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1

Assay of cisapride in pharmaceutical formulations by visible spectrophotometry  

Microsoft Academic Search

Three spectrophotometric methods (A-C) for the assay of cisapride (CPD) in pure and dosage forms are described. Method A is based on the oxidative coupling reaction of CPD with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in the presence of ferric chloride to form a coloured species (?max; 565 nm.) Method B is based on the oxidation of CPD with Fe (III) and

Chilukuri S. P. Sastry; Yaramati Srinivas; Pulugurtha V. Subba Rao

1997-01-01

2

Spectrophotometric Estimation of Nimesulide and its Formulations  

Microsoft Academic Search

Four simple and sensitive visible spectrophotometric methods (A–D) have been described for the assay of nimesulide (NMD)\\u000a either in pure form or in pharmaceutical formulations. Methods A and B are based on the oxidative coupling between the reduced\\u000a product of NMD (RNMD) and p-N,N-dimethyl phenylenediamine dihydrochloride (DMPD) in presence of chloramine – T (CAT) or 3-methyl-2-benzothiazolinone\\u000a hydrazone hydrochloride (MBTH) in

Chilukuri S. R. Lakshmi; Manda N. Reddy

1999-01-01

3

Spectrophotometric determination of clozapine in pharmaceuticals  

Microsoft Academic Search

New Spectrophotometric methods for the assay of clozapine (CZP) in pure and dosage forms are described. Method A is based on the oxidative coupling reaction of CZP with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in the presence of ceric ammonium sulphate to form a coloured species (?max 570 nm). Method B is also based on the oxidative coupling reaction of CZP withP-,N,N-dimethylpheny-lenediamine

Chilukuri S. P. Sastry; Thuta Vijaya Rekha; Atreyapurapu Satyanarayana

1998-01-01

4

Development and demonstration of an immobilised-polyphenol oxidase bioprobe for the detection of phenolic pollutants in water  

Microsoft Academic Search

The development of a portable, disposable bioprobe incorporating mushroom polyphenol oxidase immobilised on a synthetic membrane for this purpose is described for the detection and semi-quantification of phenolic pollutants in water. The enzyme, immobilised on a nylon membrane together with 3-methyl-2-benzothiazolinone hydrazone, produced ranges of maroon colours in phenolic solutions and orange colours in cresylic solutions. The colour intensities produced

Ingrid M Russell; Stephanie G. Burton

1999-01-01

5

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

6

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

PubMed

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. PMID:21237703

Ashour, Safwan; Bahbouh, Mahmoud; Khateeb, Mouhammed

2010-08-20

7

Propafenone Hydrochloride  

Center for Drug Evaluation (CDER)

Text Version... Contains Nonbinding Recommendations Guidance on Propafenone Hydrochloride ... Active ingredient: Propafenone Hydrochloride ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

8

Memantine Hydrochloride  

Center for Drug Evaluation (CDER)

Text VersionPage 1. Contains Nonbinding Recommendations Draft Guidance on Memantine Hydrochloride ... Active ingredient: Memantine Hydrochloride ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

9

Methylphenidate Hydrochloride  

Center for Biologics Evaluation and Research (CBER)

Text Version... refer to the Mirtazapine Tablet Draft Guidance ... method (with 0.1N HCl), with data ... states that “Ritalin LA® (methylphenidate hydrochloride) extended ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

10

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

PubMed Central

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

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

1992-01-01

11

Duloxetine hydrochloride  

Microsoft Academic Search

In August 2004, duloxetine hydrochloride (Cymbalta; Eli Lilly), a selective serotonin- and noradrenaline-reuptake inhibitor, was approved by the US FDA for the treatment of major depressive disorder. It has since become the first such antidepressant to be approved by the FDA for an indication outside of psychiatry, when its approval for use in the treatment of diabetic peripheral neuropathic pain

Peter Kirkpatrick; Anathea B. Waitekus

2004-01-01

12

Spectrophotometric determination of clobetasol propionate, halobetasol propionate, quinagolide hydrochloride, through charge transfer complexation  

Microsoft Academic Search

Two spectrophotometric procedures are described for the determination of clobetasol propionate(I), halobetasol propionate(II) (corticosteroids) and quinagolide hydrochloride(III) (prolactin inhibitor). For corticosteroid drugs, the procedures are based on the formation of phenyl hydrazones of the corticosteroids which are subsequently subjected to charge transfer complexation reaction with either 2,3-dichloro-5,6-dicyanobenzoquinone (DDQ) as ?-acceptor or with iodine as ?-acceptor. Prolactin inhibitor was reacted directly

Azza A. Mostafa; Lories I. Bebawy; Heba H. Refaat

2002-01-01

13

Corrosion inhibition of some novel hydrazone derivatives  

Microsoft Academic Search

A novel series of surfactants was synthesized via direct interaction of the hydrogen-accepting benzyl monophenyl hydrazone and different hydrogen-donating sulfate, sulfonate,\\u000a sulfosuccinate, or taurate species in their acid form. The double salt surfactants produced had a benzyl monophenyl hydrazonium\\u000a (PH) moiety as the cation, and lauryl sulfate, dodecylbenzene sulfonate, dioctyl sulfosuccinate, N-cetyloxycarbonyl ethyltaurate (COCET), and N-stearyloxycarbonyl ethyltaurate as the anion.

Nabel A. Negm; Salwa M. I. Morsy; Medhat M. Said

2005-01-01

14

Dutasteride; Tamsulosin Hydrochloride  

Center for Biologics Evaluation and Research (CBER)

Text Version... Draft Guidance on Dutasteride; Tamsulosin Hydrochloride ... Active ingredient: Dutasteride; Tamsulosin Hydrochloride Form/Route: Capsule/Oral ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

15

Doxorubicin hydrochloride liposome injection  

Center for Drug Evaluation (CDER)

... being exercised, Sun Pharma Global's Lipodox (Doxorubicin Hydrochloride Liposome Injection) remains unapproved by FDA for marketing in the ... More results from www.fda.gov/drugs/informationondrugs/approveddrugs

16

A Comparison of Alkylhydrazines and Their B6-Hydrazones as Convulsant Agents.  

National Technical Information Service (NTIS)

A comparative study was made of the toxicity and convulsion activity of 1,1-dimethylhydrazine (UDMH), monomethylhyrazine (MMH), and their pyridoxal and pyridoxal-5-phosphate hydrazones. The hydrazones of UDMH are more toxic than UDMH itself when 3 criteri...

A. Furst W. R. Gustavson

1966-01-01

17

Spectroscopic investigations on the highly purified lactoperoxidase Fe(III)-heme catalytic site.  

PubMed

Purification of the lactoperoxidase (LPO) major cationic isoenzyme was significantly improved by the use of preparative chromatographic and electrophoretic methods combined with analytical electrophoretic techniques and image processing. A detailed report is given of the experimental procedure. Furthermore, electron paramagnetic resonance has played a fundamental role in evaluating the enzyme purity against lactoferrin and minor LPO isoenzyme components in setting the final steps of the purification. With the aim to completely clarify the Fe(III)-heme high-spin nature of the native LPO, two samples of lactoperoxidase, LPO1 and LPO2 (RZ = 0.95) from farm and commercial milk, respectively, were purified and characterized in particular by electron paramagnetic resonance (EPR) spectroscopy, in comparison with a commercial preparation (LPOs). The LPO1 EPR spectrum, at physiological pH, is clearly indictive of the presence of an iron(III)-heme high-spin catalytic site in the native enzyme. On the contrary, in the LPO2 spectrum a thermal equilibrium between high- and low-spin iron(III)-heme species is present. The low-spin component of the spectrum has been assigned to an LPO-NO2- adduct due to the presence of some nitrite impurities originating either from commercial unpasteurized milk or from external sources. The LPOs EPR spectrum shwos the presence of some spurious lines in the g approximately equal to 6 and 4 regions due to the minor LPO isoenzyme components and to lactoferrin, respectively. The LPO EPR spectra previously reported in the literature contain a variable number of spurious lines in the g approximately equal to 4 and 2 regions as a consequence of lactoferrin impurity and LPO low-spin adducts with endogenous or exogenous anions. Furthermore, the interaction of LPO with its native substrate (the thiocyanate anion), which previously was shown by NMR and EPR (at high substrate concentration) spectroscopies, has been confirmed by EPR at low temperature and low substrate concentration and by optical spectroscopy at room temperature and high substrate concentration as a function of pH. The LPO activity at optimum pH (approximately equal to 4-5) has been measured in phosphate and acetate buffer using as an oxidizable substrate the system dimethylamino benzoic acid 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (DMAB-MBTH), which was considered a good chromogen for other peroxidases such as HRP and zucchini peroxidases. The LPO vs SCN- activity at optimum pH (approximately equal to 5.5) has been measured in phosphate and acetate buffer.(ABSTRACT TRUNCATED AT 400 WORDS) PMID:7769383

Ferrari, R P; Laurenti, E; Cecchini, P I; Gambino, O; Sondergaard, I

1995-05-01

18

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

PubMed Central

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

Daniel, Geoffrey; Volc, Jindrich; Kubatova, Elena

1994-01-01

19

Pyranose Oxidase, a Major Source of H(2)O(2) during Wood Degradation by Phanerochaete chrysosporium, Trametes versicolor, and Oudemansiella mucida.  

PubMed

The production of the H(2)O(2)-generating enzyme pyranose oxidase (POD) (EC 1.1.3.10) (synonym, glucose 2-oxidase), two ligninolytic peroxidases, and laccase in wood decayed by three white rot fungi was investigated by correlated biochemical, immunological, and transmission electron microscopic techniques. Enzyme activities were assayed in extracts from decayed birch wood blocks obtained by a novel extraction procedure. With the coupled peroxidase-chromogen (3-dimethylaminobenzoic acid plus 3-methyl-2-benzothiazolinone hydrazone hydrochloride) spectrophotometric assay, the highest POD activities were detected in wood blocks degraded for 4 months and were for Phanerochaete chrysosporium (149 mU g [dry weight] of decayed wood), Trametes versicolor (45 mU g), and Oudemansiella mucida (1.2 mU g), corresponding to wood dry weight losses of 74, 58, and 13%, respectively. Mn-dependent peroxidase activities in the same extracts were comparable to those of POD, while lignin peroxidase activity was below the detection limit for all fungi with the veratryl alcohol assay. Laccase activity was high with T. versicolor (422 mU g after 4 months), in trace levels with O. mucida, and undetectable in P. chrysosporium extracts. Evidence for C-2 specificity of POD was shown by thin-layer chromatography detection of 2-keto-d-glucose as the reaction product. By transmission electron microscopy-immunocytochemistry, POD was found to be preferentially localized in the hyphal periplasmic space of P. chrysosporium and O. mucida and associated with membranous materials in hyphae growing within the cell lumina or cell walls of partially and highly degraded birch fibers. An extracellular distribution of POD associated with slime coating wood cell walls was also noted. The periplasmic distribution in hyphae and extracellular location of POD are consistent with the reported ultrastructural distribution of H(2)O(2)-dependent Mn-dependent peroxidases. This fact and the dominant presence of POD and Mn-dependent peroxidase in extracts from degraded wood suggest a cooperative role of the two enzymes during white rot decay by the test fungi. PMID:16349330

Daniel, G; Volc, J; Kubatova, E

1994-07-01

20

Pyridoxal isonicotinoyl hydrazone analogs induce apoptosis in hematopoietic cells due to their iron-chelating properties  

Microsoft Academic Search

Analogs of pyridoxal isonicotinoyl hydrazone (PIH) are of interest as iron chelators for the treatment of secondary iron overload and cancer. PIH, salicylaldehyde isonicotinoyl hydrazone (SIH), and 2-hydroxy-1-naphthylaldehyde isonicotinoyl hydrazone (NIH), the toxicity of which vary over two orders of magnitude, were selected for a study of their mechanisms of toxicity. PIH analogs and their iron complexes caused concentration- and

Joan L. Buss; Jiri Neuzil; Nina Gellert; Christian Weber; Prem Ponka

2003-01-01

21

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

Microsoft Academic Search

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

Hussein S Seleem; Gaber A El-Inany; Bashir A El-Shetary; Marwa A Mousa

2011-01-01

22

Stability of transition metal complexes involving three isomeric quinolyl hydrazones  

NASA Astrophysics Data System (ADS)

The stability constants of three isomeric quinolyl hydrazones; {4,6-(para); 4,7-(meta) and 4,8-MeBHQ(ortho)} towards some bivalent metal ions have been determined in 75% solvent (dioxane, isopropanol, ethanol and methanol)-water by a pH-titrimetry. The insertion of the Me-group in the 8-position decreases the stability of the complexes to a great extent. The complexation of the ortho-derivative is endothermic, whereas that of the para-derivative is exothermic. Using the solvent parameters, the stability constants of the para-derivative towards Co(II), Ni(II) and Cu(II) ions were evaluated in aqueous medium by five different methods. Also, the electronic absorption spectra of the ortho-hydrazone have been studied in solvents of various polarities to investigate the dependence of the band shift (? ?) on the solvent parameters viz. 1/ D, Z, ET, DN, AN and (?, ?, ?*). The interaction of the hydrazones with CoCl 2·6H 2O afforded an octahedral complex in case of the ortho-hydrazone and square planar complexes in case of the meta- and para-hydrazones.

Seleem, H. S.; Mostafa, M.; Hanafy, F. I.

2011-05-01

23

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

Code of Federal Regulations, 2010 CFR

...2009-04-01 2009-04-01 false Ketamine hydrochloride with promazine hydrochloride...FORM NEW ANIMAL DRUGS § 522.1222b Ketamine hydrochloride with promazine hydrochloride...injection. (a) Chemical name. Ketamine hydrochloride,...

2009-04-01

24

Computational investigation of first hyperpolarizability in substituted hydrazones  

NASA Astrophysics Data System (ADS)

Density functional theory has been used to calculate the ?·?(?2?;?,?,0) on a series of solution-phase hydrazones. Using the experimental and MP2(Full) calculated data as references, the qualitative trend of the Hartree–Fock, M06-HF and range-separated hybrids have been examined. Our results propose methods with long-range corrections, and without short-range exact exchange, are capable of qualitatively predicting the nonlinear optical responses of the hydrazones when reliable geometries have been provided. The same conclusion can also be applied to solution-phase push–pull phenylpolyenes.

Lu, Shih-I.

2013-08-01

25

Hydrolysis of pyridoxal isonicotinoyl hydrazone and its analogs  

Microsoft Academic Search

An orally available iron chelator is desirable for the treatment of secondary iron overload. Pyridoxal isonicotinoyl hydrazone (PIH) and its analogs effectively mobilize iron in vivo and in vitro, and are therefore promising candidates for this purpose. PIH analogs undergo significant amino acid-catalyzed hydrolysis in cell culture medium and in serum, achieving equilibrium with their corresponding aldehydes and hydrazides with

Joan L Buss; Prem Ponka

2003-01-01

26

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

27

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

Microsoft Academic Search

2-Hydroxyacetophenone nicotinic acid hydrazone (H2ApNH) was synthesized as a part of our work, in search for non-linear optical crystal based on hydrazones, and studied spectroscopically. Complete NMR assignments for the hydrazone was made using COSY homonuclear and HMQC heteronuclear correlation techniques. Solid state reflectance was also studied in order to understand the electronic structure of the synthesized compound. The crystal

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

2003-01-01

28

The Origins of Stereoselectivity in the ?-Alkylation of Chiral Hydrazones  

PubMed Central

Density functional theory calculations and experiment reveal the origin of stereoselectivity in the deprotonation–alkylation of chiral N-amino cyclic carbamate (ACC) hydrazones. When the ACC is a rigid, camphor-derived carbamate, the two conformations of the azaenolate intermediate differ in energy due to conformational effects within the oxazolidinone ring and steric interactions between the ACC and the azaenolate. An electrophile adds selectively to the less-hindered ?-face of the azaenolate. Although it was earlier reported that use of ACC auxiliaries led to ?-alkylated ketones with ers of 82:18 to 98:2, B3LYP calculations predict higher stereoselectivity. Direct measurement of the dr of an alkylated hydrazone prior to removal of the auxiliary confirms this prediction; the removal of the auxiliary can compromise the overall stereoselectivity of the process.

Krenske, Elizabeth H.; Lim, Daniel; Wengryniuk, Sarah E.

2010-01-01

29

Oxidative stress mediates toxicity of pyridoxal isonicotinoyl hydrazone analogs  

Microsoft Academic Search

Pyridoxal isonicotinoyl hydrazone (PIH) and many of its analogs are effective iron chelators in vivo and in vitro, and are of interest for the treatment of secondary iron overload. Because previous work has implicated the Fe3+–chelator complexes as a determinant of toxicity, the role of iron-based oxidative stress in the toxicity of PIH analogs was assessed. The Fe3+ complexes of

Joan L. Buss; Jiri Neuzil; Prem Ponka

2004-01-01

30

Prevention of Postasphyxia Electroretinal Dysfunction with a Pyridoxal Hydrazone  

Microsoft Academic Search

The newborn retina is particularly sensitive and frequently subjected to peroxidative stresses that result in visual sequelae. We compared two iron chelators, deferoxamine and a newer compound, pyridoxal isonicotinoyl hydrazone (PIH), in protecting the retina of newborn pigs (1–3 d old) from asphyxia-reoxygenation insults. Animals were treated IV with either saline, deferoxamine 15.2 ?mol\\/kg (10 mg\\/kg) or PIH 34.8 ?mol\\/kg

Mousumi Bhattacharya; Premysl Ponka; Pierre Hardy; Nelly Hanna; Daya R Varma; Pierre Lachapelle; Sylvain Chemtob

1997-01-01

31

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

2012-08-28

32

Fluorescence Quenchers for Hydrazone and Oxime Orthogonal Bioconjugation  

PubMed Central

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:background 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.

Crisalli, Pete; Hernandez, Armando R.; Kool, Eric T.

2012-01-01

33

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).

2011-01-01

34

Draft Guidance on Moxifloxacin Hydrochloride Active ...  

Center for Drug Evaluation (CDER)

Text VersionPage 1. Contains Nonbinding Recommendations Draft Guidance on Moxifloxacin Hydrochloride ... Active ingredient: Moxifloxacin Hydrochloride ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

35

Guidance on Tramadol Hydrochloride Active ingredient ...  

Center for Biologics Evaluation and Research (CBER)

Text VersionPage 1. Contains Nonbinding Recommendations Guidance on Tramadol Hydrochloride ... Active ingredient: Tramadol Hydrochloride ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

36

Guidance on Tramadol Hydrochloride; Acetaminophen Active ...  

Center for Biologics Evaluation and Research (CBER)

Text Version... Guidance on Tramadol Hydrochloride; Acetaminophen ... Active ingredient: Tramadol Hydrochloride; Acetaminophen Form/Route: Tablets/Oral ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

37

Guidance on Glipizide; Metformin Hydrochloride Active ...  

Center for Biologics Evaluation and Research (CBER)

Text VersionContains Nonbinding Recommendations Guidance on Glipizide; Metformin Hydrochloride ... Active ingredient: Glipizide; Metformin Hydrochloride ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

38

Draft Guidance on Verapamil Hydrochloride Active ingredient ...  

Center for Biologics Evaluation and Research (CBER)

Text VersionPage 1. Contains Nonbinding Recommendations Draft Guidance on Verapamil Hydrochloride ... Active ingredient: Verapamil Hydrochloride ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

39

Guidance on Metformin Hydrochloride Active ingredient ...  

Center for Drug Evaluation (CDER)

Text VersionPage 1. Contains Nonbinding Recommendations Guidance on Metformin Hydrochloride ... Active ingredient: Metformin Hydrochloride ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

40

Molecular design, synthesis and bioactivity of glycosyl hydrazine and hydrazone derivatives: Notable effects of the sugar moiety  

Microsoft Academic Search

Assuming that the water solubility of our previous hydrazone derivatives would improve after modification with sugars while keeping or modulating their notable biological activities, we designed and synthesized some glycosyl hydrazine and hydrazone derivatives. Bioassay results indicated that the antitumor activity of our previously prepared hydrazones reduced or disappeared after modification with sugars. On the contrary, some glycosyl derivatives displayed

Zining Cui; Xinling Yang; Yanxia Shi; Hirotaka Uzawa; Jingrong Cui; Hirofumi Dohi; Yoshihiro Nishida

2011-01-01

41

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

42

Ligand substitution reactions of a phenolic quinolyl hydrazone; oxidovanadium (IV) complexes  

PubMed Central

Background Quinoline ring has therapeutic and biological activities. Quinolyl hydrazones constitute a class of excellent chelating agents. 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 aimed to study the competency effect of a phenolic quinolyl hydrazone (H2L; primary ligand) with some auxiliary ligands (Tmen, Phen or Oxine; secondary ligands) towards oxidovanadium (IV) ions. Results Mono- and binuclear oxidovanadium (IV) - complexes were obtained from the reaction of a phenolic quinolyl hydrazone with oxidovanadium (IV)- ion in absence and presence of N,N,N',N'- tetramethylethylenediamine (Tmen), 1,10-phenanthroline (Phen) or 8-hydroxyquinoline (Oxine). The phenolic quinolyl hydrazone ligand behaves as monobasic bidentate (NO- donor with O- bridging). All the obtained complexes have the preferable octahedral geometry except the oxinato complex (2) which has a square pyramid geometry with no axial interaction; the only homoleptic complex in this study. Conclusion The ligand exchange (substitution/replacement) reactions reflect the strong competency power of the auxiliary aromatic ligands (Phen/Oxine) compared to the phenolic quinolyl hydrazone (H2L) towards oxidovanadium (IV) ion; (complexes 2 and 3). By contrast, in case of the more flexible aliphatic competitor (Tmen), an adduct was obtained (4). The obtained complexes reflect the strength of the ligand field towards the oxidovanadium (IV)- ion; Oxine or Phen >> phenolic hydrazone (H2L) > Tmen.

2011-01-01

43

Cardiotoxicity Studies with Emetine Hydrochloride (Nsc 33669) AND WITH Dehydroemetine Hydrochloride (Nsc 129414) IN Monkeys.  

National Technical Information Service (NTIS)

Emetine hydrochloride is a hydrated hydrochloride of an alkaloid obtained from ipecac and can be synthetically prepared by methylation of cephaeline. Emetine hydrochloride is primarily used medicinally in the treatment of amebiasis. it has been demonstrat...

R. K. Morrison D. E. Brown E. K. Timmens M. A. Nieglos C. Molins

1970-01-01

44

Synthesis of Macrocyclic Bis-Hydrazone and Their Use in Metal Cations Extraction  

PubMed Central

Two new macrocyclic hydrazone Schiff bases were synthesized by reaction of succindihydrazide and adipdihydrazide with acetylacetone. Hydrazones have been characterized by elemental analyses and IR, mass, 1H?NMR, and 13C?NMR spectral data. Hydrazones have been studied by liquid-liquid extraction towards the s-metal ions (Li+, Na+, and K+) and d-metal ions (Cu2+ and Cr3+) from aqueous phase to organic phase. The effect of chloroform and dichloromethane as organic solvents over the metal chlorides extraction was investigated at 25 ± 0.1°C by using flame atomic absorption. We found differences between the two solvents in extraction selectivity.

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

2012-01-01

45

Pseudoephedrine Hydrochloride Extended Release tablets ...  

Center for Biologics Evaluation and Research (CBER)

Text Version... Draft Guidance on Pseudoephedrine Hydrochloride ... It does not create or confer any rights for or on any person and does not operate to bind FDA or ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

46

Synthesis of nalidixic acid based hydrazones as novel pesticides.  

PubMed

Thirty-one substituted hydrazones of nalidixic acid hydrazide were synthesized and characterized by spectral techniques. These compounds were evaluated for various biological activities, namely, fungicidal, insecticidal, and nitrification inhibitory activities. The antifungal activity was evaluated against five pathogenic fungi, namely, Rhizoctonia bataticola , Sclerotium rolfsii , Rhizoctonia solani , Fusarium oxysporum , and Alternaria porii . They showed maximum inihibition against A. porii with ED(50) = 34.2-151.3 microg/mL. The activity was comparable to that of a commercial fungicide, hexaconazole (ED(50) = 25.4 microg/mL). They were also screened for insecticidal activity against third-instar larvae of Spodoptera litura and adults of Callosobruchus maculatus and Tribollium castaneum . Most of them showed 70-100% mortality against S. litura through feeding method at 0.1% dose. These compounds were not found to be effective nitrification inhibitors. PMID:20131903

Aggarwal, Nisha; Kumar, Rajesh; Srivastva, Chitra; Dureja, Prem; Khurana, J M

2010-03-10

47

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

48

21 CFR 582.5875 - Thiamine hydrochloride.  

Code of Federal Regulations, 2013 CFR

...AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 § 582.5875 Thiamine hydrochloride. (a) Product. Thiamine hydrochloride....

2013-04-01

49

Possible Side Effects of Metformin hydrochloride  

Cancer.gov

Page of 1Possible Side Effects of Metformin Hydrochloride (Table Version Date: May 28, 2013) COMMON, SOME MAY BE SERIOUS In 100 people receiving Metformin Hydrochloride, more than 20 and up to 100 may have: Diarrhea, nausea, vomiting OCCASIONAL, SOME

50

Synthesis and spectroscopic characterization of fluorescent boron dipyrromethene-derived hydrazones.  

PubMed

Derivatives of 4,4-difluoro-4-bora-3a,4a,diaza-s-indacene (BODIPY® or BDP) that possess a hydrazine substituent on position 5 are potential "turn-on" fluorophores for labeling aldehydes The unnatural amino acid L-3-formyltyrosine can be incorporated into a protein or peptide; thus, these hydrazines are potentially site specific labels for such polymers. In this work, model compounds were synthesized to assess whether the photochemical properties of the BDP-hydrazone would be suitable for protein labeling. Hydrazones were synthesized from the fluorophore 3-chloro-5-hydrazino-BDP and different aldehydes, and the absorption and emission spectra of the products were compared. The hydrazone of an unsubstituted aromatic aldehyde displays absorption and emission maxima (531 nm and 559 nm, respectively in dioxane) that are red shifted relative to those of a hydrazone from an aliphatic aldehyde (513 nm and 543 nm, respectively, in dioxane) and an increased quantum yield (0.21 vs. 0.11, respectively, in dioxane). The presence of a hydroxyl group ortho- to the aldehyde produces a hydrazone in which the absorption and emission maxima are slightly red shifted (528 nm and 564 nm, respectively in dioxane) from the unsubstituted aromatic hydrazone, but the quantum yields of the two hydrazones are equivalent. Thus, an ortho-hydroxy substituted aromatic aldehyde is a suitable electrophile for "turn on" protein labeling using the hydrazino-BDP. The specificity of this labeling reaction for the unnatural amino acid was demonstrated through fluorescent labeling of just the 3-formyltyrosine-containing ?-subunit of ?,?-tubulin. PMID:20886269

Dilek, Ozlem; Bane, Susan L

2010-10-01

51

Synthesis and Spectroscopic Characterization of Fluorescent Boron Dipyrromethene-Derived Hydrazones  

PubMed Central

Derivatives of 4,4-difluoro-4-bora-3a,4a, diaza-s-indacene (BODIPY® or BDP) that possess a hydrazine substituent on position 5 are potential “turn-on” fluorophores for labeling aldehydes The unnatural amino acid L-3-formyltyrosine can be incorporated into a protein or peptide; thus, these hydrazines are potentially site specific labels for such polymers. In this work, model compounds were synthesized to assess whether the photochemical properties of the BDP-hydrazone would be suitable for protein labeling. Hydrazones were synthesized from the fluorophore 3-chloro-5-hydrazino-BDP and different aldehydes, and the absorption and emission spectra of the products were compared. The hydrazone of an unsubstituted aromatic aldehyde displays absorption and emission maxima (531 nm and 559 nm, respectively in dioxane) that are red shifted relative to those of a hydrazone from an aliphatic aldehyde (513 nm and 543 nm, respectively, in dioxane) and an increased quantum yield (0.21 vs. 0.11, respectively, in dioxane). The presence of a hydroxyl group ortho- to the aldehyde produces a hydrazone in which the absorption and emission maxima are slightly red shifted (528 nm and 564 nm, respectively in dioxane) from the unsubstituted aromatic hydrazone, but the quantum yields of the two hydrazones are equivalent. Thus, an ortho-hydroxy substituted aromatic aldehyde is a suitable electrophile for “turn on” protein labeling using the hydrazino-BDP. The specificity of this labeling reaction for the unnatural amino acid was demonstrated through fluorescent labeling of just the 3-formyltyrosine-containing ?-subunit of ?,?-tubulin.

Dilek, Ozlem

2011-01-01

52

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 NH and OH 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

53

The tautomerization between keto- to phenol-hydrazone induced by anions in the solution  

NASA Astrophysics Data System (ADS)

Two simple anion receptors, 2-[(2-hydroxy-5-nitrophenyl)methylene]hydrazone (1) and 2-[(3,5-dibromo-2-hydroxyphenyl)methylene]hydrazone (2) with -OH binding sites, were synthesized and characterized. The anion binding ability of receptors 1 and 2 with halide anions (F-, Cl-, Br- and I-), AcO- and HPO4- was investigated using visual (naked-eye), UV-vis titration experiments in dry DMSO together with DFT theoretical calculation. The addition of F-, AcO- and HPO4- to the host solution resulted in a red shift of the charge-transfer absorbance band accompanied by a color change from yellow to orange in the naked-eye experiments. Receptor 1 containing a nitro group at the para position and receptor 2 containing two bromine groups at the ortho and para positions both showed strong binding ability for HPO4- ion in the form of phenol-hydrazone. Moreover, receptor 1, induced by anion species in the solution, converted to the form of phenol-hydrazone from keto-hydrazone.

Shang, Xuefang; Yuan, Jianmei; Wang, Yingling; Zhang, Jinlian; Xu, Xiufang

2012-02-01

54

Synthesis and antibacterial activity against ralstonia solanacearum for novel hydrazone derivatives containing a pyridine moiety  

PubMed Central

Background Ralstonia solanacearum, one of the most important bacterial diseases on plants, is a devastating, soil-borne plant pathogen with a global distribution and an unusually wide host range. In order to discover new bioactive molecules and pesticides acting on tobacco bacterial wilt, we sought to combine the active structure of hydrazone and pyridine together to design and synthesize a series of novel hydrazone derivatives containing a pyridine moiety. Results A series of hydrazone derivatives containing a pyridine moiety were synthesized. Their structures were characterized by 1 H-NMR, 13 C-NMR, IR, and elemental analysis. The preliminary biological activity tests showed that compound 3e and 3g exhibited more than 80% activity against Ralstonia solanacearum at 500 mg/L, especially compound 3g displayed relatively good activity to reach 57.0% at 200 mg/L. Conclusion A practical synthetic route to hydrazone derivatives containing a pyridine moiety by the reaction of intermediates 2 with different aldehydes in ethanol at room temperature using 2-chloronicotinic acid and 2-amino-5-chloro-3-methylbenzoic acid as start materials is presented. This study suggests that the hydrazone derivatives containing a substituted pyridine ring could inhibit the growth of Ralstonia solanacearum.

2012-01-01

55

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

NASA Astrophysics Data System (ADS)

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

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

2011-12-01

56

A switching cascade of hydrazone-based rotary switches through coordination-coupled proton relays  

NASA Astrophysics Data System (ADS)

Imidazole, a subunit of histidine, plays a crucial role in proton-relay processes that are important for various biological activities, such as metal efflux, viral replication and photosynthesis. We show here how an imidazolyl ring incorporated into a rotary switch based on a hydrazone enables a switching cascade that involves proton relay between two different switches. The switching process starts with a single input, zinc(II), that initiates an E/Z isomerization in the hydrazone system through a coordination-coupled proton transfer. The resulting imidazolium ring is unusually acidic and, through proton relay, activates the E/Z isomerization of a non-coordinating pyridine-containing hydrazone switch. We hypothesize that the reduction in the acid dissociation constant of the imidazolium ring results from a combination of electrostatic and conformational effects, the study of which might help elucidate the proton-coupled electron-transfer mechanism in photosynthetic bacteria.

Ray, Debdas; Foy, Justin T.; Hughes, Russell P.; Aprahamian, Ivan

2012-09-01

57

The ligational behavior of an isatinic quinolyl hydrazone towards copper(II)- ions  

PubMed Central

Background The importance of the isatinic quinolyl hydrazones arises from incorporating the quinoline ring with the indole ring. Quinoline ring has therapeutic and biological activities whereas, the indole ring occurs in Jasmine flowers and Orange blossoms. As a ligand, the isatin moiety is potentially ambidentate and can coordinate the metal ions either through its lactam or lactim forms. In a previous study, the ligational behavior of a phenolic quinolyl hydrazone towards copper(II)- ions has been studied. As continuation of our interest, the present study is planned to check the ligational behavior of an isatinic quinolyl hydrazone. Results New homo- and heteroleptic copper(II)- complexes were obtained from the reaction of an isatinic quinolyl hydrazone (HL) with several copper(II)- salts viz. Cl?, Br?, NO3?, ClO4-, SO42- and AcO-. The obtained complexes have Oh, Td and D4h- symmetry and fulfill the strong coordinating ability of Cl?, Br?, NO3? and SO42- anions. Depending on the type of the anion, the ligand coordinates the copper(II)- ions either through its lactam (NO3? and ClO4-) or lactim (the others) forms. Conclusion The effect of anion for the same metal ion is obvious from either the geometry of the isolated complexes (Oh, Td and D4h) or the various modes of bonding. Also, the obtained complexes fulfill the strong coordinating ability of Cl?, Br?, NO3? and SO42- anions in consistency with the donor ability of the anions. In case of copper(II)- acetate, a unique homoleptic complex (5) was obtained in which the AcO- anion acts as a base enough to quantitatively deprotonate the hydrazone. The isatinic hydrazone uses its lactim form in most complexes.

2011-01-01

58

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

59

Lanthanide Complexes of Substituted ?-Diketone Hydrazone Derivatives: Synthesis, Characterization, and Biological Activities  

PubMed Central

A series of ?-diketone hydrazone derivatives have been synthesized through condensation of ?-diketone with aromatic aldehydes followed by reaction with phenylhydrazine. The structure of the ligands and intermediates are well defined through elemental and spectroscopic analyses. These hydrazones are potential ligands toward lanthanide metal ions. New complexes of trivalent Scandium, Yttrium, Lanthanum, and Cerium have been synthesized. The composition of these complexes is discussed on the basis of elemental analyses, IR, magnetic moments, and thermal analyses. The prepared complexes were screened for antibacterial and antifungal properties and have exhibited potential activity.

Hegazy, W. H.; Al-Motawaa, I. H.

2011-01-01

60

Asymmetric Synthesis of 3-Substituted 4-Oxoesters Using the SAMP\\/RAMP-Hydrazone Method  

Microsoft Academic Search

. Based on aldehydes 1a-f or ketone 1g, 3-substituted 4-oxo esters 6a-g were synthesized in three steps in moderate to good overall yield (12-50%) and in excellent enantiomeric excesses ($ee >90\\\\to 95$%) by an Umpolung-strategy employing the SAMP-\\/RAMP-hydrazone method. The key step in the synthesis is the highly diastereoselective alkylation of lithiated SAMP-hydrazones 3a-g (chiral d$^2$-nucleophiles) with tert-butyl bromoacetate (4)

D. Enders; U. Baus; P. Müller; K. C. Nicolaou; B. Jandeleit

1998-01-01

61

Synthesis of hydrazones derivatives of quinoxalinone--prospective antimicrobial and antiinflammatory agents.  

PubMed

A series of quinoxalinone derivatives was synthesized by the condensation of 1,2-diaminobenzene with alpha-ketoglutaric acid to yield 3-(3-oxo-3,4-dihydroquinoxalin-2-yl) propionic acid (2) and then treated with hydrazine hydrate to yield its hydrazones (3). This was further reacted with substituted aromatic aldehydes to produce final compounds (4a-r). These hydrazones derivatives were characterized by FT-IR and 1H-NMR data. All the synthesized compounds were evaluated for their antimicrobial and antiinflammatory activity. PMID:19719051

Khan, Suroor A; Mullick, Pooja; Pandit, Shabir; Kaushik, Darpan

62

Hydrazides/Hydrazones as Antimicrobial and Anticancer Agents in The New Millennium.  

PubMed

Hydrazide/hydrazone derivatives are of quite interest for medicinal chemists because of their vast spectrum of biological activity. Literature reports reveal that the hydrazide derivatives have been extensively studied for their biological profile during the past decade. The aim of the present work is to collect literature reports focusing the antimicrobial and anticancer study of different hydrazide/hydrazone derivatives carried out during the past decade which will serve as a valuable source of information for the researchers working in the field of antimicrobial and anticancer research. PMID:23621636

Kumar, Pradeep; Narasimhan, Balasubramanian

2013-04-25

63

Hydrazides/hydrazones as antimicrobial and anticancer agents in the new millennium.  

PubMed

Hydrazide/hydrazone derivatives are of quite interest for medicinal chemists because of their vast spectrum of biological activity. Literature reports reveal that the hydrazide derivatives have been extensively studied for their biological profile during the past decade. The aim of the present work is to collect literature reports focusing the antimicrobial and anticancer study of different hydrazide/hydrazone derivatives carried out during the past decade which will serve as a valuable source of information for the researchers working in the field of antimicrobial and anticancer research. PMID:23621689

Kumar, Pradeep; Narasimhan, Balasubramanian

2013-06-01

64

21 CFR 522.1465 - Naltrexone hydrochloride injection.  

Code of Federal Regulations, 2013 CFR

...2013-04-01 2013-04-01 false Naltrexone hydrochloride injection. 522.1465...FORM NEW ANIMAL DRUGS § 522.1465 Naltrexone hydrochloride injection. (a) Specifications...aqueous solution contains 50 milligrams of naltrexone hydrochloride. (b) Sponsor....

2013-04-01

65

21 CFR 522.1465 - Naltrexone hydrochloride injection.  

Code of Federal Regulations, 2010 CFR

...2009-04-01 2009-04-01 false Naltrexone hydrochloride injection. 522.1465...FORM NEW ANIMAL DRUGS § 522.1465 Naltrexone hydrochloride injection. (a) Specifications...aqueous solution contains 50 milligrams of naltrexone hydrochloride. (b) Sponsor....

2009-04-01

66

Guidance on Quinapril Hydrochloride Active ingredient ...  

Center for Drug Evaluation (CDER)

Text VersionPage 1. Contains Nonbinding Recommendations Guidance on Quinapril Hydrochloride This guidance represents the Food ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

67

Draft Guidance on Ziprasidone Hydrochloride Active ...  

Center for Biologics Evaluation and Research (CBER)

Text VersionPage 1. Contains Nonbinding Recommendations Draft Guidance on Ziprasidone Hydrochloride This draft guidance, once ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

68

21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.  

Code of Federal Regulations, 2013 CFR

... Proparacaine hydrochloride ophthalmic solution. 524.1982 Section 524.1982 ...Proparacaine hydrochloride ophthalmic solution. (a) Specifications. The drug is an aqueous solution containing 0.5 percent...

2013-04-01

69

Development of novel aroylhydrazone ligands for iron chelation therapy: 2-Pyridylcarboxaldehyde isonicotinoyl hydrazone analogs  

Microsoft Academic Search

Previous studies have demonstrated that aroylhydrazone iron (Fe) chelators of the pyridoxal isonicotinoyl hydrazone (PIH) class have high Fe chelation efficacy both in vitro and in vivo. Depending on their design, these drugs may have potential as agents for the treatment of Fe overload disease or cancer. Considering the high potential of this class of ligands, we have synthesized seven

Erika Becker; Des R Richardson

1999-01-01

70

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...

71

Comparison of Hydrazone Heterobifunctional Crosslinking Agents for Reversible Conjugation of Thiol-Containing Chemistry  

PubMed Central

Reversible covalent conjugation chemistries that allow site- and condition-specific coupling and uncoupling reactions are attractive components in nanotechnologies, bioconjugation methods, imaging and drug delivery systems. Here, we compare three heterobifunctional crosslinkers, containing both thiol- and amine- reactive chemistry, to form pH-labile hydrazones with hydrazide derivatives of the known and often published water-soluble polymer, poly[N-(2-hydroxypropyl methacrylamide)] (pHPMA), while subsequently coupling thiol-containing molecules to the crosslinker via maleimide addition. Two novel crosslinkers were prepared from the popular heterobifunctional crosslinking agent, succinimidyl-4-(N-maleimidomethyl) cyclohexane-1-carboxylate (SMCC), modified to contain either terminal aldehyde groups (i.e., 1-(N-3-propanal)-4-(N-maleimidomethyl) cyclohexane carboxamide, PMCA) or methylketone groups (i.e., 1-(N-3-butanone)-4-(N-maleimidomethyl) cyclohexane carboxamide, BMCA). A third crosslinking agent was the commercially available N-4-acetylphenyl maleimide (APM). PMCA and BMCA exhibited excellent reactivity towards hydrazide-derivatized pHPMA with essentially complete hydrazone conjugation to polymer reactive sites, while APM coupled only ~ 60% of available reactive sites on the polymer despite a 3-fold molar excess relative to polymer hydrazide groups. All polymer hydrazone conjugates bearing these bifunctional agents were then further reacted with thiol-modified tetramethylrhodamine dye, confirming crosslinker maleimide reactivity after initial hydrazone polymer conjugation. Incubation of dye-labeled polymer conjugates in phosphate buffered saline at 37°C showed that hydrazone coupling resulting from APM exhibited the greatest difference in stability between pH 7.4 and 5.0, with hydrolysis and dye release increased at pH 5.0 over a 24hr incubation period. Polymer conjugates bearing hydrazones formed from crosslinker BMCA exhibited intermediate stability with hydrolysis much greater at pH 5.0 at early time points, but hydrolysis at pH 7.4 was significant after 5 hrs. Hydrazones formed with the PMCA crosslinker showed no difference in release rates at pH 7.4 and 5.0.

