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Sample records for 3-methyl-2-benzothiazolinone hydrazone hydrochloride

  1. Highly sensitive reaction of nitrate with brucine and 3-methyl-2-benzothiazolinone hydrazone hydrochloride for the determination of nitrate in environmental samples.

    PubMed

    Nagaraja, Padmarajaiah; Kumar, Mattighatta Hemantha; Yathirajan, Hemmige; Prakash, Jainara

    2003-06-01

    A modified and highly sensitive spectrophotometric method for the determination of nitrate in trace quantities in environmental samples is described. The method is based on the reaction of nitrate ion with brucine and 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in sulfuric acid medium to yield a violet-colored product which is stable for over two days. The optimum photometric range for the determination of nitrate is 0.04-0.16 microg cm(-3) and the Sandell's sensitivity being 0.000279 microg cm(-2). The proposed method is applied to various water samples and the results indicate that the reaction is highly sensitive than the original brucine method.

  2. Simple and sensitive method for the quantification of total bilirubin in human serum using 3-methyl-2-benzothiazolinone hydrazone hydrochloride as a chromogenic probe

    NASA Astrophysics Data System (ADS)

    Nagaraja, Padmarajaiah; Avinash, Krishnegowda; Shivakumar, Anantharaman; Dinesh, Rangappa; Shrestha, Ashwinee Kumar

    2010-11-01

    We here describe a new spectrophotometric method for measuring total bilirubin in serum. The method is based on the cleavage of bilirubin giving formaldehyde which further reacts with diazotized 3-methyl-2-benzothiazolinone hydrazone hydrochloride giving blue colored solution with maximum absorbance at 630 nm. Sensitivity of the developed method was compared with Jendrassik-Grof assay procedure and its applicability has been tested with human serum samples. Good correlation was attained between both methods giving slope of 0.994, intercept 0.015, and R2 = 0.997. Beers law obeyed in the range of 0.068-17.2 μM with good linearity, absorbance y = 0.044 Cbil + 0.003. Relative standard deviation was 0.006872, within day precision ranged 0.3-1.2% and day-to-day precision ranged 1-6%. Recovery of the method varied from 97 to 102%. The proposed method has higher sensitivity with less interference. The obtained product was extracted and was spectrally characterized for structural confirmation with FT-IR, 1H NMR.

  3. Mixed ligand complex via zinc(II)-mediated in situ oxidative heterocyclization of hydrochloride salt of 2-chlorobenzaldehyde hydralazine hydrazone as potential of antihypertensive agent.

    PubMed

    Bakale, Raghavendra P; Naik, Ganesh N; Mangannavar, Chandrashekhar V; Muchchandi, Iranna S; Shcherbakov, I N; Frampton, Chris; Gudasi, Kalagouda B

    2014-02-12

    An unusual tetrahedral mixed ligand Zn(II) complex ZnT(L)Cl, where L = 2-chlorobenzaldehyde hydralazine hydrazone and T = in situ generated 3-(2-chlorophenyl)-1,2,4-triazolo[3,4-a]phthalazine is reported. Structure of the fused triazole has been confirmed by single crystal X-ray diffraction studies. Structure of Co(II), Ni(II), Cu(II) and Zn(II) complexes has been confirmed by spectral and analytical methods. Metal complexes have exhibited better activity in the fructose induced hypertension studies in animal model and are comparable with the standard.

  4. Development and validation of sensitive kinetic spectrophotometric method for the determination of moxifloxacin antibiotic in pure and commercial tablets

    NASA Astrophysics Data System (ADS)

    Ashour, Safwan; Bayram, Roula

    2015-04-01

    New, accurate, sensitive and reliable kinetic spectrophotometric method for the assay of moxifloxacin hydrochloride (MOXF) in pure form and pharmaceutical formulations has been developed. The method involves the oxidative coupling reaction of MOXF with 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH) in the presence of Ce(IV) in an acidic medium to form colored product with lambda max at 623 and 660 nm. The reaction is followed spectrophotometrically by measuring the increase in absorbance at 623 nm as a function of time. The initial rate and fixed time methods were adopted for constructing the calibration curves. The linearity range was found to be 1.89-40.0 μg mL-1 for initial rate and fixed time methods. The limit of detection for initial rate and fixed time methods is 0.644 and 0.043 μg mL-1, respectively. Molar absorptivity for the method was found to be 0.89 × 104 L mol-1 cm-1. Statistical treatment of the experimental results indicates that the methods are precise and accurate. The proposed method has been applied successfully for the estimation of moxifloxacin hydrochloride in tablet dosage form with no interference from the excipients. The results are compared with the official method.

  5. A novel use of oxidative coupling reactions for determination of some statins (cholesterol-lowering drugs) in pharmaceutical formulations

    NASA Astrophysics Data System (ADS)

    Ashour, Safwan; Bahbouh, Mahmoud; Khateeb, Mouhammed

    2011-03-01

    New, accurate and reliable spectrophotometric methods for the assay of three statin drugs, atorvastatin calcium (AVS), fluvastatin sodium (FVS) and pravastatin sodium (PVS) in pure form and pharmaceutical formulations have been described. All methods involve the oxidative coupling reaction of AVS, FVS and PVS with 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH) in the presence of Ce(IV) in an acidic medium to form colored products with λmax at 566, 615 and 664 nm, respectively. Beer's law was obeyed in the ranges of 2.0-20.0, 4.9-35.4 and 7.0-30.0 μg mL -1 for AVS-MBTH, FVS-MBTH and PVS-MBTH, respectively. Molar absorptivities for the above three methods were found to be 3.24 × 10 4, 1.05 × 10 4 and 0.68 × 10 4 L mol -1 cm -1, respectively. Statistical treatment of the experimental results indicates that the methods are precise and accurate. The proposed methods have been applied to the determination of the components in commercial forms with no interference from the excipients. A comparative study between the suggested procedures and the official methods for these compounds in the commercial forms showed no significant difference between the two methods.

  6. A note concerning acetate activation of peroxidative activity of catalases using 2,2'-azino-bis(3-ethylbenzthiazoline)-6-sulfonic acid as a substrate.

    PubMed

    Baker, Warren L; Key, Christopher; Lonergan, Greg T

    2005-01-01

    Beef liver catalases showed peroxidative activity using 2,2'-azino-bis-(3-ethylbenzthiazoline)-6-sulfonic acid as the electron donor and hydrogen peroxide as the acceptor at a pH of 5. This activity was not observed at pH 7. The reaction depended on acetate concentration, although succinate and propionate could partly replace the acetate as a catalyst. Other haem proteins also catalyzed a peroxidative effect. The reaction using syringaldazine or the coupling between dimethylaminobenzoic acid and 3-methyl-2-benzothiazolinone hydrazone was less effective and less sensitive. Evidence is presented that the reaction is associated with a conformational change of the catalase. PMID:15932252

  7. Ultrastructural and Immunocytochemical Studies on the H2O2-Producing Enzyme Pyranose Oxidase in Phanerochaete chrysosporium Grown under Liquid Culture Conditions

    PubMed Central

    Daniel, Geoffrey; Volc, Jindrich; Kubatova, Elena; Nilsson, Thomas

    1992-01-01

    The ultrastructural distribution of the sugar-oxidizing enzyme pyranose 2-oxidase (POD) in hyphae of Phanerochaete chrysosporium K-3 grown under liquid culture conditions optimal for the enzyme's production was studied by transmission electron microscopy immunocytochemistry. Using the 3-dimethylaminobenzoic acid-3-methyl-2-benzothiazolinone hydrazone hydrochloride H2O2 peroxidase spectrophotometric assay, POD was detected in mycelial extracts from days 7 to 18, with maximum activity recorded on day 12. Onset of POD activity occurred in the secondary phase of hyphal development at a time of stationary growth, glucose limitation, and pH increase. POD was also detected extracellularly in the culture fluid from days 7 to 18, with maximum activity recorded on day 13. At early stages of development (3 to 4 days), using anti-POD antibodies and immunogold labeling, POD was localized in multivesicular and electron-dense bodies and in cell membrane regions. After 10 to 12 days of growth, at maximum POD activity, POD was concentrated within the periplasmic space where it was associated with membrane-bound vesicles and other membrane structures. At later stages of development (17 to 18 days), when the majority of hyphae were lysed, POD was observed associated with residual intracellular membrane systems and vesicles. Transmission electron microscopy immunocytochemical studies also demonstrated an extracellular distribution of the enzyme at the stationary growth phase, showing its association with fungal extracellular slime. In studies of ligninolytic cultures of the same fungus, POD was found to have a similar intracellular and extracellular distribution in slime as that recorded for cultures grown with cornsteep. POD's peripheral cytoplasmic distribution shows similarities to the cellular distribution of that reported previously for H2O2-dependent lignin and manganese peroxidases in P. chrysosporium. Images PMID:16348809

  8. Glucosamine hydrochloride

    MedlinePlus

    ... additional ingredients are frequently chondroitin sulfate, MSM, or shark cartilage. Some people think these combinations work better ... to the skin in combination with chondroitin sulfate, shark cartilage, and camphor for osteoarthritis. Glucosamine hydrochloride is ...

  9. Therapeutic Potential of Hydrazones as Anti-Inflammatory Agents

    PubMed Central

    Bala, Suman; Sharma, Neha; Saini, Vipin

    2014-01-01

    Hydrazones are a special class of organic compounds in the Schiff base family. Hydrazones constitute a versatile compound of organic class having basic structure (R1R2C=NNR3R4). The active centers of hydrazone, that is, carbon and nitrogen, are mainly responsible for the physical and chemical properties of the hydrazones and, due to the reactivity toward electrophiles and nucleophiles, hydrazones are used for the synthesis of organic compound such as heterocyclic compounds with a variety of biological activities. Hydrazones and their derivatives are known to exhibit a wide range of interesting biological activities like antioxidant, anti-inflammatory, anticonvulsant, analgesic, antimicrobial, anticancer, antiprotozoal, antioxidant, antiparasitic, antiplatelet, cardioprotective, anthelmintic, antidiabetic, antitubercular, trypanocidal, anti-HIV, and so forth. The present review summarizes the efficiency of hydrazones as potent anti-inflammatory agents. PMID:25383223

  10. Hydrazones as Singular Reagents in Asymmetric Organocatalysis.

    PubMed

    de Gracia Retamosa, María; Matador, Esteban; Monge, David; Lassaletta, José M; Fernández, Rosario

    2016-09-12

    This Minireview summarizes strategies and developments regarding the use of hydrazones as reagents in asymmetric organocatalysis, their distinct roles in nucleophile-electrophile, cycloaddition, and cyclization reactions. The key structural elements governing the reactivity of these reagents in a preferred pathway will be discussed, as well as their different interactions with organocatalysts, leading to diverse activation modes. Along these studies, the synthetic equivalence of N-monoalkyl, N,N-dialkyl, and N-acyl hydrazones with several synthons is also highlighted. Emphasis is also put on the mechanistic studies performed to understand the observed reactivities. Finally, the functional group transformations performed from the available products has also been analyzed, highlighting the synthetic value of these methodologies, which served to access numerous families of valuable multifunctional compounds and nitrogen-containing heterocycles.

  11. Hydrazones as Singular Reagents in Asymmetric Organocatalysis.

    PubMed

    de Gracia Retamosa, María; Matador, Esteban; Monge, David; Lassaletta, José M; Fernández, Rosario

    2016-09-12

    This Minireview summarizes strategies and developments regarding the use of hydrazones as reagents in asymmetric organocatalysis, their distinct roles in nucleophile-electrophile, cycloaddition, and cyclization reactions. The key structural elements governing the reactivity of these reagents in a preferred pathway will be discussed, as well as their different interactions with organocatalysts, leading to diverse activation modes. Along these studies, the synthetic equivalence of N-monoalkyl, N,N-dialkyl, and N-acyl hydrazones with several synthons is also highlighted. Emphasis is also put on the mechanistic studies performed to understand the observed reactivities. Finally, the functional group transformations performed from the available products has also been analyzed, highlighting the synthetic value of these methodologies, which served to access numerous families of valuable multifunctional compounds and nitrogen-containing heterocycles. PMID:27552942

  12. New trimethylaluminum-induced mannich-type reaction of hydrazones.

    PubMed

    El Kaim, Laurent; Grimaud, Laurence; Perroux, Yannick; Tirla, Cornelia

    2003-10-31

    Trimethylaluminum addition to N-monoalkyl or N-monoaryl hydrazones followed by aldehyde addition leads to the formation of N-alkylated hydrazones in a new formal Mannich-type process. Addition compounds were also obtained in moderate yields with ketones. The mechanism as well as possible intermediates involved in the reaction are discussed.

  13. Bupropion Hydrochloride.

    PubMed

    Khan, S R; Berendt, R T; Ellison, C D; Ciavarella, A B; Asafu-Adjaye, E; Khan, M A; Faustino, P J

    2016-01-01

    Bupropion hydrochloride is a norepinephrine-dopamine disinhibitor (NDDI) approved for the treatment of depression and smoking cessation. Bupropion is a trimethylated monocyclic phenylaminoketone second-generation antidepressant, which differs structurally from most antidepressants, and resides in a novel mechanistic class that has no direct action on the serotonin system. Comprehensive chemical, physical, and spectroscopic profiles are presented. This analytical profile provides an extensive spectroscopic investigation utilizing mass spectrometry, one- and two-dimensional NMR, solid-state NMR, IR, NIR, Raman, UV, and X-ray diffraction. The profile also includes significant wet chemistry studies for pH, solubility, solution, and plasma stability. Both HPLC and UPLC methodology are presented for bupropion and its related impurities or major metabolites. The profile concludes with an overview of biological properties that includes toxicity, drug metabolism, and pharmacokinetics.

  14. Study and characterization of polyphenol oxidase from eggplant (Solanum melongena L.).

    PubMed

    Todaro, Aldo; Cavallaro, Rosalinda; Argento, Sergio; Branca, Ferdinando; Spagna, Giovanni

    2011-10-26

    In this study the catecholase and cresolase activities of eggplant polyphenol oxidase (PPO) were investigated. Enzyme activity was determined by measuring the increase in absorbance using catechol as substrate and 3-methyl-2-benzothiazolinone hydrazone (MBTH) as coupled reagent. The effects of substrate specificity, heat inactivation, temperature, pH, and inhibitors were investigated to understand the enzymatic alteration of ready-to-eat preparations. Browning of vegetables was determined through a colorimeter. Decrease of lightness (L*) and increase of color difference values (ΔE*) were correlated with tissue browning. Antibrowning agents were tested on PPO under the same conditions. The enzyme activity was strongly inhibited by 0.4 M citric acid. Under natural pH conditions, the enzyme was also inhibited by tartaric acid and acetic acid. All of the results were used to understand the best conditions for food transformation (ready-to-eat and grilled eggplant slices). PMID:21942648

  15. Study and characterization of polyphenol oxidase from eggplant (Solanum melongena L.).

    PubMed

    Todaro, Aldo; Cavallaro, Rosalinda; Argento, Sergio; Branca, Ferdinando; Spagna, Giovanni

    2011-10-26

    In this study the catecholase and cresolase activities of eggplant polyphenol oxidase (PPO) were investigated. Enzyme activity was determined by measuring the increase in absorbance using catechol as substrate and 3-methyl-2-benzothiazolinone hydrazone (MBTH) as coupled reagent. The effects of substrate specificity, heat inactivation, temperature, pH, and inhibitors were investigated to understand the enzymatic alteration of ready-to-eat preparations. Browning of vegetables was determined through a colorimeter. Decrease of lightness (L*) and increase of color difference values (ΔE*) were correlated with tissue browning. Antibrowning agents were tested on PPO under the same conditions. The enzyme activity was strongly inhibited by 0.4 M citric acid. Under natural pH conditions, the enzyme was also inhibited by tartaric acid and acetic acid. All of the results were used to understand the best conditions for food transformation (ready-to-eat and grilled eggplant slices).

  16. Pyranose Oxidase, a Major Source of H2O2 during Wood Degradation by Phanerochaete chrysosporium, Trametes versicolor, and Oudemansiella mucida

    PubMed Central

    Daniel, Geoffrey; Volc, Jindrich; Kubatova, Elena

    1994-01-01

    The production of the H2O2-generating enzyme pyranose oxidase (POD) (EC 1.1.3.10) (synonym, glucose 2-oxidase), two ligninolytic peroxidases, and laccase in wood decayed by three white rot fungi was investigated by correlated biochemical, immunological, and transmission electron microscopic techniques. Enzyme activities were assayed in extracts from decayed birch wood blocks obtained by a novel extraction procedure. With the coupled peroxidase-chromogen (3-dimethylaminobenzoic acid plus 3-methyl-2-benzothiazolinone hydrazone hydrochloride) spectrophotometric assay, the highest POD activities were detected in wood blocks degraded for 4 months and were for Phanerochaete chrysosporium (149 mU g [dry weight] of decayed wood-1), Trametes versicolor (45 mU g-1), and Oudemansiella mucida (1.2 mU g-1), corresponding to wood dry weight losses of 74, 58, and 13%, respectively. Mn-dependent peroxidase activities in the same extracts were comparable to those of POD, while lignin peroxidase activity was below the detection limit for all fungi with the veratryl alcohol assay. Laccase activity was high with T. versicolor (422 mU g-1 after 4 months), in trace levels with O. mucida, and undetectable in P. chrysosporium extracts. Evidence for C-2 specificity of POD was shown by thin-layer chromatography detection of 2-keto-d-glucose as the reaction product. By transmission electron microscopy-immunocytochemistry, POD was found to be preferentially localized in the hyphal periplasmic space of P. chrysosporium and O. mucida and associated with membranous materials in hyphae growing within the cell lumina or cell walls of partially and highly degraded birch fibers. An extracellular distribution of POD associated with slime coating wood cell walls was also noted. The periplasmic distribution in hyphae and extracellular location of POD are consistent with the reported ultrastructural distribution of H2O2-dependent Mn-dependent peroxidases. This fact and the dominant presence of POD and

  17. [Sevelamer:hydrochloride].

    PubMed

    Hyodo, Toru; Taira, Takayasu; Wakai, Haruki; Takemura, Toru; Yamamoto, Sumiko; Yashida, Kazunari; Baba, Shiro

    2005-01-01

    The recent global breakthrough in the field of renal osteodystrophy is the inhibitory effect of sevelamer hydrochloride on the progression of coronary artery calcification, which was revealed with EBCT (Electron beam computed tomography) 1) approximately 3). It has been found that the degree of coronary artery calcification assessed with EBCT is proportional to the mortality risk by the coronary artery stenosis and by myocardial infarction in non-hemodialysis patients 4) approximately 10). In 2004 in Japan Matsuoka and Iseki et al showed for the first time in the world that coronary artery calcification assessed by EBCT was correlated with mortality 11). In Japan, however, it is difficult to administer sevelamer hydrochloride to many patients because of constipation as its side effect. Its prescription rate is 26.8% and its single administration rate is only 15.4% 12). We explained fully to the patients that sevelamer hydrochloride seldom caused coronary artery calcification. And we used sorbitol, an osmotic purgatives, with sevelamer hydrochloride. Moreover, we gradually replaced calcium carbonate with sevelamer hydrochloride in supper at first. With protocol above, we succeeded in having 86.7% of the patients take sevelamer hydrochloride 12). We think that it is important to increase the intake rate of sevelamer hydrochloride in order to prevent coronary artery calcification and to aim at the long survival of the patients. PMID:15632474

  18. Drug release from hydrazone-containing peptide amphiphiles

    SciTech Connect

    Matson, John B.; Stupp, Samuel I.

    2012-03-15

    Hydrolytically-labile hydrazones in peptide amphiphiles were studied as degradable tethers for release of the drug nabumetone from nanofiber gels. On-resin addition of the novel compound tri-Boc-hydrazido adipic acid to a lysine E-amine allowed for precise placement of a hydrazide in a peptide sequence.

  19. 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.

  20. 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.

  1. A practical approach to semicarbazone and hydrazone derivatives via imino-isocyanates.

    PubMed

    Garland, Keira; Gan, Wei; Depatie-Sicard, Charlotte; Beauchemin, André M

    2013-08-16

    Complex hydrazone derivatives can be accessed readily from hydrazones upon heating in the presence of nucleophiles. This reactivity likely involves imino-isocyanate intermediates, and a variety of leaving groups can be used at temperatures ranging from 20 to 150 °C. Alcohols, thiols, primary, and secondary amines can be used as nucleophiles, thus providing a simple alternative to the synthesis of hydrazones via condensation on the parent carbonyl precursor and allowing late-stage derivatization.

  2. Antioxidant activity of hydrazones with sterically hindered phenol fragments

    NASA Astrophysics Data System (ADS)

    Nikolaevskii, A. N.; Kniga, O. P.; Khizhan, E. I.; Tikhonova, G. A.; Vinogradov, V. V.; Khizhan, A. I.

    2012-12-01

    Kinetic parameters of the antiradical activity of derivatives of hydrazones of 4-hydroxy-3,5-di- tert-butyl-benzaldehyde are determined photocolorimetrically in their reactions with a stable diphenylpicrylhydrazyl radical, and by chemiluminescence from the capture of peroxide radicals upon the initiated oxidation of ethylbenzene. It is found that during inhibited oxidation, the reactive centers (N-H and O-H) in hetaryl- and acylhydrazone molecules operate in parallel. Regularities of the compounds' inhibiting effect are studied in heterogeneous systems upon the initiated oxidation of ethylbenzene in emulsion, and in a water-lipid model of the oxidation of phosphatidylcholine dispersion. It is established that hydrazone derivatives are antioxidants of combined action in heterophase processes of the oxidation of unsaturated substrates, displaying properties of hydroperoxide deactivators in addition to their antiradical activity.

  3. Diaryl hydrazones as multifunctional inhibitors of amyloid self-assembly.

    PubMed

    Török, Béla; Sood, Abha; Bag, Seema; Tulsan, Rekha; Ghosh, Sanjukta; Borkin, Dmitry; Kennedy, Arleen R; Melanson, Michelle; Madden, Richard; Zhou, Weihong; Levine, Harry; Török, Marianna

    2013-02-19

    The design and application of an effective, new class of multifunctional small molecule inhibitors of amyloid self-assembly are described. Several compounds based on the diaryl hydrazone scaffold were designed. Forty-four substituted derivatives of this core structure were synthesized using a variety of benzaldehydes and phenylhydrazines and characterized. The inhibitor candidates were evaluated in multiple assays, including the inhibition of amyloid β (Aβ) fibrillogenesis and oligomer formation and the reverse processes, the disassembly of preformed fibrils and oligomers. Because the structure of the hydrazone-based inhibitors mimics the redox features of the antioxidant resveratrol, the radical scavenging effect of the compounds was evaluated by colorimetric assays against 2,2-diphenyl-1-picrylhydrazyl and superoxide radicals. The hydrazone scaffold was active in all of the different assays. The structure-activity relationship revealed that the substituents on the aromatic rings had a considerable effect on the overall activity of the compounds. The inhibitors showed strong activity in fibrillogenesis inhibition and disassembly, and even greater potency in the inhibition of oligomer formation and oligomer disassembly. Supporting the quantitative fluorometric and colorimetric assays, size exclusion chromatographic studies indicated that the best compounds practically eliminated or substantially inhibited the formation of soluble, aggregated Aβ species, as well. Atomic force microscopy was also applied to monitor the morphology of Aβ deposits. The compounds also possessed the predicted antioxidant properties; approximately 30% of the synthesized compounds showed a radical scavenging effect equal to or better than that of resveratrol or ascorbic acid.

  4. Novel dehydrogenase catalyzes oxidative hydrolysis of carbon-nitrogen double bonds for hydrazone degradation.

    PubMed

    Itoh, Hideomi; Suzuta, Tetsuya; Hoshino, Takayuki; Takaya, Naoki

    2008-02-29

    Hydrazines and their derivatives are versatile artificial and natural compounds that are metabolized by elusive biological systems. Here we identified microorganisms that assimilate hydrazones and isolated the yeast, Candida palmioleophila MK883. When cultured with adipic acid bis(ethylidene hydrazide) as the sole source of carbon, C. palmioleophila MK883 degraded hydrazones and accumulated adipic acid dihydrazide. Cytosolic NAD+- or NADP+-dependent hydrazone dehydrogenase (Hdh) activity was detectable under these conditions. The production of Hdh was inducible by adipic acid bis(ethylidene hydrazide) and the hydrazone, varelic acid ethylidene hydrazide, under the control of carbon catabolite repression. Purified Hdh oxidized and hydrated the C=N double bond of acetaldehyde hydrazones by reducing NAD+ or NADP+ to produce relevant hydrazides and acetate, the latter of which the yeast assimilated. The deduced amino acid sequence revealed that Hdh belongs to the aldehyde dehydrogenase (Aldh) superfamily. Kinetic and mutagenesis studies showed that Hdh formed a ternary complex with the substrates and that conserved Cys is essential for the activity. The mechanism of Hdh is similar to that of Aldh, except that it catalyzed oxidative hydrolysis of hydrazones that requires adding a water molecule to the reaction catalyzed by conventional Aldh. Surprisingly, both Hdh and Aldh from baker's yeast (Ald4p) catalyzed the Hdh reaction as well as aldehyde oxidation. Our findings are unique in that we discovered a biological mechanism for hydrazone utilization and a novel function of proteins in the Aldh family that act on C=N compounds. PMID:18096698

  5. Structural and spectroscopic investigation on a new potentially bioactive di-hydrazone containing thiophene heterocyclic rings

    NASA Astrophysics Data System (ADS)

    Nogueira, Vanessa de S.; Ramalho Freitas, Maria Clara; Cruz, Wellington S.; Ribeiro, Tatiana S.; Resende, Jackson A. L. C.; Rey, Nicolás A.

    2016-02-01

    Hydrazones and several substituted hydrazones are associated with a broad spectrum of biological activities, as well as compounds containing the thiophene ring. In this context, a novel di-hydrazone derived from 2-thiophenecarboxylic acid hydrazide was synthesized and completely characterized by elemental analysis, XRD, FT-IR, Raman and UV-Vis spectroscopies, thermogravimetry, 1H NMR, 1H-1H COSY and 1H-1H ROESY. A preliminary in silico pharmacological evaluation was also performed in order to assess the performance of the new compound regarding some molecular properties relevant for a drug's pharmacokinetics in the human body.

  6. Photochemistry of phenazopyridine hydrochloride.

    PubMed

    Iqbal, J; Gupta, A; Husain, A

    2006-09-01

    Phenazopyridine hydrochloride (1) is an azo dye with local analgesic and anaesthetic effects on the urinary tract. Its photochemistry was studied in different reaction media including the drug adsorbed on silica gel. This resulted in photochemical cyclodehydrogenation, reductive photodegradation and rearrangement of the drug molecule. Four major products were isolated and identified on the basis of IR, NMR and mass spectral studies. The products are: pyrido[3,4-c]cinnoline-2,4-diamine (2), N3-phenylpyridine-2,3,4,6-tetraamine (3), pyridine-2,3,6-triamine (4), 2,6-diamino-1-(4-aminophenyl)pyridin-4(1H)-one (5).

  7. Synthesis and Biological Activities of Camphor Hydrazone and Imine Derivatives

    PubMed Central

    da Silva, Emerson T.; da Silva Araújo, Adriele; Moraes, Adriana M.; de Souza, Leidiane A.; Silva Lourenço, Maria Cristina; de Souza, Marcus V. N.; Wardell, James L.; Wardell, Solange M. S. V.

    2015-01-01

    Both sonochemical and classical methodologies have been employed to convert camphor, 1,7,7-trimethylbicyclo[2.2.1]heptan-2-one, C9H16C=O, into a number of derivatives including hydrazones, C9H16C=N-NHAr 3, imines, C9H16C=N-R 7, and the key intermediate nitroimine, C9H16C=N-NO2 6. Reactions of nitroamine 6 with nucleophiles by classical methods provided the desired compounds in a range of yields. In evaluations of activity against Mycobacterium tuberculosis, compound 7j exhibited the best activity (minimal inhibitory concentration (MIC) = 3.12 µg/mL), comparable to that of the antitubercular drug ethambutol. The other derivatives displayed modest antimycobacterial activities at 25–50 µg/mL. In in vitro tests against cancer cell lines, none of the synthesized camphor compounds exhibited cytotoxic activities.

  8. The antibacterial activity of some sulfonamides and sulfonyl hydrazones, and 2D-QSAR study of a series of sulfonyl hydrazones

    NASA Astrophysics Data System (ADS)

    Aslan, H. Güzin; Özcan, Servet; Karacan, Nurcan

    2012-12-01

    Benzenesulfonicacid-1-methylhydrazide (1) and its four aromatic sulfonyl hydrazone derivatives (1a-1d), N-(3-amino-2-hydroxypropyl)benzene sulfonamide (2) and N-(2-hydroxyethyl)benzenesulfonamide (3) were synthesized and their structures were determined by IR, 1H NMR, 13C NMR, and LCMS techniques. Antibacterial activities of new synthesized compounds were evaluated against various bacteria strains by microdilution and disk diffusion methods. The experimental results show that presence of OH group on sulfonamides reduces the antimicrobial activity, and antimicrobial activities of the sulfonyl hydrazones (1a-1d) are smaller than that of the parent sulfonamide (1), except Candida albicans. In addition, 2D-QSAR analysis was performed on 28 aromatic sulfonyl hydrazones as antimicrobial agents against Escherichia coli and Staphylococcus aureus. In the QSAR models, the most important descriptor is total point-charge component of the molecular dipole for E. coli, and partial negative surface area (PNSA-1) for S. aureus.

  9. Simple hydrazone building blocks for complicated functional materials.

    PubMed

    Tatum, Luke A; Su, Xin; Aprahamian, Ivan

    2014-07-15

    CONSPECTUS: The ability to selectively and effectively control various molecular processes via specific stimuli is a hallmark of the complexity of biological systems. The development of synthetic structures that can mimic such processes, even on the fundamental level, is one of the main goals of supramolecular chemistry. Having this in mind, there has been a foray of research in the past two decades aimed at developing molecular architectures, whose properties can be modulated using external inputs. In most cases, reversible conformational, configurational, or translational motions, as well as bond formation or cleavage reactions have been used in such modulations, which are usually initiated using inputs including, irradiation, metalation, or changes in pH. This research activity has led to the development of a diverse array of impressive adaptive systems that have been used in showcasing the potential of molecular switches and machines. That being said, there are still numerous obstacles to be tackled in the field, ranging from difficulties in getting molecular switches to communicate and work together to complications in integrating and interfacing them with surfaces and bulk materials. Addressing these challenges will necessitate the development of creative new approaches in the field, the improvement of the currently available materials, and the discovery of new molecular switches. This Account will describe how our quest to design new molecular switches has led us to the development of structurally simple systems that can be used for complicated functions. Our focus on the modular and tunable hydrazone functional group was instigated by the desire to simplify the structure and design of molecular switches in order to circumvent multistep synthesis. We hypothesized that by avoiding this synthetic bottleneck, which is one of the factors that hinder fast progress in the field, we can expedite the development and deployment of our adaptive materials. It should be

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

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 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....

  11. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 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....

  12. 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....

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

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 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. Synthesis, spectroscopic characterizations, crystal structures and DFT studies of nalidixic acid carbonyl hydrazones derivatives

    NASA Astrophysics Data System (ADS)

    Bergamini, F. R. G.; Ribeiro, M. A.; Lancellotti, M.; Machado, D.; Miranda, P. C. M. L.; Cuin, A.; Formiga, A. L. B.; Corbi, P. P.

    2016-09-01

    This article describes the synthesis and characterization of the 1-ethyl-7-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carbohydrazide (hzd) and six carbonyl hydrazones derivatives of the nalidixic with 1H-pyrrol-2-ylmethylidene (hpyrr), 1H-imidazol-2-ylmethylidene (h2imi), pyridin-2-ylmethylidene (h2py), pyridin-3-ylmethylidene (h3py), pyridin-4-ylmethylidene(h4py) and (2-hydroxyphenyl)methylidene (hsali). The carbonyl hydrazones were characterized by elemental and ESI-QTOF-MS analyses, IR and detailed NMR spectroscopic measurements. The 2D NMR experiments allowed the unambiguous assignment of the hydrogen, carbon and nitrogen atoms, which have not been reported for nalidixic acid carbonyl hydrazone derivatives so far. Crystal structures of hzd and the new carbonyl hydrazones h2imi, hpyrr and h3py were determined by X-ray diffraction studies. Although the synthesis of hzd was reported decades ago, the hzd crystal structure have not been reported yet. Geometric optimizations of all the characterized structures were performed with the aid of DFT studies. Despite the fact that the hydrazones with 2-pyridine carboxylic acid (h2py) and salicyl aldehyde (hsali) were already reported by literature, a detailed spectroscopic study followed by DFT studies are also reported for such compounds in this manuscript. Antimicrobial studies of the compounds are also presented.

  15. 21 CFR 582.5875 - Thiamine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 § 582.5875 Thiamine hydrochloride. (a) Product. Thiamine hydrochloride. (b) Conditions of...

  16. 21 CFR 582.5875 - Thiamine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 § 582.5875 Thiamine hydrochloride. (a) Product. Thiamine hydrochloride. (b) Conditions of...

  17. 21 CFR 582.5875 - Thiamine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 § 582.5875 Thiamine hydrochloride. (a) Product. Thiamine hydrochloride. (b) Conditions of...

  18. Synthesis and biological evaluation of hydrazone derivatives as antifungal agents.

    PubMed

    Casanova, Bruna B; Muniz, Mauro N; de Oliveira, Thayse; de Oliveira, Luís Flavio; Machado, Michel M; Fuentefria, Alexandre M; Gosmann, Grace; Gnoatto, Simone C B

    2015-05-20

    Emerging yeasts are among the most prevalent causes of systemic infections with high mortality rates and there is an urgent need to develop specific, effective and non-toxic antifungal agents to respond to this issue. In this study 35 aldehydes, hydrazones and hydrazines were obtained and their antifungal activity was evaluated against Candida species (C. parapsilosis, C. tropicalis, C. krusei, C. albicans, C. glabrata and C. lusitaneae) and Trichosporon asahii, in an in vitro screening. The minimum inhibitory concentrations (MICs) of the active compounds in the screening was determined against 10 clinical isolates of C. parapsilosis and 10 of T. asahii. The compounds 4-pyridin-2-ylbenzaldehyde] (13a) and tert-butyl-(2Z)-2-(3,4,5-trihydroxybenzylidine)hydrazine carboxylate (7b) showed the most promising MIC values in the range of 16-32 μg/mL and 8-16 μg/mL, respectively. The compounds' action on the stability of the cell membrane and cell wall was evaluated, which suggested the action of the compounds on the fungal cell membrane. Cell viability of leukocytes and an alkaline comet assay were performed to evaluate the cytotoxicity. Compound 13a was not cytotoxic at the active concentrations. These results support the discovery of promising candidates for the development of new antifungal agents.

  19. Supramolecular arrangement in mono and bi-camphor acyl hydrazones: A structural study

    NASA Astrophysics Data System (ADS)

    Galvão, Adelino M.; Carvalho, M. Fernanda N. N.; Ferreira, Ana S. D.

    2016-03-01

    New acyl hydrazones were synthesized by condensation with camphorquinone aiming at extending the range of applications of the biologically active camphor compounds and structural studies by XRD, 1H-NMR and IR were used in conjunction with advanced computational methodologies to understand the new structural chemistry enabled by the conjugation of the camphor ketone group to the hydrazone Ndbnd C double bond. In particular, were analysed supramolecular arrangements either by hydrogen bonding to water molecules or electrostatic interactions with non protic solvents. The relative stability of all conformers (E/Z) prompted by the hydrazone bond was addressed by state of the art methods such as CR-CCSD(T) and their inter-conversion in both S0 and S1 by CR-EOM-CCSD(T).

  20. Ruthenium(II) hydrazone Schiff base complexes: Synthesis, spectral study and catalytic applications

    NASA Astrophysics Data System (ADS)

    Manikandan, R.; Viswanathamurthi, P.; Muthukumar, M.

    2011-12-01

    Ruthenium(II) hydrazone Schiff base complexes of the type [RuCl(CO)(B)(L)] (were B = PPh 3, AsPh 3 or Py; L = hydrazone Schiff base ligands) were synthesized from the reactions of hydrazone Schiff base ligand (obtained from isonicotinoylhydrazide and different hydroxy aldehydes) with [RuHCl(CO)(EPh 3) 2(B)] (where E = P or As; B = PPh 3, AsPh 3 or Py) in 1:1 molar ratio. All the new complexes have been characterized by analytical and spectral (FT-IR, electronic, 1H, 13C and 31P NMR) data. They have been tentatively assigned an octahedral structure. The synthesized complexes have exhibited catalytic activity for oxidation of benzyl alcohol to benzaldehyde and cyclohexanol to cyclohexanone in the presence of N-methyl morpholine N-oxide (NMO) as co-oxidant. They were also found to catalyze the transfer hydrogenation of aliphatic and aromatic ketones to alcohols in KOH/Isopropanol.

  1. Synthesis, antioxidant and cytoprotective evaluation of potential antiatherogenic phenolic hydrazones. A structure-activity relationship insight.

    PubMed

    Vanucci-Bacqué, Corinne; Carayon, Chantal; Bernis, Corinne; Camare, Caroline; Nègre-Salvayre, Anne; Bedos-Belval, Florence; Baltas, Michel

    2014-08-01

    A novel series of hydrazones derived from substituted benzaldehydes have been synthesized as potential antiatherogenic agents. Several methods were used for exploring their antioxidant and cytoprotective properties, such as their scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical, the inhibition of superoxide anion (O₂(·-)) generation and the measurement of cell-induced low-density lipoprotein oxidation (monitored by the formation of TBARS). The cytoprotective efficacy was also evaluated by measuring the cell viability (monitored by the MTT assay) in the presence of cytotoxic oxidized LDL. In this report, we discuss the relationship between the chemical structure of phenolic hydrazones and their antioxidant and cytoprotective activities, for subsequent application as antiatherogenic agents. This SAR study confirms that the phenolic frame is not the only prerequisite for antioxidant activity and N-methylbenzothiazole hydrazone moiety magnifies the dual required properties in two most interesting derivatives. PMID:24924425

  2. Synthesis of macrocyclic bis-hydrazone and their use in metal cations extraction.

    PubMed

    Kandil, Farouk; Chebani, Mohamad Khaled; Al Zoubi, Wail

    2012-01-01

    Two new macrocyclic hydrazone Schiff bases were synthesized by reaction of succindihydrazide and adipdihydrazide with acetylacetone. Hydrazones have been characterized by elemental analyses and IR, mass, (1)H NMR, and (13)C NMR spectral data. Hydrazones have been studied by liquid-liquid extraction towards the s-metal ions (Li(+), Na(+), and K(+)) and d-metal ions (Cu(2+) and Cr(3+)) from aqueous phase to organic phase. The effect of chloroform and dichloromethane as organic solvents over the metal chlorides extraction was investigated at 25 ± 0.1°C by using flame atomic absorption. We found differences between the two solvents in extraction selectivity. PMID:24052837

  3. Synthesis, spectral studies and structure of 2-hydroxyacetophenone nicotinic acid hydrazone

    NASA Astrophysics Data System (ADS)

    Sreeja, P. B.; Sreekanth, A.; Nayar, Chandini R.; Prathapachandra Kurup, M. R.; Usman, A.; Razak, I. A.; Chantrapromma, S.; Fun, H. K.

    2003-01-01

    2-Hydroxyacetophenone nicotinic acid hydrazone (H 2ApNH) was synthesized as a part of our work, in search for non-linear optical crystal based on hydrazones, and studied spectroscopically. Complete NMR assignments for the hydrazone was made using COSY homonuclear and HMQC heteronuclear correlation techniques. Solid state reflectance was also studied in order to understand the electronic structure of the synthesized compound. The crystal and molecular structures of H 2ApNH were determined. The compound crystallizes into an orthorhombic lattice with a non-centrosymmetric space group Pca2 1 with two crystallographically unique molecules of in an asymmetric unit. The geometry reveals quasi co planarity in the whole molecular skeleton with localization of the double bonds in the CN-N-CO with an E-configuration.

  4. Comparative metabolism and mutagenicity of azo and hydrazone dyes in the Ames test.

    PubMed

    De France, B F; Carter, M H; Josephy, P D

    1986-02-01

    Enteric bacterial and hepatic azoreductase enzymes are capable of reducing azo dyes to yield the constituent aromatic amines. Azo dyes based on benzidine and benzidine congeners have received particular attention because of their widespread use and the known carcinogenicity of benzidine to humans. Azo dyes based on beta-diketone coupling components exist preferentially as the tautomeric hydrazones. A series of hydrazone dyes based on benzidine and benzidine congeners was prepared and characterized by NMR and UV-visible spectroscopy. These dyes were tested for mutagenicity using a modified Ames assay and, unlike the true azo dyes, showed no significant mutagenic activity. The hydrazone dyes were resistant to enzymatic reduction by FMN-supplemented hamster-liver post-mitochondrial supernatant (S-9); under identical conditions, azo dyes such as trypan blue were rapidly reduced.

  5. Gold-Catalyzed Highly Selective Photoredox C(sp(2) )-H Difluoroalkylation and Perfluoroalkylation of Hydrazones.

    PubMed

    Xie, Jin; Zhang, Tuo; Chen, Fei; Mehrkens, Nina; Rominger, Frank; Rudolph, Matthias; Hashmi, A Stephen K

    2016-02-18

    The first gold-catalyzed photoredox C(sp(2) )-H difluoroalkylation and perfluoroalkylation of hydrazones with readily available RF -Br reagents is reported. The resulting gem-difluoromethylated and perfluoroalkylated hydrazones are highly functionalized, versatile molecules. A mild reduction of the coupling products can efficiently produce gem-difluoromethylated β-amino phosphonic acids and β-amino acid derivatives. In mechanistic studies, a difluoroalkyl radical intermediate was detected by an EPR spin-trapping experiment, indicating that a gold-catalyzed radical pathway is operating. PMID:26800002

  6. Synthesis, characterization and biological evaluation of some 5-methylpyrazine carbohydrazide based hydrazones.

    PubMed

    Ahmad, Mushtaq; Hameed, Shahid; Tahir, Muhammad Nawaz; Israr, Muhammad; Anwar, Muhammad; Shah, Muhammad Abdullah Shah Abdullah; Khan, Shad Ali; Din, Ghiasud

    2016-05-01

    Pyrazine carbohydrazide based hydrazones were synthesized starting from 5-methylpyrazine-2-carboxylic acid. The acid was first converted to its methyl ester, which on further treatment with hydrazine hydrate transformed to carbohydrazide. The carbohydrazide was treated with differently substituted aromatic carbonyl compounds giving hydrazones. Characterization of the synthesized compounds was carried out using modern spectroscopic techniques and unambiguously confirmed through X-ray crystallographic studies of compound 3d. The purity of the compounds was verified using elemental analysis. The target molecules were evaluated for urease inhibition, antioxidant and antimicrobial activity. PMID:27166526

  7. Tridentate hydrazone metal complexes derived from cephalexin and 2-hydrazinopyridine: Synthesis, characterization and antibacterial activity

    NASA Astrophysics Data System (ADS)

    Anacona, J. R.; Rincones, Maria

    2015-04-01

    Metal(II) coordination compounds of a tridentate hydrazone ligand (HL) derived from the condensation of cephalexin antibiotic with 2-hydrazinopyridine were synthesized. The hydrazone ligand and mononuclear [ML(OAc)(H2O)] (M(II) = Mn, Co, Ni, Cu, Zn, Ag) complexes were characterized by several techniques, including elemental and thermal analysis, molar conductance and magnetic susceptibility measurements, electronic, FT-IR, EPR and 1H NMR spectral studies. The cephalexin 2-pyridinylhydrazone ligand HL behaves as a monoanionic tridentate NNO chelating agent. The biological applications of complexes have been studied on three bacteria strains (Escherichia coli, Acinetobacter baumannii and Enterococcus faecalis) by agar diffusion disc method.

  8. Synthesis and biological activities of diflunisal hydrazide-hydrazones.

    PubMed

    Küçükgüzel, S Güniz; Mazi, Adil; Sahin, Fikrettin; Oztürk, Suzan; Stables, James

    2003-01-01

    Several diflunisal hydrazide-hydrazone derivatives namely 2',4'-difluoro-4-hydroxybiphenyl-3-carboxylic acid [(5-nitro-2-furyl/substitutedphenyl)methylene] hydrazide (3a-o) have been synthesised. Methyl 2',4'-difluoro-4-hydroxybiphenyl-3-carboxylate (1) and 2',4'-difluoro-4-hydroxybiphenyl-3-carboxylic acid hydrazide (2) were also synthesised and used as intermediate compounds. All synthesised compounds were screened for their antimycobacterial activity against Mycobacterium tuberculosis H37 Rv, antimicrobial activities against various bacteria, fungi and yeast species. Compound 3a have shown activity against Staphylococcus epidermis HE-5 and Staphylococcus aureus HE-9 at 18.75 and 37.5 microg mL(-1), respectively. Compound 3o have exhibited activity against Acinetobacter calcoaceticus IO-16 at a concentration of 37.5 microg mL(-1), whereas Cefepime, the drug used as standard, have been found less active against the microorganisms mentioned above. The synthesised compounds were found to provide 12-34% inhibition of mycobacterial growth of M. tuberculosis H37 Rv in the primary screen at 6.25 microg mL(-1). Anticonvulsant activity of the compounds were also determined by maximal electroshock (MES) and subcutaneous metrazole (scMET) tests in mice and rats following the procedures of antiepileptic drug development (ADD) program of the National Institutes of Health (NIH). Compound 3k showed 25% protection against MES induced seizures in p.o. rat screening at a dose level of 30 mg kg(-1) whereas 3n and 3o showed neurotoxicity after 4 and 0.5 h at a dose level of 100 and 300 mg kg(-1), respectively. PMID:14642333

  9. Photostabilization of papaverine hydrochloride solutions.

    PubMed

    Piotrowska, Karolina; Hermann, Tadeusz W; Pawelska, Alicja

    2010-01-01

    Abstract: The stability of aqueous and non-aqueous papaverine hydrochloride solutions exposed to the UV radiation is poor. In order to enhance its photo-stability suitable light absorbers may be used. There werefour photo-protectors considered in this work: 4-aminobenzoic acid, sodium benzoate, methyl 4-hydroxybenzoate and propyl 4-hydroxybenzoate, whose UV absorption spectra characteristics match to some extent with the UV spectrum of papaverine. Approximately 20 mg/mL papaverine chloroform solutions with the above non-toxic additives in the concentrations 0.01; 0.05; 0.10% were exposed to the UV light of 254 nm. High performance capillary electrophoresis was used to determine the papaverine hydrochloride concentration loss as a function of time exposition to the light. It was found that papaverine hydrochloride photolysis proceeds according to the first-order kinetics. Methyl 4-hydroxybenzoate was found to be the best UV radiation-protective agent, and at the concentration 0.10%, the reaction rate constant decreases from 0.143 h(-1) to 0.028 h(-1). Both 4-hydroxybenzoate esters develop a more efficient UV radiation-protective activity than sodium benzoate, because the latter additive molar extinction coefficient is less significant. However, in spite of a high value of 4-aminobenzoic acid molar absorptivity coefficient, it is an unsuitable photo-protector for papaverine hydrochloride solutions, because its UV absorption spectrum does not match with that of papaverine.

  10. Development of an indirect competitive ELISA for detection of Campylobacter jejuni subsp.jejuni O:23 in foods.

    PubMed

    Hochel, I; Viochna, D; Skvor, J; Musil, M

    2004-01-01

    An indirect enzyme immunoassay for rapid detection of Campylobacter jejuni subsp. jejuni 0:23 has been developed. Optimum concentrations of immobilized cells, polyclonal chicken IgY, and rabbit anti-IgY antibody-horseradish peroxidase conjugate were 3.1 CFU/nL, 10 microg/mL, and 8 microg/mL, respectively. Under such conditions, the detection limit reached 50 CFU/microL, limit of quantification being 480 CFU/microL. By testing 5 chromogens, viz. 1,2-benzenediamine, 2,2'-azinobis(3-ethylbenzthiazoline-6-sulfonic acid), 3,3',5,5'-tetramethylbenzidine, bi(4,4'-anisidine) and 3-methyl-2-benzothiazolinone hydrazone, in horseradish peroxidase substrate, 1,2-benzenediamine or 3,3',5,5'-tetramethylbenzidine as H-donors in the enzyme substrate provided the highest ELISA sensitivity. The applied polyclonal antibody was specific for homogeneous antigen. The cross-reactions were observed only with one strain of C. sputorum subsp. sputorum (21.5 %) and with G+ bacterium Micrococcus luteus (6.1 %). Preliminary tests have been performed with a limited number of artificially contaminated food samples. No matrix effects on the ELISA sensitivity were observed. The results (by means of ELISA) were comparable with those given by both a standard cultivation method performed according to CSN ISO 10272 and commercially available Singlepath Campylobacter GLISA-Rapid Test.

  11. An Optical Test Strip for the Detection of Benzoic Acid in Food

    PubMed Central

    Hamzah, Hairul Hisham; Yusof, Nor Azah; Salleh, Abu Bakar; Bakar, Fatimah Abu

    2011-01-01

    Fabrication of a test strip for detection of benzoic acid was successfully implemented by immobilizing tyrosinase, phenol and 3-methyl-2-benzothiazolinone hydrazone (MBTH) onto filter paper using polystyrene as polymeric support. The sensing scheme was based on the decreasing intensity of the maroon colour of the test strip when introduced into benzoic acid solution. The test strip was characterized using optical fiber reflectance and has maximum reflectance at 375 nm. It has shown a highly reproducible measurement of benzoic acid with a calculated RSD of 0.47% (n = 10). The detection was optimized at pH 7. A linear response of the biosensor was obtained in 100 to 700 ppm of benzoic acid with a detection limit (LOD) of 73.6 ppm. At 1:1 ratio of benzoic acid to interfering substances, the main interfering substance is boric acid. The kinetic analyses show that, the inhibition of benzoic is competitive inhibitor and the inhibition constant (Ki) is 52.9 ppm. The activity of immobilized tyrosinase, phenol, and MBTH in the test strip was fairly sustained during 20 days when stored at 3 °C. The developed test strip was used for detection of benzoic acid in food samples and was observed to have comparable results to the HPLC method, hence the developed test strip can be used as an alternative to HPLC in detecting benzoic acid in food products. PMID:22164018

  12. Flow injection determination of hydrogen peroxide using catalytic effect of cobalt(II) ion on a dye formation reaction.

    PubMed

    Kurihara, Makoto; Muramatsu, Miyuki; Yamada, Mari; Kitamura, Naoya

    2012-07-15

    A novel flow injection photometric method was developed for the determination of hydrogen peroxide in rainwater. This method is based on a cobalt(II)-catalyzed oxidative coupling of 3-methyl-2-benzothiazolinone hydrazone (MBTH) with N-ethyl-N-(2-hydroxy-3-sulfopropyl)-3,5-dimethoxyaniline (DAOS) as a modified Trinder's reagent to produce intensely colored dye (λ(max)=530nm) in the presence of hydrogen peroxide at pH 8.4. In this method, 1,2-dihydroxy-3,5-benzenedisulfonic acid (Tiron) acted as an activator for the cobalt(II)-catalyzed reaction and effectively increased the peak height for hydrogen peroxide. The linear calibration graphs were obtained in the hydrogen peroxide concentration range 5×10(-8) to 2.2×10(-6)mol dm(-3) at a sampling rate of 20h(-1). The relative standard deviations for ten determinations of 2.2×10(-6) and 2×10(-7)mol dm(-3) hydrogen peroxide were 1.1% and 3.7%, respectively. The proposed method was successfully applied to the determination of hydrogen peroxide in rainwater samples and the analytical results agreed fairly well with the results obtained by different two reference methods; peroxidase method and hydrogen peroxide electrode method.

  13. Preparation of magnetite/poly(styrene-divinylbenzene) nanoparticles for selective enrichment-determination of fenitrothion in environmental and biological samples.

    PubMed

    Eskandari, Habibollah; Naderi-Darehshori, Ali

    2012-09-19

    In the present study, a cross-linked nano-sized spherical magnetic poly(styrene-divinylbenzene) is synthesized and used as an adsorbent for enrichment-determination of fenitrothion. A miniemulsion polymerization procedure was used to prepare the adsorbent. The magnetic adsorbent was characterized by FT-IR, SEM and TEM. The prepared magnetic adsorbent nanoparticles were mixed with magnetite nanoparticles for faster and more efficient magnetic precipitation. The reduced fenitrothion was coupled with 3-methyl-2-benzothiazolinone hydrazone and then the blue colored complex was extracted. The blue derivative of fenitrothion was eluted by a 1 mL aliquot of 1-propanol prior to spectrophotometry at 571 nm. Beer's law was obeyed in the range of 2-230 ng mL(-1) of fenitrothion with relative standard deviation and recovery in the ranges of 0.9-5.1% and 97.2-100.0%, respectively. Selectivity of the method was evaluated, and the method was successfully applied to the determination of fenitrothion in various water, soil, urine and human plasma samples.

  14. POLYSTYRENE SULFONIC ACID CATALYZED GREENER SYNTHESIS OF HYDRAZONES IN AQUEOUS MEDIUM USING MICROWAVES

    EPA Science Inventory

    An environmentally benign aqueous protocol for the synthesis of cyclic, bi-cyclic, and heterocyclic hydrazones using polystyrene sulfonic acid (PSSA) as a catalyst has been developed; the simple reaction proceeds efficiently in water in the absence of any organic solvent under mi...

  15. Oxidative Radical Addition-Cyclization of Sulfonyl Hydrazones with Simple Olefins by Binary Acid Catalysis.

    PubMed

    Zhong, Xingren; Lv, Jian; Luo, Sanzhong

    2016-07-01

    An unprecedented binary acid accelerated oxidative radical annulation of sulfonyl hydrazones with simple olefins is described. Notably, this method provides a novel oxidative radical cycloaddition for the construction of six-member heterocycles. It offers a rapid and efficient approach to tetrahydropyridazines which are key structural motifs in pharmaceutically active compounds.

  16. Asymmetric Synthesis of 2-Substituted Azetidin-3-ones via Metalated SAMP/RAMP Hydrazones.

    PubMed

    Pancholi, Alpa K; Geden, Joanna V; Clarkson, Guy J; Shipman, Michael

    2016-09-01

    2-Substituted azetidin-3-ones can be prepared in good yields and enantioselectivities (up to 85% ee) by a one-pot procedure involving the metalation of the SAMP/RAMP hydrazones of N-Boc-azetidin-3-one, reaction with a wide range of electrophiles, including alkyl, allyl, and benzyl halides and carbonyl compounds, followed by hydrolysis using oxalic acid. PMID:27447363

  17. Synthesis and larvicidal and adult topical activity of some hydrazide-hydrazone derivatives against Aedes aegypti

    Technology Transfer Automated Retrieval System (TEKTRAN)

    A series of novel hydrazide-hydrazone derivatives were synthesized and evaluated for their larvicidal and adult topical activity against Aedes aegypti. The proposed structures of all the synthesized compounds were confirmed using elemental analysis, UV, IR, 1H-NMR, 13C-NMR and mass spectroscopy. Com...

  18. Fe-Catalyzed Olefin Hydroamination with Diazo Compounds for Hydrazone Synthesis.

    PubMed

    Zheng, Jing; Qi, Jifeng; Cui, Sunliang

    2016-01-01

    A novel Fe-catalyzed olefin hydroamination with diazo compounds for accessing hydrazones has been developed. Diazo compounds are used as radical acceptors and can be trapped by the in situ generated alkyl radical toward C-N bond formation. The reaction conditions are mild, and the substrate scope is broad. Additionally, this hydroamination protocol is applicable for intramolecular reactions to construct diverse heterocycles.

  19. The potential of iron chelators of the pyridoxal isonicotinoyl hydrazone class as effective antiproliferative agents II: the mechanism of action of ligands derived from salicylaldehyde benzoyl hydrazone and 2-hydroxy-1-naphthylaldehyde benzoyl hydrazone.

