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1

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)

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 ?M 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.

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

2010-11-01

2

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

Microsoft Academic Search

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

Safwan Ashour; Mahmoud Bahbouh; Mouhammed Khateeb

2011-01-01

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

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. PMID:24378708

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

2014-02-12

4

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

NASA Astrophysics Data System (ADS)

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 ?max 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 ?g 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.

Ashour, Safwan; Bahbouh, Mahmoud; Khateeb, Mouhammed

2011-03-01

5

Quantitative analysis of rabeprazole sodium in commercial dosage forms by spectrophotometry.  

PubMed

The main aim of this work is to develop and validate two spectrophotometric methods for the quantitative analysis of rabeprazole sodium in commercial dosage forms. Method A is based on the reaction of drug with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in the presence of ammonium cerium(IV) nitrate in acetic acid medium at room temperature to form red-brown product which absorbs maximally at 470 nm. Method B utilizes the reaction of rabeprazole sodium with 1-chloro-2,4-dinitrobenzene (CDNB) in dimethyl sulfoxide (DMSO) at 45+/-1 degrees C to form yellow colored Meisenheimer complex. The colored complex has a characteristic band peaking at 420 nm. Under the optimized reaction conditions, proposed methods are validated as per ICH guidelines. Beer's law is obeyed in the concentration ranges of 14-140 and 7.5-165 microg ml(-1) with linear regression equations of A=6.041 x 10(-4)+1.07 x 10(-2)C and A=1.020 x 10(-3)+5.0 x 10(-3)C for methods A and B, respectively. The limits of detection for methods A and B are 1.38 and 0.75 microg ml(-1), respectively. Both methods have been applied successfully for the estimation of rabeprazole sodium in commercial dosage forms. The results are compared with the reference UV spectrophotometric method. PMID:18591818

Rahman, Nafisur; Bano, Zehra; Azmi, Syed Najmul Hejaz

2008-07-01

6

Reduction of formaldehyde concentrations in the air and cadaveric tissues by ammonium carbonate.  

PubMed

The reduction of formaldehyde by ammonium carbonate was examined in cadavers and in vitro. Formaldehyde concentrations in the air (10 cm above human cadavers) and in various cadaveric tissues were measured with or without perfusion of ammonium carbonate solution into formaldehyde-fixed cadavers. Air samples were monitored using Kitagawa gas detector tubes. For measurement of formaldehyde in tissues, muscles and organs were cut into small pieces and tissue fluids were separated out by centrifugation. These specimen fluids were diluted, supplemented with 3-methyl-2-benzothiazolinone hydrazone hydrochloride and quantified by spectrophotometry. In five cadavers without ammonium carbonate treatment, the formaldehyde concentrations in the air above the thorax and in various tissue fluids were 1.2-3.0 p.p.m. and 0.15-0.53%, respectively. Arterial reperfusion of saturated ammonium carbonate solution (1.0, 1.5 or 2.0 L) into five formaldehyde-fixed cadavers successfully reduced the formaldehyde levels, both in the air (0.5-1.0 p.p.m.) and in various tissue fluids (0.012-0.36%). In vitro experiments demonstrated that formaldehyde concentrations decreased, first rapidly and then gradually, with the addition of ammonium carbonate solution into fluids containing formaldehyde. It was confirmed that formaldehyde reacted with the ammonium carbonate and was thereby changed into harmless hexamethylenetetramine. The application of ammonium carbonate solution via intravascular perfusion and, if necessary, by infusion into the thoracic and peritoneal cavities, injection into muscles and spraying on denuded tissues can be anticipated to reduce formaldehyde to satisfactorily low levels in cadaveric tissues and, consequently, in the air, which may provide safe and odorless dissecting rooms. PMID:15453616

Kawamata, Seiichi; Kodera, Haruto

2004-09-01

7

Therapeutic Potential of Hydrazones as Anti-Inflammatory Agents  

PubMed Central

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

Bala, Suman; Sharma, Neha; Saini, Vipin

2014-01-01

8

Ketamine Hydrochloride and Xylazine Hydrochloride  

Microsoft Academic Search

A combination of 100 mg ketamine hydrochloride (KH) and 20 mg xylazine hydro- chloride (XH) was used to immobilize fishers (Martes pennanti). Four adult males were in- tramuscularly injected a total of five times at dosages between 22.4 to 29.0 mg\\/kg KH and 4.1 to 6.6 mg\\/kg XH. Mean (±SE) induction time and arousal time were 3.3 ± 0.5 mm

Jerrold L. Belant

9

Water-soluble Organocatalysts for Hydrazone and Oxime Formation  

PubMed Central

The formation of oximes and hydrazones is widely used in chemistry and biology as a molecular conjugation strategy for achieving ligation, attachment and bioconjugation. However, the relatively slow rate of reaction has hindered its utility. Here we report that simple, commercially available anthranilic acids and aminobenzoic acids act as superior catalysts for hydrazone and oxime formation, speeding the reaction considerably over the traditional aniline-catalyzed reaction at neutral pH. This efficient nucleophilic catalysis, involving catalyst-imine intermediates, allows rapid hydrazone/oxime formation even with relatively low concentrations of the two reactants. The most efficient catalysts are found to be 5-methoxyanthranilic acid and 3,5-diaminobenzoic acid; we find that they can enhance rates by factors of as much as one to two orders of magnitude over the aniline-catalyzed reaction. Evidence based on a range of differently-substituted arylamines suggests that the ortho-carboxylate group in the anthranilate catalysts serves to aid in intramolecular proton transfer during imine and hydrazone formation. PMID:23289546

Crisalli, Pete; Kool, Eric T.

2013-01-01

10

Drug release from hydrazone-containing peptide amphiphiles  

SciTech Connect

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.

Matson, John B.; Stupp, Samuel I. (NWU)

2012-03-15

11

Actual new cancer-causing hydrazines, hydrazides, and hydrazones  

Microsoft Academic Search

Zwanzig aktuelle neue krebsverursachende Hydrazine, Hydrazide und Hydrazone synthetischer oder natürlicher Herkunft werden beschrieben. Diese Substanzen induzieren bei Mäusen, Hamstern und Ratten Tumoren in verschiedenen Zielgeweben. Die Bevölkerung ist neun dieser Verbindungen in Form von Arzneimitteln, Herbiziden oder natürlich vorkommenden Inhaltsstoffen von eßbaren Pilzen ausgesetzt. Bis auf eine Ausnahme ist keines der hier beschriebenen Hydrazine auf krebsinduzierende Eigenschaften beim Menschen

B. Toth

1980-01-01

12

Menthone aryl acid hydrazones: a new class of anticonvulsants.  

PubMed

A series of ten compounds (Compounds J(1)-J(10)) of (±) 3-menthone aryl acid hydrazone was synthesized and characterized by thin layer chromatography and spectral analysis. Synthesized compounds were evaluated for anticonvulsant activity after intraperitoneal (i.p) administration to mice by maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure method and minimal clonic seizure test. Minimal motor impairment was also determined for these compounds. Results obtained showed that four compounds out of ten afforded significant protection in the minimal clonic seizure screen at 6 Hz. Compound J(6), 4-Chloro-N-(2-isopropyl-5-methylcyclohexylidene) benzohydrazide was found to be the most active compound with MES ED(50) of 16.1 mg/kg and protective index (pI) of greater than 20, indicating that (±) 3-menthone aryl acid hydrazone possesses better and safer anticonvulsant properties than other reported menthone derivatives viz. menthone Schiff bases, menthone semicarbazides and thiosemicarbazides. PMID:21235520

Jain, Jainendra; Kumar, Y; Sinha, Reema; Kumar, Rajeev; Stables, James

2011-01-01

13

Diaryl Hydrazones as Multifunctional Inhibitors of Amyloid Self-Assembly†  

PubMed Central

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 were characterized. The inhibitor candidates were evaluated in multiple assays, including the inhibition of A? fibrillogenesis and oligomer formation and the reverse processes, the disassembly of preformed fibrils and oligomers. Since the structure of the hydrazone-based inhibitors mimic the redox features of the antioxidant resveratrol the radical scavenging effect of the compounds was evaluated by colorimetric assays against 2,2-diphenyl-lpicrylhydrazyl (DPPH) 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 considerable effect on the overall activity of the compounds. The inhibitors showed strong activity in the 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 A? species, as well. Atomic Force Microscopy was also applied to monitor the morphology of A? deposits. The compounds also possessed the predicted antioxidant properties; approximately 30% of the synthesized compounds showed equal or better radical scavenging effect than resveratrol or ascorbic acid. PMID:23346953

Torok, Bela; Sood, Abha; Bag, Seema; Tulsan, Rekha; Ghosh, Sanjukta; Borkin, Dmitry; Kennedy, Arleen R.; Melanson, Michelle; Madden, Richard; Zhou, Weihong; LeVine, Harry; Torok, Marianna

2013-01-01

14

Fluorescence quenchers for hydrazone and oxime orthogonal bioconjugation.  

PubMed

We describe the synthesis and properties of new fluorescence quenchers containing aldehyde, hydrazine, and aminooxy groups, allowing convenient bioconjugation as oximes or hydrazones. Conjugation to oligonucleotides proceeded in high yield with aniline as catalyst. Kinetics studies of conjugation show that, under optimal conditions, a hydrazine or aminooxy quencher can react with aldehyde-modified DNA to form a stable hydrazone or oxime adduct in as little as five minutes. The resulting quencher-containing DNAs were assessed for their ability to quench the emission of fluorescein in labeled complements and compared to the commercially available dabcyl and Black Hole Quencher 2 (BHQ2), which were conjugated as phosphoramidites. Results show that the new quenchers possess slightly different absorbance properties compared to dabcyl and are as efficient as the commercial quenchers in quenching fluorescein emission. Hydrazone-based quenchers were further successfully incorporated into molecular beacons and shown to give high signal to background ratios in single nucleotide polymorphism detection in vitro. Finally, aminooxy and hydrazine quenchers were applied to quenching of an aldehyde-containing fluorophore associated with living cells, demonstrating cellular quenching within one hour. PMID:22913527

Crisalli, Pete; Hernández, Armando R; Kool, Eric T

2012-09-19

15

21 CFR 556.350 - Levamisole hydrochloride.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 2010-04-01 false Levamisole hydrochloride. 556.350 Section...of New Animal Drugs § 556.350 Levamisole hydrochloride. A tolerance of 0...established for negligible residues of levamisole hydrochloride in the edible tissues...

2010-04-01

16

Transition metal complexes of an isatinic quinolyl hydrazone  

PubMed Central

Background The importance of the isatinic quinolyl hydrazones arises from incorporating the quinoline ring with the indole ring in the same compound. Quinoline ring has therapeutic and biological activities. On the other hand, isatin (1H-indole-2,3-dione) and its derivatives exhibit a wide range of biological activities. Also, the indole ring occurs in Jasmine flowers and Orange blossoms. Recently, the physiological and biological activities of quinolyl hydrazones arise from their tendency to form metal chelates with transition metal ions. In this context, we have reported to isolate, characterize and study the biological activity of some transition metal complexes of an isatinic quinolyl hydrazone; 3-[2-(4-methyl quinolin-2-yl)hydrazono] indolin-2-one. Results Mono- and binuclear as well as dimeric chelates were obtained from the reaction of a new isatinic quinolyl hydrazone with Fe(III), Co(II), Ni(II), Cu(II), VO(II) and Pd(II) ions. The ligand showed a variety of modes of bonding viz. (NNO)2-, (NO)- and (NO) per each metal ion supporting its ambidentate and flexidentate characters. The mode of bonding and basicity of the ligand depend mainly on the type of the metal cation and its counter anion. All the obtained Pd(II)- complexes have the preferable square planar geometry (D4h- symmetry) and depend mainly on the mole ratio (M:L). Conclusion The effect of the type of the metal ion for the same anion (Cl-) is obvious from either structural diversity of the isolated complexes (Oh, Td and D4h) or the various modes of bonding. The isatinic hydrazone uses its lactim form in all complexes (Cl-) except complex 5 (SO42-) in which it uses its lactam form. The obtained Pd(II)- complexes (dimeric, mono- and binuclear) are affected by the mole ratio (M:L) and have the square planar (D4h) geometry. Also, the antimicrobial activity is highly influenced by the nature of the metal ion and the order for S. aureus bacteria is as follows: Nickel(II) > Vanadyl(II) > Cobalt(II) > Copper(II) ? Palladium(II) >> Iron(III). PMID:21708023

2011-01-01

17

Synthesis and biological activities of diflunisal hydrazide–hydrazones  

Microsoft Academic Search

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

S. Güniz Küçükgüzel; Adil Mazi; Fikrettin Sahin; Suzan Öztürk; James Stables

2003-01-01

18

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

NASA Astrophysics Data System (ADS)

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.

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

2012-12-01

19

Possible Side Effects of Topotecan Hydrochloride, Vincristine  

Cancer.gov

Page of 1Possible Side Effects of Topotecan Hydrochloride, Vincristine (Table Version Date: August 28, 2014) COMMON, SOME MAY BE SERIOUS In 100 people receiving Topotecan Hydrochloride, Vincristine, more than 20 and up to 100 may have: Anemia which may

20

Possible Side Effects of Cyclophosphamide, Topotecan Hydrochloride  

Cancer.gov

Page of 1Possible Side Effects of Cyclophosphamide, Topotecan Hydrochloride (Table Version Date: August 28, 2014) COMMON, SOME MAY BE SERIOUS In 100 people receiving Cyclophosphamide, Topotecan Hydrochloride, more than 20 and up to 100 may have: Hair

21

Physical dependence on Ultram (tramadol hydrochloride)  

E-print Network

Physical dependence on Ultram (tramadol hydrochloride): both opioid-like and atypical withdrawal (tramadol hydrochloride) could be marketed as an analgesic drug without scheduling under the Controlled Elsevier Science Ireland Ltd. All rights reserved. Keywords: Tramadol withdrawal; Ultram ; Physical

Steinbach, Joe Henry

22

IMMOBILIZATION OF SWIFT FOXES WITH KETAMINE HYDROCHLORIDE-XYLAZINE HYDROCHLORIDE  

Microsoft Academic Search

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 hydrochlo- ride and xylazine hydrochloride at different dosages. We attempted to determine appropriate dosages to immobilize swift foxes for an

Rebecca L. Telesco; Marsha A. Sovada

2002-01-01

23

Quinazolin-4-yl-sulfanylacetyl-hydrazone derivatives; Synthesis, molecular structure and electronic properties  

NASA Astrophysics Data System (ADS)

Four new acetylhydrazone derivatives of quinazoline have been synthesized and characterized. The molecular structures and relative stabilities of four possible isomers for each acetylhydrazone are calculated using DFT/B3LYP/6-31G(d,p) method. The calculations results predicted higher stability of the E-isomers compared to the Z-isomers in the gas phase. The syn-E isomer is the predominant form in gaseous phase for all the studied hydrazones except for the hydrazone derived from salicylaldehyde where the anti-E is the most stable isomer. The latter is stabilized by two strong intramolecular H-bonds instead of one in the others. The electronic and spectroscopic properties of the most stable isomers were also calculated using the same level of theory. The calculated atomic polar tensor (APT) charges indicated an increase of the positive charge density at the H-sites involved in the H-bonding interactions. The HOMO and LUMO energies are negative indicating that the compounds under investigation are stable. The electronic transition from the ground state to the excited state belongs to ?-?* transition. The calculated vibrational spectra showed strong red shifts and increase in the vibrational intensity of the Nsbnd H and Osbnd H stretching modes due to the intramolecular H-bonding interactions. In DMSO solution, the NMR spectra of the studied hydrazones revealed that such polar solvents stabilize the syn isomers for all the studied hydrazones except for the hydrazone derived from salicylaldehyde where the anti isomer is the major.

Hagar, Mohamed; Soliman, Saied M.; Ibid, Farahate; El Ashry, El Sayed H.

2013-10-01

24

Spectral characterization and crystal structure of some 2,6-diarylthian-4-one hydrazone derivatives  

NASA Astrophysics Data System (ADS)

A series of cis and trans 2,6-diarylthian-4-one hydrazone derivatives (11-16) have been synthesized and characterized by 1H, 13C and two dimensional NMR spectroscopy. For the 2r,6t-diphenylthian-4-one N-isonicotinoylhydrazone (14) X-ray diffraction have also been recorded. The coupling constants suggested that the cis-hydrazones (11-13), which have the phenyl groups in cis orientation, largely exist in chair conformations with equatorial orientation of the phenyl groups 11C. Analysis of the vicinal coupling constants of trans-hydrazones (14-16) suggests that boat forms 14B must make significant contributions to it and the relative population is 58%. Moreover, in solution chair conformations 14C and 14C?, may contribute to 14. The NOESY and X-ray diffraction of 14 gives definite evidence for the contribution of 14C.

Sankar, C.; Umamatheswari, S.; Pandiarajan, K.

2014-11-01

25

Synthesis, characterization and anti-tubercular activity of ferrocenyl hydrazones and their ?-cyclodextrin conjugates.  

PubMed

A series of ferrocenyl hydrazones and their ?-cyclodextrin (CD) inclusion complexes were prepared and evaluated for antitubercular activity under low and high iron conditions. The inclusion complexes were characterized by Fourier Transform Infrared (FTIR), Differential Scanning Calorimetry (DSC), Powder X-ray Diffraction (PXRD), (1)H NMR, Scanning Electron Microscopy (SEM) and Cyclic Voltammetric (CV) studies. The inclusion complexes exhibited improved aqueous solubility as well as enhanced hydrolytic and thermal stability. They were also found to exhibit greater antitubercular activity than the parent ferrocenyl hydrazones against Mycobacterium tuberculosis under high iron conditions. When grown under low iron conditions these compounds exhibited lower activity suggesting requirement of iron-dependant peroxidase activation. PMID:24751257

Dandawate, Prasad; Vemuri, Kiranmayi; Khan, Ejazuddin M; Sritharan, Manjula; Padhye, Subhash

2014-08-01

26

Asymmetric Synthesis of 2-Substituted Oxetan-3-ones via Metalated SAMP/RAMP Hydrazones  

PubMed Central

2-Substituted oxetan-3-ones can be prepared in good yields and enantioselectivities (up to 84% ee) by the metalation of the SAMP/RAMP hydrazones of oxetan-3-one, followed by reaction with a range of electrophiles that include alkyl, allyl, and benzyl halides. Additionally, both chiral 2,2- and 2,4-disubstituted oxetan-3-ones can be made in high ee (86–90%) by repetition of this lithiation/alkylation sequence under appropriately controlled conditions. Hydrolysis of the resultant hydrazones with aqueous oxalic acid provides the 2-substituted oxetan-3-ones without detectable racemization. PMID:24152298

2013-01-01

27

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

Code of Federal Regulations, 2011 CFR

...promazine hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section...promazine hydrochloride and aminopentamide hydrogen sulfate injection. (a) Chemical...monohydrochloride, and aminopentamide hydrogen sulfate. (b)...

2011-04-01

28

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

Code of Federal Regulations, 2012 CFR

...promazine hydrochloride and aminopentamide hydrogen sulfate injection. 522.1222b Section...promazine hydrochloride and aminopentamide hydrogen sulfate injection. (a) Chemical...monohydrochloride, and aminopentamide hydrogen sulfate. (b)...

2012-04-01

29

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

PubMed

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. PMID:22882834

Eskandari, Habibollah; Naderi-Darehshori, Ali

2012-09-19

30

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

PubMed

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 (?(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. PMID:22817947

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

2012-07-15

31

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

PubMed

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. PMID:15702549

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

2004-01-01

32

An optical test strip for the detection of benzoic acid in food.  

PubMed

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 (K(i)) 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

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

2011-01-01

33

Highly selective suppression of melanoma cells by inducible DNA cross-linking agents: bis(catechol) derivatives.  

PubMed

A series of bis(catechol) quaternary ammonium derivatives were designed and synthesized. We investigated their ability to cross-link DNA induced by tyrosinase and found that the o-quinone is key intermediate in the process by using the nucleophile 3-methyl-2-benzothiazolinone hydrazone (MBTH) in the tyrosinase assay. Their cytotoxicities to B16F1, Hela, and CHO cells were tested by MTT assays. The specific and potent abilities to kill the tyrosinase-efficient melanoma cells kindled our interest in exploring the relationship between their abilities of cross-linking DNA and their selective cytotoxicities to cells. Through an integrated approach including intracellular imaging for detection of the dihydroxyphenyl groups, alkaline comet assays, and ?-H2AX immunofluorescence assays, the speculation was confirmed. The bis(catechol) quaternary ammonium derivatives showed notable cell selectivity because they displayed cytotoxicities after being oxidized by tyrosinase, and they were able to target the DNA efficiently in the tyrosinase-efficient melanoma cells, forming both alkylated and cross-linked species. PMID:20939569

Bai, Minghui; Huang, Jing; Zheng, Xiaolong; Song, Zhibin; Tang, Miru; Mao, Wuxiang; Yuan, Libo; Wu, Jun; Weng, Xiaocheng; Zhou, Xiang

2010-11-01

34

Spectrophotometric determination of hydrogen peroxide, glucose, uric acid, and cholesterol using peroxidase-like activity of an Fe(III) complex of thiacalix[4]arenetetrasulfonate attached to an anion-exchanger.  

PubMed

An iron(III) complex of thiacalix[4]arenetetrasulfonate attached to an anion-exchanger (Fe(3+)-TCASA-500) showed high peroxidase-like catalytic activity at pH 5 - 8 for the formation of quinoid dye, following the color reaction between 3-methyl-2-benzothiazolinone hydrazone (MBTH) and N-ethyl-N-(3-sulfopropyl)aniline (ALPS) in the presence of H2O2. This catalytic activity of Fe(3+)-TCASA-500 for the MBTH-ALPS system was applied for the spectrophotometric determination of H2O2, glucose, uric acid, and cholesterol. The calibration curves were linear in the concentration range from 1.0 to 15 ?g of H2O2 in a 1.0-mL sample solution, and from 5.0 to 60 ?g of glucose, 2.0 to 30 ?g of uric acid, and 11.6 to 116 ?g of cholesterol in a 0.5-mL sample solution. The apparent molar absorptivity of H2O2 was determined as 2.31 × 10(4) L mol(-1) cm(-1), which was about 70% of that by peroxidase under the same conditions. The determination method using Fe(3+)-TCASA-500 was applied for the determination of glucose and uric acid in both control sera I and II. PMID:24212729

Odo, Junichi; Inoguchi, Masahiko; Ohira, Susumu; Tsukikawa, Shinjiro; Aramaki, Misato; Matsuhama, Sawa; Taito, Masahiro; Takayama, Ayumi

2013-01-01

35

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

PubMed Central

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

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

2011-01-01

36

Molecular Structure of Venlafaxine hydrochloride  

NSDL National Science Digital Library

Venlafaxine hydrochloride is white to off-white crystalline solid. Venlafaxine hydrochloride is an extended-release drug prescribed for the treatment of severe mental depression, for the management of anxiety disorders or the short-term relief of the symptoms of anxiety. However, venlafaxine usually is not indicated for the treatment of anxiety or tension associated with the stress of everyday life. Venlafaxine works inhibiting both serotonin and norepinephrine reuptake. It is also used to treat OCD (obsessive-compulsive disorder) or FMS (Fibromyalgia). This drug can present adverse reactions such as tremors, nausea, hyperthermia, dizziness and seizures. Other side effects include anxiety, constipation, dry mouth, loss of appetite, loss of strength, itching, and weight loss.

2004-11-11

37

IMMOBILIZATION OF FREE-RANGING AFRICAN LIONS (PANTHERA LEO) WITH A COMBINATION OF XYLAZINE HYDROCHLORIDE AND KETAMINE HYDROCHLORIDE  

Microsoft Academic Search

The combination of 55 mg\\/ml xy!azine hydrochloride and 200 mg\\/ml ketamine hydrochloride was effective for immobilizing African lions in Tanzania. Nineteen adult females were given between 55 and 110 mg xylazmne hydrochloride in the first dart. Initial doses of 110 mg xylazine hydrochloride and 450 mg ketamine hydrochloride equivalent to >0.9 mg\\/kg xy- lazine hydrochloride were most effective in achieving

L. H. Herbst; C. Packer

38

Z Group Ketone Chain Transfer Agents for RAFT Polymer Nanoparticle Modi cation via Hydrazone Conjugation  

E-print Network

Z Group Ketone Chain Transfer Agents for RAFT Polymer Nanoparticle Modi cation via Hydrazone-fragmentation transfer (RAFT) polymerization. The ketal functionality does not interfere with RAFT polymerization agents. Accessible strategies for controlled radical polymerization such as RAFT1 and ATRP2 have enabled

Bong, Dennis

39

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...

40

Palladium-catalyzed asymmetric allylic alkylation using chiral hydrazone ligands with ferrocene skeleton  

Microsoft Academic Search

Palladium-catalyzed asymmetric allylic alkylation of 1,3-diphenyl-2-propenyl acetate (4) with a dimethyl malonate–BSA–LiOAc system has been successfully carried out in the presence of chiral phosphine–hydrazone ligands such as 3a in good yields with good enantioselectivities (up to 84% ee).

Takashi Mino; Hiroshi Segawa; Masakazu Yamashita

2004-01-01

41

Antineoplastic activity of idazoxan hydrochloride  

Microsoft Academic Search

Purpose  Idazoxan hydrochloride (IDA) is a 241 molecular weight imidazoline and adrenoreceptor ligand. It binds to mitochondrial membranes\\u000a and promotes apoptosis of pancreatic beta cells. Since IDA has not been tested against tumor cells, the purpose of our study\\u000a was to determine if IDA has antineoplastic activity.\\u000a \\u000a \\u000a \\u000a Methods  We used the conversion of a soluble tetrazolium salt to an insoluble formazan precipitate

G. F. Eilon; L. Weisenthal; M. Stupecky; G. Landucci; L. M. Slater

2009-01-01

42

Spectrophotometric determination of etilefrine hydrochloride and ritodrine hydrochloride through nitrosation and subsequent cobalt chelation.  

PubMed

A simple and rapid method for the determination of etilefrine hydrochloride and ritodrine hydrochloride, either in pure form or in pharmaceutical formulations, is described. The method is based on the development of red product in presence of sodium nitrite and cobalt(II) salt in acid medium. The reaction is thought to proceed via preliminary nitrosation of the phenolic nucleus followed by formation of the chelate in presence of cobalt(II) salt. The highly colored chelates showed wavelengths of maximum absorption of 570 and 560 nm for etilefrine hydrochloride and ritodrine hydrochloride, respectively. The reaction product showed apparent molar absorptivities of 938 and 2930 L mol-1 cm-1 for etilefrine hydrochloride and ritodrine hydrochloride, respectively. A linear correlation was found between absorbance (at the lambda max) and concentration in ranges of 0.08-0.20 and 0.04-0.10 mg ml-1 for etilefrine hydrochloride and ritodrine hydrochloride, respectively. At the same time, the resulting colors were well developed within 25 min at boiling water bath temperature and were stable for more than 1 hr. Results of analysis of pure drugs and their dosage forms by the proposed method were in good agreement with either a reported derivative spectrophotometric procedure or the USP XXII method for etilefrine hydrochloride and ritodrine hydrochloride, respectively. The validity of the method was further confirmed using the standard addition method. The proposed method demonstrate high percentage of recovery with good accuracy and precision. PMID:7572192

Bakry, R S; el Walily, A M; Belal, S F

1995-07-01

43

Thermoanalytical Investigation of Terazosin Hydrochloride  

PubMed Central

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

Attia, Ali Kamal; Mohamed Abdel-Moety, Mona

2013-01-01

44

The ligational behavior of a phenolic quinolyl hydrazone towards copper(II)- ions  

PubMed Central

Background The heterocyclic hydrazones constitute an important class of biologically active drug molecules. The hydrazones have also been used as herbicides, insecticides, nematocides, redenticides, and plant growth regulators as well as plasticizers and stabilizers for polymers. The importance of the phenolic quinolyl hydrazones arises from incorporating the quinoline ring with the phenolic compound; 2,4-dihydroxy benzaldehyde. Quinoline ring has therapeutic and biological activities whereas, phenols have antiseptic and disinfectants activities and are used in the preparation of dyes, bakelite and drugs. The present study is planned to check the effect of the counter anions on the type and geometry of the isolated copper(II)- complexes as well as the ligational behavior of the phenolic hydrazone; 4-[(2-(4,8-dimethylquinolin-2-yl)hydrazono)methyl] benzene-1,3-diol; (H2L). Results A phenolic quinolyl hydrazone (H2L) was allowed to react with various copper(II)- salts (Cl?, Br?, NO3?, ClO4?, AcO?, SO42-). The reactions afforded dimeric complexes (ClO4?, AcO? ), a binuclear complex (NO3? ) and mononuclear complexes (the others; Cl?, Br?, SO42-). The isolated copper(II)- complexes have octahedral, square pyramid and square planar geometries. Also, they reflect the strong coordinating ability of NO3?, Cl?, Br?, AcO? and SO42- anions. Depending on the type of the anion, the ligand showed three different modes of bonding viz. (NN)0 for the mononuclear complexes (3, 4, 6), (NO)- with O- bridging for the dimeric complexes (1, 5) and a mixed mode [(NN)0 + (NO)- with O- bridging] for the binuclear nitrato- complex (2). Conclusion The ligational behavior of the phenolic hydrazone (H2L) is highly affected by the type of the anion. The isolated copper(II)- complexes reflect the strong coordinating power of the SO42-, AcO?, Br?, Cl? and NO3? anions. Also, they reflect the structural diversity (octahedral, square pyramid and square planar) depending on the type of the counter anion. PMID:21223587

2011-01-01

45

Acute Psychotic Symptoms due to Benzydamine Hydrochloride Abuse with Alcohol  

PubMed Central

Benzydamine hydrochloride is a locally acting nonsteroidal anti-inflammatory drug. Benzydamine hydrochloride overdose can cause stimulation of central nervous system, hallucinations, and psychosis. We presented a young man with psychotic symptoms due to benzydamine hydrochloride abuse. He received a total dose of 1000?mg benzydamine hydrochloride with alcohol for its hallucinative effects. Misuse of benzydamine hydrochloride must be considered in differential diagnosis of first-episode psychosis and physicians should consider possibility of abuse in prescribing. PMID:25343054

Acar, Yahya Ayhan; Kalkan, Mustafa; Cetin, R?dvan; Cevik, Erdem; C?nar, Orhan

2014-01-01

46

Acute Psychotic Symptoms due to Benzydamine Hydrochloride Abuse with Alcohol.  

PubMed

Benzydamine hydrochloride is a locally acting nonsteroidal anti-inflammatory drug. Benzydamine hydrochloride overdose can cause stimulation of central nervous system, hallucinations, and psychosis. We presented a young man with psychotic symptoms due to benzydamine hydrochloride abuse. He received a total dose of 1000?mg benzydamine hydrochloride with alcohol for its hallucinative effects. Misuse of benzydamine hydrochloride must be considered in differential diagnosis of first-episode psychosis and physicians should consider possibility of abuse in prescribing. PMID:25343054

Acar, Yahya Ayhan; Kalkan, Mustafa; Cetin, R?dvan; Cevik, Erdem; C?nar, Orhan

2014-01-01

47

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

PubMed

Immobilization of North American porcupines (Erethizon dorsatum) with tiletamine hydrochloride (HCl) and zolazepam HCl (Telazol) was evaluated in central Massachusetts (USA) during 1991 and 1992. Doses between 9 and 11 mg/kg resulted in a mean (+/- SD) induction time of 3.2 +/- 1.3 min and a mean (+/- SD) immobilization time of 44.2 +/- 19.5 min. Induction time did not differ by dose, sex, capture method, or porcupine weight. Immobilization time differed by dose and porcupine weight but not by sex or capture method. Tiletamine HCl and zolazepam HCl seems to be an effective combination of drugs for immobilizing porcupines as long as sufficient time is allowed for recovery. PMID:7933289

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

1994-07-01

48

Immobilization of swift foxes with ketamine hydrochloride-xylazine hydrochloride.  

PubMed

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 < or = 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. PMID:12528444

Telesco, Rebecca L; Sovada, Marsha A

2002-10-01

49

Bradyarrhythmias secondary to topical levobunolol hydrochloride solution  

PubMed Central

An 88-year-old man was admitted with fatigue, dizziness, and heart palpitations. Both the electrocardiogram and Holter confirmed the existence of sinus bradycardia and sinus arrest. One hour prior to the onset of symptoms, he received levobunolol hydrochloride solution topically. The levobunolol hydrochloride solution was discontinued and the bradycardia resolved. He was diagnosed as having intermittent sinus bradycardia and sinus arrest, induced by topical ?-blocker therapy. Levobunolol hydrochloride solution is an effective therapy for ocular hypertension, probably by reducing aqueous fluid production. However, it can induce cardiac side effects such as bradyarrhythmia and should be used with caution in elderly patients or patients with cardiac disease. PMID:25342892

Lin, Lianjun; Wang, Yuchuan; Chen, Yan; Liu, Meilin

2014-01-01

50

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

NASA Astrophysics Data System (ADS)

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.

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

2012-01-01

51

PEGylated polyamidoamine dendrimers with bis-aryl hydrazone linkages for enhanced gene delivery.  

PubMed

Surface modification of polyamidoamine (PAMAM) dendrimers with polyethylene glycol (PEG) often results in the decrease in their buffering capacity, which is essential for gene transfer. In this work, bis-aryl hydrazone bond, which possesses protonatable pyridine and amines, was explored as a new linkage for PEGylation of PAMAM dendrimers. PEGylated polyamidoamine (PAMAM) dendrimer G4.0 conjugates with bis-aryl hydrazone (BAH) linkages were synthesized following a two-step procedure: activation of PAMAM dendrimer G4.0 and monofunctional methoxypolyethylene glycol amine (MW=5000 Da) with succinimidyl 4-hydrazinonicotinate acetone hydrazone (SANH) and succinimidyl 4-formylbenzoate (SFB), respectively, and coupling of SFB-activated PEG to SANH-activated G4.0 to generate PEGylated G4.0 with bis-aryl hydrazone linkages (G4.0-BAH-PEG). It was found that the incorporation of BAH linkages into the vector significantly enhanced the buffering capacity of the vector even with a high degree of PEGylation (42 PEG chains per dendrimer). G4.0-BAH-PEG conjugates could complex with DNA plasmid tightly at low weight ratios and display dramatically improved cytocompatibility. According to gene transfection studies in 293T and HN12 cells, this new vector has been shown to be capable of both transfecting more cells and inducing higher gene expression than the parent dendrimer. This work demonstrates that the use of the BAH linkage in coupling of PEG to the dendrimer helps maintain or increase the buffering capacity of the functionalized dendrimer and results in enhanced transfection. PMID:20593893

Yuan, Quan; Yeudall, W Andrew; Yang, Hu

2010-08-01

52

Salicylaldehyde hydrazones as fluorescent probes for zinc ion in aqueous solution of physiological pH  

Microsoft Academic Search

Salicylaldehyde hydrazones of 1 and 2 were synthesized and their potential as fluorescent probes for zinc ion was investigated in this paper. Both of the probes were found to show fluorescence change upon binding with Zn2+ in aqueous solutions, with good selectivity to Zn2+ over other metal ions such as alkali\\/alkali earth metal ions and heavy metal ions of Pb2+,

Na Li; Yu Xiang; Xiaotong Chen; Aijun Tong

2009-01-01

53

Synthesis and characterization of platinum-sterol hydrazone complexes with biological activity against Leishmania (L.) mexicana.  

PubMed

Leishmaniasis is a parasitic zoonosis caused by protozoans of the genus Leishmania transmitted by insects known as phlebotomines, which are found in wild or urban environments. The disease occurs in tropical and sub-tropical areas, mainly in Asia, Europe, Africa and the Americas. At present, there is no effective treatment for this disease. In the search for new rational chemotherapeutic alternatives, two novel trans [Pt(Hpy1)(2)(Cl)(2)] (1) and trans [Pt(Hpy2)(2) (Cl)(2)] (2) complexes were synthesized by the reaction of K(2)PtCl(4) with sterol hydrazone ligands 20-hydrazone-pyridin-2-yl-5alpha-pregnan-3beta-ol (Hpy1) and 22-hydrazone-pyridin-2-yl-chol-5-ene-3beta-ol (Hpy2). These organic compounds are specific inhibitors of sterol methyl transferase (SMT). The new platinum complexes were characterized by a combination of ESI-MS (electrospray ionization-mass spectroscopy), UV-vis, infrared and NMR spectroscopies; elemental analysis and molar conductivity. Promastigotes of Leishmania (L.) mexicana were treated for 48 h with 10 microM of the sterol hydrazones Hpy1 or Hpy2 alone or coordinated to Pt. Hpy1 produced higher leishmanistatic activity than Hpy2 (39% growth inhibition vs. 16%), which significatively increased (71%, p<0.001) when the complex trans-[Pt(Hpy1)(2)(Cl)(2)] was used. This complex represents a new chemotherapeutic alternative to be evaluated in depth in experimental models of leishmaniasis. PMID:18164763

Visbal, Gonzalo; Marchán, Edgar; Maldonado, Alexis; Simoni, Zulay; Navarro, Maribel

2008-03-01

54

Design, synthesis, computational calculation and biological evaluation of some novel 2-thiazolyl hydrazones.  

PubMed

In the present study a novel series of 1-(1-(4-isobutylphenyl)ethylidene)-2-(4-phenylthiazol-2-yl)hydrazine 2a and its derivatives 2b-2f have been synthesized by the cyclization of 1-(1-(4-isobutylphenyl)ethylidene)thiosemicarbazide with 2-bromoacetophenone/ 4-substituted 2-bromoacetophenones. The structures of the synthesized thiazolyl hydrazones 2a-2f were characterized by FT-IR, (1)H, (13)C NMR, 2D NMR and mass spectral techniques. The molecular geometries were also investigated theoretically using B3LYP functional with 6-311G(d,p) basis set. To explain the molecular properties energy gap (Eg), electronegativity (?), hardness (g), electrophilicity (?) and softness (S) were computed, natural bonding orbital (NBO) analysis and molecular electrostatic potential (MEP) were also performed at the same level of theory. All the synthesized thiazolyl hydrazones 2a-2f were screened for their in vitro antimicrobial activity against selected bacterial and fungal strains. The results showed that the heterocyclic thiazolyl hydrazone derivatives exhibit a promising selective inhibitory activity against various bacterial and fungal strains. PMID:25168236

Anbazhagan, R; Sankaran, K R

2015-01-25

55

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

PubMed Central

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

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

2012-01-01

56

Biaryl Amides and Hydrazones as Therapeutics for Prion Disease in Transgenic Mice  

PubMed Central

The only small-molecule compound demonstrated to substantially extend survival in prion-infected mice is a biaryl hydrazone termed “Compd B” (4-pyridinecarboxaldehyde,2-[4-(5-oxazolyl)phenyl]hydrazone). However, the hydrazone moiety of Compd B results in toxic metabolites, making it a poor candidate for further drug development. We developed a pharmacophore model based on diverse antiprion compounds identified by high-throughput screening; based on this model, we generated biaryl amide analogs of Compd B. Medicinal chemistry optimization led to multiple compounds with increased potency, increased brain concentrations, and greater metabolic stability, indicating that they could be promising candidates for antiprion therapy. Replacing the pyridyl ring of Compd B with a phenyl group containing an electron-donating substituent increased potency, while adding an aryl group to the oxazole moiety increased metabolic stability. To test the efficacy of Compd B, we applied bioluminescence imaging (BLI), which was previously shown to detect prion disease onset in live mice earlier than clinical signs. In our studies, Compd B showed good efficacy in two lines of transgenic mice infected with the mouse-adapted Rocky Mountain Laboratory (RML) strain of prions, but not in transgenic mice infected with human prions. The BLI system successfully predicted the efficacies in all cases long before extension in survival could be observed. Our studies suggest that this BLI system has good potential to be applied in future antiprion drug efficacy studies. PMID:23965382

Lu, Duo; Giles, Kurt; Li, Zhe; Rao, Satish; Dolghih, Elena; Gever, Joel R.; Geva, Michal; Elepano, Manuel L.; Oehler, Abby; Bryant, Clifford; Renslo, Adam R.; Jacobson, Matthew P.; DeArmond, Stephen J.; Silber, B. Michael

2013-01-01

57

21 CFR 520.2002 - Propiopromazine hydrochloride.  

...potentiate the toxicity of organophosphates and the activity of procaine hydrochloride. Overdosage may produce significant depression. (3) For use only by or on the order of a licensed veterinarian. [40 FR 13838, Mar. 27, 1975, as amended...

2014-04-01

58

21 CFR 520.2002 - Propiopromazine hydrochloride.  

Code of Federal Regulations, 2012 CFR

...potentiate the toxicity of organophosphates and the activity of procaine hydrochloride. Overdosage may produce significant depression. (3) For use only by or on the order of a licensed veterinarian. [40 FR 13838, Mar. 27, 1975, as amended...

2012-04-01

59

21 CFR 520.2002 - Propiopromazine hydrochloride.  

Code of Federal Regulations, 2013 CFR

...potentiate the toxicity of organophosphates and the activity of procaine hydrochloride. Overdosage may produce significant depression. (3) For use only by or on the order of a licensed veterinarian. [40 FR 13838, Mar. 27, 1975, as amended...

2013-04-01

60

Possible Side Effects of Cyclophosphamide, Etoposide, Topotecan Hydrochloride  

Cancer.gov

Page of 1Possible Side Effects of Cyclophosphamide, Etoposide, Topotecan Hydrochloride (Table Version Date: August 28, 2014) COMMON, SOME MAY BE SERIOUS In 100 people receiving Cyclophosphamide, Etoposide, Topotecan Hydrochloride, more than 20 and

61

21 CFR 520.1242 - Levamisole hydrochloride oral dosage forms.  

Code of Federal Regulations, 2011 CFR

...false Levamisole hydrochloride oral dosage forms. 520.1242...ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED...FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS...1242 Levamisole hydrochloride oral dosage...

2011-04-01

62

21 CFR 182.1047 - Glutamic acid hydrochloride.  

Code of Federal Regulations, 2011 CFR

21 Food and Drugs 3 2011-04-01 ...2011-04-01 false Glutamic acid hydrochloride. 182...Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT...182.1047 Glutamic acid hydrochloride....

2011-04-01

63

21 CFR 182.1047 - Glutamic acid hydrochloride.  

21 Food and Drugs 3 2014-04-01 ...2014-04-01 false Glutamic acid hydrochloride. 182...Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT...182.1047 Glutamic acid hydrochloride....

2014-04-01

64

21 CFR 182.1047 - Glutamic acid hydrochloride.  

Code of Federal Regulations, 2010 CFR

21 Food and Drugs 3 2010-04-01 ...2009-04-01 true Glutamic acid hydrochloride. 182...Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT...182.1047 Glutamic acid hydrochloride....

2010-04-01

65

21 CFR 182.1047 - Glutamic acid hydrochloride.  

Code of Federal Regulations, 2013 CFR

21 Food and Drugs 3 2013-04-01 ...2013-04-01 false Glutamic acid hydrochloride. 182...Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT...182.1047 Glutamic acid hydrochloride....

2013-04-01

66

21 CFR 182.1047 - Glutamic acid hydrochloride.  

Code of Federal Regulations, 2012 CFR

21 Food and Drugs 3 2012-04-01 ...2012-04-01 false Glutamic acid hydrochloride. 182...Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT...182.1047 Glutamic acid hydrochloride....

2012-04-01

67

21 CFR 520.1242 - Levamisole hydrochloride oral dosage forms.  

Code of Federal Regulations, 2010 CFR

...and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride oral dosage forms. 520.1242 Section 520...PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242 Levamisole hydrochloride oral dosage...

2010-04-01

68

[Simultaneous determination of pseudoephedrine hydrochloride and dextromethorphan hydrobromide in composite pseudoephedrine hydrochloride dry suspension by HPLC].  

PubMed

A simple and reliable reversed-phase high performance liquid chromatographic method (HPLC) for the routine analysis of pseudoephedrine hydrochloride and dextromethorphan hydrobromide in composite pseudoephedrine hydrochloride dry suspension has been established. HPLC determination for the drug was performed in a Lichrospher C6H6 column and detected at 220 nm. Acetonitrile-H2O-H3PO4 (50:50:0.1, v/v, pH 2.5, containing 1 g/L sodium dodecyl sulfate) was used as the mobile phase and the flow rate was 1.2 mL/min. The method was proved to be linear in the ranges of 1.03-206 mg/L and 5-200 mg/L for dextromethorphan hydrobromide and pseudoephedrine hydrochloride, respectively. The relative standard deviations of intra-assay (n = 7) and inter-assay (n = 5) were 1.0% and 1.5% for pseudoephedrine hydrochloride analysis and 1.8% and 2.2% for dextromethorphan hydrobromide analysis. The recoveries of pseudoephedrine hydrochloride and dextromethorphan hydrobromide were 95.7%-98.7% and 100.0%-101.8%, respectively. The method has been successfully applied to the simultaneous determination of pseudoephedrine hydrochloride and dextromethorphan hydrobromide in composite pseudoephedrine hydrochloride dry suspension. PMID:15881374

Li, Ke

2005-01-01

69

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

PubMed

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

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

2014-02-01

70

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

PubMed

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. PMID:25092585

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

2014-10-01

71

Synthesis, antifungal activities and qualitative structure activity relationship of carabrone hydrazone derivatives as potential antifungal agents.  

