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1

Stability indicating method for determination of nortriptyline hydrochloride using 3-methyl-2-benzothiazolinone hydrazone (MBTH).  

PubMed

A spectrophotometric procedure is described for determination of nortriptyline hydrochloride in pure and dosage form as well as in the presence of its degradate. 3-Methyl-2-benzothiazolinone hydrazone (MBTH) has been used as the chromogenic reagent, where aqueous solutions of the drug and reagent are treated with cerium(IV) ammonium sulphate in an acidic medium. Nortriptyline hydrochloride reacts to give a blue coloured product having two absorption maxima at 619 and 655 nm. Various parameters affecting the reaction have been studied. Beer's law is obeyed in the concentration range of 24-216 microg ml(-1) of nortriptyline hydrochloride, with mean percentage recoveries of 100.22+/-0.870 and 100.66+/-0.642% for both maxima, 619 and 655 nm, respectively. Results were statistically analyzed and compared with those obtained by applying the British Pharmacopoeia (1993) method. PMID:11274868

El Ragehy, N A; Abbas, S S; El-Khateeb, S Z

2001-04-01

2

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

PubMed

A modified and highly sensitive spectrophotometric method for the determination of nitrate in trace quantities in environmental samples is described. The method is based on the reaction of nitrate ion with brucine and 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in sulfuric acid medium to yield a violet-colored product which is stable for over two days. The optimum photometric range for the determination of nitrate is 0.04-0.16 microg cm(-3) and the Sandell's sensitivity being 0.000279 microg cm(-2). The proposed method is applied to various water samples and the results indicate that the reaction is highly sensitive than the original brucine method. PMID:12834245

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

2003-06-01

3

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

NASA Astrophysics Data System (ADS)

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

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

2010-11-01

4

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

PubMed

We here describe a new spectrophotometric method for measuring total bilirubin in serum. The method is based on the cleavage of bilirubin giving formaldehyde which further reacts with diazotized 3-methyl-2-benzothiazolinone hydrazone hydrochloride giving blue colored solution with maximum absorbance at 630 nm. Sensitivity of the developed method was compared with Jendrassik-Grof assay procedure and its applicability has been tested with human serum samples. Good correlation was attained between both methods giving slope of 0.994, intercept 0.015, and R(2)=0.997. Beers law obeyed in the range of 0.068-17.2 ?M with good linearity, absorbance y=0.044 C(bil)+0.003. Relative standard deviation was 0.006872, within day precision ranged 0.3-1.2% and day-to-day precision ranged 1-6%. Recovery of the method varied from 97 to 102%. The proposed method has higher sensitivity with less interference. The obtained product was extracted and was spectrally characterized for structural confirmation with FT-IR, H NMR. PMID:20829101

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

2010-11-01

5

Development of a selective and sensitive spectrophotometric method for the trace determination of thallium(III) using 3-methyl-2-benzothiazolinone hydrazone hydrochloride and N-(1-naphthyl)-ethylenediamine dihydrochloride.  

PubMed

A simple, selective, sensitive, and rapid spectrophotometric method has been developed for the determination of thallium(III) using 3-methyl-2-benzothiazolinone hydrazone hydrochloride and N-(1-naphthyl)-ethylenediamine dihydrochloride. The obtained product had an absorption maximum of 590 nm. Beer's law was valid over the concentration range of 0.15-8 microg/mL. The molar absorptivity and Sandell's sensitivity of the colored system were 2.93 x 10(4) L/mol x cm and 0.00723 microg/mL, respectively. The effect of different acids on the sensitivity of the method, interference by foreign substances, the optimum reaction conditions, and other analytical parameters were evaluated. The proposed method has been successfully applied in the analysis of T1(III) in standard reference materials, synthetic mixtures, and water and urine samples. The performance of the proposed method was evaluated in terms of Student's t-test and variance ratio F-test, which indicated the significance of the proposed method over reported methods. PMID:18980127

Nagaraja, Padmarajaiah; Al-Tayar, Naef Ghllab Saeed; Kumar, Anantharaman Shiva

2008-01-01

6

Determination of ultratrace amounts of copper (II) by its catalytic effect on the oxidative coupling reaction of 3-methyl-2-benzothiazolinone hydrazone with N-ethyl-N-(2-hydroxy-3-sulfopropyl)-3,5-dimethoxyaniline.  

PubMed

A spectrophotometric method was developed for the determination of ultratrace amounts of copper(II) based on its catalytic effect on the oxidative coupling reaction of 3-methyl-2-benzothiazolinone hydrazone with N-ethyl-N-(2-hydroxy-3-sulfopropyl)-3,5-dimethoxyaniline to produce an intensely coloured dye (lambda(max) = 525 nm) in the presence of hydrogen peroxide. In this reaction, pyridine acted as an effective activator for the catalysis of copper(II). By measuring the absorbance of the dye, copper(II) can be determined at the 0.002-0.1 ng cm(-3) (3.1 x 10(-11)-1.6 x 10(-9) mol dm(-3) level. The relative standard deviation for ten determinations of 0.06 ng cm(0-3) of copper(II) was 2.6%. The proposed method was successfully applied to the determination of copper(II) in tap water and biological material. PMID:9148646

Ohno, S; Teshima, N; Watanabe, T; Itabashi, H; Nakano, S; Kawashima, T

1996-10-01

7

Determination of doxorubicin hydrochloride by visible spectrophotometry.  

PubMed

Four simple and sensitive visible spectrophotometric methods (A-D) have been described for the assay of doxorubicin hydrochloride either in pure form or in pharmaceutical formulations. Method A was developed based on oxidation of the drug with Fe(III) to produce Fe(II), which subsequently reacts with 1.10-ortho-phenanthroline to form a red colored complex (lambda(max): 510 nm) at pH 4.6. Method B involves the reduction of Folin-Ciocalteu (F-C) reagent by the drug and the reduced species formed possesses a characteristic intense blue color (lambda(max): 770 nm). In methods C and D. oxidation of the drug with periodate at specified experimental conditions yields formaldehyde and dialdehyde, which in turn react either with 3-methyl-2-benzothiazolinone hydrazone hydrochloride to form an intensely brilliant blue cationic dye (lambda(max): 620-670 nm. method C) or by condensation with phenylhydrazine hydrochloride (PHH) to form orange-red colored product (lambda(max): 510 nm, method D) in the presence of potassium ferricyanide. All of the variables have been optimized and the reaction mechanisms presented. The concentration measurements are reproducible within a relative standard deviation of 1.0%. PMID:18966670

Sastry, C S; Lingeswara Rao, J S

1996-11-01

8

Spectrophotometric methods for the determination of prazosin hydrochloride in tablets.  

PubMed

Four simple and sensitive methods for the assay of prazosin hydrochloride (PRH) are developed. These methods are based on the formation of coloured species by treating it either with excess N-bromosuccinimide (NBS) and determining the unconsumed NBS with p-N-methyl aminophenol sulphate (metol)-sulphanilamide (SA) reagent (method A, lambda(max) 520 nm): with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in the presence of eerie ammonium sulphate (CAS) (method B, lambda(max) 620 nm) or with acidic dyes such as orange-II (O-II) (method C, lambda(max) 490 nm) and alizarin violet 3B (AV-3B) (method D, lambda(max) 570 nm) under the specified experimental conditions. Regression analysis of Beer's law plot showed good correlation in the concentration range of 1.0-10.0, 2.5-25.0, 1.0-17.5 and 2.5-30.0 mug ml for methods A, B, C and D respectively. PMID:18966673

Sreedhar, K; Sastry, C S; Narayana Reddy, M; Sankar, D G

1996-11-01

9

Spectrophotometric Analysis of Diclofenac Sodium and Piroxicam and Their Pharmaceutical Preparations  

Microsoft Academic Search

Simple spectrophotometric methods for the determination of diclofenac sodium and piroxicam in bulk samples and pharmaceutical preparations, based on the formation of colored species with 3-methyl-2-benzothiazolinone hydra-zone hydrochloride - Ce, are presented. The methods are simple, sensitive, rapid and accurate. The results obtained are reproducible with a coefficient of variation less than 2%.

