; Wang, Kangkai; Zhang, Huali; Chen, Guangwen; Liu, Meidong; Yao, Yongming; Xiao, Xianzhong

    2015-01-01

    Sepsis, a systemic inflammatory response to infection, is the major cause of death in intensive care units (ICUs). The mortality rate of sepsis remains high even though the treatment and understanding of sepsis both continue to improve. Sinomenine (SIN) is a natural alkaloid extracted from Chinese medicinal plant Sinomenium acutum, and its hydrochloride salt (Sinomenine hydrochloride, SIN-HCl) is widely used to treat rheumatoid arthritis (RA). However, its role in sepsis remains unclear. In the present study, we investigated the role of SIN-HCl in sepsis induced by cecal ligation and puncture (CLP) in BALB/c mice and the corresponding mechanism. SIN-HCl treatment improved the survival of BALB/c mice that were subjected to CLP and reduced multiple organ dysfunction and the release of systemic inflammatory mediators. Autophagy activities were examined using Western blotting. The results showed that CLP-induced autophagy was elevated, and SIN-HCl treatment further strengthened the autophagy activity. Autophagy blocker 3-methyladenine (3-MA) was used to investigate the mechanism of SIN-HCl in vitro. Autophagy activities were determined by examining the autophagosome formation, which was shown as microtubule-associated protein light chain 3 (LC3) puncta with green immunofluorescence. SIN-HCl reduced lipopolysaccharide (LPS)-induced inflammatory cytokine release and increased autophagy in peritoneal macrophages (PM). 3-MA significantly decreased autophagosome formation induced by LPS and SIN-HCl. The decrease of inflammatory cytokines caused by SIN-HCl was partially aggravated by 3-MA treatment. Taken together, our results indicated that SIN-HCl could improve survival, reduce organ damage, and attenuate the release of inflammatory cytokines induced by CLP, at least in part through regulating autophagy activities. PMID:25625512

  19. Duloxetine, a Selective Noradrenaline Reuptake Inhibitor, Increased Plasma Levels of 3-Methoxy-4-hydroxyphenylglycol but Not Homovanillic Acid in Patients with Major Depressive Disorder

    PubMed Central

    Atake, Kiyokazu; Hori, Hikaru; Katsuki, Asuka; Ikenouchi-Sugita, Atsuko; Umene-Nakano, Wakako; Nakamura, Jun

    2014-01-01

    Objective We investigated the effects of duloxetine on the plasma levels of catecholamine metabolites and serum brain-derived neurotrophic factor (BDNF) in 64 patients with major depressive disorder (MDD). Methods Major depressive episode was diagnosed using the Structured Clinical Interview for the Diagnostic and Statistical Manual of Mental Disorders-fourth edition (DSM-IV) according to the DSM-IV text revision (DSM-IV-TR) criteria. The severity of depression was evaluated using the 17-item Hamilton Rating Scale for Depression (HAMD-17). Blood sampling and clinical evaluation were performed on days 0, 28, and 56. Results Duloxetine treatment for 8 weeks significantly increased the plasma 3-methoxy-4-hydroxyphenylglycol (MHPG) levels but not the homovanillic acid (HVA) levels in responders with MDD. Conclusion These results imply that noradrenaline plays an important role in alleviating depressive symptoms. PMID:24851119

  20. Efficacy and safety of duloxetine for treatment of fibromyalgia in patients with or without major depressive disorder: Results from a 6-month, randomized, double-blind, placebo-controlled, fixed-dose trial.

    PubMed

    Russell, I Jon; Mease, Philip J; Smith, Timothy R; Kajdasz, Daniel K; Wohlreich, Madelaine M; Detke, Michael J; Walker, Daniel J; Chappell, Amy S; Arnold, Lesley M

    2008-06-01

    The primary objectives of this study were to assess the efficacy and safety of duloxetine for reducing pain severity in fibromyalgia patients with or without current major depressive disorder. This was a 6-month, multicenter, randomized, double-blind, placebo-controlled study. In total, 520 patients meeting American College of Rheumatology criteria for fibromyalgia were randomly assigned to duloxetine (20 mg/day, 60 mg/day, or 120 mg/day) or placebo, administered once daily, for 6 months (after 3 months, the duloxetine 20-mg/day group titrated to 60 mg/day). The co-primary outcome measures were the Brief Pain Inventory (BPI) average pain severity score and Patient Global Impressions of Improvement (PGI-I) score. Safety was assessed via treatment-emergent adverse events, and changes in vital sign, laboratory, and ECG measures. Compared with placebo-treated patients, those patients treated with duloxetine 120 mg/day improved significantly more on the co-primary outcome measures at 3 months (change in BPI score [-2.31 vs -1.39, P<0.001] and PGI-I [2.89 vs 3.39, P=0.004]) and at 6 months (change in BPI [-2.26 vs -1.43, P=0.003] and PGI-I [2.93 vs 3.37, P=0.012]). Compared with placebo, treatment with duloxetine 60 mg/day also significantly improved the co-primary measures at 3 months and BPI at 6 months. Duloxetine was efficacious in patients both with and without major depressive disorder. There were no clinically significant differences between treatment groups in changes in vital signs, laboratory measures, or ECG measures. Study results demonstrated that duloxetine at doses of 60 mg/day and 120 mg/day appears to be safe and efficacious in patients with fibromyalgia.

  1. 21 CFR 520.1242 - Levamisole hydrochloride oral dosage forms.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride oral dosage forms. 520... SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242 Levamisole hydrochloride oral dosage forms....

  2. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... dosage level of 1 to 2 milligrams of ethylisobutrazine hydrochloride per pound of body weight to effect.1... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ethylisobutrazine hydrochloride injection. 522.863 Section 522.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN...

  3. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... dosage level of 1 to 2 milligrams of ethylisobutrazine hydrochloride per pound of body weight to effect.1... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ethylisobutrazine hydrochloride injection. 522.863 Section 522.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN...

  4. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... dosage level of 1 to 2 milligrams of ethylisobutrazine hydrochloride per pound of body weight to effect.1... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ethylisobutrazine hydrochloride injection. 522.863 Section 522.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN...

  5. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Selegiline hydrochloride tablets. 520.2098 Section... hydrochloride tablets. (a) Specifications. Each tablet contains either 2, 5, 10, 15, or 30 milligrams of... use—Dogs—(1) Dosage. 1 milligram per kilogram (0.45 milligram per pound) of body weight....

  6. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50.... (c) Conditions of use. (1) It is administered orally to dogs as a tranquilizer.1 1 These...

  7. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ...) Related tolerances. See § 556.350 of this chapter. (d) Conditions of use. It is used for swine as follows... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Levamisole hydrochloride effervescent tablets. 520....1242e Levamisole hydrochloride effervescent tablets. (a) Specifications. Each tablet contains...

  8. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Selegiline hydrochloride tablets. 520.2098 Section... hydrochloride tablets. (a) Specifications. Each tablet contains either 2, 5, 10, 15, or 30 milligrams of... use—Dogs—(1) Dosage. 1 milligram per kilogram (0.45 milligram per pound) of body weight....

  9. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Selegiline hydrochloride tablets. 520.2098 Section... hydrochloride tablets. (a) Specifications. Each tablet contains either 2, 5, 10, 15, or 30 milligrams of... use—Dogs—(1) Dosage. 1 milligram per kilogram (0.45 milligram per pound) of body weight....

  10. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50.... (c) Conditions of use. (1) It is administered orally to dogs as a tranquilizer.1 1 These...

  11. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50.... (c) Conditions of use. (1) It is administered orally to dogs as a tranquilizer.1 1 These...

  12. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50.... (c) Conditions of use. (1) It is administered orally to dogs as a tranquilizer.1 1 These...

  13. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ...) Related tolerances. See § 556.350 of this chapter. (d) Conditions of use. It is used for swine as follows... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Levamisole hydrochloride effervescent tablets. 520....1242e Levamisole hydrochloride effervescent tablets. (a) Specifications. Each tablet contains...

  14. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863... Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50.... (c) Conditions of use. (1) It is administered orally to dogs as a tranquilizer.1 1 These...

  15. 21 CFR 520.2098 - Selegiline hydrochloride tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2098 Selegiline... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Selegiline hydrochloride tablets. 520.2098 Section... selegiline hydrochloride. (b) Sponsor. See No. 000069 in § 510.600(c) of this chapter. (c) (d) Conditions...

  16. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ketamine hydrochloride injectable dosage forms... SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  17. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ketamine hydrochloride injectable dosage forms... SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  18. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ketamine hydrochloride injectable dosage forms... SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  19. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride injectable dosage forms... SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  20. Acute Oral Toxicity of Guanidine Hydrochloride in Mice

    DTIC Science & Technology

    1989-12-29

    guanidine hydrochloride in male and female Institute of Cancer Research (ICR) mice. MATERIALS Test Substance Chemical Name: Guanidine hydrochloride Chemical ... Abstract Service Registry No.: 050-01-1 LAIR Code Number: TP28 Physical State: White powder Morgan et al.--2 Molecular Structure: NH2 + H2N- C-NH2 Cl

  1. 40 CFR 721.4460 - Amidinothiopropionic acid hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 40 Protection of Environment 32 2013-07-01 2013-07-01 false Amidinothiopropionic acid... Specific Chemical Substances § 721.4460 Amidinothiopropionic acid hydrochloride. (a) Chemical substance and... amidinothiopropionic acid hydrochloride (PMN P-91-102) is subject to reporting under this section for the...

  2. Effect of Ractopamine Hydrochloride and Zilpaterol Hydrochloride on tenderness of longissimus steaks of Bos Taurus steers

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Objectives: Three experiments were conducted to determine 1) the interaction of ractopamine hydrochloride (RH) inclusion rate (0 or 300 mg·hd-1·d-1 for last 30 to 34 d before harvest) and dietary protein level (13.5 or 17.5% CP) on LM slice shear force (SSF) at 14 d postmortem (Exp. 1); 2) the inter...

  3. 78 FR 34108 - Determination That SUBOXONE (Buprenorphine Hydrochloride and Naloxone Hydrochloride) Sublingual...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-06-06

    ... (buprenorphine hydrochloride (HCl) and naloxone HCl) sublingual tablets, 2 milligrams (mg)/0.5 mg and 8 mg/2 mg... sublingual tablets, 2 mg/0.5 mg and 8 mg/2 mg, if all other legal and regulatory requirements are met. FOR... (buprenorphine HCl and naloxone HCl) sublingual tablets, 2 mg/0.5 mg and 8 mg/2 mg,......

  4. Does Duloxetine Improve Cognitive Function Independently of Its Antidepressant Effect in Patients with Major Depressive Disorder and Subjective Reports of Cognitive Dysfunction?

    PubMed Central

    Greer, Tracy L.; Sunderajan, Prabha; Grannemann, Bruce D.; Kurian, Benji T.; Trivedi, Madhukar H.

    2014-01-01

    Introduction. Cognitive deficits are commonly reported by patients with major depressive disorder (MDD). Duloxetine, a dual serotonin/noradrenaline reuptake inhibitor, may improve cognitive deficits in MDD. It is unclear if cognitive improvements occur independently of antidepressant effects with standard antidepressant medications. Methods. Thirty participants with MDD who endorsed cognitive deficits at screening received 12-week duloxetine treatment. Twenty-one participants completed treatment and baseline and posttreatment cognitive testing. The Cambridge Neuropsychological Test Automated Battery was used to assess the following cognitive domains: attention, visual memory, executive function/set shifting and working memory, executive function/spatial planning, decision making and response control, and verbal learning and memory. Results. Completers showed significant cognitive improvements across several domains on tasks assessing psychomotor function and mental processing speed, with additional improvements in visual and verbal learning and memory, and affective decision making and response control. Overall significance tests for executive function tasks were also significant, although individual tasks were not, perhaps due to the small sample size. Most notably, cognitive improvements were observed independently of symptom reduction on all domains except verbal learning and memory. Conclusions. Patients reporting baseline cognitive deficits achieved cognitive improvements with duloxetine treatment, most of which were independent of symptomatic improvement. This trial is registered with NCT00933439. PMID:24563781

  5. Relationship between major depressive disorder and associated painful physical symptoms: analysis of data from two pooled placebo-controlled, randomized studies of duloxetine.

    PubMed

    Robinson, Michael J; Sheehan, David; Gaynor, Paula J; Marangell, Lauren B; Tanaka, Yoko; Lipsius, Sarah; Ohara, Fumihiro; Namiki, Chihiro

    2013-11-01

    The aim of this study was to evaluate the relationship between painful physical symptoms (PPS) and outcomes in major depressive disorder (MDD). Post-hoc analysis of two identically designed 8-week trials compared the efficacy of 60 mg/day duloxetine (N=523) with that of placebo (N=532) in treating PPS associated with MDD. The Montgomery-Åsberg Depression Rating Scale (MADRS) total score, the Brief Pain Inventory (BPI) average pain score, and the Sheehan Disability Scale global functional impairment score assessed depression symptoms, pain, and functioning, respectively. Remission was defined as a MADRS score of 10 or less, and the BPI response subgroup was defined as a 50% or greater reduction from baseline. Path analyses assessed relationships among variables. Duloxetine-treated patients who had a 50% or greater reduction in BPI score at endpoint had higher rates of remission. Path analysis indicated that 16% of likelihood of remission in depression symptoms was because of the direct effect of treatment, 41% because of pain reduction, and 43% because of functional improvement. Path analysis also indicated that 51% of improvement in functioning was attributed to pain improvement and 43% to mood improvement. Results demonstrate that improvement in pain and mood contributes to functional improvement, and pain reduction and functional improvement increase the likelihood of remission of depressive symptoms with duloxetine treatment in patients with both MDD and PPS at baseline.

  6. The effects of a novel anti-arrhythmic drug, acehytisine hydrochloride, on the human ether-a-go-go related gene K channel and its trafficking.

    PubMed

    Huang, Xingfu; Yang, Yanmin; Zhu, Jun; Dai, Yan; Pu, Jielin

    2009-02-01

    Many drugs cause severe side-effects such as long QT syndromes by blocking the human ether-a-go-go related gene (HERG) K(+) channels and/or disrupting HERG protein trafficking. Acehytisine hydrochloride is an anti-arrhythmic drug in phase IV clinical trial. To study whether acehytisine hydrochloride affects HERG channel activity and protein trafficking, we expressed HERG in human embryonic kidney 293 (HEK293) cells and recorded HERG channel currents with a whole-cell patch clamp technique. We also measured the protein levels by Western blot analysis. We found that acehytisine hydrochloride inhibited HERG step current (I(HERG)) in a concentration-dependent manner. However, it had little effect on the tail current (I(tail)). In addition, acehytisine hydrochloride accelerated channel inactivation and slowed recovery from inactivation. In contrast, it did not inhibit HERG protein (135 and 155 kD) trafficking, although it reduced the 155 kD band density at 2500 microM. Moreover, the F656C mutation in the S6 domain abolished acehytisine hydrochloride inhibition on the I(HERG) and enhanced the inhibitive effects on the trafficking of the 155 kD band. Acehytisine hydrochloride interrupted HERG protein trafficking at 1000 and 2500 microM. Our data showed that acehytisine hydrochloride could inhibit I(HERG), but had no effects on I(tail) until the concentration was above 1000 microM. Therefore, acehytisine hydrochloride may not induce QT interval prolongation and could be a promising anti-arrhythmic drug without severe side-effects.

  7. Identification of polymorphism in ethylone hydrochloride: synthesis and characterization

    PubMed Central

    Alarcon, Idralyn Q.; Copeland, Catherine R.; Cameron, T. Stanley; Linden, Anthony; Grossert, J. Stuart

    2015-01-01

    Ethylone, a synthetic cathinone with psychoactive properties, is a designer drug which has appeared on the recreational drug market in recent years. Since 2012, illicit shipments of ethylone hydrochloride have been intercepted with increasing frequency at the Canadian border. Analysis has revealed that ethylone hydrochloride exists as two distinct polymorphs. In addition, several minor impurities were detected in some seized exhibits. In this study, the two conformational polymorphs of ethylone hydrochloride have been synthesized and fully characterized by FTIR, FT‐Raman, powder XRD, GC‐MS, ESI‐MS/MS and NMR (13C CPMAS, 1H, 13C). The two polymorphs can be distinguished by vibrational spectroscopy, solid‐state nuclear magnetic resonance spectroscopy and X‐ray diffraction. The FTIR data are applied to the identification of both polymorphs of ethylone hydrochloride (mixed with methylone hydrochloride) in a laboratory submission labelled as 'Ocean Snow Ultra’. The data presented in this study will assist forensic scientists in the differentiation of the two ethylone hydrochloride polymorphs. This report, alongside our recent article on the single crystal X‐ray structure of a second polymorph of this synthetic cathinone, is the first to confirm polymorphism in ethylone hydrochloride. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd. PMID:26344849

  8. Identification of polymorphism in ethylone hydrochloride: synthesis and characterization.

    PubMed

    Maheux, Chad R; Alarcon, Idralyn Q; Copeland, Catherine R; Cameron, T Stanley; Linden, Anthony; Grossert, J Stuart

    2016-08-01

    Ethylone, a synthetic cathinone with psychoactive properties, is a designer drug which has appeared on the recreational drug market in recent years. Since 2012, illicit shipments of ethylone hydrochloride have been intercepted with increasing frequency at the Canadian border. Analysis has revealed that ethylone hydrochloride exists as two distinct polymorphs. In addition, several minor impurities were detected in some seized exhibits. In this study, the two conformational polymorphs of ethylone hydrochloride have been synthesized and fully characterized by FTIR, FT-Raman, powder XRD, GC-MS, ESI-MS/MS and NMR ((13) C CPMAS, (1) H, (13) C). The two polymorphs can be distinguished by vibrational spectroscopy, solid-state nuclear magnetic resonance spectroscopy and X-ray diffraction. The FTIR data are applied to the identification of both polymorphs of ethylone hydrochloride (mixed with methylone hydrochloride) in a laboratory submission labelled as 'Ocean Snow Ultra'. The data presented in this study will assist forensic scientists in the differentiation of the two ethylone hydrochloride polymorphs. This report, alongside our recent article on the single crystal X-ray structure of a second polymorph of this synthetic cathinone, is the first to confirm polymorphism in ethylone hydrochloride. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd.

  9. Simultaneous UV Spectrophotometric Estimation of Ambroxol Hydrochloride and Levocetirizine Dihydrochloride

    PubMed Central

    Prabhu, S. Lakshmana; Shirwaikar, A. A.; Shirwaikar, Annie; Kumar, C. Dinesh; Kumar, G. Aravind

    2008-01-01

    A novel, simple, sensitive and rapid spectrophotometric method has been developed for simultaneous estimation of ambroxol hydrochloride and levocetirizine dihydrochloride. The method involved solving simultaneous equations based on measurement of absorbance at two wavelengths 242 nm and 231 nm, the γ max of ambroxol hydrochloride and levocetirizine dihydrochloride, respectively. Beer's law was obeyed in the concentration range 10–50 μg/ml and 8–24 μg/ml for ambroxol hydrochloride and levocetirizine dihydrochloride respectively. Results of the method were validated statistically and by recovery studies. PMID:20046721

  10. Effect of ractopamine hydrochloride and zilpaterol hydrochloride on cardiac electrophysiologic and hematologic variables in finishing steers.

    PubMed

    Frese, Daniel A; Reinhardt, Christopher D; Bartle, Steven J; Rethorst, David N; Bawa, Bhupinder; Thomason, Justin D; Loneragan, Guy H; Thomson, Daniel U

    2016-09-15

    OBJECTIVE To investigate the effects of dietary supplementation with the β-adrenoceptor agonists ractopamine hydrochloride and zilpaterol hydrochloride on ECG and clinicopathologic variables of finishing beef steers. DESIGN Randomized controlled trial. ANIMALS 30 Angus steers. PROCEDURES Steers were grouped by body weight and randomly assigned to receive 1 of 3 diets for 23 days: a diet containing no additive (control diet) or a diet containing ractopamine hydrochloride (300 mg/steer/d) or zilpaterol hydrochloride (8.3 mg/kg [3.8 mg/lb] of feed on a dry-matter basis), beginning on day 0. Steers were instrumented with an ambulatory ECG monitor on days -2, 6, 13, and 23, and continuous recordings were obtained for 72, 24, 24, and 96 hours, respectively. At the time of instrumentation, blood samples were obtained for CBC and serum biochemical and blood lactate analysis. Electrocardiographic recordings were evaluated for mean heart rate and arrhythmia rates. RESULTS Steers fed zilpaterol or ractopamine had greater mean heart rates than those fed the control diet. Mean heart rates were within reference limits for all steers, with the exception of those in the ractopamine group on day 14, in which mean heart rate was high. No differences in arrhythmia rates were identified among the groups, nor were any differences identified when arrhythmias were classified as single, paired, or multiple (> 2) beats. CONCLUSIONS AND CLINICAL RELEVANCE Results suggested that dietary supplementation of cattle with ractopamine or zilpaterol at FDA-approved doses had no effect on arrhythmia rates but caused an increase in heart rate that remained within reference limits.

  11. Catechol-O-methyltransferase Val158Met genotype and the clinical responses to duloxetine treatment or plasma levels of 3-methoxy-4-hydroxyphenylglycol and homovanillic acid in Japanese patients with major depressive disorder

    PubMed Central

    Atake, Kiyokazu; Yoshimura, Reiji; Hori, Hikaru; Katsuki, Asuka; Nakamura, Jun

    2015-01-01

    Purpose This study investigated the relationships among the plasma levels of catecholamine metabolites, the clinical response to duloxetine treatment, and Val158Met polymorphism of the catechol-O-methyltransferase (COMT) gene. Subjects and methods Sixty-four patients and 30 healthy control subjects were recruited. Major depressive episodes were diagnosed using the Structured Clinical Interview for the Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition, Text Revision criteria. The severity of depression was evaluated using the 17-item Hamilton Rating Scale for Depression (HAMD17). Patients whose HAMD17 scores were 15 or greater were enrolled in the study. Blood sampling and clinical evaluation were performed at week 0 and week 8. The levels of plasma catecholamine metabolites were measured using high-performance liquid chromatography with electrochemical detection. Genotyping was performed using direct sequencing. Results Thirty of 45 patients (67%) responded to duloxetine treatment during the 8 weeks of treatment. The baseline plasma levels of 3-methoxy-4-hydroxyphenylglycol (MHPG), but not homovanillic acid (HVA), were lower in patients with major depressive disorder (MDD) who had the Val/Val genotype than in patients who were Met-carriers. Patients with MDD and the Val/Val genotype, but not Met carriers, had increased plasma levels of MHPG after 8 weeks of duloxetine treatment. The baseline plasma MHPG levels in healthy control subjects with the Val/Val genotype were significantly higher than those in patients with MDD. Among the subjects in the MDD group with the Val/Val genotype, the plasma MHPG levels increased to the same degree as in the healthy control subjects with the Val/Val genotype after 8 weeks of duloxetine treatment. Conclusion The relationship among the COMT Val158Met polymorphism, plasma levels of catecholamine metabolites, and responses to duloxetine is complex. Nevertheless, our results suggest that patients with MDD and the

  12. Duloxetine and pregabalin: high-dose monotherapy or their combination? The "COMBO-DN study"--a multinational, randomized, double-blind, parallel-group study in patients with diabetic peripheral neuropathic pain.

    PubMed

    Tesfaye, Solomon; Wilhelm, Stefan; Lledo, Alberto; Schacht, Alexander; Tölle, Thomas; Bouhassira, Didier; Cruccu, Giorgio; Skljarevski, Vladimir; Freynhagen, Rainer

    2013-12-01

    This multicentre, double-blind, parallel-group study in diabetic peripheral neuropathic pain addressed whether, in patients not responding to standard doses of duloxetine or pregabalin, combining both medications is superior to increasing each drug to its maximum recommended dose. For initial 8-week therapy, either 60 mg/day duloxetine (groups 1, 2) or 300 mg/day pregabalin (groups 3, 4) was given. Thereafter, in the 8-week combination/high-dose therapy period, only nonresponders received 120 mg/day duloxetine (group 1), a combination of 60 mg/day duloxetine and 300 mg/day pregabalin (groups 2, 3), or 600 mg/day pregabalin (group 4). Primary outcome (Brief Pain Inventory Modified Short Form [BPI-MSF] 24-hour average pain change after combination/high-dose therapy) was analyzed comparing combination (groups 2, 3 pooled) with high-dose monotherapy (groups 1, 4 pooled). Secondary end points included response rates, BPI-MSF severity items, and comparison of duloxetine and pregabalin in BPI-MSF average pain. Eight hundred four patients were evaluated for initial therapy and 339 for combination/high-dose therapy. There were no significant differences between combination and high-dose monotherapy regarding BPI-MSF average pain (mean change: combination: -2.35; high-dose monotherapy: -2.16; P = 0.370) and most secondary end points, which, however, consistently favoured combination therapy. Fifty-percent response rates were 52.1% for combination and 39.3% for high-dose monotherapy (P = 0.068). In exploratory analyses of the initial 8-week therapy uncorrected for multiple comparisons, 60 mg/day duloxetine was found superior to 300 mg/day pregabalin (P < 0.001). Both drugs and their combination were well tolerated. Although not significantly superior to high-dose monotherapy, combination therapy was considered to be effective, safe, and well tolerated.

  13. Spectroscopy study of ephedrine hydrochloride and papaverine hydrochloride in terahertz range

    NASA Astrophysics Data System (ADS)

    Deng, Fusheng; Shen, Jingling; Wang, Guangqin; Liang, Meiyan

    2008-12-01

    The terahertz(THz) fingerprint spectra of Ephedrine Hydrochloride and Papaverine Hydrochloride have been measured using THz time-domain Spectroscopy (THz-TDS) system in the region of 0.2~2.6 THz. To explain the spectra, both gas-phase simulation methods and solid-state simulation methods were performed in the efforts to extract pictures of the molecular interior vibrational modes. By comparing the results of various gas-phase simulation methods, It was found that using the semi-empirical theory is more applicable than the density functional theory (DFT) for some chemical compounds. In the solid-state calculations, solid-state density functional theory (DFT) was employed to obtain the vibration frequencies and Difference-Dipole Method (DDM) was used to calculate the corresponding infrared (IR) intensity. In the process of calculating the IR intensity of Papaverine Hydrochloride in terahertz range, we found that the results by Hirshfeld partitioning method agree better with the experiments than the ones derived from Mulliken atomic charges. Moreover, the accuracy of simulation results depends on the basis sets and grid size being chosen.

  14. Efficacy of Duloxetine on Painful Physical Symptoms in Major Depressive Disorder for Patients With Clinically Significant Painful Physical Symptoms at Baseline: A Meta-Analysis of 11 Double-Blind, Placebo-Controlled Clinical Trials

    PubMed Central

    Desaiah, Durisala; Spann, Melissa E.; Zhang, Qi; Russell, James M.; Robinson, Michael J.; Demyttenaere, Koen

    2011-01-01

    Objective: To review efficacy of duloxetine for physical symptoms and depressive illness in patients with at least mild to moderate major depressive disorder (MDD; DSM-IV) and clinically significant painful physical symptoms at baseline. Data Sources: Global database of duloxetine clinical trials (Eli Lilly and Company). Study Selection: All 11 acute, double-blind, placebo-controlled studies of duloxetine (7 with duloxetine 60-mg doses and 4 with non–60-mg doses) in the database that used a scale to measure painful physical symptoms and were completed before March 17, 2011. Data Extraction: For each study, patients with clinically significant pain levels at baseline (Visual Analog Scale overall pain rating ≥ 30, Numerical Rating Scale score ≥ 3, or Brief Pain Inventory 24-hour average pain rating ≥ 3) were selected in order to determine the effect sizes of duloxetine (compared with placebo for each trial) on the pain and depression measures. Overall effect sizes for both painful physical symptoms and MDD were obtained from the mean of individual-trial effect sizes, and each effect size was weighted relative to the number of patients within each study. Data Synthesis: The overall mean effect sizes were as follows: painful physical symptoms—60-mg trials, 0.29 (95% CI, 0.06 to 0.52); non–60-mg trials, 0.13 (95% CI, −0.19 to 0.45); MDD—60-mg trials, 0.29 (95% CI, 0.18 to 0.40); non–60-mg trials, 0.16 (95% CI, 0.00 to 0.32). Across the 11 studies, the weighted effect size for painful physical symptoms was 0.26 (95% CI, 0.00 to 0.51) and for MDD, 0.25 (95% CI, 0.16 to 0.34). Conclusions: According to this meta-analysis, duloxetine 60 mg once daily is as effective in improving painful physical symptoms as it is for depression in patients with MDD and clinically significant painful physical symptoms. The results of this meta-analysis indicate that duloxetine has small effect sizes in reducing painful physical symptoms and depressive symptoms in patients

  15. The role of the NMDA receptors and l-arginine-nitric oxide-cyclic guanosine monophosphate pathway in the antidepressant-like effect of duloxetine in the forced swimming test.

    PubMed

    Zomkowski, Andréa D E; Engel, Daiane; Cunha, Mauricio P; Gabilan, Nelson H; Rodrigues, Ana Lúcia S

    2012-12-01

    Duloxetine is a selective serotonin and noradrenaline reuptake inhibitor used as antidepressant. However, its mechanisms of action are not fully understood. This study investigated the effect of duloxetine in the mouse forced swimming test (FST) and in the tail suspension test (TST) and the involvement of the NMDA receptors and the l-arginine-NO-cGMP pathway in its effect in the FST. Duloxetine reduced the immobility time both in the FST and in the TST (dose range of 1-30mg/kg, i.p.), without changing locomotion in an open-field. Duloxetine administered orally (1-30mg/kg) also reduced the immobility time in the FST. The effect of duloxetine (10mg/kg, p.o.) in the FST was prevented by pre-treatment with NMDA (0.1pmol/site, i.c.v.), d-serine (30μg/site, i.c.v.), (l-arginine (750mg/kg, i.p.), S-nitroso-N-acetyl-penicillamine (SNAP, 25μg/site, i.c.v) or sildenafil (5mg/kg, i.p.). The administration of MK-801 (0.001mg/kg, i.p.), 7-nitroindazole (50mg/kg, i.p.), methylene blue (20mg/kg, i.p.) or 1H-[1,2,4]oxadiazole[4,3-a]quinoxalin-1-one (ODQ) (30pmol/site i.c.v.) in combination with a sub-effective dose of duloxetine (0.3mg/kg, p.o.) reduced the immobility time in the FST. Moreover, the administration of duloxetine (10mg/kg) produced a reduction in NOx levels in the hippocampus and cerebral cortex. Altogether the results suggest that the effect of duloxetine in the FST is dependent on either a blockade of NMDA receptors or an inhibition of NO. In addition, our results further reinforce the role of NMDA receptors and l-arginine-NO-cGMP pathway, besides the monoaminergic systems, in the mechanism of action of current prescribed antidepressant agents.

  16. In vitro and in silico investigation of electrospun terbinafine hydrochloride-loaded buccal nanofibrous sheets.

    PubMed

    Szabó, Péter; Daróczi, Tünde Beáta; Tóth, Gergő; Zelkó, Romána

    2016-11-30

    Terbinafine hydrochloride-loaded nanofibrous buccal films were formulated with the aim to improve the solubility and dissolution behavior; thus, the local effectiveness of the antifungal agent. Poly(vinyl alcohol) and chitosan polymer composites were selected as delivery base in order to enhance the mucoadhesion of the fibrous films. The dissolution of terbinafine hydrochloride was carried out applying a stainless steel disc assembly and the terbinafine concentration was determined by HPLC-MS in selective ion monitoring mode. The prediction of the absorption behavior of the prepared fibrous samples in the human oral cavity was modeled using GastroPlus™ software. The result indicates that the fibrous films enabled fast and complete dissolution of the active agent. The drug absorption from the oral cavity could be minimized by the employment of the proper oral transit model. Because of the limited absorption of terbinafine hydrochloride from the oral mucosa the formulation can be beneficial in local administration in the case of hold and expectorate administration mode.

  17. 21 CFR 522.723 - Diprenorphine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...) Specifications. Each milliliter of diprenorphine hydrochloride injection, veterinary, contains 2 mg of... injection, veterinary, the use of which is provided for in § 522.883, in wild and exotic animals. (2) It...

  18. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ...: (1) Amount. The equivalent of 8 milligrams of levamisole hydrochloride per kilogram of body weight... thoroughly. Allow 1 gallon of medicated water for each 100 pounds body weight of pigs to be treated. No...

  19. 21 CFR 522.1642 - Oxymorphone hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... milligrams of oxymorphone hydrochloride per milliliter of aqueous solution containing 0.8 percent sodium chloride. (b) Sponsor. See No. 060951 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The...

  20. 21 CFR 522.1642 - Oxymorphone hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... milligrams of oxymorphone hydrochloride per milliliter of aqueous solution containing 0.8 percent sodium chloride. (b) Sponsor. See No. 060951 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The...

  1. 21 CFR 522.1642 - Oxymorphone hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... milligrams of oxymorphone hydrochloride per milliliter of aqueous solution containing 0.8 percent sodium chloride. (b) Sponsor. See No. 060951 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The...

  2. A novel formulation for mebeverine hydrochloride.

    PubMed

    Abdel-Hamid, Sameh M; Abdel-Hady, Seham E; El-Shamy, Abdel-Hamid A; El-Dessouky, Hadir F

    2007-10-01

    The antispasmodic drug mebeverine hydrochloride was formulated into a film-forming gel to be used as a topical local anesthetic. A mixture of cellulose derivatives was used as a base. Additives were used to enhance the release as well as the residence time. Formulations were characterized in terms of drug release, mucoadhesion and rheology. Clinically, the selected formula has shown faster onset (p = 0.0156), longer duration (p = 0.0313), better film residence (p = 0.0313), and no foreign body sensation (p = 0.0313) in comparison to Solcoseryl dental paste. Histopathological examination showed no change in inflammatory cells count, concluding that this topical anesthetic is efficacious and safe orally.

  3. Efficacy and tolerance of repeated oral doses of tolperisone hydrochloride in the treatment of painful reflex muscle spasm: results of a prospective placebo-controlled double-blind trial.

    PubMed

    Pratzel, H G; Alken, R G; Ramm, S

    1996-10-01

    The efficacy and safety of oral tolperisone hydrochloride (Mydocalm) in the treatment of painful reflex muscle spasm was assessed in a prospective, randomized, double-blind, placebo-controlled trial. A total of 138 patients, aged between 20 and 75 years, with painful reflex muscle spasm associated with diseases of the spinal column or proximal joints were enrolled in eight rehabilitation centers. Patients were randomized to receive either 300 mg tolperisone hydrochloride or placebo for a period of 21 days. Both treatment groups recovered during the 3 weeks rehabilitation program. However, tolperisone hydrochloride proved to be significantly superior to placebo: the change score of the pressure pain threshold as the primary target parameter significantly increased during therapy with tolperisone hydrochloride (P = 0.03, valid-case-analysis) compared to the results obtained on placebo treatment. The overall assessment of efficacy by the patient also demonstrated significant differences in favor of tolperisone hydrochloride. Best results were seen in patients aged between 40 and 60 years with a history of complaints shorter than 1 year and with concomitant physical therapy. The evaluation of safety data, i.e., adverse events, biochemical and hematological laboratory parameters, demonstrated no differences between tolperisone hydrochloride and placebo. As a conclusion tolperisone hydrochloride represents an effective and safe treatment of painful reflex muscle spasm without the typical side effects of centrally active muscle relaxants.

  4. Comparison of neurotropic effects of L-glutamic acid and its new derivative β-phenylglutamic acid hydrochloride (RGPU-135, glutarone).

    PubMed

    Tyurenkov, I N; Bagmetova, V V; Chernysheva, Yu V; Merkushenkova, O V

    2014-04-01

    In contrast to L-glutamic acid (200 mg/kg), β-phenylglutamic acid hydrochloride (26 mg/kg) produces no anticonvulsant effects during generalized convulsions induced by "maximum electric shock". However, β-phenylglutamic acid hydrochloride was more potent than L-glutamic acid in increasing survival rate, promoting recovery of spontaneous motor activity, and maintainance locomotor and exploratory activity in the open field test and cognitive functions in conditioned passive avoidance test, i.e. exhibited neuroprotective activity. This substance did not change the threshold of pain induced by electric stimulation of paws (up to vocalization) and thermal tail stimulation (tail-flick), whereas L-glutamic acid decreased this parameter. β-Phenylglutamic acid suppressed aggression in the test for provoked unmotivated aggression, while L-glutamic acid enhanced it. Due to these neurotropic effects, β-phenylglutamic acid hydrochloride can be used as the basis for the development of drugs with antidepressant, anxiolytic, and neuroprotective actions.

  5. Simultaneous determination of pseudoephedrine hydrochloride, chlorpheniramine maleate, and dextromethorphan hydrobromide by second-derivative photodiode array spectroscopy.

    PubMed

    Murtha, J L; Julian, T N; Radebaugh, G W

    1988-08-01

    The simultaneous determination of the active ingredients in multicomponent pharmaceutical products normally requires the use of a separation technique, such as HPLC or GC, followed by quantitation. Presented here is a rapid, validated, analytical method that does not require prior separation for the simultaneous determination of three drugs, pseudoephedrine hydrochloride, chlorpheniramine maleate, and dextromethorphan hydrobromide, in a tablet formulation. A diode array spectrophotometer, capable of multicomponent analysis, was used for the quantitation. The utility of this method was demonstrated in two ways: the analysis of a chewable pediatric tablet (formulation CP) containing 7.5 mg of pseudoephedrine hydrochloride, 0.5 mg of chlorpheniramine maleate, and 2.5 mg of dextromethorphan hydrobromide, and the dissolution analysis of a hydroxypropyl methylcellulose-based sustained-release tablet (formulation SR) containing 120 mg of pseudoephedrine hydrochloride, 8 mg of chlorpheniramine maleate, and 60 mg of dextromethorphan hydrobromide. The sensitivity of this assay is 7.5 micrograms/mL for pseudoephedrine hydrochloride, 1.0 micrograms/mL for chlorpheniramine maleate, and 5.0 micrograms/mL for dextromethorphan hydrobromide, using the second-derivative spectra of the absorbance with respect to wavelength. Determinations were made in 0.1 M sodium acetate buffer at pH 5.0 using a 1-cm quartz cell. Absorbance spectra, and their first and second derivatives, from 240 to 300 nm were used for the determination. The results obtained by this method compared favorably with the results obtained by a validated HPLC method.

  6. A Post Hoc Analysis of D-Threo-Methylphenidate Hydrochloride (Focalin) Versus D,l-Threo-Methylphenidate Hydrochloride (Ritalin)

    ERIC Educational Resources Information Center

    Weiss, Margaret; Wasdell, Michael; Patin, John

    2004-01-01

    Objective: To evaluate clinical measures of the benefit/risk ratio in a post hoc analysis of a clinical trial of d-threo-methylphenidate hydrochloride (d-MPH) and d,l-threo-methylphenidate hydrochloride (d,l-MPH). Method: Data from a phase III clinical trial was used to compare equimolar doses of d-MPH and d,l-MPH treatment for…

  7. The use of tiletamine hydrochloride and zolazepam hydrochloride for sedation of the mountain brushtial possum, Trichosurus caninus Ogilby (Phalangeridae: Marsupialia).

    PubMed

    Viggers, K L; Lindenmayer, D B

    1995-06-01

    A combination of tiletamine hydrochloride and zolazepam hydrochloride in a 1:1 ration by weight was used successfully to sedate mountain brushtail possums, Trichosurus caninus, in the field. A standard total dose of 50 to 60 mg provided adequate sedation for the completion of a range of handling procedures. We describe the induction time, dose rate and side-effects associated with the use of tiletamine and zolazepam in T caninus.