PubMed

Aimed at developing novel fungicides for relieving the ever-increasing pressure of agricultural production caused by phytopathogenic fungi, 28 new hydrazone derivatives of carabrone, a natural bioactive sesquisterpene, in three types were designed, synthesized and their antifungal activities against Botrytis cinerea and Colletotrichum lagenarium were evaluated. The result revealed that all the derivatives synthesized exhibited considerable antifungal activities in vitro and in vivo, which led to the improved activities for carabrone and its analogues and further confirmed their potential as antifungal agents. PMID:24619221

Wang, Hao; Ren, Shuang-Xi; He, Ze-Yu; Wang, De-Long; Yan, Xiao-Nan; Feng, Jun-Tao; Zhang, Xing

2014-01-01

72

Synthesis, Antifungal Activities and Qualitative Structure Activity Relationship of Carabrone Hydrazone Derivatives as Potential Antifungal Agents  

PubMed Central

Aimed at developing novel fungicides for relieving the ever-increasing pressure of agricultural production caused by phytopathogenic fungi, 28 new hydrazone derivatives of carabrone, a natural bioactive sesquisterpene, in three types were designed, synthesized and their antifungal activities against Botrytis cinerea and Colletotrichum lagenarium were evaluated. The result revealed that all the derivatives synthesized exhibited considerable antifungal activities in vitro and in vivo, which led to the improved activities for carabrone and its analogues and further confirmed their potential as antifungal agents. PMID:24619221

Wang, Hao; Ren, Shuang-Xi; He, Ze-Yu; Wang, De-Long; Yan, Xiao-Nan; Feng, Jun-Tao; Zhang, Xing

2014-01-01

73

Syntheses and extraction properties of novel biscalixarene and thiacalix[4]arene hydrazone derivatives  

Microsoft Academic Search

By reacting thiacalix[4]arene with p-tosyloxyethoxylbenzaldehyde 1, 3-bis(benzaldehyde-4-oxyethyloxy)-p-tert-butylthiacalix[4]arene (2) were prepared in yield of 65%. Refluxing compound 2 with aniline, salicylic hydrazide, nicotinic hydrazide and isonicotinic hydrazide, novel ringopening 1,3-bis-arylformyl-hydrazone substituted thiacalix[4]arene derivatives (3a–3d) were obtained in yields of 77–89%. Refluxing compound 2 with o-phenylendiamine, oxalyl dihydrazide, malonic dihydrazide and adipic dihydrazide in “1 + 1” intermolecular condensation mode\\u000a under diluted condition, novel

Fafu Yang; Xia Zhao; Hongyu Guo; Jianrong Lin; Zhaohui Liu

2008-01-01

74

Immobilization of Coypus (Myocastor coypus) with Ketamine Hydrochloride and Xylazine Hydrochloride  

Microsoft Academic Search

A combination of 100 mg\\/ml of ketamine hydrochloride (Ket) and 20 mg\\/ml of xylazine hydrochloride (Xyl) was used to im- mobilize coypus (Myocastor coypus). Eight ma- ture coypus (four males and four females) were injected intramuscularly with doses ranging from 2.33 to 6.25 mg\\/kg of KET and 0.25 to 0.86 mg\\/kg of Xyl. The mean (±SE) time for in- duction,

R. F. Bo; F. Palomares; J. F. Beltr; S. Moreno; Caeser Kleberg

75

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

PubMed

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. PMID:24667418

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

2014-07-15

76

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

NASA Astrophysics Data System (ADS)

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.

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

2014-07-01

77

DMSO containing ruthenium(ii) hydrazone complexes: in vitro evaluation of biomolecular interaction and anticancer activity.  

PubMed

Synthesis, spectral, electrochemical and single crystal X-ray diffraction data of a new series of DMSO containing bivalent ruthenium hydrazone complexes are presented. XRD data of two of the new complexes revealed an octahedral coordination around the ruthenium ion satisfied by NOS2Cl2 atoms. Electrochemical studies showed the metal centred, quasi-reversible, one-electron redox behaviour of the new complexes. The binding of these complexes with biomolecules such as calf thymus DNA (CT-DNA) and bovine serum albumin (BSA) protein investigated by different spectrophotometric methods revealed an intercalative mode of interaction. The in vitro cytotoxicity of these complexes evaluated by the MTT assay on a panel of cancer and normal cell lines indicated that the above complexes are more toxic to cancer cells with a few micromolar concentrations as the IC50 value, but are significantly less toxic to normal cell lines. The observed variations in the binding interactions and cytotoxicity of the complexes were attributed to the nature of the hydrazide moiety of the hydrazones that influences their biological activities. PMID:25223849

Alagesan, M; Sathyadevi, P; Krishnamoorthy, P; Bhuvanesh, N S P; Dharmaraj, N

2014-10-01

78

40 CFR 180.1280 - Poly(hexamethylenebiguanide) hydrochloride (PHMB); exemption from the requirement of a tolerance.  

Code of Federal Regulations, 2010 CFR

...hexamethylenebiguanide) hydrochloride (PHMB); exemption from the requirement of a...hexamethylenebiguanide) hydrochloride (PHMB); exemption from the requirement of a...hexamethylenebiguanide) hydrochloride (PHMB)(CAS Reg. No....

2010-07-01

79

21 CFR 184.1875 - Thiamine hydrochloride.  

Code of Federal Regulations, 2010 CFR

...C1N4 OS·HCl, CAS Reg. No. 67-03-8) is the chloride-hydrochloride salt of thiamine. It occurs as hygroscopic white crystals or a white crystalline powder. The usual method of preparing this substance is by linking the preformed thiazole and...

2010-04-01

80

21 CFR 184.1875 - Thiamine hydrochloride.  

...C1N4 OS·HCl, CAS Reg. No. 67-03-8) is the chloride-hydrochloride salt of thiamine. It occurs as hygroscopic white crystals or a white crystalline powder. The usual method of preparing this substance is by linking the preformed thiazole and...

2014-04-01

81

21 CFR 184.1875 - Thiamine hydrochloride.  

Code of Federal Regulations, 2011 CFR

...C1N4 OS·HCl, CAS Reg. No. 67-03-8) is the chloride-hydrochloride salt of thiamine. It occurs as hygroscopic white crystals or a white crystalline powder. The usual method of preparing this substance is by linking the preformed thiazole and...

2011-04-01

82

Quality assessment of morphine hydrochloride solutions.  

PubMed

The therapeutic substances in solution prepared in pharmaceutical laboratories (prescribed drugs) must preserve their activity. Therefore, they must be stable throughout the period of storage in home conditions. The maintenance of stability is particularly difficult for morphine hydrochloride solutions administered orally to cancer patients at the last stage of the disease being at home. This study, aiming at the assessment of stability of morphine hydrochloride solutions, was performed on samples of 0.5% water solutions of the drug alone, 0.25% and 0.5% solutions of the drug in water with chloroform as well as injection solutions (Morphinum hydrochloricum, 20 mg, Polfa Warsaw). All the samples were kept at 20 degrees C for six months. Throughout this time observations were made to detect changes in their appearence and pH values. Their qualitative composition was determined by TLC and the content of morphine was checked by UV spectrophotometry in an environment of 0.1 mol/l of hydrochloric acid at 285 nm. Results of the kinetic study permitted drawing conclusions as to the mechanism of the decomposition of morphine hydrochloride in the solutions studied - according to a simple first order reaction and determination of the rate constants (k, s(-1)) of the process. Results of the chromatographic and spectrophotometric study did not show differences in the stability of water and chloroform/water solutions of morphine hydrochloride studied after 4 weeks and 6 months. After that time the decrease of morphine content was 10 and 25%, respectively. PMID:15493291

P?otkowiak, Zyta; Popielarz-Brzezi?ska, Maria; Luczak, Jacek; Kluziak, Maciej

2004-01-01

83

SOLID-STATE SYNTHESIS OF HETEROCYCLIC HYDRAZONES USING MICROWAVES UNDER CATALYST-FREE CONDITIONS: JOURNAL ARTICLE (1437A)  

EPA Science Inventory

NRMRL-CIN-1437A Jeselnik, M., Varma*, R.S., Polanc, S., and Kocevar, M. "Solid-State Synthesis of Heterocyclic Hydrazones using Microwaves under Catalyst-free Conditions http:///www.mdpi.net/ecsoc-5/." Fifth International Electronic Conference on Synthetic Organic Chemistry, h...

84

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

PubMed

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 ?-aminobutyric acid transporter 1 (GAT1), the most abundant ?-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). PMID:23336362

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

2013-02-14

85

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

PubMed Central

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

Pot??ková, Eliška; Hrušková, Kate?ina; Bureš, Jan; Kova?íková, Petra; Špirková, Iva A.; Pravdíková, Kate?ina; Kolbabová, Lucie; Hergeselová, Tereza; Hašková, Pavlína; Jansová, Hana; Machá?ek, Miloslav; Jirkovská, Anna; Richardson, Vera; Lane, Darius J. R.; Kalinowski, Danuta S.; Richardson, Des R.; Vávrová, Kate?ina; Šim?nek, Tomáš

2014-01-01

86

Treatment of allergic conjunctivitis with olopatadine hydrochloride eye drops  

PubMed Central

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

Uchio, Eiichi

2008-01-01

87

Variation in supramolecular arrangements of hydrazones, o-H2NC6H4CMedbnd NNHC6H4X (Xdbnd H, o-, m- and p-NO2), derived from o-aminoacetophenone and phenylhydrazines  

NASA Astrophysics Data System (ADS)

The crystal structures of four hydrazones, 1, derived from phenylhydrazines, XC6H4NHNH2 (Xdbnd H, o-NO2, m-NO2 or p-NO2) with 2-aminoacetophenone are reported, as is the mono hydrochloride, (2: Xdbnd m-NO2), of (1: Xdbnd m-NO2). Consistent strong intramolecular hydrogen bonds in 1 are of the type, Nsbnd H(amino)⋯N(hydrazono), while (1: Xdbnd m-NO2) portrays an additional Nsbnd H(hydrazono)⋯O(nitro), intramolecular hydrogen bond. Of interest, different sets of strong intermolecular interactions are found even among the nitro derivatives, 1. In (1: Xdbnd o-NO2), the strongest intermolecular interactions are Nsbnd H(amino)⋯O(nitro) hydrogen bonds, while in (1: Xdbnd m-NO2 and p-NO2), both Nsbnd H(hydrazono)⋯O(nitro) and Nsbnd H(amino)⋯N(amino) are present. These strong intermolecular hydrogen bonds coupled with different combinations of some of Csbnd H⋯O, ?sbnd ? stacking interactions and Nsbnd O⋯? generate different supramolecular arrays for (1: X = nitro): 2-D, 2-D and 3-D, respectively for (1: Xdbnd o-NO2), for (1: Xdbnd m-NO2) and (1: Xdbnd p-NO2). In (1: Xdbnd H), the major intermolecular interactions are Nsbnd H(hydrazono)⋯N(amino hydrogen bonds: these, supplemented by weaker Nsbnd H⋯? and Csbnd H⋯? interactions, generate a two-dimensional array. While significant changes in the intermolecular interactions result on formation of the salt, (2: Xdbnd m-NO2) from (1: Xdbnd m-NO2), the strong Nsbnd H(amino)⋯N(hydrazono) intramolecular hydrogen bonds persist. Strong intermolecular hydrogen bonds found in (2: Xdbnd m-NO2) are of the types Nsbnd H⋯Cl (both hydrazone and amine), Nsbnd H(amino)⋯O(nitro): these coupled with weaker Csbnd H⋯O, Nsbnd O⋯?, and ?sbnd ? generate a three dimensional array.

Alan Howie, R.; Baddeley, Thomas C.; Wardell, James L.; Wardell, Solange M. S. V.

2012-08-01

88

Potassium N-Iodo p-Toluenesulfonamide (TsNIK, Iodamine-T): A New Reagent for the Oxidation of Hydrazones to Diazo Compounds  

PubMed Central

A new reagent for the oxidation of hydrazones to diazo compounds is described. N-Iodo p-toluenesulfonamide (TsNIK, iodamine-T) allows the preparation of ?-diazoesters, ?-diazoamides, ?-diazoketones and ?-diazophosphonates in good yield and in high purity after a simple extractive work-up. ?-Diazoesters were also obtained in high yield from the corresponding ketones through a one-pot process of hydrazone formation/oxidation. PMID:24615944

Nicolle, Simon M; Moody, Christopher J

2014-01-01

89

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

Code of Federal Regulations, 2011 CFR

...2011-07-01 false Hydrochloride salt of a fatty polyalkkylene polyamine...721.6196 Hydrochloride salt of a fatty polyalkkylene polyamine...generically as Hydrochloride salt of a fatty polyalkkylene...uses are: (i) Release to water. Requirements as...

2011-07-01

90

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

Code of Federal Regulations, 2012 CFR

...2012-07-01 false Hydrochloride salt of a fatty polyalkkylene polyamine...721.6196 Hydrochloride salt of a fatty polyalkkylene polyamine...generically as Hydrochloride salt of a fatty polyalkkylene...uses are: (i) Release to water. Requirements as...

2012-07-01

91

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

Code of Federal Regulations, 2010 CFR

... 2010-07-01 false Hydrochloride salt of a fatty polyalkkylene polyamine...Substances § 721.6196 Hydrochloride salt of a fatty polyalkkylene polyamine...substance identified generically as Hydrochloride salt of a fatty...

2010-07-01

92

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

PubMed

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. PMID:24986657

Evranos-Aksöz, Begüm; Yabano?lu-Çiftçi, Samiye; Uçar, Gülberk; Yelekçi, Kemal; Ertan, Rahmiye

2014-08-01

93

Effect of fexofenadine hydrochloride on cedar pollinosis  

Microsoft Academic Search

Objective: To investigate the therapeutic efficacy of fexofenadine hydrochloride (Allegra® tablets), an antihistaminic launched in 2001, in patients with cedar pollinosis by dividing them into two groups for comparison, i.e. the early-treatment group in which treatment was started before the initial day of the pollen scattering, and the therapeutic-treatment group in which treatment was started after the initial day of

Satoshi Miyabe; Izumi Koizuka; Kentaro Ochi; Kenjiro Tanaka; Hisashi Kuroda; Mitsuharu Takatsu; Hirotsugu Kinoshita; Yutaka Sugiyama

2003-01-01

94

Norbornene derived doxorubicin copolymers as drug carriers with pH responsive hydrazone linker.  

PubMed

The synthesis and complete characterization of both norbornene-derived doxorubicin (mono 1) and polyethylene glycol (mono 2) monomers are clearly described, and their copolymerization by ring-opening metathesis polymerization (ROMP) to get the block copolymer (COPY-DOX) is vividly elaborated. The careful design of these conjugates exhibits properties like well-shielded drug moieties and well-defined nanostructures; additionally, they show solubility in both water and biological medium and also have the important tendency of rendering acid-triggered drug release. The drug release profile suggests the importance of having the hydrazone linker that helps to release the drug exactly at the mild acidic conditions resembling the pH of the cancerous cells. It is also observed that the drug release from micelles of COPY-DOX is significantly accelerated at a mildly acidic pH of 5.5-6, compared to the physiological pH of 7.4, suggesting the pH-responsive feature of the drug delivery system with hydrazone linkages. Confocal laser scanning microscopy (CLSM) measurements indicate that these COPY-DOX micelles are easily internalized by living cells. MTT assays against HeLa and 4T cancer cells showing COPY-DOX micelles have a high anticancer efficacy. All of these results demonstrate that these polymeric micelles that self-assembled from COPY-DOX block copolymers have great scope in the world of medicine, and they also symbolize promising carriers for the pH-triggered intracellular delivery of hydrophobic anticancer drugs. PMID:22107051

Rao N, Vijayakameswara; Mane, Shivshankar R; Kishore, Abhinoy; Das Sarma, Jayasri; Shunmugam, Raja

2012-01-01

95

Particle size distribution of cocaine hydrochloride  

NASA Astrophysics Data System (ADS)

A principal method for the detection of concealed shipments of cocaine hydrochloride relies upon the intake of an air sample taken near a surface onto an analytical instrument, and the detection of the narcotic present in the air or surface materials collected. The low vapor pressure of cocaine at normal temperatures indicates that particulate material present on the surfaces of target packages affords a higher probability of collection of detectable mass than does a vapor sample. An accurate representation of the particles in question is required, both for theoretical sampler design and for the performance of meaningful tests of instrument capabilities. Existing test methods for target particle preparation call for use of sand particles ranging in size from 20 to 100 micrometers in diameter, coated with a solution of cocaine hydrochloride. In this study, three seized samples and pharmaceutical cocaine hydrochloride were analyzed using an Aerosizer to measure the size distribution of the air-dispersed particles. The results obtained during these tests indicate that the actual size range of the particles is significantly smaller than the test particles cited. Results obtained in instrument evaluations using the larger target particles may therefore be misleading.

Kuhlman, Michael R.; Gooding, Rachel E.; Kogan, Vladimir G.; Bridges, Curtis

1997-02-01

96

A spectrophotometric method for the quantification of an enzyme activity producing 4-substituted phenols: determination of toluene-4-monooxygenase activity.  

PubMed

A spectrophotometric method for the quantitative determination of an enzyme activity resulting in the accumulation of 4-substituted phenols is described in this article. Toluene-4-monooxygenase (T4MO) activity in whole cells of Pseudomonas mendocina KR1 is used to demonstrate this method. This spectrophotometric assay is based on the coupling of T4MO activity with tyrosinase activity. The 4-substituted phenol, produced by the action of T4MO on the aromatic ring of a substituted arene, is a substrate for tyrosinase, which converts phenols to o-quinones. The latter react with the nucleophile 3-methyl-2-benzothiazolinone hydrazone (MBTH) to produce intensely colored products that absorb light maximally at different wavelengths, depending on the phenolic substrate used. The incubation of whole cells of P. mendocina KRI with fluorobenzene resulted in the accumulation of 4-fluorophenol. The coupling of T4MO activity with tyrosinase activity in the presence of fluorobenzene resulted in the formation of a colored product absorbing maximally at 480 nm. The molar absorptivity (epsilon) value for the o-quinone-MBTH adduct formed from 4-fluorophenol was determined experimentally to be 12,827 M(-1) cm(-1) with a linear range of quantification between 2.5 and 75 microM. The whole cell assay was run as a continuous indirect assay. The initial rates of T4MO activity toward fluorobenzene, as determined spectrophotometrically, were 61.8+/-4.4 nmol/min/mg P. mendocina KR1 protein (using mushroom tyrosinase), 64.9+/-4.6 nmol/min/mg P. mendocina KR1 protein (using cell extracts Pseudomonas putida F6), and, as determined by HPLC analysis, 62.6+/-1.4 nmol/min/mg P. mendocina KR1 protein. PMID:16061193

Nolan, Louise C; O'Connor, Kevin E

2005-09-15

97

21 CFR 524.1662 - Oxytetracycline hydrochloride ophthalmic and topical dosage forms.  

Code of Federal Regulations, 2010 CFR

...Oxytetracycline hydrochloride ophthalmic and topical dosage forms. 524.1662 Section...RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS ...Oxytetracycline hydrochloride ophthalmic and topical dosage...

2010-04-01

98

Synthesis, characterization, DNA binding properties and antioxidant activity of Ln(III) complexes with hesperetin-4-one-(benzoyl) hydrazone  

Microsoft Academic Search

Novel Ln(III) complexes with hesperetin-4-one-(benzoyl) hydrazone (H4L) have been synthesized and characterized. Electronic absorption spectroscopy, fluorescence spectra, ethidium bromide displacement experiments, iodide quenching experiments, salt effect and viscosity measurements indicate that the ligand and Ln(III) complexes, especially the Nd(III) complex, strongly bind to calf thymus DNA, presumably via an intercalation mechanism. The intrinsic binding constants of the Nd(III) complex and

Yong Li; Zheng-Yin Yang; Ming-Fang Wang

2009-01-01

99

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

NASA Astrophysics Data System (ADS)

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.

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

2014-11-01

100

Application of polyacrolein–isonicotinic acid hydrazone resin for the separation and concentration of Pd and Pt in road dust  

Microsoft Academic Search

A chelating resin containing isonicotinic acid hydrazone as functional group (P-NHZ) was synthesized and characterized through IR spectra and elemental analysis. The potential of this resin for the separation and preconcentration of Pd and Pt was extensively investigated. Efforts were also made for its use in the determination of Pd and Pt by Q-ICP-MS. The interferences from YO+ during Pd

Xiaopeng Ge; Iris Wendler; Peter Schramel; Antonius Kettrup

2004-01-01

101

An investigation on new ruthenium(II) hydrazone complexes as anticancer agents and their interaction with biomolecules.  

PubMed

A new set of ruthenium(II) hydrazone complexes [Ru(H)(CO)(PPh3)2(L)] (1) and [RuCl2(DMSO)2(HL)] (2), with triphenyl phosphine or DMSO as co-ligands was synthesized by reacting benzoyl pyridine furoic acid hydrazone (HL) with [Ru(H)(Cl)(CO)(PPh3)3] and [RuCl2(DMSO)4]. The single crystal X-ray data of complexes 1 and 2 revealed an octahedral geometry around the ruthenium ion in which the hydrazone is coordinated through ON and NN atoms in complexes 1 and 2 respectively. The interaction of the compounds with calf thymus DNA (CT-DNA) has been estimated by absorption and emission titration methods which indicated that the ligand and the complexes interacted with CT-DNA through intercalation. In addition, the DNA cleavage ability of these newly synthesized ruthenium complexes assessed by an agarose gel electrophoresis method demonstrated that complex 2 has a higher DNA cleavage activity than that of complex 1. The binding properties of the free ligand and its complexes with bovine serum albumin (BSA) protein have been investigated using UV-visible, fluorescence and synchronous fluorescence spectroscopic methods which indicated the stronger binding nature of the ruthenium complexes to BSA than the free hydrazone ligand. Furthermore, the cytotoxicity of the compounds examined in vitro on a human cervical cancer cell line (HeLa) and a normal mouse embryonic fibroblasts cell line (NIH 3T3) revealed that complex 2 exhibited a superior cytotoxicity than complex 1 to the cancer cells but was less toxic to the normal mouse embryonic fibroblasts under identical conditions. PMID:24519473

Alagesan, Mani; Bhuvanesh, Nattamai S P; Dharmaraj, Nallasamy

2014-04-28

102

Preparation of catalytically active, covalent ?-polylysine-enzyme conjugates via UV/vis-quantifiable bis-aryl hydrazone bond formation.  

PubMed

Covalent UV/vis-quantifiable bis-aryl hydrazone bond formation was investigated for the preparation of conjugates between ?-poly-d-lysine (PDL) and either ?-chymotrypsin (?-CT) or horseradish peroxidase (HRP). PDL and the enzymes were first modified via free amino groups with the linking reagents succinimidyl 6-hydrazinonicotinate acetone hydrazone (S-HyNic, at pH 7.6) and succinimidyl 4-formylbenzoate (S-4FB, at pH 7.2), respectively. The modified PDL and enzymes were then conjugated at pH 4.7, whereby polymer chains carrying several enzymes were obtained. Kinetics of the bis-aryl hydrazone bond formation was investigated spectrophotometrically at 354 nm. Retention of the enzymatic activity after conjugate formation was confirmed by using the substrates N-succinimidyl-l-Ala-l-Ala-l-Pro-l-Phe-p-nitroanilide (for ?-CT) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS, for HRP). Thus, not only a mild and efficient preparation and convenient quantification of a conjugate between the polycationic ?-polylysine and enzymes could be shown, but also the complete preservation of the enzymatic activity. PMID:21171644

Grotzky, Andrea; Manaka, Yuichi; Kojima, Taisuke; Walde, Peter

2011-01-10

103

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

PubMed

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 -?G° and -?H° were found to obey Mn(2+)

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

2012-12-01

104

The immobilization of wapiti with etorphine hydrochloride.  

PubMed

Data and observations on the use of Etorphine hydrochloride (M99) (in combination with Acepromazine) and its antagonist M50-50 for immobilization of captive elk (Cervus elaphus canadensis) are presented. The study period covers 3 years during which 8 adult elk were immobilized 52 times with M99. The average dose of M99 administered for each immobilization was 2.2 mg per 100 kg body weight. Reversal with M50-50 was effected by an average dose of 4.4 mg per 100 body weight. Induction averaged 5.9 minutes while reversal took an average of 4.6 minutes. PMID:916137

Magonigle, R A; Stauber, E H; Vaughn, H W

1977-07-01

105

Stability of [(N-piperidine)methylene]daunorubicin hydrochloride and [(N-pyrrolidine)methylene]daunorubicin hydrochloride in solid state.  

PubMed

The influence of temperature and relative air humidity on the stability of two novel derivatives of daunorubicin: [(N-piperidine)methylene]daunorubicin hydrochloride and [(N-pyrrolidine)methylene]daunorubicin hydrochloride was investigated. The process of degradation was studied by using high-performance liquid chromatography with ultraviolet (UV) detection. The kinetic and thermodynamic parameters of degradation were calculated. PMID:25265823

Medenecka, Beata; Zalewski, Przemys?aw; Kycler, Witold; Piekarski, Miko?aj; Lemiech, Weronika; Oszczapowicz, Irena; Jeli?ska, Anna

2014-01-01

106

A new mechanism-based inhibitor of photosynthetic water oxidation: Acetone hydrazone. I. Equilibrium reactions  

SciTech Connect

The process of photosynthetic water oxidation has been investigated by using a new type of water oxidation inhibitor, the alkyl hydrazones. Acetone hydrazone (AceH), (CH{sub 3}){sub 2}CNNH{sub 2}, inhibits water oxidation by a mechanism that is analogous to that of NH{sub 2}OH. This involves binding to the water-oxidizing complex (WOC), followed by photoreversible reduction of manganese (loss of the S{sub 1} {yields} S{sub 2} reaction). At higher AceH concentrations the S{sub 1} state is reduced in the dark and Mn is released, albeit to a lesser extent than with NH{sup 2}OH. Following extraction of Mn, AceH is able to donate electrons rapidly to the reaction center tyrosine radical Z{sup +} ({sup 161}Tyr-D{sub 1} protein), more slowly to a reaction center radical C{sup +}, and not at all to the dark-stable tyrosine radical D{sup +} ({sup 160}Tyr-D{sub 2} protein) which must be sequestered in an inaccessible site. Unexpectedly, Cl{sup {minus}} was found not to interfere or compete with AceH for binding to the WOC in the S{sub 1} state, in contrast to the reported rate of binding of N,N-dimethylhydroxylamine (CH{sub 3}){sub 2}NOH. The authors interpret the latter behavior as due to ionic screening of the thylakoid membrane, rather than a specific Cl site involved in water oxidation. AceH appears not to bind to the acceptor side of PSII as evidenced by normal EPR signals both for Q{sub A}{sup {minus}}Fe(II), the primary electron acceptor, and for the oxidized Fe(III) acceptor (Q{sub 400} species), in contrast to that observed with NH{sub 2}OH. AceH can be oxidized in solution by a variety of oxidants including Mn(III) to form a reactive diazo intermediate, (CH{sub 3}){sub 2}CNN, which reacts with carbonyl compounds. Oxidation to this diazo intermediate is postulated to be responsible for inhibition of the WOC.

Tso, J.; Dismukes, G.C. (Princeton Univ., NJ (USA)); Petrouleas, V. (Nuclear Research Center, Athens (Greece))

1990-08-21

107

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

PubMed Central

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

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

2012-01-01

108

Efficient Bioconjugation of Protein Capture Agents to Biosensor Surfaces Using Aniline-Catalyzed Hydrazone Ligation  

PubMed Central

Aniline-catalyzed hydrazone ligation between surface immobilized hydrazines and aldehyde-modified antibodies is shown to be an efficient method for attaching protein capture agents to model oxide-coated biosensor substrates. Silicon photonic microring resonators are used to directly evaluate the efficiency of this surface bioconjugate reaction at various pHs and in the presence or absence of aniline as a nucleophilic catalyst. It is found that aniline significantly increases the net antibody loading for surfaces functionalized over a pH range from 4.5 to 7.4, allowing derivatization of substrates with reduced incubation time and sample consumption. This increase in antibody loading directly results in more sensitive antigen detection when functionalized microrings are employed in a label-free immunoassay. Furthermore, these experiments also reveal an interesting pH dependent non-covalent binding trend that plays an important role in dictating the amount of antibody attached onto the substrate, highlighting the competing contributions of the bioconjugate reaction rate and the dynamic interactions that control opportunities for a solution-phase biomolecule to react with a substrate-bound reagent. PMID:20809595

Byeon, Ji-Yeon; Limpoco, F. T.; Bailey, Ryan C.

2010-01-01

109

Experimental and theoretical studies on methanesulfonic acid 1-methylhydrazide: Antimicrobial activities of its sulfonyl hydrazone derivatives  

NASA Astrophysics Data System (ADS)

Methanesulfonic acid 1-methylhydrazide ( msmh) and its sulfonyl hydrazone derivatives, salicylaldehyde- N-methylmethanesulfonylhydrazone ( salmsmh) and 2-hydroxy-1-naphthaldehyde- N-methylmethanesulfonylhydrazone ( nafmsmh) were synthesized and characterized by using FT-IR, 1H NMR, 13C NMR, LC-MS and elemental analysis. Conformation analysis of msmh based on DFT/B3LYP/6-311G(d) method was performed. 1H and 13C shielding tensors of msmh for the most stable conformer were calculated with GIAO/DFT/B3LYP/6-311++G(2d, 2p) methods in vacuo and various solvents such as DMSO, THF, acetonitrile, methanol and aqueous solution. The harmonic vibrational wavenumbers for the most stable conformer were calculated using at B3LYP/6-311G(d) level. Antimicrobial activity of the compounds was also screened against Gram-positive bacteria ( Staphylococcus aureus ATCC 25923, Bacillus cereus RSKK 863) and Gram-negative bacteria ( Escherichia coli ATCC 11230, Salmonella enterititis ATCC 40376, Pseudomonos aeruginosa ATCC 28753) by both disc diffusion and micro dilution methods.

Özbek, Neslihan; Alyar, Saliha; Karacan, Nurcan

2009-12-01

110

Design, synthesis, and insecticidal activities of phthalamides containing a hydrazone substructure.  

PubMed

Fluobendiamide is the first commercialized artificial synthetic insecticide acting on the ryanodine receptor. This new molecule possesses a combination of excellent insecticidal activity and eco-friendly characteristics with a skeleton structure of phthalamide. In this study, we incorporated hydrazone, present in many pesticidal compounds reported during the last two decades, into phthalamide derivatives via Schiff-base condensation and aminolysis to obtain 21 new compounds; these compounds were characterized by proton nuclear magnetic resonance ((1)H NMR), infrared spectroscopy (IR), and high-resolution mass spectrometry (HRMS) or elemental analysis. A preliminary bioassay against peach aphids ( Myzus persicae ) revealed that the title compounds exhibited good stomach toxicity at 600 mg/L. Twelve new compounds were found to display higher activity than postive control flubendiamide (LC(50) = 184.099 mg/L), however, LC(50) was less than 100 mg/L only for compounds 4e, 4o, 4s, 4t (59-77 mg/L). That is, combinations of a p-fluorophenyl or (methyl)thienyl group at the Ar position with an isopropyl or cyclohexyl group at the R position might improve the lethality of the designed phthalamide derivative. Preliminary results of a bioassay at 600 mg/L against diamondback moth ( Plutella xylostella , Linnaeus) showed that only the title compound 4e possessed good larvicidal activity. On comparison of the bioassay results of stomach toxicity and larvicidal activity, it is noteworthy that the compound incorporating phenylpyrazolyl exhibited good larvicidal activity and poor stomach activity. PMID:20450195

Liu, Ming; Wang, Yi; Wangyang, Wei-zi; Liu, Feng; Cui, Yong-liang; Duan, You-sheng; Wang, Min; Liu, Shang-zhong; Rui, Chang-hui

2010-06-01

111

Fluorescein hydrazones as novel nonintercalative topoisomerase catalytic inhibitors with low DNA toxicity.  

PubMed

Fluorescein hydrazones (3a-3l) were synthesized in three steps with 86-91% overall yields. Topo I- and II?-mediated relaxation and cell viability assay were evaluated. 3d inhibited 47% Topo I (camptothecin, 34%) and 20% Topo II (etoposide 24%) at 20 ?M. 3l inhibited 61% Topo II (etoposide 24%) at 20 ?M. 3d and 3l were further evaluated to determine their mode of action with diverse methods of kDNA decatenation, DNA-Topo cleavage complex, comet, DNA intercalating/unwinding, and Topo II?-mediated ATP hydrolysis assays. 3d functioned as a nonintercalative dual inhibitor against the catalytic activities of Topo I and Topo II?. 3l acted as a Topo II? specific nonintercalative catalytic inhibitor. 3d activated apoptotic proteins as it increased the level of cleaved capase-3 and cleaved PARP in a dose- and time-dependent manner. The dose- and time-dependent increase of G1 phase population was observed by treatment of 3d along with the increase of p27(kip1) and the decrease of cyclin D1 expression. PMID:25333701

Rahman, A F M Motiur; Park, So-Eun; Kadi, Adnan A; Kwon, Youngjoo

2014-11-13

112

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

NASA Astrophysics Data System (ADS)

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.

Cukurovali, Alaaddin; Yilmaz, Engin

2014-10-01

113

Berberine hydrochloride: anticancer activity and nanoparticulate delivery system  

PubMed Central

Background Berberine hydrochloride is a conventional component in Chinese medicine, and is characterized by a diversity of pharmacological effects. However, due to its hydrophobic properties, along with poor stability and bioavailability, the application of berberine hydrochloride was hampered for a long time. In recent years, the pharmaceutical preparation of berberine hydrochloride has improved to achieve good prospects for clinical application, especially for novel nanoparticulate delivery systems. Moreover, anticancer activity and novel mechanisms have been explored, the chance of regulating glucose and lipid metabolism in cancer cells showing more potential than ever. Therefore, it is expected that appropriate pharmaceutical procedures could be applied to the enormous potential for anticancer efficacy, to give some new insights into anticancer drug preparation in Chinese medicine. Methods and results We accessed conventional databases, such as PubMed, Scope, and Web of Science, using “berberine hydrochloride”, “anti-cancer mechanism”, and “nanoparticulate delivery system” as search words, then summarized the progress in research, illustrating the need to explore reprogramming of cancer cell metabolism using nanoparticulate drug delivery systems. Conclusion With increasing research on regulation of cancer cell metabolism by berberine hydrochloride and troubleshooting of issues concerning nanoparticulate delivery preparation, berberine hydrochloride is likely to become a natural component of the nanoparticulate delivery systems used for cancer therapy. Meanwhile, the known mechanisms of berberine hydrochloride, such as decreased multidrug resistance and enhanced sensitivity of chemotherapeutic drugs, along with improvement in patient quality of life, could also provide new insights into cancer cell metabolism and nanoparticulate delivery preparation. PMID:21931477

Tan, Wen; Li, Yingbo; Chen, Meiwan; Wang, Yitao

2011-01-01

114

Immobilization of coypus (Myocastor coypus) with ketamine hydrochloride and xylazine hydrochloride.  

PubMed

A combination of 100 mg/ml of ketamine hydrochloride (Ket) and 20 mg/ml of xylazine hydrochloride (Xyl) was used to immobilize coypus (Myocastor coypus). Eight mature coypus (four males and four females) were injected intramuscularly with doses ranging from 2.33 to 6.25 mg/kg of KET and 0.25 to 0.86 mg/kg of Xyl. The mean (+/- SE) time for induction, arousal, and recovery were 7.3 +/- 2 min, 23.5 +/- 0.3 min and 46 +/- 2.5 min, respectively. The mean +/- SE doses injected were 4.07 +/- 0.52 mg/kg Ket (range, 2.33 to 6.25 mg/kg) and 0.5 +/- 0.08 mg/kg Xyl (range, 0.25 to 0.86 mg/kg). No adverse responses were observed in any of the animals treated. PMID:7760499

Bo, R F; Palomares, F; Beltrán, J F; de Villafañe, G; Moreno, S

1994-10-01

115

Immobilization of fishers (Martes pennanti) with ketamine hydrochloride and xylazine hydrochloride.  

PubMed

A combination of 100 mg ketamine hydrochloride (KH) and 20 mg xylazine hydrochloride (XH) was used to immobilize fishers (Martes pennanti). Four adult males were intramuscularly injected a total of five times at dosages between 22.4 to 29.0 mg/kg KH and 4.1 to 6.6 mg/kg XH. Mean (+/- SE) induction time and arousal time were 3.3 +/- 0.5 min and 76.8 +/- 12.1 min, respectively. Respiration, heart rate, and body temperature in response to sedation appeared normal. A 5:1 mixture of KH-XH appears to be a safe immobilizing agent for fishers. PMID:2067055

Belant, J L

1991-04-01

116

Cocrystals of bis(4-hydroxy-1-methylpiperidine betaine) hydrochloride  

Microsoft Academic Search

Bis(4-hydroxy-1-methylpiperidine betaine) hydrochloride, [bis(1-carboxymethyl-4-hydroxy-1-methylpiperidinium) hydrochloride, (HO–MPB)2HCl], has been prepared from stoichiometric amounts of ?-4-hydroxy-1-methylpiperidine betaine hydrochloride with the OH group in an equatorial position and ?-4-hydroxy-1-methylpiperidine betaine inner salt with the OH group in an axial one. Cocrystals of (HO–MPB)2HCl belong to monoclinic system with C2\\/c space group. Piperidinium ring has a chair conformation with the CH2COO group in the

Z. Dega-Szafran; E. Dulewicz; G. Dutkiewicz; Z. Kosturkiewicz

2006-01-01

117

Spectroscopy study of ephedrine hydrochloride and papaverine hydrochloride in terahertz range  

NASA Astrophysics Data System (ADS)

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.

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

2008-12-01

118

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

PubMed

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

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

2007-04-01

119

Preparation of floating pellets with verapamil hydrochloride.  

PubMed

The aim of this paper is to prepare a floating drug formulation in a gelatin capsule filled with tens of pellets with verapamil hydrochloride (VH) in a dose of 40 mg. The better solubility of VH in an acidic environment of the stomach may result in a greater amount of the drug absorbed. Pellets were prepared by wet granulation of a powder mixture, spheronization of the granulated mass and coating of the cores with aqueous dispersions of polymethylmethacrylate. Sodium hydrocarbonate contained in pellet cores ensures the flotation effect. Proper rate of VH release from pellets was obtained by a coating film of 25-105 microm thickness. Pellets of 1.25-1.6 mm size with a film of 75-85 microm thickness of considerably constant rate released the whole dose of VH in 6 h. During that time the pellets floated on the surface of the receptor solution. PMID:15481243

Sawicki, Wies?aw; G?ód, Joanna

2004-01-01

120

Stability of Revex, nalmefene hydrochloride injection.  

PubMed

The stability of Revex, nalmefene hydrochloride injection, has been studied at several temperatures for periods up to 36 months. The data were obtained using a HPLC method for the potency determination, and for the level of the sole degradation product (2,2'-bisnalmefene). These methods were found to be characterized by excellent precision, linearity, and accuracy over the analyte concentration ranges established. The stability data were found to be interpretable using first-order kinetics, and essentially comparable rate constants were calculated for both the potency loss and the formation of 2,2'-bisnalmefene. Applying the Arrhenius equation to these data, a rate constant of 0.00441 month-1 was deduced for the reactions taking place at 25 degrees C. This low value is consistent with the excellent stability exhibited by the product, and amply justifies its shelf life. PMID:8846056

Brittain, H G; Lafferty, L; Bousserski, P; Diegnan, G; Lessor, R; Small, C; Pejaver, S

1996-01-01

121

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

NASA Astrophysics Data System (ADS)

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.

Adegoke, Olajire A.

2011-12-01

122

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

SciTech Connect

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.

Chanudet,V.; Filella, M.

2007-01-01

123

21 CFR 520.2098 - Selegiline hydrochloride tablets.  

Code of Federal Regulations, 2013 CFR

...HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2098 Selegiline hydrochloride...examination findings after 2 months of therapy, increase dose to a maximum of 2...

2013-04-01

124

21 CFR 520.2098 - Selegiline hydrochloride tablets.  

Code of Federal Regulations, 2012 CFR

...HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2098 Selegiline hydrochloride...examination findings after 2 months of therapy, increase dose to a maximum of 2...

2012-04-01

125

21 CFR 520.2098 - Selegiline hydrochloride tablets.  

Code of Federal Regulations, 2011 CFR

...HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2098 Selegiline hydrochloride...examination findings after 2 months of therapy, increase dose to a maximum of 2...

2011-04-01

126

21 CFR 520.2098 - Selegiline hydrochloride tablets.  

Code of Federal Regulations, 2010 CFR

...HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2098 Selegiline hydrochloride...examination findings after 2 months of therapy, increase dose to a maximum of 2...

2010-04-01

127

21 CFR 520.1242f - Levamisole hydrochloride gel.  

Code of Federal Regulations, 2010 CFR

...milligrams of levamisole hydrochloride per kilogram of body weight, as a single oral dose. (ii) Indications for use. Anthelmintic effective against the following nematode infections: Stomach worms (Haemonchus, Trichostrongylus, Ostertagia...

2010-04-01

128

21 CFR 520.1242f - Levamisole hydrochloride gel.  

Code of Federal Regulations, 2012 CFR

...milligrams of levamisole hydrochloride per kilogram of body weight, as a single oral dose. (ii) Indications for use. Anthelmintic effective against the following nematode infections: Stomach worms (Haemonchus, Trichostrongylus, Ostertagia...

2012-04-01

129

21 CFR 520.1242f - Levamisole hydrochloride gel.  

Code of Federal Regulations, 2013 CFR

...milligrams of levamisole hydrochloride per kilogram of body weight, as a single oral dose. (ii) Indications for use. Anthelmintic effective against the following nematode infections: Stomach worms (Haemonchus, Trichostrongylus, Ostertagia...

2013-04-01

130

21 CFR 520.1242f - Levamisole hydrochloride gel.  

Code of Federal Regulations, 2011 CFR

...milligrams of levamisole hydrochloride per kilogram of body weight, as a single oral dose. (ii) Indications for use. Anthelmintic effective against the following nematode infections: Stomach worms (Haemonchus, Trichostrongylus, Ostertagia...

2011-04-01

131

(6-Maleimidocaproyl)hydrazone of doxorubicin--a new derivative for the preparation of immunoconjugates of doxorubicin.  

PubMed

The (6-maleimidocaproyl)hydrazone of doxorubicin was synthesized and conjugated to several mAbs, including chimeric BR96, via a Michael addition reaction to thiol-containing mAbs. DTT reduction of disulfides present in the mAb was a reliable and general method for generating a consistent number of reactive SH groups. The conjugates, after purification by Bio-Beads, were free of unreacted linker and/or doxorubicin. All conjugates released doxorubicin under acidic conditions that mimic the lysosomal environment, while they were relatively stable at neutral pH. BR96 conjugates showed antigen-specific cytotoxicity. PMID:7508268

Willner, D; Trail, P A; Hofstead, S J; King, H D; Lasch, S J; Braslawsky, G R; Greenfield, R S; Kaneko, T; Firestone, R A

1993-01-01

132

Synthesis, characterization and antiamoebic activity of some hydrazone and azole derivatives bearing pyridyl moiety as a promising heterocyclic scaffold.  

PubMed

In an effort to develop effective antiamoebic agents, some hydrazones and azoles containing pyridyl moiety were synthesized and screened for in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica. Among all the compounds, only five compounds (1, 3, 5, 9 and 11) were found to be better inhibitors of growth of E. histolytica than the reference drug metronidazole. The cytotoxic studies of these compounds on human breast cancer MCF-7 cell line revealed that all the compounds were low-cytotoxic in the concentration range of 2.5-250 ?M. PMID:22309914

Siddiqui, Shadab Miyan; Salahuddin, Attar; Azam, Amir

2012-03-01

133

Contact dermatoconjunctivitis secondary to phenylephrine hydrochloride ophthalmic solution  

Microsoft Academic Search

The patient is an 81 year-old male evaluated by ophthalmology for cataract surgery. The patient's eyes were dilated with one drop each of the anticholinergic agent tropicamide (Mydriacyl 0.5% ®), and the sympathomimetic agent, phenylephrine hydrochloride 2.5%. The combination solution, fluorescein sodium 0.25%\\/benoxinate hydrochloride 0.4% (FluorBenox ®), was also instilled in both eyes prior to tanometry. After several hours, the

M. A. Cavuoto; S. J. Weiss; I. J. Salzman

2004-01-01

134

Characterization of the Subcritical Water Extraction of Fluoxetine-Hydrochloride.  