Suryaprakasa Sastry; A. Rama Mohana Rao; T. N. V. Prasad

1987-01-01

10

Spectrophotometric methods for the rapid determination of menadione and menadione sodium bisulphite and their application in pharmaceutical preparations  

Microsoft Academic Search

Two simple, rapid and sensitive spectrophotometric determination of menadione and its sodium bisulphite derivative (MSB) have been carried out. The first method involves the reaction of menadione and its sodium bisulphite derivative with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) is sodium hydroxide medium to give blue coloured product having maximum absorption at 625 nm and the coloured species is stable for more

P Nagaraja; R. A Vasantha; H. S Yathirajan

2002-01-01

11

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

PubMed

New, accurate, sensitive and reliable kinetic spectrophotometric method for the assay of moxifloxacin hydrochloride (MOXF) in pure form and pharmaceutical formulations has been developed. The method involves the oxidative coupling reaction of MOXF with 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH) in the presence of Ce(IV) in an acidic medium to form colored product with lambda max at 623 and 660nm. The reaction is followed spectrophotometrically by measuring the increase in absorbance at 623nm as a function of time. The initial rate and fixed time methods were adopted for constructing the calibration curves. The linearity range was found to be 1.89-40.0?gmL(-1) for initial rate and fixed time methods. The limit of detection for initial rate and fixed time methods is 0.644 and 0.043?gmL(-1), respectively. Molar absorptivity for the method was found to be 0.8910(4)Lmol(-1)cm(-1). Statistical treatment of the experimental results indicates that the methods are precise and accurate. The proposed method has been applied successfully for the estimation of moxifloxacin hydrochloride in tablet dosage form with no interference from the excipients. The results are compared with the official method. PMID:25596545

Ashour, Safwan; Bayram, Roula

2015-04-01

12

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

13

Selective and validated spectrophotometric methods for the determination of nicorandil in pharmaceutical formulations.  

PubMed

Two simple and sensitive validated spectrophotometric methods have been described for the assay of nicorandil in drug formulations. Method A is based on the reaction of the drug with phloroglucinol-sulfanilic acid reagent in sulfuric acid medium to give yellow-colored product, which absorbs maximally at 425 nm. Method B uses the oxidative coupling of 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) with DL- 3,4 - dihydroxyphenylalanine (DL-dopa) in the presence of nicorandil as oxidant in sulfuric acid medium to form an intensely colored product having maximum absorbance at 530 nm. Beer's law is obeyed in the concentration range 2.5 to 50.0 and 1.0 to 15.0 microg mL(-1) with methods A and B, respectively. Both methods have been successfully applied for the analysis of drug in pharmaceutical formulations. The reliability and the performance of the proposed methods are established by point and interval hypothesis and through recovery studies. The experimental true bias of all samples is smaller than +/-2%. PMID:15760099

Rahman, Nafisur; Ahmad, Yasmin; Azmi, Syed Najmul Hejaz

2004-01-01

14

Optimized and validated spectrophotometric methods for the determination of nicorandil in drug formulations and biological fluids.  

PubMed

Two simple, sensitive and economical spectrophotometric methods have been developed for the determination of nicorandil in drug formulations and biological fluids. Method A is based on the reaction of the drug with brucine-sulphanilic acid reagent in sulphuric acid medium producing a yellow-coloured product, which absorbs maximally at 410 nm. Method B depends on the formation of the intensely blue-coloured product which results due to the interaction of an electrophilic intermediate of 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) with oxidized product of 4-(methyl amino) phenol sulphate (metol) in the presence of nicorandil as an oxidizing agent in sulphuric acid medium. The coloured product shows absorbance maximum at 560 nm. Under the optimized experimental conditions, Beer's law is obeyed in the concentration range of 2.5-35.0 and 0.40-2.2 microg ml(-1) for Methods A and B, respectively. Both the methods have been successfully applied to the determination of nicorandil in drug formulations and biological fluids. The results are validated statistically and through recovery studies. In order to establish the bias and the performance of the proposed methods, the point and interval hypothesis tests have been performed. The experimental true bias of all samples is smaller than +/-2%. PMID:15231427

Rahman, Nafisur; Ahmad Khan, Nadeem; Hejaz Azmi, Syed Najmul

2004-07-01

15

Glucosamine hydrochloride  

MedlinePLUS

... a combination of glucosamine hydrochloride, chondroitin sulfate, and manganese ascorbate. Some evidence suggests that this combination can ... amount of glucosamine or contain excessive amounts of manganese. Ask your healthcare provider about reliable brands. Some ...

16

Chromogenic substrates for horseradish peroxidase.  

PubMed

Two new detection systems for horseradish peroxidase (HRP) have been developed for the staining of membranes used in immunoassays. These systems use dimethyl or diethyl analogues of p-phenylenediamine with 4-chloro-1-naphthol to generate a blue product or 3-methyl-2-benzothiazolinone hydrazone with 4-chloro-1-naphthol to generate a red product. These reagents offer increased sensitivity and lower background staining than currently available chromogenic detection substrates. In addition, the incorporation of these substrates increases the sensitivity of HRP labels to be comparable to that of alkaline phosphatase with the 5-bromo-4-chloro-3-indolyl phosphate + nitro blue tetrazolium substrate. PMID:2048722

Conyers, S M; Kidwell, D A

1991-01-01

17

Spectrophotometric determination of urinary oxalate with oxalate oxidase prepared from moss.  

PubMed

A novel spectrophotometric enzymic procedure for estimating oxalic acid in urine is described. Oxalate oxidase, prepared from moss species, converts oxalic acid to hydrogen peroxide and carbon dioxide. Hydrogen peroxide is determined enzymatically with horseradish peroxidase, by oxidative coupling of 3-methyl-2-benzothiazolinone hydrazone with N,N-dimethylaniline; the resulting indamine due is determined spectrophotometrically at 595 nm. Interfering substances are removed by adsorption to ion-exchange resins and oxidation with charcoal, thus avoiding oxalate recovery problems accompanying oxalate isolation. The procedure is rapid, sensitive, linear, and precise. Results agreed well with those obtained with a widely used chemical technique. PMID:7379303

Laker, M F; Hofmann, A F; Meeuse, B J

1980-06-01

18

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

PubMed

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

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

2005-01-01

19

Ketamine Hydrochloride and Xylazine Hydrochloride  

Microsoft Academic Search

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

Jerrold L. Belant

20

Research on the Synthesis of Aromatic Hydrazone in Ionic Liquids  

Microsoft Academic Search

Aromatic hydrazones are important intermediates for pesticides cibenzoline and cefxime. The methodology of synthesis of aromatic hydrazone from aromatic ketone and hydrazine hydrate in ionic liquid, was described and various aromatic hydrazones were prepared by the reaction of aromatic ketone with hydrazine hydrate in ionic 1iquid at 100C with good yields. The ionic liquids could be recycled and reused after

Haibin Wang; Li Sun; Xiaonian Li; Jiangli Duan; Wen Pei

2011-01-01

21

A sensitive spectrophotometric assay for guanase activity.  