  8. In vitro inhibitory effects of palonosetron hydrochloride, bevacizumab and cyclophosphamide on purified paraoxonase-I (hPON1) from human serum.

    PubMed

    Türkeş, Cüneyt; Söyüt, Hakan; Beydemir, Şükrü

    2016-03-01

    In this study, we investigated the effects of the drugs, palonosetron hydrochloride, bevacizumab and cyclophosphamide, on human serum paraoxonase-I (hPON1) enzyme activity in in vitro conditions. The enzyme was purified ∼231-fold with 34.2% yield by using ammonium sulphate precipitation, DEAE-Sephadex A-50 ion-exchange chromatography and Sephadex G-200 gel-filtration chromatography from human serum. hPON1 exhibited a single protein band on the SDS polyacrylamide gel electrophoresis. The inhibition studies were performed on paraoxonase activity of palonosetron hydrochloride, bevacizumab and cyclophosphamide. Ki constants were found as 0.033±0.001, 0.054±0.003 mM and 3.419±0.518 mM, respectively. Compared to the inhibition rates of the drugs, palonosetron hydrochloride has the maximum inhibition rate. However, inhibition mechanisms of the drugs were determined as noncompetitive by Lineweaver-Burk curves.

  9. The antimycotic drugs itraconazole and terbinafine hydrochloride induce the production of human β-defensin-3 in human keratinocytes.

    PubMed

    Kanda, Naoko; Kano, Rui; Ishikawa, Takeko; Watanabe, Shinichi

    2011-04-01

    The antimicrobial peptide human β-defensin-3 (hBD-3) is produced by epidermal keratinocytes, and exhibits broad killing activity against bacteria or fungi. Prostaglandin D(2) enhances hBD-3 production in human keratinocytes by stimulating a transcription factor, activator protein-1 via chemoattractant receptor-homologous molecule expressed on T helper 2 cells (CRTH2). Prostaglandin H(2), a precursor of prostaglandin D(2) can be converted to thromboxane A(2). Certain antimycotic drugs act on keratinocytes and modulate their production of chemokines. In this in vitro study, we examined the effects of antimycotics on hBD-3 production in human keratinocytes. Antimycotics itraconazole and terbinafine hydrochloride increased hBD-3 secretion and mRNA levels in parallel to the enhanced activity of activator protein-1, expression and phosphorylation of activator protein-1 component, c-Fos, but fluconazole was ineffective. These effects were abrogated by CRTH2 antagonist. Itraconazole and terbinafine hydrochloride increased prostaglandin D(2) release from keratinocytes and reduced the release of thromboxane B(2), a thromboxane A(2) metabolite. The conditioned medium from itraconazole or terbinafine hydrochloride-treated keratinocytes inhibited the growth of Candida albicans dependently on hBD-3. These results suggest that itraconazole and terbinafine hydrochloride may enhance c-Fos expression and phosphorylation, activator protein-1 activity and hBD-3 production by increasing prostaglandin D(2) release from keratinocytes. These antimycotic drugs may suppress thromboxane A(2) synthesis and redirect the conversion of prostaglandin H(2) towards prostaglandin D(2). The induction of hBD-3 in keratinocytes is another possible mechanism for the antimycrobial effects of these drugs, which may augment the cutaneous defense activity against infection.

  10. Combination therapy for erectile dysfunction: a randomized, double blind, unblinded active-controlled, cross-over study of the pharmacodynamics and safety of combined oral formulations of apomorphine hydrochloride, phentolamine mesylate and papaverine hydrochloride in men with moderate to severe erectile dysfunction.

    PubMed

    Lammers, P I; Rubio-Aurioles, E; Castell, R; Castaneda, J; Ponce de Leon, R; Hurley, D; Lipezker, M; Loehr, L A; Lowrey, F

    2002-02-01

    Oral therapy has become first line treatment for patients with mild to moderate erectile dysfunction (ED). Studies have shown that sildenafil may not be effective in all patients, and has been associated with a variety of adverse effects and an adverse interaction with nitrates and inhibitors of cytochrome P450 enzymes. The objective was to compare the efficacy and safety of three different oral combinations with the highest dose of sildenafil in men with moderate to severe ED. Randomized, double blind, unblinded active-controlled, Phase II study was carried out at three sites in Mexico. After a 4-week placebo run-in period, patients received all four of the following treatments using a 4-way cross-over design: 40 mg phentolamine (PM) +6 mg apomorphine (Apo); 40 mg PM +150 mg papaverine (Pap); 40 mg PM +6 mg Apo +150 mg Pap (Tricombo); 100 mg sildenafil (SC). With the exception of sildenafil tablets, all study medication was blinded. Moderate to severe ED was defined as a less than 50% vaginal penetration success rate during the placebo run-in period. A total of 44 patients were enrolled, of whom 36 completed all four treatment periods. All treatments produced a significant effect in primary efficacy variable (Sexual Encounter Profile) compared to baseline, however, no statistically significant differences were found between treatments. A significant period effect was observed. Also, the four treatments were found not to differ significantly in five out of six secondary efficacy variables. The lowest incidence of treatment-related adverse events (AE) occurred in the 40 mg PM +6 mg Apo group (9.8%), followed by 100 mg SC (15%), and the other two combinations (16.7 and 17.5%, respectively). Nasocongestion and headache were the most frequently reported AE. An oral combination of vasoactive agents may provide an alternative approach to sildenafil. Based on these results a combination of phentolamine and apomorphine warrants further clinical investigation.

  11. Effect of sertraline hydrochloride on dialysis hypotension.

    PubMed

    Dheenan, S; Venkatesan, J; Grubb, B P; Henrich, W L

    1998-04-01

    Hemodialysis hypotension (HH) is a very common disorder and has a multifactorial etiology. Autonomic dysfunction occurs in up to 50% of patients with end-stage renal disease (ESRD) and plays a key role in HH in some patients. Sertraline hydrochloride, a central nervous system serotonin reuptake inhibitor, has been shown to be an effective treatment of hypotension caused by autonomic dysfunction in disorders such as neurocardiogenic syncope and idiopathic orthostatic hypotension. This study sought to determine whether sertraline was effective in ameliorating HH. A retrospective chart analysis was performed that included nine consecutive patients (aged > or = 54 years, time on hemodialysis > or = 2.2 years) placed on sertraline (50 to 100 mg/d) for depression who also had HH (defined as prehemodialysis systolic blood pressure [SBP] < or = 100 mm Hg, > or = 40 mm Hg decrease in SBP during hemodialysis, SBP <90 mm Hg, any diastolic blood pressure <40 mm Hg, or a decrease in blood pressure-causing symptoms) before treatment with sertraline. The data from a 6-week pre-sertraline period were compared with the data from a 6-week sertraline period (defined as 6 weeks after drug begun). Blood pressure medications were unchanged during the trial period of sertraline. However, nadir mean arterial pressure recorded during a given dialysis session in the pre-sertraline period (55+/-4 mm Hg) was significantly lower than that recorded in the sertraline period (68+/-5 mm Hg; P < 0.05). In addition, the number of hypotensive episodes (same definition as HH) per dialysis session during the sertraline period was significantly lower than that during the pre-sertraline period (mean, 0.6+/-0.2 episodes per session v 1.4+/-0.3 episodes per session; P < 0.005). The number of therapeutic interventions required for hypotension during the sertraline period was also significantly less than that during the pre-sertraline period (mean, 1.7+/-0.8 interventions v 11.0+/-3.0 interventions; P < 0

  12. Solvent screening and crystal habit of metformin hydrochloride

    NASA Astrophysics Data System (ADS)

    Benmessaoud, Ibtissem; Koutchoukali, Ouahiba; Bouhelassa, Mohamed; Nouar, Abderrahim; Veesler, Stéphane

    2016-10-01

    A multi-well setup with video-microscopy was used to study the influence of solvent on solubility, nucleation, and crystallization of an Active Pharmaceutical Ingredient (API): metformin hydrochloride (MET.HCl). Starting with 13 solvents covering a wide variety of polarity and proticity, we found 63 crystallization medium for MET.HCl solid generation: good solvents, good co-solvents and anti-solvent systems. For toxicological reasons, we limited the number of crystallization medium to 18: 3 good solvents (class 3), 3 good co-solvent systems and 12 anti-solvent systems. In order to study the influence of crystallization medium on nucleation temperature, crystal habit and polymorphism of MET.HCl, crystallization was studied by a cooling temperature method. Different crystal habits were observed by optical and scanning electron microscopies, and solid phase were characterized by X-ray powder diffraction, indicating that all the crystals correspond to the thermodynamic stable polymorphic form A of MET.HCl. Finally, the enthalpy of fusion and the melting temperature of MET.HCl were determined by DSC and confirmed the X-ray powder diffraction results.

  13. Pharmacokinetic interactions between Japanese traditional medicine (kampo) and modern medicine (III). Effect of Sho-seiryu-to on the pharmacokinetics of azelastine hydrochloride in rats.

    PubMed

    Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-Ichi; Kano, Yoshihiro

    2004-05-01

    Sho-seiryu-to (SST) is widely used herbal formula in Japanese traditional medicine (kampo) to treat allergic diseases. Since Japanese physicians frequently prescribe this formula combined with azelastine hydrochloride, one of anti-histamine and anti-allergic medicines, we evaluated the pharmacokinetic interactions between SST and azelastine hydrochloride in rats to obtain the drug information for the prevention from disadvantage or adverse effects by their combined therapy. Oral administration of SST did not influence the plasma concentration profile of azelastine after its intravaneous injection, suggesting that SST would not change the activities of metabolic enzymes such as cytochrome P450s. However, maximum concentration (C(max)) of azelastine after oral administration of azelastine hydrochloride was significantly reduced and mean residence time (MRT) was significantly lengthened when SST was orally administered at 20 times amount of human daily dosage. There was not significant difference in the area under the plasma concentration-time curve (AUC), suggesting that SST might delay the absorption of azelastine without affecting the extent of bioavailability. Since this delay was independent of ephedrine that is a main constituent of SST and that a suppressor for gastric transit, SST might form unsoluble complex with azelastine to reduce its absorption. At the double of human daily dose, SST did not made the absorption of azelastine delay. The possibility that SST reduce the absorption of azelastine hydrochloride could not be denied completely, however, it is suggested that SST would not cause pharmacokinetic interaction with azelastine hydrochloride clinically.

  14. Development and Validation of a Stability-Indicating RP-UPLC Method for the Estimation of Impurities in Cinacalcet Hydrochloride API and its Formulation.

    PubMed

    Sunil Reddy, Pingili; Raju, Thummala Veera Raghava; Raju, Penmetsa Satyanarayana; Varma, Nadimpalli Sunil; Babu, Kondra Sudhakar

    2015-01-01

    A sensitive, stability-indicating, gradient reversed-phase ultra-performance liquid chromatography method has been developed for the quantitative estimation of cinacalcet hydrochloride impurities in active pharmaceutical ingredients and pharmaceutical formulations. Efficient chromatographic separation was achieved on an Acquity BEH Shield RP18, 100 × 2.1 mm, 1.7 µm column with the mobile phase containing pH 6.6 phosphate buffer and acetonitrile. The flow rate of the mobile phase was 0.3 mL min(-1) with a column temperature of 35°C and detection wavelength at 223 nm. The relative response factor values of (+)-R-1-(1-Naphthyl)ethylamine, regioisomer, diastereomer isomer-1, and diastereomer isomer-2 were 1.79, 0.99, 0.89, and 0.88, respectively. The cinacalcet hydrochloride formulation sample was subjected to the stress conditions of acid, base, oxidative, hydrolytic, thermal, humidity, and photolytic degradation. Cinacalcet hydrochloride was found to degrade significantly under the peroxide stress conditions. The degradation products were well-resolved from cinacalcet hydrochloride and its impurities. The peak purity test results confirmed that the cinacalcet hydrochloride peak was homogenous in all stress samples and the mass balance was found to be more than 96%, thus proving the stability-indicating power of the method. The developed method was validated according to ICH guidelines.

  15. Development and Validation of a Stability-Indicating RP-UPLC Method for the Estimation of Impurities in Cinacalcet Hydrochloride API and its Formulation

    PubMed Central

    Sunil Reddy, Pingili; Raju, Thummala Veera Raghava; Raju, Penmetsa Satyanarayana; Varma, Nadimpalli Sunil; Babu, Kondra Sudhakar

    2015-01-01

    A sensitive, stability-indicating, gradient reversed-phase ultra-performance liquid chromatography method has been developed for the quantitative estimation of cinacalcet hydrochloride impurities in active pharmaceutical ingredients and pharmaceutical formulations. Efficient chromatographic separation was achieved on an Acquity BEH Shield RP18, 100 × 2.1 mm, 1.7 µm column with the mobile phase containing pH 6.6 phosphate buffer and acetonitrile. The flow rate of the mobile phase was 0.3 mL min−1 with a column temperature of 35°C and detection wavelength at 223 nm. The relative response factor values of (+)-R-1-(1-Naphthyl)ethylamine, regioisomer, diastereomer isomer-1, and diastereomer isomer-2 were 1.79, 0.99, 0.89, and 0.88, respectively. The cinacalcet hydrochloride formulation sample was subjected to the stress conditions of acid, base, oxidative, hydrolytic, thermal, humidity, and photolytic degradation. Cinacalcet hydrochloride was found to degrade significantly under the peroxide stress conditions. The degradation products were well-resolved from cinacalcet hydrochloride and its impurities. The peak purity test results confirmed that the cinacalcet hydrochloride peak was homogenous in all stress samples and the mass balance was found to be more than 96%, thus proving the stability-indicating power of the method. The developed method was validated according to ICH guidelines. PMID:26839840

  16. Stability of cefozopran hydrochloride in aqueous solutions.

    PubMed

    Zalewski, Przemysław; Skibiński, Robert; Paczkowska, Magdalena; Garbacki, Piotr; Talaczyńska, Alicja; Cielecka-Piontek, Judyta; Jelińska, Anna

    2016-01-01

    The influence of pH on the stability of cefozopran hydrochloride (CZH) was investigated in the pH range of 0.44-13.00. Six degradation products were identified with a hybrid ESI-Q-TOF mass spectrometer. The degradation of CZH as a result of hydrolysis was a pseudo-first-order reaction. As general acid-base hydrolysis of CZH was not occurred in the solutions of hydrochloric acid, sodium hydroxide, acetate, borate and phosphate buffers, kobs = kpH because specific acid-base catalysis was observed. Specific acid-base catalysis of CZH consisted of the following reactions: hydrolysis of CZH catalyzed by hydrogen ions (kH+), hydrolysis of dications (k1H2O), monocations (k2H2O) and zwitter ions (k3H2O) and hydrolysis of zwitter ions (k1OH-) and monoanions (k2OH-) of CZH catalyzed by hydroxide ions. The total rate of the reaction was equal to the sum of partial reactions: [Formula: see text]. CZH similarly like other fourth generation cephalosporin was most stable at slightly acidic and neutral pH and less stable in alkaline pH. The cleavage of the β-lactam ring resulting from a nucleophilic attack on the carbonyl carbon in the β-lactam moiety is the preferred degradation pathway of β-lactam antibiotics in aqueous solutions.

  17. Pharmacokinetic and pharmacodynamic interactions among haloperidol, carteolol hydrochloride and biperiden hydrochloride.

    PubMed

    Isawa, S; Murasaki, M; Miura, S; Yoshioka, M; Uchiumi, M; Kumagai, Y; Aoki, S; Hisazumi, H; Kudo, S

    1999-07-01

    A beta-adrenoceptor blocker and an anticholinergic agent are often prescribed concomitantly for the treatment of neuroleptic-induced akathisia. The aim of this study was to investigate possible pharmacokinetic interactions of neuroleptic haloperidol with the beta-blocker carteolol and the anticholinergic biperiden. In a 5-step, open-labeled, oral single-dose study, eight healthy male volunteers received 2 mg haloperidol, 10 mg carteolol hydrochloride, and 2 mg biperiden hydrochloride: first each drug alone, then a combination of haloperidol and carteolol, and then all three drugs concurrently. Serum concentrations of haloperidol, carteolol, and biperiden were determined up to 24 hr postdosing, and a safety evaluation was conducted throughout the study. Carteolol increased the area under the haloperidol serum concentration-time curve (AUC0-t) 1.4-fold (P = 0.0014) and decreased the serum clearance of haloperidol up to 67% (P = 0.0127). Biperiden reduced the serum haloperidol concentrations increased by the administration of carteolol. No significant changes of the serum pharmacokinetics of carteolol and biperiden were found as a result of any drug combinations. Adverse events of the central nervous system such as sleepiness and changes in pupil size were observed, but all were mild with clinical insignificance.

  18. Duloxetine prevents the effects of prenatal stress on depressive-like and anxiety-like behavior and hippocampal expression of pro-inflammatory cytokines in adult male offspring rats.

    PubMed

    Zhang, Xiaosong; Wang, Qi; Wang, Yan; Hu, Jingmin; Jiang, Han; Cheng, Wenwen; Ma, Yuchao; Liu, Mengxi; Sun, Anji; Zhang, Xinxin; Li, Xiaobai

    2016-12-01

    Stress during pregnancy may cause neurodevelopmental and psychiatric disorders. However, the mechanisms are largely unknown. Currently, pro-inflammatory cytokines have been identified as a risk factor for depression and anxiety disorder. Unfortunately, there is very little research on the long-term effects of prenatal stress on the neuroinflammatory system of offspring. Moreover, the relationship between antidepressant treatment and cytokines in the central nervous system, especially in the hippocampus, an important emotion modulation center, is unclear. Therefore, the aim of this study was to determine the effects of prenatal chronic mild stress during development on affective-like behaviors and hippocampal cytokines in adult offspring, and to verify whether antidepressant (duloxetine) administration from early adulthood could prevent the harmful consequences. To do so, prenatally stressed and non-stressed Sprague-Dawley rats were treated with either duloxetine (10mg/kg/day) or vehicle from postnatal day 60 for 21days. Adult offspring were divided into four groups: 1) prenatal stress+duloxetine treatment, 2) prenatal stress+vehicle, 3) duloxetine treatment alone, and 4) vehicle alone. Adult offspring were assessed for anxiety-like behavior using the open field test and depression-like behavior using the forced swim test. Brains were analyzed for pro-inflammatory cytokine markers in the hippocampus via real-time PCR. Results demonstrate that prenatal stress-induced anxiety- and depression-like behaviors are associated with an increase in hippocampal inflammatory mediators, and duloxetine administration prevents the increased hippocampal pro-inflammatory cytokine interleukin-6 and anxiety- and depression-like behavior in prenatally stressed adult offspring. This research provides important evidence on the long-term effect of PNS exposure during development in a model of maternal adversity to study the pathogenesis of depression and its therapeutic interventions.

  19. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  20. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  1. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  2. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  3. 21 CFR 522.1662b - Oxytetracycline hydrochloride with lidocaine injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride with lidocaine... FORM NEW ANIMAL DRUGS § 522.1662b Oxytetracycline hydrochloride with lidocaine injection. (a) Specifications. The drug contains 50 or 100 milligrams of oxytetracycline hydrochloride and 2 percent...

  4. 77 FR 7583 - Determination That WILPO (phentermine hydrochloride) Tablets, 8 Milligrams, Was Not Withdrawn...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-02-13

    ... determined that WILPO (phentermine hydrochloride) Tablets, 8 Milligrams (mg), was not withdrawn from sale for... Applications (ANDAs) for phentermine hydrochloride tablets, 8 mg, if all other legal and regulatory... does not refer to a listed drug. WILPO (phentermine hydrochloride) Tablets, 8 mg is the subject of...

  5. The effect of excipients on the stability and phase transition rate of xylazine hydrochloride and zopiclone.

    PubMed

    Krūkle-Bērziņa, Kristīne; Actiņš, Andris

    2015-03-25

    The compatibility of thermodynamically unstable polymorph of two active pharmaceutical compounds (xylazine hydrochloride form X and zopiclone form C) with different excipients was investigated. The effects of the excipient and its amount in the sample on the thermal properties and possible chemical interactions were studied. The most commonly used excipients in the pharmaceutical industry - calcium carbonate, lactose hydrate, cellulose, magnesium stearate hydrate and calcium stearate hydrate were selected for this study. The dependence of the phase transition rate from an unstable to a more stable polymorph on the excipients and their amounts in the initial sample was analysed at 80°C, and the corresponding phase transition rate constants were calculated.

  6. Simultaneous programmed temperature GLC assay of phenol, chloroxylenol, and lidocaine hydrochloride in topical antiseptic cream.

    PubMed

    Palermo, P J; Lundberg, J B

    1978-11-01

    A simultaneous programmed temperature GLC assay for the active ingredients in a topical antiseptic cream is described. The sample is extracted directly using a dimethyl sulfoxide solution of p-cresol, 4-chlorophenol, and 2-amino-4-phenylthiazole as internal standards for phenol, chloroxylenol, and lidocaine hydrochloride, respectively. The resulting solution is chromatographed by temperature programming on an OV-225 column from 90 to 225 degrees. The internal standard calculation is accomplished using peak heights or peak areas. The relative standard deviation of all assays is less than 2%.

  7. Spectrophotometric determination of meclizine hydrochloride and pyridoxine hydrochloride in laboratory prepared mixtures and in their pharmaceutical preparation.

    PubMed

    Ibrahim, Maha M; Elzanfaly, Eman S; El-Zeiny, Mohamed B; Ramadan, Nesreen K; Kelani, Khadiga M

    2017-05-05

    In this paper, three rapid, simple, accurate and precise spectrophotometric methods were developed for the determination of meclizine hydrochloride in the presence of pyridoxine hydrochloride without previous separation. The methods under study are dual wavelength (DWL), ratio difference (RD) and continuous wavelet transform (CWT). On the other hand, pyridoxine hydrochloride (PYH) was determined directly at 291nm. The methods obey Beer's law in the range of (5-50μg/mL) for both compounds. All the methods were validated according to the ICH guidelines where the accuracy was found to be 98.29, 99.59, 100.42 and 100.62% for DWL, RD, CWT and PYH; respectively. Moreover the precision of the methods were calculated in terms of %RSD and it was found to be 0.545, 0.372, 1.287 and 0.759 for DWL, RD,CWT and PYH; respectively. The selectivity of the proposed methods was tested using laboratory prepared mixtures and assessed by applying the standard addition technique. So, they can be used for the routine analysis of pyridoxine hydrochloride and meclizine hydrochloride in quality-control laboratories.

  8. Feasibility of amlodipine besylate, chloroquine phosphate, dapsone, phenytoin, pyridoxine hydrochloride, sulfadiazine, sulfasalazine, tetracycline hydrochloride, trimethoprim and zonisamide in SyrSpend(®) SF PH4 oral suspensions.

    PubMed

    Ferreira, Anderson O; Polonini, Hudson C; Silva, Sharlene L; Patrício, Fernando B; Brandão, Marcos Antônio F; Raposo, Nádia R B

    2016-01-25

    The objective of this study was to evaluate the feasibility of 10 commonly used active pharmaceutical ingredients (APIs) compounded in oral suspensions using an internationally used suspending vehicle (SyrSpend(®) SF PH4 liquid): (i) amlodipine, (as besylate) 1.0mg/mL; (ii) chloroquine phosphate,15.0 mg/mL; (iii) dapsone, 2.0 mg/mL; (iv) phenytoin, 15.0 mg/mL; (v) pyridoxine hydrochloride, 50.0 mg/mL; (vi) sulfadiazine, 100.0 mg/mL; (vii) sulfasalazine, 100.0 mg/mL; (viii) tetracycline hydrochloride, 25.0 mg/mL; (ix) trimethoprim, 10.0 mg/mL; and (x) zonisamide, 10.0 mg/mL. All suspensions were stored both at controlled refrigeration (2-8 °C) and controlled room temperature (20-25 °C). Feasibility was assessed by measuring the percent recovery at varying time points throughout a 90-day period. API quantification was performed by high-performance liquid chromatography (HPLC-UV), via a stability-indicating method. Given the percentage of recovery of the APIs within the suspensions, the expiration date of the final products (API+vehicle) was at least 90 days for all suspensions with regard to both the controlled temperatures. This suggests that the vehicle is stable for compounding APIs from different pharmacological classes.

  9. Colestipol hydrochloride prophylaxis of diarrhea during pelvic radiotherapy

    SciTech Connect

    Stryker, J.A.; Chung, C.K.; Layser, J.D.

    1983-02-01

    Thirty-three patients were randomized prior to pelvic radiotherapy to receive the bile acid-sequestering resin colestipol hydrochloride, 5 grams qid, during the entire time of their therapy or diphenoxylate hydrochloride and atropine sulfate 2.5-20 mg per day (control) if they experienced diarrhea. The colestipol patients also took diphenoxylate if they had diarrhea. The patients in the colestipol group often experienced nausea, vomiting, and abdominal cramps and 8 were forced to discontinue the drug. There was no difference in the weekly stool frequency between the colestipol and the control patients but the colestipol patients who took at least 50% of the prescribed dose required fewer diphenoxylate tablets than the controls. The data suggest that colestipol hydrochloride is not of value in preventing radiation-induced diarrhea because of the side effects associated with the drug, but the theory on which the use of bile acid-sequestering agents is based may be correct.

  10. Degradation of Verapamil hydrochloride in water by gliding arc discharge.

    PubMed

    Krishna, Syam; Maslani, Alan; Izdebski, Tomasz; Horakova, Marta; Klementova, Sarka; Spatenka, Petr

    2016-06-01

    This study investigated the influence of gliding arc plasma discharge on the degradation of Verapamil hydrochloride in water. The plasma discharge was characterized by means of optical emission spectroscopy. Spectra of various atomic and molecular species were observed. Aqueous solution of Verapamil hydrochloride was exposed to gliding arc discharge operated in continuous discharge at atmospheric pressure and room temperature. The identification of Verapamil, the degradation mechanisms of Verapamil and its transformation products were performed using liquid chromatography - mass spectrometry (HPLC-MS). Experimental results indicate that the atmospheric pressure gliding arc plasma treatment has noticeable effects on Verapamil with satisfactory degradation efficiency. Plausible mechanisms of the degradation were discussed.

  11. A new HPLC method to determine Donepezil hydrochloride in tablets.

    PubMed

    Pappa, Horacio; Farrú, Romina; Vilanova, Paula Otaño; Palacios, Marcelo; Pizzorno, María Teresa

    2002-01-01

    A HPLC stability-indicating assay for Donepezil hydrochloride in tablets was developed and validated. Donepezil hydrochloride is a reversible inhibitor of acetylcholinesterase, indicated for the treatment of mild to moderate dementia of the Alzheimer's type. The HPLC method was performed with a reversed phase C18 column, detection at 268 nm and a mixture of methanol, phosphate buffer 0.02 M and triethylamine (50:50:0.5) as mobile phase. Typical retention time for Donepezil was 9 min. The method was statistically validated for linearity, accuracy, precision and selectivity following ICH recommendations. Due to its simplicity and accuracy, the method can be used for routine quality control analysis.

  12. A Clinical Study of Efficacy of 4% Articaine Hydrochloride Versus 2% Lignocaine Hydrochloride in Dentistry

    PubMed Central

    Darawade, Dattatraya A; Kumar, Santosh; Budhiraja, Shilpa; Mittal, Manoj; Mehta, Tanvi N

    2014-01-01

    Background: Articaine in an anesthetic agent, which is used less frequently in dentistry. It differs from other agents due to the presence of a thiophene ring in its molecular structure. Few groups of researchers claim that it is superior to lignocaine. Hence, the purpose of this study was to compare the efficacy of 4% articaine hydrochloride and 2% lignocaine hydrochloride in the orthodontic extraction. Materials and Methods: The study was carried out in 50 patients who needed the orthodontic extraction in the age group from 15 to 25 years. Experimental sites were injected with 0.5-1 ml of 4% articaine HCL containing 1:100000 adrenaline, incrementally in the buccal vestibule without palatal anaesthesia. Control sites were injected with 0.8-1 ml of 2% lignocaine HCL containing 1:100000 adrenaline, incrementally in the buccal vestibule. All the parameters, that is volume, duration, time of anesthesia and pain rating were noted and statistically compared. Result: When statistically compared mean volume of articaine (0.779 ± 0.1305) was less than lignocaine (1.337 ± 0.2369). Mean time of onset of articaine was 1.012 ± 0.2058 min, Whereas that of was 1.337 ± 0.2369. Pain rating showed not much difference, but in the lignocaine group palatal anesthesia was required in all the patients. Finally, the mean duration of anesthesia in articaine group was 69.08 ± 18.247, whereas in the lignocaine group was 55.66 ± 6.414. Conclusion: Articaine has proved its usefulness in all regards. Literatures have proved its usefulness. Like other anesthetic, it is safe and more effective. It surpasses the need of additional palatal anesthesia. Rapid inactivation in liver and plasma reduces the risk of the drug overdose. All the above factors make it an ideal anesthetic agent to be used in dentistry. PMID:25395799

  13. Inhibitory gene expression of the Cav3.1 T-type calcium channel to improve neuronal injury induced by lidocaine hydrochloride.

    PubMed

    Wen, Xianjie; Xu, Shiyuan; Zhang, Qingguo; Li, Xiaohong; Liang, Hua; Yang, Chenxiang; Wang, Hanbing; Liu, Hongzhen

    2016-03-15

    Cav3.1 is a low-voltage-activated (LVA) calcium channel that plays a key role in regulating intracellular calcium ion levels. In this study, we observed the effects of lidocaine hydrochloride on the pshRNA-CACNA1G-SH-SY5Y cells that silenced Cav3.1 mRNA by RNA interference, and investigated the roles of p38 MAPK in these effects. We constructed the pNC-puro-CACNA1G-SH-SY5Y cells and pshRNA-CACNA1G -SH-SY5Y cells by the RNA interference. All the cells were cultured with or without 10mM lidocaine hydrochloride for 24 h. The cell morphology, cell viability, Cav3.1 and p38 protein expression, cell apoptosis rate and intracellular calcium ion concentration were detected. We found that all cells treated with 10mM lidocaine hydrochloride for 24 h showed cellular rounding, axonal regression, and cellular floating. Compared with the cells in SH-SY5Y+Lido group and NC+Lido group, those in the RNAi+Lido group showed similar changes, but of smaller magnitude. Additionally, following lidocaine hydrochloride all cells displayed increased Cav3.1 and p38 MAPK protein, apoptosis rate, and intracellular calcium ion levels; however,these changes in the RNAi+Lido group were less pronounced than in the SH-SY5Y+Lido and NC+Lido groups. The cell viability decreased following lidocaine hydrochloride treatment, but viability of the cells in the RNAi+Lido group was higher than in the SH-SY5Y+Lido and NC+Lido groups. The results showed that Cav3.1 may be involved in neuronal injury induced by lidocaine hydrochloride and that p38 MAPK phosphorylation was reduced upon Cav3.1 gene silencing.

  14. Preparation of Mucoadhesive Oral Patches Containing Tetracycline Hydrochloride and Carvacrol for Treatment of Local Mouth Bacterial Infections and Candidiasis

    PubMed Central

    Obaidat, Rana M.; Bader, Ammar; Al-Rajab, Wafa; Abu Sheikha, Ghassan; Obaidat, Aiman A.

    2011-01-01

    The specific aim of this work was to prepare mucoadhesive patches containing tetracycline hydrochloride and carvacrol in an attempt to develop a novel oral drug delivery system for the treatment of mouth infections. The bilayered patches were prepared using ethyl cellulose as a backing layer and carbopol 934 as a matrix mucoadhesive layer. Patches were prepared with different loading amounts of tetracycline hydrochloride and carvacrol. The antimicrobial activity was assessed for the prepared patches using the disc-diffusion method against the yeast Candida albicans and five bacterial strains, including Pseudomonas aeruginosa, Escherichia coli, Bacillus cereus, Staphylococcus aureus, and Bacillus bronchispti. In this work, we highlighted the possibility of occurrence of a synergistic action between carvacrol and tetracycline. The best formulation was selected based on microbiological tests, drug release, ex-vivo mucoadhesive performance, and swelling index. Physical characteristics of the selected formulations were determined. These included pH, patch thickness, weight uniformity, content uniformity, folding endurance, and patch stability. PMID:21617783

  15. Development of hypertension and effects of benazepril hydrochloride in a canine remnant kidney model of chronic renal failure.

    PubMed

    Mishina, Mika; Watanabe, Toshifumi

    2008-05-01

    In order to determine whether hypertension would develop in dogs with chronic renal failure, we performed 7/8 renal ablation in 6 healthy dogs and compared pre- and post-ablation blood pressures determined by telemetry. One month after the renal ablation, blood urea nitrogen and creatinine were significantly increased (p<0.05), creatinine clearance was decreased (p<0.05), and blood pressure was increased significantly (p<0.05). Simultaneously, plasma renin activity, angiotensin I and II, and aldosterone were elevated significantly (p<0.05) compared with the values obtained from 11 healthy dogs with intact renal function. The dogs with induced renal failure and hypertension were administered an angiotensin-converting enzyme inhibitor, benazepril hydrochloride, once daily for 2 weeks at 2 mg/kg body weight, and changes in blood pressure and the renin-angiotensin-aldosterone (RAA) system were determined. During the administration of benazepril hydrochloride, blood pressure, angiotensin II and aldosterone decreased significantly (p<0.05) and, upon discontinuation of administration, increased to the pre-administration levels (p<0.05). Plasma renin activity and angiotensin I showed no significant changes throughout the administration study. These results provide experimental evidence that hypertension develops in dogs with chronic renal failure through mechanisms involving the RAA system and demonstrate that benazepril hydrochloride improves renal hypertension in dogs.

  16. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS §...

  17. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS §...

  18. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS §...

  19. 21 CFR 522.2474 - Tolazoline hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Tolazoline hydrochloride injection. 522.2474 Section 522.2474 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  20. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS §...

  1. 21 CFR 522.2474 - Tolazoline hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Tolazoline hydrochloride injection. 522.2474 Section 522.2474 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  2. 21 CFR 522.2582 - Triflupromazine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Triflupromazine hydrochloride injection. 522.2582 Section 522.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... is used in dogs, cats, and horses to relieve anxiety and to help control psychomotor overactivity...

  3. 21 CFR 522.2582 - Triflupromazine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Triflupromazine hydrochloride injection. 522.2582 Section 522.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... is used in dogs, cats, and horses to relieve anxiety and to help control psychomotor overactivity...

  4. 21 CFR 522.2582 - Triflupromazine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Triflupromazine hydrochloride injection. 522.2582 Section 522.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... is used in dogs, cats, and horses to relieve anxiety and to help control psychomotor overactivity...

  5. 21 CFR 522.2582 - Triflupromazine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Triflupromazine hydrochloride injection. 522.2582 Section 522.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... is used in dogs, cats, and horses to relieve anxiety and to help control psychomotor overactivity...

  6. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS §...

  7. Acute generalized exanthematous pustulosis caused by terazosin hydrochloride.

    PubMed

    Speck, Laura M; Wilkerson, Michael G; Perri, Anthony J; Kelly, Brent C

    2008-04-01

    Acute generalized exanthematous pustulosis (AGEP) is a rare cutaneous eruption mainly provoked by drugs. A case of AGEP in a 74-year-old male that was attributed to the ingestion of terazosin hydrochloride is presented. This is the first reported case of this association in medical literature. The history, clinical presentation, and pathogenesis of AGEP are discussed.

  8. Amides and Hydrazides from Amine and Hydrazine Hydrochlorides.

    ERIC Educational Resources Information Center

    Shama, Sami A.; Tran, Thuan L.

    1978-01-01

    This safe and efficient procedure for the synthesis of N-substituted amides and hydrazides is a modification of the Schotten-Bausmann procedure in which the amine or hydrazide is replaced by the corresponding hydrochloride salt, and the use of alkali is eliminated. (Author/BB)

  9. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ethylisobutrazine hydrochloride injection. 522.863 Section 522.863 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  10. 21 CFR 522.313b - Ceftiofur hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ceftiofur hydrochloride. 522.313b Section 522.313b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS §...

  11. 21 CFR 522.536 - Detomidine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Detomidine hydrochloride injection. 522.536 Section 522.536 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  12. 21 CFR 522.313b - Ceftiofur hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ceftiofur hydrochloride. 522.313b Section 522.313b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS §...

  13. 21 CFR 522.536 - Detomidine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Detomidine hydrochloride injection. 522.536 Section 522.536 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  14. 21 CFR 522.313b - Ceftiofur hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Ceftiofur hydrochloride. 522.313b Section 522.313b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS §...

  15. 21 CFR 522.723 - Diprenorphine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Diprenorphine hydrochloride injection. 522.723 Section 522.723 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  16. 21 CFR 522.313b - Ceftiofur hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ceftiofur hydrochloride. 522.313b Section 522.313b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS §...

  17. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Etorphine hydrochloride injection. 522.883 Section 522.883 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  18. 21 CFR 522.723 - Diprenorphine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Diprenorphine hydrochloride injection. 522.723 Section 522.723 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  19. 21 CFR 522.723 - Diprenorphine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Diprenorphine hydrochloride injection. 522.723 Section 522.723 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  20. 21 CFR 522.536 - Detomidine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Detomidine hydrochloride injection. 522.536 Section 522.536 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  1. 21 CFR 522.313b - Ceftiofur hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ceftiofur hydrochloride. 522.313b Section 522.313b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS §...

  2. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Etorphine hydrochloride injection. 522.883 Section 522.883 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  3. 21 CFR 522.883 - Etorphine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Etorphine hydrochloride injection. 522.883 Section 522.883 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  4. 21 CFR 522.536 - Detomidine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Detomidine hydrochloride injection. 522.536 Section 522.536 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL...

  5. 40 CFR 180.276 - Formetanate hydrochloride; tolerances for residues.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... for residues. 180.276 Section 180.276 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) PESTICIDE PROGRAMS TOLERANCES AND EXEMPTIONS FOR PESTICIDE CHEMICAL RESIDUES IN FOOD Specific Tolerances § 180.276 Formetanate hydrochloride; tolerances for residues. (a) General. Tolerances...

  6. Cradle-to-gate life cycle inventory of vancomycin hydrochloride.

    PubMed

    Ponder, Celia; Overcash, Michael

    2010-02-15

    A life cycle analysis on the cradle-to-gate production of vancomycin hydrochloride, which begins at natural resource extraction and spans through factory (gate) production, not only shows all inputs, outputs, and energy usage to manufacture the product and all related supply chain chemicals, but can highlight where process changes would have the greatest impact on raw material and energy consumption and emissions. Vancomycin hydrochloride is produced by a low-yield fermentation process that accounts for 47% of the total cradle-to-gate energy. The fermentation step consumes the most raw materials and energy cradle-to-gate. Over 75% of the total cradle-to-gate energy consumption is due to steam use; sterilization within fermentation is the largest user of steam. Aeration and agitation in the fermentation vessels use 65% of the cradle-to-gate electrical energy. To reduce raw materials, energy consumption, and the associated environmental footprint of producing vancomycin hydrochloride, other sterilization methods, fermentation media, nutrient sources, or synthetic manufacture should be investigated. The reported vancomycin hydrochloride life cycle inventory is a part of a larger life cycle study of the environmental consequences of the introduction of biocide-coated medical textiles for the prevention of MRSA (methicillin-resistant Staphylococcus aureus) nosocomial infections.

  7. Guanidine hydrochloride embedded polyurethanes as antimicrobial and absorptive wound dressing membranes with promising cytocompatibility.