PubMed

The characteristics of using Subcritical Water Extraction (SWE) to recover Fluoxetine-Hydrochloride from both standard solutions and the contents of commercial capsule formulations were investigated. Analysis of solutions and extracts was done by HPLC with UV detection at 254 nm. Standard solutions of Fluoxetine-Hydrochloride were exposed to a variety of SWE operating conditions, including temperatures from 125 to 275°C and periods ranging from 5 to 30 min. Fluoxetine-Hydrochloride could be quantitatively recovered from standard solutions (1.0mg/mL) that were heated up to 175°C for 30 min, up to 200°C for 15 min, or up to 225°C for 10 min. At higher temperatures and/or times, Fluoxetine-Hydrochloride recoveries were generally incomplete and often produced decomposition by-products during the process. By comparison, the concentration of Fluoxetine-Hydrochloride in the standard solution had relatively little effect on recovery. Considering these parameters, an SWE method was developed to extract Fluoxetine-Hydrochloride from the contents of Prozac(®) capsules. It was found that Fluoxetine-Hydrochloride could be quantitatively extracted from the capsule contents in 8 min at a temperature of 200°C using 3.5 mL of water as the extraction solvent. Gelatinization of the starch excipient in the capsule contents was also observed to occur temporarily during the capsule extractions, before ultimately disappearing again. The period of this phenomenon was dependent on both temperature and sample size. The results indicate that SWE can be a very useful method for Fluoxetine-Hydrochloride extraction and suggest that it may be interesting to explore other pharmaceuticals using this method as well. PMID:22552197

Murakami, Jillian N; Thurbide, Kevin B; Lambertus, Gordon; Jensen, Eric

2012-08-10

135

Effects of raloxifene hydrochloride on endometrial cancer cells in vitro  

Microsoft Academic Search

Objective. Determine effects of raloxifene hydrochloride, a selective estrogen receptor modulator (SERM), on growth and proliferation of an estrogen-responsive endometrial cancer cell line in vitro.Materials and methods. Studies were performed with Ishikawa endometrial adenocarcinoma cells, a well-differentiated cancer that expresses estrogen receptors and progesterone receptors. Raloxifene was purified as the hydrochloride salt. The four arms of the study were cells

Michael Hibner; Javier F Magrina; Scott R Lefler; Jeffrey L Cornella; Antonio R Pizarro; Joseph C Loftus

2004-01-01

136

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

PubMed

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

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

2014-01-29

137

Canine olfactory sensitivity to cocaine hydrochloride and methyl benzoate  

NASA Astrophysics Data System (ADS)

Methyl benzoate is a consistent product of cocaine hydrochloride exposed to humid air. The detection responses of dogs trained to detect illicit cocaine hydrochloride may be controlled by vapor from cocaine, methyl benzoate, or other constituents of illicit cocaine. The present study addressed the following questions: 1) How capable are dogs of detecting methyl benzoate compared to cocaine hydrochloride, 2) When dogs are trained to detect methyl benzoate, do they respond to cocaine hydrochloride as being the same or different from methyl benzoate. These questions were investigated using random source dogs trained and tested under laboratory conditions. Odor stimuli were generated and delivered by a vapor generation systems, the outputs from which were characterized by thermal desorption GC/MS. ONe group of dogs was trained to discriminate pharmaceutical grade and illicit cocaine hydrochloride from clean air and tested using a two lever procedure to determine their sensitivity to these substances. A second group of dogs was trained to discriminate between methyl benzoate and clean air and tested for their sensitivity to the substance. The dogs in this second group were then tested using a three lever procedure to determine their sensitivity to these substances. A second group of dogs was trained to discriminate between methyl benzoate and clean air and tested for their sensitivity to the substance. The dogs in this second group were then tested using a three lever procedure to determine whether they responded to cocaine hydrochloride as the same or different from methyl benzoate.

Waggoner, L. Paul; Johnston, James M.; Williams, Marc; Jackson, Jan; Jones, Meredith H.; Boussom, Teresa; Petrousky, James A.

1997-02-01

138

Stability of ondansetron hydrochloride in portable infusion-pump reservoirs.  

PubMed

The stability of ondansetron hydrochloride 0.24 and 2 mg/mL when delivered by portable infusion pump at near-body temperature over various time periods was investigated. Nine 100-mL drug reservoirs were prepared, three containing ondansetron hydrochloride 2 mg/mL and six containing ondansetron hydrochloride diluted with 0.9% sodium chloride injection to 0.24 mg/mL. Three of the reservoirs containing the diluted solution were refrigerated for up to 30 days at 3 degrees C before being attached to portable infusion pumps and pumped over 24 hours at 30 degrees C. The remaining six reservoirs were attached to pumps immediately after being filled, and the solutions were delivered for up to 24 hours (the diluted solution; three reservoirs) or up to seven days (the concentrated solution; three reservoirs) at 30 degrees C. Samples were taken initially and periodically and analyzed by high-performance liquid chromatography and with a pH meter. Both the diluted and the concentrated solutions of ondansetron hydrochloride retained at least 95% of the initial drug concentration under all the conditions studied. There was no appreciable change in pH. Ondansetron hydrochloride 0.24 mg/mL was stable when stored for up to 30 days at 3 degrees C and infused over 24 hours at 30 degrees C. Ondansetron hydrochloride 2 mg/mL was stable when infused for up to one week at 30 degrees C. PMID:1388331

Stiles, M L; Allen, L V; Fox, J L

1992-06-01

139

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

Federal Register 2010, 2011, 2012, 2013

...FDA-2012-P-1000] Determination That REV-EYES (Dapiprazole Hydrochloride Ophthalmic...Administration (FDA) has determined that REV-EYES (dapiprazole hydrochloride ophthalmic...does not refer to a listed drug. REV-EYES (dapiprazole hydrochloride...

2013-05-13

140

The stability of mixtures of morphine hydrochloride, bupivacaine hydrochloride, and clonidine hydrochloride in portable pump reservoirs for the management of chronic pain syndromes.  

PubMed

The physical and chemical stability of a combination of drugs commonly administered into the epidural or intrathecal space for the treatment of chronic pain was investigated. The concentrations of bupivacaine hydrochloride, morphine hydrochloride, and clonidine hydrochloride were measured using high performance liquid chromatography. The solutions were stored in reservoir bags for up to 90 days. No macroscopic or microbiological signs of precipitation, change in color, or contamination were observed, and pH remained stable. None of the three drugs declined in concentration during the observation period. A small increase in concentration of all three drugs did occur over time, most probably due to evaporation processes. In conclusion, no problems in physical or chemical stability are to be expected when combining morphine, bupivacaine, and/or clonidine for long-term epidural or intrathecal administration. In the case of clinically apparent loss of analgesic efficacy, other mechanisms should be considered. PMID:7963782

Wulf, H; Gleim, M; Mignat, C

1994-07-01

141

Pharmacological Evaluation and Preparation of Nonsteroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit  

PubMed Central

A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a–e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a–e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a–e are less gastrotoxic than the respective parent drug. Compounds 4b–e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a–b and 4d–e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a–e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non-steroidal anti-inflammatory drugs. PMID:24714090

de Melo, Thais Regina Ferreira; Chelucci, Rafael Consolin; Pires, Maria Elisa Lopes; Dutra, Luiz Antonio; Barbieri, Karina Pereira; Bosquesi, Priscila Longhin; Trossini, Gustavo Henrique Goulart; Chung, Man Chin; dos Santos, Jean Leandro

2014-01-01

142

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...

143

76 FR 32366 - Determination That ORLAAM (Levomethadyl Acetate Hydrochloride) Oral Solution, 10 Milligrams...  

Federal Register 2010, 2011, 2012, 2013

...Levomethadyl Acetate Hydrochloride) Oral Solution, 10 Milligrams/Milliliter, Was Not...acetate hydrochloride (HCl)) oral solution, 10 milligrams (mg)/milliliter...ANDAs) for levomethadyl acetate HCl oral solution, 10 mg/mL, if all other legal...

2011-06-06

144

21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.  

Code of Federal Regulations, 2010 CFR

...Lincomycin hydrochloride monohydrate oral dosage forms. 520.1263...ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED...FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS...Lincomycin hydrochloride monohydrate oral dosage...

2010-04-01

145

21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.  

Code of Federal Regulations, 2011 CFR

...Lincomycin hydrochloride monohydrate oral dosage forms. 520.1263...ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED...FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS...Lincomycin hydrochloride monohydrate oral dosage...

2011-04-01

146

75 FR 24710 - Determination That BREVIBLOC (Esmolol Hydrochloride) Injection, 250 Milligrams/Milliliter, 10...  

Federal Register 2010, 2011, 2012, 2013

...BREVIBLOC (Esmolol Hydrochloride) Injection, 250 Milligrams/Milliliter, 10-Milliliter...esmolol hydrochloride (HCl)) Injection, 250 milligrams (mg)/ milliliter (mL...applications (ANDAs) for esmolol HCl injection, 250 mg/mL, 10-mL ampule. FOR FURTHER...

2010-05-05

147

76 FR 53907 - Determination That TALWIN COMPOUND (Aspirin; Pentazocine Hydrochloride) Tablets, 325 Milligrams...  

Federal Register 2010, 2011, 2012, 2013

...Determination That TALWIN COMPOUND (Aspirin; Pentazocine Hydrochloride) Tablets...has determined that TALWIN COMPOUND (aspirin; pentazocine hydrochloride (HCl...abbreviated new drug applications (ANDAs) for aspirin; pentazocine HCl tablets, 325 mg;...

2011-08-30

148

78 FR 40484 - Determination That METADATE ER (Methylphenidate Hydrochloride) Extended-Release Tablet, 10...  

Federal Register 2010, 2011, 2012, 2013

...FDA-2013-P-0303] Determination That METADATE ER (Methylphenidate Hydrochloride) Extended-Release...Administration (FDA) has determined that METADATE ER (methylphenidate hydrochloride (HCl...does not refer to a listed drug. METADATE ER (methylphenidate HCl)...

2013-07-05

149

Simultaneous Spectrophotometric Determination of Drotaverine Hydrochloride and Paracetamol in Tablet  

PubMed Central

Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer's law was obeyed in the concentration range 5-50 ?g/ml for drotaverine and 5-60 ?g/ml for paracetamol. In Q analysis method, two wavelengths were selected at isobestic point (277 nm) and ?max of paracetamol (243.5 nm). In first order derivative method, zero crossing point for drotaverine hydrochloride and paracetamol were selected at 303.5 nm and 243.5 nm, respectively. The results of two methods were validated statistically and recovery studies were found to be satisfactory. PMID:20582207

Mahaparale, Sonali; Telekone, R. S.; Raut, R. P.; Damle, S. S.; Kasture, P. V.

2010-01-01

150

Temperature-dependent THz vibrational spectra of clenbuterol hydrochloride  

NASA Astrophysics Data System (ADS)

Using the high-resolution Terahertz Time-domain spectroscopy (THz-TDS) and the standard sample pellet technique, the far-infrared vibrational spectra of clenbuterol hydrochloride (CH), a ? 2-adrenergic agonist for decreasing fat deposition and enhancing protein accretion, were measured in temperature range of 77-295 K. Between 0.2 and 3.6 THz (6.6-120.0 cm-1), seven highly resolved spectral features, strong line-narrowing and a frequency blue-shift were observed with cooling. However, ractopamine hydrochloride, with some structural and pharmacological similarities to clenbuterol hydrochloride, showed no spectral features, indicating high sensitivity and strong specificity of THz-TDS. These results could be used for the rapid and nondestructive CH residual detection in food safety control.

Yang, YuPing; Lei, XiangYun; Yue, Ai; Zhang, Zhenwei

2013-04-01

151

Mucoadhesive bilayer tablets of propranolol hydrochloride.  

PubMed

The purpose of this research was to study mucoadhesive bilayer buccal tablets of propranolol hydrochloride using the bioadhesive polymers sodium alginate (Na-alginate) and Carbopol 934P (CP) along with ethyl cellulose as an impermeable backing layer. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, mucoadhesive strength, swelling index, in vitro drug release, ex vivo drug permeation, ex vivo mucoadhesion, and in vivo pharmacodynamics in rabbits. Tablets containing Na-alginate and CP in the ratio of 5:1 (F2) had the maximum percentage of in vitro drug release without disintegration in 12 hours. The swelling index was proportional to Na-alginate content and inversely proportional to CP content. The surface pH of all tablets was found to be satisfactory (7.0 +/- 1.5), close to neutral pH; hence, buccal cavity irritation should not occur with these tablets. The mechanism of drug release was found to be non-Fickian diffusion and followed zero-order kinetics. The formulation F4 was optimized based on good bioadhesive strength (28.9 +/- 0.99 g) and sustained in vitro drug permeation (68.65% +/- 3.69% for 12 hours). The behavior of formulation F4 was examined in human saliva, and both the drug and the buccal tablet were found to be stable. The formulation F4 was applied to rabbit oral mucosa for in vivo studies. The formulation inhibited isoprenaline-induced tachycardia. The studies conducted in rabbits confirmed the sustained release as compared with intravenous administration. PMID:17915827

Patel, Vishnu M; Prajapati, Bhupendra G; Patel, Harsha V; Patel, Karshanbhi M

2007-01-01

152

Stability of ondansetron hydrochloride and 12 medications in plastic syringes.  

PubMed

The stability and compatibility of ondansetron hydrochloride with neostigmine methylsulfate, naloxone hydrochloride, midazolam hydrochloride, fentanyl citrate, alfentanil hydrochloride, atropine sulfate, morphine sulfate, meperidine hydrochloride, propofol, droperidol, metoclopramide monohydrochloride, and glycopyrrolate were studied. Ondansetron 1.33 or 1.0 mg/mL was combined with 0.9% sodium chloride injection and each of the 12 drugs in duplicate in plastic syringes (or glass for propofol). The syringes were stored at 21.8-23.4 or 4 degrees C in the dark, except for those containing propofol, which were stored at ambient temperature. Samples were removed at 0, 4, 8, and 24 hours for analysis by high-performance liquid chromatography and pH measurement; the propofol-containing samples were removed at 0, 1, 2, and 4 hours. Syringes were visually assessed for color and clarity, and particulate content was measured with a particle counter at the end of the study period. All solutions containing ondansetron retained more than 90% of their initial ondansetron concentration. Solutions containing each of the other drugs except droperidol retained more than 90% of their initial concentration of these drugs. The solutions containing droperidol retained more than 90% of their initial droperidol concentration for up to eight hours at ambient temperature but precipitated quickly at 4 degrees C. In combinations of ondansetron 1.33 or 1.0 mg/mL and 10 of 12 drugs, all drugs were stable for 24 hours in plastic syringes at 23 and 4 degrees C; ondansetron hydrochloride 1.0 mg/mL and propofol 1.0 and 5.0 mg/mL in admixtures were stable for 4 hours, and droperidol on its own and combined with ondansetron 1.0 mg/mL was stable for no more than 8 hours at ambient temperature. PMID:9872702

Stewart, J T; Warren, F W; King, D T; Venkateshwaran, T G; Fox, J L

1998-12-15

153

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

PubMed Central

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

Denmark, Scott E.; Ares, Jeffrey J.

2011-01-01

154

Anticancer phytochemical analogs 37: synthesis, characterization, molecular docking and cytotoxicity of novel plumbagin hydrazones against breast cancer cells.  

PubMed

We have synthesized, structurally characterized and examined cytotoxicity of novel plumbagin hydrazones against estrogen and progesterone receptor positive (ER+/PR+) MCF-7 and triple negative MDA-MB-231 breast cancer cell lines in order to evaluate the potential of these novel phytochemical analogs. Compounds were docked into the protein cavity of p50-subunit of NF-?B protein revealing better fit and better binding energies than the parent plumbagin compound. This was also reflected in their superior cytotoxicities which were found to be mediated by inhibition of NF-?B expression. These compounds can provide a starting point for the development of novel drug molecules against triple negative breast cancers. PMID:24835626

Dandawate, Prasad; Ahmad, Aamir; Deshpande, Jyoti; Swamy, K Venkateswara; Khan, Ejazuddin M; Khetmalas, Madhukar; Padhye, Subhash; Sarkar, Fazlul

2014-07-01

155

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

PubMed Central

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.

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

2014-01-01

156

Increased Mortality in Groups of Cattle Administered the ?-Adrenergic Agonists Ractopamine Hydrochloride and Zilpaterol Hydrochloride  

PubMed Central

The United States Food and Drug Administration (FDA) approved two ?-adrenergic agonists (?AA) for in-feed administration to cattle fed in confinement for human consumption. Anecdotal reports have generated concern that administration of ?AA might be associated with an increased incidence of cattle deaths. Our objectives, therefore, were to a) quantify the association between ?AA 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 ?AA 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 ?AA 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 ?AA compared to contemporaneous controls. During the exposure period, 40 to 50% of deaths among groups administered the ?AA were attributed to administration of the drug. None of the available covariates meaningfully confounded the relationship between ?AA 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 ?AA and represents a heretofore unquantified adverse drug event. PMID:24621596

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

2014-01-01

157

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

PubMed

The United States Food and Drug Administration (FDA) approved two ?-adrenergic agonists (?AA) for in-feed administration to cattle fed in confinement for human consumption. Anecdotal reports have generated concern that administration of ?AA might be associated with an increased incidence of cattle deaths. Our objectives, therefore, were to a) quantify the association between ?AA 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 ?AA 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 ?AA 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 ?AA compared to contemporaneous controls. During the exposure period, 40 to 50% of deaths among groups administered the ?AA were attributed to administration of the drug. None of the available covariates meaningfully confounded the relationship between ?AA 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 ?AA and represents a heretofore unquantified adverse drug event. PMID:24621596

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

2014-01-01

158

Amides and Hydrazides from Amine and Hydrazine Hydrochlorides.  

ERIC Educational Resources Information Center

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

Shama, Sami A.; Tran, Thuan L.

1978-01-01

159

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

PubMed

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

Ponder, Celia; Overcash, Michael

2010-02-15

160

Stability of propranolol hydrochloride in SyrSpend SF.  

PubMed

Propranolol hydrochloride is a beta blocker used to treat high blood pressure, abnormal heart rhythms, heart disease, pheochromocytoma, and certain types of tremors. Propranolol is marketed by Wyeth (now a part of Pfizer) and AstraZeneca under the brand names Inderal, Inderal LA, Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilium, Bedranol SR (Sandoz). It is also available generically from several manufacturers. Propranolol hydrochloride is available as tablet, capsule, and oral liquid dosage forms in several strengths. Some patients are unable to tolerate oral tablets and capsules, challenging compounding pharmacies to seek alternative dosing options; namely oral solutions and suspensions. The objective of this study was to determine the stability of propranolol hydrochloride in SyrSpend SF. The drug was compounded into a 1-mg/mL suspension using SyrSpend SF and subsequently stored in a low-actinic plastic prescription bottle at room temperature conditions. Six samples were assayed at each specific time point extending to 90 days by a stability-indicating high-performance liquid chromatography method. The method was validated for its specificity through forced-degradation studies. Based on the data collected, when protected from light at room temperature, the beyond-use date of propranolol hydrochloride in SyrSpend SF was shown to be at least 90 days. PMID:23259369

Geiger, Christine M; Voudrie, Mark A; Sorenson, Bridget

2012-01-01

161

Olopatadine Hydrochloride Inhibits Capsaicin-Induced Flare Response in Humans  

Microsoft Academic Search

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

Masahisa Shindo; Yuichi Yoshida; Osamu Yamamoto

2011-01-01

162

Optical and electrical properties of hybrid photovoltaic devices from poly (3-phenyl hydrazone thiophene) (PPHT) and TiO 2 blend films  

Microsoft Academic Search

Bulk heterojunction photovoltaic devices based on blends of a conjugated polymer poly (3-phenyl hydrazone thiophene) (PPHT) as electron donor and titanium dioxide (TiO2) particles as an electron acceptor (n-type wide band gap semiconductor) have been studied. The blend films were spin coated from a common solvent mixture. The absorption peak and shape of the absorption spectra of PPHT:TiO2 (40vol%) indicate

G. D. Sharma; P. Suresh; Shailendra Kumar Sharma; M. S. Roy

2008-01-01

163

Polyacrolein-isonicotinic acid hydrazone and polyacrylic acid-thiohydrazide resins-synthesis and sorption properties for precious and base metals  

Microsoft Academic Search

This investigation carries on previous studies on polyacrolein-styrene resins. Further attempts were made to convert the reactive aldehyde groups of the polymeric support to functional acrolein-isonicotinic acid hydrazone (P-NHZ) or acrylic acid-thiohydrazide derivatives (P-THZD). The conditions of synthesis and the basic sorption and desorption properties of the polymers synthesized are described. For gold and platinum group metals the resins show

Xiao-Peng Ge; Bao-Wen Zhang; Manfred Grote

1998-01-01

164

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

PubMed Central

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

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

2014-01-01

165

The role of preorganization of hydrazone moieties on tetrathiacalix[4]arene platform for their conformational and binding properties from the view of structural investigation  

NASA Astrophysics Data System (ADS)

The IR, 1H and 13C NMR data, as well as conformation and dynamic behaviour of tetrathiacalix[4]arenes functionalized by hydrazone fragments are reported. The influence of isomers of thiacalix[4]arenes, the removal of tert-butyl groups from upper rim of macrocycle and the replacement of a phenyl substituents in the hydrazone fragments by 2-pyridyl ones on conformational properties of the compounds are discussed. The structural peculiarities of the cone isomer of 25,26,27,28-tetrakis[N 2-(2-pyridinylmethylidene)hydrazinocarbonylmethyloxy]-2,8,14,20-tetrathiacalix[4]arene and the 1, 3-alternate isomer of 25,26,27,28-tetrakis[N 2-(benzylidene)hydrazinocarbonylmethyloxy]-2,8,14,20-tetrathiacalix[4]arene in solution are compared with their crystal structures obtained by X-ray analysis. The correlation between extraction efficiency data obtained for these compounds earlier and the conformational features of calix[4]arene hydrazone derivatives studied in this work was performed.

Podyachev, Sergey N.; Gabidullin, Bulat M.; Syakaev, Victor V.; Sudakova, Svetlana N.; Gubaidullin, Aidar T.; Habicher, Wolf D.; Konovalov, Alexander I.

2011-08-01

166

New Cu(II), Co(II), Ni(II) complexes with aroyl-hydrazone based ligand. Synthesis, spectroscopic characterization and in vitro antibacterial evaluation.  

PubMed

A new aroyl-hydrazone, N-(2-pyridinecarbaldehyde)-N'-[4-(4-chloro-phenylsulfonyl) benzoyl]-hydrazone (L) and its Cu(II), Co(II) and Ni(II) complexes have been prepared. The structure of these compounds has been investigated by using elemental analysis, magnetic susceptibility, molar conductance, thermal and spectral (IR, UV, NMR, LC-MS, EPR) measurements. The semi-empirical method MM2, LC-ESI-MS, NMR and IR spectra indicate that the ligand behaves as mononegative bidentate/tridentate with NO/NON donor sequence in E isomeric form towards the metal ions. The magnetic and spectral data indicate a square-planar geometry for Ni2+ complex and an octahedral or pseudo-tetrahedral geometry for Co2+ and Cu2+ complexes. Bacterial activity of acyl-hydrazone (L) and its complexes were studied against gram-positive bacteria: Staphylococcus aureus, Bacillus subtilis and gram-negative bacteria: Pseudomonas aeruginosa, Escherichia coli by using minimum inhibitory concentrations (MICs) method. PMID:20133023

Angelusiu, Madalina Veronica; Barbuceanu, Stefania-Felicia; Draghici, Constantin; Almajan, Gabriela Laura

2010-05-01

167

Stability and compatibility of tirofiban hydrochloride during simulated Y-site administration with other drugs.  

PubMed

The stability and compatibility of tirofiban hydrochloride injection during simulated Y-site administration with various other drugs were studied. Tirofiban hydrochloride, dobutamine, epinephrine hydrochloride, furosemide, midazolam hydrochloride, and propranolol hydrochloride injections were each prepared from their respective concentrates in both 0.9% sodium chloride injection and 5% dextrose injection at both the minimum and maximum concentrations normally administered. The high-concentration solutions of midazolam hydrochloride and furosemide were used as is. Morphine sulfate was diluted in 5% dextrose injection only. Nitroglycerin premixed infusions, atropine sulfate injection, and diazepam injection were used as is. Tirofiban hydrochloride solutions were combined 1:1 with each of the secondary drug solutions in separate glass containers. Samples were stored for four hours at room temperature under ambient fluorescent light and were assayed for drug content and degradation by high-performance liquid chromatography and for pH, appearance, and turbidity. All mixtures except those containing diazepam remained clear and colorless, with no visual or turbidimetric indication of physical instability. Mixing of tirofiban hydrochloride and diazepam solutions resulted in immediate precipitation. all remaining mixtures remained clear. There was no significant loss of any of the drugs tested, no increase in known degradation products, and no appearance of unknown drug-related peaks. The pH of all test solutions remained constant. Tirofiban hydrochloride injection 0.05 mg/mL was stable for at least four hours when combined 1:1 in glass containers with atropine sulfate, dobutamine, epinephrine hydrochloride, furosemide, midazolam hydrochloride, morphine sulfate, nitroglycerin, and propranolol hydrochloride at the concentrations studied. Tirofiban hydrochloride was incompatible with diazepam. PMID:11449879

Bergquist, P A; Manas, D; Hunke, W A; Reed, R A

2001-07-01

168

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

PubMed

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 ?-relaxation together with the Johari-Goldstein (JG) ?-relaxation. Naturally the analogy leads us to name the slower and faster processes resolved in procaine hydrochloride and procainamide hydrochloride as the primary ?-conductivity relaxation and the secondary ?-conductivity relaxation, respectively. The analogy of the ?-conductivity relaxation in procaine HCl and procainamide HCl with JG ?-relaxation in non-ionic glass-formers goes further by the finding that the ?-conductivity is strongly related to the ?-conductivity relaxation at temperatures above and below T(g). At elevated pressure but compensated by raising temperature to maintain ?-conductivity relaxation time constant, the data show invariance of the ratio between the ?- and the ?-conductivity relaxation times to changes of thermodynamic condition. This property indicates that the ?-conductivity relaxation has fundamental importance and is indispensable as the precursor of the ?-conductivity relaxation, analogous to the relation found between the Johari-Goldstein ?-relaxation and the structural ?-relaxation in non-ionic glass-forming systems. The novel features of the ionic conductivity relaxation are brought out by presenting the measurements in terms of the electric modulus or permittivity. If presented in terms of conductivity, the novel features are lost. This warns against insisting that a log-log plot of conductivity vs. frequency is optimal to reveal and interpret the dynamics of ionic conductors. PMID:22559496

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

2012-04-28

169

Growth and characterization of thiosemicarbazide hydrochloride: a semiorganic NLO material.  

PubMed

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, (1)H and (13)C 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. PMID:21820946

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

2011-11-01

170

Impurity profiling of methamphetamine hydrochloride drugs seized in the Philippines  

Microsoft Academic Search

Methamphetamine hydrochloride is one of the most widely used illicit drugs in the Philippines. In this study, we describe the application of cluster analysis of trace impurities in the profiling of the seized methamphetamine drug samples.Thirty milligrams of a homogenized drug sample were dissolved in 1mL of pH 10.5 buffer solution and extracted with ethyl acetate containing three internal standards.

Fabian M Dayrit; Morphy C Dumlao

2004-01-01

171

Stability Indicating Assay of Lidocaine Hydrochloride in Solution  

Microsoft Academic Search

A simple and improved stability-indicating gas liquid chromatographic procedure using flame ionization detection is described for the determination of lidocaine hydrochloride in solution in the presence of N, N'-diethyl-methyl-glycine xylidide as internal standard (IST). This method is capable of distinguishing the intact drug from its thermal degradation products. A linear relationship between peak height ratio (lidocaine-HC1\\/IST) and lidocaine-HCl concentrations is

S. Stavchansky; B. Eghbali; R. Geary

1987-01-01

172

REACTION Of GLYCOSYL ISOTHIOCYNATES WITH 3-INDOLYLAMINOMETHYL-KETONE HYDROCHLORIDE  

Microsoft Academic Search

Reaction of glycosyl isothiocyanate 1a-c with 3-indolylaminomethyl-ketone hydrochloride(2) yielded glycosylthiourea derivatives 3a-c. Cyclodehydration of 3a-c with acetic anhydride afforded 5-(indol-3-yl)-2-[N-per-O-acetyl-D-glycopyranosyl)amino]thiazoles 4a-c. Deacetylation of 4a-c gave 5-(indol-3-yl)-2-[N-(D-glycopyranosyl) amino]thiazoles 5a-c.

Mohamed A. Saleh

2002-01-01

173

Structure and vibrational spectra of pyridine betaine hydrochloride  

Microsoft Academic Search

The crystal structure of pyridine betaine hydrochloride (PBET·HCl) was determined by X-ray diffraction to be monoclinic, space group P21c with a = 8.533(2) A?, b = 9.548(2) A?, c = 10.781(2) A?, ? = 107.228(3)° and Z = 4. Betaine is protonated and the carboxyl group forms a hydrogen bond with the chloride ion: O·Cl? distance is 2.928(3) Å.The interaction

Miros?aw Szafran; Jacek Koput; Jan Baran; Tadeusz G?owiak

1997-01-01

174

Calculation of the vibrational spectra of betaine hydrochloride  

Microsoft Academic Search

The molecular geometries of betaine hydrochloride, BET·HCl, and free protonated betaine, BET·H+, were calculated with the 6–31G(d,p) basis set at the SCF, MP2 and DFT levels of theory. At the SCF level, the minimum energy corresponds to the ionic pair, B+Htctdot;A?, however, the equilibrium Otctdot;Cl distance is 0.14 Å shorter than the X-ray value. Inclusion of the correlation effects, both

Miroslaw Szafran; Jacek Koput

1997-01-01

175

Recrystallization of tetracycline hydrochloride using supercritical anti-solvent process  

Microsoft Academic Search

Tetracycline hydrochloride (TTC) was micronized by an Aerosol Solvent Extraction System (ASES) using supercritical CO2. The effects of solvent, pressure and temperature of CO2, solution concentration, and solution feed rate on particle size were investigated. Mean particle sizes of processed TTC\\u000a were 0.16–0.31 ?m, but the morphologies of processed particles were affected by agglomeration between the primary particles.\\u000a Mean particle

Junho Chu; Hanho Lee; Hwayong Kim; Youn-Woo Lee

2009-01-01

176

Psychosedation with dexmedetomidine hydrochloride during minor oral surgery.  

PubMed

We performed intravenous sedation with dexmedetomidine hydrochloride during minor oral surgery and compared this agent with propofol. Patients were randomly divided into 2 groups: dexmedetomidine hydrochloride (D) and propofol (P) groups. In Group D, systolic blood pressure (SBP) increased immediately after the start of initial loading, although no significant differences were noted. Both SBP and diastolic blood pressure (DBP) gradually decreased during maintenance administration and were significantly lower than pretreatment values. The heart rate decreased immediately after the start of administration and was significantly lower during both initial loading and maintenance administration; the heart rate was also significantly lower than that in Group P. In Group D, arterial blood oxygen saturation (SpO2) significantly decreased after the sedation level reached an optimum level until the end of administration. The bispectral index (BIS) value gradually decreased during initial loading. At the optimal sedation level, it decreased to 80 to 85. During maintenance administration, marked changes were observed in this parameter. No marked differences in amnestic effects and comfort were noted between the 2 groups. If the sedation level can be evaluated accurately via another objective method, intravenous sedation with dexmedetomidine hydrochloride may be useful in dental treatment. PMID:19769420

Taniyama, Kiichi; Oda, Hideki; Okawa, Kazuko; Himeno, Katsuhito; Shikanai, Koki; Shibutani, Tohru

2009-01-01

177

Stability of ondansetron hydrochloride injection in various beverages.  

PubMed

The stability of ondansetron hydrochloride injection in beverages likely to be acceptable to patients was studied. Ondansetron hydrochloride injection (containing ondansetron 2 mg/mL) was added to apple juice, fruit punch, cherry-flavored drink, carbonated soft drinks, and hot tea to provide a nominal ondansetron concentration of 32.8, 64.5, or 95.2 micrograms/mL. Samples were stored at -3 to 28 degrees C (noncarbonated-beverage mixtures except tea), 2 to 28 degrees C (carbonated-beverage mixtures), and 25 degrees C (tea) and assayed for ondansetron concentration by high-performance liquid chromatography at 6, 24, 48, and 72 hours (noncarbonated-beverage mixtures except tea); 6, 24, and 48 hours (carbonated-beverage mixtures); and 1 hour (tea). More than 95% of the initial ondansetron concentration was retained in apple juice, fruit punch, cherry-flavored drink, Sprite, and Diet Coke throughout the periods studied. A precipitate formed immediately after ondansetron was added to hot tea, but the drug was chemically stable for at least one hour in this preparation. Ondansetron hydrochloride injection 32.7, 64.5, and 95.2 micrograms/mL (expressed as free base) was stable in various beverages when stored at -3 to 28 degrees C for up to 72 hours. Ondansetron at these same concentrations precipitated in hot tea preparations but was chemically stable for at least one hour. PMID:8528869

Yamreudeewong, W; Danthi, S N; Hill, R A; Fox, J L

1995-09-15

178

Stability of ondansetron hydrochloride injection in extemporaneously prepared oral solutions.  

PubMed

The stability of ondansetron hydrochloride in extemporaneously prepared oral solutions containing orange juice, cola, or cherry syrup was determined. Solutions were prepared by adding ondansetron hydrochloride to orange juice, cola, or cherry syrup to produce ondansetron concentrations of 0.267 and 0.067 mg/mL in orange juice or cola and 0.533 mg/mL in cherry syrup. The ondansetron concentration in orange juice and cola solutions was assayed at the time of preparation and at 30 minutes and one hour. The cherry syrup solution was stored at both 3-5 and 25-27 degrees C, with the ondansetron concentration being determined at the time of preparation and daily for seven days. All the solutions were prepared in triplicate. Ondansetron concentrations were measured by stability-indicating high-performance liquid chromatography. At each time interval, the mean ondansetron concentration remained > or = 97% of the initial measurement for all solutions. The appearance and color of the solutions did not change. Ondansetron hydrochloride was stable for at least one hour in orange juice or cola and at least seven days in cherry syrup. PMID:8427264

Graham, C L; Dukes, G E; Fox, J L; Kao, C F; Hak, L J

1993-01-01

179

Bendamustine hydrochloride activity against doxorubicin-resistant human breast carcinoma cell lines.  

PubMed

The cytotoxic activity of bendamustine hydrochloride was evaluated against human ovarian and breast carcinoma cell lines including cell lines resistant to cisplatin and doxorubicin in vitro. The relative degree of resistance to bendamustine hydrochloride was lower in all cell lines compared with cyclophosphamide, melphalan and BCNU, suggesting only incomplete cross-resistance. Furthermore lower levels of resistance were also observed in all breast cancer cell lines when bendamustine hydrochloride was compared with cisplatin. Bendamustine hydrochloride also presents good activity in cell line MCF 7 AD, which is approximately 80-fold resistant to doxorubicin compared with MCF 7. Basic glutathione levels and activity of glutathione-S-transferase showed no correlation to the IC50 values for bendamustine hydrochloride in the cell lines. When given at equitoxic concentrations, bendamustine hydrochloride consistently induced more DNA double-strand breaks than melphalan, cyclophosphamide or BCNU. In addition, removal of DNA double-strand breaks induced by bendamustine hydrochloride was relatively slow with the majority of DNA double-strand breaks still being detectable after 24 h. These findings indicate differences in the interaction between bendamustine hydrochloride and DNA, and may explain the lack of complete cross-resistance between bendamustine hydrochloride and the other alkylating agents. PMID:8826610

Strumberg, D; Harstrick, A; Doll, K; Hoffmann, B; Seeber, S

1996-06-01

180

Antiplatelet and antithrombotic activities of non-steroidal anti-inflammatory drugs containing an N-acyl hydrazone subunit.  

PubMed

Nonsteroidal anti-inflammatory drugs (NSAIDs) 1-5 containing an N-acyl hydrazone subunit were prepared and their antiplatelet and antithrombotic activities assessed in vitro and in vivo. Compounds 1-5 inhibited the platelet aggregation induced by adenosine diphosphate and/or arachidonic acid, with inhibition rates of 18.0%-61.1% and 65.9%-87.3%, respectively. Compounds 1 and 5 were the most active compounds, inhibiting adenosine-diphosphate-induced platelet aggregation by 57.2% and 61.1%, respectively. The inhibitory rates for arachidonic-acid-induced platelet aggregation were similar for compound 2 (80.8%) and acetylsalicylic acid (ASA, 80%). After their oral administration to mice, compounds 1, 3, and 5 showed shorter mean bleeding times than ASA. Compounds 1 and 5 also protected against thromboembolic events, with survival rates of 40% and 33%, respectively, compared with 30% for ASA. In conclusion, these results indicate that these novel NSAIDs containing an NAH subunit may offer better antiplatelet and antithrombotic activities than ASA. PMID:24549233

Chelucci, Rafael Consolin; Dutra, Luiz Antônio; Lopes Pires, Maria Elisa; de Melo, Thais Regina Ferreira; Bosquesi, Priscila Longhin; Chung, Man Chin; Dos Santos, Jean Leandro

2014-01-01

181

Synthesis, molecular docking, and biological evaluation of some novel hydrazones and pyrazole derivatives as anti-inflammatory agents.  

PubMed

2-Hydrazinyl-N-(4-sulfamoylphenyl)acetamide 3 was the key intermediate for the synthesis of novel hydrazones 4-10 and pyrazole derivatives 11-17. All compounds were tested for their in vivo anti-inflammatory activity and their ability to inhibit the production of PGE(2) in serum samples of rats. IC(50) values for the most active compounds for inhibition of COX-1 and COX-2 enzymes were determined in vitro, and they were also tested for their ulcerogenic effect. Molecular docking was performed on the active site of COX-2 to predict their mode of binding to the amino acids. Most of the synthesized compounds showed good anti-inflammatory activity especially compounds 3, 4, 8, 9, 15, and 17 which showed better activity than diclofenac as the reference drug. Compounds 3, 8, 9, 13, and 15-17 were less ulcerogenic than indomethacine as the reference drug. Most of the synthesized compounds interacted with Tyr 385 and Ser 530 in molecular docking study with additional hydrogen bond for compound 17. Compound 17 showed good selectivity index value of 11.1 for COX-1/COX-2 inhibition in vitro. PMID:24720475

Mohammed, Khaled O; Nissan, Yassin M

2014-10-01

182

Synthesis and in vitro evaluation of new nitro-substituted thiazolyl hydrazone derivatives as anticandidal and anticancer agents.  

PubMed

Fourteen new thiazolyl hydrazone derivatives were synthesized and evaluated for their anticandidal activity using a broth microdilution assay. Among the synthesized compounds, 2-[2-((5-(4-chloro-2-nitrophenyl)furan-2-yl)methylene)hydrazinyl]-4-(4-fluorophenyl)thiazole and 2-[2-((5-(4-chloro-2-nitrophenyl)furan-2-yl)methylene) hydrazinyl]-4-(4-methoxyphenyl)thiazole were found to be the most effective antifungal compounds against Candida utilis, with a MIC value of 250 µg/mL, when compared with fluconazole (MIC=2 µg/mL). Additionally, the synthesized compounds were evaluated for their in vitro cytotoxic effects on the MCF-7 and NIH/3T3 cell lines. As a result, 2-[2-((5-(4-chloro-2-nitrophenyl)furan-2-yl)methylene)hydrazinyl]-4-(4-chlorophenyl)thiazole was identified as the most promising anticancer compound against MCF-7 cancer cells due to its inhibitory effects (IC50=125 µg/mL) and relatively low toxicity towards the NIH/3T3 cell line (IC50>500 µg/mL). PMID:25232704

Alt?ntop, Mehlika Dilek; Özdemir, Ahmet; Turan-Zitouni, Gülhan; Ilg?n, Sinem; Atl?, Özlem; Demirci, Fatih; Kaplanc?kl?, Zafer As?m

2014-01-01

183

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

SciTech Connect

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.

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

2007-01-01

184

The Cytotoxicity of Benzaldehyde Nitrogen Mustard-2-Pyridine Carboxylic Acid Hydrazone Being Involved in Topoisomerase II? Inhibition  

PubMed Central

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??M , HCT-116: 57.5 ± 5.3??M, K562: 48.2 ± 4.0??M, and PC-12: 19.4 ± 2.2??M) were used to investigate its cytotoxicity and potential mechanism. In vitro experimental data showed that the BNMPH chelating Fe2+ 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 Fe2+ 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 II?. Those revealed that the cytotoxic mechanism of the BNMPH could stem from both the topoisomerase II inhibition, ROS generation and DNA alkylation. PMID:24995306

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

2014-01-01

185

Probing the adverse temperature dependence in the static fluorescence quenching of BSA induced by a novel anticancer hydrazone.  

PubMed

A novel hydrazone, 2-hydroxy-N'-(3-hydroxybenzylidene) benzohydrazide (HHB), has been designed, synthesized and characterized. HHB was designed to be an analogue of 311 and PIH with potential anticancer activity, and the IC(50) towards HeLa cell was about 3.46 × 10(-5) mol(-1) L. The interactions of HHB with bovine serum albumin (BSA) had been investigated systematically by spectroscopy, electrochemistry, and molecular modeling under simulative physiological conditions. HHB bound BSA in the sub-domains IIA to form a ground-state complex, inducing the quenching of the intrinsic fluorescence emission, the change of absorption spectrum and the increase of electrical resistance of BSA. An adverse temperature dependence in the fluorescence quenching was detected and discussed to be a reasonable consequence of the big E(a) requirement to overcome the obstructive amino acid residues in the entrance to the binding site, which were closely related to the natural structure of BSA and the molecular shape of HHB. The impact of metal ions, including Fe(2+), Fe(3+), Cu(2+), Mg(2+), Zn(2+), Ca(2+) and Al(3+), towards the interactions of HHB and BSA has been investigated and they were found to affect the HHB-BSA interactions in a mild way. PMID:22911144

Tong, Jin-Qiang; Tian, Fang-Fang; Li, Qing; Li, Li-Li; Xiang, Chen; Liu, Yi; Dai, Jie; Jiang, Feng-Lei

2012-12-01

186

Discovery of Novel Orally Active Anti-Inflammatory N-Phenylpyrazolyl-N-Glycinyl-Hydrazone Derivatives That Inhibit TNF-? Production  

PubMed Central

Herein, we describe the synthesis and pharmacological evaluation of novel N-phenylpyrazolyl-N-glycinyl-hydrazone derivatives that were designed as novel prototypes of p38 mitogen-activated protein kinase (MAPK) inhibitors. All of the novel synthesized compounds described in this study were evaluated for their in vitro capacity to inhibit tumor necrosis factor ? (TNF-? production in cultured macrophages) and in vitro MAPK p38? inhibition. The two most active anti-TNF-? derivatives, (E)-2-(3-tert-butyl-1-phenyl-1H-pyrazol-5-ylamino)-N’-((4-(2-morpholinoethoxy)naphthalen-1-yl)methylene)acetohydrazide (4a) and (E)-2-(3-tert-butyl-1-phenyl-1H-pyrazol-5-ylamino)-N’-(4-chlorobenzylidene)acetohydrazide (4f), were evaluated to determine their in vivo anti-hyperalgesic profiles in carrageenan-induced thermal hypernociception model in rats. Both compounds showed anti-inflammatory and antinociceptive properties comparable to SB-203580 used as a standard drug, by oral route at a dose of 100 µmol/kg. This bioprofile is correlated with the ability of NAH derivatives (4a) and (4f) suppressing TNF-? levels in vivo by 57.3 and 55.8%, respectively. PMID:23056531

Lacerda, Renata B.; da Silva, Leandro L.; de Lima, Cleverton K. F.; Miguez, Eduardo; Miranda, Ana Luisa P.; Laufer, Stefan A.; Barreiro, Eliezer J.; Fraga, Carlos A. M.