    PubMed

    Richardson, D R; Milnes, K

    1997-04-15

    We have recently screened 36 analogues of the lipophilic iron (Fe) chelator, pyridoxal isonicotinoyl hydrazone (PIH), for their antiproliferative effect (Richardson et al, Blood 86:4295, 1995). Of these compounds, 1 chelator derived from salicylaldehyde benzoyl hydrazone (206) and 4 ligands derived from 2-hydroxy-1-naphthylaldehyde benzoyl hydrazone (308, 309, 311, and 315) showed pronounced antiproliferative activity, being far more effective than desferrioxamine (DFO). The present study was designed to investigate in detail the mechanism of action of these PIH analogues in a variety of neoplastic cell lines. This investigation showed that the analogues were far more active than DFO at inhibiting cellular proliferation and 3H-thymidine, 3H-leucine, and 3H-uridine incorporation. Additional experiments showed that, in contrast to DFO, the 5 analogues were potent at preventing 59Fe uptake from transferrin (Tf) and increasing 59Fe release from cells at concentrations as low as 10 micromol/L. Examination of the distribution of 59Fe in neoplastic cells using native polyacrylamide gel electrophoresis (PAGE)/59Fe-autoradiography showed that most of the 59Fe taken up from Tf was incorporated into ferritin, although 3 other previously unrecognized components (bands A, B, and C) were also identified. Band C comigrated with 59Fe-citrate and was chelated on incubation of neuroblastoma cells with DFO, PIH, or the PIH analogues, with this compartment being the main intracellular target of these ligands. Further work showed that the effects of the chelators at inducing characteristics consistent with apoptosis or necrosis were cell line-specific, and while DFO increased the percentage of cells in the G0/G1 phases in all cell types, the effect of analogue 311 on the cell cycle was variable depending on the cell line. This study provides further evidence for the potential use of these Fe chelators as anticancer agents.

  20. Tetradentate metal complexes derived from cephalexin and 2,6-diacetylpyridine bis(hydrazone): Synthesis, characterization and antibacterial activity

    NASA Astrophysics Data System (ADS)

    Anacona, J. R.; Rangel, Victor; Loroño, Marcos; Camus, Juan

    2015-10-01

    Metal(II) coordination compounds of a hydrazone ligand (HL) derived from the condensation of cephalexin antibiotic with 2,6-diacetylpyridine bis(hydrazone) were synthesized. The hydrazone ligand and mononuclear [ML(H2O)2][PF6] (M(II) = Mn, Co, Ni, Zn) complexes were characterized by several techniques, including elemental and thermal analysis, molar conductance and magnetic susceptibility measurements, electronic, FT-IR, EPR and 1H NMR spectral studies. The cephalexin 2,6-diacetylpyridine bis(hydrazone) ligand HL behaves as a monoanionic tetradentate NNNO chelating agent. The biological applications of complexes have been studied on two bacteria strains (Escherichia coli and Staphylococcus aureus) by agar diffusion disc method.

  1. Tetradentate metal complexes derived from cephalexin and 2,6-diacetylpyridine bis(hydrazone): Synthesis, characterization and antibacterial activity.

    PubMed

    Anacona, J R; Rangel, Victor; Loroño, Marcos; Camus, Juan

    2015-01-01

    Metal(II) coordination compounds of a hydrazone ligand (HL) derived from the condensation of cephalexin antibiotic with 2,6-diacetylpyridine bis(hydrazone) were synthesized. The hydrazone ligand and mononuclear [ML(H2O)2][PF6] (M(II)=Mn, Co, Ni, Zn) complexes were characterized by several techniques, including elemental and thermal analysis, molar conductance and magnetic susceptibility measurements, electronic, FT-IR, EPR and (1)H NMR spectral studies. The cephalexin 2,6-diacetylpyridine bis(hydrazone) ligand HL behaves as a monoanionic tetradentate NNNO chelating agent. The biological applications of complexes have been studied on two bacteria strains (Escherichia coli and Staphylococcus aureus) by agar diffusion disc method. PMID:25942081

  2. Density functional theory studies on the nano-scaled composites consisted of graphene and acyl hydrazone molecules

    NASA Astrophysics Data System (ADS)

    Ren, J. L.; Zhou, L.; Lv, Z. C.; Ding, C. H.; Wu, Y. H.; Bai, H. C.

    2016-07-01

    Graphene, which is the first obtained single atomic layer 2D materials, has drawn a great of concern in nano biotechnology due to the unique property. On one hand, acyl hydrazone compounds belonging to the Schif bases have aroused considerable attention in medicine, pharmacy, and analytical reagent. However, few understanding about the interaction between graphene and acyl hydrazone molecules is now available. And such investigations are much crucial for the applications of these new nano-scaled composites. The current work revealed theoretical investigations on the nano-scaled composites built by acyl hydrazone molecules loaded on the surface of graphene. The relative energy, electronic property and the interaction between the counterparts of graphene/acyl hydrazone composites are investigated based on the density functional theory calculations. According to the obtained adsorption energy, the formation of the nano-scaled composite from the isolated graphene and acyl hydrazone molecule is exothermic, and thus it is energetically favorable to form these nano composites in viewpoint of total energy change. The frontier molecular orbital for the nano composite is mainly distributed at the graphene part, leading to that the energy levels of the frontier molecular orbital of the nano composites are very close to that of isolated graphene. Moreover, the counterpart interaction for the graphene/acyl hydrazone composites is also explored based on the discussions of orbital hybridization, charge redistribution and Van der Waals interaction.

  3. Topical chlormethine hydrochloride causing bullous reaction.

    PubMed

    Ngai, Ka Yan; Chan, Ho Yin; Ng, Fu

    2009-09-01

    We describe a woman misusing chlormethine hydrochloride lotion for vitiligo with dermatological complications of local urticarial and bullous reactions. Presentations, complications, and management of topical chlormethine hydrochloride overdose are discussed. Surface decontamination and follow-up for potential complications are major treatments.

  4. Novel hydrazone derivatives containing pyridine amide moiety: Design, synthesis, and insecticidal activity.

    PubMed

    Yang, Zai-Bo; Hu, De-Yu; Zeng, Song; Song, Bao-An

    2016-02-15

    A series of novel hydrazone derivatives containing pyridine amide moiety were designed, synthesized, and evaluated for their insecticidal activity. Bioassays indicated that some of the target compounds exhibited good insecticidal activities against Nilaparvata lugens (N. lugens), Plutella xylostella (P. xylostella), Mythimna separata (M. separata), Helicoverpa armigera (H. armigera), Pyrausta nubilalis (P. nubilalis), and Culex pipiens pallens (C. pipiens pallens). In particular, compound 5j revealed excellent insecticidal activity against C. pipiens pallens, with the 50% lethal concentration (LC50) and the 95% lethal concentration (LC95) values of 2.44 and 5.76 mg/L, respectively, which were similar to those of chlorpyrifos (3.26 and 6.98 mg/L, respectively), tebufenozide (1.22 and 2.49 mg/L, respectively), and RH-5849 (2.61 and 6.37 mg/L, respectively). These results indicated that hydrazone derivatives containing pyridine amide moiety could be developed as novel and promising insecticides.

  5. Hydrazone Self-Crosslinking of Multiphase Elastin-Like Block Copolymer Networks

    PubMed Central

    Krishna, Urlam Murali; Martinez, Adam W.; Caves, Jeffrey M.; Chaikof, Elliot L.

    2011-01-01

    Biosynthetic strategies for the production of recombinant elastin-like protein (ELP) triblock copolymers have resulted in elastomeric protein hydrogels, formed through rapid physical crosslinking upon warming of concentrated solutions. However, the strength of physically crosslinked networks can be limited, and options for non-toxic chemical crosslinking of these networks are not optimal. In this report, we modify two recombinant elastin-like proteins with aldehyde and hydrazide functionalities. When combined, these modified recombinant proteins self-crosslink through hydrazone bonding without requiring initiators or producing by-products. Crosslinked materials are evaluated for water content and swelling upon hydration, and subject to tensile and compressive mechanical tests. Hydrazone crosslinking is a viable method for increasing the mechanical strength of elastin-like protein polymers, in a manner that is likely to lend itself to the biocompatible in situ formation of chemically and physically crosslinked ELP hydrogels. PMID:22154858

  6. Spectroscopic and theoretical study of the o-vanillin hydrazone of the mycobactericidal drug isoniazid

    NASA Astrophysics Data System (ADS)

    González-Baró, Ana C.; Pis-Diez, Reinaldo; Parajón-Costa, Beatriz S.; Rey, Nicolás A.

    2012-01-01

    A complete and detailed study of the hydrazone obtained from condensation of antituberculous isoniazid (hydrazide of the isonicotinic acid, INH) and o-vanillin (2-hydroxy-3-methoxybenzaldehyde, o-HVa) is performed. It includes structural and spectroscopic analyses, comparing experimental and theoretical results. The compound was obtained as a chloride of the pyridinic salt (INHOVA +Cl -) but it will be referred as INHOVA for the sake of simplicity. The conformational space was searched and optimized geometries were determined both in gas phase and including solvent effects. Vibrational (IR and Raman), electronic and NMR spectra were registered and assigned with the help of computational methods based on the Density Functional Theory. Isoniazid hydrazones are good candidates for therapeutic agents against tuberculosis with conserved efficiency and lower toxicity and resistance than parent INH.

  7. Development of Chiral Bis-hydrazone Ligands for the Enantioselective Cross-Coupling Reactions of Aryldimethylsilanolates

    PubMed Central

    2015-01-01

    A palladium-catalyzed, enantioselective, aryl–aryl cross-coupling reaction using 1-naphthyldimethylsilanolates and chiral bis-hydrazone ligands has been developed. A family of glyoxal bis-hydrazone ligands containing various 2,5-diarylpyrrolidine groups was prepared to evaluate the influence of ligand structure on the rate and enantioselectivity of the cross-coupling. New synthetic routes to the 1-amino-2,5-diarylpyrrolidines were developed to enable the structure/reactivity–selectivity studies. Role reversal experiments of aryldimethylsilanolates and aryl bromides result in biaryl products with the same configuration and similar enantioselectivities implying that reductive elimination is the stereodetermining step. The origin of stereoselectivity is rationalized through computational modeling of diarylpalldium(II) complex which occurs through a conrotatory motion for the two aryl groups undergoing C–C bond formation. PMID:25494058

  8. Anion induced azo-hydrazone tautomerism for the selective colorimetric sensing of fluoride ion

    NASA Astrophysics Data System (ADS)

    Satheshkumar, A.; El-Mossalamy, E. H.; Manivannan, R.; Parthiban, C.; Al-Harbi, L. M.; Kosa, S.; Elango, Kuppanagounder P.

    2014-07-01

    The design, synthesis, characterization and their anion sensing properties of two receptors capable of exhibiting azo-hydrazone tautomerism are reported. The anion sensing properties have been investigated using electronic, fluorescence and nuclear magnetic spectral studies in addition to electrochemical and visual detection experiments. Both the receptors selectively bind fluoride ion with >100 nm red-shift in the electronic spectrum and the color changes from yellow to red. The results of the spectral studies revealed that the sensing mechanism involves fluoride ion induced change of chromophore from Cdbnd N (hydrazone form) to Ndbnd N (azo form) in these receptors leading to the visible color change. Density Functional Theory calculations were conducted to rationalize the optical response of the receptors.

  9. Synthesis and evaluation of antioxidant activity of new quinoline-2-carbaldehyde hydrazone derivatives: bioisosteric melatonin analogues.

    PubMed

    Puskullu, M Orhan; Shirinzadeh, Hanif; Nenni, Merve; Gurer-Orhan, Hande; Suzen, Sibel

    2016-01-01

    Overproduction of reactive oxygen species results in oxidative stress that can cause fatal damage to vital cell structures. It is known that the use of antioxidants could be beneficial in the prevention or delay of numerous diseases associated with oxidative stress. Melatonin (MLT) is known as a powerful free-radical scavenger and antioxidant. It was found that indole ring of MLT can be employed by bioisosteric replacement by other aromatic rings. Quinoline derivatives constitute an important class of compounds for new drug development. Owing to quinoline and hydrazones appealing physiological properties and are mostly found in numerous biologically active compounds a series of quinoline-2-carbaldehyde hydrazone derivatives were synthesized as bioisosteric analogues of MLT, characterized and in vitro antioxidant activity was investigated by evaluating their reducing effect against oxidation of a redox-sensitive fluorescent probe. Cytotoxicity potential of all compounds was investigated both by lactate dehydrogenase leakage assay and by MTT assay.

  10. Highly diastereoselective palladium-catalyzed indium-mediated allylation of chiral hydrazones.

    PubMed

    Balasubramanian, Narayanaganesh; Mandal, Tanmay; Cook, Gregory R

    2015-01-16

    The general and efficient palladium-catalyzed indium-mediated allylation of chiral hydrazones was accomplished with excellent yield (72-92%) and diastereoselectivity (up to 99:1). The development of this reaction and the substrate scope are described. The conversion was found to be proportional to the phosphine concentration, which provided insight into the mechanism and competing pathways of the redox transmetalation process.

  11. In vitro nematicidal activity of aryl hydrazones and comparative GC-MS metabolomics analysis.

    PubMed

    Eloh, Kodjo; Demurtas, Monica; Deplano, Alessandro; Ngoutane Mfopa, Alvine; Murgia, Antonio; Maxia, Andrea; Onnis, Valentina; Caboni, Pierluigi

    2015-11-18

    A series of aryl hydrazones were synthesized and in vitro assayed for their activity on the root-knot nematode Meloidogyne incognita. The phenylhydrazones of thiophene-2-carboxyaldehyde 5, 3-methyl-2-thiophenecarboxyaldehyde, 6, and salicylaldehyde, 2, were the most potent with EC50/48h values of 16.6 ± 2.2, 23.2 ± 2.7, and 24.3 ± 1.4 mg/L, respectively. A GC-MS metabolomics analysis, after in vitro nematode treatment with hydrazone 6 at 100 mg/L for 12 h, revealed elevated levels of fatty acids such as lauric acid, stearic acid, 2-octenoic acid, and palmitic acid. Whereas control samples showed the highest levels of monoacylglycerols such as monostearin and 2-monostearin, surprisingly, 2 h after treatment with hydrazone 6, nematodes excreted 3 times the levels of ammonia eliminated in the same conditions by controls. Thus, phenylhydrazones may represent a good scaffold in the discovery and synthesis of new nematicidal compounds, and a metabolomics approach may be helpful in understanding their mechanisms of toxicity and mode of action. PMID:26528945

  12. Bach Adsorption Study for the Extraction of Silver Ions by Hydrazone Compounds from Aqueous Solution

    PubMed Central

    Mohamad Ali, Abdussalam Salhin; Abdul Razak, Norfarhah; Ab Rahman, Ismail

    2012-01-01

    Sorbent materials based on a hydrazone Schiff base compound, C14H11BrN4O4, were prepared either by immobilizing the ligand into sol-gel (SG1) or bonding to silica (SG2). The sorbent materials were characterized by FT-IR, EDX, SEM, TEM, and TGA. The sorption characteristics of a matrix of eight transition metal ions (Ag+, Cu2+, Co2+, Ni2+, Fe3+, Pb2+, Zn2+, and Mn2+) using batch method were studied. Several key parameters that affected the extraction efficiency such as pH, contact time, metal ions concentration, and gel size (for SGl) were investigated and optimized. Under the optimized conditions, the physically immobilized hydrazone sorbent (SG1) exhibits highest selectivity towards Ag+ ions, while the chemically bonded hydrazone sorbent (SG2) exhibits high extraction for all metal ions tested. However, for practical applications such as the removal and preconcentration of Ag+, the physically immobilized sorbent (SG1) is preferred. PMID:22629138

  13. Effect of dexmedetomidine hydrochloride on tiletamine hydrochloride-zolazepam hydrochloride anesthesia in alpacas.

    PubMed

    Seddighi, Reza; Odoi, Agricola; Doherty, Thomas J

    2016-10-01

    OBJECTIVE To evaluate the effect of IM administration of a tiletamine hydrochloride-zolazepam hydrochloride (TZ) combination with either dexmedetomidine hydrochloride or saline (0.9% NaCl) solution (SS) on the motor response to claw clamping, selected cardiorespiratory variables, and quality of recovery from anesthesia in alpacas. ANIMALS 5 adult sexually intact male alpacas. PROCEDURES Each alpaca was given the TZ combination (2 mg/kg) with dexmedetomidine (5 [D5], 10 [D10], 15 [D15], or 20 [D20] µg/kg) or SS IM at 1-week intervals (5 experiments); motor response to claw clamping was assessed, and characteristics of anesthesia, recovery from anesthesia, and selected cardiorespiratory variables were recorded. RESULTS Mean ± SEM duration of lack of motor response to claw clamping was longest when alpacas received treatments D15 (30.9 ± 5.9 minutes) and D20 (40.8 ± 5.9 minutes). Duration of lateral recumbency was significantly longer with dexmedetomidine administration. The longest time (81.3 ± 10.4 minutes) to standing was observed when alpacas received treatment D20. Following treatment SS, 4 alpacas moved in response to claw clamping at the 5-minute time point. Heart rate decreased from pretreatment values in all alpacas when dexmedetomidine was administered. Treatments D10, D15, and D20 decreased Pao2, compared with treatment SS, during the first 15 minutes. During recovery, muscle stiffness and multiple efforts to regain a sternal position were observed in 3 SS-treated and 1 D5-treated alpacas; all other recoveries were graded as excellent. CONCLUSIONS AND CLINICAL RELEVANCE In TZ-anesthetized alpacas, dexmedetomidine (10, 15, and 20 µg/kg) administered IM increased the duration of lack of motor response to claw clamping, compared with the effect of SS. PMID:27668576

  14. Yohimbine hydrochloride as an antagonist to xylazine hydrochloride-ketamine hydrochloride immobilization of white-tailed deer

    USGS Publications Warehouse

    Mech, L.D.; DelGiudice, G.D.; Karns, P.D.; Seal, U.S.

    1985-01-01

    Thirteen captive and one free-ranging white-tailed deer (Odocoileus virginianus) were immobilized one to six times each with ketamine hydrochloride and xylazine hydrochloride during winter and spring in northern Minnesota. Administration of 0.09 to 0.53 mg of yohimbine hydrochloride per kg IV after each trial reversed the immobilization. The deer raised their heads within a median time of 2.0 min, stood in 6.0 min and walked away in 9.5 min. No adverse side effects were observed for several weeks following the immobilization.

  15. 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

  16. Structural studies and investigation on the activity of imidazole-derived thiosemicarbazones and hydrazones against crop-related fungi.

    PubMed

    Reis, Débora C; Despaigne, Angel A Recio; Da Silva, Jeferson G; Silva, Nayane F; Vilela, Camila F; Mendes, Isolda C; Takahashi, Jacqueline A; Beraldo, Heloisa

    2013-10-14

    New imidazole derived thiosemicarbazones and hydrazones were prepared by condensation of 4(5)-imidazole carboxaldehyde, 4-(1H-imidazole-1-yl)benzaldehyde and 4-(1H-imidazole-1-yl)acetophenone with a thiosemicarbazide or hydrazide. All compounds were characterized by quantitative elemental analysis, IR and NMR techniques. Eight structures were determined by single crystal X-ray diffraction. The antifungal activities of the compounds were evaluated. None of the compounds exhibited significant activity against Aspergillus flavus and Candida albicans, while 4(5)-imidazolecarboxaldehyde thiosemicarbazone (ImT) and 4-(1H-imidazole-1-yl)benzaldehyde thiosemicabazone (4ImBzT) were highly and selectively active against Cladosporium cladosporioides. 4(5)-Imidazolecarboxaldehyde benzoyl hydrazone (4(5)ImPh), 4(5)-imidazolecarboxaldehyde-para-chlorobenzoyl hydrazone (4(5)ImpClPh), 4(5)-imidazolecarboxaldehyde-para-nitrobenzoyl hydrazone (4(5)ImpNO2Ph), 4-(imidazole-1-yl)acetophenone-para-chloro-benzoyl hydrazone (4ImAcpClPh) and 4-(imidazole-1-yl)acetophenone-para-nitro-benzoylhydrazone (4ImAcpNO2Ph) were highly active against Candida glabrata. 4(5)ImpClPh and 4(5)ImpNO2Ph were very effective against C. cladosporioides. In many cases, activity was superior to that of the reference compound nystatin.

  17. 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.

  18. Monoarthritis Induced by Bupropion Hydrochloride

    PubMed Central

    Yuan, Weiqing; Williams, Barry N.

    2011-01-01

    Objective Bupropion hydrochloride is an inhibitor of dopamine and norepinephrine, which is commonly prescribed for major depression, smoking cessation, and bipolar depression. Here we report a highly unusual case of bupropion induced knee monoarthritis in a bipolar depression patient. With bupropion XL 150 mg for 2 weeks, her left knee began to swell; at the third week, this condition was worsening. The aggravation of the left knee effusion stopped after the discontinuation of bupropion XL. The effusion and swelling disappeared after 15 ml of synovial fluid was drawn out and the effusion has never returned. Analysis of the synovial fluid showed noninflammatory effusion. Her left knee swelling was most likely due to angioedema caused by bupropion XL.

  19. 21 CFR 520.1962 - Promazine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    .... (a)(1) Chemical name. 10- phenothiazine monohydrochloride. (2) Specifications. Conforms to N.F. XII... of 0.45 to 0.9 milligrams of promazine hydrochloride per pound of body weight mixed with an amount...

  20. Potent antimycobacterial activity of the pyridoxal isonicotinoyl hydrazone analog 2-pyridylcarboxaldehyde isonicotinoyl hydrazone: a lipophilic transport vehicle for isonicotinic acid hydrazide.

    PubMed

    Ellis, Samantha; Kalinowski, Danuta S; Leotta, Lisa; Huang, Michael L H; Jelfs, Peter; Sintchenko, Vitali; Richardson, Des R; Triccas, James A

    2014-02-01

    The rise in drug-resistant strains of Mycobacterium tuberculosis is a major threat to human health and highlights the need for new therapeutic strategies. In this study, we have assessed whether high-affinity iron chelators of the pyridoxal isonicotinoyl hydrazone (PIH) class can restrict the growth of clinically significant mycobacteria. Screening a library of PIH derivatives revealed that one compound, namely, 2-pyridylcarboxaldehyde isonicotinoyl hydrazone (PCIH), exhibited nanomolar in vitro activity against Mycobacterium bovis bacille Calmette-Guérin and virulent M. tuberculosis. Interestingly, PCIH is derived from the condensation of 2-pyridylcarboxaldehyde with the first-line antituberculosis drug isoniazid [i.e., isonicotinic acid hydrazide (INH)]. PCIH displayed minimal host cell toxicity and was effective at inhibiting growth of M. tuberculosis within cultured macrophages and also in vivo in mice. Further, PCIH restricted mycobacterial growth at high bacterial loads in culture, a property not observed with INH, which shares the isonicotinoyl hydrazide moiety with PCIH. When tested against Mycobacterium avium, PCIH was more effective than INH at inhibiting bacterial growth in broth culture and in macrophages, and also reduced bacterial loads in vivo. Complexation of PCIH with iron decreased its effectiveness, suggesting that iron chelation may play some role in its antimycobacterial efficacy. However, this could not totally account for its potent efficacy, and structure-activity relationship studies suggest that PCIH acts as a lipophilic vehicle for the transport of its intact INH moiety into the mammalian cell and the mycobacterium. These results demonstrate that iron-chelating agents such as PCIH may be of benefit in the treatment and control of mycobacterial infection. PMID:24243647

  1. Synthesis, Spectroscopic Properties and Antioxidant Activity of Bis-Hydrazones and Schiff's bases Derived from Terephthalic Dihydrazide.

    PubMed

    Jois, H S Vidyashree; Kalluraya, Balakrishna; Vishwanath, T

    2015-05-01

    A series of novel Schiff base containing bis-1,2,4-triazole and bis-hydrazone derived from terephthalic dihydrazide was synthesized. All the newly synthesized compounds were characterized by (1)H, (13)C NMR, mass spectra, FTIR and elemental analysis. UV-vis spectra and fluorescent spectra of the compounds were recorded. The effect of substituent such as electron withdrawing and electron donating groups on the fluorescent spectra was studied. Also, the comparative discussion on fluorescent spectra of Schiff's base and hydrazones has been described. The antioxidant activity of the compounds revealed that compound 5c and 5f are the most potent compounds in this series.

  2. Copper-catalyzed aerobic oxidative transformation of ketone-derived N-tosyl hydrazones: an entry to alkynes.

    PubMed

    Li, Xianwei; Liu, Xiaohang; Chen, Huoji; Wu, Wanqing; Qi, Chaorong; Jiang, Huanfeng

    2014-12-22

    A novel strategy involving Cu-catalyzed oxidative transformation of ketone-derived hydrazone moiety to various synthetic valuable internal alkynes and diynes has been developed. This method features inexpensive metal catalyst, green oxidant, good functional group tolerance, high regioselectivity and readily available starting materials. Oxidative deprotonation reactions were carried out to form internal alkynes and symmetrical diynes. Cross-coupling reactions of hydrazones with halides and terminal alkynes were performed to afford functionalized alkynes and unsymmetrical conjugated diynes. A mechanism proceeding through a Cu-carbene intermediate is proposed for the CC triple bond formation. PMID:25424976

  3. Low molecular weight PEIs modified by hydrazone-based crosslinker and betaine as improved gene carriers.

    PubMed

    Fang, Gang; Zeng, Fang; Yu, Changmin; Wu, Shuizhu

    2014-10-01

    Low-molecular-weight polyethyleneimine (LMW PEI) exhibits poorer transfection efficiency but lower cytotoxicity compared to high-molecular-weight polyethyleneimine (such as PEI 25kDa). To enhance the gene transfection performance of LMW PEI, we herein demonstrate a new strategy for modifying LMW PEI. A crosslinker containing an acid-labile hydrazone bond (hydrazone-based crosslinker) was synthesized and used to crosslink PEI 1.8kDa and convert it into higher-molecular-weight polycations. And the crosslinked polycations were further modified by incorporating a betaine monomer [N,N-dimethyl(acrylamidopropyl)ammonium propane sulfonate, DMAAPS] onto their surfaces. The molar percentages of the incorporated betaine molecules to amino groups on the polycations were determined as 21.2%, 36.0% and 77.2%, respectively. Molecular weights of the modified polycations were measured using capillary viscometry at pH 7.4 and 5.0, respectively, and the degradation of the polymers in acidic solution was confirmed. The PEIs modified with hydrazone and betaine (PEI-Hdz-DMAAPS) exhibit much lower cytotoxicity than PEI 25K, and they also show no or little hemolytic effect with their hemolysis rates around 5%. PEI-Hdz-DMAAPS21.2%/DNA and PEI-Hdz-DMAAPS36.0%/DNA complexes exhibit high transfection efficiencies, which are comparable to or higher than that of PEI 25K/DNA complex in the absence or presence of 10% serum. With these improved gene delivery properties, the PEI-Hdz-DMAAPS samples have great potential for serving as efficient gene carriers. This strategy may provide some insights for constructing some other biocompatible materials.

  4. Metallo-hydrazone complexes immobilized in zeolite Y: Synthesis, identification and acid violet-1 degradation

    NASA Astrophysics Data System (ADS)

    Ahmed, Ayman H.; Thabet, M. S.

    2011-12-01

    Copper(II), cobalt(II) and nickel(II) complexes of hydrazone ligand (SAPH) derived from salicylaldehyde and phenylhydrazine have been encapsulated in zeolite-Y super cages via ship-in-a-bottle synthesis. Detailed characterization of the intrazeolitic complexes were performed by elemental analysis, spectral (FT-IR, UV-Vis.) studies, magnetic measurements and X-ray diffraction. Furthers, surface texture and thermal analysis (TG, DTG, DTA) have provided further evidence for successful immobilization of the metal complexes inside zeolite Y. Investigation of the stereochemistry of these incorporated chelates pointed out that, SAPH ligand is capable to coordinate with the central metal through the (C dbnd N), phenolic (OH) and (NH) groups forming polynuclear structures. The involvement of zeolite oxygen in coordination was postulated in the hybrid materials. The intrazeolitic copper, cobalt and nickel-SAPH complexes have distorted tetrahedral, octahedral and square-pyramidal configurations, respectively. The zeolite encapsulated complexes are thermally stable up to 800 °C except Cu(II) sample which is thermally stable up to midpoint 428 °C. The assessment of the catalytic activity was performed by the use of the photo-degradation of acid violet-1 dye as a probe reaction in presence of H 2O 2 as an oxidant. Decolorization of acid violet-1 dye was examined under the same conditions whereas the unpromoted zeolite and Cu II, Co II, Ni II-hydrazone complexes supported on zeolite showed 13% and 76%, 53%, 43% color removal, respectively. The results revealed that, the zeolite encapsulated Cu(II) complex generally exhibited better catalytic efficiency (76%) compared with other investigated zeolite encapsulated metal-hydrazone samples.

  5. Stereochemistry of new nitrogen containing heterocyclic compound. XII. Polymeric uranyl complexes of hydrazone compounds

    NASA Astrophysics Data System (ADS)

    Al-Sarawy, A. A.; El-Bindary, A. A.; El-Sonbati, D. N.

    2005-06-01

    Several dioxouranium(VI) heterochelates with tetradentate monobasic hydrazone compounds (HL n) have been synthesized. The heterochelates of the type [(UO 2) 2(HL n)(L n) 2(OAc) 2(OH 2) 2] n have been characterized on the basis of elemental analyses, IR and electronic spectra, conductance and magnetic susceptibility measurements. The complexes are polymeric, non-electrolytes, diamagnetic and eight-coordinated. Wilson, G.F. matrix method, Badger's formula, Jones and El-Sonbati equations were used to determine the stretching and interaction force constants from which the U sbnd O bond distances were calculated. The bond distances of these complexes were also investigated.

  6. Flow-injection chemiluminescence method for the determination of naphazoline hydrochloride and oxymetazoline hydrochloride.

    PubMed

    Wang, Nan-Nan; Shao, Yan-Qing; Tang, Yu-Hai; Yin, He-Ping; Wu, Xiao-Zhong

    2009-01-01

    A sensitive and simple flow-injection chemiluminescence (FI-CL) method, which was based on the CL intensity generated from the redoxreaction of potassium permanganate (KMnO4)-formaldehyde in vitriol (H2SO4) medium, has been developed, validated and applied for the determination of naphazoline hydrochloride and oxymetazoline hydrochloride. Besides oxidants and sensitizers, the effect of the concentration of H(2)SO(4), KMnO4 and formaldehyde was investigated. Under the optimum conditions, the linear range was 1.0 x 10(-2)-7.0 mg/L for naphazoline hydrochloride and 5.0 x 10(-2)-10.0 mg/L for oxymetazoline hydrochloride. During seven repeated inter-day and intra-day precision tests of 0.1, 1.0 and 10.0 mg/L samples, the relative standard deviations all corresponded to reference values. The detection limit was 8.69 x 10(-3) mg/L for naphazoline hydrochloride and 3.47 x 10(-2) mg/L for oxymetazoline hydrochloride (signal-to-noise ratio < or = 3). This method has been successfully implemented for the determination of naphazoline hydrochloride and oxymetazoline hydrochloride in pharmaceuticals.

  7. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... hydrochloride per pound of body weight for profound tranquilization. It is administered intravenously at a dosage level of 1 to 2 milligrams of ethylisobutrazine hydrochloride per pound of body weight to...

  8. New palladium(II) hydrazone complexes: Synthesis, structure and biological evaluation.

    PubMed

    Ayyannan, Ganesan; Mohanraj, Maruthachalam; Raja, Gunasekaran; Bhuvanesh, Nanjan; Nandhakumar, Raju; Jayabalakrishnan, Chinnasamy

    2016-10-01

    Two new palladium(II) complexes of 4-hydoxy-benzoic acid (5-bromo-2-hydroxy-benzylidene)-hydrazide (H2L) (1) with triphenylphosphine and triphenylarsine as coligand have been synthesized and characterized by the aid of various spectral techniques. The structure of the ligand and complexes was confirmed by single crystal X-ray diffraction studies. The hydrazone ligand acts as a tridendate ligand with ONO as the donor sites and is preferably found in the enol form in all the complexes. The structural analysis of 2 and 3 confirms the square planar geometry of the two complexes. The DNA binding of these complexes and ligand calf thymus DNA (CT-DNA) was investigated by using various methods, which revealed that the compounds interacted with CT-DNA through intercalation. Binding properties of the free ligand and its complexes with bovine serum albumin (BSA) protein have been investigated using UV-visible and fluorescence spectroscopic methods which indicated the stronger binding nature of the palladium complexes to BSA than the free hydrazone ligand. In addition, concentration dependent free radical scavenging potential of all the synthesized compounds (1-3) was also carried out under in vitro conditions. Further, the in vitro cytotoxicity of the compounds was examined on a HeLa and MCF-7 cell lines, which revealed that complex 2 exhibited a superior cytotoxicity than complex 3 and ligand 1. PMID:27517347

  9. Synthesis, Antiplatelet Activity and Cytotoxicity Assessment of Indole-Based Hydrazone Derivatives

    PubMed Central

    Haj Mohammad Ebrahim Tehrani, Kamaleddin; Esfahani Zadeh, Marjan; Mashayekhi, Vida; Hashemi, Maryam; Kobarfard, Farzad; Gharebaghi, Farhad; Mohebbi, Shohreh

    2015-01-01

    A series of indole-based aryl(aroyl)hydrazone analogs of antiplatelet indole-3-carboxaldehyde phenylhydrazone were synthesized by the Schiff base formation reaction and their antiplatelet activity was assessed using human platelet rich plasma. The platelet concentrate was obtained using a two-step centrifugation protocol and ADP, arachidonic acid and collagen were used as inducers of platelet aggregation. Based on the results, substituted phenylhydrazones showed promising activity. Among them, compound 1i was the most potent derivative with an IC50 comparable to that of indomethacin as a standard drug. The hydrazone derivatives were also tested for their cytotoxicity using on platelet concentrates and fibroblast L929 cells. The majority of the derivatives showed an acceptable selectivity towards antiplatelet aggregation activity. Based on the activity data, phenylhydrazone derivatives (1a-i) exhibited considerable antiplatelet activity and minimal toxic effect on platelet cells. The results of the present study could provide a better understanding of the structure activity relationship of antiplatelet indolehydrazones. PMID:26664374

  10. In vitro antioxidant properties of the iron chelator pyridoxal isonicotinoyl hydrazone and some of its analogs.

    PubMed

    Schulman, H M; Hermes-Lima, M; Wang, E M; Ponka, P

    1995-11-01

    Since there are several problems with desferrioxamine (DFO) therapy, pyridoxal isonicotinoyl hydrazone (PIH) has been studied for more than 10 years as a promising new candidate for iron chelation therapy in iron-overload diseases. Iron chelation could also be helpful for experimental treatment of several other pathologies including rheumatoid arthritis and heart ischemia/reperfusion, due to the generation of oxyradicals and lipid peroxidation mediated by delocalized iron. We demonstrate here that sub-millimolar levels of PIH can inhibit the Fe(III)-EDTA/ascorbate-mediated formation of hydroxyl-like radicals as tested by the release of ethylene from 2-keto-4-methylthiobutyric acid (KMB assay) and the formation of malonaldehyde from 2-deoxyribose damage. PIH could also decrease the rates of Fe(III)-EDTA-mediated oxidation of ascorbate and block the peroxidation of liposomes of rat brain phospholipids induced by ferrous iron-EDTA. In all cases the in vitro antioxidant effectiveness of PIH was comparable to its analogs-including salicylaldehyde isonicotinoyl hydrazone-and to DFO. We conclude that PIH and its analogs are effective new candidates against iron-mediated oxidative stress for use in experimental medicine. PMID:27405837

  11. Novel colorimetric sensors for cyanide based on azo-hydrazone tautomeric skeletons.

    PubMed

    Adegoke, Olajire A; Adesuji, Temitope E; Thomas, Olusegun E

    2014-07-15

    The monoazo dyes, 4-carboxyl-2, 6-dinitrophenylazohydroxynaphthalenes dyes (AZ-01, AZ-03 and AZ-04), were evaluated as a highly selective colorimetric chemosensor for cyanide ion. The recognition of cyanide ion gave an obvious colour change from light yellow to brownish red and upon dilution with acetone produced a purple to lilac colour. Optimum conditions for the reaction between the azo dyes and cyanide ion were established at 30°C for 5 min, and different variables affecting the reaction were carefully studied and optimised. Under the optimum conditions, linear relationships between the CN(-) concentrations and light absorption were established. Using these azo-hydrazone molecular switch entities, excellent selectivity towards the detection of CN(-) in aqueous solution over miscellaneous competitive anions was observed. Such selectivity mainly results from the possibility of nucleophilic attack on the azo-hydrazone chemosensors by cyanide anions in aqueous system, which is not afforded by other competing anions. The cyanide chemosensor method described here should have potential application as a new family probes for detecting cyanide in aqueous solution.

  12. Synthesis and structural characterization of zinc(II) and cobalt(II) complexes based on multidentate hydrazone ligands

    NASA Astrophysics Data System (ADS)

    Li, Li; Zhang, Yuan Zhuo; Liu, E.; Yang, Chengxiong; Golen, James A.; Rheingold, Arnold L.; Zhang, Guoqi

    2016-04-01

    Two multidentate Schiff base ligands containing a hydrazone unit have been synthesized and investigated for zinc(II) and cobalt(II) coordination chemistry. The reactions of the 4-pyridyl derived hydrazone ligand HL1 with zinc(II) or cobalt(II) salts gave three mononuclear complexes that were structurally characterized by X-ray diffraction analysis. The results revealed that the ligand could adopt different coordination modes when various counter anions were employed. While in the case that zinc dichloride was used as a metal salt a neutral mononuclear mono-ligand complex was formed, the deprotonation of hydrazone occurred when zinc(II) or cobalt(II) nitrate were present and two new isostructural mononuclear bis-ligand complexes were isolated. Modification of the hydrazone ligand with oxygen donors was found to have a significant impact on the ligand reactivity, and a similar reaction of H2L2 with cobalt(II) nitrate gave a protonated product of H2L2 without the incorporation of cobalt(II), which features a one-dimensional hydrogen-bonded network in the solid state.

  13. Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1.

    PubMed

    Sindelar, Miriam; Lutz, Toni A; Petrera, Marilena; Wanner, Klaus T

    2013-02-14

    Mass spectrometric (MS) binding assays, a powerful tool to determine affinities of single drug candidates toward chosen targets, were recently demonstrated to be suitable for the screening of compound libraries generated with reactions of dynamic combinatorial chemistry when rendering libraries pseudostatic. Screening of small hydrazone libraries targeting γ-aminobutyric acid transporter 1 (GAT1), the most abundant γ-aminobutyric acid (GABA) transporter in the central nervous system, revealed two nipecotic acid derived binders with submicromolar affinities. Starting from the biphenyl carrying hit as lead structure, the objective of the present study was to discover novel high affinity GAT1 binders by screening of biphenyl focused pseudostatic hydrazone libraries formed from hydrazine 10 and 36 biphenylcarbaldehydes 11c-al. Hydrazone 12z that carried a 2',4'-dichlorobiphenyl residue was found to be the most potent binder with low nanomolar affinity (pK(i) = 8.094 ± 0.098). When stable carba analogues of representative hydrazones were synthesized and evaluated, the best binder 13z was again displaying the 2',4'-dichlorobiphenyl moiety (pK(i) = 6.930 ± 0.021).

  14. 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,...

  15. 21 CFR 522.1465 - Naltrexone hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Naltrexone hydrochloride injection. 522.1465... § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous solution contains 50 milligrams of naltrexone hydrochloride. (b) Sponsor. See 053923 in § 510.600(c)...

  16. 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....

  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, 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....

  20. Identification and determination of ketotifen hydrogen fumarate, azelastine hydrochloride, dimetindene maleate and promethazine hydrochloride by densitometric method.

    PubMed

    Wyszomirska, Elzbieta; Czerwińska, Krystyna; Kublin, Elzbieta; Mazurek, Aleksander P

    2013-01-01

    Conditions for determination of: ketotifen hydrogen fumarate, azelastine hydrochloride, dimetindene maleate and promethazine hydrochloride by densitometric method in substances and pharmaceuticals were provided. Maximum wavelenghts were: 228 nm for ketotifen hydrogen fumarate, 295 nm for azelastine hydrochloride, 265 nm for dimetindene maleate and 255 nm for promethazine hydrochloride. The limits of quantification were in the ranges of 0.2-5 microg/spot. The statistical data showed adequate accuracy and precision of developed methods. PMID:24383318

  1. Structure-Activity Relationships of Novel Salicylaldehyde Isonicotinoyl Hydrazone (SIH) Analogs: Iron Chelation, Anti-Oxidant and Cytotoxic Properties

    PubMed Central

    Potůčková, Eliška; Hrušková, Kateřina; Bureš, Jan; Kovaříková, Petra; Špirková, Iva A.; Pravdíková, Kateřina; Kolbabová, Lucie; Hergeselová, Tereza; Hašková, Pavlína; Jansová, Hana; Macháček, Miloslav; Jirkovská, Anna; Richardson, Vera; Lane, Darius J. R.; Kalinowski, Danuta S.; Richardson, Des R.; Vávrová, Kateřina; Šimůnek, Tomáš

    2014-01-01

    Salicylaldehyde isonicotinoyl hydrazone (SIH) is a lipophilic, tridentate iron chelator with marked anti-oxidant and modest cytotoxic activity against neoplastic cells. However, it has poor stability in an aqueous environment due to the rapid hydrolysis of its hydrazone bond. In this study, we synthesized a series of new SIH analogs (based on previously described aromatic ketones with improved hydrolytic stability). Their structure-activity relationships were assessed with respect to their stability in plasma, iron chelation efficacy, redox effects and cytotoxic activity against MCF-7 breast adenocarcinoma cells. Furthermore, studies assessed the cytotoxicity of these chelators and their ability to afford protection against hydrogen peroxide-induced oxidative injury in H9c2 cardiomyoblasts. The ligands with a reduced hydrazone bond, or the presence of bulky alkyl substituents near the hydrazone bond, showed severely limited biological activity. The introduction of a bromine substituent increased ligand-induced cytotoxicity to both cancer cells and H9c2 cardiomyoblasts. A similar effect was observed when the phenolic ring was exchanged with pyridine (i.e., changing the ligating site from O, N, O to N, N, O), which led to pro-oxidative effects. In contrast, compounds with long, flexible alkyl chains adjacent to the hydrazone bond exhibited specific cytotoxic effects against MCF-7 breast adenocarcinoma cells and low toxicity against H9c2 cardiomyoblasts. Hence, this study highlights important structure-activity relationships and provides insight into the further development of aroylhydrazone iron chelators with more potent and selective anti-neoplastic effects. PMID:25393531

  2. Eperisone hydrochloride-induced maculopapular rash

    PubMed Central

    Balaraddiyavar, Namrata; Bhushan, Aruna; Kotinatot, Basavaraj C.; Huggi, Gouramma

    2016-01-01

    Here, we report a case of a 30-year-old male who was prescribed eperisone hydrochloride for body pain and loose stools after which he developed severe maculopapular rash. Eperisone hydrochloride is an analgesic and antispastic drug used for spastic diseases such as spastic paralysis in cerebrovascular diseases, cervical spondylosis, and periarthritis. The drug is marketed in most of the Asian countries including India, but it is not licensed. Studies show the history of hypersensitivity in other countries, but this is the first reported case in India.

  3. Synthesis, spectroscopic, thermal and antifungal studies on lanthanum(III) and praseodymium(III) derivatives of 1,1-diacetylferrocenyl hydrazones

    NASA Astrophysics Data System (ADS)

    Sengupta, S. K.; Pandey, O. P.; Rai, Anita; Sinha, A.

    2006-09-01

    A series of new coordination complexes of La(III) and Pr(III) with hydrazones, derived from 1,1-diacetylferrocene and different aromatic acid hydrazides have been synthesized and characterized by elemental analyses, electrical conductance, magnetic moment, IR, 1H NMR, UV-vis spectra and molar conductance. The thermal behaviour of the complexes under non-isothermal condition was investigated by TG and DTG techniques. The antifungal activity of hydrazones and their corresponding complexes were also investigated.

  4. Synthesis, spectroscopic, thermal and antifungal studies on lanthanum(III) and praseodymium(III) derivatives of 1,1-diacetylferrocenyl hydrazones.

    PubMed

    Sengupta, S K; Pandey, O P; Rai, Anita; Sinha, A

    2006-09-01

    A series of new coordination complexes of La(III) and Pr(III) with hydrazones, derived from 1,1-diacetylferrocene and different aromatic acid hydrazides have been synthesized and characterized by elemental analyses, electrical conductance, magnetic moment, IR, (1)H NMR, UV-vis spectra and molar conductance. The thermal behaviour of the complexes under non-isothermal condition was investigated by TG and DTG techniques. The antifungal activity of hydrazones and their corresponding complexes were also investigated.

  5. Synthesis and luminescence properties of salicylaldehyde isonicotinoyl hydrazone derivatives and their europium complexes.

    PubMed

    Shan, Wenfei; Liu, Fen; Liu, Jiang; Chen, Yanwen; Yang, Zehui; Guo, Dongcai

    2015-09-01

    Four novel salicylaldehyde isonicotinoyl hydrazone derivatives and their corresponding europium ion complexes were synthesized and characterized, while the luminescence properties and the fluorescence quantum yields of the target complexes were investigated. The results indicated that the ligands favored energy transfers to the emitting energy level of europium ion, and four target europium complexes showed the characteristic luminescence of central europium ion. Besides the luminescence intensity of the complex with methoxy group, which possessed the highest fluorescence quantum yield (0.522), was stronger than that of other complexes. Furthermore, the electrochemical properties of the target complexes were further investigated by cyclic voltammetry, the results indicated that the highest occupied molecular orbital (HOMO), lowest unoccupied molecular orbital (LUMO) energy levels and the oxidation potential of the complexes with electron donating group increased, however, that of the complexes with accepting electron group decreased.

  6. Synthesis of some novel hydrazone and 2-pyrazoline derivatives: monoamine oxidase inhibitory activities and docking studies.

    PubMed

    Evranos-Aksöz, Begüm; Yabanoğlu-Çiftçi, Samiye; Uçar, Gülberk; Yelekçi, Kemal; Ertan, Rahmiye

    2014-08-01

    A novel series of 2-pyrazoline and hydrazone derivatives were synthesized and investigated for their human monoamine oxidase (hMAO) inhibitory activity. All compounds inhibited the hMAO isoforms (MAO-A or MAO-B) competitively and reversibly. With the exception of 5i, which was a selective MAO-B inhibitor, all derivatives inhibited hMAO-A potently and selectively. According to the experimental Ki values, compounds 6e and 6h exhibited the highest inhibitory activity towards the hMAO-A, whereas compound 5j, which carries a bromine atom at R(4) of the A ring of the pyrazoline, appeared to be the most selective MAO-A inhibitor. Tested compounds were docked computationally into the active site of the hMAO-A and hMAO-B isozymes. The computationally obtained results were in good agreement with the corresponding experimental values.

  7. Dynamic combinatorial chemistry with hydrazones: cholate-based building blocks and libraries.

    PubMed

    Simpson, Mark G; Pittelkow, Michael; Watson, Stephen P; Sanders, Jeremy K M

    2010-03-01

    We describe an efficient and general strategy for the synthesis of dimethyl acetal functionalised steroidal hydrazides based on the cholic acid skeleton with the aim of using these compounds as building blocks for dynamic combinatorial chemistry. Deprotection of the acetal protected building blocks with TFA leads to formation of libraries containing macrocyclic N-acyl hydrazone oligomers. The isolation of several of these, and their characterisation using NMR is described. The effects on the equilibrium library distribution by varying the substituents at C-7 and C-12, extending the side-chain with glycine, and inverting the configuration at C-3 are discussed. Finally, we report the exchange properties of these macrocycles and demonstrate new examples of proof-reading and self-sorting in dynamic combinatorial libraries.

  8. Synthesis and antitubercular activity of a series of hydrazone and nitrovinyl analogs derived from heterocyclic aldehydes.

    PubMed

    Sonar, Vijayakumar N; Crooks, Peter A

    2009-02-01

    A series of hydrazone and 3-nitrovinyl analogs of indole-3-carboxaldehydes and related compounds were synthesized and screened for antitubercular activity against Mycobacterium tuberculosis H37R(V) in BACTEC 12B medium using the Microplate Alamar Blue Assay (MABA). Several compounds showed inhibitory activity against M. tuberculosis in primary screening assays at a concentration of 6.25 microg/mL; subsequent dose-response studies indicated that the most active compounds, 3d, 3e & 8b, had IC(50) values of 5.96, 5.4 & 1.6 microg/mL, respectively. These compounds represent potential leads for the further development of novel antitubercular agents.

  9. 21 CFR 556.350 - Levamisole hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs § 556.350 Levamisole hydrochloride. A tolerance of 0.1 part...

  10. 21 CFR 556.350 - Levamisole hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs § 556.350 Levamisole hydrochloride. A tolerance of 0.1 part...

  11. 21 CFR 556.410 - Metoserpate hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs § 556.410 Metoserpate hydrochloride. A tolerance of 0.02 part...

  12. 21 CFR 556.410 - Metoserpate hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs § 556.410 Metoserpate hydrochloride. A tolerance of 0.02 part...

  13. 21 CFR 556.580 - Robenidine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs § 556.580 Robenidine hydrochloride. Tolerances are...

  14. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... regulations promulgated under section 412(a)(2) of the Act. (d) Prior sanctions for this ingredient different... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food..._regulations/ibr_locations.html. (c) In accordance with § 184.1(b)(1), the ingredient is used in food with...

  15. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... regulations promulgated under section 412(a)(2) of the Act. (d) Prior sanctions for this ingredient different... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food..._regulations/ibr_locations.html. (c) In accordance with § 184.1(b)(1), the ingredient is used in food with...

  16. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... regulations promulgated under section 412(a)(2) of the Act. (d) Prior sanctions for this ingredient different... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food..._regulations/ibr_locations.html. (c) In accordance with § 184.1(b)(1), the ingredient is used in food with...

  17. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ..._regulations/ibr_locations.html. (c) In accordance with § 184.1(b)(1), the ingredient is used in food with no... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Pyridoxine hydrochloride. 184.1676 Section 184.1676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED)...

  18. 21 CFR 520.222 - Bunamidine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Bunamidine hydrochloride. 520.222 Section 520.222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... days prior to their use for breeding. Do not administer to dogs or cats having known heart...

  19. 21 CFR 556.580 - Robenidine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Robenidine hydrochloride. 556.580 Section 556.580 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD...

  20. Isomerization mechanism in hydrazone-based rotary switches: lateral shift, rotation, or tautomerization?

    PubMed

    Landge, Shainaz M; Tkatchouk, Ekatarina; Benítez, Diego; Lanfranchi, Don Antoine; Elhabiri, Mourad; Goddard, William A; Aprahamian, Ivan

    2011-06-29

    Two intramolecularly hydrogen-bonded arylhydrazone (aryl = phenyl or naphthyl) molecular switches have been synthesized, and their full and reversible switching between the E and Z configurations have been demonstrated. These chemically controlled configurational rotary switches exist primarily as the E isomer at equilibrium and can be switched to the protonated Z configuration (Z-H(+)) by the addition of trifluoroacetic acid. The protonation of the pyridine moiety in the switch induces a rotation around the hydrazone C=N double bond, leading to isomerization. Treating Z-H(+) with base (K(2)CO(3)) yields a mixture of E and "metastable" Z isomers. The latter thermally equilibrates to reinstate the initial isomer ratio. The rate of the Z → E isomerization process showed small changes as a function of solvent polarity, indicating that the isomerization might be going through the inversion mechanism (nonpolar transition state). However, the plot of the logarithm of the rate constant k vs the Dimroth parameter (E(T)) gave a linear fit, demonstrating the involvement of a polar transition state (rotation mechanism). These two seemingly contradicting kinetic data were not enough to determine whether the isomerization mechanism goes through the rotation or inversion pathways. The highly negative entropy values obtained for both the forward (E → Z-H(+)) and backward (Z → E) processes strongly suggest that the isomerization involves a polarized transition state that is highly organized (possibly involving a high degree of solvent organization), and hence it proceeds via a rotation mechanism as opposed to inversion. Computations of the Z ↔ E isomerization using density functional theory (DFT) at the M06/cc-pVTZ level and natural bond orbital (NBO) wave function analyses have shown that the favorable isomerization mechanism in these hydrogen-bonded systems is hydrazone-azo tautomerization followed by rotation around a C-N single bond, as opposed to the more common

  1. Spectrophotometric, difference spectroscopic, and high-performance liquid chromatographic methods for the determination of cefixime in pharmaceutical formulations.

    PubMed

    Shah, Paresh B; Pundarikakshudu, Kilambi

    2006-01-01

    Three simple and sensitive spectrophotometric, difference spectroscopic, and liquid chromatographic (LC) methods are described for the determination of cefixime. The first method is based on the oxidative coupling reaction of cefixime with 3-methyl-2-benzothiazolinon hydrazone HCI in presence of ferric chloride. The absorbance of reaction product was measured at the maximum absorbance wavelength (wavelength(max)), 630 nm. The difference spectroscopic method is based on the measurement of absorbance of cefixime at the absorbance maximum, 268 nm, and minimum, 237 nm. The measured value was the amplitude of maxima and minima between 2 equimolar solutions of the analyte in different chemical forms, which exhibited different spectral characteristics. The conditions were optimized, and Beer's law was obeyed for cefixime at 1 to 16 microg/mL and 10 to 50 microg/mL, respectively. The third method, high-performance LC, was developed for the determination of cefixime using 50 mM potassium dihydrogen phosphate (pH 3.0)-methanol (78 + 22, v/v) as the mobile phase and measuring the response at wavelength(max) 286 nm. The analysis was performed on a Lichrospher RPC18 column. The calibration curve was obtained for cefixime at 5 to 250 microg/mL, and the mean recovery was 99.71 +/- 0.01%. The methods were validated according to the guidelines of the U.S. Pharmacopoeia and also assessed by applying the standard addition technique. The results obtained in the analysis of dosage forms agreed well with the contents stated on the labels.

  2. Synthesis and crystal structures of ethanol-coordinated molybdenum(VI) oxo complexes with tridentate hydrazone ligands.

    PubMed

    Qian, Shao-Song; Cheng, Xiao-Shan; You, Zhong-Lu; Zhu, Hai-Liang

    2013-01-01

    Reaction of [MoO2(acac)2] (where acac = acetylacetonate) with two similar hydrazone ligands in ethanol yielded two ethanol-coordinated mononuclear molybdenum(VI) oxo complexes with general formula [MoO2L(EtOH)], where L = L1 = (N'-(3,5-dibromo-2-hydroxybenzylidene)-4-nitrobenzohydrazide (H2L1), and L = L2 = (N'-(3,5-dibromo-2-hydroxybenzylidene)-2-fluorobenzohydrazide (H2L2). Crystal and molecular structures of the complexes were determined by single crystal X-ray diffraction method. All of the investigated compounds were further characterized by elemental analysis and FT-IR spectra. Single crystal X-ray structural studies indicate that the hydrazone ligands coordinate to the MoO2 cores through enolate oxygen, phenolate oxygen and azomethine nitrogen. The Mo atoms in both complexes are in octahedral coordination. Thermal stability of the complexes has also been studied.

  3. Stereoselective synthesis, spectral and antimicrobial studies of some cyanoacetyl hydrazones of 3-alkyl-2,6-diarylpiperidin-4-ones

    NASA Astrophysics Data System (ADS)

    Velayutham Pillai, M.; Rajeswari, K.; Vidhyasagar, T.

    2014-11-01

    A series of novel cyanoacetyl hydrazones of 3-alkyl-2,6-diarylpiperidin-4-ones were synthesized stereoselectively and characterized by IR, Mass, 1H NMR, 13C NMR, 1H-1H COSY and 1H-13C COSY spectra. The stereochemistry of the synthesized compounds was established using NMR spectra. Antimicrobial screening of the synthesized compounds revealed their antibacterial and antifungal potencies. Growth inhibition of Enterobacter Aerogenes by compound 15 was found to be superior to the standard drug.