Christie, R. James; Anderson, Diana J.; Grainger, David W.

2010-01-01

72

Synthesis and antifungal activity of novel pyrazolecarboxamide derivatives containing a hydrazone moiety  

PubMed Central

Background The plant pathogenic fungus (such as Gibberella zeae, Fusarium oxysporum and Cytospora mandshurica) causes devastating disease in agriculture. The pathogenic fungus is responsible for billions of dollars in economic losses worldwide each year. In order to discover new fungicidal molecule with good fungicidal activity against G. zeae, F. oxysporum, and C. mandshurica, we sought to combine the active sub-structure of hydrazone and pyrazole amide derivatives together to design and synthesize novel pyrazole amide derivatives containing a hydrazone moiety. Results A series of novel pyrazole amide derivatives bearing hydrazone moiety were synthesized. Their structures were characterized by 1?H-NMR, 13?C-NMR, IR, and elemental analysis. The preliminary biological assays revealed that most of the synthesized compounds exhibit favorable antifungal activities against G. zeae. The activity of compounds 7a, 7f, 7g, 7h, 7i, 7j, 7l and 7q were 40.82%, 47.78%, 50.32%, 40.82%, 49.05%, 48.73%, 40.19% and 45.89%, respectively, and the synthesized compounds showed certain antifungal activities against F. oxysporum and C.mandshurica. Conclusion A practical synthetic route to pyrazole amide derivatives containing a hydrazone moiety were synthesized by the condensation of intermediates 5-chloro-N-(4-subsititued-2-(hydrazinecarbonyl)-6-methylphenyl)-1,3-dimethyl-1?H-pyrazole-4-carboxamide with different aldehydes or ketones in ethanol at room temperature is presented, the results of the study suggested that the pyrazole amide derivatives containing hydrazone moieties could inhibit the growth of G. zeae, F. oxysporium and C. mandshurica to a certain extent.

2012-01-01

73

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

2012-01-11

74

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

2012-07-20

75

Immobilization of swift foxes with ketamine hydrochloride-xylazine hydrochloride  

USGS Publications Warehouse

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

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

2002-01-01

76

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.

2011-01-01

77

21 CFR 184.1676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2013 CFR

...hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food Chemicals Codex, 3d Ed. (1981), p. 260, which is incorporated by reference. Copies are available from the National Academy Press,...

2013-04-01

78

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

79

A novel asymmetric synthesis of cinacalcet hydrochloride  

PubMed Central

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

Gorentla, Laxminarasimhulu; Dubey, Pramod K

2012-01-01

80

A novel asymmetric synthesis of cinacalcet hydrochloride.  

PubMed

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

Arava, Veera R; Gorentla, Laxminarasimhulu; Dubey, Pramod K

2012-08-24

81

The time evolution of space charge limited current magnitudes in a hydrazone-doped polyester  

Microsoft Academic Search

The dc current–voltage properties of amorphous thin films of hydrazone-doped polyester samples have been monitored as a function of time following deposition of gold contacts. Hole currents injected from gold electrodes in contact with the bottom surface of the films are observed to increase in magnitude as the samples progressively age with a saturated current–voltage response eventually obtained after a

J. M Fair; D. M Goldie; R. A. G Gibson

1998-01-01

82

Some N-methyl-N-(4-chloro-1-phthalazinyl)hydrazones  

Microsoft Academic Search

N-Methyl-N-(4-chloro-1-phthalazinyl)-(E)-hydrazones of the corresponding carbonyl compounds were obtained by condensation of 1-methyl-1-(4-chloro-1-phthalazinyl)hydrazine with carbonyl compounds. The PMR spectra of the products in a number of solvents at various temperatures and the UV spectra in solution and in the solid form were recorded. It was established that a change in the nature of the substituents in the ylidene fragment leads to

B. I. Buzykin; N. N. Bystrykh; A. P. Stolyarov; S. A. Flegontov; Yu. P. Pitaev

1978-01-01

83

Pyridoxal isonicotinoyl hydrazone (PIH) prevents copper-mediated in vitro free radical formation  

Microsoft Academic Search

Pyridoxal isonicotinoyl hydrazone (PIH) is an iron chelator with antioxidant activity, low toxicity and is useful in the experimental treatment of iron-overload diseases. Previous studies on x-ray diffraction have revealed that PIH also forms a complex with Cu(II). Since the main drug of choice for the treatment of Wilson's disease, d-penicillamine, causes a series of side effects, there is an

Marcelo Hermes-Lima; Márcia S. Gonçalves; Roberto G. Andrade

2001-01-01

84

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

85

A theoretical study of the geometrical structures of the hydrazones and their protonated complexes  

Microsoft Academic Search

1.N-N and N=C bond lengths and values of the NNC valence angles have been calculated for the hydrazones and their protonated complexes. Protonation does not lead to an essential alteration of the geometrical parameters of these compounds.2.The electrostatic potential map for the protonated complex shows two minima, these corresponding to the protons at the amine and imine nitrogen atoms.3.Study of

V. V. Zverev; Z. G. Bazhanova; L. V. Ermolaeva

1979-01-01

86

Physicochemical studies and CO adsorption on zeolite-encapsulated Mn II, Mn III–hydrazone complexes  

Microsoft Academic Search

Complexes of Mn(II) and Mn(III) with N2O3 hydrazone ligand derived from salicylaldehyde and benzenesulphonylhydrazide have been encapsulated in zeolite Y- supercages by a diffusion method. The synthesized new materials have been characterized by combination of elemental analysis, FT-IR, UV–vis., magnetic measurements, XRD, thermal analysis (TG, DTG and DTA), as well as surface area measurements and nitrogen adsorption studies. Investigation of

Ayman H. Ahmed

2007-01-01

87

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

Microsoft Academic Search

Copper(II), cobalt(II) and nickel(II) complexes of hydrazone ligand (SAPH) derived from salicylaldehyde and phenylhydrazine have been encapsulated in zeolite-Y super cages via ship-in-a-bottle synthesis. Detailed characterization of the intrazeolitic complexes were performed by elemental analysis, spectral (FT-IR, UV–Vis.) studies, magnetic measurements and X-ray diffraction. Furthers, surface texture and thermal analysis (TG, DTG, DTA) have provided further evidence for successful immobilization

Ayman H. Ahmed; M. S. Thabet

88

Treatment of premature ejaculation with paroxetine hydrochloride  

Microsoft Academic Search

Aims of this study: To evaluate the efficacy of chronic and ‘on demand’ administration of paroxetine hydrochloride in the drug treatment of premature ejaculation (PE).Materials and methods: Ninety-four normally potent men, aged 18–61 y (mean 39 y) with premature ejaculation were treated between January 1996 and March 1997, with oral paroxetine hydrochloride, a selective serotonin re-uptake inhibitor (SSRI). All men

CG McMahon; K Touma

1999-01-01

89

Biaryl amides and hydrazones as therapeutics for prion disease in transgenic mice.  

PubMed

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; Prusiner, Stanley B

2013-08-21

90

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

PubMed

Ruthenium(II) hydrazone Schiff base complexes of the type [RuCl(CO)(B)(L)] (were B=PPh(3), AsPh(3) or Py; L=hydrazone Schiff base ligands) were synthesized from the reactions of hydrazone Schiff base ligand (obtained from isonicotinoylhydrazide and different hydroxy aldehydes) with [RuHCl(CO)(EPh(3))(2)(B)] (where E=P or As; B=PPh(3), AsPh(3) or Py) in 1:1 molar ratio. All the new complexes have been characterized by analytical and spectral (FT-IR, electronic, (1)H, (13)C and (31)P NMR) data. They have been tentatively assigned an octahedral structure. The synthesized complexes have exhibited catalytic activity for oxidation of benzyl alcohol to benzaldehyde and cyclohexanol to cyclohexanone in the presence of N-methyl morpholine N-oxide (NMO) as co-oxidant. They were also found to catalyze the transfer hydrogenation of aliphatic and aromatic ketones to alcohols in KOH/Isopropanol. PMID:21924947

Manikandan, R; Viswanathamurthi, P; Muthukumar, M

2011-08-27

91

Octenidine hydrochloride in hydatid disease.  

PubMed

Hydatid disease is still endemic in many devoloping countries and continues to be an important cause of morbidity. The objective of this study was to determine the in vitro scolicidal effects of octenidine hydrochloride in different concentrations using different exposure times. After hydatid cyst liquid was left to precipitate for 1 h to obtain cystic sand, various concentrations of octenidine (undiluted, 1% and 0.1% diluted) were added to concentrated hydatid cyst sediments for 5, 10, 15, 20, 25, 30, 45, and 60 min, and scolicidal effects of octenidine were compared with 20% saline and control group for the same times. It was found that undiluted octenidine had a strong scolicidal effect at 15 min compared to saline at 20%. One percent octenidine had a scolicidal effect at 30 min. However, 0.1% octenidine did not have enough scolicidal effect in 1 h. It was concluded that undiluted and 1% diluted octenidine might be used for scolicidal purpose in the treatment of hydatid disease. PMID:14761827

Altindis, Mustafa; Arikan, Yuksel; Cetinkaya, Zafer; Polat, Coskun; Yilmaz, Sezgin; Akbulut, Gökhan; Dilek, Osman Nuri; Gokce, Ozcan

92

Structural Studies and Investigation on the Activity of Imidazole-Derived Thiosemicarbazones and Hydrazones against Crop-Related Fungi.  

PubMed

New imidazole derived thiosemicarbazones and hydrazones were prepared by condensation of 4(5)-imidazole carboxaldehyde, 4-(1H-imidazole-1-yl)benzaldehyde and 4-(1H-imidazole-1-yl)acetophenone with a thiosemicarbazide or hydrazide. All compounds were characterized by quantitative elemental analysis, IR and NMR techniques. Eight structures were determined by single crystal X-ray diffraction. The antifungal activities of the compounds were evaluated. None of the compounds exhibited significant activity against Aspergillus flavus and Candida albicans, while 4(5)-imidazolecarboxaldehyde thiosemicarbazone (ImT) and 4-(1H-imidazole-1-yl)benzaldehyde thiosemicabazone (4ImBzT) were highly and selectively active against Cladosporium cladosporioides. 4(5)-Imidazolecarboxaldehyde benzoyl hydrazone (4(5)ImPh), 4(5)-imidazolecarboxaldehyde-para-chlorobenzoyl hydrazone (4(5)ImpClPh), 4(5)-imidazolecarboxaldehyde-para-nitrobenzoyl hydrazone (4(5)ImpNO2Ph), 4-(imidazole-1-yl)acetophenone-para-chloro-benzoyl hydrazone (4ImAcpClPh) and 4-(imidazole-1-yl)acetophenone-para-nitro-benzoylhydrazone (4ImAcpNO2Ph) were highly active against Candida glabrata. 4(5)ImpClPh and 4(5)ImpNO2Ph were very effective against C. cladosporioides. In many cases, activity was superior to that of the reference compound nystatin. PMID:24129274

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

2013-10-14

93

21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.  

Code of Federal Regulations, 2010 CFR

...Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section...OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage...

2010-04-01

94

21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.  

Code of Federal Regulations, 2010 CFR

...Food and Drugs 6 2009-04-01 2009-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section...OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage...

2009-04-01

95

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

NASA Astrophysics Data System (ADS)

Copper(II), cobalt(II) and nickel(II) complexes of hydrazone ligand (SAPH) derived from salicylaldehyde and phenylhydrazine have been encapsulated in zeolite-Y super cages via ship-in-a-bottle synthesis. Detailed characterization of the intrazeolitic complexes were performed by elemental analysis, spectral (FT-IR, UV-Vis.) studies, magnetic measurements and X-ray diffraction. Furthers, surface texture and thermal analysis (TG, DTG, DTA) have provided further evidence for successful immobilization of the metal complexes inside zeolite Y. Investigation of the stereochemistry of these incorporated chelates pointed out that, SAPH ligand is capable to coordinate with the central metal through the (CN), phenolic (OH) and (NH) groups forming polynuclear structures. The involvement of zeolite oxygen in coordination was postulated in the hybrid materials. The intrazeolitic copper, cobalt and nickel-SAPH complexes have distorted tetrahedral, octahedral and square-pyramidal configurations, respectively. The zeolite encapsulated complexes are thermally stable up to 800 °C except Cu(II) sample which is thermally stable up to midpoint 428 °C. The assessment of the catalytic activity was performed by the use of the photo-degradation of acid violet-1 dye as a probe reaction in presence of H2O2 as an oxidant. Decolorization of acid violet-1 dye was examined under the same conditions whereas the unpromoted zeolite and CuII, CoII, NiII-hydrazone complexes supported on zeolite showed 13% and 76%, 53%, 43% color removal, respectively. The results revealed that, the zeolite encapsulated Cu(II) complex generally exhibited better catalytic efficiency (76%) compared with other investigated zeolite encapsulated metal-hydrazone samples.

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

2011-12-01

96

Two new pseudohalide-bridged Cu(II) complexes with a hydrazone ligand: Syntheses, crystal structures and magnetic studies  

Microsoft Academic Search

Two new pseudohalide-bridged copper(II) complexes [{Cu(PBH)(?1,1-CNO)}2] (1) and {Cu(PBH)(?1,5-NCNCN)}n (2) (where HPBH=2-pyridinecarboxaldehyde benzoyl hydrazone) have been synthesised and characterised by elemental analysis, CV, IR and UV–Vis spectral studies. The tridentate hydrazone pro-ligand (HPBH) was obtained by the condensation of benzhydrazide and pyridine-2-carboxaldehyde. Structures of both complexes have been established by X-ray crystallography which shows that 1 is a ?1,1-CNO?-bridged dimer

Sambuddha Banerjee; Soma Sen; Subhra Basak; Samiran Mitra; David L. Hughes; Cédric Desplanches

2008-01-01

97

Nuclear magnetic resonance investigations of azo-hydrazone, acid-base equilibria of FD&C Yellow No. 6  

Microsoft Academic Search

Azo-hydrazone, acid-base equilibria were examined for the water-soluble dye FD&C Yellow No. 6 (Y6), with the observation of dynamic NMR effects near, and at, pH 12, where the dye converts from a predominantly hydrazone tautomer (acidic to moderately basic pH) to a prevailing azo-anion resonance hybrid (high pH). Semilogarithmatic pH-13C chemical shift plots and a 2-bond, 15N?-13C8a coupling constants vs.

William F. Reynolds; Kathy W. Nielsen; S BELL; J BARROWS; J BAILEYJR; E MOUCHAHOIR; S PRESCOTT; M ARCHER; M OLIVER

1996-01-01

98

Effects of ?-Alkoxy Substitution and Conformational Constraints on 6-exo Radical Cyclizations of Hydrazones via Reversible Thiyl and Stannyl Additions  

PubMed Central

Access to multifunctional hydrazones of relevance to dysiherbaine synthesis studies is described. Subsequent radical cyclizations of multifunctional hydrazones via a Si- and C-linked tethering strategy are shown to function effectively in 6-exo fashion. Conformational constraints are proposed to play a key role in suppressing unproductive premature reduction pathways. The stereochemical outcomes suggest that minimizing the dipole repulsion between neighboring C=N and C-O bonds favors a C?-C(=N) dihedral angle placing the C=N bond axial within a chairlike transition state, in contrast to the usual Beckwith-Houk model.

Friestad, Gregory K.; Mathies, Alex K.

2007-01-01

99

Reactions of group 6 metal carbonyls with salicylaldehyde isonicotinic acid hydrazone  

Microsoft Academic Search

Sunlight irradiation of the reactions of [M(CO)6], M?=?Cr, Mo and W with salicylaldehyde isonicotinic acid hydrazone (H2salnah) in THF were investigated. Interaction of [Cr(CO)6] with H2salnah resulted in formation [Cr2O2(H2salnah)2]. The corresponding reactions of molybdenum and tungsten carbonyls yielded dinuclear oxo complexes [M2O6(H2salnah)]. All complexes were characterized by elemental analysis, IR, mass spectrometry and H NMR spectroscopy. The IR spectra

Saadia A. Ali

2007-01-01

100

Hydrazones of 1,2-benzisothiazole hydrazides: synthesis, antimicrobial activity and QSAR investigations  

Microsoft Academic Search

A series of hydrazones of 1,2-benzisothiazole hydrazides 1a–m, 2a–m, 3a–m, 4a–m, 5a–m as well as their cyclic (1 and 4) and acyclic (2, 3 and 5) 1,2-benzisothiazole parent hydrazides, were synthesised and evaluated as antibacterial and antifungal agents. All of the 2-amino-1,2-benzisothiazol-3(2H)-one derivatives, belonging to series I and IV, showed a good antibacterial activity against Gram positive bacteria. Most of

Paola Vicini; Franca Zani; Pietro Cozzini; Irini Doytchinova

2002-01-01

101

SYNTHESIS AND STRUCTURAL STUDIES OF SOME LANTHANIDE COMPLEXES OF SALICYLALDEHYDE ANTHRANOYL HYDRAZONE  

Microsoft Academic Search

Lanthanide complexes of the types Ln(sah)(OAc)·xH2O and Ln?(Hsah)2(X)·xH2O [Ln=Y, La, Nd, Gd, Tb and Dy; Ln?=Pr and Sm, X=NO3 and Cl; H2sah=salicylaldehyde anthranoyl hydrazone were synthesized and characterized by various physico-chemical techniques. The complexes are coloured and highly soluble in methanol, DMSO and DMF. Dehydration studies indicate the presence of both lattice-held and coordinated water molecules. IR, electronic and H

T. R. Rao; Sabita Shrestha; Archana Prasad; K. K. Narang

2002-01-01

102

RP-HPLC and Spectrophotometric Estimation of Ambroxol Hydrochloride and Cetirizine Hydrochloride in Combined Dosage Form  

PubMed Central

Rapid, precise, accurate, specific and sensitive reverse phase liquid chromatographic and absorbance ratio spectrophotometric methods have been developed for the simultaneous analysis of ambroxol hydrochloride and cetirizine hydrochloride in their tablet formulation. The chromatographic methods were standardized using a HIQ SIL-C18 column (250×4.6 mm i.d., 10 ?m particle size) with UV detection at 229 nm and mobile phase consisting of methanol-acetonitrile-water (40:40:20, v/v/v). Ambroxol hydrochloride and cetirizine hydrochloride have absorbance maxima at 243 nm and 229 nm, respectively. The isoabsorptive wavelength for both the drugs was 236 nm. For absorbance ratio method developed, wavelengths selected were 243 nm and 236 nm. The proposed methods were successfully applied to the determination of ambroxol hydrochloride and cetirizine hydrochloride in tablets, with high percentage of recovery, good accuracy and acceptable precision. Different analytical performance parameters such as linearity, precision, accuracy, limit of detection, limit of quantitation and robustness were determined according to International Conference on Harmonization ICH Q2B guidelines. Results of analysis of the developed method were compared by performing ANOVA.

Bhatia, Neela M.; Ganbavale, S. K.; Bhatia, M. S.; More, H. N.; Kokil, S. U.

2008-01-01

103

21 CFR 556.580 - Robenidine hydrochloride.  

Code of Federal Regulations, 2013 CFR

...OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL...for residues of robenidine hydrochloride in edible tissues of chickens as follows: (a) 0.2 part per million in skin and...

2013-04-01

104

21 CFR 184.1875 - Thiamine hydrochloride.  

Code of Federal Regulations, 2013 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...

2013-04-01

105

Synthesis, spectral characterization, in-vitro microbiological evaluation and cytotoxic activities of novel macrocyclic bis hydrazone.  

PubMed

A macrocyclic hydrazone Schiff base was synthesized by reacting 1,4-dicarbonyl phenyl dihydrazide with 2,6-diformyl-4-methyl phenol and a series of metal complexes with this new Schiff base were synthesized by reaction with Co(II), Ni(II) and Cu(II) metal salts. The Schiff base and its complexes have been characterized by elemental analyses, IR, (1)H NMR, UV-vis, FAB mass, ESR spectra, fluorescence, thermal, magnetic and molar conductance data. The analytical data reveal that the Co(II), Ni(II) and Cu(II) complexes possess 2:1 metal-ligand ratios. All the complexes are non-electrolytes in DMF and DMSO due to their low molar conductance values. Infrared spectral data suggest that the hydrazone Schiff base behaves as a hexadentate ligand with NON NON donor sequence towards the metal ions. The ESR spectral data shows that the metal-ligand bond has considerable covalent character. The electrochemical behavior of the copper(II) complex was investigated by cyclic voltammetry. The Schiff base and its complexes have also been screened for their antibacterial (Escherichia coli, Staphylococcus aureus, Shigella dysentery, Micrococcus, Bacillus subtilis, Bacillus cereus and Pseudomonas aeruginosa) and antifungal activities (Aspergillus niger, Penicillium and Candida albicans) by MIC method. The brine shrimp bioassay was also carried out to study their in-vitro cytotoxic properties. PMID:19419802

Avaji, Prakash Gouda; Kumar, C H Vinod; Patil, Sangamesh A; Shivananda, K N; Nagaraju, C

2009-04-05

106

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...

107

SOLID-STATE SYNTHESIS OF HETEROCYCLIC HYDRAZONES USING MICROWAVES UNDER CATALYST-FREE CONDITIONS: JOURNAL ARTICLE (1605)  

EPA Science Inventory

NRMRL-CIN-1605 Jeselnik, M., Varma*, R.S., Polanc, S., and Kocevar, M. Solid-State Synthesis of Heterocyclic Hydrazones using Microwaves under Catalyst-free Conditions. Green Chemistry (White, J.D. (Ed.), Cambridge, United Kingdom: Royal Society of Chemistry) (4):35-38 (2002). ...

108

Interference of isonicotinyl hydrazone in the microbiological analysis of rifampicin from anti-tuberculosis FDC products containing isoniazid  

Microsoft Academic Search

Microbiological assay is a sensitive method for the estimation of rifampicin (R). In the present study, interference due to isonicotinyl hydrazone (HYD), an interaction product of R and isoniazid (H), was checked during microbiological analysis of R, employing Bacillus subtilis and Sarcina lutea. The assays were done by disc diffusion method. Both R and HYD showed linear log response curves

T. T. Mariappan; Thiraviam Geetha; Rajesh Pandey; K. C. Jindal; Saranjit Singh

2004-01-01

109

Enantioselective conjugate addition of donor-acceptor hydrazones to ?,?-unsaturated aldehydes through formal diaza-ene reaction: access to 1,4-dicarbonyl compounds.  

PubMed

Donor-acceptor monosubstituted hydrazones participate as suitable reagents able to undergo an enantioselective formal diaza-ene reaction with ?,?-unsaturated aldehydes under chiral secondary amine catalysis. This constitutes a new approach for the enantioselective conjugate addition of hydrazones to enals under metal-free conditions and leads to the formation of ?-hydrazono carboxylic acids after oxidation/[1,3]-H shift. The methodology is also useful for the synthesis of enantioenriched ?-substituted ?-keto-1,5-diesters by using the hydrazone moiety as a masked carbonyl group. PMID:22780683

Fernández, Maitane; Uria, Uxue; Vicario, Jose L; Reyes, Efraím; Carrillo, Luisa

2012-07-16

110

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.

Uchio, Eiichi

2008-01-01

111

Immobilisation of impala (Aepyceros melampus) with a ketamine hydrochloride/medetomidine hydrochloride combination, and reversal with atipamezole hydrochloride.  

PubMed

A combination of medetomidine hydrochloride (medetomidine) and ketamine hydrochloride (ketamine) was evaluated in 16 boma-confined and 19 free-ranging impalas (Aepyceros melampus) to develop a non-opiate immobilisation protocol. In free-ranging impala a dose of 220 +/- 34 microg/kg medetomidine and 4.4 +/- 0.7 mg/kg ketamine combined with 7500 IU of hyaluronidase induced recumbency within 4.5 +/- 1.5 min, with good muscle relaxation, a stable heart rate and blood pH. PaCO2 was maintained within acceptable ranges. The animals were hypoxic with reduced oxygen saturation and low PaO2 in the presence of an elevated respiration rate, therefore methods for respiratory support are indicated. The depth of sedation was adequate for minor manipulations but additional anaesthesia is indicated for painful manipulations. Immobilisation was reversed by 467 +/- 108 microg/kg atipamezole hydrochloride (atipamezole) intramuscularly, but re-sedation was observed several hours later, possibly due to a low atipamezole:medetomidine ratio of 2:1. Therefore, this immobilisation and reversal protocol would subject impalas to possible predation or conspecific aggression following reversal if they were released into the wild. If the protocol is used on free-ranging impala, an atipamezole:medetomidine ratio of 5:1 should probably be used to prevent re-sedation. PMID:15214689

Bush, M; Raath, J P; Phillips, L G; Lance, W

2004-03-01

112

Intracerebral penetration of carteolol hydrochloride in rats  

Microsoft Academic Search

To elucidate the penetrability of carteolol, a ?-adrenoceptor antagonist (?-blocker) into the brain of rats, intracerebral\\u000a and serum concentrations of the compound were determined in male rats receiving single or repetitive oral administration of\\u000a carteolol hydrochloride at 30?mg\\/kg. The time-course of the intracerebral concentration of carteolol following single IV administration\\u000a of the compound at 10 and 30?mg\\/kg was also studied

S. Kudo; K. Umehara; Yoshifumi Abe; Masayuki Furukawa; Masaaki Odomi

1997-01-01

113

Tapentadol hydrochloride: A centrally acting oral analgesic  

Microsoft Academic Search

Background: Tapentadol hydrochloride is a centrally acting oral analgesic approved by the US Food and Drug Administration in November 2008 for the treatment of moderate to severe acute pain. It is available as immediate-release 50-, 75-, and 100-mg tablets.Objective: The purpose of this article is to review animal studies, pharmacokinetic studies, drug-drug interaction studies, and Phase II\\/III trials of tapentadol

William E. Wade; William J. Spruill

2009-01-01

114

Treatment of premature ejaculation with sertraline hydrochloride  

Microsoft Academic Search

Purpose: To evaluate the efficacy of sertraline hydrochloride in the drug treatment of premature ejaculation (P.E.).Materials and Method: Forty-six normally potent men, aged 22 to 63 years (mean 42 years) with premature ejaculation were treated with oral sertraline in a dose ranging study. All men were either married or in a stable relationship. The mean ejaculatory interval was 1 minute

CG McMahon

1998-01-01

115

21 CFR 520.2345h - Tetracycline hydrochloride, sodium novobiocin, and prednisolone tablets.  

Code of Federal Regulations, 2010 CFR

...2009-04-01 2009-04-01 false Tetracycline hydrochloride, sodium novobiocin...NEW ANIMAL DRUGS § 520.2345h Tetracycline hydrochloride, sodium novobiocin...contains the equivalent of 60 milligrams of tetracycline hydrochloride, 60 milligrams of...

2009-04-01

116

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

Code of Federal Regulations, 2013 CFR

... 2013-07-01 false Hydrochloride salt of a fatty polyalkkylene polyamine (generic...Substances § 721.6196 Hydrochloride salt of a fatty polyalkkylene polyamine (generic...identified generically as Hydrochloride salt of a fatty polyalkkylene...

2013-07-01

117

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

Code of Federal Regulations, 2010 CFR

...Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride B Appendix B to Subpart...Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride 1. Scope This...hydrochloric acid that is liberated when hydroxylamine hydrochloride reacts with...

2009-07-01

118

Mapping Protein Surface Accessibility via an Electron Transfer Dissociation Selectively Cleavable Hydrazone Probe*  

PubMed Central

A protein's surface influences its role in protein-protein interactions and protein-ligand binding. Mass spectrometry can be used to give low resolution structural information about protein surfaces and conformations when used in combination with derivatization methods that target surface accessible amino acid residues. However, pinpointing the resulting modified peptides upon enzymatic digestion of the surface-modified protein is challenging because of the complexity of the peptide mixture and low abundance of modified peptides. Here a novel hydrazone reagent (NN) is presented that allows facile identification of all modified surface residues through a preferential cleavage upon activation by electron transfer dissociation coupled with a collision activation scan to pinpoint the modified residue in the peptide sequence. Using this approach, the correlation between percent reactivity and surface accessibility is demonstrated for two biologically active proteins, wheat eIF4E and PARP-1 Domain C.

Vasicek, Lisa; O'Brien, John P.; Browning, Karen S.; Tao, Zhihua; Liu, Hung-Wen; Brodbelt, Jennifer S.

2012-01-01

119

Bulk synthesis of exfoliated two-dimensional polymers using hydrazone-linked covalent organic frameworks.  

PubMed

Two-dimensional (2D) polymers assemble organic subunits into covalently linked, high-aspect-ratio networks with long-range order. Despite recent advances in 2D polymerization, scalable and general methods to access few- and single-layer materials are limited. Here we exfoliate a hydrazone-linked covalent organic framework (COF) to yield bulk quantities of few-layer two-dimensional (2D) polymers. Immersing the COF powder in several laboratory solvents exfoliates and disperses thin COF-43 samples, which maintain their characteristic periodic hexagonal structure. This phenomenon was characterized using infrared spectroscopy, dynamic light scattering, atomic force microscopy, transmission electron microscopy, and selected area electron diffraction. 2D COFs with reduced interlayer interaction energies offer a new means to access high-aspect-ratio 2D polymers whose structure may be designed using established principles of COF synthesis. PMID:24053107

Bunck, David N; Dichtel, William R

2013-09-26

120

7-Chloro-4-quinolinyl hydrazones: a promising and potent class of antileishmanial compounds.  

PubMed

In this work, we report the antileishmanial evaluation of twenty 7-chloro-4-quinolinyl hydrazone derivatives (1-20). Firstly, the compounds were tested against promastigotes of four different Leishmania species. After that, all derivatives were assayed against L. braziliensis amastigotes and murine macrophages. Furthermore, it was investigated whether the antiamastigote L. braziliensis effect of the compounds could be associated with nitric oxide production. Compounds 6 and 7 showed a strong leishmanicidal activity against intracellular parasite with IC50 in nanogram levels (30 and 20 ng/mL, respectively). Appreciable activity of three compounds tested can be considered an important finding for the rational design of new leads for antileishmanial compounds. PMID:23350797

Coimbra, Elaine S; Antinarelli, Luciana M R; da Silva, Adilson D; Bispo, Marcelle L F; Kaiser, Carlos R; de Souza, Marcus V N

2013-05-01

121

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

PubMed

We describe an efficient and general strategy for the synthesis of dimethyl acetal functionalised steroidal hydrazides based on the cholic acid skeleton with the aim of using these compounds as building blocks for dynamic combinatorial chemistry. Deprotection of the acetal protected building blocks with TFA leads to formation of libraries containing macrocyclic N-acyl hydrazone oligomers. The isolation of several of these, and their characterisation using NMR is described. The effects on the equilibrium library distribution by varying the substituents at C-7 and C-12, extending the side-chain with glycine, and inverting the configuration at C-3 are discussed. Finally, we report the exchange properties of these macrocycles and demonstrate new examples of proof-reading and self-sorting in dynamic combinatorial libraries. PMID:20165810

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

2010-01-11

122

Synthesis, characterization and antibacterial activity of new sulfonyl hydrazone derivatives and their nickel(II) complexes  

NASA Astrophysics Data System (ADS)

Prophane sulfonic acid hydrazide (psh: CH 3CH 2CH 2SO 2NHNH 2) derivatives as salicylaldehydeprophanesulfonylhydrazone (salpsh), 5-methylsalicylaldehydeprophanesulfonylhydrazone (5-msalpsh), 2-hydroxyacetophenoneprophanesulfonylhydrazone (afpsh), 5-methyl-2-hydroxyacetophenoneprophanesulfonylhydrazone (5-mafpsh) and their Ni(II) complexes have been synthesized. The structure of these compounds has been investigated by using elemental analysis, FTIR, 1H NMR, LC/MS, UV-vis spectrophotometric method, magnetic susceptibility and conductivity measurements. The complexes were found to have general compositions [NiL2]. Square-planer structures are proposed for the Ni(II) complexes on the basis of magnetic evidence, electronic spectra and TGA data. Bacterial activities of sulfonyl hydrazone compounds were studied against gram-positive bacteria: Staphylococcus aureus, Bacillus subtilis, Bacillus magaterium and gram-negative bacteria: Salmonella enteritidis, Escherichia coli by using minimum inhibitory concentrations (MICs) method.

Özmen, Ümmühan Özdemir; Olgun, Gülçin

2008-08-01

123

21 CFR 524.1662b - Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment.  

Code of Federal Regulations, 2010 CFR

...Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment...Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment...oxytetracycline and 10,000 units of polymyxin B sulfate. (b) Sponsor....

2009-04-01

124

21 CFR 524.1662b - Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment.  

Code of Federal Regulations, 2010 CFR

...Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment...Oxytetracycline hydrochloride, polymyxin B sulfate ophthalmic ointment...oxytetracycline and 10,000 units of polymyxin B sulfate. (b) Sponsor....

2010-04-01

125

Synthesis, characterization and anticancer evaluation of novel tri-arm star shaped 1,3,5-triazine hydrazones  

NASA Astrophysics Data System (ADS)

A series of novel trisubstituted triazine hydrazones [N3C3(OC6H4-p-CHNNHC(O)C6H4-p-X)3] (X = H, Br, Cl, F, OH, OCH3, CH3, NO2, NH2) were prepared by a three-fold condensation reaction of 2,4,6-tris(4-formylphenoxy)-1,3,5-triazine with p-substituted benzoic acid hydrazides [NH2NHC(O)C6H4-p-X] with excellent yields. The structures were confirmed by elemental analysis, FT-IR, 1H, 13C, 2D-HSQC NMR and mass spectrometry (MALDI-TOF). These derivatives bearing hydrolysable hydrazone linkages were evaluated for their invitro antiproliferative activity against the human liver carcinoma cell line (HepG2) and human cervix carcinoma cell line (HeLa).

Machakanur, Shrinath S.; Patil, Basavaraj R.; Badiger, Dayananda S.; Bakale, Raghavendra P.; Gudasi, Kalagouda B.; Annie Bligh, S. W.

2012-03-01

126

Studies of azo–hydrazone tautomerism and H-bonding in azo-functionalized dendrimers and model compounds  

Microsoft Academic Search

A 13C NMR and UV–visible study of the tautomeric behaviour of azo-functionalized PAMAM (polyamidoamine) dendrimers and the corresponding model compounds in a variety of solvents is reported. Results of these studies indicate that the azo-functionalized PAMAM dendrimers exist as an equilibrium mixture of azo and hydrazone tautomers. A comparison of the behaviour of the dendnmers with model compounds suggests that

Kap-Soo Cheon; Yong S Park; Peter M Kazmaier; Erwin Buncel

2002-01-01

127

The iron chelator pyridoxal isonicotinoyl hydrazone (PIH) protects plasmid pUC18 DNA against OH-mediated strand breaks  

Microsoft Academic Search

Pyridoxal isonicotinoyl hydrazone (PIH) has previously been studied for use in iron chelation therapy in iron-overload diseases. It is an efficient in vitro antioxidant due to its Fe(III) complexing activity (Schulman, H. M., et al. Redox Report1:373–378; 1995). Pathologies associated with iron-overload include hepatic and other cancers. Since oxidative alterations of DNA can be linked to the development of cancer,

Marcelo Hermes-Lima; Eva Nagy; Prem Ponka; Herbert M Schulman

1998-01-01

128

HIV1 Reverse Transcriptase Structure with RNase H Inhibitor dihydroxy benzoyl naphthyl Hydrazone Bound at a Novel Site  

Microsoft Academic Search

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 resolution crystal structure of HIV-1 reverse transcriptase (RT) complexed with dihydroxy benzoyl naphthyl hydrazone (DHBNH), an HIV-1 RT RNase H

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

2007-01-01

129

Physicochemical studies and CO adsorption on zeolite-encapsulated MnII, MnIII hydrazone complexes  

Microsoft Academic Search

Complexes of Mn(II) and Mn(III) with N2O3 hydrazone ligand derived from salicylaldehyde and benzenesulphonylhydrazide have been encapsulated in zeolite Y- supercages by a diffusion method. The synthesized new materials have been characterized by combination of elemental analysis, FT-IR, UV vis., magnetic measurements, XRD, thermal analysis (TG, DTG and DTA), as well as surface area measurements and nitrogen adsorption studies. Investigation

Ayman H. Ahmed

2007-01-01

130

Solid-state oxidation of aniline hydrochloride with various oxidants  

Microsoft Academic Search

Aniline hydrochloride was oxidized in the solid state with three different oxidants: ammonium peroxydisulfate, iron(III) chloride, and silver nitrate. Polyaniline salt was obtained after a few hours when ammonium peroxydisulfate was used as an oxidant. The polymerization of aniline hydrochloride with silver nitrate leads to polyaniline only after several days; in the case of iron(III) chloride, aniline oligomers were obtained.

Ivana Šed?nková; Elena N. Konyushenko; Jaroslav Stejskal; Miroslava Trchová; Jan Prokeš

2011-01-01

131

Flavoxate hydrochloride in the treatment of detrusor instability.  

PubMed

42 patients with 'unstable bladder' were treated with flavoxate hydrochloride. A previous treatment with parasympathicolytic drugs (propantheline bromide and/or emepronium bromide) was unsuccessful. The instability of the detrusor was proven by a urodynamical investigation. Flavoxate hydrochloride is a papaverine-like smooth muscle relaxant. The results and the complications of the treatment are discussed. PMID:610033

Delaere, K P; Michiels, H G; Debruyne, F M; Moonen, W A

1977-01-01

132

Experimental and theoretical study on the absorption and fluorescence properties of substituted aryl hydrazones of 1,8-naphthalimide.  

PubMed

Absorption and fluorescence spectra in acetonitrile for a series of substituted aryl hydrazones of N-hexyl-1,8-naphthalimide are studied with the aim of potential application of the compounds for enzyme activity localization. The influence of the substituents on the spectral characteristics has been evaluated. The absorption and fluorescence energies of substituted aryl-1,8-naphthalimide hydrazones have been calculated with the PCM TDDFT formalism. The M06 and PBE0 functionals, combined with the 6-31+G(d) atomic basis set, have been found to accurately model the excited state properties of the present set of solvated fluorophores. Absorption and fluorescence spectral characteristics have been rationalized in terms of experimental and theoretical electronic indices in order to assess their predictive abilities for application in designing analogues with good emitting properties. An excellent linear dependence is established between the experimental fluorescence and Hammett ?(p)(+) substituent constants and on the other hand ?(p)(+) constants correlate with the theoretically calculated values for the electrostatic potential at nuclei (EPN). A model for predicting the fluorescence properties of substituted hydrazones by means of EPN is drawn, including the polysubstituted derivatives, where Hammett constants are not applicable. PMID:21946815

Cheshmedzhieva, Diana; Ivanova, Plamena; Stoyanov, Stanimir; Tasheva, Donka; Dimitrova, Mashenka; Ivanov, Ivaylo; Ilieva, Sonia

2011-09-22

133

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

2012-09-01

134

Function and stability of abscisic acid acyl hydrazone conjugates by LC-MS2 of ex vivo samples.  

PubMed

We prepare a biotinylated conjugate of the ubiquitous plant hormone (S)-(+)-abscisic acid via an acyl hydrazone linkage at the C4' position and demonstrate in vivo cleavage of the otherwise stable acyl hydrazone linkage using LC-MS2. As part of a wider chemical genomic study, biological activity of the conjugate was assessed using standard epidermal peel and gravimetric transpiration assays, showing significant activity but at a level lower than the unconjugated hormone. When deuterated samples of the conjugate were fed to the plant, however, it was apparent by LC-MS2 experiments that significant levels of hydrolysis of the acyl hydrazone had taken place, contrary to in vitro stability assays in artificial sap. We conclude that abscisic acid is liberated in sufficient quantities to account for the observed physiological response and that LC-MS2 monitoring of conjugates is a simple and practical method by which such events may be assessed, whether in plants or other organisms. PMID:17567162

Smith, Timothy R; Clark, Andrew J; Napier, Richard; Taylor, Paul C; Thompson, Andrew J; Marsh, Andrew

2007-06-14

135

Determination of acetaldehyde in saliva by gas-diffusion flow injection analysis.  