2012-01-01

187

HIV-1 Reverse Transcriptase Structure with RNase H Inhibitor Dihydroxy Benzoyl Naphthyl Hydrazone Bound at a Novel Site  

PubMed Central

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 Å 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 Å 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. PMID:17184135

Himmel, Daniel M.; Sarafianos, Stefan G.; Dharmasena, Sanjeewa; Hossain, Mohammed M.; McCoy-Simandle, Kessler; Ilina, Tatiana; Clark, Arthur D.; Knight, Jennifer L.; Julias, John G.; Clark, Patrick K.; Krogh-Jespersen, Karsten; Levy, Ronald M.; Hughes, Stephen H.; Parniak, Michael A.; Arnold, Eddy

2010-01-01

188

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

PubMed Central

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. PMID:25097652

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

2014-01-01

189

76 FR 53908 - Determination That OPANA ER (Oxymorphone Hydrochloride) Extended-Release Tablets, 7.5 Milligrams...  

Federal Register 2010, 2011, 2012, 2013

...FDA-2011-P-0209] Determination That OPANA ER (Oxymorphone Hydrochloride) Extended...Administration (FDA) has determined that OPANA ER (oxymorphone hydrochloride (HCl)) extended-release...ANDAs that refer to the listed drug. OPANA ER (oxymorphone HCl) extended-release...

2011-08-30

190

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

PubMed Central

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

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

2011-01-01

191

The thermodynamic characteristics of swelling of novocaine hydrochloride crystals brought into isopiestic contact with water-salt solutions  

NASA Astrophysics Data System (ADS)

The interaction of water with solid Novocaine hydrochloride was studied isopiestically over a wide range of solvent relative activities. The Gibbs energy of water interaction with Novocaine hydrochloride crystals was calculated. A scheme of intermolecular interactions in the water-Novocaine hydrochloride system was suggested.

Krysanova, T. A.; Kotova, D. L.; Selemenev, V. F.

2009-02-01

192

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

SciTech Connect

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.

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

2010-12-07

193

Sustained release of verapamil hydrochloride from sodium alginate microcapsules.  

PubMed

The objective of the present study was to develop sustained release microcapsules of verapamil hydrochloride (VH) using biodegradable polymers. For this purpose microcapsules embedded verapamil hydrochloride were prepared using sodium alginate alone and also by incorporating some co polymers like methyl cellulose (MC), sodium carboxy methyl cellulose (SCMC) , poly vinyl pyrollidone (PVP) and xanthan gum by employing complex emulsion method of microencapsulation. Microcapsules were prepared in various core: coat ratios to know the effect of polymer and co polymers on drug release. Overall ten formulations were prepared and evaluated for flow behaviour, sieve analysis, drug entrapment efficiency, in vitro dissolution studies, stability studies, including scanning electron microscopy and DSC. The resulting microcapsules were discrete, large, spherical and also free flowing. The drug content in all the batches of microcapsules was found to be uniform. The release was depended on core: coat ratio and nature of the polymers. FTIR analysis revealed chemical integrity between Verapamil hydrochloride (VH), sodium alginate and between the copolymers. Among the four copolymers used methyl cellulose retarded the drug release more than the other three, hence the same formulation was subjected for in vivo studies. The drug release from the microcapsules was found to be following non fickian diffusion. Mechanism of drug release was diffusion controlled first order kinetics. Drug diffusion co efficient and correlation co efficient were also assessed by using various mathematical models. In vivo result analysis of pharmacokinetic parameters revealed that t max of reference and test formulations were almost same. From the study it was concluded that, sustained release Verapamil hydro chloride microcapsules could be achieved with success using sodium alginate alone and also in combination with other biodegradable polymers. PMID:20158489

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

2010-04-01

194

Cocrystals of bis(4-hydroxy-1-methylpiperidine betaine) hydrochloride  

NASA Astrophysics Data System (ADS)

Bis(4-hydroxy-1-methylpiperidine betaine) hydrochloride, [bis(1-carboxymethyl-4-hydroxy-1-methylpiperidinium) hydrochloride, (HO-MPB) 2HCl], has been prepared from stoichiometric amounts of ?-4-hydroxy-1-methylpiperidine betaine hydrochloride with the OH group in an equatorial position and ?-4-hydroxy-1-methylpiperidine betaine inner salt with the OH group in an axial one. Cocrystals of (HO-MPB) 2HCl belong to monoclinic system with C2/ c space group. Piperidinium ring has a chair conformation with the CH 2COO group in the equatorial position and the CH 3 group in the axial one, while the OH group occupies the equatorial or axial position in the disordered structure. There are three types of substituted piperidinium molecules A, B and C in the asymmetric unit. These isomers are distributed randomly yielding partially occupied sites of the hydroxyl groups. The disorder of molecules has been confirmed by the X-ray diffraction experiments at low temperature. The piperidinium molecules form two independent homoconjugated cations, A-B and C-C, with short asymmetrical (2.457(2) Å) and symmetrical (2.440(2) Å) OHO hydrogen bonds, respectively. The hydroxyl groups interact with the Cl - anions by the O-H⋯Cl hydrogen bonds. The A- B cation is linked with C- C by the O-H⋯O-H hydrogen bond, while C- C cations are joined together by the O-H⋯O=C hydrogen bonds, forming infinite zigzag chains. The FTIR spectrum shows an intense ?OH band in the 3300-3100 cm -1 region and a broad and intense ?(OHO) absorption in the 1500-400 cm -1 region, which confirm the presence of the O-H⋯Cl and O·H·O hydrogen bonds. The 1H and 13C NMR spectra, in the aqueous solution, prove the inequivalence of the piperidinium ring caused by two conformations of the OH group at the ring.

Dega-Szafran, Z.; Dulewicz, E.; Dutkiewicz, G.; Kosturkiewicz, Z.

2006-08-01

195

Sustaining pattern of phenformin hydrochloride using various polymers and waxes.  

PubMed

The present study was carried out to formulate matrix tablets of phenformin hydrochloride. Granules of phenformin HCl were prepared by using ethyl cellulose, eudragit RS 100, gum acacia, carnauba wax, stearyl alcohol, glyceryl monostearate and triethanol amine. Thus the granules were compressed and fourteen tablets formulations were prepared. All the physical parameters of granules and matrix tablets were studied including compatibility study. One commercial timed disintegration capsule was also included for study and comparison. The results of in vitro studies showed that sustained release matrix tablet might be prepared using carnauba wax, stearyl alcohol, triethanol amine and magnesium stearate. PMID:12481378

Pandey, V P; Kannappan, N; Manavalan, R; Subburaj, T

2002-01-01

196

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

NASA Technical Reports Server (NTRS)

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.

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

1973-01-01

197

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)

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.

Ünal, Arslan; Eren, Bilge; Eren, Erdal

2013-10-01

198

Fabrication and Development of Pectin Microsphere of Metformin Hydrochloride  

PubMed Central

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

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

2012-01-01

199

Extraocular myotoxicity of the retrobulbar anesthetic bupivacaine hydrochloride.  

PubMed

Morphopathological changes induced in the extraocular muscles by the local anesthetic agent bupivacaine hydrochloride were studied in the monkey using light and electron microscopy. Retrobulbar anesthetic blocks, using 0.75% bupivacaine hydrochloride, were performed in five adult cynomolgus monkeys. Morphological alterations in extraocular muscle fiber types were examined following survival periods of 3-27 days. Bupivacaine injections produced a mild and very limited myopathic response, with changes largely restricted to the global layer singly-innervated muscle fiber type which is characterized by low mitochondrial content. For survival times beyond 3 days, this fiber type exhibited peripheral migration and swelling of mitochondria and an outside-in pattern of myofibril dissolution. Some affected fibers also exhibited the Ringbinden or ring fiber pathology. Maximal myotoxic response was observed at 14 days after injections, and pathological changes were largely resolved by 27 days. A more limited analysis of the effects of retrobulbar injection of lidocaine revealed similar morphopathological responses, thereby suggesting that these effects are a property common to the entire class of aminoacyl anesthetics. In contrast to previous observations in other skeletal musculature, the extraocular muscles proved to be unexpectedly resistant to local anesthetic treatment as only limited alterations were observed. The observed muscle fiber type specificity was interpreted to result from differences in the relative ability of muscle fiber types to adapt to anesthetic-induced elevations of intracellular free calcium levels. PMID:3338877

Porter, J D; Edney, D P; McMahon, E J; Burns, L A

1988-02-01

200

Effect of tolazoline hydrochloride on sputum viscosity in cystic fibrosis  

PubMed Central

Comparisons have been made between the effects of autonomic dysfunction and the pathophysiological changes in the exocrine secretions from patients with cystic fibrosis (Roberts, 1959). Cotton (1966) found that administration of tolazoline hydrochloride (an alpha-adrenergic blocker) to patients with cor pulmonale in the terminal stages of cystic fibrosis was associated with an improvement in the results of their lung function tests. This effect might have been due to an alteration of the abnormal viscosity of the bronchial mucus mediated via the autonomic nervous system, thus permitting easier expectoration. Measurement, by means of a Ferranti-Shirely cone and plate viscometer, of several different aspects of sputum viscosity is described. Tolazoline hydrochloride, administered to five patients with cystic fibrosis, was shown not to differ significantly from a placebo in its effect on sputum viscosity and dynamic lung volumes. We could not relate the improved lung function seen in Cotton's series to an autonomic effect of the drug on the physical properties of bronchial mucus in this condition. PMID:5494682

Feather, Elizabeth A.; Russell, George

1970-01-01

201

Solid Lipid Nanoparticles of a Water Soluble Drug, Ciprofloxacin Hydrochloride  

PubMed Central

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

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

2012-01-01

202

Formulation and Evaluation of Tramadol hydrochloride Rectal Suppositories  

PubMed Central

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. PMID:21394263

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

2008-01-01

203

Oral administration of diazepam and promazine hydrochloride to immobilize pronghorn.  

PubMed

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

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

1982-01-01

204

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride.  

PubMed

Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h. PMID:21684848

Someshwar, Komuravelly; Chithaluru, Kalyani; Ramarao, Tadikonda; Kumar, K K Kalyan

2011-06-01

205

Bioassay of 2,4-dimethoxyaniline hydrochloride for possible carcinogenicity.  

PubMed

2,4-Dimethoxyaniline hydrochloride, the hydrochloride salt of the dye intermediate 2,4-dimethoxyaniline, was selected for bioassay by the National Cancer Institute because of the increased incidence of bladder cancer among dye manufacturing industry workers. Aromatic amines are one of several classes of chemicals thought to contribute to the increased cancer risk in this industry. A bioassay for the possible carcinogenicity of 2,4-dimethoxyaniline HCl was conducted using Fischer 344 rats and B6C3F1 mice. 2,4-Dimethoxyaniline HCl was administered in the feed, at either of two concentrations, to groups of 50 male and 50 female animals of each species. Twenty animals of each sex and species were placed on test as controls. The high and low dietary concentrations of 2,4-dimethoxyaniline HCl were, respectively, 3,000 and 1,500 ppm for rats and 5,000 and 2,500 ppm for mice. The compound was administered in the diet for 104 weeks to rats and 103 weeks to mice, followed by a 1-week observation period for both species. There were no significant positive associations between the concentrations of 2,4-dimethoxyaniline HCl administered and mortality in rats or mice of either sex. Adequate numbers of animals in all groups survived sufficiently long to be at risk from late-developing tumors. Dose-related mean body weight depression was observed for females of both species, indicating that the concentrations of 2,4-dimethoxyaniline HCl administered to these groups may have approximated the maximum tolerated concentrations. Compound-related mean body weight depression was only slight for male rats and was apparent in male mice only until week 50; however follicular-cell hyperplasias and cystic follicles of the thyroid were observed in dosed male mice, suggesting that the concentrations the male mice received may have approximated the maximum tolerated concentrations. Since no distinct mean body weight depression in relation to controls, no significant accelerated mortality, and no other signs of toxicity were associated with administration of 2,4-dimethoxyaniline HCl to male rats, it is possible that these animals may have been able to tolerate a higher dietary concentration. There was a significant positive trend between concentration of the test chemical and the incidence of a combination of hepatocellular carcinomas and adenomas in male mice and an increase in the combination of these lesions in female mice. However, no statistically significant differences in tumor incidence at any site were observed when dosed rats and mice were compared to their respective controls. Under the conditions of this bioassay there was no convincing evidence for the carcinogenicity of 2,4-dimethoxyaniline HCl in Fischer 344 rats or B6C3F1 mice. Levels of Evidence of Carcinogenicity: Male Rats: Negative Female Rats: Negative Male Mice: Negative Female Mice: Negative Synonyms: 2,4-dimethoxybenzenamine hydrochloride; 4-methoxy-o-anisidine hydrochloride; 2-methoxy-p-anisidine hydrochloride PMID:12799692

1979-01-01

206

Gemcitabine Hydrochloride-Loaded Functionalised Carbon Nanotubes as Potential Carriers for Tumour Targeting  

PubMed Central

The objective of the present work was to formulate gemcitabine hydrochloride loaded functionalised carbon nanotubes to achieve tumour targeted drug release and thereby reducing gemcitabine hydrochloride toxicity. Multiwalled carbon nanotubes were functionalised using 1,2-distearoylphosphatidyl ethanolamine-methyl polyethylene glycol conjugate 2000. Optimised ratio 1:2 of carbon nanotubes:1,2-distearoylphosphatidyl ethanolamine-methyl polyethylene glycol conjugate 2000 was taken for loading of gemcitabine hydrochloride. The formulation was evaluated for different parameters. The results showed that maximum drug loading efficiency achieved was 41.59% with an average particle size of 188.7 nm and zeta potential of ?10?1 mV. Scanning electron microscopy and transmission electron microscopy images confirmed the tubular structure of the formulation. The carbon nanotubes were able to release gemcitabine hydrochloride faster in acidic pH than at neutral pH indicating its potential for tumour targeting. Gemcitabine hydrochloride release from carbon nanotubes was found to follow Korsmeyer-Peppas kinetic model with non-Fickian diffusion pattern. Cytotoxic activity of formulation on A549 cells was found to be higher in comparison to free gemcitabine hydrochloride. Stability studies indicated that lyophilised samples of the formulation were more stable for 3 months under refrigerated condition than at room temperature. Thus carbon nanotubes can be promising carrier for the anticancer drug gemcitabine hydrochloride. PMID:24591746

Das, Shilpee; Desai, Jagruti L.; Thakkar, Hetal P.

2013-01-01

207

Neuroprotective effect of penehyclidine hydrochloride on focal cerebral ischemia-reperfusion injury?  

PubMed Central

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

Yu, Cuicui; Wang, Junke

2013-01-01

208

Multivariate Chemometric Assisted Analysis of Metformin Hydrochloride, Gliclazide and Pioglitazone Hydrochloride in Bulk Drug and Dosage Forms  

PubMed Central

Purpose: In this work a numerical method, based on the use of spectrophotometric data coupled to partial least squares (PLS) regression and net analyte preprocessing combined with classical least square (NAP/CLS) multivariate calibration, is reported for the simultaneous determination of metformin hydrochloride (MET), gliclazide (GLZ) and pioglitazone hydrochloride (PIO) in synthetic samples and combined commercial tablets. Methods: Spectra of MET, GLZ and PIO were recorded at concentrations within their linear ranges (5-25 µg/ml, 0.5-8 µg/ml and 0.5-3 µg/ml respectively) and were used to compute a total of 25 synthetic mixtures involving 15 calibration and 10 validation sets between wavelength range of 200 and 400 nm in 0.1N HCl. The suitability of the models was decided on the basis of root mean square error (RMSE) values of calibration and validation data. Results: The analytical performances of these chemometric methods were characterized by relative prediction errors and recovery studies (%) and were compared with each other. These two methods were successfully applied to pharmaceutical formulation, tablet, with no interference with excipients as indicated by the recovery study results. Mean recoveries of the commercial formulation set together with the figures of merit (calibration sensitivity, selectivity, limit of detection, limit of quantification etc.) were estimated. Conclusion: The proposed methods are simple, rapid and can be easily used as an alternative analysis tool in the quality control of drugs and formulation. PMID:24312816

Bhaskar, Radhika; Bhaskar, Rahul; Sagar, Mahendra K; Saini, Vipin

2013-01-01

209

Validated HPLC determination of the two fixed dose combinations (chlordiazepoxide hydrochloride and mebeverine hydrochloride; carvedilol and hydrochlorothiazide) in their tablets.  

PubMed

Simple, rapid, and selective RP-HPLC methods with UV detection were developed for simultaneous determination of chlordiazepoxide hydrochloride and mebeverine hydrochloride (Mixture I) and carvedilol and hydrochlorothiazide (Mixture II). The chromatographic separation in both mixtures was achieved by using an RP-C8 (octylsilyl) analytical column. For Mixture I, a mobile phase composed of acetonitrile-0.05 M disodium hydrogen phosphate-triethylamine (50 + 50 + 0.2, v/v/v), pH 2.5, was used; the detector wavelength was 247 nm. For Mixture II, the mobile phase consisted of acetonitrile-0.05 M disodium hydrogen phosphate (50 + 50, v/v), pH 4.0, and the detector was set at 220 nm. Quantification of the analytes was based on measuring their peak areas. Both mixtures were resolved in less than 6 min. The reliability and analytical performance of the proposed HPLC procedures were statistically validated with respect to linearity, range, precision, accuracy, selectivity, robustness, LOD, and LOQ. The linear dynamic ranges were 2.5-150 and 2.5-500 microg/mL for chlordiazepoxide HCI and mebeverine HCI, respectively, and 0.25-200 and 0.25-150 microg/mL for carvedilol and hydrochlorothiazide, respectively. The validated HPLC methods were successfully applied to the analysis of their commercial tablet dosage forms, for which no interfering peaks were encountered from common pharmaceutical adjuvants. PMID:20922951

Haggag, Rim S; Shaalan, Rasha A; Belal, Tarek S

2010-01-01

210

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

PubMed

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 ?g 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. PMID:23624039

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

2013-07-01

211

Molecular association of betaine and betaine hydrochloride in aqueous solutions--a study by Raman spectroscopy.  

PubMed

Raman vibrational spectroscopy, at 298 K, has been used to study the hydration of betaine hydrochloride and betaine in the concentration range 0.5-2 M. The observed changes in the internal vibrations of the solutes, namely, in the C=O, COO- and C-H stretchings, and in the components of the O-H stretching band are consonant with anionic water-betaine and betaine hydrochloride dimeric species involving simultaneously hydrogen-bonding between two solute and water molecules. In both cases, betaine hydrochloride and 'zwitterionic' betaine behave like structure-makers promoting a larger association in the 'bulk' liquid water. PMID:11342265

Amorim da Costa, A; Leite, J E

2001-02-16

212

Compatibility and stability of aztreonam and vancomycin hydrochloride.  

PubMed

The physical compatibility and chemical stability of aztreonam and vancomycin hydrochloride when combined at clinically used high and low concentrations were studied. Admixtures consisting of aztreonam 4 mg/mL and vancomycin 1 mg/mL (as the hydrochloride salt) in 5% dextrose injection, aztreonam 4 mg/mL and vancomycin 1 mg/mL in 0.9% sodium chloride injection, aztreonam 40 mg/mL and vancomycin 10 mg/mL in 5% dextrose injection, and aztreonam 40 mg/mL and vancomycin 10 mg/mL in 0.9% sodium chloride injection were prepared in triplicate in polyvinyl chloride containers. Three containers of each type of admixture were stored at 4, 23, and 32 degrees C. Samples were removed immediately and at various time points over 31 days. Compatibility was assessed by visual examination, with a turbidimeter, and with a particle sizer-counter. Stability was determined by stability-indicating high-performance liquid chromatography (HPLC). All the admixtures initially appeared clear to the unaided eye after the disappearance of a transient white swirl in the high-concentration admixtures (aztreonam 40 mg/mL and vancomycin 10 mg/mL). However, the high-concentration admixtures immediately developed unacceptable levels of a microcrystalline precipitate when viewed with a high-intensity fiber-optic light source. Easily visible gross turbidity and precipitation formed after various periods but often within 24 hours. HPLC showed aztreonam 4 mg/mL and vancomycin 1 mg/mL in 5% dextrose injection to be a stable combination for 7 days at 32 degrees C, 14 days at 23 degrees C, and 31 days at 4 degrees C. In 0.9% sodium chloride injection, the drugs in the low-concentration admixtures were stable for 7 days at 32 degrees C and for 31 days at 4 and 23 degrees C. Stability of the combination in the high-concentration admixtures was maintained for 3 days at 23 and 32 degrees C and for 14 days at 4 degrees C. Aztreonam and vancomycin hydrochloride were considerably less compatible and stable in the high-concentration admixtures than in the low-concentration ones. PMID:8590240

Trissel, L A; Xu, Q A; Martinez, J F

1995-11-15

213

Single dose pharmacokinetics of fenspiride hydrochloride: phase I clinical trial.  

PubMed

The absolute bioavailability of fenspiride has been studied in twelve healthy volunteers. It was administered IV and orally in single doses of 80 mg fenspiride hydrochloride according to a randomised crossover pattern. Following IV administration, the plasma clearance of fenspiride was about 184 ml.min-1, and its apparent volume of distribution was moderately large (215 l). When given orally as a tablet, fenspiride exhibited fairly slow ab- sorption; the maximum plasma concentration (206 ng.ml-1) was achieved 6 h after administration. The absolute bioavailability was almost complete (90%). The tablet had slow release characteristics. The elimination half-life obtained from the plasma data was 14 to 16 h independent of the route of administration. PMID:7901024

Montes, B; Catalan, M; Roces, A; Jeanniot, J P; Honorato, J M

1993-01-01

214

The crystal habit of ciprofloxacin hydrochloride monohydrate crystal  

NASA Astrophysics Data System (ADS)

Crystals with two different habits (e.g. needle-like and plate-like) of ciprofloxacin hydrochloride monohydrate (CPFX) were prepared from aqueous solution by varied methods. These crystals were identified by various means such as scanning electron microscope (SEM), differential scanning calorimetry (DSC), thermogravimetry (TG), and X-ray powder diffraction (XRPD). According to the analysis of crystals by DSC, TG and XRPD, it concludes that CPFX crystals produced in cooling or dilution crystallization experiment should have the same crystal structure. Using the XRPD data, the unit cell parameters were calculated by software TREOR90. Systematic absence and statistics of reflexion indicate that CPFX crystals in this work have a high possibility of being the space group P2 1/c. The crystal habit transition has been observed in the salting-out crystallization when 0.2 M KCl solution works as precipitant.

Liu, Yong; Wang, Jingkang; Yin, Qiuxiang

2005-03-01

215

Determination of tetracycline hydrochloride by terahertz spectroscopy with PLSR model.  

PubMed

Antibiotic residues in agricultural and food products are of great concern to legislatures and consumers. Reliable techniques for rapid and sensitive detection of these residues are necessary to ensure food safety. In this study, tetracycline hydrochloride (TC-HCl) in powder and solution form was detected and quantified using terahertz (THz) spectroscopy. Partial least-squares regression (PLSR) was used to build calibration models. The results obtained in this study indicated that the PLSR model for powder samples was excellent and could be used for quality control. However, the PLSR model for solution samples was not robust and needed to be improved. Overall, THz spectroscopy combined with PLSR model had its potential for the rapid and non-destructive prediction of TC-HCl residue without sophisticated methods, although the accuracy was not high for solution samples which should be improved in future study. PMID:25306365

Qin, Jianyuan; Xie, Lijuan; Ying, Yibin

2015-03-01

216

Verapamil hydrochloride release characteristics from new copolymer zwitterionic matrix tablets.  

PubMed

The aim of this study was to synthesize stable copolymer (vinyl acetate-co-3-dimethyl[methacryloyloxyethyl] ammonium propane sulfinate) zwitterionic latex with different compositions for the first time by emulsifier-free emulsion copolymerization. Throughout the course of the study, a proposal was made for the explanation of the relationship between the "overshooting" phenomenon (a swelling kinetics with a maximum) and the specific self-association of the zwitterionic copolymers. The zwitterionic monomer unit mole fraction, pH, and ionic strength effects on this relationship, on the swelling kinetics of the zwitterionic copolymers, and on the sustained verapamil hydrochloride release from the model tablets were established by the study's authors. PMID:18649221

Kostova, Bistra; Kamenska, Elena; Ivanov, Ivo; Momekov, George; Rachev, Dimitar; Georgiev, George

2008-01-01

217

Crystal structure of BIS(Betaine) hydrochloride monohydrate  

NASA Astrophysics Data System (ADS)

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

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

1990-11-01

218

Crystal structure of bis(pyridine betaine) hydrochloride monohydrate  

NASA Astrophysics Data System (ADS)

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

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

1990-04-01

219

Glucosamine hydrochloride for the treatment of osteoarthritis symptoms  

PubMed Central

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

Fox, Beth Anne; Stephens, Mary M

2007-01-01

220

Glucosamine hydrochloride for the treatment of osteoarthritis symptoms.  

PubMed

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

Fox, Beth Anne; Stephens, Mary M

2007-01-01

221

Coated hydralazine hydrochloride beads for sustained release after oral administration.  

PubMed

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. PMID:23057650

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

2013-09-01

222

Peganine hydrochloride dihydrate an orally active antileishmanial agent.  

PubMed

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

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

2009-05-01

223

Club drugs: methylenedioxymethamphetamine, flunitrazepam, ketamine hydrochloride, and gamma-hydroxybutyrate.  

PubMed

The abuse of methylenedioxymethamphetamine (MDMA), flunitrazepam, ketamine hydrochloride, and gamma-hydroxybutyrate (GHB) is discussed. Club drugs are chemical substances used recreationally in social settings. Use is increasingly frequent among young people, especially during all-night dance parties. All four agents have been classified as controlled substances. MDMA ("ecstasy") is available as a tablet, a capsule, and a powder; formulations may contain many adulterants. MDMA increases the release of neurotransmitters. The desired effects are euphoria, a feeling of intimacy, altered visual perception, enhanced libido, and increased energy. The most common adverse effects are agitation, anxiety, tachycardia, and hypertension. More serious adverse effects include arrhythmias, hyperthermia, and rhabdomyolysis. Flunitrazepam is a potent benzodiazepine. At higher doses, the drug can cause lack of muscle control and loss of consciousness. Other adverse effects are hypotension, dizziness, confusion, and occasional aggression. Ketamine is a dissociative anesthetic used primarily in veterinary practice. It may be injected, swallowed, snorted, or smoked. Like phencyclidine, ketamine interacts with the N-methyl-D-aspartate channel. Analgesic effects occur at lower doses and amnestic effects at higher doses. Cardiovascular and respiratory toxicity may occur, as well as confusion, hostility, and delirium. GHB, a naturally occurring fatty acid derivative of gamma-aminobutyric acid, was introduced as a dietary supplement. Increasing doses progressively produce amnesia, drowsiness, dizziness, euphoria, seizures, coma, and death. Flunitrazepam, ketamine, and GHB have been used to facilitate sexual assault. Supportive care is indicated for most cases of club drug intoxication. The increasing abuse of MDMA, flunitrazepam, ketamine hydrochloride, and GHB, particularly by young people in social settings such as clubs, should put health care professionals on guard to recognize and manage serious reactions. PMID:12063892

Smith, Kelly M; Larive, Lisa L; Romanelli, Frank

2002-06-01

224

Formulation and evaluation of verapamil hydrochloride loaded solid lipid microparticles.  

PubMed

The present study aimed to produce verapamil hydrochloride-loaded solid lipid microparticles (SLM) by the w/o/w emulsion solvent evaporation technique, using diethyl ether as solvent phase, glyceryl monostearate as biodegradable polymer and Span 60 as surfactant. SLM of spherical shape were prepared by simple dilution of the emulsion with water. To increase the lipid load the process was conducted at 50 degrees C, and in order to reach sub-micron size, a high-shear homogenizer was used. The encapsulation efficiency of prepared SLM reached 74.29 +/- 0.76%. Particle size (98.55 +/- 1.42 microm), surface morphology (spherical) and drug loading efficiency (18.57 +/- 1.25% w/w) were investigated. And optimization of drug polymer ratio (3:1), nature and concentration of emulsion stabilizer in the external aqueous (0.1%), phase viscosity of external aqueous phase (0.5%), volume of external aqueous phase and stirring rate (1000 rpm) were detected. Analysis of microsphere content after processing showed that verapamil did not undergo any chemical modification within the micro-particles. The in-vitro release of verapamil from the microparticles was very low and an initial burst effect of 17% of the dose was observed. The slow release may help to avoid a high frequency of administration. The prepared solid lipid microparticles appear to have interesting perspectives as delivery systems for the oral administration of verapamil hydrochloride with improved half-life, improved bioavailability, and minimized local and systemic gastrointestinal disturbances of the drug. PMID:21391431

Pilaniya, U; Pilaniya, K; Chandrawanshi, H K; Gupta, N; Rajput, M S

2011-01-01

225

Potentiometric batch and flow injection analysis of betaine hydrochloride.  

PubMed

Novel PVC membrane electrodes for the determination of betaine ion based on the formation of betaine-tetraphenylborate (Be-TPB) and betaine-phosphotungstate (Be-PT) ion-exchangers as electroactive materials are described. The sensors show a fast, stable, near Nernstian response for 6.92 x 10(-6) to 7.94 x 10(-3) M and 1.0 x 10(-4) to 1.0 x 10(-2) M betaine hydrochloride (Be.Cl) in case of Be-TPB electrode applying batch and flow injection analysis (FIA), respectively, and 2.95 x 10(-5) to 2.26 x 10(-3) M and 3.16 x 10(-5) to 1.0 x 10(-2) M in case of Be-PT electrode for batch and FIA electrodes, respectively, at 25 degrees C over the pH range of 3.5-10 with a cationic slope of 60.2 and 59.1 mV decade(-1) and a fast potential response of < or =15 s. The lower detection limits are 7.94 x 10(-6) and 3.18 x 10(-5) M Be.Cl for Be-TPB and Be-PT electrodes, respectively. Selectivity coefficient data for some common inorganic cations, sugars, amino acids and the components other than betaine, of the mixed drug investigated show negligible interference. The electrodes have been applied to the direct potentiometric determination of betaine hydrochloride in water and in a pharmaceutical preparation under batch and FIA conditions. Potentiometric titrations of Be.Cl with NaTPB and PTA as titrants were monitored with the developed betaine electrodes as an end point indicator electrode. The determination of Be.Cl shows an average recovery of 100.8% with mean relative standard deviation of 0.61%. The effect of temperature on the electrodes was also studied. PMID:17822229

Badawy, Sayed S; Youssef, Ahmed F A; Mutair, Ali A

2007-01-01

226

77 FR 9944 - Determination That REQUIP XL (Ropinerole Hydrochloride) Extended-Release Tablets, 3 Milligrams...  

Federal Register 2010, 2011, 2012, 2013

...approved on June 13, 2008. REQUIP XL is indicated for the treatment of treatment of signs and symptoms of idiopathic Parkinson's disease. REQUIP XL (ropinerole hydrochloride) extended-release tablets, 3 mg, are currently listed in the...

2012-02-21

227

Doxapram hydrochloride aggravates adrenaline-induced arrhythmias accompanied by bidirectional ventricular tachycardia.  

PubMed

Objectives. Doxapram hydrochloride is a respiratory stimulant that has an inhibitory effect on myocardial IK1 potassium channels and is thought to increase membrane instability and excitability in myocardial cells. We examined the arrhythmogenic effects of doxapram hydrochloride in a rat model of halothane adrenaline-induced arrhythmia. Methods. Thirteen female Wistar rats (12-14 weeks old) were used in the study. Animals were anesthetized with inhalation of halothane to permit observation of the effects of doxapram hydrochloride on halothane adrenaline-induced arrhythmia. Time-dependent changes in ECG repolarization characteristics (QT, QTc, JTp, JT, and Tp-e intervals) were studied. Results. Doxapram hydrochloride itself did not induce arrhythmia but did induce bidirectional ventricular tachycardia after addition of adrenaline. Conclusion. Drug-induced impairment of intracellular Ca(2+) regulation caused BVT in the absence of genetic abnormalities in proteins in the sarcoplasmic reticulum. PMID:24527224

Oikawa, Shota; Nomura, Hiroko; Nishio, Miki; Nagata, Rina; Hata, Tadayoshi

2014-01-01

228

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

Federal Register 2010, 2011, 2012, 2013

...DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration [Docket No. FDA-2013-N-0320...hydrochloride) Injection and Two Other Drug Products Were Not Withdrawn From Sale for...Safety or Effectiveness AGENCY: Food and Drug Administration, HHS. ACTION:...

2013-03-25

229

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

Evaluation of monoclonal antibody (MAb) fragments (e.g. Fab?, Fab or engineered fragments) as cancer-targeting reagents for therapy with the ?-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 substituent on the hydrazone was chosen for study with 211At. That reagent was conjugated with 107-1A4 Fab?, then labeled (separately) with 125I and 211At. The radiolabeled Fab? conjugates were coinjected into nude mice bearing LNCaP human tumor xenografts, and biodistribution data was obtained at 1, 4 and 24 h pi. Tumor targeting was achieved with both 125I- and 211At-labeled Fab?, but the 211At-labeled Fab? reached a higher concentration (25.56 ± 11.20 vs. 11.97 ± 1.31 %ID/g). Surprisingly, while the 125I-labeled Fab? was cleared from kidney similar to earlier studies, the 211At-labeled Fab? was not (i.e. kidney conc. for 125I vs. 211At; 4h: 13.14 ± 2.03 ID/g vs. 42.28 ± 16.38 %D/g, 24h: 4.23 ± 1.57 ID/g vs. 39.52 ± 15.87 %ID/g). Since the Fab? conjugate is identical in both cases except for the radionuclide, it seems likely that the difference in tissue clearance seen is due to an effect that 211At has on either the hydrazone cleavage or on the retention of a metabolite. Results from other studies in our laboratory suggest that the latter case is most likely. The hydrazone linkers tested do not provide the tissue clearance sought for 211At, so additional hydrazones linkers will be evaluated. However, the results support the use of hydrazone linkers when Fab? conjugated with closo-decaborate(2-) reagents are radioiodinated. PMID:21513347

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

2011-01-01

230

A study of the reaction between antimony (III) chloride and organic amine hydrochlorides  

E-print Network

A STUDY OF THE REACTION BET'WEEN ANTIMONY PII) CHLORIDE AND ORGANIC AMINE HYDROCHLORIDES A Thesis by Donald Ernst Linder Submitted to the Graduate College of the Texas ASM University in partial fulfillment of the requirements for the degree... of MASTER OF SCIENCE January, 1964 Major Subject: Chemistry A STUDY OF THE REACTION BETWEEN ANTIMONY (III) CHLORIDE AND ORGANIC AMINE HYDROCHLORIDES A Thesis by Donald Ernst Linder Approved as to style and content by: r rf (- &t r (Head...

Linder, Donald Ernst

2012-06-07

231

Compatibility and Stability of Dexamethasone Sodium Phosphate and Ketamine Hydrochloride Subcutaneous Infusions in Polypropylene Syringes  

Microsoft Academic Search

The stability of ketamine hydrochloride injection and dexamethasone sodium phosphate injection, when mixed and stored in polypropylene syringes, was studied. Formulations containing ketamine hydrochloride (50 mg or 600 mg) and dexamethasone sodium phosphate (1 mg) in 0.9% sodium chloride injection (to 14 ml) were prepared and stored at 4°C, 23°C, and 37°C, under normal fluorescent light conditions, for 192 hours.

David G. Watson; Mei Lin; Andrew Morton; Colin G. Cable; Dorothy A. McArthur

2005-01-01

232

Effect of tetracycline hydrochloride treatment on the critical thermal maximum of common shiners  

SciTech Connect

The transfer of fish from field to laboratory facilities or their propagation in closed or restricted systems frequently results in bacterial infection and ultimately large-scale mortality. In attemps to alleviate this problem, we have added tetracycline hydrochloride to the water prophylactically (pretreating tanks before wild fish were added) and therapeutically (treating tanks after bacterial outbreaks were detected.) In the present study, we examined the effect of tetracyline hydrochloride on the critical thermal maximum (CTM) of the common shiner (Notropis cornutus).

Not Available

1980-01-01

233

Sustained transdermal release of diltiazem hydrochloride through electron beam irradiated different PVA hydrogel membranes  

NASA Astrophysics Data System (ADS)

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.

Bhunia, Tridib; Goswami, Luna; Chattopadhyay, Dipankar; Bandyopadhyay, Abhijit

2011-08-01

234

Molecular association of betaine and betaine hydrochloride in aqueous solutions – a study by Raman spectroscopy  

Microsoft Academic Search

Raman vibrational spectroscopy, at 298 K, has been used to study the hydration of betaine hydrochloride and betaine in the concentration range 0.5–2 M. The observed changes in the internal vibrations of the solutes, namely, in the C?O, COO? and C–H stretchings, and in the components of the O–H stretching band are consonant with anionic water–betaine and betaine hydrochloride dimeric

António Amorim da Costa; Joana E. S. Leite

2001-01-01

235

Spectrophotometric simultaneous determination of rabeprazole sodium and itopride hydrochloride in capsule dosage form.  

PubMed

A new simple, economical, rapid, precise and accurate method for simultaneous determination of rabeprazole sodium and itopride hydrochloride in capsule dosage form has been developed. The method is based on ratio spectra derivative spectrophotometry. The amplitudes in the first derivative of the corresponding ratio spectra at 231nm (minima) and 260nm were selected to determine rabeprazole sodium and itopride hydrochloride, respectively. The method was validated with respect to linearity, precision and accuracy. PMID:17604217

Sabnis, Shweta S; Dhavale, Nilesh D; Jadhav, Vijay Y; Gandhi, Santosh V

2008-03-01

236

Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation  

PubMed Central

Premature ejaculation (PE) is the most common sexual disorder. It affects 20%–30% of adult men; the aetiology of this condition has not yet been elucidated. The aim of this study is to evaluate the efficacy, safety, tolerability, undesirable effects and improved satisfaction with sexual intercourse with tramadol hydrochloride at different dosages for the treatment of PE. A total of 300 patients who presented with lifelong (primary) PE were included in this study. The study was performed for 28 weeks, in which placebo (starch tablet) was given for 4 weeks, and active ingredient (tramadol hydrochloride) was administered at different therapeutic dosages for 24 weeks. Patients were divided into three equal groups, each consisting of 100 patients. The first group (A) was given tramadol hydrochloride capsule 25 mg. The second group (B) was given tramadol hydrochloride capsule 50 mg. The third group (C) was given tramadol hydrochloride capsule 100 mg. All of the 300 participants included completed the study voluntarily. The age of the patients varied from 25 to 50 years. After the treatment period, the recorded data were collected for each group and analysed. The results showed a highly significant increase in the mean intravaginal ejaculatory latency time (IELT) in all groups compared to baseline data (P<0.0001). We concluded that using tramadol hydrochloride at different doses on demand for the treatment of PE is effective, safe and tolerable, with minimal undesirable effects, and approval for this indication should be sought. PMID:23103596

Eassa, Bayoumy I; El-Shazly, Mohamed A

2013-01-01

237

Nitroimidazolyl hydrazones are better amoebicides than their cyclized 1,3,4-oxadiazoline analogues: In vitro studies and Lipophilic efficiency analysis.  

PubMed

Two series of compounds with hydrazone derivatives (HZ1-HZl2, series 1) and oxadiazoline derivatives (OZ1-OZ12, series 2) of the 2-methyl-5-nitro-1H-imidazole scaffold were designed and synthesized. Physicochemical properties and Lipophilic efficiency (LipE) analysis predicted higher intrinsic quality of the acylhydrazone derivatives (series 1) than their corresponding oxadiazoline analogues (series 2). In vitro antiamoebic results supported the above findings and validated that the acylhydrazone derivatives (HZ1-HZl2) show better activity than the oxadiazoline derivatives (OZ1-OZ12). MTT assay, using HepG2 cell line, revealed noncytotoxic nature of the compounds. The most promising results were observed for compounds HZ5 (IC50 = 0.96 ?M) and HZ9 (IC50 = 0.81 ?M) both in silico and in vitro. Analysis of the Lipophilic efficiency (LipE) of the compounds provided new insight for the design of potent and selective amoebicides. PMID:23644202

Wani, Mohmmad Younus; Bhat, Abdul R; Azam, Amir; Athar, Fareeda

2013-06-01

238

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

PubMed

Literature data related to the Biopharmaceutics Classification System (BCS) are presented on verapamil hydrochloride, propranolol hydrochloride, and atenolol in the form of BCS-monographs. Data on the qualitative composition of immediate release (IR) tablets containing these active substances with a Marketing Authorization (MA) in the Netherlands (NL) are also provided; in view of these MA's the assumption was made that these tablets were bioequivalent to the innovator product. The development of a database with BCS-related data is announced by the International Pharmaceutical Federation (FIP). PMID:15236445

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

2004-08-01

239

A comparison of the efficacy of topical application of Lignocaine Hydrochloride 5% gel and Bupivacaine Hydrochloride 5% gel for extraction of teeth  

Microsoft Academic Search

Background  With the advancements in dentistry the treatments are done with high perfections and patient comfort. Noninvasive, methods\\u000a reduce fear and anxiety of the patient on phobia of syringes and injections. Topical anesthesia satisfies all the above criteria.\\u000a \\u000a \\u000a \\u000a \\u000a Aim and objective  Comparison of the efficacy of topical application of lignocaine hydrochloride 5% gel and bupivacaine hydrochloride 5% gel\\u000a for extraction of teeth.

N. V. V. Satya Bhushan; Ranganath N. Nayak

2010-01-01

240

Bioassay of o-anisidine hydrochloride for possible carcinogenicity.  

PubMed

A bioassay of o-anisidine hydrochloride for possible carcinogenicity was conducted by administering the test chemical in feed to Fischer 344 rats and B6C3F1 mice. Groups of 55 rats of each sex and 55 mice of each sex were administered o-anisidine hydrochloride at one of the following doses, either 5,000 or 10,000 ppm for rats and either 2,500 or 5,000 ppm for mice, for 103 weeks, then observed for 1 or 2 additional weeks. Controls consisted of groups of 55 untreated rats of each sex and 55 untreated mice of each sex. All surviving rats were killed at 103-107 weeks, and all surviving mice at 104 or 105 weeks. Mean body weights of the dosed male and female rats and mice were lower than those of the corresponding controls throughout the bioassay. Bloody exudates and stained fur in the urogenital area were noted in many dosed animals. Sufficient numbers of animals were at risk in the mice, but not in the rats, for development of late-appearing tumors; however, survival in the rats was 80% or more at week 52. Transitional-cell carcinomas or papillomas of the urinary bladder occurred at statistically significant incidences (P<0.001) in the low- and high-dose groups of rats (males: controls 0/51, low-dose 52/54, high-dose 52/52; females: controls 0/49, low-dose 1/51, high-dose 22/50); the incidences also had significant dose-related trends (P<0.001) in both species. These lesions were observed as early as week 36 in female rats, week 40 in male rats, and week 45 in male mice. Transitional-cell carcinomas of the pelvis of the kidney occurred with a significant dose-related trend (P=0.005) in the male rats, and the incidence in the high-dose group was significantly higher (P=0.006) than that in the control group (controls 0/53, low-dose 3/55, high-dose 7/53); all rats having this tumor also has a transitional-cell carcinoma of the urinary bladder. Only one animal in the control groups of rats or mice had any tumor of the urinary system (a transitional-cell papilloma of the pelvis of the kidney in a male mouse). Follicular-cell tumors of the thyroid (carcinomas, cystadenocarcinomas, adenomas, cystadenomas, and papillary cystadenomas) occurred at statistically significant incidences (Phydrochloride was carcinogenic for Fischer 344 rats and B6C3F1 mice, inducing transitional-cell carcinomas or papillomas of the bladder in both rats and mice and in both sexes of each species, transitional-cell carcinomas of the pelvis of the kidney in male rats, and follicular-cell tumors of the thyroid in male rats. PMID:12806402

1978-01-01

241

A Double-Blind, Placebo-Controlled Trial of Dexmethylphenidate Hydrochloride and d, l-threo-Methylphenidate Hydrochloride in Children With Attention-Deficit\\/Hyperactivity Disorder  

Microsoft Academic Search

Objective:To evaluate the efficacy and safety of dexmethylphenidate hydrochloride (d-MPH, Focalin™) 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).

SHARON WIGAL; JAMES M. SWANSON; DAVID FEIFEL; R BART SANGAL; JOSEPHINE ELIA; CHARLES D. CASAT; JEROME B. ZELDIS; C KEITH CONNERS

2004-01-01

242

Compatibility and stability of ondansetron hydrochloride with morphine sulfate and with hydromorphone hydrochloride in 0.9% sodium chloride injection at 4, 22, and 32 degrees C.  