PubMed

A highly sensitive and accurate spectrophotometric method was developed for determination of guanase activity with guanine as substrate. The assay is based on the oxidative coupling of 3-methyl-2-benzothiazolinone hydrazone and N,N-diethylaniline. Xanthine formed from guanine by guanase is oxidized to uric acid and hydrogen peroxide by xanthine oxidase, and the hydrogen peroxide produced is determined by an oxidative-coupling reaction with 3-methyl-2-benzothiazolinone hydrazone and N,N-diethylaniline mediated by peroxidase. Formation of the indamine dye is greatly affected by the superoxide radical ion (O2-) and pH value. These problems can be overcome by separating the two reactions of hydrogen peroxide formation and color production and carrying out that color-producing reaction at pH 3.0. This method is very sensitive and accurate because the indamine dye has a very high molar extinction coefficient of 29,800. It can be used with various kinds of automatic analyzers such as a Hitachi, Olympus, or Technicon analyzer. Comparative studies showed that this method is more sensitive and reproducible than other methods. Furthermore, guanase activities determined by this method correlated well with those determined by the improved Ellis-Goldberg method. This method should be useful for measurement of guanase activity in banked blood for preventing transfusion hepatitis and could be valuable as a liver function test. PMID:6869816

Ando, T; Muraoka, T; Okuda, H

1983-04-15

22

Synthesis of lipopeptides using hydrazone chemical ligation.  

PubMed

In this paper we report that a hydrazinopeptide synthesized using solid-phase N-electrophilic amination with N-Boc-3-(4-cyanophenyl)oxaziridine reacted with a lipophilic peptide aldehyde to give the corresponding hydrazone plus an unexpected 1,3,4-oxadiazolidinopeptide containing two peptide aldehyde units. This methodology allows the synthesis of large lipopeptides. PMID:9774230

Melnyk, O; Bossus, M; David, D; Rommens, C; Gras-Masse, H

1998-09-01

23

4-Hydroxyanisole: the most suitable monophenolic substrate for determining spectrophotometrically the monophenolase activity of polyphenol oxidase from fruits and vegetables.  

PubMed

A continuous spectrophotometric method for determining the monophenolase activity of polyphenol oxidase from several plant sources is described. This assay method is based on the coupling reaction between 3-methyl-2-benzothiazolinone hydrazone and the quinone product of the oxidation of 4-hydroxyanisole in the presence of polyphenol oxidase. 4-Hydroxyanisole proved to be the best monophenol assayed to measure the monophenolase activity of polyphenol oxidase from apple, artichoke, avocado, medlar, pear, and strawberry. Kinetic constants of 4-hydroxyanisole were compared to those of p-hydroxyphenyl propionic acid, a very sensitive monophenol previously reported to assay the monophenolase activity of polyphenol oxidase from apple, pear, and mushroom. The high values of the maximum steady state rate obtained for 4-hydroxyanisole suggest the existence of high catalytic constant toward this monophenol. These kinetic values were supported by nuclear magnetic resonance assays which predicted the highest reactivity of 4-hydroxyanisole. Therefore nuclear magnetic resonance assays proved to be a valuable and useful tool to predict the best monophenolic substrate for plant polyphenol oxidases. The 3-methyl-2-benzothiazlolinone-adduct for 4-hydroxyanisole was stable, with high molar absorptivity at the optimum pHs of the polyphenol oxidases assayed. All this together makes the use of 4-hydroxyanisol as monophenolic substrate and 3-methyl-2-benzothiazolinone as coupling reagent the most sensitive and precise assay method up to date reported in the literature to determine the monophenolas activity of polyphenol oxidase from fruits and vegetables. PMID:9606152

Espn, J C; Tudela, J; Garca-Cnovas, F

1998-05-15

24

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

Code of Federal Regulations, 2010 CFR

...2010-04-01 2010-04-01 false Ketamine hydrochloride with promazine hydrochloride...FORM NEW ANIMAL DRUGS 522.1222b Ketamine hydrochloride with promazine hydrochloride...injection. (a) Chemical name. Ketamine hydrochloride,...

2010-04-01

25

Biomimetic Modeling of Copper Complexes: A Study of Enantioselective Catalytic Oxidation on D-(+)-Catechin and L-( ? )-Epicatechin with Copper Complexes  

PubMed Central

The biomimetic catalytic oxidations of the dinuclear and trinuclear copper(II) complexes versus two catechols, namely, D-(+)-catechin and L-( ? )-epicatechin to give the corresponding quinones are reported. The unstable quinones were trapped by the nucleophilic reagent, 3-methyl-2-benzothiazolinone hydrazone (MBTH), and have been calculated the molar absorptivities of the different quinones. The catalytic efficiency is moderate, as inferred by kinetic constants, but the complexes exhibit significant enantio-differentiating ability towards the catechols, albeit for the dinuclear complexes, this enantio-differentiating ability is lower. In all cases, the preferred enantiomeric substrate is D-(+)-catechin to respect the other catechol, because of the spatial disposition of this substrate. PMID:18825268

Mutti, Francesco G.; Pievo, Roberta; Sgobba, Maila; Gullotti, Michele; Santagostini, Laura

2008-01-01

26

Membrane solubilization technique for spectrophotometric determination of trace formaldehyde in rainwater.  

PubMed

A simple and sensitive spectrophotometry for formaldehyde in water by membrane solubilization technique was proposed. Formaldehyde was converted into a blue cationic dye with 3-methyl-2-benzothiazolinone hydrazone, and the dye was retained on a membrane filter as an ion-associate with tetraphenylborate anion. The filter retaining the blue dye was dissolved in 2-methoxyethanol containing sulfuric acid, and the absorbance of the solution was measured at 670 nm against the reagent blank. The formaldehyde from 0.007 to 0.2 mg L(-1) was determined with an RSD of less than 5%, and the detection limit was 0.002 mg L(-1). The proposed method was very simple and rapid. Twenty minutes was sufficient for the entire analytical procedure. When the method was applied to rainwater, the analytical results were in good agreement with those obtained by GC/MS. PMID:18997375

Murai, Keita; Okano, Mayumi; Kuramitz, Hideki; Hata, Noriko; Kawakami, Takanori; Taguchi, Shigeru

2008-01-01

27

Continuous-flow assay for urinary oxalate using immobilised oxalate oxidase.  

PubMed

A continuous-flow assay for measuring oxalate in urine is described. Covalently attached oxalate oxidase (EC 1.2.3.4) is used to oxidize the oxalate anion to carbon dioxide and hydrogen peroxide. The formed hydrogen peroxide is measured colorimetrically (A580) with an established reaction using horseradish peroxidase (EC 1.11.17), 3-methyl-2-benzothiazolinone hydrazone (MBTH) and 3-dimethylaminobenzoic acid (DMAB). Ascorbate interference is eliminated by treating the urine sample with sodium nitrite prior to assaying. The assay is accurate (mean recovery of added oxalate in spiked urine sample is 93 +/- 11%), sensitive (detection limit 1.0 mumol/L), reproducible (within-batch CV 3.5%; between-batch CV 5%) and relatively rapid (15 samples/h). This assay correlates well (R = 0.99) with another established enzymatic method (using oxalate decarboxylase). PMID:4037668

Kasidas, G P; Rose, G A

1985-07-01

28

Optical determination of L-tyrosine based on eggshell membrane immobilized tyrosinase.  