PubMed

The consumption of ethanol is known to increase the likelihood of oral cancer. In addition, there has been a growing concern about possible association between long term use of ethanol-containing mouthwashes and oral cancer. Acetaldehyde, known to be a carcinogen, is the first metabolite of ethanol and it can be produced in the oral cavity after consumption or exposure to ethanol. This paper reports on the development of a gas-diffusion flow injection method for the online determination of salivary acetaldehyde by its colour reaction with 3-methyl-2-benzothiazolinone hydrazone (MBTH) and ferric chloride. Acetaldehyde samples and standards (80 ?L) were injected into the donor stream containing NaCl from which acetaldehyde diffused through the hydrophobic Teflon membrane of the gas-diffusion cell into the acceptor stream containing the two reagents mentioned above. The resultant intense green coloured dye was monitored spectrophotometrically at 600 nm. Under the optimum working conditions the method is characterized by a sampling rate of 9h(-1), a linear calibration range of 0.5-15 mg L(-1) (absorbance=5.40×10(-2) [acetaldehyde, mg L(-1)], R(2)=0.998), a relative standard deviation (RSD) of 1.90% (n=10, acetaldehyde concentration of 2.5 mg L(-1)), and a limit of detection (LOD) of 12.3 ?g L(-1). The LOD and sampling rate of the proposed method are superior to those of the conventional gas chromatographic (GC) method (LOD=93.0 ?g L(-1) and sampling rate=4 h(-1)). The reliability of the proposed method was illustrated by the fact that spiked with acetaldehyde saliva samples yielded excellent recoveries (96.6-101.9%), comparable to those obtained by GC (96.4-102.3%) and there was no statistically significant difference at the 95% confidence level between the two methods when non-spiked saliva samples were analysed. PMID:23790294

Ramdzan, Adlin N; Mornane, Patrick J; McCullough, Michael J; Mazurek, Waldemar; Kolev, Spas D

2013-05-19

136

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

PubMed

Neuropharmacological properties of tolperisone hydrochloride (2,4'-dimethyl-3-piperidinopropiophenone hydrochloride) were investigated in mice, rats and cats. Tolperisone inhibited the spontaneous movement and methamphetamine-induced hyperactivity in mice and the ED50 was approx. 50 mg/kg, s.c. At this dose, tolperisone did not prolong the pentobarbital-induced sleeping time. Tolperisone inhibited convulsions induced by pentylenetetrazol, nicotine and maximum electric shock, but did not affect convulsions induced by strychnine and picrotoxin. Tolperisone induced muscle relaxation in mice and rats in several pharmacological tests, but did not affect neuro-muscular transmission. Tolperisone did not affect conditioned avoidance response in rats and methamphetamine-induced rotational behaviour in nigro-lesioned rats. Tolperisone reduced decerebrated rigidity in cats with i.v. administration of 5 approximately 10 mg/kg and intraduodenal administration of 50 approximately 100 mg/kg. Tolperisone elicited a slight drowsy pattern in the spontaneous EEG of cats at 5 approximately 10 mg/kg, i.v., and inhibited the EEG arousal response and pressor response to stimulation of mesencephalic reticular formation or posterior hypothalamic area. These results suggest that inhibition of the activity in the gamma pathway descending from the mesencephalic reticular formation may be involved in the mechanism of muscle relaxant action of tolperisone. PMID:232053

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

1979-10-01

137

Synthesis and antioxidant activity evaluations of melatonin-based analogue indole-hydrazide/hydrazone derivatives.  

PubMed

Melatonin (MLT) is a hormone synthesized from the pineal gland. It is a direct scavenger of free radicals, which is related to its capability to defend cells from oxidative stress. Recently MLT-related compounds are under investigation to establish which exhibit the maximum activity with the lowest side effects. In this study 5-chloroindole hydrazide/hydrazone derivatives were synthesized from 5-chloroindole-3-carboxaldehyde and phenyl hydrazine derivatives. All the compounds characterized and in vitro antioxidant activity was investigated against MLT and BHT. Most of the compounds showed strong inhibitory effect on the superoxide radical scavenging assay at 1?mM concentration (79 to 95%). Almost all the tested compounds possessed strong scavenging activity against the DPPH radical scavenging activity with IC(50) values (2 to 60 µM). Lastly, compound 1j revealed stronger inhibitory activity against MLT in the LP inhibitory assay at 0.1mM concentration (51%) while the rest of the compounds showed moderate inhibition. PMID:21740102

Y?lmaz, Ayse Didem; Coban, Tulay; Suzen, Sibel

2011-07-08

138

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

PubMed

A new compound, 2-boronobenzaldehyde-(2'-hydroxyl-4'-sulfonic acid) naphthalene hydrazone (1), was synthesized and its structure was characterized by proton nuclear magnetic resonance, mass and element analyses. The presence of Pb(2+) led 1 to undergo colorimetric and fluorescent changes, which were detectable with the naked eye. Thus, a dual spectral response for Pb(2+) detection was introduced. In KH2PO4-NaOH buffer aqueous solution (pH 6.0), 1 exhibited fluorescence enhancement at 568 nm and hyperchromicity at 595 nm upon the addition of Pb(2+). The fluorescent intensity change was proportionate to the concentration of Pb(2+) with a dynamic working range of 5.0×10(-7) mol L(-1) to 1.0×10(-4) mol L(-1) and a detection limit of 3.7×10(-8) mol L(-1). The fluorometric method was successfully applied for the detection of Pb(2+) water of Qianhu Lake and soil in Nanchang university campus. The recoveries were 111-116% for water and 97.6% for soil respectively, determined via the standard addition method. PMID:23542496

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

2013-03-14

139

Photophysical properties of a hydrazone-based switch: A TDDFT study and comparison.  

PubMed

The photophysical properties of a hydrazone-based switch, which can be induced using pH to yield three stable configurations (QPH-E, QPH-Z-H(+) and QPH-Z-H(2)(2+)) and another unstable configuration (QPH-Z). The three stable configuration have been investigated by means of density functional theory (DFT) and time-dependent density functional theory (TDDFT). A generalized gradient approximation (GGA) functional (PBE) and two hybrid-type functional (B3LYP and BH&HLYP) as well as four popular basis sets (6-31G(d,p), SVP, TZVP and DZP) have been selected to calculate the photophysical properties. The solvent effects were in view with the Conductor-like Polarizable Continuum Model (CPCM). Besides, the charge distribution of this switch had been investigated by the pop at the level of the B3YLP/6-31G(d,p) in gas. Results show that the B3LYP functional is more accurate in all simulations. PMID:22522299

Wu, Han; Wang, Yanni; Wang, Hongming; Ju, Yan

2012-03-29

140

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

NASA Astrophysics Data System (ADS)

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

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

2013-05-01

141

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

142

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

Technology Transfer Automated Retrieval System (TEKTRAN)

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

143

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

144

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

145

21 CFR 522.723 - Diprenorphine hydrochloride injection.  

Code of Federal Regulations, 2013 CFR

...DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND...INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.723...used for reversing the effects of etorphine hydrochloride...in wild and exotic animals. (2) It is...

2013-04-01

146

Striking stabilization of Rana catesbeiana ribonuclease 3 by guanidine hydrochloride.  

PubMed

Unfolding by chemical denaturants and the linear extrapolation method are widely used to determine the free energy of proteins. Ribonuclease 3 from bullfrog shows an extraordinary behavior in guanidinium hydrochloride in comparison to its homologues ribonuclease A and onconase with a high transition midpoint of denaturation but an apparently low cooperativity. The analysis of the interdependence of thermal, urea-, and guanidine hydrochloride-induced unfolding revealed that whereas addition of urea resulted in the expected destabilization of all three proteins, guanidine hydrochloride acted diversely: in contrast to ribonuclease A and onconase, both of which were destabilized as expected, low concentrations of guanidine hydrochloride significantly stabilize ribonuclease 3 from bullfrog. This stabilizing effect was endorsed by in silico docking studies. PMID:23395613

Solé, Magali; Brandt, Wolfgang; Arnold, Ulrich

2013-02-08

147

21 CFR 520.2345a - Tetracycline hydrochloride capsules.  

Code of Federal Regulations, 2013 CFR

...to tetracycline hydrochloride, such as bacterial gastroenteritis due to E . coli and urinary tract infections due to Staphylococcus spp. and E. coli . (3) Limitations . Federal law restricts this drug to use by or on the order of a...

2013-04-01

148

Primary Eye Irritation of Guanidine Hydrochloride in Rabbits.  

National Technical Information Service (NTIS)

The primary eye irritation potential of guanidine hydrochloride was determined in male New Zealand White rabbits using a modified Draize method. The compound produced irritation in all animals tested. Signs of irritation were erythemaz and chemosis of the...

L. D. Brown T. P. Kellner D. W. Korte

1987-01-01

149

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

PubMed

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. PMID:21943714

Adegoke, Olajire A

2011-09-09

150

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

151

Identification of the di-pyridyl ketone isonicotinoyl hydrazone (PKIH) analogues as potent iron chelators and anti-tumour agents  

PubMed Central

In an attempt to develop chelators as potent anti-tumour agents, we synthesized two series of novel ligands based on the very active 2-pyridylcarboxaldehyde isonicotinoyl hydrazone (PCIH) group. Since lipophilicity and membrane permeability play a critical role in Fe chelation efficacy, the aldehyde moiety of the PCIH series, namely 2-pyridylcarboxaldehyde, was replaced with the more lipophilic 2-quinolinecarboxaldehyde or di-2-pyridylketone moieties. These compounds were then systematically condensed with the same group of acid hydrazides to yield ligands based on 2-quinolinecarboxaldehyde isonicotinoyl hydrazone (QCIH) and di-2-pyridylketone isonicotinoyl hydrazone (PKIH). To examine chelator efficacy, we assessed their effects on proliferation, Fe uptake, Fe efflux, the expression of cell cycle control molecules, iron-regulatory protein-RNA-binding activity, and 3H-thymidine, 3H-uridine and 3H-leucine incorporation. Despite the high lipophilicity of the QCIH ligands and the fact that they have the same Fe-binding site as the PCIH series, surprisingly none of these compounds were effective. In contrast, the PKIH analogues showed marked anti-proliferative activity and Fe chelation efficacy. Indeed, the ability of these ligands to inhibit proliferation and DNA synthesis was similar or exceeded that found for the highly cytotoxic chelator, 311. In contrast to the PCIH and QCIH analogues, most of the PKIH group markedly increased the mRNA levels of molecules vital for cell cycle arrest. In conclusion, our studies identify structural features useful in the design of chelators with high anti-proliferative activity. We have identified a novel class of ligands that are potent Fe chelators and inhibitors of DNA synthesis, and which deserve further investigation.

Becker, Erika M; Lovejoy, David B; Greer, Judith M; Watts, Ralph; Richardson, Des R

2003-01-01

152

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

Microsoft Academic Search

4,6-Diacetylresorcinol (DAR) serves as precursor for the formation of different hydrazone ligands, which are di-, tetra- or hexa-basic with two symmetrical sets of O2N tridentate, O2N2 tetradentate or O4N2 hexadentate chelating sites. The condensation of 4,6-diacetylresorcinol (DAR) with oxalyldihydrazine (ODH), in the molar ratio 1:1 and 1:2, yields the corresponding hydrazone, H6La and H4Lb, ligands, respectively. The structures of these

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

2008-01-01

153

Synthesis, Magnetic, and Spectral Studies of Some Mono? and Binuclear Dioxomolybdenum(VI) Complexes with Chelating Hydrazones Derived from Acid Hydrazides and Furfural or Thiophene?2?aldehyde  

Microsoft Academic Search

This paper deals with the synthesis, magnetic and spectral studies of some mono? and binuclear dioxomolybdenum(VI) complexes with chelating hydrazones derived from salicylic acid\\/benzoic acid\\/isonicotinic acid hydrazide with thiophene?2?aldehyde or furfural. The acid hydrazones synthesized are N?(furfuralidene)?N??salicyloylhydrazine [FSAH, (I)], N?(2?thiophenidene)?N??salicyloylhydrazine [TSAH, (II)], N?(furfuralidene)?N??isonicotinoylydrazine [FINH, (III)], N?(2?thiophenidene)?N??isonicotinoylhydrazine [TINH, (IV)], N?(furfuralidene)?N??benzoylhydrazine [FBZH, (V)] and N?(2?thiophenidene)?N??benzoylhydrazine [TBZH, (VI)]. The metal complexes (1)–(6) were

R. C. Maurya; R. Verma; T. Singh

2003-01-01

154

X-ray, spectroscopic and computational studies of the tautomeric structure of a new hydrazone of 5-nitrosalicylaldehyde with indole-3-acetic hydrazide  

Microsoft Academic Search

A new hydrazone of 5-nitrosalicylaldehyde with indole-3-acetic hydrazide (NSIAH) has been obtained and its structure has been studied by X-ray, FT-IR and CPMAS in the solid as well as 1H, 13C and 15N NMR in the CH3CN-d3 and DMSO-d6 solutions. The hydrazone crystallises in the Pbca space group from the orthorhombic system with a=9.5435(7) Å, b=11.0932(8) Å and c=29.672(2) Å.

Krystian Pyta; Piotr Przybylski; Adam Huczynski; Anna Hoser; Krzysztof Wozniak; Wojciech Schilf; Bohdan Kamienski; Eugeniusz Grech; Bogumil Brzezinski

2010-01-01

155

A Rapid Stability-Indicating LC Method for Ziprasidone Hydrochloride  

Microsoft Academic Search

A simple and rapid reversed-phase liquid chromatographic method was developed for the related substances determination and\\u000a quantitative evaluation of ziprasidone hydrochloride, which is used as an antipsychotic agent. Forced degradation studies\\u000a were performed on bulk sample of ziprasidone hydrochloride using acid, base, oxidative hydrolysis, thermal stress and photolytic\\u000a degradation. Mild degradation of the drug substance was observed during thermal stress

A. Singh; B. M. Rao; G. R. Deshpande; S. Sangaraju; M. K. Srinivasu; M. Lalitha Devi; P. V. V. Satyanarayana; K. B. Chandrasekhar

2007-01-01

156

TLC DETERMINATION OF TIAPRIDE HYDROCHLORIDE AND ITS IMPURITIES IN PHARMACEUTICALS  

Microsoft Academic Search

A simple and sensitive HPTLC method for separation and determination of tiapride hydrochloride and its degradation products has been developed and evaluated. Analysis of tiapride hydrochloride and impurities III, VII, and VIII, was performed on silica gel 60 F254 HPTLC plates using methylene chloride-methanol-concentrated ammonia, 9:1.6:0.1 (v\\/v) as mobile phase. Detection was performed at 240 nm. All validation requirements, specificity, linearity (r ? 0.997),

Katarina Rankovi?; Slavica Filipi?; Katarina Nikoli?; Danica Agbaba

2012-01-01

157

Influence of the metal size in the structure of the complexes derived from a pentadentate [N(3)O(2)] hydrazone.  

PubMed

The influence of the metal size in the nuclearity of the complexes derived from the hydrazone ligand 2,6-bis(1-salicyloylhydrazonoethyl)pyridine [H(4)daps] has been investigated. We have synthesised a series of new complexes [M(H(x)daps)] x yH(2)O, (x = 2,3; y = 0-3) with M = Ag (1), Cd (2), Al (3), Sn (4) and Pb (6), using an electrochemical procedure. The crystal and molecular structures have been determined for the mononuclear complexes [Sn(H(2)daps)(H(2)O)(2)] x 4H(2)O (5) and [Pb(H(2)daps)(CN)][Et(4)N] (7). Complex is the first neutral Sn(II) complex derived from a pentadentate hydrazone Schiff base ligand. Complex shows the lead coordinated to the hydrazone donor set and a cyanide ligand, being the first reported complex with the lead atom coordinated to a monodentate cyanide group. Additionally, we have synthesised the lead complex using chemical conditions, in the presence of sodium cyanide which allowed us to isolate the neutral complex [Pb(H(2)daps)] (8). Evaporation of these mother liquors led the novel compound [Pb(Hdaphs)(CH(3)COO)] (9). Complex 9 shows the initial ligand hydrolysed in one of the imine bonds giving rise to a new tetradentate ligand [H(2)daphs] coordinated to the lead atom and a bidentate acetate group. Moreover, the solution behaviour of the complexes has been investigated by (1)H, (113)Cd, (117)Sn and (207)Pb NMR techniques. In particular multinuclear NMR has provided new useful data to correlate factors such as oxidation state, coordination number and nature of the kernel donor atoms due to the new coordination found in complexes 5 and 7. The comparative study of the structures of the complexes derived from this pentadentate [N(3)O(2)] hydrazone ligand let us to conclude that the metal size is a key factor to control the nuclearity of the complexes derived from the ligand [H(4)daps]. PMID:17088970

Pedrido, Rosa; Romero, M José; Bermejo, Manuel R; González-Noya, Ana M; Maneiro, Marcelino; Rodríguez, M Jesús; Zaragoza, Guillermo

2006-10-02

158

40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method  

Code of Federal Regulations, 2010 CFR

...Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method A Appendix...Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method 1. Scope ...hydrochloric acid that is liberated when hydroxylamine hydrochloride reacts with...

2010-07-01

159

40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method  

Code of Federal Regulations, 2010 CFR

...Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method A Appendix...Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method 1. Scope ...hydrochloric acid that is liberated when hydroxylamine hydrochloride reacts with...

2009-07-01

160

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

161

A prototype nonpeptidyl, hydrazone class, thrombopoietin receptor agonist, SB-559457, is toxic to primary human myeloid leukemia cells.  

PubMed

Biologic characterization of SB-559457 (SB), a nonpeptidyl hydrazone class of thrombopoietin receptor (Mpl) agonist, revealed toxicity toward human leukemia cells. Antiproliferative effects followed by significant, nonapoptotic, cell death within 72 hours occurred in 24 of 26 acute myeloid leukemia, 0 of 6 acute lymphoblastic leukemia, and 3 of 6 chronic myeloid leukemia patient samples exposed to SB, but not recombinant human thrombopoietin (rhTpo), in liquid suspension culture. Further investigation revealed increased phosphorylation of p70S6/S6 kinases in SB-, but not in rhTpo-, treated cells. Expression profiling of cells exposed to SB versus rhTpo revealed statistically significant, more than 2-fold changes in GAPDH and REDD1 gene expression, confirmed by quantitative reverse-transcribed polymerase chain reaction. These genes, induced in energy or hypoxia stressed cells, have been implicated in cell death pathways, and may provide important clues to the mechanism of SB-induced, leukemic cell death. These results suggest that nonpeptidyl, hydrazone class Mpl agonists may be clinically useful antileukemic agents by virtue of their combined thrombopoietic and antileukemic effects. PMID:19880492

Kalota, Anna; Gewirtz, Alan M

2009-10-30

162

Physico-chemical studies and CO adsorption on zeolite-encapsulated MnII, MnIII hydrazone complexes  

NASA Astrophysics Data System (ADS)

Complexes of Mn(II) and Mn(III) with N2O3 hydrazone ligand derived from salicylaldehyde and benzenesulphonylhydrazide have been encapsulated in zeolite Y- supercages by a diffusion method. The synthesized new materials have been characterized by combination of elemental analysis, FT-IR, UV vis., magnetic measurements, XRD, thermal analysis (TG, DTG and DTA), as well as surface area measurements and nitrogen adsorption studies. Investigation of the stereochemistry of these incorporated chelates pointed out that, Mn(II) complex is tetrahedral with involvement of zeolite oxygen in coordination meanwhile Mn(III) complex has octahedral configuration without contribution of the lattice oxygen. The intrazeolitic hydrazone complexes are thermally stable up to 1000 °C without decomposition. Catalytic activity towards CO adsorption for these zeolite encapsulated complexes has been investigated and compared with MnII-Y using in situ FT-IR spectroscopy. The results revealed that, MnII(SBSH)/Y and MnIII(SBSH)/Y give an elementary peak near 1728 cm-1 indicating a selectivity to form COOH species while MnII-Y catalyst gives a broad band in the region of 1765 1560 cm-1 assigned to different (COOH) and carbonates species. On the other hand, the in situ FT-IR data indicate that MnII(SBSH)/Y and MnIII(SBSH)/Y can be used as reactive catalysts in water gas shift reaction (WGSR).

Ahmed, Ayman H.

2007-08-01

163

Some hydrazones of 2-aroylamino-3-methylbutanohydrazide: synthesis, molecular modeling studies, and identification as stereoselective inhibitors of HIV-1.  

PubMed

In accordance with our antiviral drug development attempt, acylhydrazone derivatives bearing amino acid side chains were synthesized for the evaluation of their antiviral activity against various types of viruses. Among these compounds, 8(S) , 11(S) , and 12(S) showed anti-HIV-1 activity with a 50% inhibitory concentration (IC(50))?=123.8 µM (selectivity index, SI>3), IC(50)?=12.1 µM (SI>29), IC(50)?=17.4 µM (SI>19), respectively. Enantiomers 8(R) , 11(R) , and 12(R) were inactive against the HIV-1 strain III(B) . Hydrazones 8(S) , 11(S) , and 12(S) which were active against HIV-1 wild type showed no inhibition against a double mutant NNRTI-resistant strain (K103N;Y181C). Molecular docking calculations of R- and S-enantiomers of 8, 11, and 12 were performed using the hydrazone-bound novel site of HIV-1 RT. PMID:23280502

Tatar, Esra; Küçükgüzel, Ilkay; Daelemans, Dirk; Talele, Tanaji T; Kaushik-Basu, Neerja; De Clercq, Erik; Pannecouque, Christophe

2012-12-20

164

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

NASA Astrophysics Data System (ADS)

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

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

2005-01-01

165

Nalbuphine hydrochloride dependence in anabolic steroid users.  

PubMed

Nalbuphine hydrochloride, a nonscheduled opioid agonist/antagonist analgesic, is currently approved for the treatment of pain. Recently, nalbuphine dependence was reported in three anabolic steroid users in Britain. To further document this phenomenon, we conducted interviews on eleven subjects who reported nalbuphine use. Eight subjects were clinically dependent on nalbuphine, and seven of the subjects who were asked about tolerance and withdrawal with nalbuphine acknowledged these symptoms. Eight subjects, who had never used drugs intravenously before, reported using nalbuphine by this route. Nalbuphine-related morbidity was extensive and included medical complications and psychiatric symptoms. Nalbuphine users also exhibited a high rate of comorbid Axis I disorders, including other substance misuse. Virtually all subjects described widespread nalbuphine use in the gymnasiums they frequented. These observations, together with the recent increase in nalbuphine-related articles in the lay press, suggest that nalbuphine may represent a new drug of abuse among athletes, especially those using anabolic steroids, and that nalbuphine's scheduling status may need to be re-evaluated. PMID:10365196

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

1999-01-01

166

Ticlopidine hydrochloride use and threatened stroke.  

PubMed Central

Ticlopidine hydrochloride is an antiplatelet agent of proven antithrombotic efficacy that in December 1991 became available for general clinical use in the United States. The relative value of ticlopidine compared with aspirin, also an effective antiplatelet agent, has become a key clinical issue. Whereas ticlopidine is somewhat more effective than aspirin for preventing stroke in certain populations, it is also more expensive and potentially toxic. We recommend its use for patients with threatened stroke who are intolerant of aspirin and for patients who have cerebral ischemic symptoms despite aspirin therapy. Patients surviving major ischemic stroke make up a third group for whom ticlopidine use may be recommended in preference to aspirin. The use of ticlopidine rather than aspirin in patients with other cerebrovascular conditions is not strongly supported by existing data. The risk-benefit-cost equation involving ticlopidine versus other antithrombotic therapies is complex, rendering a wide range of acceptable management practices. If reliable laboratory monitoring for neutropenia during the first 3 months of therapy is not feasible, ticlopidine should not be used.

Rothrock, J F; Hart, R G

1994-01-01

167

The hydrazide/hydrazone click reaction as a biomolecule labeling strategy for M(CO)3 (M = Re, 99mTc) radiopharmaceuticals†  

PubMed Central

Facile reactivity of hydrazides and aldehydes was explored as potential coupling partners for incorporation into M(CO)3 (M = Re, 99mTc) based radiopharmaceuticals. Both ‘click, then chelate’ and ‘prelabel, then click’ synthetic routes produced identical products in high yields and lacked metal-hydrazide/-hydrazone interactions, highlighting the potential of this click strategy.

Ganguly, Tanushree; Kasten, Benjamin B.; Bucar, Dejan-Kresimir; MacGillivray, Leonard R.; Berkman, Clifford E.

2011-01-01

168

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

Microsoft Academic Search

Although iron chelation therapy with de- feroxamine (DFO) results in improved life expectancy of patients with thalassemia, compliance with parenteral DFO treat- ment is unsatisfactory, underlining the need for alternative drugs and innovative ways of drug administration. We exam- ined the chelating potential of pyridoxal isonicotinoyl hydrazone (PIH) analogs, alone or in combination with DFO, using hypertansfused rats with labeled

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

169

The hydrazide/hydrazone click reaction as a biomolecule labeling strategy for M(CO)3 (M = Re, (99m)Tc) radiopharmaceuticals.  

PubMed

Facile reactivity of hydrazides and aldehydes was explored as potential coupling partners for incorporation into M(CO)(3) (M = Re, (99m)Tc) based radiopharmaceuticals. Both 'click, then chelate' and 'prelabel, then click' synthetic routes produced identical products in high yields and lacked metal-hydrazide/-hydrazone interactions, highlighting the potential of this click strategy. PMID:22044929

Ganguly, Tanushree; Kasten, Benjamin B; Bu?ar, Dejan-Krešimir; MacGillivray, Leonard R; Berkman, Clifford E; Benny, Paul D

2011-11-01

170

The iron chelator pyridoxal isonicotinoyl hydrazone (PIH) and its analogues prevent damage to 2-deoxyribose mediated by ferric iron plus ascorbate  

Microsoft Academic Search

Iron chelating agents are essential for treating iron overload in diseases such as ?-thalassemia and are potentially useful for therapy in non-iron overload conditions, including free radical mediated tissue injury. Deferoxamine (DFO), the only drug available for iron chelation therapy, has a number of disadvantages (e.g., lack of intestinal absorption and high cost). The tridentate chelator pyridoxal isonicotinoyl hydrazone (PIH)

Marcelo Hermes-Lima; Prem Ponka; Herbert M. Schulman

2000-01-01

171

Partition coefficients of the iron(III) complexes of pyridoxal isonicotinoyl hydrazone and its analogs and the correlation to iron chelation efficacy  

Microsoft Academic Search

Pyridoxal isonicotinoyl hydrazone and its analogs are orally effective Fe(III) chelators which show potential as drugs to treat iron overload disease. The present investigation describes the measurement of the partition coefficient of the apochelator and Fe(III) complex of 20 of these ligands. These measurements have been done to investigate the relationship between lipophilicity and the efficacy of iron chelation in

J. T. Edward; P. Ponka; D. R. Richardson

1995-01-01

172

Pd(ii)-catalyzed direct C-H acylation of N-Boc hydrazones with aldehydes: one-pot synthesis of 1,2-diacylbenzenes.  

PubMed

A palladium(ii)-catalyzed direct acylation of acetophenone N-Boc hydrazones with aldehydes via C-H bond activation is described. This protocol provides direct access to a range of 1,2-diacylbenzenes, which are useful precursors to construct biologically interesting and pharmaceutically important compounds. PMID:24129548

Sharma, Satyasheel; Kim, Aejin; Park, Jihye; Kim, Mirim; Kwak, Jong Hwan; Jung, Young Hoon; Park, Jung Su; Kim, In Su

2013-10-16

173

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

Technology Transfer Automated Retrieval System (TEKTRAN)

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

174

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...

175

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

176

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

Code of Federal Regulations, 2013 CFR

...2013-07-01 2013-07-01 false Phenol, 5-amino-2,4-dicholoro-, hydrochloride...Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride...The chemical substance identified as phenol,...

2013-07-01

177

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

178

Teratologic Evaluation of Oxytetracycline Hydrochloride (CAS Number 2058-46-0) in CD Rats.  

National Technical Information Service (NTIS)

Oxytetracycline hydrochloride (OX), a commonly used antibiotic, was evaluated for teratogenicity following maternal exposure. Timed-pregnant CD rats were dosed by gavage (po) on gestational days (gd) 6 through 15 with oxytetracycline hydrochloride (0, 120...

R. Wolkowski-Tyl C. Jones-Price T. A. Ledoux J. R. Reel L. Langhoff-Paschke

1983-01-01

179

Protein stabilization by urea and guanidine hydrochloride.  

PubMed

The urea, guanidine hydrochloride, salt, and temperature dependence of the rate of dissociation of CO from a nonequilibrium state of CO-bound native ferrocytochrome c has been studied at pH 7. The heme iron of ferrocytochrome c in the presence of denaturing concentrations of guanidine hydrochloride (GdnHCl) and urea prepared in 0.1 M phosphate, pH 7, binds CO. When the unfolded protein solution is diluted 101-fold into CO-free folding buffer, the protein chain refolds completely, leaving the CO molecule bonded to the heme iron. Subsequently, slow thermal dissociation of the CO molecule yields to the heme coordination of the native M80 ligand. Thus, the reaction monitors the rate of thermal conversion of the CO-liganded native ferrocytochrome c to the M80-liganded native protein. The rate of this reaction, k(diss), shows a characteristic dependence on the presence of nondenaturing concentrations of the denaturants in the reaction medium. The rate decreases by approximately 1.9-3-fold as the concentration of GdnHCl in the refolding medium increases from nearly 0 to approximately 2.1 M. Similarly, the rate decreases by 1.8-fold as the urea concentration is raised from 0.l to approximately 5 M. At still higher concentrations of the denaturants the denaturing effect sets in, the protein is destabilized, and hence the CO dissociation rate increases sharply. The activation energy of the reaction, E(a), increases when the denaturant concentration in the reaction medium is raised: from 24.1 to 28.3 kcal mol(-1) for a 0.05-2.1 M rise in GdnHCl and from 25.2 to 26.9 kcal mol(-1) for a 0.1-26.9 M increase in urea. Corresponding to these increases in denaturant concentrations are also increases in the activation entropy, S(diss)/R, where R is the gas constant of the reaction. The denaturant dependence of these kinetic and thermodynamic parameters of the CO dissociation reaction suggests that binding interactions with GdnHCl and urea can increase the structural and energetic stability of ferrocytochrome c up to the limit of the subdenaturing concentrations of the additives. NaCl and Na(2)SO(4), which stabilize proteins through their salting-in effect, also decrease the rate with a corresponding increase in activation entropy of CO dissociation from CO-bound native ferrocytochrome c, lending support to the view that low concentrations of GdnHCl and urea stabilize proteins. These results have direct relevance to the understanding and interpretation of the free energy-denaturant relationship and protein folding chevrons. PMID:12416983

Bhuyan, Abani K

2002-11-12

180

[Preparation and in vitro permeation of tetramethylpyrazine hydrochloride transdermal gel].  

PubMed

The purpose of this study was to prepare tetramethylpyrazine hydrochloride transdermal gel and to study its permeation ability in vitro. The skin permeation ability was evaluated by Valian-Chien permeation cells with isolated rat skin. The concentration of tetramethylpyrazine in samples was determined by HPLC. The optimal formulation was composed with 5% azone, 5% peppermint oil, 8% sodium carboxymethylcellulose and 8% tetramethylpyrazine hydrochloride. The accumulative permeation amount of the gel was (6 731.87 +/- 102.31) microg x cm(-2) in 12 h,and the permeation rate was (535.02 +/- 33.89) microg x cm(-2) x h(-1). The release profile in vitro was in line with zero-order formulation. Tetramethylpyrazine hydrochloride gel prepared in the study would be developed as a novel transdermal preparation. PMID:24079234

Tang, Zhan; Xu, Hong-Yan; Wang, Qiao

2013-07-01

181

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.

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

2010-01-01

182

21 CFR 520.2345g - Tetracycline hydrochloride and sodium novobiocin tablets.  

Code of Federal Regulations, 2010 CFR

...2009-04-01 2009-04-01 false Tetracycline hydrochloride and sodium novobiocin...NEW ANIMAL DRUGS § 520.2345g Tetracycline hydrochloride and sodium novobiocin...contains the equivalent of 60 milligrams of tetracycline hydrochloride and 60 milligrams...

2009-04-01

183

Investigation of stability of tetracycline hydrochloride in methylcellulose gel.  

PubMed

The investigations proved that granulation of tetracycline hydrochloride with ethanol, methanol or acetone does not reduce the antibiotic activity of the preparation. At room temperature the activity of the granular preparation decreases by 10% within the time range from 994 to 1074 d. Gel containing 0.7% of methylcellulose, 5% of 1,2-propylene glycol and 5% of dimethyl acetamide proved to be very stable in respect to viscosity and pH over 3 years. Application of 20% excess of tetracycline hydrochloride and storage of the gel at 4 degrees C enables maintaining it active over 21 d. PMID:3432331

Kubis, A; Dybek, K; Krutul, H

1987-08-01

184

Immobilization of Rocky Mountain Elk with Telazol#{174} and Xylazine Hydrochloride, and Antagonism by Yohimbine Hydrochloride  

Microsoft Academic Search

ABSTRACT: Ten,trapped,Rocky,Mountain,elk (Cervus,elaphus,nelsoni),were,successfully,im- mobilized,with,a combination,of 500 mg,Tel- azol#{174} and 60 mg xylazine hydrochloride,(HC1) from,9 July to 25 August,1993 in,Custer,State Park, South Dakota (USA). Mean (SD) dosages of 2.5 (0.6) mg\\/kg,Telazol#{174} and,0.3 (0.1) mg\\/ kg xylazine HC1, respectively, were adminis- tered, resulting in a mean (SD) induction time of,4.6 (0.8) mm.,Induction,time,varied,with weight,and,dosage.,Respiratory,rate,(breaths\\/ mm),increased,following,injection,of,Telazol#{174} and,xylazine,HC1 and,remained,elevated,or con- tinued,to increase,through,10 mm,post-injection and,then,declined. There,were,no

Joshua J. Mlllspaugh; Gary C. Brundige; Jonathan A. Jenks; C. Lee Tyner

1995-01-01

185

Variable inhibitory effects on the formation of dinitrosyl iron complexes by deferoxamine and salicylaldehyde isonicotinoyl hydrazone in K562 cells.  

PubMed

A prerequisite of dinitrosyl iron complexes (DNIC) formation is the presence of nitric oxide (NO), iron (Fe) and thiol/imidazole groups. The aim of this study was to investigate the influence of Fe chelators on the formation of DNIC in erythroid K562 cells. The cells were treated with lipophilic salicylaldehyde isonicotinoyl hydrazone (SIH) (0.1 mM) and hydrophilic deferoxamine mesylate (DFO) (1 mM), a membrane permeable and non permeable Fe chelator, respectively. Dinitrosyl Fe complexes were generated by addition of 0.07 mM diethylamine NO. The DNIC formation was recorded using electron paramagnetic resonance (EPR). Both chelators inhibited DNIC formation up to 50% after 6 hours of treatment. Taken together, our data suggest that an intracellular low molecular weight labile Fe pool (LIP) and protein-bound Fe participate in DNIC formation in K562 cells to a similar extent. PMID:18274993

Meczynska, Sylwia; Lewandowska, Hanna; Sochanowicz, Barbara; Sadlo, Jaroslaw; Kruszewski, Marcin

2008-01-01

186

Stereoselective alkylations of chiral nitro imine and nitro hydrazone dianions. Synthesis of enantiomerically enriched 3-substituted 1-nitrocyclohexenes.  

PubMed

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

2008-12-19

187

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.

Denmark, Scott E.; Ares, Jeffrey J.

2011-01-01

188

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

PubMed

In continuation of our program aimed at the discovery and development of natural-product-based insecticidal agents, four series of novel cholesterol-based hydrazone derivatives were synthesized, and their insecticidal activity was tested against the pre-third-instar larvae of oriental armyworm, Mythimna separata (Walker) in vivo at 1mg/mL. All the derivatives showed the better insecticidal activity than their precursor cholesterol. Quantitative structure-activity relationship (QSAR) model demonstrated that six descriptors such as RDF085v, Mor06u, Mor11u, Dv, HATS0v and H-046, are likely to influence the insecticidal activity of these compounds. Among them, two important ones are the Mor06u and RDF085v. PMID:23891182

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

2013-07-10

189

Synthesis, characterization and DNA-binding properties of Ln(III) complexes with 6-ethoxy chromone-3-carbaldehyde benzoyl hydrazone.  

PubMed

A novel 6-ethoxy chromone-3-carbaldehyde benzoyl hydrazone (L) and its Ln(III) complexes, [Ln = Sm (1), Eu (2), Gd (3), Tb (4)], have been synthesized and characterized. The fluorescence properties of the Eu(III) and Sm(III) complexes in solid state and Eu(III) complex in different solutions (DMF, DMSO, methanol and acetonitrile) were investigated. At the same time, the DNA-binding properties of the two complexes are investigated using UV-Vis absorption spectroscopy, fluorescence spectroscopy, viscosity measurement. All the experimental evidences indicate that the two complexes can bind to CT-DNA via an intercalation mechanism. Furthermore, antioxidant activity tests in vitro showed that the complexes have significant antioxidative activity against hydroxyl free radicals from the Fenton reaction. PMID:19370403

Wang, Ju; Yang, Zheng-Yin; Wang, Bao-Dui; Yi, Xu-Yang; Liu, Yong-Chun

2009-04-16

190

Promethazine hydrochloride: use in patients with Rh isoimmunization.  

PubMed

Twenty-two babies born to 21 mothers were treated prenatally for varying periods of time with promethazine hydrochloride in doses of 150 mg. per day. Seven of the 22 babies required intrauterine transfusions. With the exception of positive clinical impressions in some cases, specific ameliorating effects of the drug in this group could not be demonstrated. PMID:637081

Stenchever, M A

1978-03-15

191

21 CFR 522.883 - Etorphine hydrochloride injection.  

Code of Federal Regulations, 2013 CFR

...DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND...of wild and exotic animals. (2) It is administered...use in reversing the effects of etorphine hydrochloride...use in wild or exotic animals only. Do not use...

2013-04-01

192

A study of variable hydration states in topotecan hydrochloride  

Microsoft Academic Search

Topotecan hydrochloride, a pharmaceutical compound developed as a treatment for cancer, exhibits variable hydration states in a crystalline solid form chosen for manufacturing. This variability requires additional controls for successful development, and presents a characterization and detection challenge for analytical methods. In this study, overall water content was determined by Karl Fischer titration and thermogravimetric analysis (TGA) on topotecan HCl

Frederick G. Vogt; Philip C. Dell’Orco; Ann. M. Diederich; Qiaogong Su; Jeffery L. Wood; Gary E. Zuber; Lee M. Katrincic; Ronald L. Mueller; David J. Busby; Charles W. DeBrosse

2006-01-01

193

21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.  

Code of Federal Regulations, 2013 CFR

... (c) Conditions of use. (1) It is used in dogs as a tranquilizer.1 (2) It is administered intramuscularly at a dosage...ethylisobutrazine hydrochloride per pound of body weight to effect.1 1 These conditions are NAS/NRC reviewed and...

2013-04-01

194

Morphine and oxycodone hydrochloride in the management of cancer pain  

Microsoft Academic Search

In a double-blind crossover study, morphine and oxycodone hydrochloride were administered to 20 patients who were experiencing severe cancer pain. The peroral doses were determined on the basis of patient-controlled intravenous titration. The assumed oral bioavailability ratios were 44% (group 1, first 10 patients) and 33% (group 2, last 10 patients) for morphine and 66% (group 1) and 50% (group

Eija Kalso; Anneli Vainio

1990-01-01

195

Synthesis and Mass spectrometry of deuterium labeled tranylcypromine hydrochloride  

Microsoft Academic Search

[2H2] Tranylcypromine hydrochloride (trans-3, 3-dideuterio-2-phenylcyclopropylamine HCl) was synthesized for application to the\\u000a metabolic studies. Mass fragmentation processes for the tranylcypromine and its two synthetic intermediates, ?-phenyl-?-butyrolactone\\u000a and trans-2-phenylcyclopropanecarboxylic acid were described based upon comparisons between labeled and unlabeled compounds.

Gun Il Kang; Suk Gil Hong

1985-01-01

196

Stability of cimetidine hydrochloride in a total nutrient admixture.  

PubMed

The stability of cimetidine hydrochloride in a total nutrient admixture was studied. A total nutrient admixture composed of 5% amino acid injection, 20% dextrose injection, and 3% intravenous fat emulsion was prepared aseptically in four 2-L ethylene-vinyl acetate bags. Cimetidine hydrochloride injection was added to three of the admixtures to yield final cimetidine concentrations of 600, 1200, and 1800 mg per 1500 mL of admixture; the fourth admixture served as a control. At 0, 24, and 48 hours, cimetidine content was measured by high-performance liquid chromatography, and the admixtures were tested for pH and visually inspected for signs of creaming, oiling out, or phase separation. Particle-size distribution in the admixtures was compared with that in 20% intravenous fat emulsion. No appreciable changes in cimetidine concentration or pH occurred over 48 hours, and no visual changes were observed. Particle sizes were comparable to those in the 20% intravenous fat emulsion control except in the admixture containing cimetidine hydrochloride 600 mg, which had significantly more particles larger than 9.9 microns at 48 hours. In the total nutrient admixture studied, cimetidine hydrochloride in concentrations up to 1800 mg per 1500 mL was stable for 24 hours at room temperature, and the lipid emulsion was apparently not altered during this period by cimetidine. PMID:3933337

Baptista, R J; Palombo, J D; Tahan, S R; Valicenti, A J; Bistrian, B R; Arkin, C F; Blackburn, G L

1985-10-01

197

Treatment of motor urge incontinence with clenbuterol and flavoxate hydrochloride.  