PubMed

The physical compatibility and chemical stability of ondansetron hydrochloride 0.1 and 1 mg/mL with morphine sulfate 1 mg/mL and with hydromorphone hydrochloride 0.5 mg/mL in 0.9% sodium chloride injection were studied. Test solutions of the drugs in 0.9% sodium chloride injection were prepared in triplicate and stored at 4, 22, and 32 degrees C. Samples were removed immediately and at various time points over 31 days and stored at -70 degrees C until analyzed. Physical compatibility was assessed visually and by measuring turbidity with a color-correcting turbidimeter and particle content with a light-obscuration particle sizer and counter. Chemical stability was determined by measuring the concentration of each drug in duplicate with stability-indicating high-performance liquid chromatography. There were no visual or subvisual changes in turbidity or particle content in any of the test solutions at any of the time points. There was little or no loss of any of the drugs. When admixed in 0.9% sodium chloride injection, ondansetron hydrochloride 0.1 and 1 mg/mL plus morphine sulfate 1 mg/mL or hydromorphone hydrochloride 0.5 mg/mL were compatible and stable for at least 7 days at 32 degrees C and for at least 31 days at 4 and 22 degrees C. PMID:7527184

Trissel, L A; Xu, Q; Martinez, J F; Fox, J L

1994-09-01

243

Formulation and evaluation of thienorphine hydrochloride sublingual delivery system.  

PubMed

Thienorphine hydrochloride (ThH) is a highly insoluble and readily metabolized partial-opioid agonist. It is used for the treatment of pain and heroin addiction. This study aimed to formulate and evaluate sublingual delivery systems containing ThH. Dimethyl-?-cyclodextrin (DM-?-CD) can enhance the solubility and permeability of hydrophobic drugs. In this paper, ThH cyclodextrin inclusion complexes were prepared and administrated sublingually with the objective of improving the drug's aqueous solubility, in vitro permeation rate, and in vivo absorption rate. The formulation was prepared with DM-?-CD using the freeze-dried method and characterized using phase solubility, differential scanning calorimetry (DSC), X-ray and NMR analyses. The results of each test indicated the formation of dynamic inclusion complexes between ThH and DM-?-CD. The inclusion complexes also showed significant increases in in vitro aqueous solubility and mucosal permeability. According to the pharmacokinetic study of the complex in rats, the AUC and C(max) values of the sublingual delivery group were 40 and 46 times higher than those of the gastrointestinal group, whereas t(max) was shorter, which proved that in vivo absorption and metabolism had been improved. It can therefore be concluded that the inclusion technology and sublingual delivery system were suitable for ThH development. PMID:23207629

Liu, Fei; Zhao, Yumei; Sun, Jianxu; Gao, Yongliang; Zhang, Zhenqing

2012-01-01

244

Development and evaluation of microporous osmotic tablets of diltiazem hydrochloride  

PubMed Central

Microporous osmotic tablet of diltiazem hydrochloride was developed for colon targeting. These prepared microporous osmotic pump tablet did not require laser drilling to deliver the drug to the specific site of action. The tablets were prepared by wet granulation method. The prepared tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan coating process. The incorporation of sodium lauryl sulfate (SLS), a leachable pore-forming agent, could form in situ delivery pores while coming in contact with gastrointestinal medium. The effect of formulation variables was studied by changing the amounts of sodium alginate and NaCMC in the tablet core, osmogen, and that of pore-forming agent (SLS) used in the semipermeable coating. As the amount of hydrophilic polymers increased, drug release rate prolonged. It was found that drug release was increased as the concentration of osmogen and pore-former was increased. Fourier transform infrared spectroscopy and Differential scanning calorimetry results showed that there was no interaction between drug and polymers. Scanning electron microscopic studies showed the formation of pores after predetermined time of coming in contact with dissolution medium. The formation of pores was dependent on the amount of pore former used in the semipermeable membrane. in vitro results showed acid-resistant, timed release at an almost zero order up to 24 hours. The developed osmotic tablets could be effectively used for prolonged delivery of Diltiazem HCl. PMID:22837961

Bathool, Afifa; Gowda, D. V.; Khan, Mohammed S.; Ahmed, Ayaz; Vasudha, S. L.; Rohitash, K.

2012-01-01

245

Novel chewable sustained-release tablet containing verapamil hydrochloride.  

PubMed

The aim of this research is to produce a compactable self-sealing chewable tablet of verapamil hydrochloride. Tablets were prepared by compressing beads coated with multiple layers including drug, hydroxypropyl methylcellulose, polyethylene oxide, ethylcellulose, lactose, and sodium starch glycolate. Dissolution studies were carried out according to the USP XXII paddle method for 14 h. A new tablet formulation was evaluated in three different forms: 1) whole tablet, 2) crushed tablet using a commercial tablet crusher, and 3) tablet chewed in the mouth and then expelled into dissolution fluid. Sustained release from the new formulation was maintained and was similar in all three different treatments, and similar to drug release from intact commercially available Isoptin SR, but crushing or chewing destroyed the sustained release property of Isoptin SR (as expected). This new formulation can be administered either by swallowing the whole tablet or by first crushing or chewing the tablet. Controlled release properties of this new formulation do not change by chewing or crushing the tablet first. Such a tablet could be valuable for all patients including those who have difficulty swallowing, such as pediatrics and geriatrics. PMID:15202577

El-Gazayerly, Omaima N; Rakkanka, Vipaporn; Ayres, James W

2004-01-01

246

Swelling behavior of hyaluronic acid/polyallylamine hydrochloride multilayer films.  

PubMed

The reversible swelling behavior of multilayer films containing hyaluronic acid and polyallylamine hydrochloride was investigated using in situ ellipsometry, since many of the natural functions and applied uses of hyaluronic acid are related to the extraordinary ability of this biopolymer to swell, and to respond conformationally to the local solution environment. This swelling was observed to be substantial, and depended strongly on the film thickness, the pH conditions used to prepare the films, and the swelling solution pH and ionic strength. The swelling results were also rationalized in terms of the dissociation behavior of the polyelectrolytes in the multilayer assemblies, measured by the zeta potential, on colloidal particles. The films were found to swell by as much as 8 times their dry thickness, and the extent of film hydration was observed to depend on the thickness of the films in a nonlinear fashion. This was related to the internal structure of the films, which is dictated by the assembly pH conditions. In addition, the swelling solution pH and ionic strength influence the electrostatic environment in the films and, in turn, have a substantial effect on the overall swelling behavior. PMID:15877361

Burke, Susan E; Barrett, Christopher J

2005-01-01

247

Structure and vibrational spectra of pyridine betaine hydrochloride  

NASA Astrophysics Data System (ADS)

The crystal structure of pyridine betaine hydrochloride (PBET·HCl) was determined by X-ray diffraction to be monoclinic, space group {P2 1}/{c} with a = 8.533(2) Å, b = 9.548(2) Å, c = 10.781(2) Å, ? = 107.228(3)° and Z = 4. Betaine is protonated and the carboxyl group forms a hydrogen bond with the chloride ion: O·Cl - distance is 2.928(3) Å. The interaction of pyridine betaine (PBET) with HCl was examined by ab initio self-consistent field (SCF), second-order Møller-Plesset (MP2) and density functional theory (DFT) methods using the 6-31G(d,p) basis set. Two minima are located in the potential surface at the SCF level (PBET?H +·Cl - and PBET·H?Cl, with the latter being 1.2 kcal mol -1 lower in energy) and only one minimum (PBET·H?Cl) at the MP2 and DFT levels. The molecular parameters of PBET?H +·Cl -, computed by the SCF method, reproduce the corresponding experimental data. The computed vibrational frequencies of PBET?H +·Cl - resemble correctly the experimental vibrational spectrum in the solid state. The root-mean-square (r.m.s.) deviations between the experimental and calculated SCF frequencies are 65 cm -1 for all bands and 15 cm -1 without the ?Cl?H band. All measured IR bands were interpreted in terms of the calculated vibrational models.

Szafran, Miros?aw; Koput, Jacek; Baran, Jan; G?owiak, Tadeusz

1997-12-01

248

Calculation of the vibrational spectra of betaine hydrochloride  

NASA Astrophysics Data System (ADS)

The molecular geometries of betaine hydrochloride, BET·HCl, and free protonated betaine, BET·H +, were calculated with the 6-31G(d,p) basis set at the SCF, MP2 and DFT levels of theory. At the SCF level, the minimum energy corresponds to the ionic pair, B +Htctdot;A -, however, the equilibrium Otctdot;Cl distance is 0.14 Å shorter than the X-ray value. Inclusion of the correlation effects, both at the MP2 and DFT levels, predicts a minimum energy for the molecular complex, Btctdot;H-A, with the equilibrium Otctdot;Cl distance close to the experimental value. The frequencies and intensities of the vibrational bands of BET·HCl, BET·DCl and BET·H + were calculated at the SCF and DFT levels and compared with the solid IR spectra. All measured IR bands were interpreted in term of the calculated vibrational modes. The rms deviations between the experimental and calculated SCF frequencies were 21 and 29 cm -1 for BET·HCl and BET·DCl, respectively. The computed band intensities agree qualitatively with the experimental data. The coupling of the CO stretching and OH bending modes are discussed. The summation bands are probably enhanced in intensity by Fermi resonance with the fundamentals responsible for the main ?(OH) (?(OD) absorption region.

Szafran, Miroslaw; Koput, Jacek

1997-02-01

249

Stability of revex, nalmefene hydrochloride injection, in injectable solutions.  

PubMed

The short-term stability of Revex, nalmefene hydrochloride injection, was determined in a number of diluents commonly employed for intravenous use. An HPLC method was used to follow the potency of the diluted solutions, and was fully validated for its intended concentration range prior to its use. Dilutions of Revex were prepared separately in 0.9% sodium chloride injection, 0.45% sodium chloride injection, 5% dextrose injection, 5% dextrose and 0.45% sodium chloride injection, lactated Ringer's injection, 5% dextrose and lactated Ringer's injection and 5% sodium hydrogencarbonate injection. Each admixture was stored at 4 degrees C, room temperature (21 degrees C) and 40 degrees C, with samples being tested after storage at each temperature for 0, 24, 48 and 72 h. Defining stability as the retention of at least 95% of the initial drug concentration at the end of the storage period, it was concluded that the diluted solutions of Revex were uniformly stable for up to 72 h in all of the injectable solutions maintained at either 4, 21 or 40 degrees C. PMID:8933423

Murthy, S S; Brittain, H G

1996-11-01

250

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

PubMed

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, ?-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 those muscles of the round (P < 0.05). Beta-agonists increased saleable yield, but these effects were not constant between all major primals. The cutout value gained by packers as a result of ?-agonist use may be influenced more by reduced fatness and increased absolute weight if musculature is primarily increased in the lower priced cuts of the carcass. PMID:24243909

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

251

Effects of ractopamine hydrochloride and zilpaterol hydrochloride supplementation on longissimus muscle shear force and sensory attributes of beef steers.  

PubMed

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 ?-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 difference in flavor profile or juiciness among treatments (P > 0.05). Results from this study indicated ?-agonists negatively affected beef tenderness and these effects may be more noticeable in steers supplemented with ZH and higher doses of RH. PMID:24166996

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

252

Ranitidine Hydrochloride-loaded Ethyl Cellulose and Eudragit RS 100 Buoyant Microspheres: Effect of pH Modifiers.  

PubMed

A floating type of dosage form of ranitidine hydrochloride in the form of microspheres capable of floating on simulated gastric fluid was prepared by solvent evaporation technique. Microspheres prepared with ethyl cellulose, Eudragit(®) RS100 alone or in combination were evaluated for percent yield, drug entrapment, percent buoyancy and drug release and the results demonstrated satisfactory performance. Microspheres exhibited ranitidine hydrochloride release influenced by changing ranitidine hydrochloride-polymer and ranitidine hydrochloride-polymer-polymer ratio. Incorporation of a pH modifier has been the usual strategy employed to enhance the dissolution rate of weakly basic drug from floating microspheres. Further citric acid, fumaric acid, tartaric acid were employed as pH modifiers. Microspheres prepared with ethyl cellulose, Eudragit(®) RS100 and their combination that showed highest release were utilized to study the effect of pH modifiers on ranitidine hydrochloride release from microspheres which is mainly affected due to modulation of microenvironmental pH. In vitro release of ranitidine hydrochloride from microspheres into simulated gastric fluid at 37° showed no significant burst effect. However the amount of release increased with time and significantly enhanced by pH modifiers. 15% w/w concentration of fumaric acid provide significant drug release from ranitidine hydrochloride microspheres prepared with ranitidine hydrochloride:ethyl cellulose (1:3), ranitidine hydrochloride:Eudragit(®) RS100 (1:2) and ranitidine hydrochloride:ethyl cellulose:Eudragit(®) RS100 (1:2:1) whereas citric acid, tartaric acid showed significant cumulative release at 20% w/w. In all this study suggest that ethyl celluose, Eudragit(®) RS100 alone or in combination with added pH modifiers can be useful in floating microspheres which can be proved beneficial to enhance the bioavailability of ranitidine hydrochloride. PMID:23112396

Kotagale, N R; Parkhe, A P; Jumde, A B; Khandelwal, H M; Umekar, M J

2011-11-01

253

Ranitidine Hydrochloride-loaded Ethyl Cellulose and Eudragit RS 100 Buoyant Microspheres: Effect of pH Modifiers  

PubMed Central

A floating type of dosage form of ranitidine hydrochloride in the form of microspheres capable of floating on simulated gastric fluid was prepared by solvent evaporation technique. Microspheres prepared with ethyl cellulose, Eudragit® RS100 alone or in combination were evaluated for percent yield, drug entrapment, percent buoyancy and drug release and the results demonstrated satisfactory performance. Microspheres exhibited ranitidine hydrochloride release influenced by changing ranitidine hydrochloride-polymer and ranitidine hydrochloride-polymer-polymer ratio. Incorporation of a pH modifier has been the usual strategy employed to enhance the dissolution rate of weakly basic drug from floating microspheres. Further citric acid, fumaric acid, tartaric acid were employed as pH modifiers. Microspheres prepared with ethyl cellulose, Eudragit® RS100 and their combination that showed highest release were utilized to study the effect of pH modifiers on ranitidine hydrochloride release from microspheres which is mainly affected due to modulation of microenvironmental pH. In vitro release of ranitidine hydrochloride from microspheres into simulated gastric fluid at 37° showed no significant burst effect. However the amount of release increased with time and significantly enhanced by pH modifiers. 15% w/w concentration of fumaric acid provide significant drug release from ranitidine hydrochloride microspheres prepared with ranitidine hydrochloride:ethyl cellulose (1:3), ranitidine hydrochloride:Eudragit® RS100 (1:2) and ranitidine hydrochloride:ethyl cellulose:Eudragit® RS100 (1:2:1) whereas citric acid, tartaric acid showed significant cumulative release at 20% w/w. In all this study suggest that ethyl celluose, Eudragit® RS100 alone or in combination with added pH modifiers can be useful in floating microspheres which can be proved beneficial to enhance the bioavailability of ranitidine hydrochloride. PMID:23112396

Kotagale, N. R.; Parkhe, A. P.; Jumde, A. B.; Khandelwal, H. M.; Umekar, M. J.

2011-01-01

254

Investigational use of metomidate hydrochloride as a shipping additive for two ornamental fishes.  

PubMed

During shipping, ornamental fish can be stressed due to handling, high stocking densities, and deteriorating water quality. Adding sedatives, such as metomidate hydrochloride, to shipping water may improve fish survival rates and the percentage of fish in saleable condition. Although the effects of metomidate hydrochloride on the stress response in fish have been studied, its application as a shipping additive has not been well investigated, particularly for tropical ornamental fishes shipped under industry conditions. Convict cichlids Cichlasoma nigrofasciatum and black mollies Poecilia sphenops were evaluated for 7 d after a 24-h period of exposure (including ground and air transport) to one of four metomidate hydrochloride concentrations: 0.0, 0.2, 0.5, and 1.0 mg/L. Immediate posttransport and cumulative mortality data, as well as 12-h and 7-d posttransport appearance and behavior scores, were generated. In convict cichlids, the highest dose of metomidate hydrochloride (1.0 mg/L) reduced mortality (0% compared with cumulative means of 5.5-9.2% in other groups) and increased the percentage of saleable fish (91.7% were immediately saleable compared with 12.5-50% in other groups). No effect was detected in black mollies at any concentration tested. Metomidate hydrochloride showed promise as a shipping additive for convict cichlids, but further studies are warranted to evaluate species-specific responses in other ornamental species. PMID:20043397

Kilgore, Kathy Heym; Hill, Jeffrey E; Powell, James F F; Watson, Craig A; Yanong, Roy P E

2009-09-01

255

Fasudil hydrochloride could promote axonal growth through inhibiting the activity of ROCK  

PubMed Central

Objective: This study aims to investigate the neuroprotective effect of Rho kinase inhibitor fasudil hydrochloride in ischemia/reperfusion injury N2a neuron. Methods: In vitro, N2a cells induced by ischemia and ischemia-reperfusion were treated with fasudil hydrochloride, cell damage was analyzed by MTT. On the other hand, the cytoskeleton of N2a cells was scanned through immunofluorescence techniques by Confocal Laser Microscopy which stained with FITC-phalloidin for F-actin visualization. Results: The activation of ROCK-II increased significantly in the damaged local during the following phase of ischemia/reperfusion injury. Ischemia induced a striking reorganization of actin cytoskeleton with a weakening of fluorescent intensity of the peripheral filament actin bands and formation of the long and thick stress fibers, but pretreatment of Fasudil hydrochloride could reversed the changes of ultra-structure on the cellular surface. MTT assay showed that Fasudil hydrochloride could prolong the survival time of the N2a cells after mimic ischemia-reperfusion for 24 h. Conclusions: The activation of ROCK-II has an exceptional hoist after ischemia/reperfusion injury, it is likely to induce the collapse of the growth cone through MLC-P. Fasudil hydrochloride could promote axonal growth on inhibitory of ROCK activity. PMID:25337198

Xiao, Wei-Dong; Yu, Ai-Xi; Liu, Dan-Li

2014-01-01

256

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

PubMed

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

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

2013-03-01

257

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

PubMed Central

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

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

2013-01-01

258

THE USE OF HYDROGEN PEROXIDE TO ENHANCE THE EFFICACY OF DOXORUBICIN HYDROCHLORIDE IN A MURINE BLADDER TUMOR CELL LINE  

Microsoft Academic Search

Purpose: We determined whether the cytotoxicity of doxorubicin hydrochloride would be enhanced by adding hydrogen peroxide as a source of oxygen free radicals. Materials and Methods: Mouse bladder tumor cells (MBT-2) were grown in RPMI 1640 medium and treated with various concentrations of doxorubicin hydrochloride for 2 hours. Protein content was assayed as a measure of cell growth. A similar

KEVIN R. LOUGHLIN; KELLEDY MANSON; DINO CRAGNALE; LISE WILSON; ROBERT A. BALL; KENNETH R. BRIDGES

2001-01-01

259

Hypercrosslinked poly(styrene-co-divinylbenzene) resin as a specific polymeric adsorbent for purification of berberine hydrochloride from aqueous solutions.  

PubMed

A hypercrosslinked poly(styrene-co-divinylbenzene) resin (TEPA) was synthesized and characterized as a specific polymeric adsorbent for concentrating berberine hydrochloride from aqueous solutions. Three organic molecules of different sizes (2-naphthol, berberine hydrochloride, and Congo red) were used as target molecules to elucidate the molecular sieving effect of the TEPA adsorbent. Because the TEPA adsorbent has a pore structure consisting mainly of micropores and mesopores, the adsorption of 2-naphthol from aqueous solutions is very efficient due to the micropore filling effect. The adsorption of berberine hydrochloride mostly takes place in the mesopores as well as macropores, while the adsorption of Congo red mainly occurs in the macropores. The smaller adsorbate molecule (2-naphthol) reaches the adsorption equilibrium much faster than the larger ones (berberine hydrochloride and Congo red). An adsorption breakthrough experiment with an aqueous solution containing 2-naphthol and berberine hydrochloride demonstrated that the TEPA adsorbent could effectively remove 2-naphthol from berberine hydrochloride at 0-107 BV (bed volume, 1 BV=10 ml), and the berberine hydrochloride concentration was increased from 66.7% to 99.4%, suggesting that this polymeric adsorbent is promising for purifying berberine hydrochloride and similar alkaloids from herbal plant extracts. PMID:23582901

Li, Yin; Cao, Ruofan; Wu, Xiaofei; Huang, Jianhan; Deng, Shuguang; Lu, Xiuyang

2013-06-15

260

Kinetics of Actin Unfolding Induced by Guanidine Hydrochloride Konstantin K. Turoverov, Vladislav V. Verkhusha,,| Mikhail M. Shavlovsky, Alexander G. Biktashev,  

E-print Network

Kinetics of Actin Unfolding Induced by Guanidine Hydrochloride Konstantin K. Turoverov, Vladislav VVed October 10, 2001 ABSTRACT: The kinetics of actin unfolding induced by guanidine hydrochloride has been studied. On the basis of obtained experimental data a new kinetic pathway of actin unfolding was proposed

Verkhusha, Vladislav V.

261

Development and in vitro evaluation of chitosan-based transdermal drug delivery systems for the controlled delivery of propranolol hydrochloride  

Microsoft Academic Search

Membrane permeation-controlled transdermal drug delivery systems were prepared using the natural polymer, chitosan. An adhesive sealing technique was used to construct the devices. Propranolol hydrochloride was selected as the model drug for the present study. Chitosan membranes with different permeability to propranolol hydrochloride obtained by controlled cross-linking with glutaraldehyde were used to regulate the drug release in the devices. Chitosan

D. Thacharodi; K. Panduranga Rao

1995-01-01

262

Photoacoustic imaging to detect rat brain activation after cocaine hydrochloride injection  

NASA Astrophysics Data System (ADS)

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.

Jo, Janggun; Yang, Xinmai

2011-03-01

263

Adduction of amiloride hydrochloride in urea through a modified technique for the dissolution enhancement.  

PubMed

Amiloride hydrochloride is a potassium-sparing diuretic since it favors sodium excretion and potassium reabsorption. In the present study, urea, a well-known adductor for linear compounds was successfully employed for inclusion of amiloride hydrochloride-a substituted cyclic organic compound through a modified technique. Formation of urea inclusion compounds was confirmed by FTIR, DSC and XRD. The minimum amount of rapidly adductible endocyte (RAE) required for adduction of amiloride hydrochloride in urea was estimated by a modified Zimmerschied calorimetric method. Urea-AH-RAE inclusion compounds containing varying proportions of guests were prepared and their thermal behavior studied by DSC. The inclusion compounds were also found to exhibit high content uniformity and markedly improved dissolution profile as demonstrated by increased dissolution efficiency. Studies reveal the possibility of exploiting co-inclusion of the drug in urea host lattice for the dissolution enhancement. PMID:17688282

Thakral, Seema; Madan, A K

2008-03-01

264

Health and environmental effects profile for 2,4-dimethylaniline and 2,4-dimethylaniline hydrochloride  

SciTech Connect

The Health and Environmental Effects Profile for 2-4-Dimethylaniline and 2,4-Dimethylaniline Hydrochloride was prepared to support listings of hazardous constituents of a wide range of waste streams under Section 3001 of the Resource Conservation and Recovery Act (RCRA) and to provide health-related limits for emergency actions under Section 101 of the Comprehensive Environmental Response, Compensation and Liability Act (CERCLA). Both published literature and information obtained from Agency program office files were evaluated as they pertained to potential human-health, aquatic-life and environmental effects of hazardous-waste constituents. The human carcinogen potency factors (q1*) for 2-4-dimethylaniline and 2,4-dimethylaniline hydrochloride are 0.75 and 0.58/(mg/kg/day) respectively, for oral exposure. The Reportable Quantity (RQ) value for 2-4-dimethylaniline and 2,4-dimethylaniline Hydrochloride is 1000.

Not Available

1987-01-01

265

Health and environmental effects profile for 4-chloro-2-methylaniline and 4-chloro-2-methylaniline hydrochloride  

SciTech Connect

The Health and Environmental Effects Profile for 4-chloro-2-methylaniline and 4-chloro-2-methylaniline hydrochloride was prepared to support listings of hazardous constituents of a wide range of waste streams under Section 3001 of the Resource Conservation and Recovery Act (RCRA) and to provide health-related limits for emergency actions under Section 101 of the Comprehensive Environmental Response, Compensation and Liability Act (CERCLA). Both published literature and information obtained from Agency program office files were evaluated as they pertained to potential human-health, aquatic-life and environmental effects of hazardous-waste constituents. The human carcinogen potency factors (q1*) for 4-chloro-2-methylaniline and 4-chloro-2-methylaniline hydrochloride are 0.58 and 0.46/(mg/kg/day), respectively, for oral exposure. The Reportable Quantity (RQ) value for 4-chloro-2-methylaniline and 4-chloro-2-methylaniline hydrochloride is 5000.

Not Available

1986-12-01

266

Stability of cimetidine hydrochloride in admixtures after microwave thawing.  

PubMed

The stability of cimetidine hydrochloride in admixtures subjected to freezing and subsequent microwave thawing was studied. Admixtures containing cimetidine 300 mg were prepared using 18 50-ml bags of 5% dextrose injection and 18 100-ml bags of 0.9% sodium chloride injection. A sample for analysis of pH and drug concentration was withdrawn from each bag, and all admixtures were frozen for 28 days. Nine admixtures of each solution were thawed at room temperature and the other nine in a microwave oven until a final solution temperature of 24 +/- 2 degrees C was reached. An additional five cimetidine admixtures in 0.9% sodium chloride injection were prepared and irradiated in the microwave oven until boiling occurred for five seconds. Samples of all admixture solutions were withdrawn within 30 minutes of thawing and again at 24 +/- 2 hours after thawing to determine pH and cimetidine concentration. Concentrations were measured by high-performance liquid chromatography. Admixtures pH after thawing did not vary substantially from baseline values. A significant difference in cimetidine concentration for each solution was observed between samples drawn at 0 and 24 hours after thawing; drug concentrations in 5% dextrose increased by 5.9% while those in 0.9% sodium chloride decreased by 1.5%. Thawing method had no significant effect on drug concentration in either admixture solution. In the solutions and drug concentrations tested, microwave thawing did not affect cimetidine stability. Increases in cimetidine concentrations in 5% dextrose solution may have been attributable to greater insensible water losses produced by heating of the small 50-ml bags. PMID:6869383

Elliott, G T; McKenzie, M W; Curry, S H; Pieper, J A; Quinn, S L

1983-06-01

267

Neuroendocrine effects of raloxifene hydrochloride in postmenopausal women.  

PubMed

Raloxifene is a selective estrogen modulator able to exert an estrogen-like action on some target tissues and a specific antiestrogenic action on the uterus and breast. In ovariectomized rats, it has been shown to stimulate the beta-endorphin and allopregnanolone concentrations of the anterior and neurointermediate pituitary lobes, the hypothalamus and the hippocampus. The present study aimed to evaluate, in 12 healthy postmenopausal women, the effect of 60 mg/day raloxifene hydrochloride administration for 6 months on plasma beta-endorphin and allopregnanolone levels, and on the dynamic changes of both beta-endorphin and allopregnanolone secretion after the administration of: (1) clonidine, an alpha 2-presynaptic adrenergic agonist; (2) naloxone, an opioid receptor antagonist; and (3) fluoxetine, a serotonin selective reuptake inhibitor. The administration of raloxifene significantly increased both circulating beta-endorphin and allopregnanolone concentrations, at both the third and sixth months of treatment (p < 0.01). Clonidine, fluoxetine and naloxone administration before therapy was not able to stimulate the release of beta-endorphin, but the response was completely restored after raloxifene administration. Before therapy, clonidine and naloxone tests were accompanied by a significant rise in allopregnanolone secretion; the same changes were observed after raloxifene administration, but with significantly higher allopregnanolone concentrations at each time considered. While the fluoxetine test before therapy failed to increase the release of allopregnanolone, the same test after 6 months of raloxifene administration was characterized by a significant release of allopregnanolone at 60 and 90 minutes. The present data indicate that raloxifene has an estrogen-like effect on neuroendocrine pathways in postmenopausal women. PMID:11727358

Florio, P; Quirici, B; Casarosa, E; Lombardi, I; Luisi, M; Genazzani, A D; Petraglia, F; Genazzani, A R

2001-10-01

268

Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.  

PubMed

The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF(4), MF(5), and MF(9) were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C (max) of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF(4), MF(5), and MF(9), respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h. PMID:22015966

Nanjwade, Basavaraj K; Deshmukh, Rucha V; Gaikwad, Kishori R; Parikh, Kemy A; Manvi, F V

2012-06-01

269

Preclinical safety studies of the combination moexipril hydrochloride/hydrochlorothiazide.  

PubMed

The general pharmacological properties of a combination of the angiotensin converting enzyme (ACE) inhibitor moexipril hydrochloride (CAS 82586-52-5) and the thiazide diuretic hydrochlorothiazide (CAS 58-93-5, HCTZ), ratio 7.5 + 12.5, were studied in generally accepted models in vitro and in vivo. In vitro, the combination showed neither agonistic nor antagonistic activities on the isolated guinea pig trachea in concentrations up to 2 x 10(-4) g/ml. In mice, there was no effect on intestinal motility or the thiopental-induced sleeping time up to 1000 mg/kg. The only activity observed in mice was an inhibition of spontaneous motility after oral dosing with 300 and 1000 mg/kg, respectively. Both HCTZ (1-10 mg/kg) alone and the combination moexipril/HCTZ (1.6 or 4.8 mg/kg) produced dose-related increases in diuresis and electrolyte excretion in rats, however, without any potentiating effects for the drug combination. On the cardiovascular system of anaesthetised dogs, the effects observed were as expected, e.g. dose-related decrease in blood pressure. Repeated dose toxicity studies in rats and dogs revealed the kidney as target organ. This effect, based on highly exaggerated pharmacological activity, is well-known for other ACE inhibitors. No potential for teratogenic effects could be observed for the drug combination. In summary, the preclinical data indicate that the combination of moexipril and HCTZ (ratio 7.5 + 12.5) represents a safe drug without relevant side effects or gross toxicity. PMID:9608878

Gietl, R; Friehe, H; Ney, P

1998-04-01

270

Pharmacokinetic and pharmacodynamic evaluation of floating microspheres of metformin hydrochloride.  

PubMed

Metformin hydrochloride (MH), a biguanide antidiabetic, is the drug of choice in obese patients. It is well absorbed from the upper part of gastrointestinal tract and has oral bioavailability of 50% to 60%. The objective of this study was to formulate MH into floating microspheres in order to increase its residence time at the site of absorption and thus improve its bioavailability; and to extend the duration of action along with possibilities of dose reduction. Microspheres were prepared by emulsion solvent evaporation method and evaluated for particle size, entrapment efficiency, buoyancy, and in vitro release; and further characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy, and differential scanning calorimetry. The pharmacokinetic and pharmacodynamic evaluation of selected formulation was carried out in male Wistar diabetic rats. The data was statistically analyzed by unpaired t-test. A 3.5-fold increase in relative bioavailability was observed. The prolongation of half-life (t(1/2)) from 4.5 ± 2.41 h to 14.12 ± 4.81 h indicated extended duration of action. Oral glucose tolerance test (OGTT) was analyzed by one-way analysis of variance followed by Dunnet multiple comparison test, a significant decrease (p < 0.05) in the blood glucose levels was observed when formulations were compared with control rats. Hence, MH floating microspheres were tested at 50 mg/kg and 100 mg/kg body weight, OGTT data showed nonsignificant difference (p >0.05). In conclusion, an effective oral antidiabetics treatment can be achieved by formulating MH into floating microspheres which results in increase in bioavailability along with extended duration of action resulting in possible reduction in dose. PMID:22372865

Pandit, Vinay; Pai, Roopa S; Yadav, Vivek; Devi, Kshama; Surekha, B B; Inamdar, Mohd N; Suresh, Sarasija

2013-01-01

271

A validated high performance thin layer chromatography method for determination of yohimbine hydrochloride in pharmaceutical preparations  

PubMed Central

Background: Yohimbine is an indole alkaloid used as a promising therapy for erectile dysfunction. A number of methods were reported for the analysis of yohimbine in the bark or in pharmaceutical preparations. Materials and Method: In the present work, a simple and sensitive high performance thin layer chromatographic method is developed for determination of yohimbine (occurring as yohimbine hydrochloride) in pharmaceutical preparations and validated according to International Conference of Harmonization (ICH) guidelines. The method employed thin layer chromatography aluminum sheets precoated with silica gel as the stationary phase and the mobile phase consisted of chloroform:methanol:ammonia (97:3:0.2), which gave compact bands of yohimbine hydrochloride. Results: Linear regression data for the calibration curves of standard yohimbine hydrochloride showed a good linear relationship over a concentration range of 80–1000 ng/spot with respect to the area and correlation coefficient (R2) was 0.9965. The method was evaluated regarding accuracy, precision, selectivity, and robustness. Limits of detection and quantitation were recorded as 5 and 40 ng/spot, respectively. The proposed method efficiently separated yohimbine hydrochloride from other components even in complex mixture containing powdered plants. The amount of yohimbine hydrochloride ranged from 2.3 to 5.2 mg/tablet or capsule in preparations containing the pure alkaloid, while it varied from zero (0) to 1.5–1.8 mg/capsule in dietary supplements containing powdered yohimbe bark. Conclusion: We concluded that this method employing high performance thin layer chromatography (HPTLC) in quantitative determination of yohimbine hydrochloride in pharmaceutical preparations is efficient, simple, accurate, and validated. PMID:23661986

Badr, Jihan M.

2013-01-01

272

Vibrational spectra of ketamine hydrochloride and 3, 4-methylenedioxymethamphetamine in terahertz range  

NASA Astrophysics Data System (ADS)

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.

Wang, Guangqin; Shen, Jingling; Jia, Yan

2007-07-01

273

Practical Synthesis of 1-(7-Fluoro-naphthalen-1-yl)piperazine Hydrochloride  

Microsoft Academic Search

A practical and scalable preparation of 1-(7-fluoronaphthalen-1-yl)-piperazine hydrochloride (1) is reported. The original route for the synthesis of this compound involved the use of 1-amino-7-fluoronaphthalene and bis(2-chloroethyl)amine hydrochloride, two highly toxic compounds. A new protocol has been developed that employs a palladium-catalyzed Buchwald–Hartwig cross-coupling reaction between 1-Boc-piperazine and 1-bromo-7-fluoronaphthalene followed by piperazine deprotection with HCl gas. In addition, an efficient

Javier Magano; Anne Akin; Michael H. Chen; Kendra Giza; Jennifer Moon; James Saenz

2008-01-01

274

The influence of relative humidity and temperature on stability of moexipril hydrochloride in solid phase.  

PubMed

Kinetic and thermodynamic parameters of the decomposition of moexipril hydrochloride in solid phase in the absence and presence of humidity were calculated. The evaluation of stability of moexipril hydrochloride was followed by the HPLC method. The applied method was validated (evaluation of the following parameters: selectivity, linearity, precision, limit of detection (LOD), limit of quantification (LOQ) and repeatability). The effect of humidity on the stability of MHCl in solid phase at 363 K was described by the equation: In ki = ax + b = (0.0676 +/- 0.016) . RH% - (15.53+/-0.78). Identification of degradation products of MHCl were carried out by the HPLC-MS method. PMID:15493289

Stanisz, Beata

2004-01-01

275

Comparative effects of zilpaterol hydrochloride and ractopamine hydrochloride on live performance and carcass characteristics of calf-fed Holstein steers.  

PubMed

Holstein steers (n = 2,275) were assigned to 1 of 3 treatments: 1) a control diet containing no ?-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 ?-agonist (24.8%, 72.0%), respectively. Feeding either ?-agonist to calf-fed Holstein steers increased live performance through increased BW, BW gain, and ADG. Furthermore, supplementing calf-fed Holstein steers with ZH provides greater improvements in HCW, LM area, and yield grade components, with a slight decrease in quality grade when compared to calf-fed Holstein steers supplemented with RH. PMID:25006068

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

276

Monosaccharide optical sensor based on ruthenium(II)-bis(bipyridine) of 4-nitrophenyl-di-2-pyridyl ketone hydrazone (dpknph), [Ru(bipy) 2(dpknph)]Cl 2  

NASA Astrophysics Data System (ADS)

Optical measurements on [Ru(bipy) 2(dpknph)]Cl 2, where bipy is 2,2'-bipyridine and dpknph is di-2-pyridyl ketone p-nitrophenyl hydrazone, in polar dimethyl sulfoxide (DMSO) in the presence and absence of NaBH 4/NaBF 4 confirmed the reversible interconversion between the high- and low-energy electronic states of [Ru(bipy) 2(dpknph)]Cl 2 at 576 and 412 nm, respectively. The addition of an external stimulus improves the optosensing behavior of [Ru(bipy) 2(dpknph)]Cl 2 because of the disturbance of the equilibrium distribution of the electronic states. Optical measurements on [Ru(bipy) 2(dpknph)]Cl 2 in the presence and absence of NaBH 4 reveal high sensitivity of the electronic states of [Ru(bipy) 2(dpknph)]Cl 2 to slight variations in the concentration of monosaccharide, glucose and fructose in this study. Monosaccharide in concentration as low as 1×10 -9 M can be detected and determined using [Ru(bipy) 2(dpknph)]Cl 2 in DMSO in the presence and absence of NaBH 4. In the presence of NaBH 4, the system shows higher sensitivity toward glucose.

Bakir, Mohammed; Gyles, Colin

2005-10-01

277

[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

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

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

2011-01-01

278

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)

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

Borisova, T.; Krisanova, N.

279

Novel potent imidazo[1,2-a]pyridine-N-Glycinyl-hydrazone inhibitors of TNF-? production: in vitro and in vivo studies.  

PubMed

In this work, we describe the design, synthesis and pharmacological evaluation of novel imidazo[1,2-a]pyridine-N-glycinyl-hydrazone derivatives (1a-k) intended for use as inhibitors of tumor necrosis factor alpha (TNF-?) production. The compounds were designed based on the orally active anti-inflammatory prototype LASSBio-1504 (2), which decreases the levels of the pro-inflammatory cytokine TNF-? in vitro and in vivo. The in vitro pharmacological evaluation of the imidazo[1,2-a]pyridine compounds (1) showed that substitution of the N-phenylpyrazole core present in prototype 2 by a bioisosteric imidazo[1,2-a]pyridine scaffold generated anti-TNF-? compounds that were more potent than the previously described N-phenylpyrazole derivative 2 and as potent as SB-203580, a p38 MAPK inhibitor. The most active derivative (E)-2-(2-tert-butylimidazo[1,2-a]pyridin-3-ylamino)-N'-(4-chlorobenzylidene) acetohydrazide, or LASSBio-1749 (1i) was orally active as an anti-inflammatory agent in a subcutaneous air pouch model, reducing expressively the levels in vivo of TNF-? and other pro-inflammatory cytokines at all of the tested doses. PMID:24632827

Lacerda, Renata B; Sales, Natália M; da Silva, Leandro L; Tesch, Roberta; Miranda, Ana Luisa P; Barreiro, Eliezer J; Fernandes, Patricia D; Fraga, Carlos A M

2014-01-01

280

Novel Potent Imidazo[1,2-a]pyridine-N-Glycinyl-Hydrazone Inhibitors of TNF-? Production: In Vitro and In Vivo Studies  

PubMed Central

In this work, we describe the design, synthesis and pharmacological evaluation of novel imidazo[1,2-a]pyridine-N-glycinyl-hydrazone derivatives (1a–k) intended for use as inhibitors of tumor necrosis factor alpha (TNF-?) production. The compounds were designed based on the orally active anti-inflammatory prototype LASSBio-1504 (2), which decreases the levels of the pro-inflammatory cytokine TNF-? in vitro and in vivo. The in vitro pharmacological evaluation of the imidazo[1,2-a]pyridine compounds (1) showed that substitution of the N-phenylpyrazole core present in prototype 2 by a bioisosteric imidazo[1,2-a]pyridine scaffold generated anti-TNF-? compounds that were more potent than the previously described N-phenylpyrazole derivative 2 and as potent as SB-203580, a p38 MAPK inhibitor. The most active derivative (E)-2-(2-tert-butylimidazo[1,2-a]pyridin-3-ylamino)-N’-(4-chlorobenzylidene) acetohydrazide, or LASSBio-1749 (1i) was orally active as an anti-inflammatory agent in a subcutaneous air pouch model, reducing expressively the levels in vivo of TNF-? and other pro-inflammatory cytokines at all of the tested doses. PMID:24632827

Lacerda, Renata B.; Sales, Natalia M.; da Silva, Leandro L.; Tesch, Roberta; Miranda, Ana Luisa P.; Barreiro, Eliezer J.; Fernandes, Patricia D.; Fraga, Carlos A. M.

2014-01-01

281

Synthesis, biological and computational study of new Schiff base hydrazones bearing 3-(4-pyridine)-5-mercapto-1,2,4-triazole moiety  

NASA Astrophysics Data System (ADS)

A series of new Schiff base hydrazones (compounds 1- 16) were synthesized by condensation reaction of 4-amino-3-(4-pyridine)-5-mercapto-1,2,4-triazole with various aldehydes and/or dialdehydes. The structure of the prepared compounds was confirmed by means of 1H NMR, 13C NMR, UV-vis, IR and elemental analyses. The all prepared compounds were assayed for antibacterial ( Escherichia coli and Staphylococcus aureus) and antifungal ( Candida albicans) activities by disc diffusion method. The results indicate that all tested compounds did not show any antibacterial activity against E. coli, as gram negative bacteria, and antifungal activity against C. albicans. But the compounds 2, 3, 4, 6 and 8 containing 4-Cl, 4-Me, 4-MeO, 2,4-di-Cl and 2-OH substituted phenyl moiety, respectively, showed good inhibition against S. aureus as compare to standard drugs. The structure of all biologically active compounds has also been theoretically studied by ab initio Hartree-Fock (HF) methods.

Khanmohammadi, Hamid; Abnosi, Mohammad H.; Hosseinzadeh, Ali; Erfantalab, Malihe

2008-12-01

282

Colon-specific drug delivery for mebeverine hydrochloride.  

PubMed

Mebeverine Hydrochloride (MB-HCl), an effective spasmolytic drug, was formulated as CODES. A colon-specific drug delivery technology CODES was designed to avoid the inherent problems associated with pH- or time-dependent systems. To achieve more protection and control of drug release, MB-HCl was prepared as microspheres and compressed as core tablets of CODES (modified CODES). The core tablets contained the drug either in free form [Formula 1 (F(1))], or as microspheres with 2 different polymer:drug:lactulose ratios (1:1:0.5 [Formula 2 (F(2))] and 2:1:0.5 [Formula 3 (F(3))]. The release profiles of the coated CODES systems were compared with uncoated compressed tablets. The uncoated tablet showed a drug release of 94% after 1 h in simulated gastric condition (pH = 1.2). The release characteristics of the coated systems revealed that the enteric coating (Eudragit L(100)) prevented any drug release in simulated gastric or duodenal conditions in the first 3 h (pH 1.2-6.1), after which drug was slightly liberated in simulated intestinal fluid (pH 7.4) {Phase 1 (P1)}. After 4 h the pH was adjusted to 7 and beta-glucose-oxidase was added, which is an enzyme produced by enterobacteria present in the colon. The acid-soluble coat (Eudragit)E(100)) dissolved and the drug release suddenly increased to reach 95, 72 and 60.4% for F(1)-F(3), respectively. IR spectrum study showed a covalent bond between the drug and the polymer in the formulae F(2) and F(3) resulting in the sustained drug release from the microspheres with a significant difference (p>0.05) to F(1). The findings were confirmed by in vivo investigation using X-ray images for Guinea pigs ingested tablets containing barium sulphate (F(4)), where the tablet began to disintegrate after 10 h of tablet intake. The results of the study indicated that MB-HCl CODES colon-specific drug delivery can act as a successful trigger for drug targeting in the colon. Furthermore, a sustained release of the drug can be achieved from modified CODES containing the drug in the form of microspheres. PMID:18041637

Omar, Samia; Aldosari, Basmah; Refai, Hanan; Gohary, Omaimah Al

2007-12-01

283

The effects upon vigilance and reaction speed of the addition of ephedrine hydrochloride to chlorpheniramine maleate  

Microsoft Academic Search

The addition of the stimulant, ephedrine hydrochloride (15 mg), to the antihistamine, chlorpheniramine maleate (10 mg) is shown significantly to reduce the adverse drowsy effects of the latter upon various components of human performance. Auditory vigilance — a test of long-term attentiveness — is shown particularly to benefit from the addition of ephedrine. Whilst ephedrine does not aid simple reaction

K. Millar; R. T. Wilkinson

1981-01-01

284

A Parent Guide To Understanding the Effects of Ritalin (Methylphenidate Hydrochloride).  