  4. New Organocatalyst Scaffolds with High Activity in Promoting Hydrazone and Oxime Formation at Neutral pH

    PubMed Central

    2015-01-01

    The discovery of two new classes of catalysts for hydrazone and oxime formation in water at neutral pH, namely 2-aminophenols and 2-(aminomethyl)benzimidazoles, is reported. Kinetics studies in aqueous solutions at pH 7.4 revealed rate enhancements up to 7-fold greater than with classic aniline catalysis. 2-(Aminomethyl)benzimidazoles were found to be effective catalysts with otherwise challenging aryl ketone substrates. PMID:25545888

  5. Synthesis, characterization, biological activity and equilibrium studies of metal(II) ion complexes with tridentate hydrazone ligand derived from hydralazine

    NASA Astrophysics Data System (ADS)

    El-Sherif, Ahmed A.; Shoukry, Mohamed M.; Abd-Elgawad, Mohamed M. A.

    2012-12-01

    In the present study, a new hydrazone ligand (2-((2-phthalazin-1-yl)hydrazono)methyl)phenol) prepared by condensation of hydralazine (1-Hydralazinophthalazine) with salicylaldehyde (SAH). The synthesized SAH-hydrazone and its metal complexes have been characterized by elemental analyses, IR, 1H NMR, solid reflectance, magnetic moment, molar conductance, mass spectra, UV-vis and thermal analysis (TGA). The analytical data of the complexes show the formation of 1:1 [M:L] ratio, where M represents Ni(II), Co(II) and Cu(II) ions, while L represents the deprotonated hydrazone ligand. IR spectra show that SAH is coordinated to the metal ions in a tridentate manner through phthalazine-N, azomethine-N and phenolic-oxygen groups. The ligand and their metal chelates have been screened for their antimicrobial activities using the disc diffusion method against the selected bacteria and fungi. Proton-ligand association constants of (SAH) and the stepwise stability constants of its metal complexes are determined potentiometrically in 0.1 M NaNO3 at different temperatures and the corresponding thermodynamic parameters were derived and discussed. The order of -ΔG° and -ΔH° were found to obey Mn2+ < Co2+ < Ni2+ < Cu2+, in accordance with the Irving-Williams order. The complexes were stabilized by enthalpy changes and the results suggest that the complexation is an enthalpy-driven process. The concentration distribution diagrams of the complexes are evaluated.

  6. Synthesis, characterization, biological activity and equilibrium studies of metal(II) ion complexes with tridentate hydrazone ligand derived from hydralazine.

    PubMed

    El-Sherif, Ahmed A; Shoukry, Mohamed M; Abd-Elgawad, Mohamed M A

    2012-12-01

    In the present study, a new hydrazone ligand (2-((2-phthalazin-1-yl)hydrazono)methyl)phenol) prepared by condensation of hydralazine (1-Hydralazinophthalazine) with salicylaldehyde (SAH). The synthesized SAH-hydrazone and its metal complexes have been characterized by elemental analyses, IR, (1)H NMR, solid reflectance, magnetic moment, molar conductance, mass spectra, UV-vis and thermal analysis (TGA). The analytical data of the complexes show the formation of 1:1 [M:L] ratio, where M represents Ni(II), Co(II) and Cu(II) ions, while L represents the deprotonated hydrazone ligand. IR spectra show that SAH is coordinated to the metal ions in a tridentate manner through phthalazine-N, azomethine-N and phenolic-oxygen groups. The ligand and their metal chelates have been screened for their antimicrobial activities using the disc diffusion method against the selected bacteria and fungi. Proton-ligand association constants of (SAH) and the stepwise stability constants of its metal complexes are determined potentiometrically in 0.1 M NaNO(3) at different temperatures and the corresponding thermodynamic parameters were derived and discussed. The order of -ΔG° and -ΔH° were found to obey Mn(2+)

  7. Yohimbine hydrochloride reversal of ketamine hydrochloride and xylazine hydrochloride immobilization of Bengal tigers and effects on hematology and serum chemistries.

    PubMed

    Seal, U S; Armstrong, D L; Simmons, L G

    1987-04-01

    Six bengal tigers (Panthera tigris tigris) were immobilized five times at 2-wk intervals with ketamine hydrochloride (ketamine) and xylazine hydrochloride (xylazine) mixtures at different dose levels. Hematology and serum chemistry analyses on blood samples collected at each immobilization remained normal during the study. There were acute changes in hematocrit, chloride, potassium, glucose, and bilirubin as a function of xylazine dose level. The effect of yohimbine hydrochloride (yohimbine) on the depth and duration of immobilization was evaluated in a crossover design with every animal serving as its own control at each dose. Administration of yohimbine resulted in recovery of the animals within 4-8 min in contrast to greater than 60 min with no yohimbine treatment. There were no adverse effects noted with the yohimbine treatment and the tigers did not exhibit a relapse over the next 24 hr. Yohimbine at a dose of 5-15 mg per adult tiger provided effective reversal of 50-150 mg of xylazine per tiger.

  8. Yohimbine hydrochloride reversal of ketamine hydrochloride and xylazine hydrochloride immobilization of Bengal tigers and effects on hematology and serum chemistries.

    PubMed

    Seal, U S; Armstrong, D L; Simmons, L G

    1987-04-01

    Six bengal tigers (Panthera tigris tigris) were immobilized five times at 2-wk intervals with ketamine hydrochloride (ketamine) and xylazine hydrochloride (xylazine) mixtures at different dose levels. Hematology and serum chemistry analyses on blood samples collected at each immobilization remained normal during the study. There were acute changes in hematocrit, chloride, potassium, glucose, and bilirubin as a function of xylazine dose level. The effect of yohimbine hydrochloride (yohimbine) on the depth and duration of immobilization was evaluated in a crossover design with every animal serving as its own control at each dose. Administration of yohimbine resulted in recovery of the animals within 4-8 min in contrast to greater than 60 min with no yohimbine treatment. There were no adverse effects noted with the yohimbine treatment and the tigers did not exhibit a relapse over the next 24 hr. Yohimbine at a dose of 5-15 mg per adult tiger provided effective reversal of 50-150 mg of xylazine per tiger. PMID:3586208

  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, 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...

  11. 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...

  12. 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...

  13. 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...

  14. 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...

  15. Biting deterrence and insecticidal activity of hydrazide–hydrazones and their corresponding 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles against Aedes aegypti

    Technology Transfer Automated Retrieval System (TEKTRAN)

    BACKGROUND: Hydrazones are important compounds for drug design and they have also good insecticidal activity. In this study, A series of hydrazide–hydrazones (1-10) and 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles (11-20) were investigated for their biting deterrent and insecticidal act...

  16. Z-Group ketone chain transfer agents for RAFT polymer nanoparticle modification via hydrazone conjugation

    PubMed Central

    Bandyopadhyay, Saibal; Xia, Xin; Maiseiyeu, Andrei; Mihai, Georgeta; Rajagopalan, Sanjay

    2012-01-01

    A ketal-containing trithiocarbonyl compound has been synthesized and characterized as a chain transfer agent (CTA) in Reversible Addition Fragmentation Transfer (RAFT) polymerization. The ketal functionality does not interfere with RAFT polymerization of acrylate monomers, which proceeds as previously reported to yield macro-CTA polymers and block co-polymers. Post-polymerization ketal cleavage revealed ketone functionality at the polar terminus of an amphiphilic block co-polymer. Hydrazone-formation was facile in both organic solution as well as in aqueous buffer where polymer nanoparticle assemblies were formed, indicating a conjugation/end-functionalization yield of 40–50%. Conjugation was verified with fluorescein, biotin and Gd-DOTA derivatives, and though the trithiocarbonate linkage is hydrolytically labile, we observed stable conjugation for several days at pH 7.4. and 37°C. As expected, streptavidin binding to biotinylated polymer micelles was observed, and size-change based relaxivity increases were observed when Gd-DOTA hydrazide was conjugated to polymer micelles. Cell-uptake of fluorescently labeled polymer micelles was also readily tracked by FACS and fluorescence microscopy. These polymer derivatives demonstrate a range of potential theranostic/biotechnological applications for this conveniently accessible keto-CTA, which include ligand-based nanoparticle targeting and fluorescent/MR nanoparticle contrast agents. PMID:23148126

  17. A dual colorimetric and fluorescent sensor for lead ion based on naphthalene hydrazone derivative

    NASA Astrophysics Data System (ADS)

    Wu, Fang-Ying; Zhang, Hua; Xiao, Ming; Han, Bing-Xin

    2013-05-01

    A new compound, 2-boronobenzaldehyde-(2'-hydroxyl-4'-sulfonic acid) naphthalene hydrazone (1), was synthesized and its structure was characterized by proton nuclear magnetic resonance, mass and element analyses. The presence of Pb2+ led 1 to undergo colorimetric and fluorescent changes, which were detectable with the naked eye. Thus, a dual spectral response for Pb2+ detection was introduced. In KH2PO4-NaOH buffer aqueous solution (pH 6.0), 1 exhibited fluorescence enhancement at 568 nm and hyperchromicity at 595 nm upon the addition of Pb2+. The fluorescent intensity change was proportionate to the concentration of Pb2+ with a dynamic working range of 5.0 × 10-7 mol L-1 to 1.0 × 10-4 mol L-1 and a detection limit of 3.7 × 10-8 mol L-1. The fluorometric method was successfully applied for the detection of Pb2+ water of Qianhu Lake and soil in Nanchang university campus. The recoveries were 111-116% for water and 97.6% for soil respectively, determined via the standard addition method.

  18. Antitumor activity of a 2-pyridinecarboxaldehyde 2-pyridinecarboxylic acid hydrazone copper complex and the related mechanism.

    PubMed

    Yang, Yingli; Huang, Tengfei; Zhou, Sufeng; Fu, Yun; Liu, Youxun; Yuan, Yanbin; Zhang, Qiongqing; Li, Shaoshan; Li, Changzheng

    2015-09-01

    In the present study, 2-pyridinecarboxaldehyde 2-pyridinecarboxylic acid hydrazone (PPAH) was prepared and its antitumor activity was evaluated. The inhibition of proliferation of PPAH against the HepG2 and HCT-116 cell lines was less effective, yet in the presence of copper ions, the mixture demonstrated excellent antitumor activity (IC50 at 2.75±0.30 µM for the HepG2 cell line, and 1.90±0.20 µM for the HCT-116 cell line, respectively) and the new active species was confirmed to be a PPAH copper complex with a 1:1 ratio by spectral analysis. The excellent antitumor activity of the copper complex prompted us to investigate the underlying mechanism. RT-PCR was performed to detect the changes in the expression of apoptotic genes induced by PPAH and its copper complex. However, no changes were observed when the cells were treated by the agents for 24 or 48 h, indicating that ROS were unlikely involved. Cell cycle analysis showed that both PPAH and its copper complex led to S phase arrest of the cells. The sDNA relaxation assay revealed that the PPAH-copper complex displayed dual topoisomerase inhibition for type I and II. The data suggest that the inhibition of proliferation exhibited by the PPAH copper complex may stem from its dual topoisomerase inhibition, which is rarely observed for a metal complex.

  19. Synthesis, characterization, investigation of biological activity and theoretical studies of hydrazone compounds containing choloroacetyl group

    NASA Astrophysics Data System (ADS)

    Cukurovali, Alaaddin; Yilmaz, Engin

    2014-10-01

    In this study, three new hydrazide-hydrazone derivative compounds which contain choloroacetyl group have been synthesized and characterized. In the characterization, spectral techniques such as IR, 1H NMR, 13C NMR and UV-Vis spectroscopy techniques were used. Antibacterial effects of the synthesized compounds were investigated against Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853. In the theoretical calculations Gaussian 09 software was used with the DFT/6-311+(d,p) basis set. Experimental X-ray analysis of compounds has not been studied. Theoretical bond lengths of synthesized compounds were compared with experimental bond lengths of a similar compound. Theoretical and experimental bond lengths are in good agreement with R2: 0.896, 0.899 and 0.900 for compounds 1, 2, and 3, respectively. For antibacterial activity, the most effective one was found to be N‧-(4-bromobenzylidene)-2-chloro-N-(4-(3-methyl-3-phenylcyclobutyl)-thiazol-2-yl) acetohydrazide against P.aeroginaosa ATTC 27853, among the studied compounds.

  20. Catalytic N-radical cascade reaction of hydrazones by oxidative deprotonation electron transfer and TEMPO mediation

    PubMed Central

    Hu, Xiao-Qiang; Qi, Xiaotian; Chen, Jia-Rong; Zhao, Quan-Qing; Wei, Qiang; Lan, Yu; Xiao, Wen-Jing

    2016-01-01

    Compared with the popularity of various C-centred radicals, the N-centred radicals remain largely unexplored in catalytic radical cascade reactions because of a lack of convenient methods for their generation. Known methods for their generation typically require the use of N-functionalized precursors or various toxic, potentially explosive or unstable radical initiators. Recently, visible-light photocatalysis has emerged as an attractive tool for the catalytic formation of N-centred radicals, but the pre-incorporation of a photolabile groups at the nitrogen atom largely limited the reaction scope. Here, we present a visible-light photocatalytic oxidative deprotonation electron transfer/2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO)-mediation strategy for catalytic N-radical cascade reaction of unsaturated hydrazones. This mild protocol provides a broadly applicable synthesis of 1,6-dihydropyradazines with complete regioselectivity and good yields. The 1,6-dihydropyradazines can be easily transformed into diazinium salts that showed promising in vitro antifungal activities against fungal pathogens. DFT calculations are conducted to explain the mechanism. PMID:27048886

  1. Dark Hydrazone Fluorescence Labeling Agents Enable Imaging of Cellular Aldehydic Load.

    PubMed

    Yuen, Lik Hang; Saxena, Nivedita S; Park, Hyun Shin; Weinberg, Kenneth; Kool, Eric T

    2016-08-19

    Aldehydes are key intermediates in many cellular processes, from endogenous metabolic pathways like glycolysis to undesired exogenously induced processes such as lipid peroxidation and DNA interstrand cross-linking. Alkyl aldehydes are well documented to be cytotoxic, affecting the functions of DNA and protein, and their levels are tightly regulated by the oxidative enzyme ALDH2. Mutations in this enzyme are associated with cardiac damage, diseases such as Fanconi anemia (FA), and cancer. Many attempts have been made to identify and quantify the overall level of these alkyl aldehydes inside cells, yet there are few practical methods available to detect and monitor these volatile aldehydes in real time. Here, we describe a multicolor fluorogenic hydrazone transfer ("DarkZone") system to label alkyl aldehydes, yielding up to 30-fold light-up response in vitro. A cell-permeant DarkZone dye design was applied to detect small-molecule aldehydes in the cellular environment. The new dye design also enabled the monitoring of cellular acetaldehyde production from ethanol over time by flow cytometry, demonstrating the utility of the DarkZone dyes for measuring and imaging the aldehydic load related to human disease. PMID:27326450

  2. Synthesis, characterization and studies on the nonlinear optical parameters of hydrazones

    NASA Astrophysics Data System (ADS)

    Naseema, K.; Sujith, K. V.; Manjunatha, K. B.; Kalluraya, Balakrishna; Umesh, G.; Rao, Vijayalakshmi

    2010-07-01

    Three hydrazones, 2-(4-methylphenoxy)- N'-[(1E)-(4-nitrophenyl)methylene]acetohydrazide (compound-1), 2-(4-methylphenoxy)- N'-[(1E)-(4-methylphenyl)methylene]acetohydrazide ((compound-2) and N'-{(1E)-[4-(dimethylamino)phenyl]methylene}-2-(4-ethylphenoxy) acetohydrazide(compound-3) were synthesized and their third order nonlinear optical properties were investigated using a single beam z-scan technique with nanosecond laser pulses at 532 nm. Open aperture data obtained from the three compounds indicates two photon absorption at this wavelength. The nonlinear refractive index n2, the nonlinear absorption coefficient β, the magnitude of the effective third order susceptibility χ(3), the second order hyperpolarizability γh and the coupling factor ρ have been estimated. The values obtained are comparable with the values obtained for 4-methoxy chalcone derivatives and dibenzylidene acetone derivatives. Among the compounds studied, compounds-1 and 3 exhibited the better optical power limiting behaviour at 532 nm. Our studies suggest that compounds-1, 2 and 3 are potential candidates for optical device applications such as optical limiters and optical switches.

  3. 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 520.2098 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 § 520.2098 Selegiline hydrochloride tablets. (a)...

  4. 21 CFR 520.1242 - Levamisole hydrochloride oral dosage forms.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 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....

  5. 21 CFR 520.1242 - Levamisole hydrochloride oral dosage forms.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 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....

  6. 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....

  7. 21 CFR 522.2474 - Tolazoline hydrochloride injection.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Tolazoline hydrochloride injection. 522.2474 Section 522.2474 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... solution contains tolazoline hydrochloride equivalent to 100 milligrams of base activity. (b) Sponsor....

  8. 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... solution contains tolazoline hydrochloride equivalent to 100 milligrams of base activity. (b) Sponsor....

  9. 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...

  10. 21 CFR 520.1263c - Lincomycin hydrochloride soluble powder.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Lincomycin hydrochloride soluble powder. 520.1263c... Lincomycin hydrochloride soluble powder. (a) Specifications. Each gram of soluble powder contains lincomycin... water containing lincomycin. Not for use in layer and breeder chickens....

  11. 21 CFR 520.1263c - Lincomycin hydrochloride soluble powder.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Lincomycin hydrochloride soluble powder. 520.1263c... Lincomycin hydrochloride soluble powder. (a) Specifications. Each gram of soluble powder contains lincomycin... water containing lincomycin. Not for use in layer and breeder chickens....

  12. 21 CFR 520.1263c - Lincomycin hydrochloride soluble powder.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Lincomycin hydrochloride soluble powder. 520.1263c... Lincomycin hydrochloride soluble powder. (a) Specifications. Each gram of soluble powder contains lincomycin... water containing lincomycin. Not for use in layer and breeder chickens....

  13. 21 CFR 522.2474 - Tolazoline hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tolazoline hydrochloride injection. 522.2474... § 522.2474 Tolazoline hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous...—(i) Amount. Administer slowly by intravenous injection 4 milligrams per kilogram of body weight or...

  14. 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... § 522.2474 Tolazoline hydrochloride injection. (a) Specifications. Each milliliter of sterile aqueous...—(i) Amount. Administer slowly by intravenous injection 4 milligrams per kilogram of body weight or...

  15. 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. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  16. 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. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... 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. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  18. 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. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms....

  19. 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...

  20. Luminescent properties of a di-hydrazone derived from the antituberculosis agent isoniazid: Potentiality as an emitting layer constituent for OLED fabrication

    NASA Astrophysics Data System (ADS)

    Moraes, Rafaela S.; Aderne, Rian E.; Cremona, Marco; Rey, Nicolás A.

    2016-02-01

    Hydrazones constitute a class of compounds presenting azomethine R‧R″Nsbnd Ndbnd CHsbnd R hydrogens, which show diverse properties and a wide range of applications. A hydrazone derived from the antituberculosis drug isoniazid, namely, N,N‧-diisonicotinoyl-2-hydroxy-5-methylisophthalaldehyde hydrazone (DMD) was synthesized and chemically characterized. Its luminescent properties were also investigated, as well as the possibility of using this compound as a constituent of the emitting layer for the fabrication of OLEDs. Co-deposited devices were fabricated using the organic molecule BSBF as matrix and DMD as dopant. All the devices presented a broad electroluminescence band, in which it was possible to recognize the DMD emission along with emissions of some of the other organic layers. The best results were obtained with 35% DMD doping, achieving a luminance of about 35 cd/m2.

  1. Hypersensitivity to the local anesthetic articaine hydrochloride.

    PubMed Central

    Malanin, K.; Kalimo, K.

    1995-01-01

    A patient developed skin erythema and wheals within 1 h after local dental anesthesia with articaine hydrochloride. Pretreatment with oral terfenadine or topical betamethasone dipropionate prevented her reaction to articaine. In contrast, neither pretreatment with oral aspirin nor topical capsaicin affected her reaction to articaine. The results of radioallergosorbent tests (RAST) to articaine and a passive transfer test were negative. The reaction was probably caused by a complement-mediated mechanism leading to the degranulation of mast cells. The patient tolerated local anesthesia with lidocaine. PMID:8934983

  2. Fast and catalyst-free hydrazone ligation via ortho-halo-substituted benzaldehydes for protein C-terminal labeling at neutral pH.

    PubMed

    Xu, Yang; Xu, Ling; Xia, Yuan; Guan, Chao-Jian; Guo, Qing-Xiang; Fu, Yao; Wang, Chen; Li, Yi-Ming

    2015-08-28

    Rapid and catalyst-free hydrazone ligation reaction between ortho-halobenzaldehyde derivatives and peptide/protein hydrazides was observed at neutral pH and room temperature. 2-Chlorobenzaldehyde exhibited the fastest reaction and highest conversion rates among the series of ortho-halobenzaldehydes. The resulting hydrazone-containing bioconjugation products were also found to be fairly stable under experimental conditions. The new ligation strategy was successfully used for protein C-terminal labeling and should provide a practical approach for the modification of proteins.

  3. Relative predominance of azo and hydrazone tautomers of 4-carboxyl-2,6-dinitrophenylazohydroxynaphthalenes in binary solvent mixtures

    NASA Astrophysics Data System (ADS)

    Adegoke, Olajire A.

    2011-12-01

    Azo-hydrazone tautomerism is a phenomenon that occurs in azo dyes possessing substituents conjugated to the azo linkage which has labile proton that can be exchanged intramolecularly. Thus the predominance of one tautomer over another is a function of many factors among which are solvent polarity, solvent type, solute-solvent interactions and the structure of the dye molecule itself. The 4-carboxyl-2,6-dinitrophenylazohydroxynaphthalenes, previously shown to exhibit azo-hydrazone tautomerism, were studied for the relative predominance of one form over another based on interaction at the microenvironment of binary solvent mixtures containing DMF and non-hydrogen bonding (CCl 4), hydrogen bond donor (toluene, chloroform), hydrogen bond acceptor (acetonitrile, acetone) and the alcohols; ethanol and methanol as solvent pairs. The three dyes gave two main bands in the 50:50 mixture of DMF with these solvents consisting of a high energy band at 250-382 nm while the low energy bands for the dyes occurred at 415-485 nm. Spectral shifts in the binary solvent mixtures were related to the solvent dipolarity, basicity of the less polar component relative to DMF, substituent type, molar transition energy, formation constant for the hydrogen-bonding solvated complexes and the standard free energy change for hydrogen bonding with DMF. The relative predominance of the hydrazone tautomer bears a direct relationship to the basicity of the solvent, presence of hydrogen bond donor substituent and was associated with high molar transition energies and low formation constant. The microenvironment surrounding the dye molecules played a major role in the stability of one tautomer relative to the other.

  4. Rhodamine 6G hydrazone bearing thiophene unit: A highly sensitive and selective off-on fluorescent chemosensor for Al3+

    NASA Astrophysics Data System (ADS)

    Wu, Wei-Na; Mao, Pan-Dong; Wang, Yuan; Zhao, Xiao-Lei; Jia, Lei; Xu, Zhou-Qing

    2016-10-01

    A rhodamine derivative (R1) has been synthesized by a hydrazone formation of rhodamine 6G hydrazide with 3-methylthiophene-2-carbaldehyde, which exhibits high selectivity and sensitivity as an "off-on" fluorescent sensor toward Al3+ in water containing media. The binding process was confirmed by UV-vis absorption, fluorescence measurements, mass spectroscopy and DFT calculation. The probe functions by Al3+ induced hydrolytic cleavage of the imine-bond to produce an intense rhodamine-based emission. To test the practical use of the probe, the determination of Al3+ in real water samples was also evaluated.

  5. Syntheses, crystal structure, Hirshfeld surfaces, fluorescence properties, and DFT analysis of benzoic acid hydrazone Schiff bases

    NASA Astrophysics Data System (ADS)

    Alam, Mohammad Sayed; Lee, Dong-Ung

    2015-06-01

    Two hydrazone Schiff base analogues, namely, (E)-N‧-(4-hydroxy-3-methoxybenzylidene)benzohydrazide (3a) and (E)-N‧-(4-methoxybenzylidene)benzohydrazide (3b), were synthesized using a mild, efficient method and characterized by 1H NMR, mass spectrometry, elemental analysis, and single-crystal X-ray diffraction. X-ray analysis of a single crystal of 3a revealed a tetragonal, space group I4(1)/a structure, with an E-configuration around the azomethine (sbnd C8dbnd N2sbnd) double bond. In this structure, the sbnd NHsbnd and sbnd OH groups act as proton donors and the >Cdbnd O and sbnd Ndbnd groups as proton acceptors, and these facilitate hydrogen bond formation in the crystal state. Plausible intermolecular interactions were studied using 3D Hirshfeld surfaces and related 2D fingerprint plots. The optimized geometry, vibrational frequencies, Mulliken charge distribution, molecular electrostatic potential (MEP) maps, frontier molecular orbitals (FMOs), and associated energies of the ground state and the first single excited state were calculated using density functional theory (DFT) and time-dependant DFT calculations using the B3LYP/6-311G method. Vibrational frequencies calculated in the gaseous phase compared with experimental values measured in the solid state and showed good agreement with each other. The chemical reactivities of 3a and 3b were predicted by mapping MEP surface over optimized geometries and comparing these with MEP map generated over crystal structures. Mulliken charge distribution analysis and MEP map of 3a and 3b revealed that N(1), O(1), O(2) and O(3) atoms could act as electron donors and coordinate with metals and that these represented the most suitable sites for electrophilic attack. In fluorescence spectra, the absorption and emission spectra of 3a and 3b were similar in different polar solvents with few exceptions. In addition, both compounds exhibited dual emission spectra in acetone due to keto-enol tautomerism induced by

  6. Reversible photochromic system based on rhodamine B salicylaldehyde hydrazone metal complex.

    PubMed

    Li, Kai; Xiang, Yu; Wang, Xiaoyan; Li, Ji; Hu, Rongrong; Tong, Aijun; Tang, Ben Zhong

    2014-01-29

    Photochromic molecules are widely applied in chemistry, physics, biology, and materials science. Although a few photochromic systems have been developed before, their applications are still limited by complicated synthesis, low fatigue resistance, or incomplete light conversion. Rhodamine is a class of dyes with excellent optical properties including long-wavelength absorption, large absorption coefficient, and high photostability in its ring-open form. It is an ideal chromophore for the development of new photochromic systems. However, known photochromic rhodamine derivatives, such as amides, exhibit only millisecond lifetimes in their colored ring-open forms, making their application very limited and difficult. In this work, rhodamine B salicylaldehyde hydrazone metal complex was found to undergo intramolecular ring-open reactions upon UV irradiation, which led to a distinct color and fluorescence change both in solution and in solid matrix. The complex showed good fatigue resistance for the reversible photochromism and long lifetime for the ring-open state. Interestingly, the thermal bleaching rate was tunable by using different metal ions, temperatures, solvents, and chemical substitutions. It was proposed that UV light promoted isomerization of the rhodamine B derivative from enol-form to keto-form, which induced ring-opening of the rhodamine spirolactam in the complex to generate color. The photochromic system was successfully applied for photoprinting and UV strength measurement in the solid state. As compared to other reported photochromic molecules, the system in this study has its advantages of facile synthesis and tunable thermal bleaching rate, and also provides new insights into the development of photochromic materials based on metal complex and spirolactam-containing dyes. PMID:24397593

  7. Iron chelation with salicylaldehyde isonicotinoyl hydrazone protects against catecholamine autoxidation and cardiotoxicity.

    PubMed

    Hašková, Pavlína; Kovaříková, Petra; Koubková, Lucie; Vávrová, Anna; Macková, Eliška; Simůnek, Tomáš

    2011-02-15

    Elevated catecholamine levels are known to induce damage of the cardiac tissue. This catecholamine cardiotoxicity may stem from their ability to undergo oxidative conversion to aminochromes and concomitant production of reactive oxygen species (ROS), which damage cardiomyocytes via the iron-catalyzed Fenton-type reaction. This suggests the possibility of cardioprotection by iron chelation. Our in vitro experiments have demonstrated a spontaneous decrease in the concentration of the catecholamines epinephrine and isoprenaline during their 24-h preincubation in buffered solution as well as their gradual conversion to oxidation products. These changes were significantly augmented by addition of iron ions and reduced by the iron-chelating agent salicylaldehyde isonicotinoyl hydrazone (SIH). Oxidized catecholamines were shown to form complexes with iron that had significant redox activity, which could be suppressed by SIH. Experiments using the H9c2 cardiomyoblast cell line revealed higher cytotoxicity of oxidized catecholamines than of the parent compounds, apparently through the induction of caspase-independent cell death, whereas co-incubation of cells with SIH was able to significantly preserve cell viability. A significant increase in intracellular ROS formation was observed after the incubation of cells with catecholamine oxidation products; this could be significantly reduced by SIH. In contrast, parent catecholamines did not increase, but rather decreased, cellular ROS production. Hence, our results demonstrate an important role for redox-active iron in catecholamine autoxidation and subsequent toxicity. The iron chelator SIH has shown considerable potential to protect cardiac cells by both inhibition of deleterious catecholamine oxidation to reactive intermediates and prevention of ROS-mediated cardiotoxicity.

  8. Syntheses, crystal structure, Hirshfeld surfaces, fluorescence properties, and DFT analysis of benzoic acid hydrazone Schiff bases.

    PubMed

    Alam, Mohammad Sayed; Lee, Dong-Ung

    2015-06-15

    Two hydrazone Schiff base analogues, namely, (E)-N'-(4-hydroxy-3-methoxybenzylidene)benzohydrazide (3a) and (E)-N'-(4-methoxybenzylidene)benzohydrazide (3b), were synthesized using a mild, efficient method and characterized by (1)H NMR, mass spectrometry, elemental analysis, and single-crystal X-ray diffraction. X-ray analysis of a single crystal of 3a revealed a tetragonal, space group I4(1)/a structure, with an E-configuration around the azomethine (C8N2) double bond. In this structure, the NH and OH groups act as proton donors and the >CO and N groups as proton acceptors, and these facilitate hydrogen bond formation in the crystal state. Plausible intermolecular interactions were studied using 3D Hirshfeld surfaces and related 2D fingerprint plots. The optimized geometry, vibrational frequencies, Mulliken charge distribution, molecular electrostatic potential (MEP) maps, frontier molecular orbitals (FMOs), and associated energies of the ground state and the first single excited state were calculated using density functional theory (DFT) and time-dependant DFT calculations using the B3LYP/6-311G method. Vibrational frequencies calculated in the gaseous phase compared with experimental values measured in the solid state and showed good agreement with each other. The chemical reactivities of 3a and 3b were predicted by mapping MEP surface over optimized geometries and comparing these with MEP map generated over crystal structures. Mulliken charge distribution analysis and MEP map of 3a and 3b revealed that N(1), O(1), O(2) and O(3) atoms could act as electron donors and coordinate with metals and that these represented the most suitable sites for electrophilic attack. In fluorescence spectra, the absorption and emission spectra of 3a and 3b were similar in different polar solvents with few exceptions. In addition, both compounds exhibited dual emission spectra in acetone due to keto-enol tautomerism induced by photoexcitation. PMID:25804368

  9. Hydrazone chelators for the treatment of iron overload disorders: iron coordination chemistry and biological activity.

    PubMed

    Bernhardt, Paul V; Chin, Piao; Sharpe, Philip C; Richardson, Des R

    2007-08-14

    The potentially tridentate ligand 2-pyridinecarbaldehyde isonicotinoyl hydrazone (HPCIH) and its analogues are an emerging class of orally effective Fe chelators that show great promise for the treatment of Fe overload diseases. Herein, we present an extensive study of the Fe coordination chemistry of the HPCIH analogues including the first crystallographically characterised Fe(II) complex of these chelators. Unlike most other clinically effective Fe chelators, the HPCIH analogues bind Fe(II) and not Fe(III). In fact, these chelators form low-spin bis-ligand Fe(II) complexes, although NMR suggests that the complexes are close to the high-spin/low-spin crossover. All the Fe complexes show a high potential Fe(III/II) redox couple (> 500 mV vs. NHE) and cyclic voltammetry in aqueous or mixed aqueous/organic solvents is irreversible as a consequence of a rapid hydration reaction that occurs upon oxidation. A number of the HPCIH analogues show high activity at inducing Fe efflux from cells and also at preventing Fe uptake by cells from the serum Fe transport protein transferrin. As a class of ligands, these chelators are more effective at reducing Fe uptake from transferrin than inducing Fe mobilisation from cells. This may be related to their ability to intercept Fe(II) after its release from transferrin within the cell. Our studies indicate that their Fe chelation efficacy is due, at least in part, to the fact that these ligands and their Fe(II) complexes are neutral at physiological pH (7.4) and sufficiently lipophilic to permeate cell membranes. PMID:17893768

  10. Syntheses, crystal structure, Hirshfeld surfaces, fluorescence properties, and DFT analysis of benzoic acid hydrazone Schiff bases.

    PubMed

    Alam, Mohammad Sayed; Lee, Dong-Ung

    2015-06-15

    Two hydrazone Schiff base analogues, namely, (E)-N'-(4-hydroxy-3-methoxybenzylidene)benzohydrazide (3a) and (E)-N'-(4-methoxybenzylidene)benzohydrazide (3b), were synthesized using a mild, efficient method and characterized by (1)H NMR, mass spectrometry, elemental analysis, and single-crystal X-ray diffraction. X-ray analysis of a single crystal of 3a revealed a tetragonal, space group I4(1)/a structure, with an E-configuration around the azomethine (C8N2) double bond. In this structure, the NH and OH groups act as proton donors and the >CO and N groups as proton acceptors, and these facilitate hydrogen bond formation in the crystal state. Plausible intermolecular interactions were studied using 3D Hirshfeld surfaces and related 2D fingerprint plots. The optimized geometry, vibrational frequencies, Mulliken charge distribution, molecular electrostatic potential (MEP) maps, frontier molecular orbitals (FMOs), and associated energies of the ground state and the first single excited state were calculated using density functional theory (DFT) and time-dependant DFT calculations using the B3LYP/6-311G method. Vibrational frequencies calculated in the gaseous phase compared with experimental values measured in the solid state and showed good agreement with each other. The chemical reactivities of 3a and 3b were predicted by mapping MEP surface over optimized geometries and comparing these with MEP map generated over crystal structures. Mulliken charge distribution analysis and MEP map of 3a and 3b revealed that N(1), O(1), O(2) and O(3) atoms could act as electron donors and coordinate with metals and that these represented the most suitable sites for electrophilic attack. In fluorescence spectra, the absorption and emission spectra of 3a and 3b were similar in different polar solvents with few exceptions. In addition, both compounds exhibited dual emission spectra in acetone due to keto-enol tautomerism induced by photoexcitation.

  11. Synthesis, Biological Evaluation and Molecular Docking Study of Hydrazone-Containing Pyridinium Salts as Cholinesterase Inhibitors.

    PubMed

    Parlar, Sulunay; Bayraktar, Gulsah; Tarikogullari, Ayse Hande; Alptüzün, Vildan; Erciyas, Ercin

    2016-01-01

    A series of pyridinium salts bearing alkylphenyl groups at 1 position and hydrazone structure at 4 position of the pyridinium ring were synthesized and evaluated for the inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. The cholinesterase (ChE) inhibitory activity studies were carried out by using the Ellman's colorimetric method. All compounds displayed considerable AChE and BuChE inhibitory activity and some of the compounds manifested remarkable anti-AChE activity compared to the reference compound, galantamine. Among the title compounds, the series including benzofuran aromatic ring exhibited the best inhibitory activity both on AChE and BuChE enzymes. Compound 3b, 4-[2-(1-(benzofuran-2-yl)ethylidene)hydrazinyl]-1-(3-phenylpropyl)pyridinium bromide, was the most active compound with IC50 value of 0.23 (0.24) µM against enantiomeric excess (ee)AChE (human (h)AChE) while compound 3a, 4-[2-(1-(benzofuran-2-yl)ethylidene)hydrazinyl]-1-phenethylpyridinium bromide, was the most active compound with IC50 value of 0.95 µM against BuChE. Moreover, 3a and b exhibited higher activity than the reference compound galantamine (eeAChE (hAChE) IC50 0.43 (0.52) µM; BuChE IC50 14.92 µM). Molecular docking studies were carried out on 3b having highest inhibitory activity against AChE. PMID:27581632

  12. 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

  13. Hydrochloride salt co-crystals: preparation, characterization and physicochemical studies.

    PubMed

    Parmar, Vijaykumar K; Shah, Shailesh A

    2013-01-01

    Co-crystallization approach for modification of physicochemical properties of hydrochloride salt is presented. The objective of this investigation was to study the effect of co-crystallization with different co-crystal formers on physicochemical properties of fluoxetine hydrochloride (FH). FH was screened for co-crystallization with a series of carboxylic acid co-formers by slow evaporation method. Photomicrographs and melting points of crystalline phases were determined. The co-crystals were characterized by FTIR, DSC and PXRD methods. Solubility of co-crystals was determined in water and buffer solutions. Powder and intrinsic dissolution profiles were assessed for co-crystals. Physical mixtures of drug and co-formers were used for comparisons at characterizations and physicochemical properties evaluation stages. Four co-crystals of FH viz. Fluoxetine hydrochloride-maleic acid (FH-MA), Fluoxetine hydrochloride-glutaric acid (FH-GA), Fluoxetine hydrochloride-L-tartaric acid (FH-LTA) and Fluoxetine hydrochloride-DL-tartaric acid (FH-DLTA) were obtained from screening experiments. Physical characterization showed that they have unique crystal morphology, thermal, spectroscopic and X-ray diffraction properties. Solubility and dissolution studies showed that Fluoxetine hydrochloride-maleic acid co-crystal possess high aqueous solubility in distilled water, pH 4.6, 7.0 buffer solutions and dissolution rate in distilled water than that of pure drug. Co-crystal formation approach can be used for ionic API to tailor its physical properties. PMID:22686294

  14. Hydrochloride salt co-crystals: preparation, characterization and physicochemical studies.

    PubMed

    Parmar, Vijaykumar K; Shah, Shailesh A

    2013-01-01

    Co-crystallization approach for modification of physicochemical properties of hydrochloride salt is presented. The objective of this investigation was to study the effect of co-crystallization with different co-crystal formers on physicochemical properties of fluoxetine hydrochloride (FH). FH was screened for co-crystallization with a series of carboxylic acid co-formers by slow evaporation method. Photomicrographs and melting points of crystalline phases were determined. The co-crystals were characterized by FTIR, DSC and PXRD methods. Solubility of co-crystals was determined in water and buffer solutions. Powder and intrinsic dissolution profiles were assessed for co-crystals. Physical mixtures of drug and co-formers were used for comparisons at characterizations and physicochemical properties evaluation stages. Four co-crystals of FH viz. Fluoxetine hydrochloride-maleic acid (FH-MA), Fluoxetine hydrochloride-glutaric acid (FH-GA), Fluoxetine hydrochloride-L-tartaric acid (FH-LTA) and Fluoxetine hydrochloride-DL-tartaric acid (FH-DLTA) were obtained from screening experiments. Physical characterization showed that they have unique crystal morphology, thermal, spectroscopic and X-ray diffraction properties. Solubility and dissolution studies showed that Fluoxetine hydrochloride-maleic acid co-crystal possess high aqueous solubility in distilled water, pH 4.6, 7.0 buffer solutions and dissolution rate in distilled water than that of pure drug. Co-crystal formation approach can be used for ionic API to tailor its physical properties.

  15. Submicron Organic Matter in a Peri-alpine, Ultra-oligotrphic Lake

    SciTech Connect

    Chanudet,V.; Filella, M.

    2007-01-01

    Combining organic carbon (OC) measurements with the classic MBTH (3-methyl-2-benzothiazolinone hydrochloride) method for carbohydrate determination and a new voltammetric method for the determination of refractory organic matter (ROM) made it possible, for the first time, to quantify the types, sources and fate of submicron organic matter present in an ultra-oligotrophic lake (Lake Brienz, Switzerland). The lake is extremely rich in suspended glacial flour in summer (glacier melting season). Measurements were taken from June 2004 to October 2005 from 1.2 {mu}m filtered samples. OC concentration remained extremely low throughout the year (below 1 mg C L{sup -1}). MBTH carbohydrate concentration was very low in the lake (0.06-0.43 mg C L{sup -1}) and in the two tributary rivers (0.06-0.25 mg C L{sup -1}). Lake carbohydrate concentration only correlated with phytoplanktonic biomass at the onset of the productivity period. The results suggest that differences in MBTH concentration may sometimes reflect differences in the nature of the carbohydrates rather than differences in carbon concentration. Extensive fibril formation was evidenced by transmission electron microscopy (TEM) observations. ROM concentration in the lake was also very low (0.1-0.2 mg C L{sup -1}). Significant variation in ROM riverine input was due to either annual occurrences (snow melting) or irregular episodes (floods). Melting snow was responsible for about 30% of the lake's annual ROM input. One box mass balance calculations showed that about 25% of ROM was lost within the lake. Evidence gleaned from TEM and STXM (scanning transmission X-ray microscopy) observations clearly indicates that this is mainly caused by ROM sedimentation after association with inorganic colloids.

  16. 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

  17. Simultaneous determination of pseudoephedrine hydrochloride and diphenhydramine hydrochloride in cough syrup by gas chromatography (GC).

    PubMed

    Raj, S V; Kapadia, S U; Argekar, A P

    1998-05-01

    A simple, rapid and precise gas chromatographic method has been developed for the simultaneous determination of pseudoephedrine hydrochloride and diphenhydramine hydrochloride in cough syrup, using a SS column of 10% OV 1 on chromosorb W-HP (80-100 mesh) and nitrogen as a carrier gas at a flow rate of 30 ml min(-1). The oven temperature was programmed at 135 degrees C for 1 min, with a rise of 10 degrees C min(-1) up to 250 degrees C (held for 5 min). The injector and detector port temperatures were maintained at 280 degrees C. Detection was carried out using Flame ionization detector. Guaphenesin was used as an internal standard. Results of assay and recovery studies were statistically evaluated for its accuracy and precision. PMID:18967146

  18. Comparative studies, synthesis, spectroscopic and characterization of N-methylisatin-3-Girard's T and P hydrazone complexes

    NASA Astrophysics Data System (ADS)

    Azhari, Shaker J.; Salah, Sabah; Farag, Rabei S.; Mostafa, Mohsen M.

    2015-02-01

    Different types of complexes derived from the reactions of N-methylisatin Girard's T hydrazone, N,N,N-trimethyl-2-[(2z)-2-(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxo-ethan ammonium chloride (MIGT) and N-methylisatin Girard's P hydrazone, 1-{2-(2z)-2-[(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxoethyl}pyridinium chloride (MIGP) with Fe3+, Al3+, Sb3+ and Sn2+ salts were synthesized. The isolated complexes were characterized by elemental analyses, molar conductivities, spectral (IR, UV-Vis., 1H NMR, mass), magnetic moments and thermal measurements. The values of conductance suggest that the complexes are conducting in polar solvents (EtOH, H2O and DMF). The IR spectra suggest that the ligands coordinate in a bidentate and/or tridentate manner via the carbonyl groups of both N-methylisatin and Girard's T and/or P and the (Cdbnd N) group. The solvents inside and outside the coordination sphere were determined by weight loss and TGA methods. The octahedral geometry of the complexes is confirmed using spectral, magnetic and DFT method from DMOL3 calculations. The ligands and their metal complexes were tested against different strains of bacteria and fungi.

  19. Synthesis and Screening of Human Monoamine Oxidase-A Inhibitor Effect of New 2-Pyrazoline and Hydrazone Derivatives.

    PubMed

    Evranos-Aksöz, Begüm; Baysal, İpek; Yabanoğlu-Çiftçi, Samiye; Djikic, Teodora; Yelekçi, Kemal; Uçar, Gülberk; Ertan, Rahmiye

    2015-10-01

    A group of 3,5-diaryl-2-pyrazoline and hydrazone derivatives was prepared via the reaction of various chalcones with hydrazide compounds in ethanol. Twenty original compounds were synthesized. Ten of these original compounds have a pyrazoline structure, nine of these original compounds have a hydrazone structure, and one of these original compounds has a chalcone structure. Structural elucidation of the compounds was performed by IR, (1)H NMR, (13)C NMR, mass spectral data, and elemental analyses. These compounds were tested for their inhibitory activities toward the A and B isoforms of human monoamine oxidase (MAO). Except for 3k and 6c, all compounds were found to be competitive, reversible, and selective inhibitors for either one of the isoforms (hMAO-A or MAO-B). Compounds 3k and 6c were found to be competitive, reversible, but non-selective MAO inhibitors. Compound 6h showed hMAO-B inhibitory activity whereas the others potently inhibited hMAO-A. Compound 5c showed higher selectivity than the standard drug moclobemide. According to the experimental K(i) values, compounds 6i, 6d, and 6a exhibited the highest inhibitory activity toward hMAO-A. The AutoDock 4.2 program was employed to perform automated molecular docking. The calculated results obtained computationally were in good agreement with the experimental values.

  20. Synthesis and spectral characterization of ternary complexes of oxovanadium(IV) containing some acid hydrazones and 2,2?-bipyridine

    NASA Astrophysics Data System (ADS)

    Sreeja, P. B.; Kurup, M. R. Prathapachandra

    2005-01-01

    An interesting series of heterocyclic base adducts of oxovanadium(IV) complexes have been synthesized by the reaction of vanadium(IV) oxide acetylacetonate with some hydrazones (H 2L) in the presence of a heterocyclic base 2,2'-bipyridine. The compounds were characterized by analytical and different physico-chemical techniques like IR, electron paramagnetic resonance (EPR) and UV-Vis spectral studies and magnetic studies. The EPR spectra indicate that the free electron is in the d xy orbital. The coordination geometry around oxovanadium(IV) in all complexes is octahedral, with one dibasic tridentate ligand L 2-, and one bidentate heterocyclic base. The IR spectra suggest that coordination takes place through azomethine nitrogen and enolate oxygen from the hydrazide moiety and phenolate oxygen. The pyridyl nitrogens of the hydrazones, H 2L 2 and H 2L 4 are not involved in the coordination. The molar conductivities show that all the complexes are non-electrolytes. All electronic transitions were assigned. All the compounds are paramagnetic. EPR studies of all compounds suggest axial symmetry. The calculated bonding parameters indicate that in-plane σ bonding is more covalent than in-plane π bonding.

  1. Synthesis and spectral characterization of ternary complexes of oxovanadium(IV) containing some acid hydrazones and 2,2'-bipyridine.

    PubMed

    Sreeja, P B; Kurup, M R Prathapachandra

    2005-01-01

    An interesting series of heterocyclic base adducts of oxovanadium(IV) complexes have been synthesized by the reaction of vanadium(IV) oxide acetylacetonate with some hydrazones (H(2)L) in the presence of a heterocyclic base 2,2'-bipyridine. The compounds were characterized by analytical and different physico-chemical techniques like IR, electron paramagnetic resonance (EPR) and UV-Vis spectral studies and magnetic studies. The EPR spectra indicate that the free electron is in the d(xy) orbital. The coordination geometry around oxovanadium(IV) in all complexes is octahedral, with one dibasic tridentate ligand L(2-), and one bidentate heterocyclic base. The IR spectra suggest that coordination takes place through azomethine nitrogen and enolate oxygen from the hydrazide moiety and phenolate oxygen. The pyridyl nitrogens of the hydrazones, H(2)L(2) and H(2)L(4) are not involved in the coordination. The molar conductivities show that all the complexes are non-electrolytes. All electronic transitions were assigned. All the compounds are paramagnetic. EPR studies of all compounds suggest axial symmetry. The calculated bonding parameters indicate that in-plane sigma bonding is more covalent than in-plane pi bonding. PMID:15556457

  2. Potential amoebicidal activity of hydrazone derivatives: synthesis, characterization, electrochemical behavior, theoretical study and evaluation of the biological activity.

    PubMed

    Toledano-Magaña, Yanis; García-Ramos, Juan Carlos; Navarro-Olivarria, Marisol; Flores-Alamo, Marcos; Manzanera-Estrada, Mayra; Ortiz-Frade, Luis; Galindo-Murillo, Rodrigo; Ruiz-Azuara, Lena; Meléndrez-Luevano, Ruth Ma; Cabrera-Vivas, Blanca M

    2015-01-01

    Four new hydrazones were synthesized by the condensation of the selected hydrazine and the appropriate nitrobenzaldehyde. A complete characterization was done employing 1H- and 13C-NMR, electrochemical techniques and theoretical studies. After the characterization and electrochemical analysis of each compound, amoebicidal activity was tested in vitro against the HM1:IMSS strain of Entamoeba histolytica. The results showed the influence of the nitrobenzene group and the hydrazone linkage on the amoebicidal activity. meta-Nitro substituted compound 2 presents a promising amoebicidal activity with an IC50 = 0.84 μM, which represents a 7-fold increase in cell growth inhibition potency with respect to metronidazole (IC50 = 6.3 μM). Compounds 1, 3, and 4 show decreased amoebicidal activity, with IC50 values of 7, 75 and 23 µM, respectively, as a function of the nitro group position on the aromatic ring. The observed differences in the biological activity could be explained not only by the redox potential of the molecules, but also by their capacity to participate in the formation of intra- and intermolecular hydrogen bonds. Redox potentials as well as the amoebicidal activity can be described with parameters obtained from the DFT analysis. PMID:26035095

  3. Synthesis, Biological Evaluation and 2D-QSAR Study of Halophenyl Bis-Hydrazones as Antimicrobial and Antitubercular Agents

    PubMed Central

    Abdel-Aziz, Hatem A.; Eldehna, Wagdy M.; Fares, Mohamed; Al-Rashood, Sara T. A.; Al-Rashood, Khalid A.; Abdel-Aziz, Marwa M.; Soliman, Dalia H.

    2015-01-01

    In continuation of our endeavor towards the development of potent and effective antimicrobial agents, three series of halophenyl bis-hydrazones (14a–n, 16a–d, 17a and 17b) were synthesized and evaluated for their potential antibacterial, antifungal and antimycobacterial activities. These efforts led to the identification of five molecules 14c, 14g, 16b, 17a and 17b (MIC range from 0.12 to 7.81 μg/mL) with broad antimicrobial activity against Mycobacterium tuberculosis; Aspergillus fumigates; Gram positive bacteria, Staphylococcus aureus, Streptococcus pneumonia, and Bacillis subtilis; and Gram negative bacteria, Salmonella typhimurium, Klebsiella pneumonia, and Escherichia coli. Three of the most active compounds, 16b, 17a and 17b, were also devoid of apparent cytotoxicity to lung cancer cell line A549. Amphotericin B and ciprofloxacin were used as references for antifungal and antibacterial screening, while isoniazid and pyrazinamide were used as references for antimycobacterial activity. Furthermore, three Quantitative Structure Activity Relationship (QSAR) models were built to explore the structural requirements controlling the different activities of the prepared bis-hydrazones. PMID:25903147

  4. Compound profiling and 3D-QSAR studies of hydrazone derivatives with activity against intracellular Trypanosoma cruzi.

    PubMed

    Costa, Lívia Bandeira; Cardoso, Marcos Veríssimo de Oliveira; de Oliveira Filho, Gevanio Bezerra; de Moraes Gomes, Paulo André Teixeira; Espíndola, José Wanderlan Pontes; de Jesus Silva, Thays Gabrielle; Torres, Pedro Henrique Monteiro; Silva Junior, Floriano Paes; Martin, Julio; de Figueiredo, Regina Célia Bressan Queiroz; Leite, Ana Cristina Lima

    2016-04-15

    Chagas disease is a tropical disease caused by the parasite Trypanosoma cruzi, which is endemic in Central and South America. Few treatments are available with effectiveness limited to the early (acute) stage of disease, significant toxicity and widespread drug resistance. In this work we report the outcome of a HTS-ready assay chemical library screen to identify novel, nontoxic, small-molecule inhibitors of T. cruzi. We have selected 50 compounds that possess hydrazone as a common group. The compounds were screened using recombinant T. cruzi (Tulahuen strain) expressing beta-galactosidase. A 3D quantitative structure-activity relationship (QSAR) analysis was performed using descriptors calculated from comparative molecular field analysis (CoMFA). Our findings show that of the fifty selected hydrazones, compounds LpQM-19, 28 and 31 displayed the highest activity against T. cruzi, leading to a selectivity index (SI) of 20-fold. The 3D-QSAR analysis indicates that a particular electrostatic arrangement, where electron-deficient atoms are aligned along the molecule main axis positively correlates with compound biological activity. These results provide new candidate molecules for the development of treatments against Chagas disease. PMID:26964673

  5. 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. PMID:27585105

  6. 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.

  7. Spectrophotometric methods for the simultaneous analysis of meclezine hydrochloride and pyridoxine hydrochloride in bulk drug and pharmaceutical formulations.

    PubMed

    Arayne, M Saeed; Sultana, Najma; Siddiqui, Farhan Ahmed; Zuberi, M Hashim; Mirza, Agha Zeeshan

    2007-04-01

    Three new spectrophotometric procedures for the simultaneous determination of pyridoxine hydrochloride and meclezine hydrochloride are described. The first method depends on the application of simultaneous equation to resolve the interference due to spectral overlapping. The analytical signals were measured at 231 and 220 nm. Calibration graphs were established for 1 to 20 microGmL(-1) for pyridoxine hydrochloride and 0.5 to 10 microGmL(-1) for meclezine hydrochloride in binary mixture. In the second method, the determination of pyridoxine hydrochloride and meclezine hydrochloride was performed by measuring the absorbances at 290 and 235 nm in the simple absorbance spectra of their mixture. In third method a yellowish orange complex of pyridoxine hydrochloride was formed with ferric chloride, which absorbs in the visible region with lambda(max) at 445 nm. Calibration curve of complex formation range was conducted in between 20 to 250 microGmL(-1). These methods were validated with respect to accuracy, precision, linearity, limit of detection and quantification. Regression analysis of Beer's plot showed good correlation in a general concentration range of 1 to 20 microGml(-1) with correlation coefficient (r = 0.9999 and 0.9999; CV < 0.858) for pyridoxine hydrochloride, whereas meclezine hydrochloride concentration range 0.5 to 10 microGmL(-1) with correlation coefficient (r = 0.9998 and 0.9998; CV < 0.826). These methods can be readily applied, without any interference from the excipients. The suggested procedures were successfully applied to the determination of these compounds in synthetic mixtures and in pharmaceutical preparations, with high percentage of recovery, good accuracy and precision. PMID:17416572

  8. 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.

  9. An Efficient Protocol for the Oxidative Hydrolysis of Ketone SAMP Hydrazones Employing SeO(2) and H(2)O(2) under Buffered (pH 7) Conditions.

    PubMed

    Smith, Amos B; Liu, Zhuqing; Simov, Vladimir

    2009-06-01

    An effective oxidative protocol for the liberation of ketones from SAMP hydrazones employing peroxyselenous acid under aqueous buffered conditions (pH 7) has been developed. The procedure proceeds without epimerization of adjacent stereocenters or dehydration, respectively, in representative SAMP alkylation and aldol reaction adducts. PMID:20657727

  10. CATALYST-FREE REACTIONS UNDER SOLVENT-FEE CONDITIONS: MICROWAVE-ASSISTED SYNTHESIS OF HETEROCYCLIC HYDRAZONES BELOW THE MELTING POINT OF NEAT REACTANTS: JOURNAL ARTICLE

    EPA Science Inventory

    NRMRL-CIN-1437 Jeselnik, M., Varma*, R.S., Polanc, S., and Kocevar, M. Catalyst-free Reactions under Solvent-fee Conditions: Microwave-assisted Synthesis of Heterocyclic Hydrazones below the Melting Point of Neat Reactants. Published in: Chemical Communications 18:1716-1717 (200...

  11. Synthesis and biological activity of hydrazide hydrazones and their corresponding 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Various new 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles (11-20) were prepared by the reaction of aryl substituted hydrazones of 4-fluorobenzoic acid hydrazide (1-10) with acetic anhydride. The structures of the newly synthesized compounds 11-20, were confirmed by UV, IR and 1H NMR spec...

  12. The electrochemistry and determination of Ligustrazine hydrochloride.

    PubMed

    Sun, Ziyi; Zheng, Xiaofeng; Hoshi, Tomonori; Kashiwagi, Yoshitomo; Anzai, Jun-ichi; Li, Genxi

    2004-10-01

    Ligustrazine is one of the active ingredients contained in Ligusticum chuanxiong Hort. (Umbelliferae), which is widely used in traditional Chinese medicine for the treatment of cardiovascular problems. In this work, the electrochemistry of Ligustrazine hydrochloride (LZC) and its determination are investigated. The detection limit is estimated to be 8.0 x 10(-8) M, with three linear ranges from 1.0 x 10(-6) to 1.0 x 10(-4) M, 1.0 x 10(-4) to 5.0 x 10(-4) M, and 6.5 x 10(-4) to 1.6 x 10(-3) M. The method has been proved to be highly sensitive, selective, and stable, and has been successfully applied to determining LZC in LZC injections.