PubMed

A controlled double-blind trial is reported of the parasympatholytic drug, flavoxate hydrochloride, and the new sympathomimetic drug, clenbuterol, in the treatment of 39 women with motor urge incontinence. The clinical results and the urodynamic findings of urethro-cystomanometry after therapy showed clenbuterol to be very effective with few side effects. PMID:6367811

Grüneberger, A

1984-03-01

198

FORMULATION DEVELOPMENT OF SERTRALINE HYDROCHLORIDE MICROEMULSION FOR INTRANASAL DELIVERY  

Microsoft Academic Search

Nasal cavity has used as alternative route for the drugs with poor water solubility, susceptible to acidic or enzymatic degradation and hepatic metabolism. The objective of the present study was to improve solubility of sertraline hydrochloride (STH), formulate microemulsions containing STH to accomplish rapid onset of action and to bypass the first-pass metabolism. A microemulsion system with Capmul MCM as

Amrish Kumar; Pankaj Sharma; Ashwani Chaturvedi; Durga Jaiswal; Meenakshi Bajpai; Mukesh Choudhary; Indranil Kumar Yadav; Hari Pratap Singh; Dinesh Chandra; D. A. Jain; Raj Kumar

199

40 CFR 180.276 - Formetanate hydrochloride; tolerances for residues.  

Code of Federal Regulations, 2012 CFR

...methylcarbamate hydrochloride) in or on raw agricultural commodities as follows: Commodity Parts per million Apple 0.50 Apple, wet pomace 1.5 Grapefruit 1.5 Lemon 0.60 Lime 0.03 Nectarine 0.40 Orange...

2012-07-01

200

40 CFR 180.276 - Formetanate hydrochloride; tolerances for residues.  

Code of Federal Regulations, 2011 CFR

...methylcarbamate hydrochloride) in or on raw agricultural commodities as follows: Commodity Parts per million Apple 0.50 Apple, wet pomace 1.5 Grapefruit 1.5 Lemon 0.60 Lime 0.03 Nectarine 0.40 Orange...

2011-07-01

201

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

2009-11-26

202

Benzydamine hydrochloride oral rinses in management of burning mouth syndrome  

Microsoft Academic Search

Objective. The purpose of this study was to evaluate the efficacy of the topical use of benzydamine hydrochloride 0.15% oral mouthwashes in the control of burning mouth syndrome symptoms. Study Design. In this double-blind, randomized, longitudinal investigation, each of 30 patients with burning mouth syndrome was assigned to one of 3 management modalities. Those in group A received an oral

Andrea Sardella; Daniela Uglietti; Federica Demarosi; Giovanni Lodi; Cristina Bez; Antonio Carrassi

1999-01-01

203

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

204

Natural-product-based insecticidal agents 14. Semisynthesis and insecticidal activity of new piperine-based hydrazone derivatives against Mythimna separata Walker in vivo.  

PubMed

In continuation of our program aimed at the discovery and development of natural-product-based insecticidal agents, twenty-six new piperine-based hydrazone derivatives were synthesized from piperine, an alkaloid isolated from Piper nigrum Linn. The single-crystal structures of 6c, 6q and 6w were unambiguously confirmed by X-ray crystallography. Their insecticidal activity was evaluated against the pre-third-instar larvae of Mythimna separata Walker in vivo. Especially compounds 6b, 6i and 6r, the final mortality rates of which, at the concentration of 1mg/mL, were 62.1%, 65.5% and 65.5%, respectively, exhibited more pronounced insecticidal activity compared to toosendanin at 1mg/mL, a commercial botanical insecticide isolated from Melia azedarach. It suggested that introduction of the substituents at the C-2 position on the phenyl ring of the hydrazone derivatives was important for their insecticidal activity. PMID:24018189

Qu, Huan; Yu, Xiang; Zhi, Xiaoyan; Lv, Min; Xu, Hui

2013-08-20

205

Spectroscopic and X-ray Crystallographic Evidence for Electrostatic Effects in 4-Substituted Cyclohexanone-Derived Hydrazones, Imines, and Corresponding Salts  

PubMed Central

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

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

2011-01-01

206

Study on DNA-binding properties and cytotoxicity in L 1210 of La(III) complex with PMBP-isonicotinoyl hydrazone  

Microsoft Academic Search

La(III) complex with 1-phenyl-3-methyl-5-hydroxy-4-pyrazolyl phenyl ketone (PMBP)-isonicotinoyl hydrazone (La-complex) was synthesized in the work. The crystal of the La-complex was determined by X-ray diffraction analyses, the crystal of the complex is rhomb, space group R3 with Z=6, the coordination polyhedron of the complex is a tricapped triprism configuration with the nine-coordinate atoms, and the La-complex molecule looks like a helix

Zheng-Yin Yang; Bao-Dui Wang; Yan-Hua Li

2006-01-01

207

Synthesis, structure and characterization of fac-[Re(CO) 3] + complexes derived from hydrazone Schiff bases: DFT–TDDFT investigation on electronic structures  

Microsoft Academic Search

The syntheses, structural and spectroscopic characterization of the complexes of general formula [ReL(CO)3Cl] bearing bifunctional hydrazone Schiff base ligand L are presented in this paper. The structure of one of the complexes is determined by X-ray crystallography. The solid-state structure of the compound is involved in a secondary interaction in lattice forming a supramolecular array. The gas phase geometry optimization

Sucharita Basak; Deepak Chopra; Kajal Krishna Rajak

2008-01-01

208

Asymmetric Formal Carbonyl-Ene Reactions of Formaldehyde tert-Butyl Hydrazone with ?-Keto Esters: Dual Activation by Bis-urea Catalysts.  

PubMed

The dual activation of ?-keto esters and formaldehyde tert-butyl hydrazone by BINAM-derived bis-ureas is the key to achieve high reactivity and excellent enantioselectivities in nucleophilic addition (formal carbonyl-ene reaction) to functionalized tertiary carbinols. Ensuing high-yielding diazene-to-aldehyde tranformations and subsequent derivatizations provides a direct entry to a variety of densely functionalized products. PMID:22823936

Crespo-Peña, Ana; Monge, David; Martín-Zamora, Eloísa; Alvarez, Eleuterio; Fernández, Rosario; Lassaletta, José M

2012-07-26

209

One-Pot Synthesis of Some New Semicarbazone, Thiosemicarbazone, and Hydrazone Derivatives of 1Phenyl3-Arylpyrazole-4-Carboxaldehyde from Acetophenone Phenylhydrazones Using Vilsmeier–Haack Reagent  

Microsoft Academic Search

Semicarbazone derivatives 3 of 1,3-diphenylpyrazole-4-carboxaldehyde have been synthesized in high yields through a one-pot procedure involving acetophenone phenylhydrazones 1 subjected to Vilsmeier double formylation and workup under new conditions (i.e., treatment with semicarbazide followed by sodium bicarbonate). This method is even suitable for preparing other derivatives (i.e., thiosemicarbazones 4 and hydrazones 5) in high yields.

Rashmi Pundeer; Pooja Ranjan; Kamaljeet Pannu; Om Prakash

2008-01-01

210

Dimensionality control of vapochromic hydrogen-bonded proton-transfer assemblies composed of a bis(hydrazone)iron(II) complex.  

PubMed

We describe the novel synthesis of a bis(hydrazone)iron(II) complex in protonated [Fe(Hpbph)(2)]Cl(2) (1) and deprotonated [Fe(pbph)(2)] (2) forms and several hydrogen-bonded proton-transfer (HBPT) assemblies having different dimensionalities of hydrogen-bonded network structures, [Fe(Hpbph)(2)](CA)·2CH(3)OH (3), [Fe(Hpbph)(2)](HCA)(2)·2THF (4), and [Fe(Hpbph)(2)](CA)(H(2)CA)(2)·2CH(3)CN (5) (Hpbph = 2-(diphenylphosphino)benzaldehyde-2-pyridylhydrazone), consisting of a deprotonated Fe(II)-hydrazone complex (2) as a proton acceptor (A) and chloranilic acid (H(2)CA) as a proton donor (D). The deprotonated complex 2 exhibited two-step reversible protonation reactions to form the double-protonated form 1, and the acid-dissociation constants were determined to be 7.6 and 10.3 in methanol solution. Utilizing this proton-accepting ability of 2, we succeeded in synthesizing HBPT assemblies 3, 4, and 5 from the reactions in CH(3)OH, THF, and CH(3)CN, respectively, with the same D/A ratio of H(2)CA/[Fe(pbph)(2)] = 10:1. These assemblies were found to have one-dimensional (1-D), two-dimensional (2-D), and three-dimensional (3-D) hydrogen-bonded networks with D/A ratios of 1:1, 2:1, and 3:1 for 3, 4, and 5, respectively. In 3, a 1-D hydrogen-bonded chain composed of the alternate arrangement of [Fe(Hpbph)(2)](2+) and CA(2-), {···[Fe(Hpbph)(2)](2+)···CA(2-)···}(?), was surrounded by solvated methanol molecules to form isolated 1-D hydrogen-bonded chains. In the HBPT assembly 4, a 2-D hydrogen-bonded sheet was formed from two types of hydrogen-bonded chains, {···[Fe(Hpbph)(2)](2+)···HCA(-)···HCA(-)···}(?) and {···HCA(-)···HCA(-)···}(?), and solvated THF molecules did not form any hydrogen bonds. In 5, two orthogonal hydrogen-bonded chains constructed from the neutral chloranilic acid molecules, {···CA(2-)···2(H(2)CA)···}(?), were formed in addition to the 1-D hydrogen-bonded chain similar to that in 3, resulting in the formation of a rigid 3-D hydrogen-bonded network structure. By controlling the dimensionality of the hydrogen bond network, we found that the 2-D HBPT assembly 4 is sufficiently flexible to exhibit interesting vapochromic behavior in response to various organic vapors. PMID:21800867

Chang, Mee; Kobayashi, Atsushi; Nakajima, Kiyohiko; Chang, Ho-Chol; Kato, Masako

2011-07-29

211

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

NASA Astrophysics Data System (ADS)

The pharmaceuticals, procaine hydrochloride and procainamide hydrochloride, are glass-forming as well as ionically conducting materials. We have made dielectric measurements at ambient and elevated pressures to characterize the dynamics of the ion conductivity relaxation in these pharmaceuticals, and calorimetric measurements for the structural relaxation. Perhaps due to their special chemical and physical structures, novel features are found in the ionic conductivity relaxation of these pharmaceuticals. Data of conductivity relaxation in most ionic conductors when represented by the electric loss modulus usually show a single resolved peak in the electric modulus loss M''(f ) spectra. However, in procaine hydrochloride and procainamide hydrochloride we find in addition another resolved loss peak at higher frequencies over a temperature range spanning across Tg. The situation is analogous to many non-ionic glass-formers showing the presence of the structural ?-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 Tg. 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.

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

2012-04-01

212

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

213

Extractive spectrophotometric determination of TRODAT-1 hydrochloride in lyophilized kit.  

PubMed

A simple, sensitive, and accurate spectrophotometric method has been developed for the assay of TRODAT-1 hydrochloride in lyophilized kit. The method is based on the formation of ion-pair association complex of TRODAT-1 with bromothymol blue (BTB) in disodium hydrogen phosphate/citric acid buffer of pH 4.0. The colored product was extracted with chloroform, and measured spectrophotometrically at 414 nm. Beer's law was obeyed in the range of 5-25 microg/ml with molar absorptivity of 2.75 x 10(4) l/mol/cm. Optimization of experimental conditions was described for the method. The proposed method has been successfully applied for the analysis of TRODAT-1 hydrochloride in lyophilized kit. No interference with pharmaceutical excipients was observed. PMID:18819514

Li, X M; Chen, Z P; Wang, S P; Tang, J; Liu, C Y; Zou, M F

2008-09-01

214

Growth and characterization of thiosemicarbazide hydrochloride: A semiorganic NLO material  

NASA Astrophysics Data System (ADS)

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

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

2011-11-01

215

14-Benzoyl-mesaconine hydro-chloride methanol monosolvate  

PubMed Central

The title compound, C31H44N3O10 +·Cl?·CH4O, is the methanol solvate of 8-benzo­yloxy-,9,11,11a-tetra­hydroxy-6,10,13-trimeth­oxy-3-meth­oxy­methyl-1-methyl­tetra­deca­hydro-1H-3,6a,12-(epiethane-1,1,2-tri­yl)-7,9-methanona­phtho[2,3-b]azocin-1-ium chloride, the amine-protonated hydro­chloride of 14-benzoyl­mesaconine hydro­chloride. The cation has an aconitine carbon skeleton with four six-membered rings of which three display chair conformations and one a boat conformation, and two five-membered rings with envelope conformations. In the crystal, the components are connected into an infinite chain by inter- and intra­molecular O—H?O, N—H?O and O—H?Cl hydrogen bonds.

Mu, Yan; Li, Lin; Wei, Hai-Liu; Kuang, Tong-Chun; Hu, Song-Qing

2011-01-01

216

Case history: the discovery of fluoxetine hydrochloride (Prozac).  

PubMed

In the early 1970s, evidence of the role of serotonin (5-hydroxytryptamine or 5-HT) in depression began to emerge and the hypothesis that enhancing 5-HT neurotransmission would be a viable mechanism to mediate antidepressant response was put forward. On the basis of this hypothesis, efforts to develop agents that inhibit the uptake of 5-HT from the synaptic cleft were initiated. These studies led to the discovery and development of the selective serotonin-reuptake inhibitor fluoxetine hydrochloride (Prozac; Eli Lilly), which was approved for the treatment of depression by the US FDA in 1987. Here, we summarize this research and discuss the many challenges that we encountered during the development of fluoxetine hydrochloride, which has now been widely acknowledged as a breakthrough drug for depression. PMID:16121130

Wong, David T; Perry, Kenneth W; Bymaster, Frank P

2005-09-01

217

Rhabdomyolysis caused by tocolytic therapy with ritodrine hydrochloride  

Microsoft Academic Search

We report a case of rhabdomyolysis with severe generalized weakness and muscle pain after administration of ritodrine hydrochloride, in a pregnant patient without history of neuromuscular disease.Laboratory tests showed an increase of blood CK value and myoglobinuria. An electromyography was performed, revealing a typical myogenic pattern and diffuse denervation activity.Muscular biopsy allowed to rule out inflammatory and metabolic myopathy.After delivery,

L. Verriello; D. D’Amico; G. Pauletto; G. L. Gigli; P. Bergonzi

2009-01-01

218

Spectrophotometric analysis of raloxifene hydrochloride in pure and pharmaceutical formulations.  

PubMed

Two simple and sensitive spectrophotometric methods (A and B) for the determination of raloxifene hydrochloride in bulk samples and pharmaceutical formulations are described. Method A is based on the oxidation of the drug with ferric chloride and coupling with potassium ferric cyanide. Method B is based on reduction of the drug with Fehling's reagent. Bluish green color formed in method A absorbs at 735 nm and brown color produced in method B absorbs at 430 nm. PMID:15497756

Dharuman, J; Ravichandran, V; Thirumoorthy, N; Dharamsi, A

2004-09-01

219

Characterization of venlafaxine hydrochloride and compatibility studies with pharmaceutical excipients  

Microsoft Academic Search

The thermal analytical study of venlafaxine hydrochloride, a third generation antidepressant, was investigated using thermogravimetry\\u000a (TG) and differential scanning calorimetry (DSC). The DSC curves have shown a sharp endothermic event at 211 °C and TG demonstrated\\u000a a single stage of mass loss between 254 and 283 °C. Solid-state characterization was carried out by DRIFT, SEM, and XRPD demonstrating\\u000a the drug physicochemical properties

L. S. Bernardi; P. R. Oliveira; F. S. Murakami; M. A. S. Silva; S. H. M. Borgmann; S. G. Cardoso

2009-01-01

220

[Ketamine hydrochloride by continuous drip intravenous infusion in thoracic surgery].  

PubMed

The Authors report an open trial on 50 patients anaesthetized with Ketamine hydrochloride, by continuous drip infusion progressively slowed, with the aid of Fentanil, in thoracic surgery. The proposed anaesthetic technique proved to be excellent as for as analgesia during and after operation as well cardiovascular stability and lackness of side effects is concerned. Recovery from anaesthesia was quick and extremely quite and free from side effects which are common in Ketamine anaesthesia. PMID:7219752

Pietrobono, P; Serafini, G; Pagnin, A; Venchi, G

1980-08-01

221

Immobilization of coastal grizzly bears with etorphine hydrochloride.  

PubMed

Seventeen coastal grizzly bears (Ursus arctos horribilis) from southwestern British Columbia were captured and immobilized a total of 27 times with etorphine hydrochloride (M99). Effective dosages administered ranged from 0.011 to 0.132 mg/kg. Drug dosages (on a body weight basis) were not significantly related to induction times (R=-.040); however, it appeared that induction could be reduced with an increased dosage. At higher dosage levels respiratory rate was reduced to 2/minute. PMID:7411738

Herbert, D M; Lay, D W; Turnbull, W G

1980-07-01

222

Spectroelectrochemical determination of chlorpromazine hydrochloride by flow-injection analysis  

Microsoft Academic Search

An original, simple and sensitive flow-injection spectroelectroanalytical method for the determination of chlorpromazine in pure form or in pharmaceutical formulations is described. The method is based on the formation of a stable cationic radical by electro-oxidation in sulfuric acid medium (0.1moll?1), monitored in situ at ?=524nm. The determination of chlorpromazine hydrochloride in pure form or in pharmaceutical formulations was explored,

Daniela Daniel; Ivano G. R. Gutz

2005-01-01

223

Synthesis of heterocyclic compounds from hydrochlorides of iminoesters of ferrocenecarboxylic acid  

Microsoft Academic Search

Heterocyclic compounds of the 2-imidazoline, benzimidazole and benzoxazole series, containing the ferrocenyl radical, were obtained from the hydrochlorides of the iminoesters of ferrocenecarboxylic acid.

N. S. Nametkin; G. A. Shvekhgeimer; V. D. Tyurin; A. I. Tutubalina; T. N. Kosheleva

1971-01-01

224

PROLONGED AND MULTIPLE IMMOBILIZATIONS OF THE SOUTHERN ELEPHANT SEAL USING KETAMINE HYDROCHLORIDE-XYLAZINE HYDROCHLORIDE OR KETAMINE HYDROCHLORIDEDIAZEPAM COMBINATIONS  

Microsoft Academic Search

Thirty seven southern elephant seals (Mirounga leonina) were singularly or repeatedly immobilized with combinations of ketamine hydrochloride (HCI) and xylazmne HC1 or ketamine HC1 and diazepam. Atropine sulphate was included in the drug combinations. To permit exper- imental procedures the seals were immobilized for periods of 30-330 mm. The mean induction dose of ketamine HC1 was 8.71 ± 0.25 mg\\/kg

Nicholas J. Gales; Harry R. Burton

225

New acyclic 1,2,4-triazole-based Schiff base hydrazone: synthesis, characterization, spectrophotometric and computational studies.  

PubMed

A new 1,2,4-triazole-based Schiff base hydrazone with N, O, S donor set of atoms, H(4)L, has been prepared by condensation reaction of N,N'-bis(3-formyl-5-methylsalicylidene)ethane-1,2-diamine, H(2)L, with 4-amino-3-(4-pyridyl)-5-mercapto-1,2,4-triazole. The structure of H(4)L was characterized by using FT-IR, UV-Vis and (1)H NMR spectroscopic methods as well as elemental analysis data. The formation constants of copper(II), cadmium(II), mercury(II) and silver(I) complexes of H(4)L in DMSO were calculated using a hard model chemometrics method applying the spectrophotometric data. The protonation constants of H(4)L were also measured in DMSO-water (1:10) mixture. Furthermore, (1)H chemical shifts of H(4)L were studied by the gauge independent atomic orbital (GIAO) and continuous set of gauge transformations (CSGTs) methods at the level of density functional theory using B3LYP/6-311++G(*) basis sets in gas phase. The computed chemical shifts are in reasonably good agreement with the experimental data. PMID:23321219

Khanmohammadi, Hamid; Erfantalab, Malihe; Azimi, Golamhassan

2012-12-20

226

Synthetic sulfonyl-hydrazone-1 positively regulates cardiomyogenic microRNA expression and cardiomyocyte differentiation of induced pluripotent stem cells.  

PubMed

Induced pluripotent stem cells (iPSCs) are obtained from adult cells through overexpression of pluripotency factors. iPSCs share many features with embryonic stem cells (ESCs), circumventing ethical issues, and, noteworthy, match donor's genotype. iPSCs represent therefore a valuable tool for regenerative medicine. Cardiac differentiation of ESCs can be enhanced via microRNAs (miRNAs) and small chemical compounds, which probably act as chromatin remodelers. Cardiomyogenic potential of iPSCs is currently intensely investigated for cell therapy or in vitro drug screening and disease modeling. However, influences of small compounds on iPSC-related cardiomyogenesis have not yet been investigated in details. Here, we compared the effects of two small molecules, bis-peroxo-vanadium (bpV) and sulfonyl-hydrazone-1 (SHZ) at varying concentrations, during cardiac differentiation of murine iPSCs. SHZ (5?µM) enhanced specific marker expression and cardiomyocyte yield, without loss of cell viability. In contrast, bpV showed negligible effects on cardiac differentiation rate and appeared to induce Casp3-dependent apoptosis in differentiating iPSCs. Furthermore, SHZ-treated iPSCs were able to increase beating foci rate and upregulate early and late cardiomyogenic miRNA expression (miR-1, miR-133a, and miR-208a). Thus, our results demonstrate that small chemical compounds, such as SHZ, can constitute a novel and clinically feasible strategy to improve iPSC-derived cardiac differentiation. PMID:21445862

Quattrocelli, Mattia; Palazzolo, Giacomo; Agnolin, Irene; Martino, Sabata; Bouché, Marina; Anastasia, Luigi; Sampaolesi, Maurilio

2011-08-01

227

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

228

Spacer-dependent structural and physicochemical diversity in copper(II) complexes with salicyloyl hydrazones: a monomer and soluble polymers.  

PubMed

Complexation of copper(II) with a series of heterodonor chelating Schiff bases (LL) of salicylic acid hydrazide and aliphatic or cycloaliphatic ketones affords soluble one-dimensional (1D) metallopolymers containing Schiff bases as bridging ligands. Single-crystal X-ray diffraction results reveal nanometer-sized metallopolymeric wires [Cu(?-LL)(2)](n) with off-axis linkers and a zigzag geometry. Octahedrally coordinated copper centers, exhibiting a Jahn-Teller distortion, are doubly bridged by two Schiff-base molecules in the ?(2)-?(1),?(2) coordination mode. The use of dibutylketone with long alkyl chains as a component for Schiff base formation leads to a distorted square planar monomeric copper(II) complex [Cu(LL)(2)], as evidenced by its X-ray crystal structure. The compounds are characterized by elemental analyses and IR and UV-vis spectroscopy, as well as magnetic susceptibility and cyclic voltammetry measurements. Electrochemical studies on the complexes reveal an existence of polymeric and monomeric forms in solution and the dependence of Cu(II)/Cu(I) reduction potentials on alkyl groups of salicyloyl hydrazone ligands. Polymeric complexes form conducting films on Pt electrodes upon multicycle potential sweeps. PMID:21428390

Matoga, Dariusz; Szklarzewicz, Janusz; Grybo?, Ryszard; Kurpiewska, Katarzyna; Nitek, Wojciech

2011-03-23

229

Acentric nonlinear optical 2,4-dihydroxyl hydrazone isomorphic crystals with large linear, nonlinear optical susceptibilities and hyperpolarizability.  

PubMed

A systematic ab initio study of the linear, nonlinear optical susceptibilities, and hyperpolarizability of noncentrosymmetric-monoclinic 2,4-dihydroxyl hydrazone isomorphic crystals (DHNPH) within density functional theory in the local density approximation (LDA), general gradient approximation (GGA), the Engel-Vosko generalized gradient approximation (EV-GGA) and modified Becke-Johnson potential (mBJ) has been performed. The complex dielectric susceptibility dispersion, its zero-frequency limit and the birefringence are studied. Using scissors’ corrected mBJ we find a large uniaxial dielectric anisotropy (-0.56) resulting in a significant birefringence (0.61). We also find that 2,4- DHNPH possess large second harmonic generation. The calculated second order susceptibility tensor components for the static limit |?(111)(2)(0)| and |?(111)(2)(?)| at ?=1.9 ?m (0.651 eV) and at ? = 1.064 ?m (1.165 eV) are 53, 91, and 209 pm/V, respectively. A remarkable finding, applying the scissors’ correction has a profound effect on value, magnitude and sign of ?(ijk)(2)(?). In additional we have calculated the microscopic hyperpolarizability, ?(111), vector component along the principal dipole moment directions for the dominant component. We find that the value of ?(111) equal to 47× 10(-30) esu, in good agreement with the measured value (48.2× 10(-30) esu). PMID:22452425

Reshak, A H; Kamarudin, H; Auluck, S

2012-04-06

230

New acyclic 1,2,4-triazole-based Schiff base hydrazone: Synthesis, characterization, spectrophotometric and computational studies  

NASA Astrophysics Data System (ADS)

A new 1,2,4-triazole-based Schiff base hydrazone with N, O, S donor set of atoms, H4L, has been prepared by condensation reaction of N,N'-bis(3-formyl-5-methylsalicylidene)ethane-1,2-diamine, H2L, with 4-amino-3-(4-pyridyl)-5-mercapto-1,2,4-triazole. The structure of H4L was characterized by using FT-IR, UV-Vis and 1H NMR spectroscopic methods as well as elemental analysis data. The formation constants of copper(II), cadmium(II), mercury(II) and silver(I) complexes of H4L in DMSO were calculated using a hard model chemometrics method applying the spectrophotometric data. The protonation constants of H4L were also measured in DMSO-water (1:10) mixture. Furthermore, 1H chemical shifts of H4L were studied by the gauge independent atomic orbital (GIAO) and continuous set of gauge transformations (CSGTs) methods at the level of density functional theory using B3LYP/6-311++G* basis sets in gas phase. The computed chemical shifts are in reasonably good agreement with the experimental data.

Khanmohammadi, Hamid; Erfantalab, Malihe; Azimi, Golamhassan

2013-03-01

231

Crystal engineering approach to forming cocrystals of amine hydrochlorides with organic acids. Molecular complexes of fluoxetine hydrochloride with benzoic, succinic, and fumaric acids.  

PubMed

A crystal engineering strategy for designing cocrystals of pharmaceuticals is presented. The strategy increases the probability of discovering useful cocrystals and decreases the number of experiments that are needed by selecting API:guest combinations that have the greatest potential of forming energetically and structurally robust interactions. Our approach involves multicomponent cocrystallization of hydrochloride salts, wherein strong hydrogen bond donors are introduced to interact with chloride ions that are underutilized as hydrogen bond acceptors. The strategy is particularly effective in producing cocrystals of amine hydrochlorides with neutral organic acid guests. As an example of the approach, we report the discovery of three cocrystals containing fluoxetine hydrochloride (1), which is the active ingredient in the popular antidepressant Prozac. A 1:1 cocrystal was prepared with 1 and benzoic acid (2), while succinic acid and fumaric acid were each cocrystallized with 1 to provide 2:1 cocrystals of fluoxetine hydrochloride:succinic acid (3) and fluoxetine hydrochloride:fumaric acid (4). The presence of a guest molecule along with fluoxetine hydrochloride in the same crystal structure results in a solid phase with altered physical properties when compared to the known crystalline form of fluoxetine hydrochloride. On the basis of intrinsic dissolution rate experiments, cocrystals 2 and 4 dissolve more slowly than 1, and 3 dissolves more quickly than 1. Powder dissolution experiments demonstrated that the solid present at equilibrium corresponds to the cocrystal for 2 and 4, while 3 completely converted to 1 upon prolonged slurry in water. PMID:15479089

Childs, Scott L; Chyall, Leonard J; Dunlap, Jeanette T; Smolenskaya, Valeriya N; Stahly, Barbara C; Stahly, G Patrick

2004-10-20

232

Minocycline hydrochloride nanoliposomes inhibit the production of TNF-? in LPS-stimulated macrophages  

PubMed Central

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

Liu, D; Yang, P S

2012-01-01

233

40 CFR 180.558 - N,N-diethyl-2-(4-methylbenz-yloxy)ethylamine hydrochloride; tolerances for residues.  

Code of Federal Regulations, 2011 CFR

...4-methylbenz-yloxy)ethylamine hydrochloride; tolerances for residues. (a) General. A tolerance for residues of the plant growth regulator N,N- diethyl-2-(4-methylenzyloxy)ethylamine hydrochloride in or on raw agricultural...

2011-07-01

234

Synthesis, characterization and biological activities of Cu(II), Co(II), Mn(II), Fe(II), and UO2(VI) complexes with a new Schiff Base hydrazone: O-hydroxyacetophenone-7-chloro-4-quinoline hydrazone.  

PubMed

The Schiff base hydrazone ligand HL was prepared by the condensation reaction of 7-chloro-4-quinoline with o-hydroxyacetophenone. The ligand behaves either as monobasic bidentate or dibasic tridentate and contain ONN coordination sites. This was accounted for be the presence in the ligand of a phenolic azomethine and imine groups. It reacts with Cu(II), Ni(II), Co(II), Mn(II), UO(2) (VI) and Fe(II) to form either mono- or binuclear complexes. The ligand and its metal complexes were characterized by elemental analyses, IR, NMR, Mass, and UV-Visible spectra. The magnetic moments and electrical conductance of the complexes were also determined. The Co(II), Ni(II) and UO(2) (VI) complexes are mononuclear and coordinated to NO sites of two ligand molecules. The Cu(II) complex has a square-planar geometry distorted towards tetrahedral, the Ni(II) complex is octahedral while the UO(2) (VI) complex has its favoured heptacoordination. The Co(II), Mn(II) complexes and also other Ni(II) and Fe(III) complexes, which were obtained in the presence of Li(OH) as deprotonating agent, are binuclear and coordinated via the NNNO sites of two ligand molecules. All the binuclear complexes have octahedral geometries and their magnetic moments are quite low compared to the calculated value for two metal ions complexes and thus antiferromagnetic interactions between the two adjacent metal ions. The ligand HL and metal complexes were tested against a strain of Gram +ve bacteria (Staphylococcus aureus), Gram -ve bacteria (Escherichia coli), and fungi (Candida albicans). The tested compounds exhibited high antibacterial activities. PMID:21996717

Al-Shaalan, Nora H

2011-10-13

235

Effects of sevelamer hydrochloride and calcium acetate on the oral bioavailability of ciprofloxacin  

Microsoft Academic Search

Background: The oral bioavailability of ciprofloxacin is significantly decreased when administered with calcium carbonate. Sevelamer hydrochloride is a phosphate-binding cationic polymer that is devoid of calcium. The authors conducted a 3-way, randomized, crossover study to determine the effects of sevelamer hydrochloride and calcium acetate on the relative oral bioavailability of ciprofloxacin. Methods: Fifteen healthy volunteers were assigned randomly to receive

Michael B Kays; Brian R Overholser; Bruce A Mueller; Sharon M Moe; Kevin M Sowinski

2003-01-01

236

Controlled release of ciprofloxacin hydrochloride from chitosan\\/polyethylene glycol blend films  

Microsoft Academic Search

Films of chitosan and polyethylene glycol (PEG), with ciprofloxacin hydrochloride as model drug incorporated at different concentrations, have been obtained by a casting\\/solvent evaporation method. Interrelated chemical, morphological and mechanical characterizations included the component ratio of chitosan and PEG, the loaded amount of ciprofloxacin hydrochloride, the pH and ionic strength of the release solution, the thickness of the drug loaded

Qun Wang; Zhanfeng Dong; Yumin Du; John F. Kennedy

2007-01-01

237

Acotiamide hydrochloride (Z-338) enhances gastric motility and emptying by inhibiting acetylcholinesterase activity in rats  

Microsoft Academic Search

In clinical trials, acotiamide hydrochloride (acotiamide: Z-338) has been reported to be useful in the treatment of functional dyspepsia. Here, we investigated the effects of acotiamide on gastric contraction and emptying activities in rats in comparison with itopride hydrochloride (itopride) and mosapride citrate (mosapride). We also examined in vitro the compound's inhibitory effect on acetylcholinesterase (AChE) activity derived from rat

Masanao Kawachi; Yugo Matsunaga; Takao Tanaka; Yuko Hori; Katsunori Ito; Kenji Nagahama; Tomoko Ozaki; Naonori Inoue; Ryoko Toda; Kazuyoshi Yoshii; Masamichi Hirayama; Yoshihiro Kawabata; Mineo Takei

2011-01-01

238

Three cases of nalbuphine hydrochloride dependence associated with anabolic steroid use  

Microsoft Academic Search

Three case reports are presented of nalbuphine hydrochloride dependence meeting DSM IIIR and ICD10 criteria for opioid dependence. Nalbuphine hydrochloride is being obtained from illicit sources and used by those using performance enhancing drugs. In some cases this leads to opioid dependence. There is a potential risks of crossover between the misuse of drugs of performance and the misuse of

A J McBride; K Williamson; T Petersen

1996-01-01

239

Benzydamine hydrochloride in prevention and management of pain in oral mucositis associated with radiation therapy  

Microsoft Academic Search

Benzydamine hydrochloride rinse reduced pain associated with radiation mucositis when it was used during the course of radiation therapy. Fewer patients using benzydamine rinse required systemic analgesics. All patients using benzydamine tolerated the rinse well and continued with regular rinsing throughout the course of radiation therapy. Benzydamine hydrochloride is currently undergoing clinical trials in the United States for application for

J. B. Epstein; P. Stevenson-Moore

1986-01-01

240

Synthesis, characterization and molecular sensing behavior of [ZnCl 2(? 3-N,N,O-dpkbh)] (dpkbh = di-2-pyridyl ketone benzoyl hydrazone)  

Microsoft Academic Search

The reaction between ZnCl2 and di-2-pyridyl ketone benzoyl hydrazone (dpkbh) in acetonitrile under ultrasonic or reflux conditions gave [ZnCl2(?3-N,N,O-dpkbh)] in good yield. The identity of the compound was established from the results of its elemental analysis and a number of spectroscopic measurements. Solid-state infrared spectra of [ZnCl2(?3-N,N,O-dpkbh)] reveal the coordination of dpkbh, the presence of the amide proton and binding

Mohammed Bakir; Orville Green; Willem H. Mulder

2008-01-01

241

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

PubMed

A comprehensive structural and vibrational study of the potential metal-protein attenuating compound 8-hydroxyquinoline-2-carboxaldehyde isonicotinoyl hydrazone is reported. X-ray diffraction data, as well as FT-IR and Raman frequencies, were compared with the respective theoretical values obtained from DFT calculations. Theory agrees well with experiment. In this context, an attempt of total assignment concerning the FT-IR and Raman spectra of the title compound was performed, shedding new light on previous partial assignments published elsewhere. PMID:23896296

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

2013-07-11

242

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

243

The oral analgesic efficacy of bicifadine hydrochloride in postoperative pain.  

PubMed

The analgesic efficacy of 75 and 150 mg bicifadine hydrochloride was compared to 650 mg aspirin and placebo in a double-blind, single-dose study. Oral doses were administered to 100 patients suffering from moderate to severe postoperative pain. Significant analgesic activity was demonstrated with 650 mg aspirin and 150 mg bicifadine as compared to 75 mg bicifadine or placebo. No significant treatment difference was found between 75 mg bicifadine and placebo. Side effects were minor and did not interfere with the course of therapy. PMID:7096604

Wang, R I; Johnson, R P; Lee, J C; Waite, E M

1982-04-01

244

Development of novel mucoadhesive pellets of metformin hydrochloride  

Microsoft Academic Search

Mucoadhesive polymer-coated pellets containing metformin hydrochloride were prepared by the powder-layering technique using\\u000a a centrifugal fluidizing (CF)-granulator. Four high-viscosity polymers were applied to make the pellets: 1) hydroxymethylcellulose\\u000a (HPMC), 2) sodium alginate (Na-Alg), 3) HPMC\\/Carbopol, and 4) sodium carboxylmethylcellulose (Na-CMC). The physical crushing\\u000a test, mucoadhesive test, zeta-potential test, in vitro release study and observation of gastroretention state of the dosage

Jingshu Piao; Ji-Eun Lee; Kwon-Yeon Weon; Dong-Wook Kim; Jung Suk Lee; James D. S. Park; Yuichi Nishiyama; Ikuo Fukui; Jin-Seok Kim

2009-01-01

245

Hemodynamic comparison of dopexamine hydrochloride and dopamine in ischemic left ventricular dysfunction.  

PubMed

The hemodynamic dose-response effects of intravenous dopexamine hydrochloride (0.5 to 2.0 micrograms/kg/min) have been compared with dopamine (2.5 to 10 micrograms/kg/min) in 12 patients with ischemic left ventricular dysfunction in an open randomized crossover study. Both drugs increased cardiac output and decreased systemic vascular resistance. Dopexamine hydrochloride appeared to increase heart rate more than dopamine although this did not reach statistical significance. Dopexamine hydrochloride produced small increases in systolic and decreases in diastolic blood pressure, whereas dopamine had a biphasic effect resulting in a decrease in mean blood pressure at low doses and an increase at the highest dose studied. With increasing dosage, there was a trend toward more vasodilator activity with dopexamine hydrochloride than with dopamine. Dopexamine hydrochloride produced fewer adverse effects than dopamine. PMID:2457305

Jackson, N C; Taylor, S H; Frais, M A

1988-08-11

246

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

247

Modulation of Venlafaxine Hydrochloride Release from Press Coated Matrix Tablet  

PubMed Central

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

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

2008-01-01

248

Application of direct crystallization for racemic compound propranolol hydrochloride.  

PubMed

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

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

2007-10-01

249

Formulation and Evaluation of Tramadol hydrochloride Rectal Suppositories.  

PubMed

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

2008-09-01

250

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

251

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.

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

2012-01-01

252

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

253

Phosgene (chlorophenyl)hydrazones, strong sensitizers found in yellow sweaters bleached with sodium hypochlorite, defined as causative allergens for contact dermatitis by an experimental screening method in animals.  

PubMed

12 young men developed allergic contact dermatitis from wearing yellow cotton sweaters. We attempted to identify the causative agents by an experimental screening method in animals. Guinea pigs were sensitized with an acetone extract of the sweater material, by means of the guinea pig maximization test (GPMT). Active ingredients were then separated from the extract, by step-by-step patch test screening of chromatographic fractions in the guinea pigs, and finally analyzed by gas chromatography-mass spectrometry (GC-MS). Although there were 2 allergens with important activity (1 in the fraction eluted from the silica gel column with hexane, and 1 in the methanol fraction), the present study is focussed on the fat-soluble allergens in the hexane fraction. GC-MS analysis revealed that 4 kinds of phosgene (chlorophenyl)hydrazones (PCPHs) were present in the hexane fraction. PCPHs prepared in our laboratory showed strong eliciting activities, not only in the guinea pigs sensitized with the extract, but also in a male volunteer sensitized by exposure to a yellow sweater during irritancy testing. Phosgene (2,5-dichlorophenyl)hydrazone, which was the main component among the PCPHs found in the sweater, sensitized guinea pigs even at the 1 ppm level. From these results, we conclude that PCPHs were one of the allergens responsible for the cases. PMID:2282792

Kojima, S; Momma, J; Kaniwa, M A; Ikarashi, Y; Sato, M; Nakaji, Y; Kurokawa, Y; Nakamura, A

1990-09-01

254

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

NASA Astrophysics Data System (ADS)

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.

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

2013-07-01

255

Use of xylazine hydrochloride-ketamine hydrochloride for immobilization of Indian fox (Vulpes bengalensis) in field situations.  

PubMed

Reports on doses of anesthetic agents for safe and effective immobilization of most wild species occurring in India are very limited. Further, the anesthetic agents available in India for field immobilizations are limited to xylazine hydrochloride and ketamine hydrochloride. A safe and effective dosage of xylazine-ketamine for Indian fox (Vulpes bengalensis) is reported, based on 37 wild Indian fox immobilizations between April 2006 and May 2007. Foxes captured for a radiotelemetry and health monitoring study were immobilized with a mixture of xylazine (2.27 +/- 0.44 mg/kg) and ketamine (13.39 +/- 2.26 mg/kg). Induction and recovery was smooth and uneventful in all foxes. The duration of anesthesia was sufficient for the fitting of radiotransmitters, morphometric measurements, and blood sampling. No life-threatening adverse effects of immobilization were documented for at least 1 mo postimmobilization. The results suggest that field immobilization of Indian foxes with 2 mg/kg xylazine and 13 mg/kg ketamine is effective and safe. PMID:24063107

Belsare, Aniruddha V; Vanak, Abi Tamim

2013-09-01

256

[The effects of flavoxate hydrochloride on the gastrointestinal motility (author's transl)].  