    PubMed

    Sahraro, Maryam; Yeganeh, Hamid; Sorayya, Marziyeh

    2016-02-01

    Preparation and assessments of novel absorptive wound dressing materials with efficient antimicrobial activity as well as very good cytocompatibility were described in this work. An amine terminated poly(hexamethylene guanidine hydrochloride) was prepared and used as curing agent of different epoxy-terminated polyurethane prepolymers. The structures of prepared materials were elucidated by evaluation of their (1)H NMR and FTIR spectra. The recorded tensile strength of membranes confirmed the excellent dimensional stability of the film type dressings even at fully hydrated conditions. Therefore, these dressings could protect the wound bed from external forces during the healing period. The structurally optimized dressing membranes could preserve the desired moist environment over the wounded area, as a result of their balanced equilibrium, water absorption and water vapor transmission rate. Therefore, a very good condition for stimulation of self-healing of wound bed was attained. Also, owing to the presence of guanidine hydrochloride moieties embedded into the structure of dressings, efficient antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans were detected. In vitro cytotoxicity assay of the prepared dressings revealed cytocompatibility of these materials against fibroblast cells. Therefore, they could support cell growth and proliferation at the wounded area.

  8. Dexmethylphenidate--Novartis/Celgene. Focalin, D-MPH, D-methylphenidate hydrochloride, D-methylphenidate, dexmethylphenidate, dexmethylphenidate hydrochloride.

    PubMed

    2002-01-01

    Celgene has developed a chirally pure form of methylphenidate (Ritalin), called dexmethylphenidate [d-methylphenidate, d-methylphenidate hydrochloride, d-MPH; Focalin]. The drug has been launched in the USA and is undergoing registration in Canada for the treatment of children with attention-deficit hyperactivity disorder (ADHD). Dexmethylphenidate is the single isomer version of racemic methylphenidate (Ritalin), which contains the active d isomer of Ritalin. Dexmethylphenidate acts via the inhibition of reuptake of norepinephrine and dopamine. Research is ongoing to further clarify the mode of therapeutic action in ADHD. Dexmethylphenidate was developed with the aim of reducing drug load, adverse events and drug interactions. Dexmethylphenidate provides effective management of attention-deficit hyperactivity disorder at half the dose of Ritalin. In April 2000, worldwide rights (excluding Canada) to dexmethylphenidate were granted to Novartis. Celgene has also granted Novartis rights to all related intellectual properties and patents. Novartis will fund all remaining development and marketing expenses required for regulatory approval and commercialisation of dexmethylphenidate. Crystaal Corporation, the marketing division of Biovail Corporation International, has exclusive Canadian marketing rights for all formulations of dexmethylphenidate. Novartis launched dexmethylphenidate (Focalin) in the USA during Q1 2002. It is available as a D-shaped tablet (2.5, 5 and 10 mg doses). Novartis had planned to use the tradename Ritadex, however the FDA recommended an alternative name due to potential prescribing errors with Ritalin. The finalized tradename to be used is Focalin. In July 2001, a new drug submission was filed with Canada's Therapeutic Products Programme for dexmethylphenidate in the treatment of attention-deficit disorder and attention-deficit hyperactivity disorder. Novartis is also developing an extended-release version of chirally pure dexmethylphenidate

  9. Chemical Immobilization of Sloth Bears (Melursus ursinus) with Ketamine Hydrochloride and Xylazine Hydrochloride: Hematology and Serum Biochemical Values.

    PubMed

    Veeraselvam, M; Sridhar, R; Perumal, P; Jayathangaraj, M G

    2014-01-01

    The present study was conducted to define the physiological responses of captive sloth bears immobilized with ketamine hydrochloride and xylazine hydrochloride and to determine and compare the values of hematology and serum biochemical parameters between sexes. A total of 15 sloth bears were immobilized using combination of ketamine hydrochloride and xylazine hydrochloride drugs at the dose rate of 5.0 milligram (mg) per kg body weight and 2.0 mg per kg body weight, respectively. The use of combination of these drugs was found satisfactory for the chemical immobilization of captive sloth bears. There were no significant differences observed in induction time and recovery time and physiological parameters such as heart rate, respiratory rate, and rectal temperature between sexes. Health related parameters comprising hematological values like packed cell volume (PCV), hemoglobin (Hb), red blood cell count (RBC), erythrocyte indices, and so forth and biochemical values like total protein, blood urea nitrogen (BUN), creatinine, alkaline amino-transferase (ALT), aspartate amino-transferase (AST), and so forth were estimated in 11 (5 males and 6 females) apparently healthy bears. Comparison between sexes revealed significant difference in PCV (P < 0.05) and mean corpuscular hemoglobin concentration (MCHC) (P < 0.05). The study might help to evaluate health profiles of sloth bears for appropriate line treatment.

  10. Effects of Duloxetine Treatment on Cognitive Flexibility and BDNF Expression in the mPFC of Adult Male Mice Exposed to Social Stress during Adolescence

    PubMed Central

    Xu, Hang; Zhang, Yu; Zhang, Fan; Yuan, San-na; Shao, Feng; Wang, Weiwen

    2016-01-01

    Early stress is a significant risk factor for the onset of mood disorders such as depression during adulthood. Impairments in cognitive flexibility mediated by prefrontal cortex (PFC) dysfunction are increasingly recognized as important etiological and pathological factors in the development of depression. Our previous study demonstrated that social defeat stress during early adolescence produced delayed deficits in cognitive flexibility in adult mice. The potential molecular mechanisms underlying these long-term consequences remain unclear. One candidate molecule is brain-derived neurotrophic factor (BDNF), which plays a vital role in neural development and synaptic plasticity. In this study, we initially examined the effects of adolescent social stress on cognitive flexibility and PFC BDNF expression within a week after the last stress exposure and 6 weeks later during adulthood. Adolescent (PND 28) male mice were subjected to stress or control manipulation for 10 days. The attentional set-shifting task (AST) was used to assess cognitive flexibility. Levels of BDNF mRNA and protein in the PFC were examined after behavioral testing. The results demonstrated that previously stressed mice exhibited delayed extra-dimensional set-shifting deficits in AST when tested as adults but not when tested as adolescents. Consistent with the cognitive alterations, adolescent stress induced dynamic alterations in BDNF expression in the medial PFC (mPFC), with a transient increase observed shortly after the stress, followed by a decrease 6 weeks later during adulthood. Next, we further determined the effects of chronic treatment with the antidepressant duloxetine during early adulthood on cognitive and molecular alterations induced by adolescent stress. Compared with the controls, duloxetine treatment reversed the cognitive deficits and increased the BDNF protein expression in the mPFC during adulthood in previously stressed mice. These findings demonstrated that BDNF expression

  11. Comparison of the antifungal efficacy of terbinafine hydrochloride and ciclopirox olamine containing formulations against the dermatophyte Trichophyton rubrum in an infected nail plate model.

    PubMed

    Täuber, Anja; Müller-Goymann, Christel C

    2014-07-07

    Onychomycosis is a fungal infection mostly induced by dermatophytes such as Trichophyton rubrum. Due to slow nail growth, the treatment takes 3-9 months depending on the nail size and infected area. Hence, high efficacy of the active ingredient without systemic side effects is of major interest. To test the efficacy of an antifungal formulation, an appropriate in vitro model reflecting the in vivo situation as close as possible is required. In this study, a variety of antifungal formulations, i.e., commercial ones (Ciclopoli and Lamisil cream), those used in compounding pharmacies (Pentravan) as well as poloxamer 407-based systems, have been evaluated in an infected nail plate model. The active pharmaceutical ingredients (APIs) were ciclopirox olamine and terbinafine hydrochloride. The poloxamer 407-based formulations consisted of poloxamer 407, double distilled water, propylene glycol, isopropyl alcohol, medium chain triglycerides and either 1% ciclopirox olamine or 1% terbinafine hydrochloride as API, respectively. Former studies have shown high permeation rates of terbinafine hydrochloride from similar poloxamer 407-based formulations with dimethyl isosorbide instead of propylene glycol. The present contribution shows superior inhibition of T. rubrum growth from poloxamer 407-based formulations in comparison to the commercial Lamisil cream. Moreover, poloxamer 407-based formulations were equally effective as the nail lacquer Ciclopoli even though the poloxamer formulations contained only 1% of the drug instead of 8% in the marketed lacquer. Poloxamer 407-based systems containing ciclopirox olamine proved to be about as effective as similar terbinafine hydrochloride systems.

  12. Differential expression on mitochondrial tryparedoxin peroxidase (mTcTXNPx) in Trypanosoma cruzi after ferrocenyl diamine hydrochlorides treatments.

    PubMed

    Kohatsu, Andréa A N; Silva, Flávia A J; Francisco, Acácio I; Rimoldi, Aline; Silva, Marco T A; Vargas, Maria D; Rosa, João A da; Cicarelli, Regina M B

    Resistance to benznidazole in certain strains of Trypanosoma cruzi may be caused by the increased production of enzymes that act on the oxidative metabolism, such as mitochondrial tryparedoxin peroxidase which catalyses the reduction of peroxides. This work presents cytotoxicity assays performed with ferrocenyl diamine hydrochlorides in six different strains of T. cruzi epimastigote forms (Y, Bolivia, SI1, SI8, QMII, and SIGR3). The last four strains have been recently isolated from triatominae and mammalian host (domestic cat). The expression of mitochondrial tryparedoxin peroxidase was analyzed by the Western blotting technique using polyclonal antibody anti mitochondrial tryparedoxin peroxidase obtained from a rabbit immunized with the mitochondrial tryparedoxin peroxidase recombinant protein. All the tested ferrocenyl diamine hydrochlorides were more cytotoxic than benznidazole. The expression of the 25.5kDa polypeptide of mitochondrial tryparedoxin peroxidase did not increase in strains that were more resistant to the ferrocenyl compounds (SI8 and SIGR3). In addition, a 58kDa polypeptide was also recognized in all strains. Ferrocenyl diamine hydrochlorides showed trypanocidal activity and the expression of 25.5kDa mitochondrial tryparedoxin peroxidase is not necessarily increased in some T. cruzi strains. Most likely, other mechanisms, in addition to the over expression of this antioxidative enzyme, should be involved in the escape of parasites from cytotoxic oxidant agents.

  13. Development and evaluation of a sublingual film of the antiemetic granisetron hydrochloride.

    PubMed

    Kalia, Vani; Garg, Tarun; Rath, Gautam; Goyal, Amit Kumar

    2016-05-01

    The objective of this study was to develop an oral transmucosal formulation of an antiemetic drug that can not only serve in the active form but also provide a controlled release profile. In this study, sublingual films based on the biodegradable and water-soluble polymers, that is HPMCK-4M and PVPK-30, were developed by the solvent casting method, and were loaded with the antiemetic drug granisetron hydrochloride (granisetron HCl). The entrapment efficiency of the developed formulation was found to be 86%. The in vitro profile showed an instant release of the drug from the sublingual film, in a pattern following the first order kinetics array. The in vivo studies showed that granisetron HCl was delivered in its active state and showed effective results, as compared to its activity in the marketed formulation.

  14. Buffered nanoemulsion for nose to brain delivery of ziprasidone hydrochloride: preformulation and pharmacodynamic evaluation.

    PubMed

    Bahadur, Shiv; Pathak, Kamla

    2012-11-01

    The study was undertaken to develop buffered nanoemulsion of ziprasidone hydrochloride (fifth generation antipshychotic) and evaluate its potential for efficacious nose to brain delivery drug delivery in animal models. Homogeneous buffered ziprasidone nanoemulsions (BZNE) were prepared by aqueous (phosphate buffer, pH 8.0) titration method using capmul MCM, labrasol and transcutol as oil, surfactant and cosurfactant respectively. The NEs (F1-F7) were characterized for pharmaceutical characteristics (% transmittance, PDI value, Zeta potential, globule size, viscosity and diffusion coefficient) and F6 with mean globule size of 145.24 ± 4.75nm (PDI = 0.186 ± 0.40) and diffusion coefficient of 0.1901± 0.04cm2/min was thermodynamically stable and was developed as buffered mucoadhesive nanoemulsions. The buffered mucoadhesive NE (βmax = 0.57) that contained 0.5% by weight of chitosan (BZMNE) exhibited 1.79 times higher diffusion coefficient (0.3418 ± 0.03) than BZNE. Pharmacodynamic study confirmed the superiority of BZMNE over BZNE in locomotor activity test (p < 0.05) and paw test (p < 0.05). Nasal ciliotoxicity study revealed the optimized BZMNE to be free from acute toxicity. Conclusively, a stable and efficacious buffered mucoadhesive NE of ziprasidone hydrochloride, that can be safely administered by intranasal route was developed.

  15. Characterization of nicardipine hydrochloride-induced cell injury in human vascular endothelial cells.

    PubMed

    Ochi, Masanori; Kawai, Yoshiko; Tanaka, Yoshiyuki; Toyoda, Hiromu

    2015-02-01

    Nicardipine hydrochloride (NIC), a dihydropyridine calcium-channel blocking agent, has been widely used for the treatment of hypertension. Especially, nicardipine hydrochloride injection is used as first-line therapy for emergency treatment of abnormally high blood pressure. Although NIC has an attractive pharmacological profile, one of the dose-limiting factors of NIC is severe peripheral vascular injury after intravenous injection. The goal of this study was to better understand and thereby reduce NIC-mediated vascular injury. Here, we investigated the mechanism of NIC-induced vascular injury using human dermal microvascular endothelial cells (HMVECs). NIC decreased cell viability and increased percent of dead cells in a dose-dependent manner (10-30 μg/mL). Although cell membrane injury was not significant over 9 hr exposure, significant changes of cell morphology and increases in vacuoles in HMVECs were observed within 30 min of NIC exposure (30 μg/mL). Autophagosome labeling with monodansylcadaverine revealed increased autophagosomes in the NIC-treated cells, whereas caspase 3/7 activity was not increased in the NIC-treated cells (30 μg/mL). Additionally, NIC-induced reduction of cell viability was inhibited by 3-methyladenine, an inhibitor of autophagosome formation. These findings suggest that NIC causes severe peripheral venous irritation via induction of autophagic cell death and that inhibition of autophagy could contribute to the reduction of NIC-induced vascular injury.

  16. Formulation and evaluation of sustained release floating capsules of nicardipine hydrochloride.

    PubMed

    Moursy, N M; Afifi, N N; Ghorab, D M; El-Saharty, Y

    2003-01-01

    Nicardipine hydrochloride, a calcium channel blocker with significant vasodilating and antihypertensive activities, was formulated in this work as sustained release floating capsules. A hydrocolloid of high viscosity grade was used for the floating systems. The inclusion of sodium bicarbonate to allow evolution of CO2 to aid buoyancy was studied. Polymers that retard drug release were included as coprecipitates with the drug and/or as additives in the formulated capsules. Both simple powder mixing of the ingredients and granule preparation via wet granulation were used. Seven capsule formulae were prepared. The prepared capsules were evaluated in vitro by testing drug dissolution, floating time and the kinetics of drug release. In vitro evaluation of a commercially available conventional 20 mg capsule of nicardipine hydrochloride, "Micard", was carried out for comparison. The hydrocolloid used succeeded in effecting capsule buoyancy. Floating time increased with increasing the proportion of the hydrocolloid. Inclusion of sodium bicarbonate increased buoyancy. All of the seven floating capsule formulae prepared proved efficient in controlling drug release. The sustained release floating capsule formulation of choice was evaluated in vivo in comparison to "Micard" capsules using rabbits. Reversed phase HPLC with UV detection was used for drug determination in rabbit plasma. Plasma concentration time curves revealed a longer drug duration for administration in the sustained release formula than the conventional "Micard" capsule being 16 h in the former versus 8 h for the latter.

  17. Effect of yohimbine hydrochloride on erectile impotence: a double-blind study.

    PubMed

    Susset, J G; Tessier, C D; Wincze, J; Bansal, S; Malhotra, C; Schwacha, M G

    1989-06-01

    A double-blind, partial crossover study on the therapeutic effect of yohimbine hydrochloride on erectile dysfunction was done in 82 sexually impotent patients. All patients underwent a multifactorial evaluation, including determination of penile brachial blood pressure index, cavernosography, sacral evoked response, testosterone and prolactin determination, Derogatis sexual dysfunction inventory and daytime arousal test. After 1 month of treatment with a maximum of 42.0 mg. oral yohimbine hydrochloride daily 14 per cent of the patients experienced restoration of full and sustained erections, 20 per cent reported a partial response to the therapy and 65 per cent reported no improvement. Three patients reported a positive placebo effect. Maximum effect takes 2 to 3 weeks to manifest itself. Yohimbine was active in some patients with arterial insufficiency and a unilateral sacral reflex arc lesion, and in 1 with low serum testosterone levels. The 34 per cent response is encouraging, particularly in a Veterans Administration population presenting with a high incidence of diabetes and vascular pathological conditions not found in regular office patients. Only few and benign side effects were recorded, which makes this medication worth an attempt, often as a first line of treatment even at a dose of 8 tablets.

  18. Management of hepatic cysts by percutaneous drainage and instillation of tetracycline hydrochloride.

    PubMed

    McFarlane, M E; Venugopal, R; McDonald, A; Ewing, R; Newnham, M S; Johnson, L

    2001-09-01

    This paper reports two cases of benign hepatic cysts successfully treated by the instillation of tetracycline hydrochloride. The patients presented with solitary large symptomatic hepatic cysts and underwent ultrasound guided needle aspiration followed by the instillation of tetracycline hydrochloride. The cyst size diminished without complication and the patients have remained symptom free. We review the treatment of this uncommon entity and propose that injection of tetracycline hydrochloride is an effective nonoperative treatment of symptomatic solitary hepatic cysts.

  19. Olopatadine hydrochloride inhibits capsaicin-induced flare response in humans.

    PubMed

    Shindo, Masahisa; Yoshida, Yuichi; Yamamoto, Osamu

    2011-01-01

    Capsaicin, a vanilloid, has the potential for releasing substance P (SP) from sensory nerves. Topical application of capsaicin induces a flare response in the skin. However, it has not been clarified whether the release of SP is involved in the process of flare response or not. A potent antihistamine drug, olopatadine hydrochloride, is known to have inhibitory action against the release of SP. We examined the effects of olopatadine (at a dose of 5 mg) on skin reaction induced by topical application of capsaicin in 10 healthy subjects. The scores of capsaicin-induced flare responses after olopatadine administration were significantly lower at 30 min than at baseline. Our findings suggest that olopatadine hydrochloride could inhibit capsaicin-induced flare responses.

  20. Asymmetric Synthesis of (+)-anti- and (-)-syn-Mefloquine Hydrochloride.

    PubMed

    Rastelli, Ettore J; Coltart, Don M

    2016-10-21

    The asymmetric (er > 99:1) total synthesis of (+)-anti- and (-)-syn-mefloquine hydrochloride from a common intermediate is described. The Sharpless asymmetric dihydroxylation is the key asymmetric transformation used in the synthesis of this intermediate. It is carried out on an olefin that is accessed in three steps from commercially available materials, making the overall synthetic sequence very concise. The common diol intermediate derived from the Sharpless asymmetric dihydroxylation is converted into either a trans- or cis-epoxide, and these are subsequently converted to (+)-anti- and (-)-syn-mefloquine, respectively. X-ray crystallographic analysis of derivatives of (+)-anti- and (-)-syn-mefloquine is used to lay to rest a 40 year argument regarding the absolute stereochemistry of the mefloquines. A formal asymmetric (er > 99:1) synthesis of (+)-anti-mefloquine hydrochloride is also presented that uses a Sharpless asymmetric epoxidation as a key step.

  1. Effect of topical application of phenylephrine hydrochloride on hyperplastic gingivitis.

    PubMed

    Pernsteiner, C L; Ash, M M

    1977-08-01

    A double blind study was conducted to evaluate the effectiveness of Phenodent Type A (brand of phenylephrine hydrochloride) on decongesting hyperplastic gingivitis. Three solutions were used: a 0.5% a placebo, and a 0.25% concentration of phenylephrine hydrochloride. The periodontal disease index was used to score variables which might have an effect on gingival response to local irritants. Impressions were taken and casts were made on 45 subjects at 0, 1, 3, and 6-week intervals. An instrument with accuracy of 0.001 inch was constructed to measure the changes in the interdental papillae of the stone casts. No significant reduction of gingival volume was established for any of the three solutions.

  2. Acute renal injury induced by valacyclovir hydrochloride: A case report

    PubMed Central

    Zhang, Yanning; Cong, Yuxi; Teng, Yan

    2016-01-01

    Acyclovir has been a frequently used antiviral agent in the clinical treatment of leukemia, acute encephalitis, malignant tumor and herpes simplex. The adverse effects of this drug have been widely described in clinical practice. In the present study, a case of a 35-year-old female patient diagnosed with herpes simplex, who developed acute renal injury following treatment with valacyclovir hydrochloride, is described. Kidney biopsy, light microscopy and laboratory examination were performed, and all findings revealed the signs of evident vacuolar degeneration of capillary endothelial and renal tubular epithelial cells, erythrocyte aggregation in partial renal tubule and microvilli exfoliation from epithelial cells. Renal interstitial edema was clearly identified. The clinical evidence observed from this female patient indicated that renal functions should be closely monitored during valacyclovir hydrochloride administration. A variety of effective measures, such as hydration, alkalizing urine, promoting the discharge of medication and the use of antagonists are recommended following the administration of antiviral agents. PMID:28101180

  3. Evaluation of sedative effects of single and repeated doses of 50 mg and 150 mg tolperisone hydrochloride. Results of a prospective, randomized, double-blind, placebo-controlled trial.

    PubMed

    Dulin, J; Kovács, L; Ramm, S; Horvath, F; Ebeling, L; Kohnen, R

    1998-07-01

    Sedative effects of single and repeated doses of 50 mg and 150 mg tolperisone hydrochloride (Mydocalm), a centrally active muscle-relaxing agent, were evaluated in a placebo-controlled double-blind clinical trial. A total of 72 healthy young adults balanced by sex were randomized to receive 50 mg or 150 mg tolperisone hydrochloride or placebo t.i.d. for a period of 8 days. Control examinations were performed in the mornings of days 1 and 8 before intake of the morning dose and at 1.5, 4 and 6 hours postdose. The psychomotoric test battery used in this trial revealed no sedative effects of tolperisone hydrochloride in the given doses at any control examination. Subjective mood ratings quantified by the Welzel Colored Scales were not impaired either. The lack of differences in sedative potentials of tolperisone hydrochloride and placebo was confirmed by tests on differences and by tests on equivalence using 95% CI. The present study substantiates clinical experience and previous clinical trials demonstrating that tolperisone hydrochloride, though being a centrally active muscle relaxant, does not cause any sedation and does not impair reaction times.

  4. Review of moxifloxacin hydrochloride ophthalmic solution in the treatment of bacterial eye infections

    PubMed Central

    Miller, Darlene

    2008-01-01

    Moxifloxacin hydrochloride ophthalmic solution 0.5% (Vigamox®) is the ocular formulation/adaptation of moxifloxacin. Moxifloxacin is a broad spectrum 8-methoxyfluoroquinolone which terminates bacterial growth by binding to DNA gyrase (topoisomerase II) and topoisomerase IV, essential bacterial enzymes involved in the replication, translation, repair and recombination of deoxyribonucleic acid. Affinity for both enzymes improves potency and reduces the probability of selecting resistant bacterial subpopulations. Vigamox is a bactericidal, concentration dependent, anti-infective. It is preservative free, and well tolerated with minimal ocular side effects. It provides increased penetration into ocular tissues and fluids with improved activity against Streptococci and Staphylococci species and moderate to excellent activity against clinically relevant, gram-negative ocular pathogens. PMID:19668391

  5. Reduced cytotoxicity of polyhexamethylene biguanide hydrochloride (PHMB) by egg phosphatidylcholine while maintaining antimicrobial efficacy.

    PubMed

    Müller, Gerald; Kramer, Axel; Schmitt, Jürgen; Harden, Daniela; Koburger, Torsten

    2011-04-25

    Liposomes or oil-in-water emulsions containing egg yolk phosphatidylcholine (EPC) were combined with aqueous polyhexamethylene biguanide hydrochloride (PHMB). The bactericidal activity of these preparations against Pseudomonas aeruginosa and Staphylococcus aureus as well as their cytotoxicity on cultured murine fibroblasts (L929 cells) was then assayed for either 30 min or 60 min in the presence of cell culture medium containing 10% fetal bovine serum as surrogate for wound fluid. We used two assay designs: in the first bactericidal activity and cytotoxicity were determined in separate experiments; in the second both were determined in one experiment. Combining PHMB and EPC containing o/w emulsions or liposomes protects mammalian cells without neutralizing the antiseptic effect. From all tested combinations the o/w emulsions containing 0.05% PHMB proved to be superior in this respect to the aqueous preparation.

  6. Anamorelin hydrochloride in the treatment of cancer anorexia-cachexia syndrome.

    PubMed

    Currow, David C; Abernethy, Amy P

    2014-04-01

    Anamorelin hydrochloride is an orally active ghrelin receptor agonist in development by Helsinn, for the treatment of non-small-cell lung cancer (NSCLC) cachexia. In preclinical and clinical studies, the potent affinity of anamorelin for the ghrelin receptor is associated with significant appetite-enhancing activity and resultant improvements in body weight, lean body mass, and handgrip strength compared with placebo. The accompanying stimulatory effects on growth hormone and IGF-1 are not associated with tumor growth, and overall survival in patients with cancer is not compromised. Anamorelin is well tolerated with no dose-limiting toxicities identified to date. The findings of ongoing Phase III studies are needed to confirm the significant potential of anamorelin to treat NSCLC cachexia.

  7. Control of recurrent supraventricular tachycardia with amiodarone hydrochloride.

    PubMed Central

    Swan, J. H.; Chisholm, A. W.

    1976-01-01

    Amiodarone hydrochloride, a new antiarrhythmic agent, controlled a recurrent supraventricular arrhythmia, refractory to conventional medical treatment, in a 57-year-old patient with an anomalous conduction system and idiopathic cardiomyopathy. For the 11 months that the patient has been taking the drug her arrhythmia has not recurred. This drug has produced no important side effects in this patient. Images FIG. 1 FIG. 2 PMID:943223

  8. [Antidepressant properties of beta-phenylglutamic acid hydrochloride (RGPU-135, glutarone) in comparison to imipramine, tianeptine, and fluoxetine].

    PubMed

    Bagmetova, V V; Chernysheva, Iu V; Merkushenkova, O V; Berestovitskaia, V M; Tiurenkov, I N

    2013-01-01

    The new glutamic acid derivative--beta-phenylglutamic acid hydrochloride (RGPU-135, glutarone) (in a dose of 26 mg/kg), imipramine (15 mg/kg), tianeptine (2.5 mg/kg) and fluoxetine (20 mg/kg), show antidepressant action in the tail suspension test and Porsolt swim test. All these drugs cause reduction in the intensity of depressive behavior and lead to increase in the rate of active behavior of avoidance of aversive situation with animals. The RGPU-135 compound shows antidepressant activity equal to that of imipramine, which is statistically significantly more pronounced than that of fluoxetine and tianeptine.

  9. Use of xylazine hydrochloride-ketamine hydrochloride for immobilization of wild leopards (Panthera pardus fusca) in emergency situations.

    PubMed

    Belsare, Aniruddha V; Athreya, Vidya R

    2010-06-01

    In India, leopards (Panthera pardus fusca) inhabit human-dominated landscapes, resulting in encounters that require interventions to prevent harm to people, as well as the leopards. Immobilization is a prerequisite for any such intervention. Such emergency field immobilizations have to be carried out with limited tools, often amidst large uncontrollable crowds. An effective and practicable approach is discussed, based on 55 wild leopard immobilizations undertaken between January 2003 and April 2008. A xylazine hydrochloride (1.4 +/- 0.3 mg/kg)--ketamine hydrochloride (5 +/- 2 mg/kg) mixture was used for immobilization of leopards, based on estimated body weight. When weight could not be estimated, a standard initial dose of 50 mg of xylazine--150 mg of ketamine was used. Supplemental doses (50-75 mg) of only ketamine were used as required. No life-threatening adverse effects of immobilization were documented for at least 1 mo postimmobilization.

  10. Development and Validation of a Rapid RP-UPLC Method for the Simultaneous Estimation of Bambuterol Hydrochloride and Montelukast Sodium from Tablets

    PubMed Central

    Yanamandra, R.; Vadla, C. S.; Puppala, U. M.; Patro, B.; Murthy, Y. L. N.; Parimi, A. R.

    2012-01-01

    A rapid, simple, sensitive and selective analytical method was developed by using reverse phase ultra performance liquid chromatographic technique for the simultaneous estimation of bambuterol hydrochloride and montelukast sodium in combined tablet dosage form. The developed method is superior in technology to conventional high performance liquid chromatography with respect to speed, resolution, solvent consumption, time, and cost of analysis. Elution time for the separation was 6 min and ultra violet detection was carried out at 210 nm. Efficient separation was achieved on BEH C18 sub-2-μm Acquity UPLC column using 0.025% (v/v) trifluoro acetic acid in water and acetonitrile as organic solvent in a linear gradient program. Resolutions between bambuterol hydrochloride and montelukast sodium were found to be more than 31. The active pharmaceutical ingredient was extracted from tablet dosage from using a mixture of methanol, acetonitrile and water as diluent. The calibration graphs were linear for bambuterol hydrochloride and montelukast sodium in the range of 6.25-37.5 μg/ml. The percentage recoveries for bambuterol hydrochloride and montelukast sodium were found to be in the range of 99.1-100.0% and 98.0-101.6%, respectively. The test solution was found to be stable for 7 days when stored in the refrigerator between 2-8°. Developed UPLC method was validated as per International Conference on Harmonization specifications for method validation. This method can be successfully employed for simultaneous estimation of bambuterol hydrochloride and montelukast sodium in bulk drugs and formulations. PMID:23325991

  11. Minocycline hydrochloride nanoliposomes inhibit the production of TNF-α in LPS-stimulated macrophages

    PubMed Central

    Liu, D; Yang, P S

    2012-01-01

    Background As an adjunctive treatment of chronic periodontitis, it seems that the application of periocline or the other antimicrobials is effective against periodontopathogens. In this study, nanoliposomes were investigated as carriers of minocycline hydrochloride and the inhibition effects of minocycline hydrochloride nanoliposomes on the proliferation and lipopolysaccharide (LPS)-stimulated production of tumor necrosis factor-α (TNF-α) of macrophages were elucidated. Methods After stimulation with 10 μg/mL LPS, murine macrophages (ANA-1) were treated with 10, 20, 40, 50 and 70 μg/mL 2% minocycline hydrochloride nanoliposomes, minocycline hydrochloride solution, and periocline for 6, 12, 24, 48 and 60 hours, respectively. A tetrazolium (MTT) assay was used to evaluate macrophages cell proliferation rate and the levels of TNF-α mRNA were measured by SYBR Green Real Time PCR. Results Ten to 70 μg/mL 2% minocycline hydrochloride nanoliposomes, minocycline hydrochloride solution, and periocline showed dose- and time-dependent inhibition of ANA-1 proliferation. Minocycline hydrochloride nanoliposomes showed dose- and ratio-dependent inhibition of LPS-stimulated TNF-α secretion of ANA-1. The inhibition effect of 10 μg/mL minocycline hydrochloride nanoliposomes was significantly better than that of two positive control groups, and equated to that of 60 or 70 μg/mL periocline. The expression of TNF-α mRNA in experimental group continued to reduce linearly with time. Conclusion All three preparations of minocycline hydrochloride showed dose- and time-dependent inhibition of proliferation of ANA-1. Minocycline hydrochloride nanoliposomes have stronger and longer inhibition effect on LPS-stimulated TNF-α secretion of macrophages cell than minocycline hydrochloride solution and periocline. PMID:22973098

  12. High-performance liquid chromatographic determination of memantine hydrochloride in rat plasma using sensitive fluorometric derivatization.

    PubMed

    Xie, Mei-Fen; Zhou, Wei; Tong, Xin-Yi; Chen, Yi-Le; Cai, Yi; Li, Yan; Duan, Geng-Li

    2011-02-01

    In this study, we investigated a simple, sensitive and reliable liquid chromatography-fluorescence detection method for the determination of memantine hydrochloride in rat plasma which was based on derivatization with 9-fluorenylmethyl chloroformate (FMOC-Cl). For the first time, FMOC-Cl was introduced into derivatization of memantine hydrochloride in rat plasma. The amino groups of memantine hydrochloride and amantadine hydrochloride (internal standard) were trapped with FMOC-Cl to form memantine hydrochloride-FMOC-Cl and amantadine hydrochloride-FMOC-Cl compositions, which can be very compatible for LC-FLD. Precipitation of plasma proteins by acetonitrile was followed by vortex mixing and centrifugation. Chromatographic separation was performed on a C(18) column (DIAMONSIL 150 × 4.6 mm, id 5 μm) with a mobile phase consisting of acetonitrile and water at a flow rate of 1.0 mL/min. The retention times of memantine hydrochloride-FMOC-Cl and amantadine hydrochloride-FMOC-Cl compositions were 23.69 and 40.27 min, respectively. Optimal conditions for the derivatization of memantine hydrochloride were also described. The limit of quantification (LOQ) was 25 ng/mL for memantine hydrochloride in plasma, the linear range was 0.025-5.0 μg/mL in plasma with a correlation coefficient (r) of 0.9999. The relative standard deviations (RSDs) of intra-day and inter-day assays were 4.46-12.19 and 5.23-11.50%, respectively. The validated method was successfully applied to the determination of memantine hydrochloride in rat plasma samples.

  13. Anomalous Electrical Conductivity Behavior at Elevated Pressure in the Protic Ionic Liquid Procainamide Hydrochloride

    NASA Astrophysics Data System (ADS)

    Wojnarowska, Z.; Roland, C. M.; Swiety-Pospiech, A.; Grzybowska, K.; Paluch, M.

    2012-01-01

    Using broadband dielectric spectroscopy, we investigated the effect of hydrostatic pressure on the conductivity relaxation time τσ of the supercooled protic ionic liquid, procainamide hydrochloride, a common pharmaceutical. The pressure dependence of τσ exhibited anomalous behavior in the vicinity of the glass transition Tg, manifested by abrupt changes in activation volume. This peculiar behavior, paralleling the change in temperature dependence of τσ near Tg, is a manifestation of the decoupling between electrical conductivity and structural relaxation. Although the latter effectively ceases in the glassy state, free ions retain their mobility but with a reduced sensitivity to thermodynamic changes. This is the first observation of decoupling of ion migration from structural relaxation in a glassy conductor by isothermal densification.

  14. A forskolin derivative, colforsin daropate hydrochloride, inhibits rat mesangial cell mitogenesis via the cyclic AMP pathway.

    PubMed

    Ogata, Junichi; Minami, Kouichiro; Segawa, Kayoko; Yamamoto, Chieko; Kim, Sung-Teh; Shigematsu, Akio

    2003-11-01

    A forskolin derivative, colforsin daropate hydrochloride (CDH), has been introduced as an inotropic agent that acts directly on adenylate cyclase to increase intracellular cyclic AMP (cAMP) levels and ventricular contractility, resulting in positive inotropic activity. We investigated the effects of CDH on rat mesangial cell (MC) proliferation. CDH (10(-7)-10(-5) mol/l) inhibited [(3)H]thymidine incorporation into cultured rat MCs in a concentration-dependent manner. CDH (10(-7)-10(-5) mol/l) also decreased cell numbers in a similar manner, and stimulated cAMP accumulation in MCs in a concentration-dependent manner. A protein kinase A inhibitor, H-89, abolished the inhibitory effects of CDH on MC mitogenesis. These findings suggest that CDH would inhibit the proliferation of rat MCs via the cAMP pathway.

  15. Terahertz spectroscopic investigation of S-(+)-ketamine hydrochloride and vibrational assignment by density functional theory.

    PubMed

    Hakey, Patrick M; Allis, Damian G; Hudson, Matthew R; Ouellette, Wayne; Korter, Timothy M

    2010-04-01

    The terahertz (THz) spectrum of (S)-(+)-ketamine hydrochloride has been investigated from 10 to 100 cm(-1) (0.3-3.0 THz) at both liquid-nitrogen (78 K) and room (294 K) temperatures. Complete solid-state density functional theory structural analyses and normal-mode analyses are performed using a single hybrid density functional (B3LYP) and three generalized gradient approximation density functionals (BLYP, PBE, PW91). An assignment of the eight features present in the well-resolved cryogenic spectrum is provided based upon solid-state predictions at a PW91/6-31G(d,p) level of theory. The simulations predict that a total of 13 infrared-active vibrational modes contribute to the THz spectrum with 26.4% of the spectral intensity originating from external lattice vibrations.

  16. 21 CFR 524.1484b - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium...

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ..., tetracaine hydrochloride, and myristyl-gamma-picolinium chloride, topical powder. 524.1484b Section 524.1484b... Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium chloride... hydrochloride and .2 milligram of myristyl-gamma-picolinium chloride in each gram of the product in a...

  17. 21 CFR 524.1484b - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium...

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ..., tetracaine hydrochloride, and myristyl-gamma-picolinium chloride, topical powder. 524.1484b Section 524.1484b... Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium chloride... hydrochloride and .2 milligram of myristyl-gamma-picolinium chloride in each gram of the product in a...

  18. 21 CFR 524.1484b - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium...

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ..., tetracaine hydrochloride, and myristyl-gamma-picolinium chloride, topical powder. 524.1484b Section 524.1484b... Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium chloride... hydrochloride and .2 milligram of myristyl-gamma-picolinium chloride in each gram of the product in a...

  19. 21 CFR 524.1484b - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium...

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ..., tetracaine hydrochloride, and myristyl-gamma-picolinium chloride, topical powder. 524.1484b Section 524.1484b... Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride, and myristyl-gamma-picolinium chloride... hydrochloride and .2 milligram of myristyl-gamma-picolinium chloride in each gram of the product in a...

  20. 78 FR 27971 - Determination That REV-EYES (Dapiprazole Hydrochloride Ophthalmic Solution), 0.5%, Was Not...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-05-13

    ... HUMAN SERVICES Food and Drug Administration Determination That REV-EYES (Dapiprazole Hydrochloride... determined that REV-EYES (dapiprazole hydrochloride ophthalmic solution), 0.5%, was not withdrawn from sale... refer to a listed drug. REV-EYES (dapiprazole hydrochloride ophthalmic solution), 0.5%, is the...

  1. Effects of metomindate hydrochloride and tricaine methanesulfonate on the short term cortisol response in channel catfish

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The effects of metomidate hydrochloride and tricaine methanesulfonate (MS-222) on cortisol stress response of channel catfish, Ictalurus punctatus, were examined during 10 minutes of sedation. Channel catfish were assigned to three treatments: 1. Metomidate hydrochloride (12.5 mg/L), 2. MS-222 (100...

  2. 21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Lincomycin hydrochloride monohydrate oral dosage... HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1263 Lincomycin hydrochloride monohydrate oral dosage forms....

  3. 77 FR 20987 - Oral Dosage Form New Animal Drugs; Change of Sponsor; Lincomycin Hydrochloride Soluble Powder...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-04-09

    ... Sponsor; Lincomycin Hydrochloride Soluble Powder; Penicillin G Potassium in Drinking Water; Tetracycline...; penicillin G potassium, USP; and tetracycline hydrochloride soluble powders administered in drinking water... ANADA 200-347 for Penicillin G Potassium, USP, all soluble powders administered in drinking water to...

  4. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Lincomycin hydrochloride monohydrate tablets and... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The sirup...) Sponsor. See No. 000009 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The drug is...

  5. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Lincomycin hydrochloride monohydrate tablets and... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The sirup...) Sponsor. See No. 000009 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The drug is...

  6. 40 CFR 180.502 - Aminoethoxyvinylglycine hydrochloride (aviglycine HCl); tolerances for residues.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... FOOD Specific Tolerances § 180.502 Aminoethoxyvinylglycine hydrochloride (aviglycine HCl); tolerances... hydrochloride (aviglycine HCl) in or on the following food commodities: Commodity Parts per million Apple 0.08 Fruit, stone, group 12, except cherry 0.170 Pear 0.08 (b) Section 18 emergency exemptions....