PubMed

An optical biosensor based on the eggshell membrane immobilized tyrosinase is described for the detection of L-tyrosine (L-Tyr). The detection scheme was based on the measurement of absorption value of color adduct resulting from the reaction of 3-methyl-2-benzothiazolinone hydrazone and dopa-quinone produced from the enzymatic oxidation of L-Tyr. The prepared biosensor demonstrated optimum activity at pH 7, optimum temperature range of 20-40 degrees C and a linear response for the L-Tyr concentration in range of 5-200 microM. It also showed good operation stability for repeated measurements (over 300 times) and storage stability after it had been kept at 4 degrees C for 3 months. PMID:21313820

Li, Yong Jin

2010-01-01

29

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

PubMed

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

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

2011-10-26

30

Biomimetic modeling of copper complexes: a study of enantioselective catalytic oxidation on d-(+)-catechin and L-( - )-epicatechin with copper complexes.  

PubMed

The biomimetic catalytic oxidations of the dinuclear and trinuclear copper(II) complexes versus two catechols, namely, D-(+)-catechin and L-( - )-epicatechin to give the corresponding quinones are reported. The unstable quinones were trapped by the nucleophilic reagent, 3-methyl-2-benzothiazolinone hydrazone (MBTH), and have been calculated the molar absorptivities of the different quinones. The catalytic efficiency is moderate, as inferred by kinetic constants, but the complexes exhibit significant enantio-differentiating ability towards the catechols, albeit for the dinuclear complexes, this enantio-differentiating ability is lower. In all cases, the preferred enantiomeric substrate is D-(+)-catechin to respect the other catechol, because of the spatial disposition of this substrate. PMID:18825268

Mutti, Francesco G; Pievo, Roberta; Sgobba, Maila; Gullotti, Michele; Santagostini, Laura

2008-01-01

31

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

32

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 PMID:16349330

Daniel, Geoffrey; Volc, Jindrich; Kubatova, Elena

1994-01-01

33

Pyrroloquinoxaline hydrazones as fluorescent probes for amyloid fibrils.  

PubMed

Here we describe the identification and preliminary characterization of a new class of pyrrolo(imidazo)quinoxaline hydrazones as florescent probes for A?(1-42) fibrils. All the newly developed compounds were able to bind amyloid fibrils formed in vitro and some of them displayed an increase of their fluorescence upon binding. When tested on brain tissue preparations presenting A? deposits, the described hydrazones selectively stained amyloid structures and did not display aspecific binding. The hydrazones did not show antifibrillogenic activity and electron microscopy analysis revealed that they do not interfere with fibrils structure. The described pyrrolo(imidazo)quinoxalines could be useful for studying amyloid structures in vitro. Moreover, their experimentally proven ability to cross the blood-brain barrier in mouse opens the possibility of developing these compounds as potential amyloid imaging agents for in vivo applications. PMID:21629961

Gemma, Sandra; Colombo, Laura; Forloni, Gianluigi; Savini, Luisa; Fracasso, Claudia; Caccia, Silvio; Salmona, Mario; Brindisi, Margherita; Joshi, Bhupendra P; Tripaldi, Pierangela; Giorgi, Gianluca; Taglialatela-Scafati, Orazio; Novellino, Ettore; Fiorini, Isabella; Campiani, Giuseppe; Butini, Stefania

2011-07-21

34

USE OF YOHIMBINE HYDROCHLORIDE TO REVERSE IMMOBILIZATION OF POLAR BEARS BY KETAMINE HYDROCHLORIDE AND XYLAZINE HYDROCHLORIDE  

Microsoft Academic Search

Yohimbine hydrochloride (YH) effectively reversed the immobilizing effects of ke- tamine hydrochloride (KH) combined with xylazine hydrochloride (XH) in 48 wild polar bears (Ursus maritimus) handled in the summer. Single intravenous doses of YH ranging between 0.029 and 0.198 mg\\/kg resulted in a median time of 10 mm (range: 1-123 mm) to post-injection recovery from KH-XH immobilization. Convulsions and muscle

Malcolm A. Ramsay; Ian Stirling; Eric Broughton

35

SPECTROPHOTOMETRIC AND STABILITY INDICATING HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC DETERMINATION OF NORTRIPTYLINE HYDROCHLORIDE AND FLUPHENAZINE HYDROCHLORIDE  

Microsoft Academic Search

Spectrophotometric and high performance liquid chromatographic procedures are described for determination of nortriptyline hydrochloride and fluphenazine hydrochloride. The first procedure is based on application of first derivative of ratio spectra (DD) for quantitative determination of nortriptyline hydrochloride in presence of fluphenazine hydrochloride. Secondly, an accurate, sensitive and stability indicating method has been introduced for determination of nortriptyline hydrochloride and fluphenazine

Nariman A. El-Ragehy; Samah S. Abbas; Sonia Z. El-Khateeb

2002-01-01

36

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

37

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; Hernndez, Armando R; Kool, Eric T

2012-09-19

38

Diaryl hydrazones as multifunctional inhibitors of amyloid self-assembly.  

PubMed

The design and application of an effective, new class of multifunctional small molecule inhibitors of amyloid self-assembly are described. Several compounds based on the diaryl hydrazone scaffold were designed. Forty-four substituted derivatives of this core structure were synthesized using a variety of benzaldehydes and phenylhydrazines and characterized. The inhibitor candidates were evaluated in multiple assays, including the inhibition of amyloid ? (A?) fibrillogenesis and oligomer formation and the reverse processes, the disassembly of preformed fibrils and oligomers. Because the structure of the hydrazone-based inhibitors mimics the redox features of the antioxidant resveratrol, the radical scavenging effect of the compounds was evaluated by colorimetric assays against 2,2-diphenyl-1-picrylhydrazyl and superoxide radicals. The hydrazone scaffold was active in all of the different assays. The structure-activity relationship revealed that the substituents on the aromatic rings had a considerable effect on the overall activity of the compounds. The inhibitors showed strong activity in fibrillogenesis inhibition and disassembly, and even greater potency in the inhibition of oligomer formation and oligomer disassembly. Supporting the quantitative fluorometric and colorimetric assays, size exclusion chromatographic studies indicated that the best compounds practically eliminated or substantially inhibited the formation of soluble, aggregated A? species, as well. Atomic force microscopy was also applied to monitor the morphology of A? deposits. The compounds also possessed the predicted antioxidant properties; approximately 30% of the synthesized compounds showed a radical scavenging effect equal to or better than that of resveratrol or ascorbic acid. PMID:23346953

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

2013-02-19

39

Possible Side Effects of Cyclophosphamide, Topotecan Hydrochloride  

Cancer.gov

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

40

21 CFR 556.350 - Levamisole hydrochloride.  

Code of Federal Regulations, 2011 CFR

...DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs 556.350 Levamisole hydrochloride. A tolerance of 0...per million is established for negligible residues of levamisole hydrochloride in the edible tissues...

2011-04-01

41

21 CFR 556.350 - Levamisole hydrochloride.  

Code of Federal Regulations, 2010 CFR

...DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs 556.350 Levamisole hydrochloride. A tolerance of 0...per million is established for negligible residues of levamisole hydrochloride in the edible tissues...

2010-04-01

42

21 CFR 556.350 - Levamisole hydrochloride.  

Code of Federal Regulations, 2013 CFR

...DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs 556.350 Levamisole hydrochloride. A tolerance of 0...per million is established for negligible residues of levamisole hydrochloride in the edible tissues...