ERIC Educational Resources Information Center

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…

Villegas, Orlando; And Others

285

Analysis of multicomponent formulations containing phenylpropanolamine hydrochloride, caffeine and diazepam by using LC  

Microsoft Academic Search

A reverse phase high performance liquid chromatography assay was carried out for the simultaneous determination of three active principles present in tablets of different origin and wide commercial use in the Province of Córdoba (Argentina). Prescriptions, commercially available as appetite suppressants, very often include the active principles Phenylpropanolamine Hydrochloride (I), Caffeine (II) and Diazepam (III). Simultaneous determination of these three

Carola Ferreyra; Cristina Ortiz

2001-01-01

286

EPR study of free-radical structure and conformation in pyridoxine hydrochloride single crystal  

NASA Astrophysics Data System (ADS)

Numerical analysis of experimental EPR spectra of ?-irradiated single crystals of pyridoxine hydrochloride (vitamin B 6) allowed determination of the structure of the radical formed. Six hyperfine couplings were distinguished. The geometrical model of the radical was found to be in good agreement with the geometry expected from the crystal structure. Semi-empirical INDO and CNDO calculations were performed.

Masiakowski, Jerzy T.; Krzyminiewski, Ryszard; Pietrzak, Jerzy

1985-05-01

287

Enhancing the Effectiveness of Relaxation--Thermal Biofeedback Training with Propranolol Hydrochloride.  

ERIC Educational Resources Information Center

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…

Holroyd, Kenneth A.; And Others

1995-01-01

288

Determination of diclofenac sodium and papaverine hydrochloride in tablets by HPLC method.  

PubMed

A HPLC method for simultaneous determination of diclofenac sodium and papaverine hydrochloride in tablets was developed and validated. The determination was performed with a Zorbax SB-C18 column, mobile phase: methanol-water (60:40, v/v), flow rate: 1 mL min(-1) and UV detection at 278 nm. PMID:19051579

Kasperek, Regina

2008-01-01

289

75 FR 64310 - Determination That BUSPAR (Buspirone Hydrochloride) Tablets, 10 Milligrams, 15 Milligrams, and 30...  

Federal Register 2010, 2011, 2012, 2013

...April 22, 1996 (15 mg and 30 mg strengths). BUSPAR is indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety. BUSPAR (buspirone hydrochloride) Tablets, 10 mg, 15 mg, and 30 mg, are...

2010-10-19

290

Terbinafine hydrochloride treatment of Microsporum canis experimentally-induced ringworm in cats  

Microsoft Academic Search

Cats represent the most important source of Microsporum canis infection to people. Terbinafine hydrochloride is commonly used in the treatment of microsporosis. Its fungicidal action permits short period of treatment. It was our objective to evaluate the effectiveness of this drug in treatment of microsporosis in cats.We treated nine experimentally M. canis infected cats with terbinafine at a dose of

Tina Kotnik; Nevenka Kožuh Eržen; Jernej Kužner; Marinka Drobni?-Košorok

2001-01-01

291

Photodegradation kinetics, cytotoxicity assay and determination by stability-indicating HPLC method of mianserin hydrochloride.  

PubMed

A stability-indicating HPLC method for the determination of mianserin hydrochloride in coated tablets was developed and validated. Also, drug photodegradation kinetics and cytotoxicity were determined. Chromatographic analyses were performed in an Ace RP-18 octadecyl silane column (250 mm x 4.6 mm i.d., particle size 5 microm) maintained at ambient temperature (25 degrees C). The mobile phase was composed of methanol, 50 mM monobasic potassium phosphate buffer and 0.3% triethylamine solution adjusted to pH 7.0 with phosphoric acid 10% (85:15, v/v) in isocratic mode at a flow rate of 1.0 mL x min(-1). The performed degradation conditions were: acid and basic media with HCl 1.0 M and NaOH 1.0 M, respectively, oxidation with H2O2 3% and the exposure to UV-C light. No interference in the mianserin hydrochloride elution was verified by degradation products formed. Linearity was assessed and ANOVA showed non-significant linearity deviation (p > 0.05). Adequate results were obtained for repeatability, intermediate precision, accuracy and robustness. The photodegradation kinetics of mianserin hydrochloride was evaluated in methanol. The degradation of mianserin could be better described as zero order kinetic (r = 0.9982). The UV-C degraded samples of mianserin hydrochloride were also studied in order to determine the preliminary cytotoxicity in vitro against mononuclear cells. PMID:22822535

Sfair, L L; Graeff, J S; Paim, C S; Passos, C S; Steppe, M; Schapoval, E E S

2012-06-01

292

FORMULATION OF MEDICATED CHEWING GUM OF ONDANSETRON HYDROCHLORIDE AND ITS PHARMACOKINETIC EVALUATIONS  

Microsoft Academic Search

An attempt has been made to formulate new chewing gum device for ondansetron hydrochloride in the form of tablet. The new drug delivery system was obtained, at room temperature, by direct compression using conventional pharmaceutical equipment. The resulting chewing gum tablets comprise a gum core combined with fillers, antioxidants, coloring agent and plasticizers, which provide smooth appearance and flexibility during

UPENDRA NAGAICH; VANDANA CHAUDHARY; ROOPA KARKI; AKASH YADAV; B. M. Reddy

2010-01-01

293

Potentiometric differential titration of ?-phenyl-?-aminobutyric acid hydrochloride and intermediate products of its synthesis  

Microsoft Academic Search

Preparations of fl-phenyl -?-aminobutyric acid hydrochloride (phenylbut, I) belong to the class of neotropic drugs, and due to their pronounced tranquilizing activity, find a multifaceted application in medicine [4, 7]. The increase in demand for medicinal preparations has resulted in a need of improvement in the technology of the synthesis and growth in the industrial production of I. For this

A. Ya. Veveris; I. A. Luse

1990-01-01

294

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

PubMed

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

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

2014-03-01

295

Clinical effects of the new phosphorus binder, bixalomer in hemodialysis patients switched from sevelamer hydrochloride.  

PubMed

It has been reported that sevelamer hydrochloride, which is often used as a polymer phosphorus (P) binder for managing serum P concentration in dialysis patients, causes gastrointestinal adverse effects such as constipation, etc. The reason for this is thought to be that sevelamer hydrochloride has high water absorption, causing it to absorb water and swell in the gastrointestinal tract. In June 2012, the new polymer P binder bixalomer was launched in Japan. Since bixalomer has low swelling due to water absorption, it can be expected to alleviate adverse effects in the gastrointestinal system. In our study, for 21 cases of maintenance hemodialysis patients undergoing treatment with sevelamer hydrochloride at our hospital, the P binder was switched from sevelamer hydrochloride to the same dosage of bixalomer, and the concentrations of serum P, corrected calcium (Ca) and whole parathyroid hormone (PTH) before and one month after the switch were compared. In addition, gastrointestinal symptoms (acid reflux, abdominal pain, indigestion, diarrhea and constipation) were evaluated before and after the switch using a questionnaire based on the Japanese version of the Gastrointestinal Symptom Rating Scale (GSRS). By switching to bixalomer, serum P concentration was significantly reduced (P=0.024), but there were no significant changes observed for serum corrected Ca and whole PTH. Furthermore, there were no significant changes observed for all five of the evaluation items of the GSRS, before and after the switch. These results suggest that although bixalomer can more potently reduce the serum P concentration than sevelamer hydrochloride, there were no significant differences in the effects of both P binders on the gastrointestinal symptoms. PMID:24975889

Gen, Shikou; Sasaki, Takaya; Saito, Kanako; Nobe, Kanako; Nodaira, Yuka; Ikeda, Naofumi

2014-06-01

296

In vitro and In vivo characterization of the transdermal delivery of sertraline hydrochloride Films  

PubMed Central

Background and the purpose of the study Sertraline hydrochloride is a selective serotonin reuptake inhibitor principally used in the treatment of major depressive disorder. To maintain the therapeutic plasma drug concentration of the drug for prolonged period, the transdermal drug delivery has been chosen as an alternative route of drug delivery. The pharmacokinetic properties of sertraline hydrochloride make it suitable for transdermal delivery. The purpose of the study was to investigate the effect of polymers and penetration enhancers on the transdermal delivery of the drug in order to improve its therapeutic efficacy. Methods In the preparation of films, Eudragit RL 100, Eudragit RS 100, hydroxy propyl methyl cellulose (HPMC) and ethyl cellulose were used as polymers. The films were characterized for thickness, tensile strength, drug content, moisture uptake, moisture content, water vapor transmission rate and drug release. The films exhibiting higher rates of drug release were subjected to study the effect of oleic acid and propylene glycol as penetration enhancers on skin permeation of sertraline hydrochloride. In vivo and skin irritation studies were performed for the optimized film. Results Films containing Eudragit RL 100, Eudragit RL 100 and HPMC showed the highest drug release of 94.34% and 96.90% respectively in a period of 42 hrs. The release data fitted into kinetic equations, yielded zero-order and fickian mechanism of drug release. There was a two-fold increase in skin permeation of sertraline hydrochloride in the presence of penetration enhancers in the film. The physical evaluation indicated the formation of smooth, flexible and translucent films. No skin irritation occurred on rabbit skin and the infrared studies showed the compatibility of the drug with the formulation excipients. The in vivo study revealed a constant plasma concentration of drug for long periods and the films containing penetration enhancers had achieved adequate plasma levels of the drug. Conclusions The obtained results indicated the feasibility for transdermal delivery of sertraline hydrochloride using eudragit RL 100 and HPMC. PMID:23008688

Vijaya, R.; Ruckmani, K.

2011-01-01

297

Synthesis, characterization of some transition metal(II) complexes of acetone p-amino acetophenone salicyloyl hydrazone and their anti microbial activity.  

PubMed

Complexes of the type [M(apash)Cl] and [M(Hapash)(H2O)SO4], where M = Mn(II), Co(II), Ni(II), Cu(II) and Zn(II); Hapash = acetone p-amino acetophenone salicyloyl hydrazone have been synthesized and characterized by elemental analyses, molar conductance, magnetic moments, electronic, ESR and IR spectra, thermal studies (TGA & DTA) and X-ray diffraction studies. The ligand coordinates through two >C=N and a deprotonated enolate group in all the chloro complexes, whereas through two >C=N- and a >C=O group in all the sulfato complexes. The electronic spectra suggest a square planar geometry for Co(II), Ni(II) and Cu(II) chloride complexes and an octahedral geometry for the sulfate complexes. ESR data show an isotropic symmetry for [Cu(apash)Cl] and [Cu(Hapash)(H2O)SO4] in solid state. However, ESR spectra of both Cu(II) complexes indicate the presence of unpaired electron in d x2-y2. The X-ray diffraction parameters for [Co(apash)Cl] and [Cu(Hapash)(H2O)SO4] complexes correspond to a tetragonal and an orthorhombic crystal lattices, respectively. Thermal studies of [Co(apash)Cl] complex shows a multi-step decomposition pattern. Most of the complexes show better antifungal activity than the standard miconazole against a number of pathogenic fungi. The antibacterial activity of these complexes has been evaluated against E. coli and Clostridium sp. which shows a moderate activity. PMID:18305909

Singh, Vinod P; Katiyar, Anshu; Singh, Shweta

2008-08-01

298

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

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. PMID:24981819

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

2014-07-28

299

The pyrolytic reaction of ketonic hydrazones from S-methyl dithiocarbazate: a combined online GC-MS pyrolysis and DFT study.  

PubMed

The gas-phase pyrolysis of ketonic hydrazones from S-methyl dithiocarbazate R(1)R(2)C=N-NHC(=S)SCH(3) (R(1), R(2) = alkyl or aryl) was investigated by online GC-MS pyrolysis and theoretical calculation. Both of these pyrolytic products, ascribed to methanethiol and the corresponding N-isothiocyanate imines, were detected in the total ion chromatography (TIC) of GC-MS. Calculation results exhibit two stable configurational structures for reactants (Re), which can interconvert with relatively low barriers (<78 kJ/mol). DFT calculations showed that the two unimolecular pyrolytic processes, a direct 1,2-elimination of CH(3)SH for syn-Re and a two-step reaction pathway for trans-Re involving tautomer interconversion followed by decomposition of CH(3)SH, are competitive in the reaction. Both syn-Re and trans-Re exhibit lower critical energies in the propagation step of the radical pyrolysis than that in the unimolecular pyrolysis process (187.76 kJ/mol via 131.91 kJ/mol for syn-Re, and 159.15 kJ/mol via 98.92 kJ/mol for trans-Re). However, much more energy is needed to excite the compound to produce the methylthio radical, with 262.03 and 253.60 kJ/mol for syn-Re and trans-Re, respectively. Therefore, the unimolecular pyrolysis rather than the radical one occurs in the condition of this study. PMID:19132845

Jiang, Kezhi; Bian, Gaofeng; Qiu, Huayu; Pan, Yuanjiang; Lai, Guoqiao

2009-01-29

300

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)

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#, ? H#, ? G#, ? 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.

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

301

Antioxidant and antimicrobial activity of Maillard reaction products from xylan with chitosan/chitooligomer/glucosamine hydrochloride/taurine model systems.  

PubMed

The structure, UV absorbance, browning intensity, fluorescence changes, antioxidant activity and antimicrobial assessment of Maillard reaction products (MRPs) derived from xylan with chitosan, chitooligomer, glucosamine hydrochloride and taurine model systems were evaluated. The results revealed that all MRPs had similar infrared spectra and molecular structures. MRPs from different model systems on the UV absorbance at 294 nm after heated 90 min and browning intensity at 420 nm showed the similar law: xylan-taurine > xylan-glucosamine hydrochloride > xylan-chitooligomer > xylan-chitosan, and the order of DPPH scavenging activity of MRPs was as follows: xylan-chitosan > xylan-chitooligomer > xylan-glucosamine hydrochloride > xylan-taurine, which revealed that the properties of MRPs were closely related to molecular weight of model systems. Moreover, the highest radical scavenging activity of MRPs from xylan with chitosan/chitooligomer/glucosamine hydrochloride/taurine model systems was 65.9%, 63.7%, 46.4% and 42.5%, respectively. PMID:24262546

Wu, Shuping; Hu, Jiao; Wei, Liuting; Du, Yumin; Shi, Xiaowen; Zhang, Lina

2014-04-01

302

77 FR 7582 - Determination That JENLOGA (Clonidine Hydrochloride) Extended-Release Tablets, 0.1 Milligram and...  

Federal Register 2010, 2011, 2012, 2013

...mg, are the subject of NDA 22-331, held by Shionogi Pharma, Inc., initially approved on September 29, 2009. JENLOGA is indicated for the treatment of hypertension. Shionogi Pharma has never marketed JENLOGA (clonidine hydrochloride)...

2012-02-13

303

Catalytic asymmetric hydrogenation of alpha-amino-beta-keto ester hydrochlorides using homogeneous chiral nickel-bisphosphine complexes through DKR.  

PubMed

Homogeneous chiral nickel-bisphosphine complexes catalyze the asymmetric hydrogenation of alpha-amino-beta-keto ester hydrochlorides through dynamic kinetic resolution to efficiently afford anti-beta-hydroxy-alpha-amino esters with high diastereo- and enantioselectivities. PMID:19082121

Hamada, Yasumasa; Koseki, Yu; Fujii, Takefumi; Maeda, Tsukuru; Hibino, Takuya; Makino, Kazuishi

2008-12-14

304

Flow-injection on-line oxidizing fluorimetry and solid phase extraction for determination of thioridazine hydrochloride in human plasma  

Microsoft Academic Search

A simple, sensitive and specific fluorimetric method has been developed for the determination of thioridazine hydrochloride in human plasma involving solid phase extraction (SPE). In a flow-injection system, thioridazine hydrochloride is on-line oxidized into a strongly fluorescent compound with a lead dioxide solid-phase reactor and the fluorescence intensity is measured with a fluorescence detector (?ex=349nm, ?em=429nm). A comparison of plasma

Zhi-Qi Zhang; Jian Ma; Ying Lei; Yue-Mei Lu

2007-01-01

305

[Experimental study of the effect of glucosamine hydrochloride on metabolic and repair processes in connective tissue structures].  

PubMed

The effects of glucosamine hydrochloride on the metabolic and repair processes were studied on a model of post-traumatic osteoarthrosis in the articular cartilage and on a model of post-traumatic keratitis in the cornea. The administration of glucosamine hydrochloride stimulated repair and favored inhibition of dystrophic post-traumatic processes in the connective-tissue structures. It is suggested that a probable mechanism of the drug action consists in stimulation of the synthesis of glucosaminoglycanes and collagen. PMID:12596539

Zupanets, I A; Bezdetko, N V; Dedukh, N V; Otrishko, I A

2002-01-01

306

Release of tetracycline hydrochloride from electrospun poly(ethylene-co-vinylacetate), poly(lactic acid), and a blend  

Microsoft Academic Search

Electrospun fiber mats are explored as drug delivery vehicles using tetracycline hydrochloride as a model drug. The mats were made either from poly(lactic acid) (PLA), poly(ethylene-co-vinyl acetate) (PEVA), or from a 50:50 blend of the two. The fibers were electrospun from chloroform solutions containing a small amount of methanol to solubilize the drug. The release of the tetracycline hydrochloride from

El-Refaie Kenawy; Gary L. Bowlin; Kevin Mansfield; John Layman; David G. Simpson; Elliot H. Sanders; Gary E. Wnek

2002-01-01

307

Comparative Study of Propranolol hydrochloride Release from Matrix Tablets with Kollidon®SR or Hydroxy Propyl Methyl Cellulose  

Microsoft Academic Search

The release of propranolol hydrochloride from matrix tablets with hydroxy propyl methyl cellulose (HPMC K15M) or Kollidon®SR\\u000a at different concentrations was investigated with a view to developing twice daily sustained release dosage form. A hydrophilic\\u000a matrix-based tablet using different concentrations of HPMC K15M or Kollidon®SR was developed using direct compression technique\\u000a to contain 80 mg of propranolol hydrochloride. The resulting matrix

J. Sahoo; P. N. Murthy; S. Biswal; S. K. Sahoo; A. K. Mahapatra

2008-01-01

308

[Preparation of ondansetron hydrochloride sustained-release tablet evaluation of its and drug release behavior in vitro].  

PubMed

For the purpose of preparing the ondansetron hydrochloride sustained-release tablets and studying the influencing factors, we prepared the ondansetron hydrochloride sustained-release tablets, using hydroxypropylmethylcellose (HPMC) as the matrix material. Then we investigated the effects of the viscosity and amount of HPMC,the sort of fillers, the preparation methods, the alcohol content in adhesives, and the pH of the dissolving solution on the release of ondansetron hydrochloride from sustained-release tablets. On the basis of pharmaceutical preformulation studies,the best formulation and preparation methods were screened out according to orthogonal experiment design method. The release behavior of the tablets followed the Higuchi equation. The viscosity of HPMC,the sort of fillers and the rotation speed had no significant effects on the release of ondansetron hydrochloride sustained-release tablets,while the preparation methods, the alcohol content in adhesives and the pH of the dissolving solution influcenced the release of ondansetron hydrochloride sustained-release tablets significantly. Ondansetron hydrochloride sustained-release tablets had good drug relase behavior for in 12 h in vitro. PMID:16856397

Zhang, Yuhong; Huang, Guihua; Yu, Yanling; Han, Jingbin; Yu, Ping

2006-06-01

309

Synthesis and Crystal Structure Determination of 6-( N Isopropyl)Amidino2-Methylbenzothiazole Hydrochloride Monohydrate and 2Amino6-( N Isopropyl)Amidinobenzothiazole Hydrochloride  

Microsoft Academic Search

Two novel substituted amidino-benzothiazoles 6-(N-isopropyl)amidino-2-methylbenzothiazole 4 and 2-amino-6-(N-isopropyl)amidinobenzothiazole 6 were prepared in multistep synthesis in form of hydrochloride salts. They were characterized by means of IR, 1H, and 13C-NMR spectroscopy and elemental analysis. The crystal structures have been also determined by X-ray analysis. Both compounds crystallize as colorless prisms in the triclinic crystal system, space group P\\u000a

Irena ?aleta; Mario Cetina; Antonija Hergold-Brundi?; Ante Nagl; Grace Karminski-Zamola

2003-01-01

310

Preparation and characterisation of mucoadhesive nasal gel of venlafaxine hydrochloride for treatment of anxiety disorders.  

PubMed

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

Basu, Shyamoshree; Maity, S

2012-09-01

311

Management of attention-deficit hyperactivity disorder in adults: focus on methylphenidate hydrochloride  

PubMed Central

Attention-deficit hyperactivity disorder (ADHD) is one of the most common psychiatric disorders in young adults and causes significant psychosocial impairment and economic burden to society. Because of the paucity of long-term evidence and lack of national guidelines for diagnosis and management of adult ADHD, most of the data are based on experience derived from management of childhood ADHD. This article reviews the current evidence for the diagnosis and management of adult ADHD with special emphasis on the role of methylphenidate hydrochloride preparations in its treatment. Methylphenidate hydrochloride, a stimulant that acts through the dopaminergic and adrenergic pathways, has shown more than 75% efficacy in controlling the symptoms of adult ADHD. Although concern for diversion of the drug exists, recent data have shown benefits in preventing substance use disorders in patients with adult ADHD. PMID:19721722

Nair, Rajasree; Moss, Shannon B

2009-01-01

312

Nonisothermal Kinetics Analysis of the Dehydration of Ziprasidone Hydrochloride Monohydrate by Thermogravimetry  

PubMed Central

In the current work the kinetics of dehydration of ziprasidone hydrochloride monohydrate was studied by nonisothermal thermogravimetry. Ziprasidone hydrochloride monohydrate was heated from 30 to 150° with a heating rate of 5° per min under nitrogen gas atmosphere and weight loss data were collected. Powder X-ray difraction was used to characterize the solid before and after dehydration. The well accepted Coats-Redfern model fitting approach was applied to the thermogravimetry data for the kinetic analysis. Thirteen solid state reaction models were studied; among them one-dimensional diffusion model was found to be the best fit model for this reaction with an excellent correlation 0.9994. The Arrhenius parameters, activation energy, and pre-exponential factor were determined, the values were found to be 28 k.cal/mol and 9.53×1013 sec?1, respectively. PMID:24082354

Ravikiran, A.; Arthanareeswari, M.; Kamaraj, P.; Praveen, C.

2013-01-01

313

The effect of polymorphism on powder compaction and dissolution properties of chemically equivalent oxytetracycline hydrochloride powders.  

PubMed

In South Africa, oxytetracycline is identified as an essential drug; many generic products are on the market, and many more are being developed. In this study, six oxytetracycline hydrochloride powders were obtained randomly from manufacturers, and suppliers were compared. It was found that compliance to a pharmacopoeial monograph was insufficient to ensure the optimum dissolution performance of a simple tablet formulation. Comparative physicochemical raw material analysis showed no major differences with regard to differential scanning calorimetry (DSC), infrared (IR) spectroscopy, powder dissolution, and particle size. However, the samples could be divided into two distinct types with respect to X-ray powder diffraction (XRD) and thus polymorphism. The two polymorphic forms had different dissolution properties in water or 0.1 N hydrochloride acid. This difference became substantial when the dissolution from tablets was compared. The powders containing form A were less soluble than that containing form B. PMID:10518242

Liebenberg, W; de Villiers, M M; Wurster, D E; Swanepoel, E; Dekker, T G; Lötter, A P

1999-09-01

314

First human studies on the safety and antitussive activity of vadocaine hydrochloride.  

PubMed

Vadocaine hydrochloride (2',4'-dimethyl-6'-methoxy-3-(2-methylpiperidyl)propionanilide+ ++ hydrochloride, OR K-242-HCl; INN: vadocaine) is a new anilide derivative which resembles lidocaine in chemical structure. The safety and antitussive effects of this new compound were studied in 6 healthy male volunteers in the first Phase I clinical trial. Vadocaine was administered in single doses of 5, 10, 15, 20, 30 and 50 mg. At these dose levels vadocaine had no effects on the cardiovascular system, the haematological variables, blood biochemistry or urinary sediment examined as safety evaluation. The antitussive properties of the compound were studied using inhaled citric acid for induction of the cough response. The antitussive properties of vadocaine were most effective at a dose of 15 mg, although no statistical significance was found. Neither was any dose-response relationship noted. However, at this dose level vadocaine is apparently safe and its antitussive properties seem promising enough for further evaluation. PMID:3395401

Karttunen, P; Tukiainen, H; Uusitupa, M; Männistö, P T

1988-04-01

315

Quantitative estimation of itopride hydrochloride and rabeprazole sodium from capsule formulation.  

PubMed

Two simple, accurate, economical and reproducible UV spectrophotometric methods and one HPLC method for simultaneous estimation of two component drug mixture of itopride hydrochloride and rabeprazole sodium from combined capsule dosage form have been developed. First developed method involves formation and solving of simultaneous equations using 265.2 nm and 290.8 nm as two wavelengths. Second method is based on two wavelength calculation, wavelengths selected for estimation of itopride hydrochloride was 278.0 nm and 298.8 nm and for rabeprazole sodium 253.6 nm and 275.2 nm. Developed HPLC method is a reverse phase chromatographic method using phenomenex C(18) column and acetonitrile: phosphate buffer (35:65 v/v) pH 7.0 as mobile phase. All developed methods obey Beer's law in concentration range employed for respective methods. Results of analysis were validated statistically and by recovery studies. PMID:21394269

Pillai, S; Singhvi, I

2008-09-01

316

Thermodynamic characteristics of the acid dissociation of dopamine hydrochloride in water-ethanol solutions  

NASA Astrophysics Data System (ADS)

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 (?r H ?, ?r G ?, and ?r 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.

Ledenkov, S. F.; Vandyshev, V. N.; Molchanov, A. S.

2012-06-01

317

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)

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.

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

2014-09-01

318

A study of the reaction between antimony (V) chloride and organic amine hydrochlorides  

E-print Network

A STUDY OF THE REACTION BETMEEN ANTIMONY (V) CHLORIDE AND ORGANIC ANINE HYDHOCHLORIDES A Thesis by Harold Dean Bier Submitted to the Graduate School of the Agricultural and. Nechanical College of Texas in partial fulfillment... of the requirements for the degree of NASTER OF SCIENCE August 1962 Na]or Sub)ect: Chemistry A STUDY OF THE REACTION BETMEEN ANTINONY (V) CHLORIDE AND ORGANIC ANINE HYDROCHLORIDES A Thesis by Harold Dean Bier Approved as to style and content by& (Chairm...

Bier, Harold Dean

2012-06-07

319

Formulation and Evaluation of Bioadhesive Buccal Drug Delivery of Tizanidine Hydrochloride Tablets  

Microsoft Academic Search

The study aim was concerned with formulation and evaluation of bioadhesive buccal drug delivery of tizanidine hydrochloride\\u000a tablets, which is extensively metabolized by liver. The tablets were prepared by direct compression using bioadhesive polymers\\u000a such as hydroxylpropyl methylcellulose K4M, sodium carboxymethyl cellulose alone, and a combination of these two polymers.\\u000a In order to improve the permeation of drug, different permeation

Gazzi Shanker; Chegonda K. Kumar; Chandra Sekhara Rao Gonugunta; B. Vijaya Kumar; Prabhakar Reddy Veerareddy

2009-01-01

320

Design, development and permeation studies of nebivolol hydrochloride from novel matrix type transdermal patches  

PubMed Central

Background: Nebivolol hydrochloride is a third generation ?-blocker with highly selective ?1-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

Jatav, Vijay Singh; Saggu, Jitender Singh; Sharma, Ashish Kumar; Sharma, Anil; Jat, Rakesh Kumar

2013-01-01

321

Adhesive properties of soy proteins modified by urea and guanidine hydrochloride  

Microsoft Academic Search

An investigation was conducted on the adhesive and water-resistance properties of soy protein isolates that were modified\\u000a by varying solutions of urea (1, 3, 5, and 8 M) or guanidine hydrochloride (GH) (0.5, 1, and 3 M) and applied on walnut, cherry,\\u000a and pine plywoods. Soy proteins modified by 1 and 3 M urea showed greater shear strengths than did

Weining Huang; Xiuzhi Sun

2000-01-01

322

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application  

PubMed Central

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 ?g/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 ?M, as compared with rigid liposomes. These ex vivo findings proved that a raloxifene hydrochloride-loaded transfersome formulation could be a superior alternative to oral delivery of the drug. PMID:25246789

Mahmood, Syed; Taher, Muhammad; Mandal, Uttam Kumar

2014-01-01

323

Effect of anionic polymers on the release of propranolol hydrochloride from matrix tablets  

Microsoft Academic Search

Anionic polymers, namely Eudragit S, Eudragit L 100-55, and sodium carboxymethylcellulose, were incorporated into hydroxypropylmethylcellulose (HPMC K100M) to modify the drug release from HPMC matrices. The effects of changing the ratio of HPMC to anionic polymers were examined in water and in media with different pH. The dissolution profiles were compared according to release rates. The interaction between propranolol hydrochloride

Sevgi Takka; Sangita Rajbhandari; Adel Sakr

2001-01-01

324

Polymeric Matrix System for Prolonged Delivery of Tramadol Hydrochloride, Part II: Biological Evaluation  

Microsoft Academic Search

This study is an extrapolation of our previous one (part I) concerned with the formulation and physicochemical evaluation\\u000a of a novel, simple, monolayer, easy-to-use, cost-effective, and aesthetically acceptable bioadhesive transdermal patch for\\u000a tramadol hydrochloride. The current work is focused on bioadhesion, skin tolerability, and pharmacodynamic evaluation. Using\\u000a naked rat skin, chitosan–Eudragit® NE30D (1:1) film attained best bioadhesive properties. During in

Hussein O. Ammar; Mahmoud Ghorab; Soheir A. El-Nahhas; Rabab Kamel

2009-01-01

325

Sevelamer hydrochloride attenuates kidney and cardiovascular calcifications in long-term experimental uremia  

Microsoft Academic Search

Sevelamer hydrochloride attenuates kidney and cardiovascular calcifications in long-term experimental uremia.BackgroundIn chronic renal failure (CRF), hyperphosphatemia and an elevated calcium-phosphate product are associated with vascular calcification and increased cardiovascular morbidity and mortality. Previous data have demonstrated that 3-month treatment of uremic rats with sevelamer was associated with less nephrocalcinosis compared to calcium carbonate (CaCO3), despite similar control of serum phosphorus,

Mario Cozzolino; Mark E. Staniforth; Helen Liapis; Jane Finch; Steven K. Burke; Adriana S. Dusso; Eduardo Slatopolsky

2003-01-01

326

An analytical chemical study of pilocarpine hydrochloride and its hydrolysis products  

E-print Network

'orm. The chloxoform 'is then removed by careful heating and the alkaloid is taken up in a measured excess oi' sulfuric acid. The free 'base is sufficiently alkaline in reaction for the titration of the reserve acid with a standaxd alkali. The ionization constants... . The pilocarpine hydrochloride was furnished by Alcon Laboratories of Fort Vcrth, Texas and assayed 100. 1$ by chloride titration. Development of Bromination Procedure It has been reported in the literature and confirmed in this laboratory that, pilocarpine...

Ibert, Edward R

2012-06-07

327

Theoretical and experimental study of vibrational spectra of two polymorphic 4-hydroxy-1-methylpiperidine betaine hydrochlorides  

Microsoft Academic Search

The molecular geometries, harmonic frequencies and intensities of the vibrational bands of ? and ? polymorphs of 4-hydroxy-1-methylpiperidine betaine hydrochloride (?-HO-MPBH·Cl, ?-HO-MPBH·Cl) and their deuterated derivatives have been calculated with the B3LYP\\/6-31G(d,p) level of theory. The calculated frequencies are compared with the solid FTIR and Raman spectra. Unequivocal assignments of the experimental infrared bands are performed on the basis of

M. Szafran; J. Koput; Z. Dega-Szafran

2008-01-01

328

Theoretical and experimental study of vibrational spectra of two polymorphic 4-hydroxy-1-methylpiperidine betaine hydrochlorides  

NASA Astrophysics Data System (ADS)

The molecular geometries, harmonic frequencies and intensities of the vibrational bands of ? and ? polymorphs of 4-hydroxy-1-methylpiperidine betaine hydrochloride (?-HO-MPBH·Cl, ?-HO-MPBH·Cl) and their deuterated derivatives have been calculated with the B3LYP/6-31G(d,p) level of theory. The calculated frequencies are compared with the solid FTIR and Raman spectra. Unequivocal assignments of the experimental infrared bands are performed on the basis of the potential energy distribution (PED).

Szafran, M.; Koput, J.; Dega-Szafran, Z.

2008-09-01

329

Short and symmetrical OHO hydrogen bond in bis(quinuclidine betaine) hydrochloride  

Microsoft Academic Search

The molecular structure of bis(quinuclidine betaine) hydrochloride, (QNB)2HCl, has been characterized by single crystal X-ray diffraction, infrared spectroscopy and by DFT calculations. The crystals are centrosymmetric, monoclinic, space group C2\\/c. Two QNB moieties are joined by a very short and centered O?H?O hydrogen bond of 2.461(2)Å. Its existence is confirmed by the broad absorption band below 1500cm?1 in the FTIR

Z. Dega-Szafran; A. Katrusiak; M. Szafran

2010-01-01

330

Alleviation of side effects induced by irinotecan hydrochloride (CPT11) in rats by intravenous infusion  

Microsoft Academic Search

PurposeIrinotecan hydrochloride (CPT-11) is a potent topoisomerase I inhibitor and is established and used widely as an antitumor agent. However, it sometimes causes severe side effects such as myelosuppression and diarrhea. These dose-limiting toxicities prevent the adoption of CPT-11 in aggressive chemotherapy. Thus we sought to determine in a rat model whether extending the period of infusion of CPT-11 would

Akinobu Kurita; Shoichi Kado; Norimasa Kaneda; Masaharu Onoue; Shusuke Hashimoto; Teruo Yokokura

2003-01-01

331

Design and evaluation of sustained-release and buccal adhesive propranolol hydrochloride tablets  

Microsoft Academic Search

The release of propranolol hydrochloride incorporated into sustained-release and buccal adhesive tablets was studied in vitro. The formulation containing 20% hydroxypropyl methylcellulose (HPMC) yielded good sustained-release matrix tablets. Buccal adhesive controlled-release tablets were prepared by compression of HPMC with polycarbophil (PAA), which served as the bioactive adhesive compound. The release behaviour of buccal adhesive tablets was found to be non-Fickian.

Buket Taylan; Yilmaz Capan; Olgun Güven; Sirri Kes; A. Atilla Hincal

1996-01-01

332

Guar Gum, Xanthan Gum, and HPMC Can Define Release Mechanisms and Sustain Release of Propranolol Hydrochloride  

Microsoft Academic Search

The objectives were to characterize propranolol hydrochloride-loaded matrix tablets using guar gum, xanthan gum, and hydroxypropylmethylcellulose\\u000a (HPMC) as rate-retarding polymers. Tablets were prepared by wet granulation using these polymers alone and in combination,\\u000a and physical properties of the granules and tablets were studied. Drug release was evaluated in simulated gastric and intestinal\\u000a media. Rugged tablets with appropriate physical properties were

Muhammad Akhlaq Mughal; Zafar Iqbal; Steven Henry Neau

2011-01-01

333

The determination of in vitro pingyangmycin hydrochloride plasma protein binding by microdialysis.  

PubMed

Microdialysis sampling was used to study the binding of pingyangmycin hydrochloride (PYM) to plasma proteins in canis familiaris blood. In vitro plasma protein binding fractions were evaluated in a series of PYM concentration. The results showed decreased protein binding with increased concentration. The data was analyzed using the Scatchard analysis and Klotz plot. The results showed that the Scatchard plot and Klotz plot were linear with good correlation coefficient, indicating a good agreement of the experimental data to the theoretical equation. PMID:17341030

Gao, Z B; Ding, P T; Xu, H; Zhang, L; Wei, J; Chen, D W

2007-02-01

334

SIMULTANEOUS DETERMINATION OF OFLOXACIN AND FLAVOXATE HYDROCHLORIDE IN HUMAN PLASMA BY RP HPLC  

Microsoft Academic Search

A sensitive RP HPLC method has been developed and validated for the determination of ofloxacin and flavoxate hydrochloride in spiked human plasma. For the estimation of drugs in plasma, sample pretreatment involved only protein precipitation by acetonitrile. Chromatographic separation was performed on a Kromasil C8 (4.6 mm × 250 mm, 5 µm) column, with mobile phase consisting of formic acid in water, methanol, and acetonitrile

Mahesh V. Attimarad; Sree Harsha N; Ramachandra S. Setty

2012-01-01

335

Determination of benzhexol hydrochloride by capillary zone electrophoresis with an end-column electrochemiluminescence detection  

Microsoft Academic Search

A capillary zone electrophoresis with end-column electrochemiluminescence (ECL) detector was described for the determination of benzhexol hydrochloride. The detection was based on the tris(2,2?-bypyridine)ruthenium(II) [Ru(bpy)32+] ECL reaction with the analyte. Electrophoresis was performed using a 25 ?m i.d. uncoated capillary. 10 mM sodium phosphate buffer (pH=8.0) was used as the running buffer. The solution in the detection cell was 80

Jilin Yan; Jifeng Liu; Weidong Cao; Xiuhua Sun; Xiurong Yang; Erkang Wang

2004-01-01

336

Effect of Moxisylyte Hydrochloride (?1Blocker) on the Retinal Circulation of Patients with Diabetes mellitus  

Microsoft Academic Search

Moxisylyte hydrochloride (?1-blocker) selectively vasodilates cerebral vessels without reducing blood pressure. We investigated the effect of the drug on retinal circulation in 15 patients (17 eyes) with diabetes mellitus, using the video-densitometric image analysis of fiuorescein angiography. We compared the build-up time (BT), the time constant of washout rate (TC) and the mean circulation time (MCT) before and after oral

Ryo Suzuki; Itsuko Sugihara; Shinji Kurimoto

1992-01-01

337

Simultaneous determination of rabeprazole sodium and itopride hydrochloride in capsule dosage form by spectrophotometry.  

PubMed

Three methods viz. Absorbance Ratio Method (I), Dual Wavelength Method (II) and First Order Derivative Spectroscopic Method (III) for simultaneous estimation of Rabeprazole sodium and Itopride hydrochloride have been developed. The drugs obey Beer's law in the concentration range 2-20 microg/ml for RAB and 5-75 microg/ml for ITO. The results of analysis of drugs have been validated statistically and by recovery studies. PMID:19957542

Sabnis, Shweta S; Gandhi, Santosh V; Madgulkar, A R; Bothara, K G

338

Effects of switching from sevelamer hydrochloride to bixalomer on laboratory parameters in hemodialysis patients.  

PubMed

In Japan, the clinical use of bixalomer, a new polymer preparation like sevelamer hydrochloride, became possible from 2012. In our study, in order to investigate the clinical characteristics of this new phosphorus (P) binder, bixalomer in a clinical practice, for 18 cases of hemodialysis patients at our hospital being treated with sevelamer hydrochloride, we switched the P binder to bixalomer, and compared the laboratory parameters before and after switching. Subjects used for analysis were nine cases in which it was possible to use bixalomer continuously for 10 months. The laboratory parameters measured were the concentrations of serum P, corrected calcium (Ca), whole parathyroid hormone (PTH), albumin and alkaline phosphatase (ALP) as indicators of mineral and bone disorder, and serum high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C) and triglyceride (TG) as indicators of lipid metabolism. Regarding the results after switching to bixalomer and starting treatment using the same dosage as the dosage previously used for sevelamer hydrochloride, there were many cases that showed increasing P concentrations that required increasing the dosage of bixalomer, the dosage after switching was increased significantly (P=0.002). In the comparison of laboratory parameters before and after switching, the concentrations of serum P and albumin decreased significantly (P=0.035 and 0.033). From these results, it was considered that the decreases in serum P concentrations were due not only to the effects of bixalomer, but that suppression of food intake by patients was another reason. There were no significant changes in corrected Ca, whole PTH or ALP. In addition, after changing the P binder, serum HDL-C concentration decreased significantly (P=0.015) and LDL-C increased significantly (P<0.001), and serum TG concentration showed no significant changes. This indicated that the beneficial effects of bixalomer on lipid metabolism may be less than those of sevelamer hydrochloride. PMID:24975888

Furukawa, Kazunori; Ikawa, Tomoyoshi; Yokoi, Sayuri; Yokouchi, Shuhei; Kato, Kieko; Ueno, Miki; Takahashi, Junichiro

2014-06-01

339

Effect of deprotenizing agent and quantification of donepezil hydrochloride in human plasma.  

PubMed

The effect of deprotenizing agents on recovery of donepezil hydrochloride in the development of a simple, rapid, selective and sensitive high performance liquid chromatography method for quantification of donepezil hydrochloride in human plasma was described. The deprotenizing agents were comprised of, perchloric acid, methanol, acetonitrile, chloroform and their mixtures. The chromatographic separation was carried out using reversed phase C18 column (Agilent Eclipse Plus C18) with UV detection at 268 nm. The mobile phase was comprised of 0.01 M potassium dihydrogen phosphate buffer, methanol and acetronitrile (50:30:20, v/v) adjusted to pH 2.7 with phosphoric acid (80%). A combination of perchloric acid and methanol gave a cleaner sample with a good recovery of donepezil hydrochloride of above 96%. The method showed intraday precision and accuracy in the range of 6.82% to 1.5% and 3.13% to 1.12% respectively, while interday precision and accuracy ranged between 1.06% to 4.71% and 13.01% to 6.43% respectively. The standard calibration curve was linear from 30ng/mL to 4000ng/mL, with a correlation coefficient of 0.9965±0.0034. The retention time of donepezil was 5.9 min with a run time of 7.0 min. The method can be applied to analyze large batch plasma samples in pharmacokinetic studies. PMID:25176366

Liew, Kai Bin; Peh, Kok Khiang; Fung Tan, Yvonne Tze

2014-09-01

340

Silicone adhesive matrix of verapamil hydrochloride to provide pH-independent sustained release.  

PubMed

Providing pH-independent oral release of weakly basic drugs with conventional matrix tablets can be challenging because of the pH-dependent solubility characteristics of the drugs and the changing pH environment along the gastrointestinal tract. The aim of the present study was to use a hydrophobic polymer to overcome the issue of pH-dependent release of weakly basic model drug verapamil hydrochloride from matrix tablets without the use of organic buffers in the matrix formulations. Silicone pressure-sensitive adhesive (PSA) polymer was evaluated because of its unique properties of low surface energy, hydrophobicity, low glass transition temperature, high electrical resistance, and barrier to hydrogen ion diffusion. Drug release, hydrogen ion diffusion, tablet contact angle, and internal tablet microenvironment pH with matrix tablets prepared using PSA were compared with those using water-insoluble ethyl cellulose (EC). Silicone PSA films showed higher resistance to hydrogen ion diffusion compared with EC films. Verapamil hydrochloride tablets prepared using silicone PSA showed higher hydrophobicity and lower water uptake than EC tablets. Silicone PSA tablets also showed pH-independent release of verapamil and decreased in dimensions during drug dissolution. By contrast, verapamil hydrochloride tablets prepared using EC did not achieve pH-independent release. PMID:24022347

Tolia, Gaurav; Li, S Kevin

2014-02-01

341

Design and in vitro testing of a floatable gastroretentive tablet of metformin hydrochloride.  

PubMed

Metformin hydrochloride, which is better absorbed in the upper intestine, was formulated as a floating (buoyant) matrix tablet using a gas generating agent (sodium bicarbonate) and a gel forming hydrophilic polymer (hydroxypropyl methylcellulose). The formulation was optimized on the basis of floating ability and in vitro drug release. The resulting formulation produced robust tablets with optimum hardness, consistent weight uniformity and low tablet friability. All tablets but one exhibited satisfactory (gradual and near complete) drug release and buoyancy. In vitro drug release tests of these tablets indicated controlled sustained release of metformin hydrochloride and 96-99% released at the end of 8 h. Two formulations of fabricated tablets containing metformin hydrochloride (500 mg), sodium bicarbonate (75 mg), hydroxypropyl methylcellulose-K 4M (170-180 mg), citric acid (between 15 and 20 mg) and polyvinyl pyrrolidone K90 (32-40 mg) with hardness between 6.8 to 7.5 kg/cm2 showed a floating time of more than 8 h and promising drug release results. The release followed the Higuchi kinetic model, indicating diffusion dominated drug release. PMID:17341036

Basak, S C; Rahman, J; Ramalingam, M

2007-02-01

342

Derivative Synchronous Fluorescence Spectroscopy for the Simultaneous Determination of Dapoxetine Hydrochloride and Vardenafil in Binary Mixtures  

NASA Astrophysics Data System (ADS)

The first and second derivative synchronous fluorescence spectroscopy (FDSFS&SDSFS) methods have been developed and validated for the simultaneous analysis of a binary mixture of dapoxetine hydrochloride and vardenafil. Method 1A describes a measurement of the normal synchronous fluorescence intensity of these drugs at ?? = 35 nm using sodium dodecyl sulfate as the fluorescence enhancer in aqueous solutions. This method was extended (Method 1B) to the use of FDSFS&SDSFS for the determination of both drugs. The fluorescence concentration plots were linear over the range of 1-10 and 0.2-2 ?g/ml for dapoxetine hydrochloride and vardenafil, respectively, with lower detection limits of 290 and 62.5 ng/ml, and quantification limits of 890 and 190 ng/ml for dapoxetine hydrochloride and vardenafil, respectively. The proposed method was applied for the simultaneous determination of DAP and VAR in different synthetic mixtures and in co-formulated pharmaceutical preparation. The results obtained were in good agreement with those obtained using a reference method.