PubMed

The experiments were performed to study the effects of Flavoxate hydrochloride on the gastrointestinal motility and its underlying mechanism. Gastrointestinal motility was inhibited at first and then accelerated markedly after the intravenous injection of Flavoxate hydrochloride (10 mg/kg) in the experiments of anesthetized dogs. For analyzing the underlying mechanism of this response the following experiments were executed. 1) The pendular movements of isolated ileum of rabbits were accelerated with administration of low concentration of Flavoxate hydrochloride less than 10(5) g/ml, while these were reduced with administration of high concentration more than 10(4) g/ml. Because the tetrodotoxin (2.5 times 10(7) g/ml) has no essential effect on these responses, it could be postulated that Flavoxate hydrochloride has direct effect on intestinal smooth muscle itself. 2) Flavoxate hydrochloride (10 mg/kg) induced the differentiated regional response of the sympathetic outflow, that is, the parallel decrease of cutaneous and cardiac sympathetic activities, and the converse increase of splanchnic activity. Therefore, Flavoxate hydrochloride is thought to have an effect on the integrating mechanism of the sympathetic nervous system. This view was also supported by the experiments with neuromuscular preparation of lobster (Panulirus japonicus). It is concluded from these results, that the change of gastrointestinal motility induced by intravenous injection of Flavoxate hydrochloride (10 mg/kg) is influenced both by its effect on the gastrointestinal smooth muscle itself and by its effect via the autonomic nervous system. PMID:1172143

Iriki, M; Tsuchiya, K; Kozawa, E; Kuramoto, T; Miura, A

1975-03-01

257

Development and validation of a paediatric oral formulation of clonidine hydrochloride.  

PubMed

Many drugs are unavailable in suitable paediatric dosage forms. We describe the development and validation of a stable paediatric oral formulation of clonidine hydrochloride 50 ?g/ml, allowing individualised paediatric dosing and easy administration. Stability of the extemporaneously compounded formulation of clonidine hydrochloride was assessed using a validated HPLC method. Clonidine hydrochloride was stable in the buffered aqueous solution at room temperature for up to 9 months. The described formulation is chemically stable for at least 9 months when stored in brown 100 ml PET bottles at room temperature, enabling adequate oral treatment in paediatric patients. PMID:22580108

de Goede, A L; Boedhram, R R; Eckhardt, M; Hanff, L M; Koch, B C P; Vermaat, C H; Vermes, A

2012-05-09

258

Spectroscopic and Electrical Conductivity Studies of Some Semicarbazide Hydrochloride Complexes  

NASA Astrophysics Data System (ADS)

The infrared and electronic absorption spectra of semicarbazide hydrochloride and its complexes with anthracene, tetracyanoquinodimethane TCNQ, Na-fluorescein and cupferron were recorded in the regions 200-4000cm-1 and 200-400nm. The new bands that appeared in the complex spectra were assigned. The effect of the complex formation on the frequency and intensity of the active vibrational bands was also studied. The internal energy changes of the complexes were calculated in a new line of calculation to give a clear insight about the stability of the investigated complexes. The electrical conductivity of the complexes was measured in the temperature range 25-130°C. The activation energy E was calculated and discussed on the basis of the spectroscopic information.

Fadly, M.; El-Manakhly, H.

1998-11-01

259

A phosphate binding assay for sevelamer hydrochloride by ion chromatography.  

PubMed

Sevelamer hydrochloride is a cross-linked polymeric amine; it is the active ingredient of Renagel capsules. Renagel is indicated for the control of hyperphosphatemia in patients with end-stage renal disease. An in vitro phosphate-binding assay is required to measure the drug's efficacy. The assay developed for this purpose involves mixing the drug (polymer) with a solution of known phosphate concentration, filtering off the polymer-phosphate complex, and quantitating the unbound phosphate concentration by ion chromatography. The binding capacity, reported as mmol of phosphate bound g of polymer(-1), is calculated from the calculated amount of bound phosphate and the weight of polymer used. The method has been validated for accuracy, precision, linearity, range, and ruggedness. PMID:10698557

Mazzeo, J R; Peters, R M; Hanus, M R; Chen, X; Norton, K A

1999-05-01

260

Rhabdomyolysis caused by tocolytic therapy with ritodrine hydrochloride.  

PubMed

We report a case of rhabdomyolysis with severe generalized weakness and muscle pain after administration of ritodrine hydrochloride, in a pregnant patient without history of neuromuscular disease. Laboratory tests showed an increase of blood CK value and myoglobinuria. An electromyography was performed, revealing a typical myogenic pattern and diffuse denervation activity. Muscular biopsy allowed to rule out inflammatory and metabolic myopathy. After delivery, the patient underwent intensive rehabilitation with progressive improvement of her clinical situation, until complete recovery. Three months later, both neurological assessment and CK levels were normal. This case highlights that rhabdomyolysis has to be considered even in patient treated with ritodrine alone and without history of neuromuscular disease. Therefore, muscular symptoms and CK levels should be monitored in women treated with ritodrine for premature labour. PMID:19556131

Verriello, L; D'Amico, D; Pauletto, G; Gigli, G L; Bergonzi, P

2009-06-24

261

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

2009-03-16

262

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.

Fox, Beth Anne; Stephens, Mary M

2007-01-01

263

Pharmaceutical development of an intravenous dosage form of diacetylmorphine hydrochloride.  

PubMed

A solid dosage form for multiple use was developed for parenteral administration of diacetylmorphine in a clinical trial on co-prescription of heroin to heroin addicts. A 300-mg/mL diacetylmorphine hydrochloride solution was lyophilised as 10-mL aliquots in 30-mL glass vials, to be reconstituted to 150 mg/mL with water for injection before use. Addition of bulking agents for improvement of the cake structure of the lyophilised product appeared unnecessary. Stability studies indicated good stability of the lyophilised product under prescribed storage conditions (25 degrees C, 60% relative humidity) and under more extreme conditions (40 degrees C, 75% relative humidity). The reconstituted product was found to be stable for six days at room temperature. Suitability of the product for multiple use was supported by the fact that the reconstituted product was found to be antimicrobially active. PMID:15663060

Klous, Marjolein G; Nuijen, Bastiaan; van den Brink, Wim; Van Ree, Jan M; Beijnen, Jos H

264

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

265

Spectroelectrochemical determination of chlorpromazine hydrochloride by flow-injection analysis.  

PubMed

An original, simple and sensitive flow-injection spectroelectroanalytical method for the determination of chlorpromazine in pure form or in pharmaceutical formulations is described. The method is based on the formation of a stable cationic radical by electro-oxidation in sulfuric acid medium (0.1 mol l(-1)), monitored in situ at lambda=524 nm. The determination of chlorpromazine hydrochloride in pure form or in pharmaceutical formulations was explored, considering the amperometric and the absorptiometric signal. The association of these two signals enhanced the selectivity of the analysis and proved decisive when other electroactive compounds or excipients like ascorbic acid were present in the formulation. The analytical parameters have been evaluated and the results obtained using standard additions are in agreement with the reference methods. PMID:15708668

Daniel, Daniela; Gutz, Ivano G R

2005-02-23

266

Identification and characterization of potential impurities in raloxifene hydrochloride.  

PubMed

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

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

2012-05-22

267

Evaluation of the Health Aspects of Pyridoxine and Pyridoxine Hydrochloride as Food Ingredients.  

National Technical Information Service (NTIS)

The report, by a group of qualified scientists designated the Select Committee on GRAS Substances (SCOGS), provides an independent evaluation of the safety of pyridoxine and pyridoxine hydrochloride, when used in food, at present or projected levels of us...

1977-01-01

268

Auto-Oxidation of Thioridazine Hydrochloride And Trifluoperazine Dihydrochloride: Implications for Clinical Practice.  

National Technical Information Service (NTIS)

The rate and extent of auto-oxidation of two phenothiazine derived pharmaceuticals, thioridazine hydrochloride and trifluoperazine dihydrochloride in solution were determined in response to two variables, pH and light. Of the two, trifluoperazine was foun...

Z. E. Estes

1970-01-01

269

Exposure of Humans to Carbon Monoxide Combined with Ingestion of Diphenhydramine Hydrochloride or Phenacetin.  

National Technical Information Service (NTIS)

The synergistic effect of CO and two commonly prescribed drugs, phenacetin and diphenhydramine hydrochloride were evaluated. The COHb saturation tested was 14 percent (above average for cigarette smokers), while drug doses were those usually prescribed. N...

1974-01-01

270

A review of flavoxate hydrochloride in the treatment of urge incontinence.  

PubMed

This article provides a review of the use of flavoxate hydrochloride in the treatment of urge incontinence. It outlines the pharmacology, mode of action, toxicology and pharmacokinetic studies which have been carried out, and then reviews the clinical studies, including those involving patients with benign prostatic hypertrophy. The effects of dosages of 600-1200 mg/day are compared, particularly regarding safety and tolerability factors. Finally, alternative therapies to flavoxate hydrochloride (alpha-adrenergic receptor blockers, oxybutinin chloride, terodiline hydrochloride, emepronium bromide and imipramine) are summarized. The article is written in the knowledge of recent evidence which indicates that flavoxate hydrochloride exhibits only weak anticholinergic activity on receptors involved in the control of the lower urinary tract. PMID:2461883

Ruffmann, R

271

[Identification of the related substances in fasudil hydrochloride with hyphenated techniques].  

PubMed

The study aims to identify the related substances in fasudil hydrochloride by hyphenated techniques. A WondaSil C18 (250 mm x 4.6 mm, 5 microm) column was used for the separation of the related substances with a mixture of methanol and ammonium acetate buffer solution as the mobile phase by gradient elution. The structures of the related substances were speculated by electrospray positive ionization LC-TOF/MS accurate ion mass and MS/MS determination and elucidation, and verified further through synthesis and spectroscopic analysis. Fasudil hydrochloride and the related substances were separated under the established HPLC condition. Three related substances in fasudil hydrochloride were characterized by hyphenated techniques. The hyphenated LC-MS method is useful for the identification of related substances in fasudil hydrochloride and the results obtained are valuable for its manufacturing process and quality control. PMID:23724655

Chen, Yue-Qin; Song, Min; Hang, Tai-Jun

2013-03-01

272

Denaturation/Renaturation of Organophosphorus Acid Anhydrolase (OPAA) Using Guanidinium Hydrochloride and Urea.  

National Technical Information Service (NTIS)

The understanding of how protein unfolds/refolds is a key to the development of any protein/enzyme based detection system. Using organophosphorus acid anhydrolase (OPAA) as the model protein, a guanidinium hydrochloride and urea denaturation/renaturation ...

K. K. Ong Z. Sun T. C. Cheng Y. Wei J. M. Yuan

2004-01-01

273

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

Code of Federal Regulations, 2012 CFR

...aminoethoxyvinylglycine hydrochloride (aviglycine HCl) in or on the following food commodities: Commodity Parts per million Apple 0.08 Fruit, stone, group 12, except cherry 0.170 Pear 0.08 (b) Section 18 emergency exemptions....

2012-07-01

274

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

Code of Federal Regulations, 2011 CFR

...aminoethoxyvinylglycine hydrochloride (aviglycine HCl) in or on the following food commodities: Commodity Parts per million Apple 0.08 Fruit, stone, group 12, except cherry 0.170 Pear 0.08 (b) Section 18 emergency exemptions....

2011-07-01

275

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

276

Isothermal Denaturation of Aqueous Staphylococcal Entertoxin B by Guanidine Hydrochloride, Urea, and Acid pH.  

National Technical Information Service (NTIS)

The denaturation of staphylococcal enterotoxin B at 23C by aqueous guanidine hydrochloride, urea, or dilute HCl was studied by measuring change in the intrinsic viscosity and near-ultraviolet difference spectrum of the protein. The native conformation of ...

J. F. Metzger J. R. Warren L. Spero

1973-01-01

277

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

PubMed

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

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

1999-12-31

278

Treating Chronic Tension-type Headache Not Responding to Amitriptyline Hydrochloride With Paroxetine Hydrochloride: A Pilot Evaluation  

PubMed Central

Context In some individuals, chronic tension-type headache fails to respond to tricyclic antidepressant medications that often serve as first-line therapy. Objective To evaluate the clinical efficacy of paroxetine hydrochloride for chronic tension-type headache not responding to amitriptyline hydrochloride. Design and Setting Open-label trial of paroxetine conducted at 2 outpatient sites in Ohio. Participants and Intervention Thirty-one adults (mean age, 37 years; 20 women) with chronic tension-type headache (mean, 25 headache days per month) who had failed to respond (less than 30% improvement) to treatment with either amitriptyline (n = 13) or matched placebo (n = 18). All participants were treated with paroxetine (up to 40 mg per day) in a 9-month protocol. Outcome Measures Monthly headache index calculated as the mean of pain ratings (0 to 10 scale) recorded by participants in a diary 4 times per day, number of days per month with at least moderate pain (pain rating of 5 or greater), and analgesic medication use. Results In patients who had not responded to amitriptyline, paroxetine failed to reduce chronic tension-type headaches or analgesic medication use. In patients who had not responded to placebo, paroxetine produced modest reductions in chronic tension-type headaches and analgesic use. Conclusions We found no evidence that chronic tension-type headaches that failed to respond to tricyclic antidepressant therapy with amitriptyline improved when subsequently treated with paroxetine. More support was found for the efficacy of paroxetine in patients with chronic tension-type headaches who had failed to respond to placebo.

Holroyd, Kenneth A.; Labus, Jennifer S.; O'Donnell, Francis J.; Cordingley, Gary E.

2007-01-01

279

Polymeric matrix membrane sensors for stability-indicating potentiometric determination of oxybutynin hydrochloride and flavoxate hydrochloride urogenital system drugs.  

PubMed

Four polyvinyl chloride (PVC) matrix membrane electrodes responsive to 2 drugs affecting the urogenital system--oxybutynin hydrochloride (OX) and flavoxate hydrochloride (FX)--were developed, described, and characterized. A precipitation-based technique with tungstophosphate (TP) and ammonium reineckate (R) anions as electroactive materials in a PVC matrix with an OX cation was used for electrode 1 and 2 fabrication, respectively. Electrode 3 and 4 fabrication was based on use of the precipitation technique of FX cation with tetrakis (4-chlorophenyl) borate and R anions as electroactive materials. Fast and stable Nernstian responses in the range 1 x 10(-2)-1 x 10(-6) M for the 2 drugs over the pH range 5-8 revealed the performance characteristics of these electrodes, which were evaluated according to International Union of Pure and Applied Chemistry recommendations. The method was applied to FX and OX in their pharmaceutical formulations and in human plasma samples. The 4 proposed sensors were found to be specific for the drugs in the presence of up to 60% of their degradation products. Validation of the method according to the quality assurance standards showed suitability of the proposed electrodes for use in the quality control assessment of these drugs. The recoveries for determination of the drugs by the 4 proposed selective electrodes were 99.5 +/- 0.5, 100.0 +/- 0.4, 99.9 +/- 0.4, and 100.1 +/- 0.4% for sensors 1-4, respectively. Statistical comparison between the results obtained by this method and the official method of the drugs was done, and no significant difference found. PMID:19202792

Heba, Mohamed; Ramadan, Nesrin; El-Laithy, Moustafa

280

Spectrophotometric Determination of Acebutolol Hydrochloride and Nicoumalone with Metol and Potassium Permanganate  

Microsoft Academic Search

A spectrophotometric method is described for the determination of Nicoumalone and Acebutolol hydrochloride based on the formation of molecular complex with the reduction product of Nicoumalone or hydrolysis product of Acebutolol hydrochloride and p-N-methyl benzoguinone monoimine [formed in situ from met01 (p-N-methylaminophenol sulfate) and potassium permanganate, PMBQMI] at pH 3.3. Quantitative measurements were made at the maximum absorption of 525

Chilukuri S. P. Sastry; T. Thirupathi Rao; A. Sailaja; M. V. Suryanarayana

1991-01-01

281

SPECTRAL ANALYSIS OF BENAZEPRIL HYDROCHLORIDE AND HYDROCHLOROTHIAZIDE IN PHARMACEUTICAL FORMULATIONS BY THREE CHEMOMETRIC TECHNIQUES  

Microsoft Academic Search

Three chemometric techniques (classical least squares and inverse least squares and principal component regression) were applied to the spectrophotometric analysis of two pharmaceutical tablet formulations containing hydrochlorothiazide and benazepril hydrochloride in the presence of their overlapping spectra. A training set was randomly prepared by using the different composition mixtures containing 0–22 µg\\/mL of hydrochlorothiazide and 0–36 µg\\/mL of benazepril hydrochloride in 0.1 M

Erdal Dinç

2002-01-01

282

Treatment of hyperphosphatemia with sevelamer hydrochloride in hemodialysis patients: A comparison with calcium acetate  

Microsoft Academic Search

Treatment of hyperphosphatemia with sevelamer hydrochloride in hemodialysis patients: A comparison with calcium acetate.BackgroundSevelamer hydrochloride is a recently approved calcium- and aluminium-free phosphate binder. A randomized study comparing sevelamer and calcium acetate was performed to assess the control of hyperphosphatemia in hemodialysis patients.MethodsAdministration of phosphate binders was discontinued during a two-week washout period. The patients were then randomized to receive

José G Hervás; Dolores Prados; Sebastián Cerezo

2003-01-01

283

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

284

QUANTITATIVE HPTLC DETERMINATION OF DIPHENHYDRAMINE HYDROCHLORIDE IN TABLET, GELCAP, AND CAPSULE ANTIHISTAMINE PHARMACEUTICALS  

Microsoft Academic Search

A quantitative method involving high-performance thin-layer chromatography (HPTLC) with automated sample application and UV-absorption scanning densitometry was developed for the determination of diphenhydramine hydrochloride in tablets, gelcaps, and capsules. Separation was performed on high performance silica gel plates containing fluorescent indicator, and the analyte was detected as fluorescence-quenched zones under short-wave UV light. Four different pharmaceutical products containing diphenhydramine hydrochloride

Erin E. Muller; Joseph Sherma

1999-01-01

285

Buprenorphine hydrochloride induces apoptosis in NG108-15 nerve cells  

Microsoft Academic Search

A morphine alkaloid derivative, buprenorphine hydrochloride, induces apoptosis in NG108-15 cells. Apoptosis was detected mainly by apoptosis-specific DNA fragmentation and morphological changes. This apoptosis was dose-dependent and the time-course experiment indicated that DNA fragmentation occurred within 4 h after administration of buprenorphine hydrochloride. Specific inhibitors of the previously characterized apoptotic signal cascade as well as antagonists for opioid receptors were

Fumihiko Kugawa; Ken Arae; Akemichi Ueno; Masatada Aoki

1998-01-01

286

Spectrophotometric simultaneous determination of Rabeprazole Sodium and Itopride Hydrochloride in capsule dosage form  

NASA Astrophysics Data System (ADS)

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 231 nm (minima) and 260 nm were selected to determine rabeprazole sodium and itopride hydrochloride, respectively. The method was validated with respect to linearity, precision and accuracy.

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

2008-03-01

287

Effects of Olopatadine Hydrochloride, a Histamine H1 Receptor Antagonist, on Histamine-Induced Skin Responses  

PubMed Central

Effects of olopatadine hydrochloride, a histamine H1 receptor antagonist, on histamine-induced skin responses were evaluated in 10 healthy subjects in comparison with placebo, fexofenadine hydrochloride, and bepotastine besilate. Olopatadine significantly suppressed histamine-induced wheal, flare, and itch, starting 30 minutes after oral administration. Olopatadine was more effective than fexofenadine and bepotastine. None of the drugs studied impaired performance of word processing tasks. These results suggest that olopatadine can suppress skin symptoms caused by histamine soon after administration.

Hashimoto, Takashi; Ishii, Norito; Hamada, Takahiro; Dainichi, Teruki; Karashima, Tadashi; Nakama, Takekuni; Yasumoto, Shinichiro

2010-01-01

288

Benzydamine hydrochloride in prevention and management of pain in oral mucositis associated with radiation therapy  

SciTech Connect

Benzydamine hydrochloride rinse reduced pain associated with radiation mucositis when it was used during the course of radiation therapy. Fewer patients using benzydamine rinse required systemic analgesics. All patients using benzydamine tolerated the rinse well and continued with regular rinsing throughout the course of radiation therapy. Benzydamine hydrochloride is currently undergoing clinical trials in the United States for application for approval from the Food and Drug Administration.

Epstein, J.B.; Stevenson-Moore, P.

1986-08-01

289

Comparison of lidocaine hydrocarbonate, lidocaine hydrochloride and mepivacaine in the axillary block  

Microsoft Academic Search

Axillary block was performed on 60 patients undergoing various types of surgical procedures on the upper limb. The patients\\u000a were divided randomly into three equal groups of 20 and received lidocaine hydrocarbonate 1% or lidocaine hydrochloride 1%\\u000a or mepivacaine 1%, each solution containing epinephrine 11400,000. A double-blind design was used. Lidocaine hydrocarbonate\\u000a and lidocaine hydrochloride were both found to have

R. Martin; L. Beauregard; Y. Lamarche; J. P. Tétrault

1987-01-01

290

Stability-indicating HPLC Method for Simultaneous Determination of Montelukast and Fexofenadine Hydrochloride  

PubMed Central

A simple, specific, accurate, and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of montelukast and fexofenadine hydrochloride, using a Lichrospher® 100, RP-18e column and a mobile phase composed of methanol:0.1% o-phosphoric acid (90:10 v/v), pH 6.8. The retention times of montelukast and fexofenadine hydrochloride were found to be 10.16 and 12.03 min, respectively. Linearity was established for montelukast and fexofenadine hydrochloride in the range of 2-10 ?g/ml and 24-120 ?g/ml, respectively. The percentage recoveries of montelukast and fexofenadine hydrochloride were found to be in the range of 99.09 and 99.81%, respectively. Both the drugs were subjected to acid and base hydrolysis, oxidation, photolytic, and thermal degradation conditions. The degradation products of montelukast and fexofenadine hydrochloride were well resolved from the pure drug with significant differences in their retention time values. This method can be successfully employed for simultaneous quantitative analysis of montelukast and fexofenadine hydrochloride in bulk drugs and formulations.

Pankhaniya, Mona; Patel, Parula; Shah, J. S.

2013-01-01

291

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

PubMed

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

2012-10-29

292

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

PubMed

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 ((211)At) has been hampered by low in vivo stability of the label and a propensity of these proteins localize to kidneys. Fortunately, our group has shown that the low stability of the (211)At label, generally a meta- or para-[(211)At]astatobenzoyl conjugate, on mAb Fab' fragments can be dramatically improved by the use of closo-decaborate(2-) conjugates. However, the higher stability of radiolabeled mAb Fab' conjugates appears to result in retention of radioactivity in the kidneys. This investigation was conducted to evaluate whether the retention of radioactivity in kidney might be decreased by the use of an acid-cleavable hydrazone between the Fab' and the radiolabeled closo-decaborate(2-) moiety. Five conjugation reagents containing sulfhydryl-reactive maleimide groups, a hydrazone functionality, and a closo-decaborate(2-) moiety were prepared. In four of the five conjugation reagents, a discrete poly(ethylene glycol) (PEG) linker was used, and one substituent adjacent to the hydrazone was varied (phenyl, benzoate, anisole, or methyl) to provide varying acid sensitivity. In the initial studies, the five maleimido-closo-decaborate(2-) conjugation reagents were radioiodinated ((125)I or (131)I), then conjugated with an anti-PSMA Fab' (107-1A4 Fab'). Biodistributions of the five radioiodinated Fab' conjugates were obtained in nude mice at 1, 4, and 24 h post injection (pi). In contrast to closo-decaborate(2-) conjugated to 107-1A4 Fab' through a noncleavable linker, two conjugates containing either a benzoate or a methyl substituent on the hydrazone functionality displayed clearance rates from kidney, liver, and spleen that were similar to those obtained with directly radioiodinated Fab' (i.e., no conjugate). The maleimido-closo-decaborate(2-) conjugation reagent containing a benzoate substituent on the hydrazone was chosen for study with (211)At. That reagent was conjugated with 107-1A4 Fab', then labeled (separately) with (125)I and (211)At. The radiolabeled Fab' conjugates were coinjected into nude mice bearing LNCaP human tumor xenografts, and biodistribution data were obtained at 1, 4, and 24 h pi. Tumor targeting was achieved with both (125)I- and (211)At-labeled Fab', but the (211)At-labeled Fab' reached a higher concentration (25.56 ± 11.20 vs 11.97 ± 1.31%ID/g). Surprisingly, while the (125)I-labeled Fab' was cleared from kidney similar to earlier studies, the (211)At-labeled Fab'was not (i.e., kidney conc. for (125)I vs (211)At; 4 h, 13.14 ± 2.03 ID/g vs 42.28 ± 16.38%D/g; 24 h, 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 (211)At 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 (211)At, 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

2011-05-05

293

Development and validation of a HPLC method for the determination of buprenorphine hydrochloride, naloxone hydrochloride and noroxymorphone in a tablet formulation  

Microsoft Academic Search

A simple isocratic reversed-phase high-performance liquid chromatographic method (RP-HPLC) was developed for the simultaneous determination of buprenorphine hydrochloride, naloxone hydrochloride dihydrate and its major impurity, noroxymorphone, in pharmaceutical tablets. The chromatographic separation was achieved with 10mmolL?1 potassium phosphate buffer adjusted to pH 6.0 with orthophosphoric acid and acetonitrile (17:83, v\\/v) as mobile phase, a C-18 column, Perfectsil Target ODS3 (150mm×4.6mm

Ali Mostafavi; Ghazaleh Abedi; Ahmad Jamshidi; Daryoush Afzali; Mohammad Talebi

2009-01-01

294

Electron paramagnetic resonance studies of gamma-irradiated DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride  

NASA Astrophysics Data System (ADS)

The electron paramagnetic resonance (EPR) of gamma irradiated powders of DL-alanine ethyl ester hydrochloride, L-theanine and L-glutamic acid dimethyl ester hydrochloride were investigated at room temperature. The observed paramagnetic species were attributed to the CH3?HCOOC2H5, -CH2?HCOOH and -CH2?HCOOCH3 radicals, respectively. Hyperfine structure constants and g-values were determined for these three radicals. Some spectroscopic properties and suggestions concerning the possible structure of the radicals were also discussed.

Ba?kan, M. Halim; Ayd?n, Murat

2013-08-01

295

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

296

Investigations on the mechanism of action of the novel antitumor agents 2-benzothiazolyl, 2-benzoxazolyl, and 2-benzimidazolyl hydrazones derived from 2-acetylpyridine.  

PubMed

2-Acetylpyridine hydrazone derivatives of benzothiazole, benzoxazole, and benzimidazole were found to exhibit potent cytotoxic activity against the growth of suspended leukemia and lymphomas. They were also active in a number of solid tumor screens, e.g. HeLa uterine carcinoma, SOS bone osteosarcoma, lung MB9812, lung A549, Mcf-7 breast growth. In L1210 lymphoid leukemia cells the compounds preferentially inhibited RNA synthesis followed by DNA synthesis at 100 microM after 60 min. The reduction of de novo purine synthesis by the compounds at the regulatory sites PRPP-amido transferase, IMP dehydrogenase and dihydrofolate reductase was responsible for the suppression of nucleic synthesis. Other minor sites where the agents have metabolic effects were thymidylate synthetase and thymidine kinase which would be additive with the overall inhibition of cell growth. The ct-DNA studies suggest that the compounds also interacted with the DNA molecule itself, probably affecting template activity. PMID:10327884

Hall, I H; Peaty, N J; Henry, J R; Easmon, J; Heinisch, G; Pürstinger, G

1999-04-01

297

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

PubMed

1H and 13C NMR spectra have been recorded for 2r,6c-diarylpiperidin-4-one (3'-hydroxy-2'-naphthoyl)hydrazones 10-17 and 3,3-dimethyl-2r,6c-bis(p-methoxyphenyl)piperidin-4-one (5). For selected compounds 2D NMR spectra have been recorded. The spectral data along with those reported for related compounds are used to study the effect of a heteroatom X on the 13C chemical shift of a ?-carbon with X C? C? C? torsional angle close to 0°, termed as ?-syn effect. Also ?-gauche and ?-effects of the alkyl groups at C-3 on the carbons of the aryl group at C-2 have been studied. The chemical shifts for the naphthalene ring are in accord with the mesomeric and steric effects of the carbonyl and hydroxy groups. PMID:20934908

Sylvestre, S; Pandiarajan, K

2010-09-17

298

Hydroxyfasudil, an Active Metabolite of Fasudil Hydrochloride, Relaxes the Rabbit Basilar Artery by Disinhibition of Myosin Light Chain Phosphatase  

Microsoft Academic Search

Fasudil hydrochloride (AT877, hexahydro-1-(5-isoquinolinesulfonyl)-1H-1,4-diazepine hydrochloride, identical to HA1077) inhibits cerebral vasospasm after subarachnoid hemorrhage in experimental animals and humans. In the current study, the vasorelaxing mechanism of hydroxyfasudil, a hydroxylated metabolite of fasudil hydrochloride, was determined in the rabbit basilar artery. The effects of hydroxyfasudil on tension, intracellular Ca2+ concentration ([Ca2+]i), and phosphorylation of the myosin light chain were examined

Kensei Nakamura; Junji Nishimura; Katsuya Hirano; Setsuro Ibayashi; Masatoshi Fujishima; Hideo Kanaide

2001-01-01

299

Clinical pharmacokinetic and pharmacodynamic profile of cinacalcet hydrochloride.  

PubMed

Cinacalcet hydrochloride (cinacalcet) is a calcimimetic approved for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease (CKD) receiving dialysis and for the treatment of hypercalcaemia in patients with parathyroid carcinoma. Following oral administration, peak plasma concentrations of cinacalcet occur within 2-6 hours. The absolute bioavailability is 20-25%, and administration of cinacalcet with low- or high-fat meals increases exposure (area under the plasma concentration-time curve from time zero to infinity [AUC(infinity)]) 1.5- to 1.8-fold. Cinacalcet has no significant interaction with calcium carbonate or sevelamer hydrochloride, phosphate binders commonly used in the treatment of patients with CKD receiving dialysis. The terminal elimination half-life is 30-40 hours, and steady-state concentrations are achieved within 7 days. The pharmacokinetics of cinacalcet are dose proportional over the dose range of 30-180 mg. The pharmacokinetic profile of cinacalcet is not notably affected by varying degrees of renal impairment. The pharmacokinetics of cinacalcet are comparable between healthy subjects, patients with primary hyperparathyroidism and patients with secondary hyperparathyroidism with reduced renal function (including those patients with secondary hyperparathyroidism receiving dialysis). Additionally, the pharmacokinetics of cinacalcet are similar in patients with secondary hyperparathyroidism receiving haemodialysis and patients with secondary hyperparathyroidism receiving peritoneal dialysis. Mild hepatic impairment does not affect the pharmacokinetics of cinacalcet, whereas moderate or severe hepatic impairment increases the exposure (AUC(infinity)) by approximately 2- and 4-fold, respectively. Age, sex, bodyweight and race do not notably affect the pharmacokinetics of cinacalcet. Cinacalcet is extensively metabolized by multiple hepatic cytochrome P450 (CYP) enzymes (primarily 3A4, 2D6 and 1A2) with <1% of the parent drug excreted in the urine. Dose adjustments of cinacalcet may be necessary, and parathyroid hormone (PTH) and serum calcium concentrations should be closely monitored if a patient initiates or discontinues therapy with a strong CYP3A4 inhibitor (e.g. ketoconazole, erythromycin, itraconazole). Cinacalcet is a strong inhibitor of CYP2D6; therefore, dose adjustment of concomitant medications that are predominantly metabolized by CYP2D6 and have a narrow therapeutic index (e.g. flecainide, vinblastine, thioridazine and most tricyclic antidepressants) may be required. Cinacalcet does not appreciably inhibit or induce the activities of CYP3A4, 1A2, 2C9 or 2C19. An inverse relationship exists between plasma PTH and cinacalcet concentrations. PTH concentrations are greatest before dose administration when the cinacalcet concentration is lowest (24 hours after the previous day's dose). Nadir PTH levels occur approximately 2-3 hours after dosing. PMID:19566113

Padhi, Desmond; Harris, Robert

2009-01-01

300

Characteristics of amorphous complex formed between indomethacin and lidocaine hydrochloride.  

PubMed

Indomethacin (IM) easily forms an amorphous complex with lidocaine (LC) by heat treatment. To know the mechanism involved in the formation of this complex, we studied temperature-dependent phase changes in mixtures of IM and lidocaine hydrochloride (LH), in which the cationic form of LC forms a salt with Cl(-), in various molar ratios by using DSC and NMR. Although heating of the mixture of IM and LC (IM+LC), formed a eutectic mixture, that of IM and LH (IM+LH) did not, and IM in the IM+LH mixture was dissolved into fused LH. Cooling of the fused IM+LH showed the glass transition in all of the samples containing various amounts of IM, suggesting that fused IM+LH took a homogenous amorphous state (IM/LH) below its glass transition temperature, in contrast to the fused IM+LC, which formed the rubber state and/or glass state depending on the molar content of IM. The results of the NMR study showed that IM in IM/LH caused the electronic structure of LH to change in such a way as to become similar to that of LC, but this effect was limited. Hence, mode of interaction of LH with IM is different from that of LC with IM. PMID:23352941

Shimada, Yohsuke; Goto, Satoru; Uchiro, Hiromi; Hirota, Keiji; Terada, Hiroshi

2012-12-31

301

Amantadine hydrochloride for refractory generalized epilepsy in adults.  

PubMed

Amantadine hydrochloride has been shown in several open studies to benefit children with refractory generalized epilepsy. We used amantadine as adjunctive therapy in 10 adolescents and adults with generalized tonic-clonic, myoclonic, or absence seizures refractory to therapeutic levels of valproate, carbamazepine, phenytoin, and benzodiazepines. Seven patients were men and 3 were women aged 18-29 years, and 8 of 10 patients were mentally retarded. All patients had generalized epileptiform paroxysms on EEG, with generalized or absence seizure recorded in 9. Five patients had both absence and tonic-clonic seizures, and 2 had all three seizure types. Amantadine was added to the existing regimens in weekly increments to 400 mg/day. Two patients had greater than 90 per cent seizure reduction, both with vomiting and somnolence. Two patients had seizure reduction between 50 and 90 per cent, 1 with anorexia and sleepiness. Three patients had no change in seizures, and 3 had worse tonic-clonic seizures. Amantadine may have some antiepileptic efficacy of unknown mechanism, but it may worsen generalized tonic-clonic seizures and is likely to be of limited value in adults. PMID:1927254

Drake, M E; Pakalnis, A; Denio, L S; Phillips, B

1991-01-01

302

Residual amount of vancomycin hydrochloride in vials after use.  

PubMed

We macroscopically observed vials of vancomycin hydrochloride (VCM) for injection (0.5 g/vial) dissolved in various solvents, and determined the presence or absence of residual VCM crystals. In addition, the residual VCM in vials after use was measured using a bioassay. In vials evaluated after use, the percentage of vials in which VCM crystals were macroscopically confirmed, the mean residual amount of VCM in the vials (residual %), and the percentage of vials with ?50 mg (10 %) of residual VCM were 28.1 %, 15.0 ± 7.5 mg (3.0 %), and 0 %, respectively, after the dissolution of a single VCM vial in 10 ml of distilled water for injection (n = 57); 63.8 %, 30.2 ± 19.1 mg (6.0 %), and 16.1 %, respectively, after the dissolution of a single VCM vial in 100 ml of physiological saline (n = 224); and 72.2 %, 38.5 ± 28.0 mg (7.7 %), and 33.3 %, respectively, after the dissolution of two VCM vials in 100 ml of physiological saline (n = 18). The mean residual VCM amount was greater when using physiological saline than when using distilled water for injection as a solvent. These results show the need to follow the dissolution method described in the package insert, which calls for the addition of 10 ml of distilled water for injection to each 0.5 g VCM vial. PMID:23266902

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

2012-12-25

303

Canine periodontal disease control using a clindamycin hydrochloride gel.  

PubMed

Stabilizing or reducing periodontal pocket depth can have a positive influence on the retention of teeth in dogs. A topical 2% clindamycin hydrochloride gel (CHgel) was evaluated for the treatment of periodontal disease in dogs. The CHgel formulation provides for the sustained erosion of the matrix, but also flows into the periodontal pocket as a viscous liquid, and then rapidly forms a gel that has mucoadhesive properties and also may function as a physical barrier to the introduction of bacteria. A professional teeth cleaning procedure including scaling and root planing was done in dogs with one group receiving CHgel following treatment. Periodontal health was determined before and after the procedure including measurement of periodontal pocket depth, gingival index, gingival bleeding sites, and number of suppurating sites. There was a statistically significant decrease in periodontal pocket depth (19%), gingival index (16%), and the number of bleeding sites (64%) at 90-days in dogs receiving CHgel. Additionally, the number of suppurating sites was lower (93%) at 90-days for the group receiving CHgel. The addition of CHgel effectively controlled the bacterial burden (e.g, Fusobacterium nucleatum) at both day 14 and 90. Gingival cells in culture were shown to rapidly incorporate clindamycin and attain saturation in approximately 20-minutes. In summary, a professional teeth cleaning procedure including root planning and the addition of CHgel improves the gingival index and reduces periodontal pocket depth. PMID:22416621

Johnston, Thomas P; Mondal, Pravakar; Pal, Dhananjay; MacGee, Scott; Stromberg, Arnold J; Alur, Hemant

2011-01-01

304

Dielectric relaxation studies and dissolution behavior of amorphous verapamil hydrochloride.  

PubMed

Verapamil hydrochloride (VH) is a very popular calcium channel blocker. Solubility of its crystalline form in the blood reaches only 10-20%. Thus, it seems to be very important to improve its bioavailability. In this article, we show that the preparation of the amorphous form of VH enhance its dissolution rate. In addition we performed dielectric measurements to describe molecular dynamics of this active pharmaceutical ingredient (API). Since examined sample is typical ionically conducting material, to gain information about structural relaxation we employed the dielectric modulus formalism. The temperature dependence of the structural relaxation time can be described over the entire measured range by a single Vogel-Fulcher-Tamman (VFT) equation. From the VFT fits the glass transition temperature was estimated as T(g) = 320.1 K. Below glass transition temperature one clearly visible secondary relaxation, with activation energy E(a) = 37.8 kJ/mol, was reported. Deviations of experimental data from KWW fits on high-frequency flank of alpha-peak indicate the presence of an excess wing in tested sample. Based on Kia Ngai's coupling model we identified the excess wing as true Johari-Goldstein process. PMID:19593787

Adrjanowicz, K; Kaminski, K; Paluch, M; Wlodarczyk, P; Grzybowska, K; Wojnarowska, Z; Hawelek, L; Sawicki, W; Lepek, P; Lunio, R

2010-02-01

305

Kinetics of degradation of imidapril hydrochloride in finished dosage formulations.  

PubMed

This study investigates the impact of relative air humidity and temperature on the stability of imidapril hydrochloride (IMD) tablets. For this purpose the forced degradation test was used and the following environmental conditions were employed: RH = 76.4% and the temperature range of 313 - 333 K. For the determination of IMD content in the analyzed samples a reversed-phase high performance liquid chromatography (RP-HPLC) technique was used. Three series of tablets were prepared: whole-blistered tablets, whole-bare tablets and halved-bare tablets, in order to analyze the influence of different in-home storage habits on IMD tablets' quality. In the course of the study, the degradation of IMD was observed in each series of tablets. The kinetic mechanisms and the thermodynamic parameters of these reactions were established. It was evidenced that halved IMD tablets stored without immediate packaging retain their quality only for 12 days while tablets stored according to label recommendations are stable for 513 days. PMID:23923397

Stanisz, Beata; Regulska, Katarzyna

306

Preliminary toxicological report of metformin hydrochloride loaded polymeric nanoparticles.  