2013-04-01

43

21 CFR 556.350 - Levamisole hydrochloride.  

Code of Federal Regulations, 2012 CFR

...DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs 556.350 Levamisole hydrochloride. A tolerance of 0...per million is established for negligible residues of levamisole hydrochloride in the edible tissues...

2012-04-01

44

21 CFR 556.350 - Levamisole hydrochloride.  

Code of Federal Regulations, 2014 CFR

...DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs 556.350 Levamisole hydrochloride. A tolerance of 0...per million is established for negligible residues of levamisole hydrochloride in the edible tissues...

2014-04-01

45

21 CFR 520.2002 - Propiopromazine hydrochloride.  

Code of Federal Regulations, 2014 CFR

...degree of tranquilization desired. Note: Not for use with organophosphates and/or procaine hydrochloride, as phenothiazine may potentiate the toxicity of organophosphates and the activity of procaine hydrochloride. Overdosage may...

2014-04-01

46

IMMOBILIZATION OF SWIFT FOXES WITH KETAMINE HYDROCHLORIDE-XYLAZINE HYDROCHLORIDE  

Microsoft Academic Search

There is an increasing need to develop field immobilization techniques that allow researchers to handle safely swift foxes (Vulpes velox) with minimal risk of stress or injury. We immobilized captive swift foxes to determine the safety and effectiveness of ketamine hydrochlo- ride and xylazine hydrochloride at different dosages. We attempted to determine appropriate dosages to immobilize swift foxes for an

Rebecca L. Telesco; Marsha A. Sovada

2002-01-01

47

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. PMID:21846387

2011-01-01

48

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

Code of Federal Regulations, 2012 CFR

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

2012-04-01

49

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

Code of Federal Regulations, 2013 CFR

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

2013-04-01

50

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

Code of Federal Regulations, 2011 CFR

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

2011-04-01

51

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

52

Betahistine hydrochloride in Mnire's disease  

Microsoft Academic Search

A double-blind, placebo-controlled, cross-over clinical trial was performed to assess the effect of betahistine hydrochloride (Serc) in Mnire's disease. The diagnosis was based on paroxysmal attacks of rotational vertigo, with tinnitus, and a fluctuating sensori-neural deafness, together with the results of auditory and vestigular tests. Twenty-eight patients were admitted to the trial over 3 years. Twenty-two patients completed the trial.

I. J. Frew; G. N. Menon

1976-01-01

53

Polarographic estimation of antazoline hydrochloride.  

PubMed

The dc-polarographic investigation of antazoline hydrochloride in aqueous acidic media is described. Using potassium chloride-hydrochloric acid mixture as the supporting electrolyte (pH = 3.25), antazoline hydrochloride was electrochemically reduced at the dropping mercury electrode, with the production of two waves with E1/2 values of --1.35 and --1.65 V respectively. As revealed from the study of the effect of mercury column height, pH of the medium and concentration of the depolarizer, the polarographic reduction of the antazolinium cation is preceded by a catalytic H-wave. The diffusion-controlled nature of the electrode process permitted the quantitative determination of antazoline hydrochloride in concentrations down to 1.0 . 10(-4)M. Application of the presented procedure to the analysis of different dosage forms of the compound studied proved successful and compared favourably with official estimations of anatazoline salts. In view of its simplicity, accuracy and sensitivity, the presented polarographic method can be recommended for routine analysis of antazoline formulations. PMID:31632

Issa, I M; Omar, N M; El-Shabouri, S R; Atwa, N I

1978-08-01

54

Transformation of ketones and aldehydes to gem-dihalides via hydrazones using copper(II) halides  

Microsoft Academic Search

Preparation of gem-dihalides by the oxidation of hydrazones which were easily prepared by the treatment of ketones and aldehydes with hydrazine hydrate in the presence of molecular sieves 4A. with copper(II) compounds was studied. The treatment of hydrazones with copper(II) bromide-lithium tert-butoxide in THF gave the corresponding gem-dibromides in good yields. gem-Dichlorides were also obtained by the similar reaction of

Takeshi Takeda; Rika Sasaki; Satoshi Yamauchi; Tooru Fujiwara

1997-01-01

55

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. Gzin; zcan, Servet; Karacan, Nurcan

2012-12-01

56

Group X Aldehyde Dehydrogenases of Pseudomonas aeruginosa PAO1 Degrade Hydrazones  

PubMed Central

Hydrazones are natural and synthetic compounds containing a C=N-N moiety. Here we found that the opportunistic pathogen Pseudomonas aeruginosa PAO1 produced NAD+- or NADP+-dependent hydrazone dehydrogenase (HDH), which converts hydrazones to the corresponding hydrazides and acids rather than to the simple hydrolytic product aldehydes. Gene cloning indicated that the HDH is part of the group X aldehyde dehydrogenase (ALDH) family, which is distributed among bacteria, although the physiological roles of the ALDH family remain unknown. The PAO1 strain upregulated HDH in the presence of the hydrazone adipic acid bis(ethylidene hydrazide) (AEH). Gene disruption of the HDH-encoding hdhA (PA4022) decreased growth rates in culture medium containing AEH as the sole carbon source, and this effect was more obvious in the double gene disruption of hdhA and its orthologous exaC (PA1984), indicating that these genes are responsible for hydrazone utilization. Recombinant proteins of group X ALDHs from Escherichia coli, Paracoccus denitrificans, and Ochrobactrum anthropi also acted as HDHs in that they produced HDH activity in the cells and degraded hydrazones. These findings indicated the physiological roles of group X ALDHs in bacteria and showed that they comprise a distinct ALDH subfamily. PMID:22267508

Taniyama, Kosuke; Itoh, Hideomi; Takuwa, Atsushi; Sasaki, Yasuyuki; Yajima, Shunsuke; Toyofuku, Masanori; Nomura, Nobuhiko

2012-01-01

57

Gold(I)-Catalyzed Intermolecular Cycloaddition of Allenamides with ?,?-Unsaturated Hydrazones: Efficient Access to Highly Substituted Cyclobutanes  

PubMed Central

?,?-Unsaturated N,N-dialkyl hydrazones undergo a mild [2 + 2] cycloaddition to allenamides when treated with a suitable gold catalyst. The method, which represents the first application of N,N-dialkyl hydrazones in gold catalysis, is compatible with a wide variety of substituents at the alkenyl moiety of the hydrazone component, proceeds with excellent levels of regio- and diastereoselectivity, and provides densely substituted cyclobutanes with good to excellent yields. PMID:25406491

2014-01-01

58

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

59

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

USGS Publications Warehouse

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

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

1985-01-01

60

Simple hydrazone building blocks for complicated functional materials.  