  13. 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...

  14. 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...

  15. 21 CFR 522.1335 - Medetomidine hydrochloride injection.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... solution contains 1.0 milligram of medetomidine hydrochloride. (b) Sponsor. See 052483 in § 510.600(c) of... diseases, dogs in shock, dogs which are severly debilitated, or dogs which are stressed due to extreme...

  16. Piperonal ciprofloxacin hydrazone induces growth arrest and apoptosis of human hepatocarcinoma SMMC-7721 cells

    PubMed Central

    Shi, Zhen-yu; Li, Yong-qiang; Kang, Yu-hua; Hu, Guo-qiang; Huang-Fu, Chao-shen; Deng, Jin-bo; Liu, Bin

    2012-01-01

    Aim: To investigate the cytotoxic effects of piperonal ciprofloxacin hydrazone (QNT4), a novel antibacterial fluoroquinolone derivative, against human hepatocarcinoma SMMC-7721 cells. Methods: Human hepatocarcinoma cells (SMMC-7721), human breast adenocarcinoma cells (MCF-7) and human colon adenocarcinoma cells (HCT-8) were tested. The effects of QNT4 on cell proliferation were examined using MTT assay. Cell apoptosis was determined using Hoechst 33258 fluorescence staining, TUNEL assay and agarose gel electrophoresis. The topoisomerase II activity was measured using agarose gel electrophoresis with the DNA plasmid pBR322 as the substrate. Mitochondrial membrane potential (Δψm) was measured using a high content screening imaging system. Protein expression of caspase-9, caspase-8, caspase-3, p53, Bcl-2, Bax, and cytochrome c was detected with Western blot analysis. Results: Treatment with QNT4 (0.625–10 μmol/L) potently inhibited the proliferation of the cancer cells in time- and dose-dependent manners (the IC50 value at 24 h in SMMC-7721 cells, MCF-7 cells and HCT-8 cells was 2.956±0.024, 3.710±0.027, and 3.694±0.030 μmol/L, respectively). Treatment of SMMC-7721 cells with QNT4 (0.2146, 2.964, and 4.600 μmol/L) for 24 h dose-dependently increased the percentage of apoptotic cells, elicited characteristic DNA “ladder” bands, and decreased the mitochondrial membrane potential. QNT4 dose-dependently increased topoisomerase II-mediated DNA breaks while inhibiting DNA relegation, thus keeping the DNA in fragments. Treatment of SMMC-7721 cells with QNT4 significantly increased cytochrome c in the cytosol, and decreased cytochrome c in the mitochondrial compartment. QNT4 (3–7.39 μmol/L) significantly increased the protein expression of p53, Bax, caspase-9, caspase-3, and the cleaved activated forms of caspase-9 and caspase-3 in SMMC-7721 cells. In contrast, the expression of Bcl-2 was decreased, while caspase-8 had no significant change. Conclusion

  17. 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…

  18. Structure–activity studies in the development of a hydrazone based inhibitor of adipose-triglyceride lipase (ATGL)

    PubMed Central

    Mayer, Nicole; Schweiger, Martina; Melcher, Michaela-Christina; Fledelius, Christian; Zechner, Rudolf; Zimmermann, Robert; Breinbauer, Rolf

    2015-01-01

    Adipose triglyceride lipase (ATGL) catalyzes the degradation of cellular triacylglycerol stores and strongly determines the concentration of circulating fatty acids (FAs). High serum FA levels are causally linked to the development of insulin resistance and impaired glucose tolerance, which eventually progresses to overt type 2 diabetes. ATGL-specific inhibitors could be used to lower circulating FAs, which can counteract the development of insulin resistance. In this article, we report about structure–activity relationship (SAR) studies of small molecule inhibitors of ATGL based on a hydrazone chemotype. The SAR indicated that the binding pocket of ATGL requests rather linear compounds without bulky substituents. The best inhibitor showed an IC50 = 10 μM in an assay with COS7-cell lysate overexpressing murine ATGL. PMID:25778769

  19. New series of aromatic/ five-membered heteroaromatic butanesulfonyl hydrazones as potent biological agents: Synthesis, physicochemical and electronic properties

    NASA Astrophysics Data System (ADS)

    Hamurcu, Fatma; Mamaş, Serhat; Ozdemir, Ummuhan Ozmen; Gündüzalp, Ayla Balaban; Senturk, Ozan Sanlı

    2016-08-01

    The aromatic/five-membered heteroaromatic butanesulfonylhydrazone derivatives; 5-bromosalicylaldehydebutanesulfonylhydrazone(1), 2-hydroxy-1-naphthaldehydebutane sulfonylhydrazone(2), indole-3-carboxaldehydebutanesulfonylhydrazone (3), 2-acetylfuran- carboxyaldehydebutanesulfonylhydrazone(4), 2-acetylthiophenecarboxyaldehydebutane- sulfonylhydrazone(5) and 2-acetyl-5-chlorothiophenecarboxyaldehydebutanesulfonyl hydrazone (6) were synthesized by the reaction of butane sulfonic acid hydrazide with aldehydes/ketones and characterized by using elemental analysis, 1H NMR, 13C NMR and FT-IR technique. Their geometric parameters and electronic properties consist of global reactivity descriptors were also determined by theoretical methods. The electrochemical behavior of the butanesulfonylhydrazones were investigated by using cyclic voltammetry (CV), controlled potential electrolysis and chronoamperometry (CA) techniques. The number of electrons transferred (n), diffusion coefficient (D) and standard heterogeneous rate constants (ks) were determined by electrochemical methods.

  20. Semisynthesis and quantitative structure-activity relationship (QSAR) study of some cholesterol-based hydrazone derivatives as insecticidal agents.

    PubMed

    Yang, Chun; Shao, Yonghua; Zhi, Xiaoyan; Huan, Qu; Yu, Xiang; Yao, Xiaojun; Xu, Hui

    2013-09-01

    In continuation of our program aimed at the discovery and development of natural-product-based insecticidal agents, four series of novel cholesterol-based hydrazone derivatives were synthesized, and their insecticidal activity was tested against the pre-third-instar larvae of oriental armyworm, Mythimna separata (Walker) in vivo at 1mg/mL. All the derivatives showed the better insecticidal activity than their precursor cholesterol. Quantitative structure-activity relationship (QSAR) model demonstrated that six descriptors such as RDF085v, Mor06u, Mor11u, Dv, HATS0v and H-046, are likely to influence the insecticidal activity of these compounds. Among them, two important ones are the Mor06u and RDF085v.

  1. Synthesis of novel hydrazone and azole functionalized pyrazolo[3,4-b]pyridine derivatives as promising anticancer agents.

    PubMed

    Nagender, P; Naresh Kumar, R; Malla Reddy, G; Krishna Swaroop, D; Poornachandra, Y; Ganesh Kumar, C; Narsaiah, B

    2016-09-15

    A series of novel pyrazolo[3,4-b]pyridine based target compounds were synthesized starting from the key intermediate ethyl 2-(3-amino-6-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-1-yl)acetate 5 on reaction with hydrazine hydrate followed by reaction with different aldehydes, acid chlorides and isothiocyanates to form hydrazones 7, oxadiazoles 8, 1,2,4 triazoles 10 and thiadiazoles 11 respectively in high yield. All the final compounds were screened for anticancer activity against four human cancer cell lines. Among them, 1,2,4 triazole derivatives showed promising activity and compound 10d is identified as a lead molecule. PMID:27528432

  2. Synthesis, molecular structure and computational study of (Z)-2-((E)-4-nitrobenzylidene)hydrazone)-1,2-diphenylethan-1-one

    NASA Astrophysics Data System (ADS)

    Elmacı, Gökhan; Aktan, Ebru; Seferoğlu, Nurgül; Hökelek, Tuncer; Seferoğlu, Zeynel

    2015-11-01

    A new benzilmonohydrazone, (Z)-2-((E)-4-nitrobenzylidene)hydrazone)-1,2-diphenylethan-1-one (BMH) has been synthesized for the first time. It was characterized by UV-vis, FT-IR, FT-Raman, 1H/13C NMR and mass spectrometry techniques. Molecular structure of the title compound was determined by single crystal X-ray diffraction study. In addition, molecular structure of BMH was determined by single crystal X-ray diffraction technique and found that the compound crystallizes in triclinic, space group P-1. Furthermore, chemical calculations employing density functional theory (DFT) method were performed to study the structural and spectroscopic properties of BMH, and the results were compared with the experimental findings.

  3. Stereoselective Alkylations of Chiral Nitro Imine and Nitro Hydrazone Dianions. Synthesis of Enantiomerically Enriched 3-Substituted 1-Nitrocyclohexenes†

    PubMed Central

    Denmark, Scott E.; Ares, Jeffrey J.

    2011-01-01

    Dianions of chiral nitro imines (generated by a combination of LDA and s-BuLi) underwent diastereoselective alkylation with methyl, butyl, isopropyl, allyl and methallyl iodides. In contrast to the behavior of simple metalloenamines, the most selective auxiliary contained no coordinating groups, but did possess a large steric difference between the two substituents. The yield and selectivity of the alkylations were improved by the addition of HMPA or DMPU. The use of (S)-1-naphthylethylamine as the auxiliary afforded the R absolute configuration of the alkylation products. This stereochemical outcome could be rationalized by simple steric approach controlled alkylation in a conformationally fixed, internally coordinated dianion. A SAMP nitro hydrazone gave poorer yields and selectivities. PMID:18855478

  4. On the roles of close shell interactions in the structure of acyl-substituted hydrazones: An experimental and theoretical approach.

    PubMed

    Saeed, Aamer; Ifzan Arshad, M; Bolte, Michael; Fantoni, Adolfo C; Delgado Espinoza, Zuly Y; Erben, Mauricio F

    2016-03-15

    The 2-(phenyl-hydrazono)-succinic acid dimethyl ester compound was synthesized by reacting phenylhydrazine with dimethylacetylene dicarboxylate at room temperature and characterized by elemental analysis, infrared, Raman, (1)H and (13)C NMR spectroscopies and mass spectrometry. Its solid state structure was determined by X-ray diffraction methods. The X-ray structure determination corroborates that the molecule is present in the crystal as the hydrazone tautomer, probably favored by a strong intramolecular N-H···O=C hydrogen bond occurring between the carbonyl (-C=O) and the hydrazone -C=N-NH- groups. A substantial fragment of the molecular skeleton is planar due to an extended π-bonding delocalization. The topological analysis of the electron densities (Atom in Molecule, AIM) allows characterization of intramolecular N-H···O interaction, that can be classified as a resonant assisted hydrogen bond (RAHB). Moreover, the Natural Bond Orbital population analysis confirms that a strong hyperconjugative lpO1→σ*(N2-H) remote interaction between the C2=O1 and N2-H groups takes place. Periodic system electron density and topological analysis have been applied to characterize the intermolecular interactions in the crystal. Weak intermolecular interactions determine the crystal packing, and the prevalence of non-directional dispersive contributions are inferred on topological grounds. The IR spectrum of the crystalline compound was investigated by means of density functional theory calculations carried out with periodic boundary conditions on the crystal, showing excellent agreement between theory and the experiments. The vibrational assignment is complemented with the analysis of the Raman spectrum. PMID:26761413

  5. On the roles of close shell interactions in the structure of acyl-substituted hydrazones: An experimental and theoretical approach

    NASA Astrophysics Data System (ADS)

    Saeed, Aamer; Ifzan Arshad, M.; Bolte, Michael; Fantoni, Adolfo C.; Delgado Espinoza, Zuly Y.; Erben, Mauricio F.

    2016-03-01

    The 2-(phenyl-hydrazono)-succinic acid dimethyl ester compound was synthesized by reacting phenylhydrazine with dimethylacetylene dicarboxylate at room temperature and characterized by elemental analysis, infrared, Raman, 1H and 13C NMR spectroscopies and mass spectrometry. Its solid state structure was determined by X-ray diffraction methods. The X-ray structure determination corroborates that the molecule is present in the crystal as the hydrazone tautomer, probably favored by a strong intramolecular N-H···Odbnd C hydrogen bond occurring between the carbonyl (-Cdbnd O) and the hydrazone -Cdbnd N-NH- groups. A substantial fragment of the molecular skeleton is planar due to an extended π-bonding delocalization. The topological analysis of the electron densities (Atom in Molecule, AIM) allows characterization of intramolecular N-H···O interaction, that can be classified as a resonant assisted hydrogen bond (RAHB). Moreover, the Natural Bond Orbital population analysis confirms that a strong hyperconjugative lpO1 → σ*(N2-H) remote interaction between the C2dbnd O1 and N2-H groups takes place. Periodic system electron density and topological analysis have been applied to characterize the intermolecular interactions in the crystal. Weak intermolecular interactions determine the crystal packing, and the prevalence of non-directional dispersive contributions are inferred on topological grounds. The IR spectrum of the crystalline compound was investigated by means of density functional theory calculations carried out with periodic boundary conditions on the crystal, showing excellent agreement between theory and the experiments. The vibrational assignment is complemented with the analysis of the Raman spectrum.

  6. Synthesis of novel flavone hydrazones: in-vitro evaluation of α-glucosidase inhibition, QSAR analysis and docking studies.

    PubMed

    Imran, Syahrul; Taha, Muhammad; Ismail, Nor Hadiani; Kashif, Syed Muhammad; Rahim, Fazal; Jamil, Waqas; Hariono, Maywan; Yusuf, Muhammad; Wahab, Habibah

    2015-11-13

    Thirty derivatives of flavone hydrazone (5-34) had been synthesized through a five-step reaction and screened for their α-glucosidase inhibition activity. Chalcone 1 was synthesized through aldol condensation then subjected through oxidative cyclization, esterification, and condensation reaction to afford the final products. The result for baker's yeast α-glucosidase (EC 3.2.1.20) inhibition assay showed that all compounds are active with reference to the IC50 value of the acarbose (standard drug) except for compound 3. Increase in activity observed for compounds 2 to 34 clearly highlights the importance of flavone, hydrazide and hydrazone linkage in suppressing the activity of α-glucosidase. Additional functional group on N-benzylidene moiety further enhances the activity significantly. Compound 5 (15.4 ± 0.22 μM), a 2,4,6-trihydroxy substituted compound, is the most active compound in the series. Other compounds which were found to be active are those having chlorine, fluorine, and nitro substituents. Compounds with methoxy, pyridine, and methyl substituents are weakly active. Further studies showed that they are not active in inhibiting histone deacetylase activity and do not possess any cytotoxic properties. QSAR model was being developed to further identify the structural requirements contributing to the activity. Using Discovery Studio (DS) 2.5, various 2D descriptors were being used to develop the model. The QSAR model is able to predict the pIC50 and could be used as a prediction tool for compounds having the same skeletal framework. Molecular docking was done for all compounds using homology model of α-glucosidase to identify important binding modes responsible for inhibition activity. PMID:26491979

  7. Bevantolol hydrochloride--preclinical pharmacologic profile.

    PubMed

    Kaplan, H R

    1986-03-01

    Bevantolol hydrochloride, a beta adrenoceptor antagonist, can be categorized using conventional schemes as being cardioselective, devoid of intrinsic sympathomimetic activity and having weak membrane-stabilizing and local anesthetic properties. The cardioselectivity of bevantolol was conferred by the incorporation of a 3,4-dimethoxyphenyl moiety into the terminal amino portion of the molecule. This portion of the molecule also appears to account for bevantolol's in vitro binding affinity at alpha-adrenoceptor sites; the in vivo significance of which remains unclear. In the various cardiovascular disease-state models, bevantolol's profile differed from that of propranolol, i.e., there was no initial pressor response in spontaneously hypertensive or renal hypertensive rats. In a myocardial ischemia model, bevantolol, unlike propranolol, increased contractile function in the ischemic myocardium. A ring hydroxylated urinary metabolite, which occurred only in trace amounts in human urine, had an interesting profile when studied in animals at pharmacologic doses. It ranked high in cardioselectivity (like bevantolol), but unlike bevantolol showed significant intrinsic beta sympathomimetic activity. The clinical significance of this metabolite, if any, remains to be established. Collectively the preclinical profile of bevantolol showed it to have an interesting profile for a beta adrenoceptor antagonist in a variety of pharmacologic test systems.

  8. 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.

  9. Nalbuphine hydrochloride dependence in anabolic steroid users.

    PubMed

    Wines, J D; Gruber, A J; Pope, H G; Lukas, S E

    1999-01-01

    Nalbuphine hydrochloride, a nonscheduled opioid agonist/antagonist analgesic, is currently approved for the treatment of pain. Recently, nalbuphine dependence was reported in three anabolic steroid users in Britain. To further document this phenomenon, we conducted interviews on eleven subjects who reported nalbuphine use. Eight subjects were clinically dependent on nalbuphine, and seven of the subjects who were asked about tolerance and withdrawal with nalbuphine acknowledged these symptoms. Eight subjects, who had never used drugs intravenously before, reported using nalbuphine by this route. Nalbuphine-related morbidity was extensive and included medical complications and psychiatric symptoms. Nalbuphine users also exhibited a high rate of comorbid Axis I disorders, including other substance misuse. Virtually all subjects described widespread nalbuphine use in the gymnasiums they frequented. These observations, together with the recent increase in nalbuphine-related articles in the lay press, suggest that nalbuphine may represent a new drug of abuse among athletes, especially those using anabolic steroids, and that nalbuphine's scheduling status may need to be re-evaluated.

  10. Amantadine hydrochloride pharmacokinetics in hemodialysis patients.

    PubMed

    Soung, L S; Ing, T S; Daugirdas, J T; Wu, M J; Gandhi, V C; Ivanovich, P T; Hano, J E; Viol, G W

    1980-07-01

    To study the fate of amantadine hydrochloride in patients with renal failure, we gave 100 mg orally to 12 such patients immediately after hemodialysis. Plasma levels did not decrease between 24 and 44 hours after drug ingestion, suggesting an extremely poor total body clearance. Apparent volume of distribution was 5.1 +/- 0.2 (SEM) L/kg of body weight. Between 44 and 48 hours, as a result of 4 hours of hemodialysis, the mean plasma drug level decreased from 268 to 225 ng/mL (P less than 0.001). Dialyzer clearance was 67.0 +/- 3.9 mL of plasma per minute. The total quantity of drug removed by the dialysis treatment, however, was only 3.9 +/- 0.25 mg. The average half-life of amantadine in eight patients studied while receiving maintenance hemodialysis was 24.3 +/- 2.4 h of dialysis administered over approximately 13 days. Plasma half-life in six nonuremic control subjects was 12.2 +/- 1.6 h. Amantadine is poorly excreted in dialysis patients and has a large volume of distribution. The amount removed by a single dialysis is only a small fraction of the total body store. PMID:7396313

  11. 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.

  12. Immobilizing wild mountain lions (Felis concolor) with ketamine hydrochloride and xylazine hydrochloride.

    PubMed

    Logan, K A; Thorne, E T; Irwin, L L; Skinner, R

    1986-01-01

    A mixture of 120 mg ketamine hydrochloride (KHCL)/20 mg xylazine hydrochloride (XHCL)/ml was used to immobilize 37 wild mountain lions (Felis concolor) 46 times. Observations were recorded during 37 trials that included kittens, adult females, and adult males. Dosages were based on 11 mg KHCL and 1.8 mg XHCL/kg estimated body weight. Actual doses for 24 lions requiring a single injection for immobilization ranged from 4.7-15.8 mg KHCL/kg and 0.8-2.6 mg XHCL/kg. Induction, duration, and recovery times did not differ (P greater than 0.05) between the sex and age classes. Two kittens were overdosed with the drug combination, but the effects were not life threatening. Eleven other lions, nine of which were initially underdosed, required additional injections of the drug combination for safe handling. Immobilization was characterized initially by semi-consciousness, open eyelids, pupillary dilation, and muscle rigidity. Later, most lions appeared unconscious, muscles relaxed, and breathing slowed considerably. No convulsions or hypersalivation occurred. The KHCL/XHCL mixture given at approximately 11 mg KHCL and 1.8 mg XHCL/kg body weight proved useful for immobilizing wild mountain lions for research purposes. Suggestions for case of immobilized cats are included. PMID:3951066

  13. 40 CFR 721.6196 - Hydrochloride salt of a fatty polyalkkylene polyamine (generic).

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 40 Protection of Environment 31 2011-07-01 2011-07-01 false Hydrochloride salt of a fatty... New Uses for Specific Chemical Substances § 721.6196 Hydrochloride salt of a fatty polyalkkylene... substance identified generically as Hydrochloride salt of a fatty polyalkkylene polyamine (PMN P-99-0618)...

  14. 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.

  15. Spectroscopic and X-ray crystallographic evidence for electrostatic effects in 4-substituted cyclohexanone-derived hydrazones, imines, and corresponding salts.

    PubMed

    Dibble, David J; Ziller, Joseph W; Woerpel, K A

    2011-10-01

    The axial conformer of several 4-substituted cyclohexanone hydrazone salts was found to predominate in solution. Changes in the charge of the molecule and the polarity of the solvent led to changes in the conformational preference of each molecule that were consistent with electrostatic stabilization of the axial conformer. (1)H NMR spectroscopic analysis was utilized to determine the structure of cyclohexanone-derived substrates by comparison to conformationally restricted trans-decalone derivatives and computational models. X-ray crystallography demonstrated that the axial configuration of a pendant benzyloxy group is the preferred conformation of an iminium ion in the solid state. The structure of a neutral hydrazone was also determined to favor the axial configuration for a pendant benzyloxy group in the solid state.

  16. 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.

  17. 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

  18. 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. PMID:27610155

  19. 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.

  20. 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.

  1. Synthesis of o-(Dimethylamino)aryl Ketones, Acridones, Acridinium Salts, and 1H-Indazoles by the Reaction of Hydrazones and Arynes

    PubMed Central

    Dubrovskiy, Anton V.; Larock, Richard C.

    2012-01-01

    A novel, efficient route to biologically and pharmaceutically important o-(dimethylamino)aryl ketones, acridones, acridinium salts, and 1H-indazoles has been developed starting from readily available hydrazones of aldehydes and o-(trimethylsilyl)aryl triflates. The reaction proceeds through arynes under mild conditions, tolerates a wide range of functional groups, and provides the final products in good to excellent yields. PMID:23206164

  2. Synthesis, structure and study of azo-hydrazone tautomeric equilibrium of 1,3-dimethyl-5-(arylazo)-6-amino-uracil derivatives

    NASA Astrophysics Data System (ADS)

    Debnath, Diptanu; Roy, Subhadip; Li, Bing-Han; Lin, Chia-Her; Misra, Tarun Kumar

    2015-04-01

    Azo dyes, 1,3-dimethyl-5-(arylazo)-6-aminouracil (aryl = -C6H5 (1), -p-CH3C6H4 (2), -p-ClC6H4 (3), -p-NO2C6H4 (4)) were prepared and characterized by UV-vis, FT-IR, 1H NMR, 13C NMR spectroscopic techniques and single crystal X-ray crystallographic analysis. In the light of spectroscopic analysis it evidences that of the tautomeric forms, the azo-enamine-keto (A) form is the predominant form in the solid state whereas in different solvents it is the hydrazone-imine-keto (B) form. The study also reveals that the hydrazone-imine-keto (B) form exists in an equilibrium mixture with its anionic form in various organic solvents. The solvatochromic and photophysical properties of the dyes in various solvents with different hydrogen bonding parameter were investigated. The dyes exhibit positive solvatochromic property on moving from polar protic to polar aprotic solvents. They are fluorescent active molecules and exhibit high intense fluorescent peak in some solvents like DMSO and DMF. It has been demonstrated that the anionic form of the hydrazone-imine form is responsible for the high intense fluorescent peak. In addition, the acid-base equilibrium in between neutral and anionic form of hydrazone-imine form in buffer solution of varying pH was investigated and evaluated the pKa values of the dyes by making the use of UV-vis spectroscopic methods. The determined acid dissociation constant (pKa) values increase according to the sequence of 2 > 1 > 3 > 4.

  3. Synthesis, structure and study of azo-hydrazone tautomeric equilibrium of 1,3-dimethyl-5-(arylazo)-6-amino-uracil derivatives.

    PubMed

    Debnath, Diptanu; Roy, Subhadip; Li, Bing-Han; Lin, Chia-Her; Misra, Tarun Kumar

    2015-04-01

    Azo dyes, 1,3-dimethyl-5-(arylazo)-6-aminouracil (aryl=-C6H5 (1), -p-CH3C6H4 (2), -p-ClC6H4 (3), -p-NO2C6H4 (4)) were prepared and characterized by UV-vis, FT-IR, 1H NMR, 13C NMR spectroscopic techniques and single crystal X-ray crystallographic analysis. In the light of spectroscopic analysis it evidences that of the tautomeric forms, the azo-enamine-keto (A) form is the predominant form in the solid state whereas in different solvents it is the hydrazone-imine-keto (B) form. The study also reveals that the hydrazone-imine-keto (B) form exists in an equilibrium mixture with its anionic form in various organic solvents. The solvatochromic and photophysical properties of the dyes in various solvents with different hydrogen bonding parameter were investigated. The dyes exhibit positive solvatochromic property on moving from polar protic to polar aprotic solvents. They are fluorescent active molecules and exhibit high intense fluorescent peak in some solvents like DMSO and DMF. It has been demonstrated that the anionic form of the hydrazone-imine form is responsible for the high intense fluorescent peak. In addition, the acid-base equilibrium in between neutral and anionic form of hydrazone-imine form in buffer solution of varying pH was investigated and evaluated the pKa values of the dyes by making the use of UV-vis spectroscopic methods. The determined acid dissociation constant (pKa) values increase according to the sequence of 2>1>3>4.

  4. Structural and vibrational study of 8-hydroxyquinoline-2-carboxaldehyde isonicotinoyl hydrazone - A potential metal-protein attenuating compound (MPAC) for the treatment of Alzheimer's disease

    NASA Astrophysics Data System (ADS)

    de Freitas, Leonardo Viana; da Silva, Cecilia C. P.; Ellena, Javier; Costa, Luiz Antônio Sodré; Rey, Nicolás A.

    2013-12-01

    A comprehensive structural and vibrational study of the potential metal-protein attenuating compound 8-hydroxyquinoline-2-carboxaldehyde isonicotinoyl hydrazone is reported. X-ray diffraction data, as well as FT-IR and Raman frequencies, were compared with the respective theoretical values obtained from DFT calculations. Theory agrees well with experiment. In this context, an attempt of total assignment concerning the FT-IR and Raman spectra of the title compound was performed, shedding new light on previous partial assignments published elsewhere.

  5. Synthesis and Biological Evaluation of New Hydrazone Derivatives of Quinoline and Their Cu(II) and Zn(II) Complexes against Mycobacterium tuberculosis

    PubMed Central

    Mandewale, Mustapha C.; Thorat, Bapu; Shelke, Dnyaneshwar; Yamgar, Ramesh

    2015-01-01

    A new series of quinoline hydrazone derivatives and their metal complexes have been synthesized and their biological properties have been evaluated against Mycobacterium tuberculosis (H37 RV strain). Most of the newly synthesized compounds displayed 100% inhibitory activity at a concentration of 6.25–25 μg/mL, against Mycobacterium tuberculosis. Fluorescence properties of all the synthesized compounds have been studied. PMID:26759537

  6. Syntheses, spectroscopic characterization and thermal behavior on novel binuclear transition metal complexes of hydrazones derived from 4,6-diacetylresorcinol and oxalyldihydrazine.

    PubMed

    Emara, Adel A A; El-Sayed, Badr A; Ahmed, El-Sayed A E

    2008-03-01

    4,6-Diacetylresorcinol (DAR) serves as precursor for the formation of different hydrazone ligands, which are di-, tetra- or hexa-basic with two symmetrical sets of O(2)N tridentate, O(2)N(2) tetradentate or O(4)N(2) hexadentate chelating sites. The condensation of 4,6-diacetylresorcinol (DAR) with oxalyldihydrazine (ODH), in the molar ratio 1:1 and 1:2, yields the corresponding hydrazone, H(6)L(a) and H(4)L(b), ligands, respectively. The structures of these ligands were elucidated by elemental analyses and IR, mass, (1)H NMR and UV-vis spectra. Reactions of the hydrazone ligands with cobalt(II), nickel(II), copper(II), zinc(II), cadmium(II), iron(III) and chromium(III) ions in 1:2 molar ratio afforded the corresponding transition metal complexes. A variety of binuclear transition metal complexes were obtained in its di-, tetra- or hexa-deprotonated forms. The structures of the newly prepared complexes were identified by elemental analyses and IR, UV-vis, mass, (1)H NMR and ESR spectra, as well as, magnetic susceptibility measurements and thermal gravimetric analysis (TGA). The bonding sites are the azomethine and CO oxygen atoms in either keto or enol forms and amino nitrogen atoms, and phenolic oxygen atoms. The metal complexes exhibit different geometrical structures such as tetrahedral and octahedral arrangements. PMID:17627871

  7. Syntheses, spectroscopic characterization and thermal behavior on novel binuclear transition metal complexes of hydrazones derived from 4,6-diacetylresorcinol and oxalyldihydrazine

    NASA Astrophysics Data System (ADS)

    Emara, Adel A. A.; El-Sayed, Badr A.; Ahmed, El-Sayed A. E.

    2008-03-01

    4,6-Diacetylresorcinol (DAR) serves as precursor for the formation of different hydrazone ligands, which are di-, tetra- or hexa-basic with two symmetrical sets of O 2N tridentate, O 2N 2 tetradentate or O 4N 2 hexadentate chelating sites. The condensation of 4,6-diacetylresorcinol (DAR) with oxalyldihydrazine (ODH), in the molar ratio 1:1 and 1:2, yields the corresponding hydrazone, H 6L a and H 4L b, ligands, respectively. The structures of these ligands were elucidated by elemental analyses and IR, mass, 1H NMR and UV-vis spectra. Reactions of the hydrazone ligands with cobalt(II), nickel(II), copper(II), zinc(II), cadmium(II), iron(III) and chromium(III) ions in 1:2 molar ratio afforded the corresponding transition metal complexes. A variety of binuclear transition metal complexes were obtained in its di-, tetra- or hexa-deprotonated forms. The structures of the newly prepared complexes were identified by elemental analyses and IR, UV-vis, mass, 1H NMR and ESR spectra, as well as, magnetic susceptibility measurements and thermal gravimetric analysis (TGA). The bonding sites are the azomethine and C dbnd O oxygen atoms in either keto or enol forms and amino nitrogen atoms, and phenolic oxygen atoms. The metal complexes exhibit different geometrical structures such as tetrahedral and octahedral arrangements.

  8. Medium effects on fluorescence of ciprofloxacin hydrochloride

    NASA Astrophysics Data System (ADS)

    Yang, Rui; Fu, Yan; Li, Long-Di; Liu, Jia-Ming

    2003-10-01

    The medium (pH, organic solvents, cyclodextrin (CD) or surfactants) effects on the fluorescence of ciprofloxacin hydrochloride (CPFX·HCl) were studied in detail. It is found that the three acid constants of ciprofloxacin (CPFX) are near to each other. Therefore the relation curve between pH and fluorescence intensity has no strident change and keeps relative stable in the pH range of 2-7. When pH was in the range of 5.5-6.0, the fluorescence intensity of CPFX reached the max. The kind and amount of organic solvent added to the luminescent system have various effects. Ethanol quenched fluorescence and the fluorescence excitation wavelength is red shift at first and then blue shift. Acetone has complicated effects on the fluorescence properties of CPFX·HCl solution. The experiment result shows that acetone is really a quencher when its volume content in the system is from 0 to 20%, but when its content is 90%, the signal intensity is unexpectedly one and a half times as much as that of no acetone. This means that there is a strong interaction between the acetone and CPFX; CPFX·H + could be included into the γ-CD but the capping effect is not notable. The effect of cationic surfactant cetyltrimethylammonium bromide and non-ionic surfactant TX-100 and TX-80 on CPFX fluorescence was unimpressive, but the anionic surfactant's effect is aberrant. The fluorescence intensity of CPFX·HCl solution experiences three stages of increasing, decreasing and increasing in turn, as sodium dodecyl sulfate is adding gradually. But for sodium lauryl sulfonate, there are only two stages of decreasing and increasing with the concentration increasing. It is problematic to illustrate clearly the effect mechanism of acetone and anionic surfactant at present. Undoubtedly, the experimental results in this paper should be useful in practice works and the research is worth studying still further.

  9. PREDICTIVE PHARMACOKINETICS OF TRAMADOL HYDROCHLORIDE FLOATING TABLETS.

    PubMed

    Wang, Jianming; Zhang, Yanzhen; Guo, Zhiling; Tao, Qingwen; Wang, Yongjun; Zhou, Wei; Ma, Xiao; Li, Zhihong

    2016-01-01

    The purpose of this study was to propose the effectiveness of convolution approach to predict pharmacokinetics of tramadol hydrochloride floating tablets, prepared by using various ratios of carbopol, HPMC K100M, and Hibiscus rosa Sinensis as excipient. The in vitro dissolution test was conducted using paddle method in 900 mL of HCl buffer with pH 1.2 to simulate the gastric condition. The stirring speed of paddles was set at 70 rpm. Temperature of dissolution medium was adjusted at 37 ± 5 °C. At predetermined time points, 5 mL of dissolution samples were taken with a replacement of same volume using fresh medium. The obtained samples were analyzed at 271 nm using UV visible spectrophotometer. The values of predicted pharmacokinetic parameters like Cmax (maximum blood drug level), Tmax (time required to attain maximum blood drug level), and AUC (area under blood drug concentration curve) ranged between 80.8 ± 3.2-119.6 ± 4.7 ng/mL, 11.4 ± 0.2-12.2 ± 0.2 h, and 1430.5 ± 209.5-1970.6 ± 287.4 ng.h/mL, respectively. This certainly is a desired feature required at the formulation development step, where the formulator requires the development of a formulation using desired in vivo features on the basis of only accessible in vitro data. It can be concluded from the results that convolution method is a practical method for the prediction of drug concentration in blood and for quality control. PMID:27476294

  10. 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.

  11. 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. PMID:26953731

  12. Formulation and Evaluation of Multilayered Tablets of Pioglitazone Hydrochloride and Metformin Hydrochloride

    PubMed Central

    Chowdary, Y. Ankamma; Raparla, Ramakrishna; Madhuri, Muramshetty

    2014-01-01

    In the treatment of type 2 diabetes mellitus a continuous therapy is required which is a more complex one. As in these patients there may be a defect in both insulin secretion and insulin action exists. Hence, the treatment depends on the pathophysiology and the disease state. In the present study, multilayered tablets of pioglitazone hydrochloride 15 mg and metformin hydrochloride 500 mg were prepared in an attempt for combination therapy for the treatment of type 2 diabetes mellitus. Pioglitazone HCl was formulated as immediate release layer to show immediate action by direct compression method using combination of superdisintegrants, namely, crospovidone and avicel PH 102. Crospovidone at 20% concentration showed good drug release profile at 2 hrs. Metformin HCl was formulated as controlled release layer to prolong the drug action by incorporating hydrophilic polymers such as HPMC K4M by direct compression method and guar gum by wet granulation method in order to sustain the drug release from the tablets and maintain its integrity so as to provide a suitable formulation. The multilayered tablets were prepared after carrying out the optimization of immediate release layer and were evaluated for various precompression and postcompression parameters. Formulation F13 showed 99.97% of pioglitazone release at 2 hrs in 0.1 N HCl and metformin showed 98.81% drug release at 10 hrs of dissolution in 6.8 pH phosphate buffer. The developed formulation is equivalent to innovator product in view of in vitro drug release profile. The results of all these evaluation tests are within the standards. The procedure followed for the formulation of these tablets was found to be reproducible and all the formulations were stable after accelerated stability studies. Hence, multilayered tablets of pioglitazone HCl and metformin HCl can be a better alternative way to conventional dosage forms. PMID:26556204

  13. 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

  14. Formulation and Evaluation of Multilayered Tablets of Pioglitazone Hydrochloride and Metformin Hydrochloride.

    PubMed

    Chowdary, Y Ankamma; Raparla, Ramakrishna; Madhuri, Muramshetty

    2014-01-01

    In the treatment of type 2 diabetes mellitus a continuous therapy is required which is a more complex one. As in these patients there may be a defect in both insulin secretion and insulin action exists. Hence, the treatment depends on the pathophysiology and the disease state. In the present study, multilayered tablets of pioglitazone hydrochloride 15 mg and metformin hydrochloride 500 mg were prepared in an attempt for combination therapy for the treatment of type 2 diabetes mellitus. Pioglitazone HCl was formulated as immediate release layer to show immediate action by direct compression method using combination of superdisintegrants, namely, crospovidone and avicel PH 102. Crospovidone at 20% concentration showed good drug release profile at 2 hrs. Metformin HCl was formulated as controlled release layer to prolong the drug action by incorporating hydrophilic polymers such as HPMC K4M by direct compression method and guar gum by wet granulation method in order to sustain the drug release from the tablets and maintain its integrity so as to provide a suitable formulation. The multilayered tablets were prepared after carrying out the optimization of immediate release layer and were evaluated for various precompression and postcompression parameters. Formulation F13 showed 99.97% of pioglitazone release at 2 hrs in 0.1 N HCl and metformin showed 98.81% drug release at 10 hrs of dissolution in 6.8 pH phosphate buffer. The developed formulation is equivalent to innovator product in view of in vitro drug release profile. The results of all these evaluation tests are within the standards. The procedure followed for the formulation of these tablets was found to be reproducible and all the formulations were stable after accelerated stability studies. Hence, multilayered tablets of pioglitazone HCl and metformin HCl can be a better alternative way to conventional dosage forms. PMID:26556204

  15. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... milligrams of triflupromazine hydrochloride. (b) Sponsor. See No. 053501 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The drug is used in dogs and cats to relieve anxiety and to help control psychomotor... preanesthetic.1 (2) The drug is administered orally to dogs and cats at a dosage level of 1 to 2 milligrams...

  16. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... milligrams of triflupromazine hydrochloride. (b) Sponsor. See No. 053501 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The drug is used in dogs and cats to relieve anxiety and to help control psychomotor... preanesthetic.1 (2) The drug is administered orally to dogs and cats at a dosage level of 1 to 2 milligrams...

  17. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... milligrams of triflupromazine hydrochloride. (b) Sponsor. See No. 053501 in § 510.600(c) of this chapter. (c) Conditions of use. (1) The drug is used in dogs and cats to relieve anxiety and to help control psychomotor... preanesthetic.1 (2) The drug is administered orally to dogs and cats at a dosage level of 1 to 2 milligrams...

  18. 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 520.2098 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... the control of clinical signs associated with canine cognitive dysfunction syndrome. (ii)...

  19. 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 520.2098 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... the control of clinical signs associated with canine cognitive dysfunction syndrome. (ii)...

  20. 21 CFR 522.2615 - Tripelennamine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tripelennamine hydrochloride injection. 522.2615 Section 522.2615 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... use—(1) Amount—(i) Dogs, cats, and horses. For intramuscular use only at a dose of 0.5 milligram...

  1. 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. PMID:19942254

  2. Effect of thiamine hydrochloride, pyridoxine hydrochloride and calcium-d-pantothenate on the patulin content of apple juice concentrate.

    PubMed

    Yazici, Serafettin; Velioglu, Y Sedat

    2002-08-01

    Thiamine hydrochloride, pyridoxine hydrochloride and calcium-d-pantothenate were applied apple juice concentrates (AJC) at various doses in order to reduce the patulin content. AJC samples containing high levels of patulin were stored at 22 +/- 2 degrees C and 4 degrees C for 6 months after vitamins were added. Patulin was fully degraded at the end of a 6-month period in samples stored at 22 +/- 2 degrees C, on the other hand, other quality parameters diminished significantly. Without any considerable reduction on other quality parameters, applications of 1000 and 2500 mg/kg calcium-d-pantothenate resulted in reduction of patulin of 73.6 and 94.3%, respectively, however, 42.1% of patulin reduction was observed in the control sample of AJC stored for 1 month at 22 +/- 2 degrees C. Addition of thiamine hydrochloride (1000 mg/kg), pyrodoxine hydrochloride (625 or 875 mg/kg) and calcium-d-pantothenate (1000 or 2500 mg/kg) into the samples and storage at 4 degrees C for 6 months yielded 55.5 to 67.7% of patulin reduction which was only 35.8% for the control while the other quality parameters were protected adequately. PMID:12224421

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

    PubMed Central

    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. PMID:24876990

  4. Synthesis, characterization, cytotoxicity and antiangiogenic activity of copper(II) complexes with 1-adamantoyl hydrazone bearing pyridine rings.

    PubMed

    Rodić, Marko V; Leovac, Vukadin M; Jovanović, Ljiljana S; Spasojević, Vojislav; Joksović, Milan D; Stanojković, Tatjana; Matić, Ivana Z; Vojinović-Ješić, Ljiljana S; Marković, Violeta

    2016-06-10

    Three novel copper complexes with tridentate N2O ligand di(2-pyridil) ketone 1-adamantoyl hydrazone (Addpy) of the formula [Cu(II)2Cu(I)2(Addpy)2Br2(μ-Br4)] (1), catena-poly[CuCl(μ-Addpy)(μ-Cl)CuCl2]n (2) and [Cu(Addpy)(NCS)2] (3) were synthesized. Complexes are characterized by X-ray crystallography, spectral (UV-Vis, FTIR), electrochemical (CV) analyses, and magnetochemical measurements. Investigation of anticancer potential of Cu(II) complexes, mode of cell death, apoptosis, and inhibition of angiogenesis were performed. All tested malignant cell lines (HeLa, LS174, A549, K562, and MDA-MB-231) showed high sensitivity to the examined Cu(II) complexes. It has been shown that the complexes induce apoptosis in the caspase 3-dependent manner, whereas the anti-angiogenic effects of 1, 2, and 3 have been confirmed in EA.hy926 cells using a tube formation assay. PMID:27084495

  5. Growth and characterization of benzaldehyde 4-nitro phenyl hydrazone (BPH) single crystal: A proficient second order nonlinear optical material

    NASA Astrophysics Data System (ADS)

    Saravanan, M.; Abraham Rajasekar, S.

    2016-04-01

    The crystals (benzaldehyde 4-nitro phenyl hydrazone (BPH)) appropriate for NLO appliance were grown by the slow cooling method. The solubility and metastable zone width measurement of BPH specimen was studied. The material crystallizes in the monoclinic crystal system with noncentrosymmetric space group of Cc. The optical precision in the whole visible region was found to be excellent for non-linear optical claim. Excellence of the grown crystal is ascertained by the HRXRD and etching studies. Laser Damage Threshold and Photoluminescence studies designate that the grown crystal contains less imperfection. The mechanical behaviour of BPH sample at different temperatures was investigated to determine the hardness stability of the grown specimen. The piezoelectric temperament and the relative Second Harmonic Generation (for diverse particle sizes) of the material were also studied. The dielectric studies were executed at varied temperatures and frequencies to investigate the electrical properties. Photoconductivity measurement enumerates consummate of inducing dipoles due to strong incident radiation and also divulge the nonlinear behaviour of the material. The third order nonlinear optical properties of BPH crystals were deliberate by Z-scan method.

  6. Structural diversity in mercury(II) coordination complexes with asymmetrical hydrazone-based ligands derived from pyridine

    NASA Astrophysics Data System (ADS)

    Masoumi, Asad; Servati Gargari, Masoumeh; Mahmoudi, Ghodrat; Miroslaw, Barbara; Therrien, Bruno; Abedi, Marjan; Hazendonk, Paul

    2015-05-01

    Three novel Hg(II) complexes 1-3 of asymmetrical hydrazone-pyridine based ligands, L1-L3, with distinct coordination structures have been prepared and characterized by a single crystal X-ray diffraction, elemental and thermal analysis, and IR spectroscopy. The complexes form either discrete units with one (1) or two (2) organic ligands, or one-dimensional polymers (3). Hence the ligands can be regarded as chelating (1), mono-dentate (2) or bridging (3) agents. The mercury center is essentially neutralized in each complex by two iodide anions. The coordination in complexes 2 and 3 adopts deformed tetrahedral shapes. In contrast the Hg(II) cation in complex 1 binds three coplanar ligating atoms (O,N,N) and, as with pincer ligands, its coordination polyhedron is supplemented with two I- anions in apical positions. The structural diversity in these complexes is strongly influenced by the position of N atom in pyridine derived moieties. The crystal structure is stabilized by N/O-H⋯N/O/I hydrogen bonds and π⋯π interactions.

  7. HIV-1 Reverse Transcriptase Structure with RNase H Inhibitor dihydroxy benzoyl naphthyl Hydrazone Bound at a Novel Site

    SciTech Connect

    Himmel,D.; Sarafianos, S.; Dharmasena, S.; Hossain, M.; McCoy-Simandle, K.; Ilina, T.; Clark, A.; Knight, J.; Julias, J.; et al.

    2007-01-01

    The rapid emergence of drug-resistant variants of human immunodeficiency virus, type 1 (HIV-1), has limited the efficacy of anti-acquired immune deficiency syndrome (AIDS) treatments, and new lead compounds that target novel binding sites are needed. We have determined the 3.15 {angstrom} resolution crystal structure of HIV-1 reverse transcriptase (RT) complexed with dihydroxy benzoyl naphthyl hydrazone (DHBNH), an HIV-1 RT RNase H (RNH) inhibitor (RNHI). DHBNH is effective against a variety of drug-resistant HIV-1 RT mutants. While DHBNH has little effect on most aspects of RT-catalyzed DNA synthesis, at relatively high concentrations it does inhibit the initiation of RNA-primed DNA synthesis. Although primarily an RNHI, DHBNH binds >50 {angstrom} away from the RNH active site, at a novel site near both the polymerase active site and the non-nucleoside RT inhibitor (NNRTI) binding pocket. When DHBNH binds, both Tyr181 and Tyr188 remain in the conformations seen in unliganded HIV-1 RT. DHBNH interacts with conserved residues (Asp186, Trp229) and has substantial interactions with the backbones of several less well-conserved residues. On the basis of this structure, we designed substituted DHBNH derivatives that interact with the NNRTI-binding pocket. These compounds inhibit both the polymerase and RNH activities of RT.

  8. The cytotoxicity of benzaldehyde nitrogen mustard-2-pyridine carboxylic acid hydrazone being involved in topoisomerase IIα inhibition.

    PubMed

    Fu, Yun; Zhou, Sufeng; Liu, Youxun; Yang, Yingli; Sun, Xingzhi; Li, Changzheng

    2014-01-01

    The antitumor property of iron chelators and aromatic nitrogen mustard derivatives has been well documented. Combination of the two pharmacophores in one molecule in drug designation is worth to be explored. We reported previously the syntheses and preliminary cytotoxicity evaluation of benzaldehyde nitrogen mustard pyridine carboxyl acid hydrazones (BNMPH) as extended study, more tumor cell lines (IC50 for HepG2: 26.1 ± 3.5 μM, HCT-116: 57.5 ± 5.3 μM, K562: 48.2 ± 4.0 μM, and PC-12: 19.4 ± 2.2 μM) were used to investigate its cytotoxicity and potential mechanism. In vitro experimental data showed that the BNMPH chelating Fe(2+) caused a large number of ROS formations which led to DNA cleavage, and this was further supported by comet assay, implying that ROS might be involved in the cytotoxicity of BNMPH. The ROS induced changes of apoptosis related genes, but the TFR1 and NDRG1 metastatic genes were not obviously regulated, prompting that BNMPH might not be able to deprive Fe(2+) of ribonucleotide reductase. The BNMPH induced S phase arrest was different from that of iron chelators (G1) and alkylating agents (G2). BNMPH also exhibited its inhibition of human topoisomerase IIα. Those revealed that the cytotoxic mechanism of the BNMPH could stem from both the topoisomerase II inhibition, ROS generation and DNA alkylation.

  9. Synthesis of Tolmetin Hydrazide-Hydrazones and Discovery of a Potent Apoptosis Inducer in Colon Cancer Cells.

    PubMed

    Küçükgüzel, Ş Güniz; Koç, Derya; Çıkla-Süzgün, Pelin; Özsavcı, Derya; Bingöl-Özakpınar, Özlem; Mega-Tiber, Pınar; Orun, Oya; Erzincan, Pınar; Sağ-Erdem, Safiye; Şahin, Fikrettin

    2015-10-01

    Tolmetin hydrazide and a novel series of tolmetin hydrazide-hydrazones 4a-l were synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, (1)H NMR) methods. N'-[(2,6-Dichlorophenyl)methylidene]-2-[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetohydrazide (4g) was evaluated in vitro using the MTT colorimetric method against the colon cancer cell lines HCT-116 (ATCC, CCL-247) and HT-29 (ATCC, HTB-38) to determine growth inhibition and cell viability at different doses. Compound 4g exhibited anti-cancer activity with an IC50 value of 76 μM against colon cancer line HT-29 (ATCC, HTB-38) and did not display cytotoxicity toward control NIH3T3 mouse embryonic fibroblast cells compared to tolmetin. In addition, this compound was evaluated for caspase-3, caspase-8, caspase-9, and annexin-V activation in the apoptotic pathway, which plays a key role in the treatment of cancer. We demonstrated that the anti-cancer activity of this compound was due to the activation of caspase-8 and caspase-9 involved in the apoptotic pathway. In addition, in this study, we investigated the catalytical effect of COX on the HT-29 cancer line, the apoptotic mechanism, and the moleculer binding of tolmetin and compound 4g on the COX enzyme active site.

  10. Effects of zilpaterol hydrochloride and zilpaterol hydrochloride withdrawal time on beef carcass cutability, composition, and tenderness.

    PubMed

    Shook, J N; VanOverbeke, D L; Kinman, L A; Krehbiel, C R; Holland, B P; Streeter, M N; Yates, D A; Hilton, G G

    2009-11-01

    The impact of zilpaterol hydrochloride (ZH) on carcass yield, composition, and tenderness was evaluated using 384 beef steers in a randomized complete block design. Main effects were the addition of 0 or 8.3 mg/kg of ZH for the final 20 d of feeding and each inclusion level was paired with withdrawal periods of 3, 10, 17, or 24 d. The 2 animals with BW closest to the pen average were selected for carcass fabrication to determine carcass yield, composition, and tenderness. The carcasses from animals fed ZH had greater (P = 0.008) individual side weights. Carcass fat determinations were unchanged (P = 0.70) by ZH. Weights of the strip loin (P = 0.01), peeled tenderloin (P = 0.02), and top sirloin butt (P < 0.001) were all improved with ZH. When expressed as a proportion of carcass weight, ZH increased percentage of carcass in the top sirloin butt (P = 0.006), bottom sirloin tri-tip (P = 0.02), top inside round (P = 0.002), bottom round flat (P = 0.001), and flank steak (P = 0.02). A longer withdrawal time (WT) increased (P < 0.001) carcass weights. Shoulder clod weights were greatest (P < 0.001) with 17-d WT from ZH, whereas chuck roll weights were greatest (P = 0.02) at 17 and 24 d of WT. Peeled tenderloins, top sirloin butts, and eye of rounds responded to WT, with increased (P < 0.001) weights seen at 10 d of WT as compared with all other WT. Shear force values were greater at each of the 3 aging times, 7 d (P < 0.001), 14 d (P < 0.001), and 21 d (P = 0.003), in steaks from ZH-fed steers compared with control steers. Protein percentages were greater in ZH steaks (P = 0.03) and ZH ground beef trim (P < 0.001). Percent moisture was increased (P < 0.001) in strip loin steaks at 3 and 10 d WT. Ground beef trim had an increase (P = 0.04) in percent moisture and a decrease (P = 0.01) in percent fat at 10 d WT. Carcass weights and yields were improved with ZH feeding and may continue to improve even up to 10 d after withdrawal of the supplement. Tenderness was slightly

  11. The antitumor mechanism of di-2-pyridylketone 2-pyridine carboxylic acid hydrazone and its copper complex in ROS generation and topoisomerase inhibition, and hydrazone involvement in oxygen-catalytic iron mobilization.

    PubMed

    Huang, Tengfei; Li, Cuiping; Sun, Xingzhi; Zhu, Zhenfu; Fu, Yun; Liu, Youxun; Yuan, Yanbin; Li, Shaoshan; Li, Changzheng

    2015-11-01

    Iron depletion and stimulation of iron-dependent free radical damage is a rapidly developing field for chelation therapy, but the iron mobilization from ferritin by chelators has received less attention. In this study, the di-2-pyridylketone 2-pyridine carboxylic acid hydrazone (DPPCAH) and its copper complex was prepared and characterized by NMR and MS spectra. The proliferation inhibition assay showed that both DPPCAH and its copper complex exhibited selectively proliferation inhibition for HepG2 (IC50, 4.6 ± 0.2 µM for DPPACH and 1.3 ± 0.2 µM for its copper complex), but less inhibition for HCT-116 cell line (IC50, >100 µM for DPPACH and 7.8 ± 0.4 µM for its copper complex). The mechanistic studies revealed that DPPACH could remove iron from ferritin in a oxygen-catalytic manner, and contributed to redox activity of labile iron pool (LIP), that is less reported for the chelators that possess significant biological activity. The reactive oxygen species (ROS) generation and DNA cleavage assay in vitro and in vivo showed that both DPPACH-Fe(II) and DPPACH-Cu were redox-active species, indicating that ROS may mediate their antitumor activity. Further study revealed that both DPPACH and its copper complex displayed certain degree of inhibition of type II topoisomerase (Top) which contributed to their antitumor activity. Thus, the mechanism that iron mobilization by DPPACH from ferritin contributed to LIP was proposed, and both DPPACH and its copper complex were involved in ROS generation and Top II inhibition for their antitumor activities.

  12. Development of a microfluidic paper-based analytical device for the determination of salivary aldehydes.

    PubMed

    Ramdzan, Adlin N; Almeida, M Inês G S; McCullough, Michael J; Kolev, Spas D

    2016-05-01

    A low cost, disposable and easy to use microfluidic paper-based analytical device (μPAD) was developed for simple and non-invasive determination of total aldehydes in saliva with a potential to be used in epidemiological studies to assess oral cancer risk. The μPAD is based on the colour reaction between aldehydes (e.g. acetaldehyde, formaldehyde), 3-methyl-2-benzothiazolinone hydrazone (MBTH) and iron(III) to form an intense blue coloured formazan dye. The newly developed μPAD has a 3D design with two overlapping paper layers. The first layer comprises 15 circular detection zones (8 mm in diameter), each impregnated with 8 μL of MBTH, while the second layer contains 15 reagent zones (4 mm in diameter). Two μL of iron(III) chloride are added to each one of the second layer zones after the addition of sample to the detection zones in the first layer. All hydrophilic zones of the μPAD are defined by wax printing using a commercial wax printer. Due to the 2-step nature of the analytical reaction, the two paper layers are separated by a cellulose acetate interleaving sheet to allow for the reaction between the aldehydes in the saliva sample with MBTH to proceed first with the formation of an azine, followed by a blue coloured reaction between the azine and the oxidized by iron(III) form of MBTH, produced after the removal of the interleaving sheet. After obtaining a high resolution image of the detection side zone of the device using a flatbed scanner, the intensity of the blue colour within each detection zone is measured with Image J software. Under optimal conditions, the μPAD is characterised by a working range of 20.4-114.0 μM, limit of detection of 6.1 μM, and repeatability, expressed as RSD, of less than 12.7% (n = 5). There is no statistically significant difference at the 95% confidence level between the results obtained by the μPAD and the reference method (Student's t-test: 0.090 < 0.38). The optimized μPAD is stable for more than 41 days

  13. Fundamentals of ionic conductivity relaxation gained from study of procaine hydrochloride and procainamide hydrochloride at ambient and elevated pressure.