Soliman, S. M.; El-Agizy, H. M. Y.; El Bayoumi, Abd El Aziz

2014-07-01

343

Kinetic and thermodynamic evaluation of phosphate ions binding onto sevelamer hydrochloride.  

PubMed

Sevelamer hydrochloride is the first non-aluminium, non-calcium-based phosphate binder developed for the management of hyperphosphatemia in end stage renal diseases. It is a synthetic ion-exchange polymer which binds and removes phosphate ions due to the high content of cationic charge associated with protonated amine groups on the polymer matrix. This is the first in-depth study investigating phosphate removal in vitro from aqueous solutions using commercially available sevelamer hydrochloride at physiological conditions of phosphate level, pH and temperature. The kinetic and thermodynamic parameters of phosphate binding onto the sevelamer hydrochloride particles were evaluated in order to define the binding process. A series of kinetic studies were carried out in order to delineate the effect of initial phosphate concentration, absorbent dose and temperature on the rate of binding. The results were analysed using three kinetic models with the best-fit of the experimental data obtained using a pseudo-second order model. Thermodynamic parameters provide in-depth information on inherent energetic changes that are associated with binding. Free energy ?G°, enthalpy ?H°, and entropy ?S° changes were calculated in this study in order to assess the relationship of these parameters to polymer morphology. The binding reaction was found to be a spontaneous endothermic process with increasing entropy at the solid-liquid interface. PMID:25102115

Elsiddig, Reem; Hughes, Helen; Owens, Eleanor; O' Reilly, Niall J; O'Grady, David; McLoughlin, Peter

2014-10-20

344

Stability of morphine sulfate and meperidine hydrochloride in a parenteral nutrient formulation.  

PubMed

The compatibility, stability, and availability of morphine sulfate and meperidine hydrochloride prepared in total parenteral nutrient (TPN) solution, 5% dextrose injection, and sterile water for injection in polyvinyl chloride (PVC) bags were evaluated. A 300-mg dose of each narcotic was mixed in 0.25-L bags of 5% dextrose injection and sterile water for injection, and in 3-L bags of TPN and sterile water for injection. Each solution was examined visually for precipitation, color change, turbidity, and the evolution of gas immediately after the addition of the drug to the bag and every 12 hours for a 36-hour period. Narcotic concentrations in each solution were determined by high-pressure liquid chromatography before and for 36 hours after the addition of the drugs to the bags. No loss of either drug because of adsorption to the PVC bags was found. Morphine sulfate and meperidine hydrochloride were chemically compatible and stable in TPN and 5% dextrose injection for 36 hours. Solutions of morphine sulfate or meperidine hydrochloride in PVC bags containing TPN or 5% dextrose injection are visually and chemically compatible, as well as stable and available for 36 hours when stored at 21.5 degrees C with no protection from environmental light. PMID:3923832

Macias, J M; Martin, W J; Lloyd, C W

1985-05-01

345

Application of Design of Experiment for Floating Drug Delivery of Tapentadol Hydrochloride  

PubMed Central

The aim of the present study was to apply design of experiment (DOE) to optimize floating drug delivery of tapentadol hydrochloride. Tapentadol hydrochloride is a synthetic opioid used as a centrally acting analgesic and effective in both experimental and clinical pain. The half-life of the drug is about 4 hours and oral dose is 50 to 250?mg twice a day. For optimization 32 full factorial design was employed for formulation of tapentadol hydrochloride tablets. Sodium bicarbonate was incorporated as a gas-generating agent. Combination of polymers Xanthan gum and Locust bean gum was used to achieve controlled release effect. The concentration of polymers was considered as the independent variables and dependent variables were floating lag time and swelling index of the tablets. From the factorial batches, it was observed that formulation containing combination of 20% sodium bicarbonate and 10% citric acid shows optimum floating ability whereas the formulation containing 20% Xanthan gum and 28% Locust bean gum shows optimum sustained drug release pattern with adequate floating. PMID:23878616

Jagdale, Swati C.; Patil, Somnath; Kuchekar, Bhanudas S.

2013-01-01

346

Stability of milrinone and epinephrine, atropine sulfate, lidocaine hydrochloride, or morphine sulfate injection.  

PubMed

The stability of both drug components of admixtures of milrinone and epinephrine, atropine sulfate, lidocaine hydrochloride, morphine sulfate, calcium chloride, or sodium bicarbonate injections was studied. Duplicate solutions of admixtures of milrinone injection 1 mg/mL and epinephrine injection 1:10,000, atropine sulfate injection 1 mg/mL, lidocaine hydrochloride injection 1%, morphine sulfate injection 8 mg/mL, calcium chloride injection 10%, or sodium bicarbonate injection 7.5% were prepared and stored in glass containers at 22-23 degrees C under fluorescent light. Samples were taken immediately and after 20 minutes for assay by high-performance liquid chromatography (HPLC). Milrinone at initial concentrations of 0.10-0.73 mg/mL showed no degradation in any of the solutions during the study period, nor was any degradation observed for lidocaine, morphine, atropine, or epinephrine. Milrinone 0.10-0.73 mg/mL is compatible with atropine sulfate, lidocaine hydrochloride, epinephrine, calcium chloride, or sodium bicarbonate in glass containers stored for 20 minutes at room temperature. These results support the use of milrinone in combination with these agents immediately after the preparation of admixtures. PMID:2278262

Wilson, T D; Forde, M D

1990-11-01

347

Stability and compatibility of binary mixtures of morphine hydrochloride with hyoscine-n-butyl bromide.  

PubMed

The aim of this study was to determine the compatibility and stability of morphine hydrochloride and hyoscine-N-butyl bromide combined in solution at three different concentrations and stored in polypropylene syringes at 4 degrees C and 25 degrees C over a period of 15 days. The doses assayed were 20, 60 and 120 mg/day for morphine hydrochloride and 40, 60 and 80 mg/day for hyoscine-N-butyl bromide. These dose ranges were chosen according to daily practice. At both temperatures, all mixtures can be considered as physically compatible since no evidence of incompatibility-that is precipitation, turbidity, colour change or opacity and gas production-were observed. After 15 days of storage, the percentages of hyoscine-N-butyl bromide remaining in the drug mixtures tested ranged between 96.07% and 92.23%. At the end of the study, the percentages of morphine hydrochloride remaining in the drug mixtures were 100% at both temperatures. PMID:15798917

Barcia, Emilia; Reyes, Rodrigo; Azuara, Maria Luz; Sánchez, Yolanda; Negro, Sofía

2005-04-01

348

Application of design of experiment for floating drug delivery of tapentadol hydrochloride.  

PubMed

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. PMID:23878616

Jagdale, Swati C; Patil, Somnath; Kuchekar, Bhanudas S

2013-01-01

349

Development and Evaluation of a Novel Modified-Release Pellet-Based Tablet System for the Delivery of Loratadine and Pseudoephedrine Hydrochloride as Model Drugs  

Microsoft Academic Search

Modified-release multiple-unit tablets of loratadine and pseudoephedrine hydrochloride with different release profiles were\\u000a prepared from the immediate-release pellets comprising the above two drugs and prolonged-release pellets containing only pseudoephedrine\\u000a hydrochloride. The immediate-release pellets containing pseudoephedrine hydrochloride alone or in combination with loratadine\\u000a were prepared using extrusion–spheronization method. The pellets of pseudoephedrine hydrochloride were coated to prolong the\\u000a drug release up

Farrukh Zeeshan; Nadeem Irfan Bukhari

2010-01-01

350

In vitro detection of possible in vivo drug interactions. Part 1. The effect of hydrochlorothiazide and frusemide on the in vitro absorption characteristics of propranolol hydrochloride.  

PubMed

The Sartorius absorption simulator was used as a device to detect possible in vivo gastrointestinal tract drug interactions. The drugs chosen were propranolol hydrochloride and two diuretics (namely hydrochlorothiazide and frusemide) commonly used in conjunction with propranolol hydrochloride for the treatment of hypertension. The results show that the presence of both diuretics increased the intestinal absorption rate constant and the percentage diffused of propranolol hydrochloride. Moreover, the presence of propranolol hydrochloride also caused the intestinal absorption rate constants and the percentages diffused of both diuretics to be increased. PMID:7279990

Anber, S A; Al-Janabi, I I; Mustafa, R M; Razzo, F N

1981-06-01

351

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

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

Ali, Mohammed Shahid; Ghori, Mohsin; Rafiuddin, Syed; Khatri, Aamer Roshanali

2007-01-01

352

Liquid Chromatographic Methods for the Determination of Vildagliptin in the Presence of its Synthetic Intermediate and the Simultaneous Determination of Pioglitazone Hydrochloride and Metformin Hydrochloride  

PubMed Central

Two reversed-phase liquid chromatographic (RP-LC) methods are described for the determination of two binary mixtures of hypoglycemic agents. In the first method, vildagliptin (VDG) was determined in the presence of 3-amino-1-adamantanol (AAD), a synthetic intermediate and impurity of VDG. In the second method, pioglitazone hydrochloride (PGZ) and metformin hydrochloride (MET) were simultaneously determined in their binary mixture. Chromatographic separation in the two methods was achieved on a Symmetry® Waters C18 column (150 mm × 4.6 mm, 5 ?m). In the first mixture, isocratic elution using a mobile phase of potassium dihydrogen phosphate buffer pH (4.6) - acetonitrile - methanol (30:50:20, v/v/v) at a flow rate of 1 mL min-1 with UV detection at 220 nm was performed. In the second method, isocratic elution based on potassium dihydrogen phosphate buffer pH (4.6) - acetonitrile (60:40, v/v) at a flow rate of 1 mL min-1 with UV detection at 210 nm was performed. Linearity, accuracy and precision were found to be acceptable over the concentration ranges of 5-200 ?g mL-1, 0.5-3 ?g mL-1 and 10-150 ?g mL-1 for VDG, PGZ and MET, respectively. The optimized methods were validated and proved to be specific, robust, precise and accurate for the quality control of the drugs in their pharmaceutical preparations. PMID:23675237

El-Bagary, Ramzia I.; Elkady, Ehab F.; Ayoub, Bassam M.

2011-01-01

353

Study on the resonance nonlinear scattering spectra of the interactions of promethazine hydrochloride and chlorpromazine hydrochloride with 12-tungstophosphoric acid and their analytical applications  

NASA Astrophysics Data System (ADS)

In pH 1.0 HCl medium, 12-tungstophosphoric acid (TP) reacted with promethazine hydrochloride (PMZ) and chlorpromazine hydrochloride (CPZ) to form ion-association complexes, which led to a great enhancement of the resonance nonlinear scattering such as second-order scattering (SOS) and frequency doubling scattering (FDS). Their maximum SOS and FDS peaks were located at 585 nm (TP-PMZ), 584 nm (TP-CPZ) and 388 nm (TP-PMZ), 329 nm (TP-CPZ), respectively. These results provided some indication for the determination of PMZ and CPZ by SOS and FDS methods. The linear range of TP-PMZ and TP-CPZ systems were 0.0069-2.5 ?g mL -1, 0.102-5.0 ?g mL -1 (SOS) and 0.079-6.0 ?g mL -1, 0.0133-5.0 ?g mL -1 (FDS), respectively. The detection limits (3 ?) of PMZ and CPZ were 2.08 ng mL -1, 3.07 ng mL -1 (SOS) and 2.22 ng mL -1, 3.98 ng mL -1 (FDS), respectively. In this work, the optimum reaction conditions, the influences of coexisting substances and ionic strength and analytical application have been investigated. The methods have been successfully applied to the determination of PMZ and CPZ in tablets. In addition, the composition of ion-association complexes and the reaction mechanism are also discussed.

Chen, Peili; Hu, Xiaoli; Liu, Shaopu; Liu, Zhongfang; Song, Yanqi

2010-09-01

354

Study on the resonance nonlinear scattering spectra of the interactions of promethazine hydrochloride and chlorpromazine hydrochloride with 12-tungstophosphoric acid and their analytical applications.  

PubMed

In pH 1.0 HCl medium, 12-tungstophosphoric acid (TP) reacted with promethazine hydrochloride (PMZ) and chlorpromazine hydrochloride (CPZ) to form ion-association complexes, which led to a great enhancement of the resonance nonlinear scattering such as second-order scattering (SOS) and frequency doubling scattering (FDS). Their maximum SOS and FDS peaks were located at 585 nm (TP-PMZ), 584 nm (TP-CPZ) and 388 nm (TP-PMZ), 329 nm (TP-CPZ), respectively. These results provided some indication for the determination of PMZ and CPZ by SOS and FDS methods. The linear range of TP-PMZ and TP-CPZ systems were 0.0069-2.5 microg mL(-1), 0.102-5.0 microg mL(-1) (SOS) and 0.079-6.0 microg mL(-1), 0.0133-5.0 microg mL(-1) (FDS), respectively. The detection limits (3sigma) of PMZ and CPZ were 2.08 ng mL(-1), 3.07 ng mL(-1) (SOS) and 2.22 ng mL(-1), 3.98 ng mL(-1) (FDS), respectively. In this work, the optimum reaction conditions, the influences of coexisting substances and ionic strength and analytical application have been investigated. The methods have been successfully applied to the determination of PMZ and CPZ in tablets. In addition, the composition of ion-association complexes and the reaction mechanism are also discussed. PMID:20541454

Chen, Peili; Hu, Xiaoli; Liu, Shaopu; Liu, Zhongfang; Song, Yanqi

2010-09-15

355

A Rapid, Stability Indicating RP-UPLC Method for Simultaneous Determination of Ambroxol Hydrochloride, Cetirizine Hydrochloride and Antimicrobial Preservatives in Liquid Pharmaceutical Formulation.  

PubMed

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 ?m (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

Trivedi, Rakshit Kanubhai; Patel, Mukesh C; Jadhav, Sushant B

2011-09-01

356

Comparative study of propranolol hydrochloride release from matrix tablets with KollidonSR or hydroxy propyl methyl cellulose.  

PubMed

The release of propranolol hydrochloride from matrix tablets with hydroxy propyl methyl cellulose (HPMC K15M) or KollidonSR at different concentrations was investigated with a view to developing twice daily sustained release dosage form. A hydrophilic matrix-based tablet using different concentrations of HPMC K15M or KollidonSR was developed using direct compression technique to contain 80 mg of propranolol hydrochloride. The resulting matrix tablets prepared with HPMC K15M or KollidonSR fulfilled all the official requirements of tablet dosage forms. Formulations were evaluated for the release of propranolol hydrochloride over a period of 12 h in pH 6.8 phosphate buffer using USP type II dissolution apparatus. Propranolol hydrochloride and pure KollidonSR or HPMC K15M compatibility interactions was investigated by using Fourier-transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). FTIR spectroscopic and DSC studies revealed that there was no well defined chemical interaction between propranolol hydrochloride with KollidonSR or HPMC K15M. Tablets were exposed to 40 degrees C/75% of RH in open disc for stability. The in vitro drug release study revealed that HPMC K15 at a concentration of 40% of the dosage form weight was able to control the release of propranolol hydrochloride for 12 h, exhibit non-Fickian diffusion with first-order release kinetics where as at 40% KollidonSR same dosage forms show zero-order release kinetics. In conclusion, the in vitro release profile and the mathematical models indicate that release of propranolol hydrochloride can be effectively controlled from a single tablet using HPMC K15M or KollidonSR matrix system. PMID:18459050

Sahoo, J; Murthy, P N; Biswal, S; Sahoo, S K; Mahapatra, A K

2008-01-01

357

Development and Validation of a HPTLC Method for Simultaneous Quantitation of Flunarizine Dihydrochloride and Propranolol Hydrochloride in Capsule Dosage Form  

PubMed Central

A simple, precise, accurate, and rapid high-performance thin layer chromatographic method has been developed and validated for the simultaneous quantitation of flunarizine dihydrochloride and propranolol hydrochloride in a combined capsule dosage form. The method was carried out on precoated silica gel 60 F254 TLC aluminum plate, (20×10 cm2). The solvent system was ethyl acetate:methanol:glacial acetic acid in the proportion of 8:1:1, (v/v/v). Rf value for flunarizine dihydrochloride and propranolol hydrochloride was found to be 0.62±0.02 and 0.18±0.02, respectively. The linearity regression analysis for calibration showed 0.999 and 0.999 for flunarizine dihydrochloride and propranolol hydrochloride with respect to peak area and height in the concentration range of 50-350 ng/spot and 500-3500 ng/spot, respectively. Accuracy of recovery studies was found to be 98-100.28 and 99.11-99.45% for flunarizine dihydrochloride and propranolol hydrochloride, respectively. The amounts of drug in marketed formulation were 100.5 and 101.25% of flunarizine dihydrochloride and propranolol hydrochloride, respectively. The method developed can be used for routine analysis in bulk drug and capsule dosage form. PMID:24082355

Shivarkar, N. A.; Dudhe, P. B.; Nagras, M. A.

2013-01-01

358

RP-HPLC method for simultaneous determination of butenafine hydrochloride and betamethasone dipropionate in a cream formulation.  

PubMed

An RP-HPLC method has been developed for the simultaneous determination of butenafine hydrochloride and betamethasone dipropionate on an Inertsil C18 column (250 x 4.6 mm id) using a mobile phase gradient consisting of methanol and water at a flow rate of 1 mL/min. Detection was carried out at 254 nm. Retention times of betamethasone dipropionate and butenafine hydrochloride were 4.82 (+/- 0.80) and 16.18 (+/- 0.17) min, respectively. The method was validated with respect to specificity, linearity, accuracy, precision, ruggedness, and robustness. This method is simple, precise, and sensitive, and applicable for the simultaneous quantification of butenafine hydrochloride and betamethasone dipropionate in a cream formulation. PMID:21391486

Bhosale, Suryakant D; Rajput, Sadhana J

2011-01-01

359

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

PubMed

In contrast to L-glutamic acid (200 mg/kg), ?-phenylglutamic acid hydrochloride (26 mg/kg) produces no anticonvulsant effects during generalized convulsions induced by "maximum electric shock". However, ?-phenylglutamic acid hydrochloride was more potent than L-glutamic acid in increasing survival rate, promoting recovery of spontaneous motor activity, and maintainance locomotor and exploratory activity in the open field test and cognitive functions in conditioned passive avoidance test, i.e. exhibited neuroprotective activity. This substance did not change the threshold of pain induced by electric stimulation of paws (up to vocalization) and thermal tail stimulation (tail-flick), whereas L-glutamic acid decreased this parameter. ?-Phenylglutamic acid suppressed aggression in the test for provoked unmotivated aggression, while L-glutamic acid enhanced it. Due to these neurotropic effects, ?-phenylglutamic acid hydrochloride can be used as the basis for the development of drugs with antidepressant, anxiolytic, and neuroprotective actions. PMID:24824696

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

2014-04-01

360

Denaverine hydrochloride and carbetocin increased welfare during and after parturition and enhanced subsequent fertility in cattle.  

PubMed

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. PMID:24731624

Zobel, Robert; Taponen, Juhani

2014-06-01

361

Safety, tolerability and pharmacokinetics of phenoprolamine hydrochloride floating sustained-release tablets in healthy Chinese subjects.  

PubMed

The present study was designed to assess the safety, tolerability and pharmacokinetics of phenoprolamine hydrochloride floating sustained tablets (PHFST) in healthy Chinese subjects. 116 volunteers were randomized into single- or multiple-dose groups for oral administration 30-240 mg of PHFST once or 60-120 mg twice daily. Safety and tolerability were appraised by monitoring adverse events and laboratory parameters. Pharmacokinetics was assessed by determining the plasma concentrations of phenoprolamine hydrochloride with a validated HPLC method. In single-dose studies, no severe adverse events were observed in volunteers, and all adverse events were mild; the percentages of treatment-emergent events judged to be possibly related to the drug were 3/6 in the 240 mg dose group, 1/6 in the 180-210 mg dose groups, and none in the 30-150 mg dose groups; system exposure (AUC, C(max)) increased with respect to dose at 30-120 mg, whereas AUC raised disproportionately with dose escalating from 120 to 240 mg; the absorption of phenoprolamine hydrochloride was unaffected by food. In multiple studies, no safety concerns were revealed up to 7 days; steady-state plasma concentration was achieved after approximately 4-5 days of repeated twice-daily dosing. PHFST is safe and well tolerated in healthy Chinese subjects. The mean C(max) of PHFST is proportional to dose, but not the AUC. Oral dosing regimen selected for subsequent Phase II/III clinical trials was 60 mg of PHFST, b.i.d., and dose up to 120 mg, b.i.d. - may be used to achieve better antihypertensive effect. PMID:19446622

Zhao, Libo; Yang, Xiaoyan; Xu, Rong; Wu, Jianhong; Gu, Shifen; Zhang, Li; Gong, Peili; Chen, Hui; Zeng, Fandian

2009-07-30

362

Preparation and in vitro/in vivo evaluation of sustained-release metformin hydrochloride pellets.  

PubMed

In this study, metformin hydrochloride (MH) sustained-release pellets were successfully prepared by centrifugal granulation. Seed cores preparation, drug layering, talc modification and coating of polymeric suspensions were carried out in a centrifugal granulator. Talc modification was performed before coating in order to overcome the high water solubility of metformin. The influence of surface modification by talc, the effects of Eudragit types and ratios, as well as the correlation between in vitro release and in vivo absorption were investigated in detail. Experimental results indicated that talc modification made a decisive contribution to controlling the drug release by avoiding drug dumping. Three dissolution media: 0.1 M HCl, distilled water and pH 6.8 phosphate buffer were employed to determine the in vitro release behaviors of the above metformin hydrochloride pellets. The relative bioavailability of the sustained-release pellets was studied in 12 healthy volunteers after oral administration in a fast state using a commercially available immediate release tablet (Glucophage) as a reference. Following coating with a blend of Eudragit L30D-55 and Eudragit NE30D (1:20), at 7% or 10% coating level, respectively (referred to as F-2, F-3), the pellets acquired perfect sustained-release properties and good relative bioavailability. The Cmax, Tmax and relative bioavailability for F-2 and F-3 coated pellets were 1.21 microg/ml, 6 h, 97.6% and 1.65 microg/ml, 8 h, 165%, respectively. Combined use of two Eudragit polymers with different features as coating materials produced the desired results. Restricted delivery of metformin hydrochloride to the small intestine from differently coated pellets resulted in increased relative bioavailability and a sustained release effect. The adoption of several different pH dissolution media established a better relationship between the in vitro release and in vivo absorption of the sustained-release pellets. PMID:16797948

Hu, Lian-Dong; Liu, Yang; Tang, Xing; Zhang, Qian

2006-10-01

363

[Optimization of the formulation of ranolazine hydrochloride sustained-release tablet and its pharmacokinetics in dogs].  

PubMed

Ranolazine hydrochloride sustained-release tablet (RH-ST) was prepared and its release behavior in vitro was studied. The pharmacokinetic characteristics and bioavailability in six Beagle dogs after oral administration of RH-ST and ranolazine hydrochloride common tablets (RH-CT) as reference were compared. Three kinds of matrix, hydroxypropylmethylcellulose (HPMC K4M), ethylcellulose (EC 100cp) and acrylic resins (Eudragit RL100) were selected as functional excipients to keep ranolazine hydrochloride (RH) release for 12 hours. Through orthogonal designs, the polymers were quantified and the optimized cumulative release profile was obtained. The single oral dose of RH-ST 500 mg and RH-CT 333.3 mg was given to six dogs using a two way crossover design. Plasma levels were determined by LC-MS and the absorption fractions were calculated according to Loo-Riegelman formula. The steady-state concentration of RH in plasma of six dogs and its pharmacokinetics behaviors after continuous oral administration of RH-ST and RH-CT at different time intervals were studied by LC-MS. The steady-state pharmacokinetic parameters were computed by software program BAPP2.0. With the increase of the amount of the matrix, the drug release was decreased. The most important factor influencing drug release is the quantity of HPMC K4M. Drug release within the period (from 0 h to 12 h) fitted well into Higuchi model. The correlation coefficient (r) between the dissolution in vitro in release media of the distilled water and the absorptin fraction in vivo was 0.9550. To compare with RH-CT, RH-ST in vivo has a steady and slow release behavior, Tmax was obviously delayed (3.00 +/- 0.50) h and the relative bioavailability was over 80 percentage. The combined use of multiple polymers can decrease the tablet weight effectively, and the drug release rate can be decreased both in vitro and in vivo. PMID:21351575

Li, Chang-jun; Yu, Yan-ling; Yang, Qing-min; Li, Ying; Zhang, Yu-hong; Wang, Jing-yi

2010-09-01

364

Hydrogen bonds in the crystal packings of mesalazine and mesalazine hydrochloride  

NASA Astrophysics Data System (ADS)

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, ? = 94.38(2)°, V = 648.7(8) Å3, Z = 4, Dc = 1.568 g cm -3 and ?( MoK?) = 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, ? = 81.329(3)°, ? = 88.026(3)°, ? = 79.317(4)°, V = 395.74(3) Å3, Z = 2, Dc = 1.591 g cm -3 and ?(CuK ?) = 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.

Bani?-Tomiši?, Z.; Koji?-Prodi?, B.; Širola, I.

1997-10-01

365

Evaluation of metomidate hydrochloride as an anesthetic in leopard frogs (Rana pipiens).  

PubMed

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

Doss, Grayson A; Nevarez, Javier G; Fowlkes, Natalie; da Cunha, Anderson F

2014-03-01

366

X-ray crystal structure of the antimalarial agent (-)-halofantrine hydrochloride supports stereospecificity for cardiotoxicity.  

PubMed Central

The crystal and molecular structures and absolute configuration of (-)-halofantrine hydrochloride were determined by X-ray diffraction. The absolute configuration of the single chiral center of (-)-halofantrine was established to be in the S configuration. Thus, (+)-halofantrine, the more cardiotoxic isomer, has the R configuration. The carbon atom adjacent to the aromatic ring has the same configuration in both (+)- halofantrine and quinidine, suggesting a stereospecific component to the cardiotoxicity produced by both agents. The intramolecular N ... O distance is 4.177 +/- 0.006 A (1 A = 0.1 nm), which is close to the N ... O distance found in the crystal structure of (+/-)-halofantrine hydrochloride, even though the N-H group points in opposite directions in racemic halofantrine and (-)-halofantrine. Both the hydroxyl group and the amine group form hydrogen bonds with the chloride anions. The crystallographic parameters for (-)-halofantrine hydrochloride were as follows: chemical formula, C26H31Cl2F6NO+. Cl-; Mr, 492.4; symmetry of unit cell, orthorhombic; space group, P2(1)2(1)2(1); parameters of unit cell, a was 6.290 +/- 0.001 A, b was 13.533 +/- 0.003 A, and c was 30.936 +/- 0.006 A; volume of the unit cell, 2,633.2 +/- 0.7 A(3); number of molecules per unit cell, 4; calculated density, 1.354 g cm(-3); source of radiation, Cu K(alpha) (lambda = 1.54178 A); mu (absorption coefficient), 3.50 mm(-1); F(000) (sum of atomic scattering factors at zero scattering angle), 1,120; room temperature was used; final R (residual index), 4.75% for 2,988 reflections, with absolute value of Fo > 3sigma(F), where Fo is the observed structure factor and F is the structure factor. PMID:9087491

Karle, J M

1997-01-01

367

"Tetracycline hydrochloride chemical burn" as self-inflicted mucogingival injury: A rare case report  

PubMed Central

Injuries to oral soft tissue can be accidental, iatrogenic, and factitious trauma. Chemical, thermal, and physical agents are the main causative agents for oral soft-tissue burns. The present case describes the chemical burn of oral mucosa caused by tetracycline hydrochloride and its management. Diagnosis was made on the basis of definitive history elicited from the patient. The early detection of the lesion by the patient and immediate institution of therapeutic measures ensure a rapid cure and possible prevention of further mucogingival damage. In addition, we believe that proper guidance and education of the patient is an important prophylactic measure in preventing this self-inflicting injury. PMID:23055601

Dayakar, Mundoor Manjunath; Pai, Prakash G.; Madhavan, Sanupa S.

2012-01-01

368

Validated LC Method, with a Chiral Mobile Phase, for Separation of the Isomers of Fexofenadine Hydrochloride  

Microsoft Academic Search

A high-performance liquid chromatographic method has been developed for resolution of the structural isomers of fexofenadine\\u000a hydrochloride in the bulk drug. The isomers were resolved to baseline on a reversed-phase ODS column with pH 3 aqueous buffer–acetonitrile\\u000a 60:40 containing 5 g L?1 ?-cyclodextrin as mobile phase additive. The aqueous buffer was prepared by dissolving 6.8 g KH2PO4 in 1,000 mL water and adjusting to the

Arvind A. Sakalgaonkar; Sunil R. Mirgane; R. P. Pawar

2008-01-01

369

In vitro release study of verapamil hydrochloride through sodium alginate interpenetrating monolithic membranes.  

PubMed

Polymeric sodium alginate interpenetrating network membranes containing verapamil hydrochloride were fabricated for transdermal application. The membranes were evaluated for their physical properties, weight and thickness uniformity, water vapor transmission, as well as drug content uniformity. All the thin patches were transparent, smooth, and flexible. The drug-loaded membranes were analyzed by X-ray diffraction to understand the drug polymorphism inside the membrane. The transdermal patches were permeable to water vapor, indicating the permeability characteristics of the polymers. The in vitro drug release was performed in distilled water using a Keshary-Chien diffusion cell. The release data were analyzed to understand the mechanism of drug release. PMID:11794813

Kurkuri, M D; Kulkarni, A R; Kariduraganavar, M Y; Aminabhavi, T M

2001-11-01

370

Molecular structure, hydrogen bonding, basicity and spectroscopic properties of 3-hydroxypyridine betaine hydrochloride monohydrate  

Microsoft Academic Search

The effect of hydrogen bonding, inter- and intramolecular electrostatic interactions on the structure of 3-hydroxy-pyridine betaine hydrochloride monohydrate (1-carboxymethyl-3-hydroxypyridinium chloride monohydrate), 3-HO-PBH·Cl·H2O, has been studied by X-ray diffraction, 1H and 13C NMR and FTIR spectroscopies, and by the B3LYP\\/6-31G(d,p) calculations. In the crystal, the Cl? anion is connected with protonated betaine via the hydrogen bond, OCOH?Cl?=2.993(2) Å and with neighboring

P. Barczynski; A. Komasa; A. Katrusiak; Z. Dega-Szafran; M. Szafran

2007-01-01

371

X-ray radiation of poly-L-arginine hydrochloride and multilayered DNA-coatings  

NASA Astrophysics Data System (ADS)

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.

Stypczy?ska, Agnieszka; Nixon, Tony; Mason, Nigel

2014-11-01

372

Physical chemical characterization of binary systems of prilocaine hydrochloride with triacetyl-?-cyclodextrin  

Microsoft Academic Search

Interaction products of prilocaine hydrochloride (PRL), a local anesthetic agent highly soluble in water, with triacetyl-?-cyclodextrin\\u000a (TA?CD), a hydrophobic CD derivative practically insoluble in water, were prepared to estimate their suitability for the development\\u000a of a prolonged-release dosage form of the drug. Equimolar PRL-TA?CD solid systems were prepared by different methods (physical\\u000a mixing, kneading, co-grinding, sealed-heating, coevaporation, spray-drying), in order

Marco Bragagni; Francesca Maestrelli; Paola Mura

2010-01-01

373

Melt-in-Mouth Pellets of Fexofenadine Hydrochloride Using Crospovidone as an Extrusion–Spheronisation Aid  

Microsoft Academic Search

Microcrystalline cellulose (MCC) is well established as an extrusion spheronisation aid for the preparation of pellets. Crospovidone\\u000a (Polyplasdone® XL-10) is compared with microcrystalline cellulose for the preparation of melt-in-mouth pellets. Taste-masked\\u000a fexofenadine hydrochloride was incorporated in the melt-in-mouth formulation. Crospovidone was found to be well suited as\\u000a extrusion–spheronisation aid for the preparation of melt-in-mouth pellets. The great advantage of crospovidone

Satishkumar P. Jain; Dharmini C. Mehta; Sejal P. Shah; Pirthi Pal Singh; Purnima D. Amin

2010-01-01

374

Intake of ethanol, sodium chloride, sucrose, citric acid, and quinine hydrochloride solutions by mice: A genetic analysis  

Microsoft Academic Search

Mice of the 129\\/J (129) and C57BL\\/6ByJ (B6) strains and their reciprocal F1 and F2 hybrids were offered solutions of ethanol, sucrose, citric acid, quinine hydrochloride, and NaCl in two-bottle choice tests.\\u000a Consistent with earlier work, the B6 mice drank more ethanol, sucrose, citric acid, and quinine hydrochloride solution and\\u000a less NaCl solution than did 129 mice. Analyses of each

A. A. Bachmanov; D. R. Reed; M. G. Tordoff; R. A. Price; G. K. Beauchamp

1996-01-01

375

Crystal and molecular structure of quinuclidine betaine hydrochloride studied by X-ray diffraction, DFT, FTIR, and NMR methods  

Microsoft Academic Search

Quinuclidine betaine hydrochloride (1-carboxymethyl-1-azabicyclo[2.2.2]octane hydrochloride, QNBH·Cl) has been synthesized and characterized by X-ray diffraction, FTIR and NMR spectroscopy, and DFT calculations. QNBH·Cl crystallizes in orthorhombic space group Pnma. In the crystal the Cl? anion is engaged in a medium–strong COOH·Cl hydrogen bond of 2.921(2)Å, in which the acidic proton is closer the carboxylate group and additionally in some C–H···Cl contacts,

Z. Dega-Szafran; A. Katrusiak; M. Szafran

2009-01-01

376

Interaction of cyproheptadine hydrochloride with human serum albumin using spectroscopy and molecular modeling methods.  

PubMed

The interaction between cyproheptadine hydrochloride (CYP) and human serum albumin (HSA) was investigated by fluorescence spectroscopy, UV-vis absorption spectroscopy, Fourier transform infrared spectroscopy (FT-IR) and molecular modeling at a physiological pH (7.40). Fluorescence of HSA was quenched remarkably by CYP and the quenching mechanism was considered as static quenching since it formed a complex. The association constants Ka and number of binding sites n were calculated at different temperatures. According to Förster's theory of non-radiation energy transfer, the distance r between donor (human serum albumin) and acceptor (cyproheptadine hydrochloride) was obtained. The effect of common ions on the binding constant was also investigated. The effect of CYP on the conformation of HSA was analyzed using FT-IR, synchronous fluorescence spectroscopy and 3D fluorescence spectra. The thermodynamic parameters ?H and ?S were calculated to be -14.37 kJ mol(-1) and 38.03 J mol(-1) K(-1), respectively, which suggested that hydrophobic forces played a major role in stabilizing the HSA-CYP complex. In addition, examination of molecular modeling indicated that CYP could bind to site I of HSA and that hydrophobic interaction was the major acting force, which was in agreement with binding mode studies. PMID:22605685

Jiang, Hua; Chen, Rongrong; Wang, Hongcui; Pu, Hanlin

2013-01-01

377

Simultaneous chemometric determination of pyridoxine hydrochloride and isoniazid in tablets by multivariate regression methods.  

PubMed

The sole use of pyridoxine hydrochloride during treatment of tuberculosis gives rise to pyridoxine deficiency. Therefore, a combination of pyridoxine hydrochloride and isoniazid is used in pharmaceutical dosage form in tuberculosis treatment to reduce this side effect. In this study, two chemometric methods, partial least squares (PLS) and principal component regression (PCR), were applied to the simultaneous determination of pyridoxine (PYR) and isoniazid (ISO) in their tablets. A concentration training set comprising binary mixtures of PYR and ISO consisting of 20 different combinations were randomly prepared in 0.1 M HCl. Both multivariate calibration models were constructed using the relationships between the concentration data set (concentration data matrix) and absorbance data matrix in the spectral region 200-330 nm. The accuracy and the precision of the proposed chemometric methods were validated by analyzing synthetic mixtures containing the investigated drugs. The recovery results obtained by applying PCR and PLS calibrations to the artificial mixtures were found between 100.0 and 100.7%. Satisfactory results obtained by applying the PLS and PCR methods to both artificial and commercial samples were obtained. The results obtained in this manuscript strongly encourage us to use them for the quality control and the routine analysis of the marketing tablets containing PYR and ISO drugs. PMID:20645279

Dinç, Erdal; Ustünda?, Ozgür; Baleanu, Dumitru

2010-08-01

378

Formulation and Characterization of Patient-Friendly Dosage Form of Ondansetron Hydrochloride  

PubMed Central

Ondansetron hydrochloride is an intensely bitter antiemetic drug used to treat nausea and vomiting following chemotherapy. The purpose of the present work was to mask the taste of ondansetron hydrochloride and to formulate its patient-friendly dosage form. Complexation technique using indion 234 (polycyclic potassium with carboxylic functionality) and an ion-exchange resin was used to mask the bitter taste and then the taste-masked drug was formulated into an orodispersible tablet (ODT). The drug loading onto the ion-exchange resin was optimized for mixing time, activation, effect of pH, mode of mixing, ratio of drug to resin and temperature. The resinate was evaluated for taste masking and characterized by X-ray diffraction study and infrared spectroscopy. ODTs were formulated using the drug–resin complex. The developed tablets were evaluated for hardness, friability, drug content, weight variation, content uniformity, friability, water absorption ratio, in vitro and in vivo disintegration time and in vitro drug release. The tablets disintegrated in vitro and in vivo within 24 and 27 s, respectively. Drug release from the tablet was completed within 2 min. The obtained results revealed that ondansetron HCl has been successfully taste masked and formulated into an ODT as a suitable alternative to the conventional tablets. PMID:21042478

Bhoyar, PK; Biyani, DM; Umekar, MJ

2010-01-01

379

Lyophilized Chitosan/xanthan Polyelectrolyte Complex Based Mucoadhesive Inserts for Nasal Delivery of Promethazine Hydrochloride.  

PubMed

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 3(2) 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

G Dehghan, Mohamed Hassan; Marzuka, Marzuka

2014-01-01

380

Development of a Floating Dosage Form of Ranitidine Hydrochloride by Statistical Optimization Technique  

PubMed Central

The objective of this study was to evaluate the effect of formulation variables on the release properties, floating lag time, and hardness, when developing floating tablets of Ranitidine hydrochloride, by the statistical optimization technique. The formulations were prepared based on 32 factorial design, with polymer ratio (HPMC 100 KM: Xanthan gum) and the amount of aerosil, as two independent formulation variables. The four dependent (response) variables considered were: percentage of drug release at the first hour, T50% (time taken to release 50% of the drug), floating lag time, and hardness of the tablet. The release profile data was subjected to a curve fitting analysis, to describe the release mechanism of the drug from the floating tablet. An increase in drug release was observed with an increase in the polymer ratio, and as the amount of aerosil increased, the hardness of the tablet also increased, without causing any change in the floating lag time. The desirability function was used to optimize the response variables, each having a different target, and the observed responses were in accordance with the experimental values. The results demonstrate the feasibility of the model in the development of floating tablets containing Ranitidine hydrochloride. PMID:21264091

Jain, S; Srinath, MS; Narendra, C; Reddy, SN; Sindhu, A

2010-01-01

381

A thermodynamic study of the amphiphilic phenothiazine drug thioridazine hydrochloride in water/ethanol solvent  

NASA Astrophysics Data System (ADS)

The thermodynamic properties of aqueous solutions of the tricyclic antidepressant amphiphilic phenothiazine drug thioridazine hydrochloride in the temperature range 20-50 °C and in the presence of ethanol have been measured. The phenothiazine tranquillizing drugs have interesting association characteristics that derive from their rigid, tricyclic hydrophobic groups. Thioridazine hydrochloride is a drug used in treatment of mental illness that shows side effects. Therefore, it is interesting to study the change of its physico-chemical properties with temperature and with the surrounding environment to understand the action mechanism of the drug. Densities, conductivities, and surface tension were measured to obtain surface and bulk solution properties. Critical concentrations, cc, at different temperatures and in the presence of ethanol, and partition coefficients, K, have been calculated, the latter using an indirect method based in the pseudophase model with the help of apparent molar volume data. This method has the advantage that allows calculating the distribution coefficients at solubilizate concentrations below the saturation. Conductivity data show two critical concentrations. The second critical concentration is not clear by density data. The effect of the alcohol is to decrease the first critical concentration due to a decrease in headgroup repulsion. The molar apparent volumes at infinite dilution and in the aggregate in water and in presence of ethanol have been also obtained.

Cheema, Mohammad Arif; Barbosa, Silvia; Taboada, Pablo; Castro, Emilio; Siddiq, Mohammad; Mosquera, Víctor

2006-09-01

382

Formulation and evaluation of a gastroretentive dosage form of labetalol hydrochloride.  

PubMed

Labetalol hydrochloride (LBT), 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl) amino] ethyl]-benzamide, a non-selective alpha, beta-adrenoceptor antagonist is used in the treatment of hypertension. It shows variable bioavailability ranging from 10-80% which may be attributed to its minimum solubility in pH range 6 to 10, the pH conditions prevailing at the major site of absorption i.e. small intestine. Also due to its half life of 3 to 6 hrs it is administered twice daily. In the present work non-effervescent sustained release gastroretentive floating tablets of labetalol hydrochloride have been developed using various grades of HPMC and Poloxamer M127 as wetting agent. The tablets were evaluated for in vitro drug release, floating time, floating lag time, swelling studies etc. The tablets formulated with HPMC K4M CR and HPMC K15M CR along with Poloxamer showed negligible floating lag time with a total floating time over 12 hrs with complete release. Formulation was optimized using Stat-Ease Design Expert 7.1 software. Optimized batch was evaluated for the effect of change of osmolarity and pH on drug release, floating and swelling behaviour. PMID:20361305

Garse, Harshal; Vij, Mohit; Yamgar, Manohar; Kadam, Vilasrao; Hirlekar, Rajashree

2010-03-01

383

Development and optimization of a novel sustained-release dextran tablet formulation for propranolol hydrochloride.  

PubMed

A novel oral controlled delivery system for propranolol hydrochloride (PPL) was developed and optimized. The in vitro dissolution profiles of sustained-release matrix tablets of racemic PPL were determined and compared with the United States Pharmacopeia (USP) tolerance specifications for Propranolol Hydrochloride Extended-Release Capsules. The influence of matrix forming agents (native dextran, hydroxypropyl methylcellulose (HPMC), cetyl alcohol) and binary mixtures of them on PPL release in vitro was investigated. A central composite design was applied to the optimization of a sustained-release tablet formulation. The sustained-release matrix tablets with good physical, mechanical and technological properties were obtained with a matrix excipient:PPL ratio of 60:40 (w/w), with a dextran:HPMC ratio of 4:1 (w/w) and with a cetyl alcohol amount of 15% (w/w). A comparative kinetic study of the present matrix tablets and commercial SUMIAL RETARD capsules (Spain) was established. The value for the similarity factor (f(2)=69.6) suggested that the dissolution profile of the present two sustained-release oral dosage forms are similar. Higuchi (diffusion) and Hixon-Crowell (erosion) kinetic profiles were achieved and this codependent mechanism of drug release was established. PMID:16584856

Gil, Eddy Castellanos; Colarte, Antonio Iraizoz; Bataille, Bernard; Pedraz, José Luis; Rodríguez, Fernand; Heinämäki, Jyrki

2006-07-01

384

Design and evaluation of 1- and 3-layer matrices of verapamil hydrochloride for sustaining its release.  

PubMed

The present study was performed to design oral controlled delivery systems for the water-soluble drug, verapamil hydrochloride, using natural and semisynthetic polymers as carriers in the forms of 1- and 3-layer matrix tablets. Verapamil hydrochloride 1-layer matrix tablets containing hydroxypropylmethylcellulose, tragacanth, and acacia either alone or mixed were prepared by direct compression technique. 3-layer matrix tablets were prepared by compressing the polymers as release retardant layers on both sides of the core containing the drug. The prepared tablets were subjected to in vitro drug release studies. Tragacanth when used as the carrier in the formulation of 1- and 3-layer matrices produced satisfactory release prolongation either alone or in combination with the other 2 polymers. On the other hand, acacia did not show enough prolonging efficiency in 1- and 3-layer matrix tablets. The results also showed that the location of the polymers in the 3-layer tablets has a pronounced effect on the drug release. Kinetic analysis of drug release from matrices exhibiting sustained release indicated that release was predominantly attributable to the contribution made by Fickian diffusion, while the erosion/relaxation mechanisms had a minor role in the release. PMID:16408864

Siahi, Mohammad Reza; Barzegar-Jalali, Mohammad; Monajjemzadeh, Farnaz; Ghaffari, Fatemeh; Azarmi, Shirzad

2005-01-01

385

Testing lyoequivalency for three commercially sustained-release tablets containing diltiazem hydrochloride.  