  7. 40 CFR 180.502 - Aminoethoxyvinylglycine hydrochloride (aviglycine HCl); tolerances for residues.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... (aviglycine HCl); tolerances for residues. 180.502 Section 180.502 Protection of Environment ENVIRONMENTAL... FOOD Specific Tolerances § 180.502 Aminoethoxyvinylglycine hydrochloride (aviglycine HCl); tolerances... hydrochloride (aviglycine HCl) in or on the following food commodities: Commodity Parts per million Apple...

  8. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ..., tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of neomycin... a lesser degree, chronic otitis externa in dogs and cats. In treatment of ear canker and...

  9. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ..., tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of neomycin... a lesser degree, chronic otitis externa in dogs and cats. In treatment of ear canker and...

  10. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ..., tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of neomycin... a lesser degree, chronic otitis externa in dogs and cats. In treatment of ear canker and...

  11. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Oxytetracycline hydrochloride implantation or injectable dosage forms. 522.1662 Section 522.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  12. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Oxytetracycline hydrochloride implantation or injectable dosage forms. 522.1662 Section 522.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  13. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Oxytetracycline hydrochloride implantation or injectable dosage forms. 522.1662 Section 522.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  14. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride implantation or injectable dosage forms. 522.1662 Section 522.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  15. 21 CFR 522.1662 - Oxytetracycline hydrochloride implantation or injectable dosage forms.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Oxytetracycline hydrochloride implantation or injectable dosage forms. 522.1662 Section 522.1662 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1662 Oxytetracycline hydrochloride implantation or...

  16. 75 FR 81617 - Determination That TRANDATE (Labetalol Hydrochloride) Tablets, 300 Milligrams and 400 Milligrams...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-12-28

    ... Administration (FDA) has determined that TRANDATE (labetalol hydrochloride) tablets, 300 milligrams (mg) and 400 mg, were not withdrawn from sale for reasons of safety or effectiveness. This determination means... hydrochloride) tablets, 300 mg and 400 mg, are the subject of NDA 18-716, held by Prometheus Laboratories,...

  17. Neuroprotection against vascular dementia after acupuncture combined with donepezil hydrochloride: P300 event related potential

    PubMed Central

    Liu, Qiang; Wang, Xiu-juan; Zhang, Zhe-cheng; Xue, Rong; Li, Ping; Li, Bo

    2016-01-01

    Acupuncture can be used to treat various nervous system diseases. Here, 168 vascular dementia patients were orally administered donepezil hydrochloride alone (5 mg/day, once a day for 56 days), or combined with acupuncture at Shenting (DU24), Tianzhu (BL10), Sishencong (Extra), Yintang (Extra), Renzhong (DU26), Neiguan (PC6), Shenmen (HT7), Fengchi (GB20), Wangu (GB12) and Baihui (DU20) (once a day for 56 days). Compared with donepezil hydrochloride alone, P300 event related potential latency was shorter with an increased amplitude in patients treated with donepezil hydrochloride and acupuncture. Mini-Mental State Examination score was also higher. Moreover, these differences in P300 latency were identified within different infarcted regions in patients treated with donepezil hydrochloride and acupuncture. These findings indicate that acupuncture combined with donepezil hydrochloride noticeably improves cognitive function in patients with vascular dementia, and exerts neuroprotective effects against vascular dementia. PMID:27127486

  18. Chitosan coated vancomycin hydrochloride liposomes: Characterizations and evaluation.

    PubMed

    Yang, Zhenlei; Liu, Junli; Gao, Jinhua; Chen, Shilei; Huang, Guihua

    2015-11-10

    The present work evaluated the feasibility of chitosan coated liposomes (c-Lips) for the intravenous delivery of vancomycin hydrochloride (VANH), a water-soluble antibiotic for the treatment of gram-positive bacterial infections like osteomyelitis, arthritis, endocarditis, pneumonia, etc. The objective of this research was to develop a suitable drug delivery system in vivo which could improve therapeutic efficacy and decrease side effects especially nephrotoxicity. Firstly, the vancomycin hydrochloride liposomes (VANH-Lips) were prepared by modified reverse phase evaporation method, then the chitosan wrapped vancomycin hydrochloride liposomes (c-VANH-Lips) nanosuspension was formulated by the method of electrostatic deposition. Based on the optimized results of single-factor screening experiment, the c-VANH-Lips were found to be relatively uniform in size (220.40 ± 3.56 nm) with a narrow polydispersity index (PI) (0.21 ± 0.03) and a positive zeta potential (25.7 ± 1.12 mV). The average drug entrapment efficiency (EE) and drug loading (DL) were 32.65 ± 0.59% and 2.18 ± 0.04%, respectively. The in vitro release profile of c-VANH-Lips possessed a sustained release Characterization and the release behavior was in accordance with the Weibull equation. Hemolysis experiments showed that its intravenous injection had preliminary safety. In vivo, after intravenous injection to mice, c-VANH-Lips showed a longer retention time and higher AUC values compared with the VANH injection (VANH-Inj) and VANH-Lips. In addition, biodistribution results clearly demonstrated that c-VANH-Lips preferentially decreased the drug distribution in kidney of mice after intravenous injection. These results revealed that injectable c-VANH-Lips may serve as a promising carrier for VANH to increase therapeutic efficacy on gram-positive bacterial infections and reduce nephrotoxicity, which provides significantly clinical value for long-term use of VANH.

  19. Sustained release of verapamil hydrochloride from sodium alginate microcapsules.

    PubMed

    Farhana, S Ayesha; Shantakumar, S M; Shyale, Somashekar; Shalam, Md; Narasu, Laxmi

    2010-04-01

    The objective of the present study was to develop sustained release microcapsules of verapamil hydrochloride (VH) using biodegradable polymers. For this purpose microcapsules embedded verapamil hydrochloride were prepared using sodium alginate alone and also by incorporating some co polymers like methyl cellulose (MC), sodium carboxy methyl cellulose (SCMC) , poly vinyl pyrollidone (PVP) and xanthan gum by employing complex emulsion method of microencapsulation. Microcapsules were prepared in various core: coat ratios to know the effect of polymer and co polymers on drug release. Overall ten formulations were prepared and evaluated for flow behaviour, sieve analysis, drug entrapment efficiency, in vitro dissolution studies, stability studies, including scanning electron microscopy and DSC. The resulting microcapsules were discrete, large, spherical and also free flowing. The drug content in all the batches of microcapsules was found to be uniform. The release was depended on core: coat ratio and nature of the polymers. FTIR analysis revealed chemical integrity between Verapamil hydrochloride (VH), sodium alginate and between the copolymers. Among the four copolymers used methyl cellulose retarded the drug release more than the other three, hence the same formulation was subjected for in vivo studies. The drug release from the microcapsules was found to be following non fickian diffusion. Mechanism of drug release was diffusion controlled first order kinetics. Drug diffusion co efficient and correlation co efficient were also assessed by using various mathematical models. In vivo result analysis of pharmacokinetic parameters revealed that t max of reference and test formulations were almost same. From the study it was concluded that, sustained release Verapamil hydro chloride microcapsules could be achieved with success using sodium alginate alone and also in combination with other biodegradable polymers.

  20. EVALUATION OF THE THERAPEUTIC EFFICACY OF LEVAMISOLE HYDROCHLORIDE ON THIRD-STAGE LARVAE OF Lagochilascaris minor IN EXPERIMENTALLY INFECTED MICE

    PubMed Central

    CAMPOS, Dulcinéa Maria Barbosa; BARBOSA, Alverne Passos; OLIVEIRA, Jayrson Araújo; BARBOSA, Carlos Augusto Lopes; LOBO, Tamara Flavia Correa; SILVA, Luana Gabriella; THOMAZ, Douglas Vieira; PEIXOTO, Josana de Castro

    2016-01-01

    Lagochilascariosis, a disease caused by Lagochilascaris minor, affects the neck, sinuses, tonsils, lungs, the sacral region, dental alveoli, eyeballs and the central nervous system of humans. A cycle of autoinfection may occur in human host tissues characterized by the presence of eggs, larvae and adult worms. This peculiarity of the cycle hinders therapy, since there are no drugs that exhibit ovicidal, larvicidal and vermicidal activity. Given these facts, we studied the action of levamisole hydrochloride on third-stage larvae in the migration phase (G1) and on encysted larvae (G3) of L. minor. To this end, 87 inbred mice of the C57BL/6 strain were divided into test groups comprising 67 animals (G1-37; G3-30) and a control group (G2-10; G4-10) with 20 animals. Each animal was inoculated orally with 2,000 infective eggs of the parasite. The animals of the test groups were treated individually with a single oral dose of levamisole hydrochloride at a concentration of 0.075 mg. The drug was administered either 30 minutes prior to the parasite inoculation (G1 animals) or 120 days after the inoculation (G3 animals). The mice in the control groups were not treated with the drug. After the time required for the migration and the encysting of L. minor larvae, all the animals were euthanized and their tissues examined. The data were analyzed using the Student's unpaired t-test and the Levene test. The groups showed no statistically significant difference. Levamisole hydrochloride was ineffective on third-stage larvae of L. minor. These findings explain the massive expulsion of live adult worms, as well as the use of long treatment schemes, owing to the persistence of larvae and eggs in human parasitic lesions. PMID:27253745

  1. Modulation of Venlafaxine Hydrochloride Release from Press Coated Matrix Tablet

    PubMed Central

    Gohel, M. C.; Soni, C. D.; Nagori, S. A.; Sarvaiya, K. G.

    2008-01-01

    The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 32 full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion). The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets. PMID:20046735

  2. Oral administration of diazepam and promazine hydrochloride to immobilize pronghorn.

    PubMed

    Pusateri, F M; Hibler, C P; Pojar, T M

    1982-01-01

    Oral tranquilizers were mixed with a grain bait and fed to pronghorn (Antilocapra americana) in an attempt to immobilize and thus facilitate their capture. Diazepam, administered at 6 mg/kg body weight immobilized a tame pronghorn fawn within 30 min. Tranquilization was still apparent after 8 h. A minimum dose of 23 mg/kg body weight was necessary to immobilize a wild adult pronghorn. Immobilization occurred after 60 min and tranquilization was apparent 24 h post ingestion. Excitement severely impeded the effect of the drug and although easily captured, the animal struggled wildly when handled. Wild pronghorn fawns showed moderate tranquilization when administered diazepam at 23 mg/kg body weight but were unapproachable. Doses of diazepam between 13 and 23 mg/kg body weight were used to capture tame yearling and adult pronghorn held in a 132 ha enclosure. A dose of 23 mg/kg body weight was excessive in that the animals did not recover for 48 to 54 h post ingestion and had difficulty maintaining a sternal bedding position. Diazepam at 13 mg/kg body weight failed to tranquilize the animals sufficiently for easy capture. Promazine hydrochloride at doses of 2 to 17 mg/kg body weight, given orally to wild pronghorn fawns and an adult, did not produce visible signs of tranquilization. Animals refused to eat bait containing doses of promazine hydrochloride greater than 17 mg/kg body weight.

  3. Transepithelial transport of biperiden hydrochloride in Caco-2 cell monolayers.

    PubMed

    Abalos, Ivana S; Rodríguez, Yanina I; Lozano, Verónica; Cereseto, Marina; Mussini, Maria V; Spinetto, Marta E; Chiale, Carlos; Pesce, Guido

    2012-09-01

    The aim of this research has been to determine the biperiden hydrochloride permeability in Caco-2 model, in order to classify it based on the Biopharmaceutics Classification System (BCS). The World Health Organization (WHO) as well as many other authors have provisionally assigned the drug as BCS class I (high solubility-high permeability) or III (high solubility-low permeability), based on different methods. We determined biperiden BCS class by comparing its permeability to 5 pre-defined compounds: atenolol and ranitidine hydrochloride (low permeability group) and metoprolol tartrate, sodium naproxen and theophylline (high permeability group). Since biperiden permeability was higher than those obtained for high permeability drugs, we classified it as a BCS class I compound. On the other hand, as no differences were obtained for permeability values when apical to basolateral and basolateral to apical fluxes were studied, this drug cannot act as a substrate of efflux transporters. As a consequence of our results, we suggest that the widely used antiparkinsonian drug, biperiden, should be candidate for a waiver of in vivo bioequivalence studies.

  4. Growth of glycine ethyl ester hydrochloride and its characterizations

    NASA Astrophysics Data System (ADS)

    Venkatesan, G.; Pari, S.

    2016-11-01

    Single crystal of glycine ethyl ester hydrochloride by slow evaporation method is reported. The grown crystal characterized by single crystal X-ray diffraction, FT-IR, UV-Vis-NIR and fluorescence spectroscopy. It is established that the crystal falls under the monoclinic system and space group P21/c with the cell parameters as: a=8.565 Å, b=12.943 Å, c=6.272 Å, α=γ=90°, β=103.630º. UV-Vis-NIR spectrum shows indirect allowed transition with a band gap of 5.21 eV and other optical properties are measured. The crystal is also shown to have a high transmittance in the visible region. The third order nonlinear property and optical limiting have been investigated using Z-Scan technique. Complex impedance spectrum measured at the dc conductivity. Dependence of dielectric constant, dielectric loss and ac conductivity on frequency at different temperature of applied ac field is analyzed. The mechanical behavior has been assessed by Vickers microhardness indenter. The thermal behavior of glycine ethyl ester hydrochloride was analyzed using TG/DTA thermal curves. From the thermal study, the material was found to possess thermal stability up to 174 °C. The predicted NLO properties, UV-Vis transmittance and Z-scan studies indicate that is an attractive material for photonics optical limiting applications.

  5. Fabrication and Development of Pectin Microsphere of Metformin Hydrochloride

    PubMed Central

    Banerjee, Pritam; Deb, Jyotirmoy; Roy, Amitava; Ghosh, Amitava; Chakraborty, Prithviraj

    2012-01-01

    Purpose. The objective of the proposed work is to evaluate the efficacy of Pectins to qualify them as polymers for designing an oral microsphere for the delivery of selected oral antidiabetic drug-like metformin hydrochloride. Methods. Different Microspheres formulations were prepared by the water in oil (w\\o) emulsion solvent evaporation technique and subsequently evaluated for its different physical parameters as well as its in vitro and in vivo drug release study. Results. The formulations F2 (98.42) and F3 (98.03) showed a constant and high release in the dissolution profile, so among these two formulations, F2 was taken for development study, due to the better result shown over in other evaluation parameters. From the HPLC determinations after in vivo study, it had been found that the test samples and the standard sample had not shown any significant fluctuation in relation to their retention time. Conclusion. From in vitro and in  vivo results, it may be concluded that drug-loaded pectin microspheres in 1 : 1 ratio are a suitable delivery system for metformin hydrochloride and may be used for effective management of NIDDM. From this experiment, it could be concluded that as a natural polymer, pectin has potentiality in novel drug delivery system. PMID:22900209

  6. Modulation of venlafaxine hydrochloride release from press coated matrix tablet.

    PubMed

    Gohel, M C; Soni, C D; Nagori, S A; Sarvaiya, K G

    2008-01-01

    The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 3(2) full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion). The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets.

  7. Quantification of antioxidants by using chlorpromazine hydrochloride: application of the method to food and medicinal plant samples.

    PubMed

    Nagaraja, Padmarajaiah; Aradhana, Narayanan; Suma, Aandamurthy; Shivakumar, Anantharaman; Chamaraja, Nelligere Arkeshwaraiah

    2014-01-01

    Chlorpromazine hydrochloride (CPH) (3-(2-chloro-phenothiazine-10-yl)-propyl] dimethylamine hydrochloride) has been the subject of a large number of studies employing a broad spectrum of oxidants, and chosen to examine the course of electron transfer reactions. We report on a method to determine the antioxidant activity of some food and medicinal plants using the oxidation of CPH by chromium(VI) to form a stable CPH radical in the 1:1 orthophosphoric acid-ethyl alcohol (OPA-EtOH) medium. The pink color of the control solution was measured at λ(max) of 530 nm. Nine standard antioxidants have been studied by this method, along with the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. The EC50, TEC50, antioxidant efficacy and the stoichiometric values for antioxidants have been evaluated. The radical scavenging activity expressed as EC50 ranged from 9.2 μg/mL in Camellia sinensis to 448.18 μg/mL in Cuminum cyminum. The application of a simple and versatile antioxidant capacity assay for dietary polyphenols and medicinal plant extracts, which are commonly used in Ayurveda opens its relevance in the field of antioxidant analysis.

  8. Second-derivative synchronous fluorescence spectroscopy for the simultaneous determination of fluphenazine hydrochloride and nortriptyline hydrochloride in pharmaceutical preparations.

    PubMed

    Walash, M I; El-Brashy, A; El-Enany, N; Kamel, M E

    2009-09-01

    A rapid, simple, and highly sensitive second-derivative synchronous fluorimetric (SDSF) method has been developed for the simultaneous analysis of binary mixtures of fluphenazine hydrochloride (FLZ) and nortriptyline hydrochloride (NTP) in their co-formulated tablets. The method is based upon measurement of the native fluorescence of these drugs at constant wavelength difference (Deltalambda) = 120 nm in acetic acid. The different experimental parameters affecting the fluorescence intensity of the studied drugs were carefully studied and optimized. The fluorescence-concentration plots were rectilinear over the range of 0.25-3.0 and 1-10 microg/ml for FLZ and NTP respectively, with lower detection limits (LOD) of 0.05 and 0.18 microg/ml and quantitation limits of 0.15 and 0.53 microg/ml for FLZ and NTP respectively. The proposed method was successfully applied for the determination of the studied compounds in their synthetic mixtures and in commercial co-formulated tablets. The results obtained were in good agreement with those obtained by the reference methods.

  9. Extractive determination of ephedrine hydrochloride and bromhexine hydrochloride in pure solutions, pharmaceutical dosage form and urine samples.

    PubMed

    Abdel-Ghani, N T; Rizk, M S; Mostafa, M

    2013-07-01

    Simple, rapid, sensitive, precise and accurate spectrophotometeric methods for the determination of ephedrine hydrochloride (E-HCl) and bromhexine hydrochloride (Br-HCl) in bulk samples, dosage form and in spiked urine samples were investigated. The methods are based on the formation of a yellow colored ion-associates due to the interaction between the examined drugs with picric acid (PA), chlorophyllin coppered trisodium salt (CLPH), alizarin red (AR) and ammonium reineckate (Rk) reagents. A buffer solution had been used and the extraction was carried out using organic solvent, the ion associates exhibit absorption maxima at 410, 410, 430 and 530 nm of (Br-HCl)with PA, CLPH, AR and Rk respectively; 410, 410, 435 and 530 of (E-HCl) with PA, CLPH, AR and Rk respectively. (E-HCl) and (Br-HCl) could be determined up to 13, 121, 120 and 160; 25, 200, 92 and 206 μg mL(-1), using PA, CLPH, AR and Rk respectively. The optimum reaction conditions for quantitative analysis were investigated. In addition, the molar absorptivity, Sandell sensitivity were determined for the investigated drug. The correlation coefficient was ≥0.995 (n=6) with a relative standard deviation (RSD) ≤1.15 for five selected concentrations of the reagents. Therefore the concentration of Br-HCl and E-HCl drugs in their pharmaceutical formulations and spiked urine samples had been determined successfully.

  10. Extractive determination of ephedrine hydrochloride and bromhexine hydrochloride in pure solutions, pharmaceutical dosage form and urine samples

    NASA Astrophysics Data System (ADS)

    Abdel-Ghani, N. T.; Rizk, M. S.; Mostafa, M.

    2013-07-01

    Simple, rapid, sensitive, precise and accurate spectrophotometeric methods for the determination of ephedrine hydrochloride (E-HCl) and bromhexine hydrochloride (Br-HCl) in bulk samples, dosage form and in spiked urine samples were investigated. The methods are based on the formation of a yellow colored ion-associates due to the interaction between the examined drugs with picric acid (PA), chlorophyllin coppered trisodium salt (CLPH), alizarin red (AR) and ammonium reineckate (Rk) reagents. A buffer solution had been used and the extraction was carried out using organic solvent, the ion associates exhibit absorption maxima at 410, 410, 430 and 530 nm of (Br-HCl)with PA, CLPH, AR and Rk respectively; 410, 410, 435 and 530 of (E-HCl) with PA, CLPH, AR and Rk respectively. (E-HCl) and (Br-HCl) could be determined up to 13, 121, 120 and 160; 25, 200, 92 and 206 μg mL-1, using PA, CLPH, AR and Rk respectively. The optimum reaction conditions for quantitative analysis were investigated. In addition, the molar absorptivity, Sandell sensitivity were determined for the investigated drug. The correlation coefficient was ⩾0.995 (n = 6) with a relative standard deviation (RSD) ⩽1.15 for five selected concentrations of the reagents. Therefore the concentration of Br-HCl and E-HCl drugs in their pharmaceutical formulations and spiked urine samples had been determined successfully.

  11. Effects of ambroxol hydrochloride on concentrations of paclitaxel and carboplatin in lung cancer patients at different administration times.

    PubMed

    Li, J; Yi, W; Jiang, P; Sun, R; Li, T

    2016-11-30

    Our previous preliminary study revealed a synergistic effect of ambroxol hydrochloride with chemotherapeutic agents such as paclitaxel and carboplatin in lung cancer. However, the optimal conditions such as administration time and drug concentration of ambroxol hydrochloride to achieve the maximum synergistic effect remained unclear. Therefore, concentration changes of the chemotherapy drugs paclitaxel and carboplatin in the sputum were observed after ambroxol hydrochloride administration at different times in order to determine the most effective time frame of ambroxol hydrochloride administration. In this study, 470 cases of non-small cell lung cancer (NSCLC) were divided into different groups with ambroxol hydrochloride administered at different time points prior to chemotherapy, while another 171 cases received no ambroxol hydrochloride prior to chemotherapy. The results showed the concentrations of paclitaxel and carboplatin in sputum of patients treated with ambroxol hydrochloride were significantly higher than those of the control group, suggesting that ambroxol hydrochloride significantly increased the local concentrations of chemotherapeutic agents in lung tissues of NSCLC. Furthermore, the intravenous administration of ambroxol hydrochloride more than 48 hours before chemotherapy showed an optimized schedule and much greater efficacy in increasing drug concentrations than that of the control group. No statistical differences were found in the rates of grade 2 or above myelosuppression between the ambroxol intervention and control groups. Taken together, these results demonstrate that ambroxol hydrochloride administered intravenously more than 48 hours prior to chemotherapy optimally increased the concentrations of paclitaxel and carboplatin in lung tissue without significantly increasing hematologic toxicity.

  12. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... contains lincomycin hydrochloride equivalent to either 25 milligrams or 50 milligrams of lincomycin. (b... pound of body weight every 12 hours, or 7 mgs per pound of body weight every 8 hours. Treatment may...

  13. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... in the polymeric form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The resin... hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of...

  14. The antidepressant drugs fluoxetine and duloxetine produce anxiolytic-like effects in a schedule-induced polydipsia paradigm in rats: enhancement of fluoxetine's effects by the α2 adrenoceptor antagonist yohimbine.

    PubMed

    Prus, Adam J; Mooney-Leber, Sean M; Berquist, Michael D; Pehrson, Alan L; Porter, Nicholas P; Porter, Joseph H

    2015-08-01

    Similar to the time-course for treating depression, several weeks of administration are required for serotonin (5-HT) reuptake inhibitors to produce anxiolytic effects. Previous studies with the schedule-induced polydipsia paradigm (a putative preclinical anxiety model) have shown that repeated administration of antidepressant drugs is necessary to produce a suppression of polydipsia, which is interpreted as an anxiolytic-like effect. The present study sought to expand past findings by evaluating the selective 5-HT reuptake inhibitor (SSRI) fluoxetine and the 5-HT-norepinephrine reuptake inhibitor duloxetine in the schedule-induced polydipsia paradigm with rats. Dose combinations of the α2 adrenoceptor antagonist yohimbine with fluoxetine were also explored to determine whether α2 adrenoceptor antagonism could enhance the anxiolytic-like effects produced by an SSRI. Fluoxetine and duloxetine significantly reduced water intake over the course of daily administrations. Daily treatment with the combination of fluoxetine and yohimbine produced a significantly greater reduction in water intake than fluoxetine alone. The present results confirmed previous findings that inhibition of 5-HT reuptake reduces water consumption in this paradigm. The results for the α2 antagonist yohimbine (in combination with fluoxetine) also indicate that α2 adrenoceptor antagonism may significantly enhance anxiolytic-like effects of SSRIs.

  15. Mucoadhesive system formed by liquid crystals for buccal administration of poly(hexamethylene biguanide) hydrochloride.

    PubMed

    Souza, Carla; Watanabe, Evandro; Borgheti-Cardoso, Livia Neves; De Abreu Fantini, Márcia Carvalho; Lara, Marilisa Guimarães

    2014-12-01

    Antimicrobial approaches are valuable in controlling the development of buccal diseases, but some antibacterial agents have a short duration of activity. Therefore, the development of prolonged delivery systems would be advantageous. Liquid crystalline systems comprising monoolein (GMO)/water have been considered to be a potential vehicle to deliver drugs to the buccal mucosa because of the phase properties that allow for controlled drug release as well as its mucoadhesive properties. Therefore, the aim of this study was to develop a GMO/water system for the slow release of poly(hexamethylene biguanide) hydrochloride (PHMB) on the buccal mucosa and test the properties of this system with regard to swelling, release profile, antimicrobial activity, and strength of mucoadhesion, with the overall goal of treating buccal infections. The tested systems were capable of modulating drug release, which is controlled by diffusion of the drug throughout the system. Furthermore, PHMB appeared to improve the mucoadhesive properties of the system and may synergistically act with the drug to promote antimicrobial activity against S. mutas and C. albicans, indicating that liquid crystals may be suitable for the administration of PHMB on the buccal mucosa. Therefore, this system could be proposed as a novel system for mucoadhesive drug delivery.

  16. Multilayer Films and Capsules of Sodium Carboxymethylcellulose and Polyhexamethylenguanidine Hydrochloride

    NASA Astrophysics Data System (ADS)

    Guzenko, Nataliia; Gabchak, Oleksandra; Pakhlov, Evgenij

    The complexation of polyhexamethylenguanidine hydrochloride (PHMG) and sodium carboxymethylcellulose (CMC) was investigated for different conditions. Mixing of equiconcentrated aqueous solutions of the polyelectrolytes was found to result in the formation of an insoluble interpolyelectrolyte complex with an overweight of carboxymethylcellulose. A step-by-step formation of stable, irreversibly adsorbed multilayer film of the polymers was demonstrated using the quartz crystal microbalance method. Unusually thick polymer shells with a large number of loops and tails of the polyanion were formed by the method of layer-by-layer self-assembly of PHMG and CMC on spherical CaCO3 particles. Hollow multilayer capsules stable in neutral media were obtained by dissolution of the inorganic matrix in EDTA solution.

  17. Glucosamine hydrochloride for the treatment of osteoarthritis symptoms

    PubMed Central

    Fox, Beth Anne; Stephens, Mary M

    2007-01-01

    Osteoarthritis is the most common arthritis in the world. It affects millions of people with age being the greatest risk factor for developing the disease. The burden of disease will worsen with the aging of the world’s population. The disease causes pain and functional disability. The direct costs of osteoarthritis include hospital and physician visits, medications, and assistive services. The indirect costs include work absences and lost wages. Many studies have sought to find a therapy to relieve pain and reduce disability. Glucosamine hydrochloride (HCl) is one of these therapies. There are limited studies of glucosamine HCl in humans. Although some subjects do report statistically significant improvement in pain and function from products combining glucosamine HCl and other agents, glucosamine HCl by itself appears to offer little benefit to those suffering from osteoarthritis. PMID:18225460

  18. Crystal structure of BIS(Betaine) hydrochloride monohydrate

    NASA Astrophysics Data System (ADS)

    Chen, Xiao-Ming; Mak, Thomas C. W.

    1990-11-01

    Bis(betaine) hydrochloride monohydrate, 2Me 3NCH 2COO·HCI·H 2O, crystallizes in space group Pnma (No. 62), with a=11.904(1), b=22.454(5), c=5.624(1) Å, and Z=4. The structure has been refined to RinF=0.046 for 863 observed (| Fo||>6σ| Fo|) Mo Kα data. the carboxylate groups of a pair of betaine molecules are bridged by a proton to form a centrosymmetric dimer featuring a very strong hydrogen bond of length 2.454(4) Å. The crystal structure comprises a packing of such [(Me 3NCH 2COO) 2H] + moieties and hydrogen-bonded (Cl -·H 2O) ∞ zigzag chains running parallel to the c axis.

  19. Crystal structure of bis(pyridine betaine) hydrochloride monohydrate

    NASA Astrophysics Data System (ADS)

    Xiao-Ming, Chen; Mak, Thomas C. W.

    1990-04-01

    Bis(pyridine betaine) hydrochloride monohydrate, 2C 5H 5NCH 2COO·HCl·H 2O, crystallizes in space group Pnna (No. 52), with a=15.623(3), b=19.707(3), c=5.069(1) Å, and Z=4. The structure has been refined to RF=0.067 for 1207 observed (| F0|>6σ| F0|) Mo Kα data. The carboxylate groups of a pair of pyridine betaine molecules are bridged by a proton to form a centrosymmetric dimer featuring a very strong hydrogen bond of length 2.436(6) Å. The crystal structure comprises a packing of such [(C 5H 5NCH 2COO) 2H] + moieties and hydrogen-bonded (Cl -{dH 2O} ∞) zigzag chains running parallel to the c axis.

  20. The relative stability of xylazine hydrochloride polymorphous forms.

    PubMed

    Bērziņs, Agris; Krūkle, Kristīne; Actiņs, Andris; Kreismanis, Juris P

    2010-01-01

    All four known xylazine hydrochloride polymorphous forms were obtained and their relative stabilities were compared directly at three different temperatures. At higher temperatures, it is possible to determine the relative stability of all forms directly by measuring the changes in the composition of the mixtures of two polymorphous forms using powder x-ray diffraction methods. At lower temperatures, a solvent was added to the mixture and the changes in composition were determined. Polymorph transition temperatures were determined directly. To predict the transition temperature which was not found using the direct method, the polymorph melting data and determined transition temperatures were used. A phase stability diagram was constructed from the acquired data. The stability of all anhydrous polymorphous forms was compared in the presence of water vapor pressure that was higher than the equilibrium pressure.

  1. Development and Statistical Optimisation of Buspirone Hydrochloride Buccoadhesive Films

    PubMed Central

    Nagaich, Upendra; Chaudhary, Vandana; Nagaich, Jaya

    2014-01-01

    The aim of the present study was to prepare unidirectional buccal films of buspirone hydrochloride by solvent casting technique. Hydroxypropylmethylcellulose (HPMC K15M) and Eudragit RL-100 were used as polymers in different proportion. Polyethylene glycol 400 and sodium lauryl sulphate were used as plasticizer and permeation enhancer, respectively, in different concentration. In the formulation, total amount of polymer (X1) and percentage of HPMC K15M (X2) were kept as independent variables. Afterwards, statistically optimized process was carried out and two optimized formulations (OF1 and OF2) were developed. The observed results of optimized formulation were showed a greater degree of percentage of similarity with predicted values. The stability studies showed that there was no significant change found in physicochemical properties, in-vitro release, and ex-vivo diffusion studies. PMID:27351002

  2. Identification and characterization of potential impurities in raloxifene hydrochloride.

    PubMed

    Reddy, Reguri Buchi; Goud, Thirumani Venkateshwar; Nagamani, Nagabushanam; Kumar, Nutakki Pavan; Alagudurai, Anandan; Murugan, Raman; Parthasarathy, Kannabiran; Karthikeyan, Vinayagam; Balaji, Perumal

    2012-01-01

    During the synthesis of the bulk drug Raloxifene hydrochloride, eight impurities were observed, four of which were found to be new. All of the impurities were detected using the gradient high performance liquid chromatographic (HPLC) method, whose area percentages ranged from 0.05 to 0.1%. LCMS was performed to identify the mass number of these impurities, and a systematic study was carried out to characterize them. These impurities were synthesized and characterized by spectral data, subjected to co-injection in HPLC, and were found to be matching with the impurities present in the sample. Based on their spectral data (IR, NMR, and Mass), these impurities were characterized as Raloxifene-N-Oxide [Impurity: 1]; EP impurity A [Impurity: 2]; EP impurity B [Impurity: 3]; Raloxifene Dimer [Impurity: 4]; HABT (6-Acetoxy-2-[4-hydroxyphenyl]-1-benzothiophene or 6-Hydroxy-2-[4-acetoxyphenyl]-1-benzothiophene) [Impurity: 5]; PEBE (Methyl[4-[2-(piperidin-1-yl)ethoxy

  3. Mini-tablet combination for sustained release of clonidine hydrochloride and hydrochlorothiazide: Preparation and pharmacokinetics in beagle dogs.

    PubMed

    Xu, Bohui; Wang, Yubin; Zhu, Hongyan

    2016-02-01

    Mini-tablets are increasingly gaining attention in solid dosage form design as multiple-unit systems combining different active compounds and providing a single or combined pattern of modified release for polypharmacy or combined treatments. A combination therapy of clonidine hydrochloride and hydrochlorothiazide achieves effective blood pressure control and reduction in adverse effects. However, the combination formulation of immediate release must be taken several times a day, which causes noticeable fluctuation of blood pressure and inconveniences to the patients. The present study was performed to develop a mini-tablet combination for sustained release of clonidine hydrochloride and hydrochlorothiazide independently, in which the two drugs and fraction doses were formulated into separate mini-tablets with different release patterns. The mini-tablets were prepared by a direct compression method followed by filling into capsules and the factors that affected drug release were addressed. Further, studies of the pharmacokinetics were performed in beagle dogs. Finally, in vivo-in vitro correlations of the sustained release systems and bioequivalence with conventional preparations were evaluated. The mini-tablet combination released the two drugs over 24h in vivo with a steady plasma concentration, a markedly lower Cmax, extended Tmax and better bioavailability. In conclusion, sustained releases of the two drugs were obtained with this mini-tablet combination, which offers a feasible formulation and promising development value for hypertensive patients who need long-term therapy.

  4. Comparative studies by IR, Raman, and surface-enhanced Raman spectroscopy of azodicarbonamide, biurea and semicarbazide hydrochloride

    NASA Astrophysics Data System (ADS)

    Xie, Yunfei; Li, Pei; Zhang, Jin; Wang, Heya; Qian, He; Yao, Weirong

    2013-10-01

    Azodicarbonamide is widely applied in the food industry as a new flour gluten fortifier in China, Canada, the United States, and some other countries, whose metabolites of biurea and semicarbazide hydrochloride are reaction products during baking. In this study, IR, Raman and surface-enhanced Raman scattering (SERS) spectra of azodicarbonamide, biurea, and semicarbazide hydrochloride have been studied, and vibrational bands have been assigned on the basis of density functional theory (DFT) calculations. The calculated Raman spectra were in good agreement with experimental Raman spectra. The SERS method coupled with active gold substrates has also been applied for detection of the three chemicals with pure water as solvent, with the limit of detection of this method being as low as 10 μg/mL (less than 45 μg/mL). These results showed that azodicarbonamide and its metabolites could be detected by the vibrational spectra technique, which might be applied as a powerful tool for the rapid detection on these species derived from agents added to flour.

  5. The use of Hibiscus esculentus (Okra) gum in sustaining the release of propranolol hydrochloride in a solid oral dosage form.

    PubMed

    Zaharuddin, Nurul Dhania; Noordin, Mohamed Ibrahim; Kadivar, Ali

    2014-01-01

    The effectiveness of Okra gum in sustaining the release of propranolol hydrochloride in a tablet was studied. Okra gum was extracted from the pods of Hibiscus esculentus using acetone as a drying agent. Dried Okra gum was made into powder form and its physical and chemical characteristics such as solubility, pH, moisture content, viscosity, morphology study using SEM, infrared study using FTIR, crystallinity study using XRD, and thermal study using DSC and TGA were carried out. The powder was used in the preparation of tablet using granulation and compression methods. Propranolol hydrochloride was used as a model drug and the activity of Okra gum as a binder was compared by preparing tablets using a synthetic and a semisynthetic binder which are hydroxylmethylpropyl cellulose (HPMC) and sodium alginate, respectively. Evaluation of drug release kinetics that was attained from dissolution studies showed that Okra gum retarded the release up to 24 hours and exhibited the longest release as compared to HPMC and sodium alginate. The tensile and crushing strength of tablets was also evaluated by conducting hardness and friability tests. Okra gum was observed to produce tablets with the highest hardness value and lowest friability. Hence, Okra gum was testified as an effective adjuvant to produce favourable sustained release tablets with strong tensile and crushing strength.

  6. Development of a microparticle-based dry powder inhalation formulation of ciprofloxacin hydrochloride applying the quality by design approach.

    PubMed

    Karimi, Keyhaneh; Pallagi, Edina; Szabó-Révész, Piroska; Csóka, Ildikó; Ambrus, Rita

    2016-01-01

    Pulmonary drug delivery of ciprofloxacin hydrochloride offers effective local antibacterial activity and convenience of easy application. Spray drying is a trustworthy technique for the production of ciprofloxacin hydrochloride microparticles. Quality by design (QbD), an up-to-date regulatory-based quality management method, was used to predict the final quality of the product. According to the QbD-based theoretical preliminary parameter ranking and priority classification, dry powder inhalation formulation tests were successfully performed in practice. When focusing on the critical parameters, the practical development was more effective and was in correlation with our previous findings. Spray drying produced spherical microparticles. The dry powder formulations prepared were examined by particle size analysis, scanning electron microscopy, Fourier-transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro drug release and aerodynamic particle size analyses were also performed. These formulations showed an appropriate particle size ranging between 2 and 4 μm and displayed an enhanced aerosol performance with fine particle fraction up to 80%.

  7. Development of a microparticle-based dry powder inhalation formulation of ciprofloxacin hydrochloride applying the quality by design approach

    PubMed Central

    Karimi, Keyhaneh; Pallagi, Edina; Szabó-Révész, Piroska; Csóka, Ildikó; Ambrus, Rita

    2016-01-01

    Pulmonary drug delivery of ciprofloxacin hydrochloride offers effective local antibacterial activity and convenience of easy application. Spray drying is a trustworthy technique for the production of ciprofloxacin hydrochloride microparticles. Quality by design (QbD), an up-to-date regulatory-based quality management method, was used to predict the final quality of the product. According to the QbD-based theoretical preliminary parameter ranking and priority classification, dry powder inhalation formulation tests were successfully performed in practice. When focusing on the critical parameters, the practical development was more effective and was in correlation with our previous findings. Spray drying produced spherical microparticles. The dry powder formulations prepared were examined by particle size analysis, scanning electron microscopy, Fourier-transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro drug release and aerodynamic particle size analyses were also performed. These formulations showed an appropriate particle size ranging between 2 and 4 μm and displayed an enhanced aerosol performance with fine particle fraction up to 80%. PMID:27784991

  8. Comparative studies by IR, Raman, and surface-enhanced Raman spectroscopy of azodicarbonamide, biurea and semicarbazide hydrochloride.

    PubMed

    Xie, Yunfei; Li, Pei; Zhang, Jin; Wang, Heya; Qian, He; Yao, Weirong

    2013-10-01

    Azodicarbonamide is widely applied in the food industry as a new flour gluten fortifier in China, Canada, the United States, and some other countries, whose metabolites of biurea and semicarbazide hydrochloride are reaction products during baking. In this study, IR, Raman and surface-enhanced Raman scattering (SERS) spectra of azodicarbonamide, biurea, and semicarbazide hydrochloride have been studied, and vibrational bands have been assigned on the basis of density functional theory (DFT) calculations. The calculated Raman spectra were in good agreement with experimental Raman spectra. The SERS method coupled with active gold substrates has also been applied for detection of the three chemicals with pure water as solvent, with the limit of detection of this method being as low as 10 μg/mL (less than 45 μg/mL). These results showed that azodicarbonamide and its metabolites could be detected by the vibrational spectra technique, which might be applied as a powerful tool for the rapid detection on these species derived from agents added to flour.