    PubMed

    Wojnarowska, Z; Swiety-Pospiech, A; Grzybowska, K; Hawelek, L; Paluch, M; Ngai, K L

    2012-04-28

    The pharmaceuticals, procaine hydrochloride and procainamide hydrochloride, are glass-forming as well as ionically conducting materials. We have made dielectric measurements at ambient and elevated pressures to characterize the dynamics of the ion conductivity relaxation in these pharmaceuticals, and calorimetric measurements for the structural relaxation. Perhaps due to their special chemical and physical structures, novel features are found in the ionic conductivity relaxation of these pharmaceuticals. Data of conductivity relaxation in most ionic conductors when represented by the electric loss modulus usually show a single resolved peak in the electric modulus loss M(")(f) spectra. However, in procaine hydrochloride and procainamide hydrochloride we find in addition another resolved loss peak at higher frequencies over a temperature range spanning across T(g). The situation is analogous to many non-ionic glass-formers showing the presence of the structural α-relaxation together with the Johari-Goldstein (JG) β-relaxation. Naturally the analogy leads us to name the slower and faster processes resolved in procaine hydrochloride and procainamide hydrochloride as the primary α-conductivity relaxation and the secondary β-conductivity relaxation, respectively. The analogy of the β-conductivity relaxation in procaine HCl and procainamide HCl with JG β-relaxation in non-ionic glass-formers goes further by the finding that the β-conductivity is strongly related to the α-conductivity relaxation at temperatures above and below T(g). At elevated pressure but compensated by raising temperature to maintain α-conductivity relaxation time constant, the data show invariance of the ratio between the β- and the α-conductivity relaxation times to changes of thermodynamic condition. This property indicates that the β-conductivity relaxation has fundamental importance and is indispensable as the precursor of the α-conductivity relaxation, analogous to the relation found

  14. Fundamentals of ionic conductivity relaxation gained from study of procaine hydrochloride and procainamide hydrochloride at ambient and elevated pressure

    NASA Astrophysics Data System (ADS)

    Wojnarowska, Z.; Swiety-Pospiech, A.; Grzybowska, K.; Hawelek, L.; Paluch, M.; Ngai, K. L.

    2012-04-01

    The pharmaceuticals, procaine hydrochloride and procainamide hydrochloride, are glass-forming as well as ionically conducting materials. We have made dielectric measurements at ambient and elevated pressures to characterize the dynamics of the ion conductivity relaxation in these pharmaceuticals, and calorimetric measurements for the structural relaxation. Perhaps due to their special chemical and physical structures, novel features are found in the ionic conductivity relaxation of these pharmaceuticals. Data of conductivity relaxation in most ionic conductors when represented by the electric loss modulus usually show a single resolved peak in the electric modulus loss M″(f ) spectra. However, in procaine hydrochloride and procainamide hydrochloride we find in addition another resolved loss peak at higher frequencies over a temperature range spanning across Tg. The situation is analogous to many non-ionic glass-formers showing the presence of the structural α-relaxation together with the Johari-Goldstein (JG) β-relaxation. Naturally the analogy leads us to name the slower and faster processes resolved in procaine hydrochloride and procainamide hydrochloride as the primary α-conductivity relaxation and the secondary β-conductivity relaxation, respectively. The analogy of the β-conductivity relaxation in procaine HCl and procainamide HCl with JG β-relaxation in non-ionic glass-formers goes further by the finding that the β-conductivity is strongly related to the α-conductivity relaxation at temperatures above and below Tg. At elevated pressure but compensated by raising temperature to maintain α-conductivity relaxation time constant, the data show invariance of the ratio between the β- and the α-conductivity relaxation times to changes of thermodynamic condition. This property indicates that the β-conductivity relaxation has fundamental importance and is indispensable as the precursor of the α-conductivity relaxation, analogous to the relation found

  15. Growth and characterization of thiosemicarbazide hydrochloride: A semiorganic NLO material

    NASA Astrophysics Data System (ADS)

    Santhakumari, R.; Ramamurthi, K.; Babu, R. Ramesh; Evans, Helen Stoeckli; Bhagavannarayana, G.; Hema, R.

    2011-11-01

    Thiosemicarbazide hydrochloride (TSCHCL) was synthesized by mixing thiosemicarbazide and hydrochloride in 1:1 molar ratio in double distilled water. Single crystals of TSCHCL were grown by slow evaporation at room temperature and were characterized by single crystal X-ray diffraction study to determine the molecular structure and by FT-IR, 1H and 13C NMR spectral analyses to confirm the synthesized compound. Thermogravimetric and differential thermal analyses reveal the thermal stability of the crystal. The transmission spectrum of TSCHCL showed that the crystal is transparent in the wavelength range 380-1100 nm. High resolution X-ray diffractometry (HRXRD) was employed to evaluate the perfection of the grown crystal. Mechanical properties of the grown crystal were studied using Vickers microhardness test. Second harmonic generation efficiency of the powdered TSCHCL was tested using Nd:YAG laser and is ˜1.5 times that of potassium dihydrogen orthophosphate.

  16. Preformed microcapsules for loading and sustained release of ciprofloxacin hydrochloride.

    PubMed

    Mao, Zhengwei; Ma, Lie; Gao, Changyou; Shen, Jiacong

    2005-05-01

    A novel pathway for ciprofloxacin hydrochloride delivery system based on spontaneous deposition mechanism was introduced with respect to encapsulation, quantitative drug loading and sustained release. Layer-by-layer assembly of oppositely charged polyelectrolytes onto melamine formaldehyde (MF) colloidal particles, followed by removal of the cores at low pH has yielded hollow microcapsules having a unique property to induce spontaneous deposition of various water-soluble substances. Observations under scanning electron microscopy, atomic force microscopy and transmission electron microscopy provided direct proofs of the spontaneous deposition. The quantitative drug loading and sustained release properties were elucidated. Results show that the loaded drug is proportional to drug feeding concentrations, temperature and salt concentrations, demonstrating tailorable deposition behavior that is crucial for the drug carrier. The deposited ciprofloxacin hydrochloride could be again released in a sustained manner and exhibited a significant antiseptic activity with high biocompatibility.

  17. The stability of oxymetazoline hydrochloride in aqueous solution.

    PubMed

    Stanisz, Beata

    2002-01-01

    The kinetics of the hydrolysis reaction of oxymetazoline hydrochloride in aqueous solution at three temperatures (343 K, 353 K, 363 K), over the pH-range 0.5-12.5 and ionic strength 0.5 has been investigated. The changes of concentration of oxymetazoline hydrochloride were followed by the HPLC method with UV detection. In the pH range from 0.45 to 12.50, the hydrolysis of oxymetazoline consists of hydrolysis of oxymetazoline molecules catalyzed by hydrogen ions, spontaneous hydrolysis of the dissociated and undissociated oxymetazoline molecules. A minimal rate of the hydrolysis oxymetazoline was observed to occur in the pH range from 2.0 to 5.0. Thermodynamic parameters of the reaction: energy, entropy and enthalpy of activation and the frequency factor for the specific rate constants were determined.

  18. 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.

  19. Shifting the Azo-hydrazone tautomeric equilibrium of methyl yellow in acidic medium by the formation of inclusion complexes with cyclodextrins

    NASA Astrophysics Data System (ADS)

    Ferreira, Ivania R.; Ando, Rômulo A.

    2012-01-01

    The protonation of methyl yellow (MY) leads to a tautomeric equilibrium involving the azo and hydrazone species, where the latter is predominant. Electronic and Raman spectroscopic data show that when MY in acidic medium is included in cyclodextrins, there is an inversion in the relative ratio of tautomers, in which the azo species become the major species. This indicates that the azo bond is included in cyclodextrin precluding its protonation. The understanding of the protonation, tautomeric and inclusion equilibria of these systems plays an important role in the designing of cyclodextrin based molecular machines controlled by light.

  20. Pyridine-Hydrazones as N,N'-Ligands in Asymmetric Catalysis: Pd(II)-Catalyzed Addition of Boronic Acids to Cyclic Sulfonylketimines.

    PubMed

    Álvarez-Casao, Yolanda; Monge, David; Álvarez, Eleuterio; Fernández, Rosario; Lassaletta, José M

    2015-10-16

    The design, synthesis, and coordination features of a novel class of chiral pyridine-hydrazone ligands are described. As a first application, L/Pd(TFA)2 complexes served as catalysts in the 1,2-addition of arylboronic acids to saccharin-derived cyclic ketimines, affording products in high yields and enantioselectivities. The method was also applied to more challenging 3,4-disubstituted 1,2,5-thiadiazole 1,1-dioxides, affording again high yields and enantioselectivities along with high regioselectivities for unsymmetrically substituted derivatives.

  1. A Facile and Convenient Synthesis of some Novel Hydrazones, Schiff’s Base and Pyrazoles Incorporating Thieno[2,3-b]thiophenes

    PubMed Central

    Mabkhot, Yahia Nasser; Barakat, Assem; Al-Majid, Abdullah Mohammed; Al-Othman, Zeid Abdullah; Alamary, Abdullah Saleh

    2011-01-01

    A facile and convenient synthesis of some novel hydrazones, schiff’s base and pyrazoles from thieno[2,3-b]thiophene derivatives 1 have been achieved in high yields assisted by microwave and classical methods. The structures of all the title compounds have been elucidated by elemental analysis, IR, MS, 1H-NMR and 13C-NMR. Generally, these findings represent a new class of sulfur and nitrogen moieties that should also be of interest as new materials. PMID:22174635

  2. Lipophilicity of analogs of pyridoxal isonicotinoyl hydrazone (PIH) determines the efflux of iron complexes and toxicity in K562 cells.

    PubMed

    Buss, Joan L; Arduini, Emmanuele; Shephard, Kyle C; Ponka, Prem

    2003-02-01

    Iron overload secondary to beta-thalassemia and other iron-loading anemias is the most serious obstacle to be overcome in the treatment of these diseases, since there is no physiological mechanism for excretion of the excess iron acquired by chronic blood transfusion. Due to the inconvenience and cost of the current iron chelation therapy, the search for an orally available iron chelator is ongoing. Pyridoxal isonicotinoyl hydrazone (PIH) and many of its analogs are effective at mobilizing iron in vivo and in vitro at doses that are not toxic. PIH analogs were approximately equally effective at binding 59Fe within K562 cells; their efficacy depended upon the kinetics of release of the iron-chelator complex from the cell, which was correlated inversely with the lipophilicity of the chelators. Addition of BSA, which has a well-characterized affinity for lipophilic species, to the extracellular medium enhanced iron-chelator efflux, such that all analogs caused 59Fe release from the cells as quickly as it was chelated; this suggests that BSA acts as an extracellular sink for the iron-chelator complexes, many of which are highly lipophilic. The toxicity of the free chelators varied over two orders of magnitude, and was correlated with the amount of intracellular 59Fe-chelator complexes, implicating the complexes in the mechanism of toxicity of the chelators. Understanding the structural features that determine the efficacy and toxicity of iron chelators in biological systems is of value in the selection of PIH analogs for in vivo examination.

  3. Torsionally Responsive C[subscript 3]-Symmetric Azo Dyes: Azo−Hydrazone Tautomerism, Conformational Switching, and Application for Chemical Sensing

    SciTech Connect

    Lee, Ho Yong; Song, Xinli; Park, Hyunsoo; Baik, Mu-Hyun; Lee, Dongwhan

    2010-12-07

    An efficient triple azo coupling reaction between anilines and phloroglucinol furnished a series of C{sub 3}-symmetric molecules 7-9 supporting multiple conjugation pathways that converge at the molecular core. A combination of {sup 1}H/{sup 13}C NMR spectroscopy, X-ray crystallography, and density functional theory computational studies provided a coherent picture of the [n,{pi}]-conjugated molecular core, which is best described as the tris(hydrazone) [rather than tris(azo)] tautomer stabilized by resonance-assisted hydrogen bonding. For a homologous series of compounds, an increase in the torsional angles between the planar molecular core and the peripheral aryl groups results in a systematic blue shift in the low-energy electronic transitions (7, 523 nm; 8, 505 nm; 9, 445 nm in CHCl{sub 3}) that qualitatively correlates with the shrinkage of effective conjugation through structural distortion. Similar spectral shifts could also be induced by amine substrates that interact with the intramolecular hydrogen-bonding network to trigger bond-twisting motions. Specifically, a brief exposure of a thin film of 7 to vapor samples of butyl-, hexyl-, diethyl-, and diisopropylamine resulted in a rapid and reversible color change from pink to dark-orange. Under similar conditions, however, triethylamine did not elicit any detectable color change, despite the fact that it has a significantly higher vapor pressure than n-hexylamine. These findings implicate that the hydrogen-bonding donor ability is a key requirement for the binding-induced conformational switching, which allows for direct naked-eye detection of volatile amines under ambient conditions.

  4. A novel kind of TSV slurry with guanidine hydrochloride

    NASA Astrophysics Data System (ADS)

    Jiao, Hong; Yuling, Liu; Baoguo, Zhang; Xinhuan, Niu; Liying, Han

    2015-10-01

    The effect of a novel alkaline TSV (through-silicon-via) slurry with guanidine hydrochloride (GH) on CMP (chemical mechanical polishing) was investigated. The novel alkaline TSV slurry was free of any inhibitors. During the polishing process, the guanidine hydrochloride serves as an effective surface-complexing agent for TSV CMP applications, the removal rate of barrier (Ti) can be chemically controlled through tuned selectivity with respect to the removal rate of copper and dielectric, which is helpful to modifying the dishing and gaining an excellent topography performance in TSV manufacturing. In this paper, we mainly studied the working mechanism of the components of slurry and the skillful application guanidine hydrochloride in the TSV slurry. Project supported by the Major National Science and Technology Special Projects (No. 2009ZX02308), the Fund Project of Hebei Provincial Department of Education, China (No. QN2014208), the Natural Science Foundation of Hebei Province, China (No. E2013202247), and Colleges and Universities Scientific research project of Hebei Province, China (No. Z2014088).

  5. 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.

  6. Interaction between lidocaine hydrochloride (with and without adrenaline) and various irrigants: A nuclear magnetic resonance analysis

    PubMed Central

    Vidhya, Nirmal; Karthikeyan, Balasubramanian Saravana; Velmurugan, Natanasabapathy; Abarajithan, Mohan; Nithyanandan, Sivasankaran

    2014-01-01

    Background: Interaction between local anesthetic solution, lidocaine hydrochloride (with and without adrenaline), and root canal irrigants such as sodium hypochlorite (NaOCl), ethylene diamine tetra-acetic acid (EDTA), and chlorhexidine (CHX) has not been studied earlier. Hence, the purpose of this in vitro study was to evaluate the chemical interaction between 2% lidocaine hydrochloride (with and without adrenaline) and commonly used root canal irrigants, NaOCl, EDTA, and CHX. Materials and Methods: Samples were divided into eight experimental groups: Group I-Lidocaine hydrochloride (with adrenaline)/3% NaOCl, Group II-Lidocaine hydrochloride (with adrenaline)/17% EDTA, Group III- Lidocaine hydrochloride (with adrenaline)/2% CHX, Group IV-Lidocaine hydrochloride (without adrenaline)/3% NaOCl, Group V-Lidocaine hydrochloride (without adrenaline)/17% EDTA, Group VI-Lidocaine hydrochloride (without adrenaline)/2% CHX, and two control groups: Group VII-Lidocaine hydrochloride (with adrenaline)/deionized water and Group VIII-Lidocaine hydrochloride (without adrenaline)/deionized water. The respective solutions of various groups were mixed in equal proportions (1 ml each) and observed for precipitate formation. Chemical composition of the formed precipitate was then analysed by nuclear magnetic resonance spectroscopy (NMR) and confirmed with diazotation test. Results: In groups I and IV, a white precipitate was observed in all the samples on mixing the respective solutions, which showed a color change to reddish brown after 15 minutes. This precipitate was then analysed by NMR spectroscopy and was observed to be 2,6-xylidine, a reported toxic compound. The experimental groups II, III, V, and VI and control groups VII and VIII showed no precipitate formation in any of the respective samples, until 2 hours. Conclusion: Interaction between lidocaine hydrochloride (with and without adrenaline) and NaOCl showed precipitate formation containing 2,6-xylidine, a toxic compound

  7. Polydopamine-based immobilization of a hydrazone covalent organic framework for headspace solid-phase microextraction of pyrethroids in vegetables and fruits.

    PubMed

    Wu, Mingxue; Chen, Gang; Liu, Ping; Zhou, Weihong; Jia, Qiong

    2016-07-22

    We designed a novel hydrazone covalent organic framework (COF) and developed a polydopamine (PDA) method to immobilize COF on a stainless steel fiber for headspace solid-phase microextraction (HS-SPME). A series of characterization studies was performed to validate the structure and property of the prepared fiber. The COF-PDA fiber was applied for the extraction of pyrethroids coupled with gas chromatography equipped with an electron capture detector (GC-ECD). Under the optimum experimental conditions, high enhancement factors of 307-2327 were achieved, indicating that the hydrazone COF possessed good extraction efficiency for pyrethroids. The detection limits ranged from 0.11 to 0.23μgkg(-1) with relative standard deviations varying in the range of 3.6-9.2% (intra-batch) and 6.9-12.1% (inter-batch), respectively. The developed method was applied to the determination of pyrethroids in fruit and vegetable samples and the accuracy was assessed through recovery experiments. PMID:27317006

  8. SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H.

    PubMed

    Raghav, Neera; Singh, Mamta

    2014-08-01

    Cathepsins have emerged as potential drug targets for melanoma therapy and engrossed attention of researchers for development and evaluation of cysteine cathepsin inhibitors as cancer therapeutics. In this direction, we have designed, synthesized, and assayed in vitro a small library of 30 low molecular weight functionalized analogs of chalcone hydrazones for evaluating structure-activity relationship aspects and inhibitory potency against cathepsin B and H. The maximum inhibitory effect was exerted by chalcone hydrazones, which are open chain analogues followed by their cyclized derivatives, pyrazolines and pyrazoles. All the synthesized compounds were established as reversible inhibitors of these enzymes. Cathepsin B was selectively inhibited by the compounds in each series. Compounds 1d, 2d and 4d were recognized as most potent inhibitors of cathepsin B in this study with Ki values of 0.042 μM, 0.053 μM and 0.131 μM whereas 1b (Ki=1.111 μM), 2b (Ki=1.174 μM) and 4b (Ki=1.562 μM) inhibited cathepsin H activity effectively. And, preeminent cathepsin B inhibitors were -NO2 functionalized however, -Cl substituted moieties were the most persuasive inhibitors for cathepsin H among all the designed compounds. Molecular docking studies performed using iGemdock provided valuable insights. PMID:24913985

  9. Investigation of the azo-hydrazone tautomeric equilibrium in an azo dye involving the naphthalene moiety by UV-vis spectroscopy and quantum chemistry

    NASA Astrophysics Data System (ADS)

    Ünal, Arslan; Eren, Bilge; Eren, Erdal

    2013-10-01

    Photophysical properties of the azo-hydrazone tautomerism of Eriochrome Blue Black B (1-(1-hydroxy-2-naphthylazo)-2-naphthol-4-sulphonic acid) in DMF, MeCN and water were investigated using UV-visible spectroscopy and quantum chemical calculations. The optimized molecular structure parameters, relative energies, mole fractions, electronic absorption spectra and HOMO-LUMO energies for possible stable tautomeric forms of EBB were theoretically calculated by using hybrid density functional theory, (B3LYP) methods with 6-31G(d) basis set level and polarizable continuum model (PCM) for solvation effect. The effects of varying pH-, dye concentration-, solvent-, temperature-, and time-dependences on the UV-vis spectra of Eriochrome Blue Black B were also investigated experimentally. The calculations showed that the dye exhibited acid-base, azo-hydrazone and aggregate equilibria in DMF solution, while the most probably preferred form in MeCN solution was azo form. Thermodynamic parameters of dimerization reaction in DMF solution proved that entropy was the driving force of this reaction.

  10. Self-assembled micelles composed of doxorubicin conjugated Y-shaped PEG-poly(glutamic acid)2 copolymers via hydrazone linkers.

    PubMed

    Sui, Bowen; Xu, Hui; Jin, Jian; Gou, Jingxin; Liu, Jingshuo; Tang, Xing; Zhang, Yu; Xu, Jinghua; Zhang, Hongfeng; Jin, Xiangqun

    2014-01-01

    In this work, micelles composed of doxorubicin-conjugated Y-shaped copolymers (YMs) linked via an acid-labile linker were constructed. Y-shaped copolymers of mPEG-b-poly(glutamate-hydrazone-doxorubicin)2 and linear copolymers of mPEG-b-poly(glutamate-hydrazone-doxorubicin) were synthesized and characterized. Particle size, size distribution, morphology, drug loading content (DLC) and drug release of the micelles were determined. Alterations in size and DLC of the micelles could be achieved by varying the hydrophobic block lengths. Moreover, at fixed DLCs, YMs showed a smaller diameter than micelles composed of linear copolymers (LMs). Also, all prepared micelles showed sustained release behaviors under physiological conditions over 72 h. DOX loaded in YMs was released more completely, with 30% more drug released in acid. The anti-tumor efficacy of the micelles against HeLa cells was evaluated by MTT assays, and YMs exhibited stronger cytotoxic effects than LMs in a dose- and time-dependent manner. Cellular uptake studied by CLSM indicated that YMs and LMs were readily taken up by HeLa cells. According to the results of this study, doxorubicin-conjugated Y-shaped PEG-(polypeptide)2 copolymers showed advantages over linear copolymers, like assembling into smaller nanoparticles, faster drug release in acid, which may correspond to higher cellular uptake and enhanced extracellular/intracellular drug release, indicating their potential in constructing nano-sized drug delivery systems.

  11. A CuAAC-Hydrazone-CuAAC Trifunctional Scaffold for the Solid-Phase Synthesis of Trimodal Compounds: Possibilities and Limitations.

    PubMed

    Fabre, Benjamin; Pícha, Jan; Vaněk, Václav; Buděšínský, Miloš; Jiráček, Jiří

    2015-10-23

    We present a trifunctional scaffold designed for the solid-phase synthesis of trimodal compounds. This scaffold holds two alkyne arms in a free and TIPS-protected form for consecutive CuAAC (copper(I)-catalyzed azide-alkyne cycloaddition), one Fmoc-protected hydrazide arm for reaction with aldehydes, and one carboxylic acid arm with CF₂ groups for attachment to the resin and (19)F-NMR quantification. This scaffold was attached to a resin and derivatized with model azides and aliphatic, electron-rich or electron-poor aromatic aldehydes. We identified several limitations of the scaffold caused by the instability of hydrazones in acidic conditions, in the presence of copper during CuAAC, and when copper accumulated in the resin. We successfully overcame these drawbacks by optimizing synthetic conditions for the derivatization of the scaffold with aromatic aldehydes. Overall, the new trifunctional scaffold combines CuAAC and hydrazone chemistries, offering a broader chemical space for the development of bioactive compounds.

  12. Sulphur promoted C(sp(3))-C(sp(2)) cross dehydrogenative cyclisation of acetophenone hydrazones with aldehydes: efficient synthesis of 3,4,5-trisubstituted 1H-pyrazoles.

    PubMed

    Vanjari, Rajeshwer; Guntreddi, Tirumaleswararao; Kumar, Saurabh; Singh, Krishna Nand

    2015-01-01

    A novel strategy for the cross dehydrogenative coupling (CDC) of acetophenone hydrazones and aldehydes has been developed for the synthesis of highly substituted pyrazoles. This work, for the first time, uses elemental sulfur as a promoter as well as a hydrogen acceptor in effecting the Csp(3)-Csp(2) bond formation via C-H activation.

  13. 40 CFR 180.502 - Aminoethoxyvinylglycine hydrochloride (aviglycine HCl); tolerances for residues.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... (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...

  14. 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...

  15. 21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 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....

  16. 21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 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....

  17. 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....

  18. 40 CFR 721.6196 - Hydrochloride salt of a fatty polyalkkylene polyamine (generic).

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... AGENCY (CONTINUED) TOXIC SUBSTANCES CONTROL ACT SIGNIFICANT NEW USES OF CHEMICAL SUBSTANCES Significant New Uses for Specific Chemical Substances § 721.6196 Hydrochloride salt of a fatty polyalkkylene... 40 Protection of Environment 31 2014-07-01 2014-07-01 false Hydrochloride salt of a...

  19. 40 CFR 721.6196 - Hydrochloride salt of a fatty polyalkkylene polyamine (generic).

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... AGENCY (CONTINUED) TOXIC SUBSTANCES CONTROL ACT SIGNIFICANT NEW USES OF CHEMICAL SUBSTANCES Significant New Uses for Specific Chemical Substances § 721.6196 Hydrochloride salt of a fatty polyalkkylene... 40 Protection of Environment 32 2012-07-01 2012-07-01 false Hydrochloride salt of a...

  20. 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...

  1. 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...

  2. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ..., 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...

  3. 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...

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

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

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

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  6. 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...

  7. 21 CFR 524.1662a - Oxytetracycline hydrochloride and hydrocortisone spray.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... spray. 524.1662a Section 524.1662a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... NEW ANIMAL DRUGS § 524.1662a Oxytetracycline hydrochloride and hydrocortisone spray. (a) Specifications. Each 3-ounce unit of oxytetracycline hydrochloride and hydrocortisone spray contains...

  8. 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

    ... titration of the hydrochloric acid that is liberated when hydroxylamine hydrochloride reacts with... resin/solvent solution to pH 4.0, using the prestandardized pH meter, 1.0 N hydrochloric acid, 0.1 N hydrochloric acid, and 0.1 N sodium hydroxide. 5.5Add 50 mL of the hydroxylamine hydrochloride...

  9. 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...

  10. 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

  11. HPLC study on the stability of bendamustine hydrochloride immobilized onto polyphosphoesters.

    PubMed

    Pencheva, Ivanka; Bogomilova, Anita; Koseva, Neli; Obreshkova, Danka; Troev, Kolio

    2008-12-01

    Novel water soluble polymer complexes of bendamustine hydrochloride, a bifunctional alkylating agent with antimetabolic and cytotoxic activity, were developed using biodegradable polymer carriers-poly(oxyethylene H-phosphonate), poly(methyloxyethylene phosphate) and poly(hydroxyoxyethylene phosphate). Bendamustine hydrochloride was immobilized onto polyphosphoesters via covalent, ionic and hydrogen bonding. The structure of the complexes formed was elucidated by (1)H, (13)C, (31)P NMR and FT-IR spectroscopy. The chemical stability of bendamustine hydrochloride in the novel complexes was studied by HPLC analysis based on a validated method with appointed analytical parameters such as specificity, repeatability, limit of quantitation, limit of detection and linearity. The results from the HPLC indicate that in neutral (pH 7) and alkaline (pH 9) media bendamustine hydrochloride in the polymer complexes is more stable than the pure bendamustine hydrochloride. The enhanced stability of the immobilized drug is explained with the drug interaction with the polymer carriers or their degradation products.

  12. 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.

  13. [Studies on transdermal delivery system of dihydroetorphine hydrochloride].

    PubMed

    Chen, X P; Guo, Q D; Shi, T S

    1996-01-01

    A transdermal delivery system of dihydroetorphine hydrochloride (DHE-TDS) was developed. The DHE-TDS mainly composed of polyvinyl alcohol, polyvinyl pyrrolidone and lactose. Tests on rabbits showed only slight skin irritation according to federal hazardous substances act. By giving DHE-TDS to rabbits, DHE release was shown to be governed by first-order mechanism. When DHE-TDS was given to Wistar rats, a relatively stable blood drug concentration was observed from 4-32 h after drug administration. Writhing tests showed that one dose of DHE-TDS would maintain the narcotic action on rats for at least 48 h.

  14. 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.

  15. 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

  16. [Examination of effectiveness of olopatadine hydrochloride in atopic dermatitis].

    PubMed

    Shimizu, Tadamichi; Mashiko, Maki; Shimizu, Hiroshi

    2005-02-01

    Subjective/objective symptoms (itching, papula, erythema, lichenification, desquamation, scratching, erosion) and the levels of IgE, LDH, interleukin (IL) -6, thymus and activation-regulated chemokine (TARC) were compared before and after administering olopatadine hydrochloride (ALLELOCK tablets) to 17 atopic dermatitis (AD) patients. Subject/objective symptoms improved significantly after administering the agent, and the total dosage of the combined topical steroids was also significantly decreased after administration (p<0.05), although IgE, IL-6 and LDH levels did not change, TARC was significantly decreased (p<0.05). The correlation between the levels of IgE, IL-6, LDH and TARC before and after the administration was examined. There was a positive correlation between IgE and TARC (r=0.62, p<0.01) and between IL-6 and TARC (r=0.78, p<0.01). Olopatadine hydrochloride is therefore useful in improving the symptoms in AD, and TARC may be used as an indicator of the symptom improvement.

  17. Formulation and Evaluation of Tramadol hydrochloride Rectal Suppositories.

    PubMed

    Saleem, M A; Taher, M; Sanaullah, S; Najmuddin, M; Ali, Javed; Humaira, S; Roshan, S

    2008-09-01

    Rectal suppositories of tramadol hydrochloride were prepared using different bases and polymers like PEG, cocoa butter, agar and the effect of different additives on in vitro release of tramadol hydrochloride was studied. The agar-based suppositories were non-disintegrating/non-dissolving, whereas PEGs were disintegrating/dissolving and cocoa butter were melting suppositories. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content and hardness. The PEG and cocoa butter suppositories were evaluated for macromelting range, disintegration and liquefaction time. In vitro release study was performed by USP type I apparatus. The prepared suppositories were within the permissible range of all physical parameters. In vitro drug release was in the order of PEG>Agar>cocoa butter. Addition of PVP, HPMC in agar suppositories retards the release. The mechanism of drug release was diffusion controlled and follows first order kinetics. The results suggested that blends of PEG of low molecular weight (1000) with high molecular weight (4000 and 6000) in different percentage and agar in 10% w/w as base used to formulate rapid release suppositories. The sustained release suppositories can be prepared by addition of PVP, HPMC in agar-based suppositories and by use of cocoa butter as base.

  18. 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. PMID:7097876

  19. Application of direct crystallization for racemic compound propranolol hydrochloride.

    PubMed

    Wang, Xiujuan; Lu, Jie; Ching, Chi Bun

    2007-10-01

    The application of direct crystallization integrating with chromatography to the resolution of a racemic compound propranolol hydrochloride was studied and the crystallization progression was clearly illustrated in terms of the diagram of solubility and metastable zone widths with different enantiomeric compositions. The solubility and metastable zone widths of propranolol hydrochloride in the mixture of methanol and isopropanol were determined using an in situ Lasentec Focused Beam Reflectance Measurement (FBRM) probe. The direct crystallizations were carried out in an automatic lab reactor (Mettler Toledo LabMax) system. The optical purity of final product crystals was examined using differential scanning calorimetry (DSC), HPLC and PXRD. The crystal size distribution and morphology were analyzed using Malvern Mastersizer and Jeol SEM. It was found that optically pure crystal product could be obtained within certain safe supersaturation limit and there was no evidence of polymorph or solvate/hydrate transformation during the crystallization process. There was no selectivity of crystal growth or nucleation between the pure enantiomer and its racemate when the solution reaches the temperature lower than saturation temperature of the racemate. Hence, the critical supersaturation control of a solution was essential to obtain pure enantiomers from a partially resolved racemate. PMID:17549769

  20. 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.

  1. 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.

  2. Intestinal Anisakiasis Treated Successfully with Prednisolone and Olopatadine Hydrochloride

    PubMed Central

    Toyoda, Hideki; Tanaka, Kyosuke

    2016-01-01

    The clinical characteristic of gastrointestinal anisakiasis is severe abdominal pain after eating raw fish. Intestinal anisakiasis is more uncommon than gastric anisakiasis. Most patients with intestinal anisakiasis need hospitalization because anisakiasis can cause intestinal obstruction, ileus, peritonitis or intestinal perforation. We report a case of intestinal anisakiasis. A 43-year-old woman presented with symptoms of intermittent abdominal pain 2 days after eating raw fish. Her brother had eaten the same food and had been suffering from gastric anisakiasis. Abdominal ultrasonography in this patient showed localized jejunal wall thickening with dilated lumen of proximal jejunum and ascites. According to the clinical course and examinations, she was diagnosed with intestinal anisakiasis. Administration of prednisolone 5 mg/day and olopatadine hydrochloride 10 mg/day improved her symptoms quickly without hospitalization. Prednisolone was administered for 10 days, and olopatadine hydrochloride was administered for a total of 6 weeks according to ultrasonographic findings. Six months after the treatment, the abdominal ultrasonography demonstrated normal findings. This case demonstrates that ultrasonography was quite useful for the diagnosis and surveillance of intestinal anisakiasis. Furthermore, treatment with corticosteroid and an antiallergic agent could be an option for patients with intestinal anisakiasis. PMID:27403099

  3. Structural characterisation and dehydration behaviour of siramesine hydrochloride.

    PubMed

    Zimmermann, Anne; Tian, Fang; de Diego, Heidi Lopez; Frydenvang, Karla; Rantanen, Jukka; Elema, Michiel Ringkjøbing; Hovgaard, Lars

    2009-10-01

    In this study the crystal structures of siramesine hydrochloride anhydrate alpha-form and siramesine hydrochloride monohydrate were determined, and this structural information was used to explain the physicochemical properties of the two solid forms. In the crystal structure of the monohydrate, each water molecule is hydrogen bonded to two chloride ions, and thus the water is relatively strongly bound in the crystal. No apparent channels for dehydration were observed in the monohydrate structure, which could allow transmission of structural information during dehydration. Instead destructive dehydration occurred, where the elimination of water from the monohydrate resulted in the formation of an oily phase, which subsequently recrystallised into one or more crystalline forms. Solubility and intrinsic dissolution rate of the anhydrate alpha-form and the monohydrate in aqueous media were investigated and both were found to be lower for the monohydrate compared to the anhydrate alpha-form. Finally, the interactions between water molecules and chloride ions in the monohydrate as well as changes in packing induced by water incorporation could be detected by spectroscopic techniques.

  4. Intestinal Anisakiasis Treated Successfully with Prednisolone and Olopatadine Hydrochloride.

    PubMed

    Toyoda, Hideki; Tanaka, Kyosuke

    2016-01-01

    The clinical characteristic of gastrointestinal anisakiasis is severe abdominal pain after eating raw fish. Intestinal anisakiasis is more uncommon than gastric anisakiasis. Most patients with intestinal anisakiasis need hospitalization because anisakiasis can cause intestinal obstruction, ileus, peritonitis or intestinal perforation. We report a case of intestinal anisakiasis. A 43-year-old woman presented with symptoms of intermittent abdominal pain 2 days after eating raw fish. Her brother had eaten the same food and had been suffering from gastric anisakiasis. Abdominal ultrasonography in this patient showed localized jejunal wall thickening with dilated lumen of proximal jejunum and ascites. According to the clinical course and examinations, she was diagnosed with intestinal anisakiasis. Administration of prednisolone 5 mg/day and olopatadine hydrochloride 10 mg/day improved her symptoms quickly without hospitalization. Prednisolone was administered for 10 days, and olopatadine hydrochloride was administered for a total of 6 weeks according to ultrasonographic findings. Six months after the treatment, the abdominal ultrasonography demonstrated normal findings. This case demonstrates that ultrasonography was quite useful for the diagnosis and surveillance of intestinal anisakiasis. Furthermore, treatment with corticosteroid and an antiallergic agent could be an option for patients with intestinal anisakiasis. PMID:27403099

  5. Reagents for astatination of biomolecules. 5. Evaluation of hydrazone linkers in (211)At- and (125)I-labeled closo-decaborate(2-) conjugates of Fab' as a means of decreasing kidney retention.

    PubMed

    Wilbur, D Scott; Chyan, Ming-Kuan; Hamlin, Donald K; Nguyen, Holly; Vessella, Robert L

    2011-06-15

    Evaluation of monoclonal antibody (mAb) fragments (e.g., Fab', Fab, or engineered fragments) as cancer-targeting reagents for therapy with the α-particle emitting radionuclide astatine-211 ((211)At) has been hampered by low in vivo stability of the label and a propensity of these proteins localize to kidneys. Fortunately, our group has shown that the low stability of the (211)At label, generally a meta- or para-[(211)At]astatobenzoyl conjugate, on mAb Fab' fragments can be dramatically improved by the use of closo-decaborate(2-) conjugates. However, the higher stability of radiolabeled mAb Fab' conjugates appears to result in retention of radioactivity in the kidneys. This investigation was conducted to evaluate whether the retention of radioactivity in kidney might be decreased by the use of an acid-cleavable hydrazone between the Fab' and the radiolabeled closo-decaborate(2-) moiety. Five conjugation reagents containing sulfhydryl-reactive maleimide groups, a hydrazone functionality, and a closo-decaborate(2-) moiety were prepared. In four of the five conjugation reagents, a discrete poly(ethylene glycol) (PEG) linker was used, and one substituent adjacent to the hydrazone was varied (phenyl, benzoate, anisole, or methyl) to provide varying acid sensitivity. In the initial studies, the five maleimido-closo-decaborate(2-) conjugation reagents were radioiodinated ((125)I or (131)I), then conjugated with an anti-PSMA Fab' (107-1A4 Fab'). Biodistributions of the five radioiodinated Fab' conjugates were obtained in nude mice at 1, 4, and 24 h post injection (pi). In contrast to closo-decaborate(2-) conjugated to 107-1A4 Fab' through a noncleavable linker, two conjugates containing either a benzoate or a methyl substituent on the hydrazone functionality displayed clearance rates from kidney, liver, and spleen that were similar to those obtained with directly radioiodinated Fab' (i.e., no conjugate). The maleimido-closo-decaborate(2-) conjugation reagent containing a

  6. Reagents for astatination of biomolecules. 5. Evaluation of hydrazone linkers in (211)At- and (125)I-labeled closo-decaborate(2-) conjugates of Fab' as a means of decreasing kidney retention.

    PubMed

    Wilbur, D Scott; Chyan, Ming-Kuan; Hamlin, Donald K; Nguyen, Holly; Vessella, Robert L

    2011-06-15

    Evaluation of monoclonal antibody (mAb) fragments (e.g., Fab', Fab, or engineered fragments) as cancer-targeting reagents for therapy with the α-particle emitting radionuclide astatine-211 ((211)At) has been hampered by low in vivo stability of the label and a propensity of these proteins localize to kidneys. Fortunately, our group has shown that the low stability of the (211)At label, generally a meta- or para-[(211)At]astatobenzoyl conjugate, on mAb Fab' fragments can be dramatically improved by the use of closo-decaborate(2-) conjugates. However, the higher stability of radiolabeled mAb Fab' conjugates appears to result in retention of radioactivity in the kidneys. This investigation was conducted to evaluate whether the retention of radioactivity in kidney might be decreased by the use of an acid-cleavable hydrazone between the Fab' and the radiolabeled closo-decaborate(2-) moiety. Five conjugation reagents containing sulfhydryl-reactive maleimide groups, a hydrazone functionality, and a closo-decaborate(2-) moiety were prepared. In four of the five conjugation reagents, a discrete poly(ethylene glycol) (PEG) linker was used, and one substituent adjacent to the hydrazone was varied (phenyl, benzoate, anisole, or methyl) to provide varying acid sensitivity. In the initial studies, the five maleimido-closo-decaborate(2-) conjugation reagents were radioiodinated ((125)I or (131)I), then conjugated with an anti-PSMA Fab' (107-1A4 Fab'). Biodistributions of the five radioiodinated Fab' conjugates were obtained in nude mice at 1, 4, and 24 h post injection (pi). In contrast to closo-decaborate(2-) conjugated to 107-1A4 Fab' through a noncleavable linker, two conjugates containing either a benzoate or a methyl substituent on the hydrazone functionality displayed clearance rates from kidney, liver, and spleen that were similar to those obtained with directly radioiodinated Fab' (i.e., no conjugate). The maleimido-closo-decaborate(2-) conjugation reagent containing a

  7. Reagents for Astatination of Biomolecules. 5. Evaluation of hydrazone linkers in 211At- and 125I-labeled closo-decaborate(2-) conjugates of Fab′ as a means of decreasing kidney retention

    PubMed Central

    Wilbur, D. Scott; Chyan, Ming-Kuan; Hamlin, Donald K.; Nguyen, Holly; Vessella, Robert L.

    2011-01-01

    Evaluation of monoclonal antibody (MAb) fragments (e.g. Fab′, Fab or engineered fragments) as cancer-targeting reagents for therapy with the α-particle emitting radionuclide astatine-211 (211At) has been hampered by low in vivo stability of the label and a propensity of these proteins localize to kidneys. Fortunately, our group has shown that the low stability of the 211At label, generally a meta- or para-[211At]astatobenzoyl conjugate, on MAb Fab′ fragments can be dramatically improved by use of closo-decaborate(2-) conjugates. However, the higher stability of radiolabeled MAb Fab′ conjugates appears to result in retention of the radioactivity in kidneys. This investigation was conducted to evaluate whether the retention of radioactivity in kidney might be decreased by the use of acid-cleavable hydrazone between the Fab′ and the radiolabeled closo-decaborate(2-) moiety. Five conjugation reagents containing sulfhydryl-reactive maleimide groups, a hydrazone functionality and a closo-decaborate(2-) moiety were prepared. In four of the five conjugation reagents, a discrete polyethylene glycol (PEG) linker was used, and one substituent adjacent to the hydrazone was varied (phenyl, benzoate, anisole or methyl) to provide varying acid-sensitivity. In the initial studies, the five maleimido-closo-decaborate(2-) conjugation reagents were radioiodinated (125I or 131I), then conjugated with an anti-PSMA Fab′ (107-1A4 Fab′). Biodistributions of the five radioiodinated Fab′ conjugates were obtained in nude mice at 1, 4 and 24 h post injection (pi). In contrast to closo-decaborate(2-) conjugated to 107-1A4 Fab′ through a non-cleavable linker, two conjugates containing either a benzoate or a methyl substituent on the hydrazone functionality displayed clearance rates from kidney, liver and spleen that were similar to those obtained with directly radioiodinated Fab′ (i.e. no conjugate). The maleimido-closo-decaborate(2-) conjugation reagent containing a benzoate

  8. [Spectroscopic studies on the binding of phenazopyridine hydrochloride and bovine serum albumin].

    PubMed

    Zhou, Hong; Chen, Chang-Yun; Xie, An-Jian

    2007-09-01

    The binding of phenazopyridine hydrochloride and bovine serum albumin under physiological conditions was studied by spectroscopic method. The quenching mechanism of the fluorescence of bovine serum albumin by phenazopyridine hydrochloride was studied with fluorescence and absorption spectroscopy. The binding constant Kb and the number of binding sites n were determined at different temperatures according to Scatchard equation, and the main binding force was discussed by thermodynamic equations. The effect of the drug on bovine serum albumin conformation was also studied by using synchronous fluorescence spectroscopy. The quenching mechanism of phenazopyridine hydrochloride to bovine serum albumin is static quenching and non-radiation energy transfer. The binding constants Kb at 15, 25 and 37 degrees C are 2.47 x 10(7), 9.15 x 10(6) and 4.36 x 10(6) mol(-1) with one binding site, respectively. The thermodynamic parameters of the reaction are DeltaH = -71.2 kJ x mol(-1), and DeltaS = 124.8 J x mol(-1) x K(-1). Binding phenazopyridine hydrochloride to bovine serum albumin is a spontaneous inter-molecular interaction in which entropy increases and Gibbs free energy decreases. The binding distance r between phenazopyridine hydrochloride and bovine serum albumin is 1.61 nm according to Forster theory of non-radiation energy transfer. The binding force is electrostatic interaction. Phenazopyridine hydrochloride can be deposited and transported by serum protein in vivo. Phenazopyridine hydrochloride does affect the serum protein conformation.

  9. Discovery of molecules for the treatment of neuropathic pain: synthesis, antiallodynic and antihyperalgesic activities of 5-(4-nitrophenyl)furoic-2-acid hydrazones.

    PubMed

    Yogeeswari, Perumal; Menon, Niloufer; Semwal, Arvind; Arjun, Muralidharan; Sriram, Dharmarajan

    2011-07-01

    Neuropathic pain is a chronic pain condition that occurs and persists in a heterogeneous group of etiologically different diseases characterized by a primary lesion or dysfunction of the peripheral or central nervous system. Current treatment options do not provide adequate relief for many patients and a significant number of the agents used have dose limiting side effects. During the course of our work on the synthesis and screening of new drugs for the treatment of neuropathic pain, we have identified 5-(4-nitrophenyl)furoic-2-acid hydrazones which showed significant antiallodynic and antihyperalgesic activities in a chronic constriction injury (CCI) model of neuropathic pain in rat. Synthesized compounds thus represent a promising lead for new drug development for the treatment of neuropathic pain. PMID:21536354

  10. NMR spectral study of some 2r,6c-diarylpiperidin-4-one (3'-hydroxy-2'-naphthoyl)hydrazones with special reference to γ-syn effect

    NASA Astrophysics Data System (ADS)

    Sylvestre, S.; Pandiarajan, K.

    2011-01-01

    1H and 13C NMR spectra have been recorded for 2r,6c-diarylpiperidin-4-one (3'-hydroxy-2'-naphthoyl)hydrazones 10-17 and 3,3-dimethyl-2r,6c-bis(p-methoxyphenyl)piperidin-4-one ( 5). For selected compounds 2D NMR spectra have been recorded. The spectral data along with those reported for related compounds are used to study the effect of a heteroatom X on the 13C chemical shift of a γ-carbon with X C α C β C γ torsional angle close to 0°, termed as γ-syn effect. Also γ-gauche and δ-effects of the alkyl groups at C-3 on the carbons of the aryl group at C-2 have been studied. The chemical shifts for the naphthalene ring are in accord with the mesomeric and steric effects of the carbonyl and hydroxy groups.

  11. An efficient PEGylated liposomal nanocarrier containing cell-penetrating peptide and pH-sensitive hydrazone bond for enhancing tumor-targeted drug delivery

    PubMed Central

    Ding, Yuan; Sun, Dan; Wang, Gui-Ling; Yang, Hong-Ge; Xu, Hai-Feng; Chen, Jian-Hua; Xie, Ying; Wang, Zhi-Qiang

    2015-01-01

    Cell-penetrating peptides (CPPs) as small molecular transporters with abilities of cell penetrating, internalization, and endosomal escape have potential prospect in drug delivery systems. However, a bottleneck hampering their application is the poor specificity for cells. By utilizing the function of hydration shell of polyethylene glycol (PEG) and acid sensitivity of hydrazone bond, we constructed a kind of CPP-modified pH-sensitive PEGylated liposomes (CPPL) to improve the selectivity of these peptides for tumor targeting. In CPPL, CPP was directly attached to liposome surfaces via coupling with stearate (STR) to avoid the hindrance of PEG as a linker on the penetrating efficiency of CPP. A PEG derivative by conjugating PEG with STR via acid-degradable hydrazone bond (PEG2000-Hz-STR, PHS) was synthesized. High-performance liquid chromatography and flow cytometry demonstrated that PHS was stable at normal neutral conditions and PEG could be completely cleaved from liposome surface to expose CPP under acidic environments in tumor. An optimal CPP density on liposomes was screened to guaranty a maximum targeting efficiency on tumor cells as well as not being captured by normal cells that consequently lead to a long circulation in blood. In vitro and in vivo studies indicated, in 4 mol% CPP of lipid modified system, that CPP exerted higher efficiency on internalizing the liposomes into targeted subcellular compartments while remaining inactive and free from opsonins at a maximum extent in systemic circulation. The 4% CPPL as a drug delivery system will have great potential in the clinical application of anticancer drugs in future. PMID:26491292

  12. An Eco-Friendly Ultrasound-Assisted Synthesis of Novel Fluorinated Pyridinium Salts-Based Hydrazones and Antimicrobial and Antitumor Screening.

    PubMed

    Rezki, Nadjet; Al-Sodies, Salsabeel A; Aouad, Mohamed R; Bardaweel, Sanaa; Messali, Mouslim; El Ashry, El Sayed H

    2016-01-01

    The present work reports an efficient synthesis of fluorinated pyridinium salts-based hydrazones under both conventional and eco-friendly ultrasound procedures. The synthetic approach first involves the preparation of halogenated pyridinium salts through the condensation of isonicotinic acid hydrazide (1) with p-fluorobenzaldehyde (2) followed by the nucleophilic alkylation of the resulting N-(4-fluorobenzylidene)isonicotinohydrazide (3) with a different alkyl iodide. The iodide counteranion of 5-10 was subjected to an anion exchange metathesis reaction in the presence of an excess of the appropriate metal salts to afford a new series of fluorinated pyridinium salts tethering a hydrazone linkage 11-40. Ultrasound irradiation led to higher yields in considerably less time than the conventional methods. The newly synthesized ILs were well-characterized with FT-IR, ¹H NMR, (13)C NMR, (11)B, (19)F, (31)P and mass spectral analyses. The ILs were also screened for their antimicrobial and antitumor activities. Within the series, the salts tethering fluorinated counter anions 11-13, 21-23, 31-33 and 36-38 were found to be more potent against all bacterial and fungal strains at MIC 4-8 µg/mL. The in vitro antiproliferative activity was also investigated against four tumor cell lines (human ductal breast epithelial tumor T47D, human breast adenocarcinoma MCF-7, human epithelial carcinoma HeLa and human epithelial colorectal adenocarcinoma Caco-2) using the MTT assay, which revealed that promising antitumor activity was exhibited by compounds 5, 12 and 14. PMID:27213367

  13. An Eco-Friendly Ultrasound-Assisted Synthesis of Novel Fluorinated Pyridinium Salts-Based Hydrazones and Antimicrobial and Antitumor Screening

    PubMed Central

    Rezki, Nadjet; Al-Sodies, Salsabeel A.; Aouad, Mohamed R.; Bardaweel, Sanaa; Messali, Mouslim; El Ashry, El Sayed H.

    2016-01-01

    The present work reports an efficient synthesis of fluorinated pyridinium salts-based hydrazones under both conventional and eco-friendly ultrasound procedures. The synthetic approach first involves the preparation of halogenated pyridinium salts through the condensation of isonicotinic acid hydrazide (1) with p-fluorobenzaldehyde (2) followed by the nucleophilic alkylation of the resulting N-(4-fluorobenzylidene)isonicotinohydrazide (3) with a different alkyl iodide. The iodide counteranion of 5–10 was subjected to an anion exchange metathesis reaction in the presence of an excess of the appropriate metal salts to afford a new series of fluorinated pyridinium salts tethering a hydrazone linkage 11–40. Ultrasound irradiation led to higher yields in considerably less time than the conventional methods. The newly synthesized ILs were well-characterized with FT-IR, 1H NMR, 13C NMR, 11B, 19F, 31P and mass spectral analyses. The ILs were also screened for their antimicrobial and antitumor activities. Within the series, the salts tethering fluorinated counter anions 11–13, 21–23, 31–33 and 36–38 were found to be more potent against all bacterial and fungal strains at MIC 4–8 µg/mL. The in vitro antiproliferative activity was also investigated against four tumor cell lines (human ductal breast epithelial tumor T47D, human breast adenocarcinoma MCF-7, human epithelial carcinoma HeLa and human epithelial colorectal adenocarcinoma Caco-2) using the MTT assay, which revealed that promising antitumor activity was exhibited by compounds 5, 12 and 14. PMID:27213367

  14. An efficient PEGylated liposomal nanocarrier containing cell-penetrating peptide and pH-sensitive hydrazone bond for enhancing tumor-targeted drug delivery.

    PubMed

    Ding, Yuan; Sun, Dan; Wang, Gui-Ling; Yang, Hong-Ge; Xu, Hai-Feng; Chen, Jian-Hua; Xie, Ying; Wang, Zhi-Qiang

    2015-01-01

    Cell-penetrating peptides (CPPs) as small molecular transporters with abilities of cell penetrating, internalization, and endosomal escape have potential prospect in drug delivery systems. However, a bottleneck hampering their application is the poor specificity for cells. By utilizing the function of hydration shell of polyethylene glycol (PEG) and acid sensitivity of hydrazone bond, we constructed a kind of CPP-modified pH-sensitive PEGylated liposomes (CPPL) to improve the selectivity of these peptides for tumor targeting. In CPPL, CPP was directly attached to liposome surfaces via coupling with stearate (STR) to avoid the hindrance of PEG as a linker on the penetrating efficiency of CPP. A PEG derivative by conjugating PEG with STR via acid-degradable hydrazone bond (PEG2000-Hz-STR, PHS) was synthesized. High-performance liquid chromatography and flow cytometry demonstrated that PHS was stable at normal neutral conditions and PEG could be completely cleaved from liposome surface to expose CPP under acidic environments in tumor. An optimal CPP density on liposomes was screened to guaranty a maximum targeting efficiency on tumor cells as well as not being captured by normal cells that consequently lead to a long circulation in blood. In vitro and in vivo studies indicated, in 4 mol% CPP of lipid modified system, that CPP exerted higher efficiency on internalizing the liposomes into targeted subcellular compartments while remaining inactive and free from opsonins at a maximum extent in systemic circulation. The 4% CPPL as a drug delivery system will have great potential in the clinical application of anticancer drugs in future. PMID:26491292

  15. 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.

  16. 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.

  17. 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.

  18. Synthesis and antitumor mechanisms of a copper(II) complex of anthracene-9-imidazoline hydrazone (9-AIH).

    PubMed

    Qin, Qi-Pin; Liu, Yan-Cheng; Wang, Hai-Lu; Qin, Jiao-Lan; Cheng, Feng-Jie; Tang, Shang-Feng; Liang, Hong

    2015-07-01

    A new anthracycline derivative, anthracene-9-imidazoline hydrazone (9-AIH), was synthesized and selected as an antitumor ligand to afford a copper(II) complex of 9-AIH, cis-[Cu(II)Cl2(9-AIH)] (1). Complex 1 was structurally characterized by IR, elemental analysis, ESI-MS and single crystal X-ray diffraction analysis. By MTT assay, it was revealed that 1 showed overall a higher in vitro cytotoxicity than 9-AIH towards a panel of human tumour cell lines, with IC50 values from 0.94–3.68 μM, in which the BEL-7404 cell line was the most sensitive to 1. By spectral analyses and gel electrophoresis, the DNA binding affinity of 9-AIH and 1 was determined. 9-AIH was suggested to bind with DNA in an intercalative mode, with a quenching constant of 1.04 × 10(4) M(−1) on the EB–DNA complex. While for 1, both intercalative and covalent binding modes were suggested. By flow cytometry, 1 was found to block the cell cycle of BEL-7404 cells in a dose-dependent mode, in which it induced the G2/M phase arrest at 0.5 μM and induced the S phase arrest at higher concentrations of 1.0 or 2.0 μM. From the cellular morphological observations under different fluorescence probe staining, a dose-dependent manner of 1 to induce cell apoptosis in the late stage was suggested. Comparatively, equivalent apoptotic cells, respectively, in the early and late stages were found when incubated with 2.0 μM of 9-AIH. The mitochondrial membrane potential measured by JC-1 staining and the ROS generation in cells detected using a DCFH-DA probe suggested that the cell apoptosis induced by 1 might undergo the ROS-related mitochondrial pathway. Accordingly, the mutant p53 expression was found to be suppressed and the caspase cascade (caspase-9/3) was consequently activated by 1. This action mechanism for 1 in the BEL-7404 cells was unique and was not found in the presence of 9-AIH under the same conditions, indicating their different antitumor mechanism. Furthermore, the in vivo acute toxicity of 1

  19. Nonlinear optical diglycine hydrochloride: Synthesis, crystal growth and structural characteristics

    NASA Astrophysics Data System (ADS)

    Narayana Moolya, B.; Darmaprakash, S. M.

    2006-07-01

    Diglycine hydrochloride (DGHCl), a new semiorganic nonlinear optical material with the molecular formula C 4H 11O 4Cl, was synthesized at ambient temperature. The solubility of DGHCl in water at varying temperatures was determined. Bulk single crystals were grown by the slow evaporation method at constant temperature. Powder X-ray diffraction patterns of the grown DGHCl were recorded and indexed. Functional groups present in the sample crystals were identified by FTIR spectral analysis. The chemical composition of the synthesized material was confirmed by CHN analysis. Thermal characteristics of DGHCl were determined from the TGA/DTA response curve. The Kurtz powder second harmonic generation (SHG) test showed potential for optical SHG. The UV cut-off of transmission was identified from the UV-VIS absorption spectra. The SHG of DGHCl is discussed on the basis of structural characteristics of the title compound.