PubMed

Nanosized materials have tremendous application in every field of human activity, with a lot of economic benefit increasing nanoparticle research and use. There are number of nanosized products already available commercially and many others are in queue. Therefore, there is a pressing need for careful consideration of benefits and side effects of the use of nanoparticles in medicine. This research work aims at providing a balanced update of this exciting potentially toxicological effect of manufactured Metformin hydrochloride loaded polymeric nanoparticles. To assess the toxicities systematically on the functions of various tissues and organs in rats, the rats were fed with the manufactured polymeric nanoparticles for a period of 30 days repeated oral administration. Variation in the protein, carbohydrate and fat metabolic profile of the rat exposed to nanoparticles were studied by hematobiochemical and pathology profiles. The haemolytic potential of these nanoparticles were determined by means of an in vitro haemolysis assay. All formulations showed haemolytic effect less than 5%. The study revealed that Metformin loaded PMMA and PLGA polymeric nanoparticle did not produce any toxicity. PMID:23293465

Lekshmi, Unnikrishnan Meenakshi Dhana; Reddy, Pully Neelakanta

2012-09-01

307

Acute and repeat-dose toxicity studies of the (6-maleimidocaproyl)hydrazone derivative of doxorubicin (DOXO-EMCH), an albumin-binding prodrug of the anticancer agent doxorubicin  

Microsoft Academic Search

The (6-maleimidocaproyl)hydrazone derivative of doxorubicin (DOXO-EMCH) is an albumin-binding prodrug of doxorubicin with acid-sensitive properties that demonstrates superior antitumor efficacy in murine tumor models, and has been evaluated in a phase I study. In order to establish the toxicity profile of this prodrug, acute and repeat-dose toxicity studies were performed with DOXO-EMCH in CD1-mice, Sprague-Dawley rats and Beagle dogs. Although

F. Kratz; G. Ehling; H. M. Kauffmann; C. Unger

2007-01-01

308

Synthesis and physicochemical properties of fac-[Re(CO)3(?-N,N-dpkfah)Cl], dpkfah=di-2-pyridyl ketone 2-furoic acid hydrazone: the molecular structure of fac-[Re(CO)3(?-N,N-dpkfah)Cl]?·?acetone  

Microsoft Academic Search

Reaction between [Re(CO)5Cl] and di-2-pyridyl ketone 2-furoic acid hydrazone (dpkfah) (1) in refluxing toluene gave fac-[Re(CO)3(?-N,N-dpkfah)Cl] (2). Spectroscopic and electrochemical measurements disclosed sensitivity of 2 to its surroundings. H-NMR measurements showed that the amide proton exchanged with solvent protons, and its chemical shift is solvent and temperature dependent, while the chemical shifts of aromatic protons are solvent and temperature independent.

Mohammed Bakir; Colin Gyles

2011-01-01

309

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.

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

2013-01-01

310

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

311

A double blind comparison of alprazolam and amitriptyline hydrochloride in the treatment of nonpsychotic depression.  

PubMed

In a six week, double-blind, parallel study of alprazolam and amitriptyline hydrochloride in 130 outpatients suffering from moderate to severe nonpsychotic depression, alprazolam was as effective as amitriptyline hydrochloride in relieving depressive symptoms and significantly more effective in relieving symptoms of anxiety and somatization. Alprazolam showed an earlier onset of activity in most measurements of efficacy and produced fewer side effects than amitriptyline hydrochloride. Anticholinergic side effects were reported more frequently by patients taking amitriptyline hydrochloride, while drowsiness was reported more frequently by patients taking alprazolam. At the end of the study, the average daily doses were 2.4 mg alprazolam and 135 mg amitriptyline hydrochloride. The Hamilton Psychiatric Rating Scale for Depression, Hamilton Anxiety Rating Scale, Physician's Global Impressions, Patients' Global Impressions, Hopkins Self-Rating Symptom Scale, and Symptom and Side Effects Checklist were evaluated at the end of weeks 1, 2, 3 and 6 to determine and compare the efficacy and safety of the two study drugs. PMID:3289717

Singh, A N; Nair, N P; Suranyi-Cadotte, B; Schwartz, G; Lizondo, E

1988-04-01

312

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

2011-10-21

313

Vernakalant hydrochloride for the treatment of atrial fibrillation.  

PubMed

Atrial fibrillation (AF) is the most common arrhythmia encountered in clinical practice. Rhythm control strategy for AF is limited by drug toxicity and side effects, and recent trials have shown that this strategy is not superior to a rate control one. New antiarrhythmic drugs, free of undesired effects, would enhance rhythm control, with the possibility of sinus rhythm restoration and maintenance. A promising find in the search for new antiarrhythmic therapies is atrial-tissue specific ion channels. The findings that the ultrarapid delayed rectifier (I(Kur)) and the inwardly rectifying, acetylcholine-regulated current (I(K-Ach)) exist in atrial but not ventricular tissue increase the probability that atrioselective drugs without ventricular proarrhythmic toxicity can be developed for treatment of patients with AF. There are also other potential targets for atrial-selective therapy: transient outward current (I(to)), rapidly and slowly activating delayed rectifier currents (I(Kr) and I(Ks)), atrial sodium current (I(Na)) and atrially expressed connexins. New drugs under development with promising atrial-selectivity include: tertiapin, NIP-142, NIP-141, JTV-519, AVE0118, AVE1231, DPO-1, AZD7009 and many others. Among such new agents, vernakalant hydrochloride is currently in an advanced phase of development and has already been evaluated in clinical trials. In this overview, we describe the history and current state of developmental process of the drug, as well as its mechanism of action and influence on electrophysiological parameters. Vernakalant seems to be effective in terminating recent-onset AF, but is not efficacious in long-lasting AF and atrial flutter. The drug may be relatively free of proarrhythmic effects, and exerts a protective effect on ventricular tissue and ventricular repolarization. It is expected that the intravenous formulation will soon be approved for the pharmacological termination of recent-onset AF. PMID:19938903

Kozlowski, Dariusz; Budrejko, Szymon; Lip, Gregory Y H; Mikhailidis, Dimitri P; Rysz, Jacek; Raczak, Grzegorz; Banach, Maciej

2009-12-01

314

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

315

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

316

Liquid-Liquid Extraction by Trilaurylamine HydroChloride; L'EXTRACTION LIQUIDE-LIQUIDE PAR LE CHLORHYDRATE DE TRILAURYLAMINE  

Microsoft Academic Search

The extraction of several trivalent actinides and lanthanides in tracer ; amounts by organic solutions of trilaurylamine hydrochloride from concentrated ; aqueous chloride solutions was investigated. From chemical analysis and ; physicochemical investigation of the organic phase (titrations of hydrochloric ; acid and water, infrared absorption, conductivity, cryoscopic, and vapor pressure ; measurements), it is concluded that trilaurylamine hydrochloride can

G. Duyckaerts; J. Fuger; W. Mueller

1963-01-01

317

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

2013-03-21

318

Determination of Montelukast Sodium and Bambuterol Hydrochloride in Tablets using RP HPLC  

PubMed Central

An accurate, specific and precise assay level gradient reverse-phase high-performance liquid chromatographic method was developed for simultaneous determination of montelukast sodium and bambuterol hydrochloride in tablet dosage form. An inertsil ODS C-18, 5 ?m column having 250×4.6 mm I.D. in gradient mode, with mobile phase A, containing 0.025 M sodium phosphate buffer: methanol (85:15) and mobile phase B, containing acetonitrile:methanol (85:15) was used at different time intervals. The flow rate was 1.5 ml/min and effluent was monitored at 218 nm. The retention times of montelukast sodium and bambuterol hydrochloride were 21.2 min and 5.8 min respectively. The linearity for both the drugs was in the range of 0.25-0.75 mg/ml with correlation coefficients of 0.9999 and 0.9996 for montelukast sodium and bambuterol hydrochloride, respectively.

Patil, Smita; Pore, Y. V.; Kuchekar, B. S.; Mane, Aruna; Khire, V. G.

2009-01-01

319

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

2011-02-01

320

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.

Badr, Jihan M.

2013-01-01

321

1-Adamantanamine hydrochloride: inhibition of Rous and Esh Sarcoma viruses in cell culture.  

PubMed

I-Adamantanamine hydrochloride, added to chick embryo cells, inhibited focus production upon subsequent inoculation of the cells with Rous and Esh sarcoma viruses. Addition of the chemical to suspensions of Rous and Esh viruses before they were added to chick cell cultures did not inactivate the viruses; and the addition to chick cells did not prevent plaque formation following their inoculation with Newcastle disease virus. This indicates that cells treated with 1-adamantanamine hydrochloride are capable of supporting viral replication, and these observations suggest that the drug inhibits growth of two oncogenic viruses by prevention of virus penetration, but not by a virucidal effect or cell intoxication. PMID:4287164

Wallbank, A M; Matter, R E; Klinikowski, N G

1966-06-24

322

The binary phase diagram of propranolol hydrochloride and crystallization-based enantioseparation.  

PubMed

Inconsistent results were reported for the solid-state nature of the racemic species of the pharmaceutical relevant compound propranolol hydrochloride. In this work the binary phase diagram of the propranolol hydrochloride enantiomers is studied. Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), and high performance liquid chromatography (HPLC) were used as analytical methods. The type of the racemic species, the presence and extent of partial solid solutions and the stability regions of polymorphic forms in the system were investigated. The identified binary phase diagram is sketched. Finally, the feasibility of crystallization-based resolution is discussed. PMID:19798754

Polenske, Daniel; Lorenz, Heike; Seidel-Morgenstern, Andreas

2010-04-01

323

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 0.2-2.6 THz, 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

324

Intra-arterial Administration of Fasudil Hydrochloride for Vasospasm Following Subarachnoid Haemorrhage: Experience of 90 Cases  

Microsoft Academic Search

\\u000a \\u000a Background: We investigated the clinical efficacy of intra-arterial administration of fasudil hydrochloride for cerebral vasospasm.\\u000a \\u000a \\u000a \\u000a Method: We reviewed 90 cases treated with intra-arterial administration of fasudil hydrochloride between August 1998 and April 2009\\u000a and investigated the clinical efficacy for cerebral vasospasm.\\u000a \\u000a \\u000a \\u000a \\u000a Findings: Angiographic improvement of vasospasm was noted in all procedures. Eight had ischemic lesion on CT at discharge in

S. Iwabuchi; T. Yokouchi; M. Hayashi; K. Sato; N. Saito; Y. Hirata; J. Harashina; H. Nakayama; M. Akahata; K. Ito; H. Kimura; K. Aoki

325

Comparison of lidocaine hydrocarbonate, lidocaine hydrochloride and mepivacaine in the axillary block.  

PubMed

Axillary block was performed on 60 patients undergoing various types of surgical procedures on the upper limb. The patients were divided randomly into three equal groups of 20 and received lidocaine hydrocarbonate 1% or lidocaine hydrochloride 1% or mepivacaine 1%, each solution containing epinephrine 1/400,000. A double-blind design was used. Lidocaine hydrocarbonate and lidocaine hydrochloride were both found to have a shorter latency of analgesia than mepivacaine. Duration of analgesia, quality of the sensory and motor block were not found to be statistically different between the three groups. PMID:3677281

Martin, R; Beauregard, L; Lamarche, Y; Tétrault, J P

1987-11-01

326

A monoclinic polymorph with Z = 4 of (E)-2,4-dihy-droxy-acetophenone 2,4-dinitro-phenyl-hydrazone N,N-dimethyl-formamide monosolvate.  

PubMed

The title compound, C(14)H(12)N(4)O(6)·C(3)H(7)NO, is a monoclinic polymorph of an already published structure [Baughman et al. (2004 ?). Acta Cryst. C60, 103-106]. In the previously reported structure, the compound crystallized in the triclinic space group P[Formula: see text] (Z = 2), whereas the structure reported here is monoclinic (P2(1)/n, Z = 4). In both forms, two intra-molecular hydrogen bonds result in the formation of a fairly planar hydrazone skeleton (r.m.s. deviations for all non-H atoms = 0.127?Å for the monoclinic from and 0.131?Å for the triclinic form) and each mol-ecule is hydrogen bonded to one solvent mol-ecule. The principal difference between the two forms lies in the different orientation of the two mol-ecules. In the monoclinic form, the two mol-ecules are almost coplanar [dihedral angle = 3.27?(2)°], whereas in the triclinic form the two mol-ecules are almost mutulally perpendicular (dihedral angle = 85.3°). PMID:22199915

Han, Hongfei; Liu, Yaohua

2011-11-25

327

A monoclinic polymorph with Z = 4 of (E)-2,4-dihy-droxy-acetophenone 2,4-dinitro-phenyl-hydrazone N,N-dimethyl-formamide monosolvate  

PubMed Central

The title compound, C14H12N4O6·C3H7NO, is a monoclinic polymorph of an already published structure [Baughman et al. (2004 ?). Acta Cryst. C60, 103–106]. In the previously reported structure, the compound crystallized in the triclinic space group P (Z = 2), whereas the structure reported here is monoclinic (P21 /n, Z = 4). In both forms, two intra­molecular hydrogen bonds result in the formation of a fairly planar hydrazone skeleton (r.m.s. deviations for all non-H atoms = 0.127?Å for the monoclinic from and 0.131?Å for the triclinic form) and each mol­ecule is hydrogen bonded to one solvent mol­ecule. The principal difference between the two forms lies in the different orientation of the two mol­ecules. In the monoclinic form, the two mol­ecules are almost coplanar [dihedral angle = 3.27?(2)°], whereas in the triclinic form the two mol­ecules are almost mutulally perpendicular (dihedral angle = 85.3°).

Han, Hongfei; Liu, Yaohua

2011-01-01

328

Mechanisms of the cascade synthesis of substituted 4-amino-1,2,4-triazol-3-one from Huisgen zwitterion and aldehyde hydrazone: a DFT study.  

PubMed

The detailed reaction mechanisms of the title reaction are shed light on by using the density functional theory (DFT). The calculated results have demonstrated that the whole reaction takes place via four processes (processes (I-IV)), among which, three possible reaction mechanisms are proposed for process (II) (channels 1-3) and two for process (IV) (channels 4-5). According to our calculated results, channel 3 and channel 5 are verified to be most energetically favorable. As interpreted in the text, in process (II), the proton transfer should be performed prior to the nucleophilic attack, and the AA-Type transfer strategy is more likely to occur. The global reactivity index (GRI) and frontier molecular orbital (FMO) analyses of the aldehyde hydrazone have further supported the AA-Type mechanism. In process (IV), however, the titled product has been demonstrated to be formed by the synergetic elimination of two protons via a six-membered ring transition state. Taking an integrated view, the highest energy barrier for the whole reaction along the most favorable pathway is 32.19 kcal/mol, which is consistent with the mild thermal experimental conditions. More interestingly, the qualified mechanisms in this work have given a perfect explanation to the optimal reactants molar ratio of highest yields (R1/R2/R3 = 2/1/1) employed in the experiment. PMID:22223156

Zhang, Wenjing; Zhu, Yanyan; Wei, Donghui; Tang, Mingsheng

2012-01-06

329

Cellular Delivery of Doxorubicin via pH-Controlled Hydrazone Linkage Using Multifunctional Nano Vehicle Based on Poly(?-L-Malic Acid)  

PubMed Central

Doxorubicin (DOX) is currently used in cancer chemotherapy to treat many tumors and shows improved delivery, reduced toxicity and higher treatment efficacy when being part of nanoscale delivery systems. However, a major drawback remains its toxicity to healthy tissue and the development of multi-drug resistance during prolonged treatment. This is why in our work we aimed to improve DOX delivery and reduce the toxicity by chemical conjugation with a new nanoplatform based on polymalic acid. For delivery into recipient cancer cells, DOX was conjugated via pH-sensitive hydrazone linkage along with polyethylene glycol (PEG) to a biodegradable, non-toxic and non-immunogenic nanoconjugate platform: poly(?-l-malic acid) (PMLA). DOX-nanoconjugates were found stable under physiological conditions and shown to successfully inhibit in vitro cancer cell growth of several invasive breast carcinoma cell lines such as MDA-MB-231 and MDA-MB- 468 and of primary glioma cell lines such as U87MG and U251.

Patil, Rameshwar; Portilla-Arias, Jose; Ding, Hui; Konda, Bindu; Rekechenetskiy, Arthur; Inoue, Satoshi; Black, Keith L.; Holler, Eggehard; Ljubimova, Julia Y.

2012-01-01

330

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

SciTech Connect

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

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

2012-10-11

331

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

332

HEALTH AND ENVIRONMENTAL EFFECTS PROFILE FOR 4-CHLORO-2-METHYLANILINE AND 4-CHLORO-2-METHYLANILINE HYDROCHLORIDE  

EPA Science Inventory

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)...

333

Simultaneous Determination of Hydrochlorothiazide and Propranolol Hydrochloride in Tablets by High-Performance Liquid Chromatography  

Microsoft Academic Search

A simple and stability indicating HPLC procedure is described for the simultaneous determination of hydrochlorothiazide and propranolol hydrochloride in tablet formulations. Potential degradation products of both drugs and synthesis impurities of hydrochlorothiazide were separated, making the determination stability indicating for both drugs and selective for hydrochlorothiazide. All compounds were chromatographed on a cyanopropylsilane column, eluted with a 15:85 mixture of

Michael E. Hitscherich; Elaine M. Rydberg; Dimitri C. Tsilifonis; Robert E. Daly

1987-01-01

334

Use of diethazine hydrochloride for the extractive spectrophotometric determination of uranium and as a redox indicator.  

PubMed

Optimum conditions have been established for the formation and extraction of the complex formed from diethazine, thiocyanate and uranium(VI). An extractive spectrophotometric method for the determination of uranium(VI) is described. Experimental conditions have been also established for the direct titrimetric determination of uranium(IV) with potassium dichromate, using diethazine hydrochloride as redox indicator. Interferences have been considered. PMID:18962157

Puzanowska-Tarasiewicz, H; Tarasiewicz, M; Grudniewska, A

1977-10-01

335

COMPARATIVE ANAESTHETIC EFFICACY OF PROPOFOL, THIOPENTAL SODIUM AND COMBINATION OF PROPOFOL WITH KETAMINE HYDROCHLORIDE IN DOGS  

Microsoft Academic Search

The present study was undertaken to determine the comparative efficacy of propofol alone at two dosages, thiopental sodium and propofol in combination with ketamine hydrochloride in dogs. For this purpose, 24 healthy stray dogs were randomly divided into four equal groups viz. A, B, C and D. Groups A and B were treated with propofol at the dose rates of

N. MUHAMMAD; M. A. ZAFAR; G. MUHAMMAD; M. Z. MASOOD; A. MANZOOR; I. SARFARAZ

336

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

PubMed

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

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

2012-03-01

337

Elastic liposomes mediated transdermal delivery of an anti-hypertensive agent: propranolol hydrochloride.  

PubMed

One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present investigation ultradeformable lipid vesicles, that is, elastic liposomes were prepared incorporating propranolol hydrochloride for enhanced transdermal delivery. Elastic liposomes bearing propranolol hydrochloride were prepared by conventional rotary evaporation method and characterized for various parameters including vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity, and in vitro drug release. In vitro flux, enhancement ratio (ER), and release pattern of propranolol hydrochloride were calculated for transdermal delivery. In vivo study conducted on male albino rats (Sprague Dawley) was also taken as a measure of performance of elastic liposomal, liposomal, and plain drug solution. The better permeation through the skin was confirmed by confocal laser scanning microscopy (CLSM). Results indicate that the elastic liposomal formulation for transdermal delivery of propranolol hydrochloride provides better transdermal flux, higher entrapment efficiency, ability as a self-penetration enhancer and effectiveness for transdermal delivery as compared to liposomes. PMID:16960826

Mishra, Dinesh; Garg, Minakshi; Dubey, Vaibhav; Jain, Subheet; Jain, N K

2007-01-01

338

Observations on the use of cyproheptadine hydrochloride as an antipruritic agent in allergic cats.  

PubMed Central

Cyproheptadine hydrochloride was administered to 20 presumed or proven allergic cats to determine its efficacy in controlling pruritus. Each cat received 2 mg, orally, every 12 h. The pruritus was satisfactorily controlled in 9 cats. Side effects were seen in 8 cats, and included polyphagia, sedation, vocalization, affectionate behavior, and vomiting.

Scott, D W; Rothstein, E; Beningo, K E; Miller, W H

1998-01-01

339

Simultaneous HPLC determination of butenafine hydrochloride and betamethasone in a cream formulation.  

PubMed

A fast, specific, accurate and precise reverse phase high performance liquid chromatographic method was developed for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. The determination was carried out on licrocart licrosphere RP-select B (250x4.6 mm, 5 mu) column in isocratic mode, the mobile phase consisting of 50 mM ammonium acetate buffer and acetonitrile in the ratio of 60:40, adjusted to pH 4.5 +/- 0.1 with glacial acetic acid. The flow rate was 2.0 ml/min and eluent was monitored at 254 nm. The retention times of butenafine hydrochloride and betamethasone were 4.70 min and 7.76 min, respectively, and the resolution factor was greater than 4.0. Linearity of butenafine hydrochloride and betamethasone were in the range of 100-300 mug/ml and 5-15 mug/ml, respectively. The proposed method is also found to be precise and robust for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. PMID:20502575

Ankam, R; Mukkanti, K; Durgaprasad, S; Khan, M

2009-09-01

340

In vitro Release Kinetics Study of Diltiazem Hydrochloride from Wax and Kollidon SR Based Matrix Tablets  

Microsoft Academic Search

Extended-release matrix tablets of diltiazem hydrochloride (DTZ) were prepared using waxy materials alone or in combination with Kollidon SR. Matrix waxy materials were carnauba wax (CW), bees wax (BW), cetyl alcohol (CA) and glyceryl monostearate (GMS). Dissolution studies were carried out by using a six stations USP XXII type 1 apparatus. The in vitro drug release study was done in

Mohammad Safiqul Islam; Selim Reza; Habibur Rahman

2008-01-01

341

HEALTH AND ENVIRONMENTAL EFFECTS PROFILE FOR 1-AMINO-2-NAPHTHOL AND 1-AMINO-2-NAPHTHOL HYDROCHLORIDE  

EPA Science Inventory

The Health and Environmental EFfects Profile for 1-amino-2-naphthol and 1-amino-2-naphthol 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 prov...

342

Health and Environmental Effects Profile for 1-Amino-2-Naphthol and 1-Amino-2-Naphthol Hydrochloride.  

National Technical Information Service (NTIS)

The Health and Environmental EFfects Profile for 1-amino-2-naphthol and 1-amino-2-naphthol hydrochloride was prepared to support listings of hazardous constituents of a wide range of waste streams under Section 3001 of the Resource Conservation and Recove...

1986-01-01

343

Simultaneous HPLC Determination of Butenafine Hydrochloride and Betamethasone in a Cream Formulation  

PubMed Central

A fast, specific, accurate and precise reverse phase high performance liquid chromatographic method was developed for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation. The determination was carried out on licrocart licrosphere RP-select B (250×4.6 mm, 5 ?) column in isocratic mode, the mobile phase consisting of 50 mM ammonium acetate buffer and acetonitrile in the ratio of 60:40, adjusted to pH 4.5 ± 0.1 with glacial acetic acid. The flow rate was 2.0 ml/min and eluent was monitored at 254 nm. The retention times of butenafine hydrochloride and betamethasone were 4.70 min and 7.76 min, respectively, and the resolution factor was greater than 4.0. Linearity of butenafine hydrochloride and betamethasone were in the range of 100-300 ?g/ml and 5-15 ?g/ml, respectively. The proposed method is also found to be precise and robust for the simultaneous determination of butenafine hydrochloride and betamethasone in cream formulation.

Ankam, R.; Mukkanti, K.; Durgaprasad, S.; Khan, M.

2009-01-01

344

Simultaneous estimation of Montelukast sodium and Bambuterol hydrochloride in tablets by spectrophotometry.  

PubMed

Two simple, rapid, accurate and precise methods have been developed for simultaneous estimation of Montelukast sodium and Bambuterol hydrochloride from tablet dosage form. In the first method, the first derivative spectrum was determined. Montelukast sodium showed zero crossing point at 209.5 nm and Bambuterol hydrochloride showed zero crossing point at 238.5 nm. The dA/dlambda was measured at 209.5 nm for Bambuterol hydrochloride and 238.5 nm for Montelukast sodium and calibration curves were plotted as dA/dlambda versus concentration respectively. Quantitative determination of Montelukast sodium and Bambuterol hydrochloride in tablets was carried out using calibration curve by interpolation method. In the second method, Multicomponent mode of analysis was used and the measurement of absorbances at two wavelengths, 283.6 nm (lambda-max of MKST) and 211.8 nm (working wavelength selected for BHC) in 95% methanol, was carried out. These methods were validated statistically as per ICH guidelines. The recovery studies confirm the accuracy of the proposed method. PMID:19957541

Nanda, R K; Pangarkar, V B; Thomas, A B; Kothapalli, L P; Pawar, A A

345

Bioassay of Phenoxybenzamine Hydrochloride for Possible Carcinogenicity. CAS No. 63-92-3.  

National Technical Information Service (NTIS)

A bioassay of phenoxybenzamine hydrochloride for possible carcinogenicity was conducted by administering the test chemical by intraperitoneal injection to Sprague-Dawley rats and B6C3F1 mice. Groups of 35 rats of each sex were administered phenoxybenzamin...

1978-01-01

346

Double Blind Trial of Yohimbine Hydrochloride in the Treatment of Erection Inadequacy  

Microsoft Academic Search

For many years yohimbine was a common treatment for disorders of potency and libido. However, yohimbine was withdrawn from use in the United Kingdom on account of inadequacy of the documentation confirming its efficiency. We report here the results of a double blind, cross over, placebo controlled trial of yohimbine hydrochloride 5.4 mg three times daily in the treatment of

Alan J. Riley; Raymond E. Goodman; John M. Kellett; Richard Orr

1989-01-01

347

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

348

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

Microsoft Academic Search

A quantitative high-performance liquid chromatography (HPLC) laboratory experiment which entails the isocratic separation and simultaneous determination of the two active components of a commercial antipsychotic tablet has been developed. The prescription formulation used in this experiment contains amitriptyline hydrochloride (a tricyclic antidepressant) and perphenazine (a tranquilizer). Our experiment makes use of a straightforward HPLC separation on a cyanopropyl-packed column with

Glenda K. Ferguson

1998-01-01

349

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

350

Teratologic Evaluation of Oxytetracycline Hydrochloride (CAS No. 2058-46-0) in CD-1 Mice.  

National Technical Information Service (NTIS)

No evidence for teratogenicity of oxytetracycline hydrochloride was seen in pregnant CD-1 mice when administered by oral gavage during the time of organogenesis at doses which produced little evidence of maternal toxicity (1325-2100 mg/kg/day). However, a...

R. Wolkowski-Tyl T. A. Ledoux J. R. Reel C. Jones-Price L. Langhoff-Paschke

1982-01-01

351

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

352

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

353

Efficacy of topical benzydamine hydrochloride gel on oral mucosal ulcers: an in vivo animal study  

Microsoft Academic Search

The aim of this study was to investigate the effect of benzydamine hydrochloride bioadhesive gel on healing of oral mucosal ulceration in an animal model. For in vivo determination of the effects of the bioadhesive gel, 36 rabbits were separated into three groups: the first group was treated with the gel formulation without active agent, the second group with the

B. Sezer; P. Güneri; A. Veral; H. Boyacio?lu; G. Ertan; J. B. Epstein

2011-01-01

354

Stability of fluorouracil, cytarabine, or doxorubicin hydrochloride in ethylene vinylacetate portable infusion-pump reservoirs.  

PubMed

The stability of fluorouracil, cytarabine, and doxorubicin hydrochloride in admixtures stored in portable infusion-pump reservoirs was investigated. Admixtures containing fluorouracil 50 or 10 mg/mL, cytarabine 25 or 1.25 mg/mL, or doxorubicin hydrochloride 1.25 or 0.5 mg/mL in 0.9% sodium chloride injection or 5% dextrose injection were placed in 80-mL ethylene vinylacetate drug reservoirs protected from light, and 1-mL quantities were withdrawn immediately after preparation and after storage for 1, 2, 3, 4, 7, 14, and 28 days at 4, 22, or 35 degrees C. For each condition, three samples from each admixture were tested for drug concentration by stability-indicating high-performance liquid chromatography. The admixtures were also monitored for precipitation, color change, and pH. Evaporative water loss from the containers was measured. Fluorouracil was stable at all temperatures for 28 days. Cytarabine was stable for 28 days at 4 and 22 degrees C and for 7 days at 35 degrees C. Doxorubicin hydrochloride was stable for 14 days at 4 and 22 degrees C and for 7 days at 35 degrees C. No color change or precipitation was observed, and pH values were stable. Loss of water through the reservoirs was substantial only at 35 degrees C for 28 days. When stored in ethylene vinylacetate portable infusion-pump reservoirs, fluorouracil, cytarabine, and doxorubicin hydrochloride were each stable for at least one week at temperatures up to 35 degrees C. Cytarabine and doxorubicin hydrochloride showed decreasing stability at longer storage times and higher temperatures. PMID:1598939

Rochard, E B; Barthès, D M; Courtois, P Y

1992-03-01

355

Preparation and the in vitro evaluation of nanoemulsion system for the transdermal delivery of granisetron hydrochloride.  

PubMed

The objective of this study was to develop and evaluate nanoemulsion system for transdermal delivery of granisetron hydrochloride. Pseudo-ternary phase diagram was constructed to ascertain the concentration range of components of nanoemulsion composed of isopropyl myristate (IPM) as an oil phase, tween 85 as surfactant, ethanol as cosurfactant, water as aqueous phase. The effects of the content of IPM as an oil phase and n-methyl pyrrolidone (NMP) as transdermal enhancer on rat skin permeation of granisetron hydrochloride nanoemulsion were studied in vitro. The results showed that the mean particle size of nanoemulsion ranged from 50.4+/-1.5 to 82.4+/-0.9 nm with homogeneous size distribution. The resulted optimum formulation composed of 2.5% granisetron hydrochloride, 4% IPM, 40% tween 85/ethanol (1 : 1) and 10% NMP showed that the skin permeation rate was the highest (85.39+/-2.90 microg/cm(2)/h) and enhancement of drug permeability was 4.1-fold for transdermal delivery of granisetron hydrochloridein comparison with the control group (20% of tween 85 and 20% of ethanol micelle solution containing 2.5% of granisetron hydrochloride without IPM), and cumulative permeation amount was the highest (891.8+/-2.86 microg/cm(2)) with the shortest lag time (0.11+/-0.02 h) and was stable for at least 12 months. Therefore, the nanoemulsion system developed in this study offers a promising vehicle for the transdermal delivery system of granisetron hydrochloride, which may be as effective as oral or intravenous dosage forms and avoid some difficulties associated with these dosage forms. PMID:20686252

Zheng, Wen-wu; Zhao, Ling; Wei, Yu-meng; Ye, Yun; Xiao, Shun-han

2010-08-01

356

Is planarity of pyridin-2-yl- and pyrazin-2-yl-formamide thiosemicarbazones related to their tuberculostatic activity? X-ray structures of two pyrazine-2-carboxamide-N?-carbonothioyl-hydrazones  

NASA Astrophysics Data System (ADS)

Crystal structures of two title compounds and several their relatives known earlier reveal conservative and characteristic features, which may be related to their tuberculostatic activity. The molecules are predominantly planar due to conjugation through five successive bonds in the zwitterionic fragment S- C(sp2) N NH+ C(sp2) NH2 and intramolecular hydrogen bonds, which prevent rotation of the adjacent pyrazine (or pyridine) ring. It has been suggested that in spatial sense such planar molecules resemble acridines intercalating with nucleic acids and that similar process may be responsible for tuberculostatic activity of the title pyrazine-2-carboxamide-N?-carbonothioyl-hydrazones.

Olczak, Andrzej; G?ówka, Marek L.; Go?ka, Jolanta; Szczesio, Ma?gorzata; Bojarska, Joanna; Koz?owska, Krystyna; Foks, Henryk; Orlewska, Czes?awa

2007-03-01

357

A study on the electronic effect of para substituents in the aryloxy ring of the hydrazone ligands on the vanadium centre in a family of mixed-ligand [V V O(ONO)(OO)] complexes  

Microsoft Academic Search

[VIVO(acac)2] reacts with the methanolic solutions of tridentate dibasic ONO donor hydrazone ligands derived from the condensation of\\u000a benzoyl hydrazine with either 2-hydroxyacetophenone (H2L1) or its para-substituted derivatives (H2L2–4) (general abbreviation H2L), in the presence of vanillin (Hvan) in equimolar ratio under aerobic conditions generating the mixed-ligand oxovanadium(V)\\u000a complexes of the type [VVO(L)(van)], (1)–(4) in good yield. All the complexes

Tapas Ghosh; Bipul Mondal; Ranjan Patra

2007-01-01

358

Guidance for the Reregistration of Pesticide Products Containing Oxytetracycline, Oxytetracycline Hydrochloride and Oxytetracycline Calcium Complex as the Active Ingredient.  

National Technical Information Service (NTIS)

The document contains information regarding the registration of pesticide products containing oxytetracycline, oxytetracycline hydrochloride or oxytetracycline calcium complex. The document includes how to register under a registration standard, regulator...

1988-01-01

359

Curly-curly, loop-loop: homoleptic metal(ii) complexes of pyridinecarbaldehyde 4'-(2,2':6',2''-terpyridyl)hydrazones and their coordination polymers.  

PubMed

The ligands 4-, 3- and 2-pyridinecarbaldehyde 4'-(2,2':6',2''-terpyridyl)hydrazone (, and ) have been prepared and characterized. In the homoleptic iron(ii) and ruthenium(ii) complexes, the nitrogen donor atoms of the pendant pyridine rings subtend an obtuse angle ( approximately 155 degrees ) at the metal centre, thus providing an expanded ligand, which can be used for the assembly one-dimensional coordination polymers with an undulating backbone. Protonation of the pendant pyridine rings in [FeL(2)](2+) (L = , , ) or [RuL(2)](2+) (L = , ) leads to a colour change from purple to blue, or red to pink, respectively, as the MLCT band shifts to a lower energy. The structural data for [Fe(H)()][PF(6)](3).3.5MeCN.2.5H(2)O (where [H](+) is the monoprotonated ligand) show that the [Fe(H)()](3+) cations form one-dimensional chains supported by N(py)HN(py) hydrogen bonds and that the undulating chains pack to give a porous material, with channels that accommodate the anions and solvent molecules. A single-crystal X-ray diffraction determination of {[Fe(NCS)(2)(Ru()(2))(2)][Fe(2)(NCS)(6)(OEt)(2)(EtOH)(2)][NCS](2).4EtOH.H(2)O}(n) reveals that pairs of [Ru()(2)](2+) cations connect {Fe(NCS)(2)} units to give a one-dimensional polymer comprising of linked metallamacrocycles. PMID:19153622

Beves, Jonathon E; Constable, Edwin C; Housecroft, Catherine E; Kepert, Cameron J; Neuburger, Markus; Price, David J; Schaffner, Silvia; Zampese, Jennifer A

2008-10-16

360

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.

361

Synthesis and Quantitative Structure-Activity Relationship (QSAR) Study of Novel N-Arylsulfonyl-3-acylindole Arylcarbonyl Hydrazone Derivatives as Nematicidal Agents.  

PubMed

In continuation of our program aimed at the discovery and development of natural-product-based pesticidal agents, 54 novel N-arylsulfonyl-3-acylindole arylcarbonyl hydrazone derivatives were prepared, and their structures were well characterized by (1)H NMR, (13)C NMR, HRMS, ESI-MS, and mp. Their nematicidal activity was evaluated against that of the pine wood nematode, Bursaphelenchus xylophilus in vivo. Among all of the derivatives, especially V-12 and V-39 displayed the best promising nematicidal activity with LC50 values of 1.0969 and 1.2632 mg/L, respectively. This suggested that introduction of R(1) and R(2) together as the electron-withdrawing substituents, R(3) as the methyl group, and R(4) as the phenyl with the electron-donating substituents could be taken into account for further preparation of these kinds of compounds as nematicidal agents. Six selected descriptors are a WHIM descriptor (E1m), two GETAWAY descriptors (R1m+ and R3m+), a Burden eigenvalues descriptor (BEHm8), and two edge-adjacency index descriptors (EEig05x and EEig13d). Quantitative structure-activity relationship (QSAR) studies demonstrated that the structural factors, such as molecular mass (a negative correlation with the bioactivity) and molecular polarity (a positive correlation with bioactivity), are likely to govern the nematicidal activities of these compounds. For this model, the correlation coefficient (R(2)training set), the leave-one-out cross-validation correlation coefficient (Q(2)LOO), and the 7-fold cross-validation correlation coefficient (Q(2)7-fold) were 0.791, 0.701, and 0.715, respectively. The external cross-validation correlation coefficient (Q(2)ext) and the root-mean-square error for the test set (RMSEtest set) were 0.774 and 3.412, respectively. This study will pave the way for future design, structural modification, and development of indole derivatives as nematicidal agents. PMID:23738496

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

2013-06-01

362

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

363

Hydrazone-based ligands for micro-solid phase extraction-high performance liquid chromatographic determination of biogenic amines in orange juice.  

PubMed

Eight hydrazone-based ligands were synthesized, trapped in a silica sol-gel matrix, and were subsequently used in the micro-solid phase extraction (?-SPE) of biogenic amines (BAs). The BAs investigated were tryptamine, phenylethylamine, putrescine, histamine, tyramine and spermidine. Prior to the extraction, dansyl chloride was added to the samples which were heated to 70°C for 10 min. The samples were extracted with ?-SPE, after which analytes were desorbed using acetonitrile via ultrasonication. The extracts were analysed by high performance liquid chromatography (HPLC) with ultraviolet detection. Of the eight ligands investigated as sorbents, benzophenone 2,4-dinitrophenylhydrazone was found to be the most promising. The enhanced ?-? interaction between the analytes and the ligand facilitated the adsorption process. Under the most suitable extraction conditions, the method demonstrated good linearity with correlation coefficient of more than 0.985 over a concentration range of 1-50 ?g L(-1). Satisfactory repeatability with relative standard deviations of 7.43-11.30% (n=3) were obtained. Detection limits ranged from 3.8 to 31.3 ng L(-1). The ?-SPE method exhibited lower recoveries (71.5-87.4%) when compared to the solid phase extraction technique (79.7-95.0%), but enrichment factors of 94-460 were obtained. The proposed ?-SPE-HPLC method was applied to the determination of BAs in orange juice purchased from local supermarkets, with satisfactory results. The orange juices were characterized by the presence of relatively high levels of putrescine (range, 550-2210 ?g L(-1)) but tryptamine and phenylethylamine were not detected in any of the tested samples. PMID:21621782

Basheer, Chanbasha; Wong, Weishan; Makahleh, Ahmad; Tameem, Abdassalam Abdelhafiz; Salhin, Abdussalam; Saad, Bahruddin; Lee, Hian Kee

2011-05-06

364

Oxygen isotope ratio measurements on carbon dioxide generated by reaction of microliter quantities of biological fluids with guanidine hydrochloride  

Microsoft Academic Search

Guanidine hydrochloride was used to convert water in biological fluids to carbon dioxide for oxygen isotope ratio measurements. Five 10-..mu..L aliquots each of five different saliva, urine, plasma, and human milk samples were allowed to react with 100 mg of guanidine hydrochloride at 260°C to produce ammonia and carbon dioxide. Ammonia was removed with 100% phosphoric acid and carbon dioxide

William W. Wong; Lucinda S. Lee; Peter D. Klein

1987-01-01

365

Stability-Indicating Method for the Determination of Hydrochlorothiazide, Benzydamine Hydrochloride and Clonazepam in the Presence of Their Degradation Products  

Microsoft Academic Search

Spectrophotometric, colorimetric and densitometric methods for the determination of hydrochlorothiazide, benzydamine hydrochloride and clonazepam in the presence of their degradation products are described. Hydrochlorothiazide was determined in the presence of its degradation products methoxyhydrothiazide, hydroxyhydrothiazide and 5-chloro-2,4-disulfonamidoaniline applying the first and second derivative spectrophotometer at 278.8 nm and 254.4 nm, respectively, while benzydamine hydrochloride was determined in the presence of

L. I. Bebawy; N. El Kousy

1997-01-01

366

Spectrofluorimetric method for determination of duloxetine hydrochloride in bulk and pharmaceutical dosage forms.  

PubMed

A simple accurate, sensitive and reproducible spectrofluorimetric method was developed for the analysis of duloxetine hydrochloride in pure and pharmaceutical dosage form. Duloxetine hydrochloride showed strong native fluorescence in 0.05 M acetic acid having excitation at 225 nm and emission at 340 nm. Effect of different solvents were thoroughly investigated. The calibration graph was linear in the range from 0.020 to 0.400 mug/ml. The proposed method was statistically validated and successfully applied for analysis of capsule dosage forms. The limit of detection and limit of quantification were found to be 0.003 mug/ml and 0.010 mug/ml, respectively. The percentage recovery was found to be in the range of 98.71% to 99.17%. PMID:20046780

Prabu, S L; Shahnawaz, S; Kumar, C Dinesh; Shirwaikar, A

367

Spectrofluorimetric Method for Determination of Duloxetine Hydrochloride in Bulk and Pharmaceutical Dosage Forms  

PubMed Central

A simple accurate, sensitive and reproducible spectrofluorimetric method was developed for the analysis of duloxetine hydrochloride in pure and pharmaceutical dosage form. Duloxetine hydrochloride showed strong native fluorescence in 0.05 M acetic acid having excitation at 225 nm and emission at 340 nm. Effect of different solvents were thoroughly investigated. The calibration graph was linear in the range from 0.020 to 0.400 ?g/ml. The proposed method was statistically validated and successfully applied for analysis of capsule dosage forms. The limit of detection and limit of quantification were found to be 0.003 ?g/ml and 0.010 ?g/ml, respectively. The percentage recovery was found to be in the range of 98.71% to 99.17%.