  9. Investigation of Biowaivers for Immediate Release Formulations Containing BCS III Drugs, Acyclovir, Atenolol, and Ciprofloxacin Hydrochloride, Using Dissolution Testing.

    PubMed

    Reddy, Nallagundla H S; Patnala, Srinivas; Kanfer, Isadore

    2017-02-01

    The dissolution of several products containing Biopharmaceutical Classification System (BCS) class III drugs, acyclovir, atenolol, and ciprofloxacin hydrochloride, listed in the WHO essential drug list (EDL), was tested and compared with their respective comparator pharmaceutical products (CPPs) marketed in South Africa and India. US Pharmacopeia (USP) buffers of pH 1.2, 4.5, and 6.8 were used as dissolution media and tested using USP apparatus 2 at 75 rpm and 900 ml. Nine acyclovir products were tested, and only three dissolved very rapidly in all media; i.e., they showed a release of >85% in 15 min. Eight atenolol products tested were all very rapidly dissolving in all three pH media. Ten ciprofloxacin hydrochloride products were tested, and the results showed that only five products met the WHO biowaiver criteria. This study indicates that not all marketed products containing the same BCS III active pharmaceutical ingredient (API) in similar strength and dosage form are necessarily in vitro equivalent as per the WHO biowaiver criteria. Furthermore, selection and availability of an innovator product as CPP are important considerations that can affect the outcomes of such studies.

  10. Determination of Propranolol Hydrochloride in Pharmaceutical Preparations Using Near Infrared Spectrometry with Fiber Optic Probe and Multivariate Calibration Methods

    PubMed Central

    Marques Junior, Jucelino Medeiros; Muller, Aline Lima Hermes; Foletto, Edson Luiz; da Costa, Adilson Ben; Bizzi, Cezar Augusto; Irineu Muller, Edson

    2015-01-01

    A method for determination of propranolol hydrochloride in pharmaceutical preparation using near infrared spectrometry with fiber optic probe (FTNIR/PROBE) and combined with chemometric methods was developed. Calibration models were developed using two variable selection models: interval partial least squares (iPLS) and synergy interval partial least squares (siPLS). The treatments based on the mean centered data and multiplicative scatter correction (MSC) were selected for models construction. A root mean square error of prediction (RMSEP) of 8.2 mg g−1 was achieved using siPLS (s2i20PLS) algorithm with spectra divided into 20 intervals and combination of 2 intervals (8501 to 8801 and 5201 to 5501 cm−1). Results obtained by the proposed method were compared with those using the pharmacopoeia reference method and significant difference was not observed. Therefore, proposed method allowed a fast, precise, and accurate determination of propranolol hydrochloride in pharmaceutical preparations. Furthermore, it is possible to carry out on-line analysis of this active principle in pharmaceutical formulations with use of fiber optic probe. PMID:25861516

  11. The Use of Hibiscus esculentus (Okra) Gum in Sustaining the Release of Propranolol Hydrochloride in a Solid Oral Dosage Form

    PubMed Central

    Noordin, Mohamed Ibrahim; Kadivar, Ali

    2014-01-01

    The effectiveness of Okra gum in sustaining the release of propranolol hydrochloride in a tablet was studied. Okra gum was extracted from the pods of Hibiscus esculentus using acetone as a drying agent. Dried Okra gum was made into powder form and its physical and chemical characteristics such as solubility, pH, moisture content, viscosity, morphology study using SEM, infrared study using FTIR, crystallinity study using XRD, and thermal study using DSC and TGA were carried out. The powder was used in the preparation of tablet using granulation and compression methods. Propranolol hydrochloride was used as a model drug and the activity of Okra gum as a binder was compared by preparing tablets using a synthetic and a semisynthetic binder which are hydroxylmethylpropyl cellulose (HPMC) and sodium alginate, respectively. Evaluation of drug release kinetics that was attained from dissolution studies showed that Okra gum retarded the release up to 24 hours and exhibited the longest release as compared to HPMC and sodium alginate. The tensile and crushing strength of tablets was also evaluated by conducting hardness and friability tests. Okra gum was observed to produce tablets with the highest hardness value and lowest friability. Hence, Okra gum was testified as an effective adjuvant to produce favourable sustained release tablets with strong tensile and crushing strength. PMID:24678512

  12. Instability of the hydrochloride salts of cathinone derivatives in air.

    PubMed

    Tsujikawa, Kenji; Yamamuro, Tadashi; Kuwayama, Kenji; Kanamori, Tatsuyuki; Iwata, Yuko T; Inoue, Hiroyuki

    2015-03-01

    We observed the decomposition of the hydrochloride salt of α-pyrrolidinoheptanophenone (α-PHPP-HCl), a newly distributed pyrrolidine-type cathinone derivative when 2.5ng of this substance was placed in glass test tubes and stored in a refrigerator for 3 days. To further investigate this phenomenon, we studied the (i) time course of the residual ratios of α-PHPP-HCl when a small amount (10μg) of α-PHPP-HCl was stored in glass vials in air at room temperature; (ii) identification of the decomposition products of α-PHPP-HCl; (iii) effect of air on the decomposition process; (iv) effect of the added amounts of α-PHPP-HCl on its decomposition; and (v) comparison of the stability between various cathinone derivatives and their decomposition products. The decomposition of α-PHPP-HCl occurred in air and increased with time. Two possible decomposition products, α-(2″-oxopyrrolidino)heptanophenone and α-PHPP-N-oxide, were identified. These products were formed by oxygen in air because the yield significantly decreased by storing them in a vacuum desiccator. With the decrease in the amount of α-PHPP-HCl, the residual ratios decreased and amount of the decomposition products increased. This indicates that the decomposition of α-PHPP-HCl occurred on the upper surface of the samples. The hydrochloride salts of other cathinone derivatives were also unstable in air, and the residual ratios observed were different depending on the compounds. The pyrrolidine-type cathinone derivatives afforded two types of decomposition products, which were presumed to be 2″-oxo and N-oxide derivatives, similar to α-PHPP-HCl. In contrast, secondary amine-type cathinone derivatives showed different decomposition patterns, possibly including the dealkylated derivative. These findings may be very useful for the future toxicological analysis of cathinone derivatives.

  13. Formulation optimization of propranolol hydrochloride microcapsules employing central composite design.

    PubMed

    Shivakumar, H N; Patel, R; Desai, B G

    2008-01-01

    A central composite design was employed to produce microcapsules of propranolol hydrochloride by o/o emulsion solvent evaporation technique using a mixture of cellulose acetate butyrate as coat material and span-80 as an emulsifier. The effect of formulation variables namely levels of cellulose acetate butyrate (X(1)) and percentage of Span-80 (X(2)) on encapsulation efficiency (Y(1)), drug release at the end of 1.5 h (Y(2)), 4 h (Y(3)), 8 h (Y(4)), 14 h (Y(5)), and 24 h (Y(6)) were evaluated using the F test. Mathematical models containing only the significant terms were generated for each response parameter using multiple linear regression analysis and analysis of variance. Both the formulation variables exerted a significant influence (P <0.05) on Y(1) whereas the cellulose acetate butyrate level emerged as the lone factor which significantly influenced the other response parameters. Numerical optimization using desirability approach was employed to develop an optimized formulation by setting constraints on the dependent and independent variables. The experimental values of Y(1), Y(2), Y(3), Y(4), Y(5), and Y(6) for the optimized formulation was found to be 92.86+/-1.56% w/w, 29.58+/-1.22%, 48.56+/-2.56%, 60.85+/-2.35%, 76.23+/-3.16% and 95.12+/-2.41%, respectively which were in close agreement with those predicted by the mathematical models. The drug release from microcapsules followed first order kinetics and was characterized by Higuchi diffusion model. The optimized microcapsule formulation developed was found to comply with the USP drug release test-1 for extended release propranolol hydrochloride capsules.

  14. Pharmacokinetics of Lidocaine Hydrochloride Metabolized by CYP3A4 in Chinese Han Volunteers Living at Low Altitude and in Native Han and Tibetan Chinese Volunteers Living at High Altitude.

    PubMed

    Zhang, Juanling; Zhu, Junbo; Yao, Xingchen; Duan, Yabin; Zhou, Xuejiao; Yang, Meng; Li, Xiangyang

    2016-01-01

    To investigate the pharmacokinetics of lidocaine hydrochloride metabolized by cytochrome P450 3A4 (CYP3A4) in Chinese Han volunteers living at low altitude (LA) and in native Han and Tibetan Chinese volunteers living at high altitude, lidocaine hydrochloride 10 mg was given by intramuscular injection to 3 groups: Han volunteers living at LA, and native Han and Tibetan volunteers living at a high altitude. Blood samples were collected before the (baseline) study drug was given and at 0.25, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0 h after study drug administration. Lidocaine hydrochloride in plasma was determined by RP-HPLC. Pharmacokinetics parameters of lidocaine hydrochloride showed that there were no significant difference between the native Han and Tibetan volunteers, but the t(1/2) was 29.8 and 29.8% higher in 2 groups, respectively, than in the LA group. To study related mechanism, the effects of exposure to chronic high-altitude hypoxia (CHH) on the activity and expression of CYP3A1 were examined in rats. Rats were divided into LA, chronic moderate altitude hypoxia, and CHH groups. CHH caused significant decreases in the activity and protein and mRNA expression of rat CYP3A1 in vivo. This study found significant changes in the disposition of lidocaine hydrochloride in native healthy Tibetan and Han Chinese subjects living at a high altitude in comparison to healthy Han Chinese subjects living at LA, it might be due to significant decreases in the activity and protein and mRNA expression of CYP3A4 under CHH condition.

  15. Sustained transdermal release of diltiazem hydrochloride through electron beam irradiated different PVA hydrogel membranes

    NASA Astrophysics Data System (ADS)

    Bhunia, Tridib; Goswami, Luna; Chattopadhyay, Dipankar; Bandyopadhyay, Abhijit

    2011-08-01

    Extremely fast release of diltiazem hydrochloride (water soluble, anti anginal drug used to treat chest pain) together with its faster erosion has been the primary problem in conventional oral therapy. It has been addressed in this paper by encapsulating the drug in electron beam irradiated various poly (vinyl alcohol) hydrogel membranes and delivering it through transdermal route. Results show excellent control over the release of diltiazem hydrochloride through these membranes subject to their physico-mechanicals.

  16. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... hydrochloric acid that is liberated when hydroxylamine hydrochloride reacts with formaldehyde to form..., using the prestandardized pH meter, 1.0 N hydrochloric acid, 0.1 N hydrochloric acid, and 0.1 N sodium... hydrochloride solution, 100 grams per liter, pH adjusted to 4.00. 4.3Hydrochloric acid solution, 1.0 N and 0.1...

  17. Co-Amorphous Combination of Nateglinide-Metformin Hydrochloride for Dissolution Enhancement.

    PubMed

    Wairkar, Sarika; Gaud, Ram

    2016-06-01

    The aim of the present work was to prepare a co-amorphous mixture (COAM) of Nateglinide and Metformin hydrochloride to enhance the dissolution rate of poorly soluble Nateglinide. Nateglinide (120 mg) and Metformin hydrochloride (500 mg) COAM, as a dose ratio, were prepared by ball-milling technique. COAMs were characterized for saturation solubility, amorphism and physicochemical interactions (X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR)), SEM, in vitro dissolution, and stability studies. Solubility studies revealed a sevenfold rise in solubility of Nateglinide from 0.061 to 0.423 mg/ml in dose ratio of COAM. Solid-state characterization of COAM suggested amorphization of Nateglinide after 6 h of ball milling. XRPD and DSC studies confirmed amorphism in Nateglinide, whereas FTIR elucidated hydrogen interactions (proton exchange between Nateglinide and Metformin hydrochloride). Interestingly, due to low energy of fusion, Nateglinide was completely amorphized and stabilized by Metformin hydrochloride. Consequently, in vitro drug release showed significant increase in dissolution of Nateglinide in COAM, irrespective of dissolution medium. However, little change was observed in the solubility and dissolution profile of Metformin hydrochloride, revealing small change in its crystallinity. Stability data indicated no traces of devitrification in XRPD of stability sample of COAM, and % drug release remained unaffected at accelerated storage conditions. Amorphism of Nateglinide, proton exchange with Metformin hydrochloride, and stabilization of its amorphous form have been noted in ball-milled COAM of Nateglinide-Metformin hydrochloride, revealing enhanced dissolution of Nateglinide. Thus, COAM of Nateglinide-Metformin hydrochloride system is a promising approach for combination therapy in diabetic patients.

  18. A Randomized Clinical Trial of Berberine Hydrochloride in Patients with Diarrhea-Predominant Irritable Bowel Syndrome.

    PubMed

    Chen, Chunqiu; Tao, Chunhua; Liu, Zhongchen; Lu, Meiling; Pan, Qiuhui; Zheng, Lijun; Li, Qing; Song, Zhenshun; Fichna, Jakub

    2015-11-01

    We aimed to evaluate clinical symptoms in diarrhea predominant irritable bowel syndrome (IBS-D) receiving berberine hydrochloride in a randomized double-blind placebo-controlled clinical trial. Overall, 196 patients with IBS-D were recruited for this study; consequently, 132 patients randomized to receive daily 400 mg of berberine hydrochloride, delivered twice daily or placebo for 8 weeks followed by a 4-week washout period. After a 2-week run-in period, diarrhea, abdominal pain, urgent need for defecation frequency and any adverse events were recorded daily. Prior to administration of the medication and after completing the treatment, assessment of IBS symptom scores, depression and anxiety scale scores and the IBS scale for quality of life (QOL) was carried out. The effects of berberine hydrochloride on IBS-D, defined by a reduction of diarrhea frequency (P = 0.032), abdominal pain frequency (P < 0.01) and urgent need for defecation frequency (P < 0.01), were significantly more pronounced in the berberine group than the placebo group in the 8 weeks of treatment. A trend of improvement (P < 0.05) was observed with berberine hydrochloride for IBS symptom score, depression score and anxiety score and the IBSQOL, compared with placebo. At last, berberine hydrochloride was well tolerated. So we concluded that berberine hydrochloride is well tolerated and reduces IBS-D symptoms, which effectively improved patients QOL.

  19. Stability-indicating HPLC Method for Simultaneous Determination of Montelukast and Fexofenadine Hydrochloride

    PubMed Central

    Pankhaniya, Mona; Patel, Parula; Shah, J. S.

    2013-01-01

    A simple, specific, accurate, and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of montelukast and fexofenadine hydrochloride, using a Lichrospher® 100, RP-18e column and a mobile phase composed of methanol:0.1% o-phosphoric acid (90:10 v/v), pH 6.8. The retention times of montelukast and fexofenadine hydrochloride were found to be 10.16 and 12.03 min, respectively. Linearity was established for montelukast and fexofenadine hydrochloride in the range of 2-10 μg/ml and 24-120 μg/ml, respectively. The percentage recoveries of montelukast and fexofenadine hydrochloride were found to be in the range of 99.09 and 99.81%, respectively. Both the drugs were subjected to acid and base hydrolysis, oxidation, photolytic, and thermal degradation conditions. The degradation products of montelukast and fexofenadine hydrochloride were well resolved from the pure drug with significant differences in their retention time values. This method can be successfully employed for simultaneous quantitative analysis of montelukast and fexofenadine hydrochloride in bulk drugs and formulations. PMID:24082344

  20. Electron paramagnetic resonance studies of gamma-irradiated DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride

    NASA Astrophysics Data System (ADS)

    Başkan, M. Halim; Aydın, Murat

    2013-08-01

    The electron paramagnetic resonance (EPR) of gamma irradiated powders of DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride were investigated at room temperature. The observed paramagnetic species were attributed to the CH3ĊHCOOC2H5, -CH2ĊHCOOH and -CH2ĊHCOOCH3 radicals, respectively. Hyperfine structure constants and g-values were determined for these three radicals. Some spectroscopic properties and suggestions concerning the possible structure of the radicals were also discussed.

  1. Comparative effects of ractopamine hydrochloride and zilpaterol hydrochloride on growth performance, carcass traits, and longissimus tenderness of finishing steers.

    PubMed

    Scramlin, S M; Platter, W J; Gomez, R A; Choat, W T; McKeith, F K; Killefer, J

    2010-05-01

    Ractopamine hydrochloride (RAC) and zilpaterol hydrochloride (ZH) are beta-adrenergic agonists that improve growth performance and affect carcass characteristics. The objective of this study was to evaluate the comparative effects of RAC and ZH when fed to beef steers during the last 33 d of the finishing period. Three hundred crossbred beef steers (516 +/- 8 kg) were grouped by BW, BCS, and breed type and randomly assigned to 1 of 3 treatments (10 steers per pen; 10 pens per treatment). Treatments were control (no beta-agonists added), RAC (200 mg of ractopaminexhdx(-1)d(-1), for 33 d), or ZH (75 mg of zilpaterolxanimalx(-1)d(-1), for 30 d, removed 3 d for required withdrawal period). Steers were slaughtered, carcass characteristics were evaluated, and cut-out yields were determined. Both RAC and ZH increased final BW, ADG, feed efficiency (G:F), and HCW compared with controls (P < 0.05). Compared with RAC, ZH decreased ADG, ADFI, and final BW, but increased HCW and dressing percentage (P < 0.05). Carcass yield was not affected by RAC in this experiment, whereas ZH decreased adjusted fat thickness and KPH, increased ribeye area, improved yield grade, and increased cut-out yields, when compared with controls (P < 0.05). Marbling, lean maturity, and skeletal maturity were not different between treatments (P > 0.05). Steaks from RAC steers had greater (P < 0.05) Warner-Bratzler shear force (WBSF) values than steaks from control steers at 3 and 7 d of aging, but did not differ from controls after 14 d of aging. Steaks from ZH steers had greater WBSF values (P < 0.05) than steaks from controls and RAC steaks throughout the 21-d postmortem aging period. Although both beta-adrenergic agonists were effective at improving feedlot performance, RAC showed no negative effect on WBSF after 14 d, whereas WBSF values for ZH steaks were significantly greater than controls after 21 d.

  2. Effects of guanidine hydrochloride and high pressure on subsite flexibility of beta-amylase.

    PubMed

    Tanaka, Naoki; Kajimoto, Sachie; Mitani, Daisuke; Kunugi, Shigeru

    2002-04-29

    We investigated the effects of guanidine hydrochloride (GuHCl) and high pressure on the conformational flexibility of the active site of sweet potato beta-amylase by monitoring the sulfhydryl reaction and the enzymatic activity. The reactivity of Cys345 at the active site, one of six inert half cystine residues of this enzyme, was enhanced by GuHCl at concentrations below 0.5 M. A GuHCl-induced change of the active site was also observed through an intensity change in the near-UV circular dichroism (CD) spectrum. On the other hand, the native conformation of sweet potato beta-amylase observed through fluorescence polarization, far-UV CD spectrum and intrinsic fluorescence was not influenced by GuHCl at concentrations below 0.5 M. Therefore, Cys345 reaction caused by GuHCl was due to an alteration of the local conformation of the active site. GuHCl-induced reaction of Cys345, located in the vicinity of subsites 3 and 4, is attributed to enhanced subsite flexibility, which is responsible for substrate slipping in a single-chain attack mechanism. Due to the flexible conformation, the local region of the subsite is more susceptible to GuHCl perturbation than the molecule overall. The enzymatic activity of sweet potato beta-amylase was reversibly inhibited by GuHCl at concentrations below 0.5 M, and kinetic analysis of the enzymatic mechanism showed that GuHCl decreases the kcat value. High pressure below 400 MPa also inactivated sweet potato beta-amylase with an increase in Cys345 reactivity. These findings indicated that excessively enhanced subsite flexibility reduced the enzymatic activity of sweet potato beta-amylase.

  3. New copper(II) complexes with dopamine hydrochloride and vanillymandelic acid: Spectroscopic and thermal characterization

    NASA Astrophysics Data System (ADS)

    Mohamed, Gehad G.; Nour El-Dien, F. A.; El-Nahas, R. G.

    2011-10-01

    The dopamine derivatives participate in the regulation of wide variety of physiological functions in the human body and in medication life. Increase and/or decrease in the concentration of dopamine in human body reflect an indication for diseases such as Schizophrenia and/or Parkinson diseases. The Cu(II) chelates with coupled products of dopamine hydrochloride (DO.HCl) and vanillymandelic acid (VMA) with 4-aminoantipyrine (4-AAP) are prepared and characterized. Different physico-chemical techniques namely IR, magnetic and UV-vis spectra are used to investigate the structure of these chelates. Cu(II) forms 1:1 (Cu:DO) and 1:2 (Cu:VMA) chelates. DO behave as a uninegative tridentate ligand in binding to the Cu(II) ion while VMA behaves as a uninegative bidentate ligand. IR spectra show that the DO is coordinated to the Cu(II) ion in a tridentate manner with ONO donor sites of the phenolic- OH, -NH and carbonyl- O, while VMA is coordinated with OO donor sites of the phenolic- OH and -NH. Magnetic moment measurements reveal the presence of Cu(II) chelates in octahedral and square planar geometries with DO and VMA, respectively. The thermal decomposition of Cu(II) complexes is studied using thermogravimetric (TG) and differential thermal analysis (DTA) techniques. The activation thermodynamic parameters, such as, energy of activation, enthalpy, entropy and free energy change of the complexes are evaluated and the relative thermal stability of the complexes are discussed.

  4. Benexate hydrochloride betadex modulates nitric oxide synthesis and cytokine expression in gastric ulcers

    PubMed Central

    Lee, Jae Min; Lim, Ji-Youn; Kim, Yoonjin; Kim, Ye Ji; Choi, Hyuk Soon; Kim, Eun Sun; Keum, Bora; Seo, Yeon Seok; Jeen, Yoon Tae; Lee, Hong Sik; Um, Soon Ho; Kim, Chang Duck; Ryu, Ho Sang; Sul, Donggeun; Hong, Junghwa; Chun, Hoon Jai

    2016-01-01

    The present study investigated benexate hydrochloride betadex (BHB)-mediated ulcer healing, and changes to microcirculation modulated through nitric oxide synthase (NOS) and anti-inflammatory activity. A rat model of gastric mucosal injury was established through injection of a 60% acetic acid solution into the stomach. Following ulcer induction, the rats were administered BHB orally for 5 days at doses of 0, 100, 300 or 1,000 mg/kg. The highest dose of BHB was also administered with or without L-NG-nitroarginine methyl ester (L-NAME). The area of gastric ulcers was determined by planimetry, and expression of cyclooxygenases (COX), cytokines and NOS in stomach tissues were measured using western blotting. Compared with the control group, gastric ulcer size was significantly decreased in the 1,000 mg/kg BHB-treated group (P<0.05). Administration of BHB led to a significant increase in endothelial (e)NOS expression (P<0.05). Although acetic acid co-treatment with L-NAME induced more severe mucosal damage, BHB decreased COX expression and tumor necrosis factor-α levels when administered with the nitric oxide inhibitor, L-NAME (P<0.05). BHB exhibited protective effects in a rat model of gastric ulcers, which were associated with a decrease in pro-inflammatory cytokine levels and the activation of eNOS. PMID:27446246

  5. Ephedrine hydrochloride protects mice from LPS challenge by promoting IL-10 secretion and inhibiting proinflammatory cytokines.

    PubMed

    Zheng, Yuejuan; Guo, Ziyi; He, Weigang; Yang, Yang; Li, Yuhu; Zheng, Aoxiang; Li, Ping; Zhang, Yan; Ma, Jinzhu; Wen, Mingyue; Yang, Muyi; An, Huazhang; Ji, Guang; Yu, Yizhi

    2012-05-01

    Sepsis and its derivative endotoxic shock are still serious conditions with high mortality in the intensive care unit. The mechanisms that ensure the balance of proinflammatory cytokines and anti-inflammatory cytokine production are of particular importance. As an active α- and β-adrenergic agonist, ephedrine hydrochloride (EH) is a widely used agent for cardiovascular diseases, especially boosting blood pressure. Here we demonstrate that EH increased Toll-like receptor 4 (TLR4)-mediated production of interleukin 10 (IL-10) through p38 MAPK activation. Simultaneously, EH negatively regulated the production of proinflammatory cytokines. Consistently, EH increased lipopolysaccharide (LPS)-induced serum IL-10 and inhibited tumor necrotic factor-α (TNFα) production in vivo. As a result, EH treatment protected mice from endotoxic shock by lethal LPS challenge. In brief, our data demonstrated that EH could contribute to immune homeostasis by balancing the production of proinflammatory cytokines and anti-inflammatory cytokine in TLR4 signaling. This study provides a potential usage of EH in autoimmunologic diseases or other severe inflammations.

  6. The behavioral pharmacology of butaclamol hydrochloride (AY-23,028), a new potent neuroleptic drug.

    PubMed

    Voith, K; Herr, F

    1975-04-30

    Butaclamol hydrochloride (AY-23,028) is a member of a new chemical class for which antipsychotic activity in humans has recently been demonstrated. The compound antagonized amphetamine-induced stereotyped behavior in rats, amphetamine toxicity in aggregated mice and apomorphine-induced emesis in dogs. It depressed both discriminated avoidance and continuous lever-pressing behavior in rats and inhibited ambulation and rearing in the open field. At higher doses, AY-23,028 induced catalepsy. Adrenergic blocking activity, measured by the antagonism of epinephrine-induced mortality, was weak. These pharmacological actions are characteristic of neuroleptic drugs. In the dose range where the aforementioned effects were observed AY-23,028 did not antagonize either the tetrabenazine-induced ptosis or the tremorine syndrome and did not cause either hypothermia or ataxia. The potency and onset of action of AY-23,028 were comparable to those of fluphenazine but AY-23,028 was of longer duration. The results are discussed in relation to current concepts of neuroleptic mechanisms.

  7. Alginate/chitosan based bi-layer composite membrane as potential sustained-release wound dressing containing ciprofloxacin hydrochloride

    NASA Astrophysics Data System (ADS)

    Han, Fei; Dong, Yang; Song, Aihua; Yin, Ran; Li, Sanming

    2014-08-01

    The aims of this research were to develop and evaluate a novel ciprofloxacin hydrochloride loaded bi-layer composite membrane based on alginate and chitosan. In vitro antimicrobial activity, drug permeation study, morphology, cytotoxicity, primary skin irritation and in vivo pharmacodynamics were investigated. Results showed that the membranes could inhibit the growth of microorganisms for longer than 7 days. And there was no significant decrease in the metabolic activity of the Hacat fibroblasts cells were treated with the membranes. No edema and erythema were observed after administration of membranes on the rabbit skin after 14 days. Moreover, the results of pharmacodynamics showed that the membranes were more effective in improving the wound healing process. In conclusion, a novel bi-layer composite membrane was developed and results suggested that it could be exploited as sustained-release wound dressings.

  8. Stability-indicating HPTLC determination of ambroxol hydrochloride in bulk drug and pharmaceutical dosage form.

    PubMed

    Jain, P S

    2010-01-01

    A simple, selective, precise, and stability-indicating high-performance thin-layer chromatographic (HPTLC) method for the analysis of ambroxol hydrochloride both as a bulk drug and in formulations was developed and validated. The method employed HPTLC aluminium plates precoated with silica gel 60F-254 as the stationary phase. The solvent system consisted of methanol-triethylamine (4:6 v/v). The system was found to give a compact spot for ambroxol hydrochloride (R(f) value of 0.53 +/- 0.02). Densitometric analysis of ambroxol hydrochloride was carried out in the absorbance mode at 254 nm. The linear regression analysis data for the calibration plots showed good linear relationship with r(2) = 0.9966 +/- 0.0013 with respect to peak area in the concentration range 100-1000 ng/spot. The mean value +/- standard deviation of slope and intercept were 164.85 +/- 0.72 and 1168.3 +/- 8.26 with respect to peak area. The method was validated for precision, recovery, and robustness. The limits of detection and quantitation were 10 and 30 ng/spot, respectively. Ambroxol hydrochloride was subjected to oxidation and thermal degradation. The drug undergoes degradation under oxidation and heat conditions. This indicates that the drug is susceptible to oxidation and heat. Statistical analysis proves that the method is repeatable, selective, and accurate for the estimation of said drug. Stability indicating of new chemical entities is an important part for the drug development of ambroxol hydrochloride and for its estimation in plasma and other biological fluids; the novel Statistical analysis proves that the method is repeatable and selective for the analysis of ambroxol hydrochloride as bulk drug and in pharmaceutical formulations. The proposed developed HPTLC method can be applied for identification and quantitative determination of ambroxol hydrochloride in bulk drug and dosage forms. This work is to determine the purity of the drug available from the various sources by detecting

  9. Microneedle-assisted delivery of verapamil hydrochloride and amlodipine besylate.

    PubMed

    Kaur, Monika; Ita, Kevin B; Popova, Inna E; Parikh, Sanjai J; Bair, Daniel A

    2014-02-01

    The aim of this project was to study the effect of stainless steel solid microneedles and microneedle rollers on percutaneous penetration of verapamil hydrochloride and amlodipine besylate. Verapamil, 2-(3,4-dimethooxyphenyl)-5-[2-(3,4 dimethoxyphenyl)ethyl-methyl-amino]-2-propan-2-yl-pentanenitrile is a calcium channel blocker agent that regulates high blood pressure by decreasing myocardial contractilty, heart rate and impulse conduction. Amlodipine, (R, S)-2-[(2-aminoethoxy) methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1, 4-dihydropyridine, is a calcium channel blocker that is used for the management of hypertension and ischemic heart disease. Passive penetration of verapamil and amlodipine across the skin is low. In vitro studies were performed with microneedle-treated porcine ear skin using vertical static Franz diffusion cells (PermeGear, Hellertown, PA, USA). The receiver chamber contained 5ml of PBS (pH7.4) and was constantly maintained at 37°C temperature with a water circulation jacket. The diffusion area of the skin was 1.77cm(2). The donor compartment was loaded with 1ml of the solution containing 2.5mg/ml of amlodipine besylate. The donor chamber was covered with parafilm to avoid evaporation. Passive diffusion across untreated porcine skin served as control. Aliquots were taken every 2h for 12h and analyzed by liquid chromatography-mass spectrometry. Transcutaneous flux of verapamil increased significantly from 8.75μg/cm(2)/h to 49.96μg/cm(2)/h across microneedle-roller treated porcine skin. Percutaneous flux of amlodipine besylate following the use of stainless steel microneedles was 22.39μg/cm(2)/h. Passive flux for the drug was 1.57μg/cm(2)/h. This enhancement of amlodipine flux was statistically significant. Transdermal flux of amlodipine with microneedle roller was 1.05μg/cm(2)/h in comparison with passive diffusion flux of 0.19μg/cm(2)/h. The difference in flux values was also statistically significant. Stainless

  10. A Double-Blind, Placebo-Controlled Trial of Dexmethylphenidate Hydrochloride and D,l-Threo-Methylphenidate Hydrochloride in Children with Attention-Deficit-Hyperactivity Disorder

    ERIC Educational Resources Information Center

    Wigal, Sharon; Swanson, James M.; Feifel, David; Sangal, R. Bart; Elia, Josephine; Casat, Charles D.; Zeldis, Jerome B.; Conners, C. Keith

    2004-01-01

    Objective: To evaluate the efficacy and safety of dexmethylphenidate hydrochloride (d-MPH, Focalin[TM]) for the treatment of attention-deficit/hyperactivity disorder (ADHD) and to test an a priori hypothesis that d-MPH would have a longer duration of action than d,l-threo-methylphenidate (d,l-MPH). Method: This was a randomized, double-blind study…

  11. Pharmacological properties of 2,3,3a,4,5,6-hexahydro-8-methyl-1H-pyrazino [3,2,1-j,k]carbazol hydrochloride (pirlindole), a new antidepressant.

    PubMed

    Mashkovsky, M D; Andrejeva, N I

    1981-01-01

    The hydrochloride salt of 2,3,3a,4,5,6-hexahydro-8-methyl-1H-pyrazino[3,2,1-j,k]carbazol hydrochloride (pirlindole) exerts pharmacological effects typical of antidepressants. This compound antagonizes the depressant effects of reserpine and tetrabenazine and potentiates the central effects of amphetamine and l-dopa. It also enhances the head-twitch effect of 5-hydroxy-tryptophan, the effects of noradrenaline, adrenaline, serotonin, tyramine on blood pressure as well as the hypertensive and tremor activities of tryptamine. Pirlindole inhibits the neuronal uptake of noradrenaline and exerts reversible, short-lasting anti-MAO activity. It does not possess anti-cholinergic activity. Clinical trials have shown pirlindole to be effective as an antidepressive drug.

  12. Is there any association between imidapril hydrochloride stability profile under dry air conditions and cancer initiation?

    PubMed

    Regulska, Katarzyna; Murias, Marek; Stanisz, Beata; Regulski, Miłosz

    2013-11-18

    Stability study for imidapril hydrochloride (IMD) was performed under stress conditions of increased temperature (T=373 K) and decreased relative air humidity (RH=0%) in order to obtain and identify its degradation product. The degradation sample stored for 15 days under the above environmental conditions was analyzed by LC-MS technique and it was found that the only degradation impurity formed in the course of the investigated drug degradation was IMD diketopiperazine derivative (DKP) which was produced by dehydration and intramolecular cyclization. The kinetics of its formation was analyzed by a revalidated RP-HPLC method and the kinetic model of this reaction was established. It was concluded that the DKP formation follows Prout-Tompkins kinetics with the rate constant k±Δk=2.034±0.157×10(-6) [s(-1)]. The obtained degradation impurity was further assessed with respect to its mutagenic potential using commercial Ames MPF 98/100 microplate format mutagenicity assay kit equipped with Salmonella typhimurium strains TA 98 and TA 100. Both strains were exposed to six concentrations (in a range of 0.16-5.0mg/mL) of DKP in the presence and absence of metabolic activation system. No mutagenic effect was observed confirming that the presence of DKP in IMD final dosage form has no impact on cancer initiation.

  13. Investigation of radiosterilization of Benzydamine Hydrochloride by electron spin resonance spectroscopy

    NASA Astrophysics Data System (ADS)

    Çolak, Şeyda

    2016-10-01

    The use of ionizing radiation for sterilization of pharmaceuticals is an attractive and growing technology. In the present work, the spectroscopic and kinetic features of the radicals induced in gamma irradiated solid Benzydamine Hydrochloride (BH) sample is investigated in the dose range of 3-34 kGy at different temperatures using Electron Spin Resonance (ESR) spectroscopy. Gamma irradiated BH indicated eight resonance peaks centered at g=2.0029 originating from two different radical species. Decay activation energy of the radical mostly responsible from central intense resonance line was calculated to be 25.6±1.5 kJ/mol by using the signal intensity decay data derived from annealing studies performed at high temperatures. A linear function of the applied dose was found to describe best the experimental dose-response data. However, the discrimination of irradiated BH from unirradiated one was possible even 3 months after storage at normal conditions. Basing on these findings it was concluded that BH and BH containing drugs could be safely sterilized by gamma radiation and that ESR spectroscopy could be successfully used as a potential technique for monitoring their radiosterilizations.

  14. Anti-ulcer actions of phytosphingosine hydrochloride in different experimental rat ulcer models.

    PubMed

    Baek, Seung Woo; Kim, Nam Ki; Jin, Hwan-Jun; Koh, Chang-Woong; Kim, Chul Kyung; Kwon, O-Hyep; Kim, Jun-Sung; Cho, Myung-Haing; Park, Chan-Koo

    2005-01-01

    The gastroprotective activity of phytosphingosine hydrochloride (PS-HCl, CAS 554-62-1) was assessed in four different rat models of experimentally induced gastric ulcer. Various doses (2.5-10 mg/kg) of PS-HCI were orally administered to rats 30 min before the treatment with HCl/ethanol, indometacin, cysteamine, or to rats with ligated pylorus. Oral administration of PS-HCl (2.5-10 mg/kg) to rats prevented the acute ulcer formation in 4 different types of ulcer in a dose-dependent manner as follows: (1) HCl/ethanol-induced gastric mucosal membrane lesions (20.1-47.8% inhibition), (2) indometacin-induced gastric mucosal membrane lesions (4.6-31.9% inhibition), (3) duodenal ulcer induced by cysteamine (10-20% inhibition), (4) gastric secretion and ulceration following pylorus ligation (33.3-61.9% inhibition). These results indicate that PS-HCI may be useful for the prevention of gastric ulcer.

  15. The In vitro/vivo Evaluation of Prepared Gastric Floating Tablets of Berberine Hydrochloride.

    PubMed

    Ji, Jun; He, Xin; Yang, Xiao-Lin; Du, Wen-Juan; Cui, Cheng-Long; Wang, Ling; Wang, Xue; Zhang, Chun-Feng; Guo, Chang-Run

    2016-12-29

    Currently available antiulcer drugs suffered from serious side effects which limited their uses and prompted the need for a safe and efficient new antiulcer agent. The objective of this project work was to retain the drug in the stomach for better antiulcer activity and less side effects. Hence, the aim of our present work was to prepare a gastric floating tablet of Berberine hydrochloride (Ber) with suitable in vitro/vivo properties. In this study, different Ber gastric floating tablets were prepared by simple direct compression using various amounts of HPMCK15M and Carbopol 971PNF combined with other tablet excipients. The properties of the tablets including hardness, buoyancy, swelling ability, in vitro drug release, and in vivo pharmacokinetic study were evaluated. The obtained results disclosed that hardness, floating, swelling, and in vitro drug release of the Ber tablets depended mainly on the ratio of polymer combinations. Moreover, among six formulations, F3 exhibited desirable floating, swelling, and extended drug release. In addition, in vivo pharmacokinetic study suggested that prepared gastric floating tablets had significantly sustained-releasing effects compared with market tablets. Therefore, the developed gastric floating tablets of Ber could be an alternative dosage form for treatment of gastrointestinal disease.

  16. A new simple electrochemical Moxifloxacin Hydrochloride sensor built on carbon paste modified with silver nanoparticles.

    PubMed

    Fekry, Amany M

    2017-01-15

    A new sensitive simple electrochemical sensor for Moxifloxacin Hydrochloride (MOXI) detection has been successfully performed. The sensor built on carbon paste (CP) modified with silver nanoparticles (AgNPs). AgNPs are biocompatible stable noble materials especially in biological sensing. The silver nanoparticles modified carbon paste electrode (SNMCPE) displayed high electrocatalytic activity towards oxidation of 1.0mM MOXI in Britton Robinson (BR) buffer of pH range (2.0-9.0). The techniques used to do this work are cyclic voltammetry (CV), linear sweep voltammetry (LSV), chronoamperometry (CA) and electrochemical impedance spectroscopy (EIS). Surface characteristics were achieved using scanning electron microscopic (SEM) and Energy Dispersive X-Ray Analysis (EDX) techniques. The effect of changing MOXI concentration (7.0×10(-7) to 1.8×10(-4)M) was studied in BR buffer (pH =7.4) at a scan rate of 50mV/s using SNMCPE. The detection and quantification limits were found to be 2.9×10(-9)M and 9.6×10(-8)M, respectively. In order to assess the applicability of MOXI detection method in real samples; this method was tested in Delmoxa tablet and human urine sample. Good sensible results were attained for MOXI detection.