PubMed

CONSPECTUS: The ability to selectively and effectively control various molecular processes via specific stimuli is a hallmark of the complexity of biological systems. The development of synthetic structures that can mimic such processes, even on the fundamental level, is one of the main goals of supramolecular chemistry. Having this in mind, there has been a foray of research in the past two decades aimed at developing molecular architectures, whose properties can be modulated using external inputs. In most cases, reversible conformational, configurational, or translational motions, as well as bond formation or cleavage reactions have been used in such modulations, which are usually initiated using inputs including, irradiation, metalation, or changes in pH. This research activity has led to the development of a diverse array of impressive adaptive systems that have been used in showcasing the potential of molecular switches and machines. That being said, there are still numerous obstacles to be tackled in the field, ranging from difficulties in getting molecular switches to communicate and work together to complications in integrating and interfacing them with surfaces and bulk materials. Addressing these challenges will necessitate the development of creative new approaches in the field, the improvement of the currently available materials, and the discovery of new molecular switches. This Account will describe how our quest to design new molecular switches has led us to the development of structurally simple systems that can be used for complicated functions. Our focus on the modular and tunable hydrazone functional group was instigated by the desire to simplify the structure and design of molecular switches in order to circumvent multistep synthesis. We hypothesized that by avoiding this synthetic bottleneck, which is one of the factors that hinder fast progress in the field, we can expedite the development and deployment of our adaptive materials. It should be noted though that designing structurally simple switches cannot be an end goal by itself! Therefore, we showed that our molecules can be used in applications that are beyond a simple molecular switching event (i.e., the control of the photophysical properties of liquid crystals and multistep switching cascades). While focusing on these switches, we discovered that the hydrazones can be easily transformed, using straightforward one-step reactions, into visible light activated azo switches, and two different families of fluorophores that can be used in sensing applications. These findings demonstrate that our approach of developing simple systems for sophisticated functions is not limited to the field of molecular switches and machines but can also encompass other adaptive materials. PMID:24766362

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

2014-07-15

61

FUNCTIONALIZED BETA-C-GLYCOSIDIC KETONE HYDRAZONES: NOVEL DERIVATIVES FOR CARBOHYDRATE ANALYSIS BY MALDI-TOF MASS SPECTROMETRY  

Technology Transfer Automated Retrieval System (TEKTRAN)

Hydrazones constitute one of the best derivatives for the analysis of aldehydes and ketones yielding crystalline solids that are readily precipitated from water. Unlike simple aldehydes and ketones, sugars do not usually form simple hydrazones. They react with three equivalents of aryl- or acylhyd...

62

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

63

Immobilization of swift foxes with ketamine hydrochloride-xylazine hydrochloride.  

PubMed

There is an increasing need to develop field immobilization techniques that allow researchers to handle safely swift foxes (Vulpes velox) with minimal risk of stress or injury. We immobilized captive swift foxes to determine the safety and effectiveness of ketamine hydrochloride and xylazine hydrochloride at different dosages. We attempted to determine appropriate dosages to immobilize swift foxes for an adequate field-handling period based on three anesthesia intervals (induction period, immobilization period, and recovery period) and physiologic responses (rectal temperature, respiration rate, and heart rate). Between October 1998-July 1999, we conducted four trials, evaluating three different dosage ratios of ketamine and xylazine (2.27:1.2, 5.68:1.2, and 11.4:1.2 mg/kg ketamine:mg/kg xylazine, respectively), followed by a fourth trial with a higher dosage at the median ratio (11.4 mg/kg ketamine: 2.4 mg/kg xylazine). We found little difference in induction and recovery periods among trials 1-3, but immobilization time increased with increasing dosage (P < 0.08). Both the immobilization period and recovery period increased in trial 4 compared with trials 1-3 (P < or = 0.03). There was a high variation in responses of individual foxes across trials, making it difficult to identify an appropriate dosage for field handling. Heart rate and respiration rates were depressed but all physiologic measures remained within normal parameters established for domestic canids. We recommend a dosage ratio of 10 mg/kg ketamine to 1 mg/kg xylazine to immobilize swift foxes for field handling. PMID:12528444

Telesco, Rebecca L; Sovada, Marsha A

2002-10-01

64

Solid-state characterization of falicaine hydrochloride and isomorphic dyclonine hydrochloride  

Microsoft Academic Search

Two homologous local anaesthetic drugs, falicaine (propipocaine) hydrochloride (1-(4-propoxyphenyl)-3-(1-piperidinyl)-1-propanone hydrochloride, PPCHC) and dyclonine hydrochloride (1-(4-butoxyphenyl)-3-(1-piperidinyl)-1-propanone hydrochloride, DCNHC) were characterized by thermal analysis (hot-stage-microscopy, differential scanning calorimetry, thermogravimetry), vibrational spectroscopic methods (FTIR-, FT-Raman-spectroscopy), powder X-ray diffractometry, solid-state-\\/solution-NMR and water-vapor sorption analysis. The formation and thermodynamic stability of the two different solid phases of both the compounds is described and presented in

Andrea C. Schmidt

2005-01-01

65

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

NASA Astrophysics Data System (ADS)

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

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

2014-11-01

66

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

67

21 CFR 520.2002 - Propiopromazine hydrochloride.  

Code of Federal Regulations, 2012 CFR

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

2012-04-01

68

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

69

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. PMID:23019473

Gorentla, Laxminarasimhulu; Dubey, Pramod K

2012-01-01

70

Propranolol hydrochlorideanionic polymer binding interaction  

Microsoft Academic Search

Three different anionic polymers namely Eudragit S 100, Eudragit L 100-55 (methacrylic acid copolymers), and sodium carboxymethylcellulose (NaCMC) were used to evaluate the propranolol hydrochlorideanionic polymer interaction. The physical and chemical properties of propranolol hydrochloride and anionic polymer complex were investigated using Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The DSC profiles demonstrated that the characteristic peak

Sevgi Takka

2003-01-01

71

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. PMID:21504614

2011-01-01

72

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

PubMed

Metal(II) coordination compounds of a tridentate hydrazone ligand (HL) derived from the condensation of cephalexin antibiotic with 2-hydrazinopyridine were synthesized. The hydrazone ligand and mononuclear [ML(OAc)(H2O)] (M(II)=Mn, Co, Ni, Cu, Zn, Ag) complexes were characterized by several techniques, including elemental and thermal analysis, molar conductance and magnetic susceptibility measurements, electronic, FT-IR, EPR and (1)H NMR spectral studies. The cephalexin 2-pyridinylhydrazone ligand HL behaves as a monoanionic tridentate NNO chelating agent. The biological applications of complexes have been studied on three bacteria strains (Escherichia coli, Acinetobacter baumannii and Enterococcus faecalis) by agar diffusion disc method. PMID:25677531

Anacona, J R; Rincones, Maria

2015-04-15

73

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

PubMed

A sensitive and simple flow-injection chemiluminescence (FI-CL) method, which was based on the CL intensity generated from the redoxreaction of potassium permanganate (KMnO4)-formaldehyde in vitriol (H2SO4) medium, has been developed, validated and applied for the determination of naphazoline hydrochloride and oxymetazoline hydrochloride. Besides oxidants and sensitizers, the effect of the concentration of H(2)SO(4), KMnO4 and formaldehyde was investigated. Under the optimum conditions, the linear range was 1.0 x 10(-2)-7.0 mg/L for naphazoline hydrochloride and 5.0 x 10(-2)-10.0 mg/L for oxymetazoline hydrochloride. During seven repeated inter-day and intra-day precision tests of 0.1, 1.0 and 10.0 mg/L samples, the relative standard deviations all corresponded to reference values. The detection limit was 8.69 x 10(-3) mg/L for naphazoline hydrochloride and 3.47 x 10(-2) mg/L for oxymetazoline hydrochloride (signal-to-noise ratio < or = 3). This method has been successfully implemented for the determination of naphazoline hydrochloride and oxymetazoline hydrochloride in pharmaceuticals. PMID:19253271

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

2009-01-01

74

An efficient large scale resolution of ()- threo-methylphenidate hydrochloride (Ritalin hydrochloride)  

Microsoft Academic Search

An efficient and large scale preparation of (2R,2?R)-(+)-threo-methylphenidate hydrochloride (3) by the resolution of ()-threo-methylphenidate hydrochloride (1) salt with O,O?-dibenzoyl-d-(+)-tartaric acid in the presence of 4-methylmorpholine is described.