PubMed

In vitro release kinetics of three commercially available sustained release tablets (SR) diltiazem hydrochloride were studied at pH 1.1 for 2 h and for another 6 h at pH 6.8 using the USP dissolution apparatus with the paddle assemble. The kinetics of the dissolution process was studied by analyzing the dissolution data using five kinetic equations: the zero-order equation, the first-order equation, the Higuchi square root equation, the Hixson-Crowell cube root law and the Peppas equation. Analyses of the dissolution kinetic data for diltiazem hydrochloride commercial SR tablets showed that both Dilzacard and Dilzem SR tablets released drug by Non-Fickian (Anomalous transport) release with release exponent (n) equal to 0.59 and 0.54, respectively, which indicate the summation of both diffusion and dissolution controlled drug release. Bi-Tildiem SR tablets released drug by super case II (n = 1.29) which indicate zero-order release due to the dissolution of polymeric matrix and relaxation of the polymer chain. This finding was also in agreement with results obtained from application of zero-order and Hixson-Crowell equations. A dissolution profile comparative study was done to test the lyoequivelancy of the three products by using the mean dissolution time (MDT), dissimilarity factor f1 and similarity factor f2. Results showed that the three products are different and not lyoequivalent. PMID:20210085

Maswadeh, Hamzah A; Al-Hanbali, Othman A; Kanaan, Reem A; Shakya, Ashok K; Maraqa, Anwar

2010-01-01

386

Evaluating tamsulosin hydrochloride-released microparticles prepared using single-step matrix coating.  

PubMed

The objective of the present study was to determine the optimum composition for sustained-release of tamsulosin hydrochloride from microparticles intended for orally disintegrating tablets. Microparticles were prepared from an aqueous ethylcellulose dispersion (Aquacoa®), and an aqueous copolymer based on ethyl acrylate and methyl methacrylate dispersion (Eudragit®) NE30D), with microcrystalline cellulose as core particles with a fluidized bed coating process. Prepared microparticles were about 200 ?m diameter and spherical. The microparticles were evaluated for in vitro drug release and in vivo absorption to assess bioequivalence in a commercial product, Harnal® pellets. The optimum ratio of Aquacoat® and Eudragit® NE30D in the matrix was 9:1. We observed similar drug release profiles in microparticles and Harnal® pellets. Higuchi model analysis of the in vitro drug release from microparticles was linear up to 80% release, typical of Fickian diffusion sustained-release profile. The in vivo absorption properties from microparticles were comparable to Harnal® pellets, and there was a linear relationship between in vitro drug release and in vivo drug release. In conclusion, this development produces microparticles in single-step coating, that provided a sustained-release of tamsulosin hydrochloride comparable to Harnal® pellets. PMID:21291970

Maeda, Atsushi; Shinoda, Tatsuki; Ito, Naoki; Baba, Keizo; Oku, Naoto; Mizumoto, Takao

2011-04-15

387

Preparation and evaluation of a novel delayed-onset sustained-release system of propranolol hydrochloride.  

PubMed

The objective of this work was to prepare and evaluate a new delayed-onset sustained-release system, comprising a sustained-release core tablet with hydroxypropyl methylcellulose as polymer matrix and an ethylcellulose/Eudragit L coating capable of delaying the drug release. The sustained core containing propranolol hydrochloride as the model drug was prepared by granulate tableting and the polymer coating was applied in a computer-controlled coating pan. The dissolution tests demonstrated that the in-vitro drug release was pH-dependent with sufficient gastric resistance, and the lag time (t(10%)) could be controlled by adjusting the coating level. Three dosage forms including commercial tablet, sustained-release tablet and the delayed-onset sustained-release tablet were administrated to six beagle dogs and the plasma levels of propranolol hydrochloride were measured with high-performance liquid chromatography. The delayed-onset sustained-release tablet had a lag time of 3.0 h in-vitro and 3.5 h in-vivo, and a t(max) of 7.0 h. The relative bioavailability for delayed-onset sustained-release tablet was 96.98% compared with commercial tablets. The results indicate that the new propranolol delayed-onset sustained-release system could achieve a relatively constant drug release followed by a programmed lag time, and this may provide a promising drug delivery form for chronopharmacotherapy of certain cardiovascular diseases. PMID:18549667

Feng, Xue-mei; Ren, Qi; Zhang, Wen-zhi; Shen, Hui-feng; Rong, Zheng-xing; Fang, Chao; Chen, Hong-zhuan

2008-07-01

388

Role of 1-methyl-3-octylimidazolium chloride in the micellization behavior of amphiphilic drug amitriptyline hydrochloride.  

PubMed

The mixed micellization behaviour of amitriptyline hydrochloride (AMT) with ionic liquid (IL) 1-methyl-3-octylimidazolium hydrochloride, [C8mim][Cl], have been investigated using electrical conductivity, at different temperatures. The non-ideal behaviour (i.e., synergistic interaction) of AMT-[C8mim][Cl] binary mixtures, explained by the deviations in critical micelle concentration (cmc) from ideal critical micelle concentration (cmc*) and micellar mole fraction (X(m)) from ideal micellar mole fraction (X(ideal)) values. The values of interaction parameter (?) and activity coefficients (f1 and f2), also confirm the synergistic interaction. The excess free energy (?Gex) for the AMT-[C8mim][Cl] binary mixtures explains, stability of mixed micelles in comparison to micelles of pure, AMT and [C8mim][Cl]. The calculated thermodynamic parameters (viz., the standard Gibbs energy change, ?Gm(?), the standard enthalpy change, ?Hm(?), the standard entropy change, ?Sm(?)), suggest the dehydration of hydrophobic part of the drug at higher temperatures (>313K), not only in case of AMT but also in the presence of [C8mim][Cl]. PMID:24077084

Khan, Abbul Bashar; Ali, Maroof; Malik, Nisar Ahmad; Ali, Anwar; Patel, Rajan

2013-12-01

389

Stability-indicating spectrofluorimetric method for determination of itopride hydrochloride in raw material and pharmaceutical formulations.  

PubMed

A simple, sensitive and rapid spectrofluorimetric method for determination of itopride hydrochloride in raw material and tablets has been developed. The proposed method is based on the measurement of the native fluorescence of the drug in water at 363 nm after excitation at 255 nm. The relative fluorescence intensity-concentration plot was rectilinear over the range of 0.1-2 ?g/mL (2.5?×?10(-7)-5.06?×?10(-6) mole/L), with good correlation (r?=?0.9999), limit of detection of 0.015 ?g/mL and a lower limit of quantification of 0.045 ?g/mL. The described method was successfully applied for the determination of itopride hydrochloride in its commercial tablets with average percentage recovery of 100.11?±?0.32 without interference from common excipients. Additionally, the proposed method can be applied for determination of itopride in combined tablets with rabeprazole or pantoprazole without prior separation. The method was extended to stability study of itopride. The drug was exposed to acidic, alkaline, oxidative and photolytic degradation according to ICH guidelines. Moreover, the method was utilized to investigate the kinetics of the alkaline, acidic and oxidative degradation of the drug. A proposal for the degradation pathways was postulated. PMID:23852162

Walash, Mohamed I; Ibrahim, Fawzia; Eid, Manal I; El Abass, Samah Abo

2013-11-01

390

Effect of thiamine hydrochloride on the redox reactions of iron at pyrite surface  

SciTech Connect

The present investigation is a part of our studies on the electro chemical aspects of pyrite bioleaching involving Thiobacillus ferrooxidans. Previously (1,2) we have examined the effect of T. ferrooxidans and their metabolic products on the redox reactions of Fe[sup 2+]/Fe[sup 3+] couple at the pyrite surface. Results obtained suggest that beyond 1. 5 days during their growth in a batch fermenter, the bacteria and their metabolic products completely cover the pyrite surface and shut down all electron transfer across the electrode-solution interface. In addition, it has been observed that the bacteria serve as the nucleation site for jarosite formation, which is found detrimental to bioleaching. In the present work we have focussed on the effect of the presence of vitamins on the redox chemistry of iron. Our examination of the effect of the presence of thiamine hydrochloride in the redox behavior of Fe[sup 2+]/Fe[sup 3+] at the pyrite surface has revealed that thiamine hydrochloride does not undergo chemical interaction with ferrous or ferric iron. However, it may adsorb onto the pyrite surface causing polarization of the pyrite electrode.

Pesic, B.; Oliver, D.J.

1990-01-01

391

Lyophilized Chitosan/xanthan Polyelectrolyte Complex Based Mucoadhesive Inserts for Nasal Delivery of Promethazine Hydrochloride  

PubMed Central

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.

G Dehghan, Mohamed Hassan; Marzuka, Marzuka

2014-01-01

392

Effect of guanidine hydrochloride on removal rate selectivity and wafer topography modification in barrier CMP  

NASA Astrophysics Data System (ADS)

We propose an alkaline barrier slurry containing guanidine hydrochloride (GH) and hydrogen peroxide. The slurry does not contain any corrosion inhibitors, such as benzotriazole (BTA). 3-inch samples of tantalum copper and oxide were polished to observe the removal rate. The effect of GH on removal rate selectivity along with hydrogen peroxide was investigated by comparing slurry containing GH and H2O2 with slurry containing only GH. Details about the tantalum polishing mechanism in an alkaline guanidine-based slurry and the electrochemical reactions are discussed. The results show that guanidine hydrochloride can increase the tantalum polishing rate and the selectivity of copper and barrier materials. The variation of the dishing and wire line resistance with the polishing time was measured. The dishing value after a 300 mm pattern wafer polishing suggests that the slurry has an effective performance in topography modification. The result obtained from the copper wire line resistance test reveals that the wire line in the trench has a low copper loss.

Hailong, Li; Jin, Kang; Yuling, Liu; Chenwei, Wang; Hong, Liu; Jiaojiao, Gao

2014-03-01

393

UPLC and LC-MS studies on degradation behavior of irinotecan hydrochloride and development of a validated stability-indicating ultra-performance liquid chromatographic method for determination of irinotecan hydrochloride and its impurities in pharmaceutical dosage forms.  

PubMed

The objective of the current investigation was to study the degradation behavior of irinotecan hydrochloride under different International Conference on Harmonization (ICH) recommended stress conditions using ultra-performance liquid chromatography and liquid chromatography-mass spectrometry and to establish a validated stability-indicating reverse-phase ultra-performance liquid chromatographic method for the quantitative determination of irinotecan hydrochloride and its seven impurities and degradation products in pharmaceutical dosage forms. Irinotecan hydrochloride was subjected to the stress conditions of oxidative, acid, base, hydrolytic, thermal and photolytic degradation. Irinotecan hydrochloride was found to degrade significantly in oxidative and base hydrolysis and photolytic degradation conditions. The degradation products were well resolved from the main peak and its impurities, thus proving the stability-indicating power of the method. Chromatographic separation was achieved on a Waters Acquity BEH C8 (100 × 2.1 mm) 1.7-µm column with a mobile phase containing a gradient mixture of solvent A (0.02M KH(2)PO(4) buffer, pH 3.4) and solvent B (a mixture of acetonitrile and methanol in the ratio of 62:38 v/v). The mobile phase was delivered at a flow rate of 0.3 mL/min with ultraviolet detection at 220 nm. The run time was 8 min, within which irinotecan and its seven impurities and degradation products were satisfactorily separated. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision and robustness. This method was also suitable for the assay determination of irinotecan hydrochloride in pharmaceutical dosage forms. PMID:22661461

Kumar, Navneet; Sangeetha, Dhanaraj; Reddy, Sunil P

2012-10-01

394

I2-catalyzed oxidative cross-coupling of methyl ketones and benzamidines hydrochloride: a facile access to ?-ketoimides.  

PubMed

An iodine-catalyzed oxidative cross-coupling of C-H/N-H has been demonstrated. This simple and efficient approach constructed ?-ketoimides in good to excellent yields from methyl ketones and benzamidines hydrochloride under metal-free and peroxide-free conditions. This synthetic strategy was achieved via an in situ iodination-based oxidative coupling pathway. PMID:24831723

Wu, Xia; Gao, Qinghe; Liu, Shan; Wu, Anxin

2014-06-01

395

SIMULTANEOUS DETERMINATION OF PARACETAMOL, PSEUDOEPHEDRINE HYDROCHLORIDE, AND DEXTROMETHORPHAN HYDROBROMIDE IN TABLETS USING MULTIVARIATE CALIBRATION METHODS COUPLED WITH HPLC-DAD  

Microsoft Academic Search

A new method using high performance liguid chromatography (HPLC) with diode array detection (DAD) was developed and validated for the simultaneous determination of paracetamol (PAR), pseudoephedrine hydrochloride (PSE), and dextromethorphan hydrobromide (DEX) in tablets. The spectrochromatograms of these compounds give the severely overlapping spectrochromatogram. This makes the use of univariate calibration impossible. Therefore, PLS and PCR were used to analyze

Bürge A?ç?; Özlem Aksu Dönmez; Abdürrezzak Bozdo?an; S?d?ka Sungur

2011-01-01

396

An EPR study of the transfer and trapping of holes produced by radiation in guanine(thioguanine) hydrochloride single crystals.  

PubMed

Single crystals of guanine hydrochloride monohydrate, guanine hydrochloride dihydrate and anhydrous guanine dihydrochloride, doped with thioguanine, were irradiated with X and gamma rays. In all three systems the dominant radicals were associated with thioguanine. In the former two systems the stabilized species is the thiyl radical, formed by initial loss of an electron at some of the guanines in the crystal lattice, followed by hole migration to thioguanine and subsequent deprotonation of the radical formed. In the anhydrous guanine(thioguanine) dihydrochloride, that process is followed by acquisition of a chlorine ion. In the guanine hydrochloride monohydrate and guanine hydrochloride dihydrate lattices, systems of interacting closely spaced stacked bases and strings of chloride ions might support the migration of electrons and/or holes. In anhydrous guanine dihydrochloride, neither the bases nor the Cl- ions alone are capable of providing the means for the long-range electron, energy and spin transfer. It is the interchangeable sequence of the charged bases and the Cl- ions that makes the supporting strings or networks. The ultimate chlorination of the thioguanine-centered electron-loss radicals depends mainly on the availability of the Cl- ions and the space for their accommodation in the vicinity of the sulfur atom. PMID:10073670

Herak, J N; Sankovi?, K; Krilov, D; Hüttermann, J

1999-03-01

397

The effect of palonosetron hydrochloride in the prevention of chemotherapy-induced moderate and severe nausea and vomiting  

PubMed Central

The current study aimed to evaluate the efficacy and safety of palonosetron hydrochloride injection for preventing chemotherapy-induced moderate and severe nausea and vomiting. A multi-centered, randomly stratified, double-blind, double-dummy, parallel-group and positive-controlled trial was performed. A total of 240 patients who underwent chemotherapy treatment which induced moderate or severe vomiting were divided into the experimental and control groups. Half an hour before chemotherapy, the experimental group received a 0.25-mg palonosetron hydrochloride injection, whereas the control group received a 3-mg granisetron injection. The acute vomiting complete remission rate (CRR) of the experimental group was not significantly different compared with that of the control group (P=0.35). The delayed vomiting CRR of the experimental group was significantly higher compared with that of the control group (P=0.002). No difference in full course vomiting CRR, vomiting control time, treatment failure time or acute nausea CRR was identified between the two groups. No significant differences in adverse events were observed between the experimental group and the control group. No significant differences in adverse reactions occurred between the experimental group and the control group (12.50%). Palonosetron hydrochloride injection had a better effect on delayed vomiting CRR than granisetron hydrochloride injection. The two injections exhibited similar effects on acute vomiting CRR, full course vomiting CRR, vomiting control time, treatment failure time (days), acute nausea CRR and adverse events. PMID:23737892

HUANG, JIAN; WANG, XIAO-JIA; YU, DING; JIN, YE-NING; ZHEN, LEI-ZHEN; XU, NONG; LIU, WEI; DENG, YONG-CHUAN; WU, SHI-XIU; HE, JIA

2013-01-01

398

In vitro Release Kinetics Study of Ambroxol Hydrochloride Pellets Developed by Extrusion Spheronization Technique Followed by Acrylic Polymer Coating  

Microsoft Academic Search

The aim of the present study was to investigate the effect of Ammonio Methacrylate Copolymer Dispersion Type A (Eudragit RL 30 D) and Ammonio Methacrylate Copolymer Dispersion Type B (Eudragit RS 30 D) combination in different weight ratios on the release kinetics of Ambroxol Hydrochloride from coated pellets. Microcrystalline cellulose, lactose, maize starch, hydroxypropyl methylcellulose and the drug was incorporated

Ishtiaq Ahmed; Monzurul Amin Roni; Golam Kibria; Muhammad Rashedul Islam; Reza-ul Jalil

2008-01-01

399

A validated stability-indicating HPLC method for the simultaneous determination of pheniramine maleate and naphazoline hydrochloride in pharmaceutical formulations  

PubMed Central

Background A simple, rapid, and accurate stability-indicating reverse phase liquid chromatographic method was developed and validated for the simultaneous determination of pheniramine maleate and naphazoline hydrochloride in bulk drugs and pharmaceutical formulations. Results Optimum chromatographic separations among pheniramine maleate, naphazoline hydrochloride and stress-induced degradation products have been achieved within 10 minutes by using an Agilent zorbax eclipse XDB C18 column (150 mm?×?4.6 mm, 5 ?m) as the stationary phase with a mobile phase consisted of 10 mM phosphate buffer pH 2.8 containing 0.5% triethlamine and methanol (68:32, v/v) at a flow rate of 1 mL min-1. Detection was performed at 280 nm using a diode array detector. Theoretical plates for pheniramine maleate and naphazoline hydrochloride were calculated to be 6762 and 6475, respectively. The method was validated in accordance with ICH guidelines with respect to linearity, accuracy, precision, robustness, specificity, limit of detection and quantitation. Regression analysis showed good correlations (R2?>?0.999) for pheniramine maleate in the concentration range of 150–1200 ?g mL-1 and naphazoline hydrochloride in 12.5-100 ?g mL-1. The method results in excellent separation of both the analytes and degradation products. The peak purity factor is ?980 for both analytes after all types of stress, indicating complete separation of both analyte peaks from the stress induced degradation products. Conclusions Overall, the proposed stability-indicating method was suitable for routine quality control and drug analysis of pheniramine maleate and naphazoline hydrochloride in pharmaceutical formulations. PMID:24485011

2014-01-01

400

Studies on binding interactions between clenbuterol hydrochloride and two serum albumins by multispectroscopic approaches in vitro.  

PubMed

In this study, binding properties of clenbuterol hydrochloride (CL) with human serum albumin (HSA) and bovine serum albumin (BSA) were examined using constant protein concentrations and various CL contents under physiological conditions. The binding parameters were confirmed using fluorescence quenching spectroscopy at various temperatures. The experimental results confirmed that the quenching mechanisms of CL and HSA/BSA were both static quenching processes. The thermodynamic parameters, namely, enthalpy change (?H) and entropy change (?S), were calculated according to the van't Hoff equation, which suggested that the electrostatic interactions were the predominant intermolecular forces in stabilizing the CL-HSA complex, and hydrogen bonds and van der Waals force were the predominant intermolecular forces in stabilizing the CL-BSA complex. Furthermore, the conformational changes of HSA/BSA in the presence of CL were determined using the data obtained from three-dimensional fluorescence spectroscopy, ultraviolet-visible absorption spectroscopy and circular dichroism spectroscopy. PMID:24030872

Wang, Qin; Zhang, Shengrui

2014-08-01

401

Assay of lercanidipine hydrochloride in dosage forms using nucleophilic substitution reaction.  

PubMed

A simple and sensitive spectrophotometric method has been developed for the assay of lercanidipine hydrochloride (LER) in bulk and in formulations. The method is based on the formation of coloured species between the drug and 1,2-naphthaquinone-4-sulphonic acid sodium salt (NQS) by means of nucleophilic substitution reaction. Absorbance was measured at ?(max) = 460 nm. The method was analyzed statistically. The system obeyed the Beer's law in the range 20-100 ?g mL?¹. Molar absorptivity value was found to be 4.79 × 10³ L mol?¹ cm?¹. Limits of detection and quantification were found to be as low as 0.04 and 0.13 ?g mL?¹. Precision (RSD, 0.4%) and accuracy (recovery 99.2 ± 0.6 to 101.1 ± 0.8%) of the developed method were evaluated. PMID:22202204

Sastry, Thuttagunta Manikya; Ramakrishna, Karipeddi

2011-12-01

402

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

NASA Astrophysics Data System (ADS)

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

Jo, Janggun; Yang, Xinmai

2011-09-01

403

Development and validation of simultaneous spectrophotometric methods for drotaverine hydrochloride and aceclofenac from tablet dosage form.  

PubMed

Two simple spectrophotometric methods have been developed for simultaneous estimation of drotaverine hydrochloride and aceclofenac from tablet dosage form. Method I is a simultaneous equation method (Vierodt's method), wavelengths selected are 306.5 and 276 nm. Method II is the absorbance ratio method (Q-Analysis), which employs 298.5 nm as ?(1) and 276 nm as ?(2) (?max of AF) for formation of equations. Both the methods were found to be linear between the range of 8-32 ?g/ml for drotaverine and 10-40 ?g/ml for aceclofenac. The accuracy and precision were determined and found to comply with ICH guidelines. Both the methods showed good reproducibility and recovery with % RSD in the desired range. The methods were found to be rapid, specific, precise and accurate and can be successfully applied for the routine analysis of drotaverine and aceclofenac in their combined tablet dosage form. PMID:22457554

Shah, S A; Shah, D R; Chauhan, R S; Jain, J R

2011-05-01

404

The density, viscosity and structural properties of aqueous ethambutol hydrochloride solutions  

NASA Astrophysics Data System (ADS)

Ethambutol (EMB) is a bacteriostatic antimycobacterial drug prescribed to treat tuberculosis. It is bacteriostatic against actively growing TB bacilli. The density and viscosity of aqueous ethambutol hydrochloride solutions have been studied at 298.15, 301.15 and 304.15 K and at different concentrations (0.255, 0.168, 0.128, 0.087, 0.041, and 0.023 mol dm-3). The apparent molar volume of these solutions for different temperatures and concentrations was calculated from the density data. The relative viscosities of drug solutions have been analysed by Jones-Dole equation. The limiting apparent molar volumes have been evaluated for different temperatures. The different properties have been used to study structural properties, structure formation and breaking properties of drug and solute-solvent interactions in solutions.

Deosarkar, S. D.; Puyad, A. L.; Kalyankar, T. M.

2012-05-01

405

Biogenic gold nanoparticles as fotillas to fire berberine hydrochloride using folic acid as molecular road map.  

PubMed

Use of biologically modified gold nanoparticles (GNPs) as molecular vehicle to ferry potential anti-cancer drug berberine hydrochloride (BHC) using folic acid (FA) as targeting molecule is reported in this work. A tropical fruit peel, Trapa bispinosa is used to fabricate highly monodispersed GNPs, passivated with essential functional groups which were used as linkers to attach FA and BHC via amide linkage. Flocculation Parameter (FP) of biologically synthesized GNPs was calculated under different salt concentrations which were found to be very ideal under a physiological condition. Various statistical models were used to find drug release profile out of which Higuchi was found to be the most ideal. GNP-FA-BHC complexes were found to be active against folic acid expressing HeLa cells. PMID:23910269

Pandey, Sunil; Mewada, Ashmi; Thakur, Mukeshchand; Shah, Ritu; Oza, Goldie; Sharon, Madhuri

2013-10-01

406

Taro corms mucilage/HPMC based transdermal patch: an efficient device for delivery of diltiazem hydrochloride.  

PubMed

The aim of this work is to examine the effectiveness of mucilage/hydroxypropylmethylcellulose (HPMC) based transdermal patch (matrix type) as a drug delivery device. We have successfully extracted mucilage from Colocasia esculenta (Taro) corms and prepared diltiazem hydrochloride incorporated mucilage/HPMC based transdermal patches using various wt% of mucilage by the solvent evaporation technique. Characterization of both mucilage and transdermal patches has been done by several techniques such as Molisch's test, organoleptic evaluation of mucilage, mechanical, morphological and thermal analysis of transdermal patches. Skin irritation test is studied on hairless Albino rat skin showing that transdermal patches are apparently free of potentially hazardous skin irritation. Fourier transform infrared analysis shows that there is no interaction between drug, mucilage and HPMC while scanning electron microscopy shows the surface morphology of transdermal patches. In vitro drug release time of mucilage-HPMC based transdermal patches is prolonged with increasing mucilage concentration in the formulation. PMID:24556117

Sarkar, Gunjan; Saha, Nayan Ranjan; Roy, Indranil; Bhattacharyya, Amartya; Bose, Madhura; Mishra, Roshnara; Rana, Dipak; Bhattacharjee, Debashis; Chattopadhyay, Dipankar

2014-05-01

407

Bladder tissue permeability and transport modelling of intravesical alum, lidocaine hydrochloride, methylprednisolone hemisuccinate and mitomycin C.  

PubMed

The aims of this study were to assess the tissue permeability of the bladder and to characterize the transport of four drugs displaying different physico-chemical properties and commonly used in intravesical delivery, through porcine bladder. The transport of aluminium through porcine bladder was assessed by using a vertical static diffusion cell. Lidocaine hydrochloride, methylprednisolone hemisuccinate and mitomycin C were tested by using three different experimental setups, including vertical static diffusion cell, microdialyseur and lab-patented device. Penetration results on different experimental setups were homogenous suggesting dependency on physico-chemical characteristics of drug and subsequent interaction with bladder wall structure. Oppositely, permeation varied consistently with experimental setup characteristics (i.e., permeation surface, receptor fluid volume and hydrodynamic). Mathematical modelling of drug transport through bladder wall is proposed considering scarce literature on this route of administration. Practical outcome of this study could drive compounding optimization towards improvement of safety and efficacy in patient undergoing intravesical administration. PMID:24463072

Moch, Céline; Salmon, Damien; Rodríguez Armesto, Laura; Colombel, Marc; Pivot, Christine; Pirot, Fabrice

2014-04-10

408

Bioadhesive ranitidine hydrochloride for gastroretention with controlled microenvironmental pH.  

PubMed

Ranitidine hydrochloride is a H(2) receptor blocker used in the treatment of gastric ulcers. Pharmacological factors, in addition to the dosage regimen, favor development of a sustained-release system for ranitidine especially in the therapeutic condition of erosive esophagitis. This investigation delves into the development of bioadhesive type of gastroretentive formulation (tablets) of ranitidine. The effect of mucoadhesive polymers such as Carbopol, hydroxypropyl methyl cellulose, and dextrose were studied. Mucoadhesion, in vitro drug release profile, water uptake, and swelling of the tablet were evaluated. Alkalizing agents were incorporated in an attempt to maintain an alkaline microenvironment within the tablet and improve the stability of the drug in acidic medium. The stability was evaluated using dye test and degradation studies. The drug release profiles were fit into various kinetic models. PMID:18618306

Adhikary, Anuradha; Vavia, Pradeep R

2008-08-01

409

New co-polymer zwitterionic matrices for sustained release of verapamil hydrochloride.  

PubMed

Stable co-polymer [vinyl acetate-co-3-dimethyl(methacryloyloxyethyl) ammonium propane sulfonate, p(VA-co-DMAPS)] latex of different compositions has been synthesized for the first time by emulsifier-free emulsion copolymerization. The unusual >overshooting< behavior of the co-polymer tablets has been explained by the formation of specific clusters from the opposite oriented dipoles-zwitterionic species. The change of their concentration with the DMAPS unit fraction (mDMAPS), pH and ionic strength has been considered responsible for the differences observed in the swelling kinetics. The results obtained prove that mDMAPS and ionic strength could be used to control the swelling degree of the p(VA-co-DMAPS) matrices and their sustained drug delivery. In this way, p(VA-co-DMAPS) matrices could be effectively used to control the sustained release of drugs with basic properties like verapamil hydrochloride from model tablets. PMID:18165187

Kostova, Bistra; Rachev, Dimitar

2007-12-01

410

Formulation and Evaluation of Extended-Release Solid Dispersion of Metformin Hydrochloride  

PubMed Central

The purpose of this research was to formulate and characterize solid dispersion (SD) of metformin hydrochloride using methocel K100M as the carrier by the solvent evaporation and cogrinding method. The influence of drug polymer ratio on drug release was studied by dissolution tests. Characterization was performed by fourier transform spectroscopy (FTIR), ultraviolet, differential scanning calorimetry and X-ray powder diffractometry. The optimized formulation was subjected to accelerated stability testing as per ICH guidelines. Release data were examined kinetically. SD with 1:4 and 1:5 ratio of drug to polymer obtained by solvent evaporation and cogrinding were selected as the best candidates suitable for prolonged-release oral dosage form of metformin. PMID:21264113

Patil, SA; Kuchekar, BS; Chabukswar, AR; Jagdale, SC

2010-01-01

411

[Study on dissolution test in vitro and bioavailability of oral osmotic pump of verapamil hydrochloride].  

PubMed

This paper deals with the evaluation of osmotic pump of verapamil hydrochloride tablet (C) by measuring in vitro/in vivo test. The results showed that the dissolution behaviors were of zero-order kinetic and release constant in vitro (Kr) of C was 9.9450. The plasma levels of Ver.HCl in eight volunteers following single and multiple oral doses of these dosage forms were determined using HPLC method. The pharmacokinetic parameters were fitted by nonlinear least square method with a computer on the basis of two-compartment model. The pharmacokinetic parameters of Cmax, Tmax, t1/2, Ka, K10 and K21 were calculated. The bioavailability of tablet C relative to B and A was 101.7%, 96.16% respectively. A significant correlation was found between in vitro dissolution and in vivo absorption. PMID:8010021

Guo, J L; Jing, G W; Cao, D S; Li, Y Q; He, H Y; Ling, L X; Li, Z

1993-01-01

412

Simultaneous determination of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate in pharmaceutical preparations using multivariate calibration 1  

NASA Astrophysics Data System (ADS)

Resolution of binary mixtures of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate with minimum sample pre-treatment and without analyte separation has been successfully achieved by methods of partial least squares algorithm with one dependent variable, principal component regression and hybrid linear analysis. Data of analysis were obtained from UV-vis spectra of the above compounds. The method of central composite design was used in the ranges of 1-15 mg L -1 for both calibration and validation sets. The models refinement procedure and their validation were performed by cross-validation. Figures of merit such as selectivity, sensitivity, analytical sensitivity and limit of detection were determined for all three compounds. The procedure was successfully applied to simultaneous determination of the above compounds in pharmaceutical tablets.

Samadi-Maybodi, Abdolraouf; Hassani Nejad-Darzi, Seyed Karim

2010-04-01

413

Polymeric matrix system for prolonged delivery of tramadol hydrochloride, part II: biological evaluation.  

PubMed

This study is an extrapolation of our previous one (part I) concerned with the formulation and physicochemical evaluation of a novel, simple, monolayer, easy-to-use, cost-effective, and aesthetically acceptable bioadhesive transdermal patch for tramadol hydrochloride. The current work is focused on bioadhesion, skin tolerability, and pharmacodynamic evaluation. Using naked rat skin, chitosan-Eudragit NE30D (1:1) film attained best bioadhesive properties. During in vivo studies, it also showed a significantly extended analgesic effect compared to both oral formula and chitosan single polymeric film using the hot plate test method. All the polymeric films were skin tolerable for the intended period of application according to the Draize test. The success of our approach can proudly, positively contribute into the world of pain management and arguably push transdermal delivery to realize its great promise. PMID:19653102

Ammar, Hussein O; Ghorab, Mahmoud; El-Nahhas, Soheir A; Kamel, Rabab

2009-01-01

414

Effects of indeloxazine hydrochloride on passive avoidance behavior of senescence-accelerated mice.  

PubMed

The effects of indeloxazine hydrochloride on disturbances of passive avoidance behavior in senescence-accelerated mice (SAM) were observed. The step-through latency of SAM-P/8/Ta (SAM-P/8, senescence-prone substrain) was significantly shorter than that of SAM-R/1/Ta (SAM-R/1, senescence-resistant substrain). The administration of indeloxazine (10-30 mg/kg p.o.) or dihydroergotoxine (1 mg/kg i.p.) for 3 weeks significantly prolonged the step-through latency of SAM-P/8/Ta whereas piracetam (30-300 mg/kg p.o.) did not. These results suggest that indeloxazine has a facilitatory effect on cerebral functions and that it has a broader pharmacological profile in anti-amnesic activities than piracetam. PMID:2792199

Yamamoto, M; Iwai, A; Kawabata, S; Ozawa, Y; Shimizu, M

1989-07-18

415

A comparative study of two polymorphs of L-aspartic acid hydrochloride.  

PubMed

Two polymorphs of L-aspartic acid hydrochloride, C4H8NO4(+)·Cl(-), were obtained from the same aqueous solution. Their crystal structures have been determined from single-crystal data collected at 100?K. The crystal structures revealed three- and two-dimensional hydrogen-bonding networks for the triclinic and orthorhombic polymorphs, respectively. The cations and anions are connected to one another via N-H···Cl and O-H···Cl interactions and form alternating cation-anion layer-like structures. The two polymorphs share common structural features; however, the conformations of the L-aspartate cations and the crystal packings are different. Furthermore, the molecular packing of the orthorhombic polymorph contains more interesting interactions which seems to be a favourable factor for more efficient charge transfer within the crystal. PMID:24992112

Benali-Cherif, Rim; Takouachet, Radhwane; Bendeif, El-Eulmi; Benali-Cherif, Nourredine

2014-07-15

416

Guanidine hydrochloride induced reversible dissociation and denaturation of duck delta2-crystallin.  

PubMed

The tetrameric delta2-crystallin from duck lens exhibits a reversible dissociation-denaturation process in solutions containing guanidine hydrochloride (GdnHCl). Sigmoidal or biphasic curves for the dissociation/denaturation processes, obtained using different methods of structural analysis, as a function of GdnHCl concentration were not coincidental with each other. delta2-crystallin in 0.91 M GdnHCl existed primarily as a monomer, which had no endogenous argininosuccinate lyase activity. After dilution of the GdnHCl-treated protein, the monomers reassociated into tetramers with concomitant recovery of enzyme activity. The sigmoidal recovery of enzyme activity demonstrates a cooperative hysteretic reactivation process. When the concentration of GdnHCl was higher than 1.2 M, various partially unfolded soluble forms of delta2-crystallin were produced from the dissociated monomers as shown by size-exclusion chromatography. The formation of a partially unfolded intermediate during the dissociation-denaturation process is proposed. PMID:10866796

Lee, H J; Chang, G G

2000-07-01

417

Thiocytosine as a radiation energy trap in a single crystal of cytosine hydrochloride.  

PubMed

Single crystals of cytosine hydrochloride with thiocytosine as an impurity were found suitable for the study of a possible new mechanism of long-range migration of energy deposited by ionizing radiation. In a crystal containing thiocytosine, two kinds of chlorine-containing paramagnetic centres are present that are completely absent in the pure cytosine. HCl crystals irradiated under the same condition. The thiocytosine molecules in conjunction with Cl- ions behave as hole traps. The centres have been characterized by EPR spectroscopy. One of the centres is derived from the cationic thiocytosine radical by interaction with a Cl- ion, and the other centre is formed by interaction of Cl. with a thiocytosine molecule. It is suggested that the transfer of an electron-loss site (a hole) in the Cl- network is the actual mechanism of the long-range energy transfer. PMID:8027610

Herak, J N; Sankovic, K; Hütterman, J

1994-07-01

418

[Interaction between ambroxol hydrochloride and human serum albumin studied by spectroscopic and molecular modeling methods].  

PubMed

In the present paper, the interaction between ambroxol hydrochloride (ABX) and human serum albumin (HSA) was studied under simulative physiological condition by spectroscopy and molecular modeling method. Stern-Volmer curvers at different temperatures and UV-Vis absorption spectroscopy showed that ABX quenched the fluorescence of HSA mainly through dynamic quenching mode. On the basis of the thermodynamic data, the main binding force between them is hydrophobic interaction. According to the theory of Forster non-radiation energy transfer, the binding distance between the donor and the acceptor was 3.01 nm. The effect of ABX on the conformation of HSA was analyzed by the synchronous and three-dimensional fluorescence spectroscopy. Furthermore, using the molecular modeling method, the interaction between them was predicted from molecular angle: ABX might locate in the subdomain III A of HSA. PMID:21714251

Liang, Jing; Feng, Su-Ling

2011-04-01

419

Ultrasonic Studies of 4-Aminobutyric Acid in Aqueous Metformin Hydrochloride Solutions at Different Temperatures  

NASA Astrophysics Data System (ADS)

Ultrasonic speeds and density data of 4-aminobutyric acid in 0.05 M, 0.10 M, and 0.15 M aqueous metformin hydrochloride (MFHCl) solutions are measured at 308.15 K, 313.15 K, and 318.15 K. The isentropic compressibility ( k S ), the change in isentropic compressibility (? k S ), the relative change in isentropic compressibility ({? k_S/k_S^0}), the apparent molal compressibility ({k_?}), the limiting apparent molal compressibility ({k_?^0 }), the transfer limiting apparent molal compressibility ({? k_?^0}), the hydration number ( n H), and the pair and triplet interaction parameters ( k AH, k AHH) are estimated. The above parameters are used to interpret the solute-solute and solute-solvent interactions of 4-aminobutyric acid in aqueous MFHCl solutions.

Rajagopal, K.; Jayabalakrishnan, S. S.

2010-12-01

420

Evaluation of anti-GERD activity of gastro retentive drug delivery system of itopride hydrochloride.  

PubMed

The present work describes the formulation and evaluation of the gastroretentive system of Itopride hydrochloride. In this research, we have formulated floating hydrogel-based microspheres employing calcium carbonate (CaCO(3)) as a gas forming agent dispersed in alginate matrix. In vitro characterizations such as drug content, particle size, and drug release were carried out. GI motility was determined by administration of charcoal meal to rats. Results demonstrated that prepared microspheres were spherical in shape with smooth surface, good loading efficiency, and excellent buoyancy. The gastro retentive dosage form of itiopride demonstrated significant antacid, anti-ulcer, and anti-GERD activity after 12 hours in comparison with the conventional dosage form. PMID:20515421

Satapathy, Trilochan; Panda, Prasana K; Goyal, Amit K; Rath, Goutam

2010-08-01

421

The permeation of nalmefene hydrochloride across different regions of ovine nasal mucosa.  

PubMed

The permeability of nalmefene hydrochloride (NH) across different regions of ovine nasal mucosa was investigated in vitro. Five different regions of ovine nasal mucosa (superior turbinate mucosa, middle turbinate mucosa, inferior turbinate mucosa, posterior septum mucosa, and anterior septum mucosa) were studied. The results showed that the permeability coefficients of NH through different regions of nasal mucosa were different, and the suitable regions for the absorption of NH were the middle turbinate mucosa, the posterior septum mucosa and the superior turbinate. At the same time, the middle turbinate mucosa was the largest region among the five regions, thus it was the main absorption region for NH. The high uniformity of the middle turbinate mucosa also made it the most suitable model for the permeation of NH in vitro. PMID:17139110

Du, Gani; Gao, Yongliang; Nie, Shufang; Pan, Weisan

2006-12-01

422

Dissolution profile study on the novel doxycycline hydrochloride sustained-release capsules.  

PubMed

In present study, a novel doxycycline hydrochloride (DC) sustained-release capsule was prepared with the new manufacturing technology, extrusion-spheronization method. The release studies were performed using marketed sample as a reference and data were analyzed in terms of cumulative release amounts as a function of time. Results demonstrated that our developed sample was similar to reference preparation in release characteristics in vitro. The in vitro release characteristics of different batches of preparations were quite similar with each other, the total release proportions of DC from sustained-release capsule reached higher than 90 % within 4 h. Similarity factors f2 of two preparations were all higher than 50, the release mechanism of drugs from capsules fitted to non-Fichian diffusion.The developed sustained-release preparation may be a promising alternative dosage form for treatment of related diseases. PMID:25262507

Yang, Shuoye; Li, Kun

2014-09-01

423

Development and optimization of multiparticulate drug delivery system of alfuzosin hydrochloride.  

PubMed

The purpose of present research was to develop and optimize sustained release floating pellets of alfuzosin hydrochloride which has narrow absorption window in proximal intestine to improve patient compliance and therapeutic efficacy in the treatment of benign prostatic hyperplasia. The system was designed to provide drug loaded pellets coated with three successive coatings over Celphere(®) (microcrystalline cellulose pellets) - drug layer, effervescent layer (HPMC and sodium bicarbonate) and gas entrapped polymeric membrane (Kollicoat(®) SR 30D). A 3(2) factorial design was employed with HPMC:sodium bicarbonate and Kollicoat(®) SR 30D concentration as independent variables while drug release and floating lag time were the dependent variables. Regression analysis was performed to identify best formulation conditions. Scanning electron microscopy was used to study pellet morphology. The floating ability and in vitro drug release of the system were dependent on amount of sodium bicarbonate layered onto pellets and coating level of Kollicoat(®) SR 30D. PMID:23010113

Pagariya, Tarun P; Patil, Sanjay B

2013-02-01

424

Enthalpies of solvation for dopamine hydrochloride in water-ethanol solutions  

NASA Astrophysics Data System (ADS)

The enthalpies of dissolution of dopamine hydrochloride (H2Dop · HCl) in water-ethanol solvents containing from 0 to 0.8 mole fraction of ethanol are measured by calorimetry at 298.15 K. Standard enthalpies of transfer (?tr H ?) for the molecular (H2Dop) and cationic (H3Dop+) forms of dopamine from water into binary solvents are calculated from the obtained data. The enthalpies of transfer of H3Dop+ cation are determined from the enthalpies of dissolution of H2Dop · HCl using the familiar method of separating the molar quantities into ionic contributions (Ph4P+ = BPh{4/-}), and by an original alternative procedure. The effect of the composition of the binary solvent on the solvation of dopamine is considered.

Vandyshev, V. N.; Ledenkov, S. F.; Molchanov, A. S.

2012-10-01

425

High pressure study of molecular dynamics of protic ionic liquid lidocaine hydrochloride  

NASA Astrophysics Data System (ADS)

In this paper, we investigate the effect of pressure on the molecular dynamics of protic ionic liquid lidocaine hydrochloride, a commonly used pharmaceutical, by means of dielectric spectroscopy and pressure-temperature-volume methods. We observed that near Tg the pressure dependence of conductivity relaxation times reveals a peculiar behavior, which can be treated as a manifestation of decoupling between ion migration and structural relaxation times. Moreover, we discuss the validity of thermodynamic scaling in lidocaine HCl. We also employed the temperature-volume Avramov model to determine the value of pressure coefficient of glass transition temperature, dTg/dP|P = 0.1. Finally, we investigate the role of thermal and density fluctuations in controlling of molecular dynamics of the examined compound.

Swiety-Pospiech, A.; Wojnarowska, Z.; Pionteck, J.; Pawlus, S.; Grzybowski, A.; Hensel-Bielowka, S.; Grzybowska, K.; Szulc, A.; Paluch, M.

2012-06-01

426

Liquisolid technique as a new approach to sustain propranolol hydrochloride release from tablet matrices.  

PubMed

It is suggested here that liquisolid technique has the potential to be optimized for the reduction of drug dissolution rate and thereby production of sustained release systems. In the present study, propranolol hydrochloride was dispersed in polysorbate 80 as the liquid vehicle. Then a binary mixture of carrier-coating materials (Eudragit RL or RS as the carrier and silica as the coating material) was added to the liquid medication under continuous mixing in a mortar. The final mixture was compressed using the manual tableting machine. The effect of drug concentration, loading factor, thermal treating and aging on release profile of propranolol hydrochloride from liquisolid compacts were investigated at two pH values (1.2 and 6.8). The release rate of propranolol HCl from liquisolid compacts was compared to the release of propranolol HCl from conventional tablets. X-ray crystallography and DSC were used to investigate the formation of any complex between drug and excipients or any crystallinity changes during the manufacturing process. Propranolol HCl tablets prepared by liquisolid technique showed greater retardation properties in comparison with conventional matrix tablets. This investigation provided evidence that polysorbate 80 (Tween 80) has important role in sustaining the release of drug from liquisolid matrices, and a reduction of T(g) of the polymer can be the reason for the release prolongation of liquisolid tablets. The results also showed that wet granulation had remarkable impact on release rate of propranolol HCl from liquisolid compacts, reducing the release rate of drug from liquisolid compacts. The results showed that aging (liquisolid