  17. Spectroscopic and quantum chemical analysis of a natural product - Hayatin hydrochloride

    NASA Astrophysics Data System (ADS)

    Mishra, Rashmi; Srivastava, Anubha; Tandon, Poonam; Jain, Sudha

    2015-08-01

    Majority of drugs in use today are natural products, natural product mimics or semi synthetic derivatives. Therefore in recent times, focus on plant research has increased all over the world and large body of evidence has been collected to show immense potential of medicinal plants used in various traditional systems. Therefore, in the present communication to aid that research, structural and spectroscopic analysis of a natural product, an alkaloid Hayatin hydrochloride was performed. Both ab initio Hartree-Fock and density functional theory employing B3LYP with complete relaxation in the potential energy surface using 6-311G (d,p) basis set were used for the calculations. The vibrational frequencies were calculated and scaled values were compared with experimental FT-IR and micro-Raman spectra. The complete assignments were performed on the basis of potential energy distribution. The structure-activity relationship has also been interpreted by mapping electrostatic potential surface, which are valuable information for the quality control of medicines and drug-receptor interactions. Electronic properties have been analysed employing TD-DFT for both gaseous and solvent phase. The calculated HOMO and LUMO energies show that charge transfer occurs within the molecule. Stability of the molecule arising from hyper conjugative interactions, charge delocalization has been analyzed using natural bond orbital (NBO) analysis.

  18. Multifunctional liposomes for nasal delivery of the anti-Alzheimer drug tacrine hydrochloride.

    PubMed

    Corace, Giuseppe; Angeloni, Cristina; Malaguti, Marco; Hrelia, Silvana; Stein, Paul C; Brandl, Martin; Gotti, Roberto; Luppi, Barbara

    2014-12-01

    The purpose of this study was the development of multifunctional liposomes for nasal administration of tacrine hydrochloride. Liposomes were prepared using traditional excipients (cholesterol and phosphatidylcholine), partly enriched with α-tocopherol and/or Omega3 fatty acids. This approach was chosen in order to obtain at the same time two positive results: an enhanced drug permeation through nasal mucosa and a concomitant neuroprotective effect. Several liposome formulations were prepared using the Reverse Phase Evaporation technique followed by membrane filter extrusion. In particular, liposome capacity to enhance drug permeation was evaluated by means of membrane permeation and cellular uptake studies. Furthermore, liposome effect on neuronal viability and intracellular ROS production was evaluated as well as their cytoprotective effect against oxidative stress. All liposome formulations showed a mean diameter in the range of 175 nm to 219 nm with polydispersity index lower than 0.22, a lightly negative zeta potential and excellent encapsulation efficiency. Moreover, along with good mucoadhesive properties, multifunctional liposomes showed a markedly increase in tacrine permeability, which can be related to liposome fusion with cellular membrane, a hypothesis, which was also supported by cellular uptake studies. Finally, the addition of α-tocopherol without Omega3 fatty acids, was found to increase the neuroprotective activity and antioxidant properties of liposomes.

  19. A degradation study of cefepime hydrochloride in solutions under various stress conditions by TLC-densitometry.

    PubMed

    Dąbrowska, Monika; Starek, Małgorzata; Krzek, Jan; Papp, Elżbieta; Król, Piotr

    2015-03-01

    A rapid, accurate and sensitive thin-layer chromatography (TLC) method with densitometric detection has been developed and validated for the determination of cefepime in pharmaceuticals. Chromatographic separation was achieved on a silica gel TLC F254 plates with a mobile phase consisting of ethanol-2-propanol-glacial acetic acid 99.5%-water (4:4:1:3, v/v). Densitometric detection was carried out at wavelength of 266 nm in reflectance/absorbance mode. The validation of the method was found to be satisfactory with high accuracy (from 99.24 to 101.37%) and precision (RSD from 0.06 to 0.36%). Additionally, the stability of cefepime in solution was investigated, including the effect of pH, temperature and incubation time. Favorable retention parameters (Rf , Rs, α) were obtained under the developed conditions, which guaranteed good separation of the studied components. The degradation process of cefepime hydrochloride was described by kinetic and thermodynamic parameters (k, t0.1 , t0.5 and Ea ). Moreover, the chemical properties of degradation products were characterized by the Rf values, absorption spectra, HPLC-MS/MS and TLC-densitometry analysis. As the method could effectively separate the active substance from its main degradation product (1-methylpyrrolidine), it can be employed as a method to indicate the stability of this drug.

  20. Cryogenic terahertz spectrum of (+)-methamphetamine hydrochloride and assignment using solid-state density functional theory.

    PubMed

    Hakey, Patrick M; Allis, Damian G; Ouellette, Wayne; Korter, Timothy M

    2009-04-30

    The cryogenic terahertz spectrum of (+)-methamphetamine hydrochloride from 10.0 to 100.0 cm(-1) is presented, as is the complete structural analysis and vibrational assignment of the compound using solid-state density functional theory. This cryogenic investigation reveals multiple spectral features that were not previously reported in room-temperature terahertz studies of the title compound. Modeling of the compound employed eight density functionals utilizing both solid-state and isolated-molecule methods. The results clearly indicate the necessity of solid-state simulations for the accurate assignment of solid-state THz spectra. Assignment of the observed spectral features to specific atomic motions is based on the BP density functional, which provided the best-fit solid-state simulation of the experimental spectrum. The seven experimental spectral features are the result of thirteen infrared-active vibrational modes predicted at a BP/DNP level of theory with more than 90% of the total spectral intensity associated with external crystal vibrations.

  1. Effects of a new centrally acting muscle relaxant, NK433 (lanperisone hydrochloride) on spinal reflexes.

    PubMed

    Sakitama, K; Ozawa, Y; Aoto, N; Tomita, H; Ishikawa, M

    1997-10-22

    (-)-(R)-2-methyl-3-(1-pyrrolidinyl)-4'-trifluoromethylpropiophenone++ + monohydrochloride, lanperisone hydrochloride (NK433) administered intravenously or orally depressed the mono- and polysynaptic reflex potential, dorsal root reflex potential, flexor reflex mediated by group II afferent fibers, patellar and flexor reflexes. These effects were reduced by spinal transection. NK433 inhibited the facilitation of the flexor reflex mediated by group II afferent fibers that was induced by intrathecal administration of noradrenaline-HCl. (+)-(1R,2R)-2-methyl-3-(1-pyrrolidinyl)-1-(4-trifluoromethylphenyl)-1-pr opanol (LPS-9)-HCl, a metabolite of NK433, also inhibited the spinal reflexes. Given orally, NK433 had effects more than three times stronger and tending to be longer-lasting than those of eperisone-HCl. These results suggest that NK433 exerts a non-selective inhibition on spinal reflexes and that inhibition of the descending noradrenergic tonic facilitation within the spinal cord is involved in the mechanism of spinal reflex depression by NK433. LPS-9 could contribute to the potent activity of NK433 after oral administration.

  2. Ranitidine Hydrochloride-loaded Ethyl Cellulose and Eudragit RS 100 Buoyant Microspheres: Effect of pH Modifiers

    PubMed Central

    Kotagale, N. R.; Parkhe, A. P.; Jumde, A. B.; Khandelwal, H. M.; Umekar, M. J.

    2011-01-01

    A floating type of dosage form of ranitidine hydrochloride in the form of microspheres capable of floating on simulated gastric fluid was prepared by solvent evaporation technique. Microspheres prepared with ethyl cellulose, Eudragit® RS100 alone or in combination were evaluated for percent yield, drug entrapment, percent buoyancy and drug release and the results demonstrated satisfactory performance. Microspheres exhibited ranitidine hydrochloride release influenced by changing ranitidine hydrochloride-polymer and ranitidine hydrochloride-polymer-polymer ratio. Incorporation of a pH modifier has been the usual strategy employed to enhance the dissolution rate of weakly basic drug from floating microspheres. Further citric acid, fumaric acid, tartaric acid were employed as pH modifiers. Microspheres prepared with ethyl cellulose, Eudragit® RS100 and their combination that showed highest release were utilized to study the effect of pH modifiers on ranitidine hydrochloride release from microspheres which is mainly affected due to modulation of microenvironmental pH. In vitro release of ranitidine hydrochloride from microspheres into simulated gastric fluid at 37° showed no significant burst effect. However the amount of release increased with time and significantly enhanced by pH modifiers. 15% w/w concentration of fumaric acid provide significant drug release from ranitidine hydrochloride microspheres prepared with ranitidine hydrochloride:ethyl cellulose (1:3), ranitidine hydrochloride:Eudragit® RS100 (1:2) and ranitidine hydrochloride:ethyl cellulose:Eudragit® RS100 (1:2:1) whereas citric acid, tartaric acid showed significant cumulative release at 20% w/w. In all this study suggest that ethyl celluose, Eudragit® RS100 alone or in combination with added pH modifiers can be useful in floating microspheres which can be proved beneficial to enhance the bioavailability of ranitidine hydrochloride. PMID:23112396

  3. Release Kinetics of Papaverine Hydrochloride from Tablets with Different Excipients

    PubMed Central

    Kasperek, Regina; Polski, Andrzej; Zimmer, Łukasz; Poleszak, Ewa

    2014-01-01

    Abstract The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, (3-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release. PMID:25853076

  4. Release kinetics of papaverine hydrochloride from tablets with different excipients.

    PubMed

    Kasperek, Regina; Polski, Andrzej; Zimmer, Łukasz; Poleszak, Ewa

    2014-01-01

    The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, (3-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release.

  5. Echocardiographic reference values in healthy cats sedated with ketamine hydrochloride.

    PubMed

    Fox, P R; Bond, B R; Peterson, M E

    1985-07-01

    An M-mode echocardiographic examination was performed in a consistent manner in 30 clinically healthy cats under light ketamine hydrochloride sedation. There was a significant linear relationship between increasing body size and increasing cardiac dimensions for several echocardiographic values. Positive correlation existed between body weight and body surface area with aortic root, left ventricular caudal wall thickness (LVCW), interventricular septal thickness (IVS), IVS/LVCW, and mean velocity of circumferential fiber shortening (Vcf); there was a negative correlation between body weight and body surface area with left ventricular ejection time (LVET). Body surface area also correlated positively with percentage of ventricular minor axis dimensional change (% delta D). Positive correlations were recorded between left ventricular end-diastolic dimension (LVEDD) and left ventricular endsystolic dimension (LVESD), LVESD and LVET, LVCW and IVS, LVET (calculated by LVCW motion) and LVET (calculated by aortic valve motion), % delta D and Vcf, heart rate and Vcf, and Vcf (calculated using aortic valve motion to compute LVET) and Vcf (using LVCW motion to compute LVET). There were negative correlations between LVEDD and % delta D, LVEDD and Vcf, LVESD and Vcf, LVET and Vcf, LVET and heart rate, LVET and % delta D. Significant differences were recorded between means of echocardiographic reference values generated in this and other studies, except for LVESD.

  6. Flow injection chemiluminescence determination of naphazoline hydrochloride in pharmaceuticals.

    PubMed

    Iranifam, Mortaza; Sorouraddin, Mohammad H

    2014-02-01

    A simple and sensitive flow injection chemiluminescence (FI-CL) method was developed for the determination of naphazoline hydrochloride (NPZ). The method is based on the enhancing effect of NPZ on the weak CL signal from the reaction of KIO4 with H2 O2 . Experimental parameters that affected the CL signal, including the pH of the KIO4 solution, concentrations of KIO4 , H2 O2 and disodium-EDTA and flow rate were optimized. Under the optimum conditions, the increment of CL intensity was linearly proportional to the concentration of NPZ in the range 5.0 × 10(-6) to 70 × 10(-6) mol/L. The detection limit was 1.0 × 10(-6) mol/L and the relative standard deviation for 50 × 10(-6) mol/L NPZ solution was 2.8% (n = 11). In addition, a high throughput of 120 samples/h was achieved. The utility of this method was demonstrated by determining NPZ in pharmaceuticals.

  7. Trans-ungual delivery of itraconazole hydrochloride by iontophoresis.

    PubMed

    Kushwaha, Avadhesh; Jacob, Melissa; Shiva Kumar, H N; Hiremath, Shobharani; Aradhya, Sacchidanand; Repka, Michael A; Murthy, S Narasimha

    2015-01-01

    Itraconazole (ITR) is a potent antifungal drug. However, poor aqueous solubility limits its permeation ability across the human nail plate. Therefore, in this project, ITR was converted to hydrochloride salt (ITR-HCl) to improve its solubility and to render it amenable to iontophoresis. ITR-HCl was characterized by spectroscopic methods and antifungal efficacy was evaluated in comparison to the base. In vitro and ex vivo transport studies (passive and iontophoresis) were carried out across the porcine hoof membrane and excised human cadaver toe using two different protocols; continuous delivery of drug for 24 h and pulsed delivery of drug for 3 days (8 h/day). The antifungal efficacy of ITR-HCL was comparable to ITR. Iontophoresis was found to be more effective than passive mode of delivery of ITR-HCL. In both iontophoresis as well as passive mode of delivery, the pulsed protocol resulted in more ungual and trans-ungual delivery of drug than continuous protocol. ITR-HCL could be delivered into and across the nail plate by iontophoresis. Human cadaver toe appears to be a good model to investigate the ungual delivery of drugs.

  8. Facile colorimetric methods for the quantitative determination of tetramisole hydrochloride

    NASA Astrophysics Data System (ADS)

    Amin, A. S.; Dessouki, H. A.

    2002-10-01

    A facile, rapid and sensitive methods for the determination of tetramisole hydrochloride in pure and in dosage forms are described. The procedures are based on the formation of coloured products with the chromogenic reagents alizarin blue BB (I), alizarin red S (II), alizarin violet 3R (III) and alizarin yellow G (IV). The coloured products showed absorption maxima at 605, 468, 631 and 388 nm for I-IV, respectively. The colours obtained were stable for 24 h. The colour system obeyed Beer's law in the concentration range 1.0-36, 0.8-32, 1.2-42 and 0.8-30 μg ml -1, respectively. The results obtained showed good recoveries with relative standard deviations of 1.27, 0.96, 1.13 and 1.35%, respectively. The detection and determination limits were found to be 1.0 and 3.8, 1.2 and 4.2, 1.0 and 3.9 and finally 1.4 and 4.8 ng ml -1 for I-IV complexes, respectively. Applications of the method to representative pharmaceutical formulations are represented and the validity assessed by applying the standard addition technique, which is comparable with that obtained using the official method.

  9. Cinchocaine hydrochloride determination by atomic absorption spectrometry and spectrophotometry.

    PubMed

    Abdel-Ghani, Nour T; Youssef, Ahmed F A; Awady, Mohamed A

    2005-05-01

    Two sensitive spectrophotometric and atomic absorption spectrometric procedures have been developed for determination of cinchocaine hydrochloride (Cin.Cl) in pure form and in pharmaceutical formulation. The spectrophotometric method was based on formation of an insoluble colored ion-associate between the cited drug and tetrathiocyanatocobaltate (CoTC) or hexathiocyanatochromate (CrTC) which dissolved and extracted in an organic solvent. The optimal experimental conditions for quantitative extraction such as pH, concentration of the reagents and solvent were studied. Toluene and iso-butyl alcohol proved to be the most suitable solvents for quantitative extraction of Cin-CoTC and Cin-CrTC ion-associates with maximum absorbance at 620 and 555 nm, respectively. The optimum concentration ranges, molar absorptivities, Ringbom ranges and Sandell sensitivities were also evaluated. The atomic absorption spectrometric method is based on measuring of the excess cobalt or chromium in the aqueous solution, after precipitation of the drug, at 240.7 and 357.9 nm, respectively. Linear application ranges, characteristic masses and detection limits were 57.99-361.9, 50.40 and 4.22 microg ml(-1) of Cin.Cl, in case of CoTC, while 37.99-379.9, 18.94 and 0.81 microg ml(-1) in case of CrTC.

  10. Conformation and interactions of dopamine hydrochloride in solution

    SciTech Connect

    Callear, Samantha K.; Imberti, Silvia; Johnston, Andrew; McLain, Sylvia E.

    2015-01-07

    The aqueous solution of dopamine hydrochloride has been investigated using neutron and X-ray total scattering data together with Monte-Carlo based modelling using Empirical Potential Structure Refinement. The conformation of the protonated dopamine molecule is presented and the results compared to the conformations found in crystal structures, dopamine-complexed protein crystal structures and predicted from theoretical calculations and pharmacophoric models. It is found that protonated dopamine adopts a range of conformations in solution, highlighting the low rotational energy barrier between different conformations, with the preferred conformation being trans-perpendicular. The interactions between each of the species present (protonated dopamine molecules, water molecules, and chloride anions) have been determined and are discussed with reference to interactions observed in similar systems both in the liquid and crystalline state, and predicted from theoretical calculations. The expected strong hydrogen bonds between the strong hydrogen bond donors and acceptors are observed, together with evidence of weaker CH hydrogen bonds and π interactions also playing a significant role in determining the arrangement of adjacent molecules.

  11. Effects of ractopamine hydrochloride and zilpaterol hydrochloride supplementation on longissimus muscle shear force and sensory attributes of beef steers.

    PubMed

    Arp, T S; Howard, S T; Woerner, D R; Scanga, J A; McKenna, D R; Kolath, W H; Chapman, P L; Tatum, J D; Belk, K E

    2013-12-01

    Effect of ractopamine hydrochloride (RH) and zilpaterol hydrochloride (ZH) on LM shear force and sensory attributes was determined using pens (n = 40) British × Continental crossbred steers randomly allocated to one of the following treatments: control; RH fed at 200 (RH 200) or 300 mg • steer(-1) • d(-1) (RH 300), or 400 mg • steer(-1) • d(-1) (RH 400) top-dressed for the final 30 d of feeding; or ZH fed at 7.5 mg/kg, beginning 23 d before slaughter with a 3-d withdrawal. Two replicates (pens) per treatment were represented in four blocks. Eighteen carcasses per pen were randomly selected and one 5-cm LM sample was removed from both carcass sides to be used for shear force and sensory evaluation. Samples were aged for 14 d, frozen at -28.8 °C, and cut into 2.5-cm steaks. All steaks were cooked to an internal temperature of 71.1 °C before being evaluated for Warner-Bratzler shear force (WBSF), slice shear force (SSF), or being fed to trained sensory panelists. Increasing dose and potency of β-agonist increased WBSF by 4 to 17% and SSF by 5 to 24% (P < 0.05). Steaks from steers fed ZH had higher WBSF and SSF values compared with all other treatments (P < 0.05), whereas steaks from controls and steers fed RH 200 were not different (P > 0.05). Probability of steaks failing to meet shear force standards to be certified tender (WBSF <4.4 kg, SSF < 20 kg) was increased from an initial probability of <0.06 in steaks from steers in the control treatment to 0.10 to 0.20 in steers fed RH 400 or ZH (P < 0.05). No difference was detected in panel ratings for overall tenderness of steaks from steers fed RH 200 compared with controls (P > 0.05). Steaks from steers fed RH 300 and RH 400 were comparable for all sensory attributes; however, both RH 300 and RH 400 were rated lower for overall tenderness than controls (P < 0.05). Panelists failed to detect differences in overall tenderness of steaks from steers fed RH 400 and ZH (P < 0.05). Panelists detected no

  12. Interaction of polyhexamethylene biguanide hydrochloride (PHMB) with phosphatidylcholine containing o/w emulsion and consequences for microbicidal efficacy and cytotoxicity.

    PubMed

    Müller, Gerald; Koburger, Torsten; Kramer, Axel

    2013-01-25

    Oil-in-water (o/w) emulsions containing egg yolk phosphatidylcholine (EPC) were combined with aqueous polyhexamethylene biguanide hydrochloride (PHMB). The PHMB concentration in the aqueous phase was estimated by filtration centrifugation experiments. In parallel, PHMB concentration was assessed utilizing cytotoxicity assays (neutral red) on cultured murine fibroblasts (L929 cells) and tests of bactericidal efficacy on either Pseudomonas aeruginosa or Staphylococcus aureus. Biological tests were performed in cell culture medium. Filtration centrifugation experiments demonstrated much higher aqueous PHMB concentrations than did the assays for biologically effective PHMB. Therefore, biological test systems should preferably be used to verify effective PHMB concentrations. Tests of microbicidal efficacy in which the same 0.05% PHMB o/w emulsion was re-used 8 times revealed a drug delivery system activated by the presence of test bacteria.

  13. Fabrication and photoelectric response of poly(allylamine hydrochloride)/PM thin films by layer-by-layer deposition technique.

    PubMed

    Chu, Jinfang; Li, Xingchang; Zhang, Jianping; Tang, Ji'an

    2003-05-23

    Thin films of poly(allylamine hydrochloride) (PAH) and bacteriorhodopsin (bR) embedded in purple membrane (PM) have been prepared by layer-by-layer (LBL) self-assembly technique. The results obtained by UV-Vis spectroscopy and atomic force microscopy (AFM) analysis showed that the biological activity of bR was preserved and PM fragments could be well oriented onto the ITO substrate. A photo-electrochemical cell with the structure of ITO/(PAH/PM)(n)/electrolyte (0.5M KCl)/Pt was fabricated and studied. The photocurrent peaks of (PAH/PM)(6) corresponding to light-on and light-off were about 200 and 100 nA/cm(2), respectively, with the former enhanced 30% higher than that of the reference films made of (PDAC/PM)(6).

  14. Beneficial Effect of Sugar Osmolytes on the Refolding of Guanidine Hydrochloride-Denatured Trehalose-6-phosphate Hydrolase from Bacillus licheniformis

    PubMed Central

    Chen, Jiau-Hua; Chi, Meng-Chun; Lin, Min-Guan; Lin, Long-Liu; Wang, Tzu-Fan

    2015-01-01

    The influence of three sugar osmolytes on the refolding of guanidine hydrochloride- (GdnHCl-) denatured trehalose-6-phosphate hydrolase of Bacillus licheniformis (BlTreA) was studied by circular dichroism (CD) spectra, fluorescence emission spectra, and the recovery of enzymatic activity. These experimental results clearly indicated that sorbitol, sucrose, and trehalose at a concentration of 0.75 M improved the refolding yields of GdnHCl-denatured  BlTreA, probably due to the fact that these sugars favored the formation of tertiary architectures. Far-UV CD measurements demonstrated the ability of sugar osmolytes to shift the secondary structure of GdnHCl-denatured enzyme towards near-native conformations. ANS fluorescence intensity measurements revealed a reduction of exposed hydrophobic surfaces upon the treatment of denatured enzyme with sugar osmolytes. These observations suggest that sugar osmolytes possibly play a chaperone role in the refolding of chemically denatured BlTreA. PMID:25667926

  15. Beneficial effect of sugar osmolytes on the refolding of guanidine hydrochloride-denatured trehalose-6-phosphate hydrolase from Bacillus licheniformis.

    PubMed

    Chen, Jiau-Hua; Chi, Meng-Chun; Lin, Min-Guan; Lin, Long-Liu; Wang, Tzu-Fan

    2015-01-01

    The influence of three sugar osmolytes on the refolding of guanidine hydrochloride- (GdnHCl-) denatured trehalose-6-phosphate hydrolase of Bacillus licheniformis (BlTreA) was studied by circular dichroism (CD) spectra, fluorescence emission spectra, and the recovery of enzymatic activity. These experimental results clearly indicated that sorbitol, sucrose, and trehalose at a concentration of 0.75 M improved the refolding yields of GdnHCl-denatured  BlTreA, probably due to the fact that these sugars favored the formation of tertiary architectures. Far-UV CD measurements demonstrated the ability of sugar osmolytes to shift the secondary structure of GdnHCl-denatured enzyme towards near-native conformations. ANS fluorescence intensity measurements revealed a reduction of exposed hydrophobic surfaces upon the treatment of denatured enzyme with sugar osmolytes. These observations suggest that sugar osmolytes possibly play a chaperone role in the refolding of chemically denatured BlTreA.

  16. Pharmacokinetics of hydromorphone hydrochloride after intravenous and intramuscular administration of a single dose to American kestrels (Falco sparverius)

    USGS Publications Warehouse

    Guzman, David Sanchez-Migallon; KuKanich, Butch; Drazenovich, Tracy L.; Olsen, Glenn H.; Paul-Murphy, Joanne R.

    2014-01-01

    Results indicated hydromorphone hydrochloride had high bioavailability and rapid elimination after IM administration, with a short terminal half-life, rapid plasma clearance, and large volume of distribution in American kestrels. Further studies regarding the effects of other doses, other administration routes, constantrate infusions, and slow release formulations on the pharmacokinetics of hydromorphone hydrochloride and its metabolites in American kestrels may be indicated.

  17. 40 CFR 180.558 - N,N-diethyl-2-(4-methylbenz-yloxy)ethylamine hydrochloride; tolerances for residues.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ...)ethylamine hydrochloride; tolerances for residues. 180.558 Section 180.558 Protection of Environment... RESIDUES IN FOOD Specific Tolerances § 180.558 N,N-diethyl-2-(4-methylbenz-yloxy)ethylamine hydrochloride; tolerances for residues. (a) General. A tolerance for residues of the plant growth regulator...

  18. Stability-indicating HPLC Method for Simultaneous Determination of Terbutaline Sulphate, Bromhexine Hydrochloride and Guaifenesin

    PubMed Central

    Porel, A.; Haty, Sanjukta; Kundu, A.

    2011-01-01

    The aim of the present study was the development and subsequent validation of a simple, precise and stability-indicating reversed phase HPLC method for the simultaneous determination of guaifenesin, terbutaline sulphate and bromhexine hydrochloride in the presence of their potential impurities in a single run. The photolytic as well as hydrolytic impurities were detected as 3,5-dihydroxybenzoic acid, 3,5-dihydroxybenzaldehyde, 1-(3,5-dihydroxyphenyl)-2-[(1,1-dimethylethyl) amino]-ethanone from terbutaline, 2-methoxyphenol and an unknown impurity identified as (2RS)-3-(2-hydroxyphenoxy)-propane-1,2-diol from guaifenesin. The chromatographic separation of all the three active components and their impurities was achieved on Wakosil II column, using phosphate buffer (pH 3.0) and acetonitrile as mobile phase which was delivered initially in the ratio of 80:20 (v/v) for 18 min, then changed to 60:40 (v/v) for next 12 min, and finally equilibrated back to 80:20 (v/v) for 10 min. Other HPLC parameters were: Flow rate at 1.0 ml/min, detection wavelengths 248 and 280 nm, injection volume 10 μl. The calibration graphs plotted with five concentrations of each component were linear with a regression coefficient R2 >0.9999. The limit of detection and limit of quantitation were estimated for all the five impurities. The established method was then validated for linearity, precision, accuracy, and specificity and demonstrated to be applicable to the determination of the active ingredients in commercial and model cough syrup. No interference from the formulation excipients was observed. These results suggest that this LC method can be used for the determination of multiple active ingredients and their impurities in a cough and cold syrup. PMID:22131621

  19. Stability-indicating HPLC Method for Simultaneous Determination of Terbutaline Sulphate, Bromhexine Hydrochloride and Guaifenesin.

    PubMed

    Porel, A; Haty, Sanjukta; Kundu, A

    2011-01-01

    The aim of the present study was the development and subsequent validation of a simple, precise and stability-indicating reversed phase HPLC method for the simultaneous determination of guaifenesin, terbutaline sulphate and bromhexine hydrochloride in the presence of their potential impurities in a single run. The photolytic as well as hydrolytic impurities were detected as 3,5-dihydroxybenzoic acid, 3,5-dihydroxybenzaldehyde, 1-(3,5-dihydroxyphenyl)-2-[(1,1-dimethylethyl) amino]-ethanone from terbutaline, 2-methoxyphenol and an unknown impurity identified as (2RS)-3-(2-hydroxyphenoxy)-propane-1,2-diol from guaifenesin. The chromatographic separation of all the three active components and their impurities was achieved on Wakosil II column, using phosphate buffer (pH 3.0) and acetonitrile as mobile phase which was delivered initially in the ratio of 80:20 (v/v) for 18 min, then changed to 60:40 (v/v) for next 12 min, and finally equilibrated back to 80:20 (v/v) for 10 min. Other HPLC parameters were: Flow rate at 1.0 ml/min, detection wavelengths 248 and 280 nm, injection volume 10 μl. The calibration graphs plotted with five concentrations of each component were linear with a regression coefficient R(2) >0.9999. The limit of detection and limit of quantitation were estimated for all the five impurities. The established method was then validated for linearity, precision, accuracy, and specificity and demonstrated to be applicable to the determination of the active ingredients in commercial and model cough syrup. No interference from the formulation excipients was observed. These results suggest that this LC method can be used for the determination of multiple active ingredients and their impurities in a cough and cold syrup.

  20. Efficacy and safety of vortioxetine (Lu AA21004), 15 and 20 mg/day: a randomized, double-blind, placebo-controlled, duloxetine-referenced study in the acute treatment of adult patients with major depressive disorder

    PubMed Central

    Loft, Henrik; Olsen, Christina Kurre

    2014-01-01

    This study assessed the efficacy, tolerability and safety of vortioxetine versus placebo in adults with recurrent major depressive disorder. This double-blind, randomized, placebo-controlled study included 608 patients [Montgomery–Åsberg Depression Rating Scale (MADRS) total score≥26 and Clinical Global Impression – Severity score≥4]. Patients were randomly assigned (1 : 1 : 1 : 1) to vortioxetine 15 mg/day, vortioxetine 20 mg/day, duloxetine 60 mg/day or placebo. The primary efficacy endpoint was change from baseline in MADRS total score at week 8 (mixed model for repeated measurements). Key secondary endpoints were: MADRS responders; Clinical Global Impression – Improvement scale score; MADRS total score in patients with baseline Hamilton Anxiety Rating Scale ≥20; remission (MADRS≤10); and Sheehan Disability Scale total score at week 8. On the primary efficacy endpoint, both vortioxetine doses were statistically significantly superior to placebo, with a mean difference to placebo (n=158) of −5.5 (vortioxetine 15 mg, P<0.0001, n=149) and −7.1 MADRS points (vortioxetine 20 mg, P<0.0001, n=151). Duloxetine (n=146) separated from placebo, thus validating the study. In all key secondary analyses, both vortioxetine doses were statistically significantly superior to placebo. Vortioxetine treatment was well tolerated; common adverse events (incidence≥5%) were nausea, headache, diarrhea, dry mouth and dizziness. No clinically relevant changes were seen in clinical safety laboratory values, weight, ECG or vital signs parameters. Vortioxetine was efficacious and well tolerated in the treatment of patients with major depressive disorder. PMID:24257717

  1. Efficacy and safety of vortioxetine (Lu AA21004), 15 and 20 mg/day: a randomized, double-blind, placebo-controlled, duloxetine-referenced study in the acute treatment of adult patients with major depressive disorder.

    PubMed

    Boulenger, Jean-Philippe; Loft, Henrik; Olsen, Christina Kurre

    2014-05-01

    This study assessed the efficacy, tolerability and safety of vortioxetine versus placebo in adults with recurrent major depressive disorder. This double-blind, randomized, placebo-controlled study included 608 patients [Montgomery-Åsberg Depression Rating Scale (MADRS) total score ≥ 26 and Clinical Global Impression - Severity score ≥ 4]. Patients were randomly assigned (1 : 1 : 1 : 1) to vortioxetine 15 mg/day, vortioxetine 20 mg/day, duloxetine 60 mg/day or placebo. The primary efficacy endpoint was change from baseline in MADRS total score at week 8 (mixed model for repeated measurements). Key secondary endpoints were: MADRS responders; Clinical Global Impression - Improvement scale score; MADRS total score in patients with baseline Hamilton Anxiety Rating Scale ≥ 20; remission (MADRS ≤ 10); and Sheehan Disability Scale total score at week 8. On the primary efficacy endpoint, both vortioxetine doses were statistically significantly superior to placebo, with a mean difference to placebo (n = 158) of -5.5 (vortioxetine 15 mg, P < 0.0001, n = 149) and -7.1 MADRS points (vortioxetine 20 mg, P < 0.0001, n = 151). Duloxetine (n = 146) separated from placebo, thus validating the study. In all key secondary analyses, both vortioxetine doses were statistically significantly superior to placebo. Vortioxetine treatment was well tolerated; common adverse events (incidence ≥ 5%) were nausea, headache, diarrhea, dry mouth and dizziness. No clinically relevant changes were seen in clinical safety laboratory values, weight, ECG or vital signs parameters. Vortioxetine was efficacious and well tolerated in the treatment of patients with major depressive disorder.

  2. Identification of impurities and statistical classification of methamphetamine hydrochloride drugs seized in the China

    PubMed Central

    Zhang, Jian Xin; Zhang, Da Ming; Han, Xu Guang

    2008-01-01

    A total of 48 methamphetamine hydrochloride samples from eight seizures were analyzed using gas chromatography–mass spectrometry (GC–MS) and a flame ionization detector (GC–FID). Major impurities detected include 1,2-dimethyl-3-phenylaziridine, Ephedrine/pseudoephedrine, 1,3-dimethyl-2-phenylnaphthalene, 1-benzyl-3-methylnaphthalene. These data are suggestive of ephedrine/pseudoephedrine as the main precursor of the methamphetamine hydrochloride samples seized during 2006–2007. Additionally the presence of 1,3-dimethyl-2-phenylnaphthalene, 1-benzyl-3-methylnaphthalene is indicative that six seizures were synthesized via the more specific ephedrine/hydriodic acid/red phosphorus method. In addition, five impurities were found for the first time in methamphetamine hydrochloride samples. Seventeen impurity peaks were selected from the GC–FID chromatograms. The peak areas of the selected peaks were then grouped for cluster analysis. PMID:19008060

  3. Voltammetric Assay of Metformin Hydrochloride Using Pyrogallol Modified Carbon Paste Electrode.

    PubMed

    Attia, Ali K; Salem, Waheed M; Mona, A Mohamed

    2015-01-01

    The electrooxidative behavior and determination of metformin hydrochloride, anti-hyperglycemic drug, on a pyrogallol modified carbon paste electrode were investigated using cyclic voltammetry and differential pulse voltammetry. Metformin hydrochloride shows an irreversible oxidation behavior over a wide interval of pH (Britton-Robinson buffers, pH 2-9). The peak current varied linearly in the range comprised between 8.0 × 10(-7) and 6.0 × 10(-6) mol/L with detection limit of 6.63 × 10(-8) mol/L and limit of quantification of 2.21 × 10(-7) mol/L. The method was proposed for the determination of metformin hydrochloride in dosage forms and urine.

  4. Regression of recurrent glioblastoma infiltrating the brainstem after convection-enhanced delivery of nimustine hydrochloride.

    PubMed

    Saito, Ryuta; Sonoda, Yukihiko; Kumabe, Toshihiro; Nagamatsu, Ken-ichi; Watanabe, Mika; Tominaga, Teiji

    2011-05-01

    This 13-year-old boy with a history of cranial irradiation for the CNS recurrence of acute lymphocytic leukemia developed a glioblastoma in the right cerebellum. Resection and chemo- and radiotherapy induced remission of the disease. However, recurrence was noted in the brainstem region 8 months later. Because no effective treatment was available for this recurrent lesion, the authors decided to use convection-enhanced delivery (CED) to infuse nimustine hydrochloride. On stereotactic insertion of the infusion cannula into the brainstem lesion, CED of nimustine hydrochloride was performed with real-time MR imaging to monitor the co-infused chelated gadolinium. The patient's preinfusion symptom of diplopia disappeared after treatment. Follow-up MR imaging revealed the response of the tumor. The authors report on a case of recurrent glioblastoma infiltrating the brainstem that regressed after CED of nimustine hydrochloride.

  5. A validated high performance thin layer chromatography method for determination of yohimbine hydrochloride in pharmaceutical preparations

    PubMed Central

    Badr, Jihan M.

    2013-01-01

    Background: Yohimbine is an indole alkaloid used as a promising therapy for erectile dysfunction. A number of methods were reported for the analysis of yohimbine in the bark or in pharmaceutical preparations. Materials and Method: In the present work, a simple and sensitive high performance thin layer chromatographic method is developed for determination of yohimbine (occurring as yohimbine hydrochloride) in pharmaceutical preparations and validated according to International Conference of Harmonization (ICH) guidelines. The method employed thin layer chromatography aluminum sheets precoated with silica gel as the stationary phase and the mobile phase consisted of chloroform:methanol:ammonia (97:3:0.2), which gave compact bands of yohimbine hydrochloride. Results: Linear regression data for the calibration curves of standard yohimbine hydrochloride showed a good linear relationship over a concentration range of 80–1000 ng/spot with respect to the area and correlation coefficient (R2) was 0.9965. The method was evaluated regarding accuracy, precision, selectivity, and robustness. Limits of detection and quantitation were recorded as 5 and 40 ng/spot, respectively. The proposed method efficiently separated yohimbine hydrochloride from other components even in complex mixture containing powdered plants. The amount of yohimbine hydrochloride ranged from 2.3 to 5.2 mg/tablet or capsule in preparations containing the pure alkaloid, while it varied from zero (0) to 1.5–1.8 mg/capsule in dietary supplements containing powdered yohimbe bark. Conclusion: We concluded that this method employing high performance thin layer chromatography (HPTLC) in quantitative determination of yohimbine hydrochloride in pharmaceutical preparations is efficient, simple, accurate, and validated. PMID:23661986

  6. Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride.

    PubMed

    Ranpise, Nisharani S; Korabu, Swati S; Ghodake, Vinod N

    2014-04-01

    Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension. It is a poor water soluble drug with absolute bioavailability of 10%. The aim of this study was to design lercanidipine hydrochloride-loaded nanostructured lipid carriers to investigate whether the bioavailability of the same can be improved by oral delivery. Lercanidipine hydrochloride nanostructured lipid carriers were prepared by the method of solvent evaporation at a high temperature and solidification by freeze drying. The nanostructured lipid carriers were evaluated for particle size analysis, zeta potential, entrapment efficiency, in vitro drug diffusion, ex vivo permeation studies and pharmacodynamic study. The resultant nanostructured lipid carriers had a mean size of 214.97 nm and a zeta potential of -31.6 ± 1.5 mV. More than 70% lercanidipine hydrochloride was entrapped in the NLCs. The SEM studies indicated the formation of type 2 nanostructured lipid carriers. The in vitro release studies demonstrated 19.36% release in acidic buffer pH 1.2 indicating that the drug entrapped in the nanostructured lipid carriers remains entrapped at acidic pH. The ex vivo studies indicated that the drug release was enhanced from 10% to 60.54% at blood pH in 24h. The in vivo pharmacodynamic study showed that NLCs released lercanidipine hydrochloride in a controlled manner for a prolonged period of time as compared to plain drug. These results clearly indicate that nanostructured lipid carriers are a potential controlled release formulation for lercanidipine hydrochloride and may be a promising drug delivery system for the treatment of hypertension.

  7. [Simultaneous determination of five cold medicine ingredients in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets by pH/organic solvent double-gradient high performance liquid chromatography].

    PubMed

    Xuan, Xueyi; Huang, Lina; Pan, Xiaoling; Li, Ning

    2013-02-01

    A pH/organic solvent double-gradient mode in reversed-phase high performance liquid chromatography (HPLC) has been established as a new approach to the simultaneous determination of acetaminophen, caffeine, salicylamide, pseudoephedrine hydrochloride and triprolidine hydrochloride in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets. Through the optimization of the organic solvent gradient mode and pH/organic solvent double-gradient mode, the optimum double-gradient HPLC system of the five cold medicine ingredients has been built. The determination was carried out on a Diamonsiol C18 column (250 mm x 4.6 mm, 5 microm). The mobile phase consisted of methanol, 0.05 mol/L ammonium acetate solution and 0.08 mol/L acetic acid solution. The column temperature was set at 30 degrees C. The flow rate was 1.0 mL/min. The sample was measured at multiple wavelengths: 0-6 min, 280 nm; 6-7 min, 257 nm; 7-14 min, 280 nm; 14 min, 233 nm. The separation of the five cold medicine ingredients in the tablets was achieved in 25.5 min. The linear ranges of acetaminophen, pseudoephedrine hydrochloride, caffeine, salicylamide and triprolidine hydrochloride were 0.055 -0.998 g/L, 0.053-0.946 g/L, 0.007-0.129 g/L, 0.035-0.622 g/L and 0.002-0.039 g/L, respectively, with their correlation coefficients greater than 0.999 0. The detection limits (S/N = 3) were 0.09, 6, 0.02, 0.128 and 0.02 mg/L, respectively. Their mean recoveries were 97.9%-102.8%. The advantage of the method is the simultaneous determination of acidic, neutral and basic compounds. It also can improve the column efficiency of the analyte, compress the half-peak width and reduce the trailing. The optimized and validated method can be used for the simultaneous determination of the five cold medicine ingredients in the tablets.