  20. Peganine hydrochloride dihydrate an orally active antileishmanial agent.

    PubMed

    Khaliq, Tanvir; Misra, Pragya; Gupta, Swati; Reddy, K Papi; Kant, Ruchir; Maulik, P R; Dube, Anuradha; Narender, T

    2009-05-01

    Protozoic infections caused by genus Leishmania pose an enormous public health threat in developing countries, compounded by the toxicity and resistance to current therapies. Under the aegis of our ongoing program on drug discovery and development on antileishmanial agents from plants, we carried out bioassay guided fractionation on Peganum harmala seeds which resulted in the isolation of 1 as an antileishmanial agent. 2D-NMR spectral data and single crystal X-ray crystallography data indicated 1 as peganine hydrochloride in dihydrated form. The compound 1 exhibited in-vitro activity against both extracellular promastigotes as well as intracellular amastigotes residing within murine macrophages in Leishmania donovani. Furthermore, 1 also exhibited in-vivo activity, 79.6 (+/-8.07)% against established VL in hamsters at a dose of 100mg/kgb.wt. PMID:19339182

  1. Simple colorimetric method for determination of thiamine hydrochloride in pharmaceuticals.

    PubMed

    Sane, R T; Doshi, V J; Jukar, S; Joshi, S K; Sawant, S V; Pandit, U R

    1985-01-01

    A simple colorimetric method is described for the determination of thiamine hydrochloride (vitamin B1) in dosage forms. The method is based on measurement of a yellow complex formed when thiamine HCl is treated with p-methylaminophenol sulfate (Metol) under alkaline conditions. Compounds such as vitamins A, B2, B6, B12, C, D, and E, and niacinamide, citric acid, liquid glucose, calcium pantothenate, biotin, liver extract, and folic acid do not interfere in the reaction. Extracting the complex into chloroform before quantitation enhances the stability of the reaction product and removes interference of water-soluble colored constituents in syrup samples. Statistical validation shows that the method is precise and accurate. Results agree well with those obtained by other methods in the literature. PMID:3980419

  2. 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.

  3. Coated hydralazine hydrochloride beads for sustained release after oral administration.

    PubMed

    Mughal, M Akhlaq; Saripella, Kalyan K; Kouba, Chahinaz; Iqbal, Zafar; Neau, Steven H

    2013-09-01

    Hydralazine hydrochloride is an antihypertensive used alone or in combination with isosorbide nitrate for the treatment of congestive heart failure. Since control of blood pressure should be continuous, sustained release delivery of this drug is considered therapeutically beneficial. Core beads for oral administration of this drug were prepared by extrusion-spheronization. Using experimental design to define the coat that was applied, the core beads were coated using a fluid bed coater to different coat thickness with combinations of two commercially available products dissolved in a hydroalcoholic solvent. The coat is a film with a combination of ethylcellulose and hydroxypropylcellulose that can provide desirable release profiles. Visually spherical and rugged bead products were obtained. Two products were identified that exhibited essentially a zero order release profile following a 2-h lag time with release of greater than 70% of the drug over the next 10 h in simulated intestinal fluid.

  4. 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...

  5. The effect of tramadol hydrochloride on early life stages of fish.

    PubMed

    Sehonova, Pavla; Plhalova, Lucie; Blahova, Jana; Berankova, Petra; Doubkova, Veronika; Prokes, Miroslav; Tichy, Frantisek; Vecerek, Vladimir; Svobodova, Zdenka

    2016-06-01

    The aim of this study was to perform the fish embryo acute toxicity test (FET) on zebrafish (Danio rerio) and the early-life stage toxicity test on common carp (Cyprinus carpio) with tramadol hydrochloride. The FET was performed using the method inspired by the OECD guideline 236. Newly fertilized zebrafish eggs were exposed to tramadol hydrochloride at concentrations of 10; 50; 100 and 200μg/l for a period of 144h. An embryo-larval toxicity test on C. carpio was performed according to OECD guideline 210 also with tramadol hydrochloride at concentrations 10; 50; 100 and 200μg/l for a period of 32 days. Hatching was significantly influenced in both acute and subchronic toxicity assays. Subchronic exposure also influenced early ontogeny, both morphometric and condition characteristics and caused changes in antioxidant enzyme activity. The LOEC value was found to be 10μg/l tramadol hydrochloride.

  6. 78 FR 16685 - Impax Laboratories, Inc.; Withdrawal of Approval of Bupropion Hydrochloride Extended-Release...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-03-18

    ... HUMAN SERVICES Food and Drug Administration Impax Laboratories, Inc.; Withdrawal of Approval of Bupropion Hydrochloride Extended-Release Tablets, 300 Milligrams AGENCY: Food and Drug Administration, HHS. ACTION: Notice. SUMMARY: The Food and Drug Administration (FDA) is withdrawing approval of...

  7. The effect of tramadol hydrochloride on early life stages of fish.

    PubMed

    Sehonova, Pavla; Plhalova, Lucie; Blahova, Jana; Berankova, Petra; Doubkova, Veronika; Prokes, Miroslav; Tichy, Frantisek; Vecerek, Vladimir; Svobodova, Zdenka

    2016-06-01

    The aim of this study was to perform the fish embryo acute toxicity test (FET) on zebrafish (Danio rerio) and the early-life stage toxicity test on common carp (Cyprinus carpio) with tramadol hydrochloride. The FET was performed using the method inspired by the OECD guideline 236. Newly fertilized zebrafish eggs were exposed to tramadol hydrochloride at concentrations of 10; 50; 100 and 200μg/l for a period of 144h. An embryo-larval toxicity test on C. carpio was performed according to OECD guideline 210 also with tramadol hydrochloride at concentrations 10; 50; 100 and 200μg/l for a period of 32 days. Hatching was significantly influenced in both acute and subchronic toxicity assays. Subchronic exposure also influenced early ontogeny, both morphometric and condition characteristics and caused changes in antioxidant enzyme activity. The LOEC value was found to be 10μg/l tramadol hydrochloride. PMID:27208654

  8. 77 FR 14810 - Determination That DURANEST (Etidocaine Hydrochloride) Injection, 0.5%, and Five Other DURANEST...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-03-13

    ... From the Federal Register Online via the Government Publishing Office DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration Determination That DURANEST (Etidocaine Hydrochloride... Effectiveness AGENCY: Food and Drug Administration, HHS. ACTION: Notice. SUMMARY: The Food and...

  9. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 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...

  10. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 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...

  11. 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

    ... formaldehyde so that the initial reaction with hydroxylamine hydrochloride will produce sufficient hydrogen... prepared by K. K. Tutin and M. L. Foster, Tacoma R&D Laboratory, Georgia-Pacific Resins, Inc....

  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. 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.

  14. 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.

  15. 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.

  16. 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.

  17. 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. PMID:27484376

  18. Direct, preparative enantioselective chromatography of propranolol hydrochloride and thioridazine hydrochloride using carbon dioxide-based mobile phases.

    PubMed

    Geiser, F; Schultz, M; Betz, L; Shaimi, M; Lee, J; Champion, W

    1999-12-31

    In this paper, we describe the direct, preparative enantioselective chromatography of racemic (rac)-propranolol hydrochloride (HCI) and rac-thioridazine.HCl using Chiralpak AD chiral stationary phase and mobile phase systems containing carbon dioxide and methanol without the use of basic or acidic additives. Isolated fractions of propranolol.HCl were positively identified by mass spectrometry, Beilstein flame test, melting point, and chemical analysis to be HCI enantiomers of propranolol-HCl salts exhibited characteristic mass spectra peaks at 36 and 38 mass-to-charge ratio in the expected 3:1 isotopic ratio for the solute that were absent in the mass spectra for the free-base forms. To our knowledge, the direct, preparative enantioselective isolation of HCI enantiomeric salts of rac-propranolol and of rac-thioridazine have not been previously demonstrated and published. PMID:10674944

  19. Direct, preparative enantioselective chromatography of propranolol hydrochloride and thioridazine hydrochloride using carbon dioxide-based mobile phases.

    PubMed

    Geiser, F; Schultz, M; Betz, L; Shaimi, M; Lee, J; Champion, W

    1999-12-31

    In this paper, we describe the direct, preparative enantioselective chromatography of racemic (rac)-propranolol hydrochloride (HCI) and rac-thioridazine.HCl using Chiralpak AD chiral stationary phase and mobile phase systems containing carbon dioxide and methanol without the use of basic or acidic additives. Isolated fractions of propranolol.HCl were positively identified by mass spectrometry, Beilstein flame test, melting point, and chemical analysis to be HCI enantiomers of propranolol-HCl salts exhibited characteristic mass spectra peaks at 36 and 38 mass-to-charge ratio in the expected 3:1 isotopic ratio for the solute that were absent in the mass spectra for the free-base forms. To our knowledge, the direct, preparative enantioselective isolation of HCI enantiomeric salts of rac-propranolol and of rac-thioridazine have not been previously demonstrated and published.

  20. Increased mortality in groups of cattle administered the β-adrenergic agonists ractopamine hydrochloride and zilpaterol hydrochloride.

    PubMed

    Loneragan, Guy H; Thomson, Daniel U; Scott, H Morgan

    2014-01-01

    The United States Food and Drug Administration (FDA) approved two β-adrenergic agonists (βAA) for in-feed administration to cattle fed in confinement for human consumption. Anecdotal reports have generated concern that administration of βAA might be associated with an increased incidence of cattle deaths. Our objectives, therefore, were to a) quantify the association between βAA administration and mortality in feedlot cattle, and b) explore those variables that may confound or modify this association. Three datasets were acquired for analysis: one included information from randomized and controlled clinical trials of the βAA ractopamine hydrochloride, while the other two were observational data on zilpaterol hydrochloride administration to large numbers of cattle housed, fed, and cared for using routine commercial production practices in the U.S. Various population and time at-risk models were developed to explore potential βAA relationships with mortality, as well as the extent of confounding and effect modification. Measures of effect were relatively consistent across datasets and models in that the cumulative risk and incidence rate of death was 75 to 90% greater in animals administered the βAA compared to contemporaneous controls. During the exposure period, 40 to 50% of deaths among groups administered the βAA were attributed to administration of the drug. None of the available covariates meaningfully confounded the relationship between βAA and increased mortality. Only month of slaughter, presumably a proxy for climate, consistently modified the effect in that the biological association was generally greatest during the warmer months of the year. While death is a rare event in feedlot cattle, the data reported herein provide compelling evidence that mortality is nevertheless increased in response to administration of FDA-approved βAA and represents a heretofore unquantified adverse drug event.

  1. Increased Mortality in Groups of Cattle Administered the β-Adrenergic Agonists Ractopamine Hydrochloride and Zilpaterol Hydrochloride

    PubMed Central

    Loneragan, Guy H.; Thomson, Daniel U.; Scott, H. Morgan

    2014-01-01

    The United States Food and Drug Administration (FDA) approved two β-adrenergic agonists (βAA) for in-feed administration to cattle fed in confinement for human consumption. Anecdotal reports have generated concern that administration of βAA might be associated with an increased incidence of cattle deaths. Our objectives, therefore, were to a) quantify the association between βAA administration and mortality in feedlot cattle, and b) explore those variables that may confound or modify this association. Three datasets were acquired for analysis: one included information from randomized and controlled clinical trials of the βAA ractopamine hydrochloride, while the other two were observational data on zilpaterol hydrochloride administration to large numbers of cattle housed, fed, and cared for using routine commercial production practices in the U.S. Various population and time at-risk models were developed to explore potential βAA relationships with mortality, as well as the extent of confounding and effect modification. Measures of effect were relatively consistent across datasets and models in that the cumulative risk and incidence rate of death was 75 to 90% greater in animals administered the βAA compared to contemporaneous controls. During the exposure period, 40 to 50% of deaths among groups administered the βAA were attributed to administration of the drug. None of the available covariates meaningfully confounded the relationship between βAA and increased mortality. Only month of slaughter, presumably a proxy for climate, consistently modified the effect in that the biological association was generally greatest during the warmer months of the year. While death is a rare event in feedlot cattle, the data reported herein provide compelling evidence that mortality is nevertheless increased in response to administration of FDA-approved βAA and represents a heretofore unquantified adverse drug event. PMID:24621596

  2. 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.

  3. 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

  4. 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…

  5. Spectrophotometric estimation of tamsulosin hydrochloride by acid-dye method

    PubMed Central

    Shrivastava, Alankar; Saxena, Prachi; Gupta, Vipin B.

    2011-01-01

    A new spectrophotometric method for the estimation of tamsulosin hydrochloride in pharmaceutical dosage forms has been developed and validated. The method is based on reaction between drug and bromophenol blue and complex was measured at 421 nm. The slope, intercept and correlation coefficient was found to be 0.054, -0.020 and 0.999, respectively. Method was validated in terms of specificity, linearity, range, precision and accuracy. The developed method can be used to determine drug in both tablet and capsule formulations. Reaction was optimized using three parameters i.e., concentration of the dye, pH of the buffer, volume of the buffer and shaking time. Maximum stability of the chromophore was achieved by using pH 2 and 2 ml volume of buffer. Shaking time kept was 2 min and concentration of the dye used was 2 ml of 0.05% w/v solution. Method was validated in terms of linearity, precision, range, accuracy, LOD and LOQ and stochiometry of the method was also established using Mole ratio and Job's method of continuous variation. The dye benzonoid form (blue color) of dye ionized into quinonoid form (purple color) in presence of buffer and reacts with protonated form of drug in 1:1 ratio and forms an ion-pair complex (yellow color). PMID:23781431

  6. 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. PMID:25482587

  7. Lipomer of doxorubicin hydrochloride for enhanced oral bioavailability.

    PubMed

    Benival, Derajram M; Devarajan, Padma V

    2012-02-28

    The present study discusses design of doxorubicin hydrochloride (Dox) loaded lipid based nanocarrier (LIPOMER) for oral delivery. High entrapment (>90 %) and high loading (38.11 ± 0.37 %w/w) of hydrophilic Dox in lipid nanocarrier of polyglyceryl-6-distearate was achieved using poly(methyl vinyl ether-co-maleic anhydride) (Gantrez AN 119) and a modified nanoprecipitation method. Dox-LIPOMER revealed nanosize (314 ± 16.80 nm) and negative zeta potential (-25.00 ± 2.41 mV). Dox-LIPOMER exhibits sustained release in vitro and was influenced by ionic strength of dissolution medium. DSC and XRD studies suggested amorphous nature of Dox in LIPOMER. TEM revealed spherical morphology of Dox-LIPOMER. Dox-LIPOMER was stable up to 12 months at 25 °C/60 % RH. A 384 % enhancement in oral bioavailability compared to Dox solution was observed following Dox-LIPOMER administration at 10 mg/kg body weight. Superoxide dismutase (SOD), catalase (CAT) and malondialdehyde (MDA) assay data of heart and kidney tissues of rats treated with Dox-LIPOMER were comparable with untreated rats. Dox-LIPOMER represents a potential safe drug delivery system for oral administration. PMID:22155412

  8. Prednisone and vardenafil hydrochloride for refractory levamisole-induced vasculitis.

    PubMed

    Mandrell, Joshua; Kranc, Christina L

    2016-08-01

    Levamisole is an immunomodulatory drug that was previously used to treat various medical conditions, including parasitic infections, nephrotic syndrome, and colorectal cancer. Over the last few years, increasing amounts of levamisole have been used as an adulterant in cocaine. Levamisole-cut cocaine has become a concern because it is known to cause a necrotizing purpuric rash, autoantibody production, and life-threatening leukopenia. Mixed histologic findings of vasculitis and thrombosis are characteristic of levamisole-induced purpura. The recommended management of levamisole-induced vasculitis currently involves withdrawal of the culprit along with supportive treatment. We describe a patient with levamisole-induced vasculitis who continued to develop skin lesions despite self-reported cocaine cessation. Complete resolution of cutaneous disease occurred with the addition of oral prednisone and vardenafil hydrochloride, suggesting the possibility of a new treatment option in patients with refractory disease. In addition, we review the clinical presentation, disease course, diagnostic approach, laboratory findings, histology, and management of levamisole-induced vasculitis. The harmful effects of levamisole-cut cocaine are serious enough that public alerts have been issued to increase awareness. Clinicians should consider the possibility of levamisole exposure in cocaine users presenting with any combination of fever, neutropenia, and necrotic skin lesions, especially in acral areas including the ears. PMID:27622263

  9. 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.

  10. Solubility analysis of buspirone hydrochloride polymorphs: measurements and prediction.

    PubMed

    Sheikhzadeh, M; Rohani, S; Taffish, M; Murad, S

    2007-06-29

    In this paper, the solubility of two polymorphs of buspirone hydrochloride (BUS-HCl) in isopropanol, water and mixture of these two solvents has been investigated. The solubility of BUS-HCl Form 2 in water and isopropanol is higher than BUS-HCl Form 1. According to thermodynamic properties and Burger and Ramberger polymorphic rules (Bernstein, 2002), BUS-HCl Forms 1 and 2 are enantiotropes (Sheikhzadeh et al., 2007). Using the solubility data, transformation analysis has been done and the results confirm these two polymorphs are enantiotropes and Form 1 converts to Form 2 at 95 degrees C. The UNIQUAC binary adjustable parameters have been found and based on these parameters, the solubility of these molecules has been predicted and compared with the experimental solubility. The solubility prediction has been performed by using different UNIFAC equations for binary and ternary systems. The UNIQUAC and original UNIFAC showed better prediction capability. Different general solubility equations (GSE) have been used for estimation of solubility which works based on partial charge, hydrogen bond factors and partition coefficients. PMID:17317053

  11. 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.

  12. 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. PMID:15910814

  13. 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.

  14. 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

  15. Solubility analysis of buspirone hydrochloride polymorphs: measurements and prediction.

    PubMed

    Sheikhzadeh, M; Rohani, S; Taffish, M; Murad, S

    2007-06-29

    In this paper, the solubility of two polymorphs of buspirone hydrochloride (BUS-HCl) in isopropanol, water and mixture of these two solvents has been investigated. The solubility of BUS-HCl Form 2 in water and isopropanol is higher than BUS-HCl Form 1. According to thermodynamic properties and Burger and Ramberger polymorphic rules (Bernstein, 2002), BUS-HCl Forms 1 and 2 are enantiotropes (Sheikhzadeh et al., 2007). Using the solubility data, transformation analysis has been done and the results confirm these two polymorphs are enantiotropes and Form 1 converts to Form 2 at 95 degrees C. The UNIQUAC binary adjustable parameters have been found and based on these parameters, the solubility of these molecules has been predicted and compared with the experimental solubility. The solubility prediction has been performed by using different UNIFAC equations for binary and ternary systems. The UNIQUAC and original UNIFAC showed better prediction capability. Different general solubility equations (GSE) have been used for estimation of solubility which works based on partial charge, hydrogen bond factors and partition coefficients.

  16. 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.

  17. 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.

  18. 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

  19. Effects of ractopamine hydrochloride and zilpaterol hydrochloride supplementation on carcass cutability of calf-fed Holstein steers.

    PubMed

    Howard, S T; Woerner, D R; Vote, D J; Scanga, J A; Acheson, R J; Chapman, P L; Bryant, T C; Tatum, J D; Belk, K E

    2014-01-01

    Effects of ractopamine hydrochloride (RH) and zilpaterol hydrochloride (ZH) on saleable yield of carcass sides from calf-fed Holstein steers were evaluated using steers implanted with a progesterone (100 mg) plus estradiol benzoate (10 mg) implant followed by a terminal trenbolone acetate (200 mg) plus estradiol (40 mg) implant. Steers were blocked by weight into pens (n = 32) randomly assigned to one of four treatments: control, RH fed at 300 mg•steer(-1)/d(-1) (RH 300) or RH fed at 400 mg•steer(-1)/d(-1) (RH 400) the final 31 d of finishing, and ZH fed at 60 to 90 mg•steer(-1)/d(-1) (7.56 g/ton on a 100% DM basis) for 21 d with a 5 d withdrawal before harvest. Eight to nine carcass sides were randomly selected from each pen; carcass sides with excessive hide pulls, fat pulls or bruises were avoided. Cutout data were collected within a commercial facility using plant personnel to fabricate sides at a rate of one every 3 to 4 min into items typically merchandised by the facility. All lean, fat and bone were weighed and summed back to total chilled side weight with a sensitivity of ± 2% to be included in the data set. Compared to controls, β-agonists increased saleable yield of whole-muscle cuts by 0.61%, 0.86% and 1.95% for RH 300, RH 400 and ZH, respectively (P < 0.05). Percent fat was less in carcasses from the ZH treatment compared to controls (P < 0.05); however, this difference was not observed between RH treatments and controls (P > 0.05). Percent bone was less in the ZH treatment due to increased muscle (P < 0.05). The percent of chilled side weight comprised of trimmings was unchanged between treatments, but on a 100% lean basis, RH 400 and ZH increased trim yields (P < 0.05). Analysis of saleable yield by primal showed a fundamental shift in growth and development. Beta-agonists caused a shift in proportion of saleable yield within individual primals, with a greater portion produced from the hindquarter relative to the forequarter, specifically in

  20. Design and Development of Polyethylene Oxide Based Matrix Tablets for Verapamil Hydrochloride

    PubMed Central

    Vidyadhara, S.; Sasidhar, R. L. C.; Nagaraju, R.

    2013-01-01

    In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil hydrochloride. Verapamil hydrochloride was formulated as oral controlled release matrix tablets by using the polyethylene oxides (Polyox WSR 303). The aim of this study was to investigate the influence of polymer level and type of fillers namely lactose (soluble filler), swellable filler (starch 1500), microcrystalline cellulose and dibasic calcium phosphate (insoluble fillers) on the release rate and mechanism of release for verapamil hydrochloride from matrix tablets prepared by direct compression process. Higher polymeric content in the matrix decreased the release rate of drug. On the other hand, replacement of lactose with anhydrous dibasic calcium phosphate and microcrystalline cellulose has significantly retarded the release rate of verapamil hydrochloride. Biopharmaceutical evaluation of satisfactory formulations were also carried out on New Zealand rabbits and parameters such as maximum plasma concentration, time to reach peak plasma concentration, area under the plasma concentration time curve(0-t) and area under first moment curve(0-t) were determined. In vivo pharmacokinetic study proves that the verapamil hydrochloride from matrix tablets showed prolonged release and were be able to sustain the therapeutic effect up to 24 h. PMID:24019567

  1. In vitro effects of Pilocarpus microphyllus extracts and pilocarpine hydrochloride on Rhipicephalus (Boophilus) microplus.

    PubMed

    Castro, Karina Neoob de Carvalho; Lima, David Fernandes; Wolschick, Dolores; Andrade, Ivanilza Moreira de; Santos, Raimunda Cardoso Dos; Santos, Francisco José de Seixas Dos; Veras, Leiz Maria Costa; Costa-Júnior, Lívio Martins

    2016-06-01

    The aim of this study was to assess the activity of aqueous (AE) and ethanolic extracts (EE) and pilocarpine hydrochloride, which were extracted and isolated from Pilocarpus microphyllus (Jaborandi), respectively, on Rhipicephalus (Boophilus) microplus. High performance liquid chromatography (HPLC) was performed to quantify these compounds. Larval packet and adult immersion tests were conducted with different concentrations. Five AE and EE concentrations, ranging from 6.2 to 100.0 mg mL-1, and six concentrations of pilocarpine hydrochloride, ranging from 0.7 to 24.0 mg mL-1, were tested. The lethal concentration (LC50) of each extract for larvae and engorged females was calculated through Probit analysis. The concentration of pilocarpine hydrochloride obtained from the EE and the AE was 1.3 and 0.3% (m/m), respectively. Pilocarpine hydrochloride presented the highest acaricidal activity on larvae (LC50 2.6 mg mL-1) and engorged females (LC50 11.8 mg mL-1) of R.(B.) microplus, followed by the EE which presented LC50 of 56.4 and 15.9 mg mL-1, for larvae and engorged females, respectively. Such results indicate that pilocarpine hydrochloride has acaricidal activity, and may be the primary compound responsible for this activity by P. microphyllus EE. PMID:27276670

  2. In vitro effects of Pilocarpus microphyllus extracts and pilocarpine hydrochloride on Rhipicephalus (Boophilus) microplus.

    PubMed

    Castro, Karina Neoob de Carvalho; Lima, David Fernandes; Wolschick, Dolores; Andrade, Ivanilza Moreira de; Santos, Raimunda Cardoso Dos; Santos, Francisco José de Seixas Dos; Veras, Leiz Maria Costa; Costa-Júnior, Lívio Martins

    2016-06-01

    The aim of this study was to assess the activity of aqueous (AE) and ethanolic extracts (EE) and pilocarpine hydrochloride, which were extracted and isolated from Pilocarpus microphyllus (Jaborandi), respectively, on Rhipicephalus (Boophilus) microplus. High performance liquid chromatography (HPLC) was performed to quantify these compounds. Larval packet and adult immersion tests were conducted with different concentrations. Five AE and EE concentrations, ranging from 6.2 to 100.0 mg mL-1, and six concentrations of pilocarpine hydrochloride, ranging from 0.7 to 24.0 mg mL-1, were tested. The lethal concentration (LC50) of each extract for larvae and engorged females was calculated through Probit analysis. The concentration of pilocarpine hydrochloride obtained from the EE and the AE was 1.3 and 0.3% (m/m), respectively. Pilocarpine hydrochloride presented the highest acaricidal activity on larvae (LC50 2.6 mg mL-1) and engorged females (LC50 11.8 mg mL-1) of R.(B.) microplus, followed by the EE which presented LC50 of 56.4 and 15.9 mg mL-1, for larvae and engorged females, respectively. Such results indicate that pilocarpine hydrochloride has acaricidal activity, and may be the primary compound responsible for this activity by P. microphyllus EE. PMID:27334829

  3. Design and development of polyethylene oxide based matrix tablets for verapamil hydrochloride.

    PubMed

    Vidyadhara, S; Sasidhar, R L C; Nagaraju, R

    2013-03-01

    In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil hydrochloride. Verapamil hydrochloride was formulated as oral controlled release matrix tablets by using the polyethylene oxides (Polyox WSR 303). The aim of this study was to investigate the influence of polymer level and type of fillers namely lactose (soluble filler), swellable filler (starch 1500), microcrystalline cellulose and dibasic calcium phosphate (insoluble fillers) on the release rate and mechanism of release for verapamil hydrochloride from matrix tablets prepared by direct compression process. Higher polymeric content in the matrix decreased the release rate of drug. On the other hand, replacement of lactose with anhydrous dibasic calcium phosphate and microcrystalline cellulose has significantly retarded the release rate of verapamil hydrochloride. Biopharmaceutical evaluation of satisfactory formulations were also carried out on New Zealand rabbits and parameters such as maximum plasma concentration, time to reach peak plasma concentration, area under the plasma concentration time curve(0-t) and area under first moment curve(0-t) were determined. In vivo pharmacokinetic study proves that the verapamil hydrochloride from matrix tablets showed prolonged release and were be able to sustain the therapeutic effect up to 24 h. PMID:24019567

  4. Reactivity Differences between [alpha, beta]-Unsaturated Carbonyls and Hydrazones Investigated by Experimental and Theoretical Electron Density and Electron Localizability Analyses

    SciTech Connect

    Grabowsky, Simon; Weber, Manuela; Jayatilaka, Dylan; Chen, Yu-Sheng; Grabowski, Matthias T.; Brehme, Rainer; Hesse, Malte; Schirmeister, Tanja; Luger, Peter

    2012-10-11

    It is still a challenge to predict a compound's reactivity from its ground-state electronic nature although Bader-type topological analyses of the electron density (ED) and electron localizability indicator (ELI) give detailed and useful information on electron concentration and electron-pair localization, respectively. Both ED and ELI can be obtained from theoretical calculations as well as high-resolution X-ray diffraction experiments. Besides ED and ELI descriptors, the delocalization index is used here; it is likewise derived from theoretical calculations as well as from experimental X-ray results, but in the latter case, demonstrated here for the first time. We investigate {alpha},{beta}-unsaturated carbonyl and hydrazone compounds because resonance exhibited by these compounds in the electronic ground-state determines their reactive behavior. The degree of resonance as well as the reactivity contrast are quantified with the electronic descriptors. Moreover, competitive mesomeric substituent effects are studied using the two biologically important compounds acrolein and acrylamide. The reactivity differences predicted from the analyses are in line with the known reactivity of these compounds in organic synthesis. Hence, the capability of the ED and ELI for rationalizing and predicting different and competing substituent effects with respect to reactivity is demonstrated.

  5. Interaction of Di-2-pyridylketone 2-pyridine Carboxylic Acid Hydrazone and Its Copper Complex with BSA: Effect on Antitumor Activity as Revealed by Spectroscopic Studies.

    PubMed

    Li, Cuiping; Huang, Tengfei; Fu, Yun; Liu, Youxun; Zhou, Sufeng; Qi, Zhangyang; Li, Changzheng

    2016-04-28

    The drug, di-2-pyridylketone-2-pyridine carboxylic acid hydrazone (DPPCAH) and its copper complex (DPPCAH-Cu) exhibit significant antitumor activity. However, the mechanism of their pharmacological interaction with the biological molecule bovine serum albumin (BSA) remains poorly understood. The present study elucidates the interactions between the drug and BSA through MTT assays, spectroscopic methods and molecular docking analysis. Our results indicate that BSA could attenuate effect on the cytotoxicity of DPPCAH, but not DPPCAH-Cu. Data from fluorescence quenching measurements demonstrated that both DPPCAH and DPPCAH-Cu could bind to BSA, with a reversed effect on the environment of tryptophan residues in polarity. CD spectra revealed that the DPPCAH-Cu exerted a slightly stronger effect on the secondary structure of BSA than DPPCAH. The association constant of DPPCAH with BSA was greater than that of DPPCAH-Cu. Docking studies indicated that the binding of DPPCAH to BSA involved a greater number of hydrogen bonds compared to DPPCAH-Cu. The calculated distances between bound ligands and tryptophans in BSA were in agreement with fluorescence resonance energy transfer results. Thus, the binding affinity of the drug (DPPCAH or DPPCAH-Cu) with BSA partially contributes to its antitumor activity; the greater the drug affinity is to BSA, the less is its antitumor activity.

  6. Effect of the protonophore carbonyl cyanide-p-trifluoromethoxyphenyl-hydrazon on the glutamate release from rat brain nerve terminals under altered gravity conditions.

    NASA Astrophysics Data System (ADS)

    Borisova, T.; Krisanova, N.

    L-glutamate acts within the mammalian central nervous system as the predominant excitatory neurotransmitter and as a potent neurotoxin The balance between these physiological and pathological actions of glutamate is thought to be kept in check by the rapid removal of the neurotransmitter from the synaptic cleft The majority of uptake is mediated by the high-affinity Na -dependent glutamate transporters Depolarization leads to stimulation of glutamate efflux mediated by reversal of the high-affinity glutamate transporters The effects of the protonophore carbonyl cyanide-p-trifluoromethoxyphenyl-hydrazon FCCP on the glutamate release from isolated nerve terminals rat brain synaptosomes were investigated in control and after centrifuge-induced hypergravity rats were rotated in a long-arm centrifuge at ten-G during one-hour period The treatment of synaptosomes with 1 mu M FCCP during 11 min resulted in the increase in L- 14 C glutamate release by 23 0 pm 2 3 of total accumulated synaptosomal label in control animals and 24 0 pm 2 3 animals subjected to hypergravity FCCP evoked release of L- 14 C glutamate from synaptosomes was not altered in animals exposed to hypergravity as compared to control Glutamate transport is of electrogenic nature and thus depends on the membrane potential The high-KCl stimulated L- 14 C glutamate release in Ca 2 -free media occurred due to reversal of the glutamate transporters Carrier --mediated release of L- 14 C glutamate 6 min slightly increased as a result of

  7. Interaction of Di-2-pyridylketone 2-pyridine Carboxylic Acid Hydrazone and Its Copper Complex with BSA: Effect on Antitumor Activity as Revealed by Spectroscopic Studies.

    PubMed

    Li, Cuiping; Huang, Tengfei; Fu, Yun; Liu, Youxun; Zhou, Sufeng; Qi, Zhangyang; Li, Changzheng

    2016-01-01

    The drug, di-2-pyridylketone-2-pyridine carboxylic acid hydrazone (DPPCAH) and its copper complex (DPPCAH-Cu) exhibit significant antitumor activity. However, the mechanism of their pharmacological interaction with the biological molecule bovine serum albumin (BSA) remains poorly understood. The present study elucidates the interactions between the drug and BSA through MTT assays, spectroscopic methods and molecular docking analysis. Our results indicate that BSA could attenuate effect on the cytotoxicity of DPPCAH, but not DPPCAH-Cu. Data from fluorescence quenching measurements demonstrated that both DPPCAH and DPPCAH-Cu could bind to BSA, with a reversed effect on the environment of tryptophan residues in polarity. CD spectra revealed that the DPPCAH-Cu exerted a slightly stronger effect on the secondary structure of BSA than DPPCAH. The association constant of DPPCAH with BSA was greater than that of DPPCAH-Cu. Docking studies indicated that the binding of DPPCAH to BSA involved a greater number of hydrogen bonds compared to DPPCAH-Cu. The calculated distances between bound ligands and tryptophans in BSA were in agreement with fluorescence resonance energy transfer results. Thus, the binding affinity of the drug (DPPCAH or DPPCAH-Cu) with BSA partially contributes to its antitumor activity; the greater the drug affinity is to BSA, the less is its antitumor activity. PMID:27136517

  8. [Synthesis and antituberculosis activity of the derivatives of glycoside steviolbioside from the plant Stevia rebaudiana and diterpenoid isosteviol containing hydrazone, hydrazide and pyridinoyl moieties].

    PubMed

    Kataev, V E; Strobykina, I Iu; Andreeva, O V; Garifullin, B F; Sharipova, R R; Mironov, V F; Chestnova, R V

    2011-01-01

    Conjugates of antitubercular drug Isoniazid (hydrazide of isonicotinic acid), nicotinic and alpha-picolinic acid hydrazides and glycoside steviolbioside from the plant Stevia rebaudiana as well as the product of its acid hydrolysis, diterpenoid isosteviol, were synthesized. Besides, isosteviol hydrazide and hydrazone derivatives as well as conjugates containing two isosteviol moieties connected by dihydrazide linker were also obtained. Both initial compounds and their synthetic derivatives inhibit the growth of Mycobacterium tuberculosis (H37Rv in vitro). The minimum concentration at which the growth of M. tuberculosis was inhibited by 100% (MIC) for stevioside and steviolbioside equals 7.5 and 3.8 microg/mL, respectively. MIC values for conjugates of the hydrazides of pyridine carbonic acids and steviolbioside as well as isosteviol are in the ranges 5-10 and 10-20 microg/mL, respectively. Maximum inhibitory effect against M. tuberculosis showed the conjugates of isosteviol and adipic acid dihydrazide (MIC values ranged from 1.7 to 3.1 microg/mL). Antitubercular activity of the compounds studied is higher than the activity of antitubercular drug Pyrizanamide (MIC = 12.5-20 microg/mL) but lower than the activity of antitubercular drug Isoniazid (MIC = 0.02-0.04 microg/mL). PMID:22096997

  9. Tautomeric effect of hydrazone Schiff bases in tetranuclear Cu(II) complexes: magnetism and catalytic activity towards mild hydrocarboxylation of alkanes.

    PubMed

    Sutradhar, Manas; Kirillova, Marina V; Guedes da Silva, M Fátima C; Liu, Cai-Ming; Pombeiro, Armando J L

    2013-12-21

    Three new tetranuclear copper(II) complexes [Cu(HL(1))]4·4EtOH (1·4EtOH), [Cu(HL(2))]4 (2) and [Cu(H2L(3))]4(NO3)4·2H2O (3·2H2O) have been synthesized using three different hydrazone Schiff base ligands derived from the condensation of the aromatic acid hydrazides 2-hydroxybenzo-, 2-aminobenzo- or benzo-hydrazide, with 2,3-dihydroxybenzaldehyde. Complexes 1 and 3 have been characterized by single crystal X-ray diffraction analysis. The coordinating behaviour of the ligand depends on the nature of the ortho substituent present in the hydrazide moiety. The ligands bearing a strong electron donating group (by resonance) in the ortho position undergo complexation via enolization and deprotonation, whereas the absence of such an effect leads to complexation via the keto form, and two different types of tetranuclear Cu(II) clusters, viz. open-cubane and cubane, are obtained. Variable temperature magnetic susceptibility measurements of complexes 1 and 3 have been carried out to examine the nature of magnetic interaction between the Cu(II) centres. All the three complexes (1-3) act as good catalyst precursors towards mild hydrocarboxylation of linear and cyclic alkanes into carboxylic acids in water-acetonitrile medium. PMID:24068161

  10. Mono- and binuclear copper(II) complexes of new hydrazone ligands derived from 4,6-diacetylresorcinol: Synthesis, spectral studies and antimicrobial activity

    NASA Astrophysics Data System (ADS)

    Shebl, Magdy; El-ghamry, Mosad A.; Khalil, Saied M. E.; Kishk, Mona A. A.

    Two new hydrazone ligands, H2L1 and H2L2, were synthesized by the condensation of 4,6-diacetylresorcinol with 3-hydrazino-5,6-diphenyl-1,2,4-triazine and isatin monohydrazone, respectively. The structures of the ligands were elucidated by elemental analyses, IR, 1H NMR, electronic and mass spectra. Reactions of the ligands with several copper(II) salts, including AcO-, NO3-, SO42-, Cl- and Br- afforded mono- and binuclear metal complexes. Also, the ligands were allowed to react with Cu(II) ion in the presence of a secondary ligand (L‧) [N,O-donor; 8-hydroxyquinoline, N,N-donor; 1,10-phenanthroline or O,O-donor; benzoylacetone]. Characterization and structure elucidation of the prepared complexes were achieved by elemental and thermal analyses, IR, electronic, mass and ESR spectra as well as conductivity and magnetic susceptibility measurements. The ESR spin Hamiltonian parameters of some complexes were calculated. The spectroscopic data showed that the H2L1 ligand acts as a neutral or monobasic tridentate ligand while the H2L2 ligand acts as a bis(monobasic tridentate) ligand. The coordination sites with the copper(II) ion are phenolic oxygen, azomethine nitrogen and triazinic nitrogen (H2L1 ligand) or isatinic oxygen (H2L2 ligand). The metal complexes exhibited octahedral and square planar geometrical arrangements depending on the nature of the anion. The ligands and some metal complexes showed antimicrobial activity.

  11. Synthesis and biological evaluation of (acyl)hydrazones and thiosemicarbazones obtained via in situ condensation of iminium salts with nitrogen-containing nucleophiles.

    PubMed

    Caneva, Chiara; Alfei, Silvana; De Maria, Monica; Ibba, Cristina; Delogu, Ilenia; Spallarossa, Andrea; Loddo, Roberta

    2015-11-01

    An unprecedented, highly convergent, high-yielding, one-pot synthesis of (acyl)hydrazones and thiosemicarbazones was carried out by the in situ condensation of isolable iminium chlorides of imidazolidin-2-(thio)one, tetrahydropyrimidin-2-thione and indole derivatives with nitrogen nucleophiles in the presence of a base. The developed reaction procedure is largely advantageous. It is highly parallelizable, no intermediates need to be isolated and minimal sample handling is required during the purification steps. Some relevant reaction parameters including reaction temperature and p[Formula: see text] of the base are discussed. NMR analysis was carried out to assess the stereochemistry of the obtained compounds. The stereochemical outcome of the reaction was found to be affected by the nature of the nitrogen-containing nucleophile being the majority of the derivatives isolated as single geometric isomers. The cytotoxicity and antiviral activities of the prepared compounds have been preliminary assessed. In cell-based screenings some of the derivatives proved to be cytotoxic at low micromolar concentrations and interesting anti-Reo-1 properties have been detected. PMID:26077842

  12. 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.

  13. The effects of clomipramine hydrochloride in cats with psychogenic alopecia: a prospective study.

    PubMed

    Mertens, Petra A; Torres, Sheila; Jessen, Carl

    2006-01-01

    A double-blind, placebo-controlled clinical trial was conducted to determine the efficacy of clomipramine hydrochloride in cats with psychogenic alopecia. Twenty-five cats were randomly assigned to receive clomipramine hydrochloride (0.5 mg/kg orally q 24 hours) or placebo for 56 days. Eleven cats in each group completed the trial. The results of this study showed that clomipramine hydrochloride failed to demonstrate significant changes in the number of grooming bouts, hair regrowth, and the area of alopecia in cats with psychogenic alopecia when compared to a placebo. It was uncertain whether these results reflected a lack of drug efficacy, insufficient treatment duration, or an insufficient number of cases enrolled.

  14. 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.

  15. 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.

  16. 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.

  17. Thermal Analysis Investigation of Dapoxetine and Vardenafil Hydrochlorides using Molecular Orbital Calculations

    PubMed Central

    Attia, Ali Kamal; Souaya, Eglal R.; Soliman, Ethar A.

    2015-01-01

    Purpose: Thermal analysis techniques have been used to study the thermal behavior of dapoxetine and vardenafil hydrochlorides and confirmed using semi-empirical molecular orbital calculations. Methods: Thermogravimetric analysis, derivative thermogravimetry, differential thermal analysis and differential scanning calorimetry were used to determine the thermal behavior and purity of the drugs under investigation. Thermodynamic parameters such as activation energy, enthalpy, entropy and Gibbs free energy were calculated. Results: Thermal behavior of DAP and VAR were confirmed using by semi-empirical molecular orbital calculations. The purity values were found to be 99.97% and 99.95% for dapoxetine and vardenafil hydrochlorides, respectively. The purity of dapoxetine and vardenafil hydrochlorides is similar to that found by reported methods according to DSC data. Conclusion: Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs. PMID:26819925

  18. [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.

  19. Residual amount of vancomycin hydrochloride in vials after use.

    PubMed

    Yamasaki, Hirofumi; Oie, Shigeharu; Miyano, Naoyuki; Furukawa, Hiroyuki

    2013-08-01

    We macroscopically observed vials of vancomycin hydrochloride (VCM) for injection (0.5 g/vial) dissolved in various solvents, and determined the presence or absence of residual VCM crystals. In addition, the residual VCM in vials after use was measured using a bioassay. In vials evaluated after use, the percentage of vials in which VCM crystals were macroscopically confirmed, the mean residual amount of VCM in the vials (residual %), and the percentage of vials with ≥50 mg (10 %) of residual VCM were 28.1 %, 15.0 ± 7.5 mg (3.0 %), and 0 %, respectively, after the dissolution of a single VCM vial in 10 ml of distilled water for injection (n = 57); 63.8 %, 30.2 ± 19.1 mg (6.0 %), and 16.1 %, respectively, after the dissolution of a single VCM vial in 100 ml of physiological saline (n = 224); and 72.2 %, 38.5 ± 28.0 mg (7.7 %), and 33.3 %, respectively, after the dissolution of two VCM vials in 100 ml of physiological saline (n = 18). The mean residual VCM amount was greater when using physiological saline than when using distilled water for injection as a solvent. These results show the need to follow the dissolution method described in the package insert, which calls for the addition of 10 ml of distilled water for injection to each 0.5 g VCM vial.

  20. Design, Optimization, and Evaluation of Lurasidone Hydrochloride Nanocrystals.

    PubMed

    Shah, Sunny; Parmar, Bhavin; Soniwala, Moinuddin; Chavda, Jayant

    2016-10-01

    The present investigation was carried out to design, optimize, and evaluate lurasidone hydrochloride nanocrystals for improving its solubility and dissolution characteristics. Nanocrystals were prepared by media milling technique using zirconium oxide beads with 0.1 mm diameter. Various stabilizers, viz. poloxamer 188, PVP K30, SLS, HPMC E15, and PVP S 630 D, were evaluated to stabilize the nanocrystals. The Pareto chart obtained through Plackett-Burman screening design revealed that HPMC E 15 showed the highest standardized effect (p value <0.05) on percent dissolution efficiency at 2 min. In subsequent studies, a 3(2) factorial design was employed to quantify the effect of two independent variables, namely amount of stabilizer and milling time on predetermined response variables mean particle size, saturation solubility, and percent dissolution efficiency at 2 min. Statistical analysis of the factorial design revealed that all predetermined response variables were significantly dependent (p value <0.05) on the independent variables. The observed response of the optimized batch prepared as per the desirability function was in close agreement with predicted response, and mathematical model generated was validated. The optimized batch was lyophilized, and X-ray powder diffraction studies indicated that there was no substantial change in crystallinity of the drug. The optimized formulation showed mean particle size of 228 nm and released almost all the drug within first 5 min. Since the crystallinity of the drug is maintained, improvement in saturation solubility and dissolution efficiency could be attributed to decrease in mean particle size of the drug. PMID:26586537

  1. Design, Optimization, and Evaluation of Lurasidone Hydrochloride Nanocrystals.

    PubMed

    Shah, Sunny; Parmar, Bhavin; Soniwala, Moinuddin; Chavda, Jayant

    2016-10-01

    The present investigation was carried out to design, optimize, and evaluate lurasidone hydrochloride nanocrystals for improving its solubility and dissolution characteristics. Nanocrystals were prepared by media milling technique using zirconium oxide beads with 0.1 mm diameter. Various stabilizers, viz. poloxamer 188, PVP K30, SLS, HPMC E15, and PVP S 630 D, were evaluated to stabilize the nanocrystals. The Pareto chart obtained through Plackett-Burman screening design revealed that HPMC E 15 showed the highest standardized effect (p value <0.05) on percent dissolution efficiency at 2 min. In subsequent studies, a 3(2) factorial design was employed to quantify the effect of two independent variables, namely amount of stabilizer and milling time on predetermined response variables mean particle size, saturation solubility, and percent dissolution efficiency at 2 min. Statistical analysis of the factorial design revealed that all predetermined response variables were significantly dependent (p value <0.05) on the independent variables. The observed response of the optimized batch prepared as per the desirability function was in close agreement with predicted response, and mathematical model generated was validated. The optimized batch was lyophilized, and X-ray powder diffraction studies indicated that there was no substantial change in crystallinity of the drug. The optimized formulation showed mean particle size of 228 nm and released almost all the drug within first 5 min. Since the crystallinity of the drug is maintained, improvement in saturation solubility and dissolution efficiency could be attributed to decrease in mean particle size of the drug.

  2. 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).

  3. Potentiometric sensor for the high throughput determination of tetramisole hydrochloride.

    PubMed

    Gupta, Vinod Kumar; Singh, Ashok Kumar; Gupta, Barkha

    2007-08-01

    The electrochemical response characteristics of poly(vinyl)chloride (PVC) based membrane sensors for determination of tetramisole hydrochloride (TmCl) is described. The membranes of these electrodes consist of tetramisole-tetraphenyl borate (Tm-TPB), chlorophenyl borate (Tm-ClPB), and phosphotungstate (Tm(3)-PT) ion associations dispersed in a PVC matrix with dibutylpthalate as a plasticizer. The electrodes were fully characterized in terms of composition, life span, usable pH range, and working concentration range and ionic strength. The electrodes showed Nernstian response over the concentration ranges of 7.4 x 10(-7) to 1.0 x 10(-2) M, 1.7 x 10(-6) to 1.0 x 10(-2) M, and 5.6 x 10(-6) to 1.0 x 10(-2) M TmCl, respectively, and were applied to the potentiometric determination of tetramisole ion in pure solutions and pharmaceutical preparations. The potentiometric determination was also used in the determination of tetramisole in pharmaceutical preparations in four batches of different expiration dates. The electrodes exhibited good selectivity for TmCl with respect to a large number of excipients such as inorganic cations, organic cations, amino acids, and sugars. The solubility product of the ion-pair and the formation constant of the precipitation reaction leading to the ion-pair formation were determined conductometrically. The new potentiometric method offers the advantages of high-throughput determination, simplicity, accuracy, automation feasibility, and applicability to turbid and colored sample solutions. PMID:17979641

  4. Three cases of nalbuphine hydrochloride dependence associated with anabolic steroid use.

    PubMed Central

    McBride, A J; Williamson, K; Petersen, T

    1996-01-01

    Three case reports are presented of nalbuphine hydrochloride dependence meeting DSM IIIR and ICD10 criteria for opioid dependence. Nalbuphine hydrochloride is being obtained from illicit sources and used by those using performance enhancing drugs. In some cases this leads to opioid dependence. There is a potential risks of crossover between the misuse of drugs of performance and the misuse of psychoactive drugs by injection. Further research into the dependence potential of nalbuphine and the extent of the crossover between steroid misuse and other psychoactive drug misuse is required. The legal status of nalbuphine should be reviewed in the light of its availability on the black market. PMID:8665124

  5. 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.

  6. The compatibility and stability of octreotide acetate in the presence of diamorphine hydrochloride in polypropylene syringes.

    PubMed

    Fielding, H; Kyaterekera, N; Skellern, G G; Tettey, J N; McDade, J R; Msuya, Z; Watson, D G; Urie, J

    2000-05-01

    Varying concentrations of octreotide acetate (Sandostatin) and diamorphine hydrochloride were prepared and stored in polypropylene syringes at 37 degrees C in the dark. The solutions were analysed for octreotide acetate content using a validated HPLC method at regular intervals over a 48-h period. The results indicate that octreotide acetate remains stable in the presence of diamorphine hydrochloride at 37 degrees C for 24 h. In addition, the solutions prepared maintained their clarity, with no signs of precipitation upon visual examination under normal light conditions.

  7. LC determination of octreotide acetate in compound formulations of Sandostatin and diamorphine hydrochloride.

    PubMed

    Kyaterekera, N; Tettey, J N; Skellern, G G; Watson, D G; Urie, J; McDade, J R; Fielding, H

    1999-11-01

    The determination of octreotide acetate in compound formulations of Sandostatin and diamorphine hydrochloride by RP-LC is described. Octreotide acetate, diamorphine hydrochloride and their respective degradants, [des-Thr-ol8]-octreotide and 6-O-acetylmorphine, were baseline resolved using a Lichrospher-60 RP-select B column with a mobile phase composition of acetonitrile/phosphate buffer (pH 7.4, 20 mM) (35:65 v/v) with UV detection at 210 nm. The method is simple, selective, precise and suitable for the determination of octreotide acetate in admixture.

  8. [On the crystallisation of amphetaminil base into its hydrochloride salt (author's transl)].

    PubMed

    Klosa, J

    1975-01-01

    In an aqueous medium in the presence of hydrochloric acid, amphetaminil (AN 1¿R) directly crystallises into the needle forming hydrochloride. The hydrochloride and base of the substance AN 1 have the same degree of insolubility in water. Such a reaction is relatively seldom observed in organic substances. Correspondingly, there is no similarity between the physical and chemical reactions of AN 1 and other well-known substances. In order to attain suitable judgement on the pharmaceutical/dynamic effect of AN 1, the clinical results known to date should not be disregarded. PMID:1243655

  9. 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

  10. Effects of combined chelation treatment with pyridoxal isonicotinoyl hydrazone analogs and deferoxamine in hypertransfused rats and in iron-loaded rat heart cells.

    PubMed

    Link, Gabriela; Ponka, Prem; Konijn, Abraham M; Breuer, William; Cabantchik, Z Ioav; Hershko, Chaim

    2003-05-15

    Although iron chelation therapy with deferoxamine (DFO) results in improved life expectancy of patients with thalassemia, compliance with parenteral DFO treatment is unsatisfactory, underlining the need for alternative drugs and innovative ways of drug administration. We examined the chelating potential of pyridoxal isonicotinoyl hydrazone (PIH) analogs, alone or in combination with DFO, using hypertransfused rats with labeled hepatocellular iron stores and cultured iron-loaded rat heart cells. Our in vivo studies using 2 representative PIH analogs, 108-o and 109-o, have shown that PIH analogs given orally are 2.6 to 2.8 times more effective in mobilizing hepatocellular iron in rats, on a weight-per-weight basis, than parenteral DFO administered intraperitoneally. The combined effect of DFO and 108-o on hepatocellular iron excretion was additive, and response at a dose range of 25 to 200 mg/kg was linear. In vitro studies in heart cells showed that DFO was more effective in heart cell iron mobilization than all PIH analogs studied. Response to joint chelation with DFO and PIH analogs was similar to an increase in the equivalent molar dose of DFO alone, rather than the sum of the separate effects of the PIH analog and DFO. This finding was most likely the result of iron transfer from PIH analogs to DFO, a conclusion supported directly by iron-shuttle experiments using fluorescent DFO. These findings provide a rationale for the combined, simultaneous use of iron-chelating drugs and may have useful, practical implications for designing novel strategies of iron chelation therapy.

  11. Mobilization of intracellular iron by analogs of pyridoxal isonicotinoyl hydrazone (PIH) is determined by the membrane permeability of the iron-chelator complexes.

    PubMed

    Buss, Joan L; Arduini, Emmanuele; Ponka, Prem

    2002-12-15

    In the ongoing search for an effective, orally active iron-chelator, the capacity of a series of halogenated analogs of pyridoxal isonicotinoyl hydrazone (PIH) to bind intracellular 59Fe and cause its release from cells was investigated. Reticulocytes labeled with 59Fe(2)-transferrin in which heme synthesis was inhibited by succinylacetone were used as a model of 59Fe mobilization. The kinetics of iron binding were similar for all the chelators tested (half-time of approximately 1 hr), and all bound more than twice as much 59Fe as PIH. The rate of release of the 59Fe-chelator complexes from cells depended upon the structure of the chelators. Ortho-substituted analogs were more effective at mobilizing cellular iron than meta and para isomers, due to a more efficient release of the iron complexes from the cell. The iron-chelator complexes which were released slowly from cells had a high affinity for erythrocyte ghost membranes, indicating the role of membrane permeability in the release mechanism of the complexes. The addition of BSA to the extracellular medium increased the extent of iron release by lipophilic analogs in a concentration-dependent manner, presumably by acting as a sink for the lipophilic complexes. The affinity of BSA for the chelators and their Fe(3+) complexes, determined spectrophotometrically, demonstrated that all chelators and their iron complexes bound BSA with dissociation constants ranging from 7,000 to >500,000 M(-1). Understanding the importance of the rate of release of the iron-chelator complex will direct the search for iron-chelators with improved efficacy.

  12. Bivalent transition metal complexes of o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone: Spectroscopic, antibacterial, antifungal activity and thermogravimetric studies

    NASA Astrophysics Data System (ADS)

    Zaky, R. R.; Ibrahim, K. M.; Gabr, I. M.

    2011-10-01

    Schiff base complexes of Cu(II), Ni(II) and Zn(II) with the o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone (H 2o-HAHNH) containing N and O donor sites have been synthesized. Both ligand and its metal complexes were characterized by different physicochemical methods, elemental analysis, molar conductivity ( 1H NMR, 13C NMR, IR, UV-visible, ESR, MS spectra) and also thermal analysis (TG and DTG) techniques. The discussion of the outcome data of the prepared complexes indicates that the ligand behave as a bidentate and/or tridentate ligand. The electronic spectra of the complexes as well as their magnetic moments suggest octahedral geometries for all isolated complexes. The room temperature solid state ESR spectrum of the Cu(II) complex shows d x2- y2 as a ground state, suggesting tetragonally distorted octahedral geometry around Cu(II) centre. The molar conductance measurements proved that the complexes are non-electrolytes. The kinetic thermodynamic parameters such as: E#, Δ H#, Δ G#, Δ S# are calculated from the DTG curves, for the [Ni(H O-HAHNH) 2] and [Zn(H 2 O-HAHNH)(OAc) 2]·H 2O complexes using the Coats-Redfern equation. Also, the antimicrobial properties of all compounds were studied using a wide spectrum of bacterial and fungal strains. The [Cu(H o-HAHNH)(OAc)(H 2O) 2] complex was the most active against all strains, including Aspergillus sp., Stemphylium sp. and Trichoderma sp. Fungi; E. coli and Clostridium sp. Bacteria.

  13. Synthesis and quantitative structure-activity relationship (QSAR) study of novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives as nematicidal agents.