Prabu, S. L.; Shahnawaz, S.; Kumar, C. Dinesh; Shirwaikar, A.

2008-01-01

368

Liquid chromatographic determinations of meta-chlorobenzoic acid in bupropion hydrochloride  

PubMed Central

A simple, sensitive method for the determination of meta-chlorobenzoic acid in bupropion hydrochloride is described. Chromatographic separation of m-chlorobenzoic acid is achieved using a mobile phase consisting of n-hexane and ethanol (1000:50, v/v) at a flow rate of 1.0 ml/min on a Chiralpak ADH (250 × 4.6 mm). Absorbance is monitored at 235 nm. The method is linear for m-chlorobenzoic acid over concentration range of LOQ, 5.0 ?g/ml to 15.0 ?g/ml for m-chlorobenzoic acid with correlation coefficient greater than 0.99. This method is more selective and accurate than United States Pharmacopoeia method for the determination of m-chlorobenzoic acid in bupropion hydrochloride.

Sinha, Sukumar; Parashar, Vikas; Reddy, K. Swamy; Khan, Mohammad A.; Haque, S. K. Manirul

2013-01-01

369

Optimization and validation of a CZE method for rufloxacin hydrochloride determination in coated tablets.  

PubMed

A simple and rapid capillary electrophoresis method with UV detection was developed and validated for the determination of rufloxacin hydrochloride in coated tablets. An experimental design strategy (Doehlert design and desirability function) allowed the analytical parameters to be simultaneously optimized in order to determine rufloxacin hydrochloride with high peak area/migration time ratio, good efficiency and short analysis time. Optimized analyses were run using boric acid 0.10 M adjusted to pH 8.8 as BGE and setting voltage and temperature at 18 kV and 27 degrees C, respectively. Pefloxacin mesylate was used as internal standard and run time was about three minutes. The method was validated for the drug substance and the drug product according to the ICH3 guidelines. Robustness was tested by experimental design using an eight-run Plackett-Burman matrix. PMID:12049980

Furlanetto, S; Orlandini, S; Porta, E La; Coran, S; Pinzauti, S

2002-06-15

370

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

371

Inhibition of in vitro proliferative responses of human lymphocytes by rimantadine hydrochloride.  

PubMed Central

Rimantadine hydrochloride (alpha-methyl-1-adamantanemethylamine hydrochloride) inhibits the in vitro proliferative response of human peripheral blood lymphocytes to mitogenic and antigenic stimulation. Addition of drug (25 micrograms/ml) at the initiation of 5-day cultures suppressed the responses to phytohemagglutinin, pokeweed mitogen, and concanavalin A by 25, 65, and 90%, respectively. Similarly, responses to streptokinase-streptodornase, tetanus toxoid, and A2/Aichi influenza vaccine were significantly inhibited at concentrations as low as 10 micrograms of rimantadine per ml. Viability studies on 5-day cultures using trypan blue exclusion showed no significant difference between drug-treated and untreated controls. Furthermore, addition of drug on day 3 of 8-day cultures, at a time when the majority of cells had undergone blastogenesis, greatly suppressed the responses to these mitogens. These studies suggest that, in addition to its antiviral action, rimantadine interferes with the generation of cellular immune responses.

Koff, W C; Peavy, D L; Knight, V

1979-01-01

372

Stability of lidocaine hydrochloride in 5% dextrose injection in plastic bags  

SciTech Connect

The stability of lidocaine injection mixed with 5% dextrose injection and refrigerated or stored at room temperature was studied. Lidocaine injection was added to 5% dextrose injection to provide a lidocaine hydrochloride concentration of 4 mg/ml. Samples were assayed for lidocaine and its degradation product, 2,6-dimethylaniline, after 30, 60, and 120 days of storage at room temperature (30 degrees C) and refrigerated temperature (4 degrees C). The analysis was by a stability-indicating HPLC method. Degradation product 2,6-dimethylaniline was not detected at any assay time at either temperature. No statistically significant loss of lidocaine occurred at either temperature. Lidocaine hydrochloride injection is chemically stable for up to 120 days at either 30 degrees C or 4 degrees C when mixed with 5% dextrose injection in plastic infusion bags.

Smith, F.M.; Nuessle, N.O.

1981-11-01

373

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.

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

2013-01-01

374

High-performance liquid chromatographic determination of flavoxate hydrochloride and its hydrolysis product.  

PubMed

Liquid chromatographic method was presented for the determination of flavoxate hydrochloride (FX) and its hydrolysis product. The method was based on high-performance liquid chromatographic (HPLC) separation of FX from its hydrolysis product on CN column using a mobile phase consisting of acetonitrile-12 mM ammonium acetate (45:55, vol/vol, pH 4.0) with UV detection at 220 nm and flow rate of 1.5 mL min(-1). The proposed HPLC method for the determination of FX was utilized to investigate the kinetics of acidic hydrolytic process at different temperatures and to calculate its activation energy. In addition, the proposed HPLC method was used for pH-rate profile study of hydrolysis of FX in Britton-Robinson buffer solutions. The 3-methylflavone-8-carboxylic acid ethyl ester, as impurity of flavoxate hydrochloride, can be separated by the proposed HPLC method. PMID:18850365

el-Gindy, Alaa; Abdel-Salam, Randa A; Sallam, Shehab

2008-12-01

375

Quantitative Estimation of Itopride Hydrochloride and Rabeprazole Sodium from Capsule Formulation  

PubMed Central

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 C18 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.

Pillai, S.; Singhvi, I.

2008-01-01

376

Preparation and Characterisation of Mucoadhesive Nasal Gel of Venlafaxine Hydrochloride for Treatment of Anxiety Disorders  

PubMed Central

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.

Basu, Shyamoshree; Maity, S.

2012-01-01

377

Gastroretentive drug delivery system of ranitidine hydrochloride: Formulation and in vitro evaluation  

Microsoft Academic Search

The purpose of this research was to prepare a gastroretentive drug delivery system of ranitidine hydrochloride. Guar gum,\\u000a xanthan gum, and hydroxypropyl methylcellulose were evaluated for gel-forming properties. Sodium bicarbonate was incorporated\\u000a as a gas-generating agent. The effects of citric acid and stearic acid on drug release profile and floating properties were\\u000a investigated. The addition of stearic acid reduces the

Brijesh S. Dave; Avani F. Amin; Madhabhai M. Patel

2004-01-01

378

High Performance Liquid Chromatographic Assay of Verapamil Hydrochloride in Dosage Formsk  

Microsoft Academic Search

A stability indicating high-performance liquid chromatographic (HPLC) method for determining verapamil hydrochloride in dosage forms is described. The assay affords baseline separation of the drug from its synthesis impurities and from photolytic degradation products, as well as from formulation excipients. The drug was extracted in 0.05 N hydrochloric acid, chromatographed on a C18 reverse-phase column, eluted with methanol-water-acetic acid-triethylamine (55:44:1:0.1)

Dimitri C. Tsilifonis; Karen Wilk; Robert Reisch Jr; Robert E. Daly

1985-01-01

379

Coenzyme Q10 and remacemide hydrochloride ameliorate motor deficits in a Huntington's disease transgenic mouse model  

Microsoft Academic Search

Huntington's disease (HD) is a progressive inherited neurodegenerative disorder, for which there is no effective therapy. The CARE-HD study, recently published, evaluated the ability of a combination of coenzyme Q10 (CoQ10) and remacemide hydrochloride (R) to ameliorate symptoms, which might arise from glutamate-mediated excitotoxicity and abnormalities in mitochondrial energy production. In this study, we examined the efficacy of CoQ10\\/R therapy

Gabriele Schilling; Michael L Coonfield; Christopher A Ross; David R Borchelt

2001-01-01

380

Scale-up effects on dissolution and bioavailability of propranolol hydrochloride and metoprolol tartrate tablet formulations  

Microsoft Academic Search

1bstract  This study evaluated the effects of batch size on the in vitro dissolution and the in vivo bioavailability of immediate release\\u000a formulations of propranolol hydrochloride and metoprolol tartrate. The formulations were manufactured as small and large batches\\u000a (6 kg and 60 kg for propranolol; 14 kg and 66 kg for metoprolol), and dissolution was performed using USP Apparatus I at

Natalie D. Eddington; Guvinder Singh Rekhi; Larry J. Lesko; Larry L. Augsburger

2000-01-01

381

Formulation, evaluation, and comparison of bilayered and multilayered mucoadhesive buccal devices of propranolol hydrochloride  

Microsoft Academic Search

The purpose of this research work was to establish mucoadhesive buccal devices of propranolol hydrochloride (PRH) in the forms\\u000a of bilayered and multilayered tablets. The tablets were prepared using sodium carboxymethylcellulose (SCMC) and Carbopol-934\\u000a (CP) as bioadhesive polymers to impart mucoadhesion and ethyl cellulose (EC) to act as an impermeable backing layer. Buccal\\u000a devices were evaluated by different parameters such

Vishnu M. Patel; Bhupendra G. Prajapati; Madhabhai M. Patel

2007-01-01

382

Design and Optimization of Mefloquine Hydrochloride Microparticles for Bitter Taste Masking  

Microsoft Academic Search

The objective of the present investigation was to reduce the bitterness with improved dissolution, in acidic medium (pH 1.2),\\u000a of mefloquine hydrochloride (MFL). Microparticles were prepared by coacervation method using Eudragit E (EE) as polymer and\\u000a sodium hydroxide as precipitant. A 32 full factorial design was used for optimization wherein the drug concentration (A) and polymer concentration (B) were selected\\u000a as

Punit P. Shah; Rajashree C. Mashru; Yogesh M. Rane; Arti Thakkar

2008-01-01

383

Supramolecular interaction of ethylenediamine linked ?-cyclodextrin dimer and berberine hydrochloride by spectrofluorimetry and its analytical application  

Microsoft Academic Search

The supramolecular interaction of ?-cyclodextrin dimer with berberine hydrochloride was studied in aqueous KH2PO4–H3PO4 buffer solution of pH 2.00 at room temperature by spectrofluorimetry. The apparent association constant of the complex was 1.53×104Lmol?1. Based on the significant enhancement of fluorescence intensity of supramolecular sandwich complexes, a spectrofluorimetric method with high sensitivity and selectivity was developed for the determination of berberine

Fang Liu; Hui-ling Liang; Ke-hua Xu; Li-li Tong; Bo Tang

2007-01-01

384

Effect of hydrophilic polymers on buccoadhesive eudragit patches of propranolol hydrochloride using factorial design  

Microsoft Academic Search

The purpose of this study was to develop formulations and systematically evaluate in vitro performances of buccoadhesive patches\\u000a of propranolol hydrochloride using the hydrophobic polymer Eudragit L-100 as the base matrix. The hydrophilic polymers Carbopol\\u000a 934 and polyvinyl pyrrolidone (PVP) K30 were incorporated into the Eudragit patches, to provide the patches with bioadhesive\\u000a properties and to modify the rate of

Vishnu M. Patel; Bhupendra G. Prajapati; Madhabhai M. Patel

2007-01-01

385

Properties of lipophilic matrix tablets containing phenylpropanolamine hydrochloride prepared by hot-melt extrusion  

Microsoft Academic Search

The objective of the present study was to investigate the influence of formulation factors on the physical properties of hot-melt extruded granules and compressed tablets containing wax as a thermal binder\\/retarding agent, and to compare the properties of granules and tablets with those prepared by a high-shear melt granulation (MG) method. Powder blends containing phenylpropanolamine hydrochloride, Precirol® and various excipients

Jiping Liu; Feng Zhang; James W McGinity

2001-01-01

386

DSC study of cold and heat denaturation processes of ?-lactoglobulin A with guanidine hydrochloride  

Microsoft Academic Search

The cold and heat denaturations of bovine P-lactoglobulin A ((?-lg A) has been studied in solutions of guanidine hydrochloride\\u000a (GuHCI) by differential scanning calorimetry (DSC). The experimental results are presented and discussed. It is shown that\\u000a the number of protons bound by the monomeric molecules of ?-lg A was unchanged before and after its heat denaturation below\\u000a pH 3, and

Bangning Wang; Fu Tan

1997-01-01

387

Impact of polyhexamethylene guanidine hydrochloride on the process of coagulation treatment of river waters  

Microsoft Academic Search

The paper has investigated flocculation capacity of polyhexamethylene guanidine hydrochloride during joint treatment with\\u000a aluminum sulfate of the Dnieper and Desna River water in the spring period. It has been shown that additives 1–5 mg\\/dm3 of the matter under study during coagulation treatment of the river waters improves the process of their clarification, increases\\u000a the filtrate quality in terms of

V. V. Goncharuk; V. F. Vakulenko; Yu. O. Shvadchina; L. M. Oleinik; T. N. Sitnichenko

2008-01-01

388

Suppression of respiratory burst of polymorphonuclear leukocytes by Azelastine hydrochloride (Azeptin)  

Microsoft Academic Search

The inhibitory action of azelastine hydrochloride (Azeptin) on the respiratory burst in peripheral polymorphonuclear leukocytes (PMN) and pulmonary alveolar macrophages (PAM) has been studied. Azeptin in vitro suppressed chemiluminescence and superoxide (O2-) generation by human PMN in a dose-and time-dependent manner. Phorbol myristyl acetate (PMA) and formyl-methionyl-leucyl-phenylalanine (FMLP)-induced O2-generation were strongly suppressed by 10-6M and 10-5M Azeptin, respectively. PMN and

E. Ueta; T. Osaki; N. Kawasaki; Y. Nomura

1994-01-01

389

Preparation and Evaluation of Diltiazem Hydrochloride Diffusion-Controlled Transdermal Delivery System  

Microsoft Academic Search

The objective was to investigate the suitable polymeric films for the development of diltiazem hydrochloride (diltiazem HCl)\\u000a transdermal drug delivery systems. Hydroxypropyl methylcellulose (HPMC) and ethylcellulose (EC) were used as hydrophilic and\\u000a hydrophobic film formers, respectively. Effects of HPMC\\/EC ratios and plasticizers on mechanical properties of free films\\u000a were studied. Effects of HPMC\\/EC ratios on moisture uptake, in vitro release

Ekapol Limpongsa; Kraisri Umprayn

2008-01-01

390

Single-step recovery of ephedrine hydrochloride from raw materials using expanded bed adsorption.  

PubMed

Expanded bed adsorption, using a cation resin 001 x 7 Styrene-DVB, was used to recover and purify ephedrine hydrochloride from a powdered herb. The axial liquid-phase dispersion coefficient was about 10(-5) m(2) s(-1) and the recovery yield and purification reached 86% and 22, respectively. Compared with using conventional extraction with dimethylbenzene, this method is safer and also more efficient. PMID:15289679

Chen, Wei-Dong; Wang, Yan-Dong; Zha, Li-Hang; Ma, Guang-Hui; Su, Zhi-Guo

2004-08-01

391

Conformations of poly(allylamine hydrochloride) in electrolyte solutions: Experimental measurements and theoretical modeling  

Microsoft Academic Search

In this work, the conformations of poly(allylamine hydrochloride) (PAH) molecules in electrolyte solutions were determined experimentally for various pH and ionic strength by dynamic light scattering (DLS), microelectrophoresis and dynamic viscosity measurements. The molecular weight of the polymer exhibited a narrow size distribution and the average value of 15kDa. Using the diffusion coefficient data obtained by DLS, the hydrodynamic radius

B. Jachimska; T. Jasi?ski; P. Warszy?ski; Z. Adamczyk

2010-01-01

392

Development of Gelucire 43\\/01 Beads of Metformin Hydrochloride for Floating Delivery  

Microsoft Academic Search

The objective of this study was to prepare and characterize beads of Gelucire 43\\/01 for floating delivery of metformin hydrochloride\\u000a (MH). The beads were evaluated for particle size, surface morphology, percent drug entrapment, percent yield, differential\\u000a scanning calorimetry (DSC), in vitro floating ability, and in vitro drug release. Aging effect on storage was evaluated using hot stage microscopy (HSM), DSC,

Sunil K. Jain; Anuj Gupta

2009-01-01

393

The genetic toxicology of methylphenidate hydrochloride in non-human primates  

Microsoft Academic Search

The studies presented in this work were designed to evaluate the genetic toxicity of methylphenidate hydrochloride (MPH) in non-human primates (NHP) using a long-term, chronic dosing regimen. Thus, approximately two-year old, male rhesus monkeys of Indian origin were orally exposed to MPH diluted in the electrolyte replenisher, Prang®, five days per week over a 20-month period. There were 10 animals

Suzanne M. Morris; Vasily N. Dobrovolsky; Joseph G. Shaddock; Roberta A. Mittelstaedt; Michelle E. Bishop; Mugimane G. Manjanatha; Sharon D. Shelton; Daniel R. Doerge; Nathan C. Twaddle; James J. Chen; Chien-Ju Lin; Merle G. Paule; William Slikker; Charlotte E. Hotchkiss; Dayton Petibone; James D. Tucker; Donald R. Mattison

2009-01-01

394

Acrylamide Quenching of apo- and holo-?-Lactalbumin in Guanidine Hydrochloride  

Microsoft Academic Search

We have examined the fluorescence properties and acrylamide quenching of calcium-loaded (holo) and calcium-depleted (apo) ?-lactalbumin (?-LA) as a function of guanidine hydrochloride (GDN\\/HCl) concentration. The spectral changes accompanying increasing GDN\\/HCl are consistent with protein unfolding and a release of internal fluorescence quenching, which occurs among the three tryptophan residues located in the region of the so-called “tertiary fold.” Values

Richard M. France; Steven H. Grossman

2000-01-01

395

Quinacrine Hydrochloride Pellets: Preliminary , Data on a Nonsurgical Method of Female Sterilization  

Microsoft Academic Search

Zipper J, Cole Goldsmith A, Wheeler R,(Depts de Fisiologia y Escuela deUniversidad de Chile, Santiago, y Ginecologia,Hospital Sotero Rio, Puente Chile, and International Fertility Research Program, Research Triangle Park,NC, USA). hydrochloride pellets: preliminary data on a nonsurgical method sterilization.J Obstet 18: 275-279, 1980The efficacy of transcervical insertions of quinacrine hydrochloridepellets to produce tubal occlusion has beenuated in a study of

Jaime Lynda Painter Cole

1980-01-01

396

Formulation and Evaluation of Bilayer Tablet of Metoclopramide Hydrochloride and Ibuprofen  

Microsoft Academic Search

The aim of this study was to prepare bi-layer tablet of Metoclopramide Hydrochloride (MTH) and Ibuprofen (IB) for the effective\\u000a treatment of migraine. MTH and IB were formulated as immediate and sustained release layer respectively. MTH was formulated\\u000a as immediate release layer by using various disintegrants like Ac-Di-Sol, Polyplasdone XL, Explotab, Agar and Gellan Gum.\\u000a Treated form of gellan gum

Bhavesh Shiyani; Surendra Gattani; Sanjay Surana

2008-01-01

397

Redispersion of dried gold nanorods in the presence of 6-amino-1-hexanethiol hydrochloride  

Microsoft Academic Search

Aggregates of phosphatidylcholine-passivated gold nanorods were prepared by the addition of hydrochloric acid in the presence\\u000a of 6-amino-1-hexanethiol hydrochloride (AHT). The aggregates dried in vacuum formed a solid film showing a metallic gold color.\\u000a In spite of the absence of the stable surface-wrapping agents, such as balky polymer or thiol-molecules that form stable self-organized\\u000a films on a gold surface, the

Kanako Honda; Hirofumi Kawazumi; Naotoshi Nakashima; Yasuro Niidome

398

EFFECTS OF DRC1339 (3-CHLORO-4METHYLANILINE HYDROCHLORIDE) AVICIDE ON PHEASANT REPRODUCTION  

Microsoft Academic Search

We performed a laboratory experiment to investigate the effects of 2 levels of 3 repeated dosages of compound DRC- 1339 (3-chloro-4-methylaniline hydrochloride) on ring-necked pheasants (Phasianus colchicus). Twelve females and 4 males were administered 3 doses of 4 mg each (HIGH), a second group received 3 doses of 2 mg each (LOW), and a third group served as controls. Doses

DANIEL E. HUBBARD; REGG D. NEIGER

399

Intra-Arterial Infusion of Fasudil Hydrochloride for Treating Vasospasm Following Subarachnoid Haemorrhage  

Microsoft Academic Search

Summary  ?In this pilot study we treated cerebral vasospasm in patients with subarachnoid haemorrhage to assess intra-arterial fasudil\\u000a hydrochloride. We analysed effects of intra-arterial infusion on angiographically evident cerebral vasospasm in 10 patients\\u000a including 3 with symptoms of vasospasm. Over 10 to 30 min 15 to 60 mg was administered via the proximal internal carotid artery\\u000a or vertebral artery following standard

E. Tachibana; T. Harada; M. Shibuya; K. Saito; M. Takayasu; Y. Suzuki; J. Yoshida

1999-01-01

400

HPLC and chemometric-assisted spectrophotometric methods for simultaneous determination of atenolol, amiloride hydrochloride and chlorthalidone  

Microsoft Academic Search

Three methods are presented for the simultaneous determination of atenolol (AT), amiloride hydrochloride (AM) and chlorthalidone (CD). The high performance liquid chromatographic (HPLC) method depends on the separation of each drug on a reversed phase, RP 18 column. Elution was carried out with a mobile phase consisting of acetonitrile -5mM heptansulphonic acid sodium salt (20:80, v\\/v, pH 4.4). Quantitation was achieved

Alaa El-Gindy; Samy Emara; Ahmed Mostafa

2005-01-01

401

Simultaneous Determination of Metformin Hydrochloride, Cyanoguanidine and Melamine in Tablets by Mixed-Mode HILIC  

Microsoft Academic Search

A simple and specific hydrophilic interaction liquid chromatography (HILIC) procedure for the quantification of metformin\\u000a hydrochloride (MFH) and its impurities in bulk pharmaceuticals and finished dosage forms has been developed. The method is\\u000a based on hydrophilic interaction of the analytes with silica. The influence of the weaker solvent, acetonitrile, pH and the\\u000a nature and ionic strength of the buffer was

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

2008-01-01

402

Determination of the Enantiomers of Tamsulosin Hydrochloride and its Synthetic Intermediates by Chiral Liquid Chromatography  

Microsoft Academic Search

A chiral liquid chromatographic method is described for the determination of the enantiomers of tamsulosin hydrochloride and its synthetic intermediates. Enantioseparation was achieved on a Chiralcel OD-R column (250 mm × 4.6 mm, 10 µm) using a mobile phase consisting of a mixture of 0.5 mol L -1 sodium perchlorate and acetonitrile (80:20, v\\/v, pH 4.0). The flow rate was

Meiling Qi; Peng Wang; Ruihua Cong

2004-01-01

403

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

404

Taste masking and molecular properties of metformin hydrochloride-indion 234 complexes.  

PubMed

Metformin hydrochloride is an oral antidiabetic biguinide agent, used in the management of non-insulin-dependent (type-2) diabetes mellitus. The purpose of present work was to formulate tasteless complexes of metformin hydrochloride with indion 234 and to evaluate molecular properties of drug complexes. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, mode of mixing, ratio of drug to resin, and temperature. Drug resin complexes (DRC) were evaluated for taste masking and characterized by x-ray diffraction study and infrared spectroscopy. Metformin hydrochloride release from DRC is obtained at salivary and gastric pH and in the presence of electrolytes. The efficient drug loading was evident in batch process using activated indion 234 with a pH of 3.5 and drug-resin ratio of 1:1.2, while temperature enhances the complexation process. Infrared spectroscopy revealed complexation of -NH (drug) with indion 234. DRC are amorphous in nature. Drug release from DRC in salivary pH was insufficient to impart bitter taste. Volunteers rated the complex as tasteless and agreeable. Complete drug release was observed at gastric pH in 3 h. The drug release was accelerated in the presence of electrolytes. Indion 234 is inexpensive, and the simple technique is effective for bitterness masking of metformin. PMID:21731355

Bhoyar, Pk; Amgaonkar, Ym

2011-04-01

405

Taste Masking and Molecular Properties of Metformin Hydrochloride-Indion 234 Complexes  

PubMed Central

Metformin hydrochloride is an oral antidiabetic biguinide agent, used in the management of non-insulin-dependent (type-2) diabetes mellitus. The purpose of present work was to formulate tasteless complexes of metformin hydrochloride with indion 234 and to evaluate molecular properties of drug complexes. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, mode of mixing, ratio of drug to resin, and temperature. Drug resin complexes (DRC) were evaluated for taste masking and characterized by x-ray diffraction study and infrared spectroscopy. Metformin hydrochloride release from DRC is obtained at salivary and gastric pH and in the presence of electrolytes. The efficient drug loading was evident in batch process using activated indion 234 with a pH of 3.5 and drug-resin ratio of 1:1.2, while temperature enhances the complexation process. Infrared spectroscopy revealed complexation of –NH (drug) with indion 234. DRC are amorphous in nature. Drug release from DRC in salivary pH was insufficient to impart bitter taste. Volunteers rated the complex as tasteless and agreeable. Complete drug release was observed at gastric pH in 3 h. The drug release was accelerated in the presence of electrolytes. Indion 234 is inexpensive, and the simple technique is effective for bitterness masking of metformin.

Bhoyar, PK; Amgaonkar, YM

2011-01-01

406

HPLC and chemometric methods for the simultaneous determination of cyproheptadine hydrochloride, multivitamins, and sorbic acid.  

PubMed

Three methods are presented for the simultaneous determination of cyproheptadine hydrochloride (CP), thiamine hydrochloride (B1), riboflavin-5-phosphate sodium dihydrate (B2), nicotinamide (B3), pyridoxine hydrochloride (B6), and sorbic acid (SO). The chromatographic method depends on a high performance liquid chromatographic (HPLC) separation on a reversed-phase, RP 18 column. Elution was carried out with 0.1% methanolic hexane sulphonic acid sodium salt (solvent A) and 0.01 M phosphate buffer containing 0.1% hexane sulphonic acid sodium salt, adjusted to an apparent pH of 2.7 (solvent B). Gradient HPLC was used with the solvent ratio changed from 20:80 to 70:30 (over 9 min), then to 80:20 (over 11 min) for solvent A:B, respectively. Quantitation was achieved with UV detection at 220 and 288 nm based on peak area. The other two chemometric methods applied were principal component regression (PCR) and partial least squares (PLS). These approaches were successfully applied to quantify each drug in the mixture using the information included in the UV absorption spectra of appropriate solutions in the range 250-290 nm with the intervals Deltalambda = 0.4 nm at 100 wavelengths. The chemometric methods do not require any separation step. The three methods were successfully applied to a pharmaceutical formulation and the results were compared with each other. PMID:15193715

el-Gindy, Alaa; el-Yazby, Fawzy; Mostafa, Ahmed; Maher, Moustafa M

2004-06-29

407

The clinical pharmacology of viloxazine hydrochloride--a new anti-depressant of novel chemical structure  

PubMed Central

1 The clinical pharmacological properties of viloxazine hydrochloride (ICI 58,834, Vivalan), a new antidepressant of novel chemical structure, have been investigated in a series of double-blind randomized studies comparing it with placebo and imipramine. Throughout the studies, viloxazine hydrochloride was given in single doses of 100 mg (expressed as base), and imipramine hydrochloride was given in single doses of 50 mg (expressed as salt). 2 The effect of viloxazine upon the following parameters was measured: pulse rate, blood pressure, forced expiratory volume, reaction time, critical flicker frequency, salivary flow, pupil size and palpebral fissure size. In addition, the possible interaction between viloxazine and alcohol was investigated using measurements of reaction time. 3 Both viloxazine and imipramine produced a transient tachycardia, but no consistent effect on blood pressure was seen. Neither drug had any effect upon forced expiratory volume. 4 The differences that emerged between viloxazine and imipramine were that viloxazine depressed critical flicker frequency whereas imipramine did not, and imipramine prolonged reaction time whilst viloxazine did not. Imipramine reduced salivary flow and increased the size of the pupil and palpebral fissure. Viloxazine did neither. 5 Imipramine was shown to potentiate alcohol whereas, at the doses used, viloxazine did not. 6 It is concluded that viloxazine appears to have less anticholinergic and possibly less sympathomimetic properties than imipramine. It is also concluded that viloxazine, unlike imipramine, does not potentiate alcohol.

Bayliss, P. F. C.; Duncan, S. M.

1974-01-01

408

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.

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

2013-01-01

409

Molecular dynamics of the cryomilled base and hydrochloride ziprasidones by means of dielectric spectroscopy.  

PubMed

Cryomilling was applied to obtain amorphous forms of the base ziprasidone and its hydrochloride salt. Complete amorphization of both samples was confirmed by differential scanning calorimetry and X-ray measurements. As it turned out, cryogrinding is very effective way to obtain these drugs in the amorphous state, especially because melting of both ziprazidones accompanies significant chemical decomposition as revealed by ultra performance liquid chromatography examination. Consequently, the glassy state cannot be reached in conventional way, that is, by supercooling of melt. Broadband dielectric relaxation measurements were performed on both drugs to describe their molecular dynamics above as well as below their glass transition temperatures (T(g)). We found out that ziprasidone base and its hydrochloride salt differ in T(g) in the same way as it was previously reported for tramadol monohydrate and its hydrochloride. Moreover, our dielectric studies revealed that molecular mobility is not the main factor controlling kinetics of crystallization of both ziprasidones above their T(g) . Below the T(g) relaxation related to water as well as secondary relaxation process originating from the intermolecular interaction (Johari-Goldstein) were identified in the loss spectra of both materials. We have demonstrated that except of local mobility, water is the dominant factor moving both ziprasidones toward recrystallization process. Finally, we have also carried out solubility measurements to show that dissolution rate of the amorphous ziprasidones is much higher with respect to the crystalline samples. PMID:21271564

Kaminski, K; Adrjanowicz, K; Wojnarowska, Z; Grzybowska, K; Hawelek, L; Paluch, M; Zakowiecki, D; Mazgalski, J

2011-01-26

410

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

411

The analysis of methamphetamine hydrochloride by thermal desorption ion mobility spectrometry and SIMPLISMA.  

PubMed

Ion mobility spectrometry (IMS) has been successfully developed to yield an advanced portable instrument. Such instruments may detect trace quantities of regulated substances at the crime scene. The atmospheric ion chemistry that occurs within the instrument may hinder the determination of analytes in real-world samples. The use of temperature programming adds an extra dimension to the data that improves the selectivity of the IMS data when chemometric processing is applied. The SIMPLISMA (SIMPLe-to-use-Interactive Self-Modeling Mixture Analysis) method is demonstrated for modeling variances in IMS data that are introduced from the temperature program. Methamphetamine hydrochloride IMS peaks are obscured by chemical interferences that arise from cigarette smoke residue. Cigarette smoke residue is pervasive at crime scenes. The ability of SIMPLISMA to resolve the analyte peaks that correspond to methamphetamine hydrochloride from interfering cigarette smoke has been demonstrated. A reduced mobility of 1.62 cm2V-1s-1 was observed for a methamphetamine hydrochloride monomer. With the IMS drift tube at room temperature, a second peak was observed at 1.24 cm2V-1s-1, which is consistent with a dimer ion. This peak has not been previously reported. PMID:9987872

Reese, E S; Harrington, P B

1999-01-01

412

Voltammetric behaviour of drotaverine hydrochloride in surfactant media and its enhancement determination in Tween-20.  

PubMed

Simple, sensitive and rapid adsorptive voltammetric behaviour of drotaverine hydrochloride onto the HMDE has been explored and validated in surfactant media by using cyclic, differential pulse and square-wave voltammetry. Addition of Tween-20 to the drotaverine hydrochloride containing electrolyte enhances the reduction current signal. The voltammograms of the drug with Tween-20 in phosphate buffers of pH 2.5-11.0 exhibit a single well defined reduction peak which may be due to the reduction of -CC- group. The cyclic voltammetric studies indicated the reduction of drotaverine hydrochloride at the electrode surface through two electron irreversible step and diffusion-controlled. The peak current showed a linear dependence with the drug concentration over the range 0.8-7.2?gmL(-1). The calculated LOD and LOQ are 1.8 and 6.0ngmL(-1) by SWCAdSV and 8.1 and 27.2ngmL(-1) by DPCAdSV, respectively. The procedure was applied to the assay of the drug in tablet form with mean percentage recoveries of 100.2% with SWCAdSV and 99.7% with DPCAdSV. The validity of the proposed methods was further assessed by applying a standard addition technique. PMID:20889317

Jain, Rajeev; Vikas; Rather, Jahangir Ahmad

2010-09-15

413

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

PubMed Central

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.

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

2011-01-01

414

In vitro interactions of amantadine hydrochloride, R-(-)-deprenyl hydrochloride and valproic acid sodium salt with antifungal agents against filamentous fungal species causing central nervous system infection.  

PubMed

The mortality rates of fungal infections that affect the central nervous system are high in consequence of the absence of effective antifungal drugs with good penetration across the blood-brain barrier and the blood-cerebrospinal fluid barrier. In the present work in vitro antifungal activities of three good penetrating non-antifungal drugs (amantadine hydrochloride, R-(-)-deprenyl hydrochloride, valproic acid sodium salt) and their combinations with three antifungal agents (amphotericin B, itraconazole, terbinafine) were tested with broth microdilution method against eight fungal isolates belonging to Zygomycetes (Lichtheimia corymbifera, Rhizomucor miehei, Rhizopus microsporus var. rhizopodiformis, Saksenaeavasiformis) and Aspergillus genus (A. flavus, A. fumigatus, A. nidulans, A. terreus). These are known to be possible agents of central nervous fungal infections (CNFI). When used alone, the investigated nonantifungal drugs exerted slight antifungal effects. In their combinations with antifungal agents they acted antagonistically, additively and synergistically against zygomyceteous isolates. Primarily antagonistic interactions were revealed between the investigated drugs in case of Aspergilli, but additive and synergistic interactions were also observed. The additive and synergistic combinations allowed the usage of reduced concentrations of antifungal agents to inhibit the fungal growth in our study. These combinations would be a basis of an effective, less toxic therapy for treatment of CNFI. PMID:23134606

Galgóczy, L; Tóth, Liliána; Virágh, M; Papp, T; Vágvölgyi, C S

2012-12-01

415

Synthesis, characterisation, reactivity and in vitro antiamoebic activity of hydrazone based oxovanadium(IV), oxovanadium(V) and mu-bis(oxo)bis{oxovanadium(V)} complexes.  

PubMed

Binuclear, mu-bis(oxo)bis{oxovanadium(V)} complexes [(VOL)2(mu-O)2](2 and 7)(where HL are the hydrazones Hacpy-nah I or Hacpy-fah II; acpy = 2-acetylpyridine, nah = nicotinic acid hydrazide and fah = 2-furoic acid hydrazide) were prepared by the reaction of [VO(acac)2] and the ligands in methanol followed by aerial oxidation. The paramagnetic intermediate complexes [VO(acac)(acpy-nah)](1) and [VO(acac)(acpy-fah)](6) have also been isolated. Treatment of [VO(acac)(acpy-nah)] and [VO(acac)(acpy-fah)] with aqueous H2O2 yields the oxoperoxovanadium(V) complexes [VO(O2)(acpy-nah)](3) and [VO(O2)(acpy-fah)](8). In the presence of catechol (H2cat) or benzohydroxamic acid (H2bha), 1 and 6 give the mixed chelate complexes [VO(cat)L](HL =I: 4, HL =II: 9) or [VO(bha)L](HL =I: 5, HL =II: 10). Complexes 4, 5, 9 and 10 slowly convert to the corresponding oxo-mu-oxo species 2 and 7 in DMF solution. Ascorbic acid enhances this conversion under aerobic conditions, possibly through reduction of these complexes with concomitant removal of coordinated catecholate or benzohydroxamate. Acidification of 7 with HCl dissolved in methanol afforded a hydroxo(oxo) complex. The crystal and molecular structure of 2.1.5H2O has been determined, and the structure of 7 re-determined, by single crystal X-ray diffraction. Both of these binuclear complexes contain the uncommon asymmetrical {VO(mu-O)}2 diamond core. The in vitro tests of the antiamoebic activity of ligands I and II and their binuclear complexes 2 and 7 against the protozoan parasite Entamoeba histolytica show that the ligands have no amoebicidal activity while their vanadium complexes 2 and 7 display more effective amoebicidal activity than the most commonly used drug metronidazole (IC50 values are 1.68 and 0.45 microM, respectively vs 1.81 microM for metronidazole). Complexes 2 and 7 catalyse the oxidation of styrene and ethyl benzene effectively. Oxidation of styrene, using H2O2 as an oxidant, gives styrene epoxide, 2-phenylacetaldehyde, benzaldehyde, benzoic acid and 1-phenyl-ethane-1,2-diol, while ethyl benzene yields benzyl alcohol, benzaldehyde and 1-phenyl-ethane-1,2-diol. PMID:16462954

Maurya, Mannar R; Agarwal, Shalu; Abid, Mohammad; Azam, Amir; Bader, Cerstin; Ebel, Martin; Rehder, Dieter

2005-11-07

416

The iron chelator pyridoxal isonicotinoyl hydrazone (PIH) and its analogues prevent damage to 2-deoxyribose mediated by ferric iron plus ascorbate.  

PubMed

Iron chelating agents are essential for treating iron overload in diseases such as beta-thalassemia and are potentially useful for therapy in non-iron overload conditions, including free radical mediated tissue injury. Deferoxamine (DFO), the only drug available for iron chelation therapy, has a number of disadvantages (e.g., lack of intestinal absorption and high cost). The tridentate chelator pyridoxal isonicotinoyl hydrazone (PIH) has high iron chelation efficacy in vitro and in vivo with high selectivity and affinity for iron. It is relatively non-toxic, economical to synthesize and orally effective. We previously demonstrated that submillimolar levels of PIH and some of its analogues inhibit lipid peroxidation, ascorbate oxidation, 2-deoxyribose degradation, plasmid DNA strand breaks and 5,5-dimethylpyrroline-N-oxide (DMPO) hydroxylation mediated by either Fe(II) plus H(2)O(2) or Fe(III)-EDTA plus ascorbate. To further characterize the mechanism of PIH action, we studied the effects of PIH and some of its analogues on the degradation of 2-deoxyribose induced by Fe(III)-EDTA plus ascorbate. Compared with hydroxyl radical scavengers (DMSO, salicylate and mannitol), PIH was about two orders of magnitude more active in protecting 2-deoxyribose from degradation, which was comparable with some of its analogues and DFO. Competition experiments using two different concentrations of 2-deoxyribose (15 vs. 1.5 mM) revealed that hydroxyl radical scavengers (at 20 or 60 mM) were significantly less effective in preventing degradation of 2-deoxyribose at 15 mM than 2-deoxyribose at 1.5 mM. In contrast, 400 microM PIH was equally effective in preventing degradation of both 15 mM and 1.5 mM 2-deoxyribose. At a fixed Fe(III) concentration, increasing the concentration of ligands (either EDTA or NTA) caused a significant reduction in the protective effect of PIH towards 2-deoxyribose degradation. We also observed that PIH and DFO prevent 2-deoxyribose degradation induced by hypoxanthine, xanthine oxidase and Fe(III)-EDTA. The efficacy of PIH or DFO was inversely related to the EDTA concentration. Taken together, these results indicate that PIH (and its analogues) works by a mechanism different than the hydroxyl radical scavengers. It is likely that PIH removes Fe(III) from the chelates (either Fe(III)-EDTA or Fe(III)-NTA) and forms a Fe(III)-PIH(2) complex that does not catalyze oxyradical formation. PMID:11042379

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

2000-10-18

417

Versatility of 2,6-diacetylpyridine (dap) hydrazones in stabilizing uncommon coordination geometries of Mn(II): synthesis, spectroscopic, magnetic and structural characterization.  

PubMed

Five seven- or eight-coordinate manganese complexes of hydrazone ligands have been prepared. Three seven-coordinate neutral Mn(II) complexes: [Mn(dapA2)]n (1), [Mn(dapB2)(H2O)2] (2), [Mn(dapS2)(H2O)2] (3) have been synthesized from the bis-Schiff bases of 2,6-diacetylpyridine: dap(AH)2, dap(BH)2 and dap(SH)2 (AH = anthraniloyl hydrazide, BH = benzoyl hydrazide, SH = salicyloyl hydrazide), respectively. Two eight-coordinate Mn(II) complexes: [Mn(dapS)2] (4) and [Mn(dapB)2].3H2O (5) have been synthesized from the mono-Schiff bases dapBH and dapSH, respectively. The complexes have been characterized by elemental analyses and by IR, UV-Vis., FAB mass, EI mass and EPR spectroscopy. The molecular structures of 1, 3.DMF and 4.DMF have been determined by single-crystal X-ray diffraction. The mono-Schiff bases are monoanionic and the bis-Schiff bases are dianionic. The octa-coordinated mono-Schiff base complex 4 adopts a dodecahedral geometry, while the hepta-coordinated bis-Schiff base complex 1 forms a one-dimensional linear polymeric chain. A weak antiferromagnetic exchange interaction (J=-0.15 cm(-1)) between the Mn(II) ions in is attributed to weak Mn...Mn interaction through the PhNH(2) moiety of the ligand, as indicated by extended-Hückel molecular orbital calculations. A good simulation of the EPR spectrum of a frozen solution (DMSO at 4 K) of compound 1 was obtained with g=2.0, D=0.1 cm(-1), E=0.01 cm(-1). The EPR spectrum of a powdered sample of compound 1 shows a large broadening of the signal, due in part, to the important zero-field splitting of the hepta-coordinated Mn(II) ion. PMID:15995753

Naskar, Subhendu; Mishra, Dipankar; Chattopadhyay, Shyamal Kumar; Corbella, Montserrat; Blake, Alexander J

2005-06-15

418

Vanadium complexes having [VO]2+, [VO]3+ and [VO2]+ cores with hydrazones of 2,6-diformyl-4-methylphenol: synthesis, characterization, reactivity, and catalytic potential.  