Mahavir Prashad; Denis Har; Oljan Repic; Thomas J. Blacklock; Peter Giannousis

1999-01-01

75

Imipramine hydrochloride and desipramine hydrochloride as new reagents for detection of microamounts of blood in urine  

Microsoft Academic Search

Benzidine and o-tolidine, the hazardous carcinogens are still in use for the detection of blood in urine. Development of safer substitutes are of paramount importance. Unfortunately, the alternate available reagents lack specificity, sensitivity and reproducibility. Imipramine hydrochloride (IPH) and desipramine hydrochloride (DPH) are proposed as new reagents for the detection of blood in urine. Both the reagents impact to blood

Akheel A Syed; Mohammed F Silwadi; Bibi A Khatoon

2002-01-01

76

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

77

21 CFR 520.2582 - Triflupromazine hydrochloride tablets.  

Code of Federal Regulations, 2012 CFR

...2012-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and...520.2582 Triflupromazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 25...

2012-04-01

78

21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.  

Code of Federal Regulations, 2011 CFR

...false Levamisole hydrochloride effervescent tablets. 520.1242e Section 520.1242e Food...1242e Levamisole hydrochloride effervescent tablets. (a) Specifications. Each tablet contains 907 milligrams of levamisole...

2011-04-01

79

21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.  

Code of Federal Regulations, 2013 CFR

...2013-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and...520.863 Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50...

2013-04-01

80

21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.  

Code of Federal Regulations, 2011 CFR

...2011-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and...520.863 Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50...

2011-04-01

81

21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.  

Code of Federal Regulations, 2014 CFR

...2014-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and...520.863 Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50...

2014-04-01

82

21 CFR 520.2098 - Selegiline hydrochloride tablets.  

Code of Federal Regulations, 2014 CFR

...2014-04-01 false Selegiline hydrochloride tablets. 520.2098 Section 520.2098 Food and...DRUGS 520.2098 Selegiline hydrochloride tablets. (a) Specifications. Each tablet contains either 2, 5, 10, 15, or 30...

2014-04-01

83

21 CFR 520.2582 - Triflupromazine hydrochloride tablets.  

Code of Federal Regulations, 2013 CFR

...2013-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and...520.2582 Triflupromazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 25...

2013-04-01

84

21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.  

Code of Federal Regulations, 2012 CFR

...2012-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and...520.863 Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50...

2012-04-01

85

21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.  

Code of Federal Regulations, 2014 CFR

...false Levamisole hydrochloride effervescent tablets. 520.1242e Section 520.1242e Food...1242e Levamisole hydrochloride effervescent tablets. (a) Specifications. Each tablet contains 907 milligrams of levamisole...

2014-04-01

86

21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and...520.863 Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50...

2010-04-01

87

21 CFR 520.2582 - Triflupromazine hydrochloride tablets.  

Code of Federal Regulations, 2014 CFR

...2014-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and...520.2582 Triflupromazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 25...

2014-04-01

88

21 CFR 520.2582 - Triflupromazine hydrochloride tablets.  

Code of Federal Regulations, 2011 CFR

...2011-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and...520.2582 Triflupromazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 25...

2011-04-01

89

Possible Side Effects of Cyclophosphamide, Etoposide, Topotecan Hydrochloride  

Cancer.gov

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

90

40 CFR 721.4460 - Amidinothiopropionic acid hydrochloride.  

Code of Federal Regulations, 2010 CFR

40 Protection of Environment 30 2010-07-01 2010-07-01...false Amidinothiopropionic acid hydrochloride. 721.4460...721.4460 Protection of Environment ENVIRONMENTAL PROTECTION...4460 Amidinothiopropionic acid hydrochloride. (a)...

2010-07-01

91

40 CFR 721.4460 - Amidinothiopropionic acid hydrochloride.  

Code of Federal Regulations, 2011 CFR

40 Protection of Environment 31 2011-07-01 2011-07-01...false Amidinothiopropionic acid hydrochloride. 721.4460...721.4460 Protection of Environment ENVIRONMENTAL PROTECTION...4460 Amidinothiopropionic acid hydrochloride. (a)...

2011-07-01

92

21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.  

Code of Federal Regulations, 2012 CFR

...information. (3) It is not to be used in conjunction with organophosphates and/or procaine hydrochloride because phenothiazines may potentiate the toxicity of organophosphates and the activity of procaine hydrochloride.1 (4)...

2012-04-01

93

21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.  

Code of Federal Regulations, 2010 CFR

...information. (3) It is not to be used in conjunction with organophosphates and/or procaine hydrochloride because phenothiazines may potentiate the toxicity of organophosphates and the activity of procaine hydrochloride.1 (4)...

2010-04-01

94

21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.  

Code of Federal Regulations, 2011 CFR

...information. (3) It is not to be used in conjunction with organophosphates and/or procaine hydrochloride because phenothiazines may potentiate the toxicity of organophosphates and the activity of procaine hydrochloride.1 (4)...

2011-04-01

95

21 CFR 522.2002 - Propiopromazine hydrochloride injection.  

Code of Federal Regulations, 2013 CFR

...body weight. (2) It is not to be used in conjunction with organophosphates and/or procaine hydrochloride since phenothiazines may potentiate the toxicity of organophosphates and the activity of procaine hydrochloride. (3) For...

2013-04-01

96

21 CFR 522.2002 - Propiopromazine hydrochloride injection.  

Code of Federal Regulations, 2010 CFR

...body weight. (2) It is not to be used in conjunction with organophosphates and/or procaine hydrochloride since phenothiazines may potentiate the toxicity of organophosphates and the activity of procaine hydrochloride. (3) For...

2010-04-01

97

21 CFR 522.2002 - Propiopromazine hydrochloride injection.  

Code of Federal Regulations, 2012 CFR

...body weight. (2) It is not to be used in conjunction with organophosphates and/or procaine hydrochloride since phenothiazines may potentiate the toxicity of organophosphates and the activity of procaine hydrochloride. (3) For...

2012-04-01

98

21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.  

Code of Federal Regulations, 2013 CFR

...information. (3) It is not to be used in conjunction with organophosphates and/or procaine hydrochloride because phenothiazines may potentiate the toxicity of organophosphates and the activity of procaine hydrochloride.1 (4)...

2013-04-01

99

21 CFR 522.2002 - Propiopromazine hydrochloride injection.  

Code of Federal Regulations, 2011 CFR

...body weight. (2) It is not to be used in conjunction with organophosphates and/or procaine hydrochloride since phenothiazines may potentiate the toxicity of organophosphates and the activity of procaine hydrochloride. (3) For...

2011-04-01

100

Synthesis of 3,3-dichloroindolin-2-ones from isatin-3-hydrazones and (dichloroiodo)benzene.  

PubMed

Aryl- and N-substituted isatins were converted to isatin-3-hydrazones and subjected to a dichlorination reaction with PhICl2. Lewis base-catalysis was key to the reaction occurring rapidly and chemoselectively, providing 3,3-dichloroindolin-2-ones in 49-99% yield, and offering a new approach to the deoxygenative dihalogenation reaction. PMID:25425196

Coffey, Keith E; Moreira, Ryan; Abbas, Farhana Z; Murphy, Graham K

2015-01-21

101

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...

102

Conformational analysis of 2 -diphenylacetyl- 1,3 - indandione- 1 -hydrazone and its derivatives  

NASA Astrophysics Data System (ADS)

Conformational analysis in solution of 2-diphenylacetyl-1,3-indandione-1-hydrazone (DI- PAIN, 1) and its derivatives was achieved by NMR, FT-IR and fluorescence spectroscopy. The spectral evidence indicates that the enamine tautomer is the only isomeric form adopted in solution.