    PubMed

    Che, Zhiping; Zhang, Shaoyong; Shao, Yonghua; Fan, Lingling; Xu, Hui; Yu, Xiang; Zhi, Xiaoyan; Yao, Xiaojun; Zhang, Rui

    2013-06-19

    In continuation of our program aimed at the discovery and development of natural-product-based pesticidal agents, 54 novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives were prepared, and their structures were well characterized by ¹H NMR, ¹³C NMR, HRMS, ESI-MS, and mp. Their nematicidal activity was evaluated against that of the pine wood nematode, Bursaphelenchus xylophilus in vivo. Among all of the derivatives, especially V-12 and V-39 displayed the best promising nematicidal activity with LC₅₀ values of 1.0969 and 1.2632 mg/L, respectively. This suggested that introduction of R¹ and R² together as the electron-withdrawing substituents, R³ as the methyl group, and R⁴ as the phenyl with the electron-donating substituents could be taken into account for further preparation of these kinds of compounds as nematicidal agents. Six selected descriptors are a WHIM descriptor (E1m), two GETAWAY descriptors (R1m+ and R3m+), a Burden eigenvalues descriptor (BEHm8), and two edge-adjacency index descriptors (EEig05x and EEig13d). Quantitative structure-activity relationship (QSAR) studies demonstrated that the structural factors, such as molecular mass (a negative correlation with the bioactivity) and molecular polarity (a positive correlation with bioactivity), are likely to govern the nematicidal activities of these compounds. For this model, the correlation coefficient (R²(training set)), the leave-one-out cross-validation correlation coefficient (Q²(LOO)), and the 7-fold cross-validation correlation coefficient (Q²(7-fold)) were 0.791, 0.701, and 0.715, respectively. The external cross-validation correlation coefficient (Q²ext) and the root-mean-square error for the test set (RMSE(test set)) were 0.774 and 3.412, respectively. This study will pave the way for future design, structural modification, and development of indole derivatives as nematicidal agents.

  14. Tuning a single ligand system to stabilize multiple spin states of manganese: a first example of a hydrazone-based manganese(III) spin-crossover complex.

    PubMed

    Shongwe, Musa S; Al-Barhi, Kaltham S; Mikuriya, Masahiro; Adams, Harry; Morris, Michael J; Bill, Eckhard; Molloy, Kieran C

    2014-07-28

    A series of bis-chelate pseudo-octahedral mononuclear coordination complexes of manganese with the chromophore [MnN4 O2 ](n+) (n=0, 1) have been generated in all three principal oxidation states of this transition-metal center under ambient conditions by utilizing a readily tunable, versatile phenolic pyridylhydrazone ligand system (i.e., H2 (3,5-R(1) ,R(2) )-L; L=ligand). Strategic combinations of the nature and position of a variety of substituent groups afforded selective, spontaneous stabilization of multiple spin states of the manganese center, which, upon close crystallographic scrutiny, appears to be in part due to the occurrence or absence of hydrogen-bonding interactions that involve the phenolate/phenolic oxygen atom. The divalent complexes are isolable in two forms, namely, molecular [Mn(II) {H(3,5-R(1) ,R(2) )-L}2 ] and ionic [Mn(II) {H2 (3,5-R(1) ,R(2) )-L}{H(3,5-R(1) ,R(2) )-L}]ClO4 , with the latter complex converting easily into the former complex on deprotonation. Accessibility of the higher-valent states is achievable only when the phenolate oxygen atom is sterically hindered from participation in hydrogen bonding. The [Mn(III) {H(3,5-tBu2 )-L}2 ]ClO4 complex is the first example of a hydrazone-based Mn(III) complex to exhibit spin crossover. Formation of the tetravalent complexes [Mn(IV) {(3,5-R(1) ,R(2) )-L}2 ] (R(1) =tBu, R(2) =H; R(1) =R(2) =tBu) necessitates base-assisted abstraction of the hydrazinic proton.

  15. Weakly-bridged dimeric diorganotin(IV) compounds derived from pyruvic acid hydrazone Schiff base ligands: Synthesis, characterization and crystal structures

    NASA Astrophysics Data System (ADS)

    Hong, Min; Yin, Han-Dong; Cui, Ji-Chun

    2011-03-01

    We report the synthesis of four diorganotin(IV) compounds of Schiff base pyruvic acid hydrazone derivatives formulated as [R 2SnLY] 2, where L 1 is 2-SC 4H 3CON 2C(CH 3)CO 2 with Y = CH 3CH 2CH 2CH 2OH, R = n-Bu ( 1); L 2 is C 6H 5CON 2C(CH 3)CO 2 with Y = CH 3CH 2OH, R = p-F-Bz ( 2); L 3 is 2-HOC 6H 4CON 2C(CH 3)CO 2 with Y dbnd H 2O, R = p-CN -Bz ( 3); and L 4 is 4-NO 2-C 6H 4CON 2C(CH 3)CO 2 with Y dbnd CH 3CH 2OH, R = Bz ( 4). The structures of all compounds have been established by a combination of single-crystal X-ray diffraction analysis, 1H and 119Sn NMR spectroscopy, IR spectroscopy, and elemental analysis. Studies reveal that four ligands present the same coordination mode with tin center, which all present tridentate ONO donor Schiff bases and coordinate to the tin center in an enolic form. In compounds 1- 4, each tin atom is seven-coordinated and exhibits a distorted pentagonal bipyramid with a planar SnO 4N unit and two apical alkyl carbon atoms, thus forming a weakly-bridged dimeric molecule. Additionally, the distance of Sn⋯O bridge in each compound is obviously affected by the choice of different alkyl groups and coordination solvent molecules, which fluctuates in the range of 2.571(5)-2.839(4) Å. Furthermore, the supramolecular structure analysis show that there are two types of supramolecular infrastructures, 1D chain or 2D network, which are formed by intermolecular O-H···N or C-H⋯X (X = O, N or F) hydrogen bonds.

  16. Mono- and binuclear copper(II) complexes of new hydrazone ligands derived from 4,6-diacetylresorcinol: Synthesis, spectral studies and antimicrobial activity.

    PubMed

    Shebl, Magdy; El-ghamry, Mosad A; Khalil, Saied M E; Kishk, Mona A A

    2014-05-21

    Two new hydrazone ligands, H2L(1) and H2L(2), were synthesized by the condensation of 4,6-diacetylresorcinol with 3-hydrazino-5,6-diphenyl-1,2,4-triazine and isatin monohydrazone, respectively. The structures of the ligands were elucidated by elemental analyses, IR, (1)H NMR, electronic and mass spectra. Reactions of the ligands with several copper(II) salts, including AcO(-), NO3(-), SO4(2-), Cl(-) and Br(-) afforded mono- and binuclear metal complexes. Also, the ligands were allowed to react with Cu(II) ion in the presence of a secondary ligand (L') [N,O-donor; 8-hydroxyquinoline, N,N-donor; 1,10-phenanthroline or O,O-donor; benzoylacetone]. Characterization and structure elucidation of the prepared complexes were achieved by elemental and thermal analyses, IR, electronic, mass and ESR spectra as well as conductivity and magnetic susceptibility measurements. The ESR spin Hamiltonian parameters of some complexes were calculated. The spectroscopic data showed that the H2L(1) ligand acts as a neutral or monobasic tridentate ligand while the H2L(2) ligand acts as a bis(monobasic tridentate) ligand. The coordination sites with the copper(II) ion are phenolic oxygen, azomethine nitrogen and triazinic nitrogen (H2L(1) ligand) or isatinic oxygen (H2L(2) ligand). The metal complexes exhibited octahedral and square planar geometrical arrangements depending on the nature of the anion. The ligands and some metal complexes showed antimicrobial activity. PMID:24607473

  17. Application of 3-methylbenzothiazolin-2-one hydrazone for the quantitative spectrophotometric determination of oxcarbazepine in pharmaceuticals with cerium(IV) and periodate

    NASA Astrophysics Data System (ADS)

    Rajendraprasad, N.; Basavaiah, K.; Vinay, K. B.

    2012-09-01

    Two simple, sensitive, selective, accurate, and cost-effective spectrophotometric methods are described for the assay of oxcarbazepine (OXC) in bulk drug and in tablets. The methods are based on an oxidative coupling reaction involving OXC, 3-methylbenzothiazolin-2-one hydrazone (MBTH), and cerium(IV) sulfate at pH 4.28 ± 0.07 (method A) or sodium periodate at pH > 4.0 (method B) to form an orange colored product with an absorption maximum at 450 nm. Under optimized experimental conditions, the calibration graphs are linear over the ranges of 4-80 and 2-32 μg/ml for methods A and B, respectively, with correlation coefficient (r) values of 0.9984 and 0.9976. The apparent molar absorptivity values are 3.13ṡ103 and 9.13ṡ103 l/molṡcm for methods A and B, respectively. The other optical characteristics such as Sandell's sensitivity, limits of detection (LOD) and quantification (LOQ) values are also reported. The accuracy and precision of the methods were evaluated based on intra-day and inter-day variations. The proposed methods were successfully applied to the determination of OXC in tablets: the results were comparable with the published data obtained using the reference method. The reaction stoichiometry of OXC with MBTH (1:1 in method A and 1:2 in method B) was also evaluated using the limiting logarithmic method, and a possible reaction pathway is presented for the both methods.

  18. 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...

  19. 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,...

  20. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 40 Protection of Environment 31 2011-07-01 2011-07-01 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,...

  1. 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...

  2. 78 FR 17933 - Determination That BENADRYL (diphenhydramine hydrochloride) Injection and Two Other Drug Products...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-03-25

    ... HUMAN SERVICES Food and Drug Administration Determination That BENADRYL (diphenhydramine hydrochloride... AGENCY: Food and Drug Administration, HHS. ACTION: Notice. SUMMARY: The Food and Drug Administration (FDA... Evaluation and Research, Food and Drug Administration, 10903 New Hampshire Ave., Bldg. 51, Rm. 6206,...

  3. 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…

  4. 78 FR 2416 - Notice of Issuance of Final Determination Concerning Rybix® (Tramadol Hydrochloride) Tablets

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-01-11

    .... FACTS: Rybix ODT is a pharmaceutical product used for the management of moderate to moderately severe pain in adults. The active pharmaceutical ingredient (``API''), tramadol hydrochloride, is manufactured... pharmaceutical products from bulk form into measured doses, filtering and packaging does not result in...

  5. Improved compressibility, flowability, dissolution and bioavailability of pioglitazone hydrochloride by emulsion solvent diffusion with additives.

    PubMed

    Patil, S V; Pawar, A P; Sahoo, S K

    2012-03-01

    Spherical agglomerates of pioglitazone hydrochloride were prepared by the emulsion solvent diffusion method with additives (polyethylene glycol 6000, polyvinyl pyrrolidone, beta cyclodextrin, eudragit RS100, low acyl gellan gum and xanthan gum) using methanol, chloroform and water as a good solvent, bridging liquid and poor solvent respectively. Prepared agglomerates were evaluated for compressibility, solubility, dissolution rate and bioavailability, and characterized by SEM, XRPD, DSC and FTIR spectroscopy. Particle size, flowability, compactibility, packability, solubility, dissolution rate and bioavailability of plain agglomerates and agglomerates with additives (except with polyvinyl pyrrolidone) were advantageously improved compared with raw crystalline pioglitazone hydrochloride. These improved properties for direct compression were due to their large-spherical shape and enhanced fragmentation during compaction, together with increased tensile strength and reduced elastic recovery of the compacts. XRPD and DSC studies indicated polymorphic transition of pioglitazone hydrochloride from form II to I during recrystallization but this was not associated with any chemical transition, as indicated by FTIR spectra, well supported by stability studies. Thus spherical crystallization by the emulsion solvent diffusion method with selected additives is a satisfactory method for direct tableting of pioglitazone hydrochloride giving improved bioavailability. PMID:22530302

  6. 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…

  7. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 40 Protection of Environment 32 2013-07-01 2013-07-01 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. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... 40 Protection of Environment 31 2014-07-01 2014-07-01 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,...

  9. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... 40 Protection of Environment 32 2012-07-01 2012-07-01 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,...

  10. 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...

  11. Effects of zilpaterol hydrochloride on blood gas, electrolyte balance, and pH in feedlot cattle

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The objective of this study was to examine the effects of zilpaterol hydrochloride (ZH) on blood gas, electrolyte balance and pH in feedlot cattle. Black-hided steers and heifers (n=96) were sourced from a commercial feedlot and transported to the Texas Tech University Beef Center in New Deal, TX. C...

  12. Evaluation of objective and subjective mobility variables in feedlot cattle supplemented with zilpaterol hydrochloride

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The objective of this study was to examine the effects of zilpaterol hydrochloride (ZH) on mobility in feedlot cattle. Black-hided steers and heifers (n=96) were sourced from a commercial feedlot and transported to the Texas Tech University Beef Center in New Deal, TX. Cattle were weighed and scan...

  13. 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...

  14. Performance of finishing beef steers in response to anabolic implant dose and zilpaterol hydrochloride

    Technology Transfer Automated Retrieval System (TEKTRAN)

    British × Continental steers (n = 168; 7 pens/treatment; initial BW = 362 kg) were used to evaluate the dose of trenbolone acetate (TBA) and estradiol-17ß (E2) and feeding of zilpaterol hydrochloride (ZH) on performance and carcass characteristics. A randomized complete block design was used with a ...

  15. Cystic fibrosis: comparison of two mucolytic drugs for inhalation treatment (acetylcysteine and arginine hydrochloride).

    PubMed

    Dietzsch, H J; Gottschalk, B; Heyne, K; Leupoid, W; Wunderlich, P

    1975-01-01

    Clinical, bronchoscopic, spirographic, scintigraphic, and chemical analyses were done in 24 children with cystic fibrosis to assess the mucolytic effects of acetylcysteine inhalations versus L-arginine hydrochloride aerosols. The latter drug is less active than acetylcysteine and should not be used to treat children with cystic fibrosis.

  16. Compatibility of amiodarone hydrochloride with vasopressin during simulated Y-site administration.

    PubMed

    Ramaley, Corinne C; Li, Feng; Du, Chengan

    2013-01-01

    The objective of this study was to determine the compatibility of amiodarone hydrochloride with vasopressin during simulated Y-site administration. Amiodarone hydrochloride is compatible with vasopressin under simulated-use conditions when administered according to the Advanced Cardiac Life Support Guidelines. A simulated-use approach is a more appropriate way to evaluate compatibility of drug solutions and to assure safe and adequate drug delivery to the patient, particularly when the drug being evaluated is well-documented to have physical or chemical incompatibility concerns with various drugs. When amiodarone hydrochloride (50 mg/mL) was diluted to 6 mg/mL with 5% dextrose injection, then mixed with an equal volume of vasopressin (0.2 units/mL in normal saline) in a glass test tube, no visual incompatibility was observed for up to 24 hours. The purpose of our study was to assess compatibility of the two drugs under simulated-use conditions and to measure the recovery of amiodarone by high-performance liquid chromatography after sequential administration of vasopressin and amiodarone hydrochloride according to the Advanced Cardiac Life Support Guidelines. PMID:24459790

  17. 40 CFR 721.1075 - Benzenamine, 4-(1-methyl-bu-toxy)-, hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ...) TOXIC SUBSTANCES CONTROL ACT SIGNIFICANT NEW USES OF CHEMICAL SUBSTANCES Significant New Uses for Specific Chemical Substances § 721.1075 Benzenamine, 4-(1-methyl-bu-toxy)-, hydrochloride. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified...

  18. Evaluation of phenazopyridine hydrochloride as a tool in the diagnosis of premature rupture of the membranes.

    PubMed

    Meyer, B A; Gonik, B; Creasy, R K

    1991-09-01

    This is a prospective study to determine whether a maternal orally administered azo dye, phenazopyridine hydrochloride, would cross into amniotic fluid, and thus be of potential aid in the diagnosis of rupture of the membranes. Based on anecdotal experience, we hypothesized that this compound would cross the placenta and be excreted in the fetal urine, causing discoloration of the amniotic fluid. Ten patients with uncomplicated pregnancies undergoing elective amniocentesis for obstetric indications received an oral dose of 400 mg of phenazopyridine hydrochloride 4 hours prior to the procedure. Amniotic fluid was also available from five control patients who did not receive phenazopyridine hydrochloride. The typical orange-to-red discoloration of the urine was seen in all study patients, indicating ingestion of the dye. None of the ten patients had evidence of the azo dye in their amniotic fluid by visual inspection or by spectrophotometric absorbance. After the amniotic fluid samples were acidified, the presence of the azo dye was visually demonstrable, and spectrophotometry confirmed measurable concentrations (mean +/- SE: 13.08 +/- 0.72 micrograms/ml). We conclude that although phenazopyridine hydrochloride does cross the placenta into the fetal compartment, its presence causes a visual and spectrophotometric change in the color of amniotic fluid only when the normal basic pH of amniotic fluid is acidified.

  19. Stability studies of lincomycin hydrochloride in aqueous solution and intravenous infusion fluids

    PubMed Central

    Czarniak, Petra; Boddy, Michael; Sunderland, Bruce; Hughes, Jeff D

    2016-01-01

    Purpose The purpose of this study was to evaluate the chemical stability of Lincocin® (lincomycin hydrochloride) in commonly used intravenous fluids at room temperature (25°C), at accelerated-degradation temperatures and in selected buffer solutions. Materials and methods The stability of Lincocin® injection (containing lincomycin 600 mg/2 mL as the hydrochloride) stored at 25°C±0.1°C in sodium lactate (Hartmann’s), 0.9% sodium chloride, 5% glucose, and 10% glucose solutions was investigated over 31 days. Forced degradation of Lincocin® in hydrochloric acid, sodium hydroxide, and hydrogen peroxide was performed at 60°C. The effect of pH on the degradation rate of lincomycin hydrochloride stored at 80°C was determined. Results Lincomycin hydrochloride w as found to maintain its shelf life at 25°C in sodium lactate (Hartmann’s) solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution, with less than 5% lincomycin degradation occurring in all intravenous solutions over a 31-day period. Lincomycin hydrochloride showed less rapid degradation at 60°C in acid than in basic solution, but degraded rapidly in hydrogen peroxide. At all pH values tested, lincomycin followed first-order kinetics. It had the greatest stability near pH 4 when stored at 80°C (calculated shelf life of 4.59 days), and was least stable at pH 2 (calculated shelf life of 0.38 days). Conclusion Lincocin® injection was chemically found to have a shelf life of at least 31 days at 25°C when added to sodium lactate (Hartmann’s) solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution. Solutions prepared at approximately pH 4 are likely to have optimum stability. PMID:27022242

  20. A clinical pharmacokinetic study comparing two azelastine hydrochloride nasal formulations in a single-dose design.

    PubMed

    Du, Daniel; Targett, Darren; Stolberg, Erhard; Canali, Alessandra

    2014-03-01

    Azelastine hydrochloride is a potent second-generation antihistamine, available in Europe and the USA as a nasal spray formulation for the treatment of allergic rhinitis symptoms. GlaxoSmithKline (GSK) Consumer Healthcare has developed a new nasal formulation of azelastine hydrochloride. The present study was aimed at comparing the clinical pharmacokinetic profiles and assessing the bioequivalence of the new formulation of azelastine hydrochloride with a marketed reference nasal spray product. This was a randomized, two-way crossover, two-stage, single-dose pharmacokinetic study with 2 weeks washout between the two treatment periods. A dosage of 0.28 mg of the test and reference products was administered as a single dose to healthy volunteers according to the crossover design. Twenty-three subjects (15 subjects from stage 1 and 8 subjects from stage 2) were enrolled in the study. Adjusted mean values for AUC0-t were 1,526.8 h pg/mL for the test drug and 1,441.5 h pg/mL for the reference drug; for C max the values were 61.59 pg/mL for the test drug and 58.21 pg/mL for the reference drug. The 94.12 % CI of geometric mean ratios (test/reference) were 0.99-1.13 and 0.95-1.18 for AUC0-t and C max. This met the predefined criteria for bioequivalence between test and reference drugs. Secondary pharmacokinetic parameters for azelastine and for the metabolite desmethyl azelastine, AUC(0-∞) and t max, were numerically similar between the two study treatments. Both test and reference azelastine hydrochloride formulations were well tolerated at single dose. This study demonstrated the bioequivalence between the new azelastine hydrochloride nasal spray formulation and the marketed reference Allergodil(®) after single-dose administration. PMID:23681835

  1. Optimization of mesoporous carbons for efficient adsorption of berberine hydrochloride from aqueous solutions.

    PubMed

    Li, Yin; Fu, Jie; Deng, Shuguang; Lu, Xiuyang

    2014-06-15

    Sixteen mesoporous carbon adsorbents were synthesized by varying the ratio of soft to hard templates in order to optimize the pore textural properties of these adsorbents. The mesoporous carbon adsorbents have a high BET specific surface area (1590.3-2193.5 m(2)/g), large pore volume (1.72-2.56 cm(3)/g), and uniform pore size distribution with a median pore diameter ranging from 3.51 nm to 4.52 nm. It was observed that pore textural properties of the carbon adsorbents critically depend on the molar ratio of carbon sources to templates, and the hard template plays a more important role than the soft template in manipulating the pore textures. Adsorption isotherms of berberine hydrochloride at 303 K were measured to evaluate the adsorption efficacy of these adsorbents. The adsorption of berberine hydrochloride from aqueous solutions on the sixteen mesoporous carbon adsorbents synthesized in this work is very efficient, and the adsorption equilibrium capacities on all samples are more than double the adsorption capacities of berberine hydrochloride of the benchmark adsorbents (polymer resins and spherical activated carbons) at similar conditions. It was observed from the adsorption experiments that the equilibrium adsorption amounts of berberine hydrochloride are strongly correlated with the BET specific surface area and pore volume of the adsorbents. The adsorbent with the highest BET of 2193.5 m(2)/g displayed the largest adsorption capacity of 574 mg/g at an equilibrium concentration of 0.10mg/mL of berberine hydrochloride in an aqueous solution. PMID:24767505

  2. Effect of local application of delmopinol hydrochloride on developing and early established supragingival plaque in humans.

    PubMed

    Klinge, B; Matsson, L; Attström, R; Edwardsson, S; Sjödin, T

    1996-06-01

    The aim of the study was to investigate the effect of delmopinol hydrochloride on the development of dental plaque and on newly established plaque. In addition, the influence of this compound on the composition of the microbiota colonizing the gingival mucous membrane was studied. 14 healthy male volunteers took part. After a 3 week pre-experimental period of intense oral hygiene, the participants refrained from all oral hygiene for 14 days. The buccal surfaces of cuspids and bicuspids on one side of the jaws were treated with a 1% aqueous solution of delmopinol hydrochloride (applied with a paint brush) 2 x a day for 7 days, while the contralateral side received placebo solution. On day 7, the application procedures were changed in that the test compound was applied on the teeth previously treated with placebo and vice versa. Plaque development was assessed clinically and by photo-based planimetric determination. The clinical recordings revealed that 89.3% of the placebo-treated surfaces displayed visible plaque on day 7, compared to 6.0% of the delmopinol hydrochloride treated surfaces. Delmopinol hydrochloride treatment of the previously placebo-treated surfaces resulted in a decrease in the number of surfaces with visible plaque from 89.3% on day 7 to 6% on day 14. These results were confirmed by the planimetric data. No significant change in the composition of the mucosal flora was observed during the experimental period. The present results indicate that delmopinol hydrochloride markedly reduces the formation of dental plaque on a clean tooth surface exposed to conditions which favour bacterial colonization. Furthermore, the substance appears to possess plaque-dissolving properties. PMID:8811473

  3. Spectral characterization, molecular modeling and antimicrobial studies on hydrazone metal complexes of 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)dione and S-methyl dithiocarbazate.

    PubMed

    Taha, Ali; Emara, Adel A A; Mashaly, Mahmoud M; Adly, Omima M I

    2014-09-15

    Metal complexes of copper(II), nickel(II), cobalt(II), oxovanadium(IV), chromium(III) and cadmium(II) with a new bridged ONS dibasic tridentate hydrazone (H2L) derived from 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione with S-methyl dithiocarbazate have been synthesized and characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, spectral (infrared, electronic, mass, 1H NMR and ESR) studies as well as thermal gravimetric analysis (TGA). The synthesized complexes have dimeric structures with the general formula [ML(NO3)m(H2O)x]2·nH2O·zMeOH, L=dianion of the hydrazone, m=0-1, x=0-2, n=0-4 and z=0-1. The metal complexes exhibited square planar, tetrahedral and octahedral geometrical arrangements, the molar conductivity data indicates that all complexes are neutral. The Coats-Redfern equation was used to calculate the kinetic and thermodynamic parameters for the different thermal decomposition stages of some complexes. Structural parameters of the ligand and its metal complexes have been theoretically computed on the basis of semiempirical PM3 level and the results were correlated with their experimental data. Antibacterial activities of the free ligand and its metal complexes were screened against various organisms.

  4. Spectral characterization, molecular modeling and antimicrobial studies on hydrazone metal complexes of 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)dione and S-methyl dithiocarbazate

    NASA Astrophysics Data System (ADS)

    Taha, Ali; Emara, Adel A. A.; Mashaly, Mahmoud M.; Adly, Omima M. I.

    2014-09-01

    Metal complexes of copper(II), nickel(II), cobalt(II), oxovanadium(IV), chromium(III) and cadmium(II) with a new bridged ONS dibasic tridentate hydrazone (H2L) derived from 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione with S-methyl dithiocarbazate have been synthesized and characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, spectral (infrared, electronic, mass, 1H NMR and ESR) studies as well as thermal gravimetric analysis (TGA). The synthesized complexes have dimeric structures with the general formula [ML(NO3)m(H2O)x]2·nH2O·zMeOH, L = dianion of the hydrazone, m = 0-1, x = 0-2, n = 0-4 and z = 0-1. The metal complexes exhibited square planar, tetrahedral and octahedral geometrical arrangements, the molar conductivity data indicates that all complexes are neutral. The Coats-Redfern equation was used to calculate the kinetic and thermodynamic parameters for the different thermal decomposition stages of some complexes. Structural parameters of the ligand and its metal complexes have been theoretically computed on the basis of semiempirical PM3 level and the results were correlated with their experimental data. Antibacterial activities of the free ligand and its metal complexes were screened against various organisms.

  5. Solvent assisted formation of ruthenium(III) and ruthenium(II) hydrazone complexes in one-pot with potential in vitro cytotoxicity and enhanced LDH, NO and ROS release.

    PubMed

    Jayanthi, Eswaran; Kalaiselvi, Sivalingam; Padma, Viswanatha Vijaya; Bhuvanesh, Nattamai S P; Dharmaraj, Nallasamy

    2016-01-28

    A set each of new bivalent and trivalent ruthenium complexes, [Ru(III)(HL)Cl2(EPh3)2] and [Ru(II)(L)(CO)(EPh3)2] (E = P (complexes and ) or As (complexes and )) were synthesised from the reactions of [Ru(III)Cl3(EPh3)3] with 2-hydroxynaphthaldehyde benzoic acid hydrazone (H2L) in methanol-chloroform and characterized by elemental analysis, spectral data and XRD study. A suitable mechanism to account for the formation of bivalent ruthenium carbonyl complexes from the corresponding trivalent precursors is provided by considering the role of added base in the reaction. Interaction of complexes with CT-DNA/bovine serum albumin was analysed with absorption and emission spectral titration studies. In vitro cytotoxic potential of the above ruthenium hydrazone complexes assayed against the A549 cell line revealed a significant growth inhibition. The test complexes added in IC50 concentration into the cell culture medium enhanced the release of lactate dehydrogenase, NO and reactive oxygen species in comparison with the control. Cell death induced by the complexes was studied using a propidium iodide staining assay and showed noticeable changes in the cell morphology which resembled apoptosis.

  6. Solvent assisted formation of ruthenium(III) and ruthenium(II) hydrazone complexes in one-pot with potential in vitro cytotoxicity and enhanced LDH, NO and ROS release.

    PubMed

    Jayanthi, Eswaran; Kalaiselvi, Sivalingam; Padma, Viswanatha Vijaya; Bhuvanesh, Nattamai S P; Dharmaraj, Nallasamy

    2016-01-28

    A set each of new bivalent and trivalent ruthenium complexes, [Ru(III)(HL)Cl2(EPh3)2] and [Ru(II)(L)(CO)(EPh3)2] (E = P (complexes and ) or As (complexes and )) were synthesised from the reactions of [Ru(III)Cl3(EPh3)3] with 2-hydroxynaphthaldehyde benzoic acid hydrazone (H2L) in methanol-chloroform and characterized by elemental analysis, spectral data and XRD study. A suitable mechanism to account for the formation of bivalent ruthenium carbonyl complexes from the corresponding trivalent precursors is provided by considering the role of added base in the reaction. Interaction of complexes with CT-DNA/bovine serum albumin was analysed with absorption and emission spectral titration studies. In vitro cytotoxic potential of the above ruthenium hydrazone complexes assayed against the A549 cell line revealed a significant growth inhibition. The test complexes added in IC50 concentration into the cell culture medium enhanced the release of lactate dehydrogenase, NO and reactive oxygen species in comparison with the control. Cell death induced by the complexes was studied using a propidium iodide staining assay and showed noticeable changes in the cell morphology which resembled apoptosis. PMID:26699435

  7. 40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 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...

  8. 40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... 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...

  9. 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...

  10. 40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of the.... Tutin and M.L. Foster, Tacoma R&D Laboratory, Georgia-Pacific Resins, Inc. (Principle written by R....

  11. 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.

  12. A hydrazone covalent organic polymer based micro-solid phase extraction for online analysis of trace Sudan dyes in food samples.

    PubMed

    Zhang, Chengjiang; Li, Gongke; Zhang, Zhuomin

    2015-11-01

    Covalent organic polymers (COPs) connected by covalent bonds are a new class of porous network materials with large surface area and potential superiority in sample pretreatment. In this study, a new hydrazone linked covalent organic polymer (HL-COP) adsorbent was well-designed and synthesized based on a simple Schiff-base reaction. The condensation of 1,4-phthalaldehyde and 1,3,5-benzenetricarbohydrazide as organic building blocks led to the synthesis of HL-COP with uniform particle size and good adsorption performance. This HL-COP adsorbent with high hydrophobic property and rich stacking π electrons contained abundant phenyl rings and imine (CN) groups throughout the entire molecular framework. The adsorption mechanism was explored and discussed based on π-π affinity, hydrophobic effect, hydrogen bonding and electron-donor-acceptor (EDA) interaction, which contributed to its strong recognition affinity to target compounds. Enrichment factors were 305-757 for six Sudan dyes by HL-COP micro-solid phase extraction (μ-SPE), indicating its remarkable preconcentration ability. Furthermore, the adsorption amounts by HL-COP μ-SPE were 1.0-11.0 folds as those by three commonly used commercial adsorbents. Then, HL-COP was applied as adsorbent of online μ-SPE coupled with high performance liquid chromatography (HPLC) for enrichment and analysis of trace Sudan dyes in food samples with detection limit of 0.03-0.15μg/L. The method was successfully applied for online analysis of chilli powder and sausage samples. Sudan II and Sudan III in one positive chilli powder sample were actually found and determined with concentrations of 8.3 and 6.8μg/kg, respectively. The recoveries of chilli powder and sausage samples were in range of 75.8-108.2% and 73.8-112.6% with relative standard deviations of 1.2-8.5% and 1.9-9.4% (n=5), respectively. The proposed method was accurate, reliable and convenient for the online simultaneous analysis of trace Sudan dyes in food samples. PMID

  13. A hydrazone covalent organic polymer based micro-solid phase extraction for online analysis of trace Sudan dyes in food samples.

    PubMed

    Zhang, Chengjiang; Li, Gongke; Zhang, Zhuomin

    2015-11-01

    Covalent organic polymers (COPs) connected by covalent bonds are a new class of porous network materials with large surface area and potential superiority in sample pretreatment. In this study, a new hydrazone linked covalent organic polymer (HL-COP) adsorbent was well-designed and synthesized based on a simple Schiff-base reaction. The condensation of 1,4-phthalaldehyde and 1,3,5-benzenetricarbohydrazide as organic building blocks led to the synthesis of HL-COP with uniform particle size and good adsorption performance. This HL-COP adsorbent with high hydrophobic property and rich stacking π electrons contained abundant phenyl rings and imine (CN) groups throughout the entire molecular framework. The adsorption mechanism was explored and discussed based on π-π affinity, hydrophobic effect, hydrogen bonding and electron-donor-acceptor (EDA) interaction, which contributed to its strong recognition affinity to target compounds. Enrichment factors were 305-757 for six Sudan dyes by HL-COP micro-solid phase extraction (μ-SPE), indicating its remarkable preconcentration ability. Furthermore, the adsorption amounts by HL-COP μ-SPE were 1.0-11.0 folds as those by three commonly used commercial adsorbents. Then, HL-COP was applied as adsorbent of online μ-SPE coupled with high performance liquid chromatography (HPLC) for enrichment and analysis of trace Sudan dyes in food samples with detection limit of 0.03-0.15μg/L. The method was successfully applied for online analysis of chilli powder and sausage samples. Sudan II and Sudan III in one positive chilli powder sample were actually found and determined with concentrations of 8.3 and 6.8μg/kg, respectively. The recoveries of chilli powder and sausage samples were in range of 75.8-108.2% and 73.8-112.6% with relative standard deviations of 1.2-8.5% and 1.9-9.4% (n=5), respectively. The proposed method was accurate, reliable and convenient for the online simultaneous analysis of trace Sudan dyes in food samples.

  14. Vanadium complexes having [VO]2+, [VO]3+ and [VO2]+ cores with hydrazones of 2,6-diformyl-4-methylphenol: synthesis, characterization, reactivity, and catalytic potential.

    PubMed

    Maurya, Mannar R; Haldar, Chanchal; Kumar, Amit; Kuznetsov, Maxim L; Avecilla, Fernando; Costa Pessoa, João

    2013-09-01

    The Schiff bases H3dfmp(L)2 obtained by the condensation of 2,6-diformyl-4-methylphenol and hydrazones [L = isonicotinoylhydrazide (inh), nicotinoylhydrazide (nah) and benzoylhydrazide (bhz)] are prepared and characterized. By reaction of [V(IV)O(acac)2] and the H3dfmp(L)2 in methanol the V(IV)O-complexes [V(IV)O{Hdfmp(inh)2}(H2O)] (1), [V(IV)O{Hdfmp(nah)2}(H2O)] (2) and [V(IV)O{Hdfmp(bhz)2}(H2O)] (3) were obtained. Upon their aerial oxidation in methanol [V(V)O(OMe)(MeOH){Hdfmp(inh)2}] (4), [V(V)O(OMe)(MeOH){Hdfmp(nah)2}] (5) and [V(V)O(OMe)(MeOH){Hdfmp(bhz)2}] (6) were isolated. In the presence of KOH, oxidation of 1-3 results in the formation of [V(V)O2{H2dfmp(inh)2}]n·5H2O (7), K[V(V)O2{Hdfmp(nah)2}] (8) and K[V(V)O2{Hdfmp(bhz)2}] (9). All compounds are characterized in the solid state and in solution, namely by spectroscopic techniques (IR, UV-Vis, EPR, (1)H, (13)C and (51)V NMR), and DFT is also used to calculate the V(IV) hyperfine coupling constants of V(IV)-compounds and (51)V NMR chemical shifts of several V(V)-species and assign them to those formed in solution. Single crystal X-ray analysis of [V(V)O(OMe)(MeOH){Hdfmp(bhz)2}] (6) and [V(V)O2{H2dfmp(inh)2}]n·5H2O (7) confirm the coordination of the ligand in the dianionic (ONO(2-)) enolate tautomeric form, one of the hydrazide moieties remaining non-coordinated. In the case of 7 the free N(pyridine) atom of the inh moiety coordinates to the other vanadium center yielding a polynuclear complex in the solid state. It is also demonstrated that the V(V)O2-complexes are catalyst precursors in the oxidative bromination of styrene by H2O2, therefore acting as functional models of vanadium dependent haloperoxidases. Plausible intermediates involved in the catalytic process are established by UV-Vis, (51)V NMR and DFT studies. PMID:23680862

  15. Synthesis, structure, and solution reduction reactions of volatile and thermally stable mid to late first row transition metal complexes containing hydrazonate ligands.

    PubMed

    Kalutarage, Lakmal C; Martin, Philip D; Heeg, Mary Jane; Winter, Charles H

    2013-05-01

    Treatment of MCl2 (M = Ni, Co, Fe, Mn, Cr) with 2 equiv of the hydrazonate salts K(tBuNNCHCtBuO), K(tBuNNCHCiPrO), or K(tBuNNCMeCMeO) afforded the complexes M(tBuNNCHCtBuO)2 (M = Ni, 65%; Co, 80%; Fe, 83%; Mn, 68%; Cr, 64%), M(tBuNNCHCiPrO)2 (M = Ni, 63%; Co, 86%; Fe, 75%), and M(tBuNNCMeCMeO)2 (M = Ni, 34%; Co, 29%; Fe, 27%). Crystal structure determinations of Co(tBuNNCHCtBuO)2, M(tBuNNCHCiPrO)2 (M = Ni, Co), and M(tBuNNCMeCMeO)2 (M = Ni, Co, Fe) revealed monomeric complexes with tetrahedral geometries about the metal centers. To evaluate the potential of these new complexes as film growth precursors, preparative sublimations, thermogravimetric analyses, solid state decomposition studies, and solution reactions with reducing coreagents were carried out. M(tBuNNCHCtBuO)2 sublime between 120 and 135 °C at 0.05 Torr, whereas M(tBuNNCHCiPrO)2 and M(tBuNNCMeCMeO)2 sublime between 100 and 105 °C at the same pressure. All complexes afforded ≥96% recovery of sublimed material, with ≤3% of nonvolatile residues. The solid state decomposition temperatures were highest for M(tBuNNCHCiPrO)2 (273-308 °C), intermediate for M(tBuNNCHCtBuO)2 (241-278 °C), and lowest for M(tBuNNCMeCMeO)2 (235-250 °C). Treatment of Co(tBuNNCHCtBuO)2 in tetrahydrofuran with hydrazine, BH3(L) (L = NHMe2, SMe2, THF), pinacol borane, and LiAlH4 led to rapid formation of cobalt metal, while analogous reductions of Mn(tBuNNCHCtBuO)2 with BH3(THF), pinacol borane, and LiAlH4 appeared to afford manganese metal. The new complexes M(tBuNNCHCtBuO)2, M(tBuNNCHCiPrO)2, and M(tBuNNCMeCMeO)2 have very promising properties for use as precursors for the growth of the respective metals in atomic layer deposition film growth processes.

  16. Bismuth(III) complexes with 2-acetylpyridine- and 2-benzoylpyridine-derived hydrazones: Antimicrobial and cytotoxic activities and effects on the clonogenic survival of human solid tumor cells.

    PubMed

    Ferreira, Isabella P; Piló, Elisa D L; Recio-Despaigne, Angel A; Da Silva, Jeferson G; Ramos, Jonas P; Marques, Lucas B; Prazeres, Pedro H D M; Takahashi, Jacqueline A; Souza-Fagundes, Elaine M; Rocha, Willian; Beraldo, Heloisa

    2016-07-01

    Complexes [Bi(2AcPh)Cl2]·0.5H2O (1), [Bi(2AcpClPh)Cl2] (2), [Bi(2AcpNO2Ph)Cl2] (3), [Bi(2AcpOHPh)Cl2]·2H2O (4), [Bi(H2BzPh)Cl3]·2H2O (5), [Bi(H2BzpClPh)Cl3] (6), [Bi(2BzpNO2Ph)Cl2]·2H2O (7) and [Bi(H2BzpOHPh)Cl3]·2H2O (8) were obtained with 2-acetylpyridine phenylhydrazone (H2AcPh), its -para-chloro-phenyl- (H2AcpClPh), -para-nitro-phenyl (H2AcpNO2Ph) and -para-hydroxy-phenyl (H2AcpOHPh) derivatives, as well as with the 2-benzoylpyridine phenylhydrazone analogues (H2BzPh, H2BzpClPh, H2BzpNO2Ph, H2BzpOHPh). Upon coordination to bismuth(III) antibacterial activity against Gram-positive and Gram-negative bacterial strains significantly improved except for complex (4). The cytotoxic effects of the compounds under study were evaluated on HL-60, Jurkat and THP-1 leukemia, and on MCF-7 and HCT-116 solid tumor cells, as well as on non-malignant Vero cells. In general, 2-acetylpyridine-derived hydrazones proved to be more potent and more selective as cytotoxic agents than the corresponding 2-benzoylpyridine-derived counterparts. Exposure of HCT-116 cells to H2AcpClPh, H2AcpNO2Ph and complex (3) led to 99% decrease of the clonogenic survival. The IC50 values of these compounds were three-fold smaller when cells were cultured in soft-agar (3D) than when cells were cultured in monolayer (2D), suggesting that they constitute interesting scaffolds, which should be considered in further studies aiming to develop new drug candidates for the treatment of colon cancer. PMID:27209169

  17. 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).

  18. 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. PMID:25479718

  19. Treatment with olopatadine and naphazoline hydrochloride reduces allergic conjunctivitis in mice through alterations in inflammation, NGF and VEGF.

    PubMed

    Quan, Lin; He, Hua

    2016-04-01

    The aim of the current study was to investigate whether olopatadine and naphazoline hydrochloride reduce allergic conjunctivitis in mice through alterations in inflammation, NGF and VEGF. An allergic conjunctivitis mouse model was established using histamine or an antigen (ovalbumin), following which mice were treated with 1% olopatadine solution and/or 0.2 mg/ml of naphazoline hydrochloride. Histamine or antigen‑induced conjunctival vascular hyperpermeability was examined and the levels of inflammatory factors, cytokines, IgE, GMCSF and NGF were analyzed using ELISA in antigen‑induced conjunctival vascular hyperpermeability mice. In addition, VEGF protein expression was measured using western blotting in antigen‑induced mice. The results indicated that olopatadine and naphazoline hydrochloride significantly suppressed conjunctival dye leakage in mice with histamine or antigen‑induced conjunctival vascular hyperpermeability. In addition, treatment with olopatadine and naphazoline hydrochloride was able to reduce the levels of inflammatory factors (TNF‑α, IL‑1β and IL‑6), cytokines (IFN‑γ and IL‑4), IgE, GMCSF, and NGF in antigen‑induced conjunctival vascular hyperpermeability mice. The protein expression levels of VEGF in antigen‑induced conjunctival vascular hyperpermeability mice were reduced following treatment with olopatadine and naphazoline hydrochloride. These results suggest that treatment with olopatadine and naphazoline hydrochloride reduces conjunctivitis in mice via effects on inflammation, NGF and VEGF.

  20. Effect of L-ornithine hydrochloride ingestion on intermittent maximal anaerobic cycle ergometer performance and fatigue recovery after exercise.

    PubMed

    Demura, Shinichi; Morishita, Koji; Yamada, Takayoshi; Yamaji, Shunsuke; Komatsu, Miho

    2011-11-01

    L-Ornithine plays an important role in ammonia metabolism via the urea cycle. This study aimed to examine the effect of L-ornithine hydrochloride ingestion on ammonia metabolism and performance after intermittent maximal anaerobic cycle ergometer exercise. Ten healthy young adults (age, 23.8 ± 3.9 year; height, 172.3 ± 5.5 cm; body mass, 67.7 ± 6.1 kg) with regular training experience ingested L-ornithine hydrochloride (0.1 g/kg, body mass) or placebo after 30 s of maximal cycling exercise. Five sets of the same maximal cycling exercise were conducted 60 min after ingestion, and maximal cycling exercise was conducted after a 15 min rest. The intensity of cycling exercise was based on each subject's body mass (0.74 N kg(-1)). Work volume (watt), peak rpm (rpm) before and after intermittent maximal ergometer exercise and the following serum parameters were measured before ingestion, immediately after exercise and 15 min after exercise: ornithine, ammonia, urea, lactic acid and glutamate. Peak rpm was significantly greater with L-ornithine hydrochloride ingestion than with placebo ingestion. Serum ornithine level was significantly greater with L-ornithine hydrochloride ingestion than with placebo ingestion immediately and 15 min after intermittent maximal cycle ergometer exercise. In conclusion, although maximal anaerobic performance may be improved by L-ornithine hydrochloride ingestion before intermittent maximal anaerobic cycle ergometer exercise, the above may not depend on increase of ammonia metabolism with L-ornithine hydrochloride.

  1. Effect of fasudil hydrochloride, a protein kinase inhibitor, on cerebral vasospasm and delayed cerebral ischemic symptoms after aneurysmal subarachnoid hemorrhage.

    PubMed

    Zhao, Jizong; Zhou, Dingbiao; Guo, Jing; Ren, Zyuan; Zhou, Liangfu; Wang, Shuo; Xu, Bainan; Wang, Renzhi

    2006-09-01

    The efficacy and safety of fasudil hydrochloride, a novel protein kinase inhibitor, were evaluated for the treatment of cerebral vasospasm and associated cerebral ischemic symptoms in patients with ruptured cerebral aneurysm. This randomized open trial with nimodipine as the control included 72 patients who underwent subarachnoid hemorrhage surgery for ruptured cerebral aneurysm of Hunt and Hess grades I to IV. For 14 days following surgery, patients were administered either 30 mg of fasudil hydrochloride by intravenous injection over a period of 30 minutes three times a day or 1 mg/hr of nimodipine by continuous intravenous infusion. Fasudil hydrochloride and nimodipine both showed inhibitory effects on cerebral vasospasm. The incidence of symptomatic vasospasm was five of 33 patients in the fasudil group and nine of 32 patients in the nimodipine group. Good recovery evaluated by the Glasgow Outcome Scale was achieved by 23 of 33 patients in the fasudil group and 19 of 34 patients in the nimodipine group. Both drugs significantly improved consciousness levels and neurological deficits such as aphasia. However, fasudil hydrochloride improved motor disturbance more than nimodipine. Adverse reactions occurred in 13 of 37 patients receiving fasudil hydrochloride and 15 of 35 patients receiving nimodipine. There were no serious adverse events in the fasudil group. The results of this clinical trial indicate that fasudil hydrochloride is a safe and efficient agent for suppressing cerebral vasospasm after subarachnoid hemorrhage surgery for ruptured cerebral aneurysm.

  2. Preparation and Characterisation of Mucoadhesive Nasal Gel of Venlafaxine Hydrochloride for Treatment of Anxiety Disorders

    PubMed Central

    Basu, Shyamoshree; Maity, S.

    2012-01-01

    The aim of the present study is to prepare and evaluate mucoadhesive nasal gels of venlafaxine hydrochloride. Mucoadhesive nasal gels were prepared using polymers like carbopol 934 and sodium alginate and characterized in terms of viscosity, texture profile analysis, ex vivo drug permeation profiles and histopathological studies. The results show that values of viscosity, hardness and adhesiveness increase while those of cohesiveness decrease with corresponding increase in concentration of the polymers. Ex vivo drug permeation profiles showed that formulation containing 5% sodium alginate provided a better controlled release of the drug than the other formulations over a period of 12 h. Histopathological studies assured that gels containing different polymers did not produce any significant change in the nasal mucosae of goat even after 12 h permeation study. Mucoadhesive nasal gel of venlafaxine hydrochloride is a novel dosage form which delivers the drug directly into systemic circulation and provides controlled release of the drug. PMID:23716871

  3. Evaluation of genotoxic effects of Apitol (cymiazole hydrochloride) in vitro by measurement of sister chromatid exchange.

    PubMed

    Stanimirovic, Zoran; Stevanovic, Jevrosima; Jovanovic, Slobodan; Andjelkovic, Marko

    2005-12-30

    Apitol, with cymiazole hydrochloride as the active ingredient, is used in bee-keeping against the ectoparasitic mite Varroa destructor. The preparation was evaluated for genotoxicity in cultured human peripheral blood lymphocytes. Sister chromatid exchange, the mitotic index and the cell proliferation index were determined for three experimental concentrations of Apitol (0.001, 0.01 and 0.1 mg/ml). All concentrations significantly (p < 0.001) increased the mitotic index (MI = 7.35+/-0.18%, 8.31+/-0.20% and 12.33+/-0.25%, respectively), the proliferative index (PI = 1.83+/-0.01, 1.84+/-0.01 and 1.88+/-0.02, respectively) and the frequency of sister chromatid exchange (SCE = 8.19+/-1.81, 8.78+/-1.80 and 13.46+/-1.88, respectively), suggesting that cymiazole hydrochloride has genotoxic potential. PMID:16309949

  4. Thermodynamic characteristics of the acid dissociation of dopamine hydrochloride in water-ethanol solutions

    NASA Astrophysics Data System (ADS)

    Ledenkov, S. F.; Vandyshev, V. N.; Molchanov, A. S.

    2012-06-01

    Enthalpies of the interaction of protonated dopamine with a hydroxide ion in water-ethanol mixtures in the concentration range of 0-0.8 EtOH mole fractions are measured calorimetrically. The neutralization process of dopamine hydrochloride is shown to occur endothermally in solvents with an ethanol concentration of ≥0.5 mole fractions. Standard thermodynamic characteristics (Δr H ○, Δr G ○, and Δr S ○) of the first-step acid dissociation of dopamine hydrochloride in solutions are calculated with regard to the autoprotolysis enthalpy of binary solvents. It is found that dissociation enthalpies vary within 9.1-64.8 kJ/mol, depending on the water-ethanol solvent composition.

  5. Esterification of pseudoephedrine hydrochloride by citric acid in a solid dose pharmaceutical preparation.

    PubMed

    Goel, Alok; Zhao, Zhicheng; Sørensen, Dan; Zhou, Jay; Zhang, Fa

    2016-09-10

    Esterification of pseudoephedrine hydrochloride (PSE) by citric acid was observed in a solid dose pharmaceutical preparation at room temperature and accelerated stability condition (40°C/75% relative humidity). The esterification of PSE with citric acid was confirmed by a solid-state binary reaction in the presence of minor level of water at elevated temperature to generate three isomeric esters. The structures of the pseudoephedrine citric acid esters were elucidated using high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy (NMR). Occurrence of esterification in solid state, instead of amidation which is generally more favorable than esterification, is likely due to remaining HCl salt form of solid pseudoephedrine hydrochloride to protect its amino group from amidation with citric acid. In contrast, the esterification was not observed from solution reaction between PSE and citric acid.

  6. Evaluation of genotoxic effects of Apitol (cymiazole hydrochloride) in vitro by measurement of sister chromatid exchange.

    PubMed

    Stanimirovic, Zoran; Stevanovic, Jevrosima; Jovanovic, Slobodan; Andjelkovic, Marko

    2005-12-30

    Apitol, with cymiazole hydrochloride as the active ingredient, is used in bee-keeping against the ectoparasitic mite Varroa destructor. The preparation was evaluated for genotoxicity in cultured human peripheral blood lymphocytes. Sister chromatid exchange, the mitotic index and the cell proliferation index were determined for three experimental concentrations of Apitol (0.001, 0.01 and 0.1 mg/ml). All concentrations significantly (p < 0.001) increased the mitotic index (MI = 7.35+/-0.18%, 8.31+/-0.20% and 12.33+/-0.25%, respectively), the proliferative index (PI = 1.83+/-0.01, 1.84+/-0.01 and 1.88+/-0.02, respectively) and the frequency of sister chromatid exchange (SCE = 8.19+/-1.81, 8.78+/-1.80 and 13.46+/-1.88, respectively), suggesting that cymiazole hydrochloride has genotoxic potential.

  7. 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).

  8. Spectrofluorimetric Method for Determination of Duloxetine Hydrochloride in Bulk and Pharmaceutical Dosage Forms

    PubMed Central

    Prabu, S. L.; Shahnawaz, S.; Kumar, C. Dinesh; Shirwaikar, A.

    2008-01-01

    A simple accurate, sensitive and reproducible spectrofluorimetric method was developed for the analysis of duloxetine hydrochloride in pure and pharmaceutical dosage form. Duloxetine hydrochloride showed strong native fluorescence in 0.05 M acetic acid having excitation at 225 nm and emission at 340 nm. Effect of different solvents were thoroughly investigated. The calibration graph was linear in the range from 0.020 to 0.400 μg/ml. The proposed method was statistically validated and successfully applied for analysis of capsule dosage forms. The limit of detection and limit of quantification were found to be 0.003 μg/ml and 0.010 μg/ml, respectively. The percentage recovery was found to be in the range of 98.71% to 99.17%. PMID:20046780

  9. Spectrofluorimetric method for determination of duloxetine hydrochloride in bulk and pharmaceutical dosage forms.

    PubMed

    Prabu, S L; Shahnawaz, S; Kumar, C Dinesh; Shirwaikar, A

    2008-01-01

    A simple accurate, sensitive and reproducible spectrofluorimetric method was developed for the analysis of duloxetine hydrochloride in pure and pharmaceutical dosage form. Duloxetine hydrochloride showed strong native fluorescence in 0.05 M acetic acid having excitation at 225 nm and emission at 340 nm. Effect of different solvents were thoroughly investigated. The calibration graph was linear in the range from 0.020 to 0.400 mug/ml. The proposed method was statistically validated and successfully applied for analysis of capsule dosage forms. The limit of detection and limit of quantification were found to be 0.003 mug/ml and 0.010 mug/ml, respectively. The percentage recovery was found to be in the range of 98.71% to 99.17%. PMID:20046780

  10. Esterification of pseudoephedrine hydrochloride by citric acid in a solid dose pharmaceutical preparation.

    PubMed

    Goel, Alok; Zhao, Zhicheng; Sørensen, Dan; Zhou, Jay; Zhang, Fa

    2016-09-10

    Esterification of pseudoephedrine hydrochloride (PSE) by citric acid was observed in a solid dose pharmaceutical preparation at room temperature and accelerated stability condition (40°C/75% relative humidity). The esterification of PSE with citric acid was confirmed by a solid-state binary reaction in the presence of minor level of water at elevated temperature to generate three isomeric esters. The structures of the pseudoephedrine citric acid esters were elucidated using high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy (NMR). Occurrence of esterification in solid state, instead of amidation which is generally more favorable than esterification, is likely due to remaining HCl salt form of solid pseudoephedrine hydrochloride to protect its amino group from amidation with citric acid. In contrast, the esterification was not observed from solution reaction between PSE and citric acid. PMID:27474946

  11. Spectrophotometric Determination of Cefetamet Pivoxil Hydrochloride and Pitavastatin Calcium in Tablet Dosage form.

    PubMed

    Vadia, N H; Patel, Vandana; Bhalara, H N

    2008-09-01

    Two simple, rapid, specific and accurate analytical methods for the estimation of cefetamet pivoxil hydrochloride and pitavastatin calcium in bulk drug and in their tablet formulations are described. These methods are based on difference spectrophotometry, wherein the measurement is done at maximum 221 nm and minimum 275 nm for cefetamet whereas at maximum 240 nm and minimum 259 nm for pitavastatin. The Beer's law was obeyed in the concentration range of 1-35 μg/ml and 1-25 μg/ml and the molar absorptivities were 1.3×10(4) lit mol(-1) cm(-1) and 2.4×10(4) lit mol(-1) cm(-1) for cefetamet pivoxil hydrochloride and pitavastatin calcium, respectively. The proposed methods were validated and successfully applied to the estimation of drugs in tablet formulations.

  12. Pupil Dilation with Intracameral Epinephrine Hydrochloride during Phacoemulsification and Intraocular Lens Implantation

    PubMed Central

    Yu, A-Yong; Guo, Hua; Wang, Qin-Mei; Bao, Fang-Jun; Huang, Jing-Hai

    2016-01-01

    Objective. To investigate mydriatic effect of intracamerally injected epinephrine hydrochloride during phacoemulsification and intraocular lens (IOL) implantation. Methods. Eighteen cataract patients for bilateral phacoemulsification were enrolled. To dilate pupil, one eye was randomly selected to receive intracamerally 1 mL epinephrine hydrochloride 0.001% for 1 minute after corneal incision (intracameral group), and the contralateral eye received 3 drops of compound tropicamide 0.5% and phenylephrine 0.5% at 5-minute intervals 30 minutes before surgery (topical group). Pupil diameters were measured before corneal incision, before ophthalmic viscoelastic device (OVD) injection, after OVD injection, before IOL implantation, and at the end of surgery. Results. At each time point, the mean pupil diameter in the intracameral group was 2.20 ± 0.08, 5.09 ± 0.20, 6.76 ± 0.19, 6.48 ± 0.18, and 5.97 ± 0.24 mm, respectively, and in the topical group it was 7.98 ± 0.15, 7.98 ± 0.15, 8.53 ± 0.14, 8.27 ± 0.16, and 7.93 ± 0.20 mm, respectively. The topical group consistently had larger mydriatic effects than the intracameral group (P < 0.05). The onset of mydriatic effect was rapid in the intracameral group. There was no difference in surgical performance or other parameters between groups. Conclusions. Intracameral epinephrine hydrochloride appears to be an alternative to the mydriatic modalities for phacoemulsification and IOL implantation. In comparison with topical mydriatics, intracameral epinephrine hydrochloride offers easier preoperative preparation, more rapid pupil dilation, and comparable surgical performance. PMID:26904274

  13. Derivatives of benzimidazole: vasodilator activity of 2-(p-chloro-alpha-hydroxybenzyl)-benzimidazole hydrochloride. Preliminary study.