PubMed

The Schiff bases H3dfmp(L)2 obtained by the condensation of 2,6-diformyl-4-methylphenol and hydrazones [L = isonicotinoylhydrazide (inh), nicotinoylhydrazide (nah) and benzoylhydrazide (bhz)] are prepared and characterized. By reaction of [V(IV)O(acac)2] and the H3dfmp(L)2 in methanol the V(IV)O-complexes [V(IV)O{Hdfmp(inh)2}(H2O)] (1), [V(IV)O{Hdfmp(nah)2}(H2O)] (2) and [V(IV)O{Hdfmp(bhz)2}(H2O)] (3) were obtained. Upon their aerial oxidation in methanol [V(V)O(OMe)(MeOH){Hdfmp(inh)2}] (4), [V(V)O(OMe)(MeOH){Hdfmp(nah)2}] (5) and [V(V)O(OMe)(MeOH){Hdfmp(bhz)2}] (6) were isolated. In the presence of KOH, oxidation of 1-3 results in the formation of [V(V)O2{H2dfmp(inh)2}]n·5H2O (7), K[V(V)O2{Hdfmp(nah)2}] (8) and K[V(V)O2{Hdfmp(bhz)2}] (9). All compounds are characterized in the solid state and in solution, namely by spectroscopic techniques (IR, UV-Vis, EPR, (1)H, (13)C and (51)V NMR), and DFT is also used to calculate the V(IV) hyperfine coupling constants of V(IV)-compounds and (51)V NMR chemical shifts of several V(V)-species and assign them to those formed in solution. Single crystal X-ray analysis of [V(V)O(OMe)(MeOH){Hdfmp(bhz)2}] (6) and [V(V)O2{H2dfmp(inh)2}]n·5H2O (7) confirm the coordination of the ligand in the dianionic (ONO(2-)) enolate tautomeric form, one of the hydrazide moieties remaining non-coordinated. In the case of 7 the free N(pyridine) atom of the inh moiety coordinates to the other vanadium center yielding a polynuclear complex in the solid state. It is also demonstrated that the V(V)O2-complexes are catalyst precursors in the oxidative bromination of styrene by H2O2, therefore acting as functional models of vanadium dependent haloperoxidases. Plausible intermediates involved in the catalytic process are established by UV-Vis, (51)V NMR and DFT studies. PMID:23680862

Maurya, Mannar R; Haldar, Chanchal; Kumar, Amit; Kuznetsov, Maxim L; Avecilla, Fernando; Costa Pessoa, João

2013-09-01

419

An HPLC method for the determination of nifekalant hydrochloride in canine plasma and its application to a pharmacokinetic study.  

PubMed

In this study, a simple and selective high-performance liquid chromatography method was developed and validated for the determination of nifekalant hydrochloride in canine plasma. Liquid-liquid extraction was used to separate nifekalant hydrochloride from canine plasma and the mean extraction recoveries of nifekalant hydrochloride and the internal standard were 82.31 and 94.81%, respectively. The chromatographic separation was performed on a Dikma Diamonsil column with a mobile phase consisting of acetonitrile-20mM phosphate buffer (pH 6.2; 30:70, v/v) with flow rate of 1.0 mL/min. The standard curve was linear over the concentration range of 20-10,000 ng/mL (r(2) > 0.99). The intra-batch and inter-batch accuracy for nifekalant hydrochloride at four concentrations were 93.14-100.47% and 96.12-103.77%, respectively. The relative standard deviations were less than 15%. The method was successfully applied to a pharmacokinetic study after the intravenous administration of nifekalant hydrochloride to beagle dogs. PMID:23169932

Zhou, Yi; Liu, Xiu-Mei; Wang, Ling; Jiang, Xue-Hua

2012-11-20

420

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.

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

2013-01-01

421

Penehyclidine hydrochloride: a potential drug for treating COPD by attenuating Toll-like receptors  

PubMed Central

Background The aim of this review was to evaluate and summarize the available scientific information on penehyclidine hydrochloride (PHC) for the treatment of chronic obstructive pulmonary disease (COPD) as a result of its ability to attenuate Toll-like receptors. Penehyclidine hydrochloride is an anticholinergic drug manufactured in China, with both antimuscarinic and antinicotinic activity. PHC is used widely in the clinic as a reversal agent in cases of organic phosphorus poisoning and soman poisoning, but also may also have an important role as a bronchodilator in the treatment of obstructive airway disease, including asthma and, in particular, COPD. Methods Our bibliographic sources included the CAPLUS, MEDLINE, REGISTRY, CASREACT, CHEMLIST, CHEMCATS, and CNKI databases, updated to September 2012. In order to assess the data in detail, we used the search terms “penehyclidine hydrochloride,” “COPD,” “muscarinic receptor,” and “toll-like receptors.” Papers were restricted to those published in the English and Chinese languages, and to “paper” and “review” as the document type. Patents were also reviewed. Results Our survey mainly yielded the results of research on PHC and the mechanisms of COPD. COPD is a preventable and treatable disease with some significant extrapulmonary manifestations that may contribute to its severity in some patients. Recently, it has been shown that muscarinic receptors may interact with Toll-like receptors. Basic and clinical studies of the relationship between the mechanism of action and the effects of PHC in the respiratory tract have been studied by a number of laboratories and institutions. The main advantages of PHC are that it has few M2 receptor-associated cardiovascular side effects and attenuates Toll-like receptors. Conclusion PHC may be a promising candidate agent in the treatment of COPD in the future because of its ability to attenuate Toll-like receptors. This review should be of help to those intending to research this topic further.

Xiao, Hong-Tao; Liao, Zhi; Tong, Rong-Sheng

2012-01-01

422

[Bronchial asthma attack with lactic acidosis and hypokalemia in a case receiving high dose inhalation of procaterol hydrochloride].  

PubMed

We report a case of bronchial asthma attack with lactic acidosis and hypokalemia in a patient receiving high-dose inhalation of procaterol hydrochloride. A 28-year-old man was transferred to our hospital because of adynamia, nausea and dyspnea. He had used inhaled procaterol hydrochloride with a pressurized metered dose inhaler about 20 times before admission. On admission, there were no signs of shock state or hypoxemia and laboratory data showed hypokalemia, hyperglycemia and metabolic acidosis with elevated anion gap. Lactic acidosis was identified as the reason for the metabolic acidosis with elevated anion gap. Lactic acidosis improved after 12 hours. Lactic acidosis due to high dose inhalation of procaterol hydrochloride was suggested. PMID:17491317

Noma, Satoshi; Kubota, Shingo; Matsukizono, Kazuya; Tanoue, Asako; Kumamoto, Tomohiro; Taira, Tetsuhiko; Mitsuyama, Hideo; Kawabata, Toshihumi; Suetsugu, Takayuki; Iwakaw, Jun; Koreed, Yoshimizu; Matsuyama, Wataru; Mizuno, Keiko; Higashimoto, Ikkou; Osame, Mitsuhiro; Arimura, Kimiyoshi

2007-04-01

423

Detection, Isolation and Characterization of Principal Synthetic Route Indicative Impurities in Verapamil Hydrochloride  

PubMed Central

Two unknown impurities were detected in verapamil hydrochloride bulk drug using isocratic reversed-phase high performance liquid chromatography (HPLC). These impurities were isolated by preparative HPLC. Spectral data for the isolated impurities were collected. Based on the spectral data derived from two-dimensional nuclear magnetic resonance (2D-NMR) spectroscopy and mass spectrometry (MS), impurity-1 and impurity-2 were characterized as 2-(3,4-dimethoxyphenyl)-3-methylbut-2-enenitrile and 2-(3,4-dimethoxyphenyl)-2-isopropyl-3-methylbutanenitrile, respectively.

Srinivasan, Viswanathan; Sivaramakrishnan, Hariharan; Karthikeyan, Balakrishnan

2011-01-01

424

Sustained-release dosage form of phenylpropanolamine hydrochloride (3). Application of factorial design.  

PubMed

In this study a 2(2) factorial design has been applied to the evaluation of dissolution characteristics of phenylpropranolamine hydrochloride (PPA.HCl) from tableted microcapsules. The kinetic model according to the Rosin-Rimmler-Sperling-Bennet-Weillbull (RRSBW) distribution was applied for the parametric representation of the dissolution curves. The effect of two factors; drug particle size and kind of disintegrating agent, on the dissolution rate of PPA.HCl were studied at two levels. The factorial design method proved to be useful for the examination of tableted microcapsules. PMID:7931943

Sevgi, F; Ozyazici, M; Güneri, T

425

Sustained-release dosage form of phenylpropanolamine hydrochloride. Part I: Microencapsulation and in vitro release kinetics.  

PubMed

Microcapsules of phenylpropanolamine hydrochloride with core:wall ratios of 1:1, 2:1 and 1:2 were prepared by the coacervation-phase separation method, using ethylcellulose as the coating material. Two batches of PPA.HCl powder with different particle sizes (> 58 microns and < 28 microns) were used as the core material. The different sizes of microcapsules were separated using a range of standard sieves (840-247 microns). The effects of drug particle size, the media pH and the core:wall ratio on the dissolution kinetics were studied, and evaluated kinetically. PMID:8064556

Sevgi, F; Ozyazici, M; Güneri, T

426

Metabolomic Analyses of Blood Plasma after Oral Administration of D-Glucosamine Hydrochloride to Dogs  

PubMed Central

D-Glucosamine hydrochloride (GlcN?HCl) is an endogenous amino monosaccharide synthesized from glucose that is useful in the treatment of joint diseases in both humans and animals. The aim of this study was to examine amino acid metabolism in dogs after oral administration of GlcN?HCl. Accelerated fumarate respiration and elevated plasma levels of lactic acid and alanine were observed after administration. These results suggest that oral administration of GlcN?HCl induces anaerobic respiration and starvation in cells, and we hypothesize that these conditions promote cartilage regeneration. Further studies are required to evaluate the expression of transforming growth factor-beta (TGF-?).

Osaki, Tomohiro; Azuma, Kazuo; Kurozumi, Seiji; Takamori, Yoshimori; Tsuka, Takeshi; Imagawa, Tomohiro; Okamoto, Yoshiharu; Minami, Saburo

2012-01-01

427

Photostabilization of doxorubicin hydrochloride with radioprotective and photoprotective agents: Potential mechanism for enhancing chemotherapy during radiotherapy  

SciTech Connect

p-Aminobenzoic acid (PABA), urocanic acid, and sodium urate were found to significantly enhance the photostability of doxorubicin hydrochloride (adriamycin, (ADR)). d1-Methionine, thiourea, and glycine also increased the photostability of this drug, but to a lesser degree. Sodium thiosulfate on the other hand, was found to be detrimental to the photostability of ADR. The photostabilizing effect of PABA was found to increase with increase of its concentration and was influenced by the pH and the buffer species of the vehicle. The findings would have an impact on the enhancement of therapeutic efficacy of adriamycin when administered during radiation therapy.

Habib, M.J.; Asker, A.F.

1989-11-01

428

Treatment of neoplastic pleural effusions with local instillations of quinacrine (mepacrine) hydrochloride  

PubMed Central

The local instillation of quinacrine (mepacrine) hydrochloride is used widely in the United States of America for the treatment of neoplastic pleural effusions. To date, there has been no report of the use of this treatment in the United Kingdom. We have studied the effect of treatment in 12 consecutive patients presenting with a variety of types of malignant pleural effusion and report our experiences. In all of our patients the effusion was successfully controlled and sideeffects were not unduly troublesome. We conclude that quinacrine is at least as effective as other forms of treatment of neoplastic pleural effusion and merits more attention.

Hickman, J. A.; Jones, M. C.

1970-01-01

429

"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.

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

2012-01-01

430

Ultrasonic Studies of 4-Aminobutyric Acid in Aqueous Metformin Hydrochloride Solutions at Different Temperatures  

Microsoft Academic Search

Ultrasonic speeds and density data of 4-aminobutyric acid in 0.05 M, 0.10 M, and 0.15 M aqueous metformin hydrochloride (MFHCl)\\u000a solutions are measured at 308.15 K, 313.15 K, and 318.15 K. The isentropic compressibility (k\\u000a \\u000a S\\u000a ), the change in isentropic compressibility (?k\\u000a \\u000a S\\u000a ), the relative change in isentropic compressibility ($${\\\\Delta k_S\\/k_S^0}$$), the apparent molal compressibility ($${k_\\\\phi}$$), the limiting

K. Rajagopal; S. S. Jayabalakrishnan

2010-01-01

431

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

Microsoft Academic Search

Interaction products of metformin hydrochloride (MF·HCl), an oral anti-hyperglycaemic agent highly soluble in water, with triacetyl-?-cyclodextrin (TA?CyD), a hydrophobic CyD derivative practically insoluble in water, were prepared to evaluate their suitability for the development of a sustained-release dosage form of the drug. Equimolar MF·HCl–TA?CyD solid compounds were obtained by different techniques, i.e., physical mixing, kneading, co-grinding, sealed-heating, and spray-drying, in

Giovanna Corti; Gaetano Capasso; Francesca Maestrelli; Marzia Cirri; Paola Mura

2007-01-01

432

Spectroscopic studies on the interaction of carteolol hydrochloride and urea-induced bovine serum albumin  

NASA Astrophysics Data System (ADS)

The interaction of carteolol hydrochloride, to 0.2 mol L-1 urea-induced bovine serum albumin in aqueous solution has been first investigated by fluorescence spectra and ultraviolet-visible (UV-vis) spectra at pH 7.40. The quenching mechanism, binding parameter and sites (n), the binding mode (?G, ?H, and ?S) as well as the binding distance (r) have been obtained according to the experimental results. We also use the synchronous fluorescence method to study the effect of CTL on the conformation change of urea-induced BSA.

Yao, Qing; Yu, Xianyong; Zheng, Tongyin; Liu, Heting; Yang, Ying; Yi, Pinggui

2013-09-01

433

[Clinical evaluation of supplemental administration of flavoxate hydrochloride in benign prostatic hyperplasia patients with nocturia resistant to an alpha1-adrenoceptor blocker].  

PubMed

We examined the effectiveness of supplemental administration of flavoxate hydrochloride in patients with benign prostatic hyperplasia (BPH) whose nocturia was not adequately relieved by an alpha1-adrenoceptor blocker. Fifty-two patients who had two or more nocturnal micturition after administration of tamsulosin hydrochloride or naftopidil for 4 weeks or more received 400-600 mg of flavoxate hydrochloride in addition to an alpha1-adrenoceptor blocker for another 8-12 weeks. With supplemental administration of flavoxate hydrochloride, significant improvement was observed in the number of nocturnal micturition, total International Prostate Sympton Score, quality of life score and BPH impact index. No significant change was observed in the voided volume, Qmax, voiding time and residual urine volume. Supplemental administration of flavoxate hydrochloride is therefore effective for the improvement of nocturia and QOL in BPH patients resistant to an alpha1-adrenoceptor blocker. PMID:18411771

Kato, Shinobu; Kusaka, Mamoru; Shiroki, Ryoichi; Izumitani, Masanobu; Asano, Haruyoshi; Ooki, Takahiro; Yanaoka, Masanori; Hoshinaga, Kiyotaka

2008-03-01

434

Synthesis and properties of new dinuclear organoiron(II) hydrazones combining the potent electron-donating [?(? 5-C 5H 4)FeCp] fragment with [CpFe(? 6-arene)?] +-type acceptors  

Microsoft Academic Search

The stereoselective condensation reaction between organometallic hydrazine precursors [CpFe(?6-p-RC6H4?NHNH2)]+PF6? (R=H, (1)+PF6?; Me, (2)+PF6?; MeO, (3)+PF6?; Cl, (4)+PF6?) and (E)-(2-ferrocenylvinyl)-methyl ketone, [(E)-[CpFe(?5-C5H4)?CH?CH?CO?Me] (5), allowed the synthesis of a family of four new push–pull-type homodinuclear hydrazones complexes formulated as (E,E)-[CpFe(?6-p-RC6H4)?NHN?CMe?CH?CH?(?5-C5H4)FeCp]+PF6? (R=H, (6)+PF6?; Me, (7)+PF6?; MeO, (8)+PF6?; Cl, (9)+PF6?). These compounds were fully characterized by a combination of elemental analysis and spectroscopic techniques

Alexander Trujillo; Mauricio Fuentealba; Carolina Manzur; David Carrillo; Jean-René Hamon

2003-01-01

435

Transition metal complexes with Girard reagent-based ligands. Part IV. Synthesis and characterization of pyridoxilidene Girard-T hydrazone complexes. Crystal structure of the copper(II) complex  

Microsoft Academic Search

\\u000a Abstract  The monoligand complexes of the formula M(HPLGT)(NCS)2 (M = Cu(II), Zn(II)) in which the ligand tridentate ONO pyridoxilidene Girard-T hydrazone, [H3PLGT]Cl2 · 2H2O, was coordinated in neutral doubly deprotonated form were synthesized. Also, the first complexes with the ligand coordinated\\u000a in triply deprotonated monoanionic form of the formula [Cu(PLGT)N3] and [Co(PLGT)(NO2)2NH3] · 3H2O are reported. The single crystal X-ray analysis of [Cu(HPLGT)(NCS)2] showed that Cu(II) is

Ljiljana S. Vojinovi?-Ješi?; Goran A. Bogdanovi?; Vukadin M. Leovac; Valerija I. ?ešljevi?; Ljiljana S. Jovanovi?

2008-01-01

436

Synthesis, Crystal Structures, and Antibacterial Activity of Two Hydrazone Derivatives 3Methoxy N ?-(3,5-Dibromo-2-Hydroxybenzylidene)Benzohydrazide Methanol Solvate and 3Methoxy N ?-(2,4-Diclorobenzylidene)Benzohydrazide  

Microsoft Academic Search

\\u000a Abstract  Two new hydrazone compounds with the formulae C15H12Br2N2O3·CH3OH (1) and C15H12Cl2N2O2 (2), were prepared and characterized by elemental analysis, IR spectra and single-crystal X-ray determination. Compound (1)\\u000a crystallizes in the triclinic space group P-1 with unit cell dimensions a = 7.654(1) Å, b = 13.801(2) Å, c = 16.904(2) Å, ? = 90.772(2)o, ? = 101.721(2)o, ? = 95.891(2)o, V = 1738.1(4) ?3, Z = 4, R\\u000a 1 = 0.0495 and wR\\u000a 2 = 0.1161. Compound (2) crystallizes in the triclinic

San-Jun Peng

2011-01-01

437

Suppression of Glutamate-Induced Excitotoxicity by 2-Cyclopropylimino-3-methyl-1,3-thiazoline Hydrochloride in Rat Glial Cultures  

Microsoft Academic Search

We have screened new drugs with a view to developing effective drugs against glutamate-induced excitotoxicity. In the present\\u000a work, we show effects of a new drug, 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride against glutamate-induced excitotoxicity\\u000a in primary rat glial cultures. Pretreatment of glial cells with 2-cyclopropylimino-3-methyl-1,3-thiazoline hydrochloride for\\u000a 2 h significantly protected glial cells against glutamate-induced excitotoxicity in a time- and dose-dependent manner with\\u000a an

Eun-A Kim; Hoh-Gyu Hahn; Key-Sun Kim; Tae Ue Kim; Soo Young Choi; Sung-Woo Cho

2010-01-01

438

Cerebral perfusion imaging in Alzheimer's disease. Use of single photon emission computed tomography and iofetamine hydrochloride I 123  

SciTech Connect

We used single photon emission computed tomography (SPECT) to study 15 patients with Alzheimer's disease and nine controls. Iofetamine hydrochloride I 123 uptake data were recorded from the entire brain using a rotating gamma camera. Activity ratios were measured for the frontal, posterior parietal, posterior, medial, and lateral cortical temporal regions and striate cortex and were normalized by the activity in the cerebellum. Abnormalities in iofetamine hydrochloride I 123 activity were similar to the abnormalities in glucose metabolism observed with positron emission tomography. Cortical tracer activity was globally depressed in patients with Alzheimer's disease, with the greatest reduction in the posterior parietal cortex.

Johnson, K.A.; Mueller, S.T.; Walshe, T.M.; English, R.J.; Holman, B.L.

1987-02-01

439

Quantification of Hydrazines and Hydrazones.  

National Technical Information Service (NTIS)

Nanomole quantities of hydrazine (Hz), monomethylhydrazine (MMH), and unsymmetrical dimethylhydrazine (UDMH) can be determined by constant-current coulometry. The hydrazines are titrated in an acidic solution with electrically-generated bromine or chlorin...

E. L. Miller R. P. Johnson

1984-01-01

440

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

2013-07-14

441

Formulation and characterization of patient-friendly dosage form of ondansetron hydrochloride.  

PubMed

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

2010-07-01

442

Statistical optimization of tamsulosin hydrochloride controlled release pellets coated with the blend of HPMCP and HPMC.  

PubMed

The objective of the present study was to evaluate three coating parameters for the application of a blend of HPMCP and HPMC in ethylcellulose aqueous dispersions (Surelease) in order to obtain controlled release of tamsulosin hydrochloride. The selected independent variables, HPMCP content (X1), HPMC content (X2) and coating level (X(3)), were optimized with a three-factor, three-level Box-Behnken design. The selected dependent variables were the cumulative percentage values of tamsulosin hydrochloride that had dissolved after 2, 3 and 5 h. Various dissolution profiles of the drug from controlled release pellets were obtained. Optimization was performed for X1, X2 and X3 using the following target ranges; 15% < or = Y1 < or= 30%; 50% < or = Y2 < or = 65%; 80% < or = Y3 < or = 95%. Results of the optimization procedure indicated that the optimized levels of HPMCP content (X1), HPMC content (X2) and coating level (X3) were 30%, 15% and 25%, respectively. Controlled release pellets coated with the optimized formulation provided a release profile that was close to predicted values. In addition, the dissolution profiles of the controlled release pellets coated with the optimized formulation were similar to those of the commercial product Harunal capsule (f1 = 4.6, f2 = 78.7). PMID:17541199

Kim, Jeong-Soo; Kim, Min-Soo; Park, Hee Jun; Lee, Sibeum; Park, Jeong-Sook; Hwang, Sung-Joo

2007-06-01

443

Efficacy of topical benzydamine hydrochloride gel on oral mucosal ulcers: an in vivo animal study.  

PubMed

The aim of this study was to investigate the effect of benzydamine hydrochloride bioadhesive gel on healing of oral mucosal ulceration in an animal model. For in vivo determination of the effects of the bioadhesive gel, 36 rabbits were separated into three groups: the first group was treated with the gel formulation without active agent, the second group with the gel formulation containing benzydamine, and the third group received no treatment. Clinical healing was established by measuring the area of the ulcer in each test group on days 3, 6, 9 and 12. Histological healing was determined on the same days. Benzydamine containing gel applications resulted in a decrease in the ulcer area in 12 days (p=0.000). Histological evaluation showed that the benzydamine group had a higher mean histological score than the base and the control groups during the whole test period, and the difference between the benzydamine group and the control group was significant (p=0.04). The bioadhesive gel formulation of benzydamine hydrochloride showed a statistically significant increased rate of mucosal repair in this experimental standard mucosal wound animal study. It is a candidate for the topical treatment of oral mucosal ulcerative lesions. PMID:21549562

Karavana Hizarcio?lu, S Y; Sezer, B; Güneri, P; Veral, A; Boyacio?lu, H; Ertan, G; Epstein, J B

2011-05-05

444

[Discovery and development of donepezil hydrochloride for the treatment of Alzheimer's disease].  

PubMed

The most consistent change of neurotransmitter in the brain of Alzheimer's patients is the dramatic decrease of cholinergic innervation due to the loss of neurons in the basal forebrain. The most widely studied acetylcholinesterase inhibitors (AChEIs) have been physostigmine and tacrine. Physostigmine has very short duration, and tacrine has liability to hepatotoxicity. These are the defects of the inhibitors. Our objective was to find a new type of AChEIs that would overcome the disadvantages of physostigmine and tacrine. Through a random screening, we incidentally found an N-benzylpiperazine derivative which showed positive cholinergic behavior in rats. We replaced the N-benzylpiperazine moiety with N-benzylpiperidine moiety and found a dramatic increase in anti-AChE activity. Even after the replacement of an amide group with a ketone group the activity was held. Furthermore, the cyclic-amide derivative showed enhanced inhibitory activity. On the basis of these results, an indanone derivative was designed. Among these indanone derivatives, donepazil hydrochloride (E2020), brand name ARICEPT was found to be the most balanced compound. The clinical studies of donepezil hydrochloride demonstrated statistically significant effects on ADAS-cog (Alzheimer's Disease Assessment Scale cognitive sub.) and CIBIC Plus (Clinician's Interview-Based Impression of Change plus). PMID:10067428

Sugimoto, H; Yamanishi, Y; Ogura, H; Iimura, Y; Yamatsu, K

1999-02-01

445

An experimental and theoretical investigation of loperamide hydrochloride-glutaric acid cocrystals.  

PubMed

Cocrystallization is a powerful method to improve the physicochemical properties of drugs. Loperamide hydrochloride is a topical analgesic for the gastrointestinal tract showing low and pH-dependent solubility; for this reason, an enhancement of its solubility or dissolution rate, particularly at the pH of the intestinal tract, could improve its local efficacy. Here we prepared cocrystals of this active principle with glutaric acid and so obtained a new crystalline solid representing a viable alternative to improve the physicochemical properties and thus the pharmaceutical behavior of the drug. Differential scanning calorimetry, X-ray powder diffraction, Fourier infrared spectroscopy, solid-state NMR, and scanning electron microscopy coupled to the energy-dispersive X-ray spectrometry were used to investigate the new solid-phase formation. DFT calculations at B3LYP/6-31G(d) level of theory, in the gas phase, including frequencies computation, provided a rationale for the interaction between loperamide hydrochloride and glutaric acid. The cocrystals showed improved water solubility in comparison with loperamide HCl, and the pharmaceutical formulation proposed was able to release the drug more rapidly in comparison with three reference commercial products when tested at neutral pH values. PMID:23763498

Bruni, Giovanna; Maietta, Mariarosa; Maggi, Lauretta; Mustarelli, Piercarlo; Ferrara, Chiara; Berbenni, Vittorio; Freccero, Mauro; Scotti, Federico; Milanese, Chiara; Girella, Alessandro; Marini, Amedeo

2013-06-26

446

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

447

Development of an enhanced formulation for delivering sustained release of buprenorphine hydrochloride.  

PubMed

To control the minimum effective dose, and reduce the number and quantity of administered potent drugs are unique features of advanced drug delivery in situ forming gel formulation. The efficacy, consistency, and increasing the application of existing injection therapies can be enhanced through optimization of controlled released systems by using FDA approved biodegradable PLGA (poly-d,l-lactide-co-glycolide) polymer. The purpose of this study was to develop different in situ forming implant (ISFI) formulations of buprenorphine hydrochloride for post treatment of drug addicts, acute and chronic pains. The drug releases from different ISFIs membranes with and without Tween 80 were compared over a period of time. Kinetic equation followed the Korsmeyer-Peppas model, as the plots showed high linearity. The influence of this additive on polymer properties was investigated using differential scanning calorimetry (DSC), and the membranes structure was studied by X-ray diffractometry (XRD) and scanning electron microscope (SEM). Data revealed that Tween 80 modified the drug release pattern using diffusion mechanism and decreased the glass transition temperature (T g) significantly. The degree of crystallinity was decreased after phase inversion which helps the dissolution of drug from membrane. The porosity of modified membranes was in accordance with release profiles. These findings suggest four different in situ forming implant formulations which can release various dose of the buprenorphine hydrochloride in a prolonged time. Also this surfactant can be an attractive additive for modifying the release rate of drugs from PLGA-based membrane drug delivery systems. PMID:23960766

Koocheki, S; Madaeni, S S; Niroomandi, P

2011-05-12

448

High doses of pseudoephedrine hydrochloride accelerate onset of CNS oxygen toxicity seizures in unanesthetized rats.  

PubMed

Pseudoephedrine (PSE) salts (hydrochloride and sulfate) are commonly used as nasal and paranasal decongestants by scuba divers. Anecdotal reports from the Divers Alert Network suggest that taking PSE prior to diving while breathing pure O? increases the risk for CNS oxygen toxicity (CNS-OT), which manifests as seizures. We hypothesized that high doses of PSE reduce the latency time to seizure (LS) in unanesthetized rats breathing 5 atmospheres absolute (ATA) of hyperbaric oxygen. Sixty-three male rats were implanted with radio-transmitters that recorded electroencephalogram activity and body temperature. After ?7-day recovery, and 2 h before "diving", each rat was administered either saline solution (control) or PSE hydrochloride intragastrically at the following doses (mg PSE/kg): 0, 40, 80, 100, 120, 160, and 320. Rats breathed pure O? and were dived to 5ATA until the onset of behavioral seizures coincident with neurological seizures. LS was the time elapsed between reaching 5ATA and exhibiting seizures. We observed a significant dose-dependent decrease in the LS at doses of 100-320 mg/kg, whereas no significant differences in LS from control value were observed at doses ?80 mg/kg. Our findings showed that high doses of PSE accelerate the onset of CNS-OT seizures in unanesthetized rats breathing 5ATA of poikilocapnic hyperoxia. Extrapolating our findings to humans, we conclude that the recommended daily dose of PSE should not be abused prior to diving with oxygen-enriched gas mixes or pure O?. PMID:23624060

Pilla, R; Held, H E; Landon, C S; Dean, J B

2013-04-24

449

Formulation and optimization of ethosomes for transdermal delivery of ropinirole hydrochloride.  

PubMed

The present study focuses on the formulation of ethosomal gel of ropinirole hydrochloride (ropinirole HCl), an anti-Parkinsonian drug, for delivery as a carrier for transdermal application. The ethosomes were prepared using different concentrations of phospholipids (2-5 % w/v), ethanol (20-50 % w/v), ropinirole HCl (5 % w/v) and water. They were optimized using 3(2) full factorial designs to study the effect of independent variables, concentrations of ethanol and lecithin on dependent variables, entrapment efficiency and in-vitro drug release at 24 hrs. The drug release profile exhibited Higuchi's and zero order kinetics. From the regression analysis, it was observed that independent variables had significant effect on response variables. Formulations were optimized using contour plot and response surface plot. The optimized formulation was found to be RS10 containing 30 % w/v ethanol and 4% w/v lecithin. The optimized formulation was evaluated for assay, particle characteristics, zeta potential, skin retention and stability. Ethosomal gel was prepared by incorporation of optimized ethosomal suspension into gel base. The ethosomal gel was characterized for physical appearance, pH, content uniformity, rheological behaviour, skin-retention, in-vitro and in-vivo drug release and stability. From the results it can fairly be concluded that ethosomes are capable of delivering ropinirole hydrochloride into systemic circulation by transdermal route. The amounts thus delivered are also equitable to those delivered orally and are delivered at a rate slow enough to achieve longer blood levels. PMID:23410071

Mishra, Ashish D; Patel, C N; Shah, Dinesh R

2013-10-01

450

Development of an enhanced formulation for delivering sustained release of buprenorphine hydrochloride  

PubMed Central

To control the minimum effective dose, and reduce the number and quantity of administered potent drugs are unique features of advanced drug delivery in situ forming gel formulation. The efficacy, consistency, and increasing the application of existing injection therapies can be enhanced through optimization of controlled released systems by using FDA approved biodegradable PLGA (poly-d,l-lactide-co-glycolide) polymer. The purpose of this study was to develop different in situ forming implant (ISFI) formulations of buprenorphine hydrochloride for post treatment of drug addicts, acute and chronic pains. The drug releases from different ISFIs membranes with and without Tween 80 were compared over a period of time. Kinetic equation followed the Korsmeyer–Peppas model, as the plots showed high linearity. The influence of this additive on polymer properties was investigated using differential scanning calorimetry (DSC), and the membranes structure was studied by X-ray diffractometry (XRD) and scanning electron microscope (SEM). Data revealed that Tween 80 modified the drug release pattern using diffusion mechanism and decreased the glass transition temperature (Tg) significantly. The degree of crystallinity was decreased after phase inversion which helps the dissolution of drug from membrane. The porosity of modified membranes was in accordance with release profiles. These findings suggest four different in situ forming implant formulations which can release various dose of the buprenorphine hydrochloride in a prolonged time. Also this surfactant can be an attractive additive for modifying the release rate of drugs from PLGA-based membrane drug delivery systems.

Koocheki, S.; Madaeni, S.S.; Niroomandi, P.

2011-01-01

451

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.

Bhoyar, PK; Biyani, DM; Umekar, MJ

2010-01-01

452

An evaluation of lidocaine hydrocarbonate compared with lidocaine hydrochloride for inferior alveolar nerve block.  

PubMed Central

The purpose of this study was to measure the degree of anesthesia obtained with 2.2% lidocaine hydrocarbonate, 2.2% lidocaine hydrocarbonate with 1:100,000 epinephrine, and 2% lidocaine hydrochloride with 1:100,000 epinephrine for inferior alveolar nerve block. Using a repeated-measures design, 30 subjects randomly received an inferior alveolar injection of each solution over the course of three successive appointments. The first molar, first premolar, lateral incisor, and contralateral canine (control) were blindly tested with an Analytic Technology pulp tester at 3-min cycles for 60 min. Anesthetic success was defined as no subject response to the maximum output (80 reading) of the pulp tester within 16 min and maintenance of this reading for the remainder of the testing period. Although subjects felt numb subjectively, anesthetic success as defined here ranged from 3% to 10% for the plain lidocaine hydrocarbonate; for the lidocaine hydrocarbonate and lidocaine hydrochloride solutions with epinephrine, success ranged from 37% to 63%. We conclude that 2.2% lidocaine hydrocarbonate without vasoconstrictor is not as effective as the other two preparations for inferior alveolar nerve block. The 2.2% lidocaine hydrocarbonate with epinephrine and 2%.

Chaney, M. A.; Kerby, R.; Reader, A.; Beck, F. M.; Meyers, W. J.; Weaver, J.

1991-01-01

453

An approach to controlled-release dosage form of propranolol hydrochloride.  

PubMed

It is possible to release a drug with only limited diffusion from a membrane-coated system using osmotic pumping. In this study, a propranolol osmotic pump was produced by coating the core tablets with cellulose acetate. The effects of membrane thickness, pore size, and stirring rate on the release rate of propranolol hydrochloride were studied. It was found that the thickness of cellulose acetate membrane had a profound effect on the release rate of propranolol hydrochloride from the membrane-coated tablets. The results showed that, when the membrane thickness increased, the release rate of propranolol decreased. The drug release follows a zero-order release when the delivery orifice is between 200 and 800 microns, but when the delivery orifice size is increased to 1000 microns, the release kinetic is abnormal. Fluid dynamics have an important effect on the delivery rate of propranolol from this device; the delivery rate increases as a function of the fluid flow. The drug release is higher under a turbulent condition with high rate of stirring. PMID:10677815

Mohammadi-Samani, S; Adrangui, M; Siahi-Shadbad, M R; Nokhodchi, A

2000-01-01

454

Evaluation of butorphanol tartrate and buprenorphine hydrochloride on the inflammatory reaction of the Sereny Test.  

PubMed

Invasion of the ocular epithelia of guinea pigs by virulent Shigella organisms, eliciting keratoconjunctivitis, is the basis of the Sereny Test (ST). This test has been used to ascertain the virulence of Shigella strains and more recently to screen candidate Shigella vaccines for efficacy. This test undoubtedly causes pain in test animals; however, recommendation for use of local analgesics/anesthetics has not been accepted because of concern that these topical agents may affect the ability of the Shigella organisms to invade the ocular epithelia or have a physiologic effect on the inflammatory process. Similarly, investigators are hesitant to use systemic analgesics in conjunction with the ST. Two blinded studies were conducted to evaluate the effects of selected systemic analgesics on the ST in outbred Hartley guinea pigs. Study 1 evaluated the recommended dosages for two systemic analgesics; study groups consisted of those receiving butorphanol tartrate (n = 16), those receiving buprenorphine hydrochloride (n = 16), and untreated controls (n = 5). Study 2 evaluated a low-dose buprenorphine hydrochloride group (n = 16) and an untreated control group (n = 5). All animals were inoculated with Shigella flexneri, strain 2a 2457T, onto the cornea and conjunctiva of each eye. At the onset of clinical signs, analgesics were administered to test groups. The degree of keratoconjunctivitis was evaluated per standard procedure; animals were weighed daily. After 7 days, animals were euthanatized and the eyes were removed for histologic morphometric evaluation.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:8277729

Swearengen, J R; Cockman-Thomas, R A; Davis, J A; Weina, P J

1993-10-01

455

Development of a floating dosage form of ranitidine hydrochloride by statistical optimization technique.  

PubMed

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 3(2) 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, T(50%) (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

2010-10-01

456

Screening of Venlafaxine Hydrochloride for Transdermal Delivery: Passive Diffusion and Iontophoresis  

PubMed Central

The objective of the study was to investigate in vitro transdermal delivery of venlafaxine hydrochloride across the pigskin by passive diffusion and iontophoresis. For passive diffusion, experiments were carried out in Franz diffusion cell whereas for iontophoretic permeation, the diffusion cell was modified to contain both the donor and return electrode on the same side of skin. Anodal iontophoresis was carried out using a current density of 0.5 mA/cm2. Donor concentrations used were 585.5 mg/ml (saturated solution) and 100 mg/ml. Experiments initially performed to determine the transport efficiency of venlafaxine ions showed promising results. Iontophoresis increased the permeation rate at both concentration levels over their passive counterparts (P?hydrochloride is approximately 9.956 ?mol/h, the results suggested that the drug is a promising candidate for iontophoretic delivery.

Singh, Gursharanjit; Kaushalkumar, Dave; Somsekhar, Vanita

2008-01-01

457

Simultaneous derivative spectrophotometric analysis of doxylamine succinate, pyridoxine hydrochloride and folic Acid in combined dosage forms.  

PubMed

Two UV spectrophotometric methods have been developed, based on first derivative spectrophotometry for simultaneous estimation of doxylamine succinate, pyridoxine hydrochloride, and folic acid in tablet formulations. In method I, the concentrations of these drugs were determined by using linear regression equation. Method II is also based on first derivative spectrophotometry however simultaneous equations (Vierdot's method) were derived on derivative spectra. The first derivative amplitudes at 270.0, 332.8 and 309.2 nm were utilized for simultaneous estimation of these drugs respectively by both methods. In both the methods, linearity was obtained in the concentration range 2.5-50 mug/ml, 1-40 mug/ml and 1-30 mug/ml for doxylamine succinate, pyridoxine hydrochloride, and folic acid respectively. The developed methods show best results in terms of linearity, accuracy, precision, LOD, LOQ and ruggedness for standard laboratory mixtures of pure drugs and marketed formulations. The common excipients and additives did not interfere in their determinations. PMID:20046784

Pathak, A; Rajput, S J

458

Simultaneous Derivative Spectrophotometric Analysis of Doxylamine Succinate, Pyridoxine Hydrochloride and Folic Acid in Combined Dosage Forms  

PubMed Central

Two UV spectrophotometric methods have been developed, based on first derivative spectrophotometry for simultaneous estimation of doxylamine succinate, pyridoxine hydrochloride, and folic acid in tablet formulations. In method I, the concentrations of these drugs were determined by using linear regression equation. Method II is also based on first derivative spectrophotometry however simultaneous equations (Vierdot's method) were derived on derivative spectra. The first derivative amplitudes at 270.0, 332.8 and 309.2 nm were utilized for simultaneous estimation of these drugs respectively by both methods. In both the methods, linearity was obtained in the concentration range 2.5-50 ?g/ml, 1-40 ?g/ml and 1-30 ?g/ml for doxylamine succinate, pyridoxine hydrochloride, and folic acid respectively. The developed methods show best results in terms of linearity, accuracy, precision, LOD, LOQ and ruggedness for standard laboratory mixtures of pure drugs and marketed formulations. The common excipients and additives did not interfere in their determinations.

Pathak, A.; Rajput, S. J.

2008-01-01

459

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

2012-05-18

460

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

Code of Federal Regulations, 2011 CFR

...hydrochloride (PHMB)(CAS Reg. No. 32289-58-0) is exempt from the requirement of a tolerance for residues of the antimicrobial in or on all food commodities when the residues are the result of the lawful application of a food contact surface...

2011-07-01