  8. Immobilization of the endangered Iberian lynx with xylazine- and ketamine-hydrochloride.

    PubMed

    Ferreras, P; Aldama, J J; Beltrán, J F; Delibes, M

    1994-01-01

    A combination of the dissociative anesthetic ketamine hydrochloride (KH) and the sedative xylazine hydrochloride (XH) was used to immobilize 31 wild Iberian lynx (Felis pardina) 45 times at Doñana National Park, Spain. A mean (+/- SE) dose of 4.6 (+/- 0.2) mg/kg KH and 4.0 (+/- 0.2) mg/kg XH resulted in mean (+/- SE) induction time of 5.6 (+/- 0.3) min and mean (+/- SE) first reaction time of 59.3 (+/- 6.5) min. Convulsions occurred four times (9%), but with no noteworthy consequences.

  9. Biowaiver monographs for immediate release solid oral dosage forms: ranitidine hydrochloride.

    PubMed

    Kortejärvi, H; Yliperttula, M; Dressman, J B; Junginger, H E; Midha, K K; Shah, V P; Barends, D M

    2005-08-01

    Literature and experimental data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate release (IR) solid oral dosage forms containing ranitidine hydrochloride are reviewed. According to the current Biopharmaceutics Classification System (BCS), ranitidine hydrochloride should be assigned to Class III. However, based on its therapeutic and therapeutic index, pharmacokinetic properties and data related to the possibility of excipient interactions, a biowaiver can be recommended for IR solid oral dosage forms that are rapidly dissolving and contain only those excipients as reported in this study.

  10. Vibrational spectra of ketamine hydrochloride and 3, 4-methylenedioxymethamphetamine in terahertz range

    NASA Astrophysics Data System (ADS)

    Wang, Guangqin; Shen, Jingling; Jia, Yan

    2007-07-01

    The terahertz spectrum of ketamine hydrochloride at room temperature, in the range of 0.2-2.6THz, has been measured by terahertz time-domain spectroscopy (TDS). Full-geometry optimizations and frequency calculations using the density functional theory (DFT) are also applied to predict the absorption spectra of ketamine hydrochloride and 3, 4-methylenedioxymethamphetamine (MDMA). The results of the simulation show qualitative agreement with the experimental data especially for MDMA, and the observed spectra features are assigned based on the DFT calculation. The results suggest that use of the terahertz TDS technique can be an effective method for the detection and inspection of illicit drugs.

  11. Synthesis and characterization of impurities of barnidipine hydrochloride, an antihypertensive drug substance.

    PubMed

    Cheng, Zhi-Gang; Dai, Xu-Yong; Li, Li-Wei; Wan, Qiong; Ma, Xiang; Xiang, Guang-Ya

    2014-01-21

    Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC) with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm×4.6 mm, 5 µm). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR). The identification of these impurities should be useful for quality control in the manufacture of barnidipine.

  12. [The determination of pyridoxine hydrochloride (vitamin B6) according to European Pharmacopoeia 4.0].

    PubMed

    Kos, N; Surmann, J P

    2006-05-01

    Determination of pyridoxine hydrochloride according to the European Pharmacopoeia 4.0 In the Ph.Eur. 4.0 assay pyridoxine hydrochloride is titrated by sodium hydroxide 0.1 mol x 1(-1) in ethanolic solution. The impossibility of a correct evaluation of the titration curve is shown both in theory and practice. The new method in Ph.Eur. 4.04 is an acidimetric titration of the base chloride. In a mixture of formic acid/acetic anhydride the titration is made by perchloric acid. Because some critical points in this assay an alternative method is developed. This method is robust and should give results with high accuracy.

  13. Simple and sensitive spectrophotometric methods for determination of amantadine hydrochloride

    NASA Astrophysics Data System (ADS)

    Darwish, I. A.; Khedr, A. S.; Askal, H. F.; Mahmoud, R. M.

    2006-11-01

    Three simple and sensitive spectrophotometric methods (A-C) for determination of amantadine hydro-chloride have been developed and validated. The first method (A) is based on the oxidation of the drug by ammonium molybdate. The second method (B) was based on the charge-transfer complexation reaction between the amantadine base as an electron donor and iodine as a σ-acceptor. The third method (C) is based on the reaction of N-alkylvinylamine formed from the interaction of the free amino group in amantadine molecule and acetalde-hyde with chloranil to give colored vinylamino-substituted benzoquinone. The colored products of these reactions were measured at their corresponding maximum absorption peaks. Different variables affecting the reactions were carefully studied and optimized. Under the optimum conditions, linear relationships with good correlation coefficients 0.9993-0.9998 were found between the reading and the corresponding concentration of the drug in the range 2-90 µg·ml-1. The limits of detection ranged from 0.16 to 1.91 µg·ml-1. The precision of the methods was satisfactory: the values of relative standard deviation did not exceed 1.63%. The proposed methods were successfully applied to the analysis of amantadine HCl in its capsules with good accuracy and precision; the label claim percentages ranged from 99.8 to 100.5 ± (0.52-1.22) %. The results obtained by the proposed spectrophotometric methods were comparable with those obtained by the official method.

  14. Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.

    PubMed

    Nanjwade, Basavaraj K; Deshmukh, Rucha V; Gaikwad, Kishori R; Parikh, Kemy A; Manvi, F V

    2012-06-01

    The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF(4), MF(5), and MF(9) were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C (max) of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF(4), MF(5), and MF(9), respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h.

  15. Determination of phenformin hydrochloride employing a sensitive fluorescent probe

    NASA Astrophysics Data System (ADS)

    Shi, Lin; Xie, Jian-Hong; Du, Li-Ming; Chang, Yin-xia; Wu, Hao

    2016-06-01

    A complexation of non-fluorescent phenformin hydrochloride (PFH) with cucurbit [7]uril (CB [7]) in aqueous solution was investigated using the fluorescent probe of palmatine (PAL) coupled with CB [7]. The fluorescent probe of CB [7]-PAL exhibited strong fluorescence in aqueous solution, which was quenched gradually with the increase of PFH. This effect is observed because when PFH was added to the host-guest system of CB [7]-PAL, PFH and PAL competed to occupy the CB [7] cavity. Portions of the PAL molecule were expelled from the CB [7] cavity owing to the introduction of PFH. Based on the significant quenching of the supramolecular complex fluorescence intensity, a fluorescence method of high sensitivity and selectivity was developed to determine PFH with good precision and accuracy for the first time. The linear range of the method was 0.005-1.9 μg mL- 1 with a detection limit of 0.003 μg mL- 1. In this work, association constants (K) of PFH with CB [7] were also determined. KCB [7]-PFH = (2.52 ± 0.05) × 105 L mol- 1. The ability of PFH to bind with CB [7] is stronger than that of PAL. The results of a density functional theory calculation authenticated that the moiety of PFH was embedded in the hydrophobic cavity of CB [7] tightly, and the nitrogen atom is located in the vicinity of a carbonyl-laced portal in the energy-minimized structure. The molecular modelling of the interaction between PFH and CB [7] was also confirmed by 1H NMR spectra (Bruker 600 MHz).

  16. Terbinafine hydrochloride loaded liposome film formulation for treatment of onychomycosis: in vitro and in vivo evaluation.

    PubMed

    Tanrıverdi, Sakine Tuncay; Hilmioğlu Polat, Süleyha; Yeşim Metin, Dilek; Kandiloğlu, Gülşen; Özer, Özgen

    2016-01-01

    Onychomycosis is a fungal infection of nail unit that is caused by dermatophytes. Oral Terbinafine hydrochloride (TBF-HCl) is being used for the treatment of onychomycosis since 24 years. The side effects caused by the systemic application and limitations of topical administration of this drug regarding the diffusion through nail lead to the development of a new formulation based on, TBF-HCl-loaded liposome. The newly obtained film formulations were prepared and characterized via several parameters, such as physical appearance, drug content, thickness, bioadhesive properties and tensile strength. In vitro and ex vivo permeation studies were performed to select an optimum film formulation for antifungal activity to show the efficiency of formulations regarding the treatment of onychomycosis. The in vitro release percentages of drug were found 71.6 ± 3.28, 54.4 ± 4.26, 56.1 ± 7.48 and 46.0 ± 2.43 for liposome loaded pullulan films (LI-P, LII-P) and liposome loaded Eudragit films (LI-E, LII-E), respectively. The accumulated drug in the nail plates were found 31.16 ± 4.22, 24.81 ± 5.35, 8.17 ± 1.81 and 8.92 ± 3.37 for LI-P, LII-P, LI-E and LII-E, respectively, which within therapeutic range for all film formulations. The accumulated drug in the nail plate was found within therapeutic range for all film formulations. The efficacy of the selected TBF-HCl-loaded liposome film formulation was compared with TBF-HCl-loaded liposome, ethosome, liposome poloxamer gel and ethosome chitosan gel formulations. It was found that TBF-HCl-loaded liposome film formulation had better antifungal activity on fungal nails which make this liposome film formulation promising for ungual therapy of fungal nail infection.

  17. Anti-secretory and cyto-protective effects of peganine hydrochloride isolated from the seeds of Peganum harmala on gastric ulcers.

    PubMed

    Singh, Vinay Kumar; Mishra, Vaibhav; Tiwari, Sriniwas; Khaliq, Tanvir; Barthwal, Manoj Kumar; Pandey, Haushila Prasad; Palit, Gautam; Narender, Tadigoppula

    2013-10-15

    Gastroprotective mechanism of peganine hydrochloride isolated from Peganum harmala seeds was investigated. Peganine hydrochloride was evaluated against cold restraint (CRU), aspirin (AS), alcohol (AL) and pyloric ligation (PL) induced gastric ulcer models in rats. Potential anti-ulcer activity of peganine was observed against CRU (50.0%), AS (58.5%), AL (89.41%) and PL (62.50%) induced ulcer models. The reference drug omeprazole (10mg/kg, p.o.) showed 77.45% protection against CRU, 49.97% against AS and 69.42% against PL model. Sucralfate, another reference drug (500mg/kg, p.o.) showed 62.50% protection in AL induced ulcer model. Peganine significantly reduced free acidity (33.38%), total acidity (38.09%) and upregulated mucin secretion by 67.91%, respectively. Further, peagnine significantly inhibited H(+) K(+)-ATPase activity in vitro with IC50 of 73.47μg/ml as compared to the IC50 value of omeprazole (30.24μg/ml) confirming its anti-secretory activity.

  18. Comparative effects of zilpaterol hydrochloride and ractopamine hydrochloride on live performance and carcass characteristics of calf-fed Holstein steers.

    PubMed

    Brown, T R; Sexten, A K; Lawrence, T E; Miller, M F; Thomas, C L; Yates, D A; Hutcheson, J P; Hodgen, J M; Brooks, J C

    2014-09-01

    Holstein steers (n = 2,275) were assigned to 1 of 3 treatments: 1) a control diet containing no β-agonists, 2) a diet that contained zilpaterol hydrochloride (ZH; 8.3 mg/kg [100% DM basis]) for 20 d with a 3-d withdrawal period before harvest, and 3) a diet that contained ractopamine hydrochloride (RH; 30.1 mg/kg [100% DM basis]) for 28 d before harvest. No differences (P ≥ 0.18) were detected between treatments for initial BW, BW at d 28, or DMI. Final BW, BW gain for the last 28 d, total BW gain, ADG for the last 28 d, and overall ADG were greater (P < 0.05) for steers fed ZH or RH than for steers fed the control diet. Additionally, G:F for the last 28 d and G:F for the entire trial was increased (P < 0.02) for steers fed ZH (0.147, 0.147) or RH (0.153, 0.151) compared to steers fed the control diet (0.134, 0.143), respectively. Steers fed ZH or RH had HCW that were 15.5 and 8.2 kg heavier (P ≤ 0.01) and LM areas that were 7.1 and 2.3 cm(2) larger (P < 0.01) than control cattle. Steers fed ZH also had dressed carcass yields that were 1.3% to 1.5% greater and USDA calculated yield grades that were decreased 0.16 to 0.23 units compared to RH and control steers. No differences (P ≥ 0.39) were found between treatments for marbling score, fat thickness, and percentage KPH. Steers fed ZH had an increased (P ≤ 0.04) percentage of yield grade 1 and 2 carcasses (15.1, 55.0) and a reduced (P ≤ 0.02) percentage of yield grade 3 carcasses (27.1) compared with those fed RH (10.5, 49.1, 36.1) or the control diet (9.0, 47.4, 36.4), respectively. Additionally, ZH-fed steers had a decreased (P ≤ 0.04) percentage of yield grade 4 and 5 carcasses (2.8) compared with steers fed the control diet (6.9). Steers fed ZH had an increased (P ≤ 0.01) percentage of USDA Select grading carcass (31.0%) and a decreased (P ≤ 0.01) percentage of USDA Choice grading carcasses (65.0%) compared with steers fed RH (25.8%, 70.2%) and no β-agonist (24.8%, 72.0%), respectively. Feeding

  19. Growth, spectral, optical, and dielectric studies on novel semiorganic NLO single crystal: d-phenylglycine hydrochloride

    NASA Astrophysics Data System (ADS)

    Uma, B.; Sakthi Murugesan, K.; Jayavel, R.; Krishnan, S.; Boaz, B. Milton

    2014-05-01

    Good quality novel semiorganic nonlinear optical single crystal of d-phenylglycine hydrochloride has been grown from the aqueous solution by low temperature solution growth method. X-ray diffraction reveals that the crystal crystallises into orthorhombic system with noncentrosymmetric space group P212121. Experimental parameters are evaluated based on single-crystal XRD and the calculated values of the polarisability were compared with the values of polarisability using Clausius-Mossotti equation. The functional groups present in the grown crystal were confirmed by Fourier transform infrared spectral analysis. The 1H and 13C FT-NMR has been recorded to elucidate the molecular structure. Ultraviolet-visible-near infra-red absorption studies on this crystal reveal that the minimum absorption region is around 228 nm. The optical band gap of the crystal was found to be 2.9 eV. The scanning electron microscope study has been carried out to determine the surface morphology of the grown crystal. Photoluminescence studies show that the material emits violet fluorescence. Thermal studies bring forth that the crystal is thermally stable up to 255 °C. Dielectric studies reveal that both the dielectric constant and dielectric loss decrease with the increase in frequency as like the typical semiorganic nonlinear optical crystals such as bisthiourea zinc chloride, bisthiourea cadmium chloride and l-arginine dihydrogen phosphate. Electrical conductivity measurements were carried out and the Arrhenius plot is used to determine the value of activation energy. The Kurtz powder analysis on the crystal confirms the existence of second harmonic generation properties. The SHG efficiency was found to be 1.15 times that of KDP crystal.

  20. Controlled release of metformin hydrochloride and repaglinide from sandwiched osmotic pump tablet.

    PubMed

    Qin, Chao; He, Wei; Zhu, Chunli; Wu, Mengmeng; Jin, Zhu; Zhang, Qiang; Wang, Guangji; Yin, Lifang

    2014-05-15

    The marketed compound tablet of metformin hydrochloride (MH) and repaglinide (RG) exhibits perfect multidrug therapeutic effect of type 2 diabetes. However, due to the short half life of the drugs, the tablet has to be administered 2 to 3 times a day, causing inconvenience to patient and fluctuations of plasma concentration. Here, a sandwiched osmotic pump tablet was developed to deliver the two drugs simultaneously at zero-order rate, in which MH and RG were loaded in different layers separated by a push layer. The osmotic pump tablet was prepared by a combination of three tableting procedure and film coating method. The factors including type and amount of propellant, osmotic active agents, amount of porogenic agent, coating weight, orifice diameter were optimized. The pharmacokinetic study was performed in beagle dogs, and the drug concentration in plasma samples was assayed by HPLC-MS/MS method. Simultaneous, controlled release of MH and RG in the first 12 and 8h was achieved from the optimized formulation. A significantly decreased Cmax, prolonged Tmax and satisfactory bioavailability of the osmotic pump tablet were obtained, and a good in vivo-in vitro correlation of the two drugs was also established. In summary, the sandwiched osmotic pump tablet released the MH and RG simultaneously at zero-order rate, and exhibited significant sustained release effect in vivo and good in vivo-in vitro correlation. The designed controlled release system for MH and RG proposed a promising replacement for the marked compound product in the therapy of type 2 diabetes.

  1. Evaluation of the antibacterial effects of vancomycin hydrochloride released from agar-gelatin-bioactive glass composites.

    PubMed

    Rivadeneira, Josefina; Di Virgilio, Ana Laura; Audisio, M Carina; Boccaccini, Aldo R; Gorustovich, Alejandro A

    2015-01-13

    The aim of this work was to evaluate the perfomance of agar-gelatin (AG) composites and AG-containing 45S5 bioactive glass (BG) microparticles (AGBG) in relation to their water uptake capacity, sustained release of a drug over time, and antibacterial effects. The composites were fabricated by the gel-casting method. To impart the local drug release capacity, vancomycin hydrochloride (VC) was loaded in the composites in concentrations of 0.5 and 1 mg ml(-1). VC release was assessed in distilled water at 37 °C up to 72 h and quantified spectrophotometrically. The antibacterial activity of composites was evaluated by the inhibition zone test and the plate count method. The experiments were performed in vitro up to 48 h on three staphylococcus strains: Staphylococcus aureus ATCC29213, S. aureus ATCC6538 and Staphylococcus epidermidis ATCC12228. The results showed that the addition of BG to AG composites did not affect the degree of water uptake. The release of VC was significantly affected by the presence of BG. VC release was higher from AGBGVC films than from AGVC ones over prolonged incubation times. Bacterial inhibition zones were found around the composites. The halos were larger when the cells were put in contact with AGVC composites than when they were put in contact with AGBGVC ones. Nevertheless, the viable count method demonstrated that the composites inhibited Staphylococcus cell growth with no statistical differences. In conclusion, the addition of BG did not reflect an improvement in the parameters studied. On the other hand, composites loaded with VC would have a role in prophylaxis against bacterial infection.

  2. Neuroprotective effects of amlodipine besylate and benidipine hydrochloride on oxidative stress-injured neural stem cells.

    PubMed

    Choi, Na-Young; Choi, Hojin; Park, Hyun-Hee; Lee, Eun-Hye; Yu, Hyun-Jeung; Lee, Kyu-Yong; Joo Lee, Young; Koh, Seong-Ho

    2014-03-10

    Hypertension is associated with oxidative stress. Amlodipine besylate (AB) and benidipine hydrochloride (BH), which are Ca(2+) antagonists, have been reported to reduce oxidative stress. In this study, we examined the neuroprotective effects of AB and BH on oxidative stress-injured neural stem cells (NSCs), with a focus on the phosphatidylinositol 3-kinase (PI3K) pathway and the extracellular signal-regulated kinase (ERK) pathway. After treatment with H2O2, the viability of NSCs decreased in a concentration-dependent manner; however, co-treatment with AB or BH restored the viability of H2O2-injured NSCs. H2O2 increased free radical production and apoptosis in NSCs, whereas co-treatment with AB or BH attenuated these effects. To evaluate the effects of AB or BH on the H2O2-inhibited proliferation of NSCs, we performed BrdU labeling and colony formation assays and found that NSC proliferation decreased upon H2O2 treatment but that combined treatment with AB or BH restored this proliferation. Western blot analysis showed that AB and BH increased the expression of cell survival-related proteins that were linked with the PI3K and ERK pathways but decreased the expression of cell death-related proteins. To investigate whether the PI3K and ERK pathways were directly involved in the neuroprotective effects of AB and BH on H2O2-treated NSCs, NSCs were pretreated with the PI3K inhibitor, LY294002, or the ERK inhibitor, FR180204, which significantly blocked the effects of AB and BH. Together, our results suggest that AB and BH restore the H2O2-inhibited viability and proliferation of NSCs by inhibiting oxidative stress and by activating the PI3K and ERK pathways.

  3. Terbinafine Hydrochloride Trans-ungual Delivery via Nanovesicular Systems: In Vitro Characterization and Ex Vivo Evaluation.

    PubMed

    Elsherif, Noha Ibrahim; Shamma, Rehab Nabil; Abdelbary, Ghada

    2017-02-01

    Treating a nail infection like onychomycosis is challenging as the human nail plate acts as a formidable barrier against all drug permeation. Available oral and topical treatments have several setbacks. Terbinafine hydrochloride (TBH), belonging to the allylamine class, is mainly used for treatment of onychomycosis. This study aims to formulate TBH in a nanobased spanlastic vesicular carrier that enables and enhances the drug delivery through the nail. The nanovesicles were formulated by ethanol injection method, using either Span® 60 or Span® 65, together with Tween 80 or sodium deoxycholate as an edge activator. A full factorial design was implemented to study the effect of different formulation and process variables on the prepared TBH-loaded spanlastic nanovesicles. TBH entrapment efficiency percentages, particle size diameter, percentage drug released after 2 h and 8 h were selected as dependent variables. Optimization was performed using Design-Expert® software to obtain an optimized formulation with high entrapment efficiency (62.35 ± 8.91%), average particle size of 438.45 ± 70.5 nm, and 29.57 ± 0.93 and 59.53 ± 1.73% TBH released after 2 and 8 h, respectively. The optimized formula was evaluated using differential scanning calorimetry and X-ray diffraction and was also morphologically examined using transmission electron microscopy. An ex vivo study was conducted to determine the permeation and retainment of the optimized formulation in a human cadaver nail plate, and confocal laser scanning microscope was used to show the extent of formulation permeation. In conclusion, the results confirmed that spanlastics exhibit promising results for the trans-ungual delivery of TBH.

  4. Biowaiver monographs for immediate release solid oral dosage forms: amodiaquine hydrochloride.

    PubMed

    Nair, Anita; Abrahamsson, Bertil; Barends, Dirk M; Groot, D W; Kopp, Sabine; Polli, James E; Shah, Vinod P; Dressman, Jennifer B

    2012-12-01

    The present monograph reviews data relevant to applying the biowaiver procedure for the approval of immediate release (IR) multisource solid dosage forms containing amodiaquine hydrochloride (ADQ) as the single active pharmaceutical ingredient (API). Both biopharmaceutical and clinical data of ADQ were assessed. Solubility studies revealed that ADQ meets the "highly soluble" criteria according to World Health Organization (WHO) and European Medicines Agency (EMA) but fails to comply with the United States Food and Drug Administration (US FDA) specifications. Although metabolism hints at high permeability, available permeability data are too scanty to classify ADQ inequivocably as a Class I drug substance. According to WHO and EMA guidances, ADQ would be conservatively categorized as a Class III drug, whereas according to the US FDA specifications, it would fall into Class IV. ADQ has a wide therapeutic index. Furthermore, no cases of bioinequivalent products have been reported in the open literature. As risks associated with biowaiving appear minimal and requirements for "highly soluble" API are met in the WHO and EMA jurisdictions, the biowaiver procedure can be recommended for bioequivalence (BE) testing of multisource IR products containing ADQ as the only API, provided the test product contains excipients used in ADQ products approved in International Conference of Harmonisation and associated countries, and in similar amounts. Furthermore, both comparator and test should conform to "very rapidly dissolving" product criteria (≥85% dissolution of the API in 15 min at pH 1.2, 4.5, and 6.8) and the labeling should specify that the product not be coadministered with high-fat meals. If the comparator and/or test product fails to meet these criteria, BE needs to be established by pharmacokinetic studies in humans.

  5. Determination and characterization of two degradant impurities in bendamustine hydrochloride drug product.

    PubMed

    Chen, Wenhua; Zou, Limin; Zhang, Fei; Xu, Xiangyang; Zhang, Liandi; Liao, Mingyi; Li, Xiaoqiang; Ding, Li

    2015-01-01

    Bendamustine hydrochloride is an alkylating antitumor agent with a good efficacy in the treatment of chronic lymphocytic leukemia (CLL) and B-cell non-Hodgkin's lymphoma (B-NHL). Under the stressed conditions, two degradant impurities in bendamustine hydrochloride drug product were detected by high-performance liquid chromatography. These two degradant impurities were isolated from preparative liquid chromatography, and were further characterized using Q-TOF/MS and nuclear magnetic resonance (NMR). Based on the MS and NMR spectral data, they were characterized as 4-[5-(2-chloro-ethylamino)-1-methyl-1H-benzoimidazol-2-yl] butyric acid hydrochloride (impurity-A) and 4-{5-[[2-(4-{5-[bis-(2-chloroethyl) amino]-1-methyl-1H-benzoimidazol-2-yl}-butyryloxy)-ethyl]-(2-chloroethyl)amino]-1-methyl-3a, 7a-dihydro-1H-benzoimidazol-2-yl} butyric acid hydrochloride (impurity-B). Isolation, structural elucidation of these two impurities by spectral data (Q-TOF/MS, (1)H NMR, (13)C NMR, D2O exchange NMR and two-dimensional NMR) and the probable formation mechanism of the impurities were discussed.

  6. Observations on the use of cyproheptadine hydrochloride as an antipruritic agent in allergic cats.

    PubMed Central

    Scott, D W; Rothstein, E; Beningo, K E; Miller, W H

    1998-01-01

    Cyproheptadine hydrochloride was administered to 20 presumed or proven allergic cats to determine its efficacy in controlling pruritus. Each cat received 2 mg, orally, every 12 h. The pruritus was satisfactorily controlled in 9 cats. Side effects were seen in 8 cats, and included polyphagia, sedation, vocalization, affectionate behavior, and vomiting. PMID:9789674

  7. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Phenol, 5-amino-2,4-dicholoro... Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as phenol,...

  8. Performance of finishing beef steers in response to anabolic implant and zilpaterol hydrochloride supplementation

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Our objectives were to evaluate the dose/payout pattern of trenbolone acetate (TBA) and estradiol-17b (E2) implants and feeding of zilpaterol hydrochloride (ZH) on performance and carcass characteristics of finishing beef steers. A randomized complete block design was used with a 3 × 2 factorial arr...

  9. 78 FR 66263 - New Animal Drugs; Afoxolaner; Carprofen; Ceftiofur Hydrochloride; Monensin

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-11-05

    ... HUMAN SERVICES Food and Drug Administration 21 CFR Parts 510, 520, 522, and 558 New Animal Drugs; Afoxolaner; Carprofen; Ceftiofur Hydrochloride; Monensin AGENCY: Food and Drug Administration, HHS. ACTION: Final rule. SUMMARY: The Food and Drug Administration (FDA) is amending the animal drug regulations...

  10. Acute toxicity and toxicokinetics of dipfluzine hydrochloride, a novel calcium channel blocker.

    PubMed

    Hu, Huiqing; Wang, Yongli; Pei, Tingmei; Dong, Lei; Xu, Yanfang

    2009-06-01

    Dipfluzine hydrochloride, diphenylpiperazine calcium channel blocker, is a promising candidate to treat ischemic stroke. The purpose of the study is to evaluate the acute toxicity and toxicokinetics of dipfluzine hydrochloride after single intravenous doses in rats. Acute toxicity study was performed in rats at doses of 5, 6, 10, 15, 25, 30, 35, and 40mg/kg. Concentrations of dipfluzine in plasma and tissues were determined with a reverse-phase HPLC method after single doses of 5, 15 and 30mg/kg. The results demonstrated that no-observed-adverse-effect level (NOAEL), lowest-observed-adverse-effect level (LOAEL), maximal tolerance dose (MTD), and minimal lethal dose (MLD) were respectively 5, 6, 30, 35mg/kg for i.v. administration of dipfluzine hydrochloride. The toxicokinetic study revealed that the severity of toxicity was linear with the level of systemic exposure. The highest tissue exposure was detected in lung tissue and it may primarily contribute to the pulmonary congestion in dead rats. Longer elimination half-lives of dipfluzine in kidney, brain, liver, and pancreas imply a possible accumulation of dipfluzine in these tissues for long-term exposure. In addition, a temporary impairment in liver and heart was observed for clinical chemistry in 30mg/kg dose group. The findings will help to design further studies to characterize the repeat-dose toxicity of dipfluzine hydrochloride.

  11. 21 CFR 524.1484f - Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1484f Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride... lesions may be due to the presence of nonsusceptible organisms or to prolonged use of...

  12. The detection properties of ammonia SAW gas sensors based on L-glutamic acid hydrochloride.

    PubMed

    Shen, Chi-Yen; Huang, Chun-Pu; Huang, Wang-Tsung

    2005-10-01

    This study has investigated an improved surface acoustic wave (SAW) ammonia gas sensor based on L-glutamic acid hydrochloride. It presents an excellent reversibility, sensitivity, and repeatability to ammonia. The frequency shift versus ammonia concentration above 40 degrees C was a monotonic function, and the limit of detection of the sensor at 50 degrees C was 80 ppb.

  13. Simultaneous HPLC Determination of Butenafine Hydrochloride and Betamethasone in a Cream Formulation

    PubMed Central

    Ankam, R.; Mukkanti, K.; Durgaprasad, S.; Khan, M.

    2009-01-01

    A fast, specific, accurate and precise reverse phase high performance liquid chromatographic method was developed for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. The determination was carried out on licrocart licrosphere RP-select B (250×4.6 mm, 5 μ) column in isocratic mode, the mobile phase consisting of 50 mM ammonium acetate buffer and acetonitrile in the ratio of 60:40, adjusted to pH 4.5 ± 0.1 with glacial acetic acid. The flow rate was 2.0 ml/min and eluent was monitored at 254 nm. The retention times of butenafine hydrochloride and betamethasone were 4.70 min and 7.76 min, respectively, and the resolution factor was greater than 4.0. Linearity of butenafine hydrochloride and betamethasone were in the range of 100-300 μg/ml and 5-15 μg/ml, respectively. The proposed method is also found to be precise and robust for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. PMID:20502575

  14. A Parent Guide To Understanding the Effects of Ritalin (Methylphenidate Hydrochloride).

    ERIC Educational Resources Information Center

    Villegas, Orlando; And Others

    This guide provides information to help parents decide whether their child with attention deficit hyperactivity disorder (ADHD) should take methylphenidate hydrochloride (Ritalin). Information is provided in a question-and-answer format on various concerns, including: the meaning of ADHD, whether Ritalin is overprescribed, when this medication is…

  15. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 40 Protection of Environment 12 2014-07-01 2014-07-01 false Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride B Appendix B to Subpart NNN of Part 63 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) AIR PROGRAMS (CONTINUED) NATIONAL EMISSION STANDARDS FOR HAZARDOUS AIR POLLUTANTS FOR...

  16. 77 FR 53892 - Determination That ALOXI (Palonosetron Hydrochloride) Capsules, 0.5 Milligram (Base), Were Not...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-09-04

    ...) Capsules, 0.5 Milligram (Base), Were Not Withdrawn From Sale for Reasons of Safety or Effectiveness AGENCY... determined that ALOXI (palonosetron hydrochloride (HCl)) Capsules, 0.5 milligram (mg) (base), were not... abbreviated new drug applications (ANDAs) for palonosetron HCl capsules, 0.5 mg (base), if all other legal...

  17. 76 FR 20685 - Determination That NOVANTRONE (Mitoxantrone Hydrochloride) Injection, Equivalent to 25 Milligrams...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2011-04-13

    ...) Injection, Equivalent to 25 Milligrams Base/12.5 Milliliter and Equivalent to 30 Milligrams Base/15... NOVANTRONE (mitoxantrone hydrochloride) Injection, equivalent to (EQ) 25 milligrams (mg) base/12.5 milliliters (mL) and EQ 30 mg base/15 mL, was not withdrawn from sale for reasons of safety or...

  18. 78 FR 2416 - Notice of Issuance of Final Determination Concerning Rybix® (Tramadol Hydrochloride) Tablets

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-01-11

    ... determination that India is the country of origin of the Rybix (tramadol hydrochloride) tablets for purposes of... India, blended with excipients and packaged into dosage form in France, was not substantially transformed in France, ] such that India is the country of origin of the finished Rybix...

  19. 21 CFR 524.1484c - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment. 524.1484c Section 524.1484c Food and Drugs FOOD AND DRUG ADMINISTRATION... observe animals being treated for evidence of hypersensitivity or allergy to the drug. If such signs...

  20. 21 CFR 524.1484c - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment. 524.1484c Section 524.1484c Food and Drugs FOOD AND DRUG ADMINISTRATION... observe animals being treated for evidence of hypersensitivity or allergy to the drug. If such signs...

  1. 21 CFR 524.1484c - Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Neomycin sulfate, isoflupredone acetate, tetracaine hydrochloride ointment. 524.1484c Section 524.1484c Food and Drugs FOOD AND DRUG ADMINISTRATION... observe animals being treated for evidence of hypersensitivity or allergy to the drug. If such signs...

  2. Stability profiles of nepenthesin in urea and guanidine hydrochloride: comparison with porcine pepsin A.

    PubMed

    Kubota, Keiko; Metoki, Yuya; Athauda, Senarath B P; Shibata, Chiaki; Takahashi, Kenji

    2010-01-01

    Nepenthesin, an aspartic endopeptidase from the pitcher fluid of Nepenthes, was found to be markedly less stable than porcine pepsin A when treated with urea or guanidine hydrochloride. This is in sharp contrast with its remarkably high pH/temperature stability as compared with porcine pepsin A. No protein with such a stability profile has been reported to date.

  3. Enhancing the Effectiveness of Relaxation--Thermal Biofeedback Training with Propranolol Hydrochloride.

    ERIC Educational Resources Information Center

    Holroyd, Kenneth A.; And Others

    1995-01-01

    Evaluated the ability of propranolol hydrochloride to enhance results achieved with relaxation-biofeedback training. Results suggest that concomitant propranolol therapy (CPT) significantly enhanced the effectiveness of relaxation-biofeedback training. CPT also yielded larger reductions in analgesic use and greater improvements in quality-of-life…

  4. 76 FR 1620 - Trials to Verify and Describe Clinical Benefit of Midodrine Hydrochloride; Establishment of...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2011-01-11

    ... HUMAN SERVICES Food and Drug Administration Trials to Verify and Describe Clinical Benefit of Midodrine Hydrochloride; Establishment of Public Docket AGENCY: Food and Drug Administration, HHS. ACTION: Notice. SUMMARY: The Food and Drug Administration (FDA) is announcing the opening of a public docket to provide a...

  5. HPLC analysis of raloxifene hydrochloride and its application to drug quality control studies.

    PubMed

    Trontelj, Jurij; Vovk, Tomaz; Bogataj, Marija; Mrhar, Ales

    2005-10-01

    Raloxifene hydrochloride is a selective estrogen receptor modulator and is currently being used for prevention of osteoporosis in postmenopausal women. In this article, a high performance liquid chromatography (HPLC) method for detection of raloxifene hydrochloride was developed and validated using an ultraviolet (UV) and coulometric detectors. Limit of quantification (LOQ) was 0.336 and 0.610 mg L(-1) for coulometric and ultraviolet detectors, respectively. Acceptable accuracy (93.1-100.3%) as well as intra- and inter-day precision (CVhydrochloride content in tablets and to the in vitro dissolution studies. The proposed method could be used for routine quality control. Moreover, due to its low LOQ, excellent accuracy, precision and selectivity, the coulometric detection could be applied to in vitro metabolism experiments such as microsome or hepatocyte preparations and for studies of transport of raloxifene hydrochloride across biological membranes.

  6. The effects of zilpaterol hydrochloride and shade on blood metabolites of finishing beef steers

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The effects of feeding zilpaterol hydrochloride (ZH) and shade were evaluated on blood metabolites and lung score in finishing beef steers. Cattle were fed 0 or 8.33 mg/kg ZH for 21 d with a 3- or 4-d withdrawal before harvest and were housed in open or shaded pens. Blood samples and lung scores w...

  7. 76 FR 32366 - Determination That ORLAAM (Levomethadyl Acetate Hydrochloride) Oral Solution, 10 Milligrams...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2011-06-06

    ... determined that ORLAAM (levomethadyl acetate hydrochloride (HCl)) oral solution, 10 milligrams (mg... solution, 10 mg/mL, if all other legal and regulatory requirements are met. FOR FURTHER INFORMATION CONTACT... HCl) oral solution, 10 mg/mL, is the subject of NDA 20-315, held by Roxane Laboratories, Inc....

  8. 78 FR 66742 - Determination That MOBAN (Molindone Hydrochloride) Tablets (5 Milligrams, 10 Milligrams, 25...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-11-06

    ... Administration (FDA) has determined that MOBAN (molindone hydrochloride (HCl)) tablets (5 milligrams (mg), 10 mg, 25 mg, 50 mg, and 100 mg) and capsules (5 mg, 10 mg, and 25 mg) were not withdrawn from sale for... applications (ANDAs) for MOBAN (molindone HCl) tablets (5 mg, 10 mg, 25 mg, 50 mg, and 100......

  9. 76 FR 53907 - Determination That TALWIN COMPOUND (Aspirin; Pentazocine Hydrochloride) Tablets, 325 Milligrams...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2011-08-30

    ... hydrochloride (HCl)) tablets, 325 milligrams (mg); equivalent to (EQ) 12.5 mg base, were not withdrawn from sale... drug applications (ANDAs) for aspirin; pentazocine HCl tablets, 325 mg; EQ 12.5 mg base, if all other... ANDA that does not refer to a listed drug. TALWIN COMPOUND (aspirin; pentazocine HCl) tablets, 325...

  10. 77 FR 9944 - Determination That REQUIP XL (Ropinerole Hydrochloride) Extended-Release Tablets, 3 Milligrams...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-02-21

    ... milligrams (mg), were not withdrawn from sale for reasons of safety or effectiveness. This determination will...- release tablets, 3 mg, if all other legal and regulatory requirements are met. FOR FURTHER INFORMATION... drug. REQUIP XL (ropinerole hydrochloride) extended-release tablets, 3 mg, are the subject of NDA...

  11. 75 FR 14444 - Determination That DIDREX (Benzphetamine Hydrochloride) Tablets, 25 Milligrams, Were Not...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-03-25

    ... Administration (FDA) has determined that DIDREX (benzphetamine hydrochloride (HCl)) Tablets, 25 milligrams (mg... to approve abbreviated new drug applications (ANDAs) for benzphetamine HCl 25 mg tablets, if all... to a listed drug. DIDREX (benzphetamine HCl) Tablets, 25 mg, are the subject of approved NDA...

  12. A randomized double-blind clinical trial of the effect of chondroitin sulfate and glucosamine hydrochloride on temporomandibular joint disorders: a pilot study.

    PubMed

    Nguyen, P; Mohamed, S E; Gardiner, D; Salinas, T

    2001-04-01

    Previous studies have shown chondroitin sulfate and glucosamine hydrochloride have beneficial effects on symptoms of osteoarthritis of the knee. Our aim was to study the effect of a daily dose of 1500 mg of glucosamine hydrochloride (GH) and 1200 mg of chondroitin sulfate (CS) taken for twelve weeks on subjects diagnosed with capsulitis, disk displacement, disk dislocation, or painful osteoarthritis of the temporomandibular joint (TMJ). Forty-five subjects were enrolled in the study and were randomly assigned to either an active medication group or a placebo group. Eleven subjects were lost from the study for various reasons, resulting in fourteen subjects remaining in the active medication group and twenty subjects remaining in the placebo group. Subjects taking CS-GH had improvements in their pain as measured by one index of the McGill Pain Questionnaire, in TMJ tenderness, in TMJ sounds, and in the number of daily over-the-counter medications needed. Subjects taking the placebo medication had improvements in their pains as measured by the visual analog scale and by four indices of the McGill Pain Questionnaire. Additional studies are required to evaluate the clinical effectiveness of CS-GH and to determine the exact mechanism by which CS-GH affects the articular cartilage of synovial joints.