    PubMed

    Demenge, P; Carraz, G; Luu Duc, C; Silice, C

    1979-01-01

    The effects of 2-(p-chloro-alpha-hydroxybenzyl)-benzimidazole hydrochloride (HBBPC) have been studied in the rabbit and rat. Most of these studies were performed comparatively with reference vasodilators and papaverine. HBBPC vasodilator activity is nearly the same as that of papaverine in the isolated rabbit ear. The characteristic of the vasoactive action of HBBPC seems to reside in its duration. The mechanism of action of HBBPC seems of peripheral type, that is to say it acts on the vascular smooth muscle.

  14. Design, development and permeation studies of nebivolol hydrochloride from novel matrix type transdermal patches

    PubMed Central

    Jatav, Vijay Singh; Saggu, Jitender Singh; Sharma, Ashish Kumar; Sharma, Anil; Jat, Rakesh Kumar

    2013-01-01

    Background: Nebivolol hydrochloride is a third generation β-blocker with highly selective β1-receptor antagonist with antihypertensive properties having plasma half life of 10 h and 12% oral bioavailability. The aim of the present investigation was to form matrix type transdermal patches containing Nebivolol hydrochloride to avoid its extensive hepatic first pass metabolism, lesser side effect and increase bioavailability of drug. Materials and Methods: Matrix type transdermal patches containing Nebivolol hydrochloride were prepared using EudragitRS100, HPMC K100M (2:8) polymers by solvent evaporation technique. Aluminum foil was used as a backing membrane. Polyethylene glycol (PEG) 400 was used as plasticizer and Dimethyl sulfoxide (DMSO) was used as a penetration enhancer. Drug polymer interactions determined by FTIR and standard calibration curve of Nebivolol hydrochloride were determined by using UV estimation. Result: The systems were evaluated physicochemical parameters and drug present in the patches was determined by scanning electron microscopy. All prepared formulations indicated good physical stability. In vitro drug permeation studies of formulations were performed by using Franz diffusion cells using abdomen skin of Wistar albino rat. Result showed best in vitro skin permeation through rat skin as compared to all other formulations prepared with hydrophilic polymer containing permeation enhancer. Conclusions: It was observed that the formulation containing HPMC: EudragitRS100 (8:2) showed ideal higuchi release kinetics. On the basis of in vitro drug release through skin permeation performance, Formulation F1 was found to be better than other formulations and it was selected as the optimized formulation. PMID:24223377

  15. [Forensic chemical investigation of alcohol-containing liquids contained polyhexamethylene guanidine hydrochloride and diethylphthalate].

    PubMed

    Tsisanova, E S; Salomatin, E M

    2010-01-01

    Alcoholism remains one of the main causes of premature death in the population of Russia. Hence, the importance of the problem of uncontrolled distribution and consumption of surrogate alcoholic products, such as alcohol-containing liquids of uncertain origin. The objective of the present study was to detect ethyl alcohol, polyhexamethylene guanidine hydrochloride, and diethylphthalate in disinfectant liquids, biological fluids and human tissues and to analyse qualitative and quantitative composition of these materials. PMID:20821990

  16. 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

  17. 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

  18. HPLC and chemometric methods for the simultaneous determination of cyproheptadine hydrochloride, multivitamins, and sorbic acid.

    PubMed

    el-Gindy, Alaa; el-Yazby, Fawzy; Mostafa, Ahmed; Maher, Moustafa M

    2004-06-29

    Three methods are presented for the simultaneous determination of cyproheptadine hydrochloride (CP), thiamine hydrochloride (B1), riboflavin-5-phosphate sodium dihydrate (B2), nicotinamide (B3), pyridoxine hydrochloride (B6), and sorbic acid (SO). The chromatographic method depends on a high performance liquid chromatographic (HPLC) separation on a reversed-phase, RP 18 column. Elution was carried out with 0.1% methanolic hexane sulphonic acid sodium salt (solvent A) and 0.01 M phosphate buffer containing 0.1% hexane sulphonic acid sodium salt, adjusted to an apparent pH of 2.7 (solvent B). Gradient HPLC was used with the solvent ratio changed from 20:80 to 70:30 (over 9 min), then to 80:20 (over 11 min) for solvent A:B, respectively. Quantitation was achieved with UV detection at 220 and 288 nm based on peak area. The other two chemometric methods applied were principal component regression (PCR) and partial least squares (PLS). These approaches were successfully applied to quantify each drug in the mixture using the information included in the UV absorption spectra of appropriate solutions in the range 250-290 nm with the intervals Deltalambda = 0.4 nm at 100 wavelengths. The chemometric methods do not require any separation step. The three methods were successfully applied to a pharmaceutical formulation and the results were compared with each other.

  19. Denaverine hydrochloride and carbetocin increased welfare during and after parturition and enhanced subsequent fertility in cattle.

    PubMed

    Zobel, Robert; Taponen, Juhani

    2014-01-01

    The objectives of the current study were to investigate the influence of denaverine hydrochloride and carbetocin on softening and dilatation of the birth canal, the need for assistance during parturition, calf mortality, retention of fetal membranes, endometritis, and subsequent fertility. Altogether 200 animals (100 cows and 100 heifers) of the Simmental breed were divided into 2 groups: treatment (n = 100) and control (n = 100). Animals in the treatment group received denaverine hydrochloride and carbetocin (a maximum of twice for each, depending on the progression of labor) during delivery over a maximum of 4 waiting periods (30 min each), whereas control animals experienced the same waiting periods but received no treatment. The treatment protocol had a positive influence on the ease of calving and postpartum reproductive health. The treatment increased the number of animals with the birth canal dilated by more than 25 cm, and halved the need for any assistance at parturition. In addition, treatment decreased the occurrence of difficult calving, the need for episiotomy, the appearance of birth canal lesions, and clinical endometritis. The treatment protocol had an effect throughout the entire puerperal period, as treated animals conceived with fewer artificial inseminations (1.3 vs. 1.6 artificial inseminations/pregnancy) and sooner (67 vs. 78 d open) compared with control animals. Denaverine hydrochloride and carbetocin administered in combination during parturition affected the progression and ease of calving, and thus the welfare of cows in labor and subsequently. However, further studies are needed to confirm the findings and to establish best practices.

  20. Effect of modulated alternating and direct current iontophoresis on transdermal delivery of lidocaine hydrochloride.

    PubMed

    Bhatia, Gaurav; Banga, Ajay K

    2014-01-01

    The objective of this study was to investigate the iontophoretic delivery of lidocaine hydrochloride through porcine skin and to compare the effects of modulated alternating and direct current iontophoresis. Continuous and modulated iontophoresis was applied for one hour and two hours (0-1 h and 4-5th h) using a 1% w/v solution of lidocaine hydrochloride. Tape stripping was done to quantify the amount of drug permeated into stratum corneum and skin extraction studies were performed to determine the amount of drug in stripped skin. Receptor was sampled and analyzed over predefined time periods. The amount of lidocaine delivered across porcine skin after modulated direct current iontophoresis for 2 h was 1069.87 ± 120.03 μ g/sq · cm compared to 744.81 ± 125.41 μ g/sq · cm after modulated alternating current iontophoresis for 2 h. Modulated direct current iontophoresis also enhanced lidocaine delivery by twelvefold compared to passive delivery as 91.27 ± 18.71 μ g/sq · cm of lidocaine was delivered after passive delivery. Modulated iontophoresis enhanced the delivery of lidocaine hydrochloride across porcine skin compared to the passive delivery. Modulated alternating current iontophoresis for duration of 2 h at frequency of 1 kHz was found to be comparable to the continuous direct current iontophoresis for 1 h.

  1. Controlled delivery of ropinirole hydrochloride through skin using modulated iontophoresis and microneedles.

    PubMed

    Singh, Neha D; Banga, Ajay K

    2013-05-01

    The objective of this study was to investigate the effect of modulated current application using iontophoresis- and microneedle-mediated delivery on transdermal permeation of ropinirole hydrochloride. AdminPatch® microneedles and microchannels formed by them were characterized by scanning electron microscopy, dye staining and confocal microscopy. In vitro permeation studies were carried out using Franz diffusion cells, and skin extraction was used to quantify drug in underlying skin. Effect of microneedle pore density and ions in donor formulation was studied. Active enhancement techniques, continuous iontophoresis (74.13 ± 2.20 µg/cm(2)) and microneedles (66.97 ± 10.39 µg/cm(2)), significantly increased the permeation of drug with respect to passive delivery (8.25 ± 2.41 µg/cm(2)). Modulated iontophoresis could control the amount of drug delivered at a given time point with the highest flux being 5.12 ± 1.70 µg/cm(2)/h (5-7 h) and 5.99 ± 0.81 µg/cm(2)/h (20-22 h). Combination of modulated iontophoresis and microneedles (46.50 ± 6.46 µg/cm(2)) showed significantly higher delivery of ropinirole hydrochloride compared to modulated iontophoresis alone (84.91 ± 9.21 µg/cm(2)). Modulated iontophoresis can help in maintaining precise control over ropinirole hydrochloride delivery for dose titration in Parkinson's disease therapy and deliver therapeutic amounts over a suitable patch area and time.

  2. Effect of Modulated Alternating and Direct Current Iontophoresis on Transdermal Delivery of Lidocaine Hydrochloride

    PubMed Central

    Banga, Ajay K.

    2014-01-01

    The objective of this study was to investigate the iontophoretic delivery of lidocaine hydrochloride through porcine skin and to compare the effects of modulated alternating and direct current iontophoresis. Continuous and modulated iontophoresis was applied for one hour and two hours (0-1 h and 4-5th h) using a 1% w/v solution of lidocaine hydrochloride. Tape stripping was done to quantify the amount of drug permeated into stratum corneum and skin extraction studies were performed to determine the amount of drug in stripped skin. Receptor was sampled and analyzed over predefined time periods. The amount of lidocaine delivered across porcine skin after modulated direct current iontophoresis for 2 h was 1069.87 ± 120.03 μg/sq·cm compared to 744.81 ± 125.41 μg/sq·cm after modulated alternating current iontophoresis for 2 h. Modulated direct current iontophoresis also enhanced lidocaine delivery by twelvefold compared to passive delivery as 91.27 ± 18.71 μg/sq·cm of lidocaine was delivered after passive delivery. Modulated iontophoresis enhanced the delivery of lidocaine hydrochloride across porcine skin compared to the passive delivery. Modulated alternating current iontophoresis for duration of 2 h at frequency of 1 kHz was found to be comparable to the continuous direct current iontophoresis for 1 h. PMID:24959580

  3. Application of design of experiment for floating drug delivery of tapentadol hydrochloride.

    PubMed

    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 3(2) 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.

  4. The analysis of methamphetamine hydrochloride by thermal desorption ion mobility spectrometry and SIMPLISMA.

    PubMed

    Reese, E S; Harrington, P B

    1999-01-01

    Ion mobility spectrometry (IMS) has been successfully developed to yield an advanced portable instrument. Such instruments may detect trace quantities of regulated substances at the crime scene. The atmospheric ion chemistry that occurs within the instrument may hinder the determination of analytes in real-world samples. The use of temperature programming adds an extra dimension to the data that improves the selectivity of the IMS data when chemometric processing is applied. The SIMPLISMA (SIMPLe-to-use-Interactive Self-Modeling Mixture Analysis) method is demonstrated for modeling variances in IMS data that are introduced from the temperature program. Methamphetamine hydrochloride IMS peaks are obscured by chemical interferences that arise from cigarette smoke residue. Cigarette smoke residue is pervasive at crime scenes. The ability of SIMPLISMA to resolve the analyte peaks that correspond to methamphetamine hydrochloride from interfering cigarette smoke has been demonstrated. A reduced mobility of 1.62 cm2V-1s-1 was observed for a methamphetamine hydrochloride monomer. With the IMS drift tube at room temperature, a second peak was observed at 1.24 cm2V-1s-1, which is consistent with a dimer ion. This peak has not been previously reported.

  5. 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.

  6. A new hydrophilic interaction liquid chromatographic (HILIC) procedure for the simultaneous determination of pseudoephedrine hydrochloride (PSH), diphenhydramine hydrochloride (DPH) and dextromethorphan hydrobromide (DXH) in cough-cold formulations.

    PubMed

    Ali, Mohammed Shahid; Ghori, Mohsin; Rafiuddin, Syed; Khatri, Aamer Roshanali

    2007-01-01

    A new HILIC method has been developed for the simultaneous determination of pseudoephedrine hydrochloride (PSH), diphenhydramine hydrochloride (DPH) and dextromethorphan hydrobromide (DXH) in cough-cold syrup. Mobile phase consists of methanol:water (containing 6.0 g of ammonium acetate and 10 mL of triethylamine per liter, pH adjusted to 5.2 with orthophosphoric acid), 95:5 (v/v). Column containing porous silica particles (Supelcosil LC-Si, 25 cm x 4.6 mm, 5 microm) is used as stationary phase. Detection is carried out using a variable wavelength UV-vis detector at 254 nm for PSH and DPH, and at 280 nm for DXH. Solutions are injected into the chromatograph under isocratic condition at constant flow rate of 1.2 mL/min. Linearity range and percent recoveries for PSH, DPH and DXH were 150-600, 62.5-250, 75-300 microg/mL and 100.7%, 100.1% and 100.8%, respectively. Method is stability indicating and excipients like saccharin sodium, sodium citrate, flavour and sodium benzoate did not interfere in the analysis. Compounds elute in order of increasing ionization degree caused by cation-exchange mechanism in a run time of less than 15 min. Mobile phase pH is manipulated to regulate ionization and ion-exchange interaction and thereby retention of compounds. PMID:16887317

  7. 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. PMID:26540625

  8. A Rapid, Stability Indicating RP-UPLC Method for Simultaneous Determination of Ambroxol Hydrochloride, Cetirizine Hydrochloride and Antimicrobial Preservatives in Liquid Pharmaceutical Formulation

    PubMed Central

    Trivedi, Rakshit Kanubhai; Patel, Mukesh C.; Jadhav, Sushant B.

    2011-01-01

    A stability indicating reversed phase ultra performance liquid chromatography (RP-UPLC) method was developed for simultaneous determination of ambroxol hydrochloride (AMB), cetirizine hydrochloride (CTZ), methylparaben (MP) and propylparaben (PP) in liquid pharmaceutical formulation. The desired chromatographic separation was achieved on an Agilent Eclipse plus C18, 1.8 μm (50 × 2.1 mm) column using gradient elution at 237 nm detector wavelength. The optimized mobile phase consists of a mixture of 0.01 M phosphate buffer and 0.1 % triethylamine as a solvent-A and acetonitrile as a solvent-B. The developed method separates AMB, CTZ, MP and PP in presence of twelve known impurities/degradation products and one unknown degradation product within 3.5 min. Stability indicating capability was established by forced degradation experiments and seperation of known and unknown degradation products. The lower limit of quantification was established for AMB, CTZ, MP and PP. The developed RP-UPLC method was validated according to the International Conference on Harmonization (ICH) guidelines. This validated method is applied for simultaneous estimation of AMB, CTZ, MP and PP in commercially available syrup samples. Further, the method can be extended for estimation of AMB, CTZ, MP, PP and levo-cetirizine (LCTZ) in various commercially available dosage forms. PMID:21886901

  9. Dietary zilpaterol hydrochloride. II. Carcass composition and meat palatability of beef cattle.

    PubMed

    Leheska, J M; Montgomery, J L; Krehbiel, C R; Yates, D A; Hutcheson, J P; Nichols, W T; Streeter, M; Blanton, J R; Miller, M F

    2009-04-01

    Experiments were conducted at 3 US locations (California, Idaho, and Texas) to determine the effects of dietary zilpaterol hydrochloride and duration of zilpaterol feeding on carcass composition and beef palatability. At each site, 160 steers and 160 heifers were stratified within sex by initial BW (study d -1) and assigned randomly within BW strata to 1 of 4 treatments in a randomized complete block design (4 blocks/treatment for each sex). The 4 treatments were arranged in a 2 (no zilpaterol vs. zilpaterol) x 2 (20- or 40-d duration of zilpaterol feeding) factorial. When included in the diet, zilpaterol was supplemented at 8.3 mg/kg (DM basis). Each pen consisted of 10 animals. After slaughter 2 carcasses per pen (n=64 per trial site) were selected. The entire right side of the selected carcasses was collected for dissection and chemical analysis of the soft tissue. Additionally, the left strip loin was collected for Warner-Bratzler shear force determinations and aged to 28 d postmortem. Sensory analysis was conducted on the Idaho trial site samples only. All data were pooled for analyses. Feeding zilpaterol hydrochloride increased carcass muscle deposition (P<0.01) of both steer and heifer carcasses. However, carcass percentage fat of steers and heifers was not affected (P>0.11) by the zilpaterol treatment. In heifer carcasses, carcass moisture percentage was increased (P=0.04) and bone percentage was decreased (P=0.02), whereas in steer carcasses, carcass moisture and bone percentage were not affected (P>0.10). In heifer carcasses, carcass ash percentage was not affected (P=0.61) by zilpaterol, whereas in steer carcasses, carcass ash percentage tended (P=0.07) to be increased. The protein-to-bone ratio was increased (P<0.001) by zilpaterol hydrochloride treatment in both steers and heifers, whereas the protein-to-fat ratio was not affected (P=0.10). Cooking loss of the LM was not affected (P=0.41) by zilpaterol treatment of steers or heifers. However, LM Warner

  10. Dietary zilpaterol hydrochloride. I. Feedlot performance and carcass traits of steers and heifers.

    PubMed

    Montgomery, J L; Krehbiel, C R; Cranston, J J; Yates, D A; Hutcheson, J P; Nichols, W T; Streeter, M N; Bechtol, D T; Johnson, E; TerHune, T; Montgomery, T H

    2009-04-01

    Experiments were conducted at 3 US locations (CA, ID, and TX) to determine the effects of dietary zilpaterol hydrochloride (Zilmax, Intervet Inc., Millsboro, DE) and duration of zilpaterol feeding on performance and carcass merit of finishing steers and heifers. At each site, 160 steers and 160 heifers were stratified within sex by initial BW (study d -1) and assigned randomly within BW strata to 1 of 4 treatments in a randomized complete block design (4 blocks/treatment for each sex). The 4 treatments were arranged in a 2 (no zilpaterol vs. zilpaterol) x 2 (20 or 40 d duration of zilpaterol feeding) factorial arrangement of treatments. When included in the diet, zilpaterol was supplemented at 8.3 mg/kg of DM. Each pen consisted of 10 animals. Each animal was individually weighed unshrunk on d 1, 21 or 41, and 66 of the experiment. Following d 66, cattle were slaughtered and carcass data collected. Feeding zilpaterol increased (P<0.01) final BW of steers and heifers by 11.6 and 6.7 kg, respectively. In addition, feeding zilpaterol hydrochloride increased (P or= 0.12) and KPH (P >or= 0.70) were not affected by feeding zilpaterol to steers or heifers. Feeding zilpaterol decreased (i.e., improved; P=0.02) calculated yield grade of steer and heifer carcasses. Marbling score (P=0.002) and quality grade (P=0.002) were decreased when zilpaterol hydrochloride was fed to steers, and the decrease in marbling score and quality grade tended to be greater when zilpaterol was fed for 40 compared with 20 d (zilpaterol x duration interaction, P=0

  11. A validated stability-indicative UPLC method for nilotinib hydrochloride for the determination of process-related and degradation impurities.

    PubMed

    Kondra, Sudhakar Babu; Madireddy, Venkataramanna; Chilukuri, Mohanareddy; Papadasu, Narayanareddy; Jonnalagadda, Latha

    2014-09-01

    A novel stability-indicating ultra performance liquid chromatographic (UPLC) method has been developed for quantitative determination of nilotinib hydrochloride in active pharmaceutical ingredients along with four impurities (imp-1, imp-2, imp-3 and imp-4). The method is applicable to the quantification of related compounds and assay of nilotinib hydrochloride drug. Efficient chromatographic separation was achieved on a Shim-pack XR-ODS II, 75 × 3.0 mm, 1.8-µm column with a gradient mobile phase combination. Quantification was carried at 260 nm at a flow rate of 0.6 mL min(-1). Stress degradation conditions were established for nilotinib hydrochloride by subjecting it to acid, base, oxidation, humidity, thermal and photolysis. The stress samples were assayed against a qualified reference standard and the mass balance was found close to 97.0%. The developed UPLC method was validated according to the present International Conference on Harmonisation guidelines for specificity, detection limit, quantitation limit, linearity, accuracy, precision, intermediate precision and robustness. The resolution between nilotinib hydrochloride and four potential impurities is found to be >2.0. Regression analysis shows as r value (correlation coefficient) of >0.999 for nilotinib hydrochloride and four potential impurities.

  12. Alpha-substituted 1-aryl-3-dimethylaminopropanone hydrochlorides: potent cytotoxins towards human WiDr colon cancer cells.

    PubMed

    Pati, Hari Narayan; Das, Umashankar; Ramirez-Erosa, Irving Javier; Dunlop, Donna Mae; Hickie, Robert Allan; Dimmock, Jonathan Richard

    2007-04-01

    A series of 1-aryl-2-dimethylaminomethyl-2-propenone hydrochlorides 1 were prepared which possessed IC(50) values of less than 10 microM when examined towards human WiDr colon cancer cells. The related 1-aryl-2-dimethylaminomethyl-3-hydroxypropanone hydrochlorides 2, formed by hydration of the analogs in series 1, also had IC(50) values in the low micromolar range. On the other hand, conversion of 2-dimethylaminomethyl-1-(4-nitrophenyl)-2-propenone hydrochloride 1c into the corresponding 2-mercaptoethanol of adduct 3c led to a 37-fold reduction in potency. Two thirds of the compounds prepared in this study were more potent than a reference drug cisplatin while one third of these molecules displayed greater cytotoxicity to the WiDr cells than human CRL-2522 fibroblasts. A stability study of the 4-nitrophenyl analog in each of the series 1-3 in deuterium oxide was undertaken. In the case of 1c, replacement of the dimethylamino hydrochloride group by a hydroxy function was noted while in series 2, the loss of both water and dimethylamine hydrochloride gave rise to a mixture of two enones. The mercaptoethanol adduct 3c underwent deamination. The data obtained provide guidelines for amplifying the project in the future. PMID:17409538

  13. p53, Bcl-2 and cox-2 are involved in berberine hydrochloride-induced apoptosis of HeLa229 cells.

    PubMed

    Wang, Hai-Yan; Yu, Hai-Zhong; Huang, Sheng-Mou; Zheng, Yu-Lan

    2016-10-01

    The present study aimed to investigate the effects of berberine hydrochloride on the proliferation and apoptosis of HeLa229 human cervical cancer cells. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was performed to examine the cytotoxicity of berberine hydrochloride against HeLa229 cells. The effects of berberine hydrochloride on the apoptosis of HeLa229 cells was detected by immunofluorescence and flow cytometry, and the mRNA expression levels of p53, B‑cell lymphoma 2 (Bcl‑2) and cyclooxygenase‑2 (cox‑2) were analyzed by reverse transcription-quantitative polymerase chain reaction. Berberine hydrochloride inhibited the proliferation of HeLa229 cells in a dose‑dependent manner; minimum cell viability (3.61%) was detected following treatment with 215.164 µmol/l berberine hydrochloride and the half maximal inhibitory concentration value was 42.93 µmol/l following treatment for 72 h. In addition, berberine hydrochloride induced apoptosis in HeLa229 cells in a dose‑ and time‑dependent manner. Berberine hydrochloride upregulated the mRNA expression levels of p53, and downregulated mRNA expression levels of Bcl‑2 and cox‑2, in a dose‑dependent manner. In conclusion, berberine hydrochloride inhibited the proliferation and induced apoptosis of HeLa229 cells, potentially via the upregulation of p53 and the downregulation of Bcl‑2 and cox‑2 mRNA expression levels. PMID:27601129

  14. Pharmacokinetics and in vivo chemosuppressive activity studies on cryptolepine hydrochloride and cryptolepine hydrochloride-loaded gelatine nanoformulation designed for parenteral administration for the treatment of malaria.

    PubMed

    Kuntworbe, N; Ofori, M; Addo, P; Tingle, M; Al-Kassas, R

    2013-09-01

    The main objective of this investigation was to establish the pharmacokinetics profile and in vivo chemosuppressive activities of cryptolepine hydrochloride-loaded gelatine nanoparticles (CHN) designed for parenteral administration for the treatment of malaria in comparison to the drug free in solution (CHS). Single-dose pharmacokinetics was investigated in Wistar rats by administering CHN or CHS (equivalent to 10 mg/kg of drug) by IV bolus injection via the lateral tail vein. The drug concentration in plasma was monitored over a 24-h period following administration. Chemosuppressive activity was investigated in Wistar rats challenged with P berghei parasites. Animals were given a daily dose of either CHN or CHS, equivalent to 2.5-100 mg/kg by intraperitoneal injection. The level of parasitaemia was determined by light microscopy by examining Giemsa-stained thin blood smears prepared from the tail end on day four of infection. It was found that CHN attained a higher (4.5-folds) area under the curve (AUC (0-24)) compared to CHS. CHS however produced a higher volume of distribution (4-folds). Distribution and elimination rates were higher with CHS which resulted in a lower (11.7 h) elimination half-life compared to that of CHN (21.85 h). The superior pharmacokinetic profile of CHN translated into superior chemosuppressive activity at all dose levels relative to CHS. As a conclusion, loading cryptolepine hydrochloride into gelatine nanoparticles improved both pharmacokinetics and in vivo antiplasmodial activity of the compound with the highest chemosuppression (97.89 ± 3.10) produced by 100 mg/kg of CHN.

  15. A novel spectrofluorimetric method for the assay of pseudoephedrine hydrochloride in pharmaceutical formulations via derivatization with 4-chloro-7-nitrobenzofurazan.

    PubMed

    El-Didamony, Akram M; Gouda, Ayman A

    2011-01-01

    A new highly sensitive and specific spectrofluorimetric method has been developed to determine a sympathomimetic drug pseudoephedrine hydrochloride. The present method was based on derivatization with 4-chloro-7-nitrobenzofurazan in phosphate buffer at pH 7.8 to produce a highly fluorescent product which was measured at 532 nm (excitation at 475 nm). Under the optimized conditions a linear relationship and good correlation was found between the fluorescence intensity and pseudoephedrine hydrochloride concentration in the range of 0.5-5 µg mL(-1). The proposed method was successfully applied to the assay of pseudoephedrine hydrochloride in commercial pharmaceutical formulations with good accuracy and precision and without interferences from common additives. Statistical comparison of the results with a well-established method showed excellent agreement and proved that there was no significant difference in the accuracy and precision. The stoichiometry of the reaction was determined and the reaction pathway was postulated.

  16. Angiotensin II receptor blocker candesartan cilexetil, but not hydralazine hydrochloride, protects against mouse cardiac enlargement resulting from undernutrition in utero.

    PubMed

    Kawamura, Makoto; Itoh, Hiroaki; Yura, Shigeo; Mogami, Haruta; Fujii, Tsuyoshi; Kanayama, Naohiro; Konishi, Ikuo

    2009-10-01

    Epidemiologic studies have shown that malnutrition in utero is a risk factor for cardiovascular disease (CVD) in adulthood. Recently, we reported a mouse animal model of 30% maternal caloric reduction, in which adult offspring (undernourished [UN] offspring) showed a significant increase in cardiac remodeling-associated parameters, such as cardiac enlargement (CE) and coronary perivascular fibrosis (CPVF), as risk factors for CVD. To investigate the possible involvement of the angiotensin system, an angiotensin II receptor antagonist, candesartan cilexetil, or a nonspecific vasodilator, hydralazine hydrochloride, was administrated via a subcutaneously implanted miniosmotic pump to the UN offspring from 9 to 17 weeks after birth. Administration of candesartan cilexetil, but not hydralazine hydrochloride, significantly protected against CE. While administration of not only candesartan cilexetil but also hydralazine hydrochloride prevented an augmentation of CPVF. The angiotensin system seems to make a critical contribution to the developmental origins of cardiac enlargement.

  17. Hydrogen bonds in the crystal packings of mesalazine and mesalazine hydrochloride

    NASA Astrophysics Data System (ADS)

    Banić-Tomišić, Z.; Kojić-Prodić, B.; Širola, I.

    1997-10-01

    The crystal structures of pharmaceutical product mesalazine (marketed also under different proprietary names as Salofalk, Asacol, Asacolitin, and Claversal) and its hydrochloride are reported. In the crystal mesalazine is in zwitterion form as 5-ammoniosalicylate ( 1) whereas mesalazine hydrochloride crystallizes in an ionized form as 5-ammoniosalicylium chloride ( 2). Compound 1 (C 7H 7O 3N) crystallizes in the monoclinic space group {P2 1}/{n} with a = 3.769(1) Å, b = 7.353(2) Å, c = 23.475(5) Å, β = 94.38(2)°, V = 648.7(8) Å3, Z = 4, Dc = 1.568 g cm -3 and μ( MoKα) = 1.2 cm -1. Compound 2 (C 7H 8O 3NCl) crystallizes in the triclinic space group P 1¯ with a = 4.4839(2) Å, b = 5.7936(2) Å, c = 15.6819(5) Å, α = 81.329(3)°, β = 88.026(3)°, γ = 79.317(4)°, V = 395.74(3) Å3, Z = 2, Dc = 1.591 g cm -3 and μ(CuK α) = 40.8 cm -1. The crystal structures were solved by direct methods and refined to R = 0.041 for 1 and 0.028 for 2, using 607 and 1374 observed reflections, respectively. The configuration of both molecules, with the ortho hydroxyl to a carboxyl group, favours the intramolecular hydrogen bonds. Very complex systems of intermolecular hydrogen bonds were observed in both crystal packings. They are discussed in terms of graph-set notation. The mesalazine crystal structure is characterized by two-dimensional network of hydrogen bonds in the ab plane. The crystal structure pattern of mesalazine hydrochloride is a three-dimensional network significantly supported by N +H⋯Cl - interactions.

  18. [Preparation characterization and antitumor activity in vitro of berberine hydrochloride polymeric micelles].

    PubMed

    Ma, Wen-zhuan; Wang, Jin-ling; Tu, Peng-fei

    2015-11-01

    With polyethylene glycol vitamin E succinate (TPGS) as the carrier materials, and berberine hydrochloride ( BER) as model drug, we formed berberine hydrochloride (BER) -loaded TPGS nanomicells (BER-PMs) using filming-rehydration method to improve its solubility and in vitro anti-tumor effect. The transmission electron microscope (TEM) was used to observe the particle appearance; particle detector was used to detect the diameter and Zeta potential; and ultracentrifugation was utilized to determine the encapsulation efficiency (EE) and drug-loading (DD); dynamic dialysis method was used to study the in vitro release behavior of BER-PMs, and the anti-tumor activity against MCF-7 cells was determined by MTT method. Results showed that the average particle size of BER-PMs was (12.45 ± 1.46) nm; particle size was uniform and spherical; drug loading and encapsulation efficiency were (5.7 ± 0.22)% and (95.67 ± 5.35)%, respectively. Zeta potential was (-1.12 ± 0.23) mV; release rate within 24 h was 37.20% and 41.14% respectively in pH 7.4 and pH 6.5 phosphate buffer in vitro; compared with BER, BER-PMs can significantly inhibit MCF-7 cell proliferation (P < 0.05), promote cell apoptosis and improve the anti-tumor activity of BER in vitro. Therefore, the formed berberine hydrochloride micelle can more effectively promote the apoptosis of MCF-7 cell, and improve the drug's in vitro anti-tumor effect. PMID:27071253

  19. Evaluation of metomidate hydrochloride as an anesthetic in leopard frogs (Rana pipiens).

    PubMed

    Doss, Grayson A; Nevarez, Javier G; Fowlkes, Natalie; da Cunha, Anderson F

    2014-03-01

    Metomidate hydrochloride is an imidazole-based, nonbarbiturate hypnotic drug primarily used as an immersion sedation and anesthetic agent in freshwater and marine finfish. To the authors' knowledge, there is no documentation in the literature of its use in amphibians. In this study, 7 male and 4 female leopard frogs (Rana pipiens) were induced with metomidate hydrochloride via immersion bath at a concentration of 30 mg/L for 60 min. The pH of the induction solution ranged from 7.63 to 7.75. Each frog was then removed from the induction solution, rinsed, and recovered in 26.6 degrees C amphibian Ringer's solution. After 210 min in the Ringer's solution, the frogs were transferred to moist paper towels for recovery. Heart rate, gular and abdominal respiration rates, righting reflex, superficial and deep pain withdrawal reflexes, corneal and palpebral reflexes, and escape response were monitored and recorded at defined intervals during both induction and recovery. The average time to loss of righting reflex and escape response was 17.36 min and 17.82 min, respectively. Metomidate produced clinical sedation in all frogs (n = 11). Surgical anesthesia was achieved in only 27% (3/11), with an anesthetic duration that ranged from 9 to 20 min. Recovery times were extremely prolonged and varied, with a range from 313 min to longer than 600 min. The findings of this study indicate that metomidate hydrochloride is unsuitable as a sole anesthetic agent in leopard frogs, and further research is needed to evaluate its suitability in other amphibians. PMID:24712162

  20. Cardiovascular effects in man of intravenous prizidilol hydrochloride (SK&F 92657); a new antihypertensive agent.

    PubMed Central

    Edmonstone, W M; Manghani, K K; Bell, A J; McLeod, M; Milton-Thompson, G J; Burland, W L

    1981-01-01

    1 Cardiovascular responses to intravenous prizidilol hydrochloride (SK&F 92657) 0.86 mg/kg were studied in eight supine resting healthy volunteers. Five subjects were slow and the remaining three were fast acetylators of sulphamethazine. Compared with pre-infusion values, mean resting systolic and diastolic blood pressures were significantly reduced, while mean resting pulse rate was significantly increased at 30 min after the start of the twenty minute infusion. 2 During the 6 h study period the lowest mean +/- s.e. mean systolic blood pressure (108.8 +/- 1.7) was recorded 30 min after the start of the infusion. This represented a mean reduction of 5.2 mmHg. Reductions in mean diastolic blood pressure were greater and of longer duration, the lowest mean value (44.8 +/- 2.0 mmHg) being recorded 3.5 h after the start of the infusion and representing a reduction of 18.5 mmHg from the pre-dosing value. At 6 h after the start of the infusion mean diastolic blood pressure was still significantly reduced (by 15.3 mmHg). 3 The maximum mean +/- s.e. mean resting pulse rate (79.3 +/- 4.4 beats/min) occurred 3 h after the start of the infusion, an increase of 23.0 beats/min over the pre-infusion value. At the end of the study the pulse rate was still significantly raised (by 17.7 beats/min). 4 The left ventricular ejection fraction, evaluated in five subjects, 45 min after the start of the infusion, was not altered by prizidilol hydrochloride, but the left ventricular area decreased significantly. 5 Intravenous prizidilol hydrochloride decreases resting blood pressure and left ventricular area, increases pulse rate and has virtually no effect on left ventricular ejection fraction. PMID:7295490

  1. Simple Isocratic HPLC Method for Determination of Enantiomeric Impurity in Besifloxacin Hydrochloride.

    PubMed

    Kumar, G Pradeep; Srivastava, Vishal; Khandelwal, Kiran; Kumar, Rajesh; Hiriyanna, S G; Kumar, Ajay; Kumar, Pramod

    2016-09-01

    Besifloxacin is a unique chiral broad-spectrum flouroquinolone used in the treatment of bacterial conjunctivitis. R-form of besifloxacin hydrochloride shows higher antibacterial activity as compared to the S-isomer. Therefore, it is necessary to establish chiral purity. To establish chiral purity a high-performance liquid chromatography (HPLC) method for determination of R-besifloxacin and S-besifloxacin (BES impurity A) was developed and validated for in-process quality control and stability studies. The analytical performance parameters such as linearity, precision, accuracy, specificity, limit of detection (LOD), and lower limit of quantification (LOQ) were determined according to International Council for Harmonization ICH Q2(R1) guidelines. HPLC separation was achieved on Chiralpak AD-H (250 x 4.6 mm, 5 μm) column using n-heptane: ethanol: ethylenediamine: acetic acid (800:200:0.5:0.5) (v/v/v/v) as the mobile phase in an isocratic elution. The eluents were monitored by UV/Visible detector at 290 nm. The resolution between S-isomer and besifloxacin hydrochloride was more than 2.0. Based on a signal-to-noise ratio of 3 and 10 the LOD of besifloxacin was 0.30 μg/mL, while the LOQ was 0.90 μg/mL. The calibration curves were linear in the range of 0.9-7.5 μg/mL. Precision of the method was established within the acceptable range. The method was suitable for the quality control enantiomeric impurity in besifloxacin hydrochloride. Chirality 28:628-632, 2016. © 2016 Wiley Periodicals, Inc. PMID:27563753

  2. Thermodynamics of Micellization of Surfactants of Low Aggregation Number: The Aggregation of Propranolol Hydrochloride.

    PubMed

    Mosquera; Ruso; Attwood; Jones; Prieto; Sarmiento

    1999-02-01

    The self-association of propranolol hydrochloride in aqueous solution has been studied as a function of temperature. The critical concentration (C*) and the degree of ionization (alpha) were determined by conductivity measurements at temperatures over the range 298.15 to 313.15 K. The enthalpy change on aggregation in water was measured by microcalorimetry. To calculate changes in the thermodynamic properties of aggregation the mass action model for high and low aggregation numbers was applied, the latter model giving better agreement between experimental and theoretical enthalpy changes. Copyright 1999 Academic Press.

  3. X-ray radiation of poly-L-arginine hydrochloride and multilayered DNA-coatings

    NASA Astrophysics Data System (ADS)

    Stypczyńska, Agnieszka; Nixon, Tony; Mason, Nigel

    2014-11-01

    The aim of this work was to determine the chemical changes induced in thin films of the dry polypeptide poly-L-arginine hydrochloride and its mixture with calf thymus deoxyribonucleic acid (DNA) during 5 h of soft X-ray exposure. The physical and chemical effects of the soft X-ray irradiation were studied using X-ray Photoelectron Spectroscopy (XPS). Analysis of O1 s, N1 s and C1 s features in XPS spectra reveals the existence of several routes of radiation-induced decomposition and shows quantitative and qualitative changes.

  4. Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

    PubMed Central

    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/cm2/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

  5. Selectivity of bevantolol hydrochloride towards alpha- and beta-adrenoceptor subtypes in rat cerebral cortex.

    PubMed

    Takita, M; Kigoshi, S; Muramatsu, I

    1992-02-01

    Selectivity of bevantolol hydrochloride (NC-1400) towards alpha- and beta-adrenoceptor subtypes of rat cerebral cortex was examined in binding experiments and compared with propranolol. Bevantolol biphasically displaced the 3H-dihydroalprenolol binding. The affinity of bevantolol to beta 1-adrenoceptor was equal to that of propranolol. Bevantolol displaced 3H-prazosin binding monophasically but not 3H-p-aminoclonidine binding. These results suggest that bevantolol is a beta 1-adrenoceptor antagonist with a relatively high affinity to alpha 1-adrenoceptor subtypes.

  6. Hydroxylamine hydrochloride-acetic acid-soluble and -insoluble fractions of pelagic sediment: Readsorption revisited

    USGS Publications Warehouse

    Piper, D.Z.; Wandless, G.A.

    1992-01-01

    The extraction of the rare earth elements (REE) from deep-ocean pelagic sediment, using hydroxylamine hydrochloride-acetic acid, leads to the separation of approximately 70% of the bulk REE content into the soluble fraction and 30% into the insoluble fraction. The REE pattern of the soluble fraction, i.e., the content of REE normalized to average shale on an element-by-element basis and plotted against atomic number, resembles the pattern for seawater, whereas the pattern, as well as the absolute concentrations, in the insoluble fraction resembles the North American shale composite. These results preclude significant readsorption of the REE by the insoluble phases during the leaching procedure.

  7. [Successful administration of nifekalant hydrochloride for postoperative junctional ectopic tachycardia in congenital cardiac surgery].

    PubMed

    Sasaki, Tomoyasu; Nemoto, S; Ozawa, H; Katsumata, T; Ozaki, N; Okumura, K; Katayama, H; Tamai, H; Kishida, H

    2007-10-01

    Two episode of junctional ectopic tachycardia (JET) caused hemodynamic deterioration early after tetralogy of Fallot repair in an 8-month-old infant. Sinus rhythm resumed in each of the episodes immediately after intravenous administration of nifekalant hydrochloride (NIF), a newly developed Vaughan-Williams class III antiarrhythmic drug in Japan. Although QT interval was modestly prolonged with NIF, no life-threatening ventricular arrhythmia (i.e., torsades de pointes) occurred. NIF might be an effective alternative in the treatment of postoperative JET in congenital cardiac surgery.

  8. AB212. Clinical study on the treatment of lifelong premature ejaculation with Paroxetine hydrochloride and tamsulosin

    PubMed Central

    Li, Yan-Feng; Zhang, Chao; Li, Bo-Jun

    2016-01-01

    Objective There are quite a few researches about SSRIs and alpha-receptor blockers on the treatment of premature ejaculation (PE), but few researches focus on the combination use of them. In this study, we evaluate the efficacy and safety of combine and alone use of paroxetine hydrochloride and tamsulosin on the treatment of lifelong PE. Methods 352 cases of men with 18–65 years of age, a history of lifelong PE and an intra-vaginal ejaculation latency time (IELT) <120 sec were included in this study. The patients were randomized divided into three groups. Group A were treated by paroxetine hydrochloride 20 mg/d for 8 weeks; group B were treated by tamsulosin 0.2 mg/d for 8 weeks; group C were treated by paroxetine hydrochloride and tamsulosin at the same dosage as above for 8 weeks. The effects were evaluated by the mean change and folds increase in geometric mean IELT and the mean change in all four measures of the premature ejaculation profile (PEP), the adverse events (AEs) and vital sign measurements were recorded at each visit. All the data were statistically analyzed. Results The reliable data from 322 patients were achieved. The geometric mean IELT in group A was significantly increased from 1.15 to 8.13 min after treatment (P<0.001); the geometric mean IELT in group B was significantly increased from 1.26 to 2.78 min after treatment (P<0.01); the geometric mean IELT in group C was significantly increased from 1.18 to 9.52 min after treatment (P<0.001). The increased folds of geometric mean IELT in group C (8.07 folds) was significantly higher than that in group B (2.21 folds) and group A (7.07 folds) (P<0.001). The mean PEP scores that include measures of perceived control over ejaculation, satisfaction with sexual intercourse, ejaculation-related personal distress, and ejaculation-related interpersonal difficulty were significantly improved in all groups after treatment (P<0.001). The mean PEP scores in group C have more significant improvements than

  9. The investigation of the interaction between Oxymetazoline hydrochloride and mucin by spectroscopic approaches

    NASA Astrophysics Data System (ADS)

    Yu, Xianyong; Liu, Heting; Yang, Ying; Lu, Shiyu; Yao, Qin; Yi, Pinggui

    2013-02-01

    The fluorescence and ultraviolet spectroscopy were explored to study the interaction between Oxymetazoline hydrochloride (OMZH) and mucin under imitated physiological condition. The results demonstrated that the fluorescence quenching mechanism between OMZH and mucin is a combined quenching process. The binding constants (Ka), binding sites (n) and the corresponding thermodynamic parameters (ΔG, ΔH, and ΔS) of the interaction system were calculated at different temperatures. The hydrogen bonds and van der Waals forces play a major role in the interaction between OMZH and mucin. According to Förster non-radiation energy transfer theory, the binding distance between OMZH and mucin was calculated.

  10. The investigation of the interaction between Oxymetazoline hydrochloride and mucin by spectroscopic approaches.

    PubMed

    Yu, Xianyong; Liu, Heting; Yang, Ying; Lu, Shiyu; Yao, Qin; Yi, Pinggui

    2013-02-15

    The fluorescence and ultraviolet spectroscopy were explored to study the interaction between Oxymetazoline hydrochloride (OMZH) and mucin under imitated physiological condition. The results demonstrated that the fluorescence quenching mechanism between OMZH and mucin is a combined quenching process. The binding constants (K(a)), binding sites (n) and the corresponding thermodynamic parameters (ΔG, ΔH, and ΔS) of the interaction system were calculated at different temperatures. The hydrogen bonds and van der Waals forces play a major role in the interaction between OMZH and mucin. According to Förster non-radiation energy transfer theory, the binding distance between OMZH and mucin was calculated.

  11. In vivo comet assay of acrylonitrile, 9-aminoacridine hydrochloride monohydrate and ethanol in rats.

    PubMed

    Nakagawa, Yuzuki; Toyoizumi, Tomoyasu; Sui, Hajime; Ohta, Ryo; Kumagai, Fumiaki; Usumi, Kenji; Saito, Yoshiaki; Yamakage, Kohji

    2015-07-01

    As part of the Japanese Center for the Validation of Alternative Methods (JaCVAM)-initiative international validation study of the in vivo rat alkaline comet assay, we examined the ability of acrylonitrile, 9-aminoacridine hydrochloride monohydrate (9-AA), and ethanol to induce DNA damage in the liver and glandular stomach of male rats. Acrylonitrile is a genotoxic carcinogen, 9-AA is a genotoxic non-carcinogen, and ethanol is a non-genotoxic carcinogen. Positive results were obtained in the liver cells of male rats treated with known genotoxic compounds, acrylonitrile and 9-AA.

  12. Preparation and Antiproliferative Activity of Liposomes Containing a Combination of Cisplatin and Procainamide Hydrochloride.

    PubMed

    Viale, Maurizio; Fontana, Antonella; Maric, Irena; Monticone, Massimiliano; Angelini, Guido; Gasbarri, Carla

    2016-09-19

    We have previously reported the enhancement of the antiproliferative and apoptotic activities of cis-diamminedichloroplatinum(II) (DDP) when it is coadministered with a class I antiarrhythmic drug procainamide hydrochloride (PA). Here, we determined the antiproliferative activity of DDP, either in solution or loaded in liposomes, in the presence of PA, in the bulk solution, or directly embedded in liposomes together with DDP. Our results show that PA potentiates the activity of DDP-liposomes and that this effect is maintained at least in some of the investigated cell types when both drugs were mixed and loaded together into liposomes. PMID:27501273

  13. Nitrogen mustard hydrochloride-induced acute respiratory failure and myelosuppression: A case report

    PubMed Central

    ZHANG, XIAOJUAN; ZHANG, ZHIDAN; CHEN, SONG; ZHAO, DONGMEI; ZHANG, FANGXIAO; HU, ZIWEI; XIAO, FENG; MA, XIAOCHUN

    2015-01-01

    Nitrogen mustards are chemical agents that are similar to sulfur mustards, with similar toxicities. The present study describes a case of nitrogen mustard-induced acute respiratory failure and myelosuppression in a 33-year-old man. The patient, who was accidentally exposed to nitrogen mustard hydrochloride in a pharmaceutical factory, exhibited severe inhalation injury and respiratory symptoms. Laboratory tests revealed reduced white blood cell counts and lowered platelet levels during the first 6 days after the skin exposure to nitrogen mustard. Following treatment with mechanical ventilation, immunity-enhancing agents and nutritional supplements for 1 month, the patient successfully recovered and was released from hospital. PMID:26622480

  14. Lyophilized Chitosan/xanthan Polyelectrolyte Complex Based Mucoadhesive Inserts for Nasal Delivery of Promethazine Hydrochloride

    PubMed Central

    G Dehghan, Mohamed Hassan; Marzuka, Marzuka

    2014-01-01

    The objective of this investigation was the development of chitosan/xanthan polyelectrolyte complex based mucoadhesive nasal insert of promethazine hydrochloride a drug used in the treatment of motion sickness. A 32 factorial design was applied for preparing chitosan/xanthan polyelectrolyte complex and to study the effect of independent variables i.e. concentration of xanthan [X1] and concentration of chitosan [X2] on various responses i.e. viscosity of polyelectrolyte complex solution, water uptake of nasal inserts (at pH 2, 5.5, 7.4), bioadhesion potential of nasal inserts and in-vitro drug release at Q6h through nasal inserts. FTIR and DSC analysis were carried out to confirm complex formation and on loaded and unloaded nasal insert to investigate any drug excipient interaction. The nasal inserts were also characterized by powder X-ray diffractometry (PXRD) and Scanning electron microscopy (SEM) and for ex-vivo permeation studies. The results show that higher amount of xanthan in polyelectrolyte complexes with respect to higher amount of chitosan retarded in-vitro drug release. The water uptake behaviour of nasal insert was strongly influenced by pH of the medium and by polycation/ polyanion concentration. The investigation verifies the formation of polyelectrolyte complexes formation between chitosan and xanthan at pH values in the vicinity of pKa intervals of the two polymers and confirms their potential for the nasal delivery of promethazine hydrochloride. PMID:25276178

  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. Bupivacaine hydrochloride complexation with some alpha- and beta-cyclodextrins studied by potentiometry with membrane electrodes.

    PubMed

    Kopecký, Frantisek; Vojteková, Mária; Kaclík, Pavol; Demko, Marek; Bieliková, Zuzana

    2004-05-01

    Membrane electrodes selective to bupivacaine cations were developed and those with PVC-dibutylphthalate membrane containing sparingly soluble bupivacaine phosphotungstate appeared to be the most suitable. Inclusion complexation of bupivacaine cations with cyclodextrins was studied by potentiometric measurements of the free bupivacaine cation concentration in aqueous solutions of bupivacaine hydrochloride with cyclodextrin using the prepared electrodes. Native alpha-cyclodextrin (alpha-CD) and beta-cyclodextrin (beta-CD), as well as their random-substituted derivatives hydroxypropyl-alpha-cyclodextrin (HP-alpha-CD), hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and methyl-beta-cyclodextrin (M-beta-CD), were chosen for the study. The measured potentiometric data processed both by a linear and nonlinear regression corroborated the formation of weak 1:1 bupivacaine cation-cyclodextrin complexes and the corresponding complexation constants K(11) approximately 50-155 M(-1) were evaluated by the non-linear least-squares method. The mutual order of K(11) values, especially alpha-CD > beta-CD, suggested that the bupivacaine butyl group was mainly responsible for the inclusion complexation; the highest K(11) was exhibited by M-beta-CD followed by alpha-CD. The observed complexation may substantially modify properties of bupivacaine hydrochloride dosage forms with sufficient concentration of cyclodextrin but bupivacaine cations are readily released from the weak cyclodextrin complexes by dilution.

  17. Evaluation of the In Vitro Efficacy of Sevelamer Hydrochloride and Sevelamer Carbonate.

    PubMed

    Yang, Yongsheng; Mohammad, Adil; Berendt, Robert T; Carlin, Alan; Khan, Mansoor A; Faustino, Patrick J

    2016-02-01

    The objective of this project is to develop an in vitro approach that can be used to determine the phosphate binding capacity of sevelamer hydrochloride and carbonate for both drug products and active pharmaceutical ingredients (APIs). A simple and efficient inductively coupled plasma spectrometer method for analysis of phosphate at physiologically relevant pH conditions has been developed and validated. The method addresses each of the analytical validation characteristics such as linearity, accuracy, precision, stability, and selectivity, and meets the acceptance criteria defined in the United States Food and Drug Administration guidance (Food and Drug Administration, Center for Drug Evaluation and Research. 2001. Guidance for industry-Bioanalytical method validation, May). The in vitro phosphate binding efficacies were systematically evaluated and compared for two drug products and two APIs. The phosphate binding profiles appeared similar between the drug products. Under all conditions, the sevelamer-phosphate binding reached equilibrium at 6 h. The 90% confidence interval for the k2 ratio (sevelamer carbonate vs. sevelamer hydrochloride) was well within 80%-125% under all pH conditions. However, the k1 ratio varied, indicating that there exists difference in the binding affinity. Our findings will be useful in assisting with "in vivo" biowaiver for the approval of generic sevelamer drug products. PMID:26219932

  18. Mucoadhesive Buccal Tablets Based on Chitosan/Gelatin Microparticles for Delivery of Propranolol Hydrochloride.

    PubMed

    Abruzzo, Angela; Cerchiara, Teresa; Bigucci, Federica; Gallucci, Maria Caterina; Luppi, Barbara

    2015-12-01

    Propranolol administration through buccal route offers some distinct advantages thanks to the easy access to the oral mucosa, fast onset of action, and avoidance of hepatic and intestinal degradation mechanisms. To overcome the effective removal existing in the buccal cavity, mucoadhesive delivery systems are considered a promising approach as they facilitate a close contact with the buccal mucosa. The aim of this study was to prepare mucoadhesive tablets based on chitosan/gelatin microparticles for buccal delivery of propranolol hydrochloride. Spray-dried microparticles were prepared with different chitosan-gelatin weight ratios and characterized in terms of yield and morphology. Microparticles were subsequently compressed with the drug to obtain loaded buccal tablets. In vitro water uptake, mucoadhesion, release, and permeation tests were performed to investigate tablet ability to hydrate, to adhere to the mucosa, and to deliver drug through buccal mucosa. Microparticles showed a different morphology based on the different chitosan-gelatin weight ratios. Moreover, buccal tablets based on the prepared microparticles showed different technological and functional characteristics in virtue of their composition. In particular, tablets with an excess of chitosan showed the best mucoadhesive properties, allowed the permeation of the greatest drug amount among all formulations, and could be promising for buccal administration of propranolol hydrochloride.

  19. Formulation Development and Characterization of Meclizine Hydrochloride Sublimated Fast Dissolving Tablets.

    PubMed

    Vemula, Sateesh Kumar; Vangala, Mohan

    2014-01-01

    The intention of present research is to formulate and develop the meclizine hydrochloride fast dissolving tablets using sublimation method to enhance the dissolution rate. In this study an attempt was made to fasten the drug release from the oral tablets by incorporating the superdisintegrants and camphor as sublimating agent. The prepared fast dissolving tablets were subjected to precompression properties and characterized for hardness, weight variation, friability, wetting time, water absorption ratio, and disintegration time. From in vitro release studies, the formulation F9 exhibited fast release profile of about 98.61% in 30 min, and disintegration time 47 sec when compared with other formulations. The percent drug release in 30 min (Q 30) and initial dissolution rate for formulation F9 was 98.61 ± 0.25%, 3.29%/min. These were very much higher compared to marketed tablets (65.43 ± 0.57%, 2.18%/min). The dissolution efficiency was found to be 63.37 and it is increased by 1.4-fold with F9 FDT tablets compared to marketed tablets. Differential scanning calorimetry and Fourier transform infrared spectroscopy studies revealed that there was no possibility of interactions. Thus the development of meclizine hydrochloride fast dissolving tablets by sublimation method is a suitable approach to improve the dissolution rate. PMID:27355021

  20. Selectivity of bevantolol hydrochloride, a beta 1-adrenoceptor antagonist, in asthmatic patients.

    PubMed

    Löfdahl, C G; Svedmyr, K; Svedmyr, N

    1984-01-01

    Bevantolol hydrochloride, a new beta-adrenoceptor antagonist, has been shown to be cardioselective in animals. To evaluate its selectivity in humans, a double-blind, crossover study was conducted in 8 asthmatics. Following a single oral dose of placebo, bevantolol 75 or 150 mg or propranolol hydrochloride 40 mg, forced expiratory volume in 1 second (FEV1), heart rate, blood pressure and skeletal muscle tremor were measured before and after 4 increasing intravenous doses of terbutaline sulfate to establish terbutaline dose-response curves. The FEV1 decreased after all active treatments. During terbutaline infusions there was an increase in FEV1 after both bevantolol doses and placebo. The terbutaline dose-response curve after bevantolol shifted to the right, however. After propranolol, there was no increase in FEV1 during terbutaline stimulation. Heart rate and skeletal muscle tremor showed a similar pattern during the experiment. In dosages that have previously been shown to produce at least the same degree of blockade of exercise-induced tachycardia, bevantolol has less influence on terbutaline-induced bronchodilation, heart rate increase and skeletal muscle tremor than did propranolol. Thus bevantolol has relative beta 1-adrenoceptor antagonist selectivity. Drawing upon the results of a previous study in the same patients, we believe bevantolol, atenolol and metoprolol have similar beta 1-selectivity.