  13. Multiple effects of 1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole hydrochloride (SKF 96365) on Ca2+ signaling in MDCK cells: depletion of thapsigargin-sensitive Ca2+ store followed by capacitative Ca2+ entry, activation of a direct Ca2+ entry, and inhibition of thapsigargin-induced capacitative Ca2+ entry.

    PubMed

    Jan, C R; Ho, C M; Wu, S N; Tseng, C J

    1999-02-01

    The effect of 1-[beta-[3-(4-methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole hydrochloride (SKF 96365) on Ca2+ signaling in Madin Darby canine kidney (MDCK) cells was examined. SKF 96365 at 25-100 microM evoked a robust [Ca2+]i transient in a dose-dependent manner, measured by fura-2 fluorimetry. A concentration of 10 microM SKF 96365 did not have an effect. The transient consisted of a slow rise, a gradual decay, and a sustained plateau in physiological Ca2+ medium. Removal of extracellular Ca2+ reduced the Ca2+ signals evoked by 50-100 microM SKF 96365 by nearly half in the area under the curve, suggesting that SKF 96365 induced intracellular Ca2+ release and also extracellular Ca2+ influx. A concentration of 100 microM SKF 96365 caused significant Mn2+ quench of fura-2 fluorescence, which was partly inhibited by La3+ (1 mM) or Gd3+ (0.1 mM), indicating that the SKF 96365-induced Ca2+ influx had two components: one is sensitive to La3+ (1 mM) or Gd3+ (0.1 mM), the other is not. The internal Ca2+ source for the SKF 96365-induced [Ca2+]i transient was the endoplasmic reticulum Ca2+ store because, pretreatment with thapsigargin and cyclopiazonic acid, two inhibitors of the endoplasmic reticulum Ca2+ pump nearly abolished the SKF 96365-induced [Ca2+]i increase in Ca2+-free medium. In contrast, pretreatment with 100 microM SKF 96365 only partly depleted the thapsigargin-sensitive Ca2+ store. Addition of 10 mM Ca2+ induced a significant [Ca2+]i increase after prior incubation with 100 microM SKF 96365 in Ca2+-free medium, demonstrating that SKF 96365 induced capacitative Ca2+ entry. This capacitative Ca2+ entry was about 40% of that induced by 1 microM thapsigargin. Additional to inducing its own capacitative Ca2+ entry, 100 microM SKF 96365 partly inhibited thapsigargin- or uridine trisphosphate (UTP)-induced capacitative Ca2+ entry. We also investigated the mechanisms underlying the decay of the SKF 96365-induced [Ca2+]i transient. Inhibition of the plasma

  14. Autonomic actions and interactions of mianserin hydrochloride (Org. GB 94) and amitriptyline in patients with depressive illness.

    PubMed

    Ghose, K; Coppen, A; Turner, P

    1976-09-17

    The clinical pharmacology of mianserin hydrochloride was studied in patients suffering from a primary depressive illness after steady-state plasma concentration of the drug had been achieved. The results were compared with those found with amitriptyline in both open and double-blind studies. The two drugs are equally effective in their antidepressive effect. Mianserin hydrochloride appears to be free of anticholinergic effects as assessed by the measurement of salivary volume, pupil diameter and the interactions with guanethidine and thymoxamine on the pupil. No peripheral adrenergic interaction as studied by the tyramine dose-pressor-response test were observed in patients treated with mianserin hydrochloride (20 mg three times daily).

  15. [Pharmacokinetic interaction of pioglitazone hydrochloride and atorvastatin calcium in Beagle dogs].

    PubMed

    Chen, He-Li; Zhang, Wen-Ping; Yang, Fu-Ying; Wang, Xin-Yu; Yang, Wen-Cheng; Dang, Hong-Wan

    2013-05-01

    The object of this study is to investigate the pharmacokinetic interaction of pioglitazone hydrochloride and atorvastatin calcium in healthy adult Beagle dogs following single and multiple oral dose administration. A randomized, cross-over study was conducted with nine healthy adult Beagle dogs assigned to three groups. Each group was arranged to take atorvastatin calcium (A), pioglitazone hydrochloride (B), atorvastatin calcium and pioglitazone hydrochloride (C) orally in the first period, to take B, C, A in the second period, and to take C, A, B in the third period for 6 days respectively. The blood samples were collected at the first and the sixth day after the administration, plasma drug concentrations were determined by LC-MS/MS, a one-week wash-out period was needed between each period. The pharmacokinetic parameters of drug combination group and the drug alone group were calculated by statistical moment method, calculation of C(max) and AUC(0-t) was done by using 90% confidence interval method of the bioequivalence and bioavailability degree module DAS 3.2.1 software statistics. Compared with the separate administration, the main pharmacokinetic parameters (C(max) and AUC(0-t)) of joint use of pioglitazone hydrochloride and atorvastatin calcium within 90% confidence intervals for bioequivalence statistics were unqualified, the mean t(max) with standard deviation used paired Wilcoxon test resulted P > 0.05. There was no significant difference within t1/2, CL(int), MRT, V/F. Pioglitazone hydrochloride and atorvastatin calcium had pharmacokinetic interaction in healthy adult Beagle dogs.

  16. In vitro and In vivo characterization of the transdermal delivery of sertraline hydrochloride Films

    PubMed Central

    Vijaya, R.; Ruckmani, K.

    2011-01-01

    Background and the purpose of the study Sertraline hydrochloride is a selective serotonin reuptake inhibitor principally used in the treatment of major depressive disorder. To maintain the therapeutic plasma drug concentration of the drug for prolonged period, the transdermal drug delivery has been chosen as an alternative route of drug delivery. The pharmacokinetic properties of sertraline hydrochloride make it suitable for transdermal delivery. The purpose of the study was to investigate the effect of polymers and penetration enhancers on the transdermal delivery of the drug in order to improve its therapeutic efficacy. Methods In the preparation of films, Eudragit RL 100, Eudragit RS 100, hydroxy propyl methyl cellulose (HPMC) and ethyl cellulose were used as polymers. The films were characterized for thickness, tensile strength, drug content, moisture uptake, moisture content, water vapor transmission rate and drug release. The films exhibiting higher rates of drug release were subjected to study the effect of oleic acid and propylene glycol as penetration enhancers on skin permeation of sertraline hydrochloride. In vivo and skin irritation studies were performed for the optimized film. Results Films containing Eudragit RL 100, Eudragit RL 100 and HPMC showed the highest drug release of 94.34% and 96.90% respectively in a period of 42 hrs. The release data fitted into kinetic equations, yielded zero-order and fickian mechanism of drug release. There was a two-fold increase in skin permeation of sertraline hydrochloride in the presence of penetration enhancers in the film. The physical evaluation indicated the formation of smooth, flexible and translucent films. No skin irritation occurred on rabbit skin and the infrared studies showed the compatibility of the drug with the formulation excipients. The in vivo study revealed a constant plasma concentration of drug for long periods and the films containing penetration enhancers had achieved adequate plasma levels

  17. Distribution and elimination of [14C] sarafloxacin hydrochloride from tissues of juvenile channel catfish (Ictalurus punctatus)

    USGS Publications Warehouse

    Gingerich, W.H.; Meinertz, J.R.; Dawson, V.K.; Gofus, J.E.; Delaney, L.J.; Bunnell, P.R.

    1995-01-01

    The distribution and loss of radioactivity from tissues were determined in 60 juvenile channel catfish (Ictalurus punctatus) following oral dosing with the candidate fish therapeutant Sarafin® ([14C] sarafloxacin hydrochloride) at 10 mg/kg for 5 consecutive days. Twelve groups of 5 fish each were sampled at selected times ranging from 3 to 240 h after the last dose was administered, The concentration and content of sarafloxacin-equivalent activity was determined in liver, gallbladder, kidney, skin, and skinless fillet by sample oxidation and liquid scintillation counting; content of sarafloxacin-equivalent activity was determined in stomach and anterior and posterior intestines, Skinless fillet tissues were also analyzed for sarafloxacin and for potential metabolites by gradient-elution high-performance liquid chromatography (HPLC) with in-line radiometric and fluorescence detection, Loss of radioactivity from the whole body conformed to a bimodal elimination pattern with a rapid initial phase (t1/2=11 h) and a slower secondary phase (t1/2=222 h). Tissue and contents of the gastrointestinal tract (i.e. stomach and anterior and posterior intestines) were a principal depot of activity during the first four sample times (3, 6, 12, and 24 h); the combined head, skeleton, and fins (i.e. residual carcass) were the principal depot of activity in samples taken after 24 h. Of those tissues sampled 3 h after the last dose, relative sarafloxacin concentration was greatest in the liver (4.06 μg equivalents/g) and least in the residual carcass (1.13 μg equivalents/g), Intermediate concentrations were found in the kidney (2.04 μg equivalents/g), skinless fillet (1.71 μg equivalents/ g), and the skin (1.51 μg equivalents/g). Concentrations of sarafloxacin-equivalent residues in edible skinless fillet were consistently among the lowest of all tissues examined. The highest mean concentration of parent-equivalent material in the fillet tissue was found 12 h after

  18. NTP Comparative Toxicity and Carcinogenicity Studies of o-Nitrotoluene and o-Toluidine Hydrochloride (CAS Nos. 88-72-2 and 636-21-5) Administered in Feed to Male F344/N Rats.

    PubMed

    Elwell, M

    1996-03-01

    cholangiocarcinomas that occurred in three rats with the normal flora did not occur in groups with the altered intestinal flora. Subsequent studies determined that the antibiotic regimen used was effective only in reducing the gut population of aerobic microorganisms and had little effect on obligate anaerobes, which are thought to play a mayor role in nitro group reduction. In summary, these studies confirmed the target organs and compared the relative toxicity for o-nitrotoluene and o-toluidine hydrochloride administered to male F344/N rats at equimolar concentrations in feed. With the exception of the spleen toxicity observed with each chemical, but more prominently with o-toluidine hydrochloride, morphologic effects of exposure to each of these chemicals in the testis/epididymis, liver, kidney, and urinary bladder were different. The results of these studies demonstrate the somewhat greater relative carcinogenic potential of o-nitrotoluene compared to o-toluidine hydrochloride after 13 or 26 weeks of administration based on the occurrence of mesothelioma and cholangiocarcinoma. The apparently lower potency of o-toluidine hydrochloride relative to o-o-nitrotoluene in the induction of mesothelioma suggests that simple intestinal reduction of the nitro group may not be sufficient for carcinogenic activity in the mesothelium.

  19. 40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... be in the polymeric form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The... hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of...

  20. 21 CFR 341.12 - Antihistamine active ingredients.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 5 2013-04-01 2013-04-01 false Antihistamine active ingredients. 341.12 Section...-COUNTER HUMAN USE Active Ingredients § 341.12 Antihistamine active ingredients. The active ingredient of... ingredient: (a) Brompheniramine maleate. (b) Chlorcyclizine hydrochloride. (c) Chlorpheniramine maleate....

  1. The relative bioavailability of paracetamol after rectal administration of suppositories containing a mixture of paracetamol, codeine phosphate and buclizine hydrochloride in healthy volunteers.

    PubMed

    Burgess, H A; Merrington, D M; Oliver, W J; Thomson, A; Rogers, H J

    1985-01-01

    'New' and 'old' suppositories (6 months and 30 months since manufacture) containing 800 mg paracetamol, 16 mg codeine phosphate and 12.5 mg buclizine hydrochloride in an identical base were administered to 10 normal volunteers at an interval of 2 weeks. Blood samples were taken at intervals up to 300 minutes after administration for estimation of paracetamol plasma concentrations using high pressure liquid chromatography. Mean peak concentrations were obtained of 4.75 +/- 0.74 mg/ml at 1.75 hours with the new suppositories and of 4.6 +/- 0.67 mg/ml at 2.0 hours with the old suppositories. The difference was not significant. Mean elimination half-life was 4.4 +/- 0.42 hours and 3.73 +/- 0.28 hours, respectively. Again, the difference was not significant, indicating that the absorption characteristics for the suppositories did not appear to deteriorate with ageing for 24 months. Bioavailability data for paracetamol derived from the results were similar to those reported by other workers who studied suppositories containing paracetamol as the only active ingredient. This indicates that the inclusion of codeine phosphate and buclizine hydrochloride in the suppository formulation investigated in the present study did not affect adversely the absorption of paracetamol.

  2. Pharmacokinetics of hydromorphone hydrochloride after intravenous and intramuscular administration of a single dose to American kestrels (Falco sparverius)

    USGS Publications Warehouse

    Sanchez-Migallon Guzman, David; KuKanich, Butch; Drazenovich, Tracy L.; Olsen, Glenn H.; Paul-Murphy, Joanne R.

    2014-01-01

    Conclusion and Clinical Relevance—Results indicated hydromorphone hydrochloride had high bioavailability and rapid elimination after IM administration, with a short terminal half-life, rapid plasma clearance, and large volume of distribution in American kestrels. Further studies regarding the effects of other doses, other administration routes, constantrate infusions, and slow release formulations on the pharmacokinetics of hydromorphone hydrochloride and its metabolites in American kestrels may be indicated.

  3. Spectrophotometric determination of procaine hydrochloride in pharmaceutical products using 1,2-naphthoquinone-4-sulfonic acid as the chromogenic reagent

    NASA Astrophysics Data System (ADS)

    Xu, Li Xiao; Shen, Yun Xiu; Wang, Huai You; Jiang, Ji Gang; Xiao, Yan

    2003-11-01

    Spectrophotometric determination of procaine hydrochloride is described. The procaine hydrochloride reacts with 1,2-naphthoquinone-4-sulfonic acid in pH 3.60 buffer solution to form a salmon pink compound, and its maximum absorption wavelength is at 484 nm, ɛ 484=5.22×10 3.The absorbance for procaine hydrochloride from 0.30 to 100 μg ml -1 obeys Beer's law. The linear regression equation of the calibration graph is C=19.23A-0.03, with a linear regression correlative coefficient is 0.9996, the detection limit is 0.28 μg ml -1; recovery is from 98.0 to 105.2%. Effects of pH, surfactant, organic solvent, foreign ions, and standing time on the determination of procaine hydrochloride have been examined. This method is rapid and simple, and can be used for the determination of procaine hydrochloride in injection solution of procaine hydrochloride. The results obtained by this method agreed with those by the official method (dead-stop titration).

  4. Subcutaneously Administered Ultrafine PLGA Nanoparticles Containing Doxycycline Hydrochloride Target Lymphatic Filarial Parasites.

    PubMed

    Singh, Yuvraj; Srinivas, Adepu; Gangwar, Mamta; Meher, Jaya Gopal; Misra-Bhattacharya, Shailja; Chourasia, Manish K

    2016-06-06

    Systemic chemotherapeutic targeting of filarial parasites is unfocused due to their deep seated location in lymphatic vessels. This warrants a prolonged dosing regimen in high doses for an anthelmintic like doxycycline hydrochloride (DOX). In order to provide an alternative, we have constructed ultrafine PLGA nanoparticles of DOX (DPNPs), so as to exploit the peculiarity of lymphatic vasculature underneath the subcutaneous layer of skin, which preferentially allows entry of only 10-100 nm sized particles. DPNPs were constructed using a novel solvent diffusion method aided by probe sonication, which resulted in an average size 95.43 ± 0.8 nm as per DLS, PDI 0.168 ± 0.03, zeta potential -7.38 ± 0.32, entrapment efficiency 75.58 ± 1.94%, and refrigerator stability of 7 days with respect to size in the optimized batch. TEM further substantiated the spherical shape of DPNPs along with their actual nonhydrated size as being well below 100 nm. FTIR analysis of DOX, dummy nanoparticles, and freeze-dried DPNPs revealed that the formulation step did not induce prominent changes in the chemical nature of DOX. The drug release was significantly altered (p < 0.05) with 64.6 ± 1.67% release in 48 h from DPNPs and was dictated by Fickian diffusion. Pharmacokinetic studies in Wistar rats further revealed that DPNPs caused a 16-fold prolongation in attainment of plasma Tmax and a 2-fold extension of elimination half-life (28.569 ± 1.27 h) at a dose of 5 mg/kg when compared to native drug (DOX solution) of the same strength. Contrastingly the trend was reversed in regional lymph nodes where Cmax for DPNPs (820 ± 84 ng/mg) was 4-fold greater, and lymphatic Tmax was attained in one-fourth of what was required for DOX solution. This size based preferential lymphatic targeting resulted in significantly greater in vivo antifilarial activity of DPNPs when compared to DOX solution as gauged by several parameters in Brugia malayi infected Mastomys coucha. Interestingly, the

  5. Photodynamic action of palmatine hydrochloride on colon adenocarcinoma HT-29 cells.

    PubMed

    Wu, Juan; Xiao, Qicai; Zhang, Na; Xue, Changhu; Leung, Albert Wingnang; Zhang, Hongwei; Xu, Chuanshan; Tang, Qing-Juan

    2016-09-01

    Palmatine hydrochloride (PaH) is a natural active compound from a traditional Chinese medicine (TCM). The present study aims to evaluate the effect of PaH as a new photosensitizer on colon adenocarcinoma HT-29 cells upon light irradiation. Firstly, the absorption and fluorescence spectra of PaH were measured using a UV-vis spectrophotometer and RF-1500PC spectrophotometer, respectively. Singlet oxygen ((1)O2) production of PaH was determined using 1, 3-diphenylisobenzofuran (DPBF). Dark toxicity of PaH was estimated using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Cellular uptake of PaH in HT-29 cells was detected at different time intervals. Subellular localization of PaH in HT-29 cells was observed using confocal laser fluorescence microscopy. For photodynamic treatment, HT-29 cells were incubated with PaH and then irradiated by visible light (470nm) from a LED light source. Photocytotoxicity was investigated 24h after photodynamic treatment using MTT assay. Cell apoptosis was observed 18h after photodynamic treatment using a flow cytometry with Annexin V/PI staining. Results showed that PaH has an absorption peak in the visible region from 400nm to 500nm and a fluorescence emission peak at 406nm with an excitation wavelength of 365nm. PaH was activated by the 470nm visible light from a LED light source to produce (1)O2. Dark toxicity showed that PaH alone treatment had no cytotoxicity to HT-29 cancer cells and NIH-3T3 normal cells after incubation for 24h. After incubation for 40min, the cellular uptake of PaH reached to the maximum and PaH was located in mitochondria. Photodynamic treatment of PaH demonstrated a significant photocytotoxicity on HT-29 cells. The rate of cell death increased significantly in a PaH concentration-dependent and light dose-dependent manner. Further evaluation revealed that the early and late apoptotic rate of HT-29 cells increased remarkably up to 21.54% and 5.39% after photodynamic treatment of

  6. Implantable biodegradable sponges: effect of interpolymer complex formation of chitosan with gelatin on the release behavior of tramadol hydrochloride.

    PubMed

    Foda, Nagwa H; El-laithy, Hanan M; Tadros, Mina I

    2007-01-01

    The effect of interpolymer complex formation between positively charged chitosan and negatively charged gelatin (Type B) on the release behavior of tramadol hydrochloride from biodegradable chitosan-gelatin sponges was studied. Mixed sponges were prepared by freeze-drying the cross-linked homogenous stable foams produced from chitosan and gelatin solutions where gelatin acts as a foam builder. Generation of stable foams was optimized where concentration, pH of gelatin solution, temperature, speed and duration of whipping process, and, chitosan-gelatin ratio drastically affect the properties and the stability of the produced foams. The prepared sponges were evaluated for their morphology, drug content, and microstructure using scanning electron microscopy, mechanical properties, uptake capacity, drug release profile, and their pharmacodynamic activity in terms of the analgesic effect after implantation in Wistar rats. It was revealed that whipping 7% (w/w) gelatin solution, of pH 5.5, for 15 min at 25 degrees C with a stirring speed of 1000 rpm was the optimum conditions for stable gelatin foam generation. Moreover, homogenous, uniform chitosan-gelatin foam with small air bubbles were produced by mixing 2.5% w/w chitosan solution with 7% w/w gelatin solution in 1:5 ratio. Indeed, polyionic complexation between chitosan and gelatin overcame the drawbacks of chitosan sponge mechanical properties where, pliable, soft, and compressible sponge with high fluid uptake capacity was produced at 25 degrees C and 65% relative humidity without any added plasticizer. Drug release studies showed a successful retardation of the incorporated drug where the t50% values of the dissolution profiles were 0.55, 3.03, and 4.73 hr for cross-linked gelatin, un-cross-linked chitosan-gelatin, and cross-linked chitosan-gelatin sponges, respectively. All the release experiments followed Higuchi's diffusion mechanism over 12 hr. The achieved drug prolongation was a result of a combined effect

  7. NTP toxicity studies of dimethylaminopropyl chloride, hydrochloride (CAS No. 5407-04-5) administered by Gavage to F344/N rats and B6C3F1 mice.

    PubMed

    Abdo, Km

    2007-07-01

    included lethargy in one 50 mg/kg male and one 100 mg/kg male, tremors in one 100 mg/kg male, and ataxia in one 50 mg/kg male and two 100 mg/kg males. Absolute lung weights in the 25, 50, and 100 mg/kg groups of female mice were significantly less than those of the vehicle controls. Total serum bile acid concentrations were increased in 50 mg/kg male rats and 100 mg/kg male and female rats. The incidence of goblet cell hypertrophy of the nose was significantly increased in 100 mg/kg male rats compared to the vehicle controls. There were no significant histopathologic findings in mice. Dimethylaminopropyl chloride, hydrochloride was mutagenic in the Salmonella typhimurium base substitution strains TA100 and TA1535, with and without hamster or rat liver S9 activation enzymes; no mutagenic activity was seen in TA97 or TA98. No increase in the frequency of micronucleated erythrocytes was seen in peripheral blood of male or female mice administered dimethylaminopropyl chloride, hydrochloride for 3 months by gavage. In summary, dimethylaminopropyl chloride, hydrochloride caused increased incidences of goblet cell hypertrophy in the nose of male rats and increased serum bile acid concentrations in male and female rats. In mice, dimethylaminopropyl chloride, hydrochloride caused deaths in females administered 100 mg/kg. The estimated no-observed-effect levels were 50 mg/kg per day for male rats and female mice, 100 to 200 mg/kg per day for female rats, and greater than 100 mg/kg per day for male mice. Synonyms: 3-Chloropropyldimethyl-ammonium chloride; (3-chloropropyl)dimethylamine, hydrochloride; N-(3-chloropropyl)-N,N-dimethylammonium chloride; 3-dimethylamino-1-propyl chloride hydrochloride; 3-dimethylaminopropyl chloride hydrochloride; DMPC; 1-propylamine, 3-chloro-N,N-dimethyl-, hydrochloride.

  8. Ambroxol hydrochloride in the management of idiopathic pulmonary fibrosis: Clinical trials are the need of the hour

    PubMed Central

    Gupta, P. R.

    2014-01-01

    Idiopathic pulmonary fibrosis (IPF) is a debilitating lung disease of unknown etiology. Its pathogenesis remains poorly elucidated but aberrant wound healing is central to its pathology. It has a median survival time of 3 to 5 years. None of the treatment modality or drugs tried in its management has so far changed the overall outcome. Recent in vitro and experimental studies have shown that ambroxol hydrochloride exerts several newer actions, namely the surfactant stimulatory, anti-imflammatory and anti-oxidant actions, in addition to its being a secrrtolytic and mucokinetic agent. The anti inflammatory and anti-fibrotic properties of the drug are due to its ability to block the release of oxidant stress markers, cytokines, leukotrienes, MPO activity, hydroxyproline content, nitic oxide and/or collagen I & III mRNA in the local milieu while preserving the SOD and GSH-PX activities. In human studies also, the agent was able to block the expression of TGF-beta and TNF-alpha in plasma and preserving the carbon monoxide diffusion capacity of the lungs in lung cancer patients on radiation therapy. Thus, ambroxol may have the potential to check the dysregulated healing process that is typical of IPF. This, coupled with its safety profile for human use, warrants clinical trials of the drug in the management of IPF. PMID:24669082

  9. Calcium alginate particles for the combined delivery of platelet lysate and vancomycin hydrochloride in chronic skin ulcers.

    PubMed

    Mori, Michela; Rossi, Silvia; Bonferoni, Maria Cristina; Ferrari, Franca; Sandri, Giuseppina; Riva, Federica; Del Fante, Claudia; Perotti, Cesare; Caramella, Carla

    2014-01-30

    The aim of the present work was the development of a powder formulation for the combined delivery of platelet lysate and of a model antibiotic drug, vancomycin hydrochloride (VCM), in chronic skin ulcers. Calcium alginate particles were prepared by freeze-drying beads obtained by ionic gelation method. The experimental conditions adopted permitted the complete loading of VCM and of PDGF AB, the growth factor chosen as representative of those contained in PL. Such particles where able to absorb PBS (mimicking wound exudate), to form a gel and to modulate the release of VCM and of PDGF AB. They are characterized by enhancement properties of human fibroblast proliferation due to PL presence. In particular, PL, when loaded in alginate particles, was able not only to increase the number of viable cells, but also the number of cells in proliferative phase. Such properties were comparable to those of fresh PL indicating the capability of calcium alginate particles to load PL bioactive substances without altering their activity. The formulation developed is characterized by an easier and a less painful administration with respect to traditional gauzes and semisolid preparations and permits the loading in the same dosage form of active substances of different nature avoiding eventual incompatibility problems.

  10. Stability of lidocaine hydrochloride in 5% dextrose injection in plastic bags

    SciTech Connect

    Smith, F.M.; Nuessle, N.O.

    1981-11-01

    The stability of lidocaine injection mixed with 5% dextrose injection and refrigerated or stored at room temperature was studied. Lidocaine injection was added to 5% dextrose injection to provide a lidocaine hydrochloride concentration of 4 mg/ml. Samples were assayed for lidocaine and its degradation product, 2,6-dimethylaniline, after 30, 60, and 120 days of storage at room temperature (30 degrees C) and refrigerated temperature (4 degrees C). The analysis was by a stability-indicating HPLC method. Degradation product 2,6-dimethylaniline was not detected at any assay time at either temperature. No statistically significant loss of lidocaine occurred at either temperature. Lidocaine hydrochloride injection is chemically stable for up to 120 days at either 30 degrees C or 4 degrees C when mixed with 5% dextrose injection in plastic infusion bags.

  11. [Successful anesthetic management of a patient with giant pheochromocytoma using high-dose landiolol hydrochloride].

    PubMed

    Kitano, Manabu; Komasawa, Nobuyasu; Sawai, Toshiyuki; Minami, Toshiaki

    2014-08-01

    We report successful anesthetic management of a patient with pheochromocytoma using high-dose landiolol hydrochloride. A 55-year-old man was scheduled to undergo resection of giant pheochromocytoma. Epidural anesthesia was not performed due to anticoagulant therapy for lower limb thrombus. Tracheal intubation was performed with the Pentax-AWS Airwayscope. Preoperative screening revealed urine adrenaline 2.567.0 microg x day(-1) urine noradrenaline 1,734.0 microg x day(-1), and a tumor diameter of 96 x 60 mm. Catecholamine surge was controlled with 50 microg x kg(-1) x min(-1) continuous infusion of landiolol hydrochloride and IV bolus phentolamine. On tumor resection, although systemic blood pressure increased to 294 mmHg and was unresponsive to repeated phentolamine administration, the heart rate remained at 70-105 beats x min(-1) and there were no significant ST changes.

  12. Electron paramagnetic resonance and FT-IR spectroscopic studies of glycine anhydride and betaine hydrochloride

    NASA Astrophysics Data System (ADS)

    Halim Başkan, M.; Kartal, Zeki; Aydın, Murat

    2015-12-01

    Gamma irradiated powders of glycine anhydride and betaine hydrochloride have been investigated at room temperature by electron paramagnetic resonance (EPR). In these compounds, the observed paramagnetic species were attributed to the R1 and R2 radicals, respectively. It was determined that the free electron interacted with environmental protons and 14N nucleus in both radicals. The EPR spectra of gamma irradiated powder samples remained unchanged at room temperature for two weeks after irradiation. Also, the Fourier Transform Infrared (FT-IR), FT-Raman and thermal analyses of both compounds were investigated. The functional groups in the molecular structures of glycine anhydride and betaine hydrochloride were identified by vibrational spectroscopies (FT-IR and FT-Raman).

  13. Spectrophotometric and spectrofluorimetric methods for analysis of acyclovir and acebutolol hydrochloride

    NASA Astrophysics Data System (ADS)

    Ayad, Magda M.; Abdellatef, Hisham E.; El-Henawee, Magda M.; El-Sayed, Heba M.

    2007-01-01

    Simple and sensitive spectrophotometric and spectrofluorimetric methods are described for analysis of acyclovir and acebutolol hydrochloride. The proposed methods are based on oxidation of the selected drugs with cerium(IV) ion in acidic medium with subsequent measurement of either the decrease in absorbance at 320 nm or the fluorescence intensity of the produced cerous(III) ion at 361-363 nm (excitation at 250 nm). Beer's law obeyed from 2 to 8, 0.25 to 2.5 μg cm -1 acyclovir, 1 to 7 and 0.25 to 2.5 μg ml -1 acebutolol hydrochloride, using the spectrophotometric and spectrofluorimetric method, respectively. The proposed method were successfully applied for determination of the selected drugs in their pharmaceutical preparations with good recoveries.

  14. Spectrophotometric and spectrofluorimetric methods for analysis of acyclovir and acebutolol hydrochloride

    NASA Astrophysics Data System (ADS)

    Abdellatef, Hisham E.; El-Henawee, Magda M.; El-Sayed, Heba M.; Ayad, Magda M.

    2006-11-01

    Simple and sensitive spectrophotometric and spectrofluorimetric methods are described for analysis of acebutolol hydrochloride. The proposed methods are based on oxidation of the selected drug with cerium(IV) ion in acidic medium with subsequent measurement of either the decrease in absorbance at 320 nm or the fluorescence intensity of the produced cerous(III) ion at 363 nm (excitation at 250 nm). Beer's law obeyed from 1.0-7.0 μg ml -1 and 0.25-2.5 μg ml -1 acebutolol hydrochloride, using the spectrophotometric and spectrofluorimetric method, respectively. The proposed methods were successfully applied for determination of the selected drug in its pharmaceutical preparation with good recoveries.

  15. Transdermal delivery of betahistine hydrochloride using microemulsions: physical characterization, biophysical assessment, confocal imaging and permeation studies.

    PubMed

    Hathout, Rania M; Nasr, Maha

    2013-10-01

    Transdermal delivery of betahistine hydrochloride encapsulated in various ethyl oleate, Capryol 90(®), Transcutol(®) and water microemulsion formulations was studied. Two different kinds of phase diagrams were constructed for the investigated microemulsion system. Pseudoplastic flow that is preferable for skin delivery was recorded for the investigated microemulsions. A balanced and bicontinuous microemulsion formulation was suggested and showed the highest permeation flux (0.50±0.030mgcm(-2)h(-1)). The effect of the investigated microemulsions on the skin electrical resistance was used to explain the high permeation fluxes obtained. Confocal laser scanning microscopy was used to confirm the permeation enhancement and to reveal the penetration pathways. The results obtained suggest that the proposed microemulsion system highlighted in the current work can serve as a promising alternative delivery means for betahistine hydrochloride.

  16. The discovery of Yuanzhi-1, a triterpenoid saponin derived from the traditional Chinese medicine, has antidepressant-like activity.

    PubMed

    Jin, Zeng-liang; Gao, Nana; Zhang, Jian-rui; Li, Xiao-rong; Chen, Hong-xia; Xiong, Jie; Li, Yun-feng; Tang, Yu

    2014-08-04

    Yuanzhi, the dried root of Polygala tenuifolia Willd., is a well-known traditional Chinese medicine used for its sedative, antipsychotic, cognitive improving, neuroprotective, and antidepressant effects. The present study was designed to screen and identify the antidepressant-like effect of six triterpenoid saponin components derived from Yuanzhi (Yuanzhi-1 to Yuanzhi-6) using in vitro radioligand receptor binding assays and in vivo behavioral tests. Yuanzhi-1, -3, -5 and -6 were shown to have antidepressant-like activity in the tail suspension test and forced swim test in mice, with no stimulant effect on locomotor activity. The minimal effective dose of Yuanzhi-1 (2.5 mg/kg) was lower than that of duloxetine (5mg/kg), a serotonin and norepinephrine reuptake inhibitor commonly used in the treatment of depression. Yuanzhi-1 (1 nM) had a high affinity for serotonin, norepinephrine and dopamine transporters. Acute toxicity tests indicated that the LD50 of Yuanzhi-1 (86.5mg/kg) was similar to that of duloxetine (73.2 mg/kg). These findings demonstrate that Yuanzhi-1 has a potential to be a novel triple monoamine reuptake inhibitor of antidepressant-like activity.

  17. Gastrointestinal symptoms after the substitution of sevelamer hydrochloride with lanthanum carbonate in Japanese patients undergoing hemodialysis.

    PubMed

    Suzuki, D; Ichie, T; Hayashi, H; Sugiura, Y; Sugiyama, T

    2015-08-01

    Lanthanum carbonate has the same phosphorus depressant effect as the other phosphorus adsorbents, and is expected to decrease digestive symptom onset such as constipation in Japanese patients undergoing hemodialysis compared to sevelamar hydrochloride. In this study, we investigated the short- and long-term changes in digestive symptoms in these patients after substituting sevelamar hydrochloride with lanthanum carbonate. We studied 16 patients (4 men, 12 women) and evaluated their gastrointestinal symptoms before administration, at the time of administration, and 2, 4, 8, and 12 weeks after administration, using the Gastrointestinal Symptom Rating Scale. In addition, we conducted repeat evaluations 52 weeks after administration for the patients in whom lanthanum carbonate was administered continuously for 52 weeks. Fourteen (87.5%) out of the 16 patients could tolerate continuous administration for 12 weeks. The constipation score was 3.21 ± 1.74 before administration, 2.07 ± 0.83 2 weeks after administration, 1.76 ± 0.83 4 weeks after administration, 1.57 ± 0.56 8 weeks after administration, and 11.41 ± 0.48 12 weeks after administration. The scores improved significantly 4 weeks after administration (p < 0.05) and even 12 weeks after continuous administration. Among the 16 study patients, 9 patients (1 men, 8 women) were received lanthanum carbonate continuously for 52 weeks. The constipation score was 3.74 ± 1.92 at the start of administration, 1.37 ± 0.56 12 weeks after administration, and 1.85 ± 0.63 52 weeks after administration, with significant improvement even 52 weeks after administration (p < 0.05). This study shows that substituting sevelamar hydrochloride with lanthanum carbonate improves constipation symptoms in hemodialysis patients from an early stage, which indicates its usefulness in improving constipation symptoms caused by sevelamar hydrochloride.

  18. Preparation and controlled release of mesoporous MCM-41/propranolol hydrochloride composite drug.

    PubMed

    Zhai, Qing-Zhou

    2013-01-01

    This article used MCM-41 as a carrier for the assembly of propranolol hydrochloride by the impregnation method. By means of chemical analysis, powder X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FT-IR) spectroscopy and low-temperature N(2) adsorption-desorption at 77 K, the characterization was made for the prepared materials. The propranolol hydrochloride guest assembly capacity was 316.20 ± 0.31 mg/g (drug/MCM-41). Powder XRD test results indicated that during the process of incorporation, the frameworks of the MCM-41 were not destroyed and the crystalline degrees of the host-guest nanocomposite materials prepared still remained highly ordered. Characterization by SEM and TEM showed that the composite material presented spherical particle and the average particle size of composite material was 186 nm. FT-IR spectra showed that the MCM-41 framework existed well in the (MCM-41)-propranolol hydrochloride composite. Low-temperature nitrogen adsorption-desorption results at 77 K showed that the guest partially occupied the channels of the molecular sieves. Results of the release of the prepared composite drug in simulated body fluid indicated that the drug can release up to 32 h and its maximum released amount was 99.20 ± 0.11%. In the simulated gastric juice release pattern of drug, the maximum time for the drug release was discovered to be 6 h and the maximum cumulative released amount of propranolol hydrochloride was 45.13 ± 0.23%. The drug sustained-release time was 10 h in simulated intestinal fluid and the maximum cumulative released amount was 62.05 ± 0.13%. The prepared MCM-41 is a well-controlled drug delivery carrier.

  19. Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application.

    PubMed

    Mahmood, Syed; Taher, Muhammad; Mandal, Uttam Kumar

    2014-01-01

    Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer and osteoporosis in post-menopausal women, shows poor oral bioavailability of 2%. The aim of this study was to develop, statistically optimize, and characterize raloxifene hydrochloride-loaded transfersomes for transdermal delivery, in order to overcome the poor bioavailability issue with the drug. A response surface methodology experimental design was applied for the optimization of transfersomes, using Box-Behnken experimental design. Phospholipon(®) 90G, sodium deoxycholate, and sonication time, each at three levels, were selected as independent variables, while entrapment efficiency, vesicle size, and transdermal flux were identified as dependent variables. The formulation was characterized by surface morphology and shape, particle size, and zeta potential. Ex vivo transdermal flux was determined using a Hanson diffusion cell assembly, with rat skin as a barrier medium. Transfersomes from the optimized formulation were found to have spherical, unilamellar structures, with a homogeneous distribution and low polydispersity index (0.08). They had a particle size of 134±9 nM, with an entrapment efficiency of 91.00%±4.90%, and transdermal flux of 6.5±1.1 μg/cm(2)/hour. Raloxifene hydrochloride-loaded transfersomes proved significantly superior in terms of amount of drug permeated and deposited in the skin, with enhancement ratios of 6.25±1.50 and 9.25±2.40, respectively, when compared with drug-loaded conventional liposomes, and an ethanolic phosphate buffer saline. Differential scanning calorimetry study revealed a greater change in skin structure, compared with a control sample, during the ex vivo drug diffusion study. Further, confocal laser scanning microscopy proved an enhanced permeation of coumarin-6-loaded transfersomes, to a depth of approximately160 μM, as compared with rigid liposomes. These ex vivo findings proved that a raloxifene hydrochloride

  20. Application of Design of Experiment for Floating Drug Delivery of Tapentadol Hydrochloride

    PubMed Central

    Jagdale, Swati C.; Patil, Somnath; Kuchekar, Bhanudas S.

    2013-01-01

    The aim of the present study was to apply design of experiment (DOE) to optimize floating drug delivery of tapentadol hydrochloride. Tapentadol hydrochloride is a synthetic opioid used as a centrally acting analgesic and effective in both experimental and clinical pain. The half-life of the drug is about 4 hours and oral dose is 50 to 250 mg twice a day. For optimization 32 full factorial design was employed for formulation of tapentadol hydrochloride tablets. Sodium bicarbonate was incorporated as a gas-generating agent. Combination of polymers Xanthan gum and Locust bean gum was used to achieve controlled release effect. The concentration of polymers was considered as the independent variables and dependent variables were floating lag time and swelling index of the tablets. From the factorial batches, it was observed that formulation containing combination of 20% sodium bicarbonate and 10% citric acid shows optimum floating ability whereas the formulation containing 20% Xanthan gum and 28% Locust bean gum shows optimum sustained drug release pattern with adequate floating. PMID:23878616