Partridge, Ashton C.; Charlesworth, John M.

1991-10-01

103

Hydrazone-palladium-catalyzed allylic arylation of cinnamyloxyphenylboronic acid pinacol esters.  

PubMed

Allylic arylation of cinnamyloxyphenylboronic acid pinacol esters 3, which have arylboronic acid moiety and allylic ether moiety, using a hydrazone 1d-Pd(OAc)2 system proceeded and gave the corresponding 1,3-diarylpropene derivatives 4 with a phenolic hydroxyl group via a selective coupling reaction of the ?-allyl intermediate to the boron-substituted position of the leaving group. PMID:24962496

Watanabe, Kohei; Mino, Takashi; Abe, Taichi; Kogure, Taketo; Sakamoto, Masami

2014-07-18

104

Potentially cytotoxic new copper(II) hydrazone complexes: synthesis, crystal structure and biological properties.  

PubMed

A new set of penta-coordinated copper(II) hydrazone complexes containing solvated methanol were synthesized by reacting the hydrazone ligands, 2-acetylpyridine benzoyl hydrazone (HL1) and 2-acetylpyridine thiophene-2-carboxylic acid hydrazone (HL2), with [CuCl2(DMSO)2] and characterized by different spectral methods. Single crystal X-ray diffraction studies of the complexes revealed that both of them, [CuCl(L1)(MeOH)] (1) and [CuCl(L2)(MeOH)] (2), have square pyramidal geometry around the cupric ion, in which the hydrazone is coordinated through NNO atoms along with a molecule of methanol in the apical position. Interaction of the ligands HL1 and HL2 along with the corresponding copper complexes 1 and 2 with calf thymus DNA (CT-DNA) has been estimated by absorption and emission titration methods which revealed that the compounds interacted with CT-DNA through intercalation. Binding of the compounds, i.e., free ligands and complexes (1) and (2) with bovine serum albumin (BSA) protein investigated using UV-visible, fluorescence and synchronous fluorescence spectroscopic methods indicated that there occurred strong binding of copper complexes to BSA over the ligands. Further, the cytotoxicity of the compounds examined in vitro on a panel of cancerous cell lines such as a human cervical cancer cell line (HeLa), a pancreatic cancer cell line (PANC-1), an Ehrlich ascites cancer cell line (EAC) and Dalton's lymphoma ascitic cancer cells (DLA) and a normal mouse embryonic fibroblasts cell line (NIH3) demonstrated that the complexes 1 and 2 possessed superior cytotoxicity than that of well-known commercial anticancer drug cisplatin to the tumor cells but are less toxic to the normal cell line and have emerged as potential candidates for further studies. PMID:23529726

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

2013-05-21

105

Synthesis, characterization and antitumor activities of some steroidal derivatives with side chain of 17-hydrazone aromatic heterocycle.  

PubMed

Here a series of dehydroepiandrosterone-17-hydrazone and estrone-17-hydrazone derivatives possessing various aromatic heterocycle structures in 17-side chain of their steroidal nucleus were synthesized and their structures were evaluated. The antiproliferative activity of synthesized compounds against some cancer cells was investigated. The results have demonstrated that some dehydroepiandrosterone-17-hydrazone derivatives show distinct antiproliferative activity against some cancer cells through inducing cancer cell apoptosis, and compound 8 with a quinoline structure in 17-side chain displays excellent antiproliferative activity in vitro against SGC 7901 cancer cell (human gastric carcinoma) with an IC50 value of 1?M. In addition, estrone-17-hydrazone derivatives having a key feature of indole group in the structure showed a special obvious cytotoxicity against HeLa cells, but almost inactive against other cells. The information obtained from the studies is valuable for the design of novel steroidal chemotherapeutic drugs. PMID:25578734

Cui, Jianguo; Liu, Liang; Zhao, Dandan; Gan, Chunfang; Huang, Xin; Xiao, Qi; Qi, Binbin; Yang, Lei; Huang, Yanmin

2015-03-01

106

X-ray crystallographic, electrochemical and spectroscopic properties of 2-pyridinio 2-pyridyl ketone phenyl hydrazone chloride hydrate  

Microsoft Academic Search

In contrast to the reaction between di-2-pyridyl ketone with a variety of hydrazines or hydrazides in refluxing acidified alcoholic solution to form unprotonated di-2-pyridyl ketone hydrazones (dpkhydrazones), the reaction between di-2-pyridyl ketone and phenyl hydrazine hydrochloric acid under the same conditions gave unprecedented pyridyl protonated 2-pyridinio 2-pyridyl ketone phenyl hydrazone chloride hydrate, dpkphhHCl3H2O. Crystals of dpkphhHCl3H2O obtained from an ethanolic

Mohammed Bakir; Ishmael Hassan; Toni Johnson; Ordel Brown; Orville Green; Colin Gyles; Michael D. Coley

2004-01-01

107

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

Microsoft Academic Search

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

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

108

21 CFR 184.1875 - Thiamine hydrochloride.  

Code of Federal Regulations, 2010 CFR

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

2010-04-01

109

21 CFR 184.1875 - Thiamine hydrochloride.  

Code of Federal Regulations, 2011 CFR

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

2011-04-01

110

21 CFR 184.1676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2010 CFR

...170.3(n)(31) of this chapter; plant protein products as defined in 170.3(n)(33) of this chapter; and snack foods as defined in 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in infant formula in...

2010-04-01

111

21 CFR 184.1676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2013 CFR

...170.3(n)(31) of this chapter; plant protein products as defined in 170.3(n)(33) of this chapter; and snack foods as defined in 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in infant formula in...

2013-04-01

112

21 CFR 184.1676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2012 CFR

...170.3(n)(31) of this chapter; plant protein products as defined in 170.3(n)(33) of this chapter; and snack foods as defined in 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in infant formula in...

2012-04-01

113

21 CFR 184.1676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2011 CFR

...170.3(n)(31) of this chapter; plant protein products as defined in 170.3(n)(33) of this chapter; and snack foods as defined in 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in infant formula in...

2011-04-01

114

21 CFR 184.1676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2014 CFR

...170.3(n)(31) of this chapter; plant protein products as defined in 170.3(n)(33) of this chapter; and snack foods as defined in 170.3(n)(37) of this chapter. Pyridoxine hydrochloride may be used in infant formula in...

2014-04-01

115

LC-UV/MS methods for the analysis of prochelator-boronyl salicylaldehyde isonicotinoyl hydrazone (BSIH) and its active chelator salicylaldehyde isonicotinoyl hydrazone (SIH).  

PubMed

Salicylaldehyde isonicotinoyl hydrazone (SIH) is an intracellular iron chelator with well documented potential to protect against oxidative injury both in vitro and in vivo. However, it suffers from short biological half-life caused by fast hydrolysis of the hydrazone bond. Recently, a concept of boronate prochelators has been introduced as a strategy that might overcome these limitations. This study presents two complementary analytical methods for detecting the prochelator-boronyl salicylaldehyde isonicotinoyl hydrazone-BSIH along with its active metal-binding chelator SIH in different solution matrices and concentration ranges. An LC-UV method for determination of BSIH and SIH in buffer and cell culture medium was validated over concentrations of 7-115 and 4-115 ?M, respectively, and applied to BSIH activation experiments in vitro. An LC-MS assay was validated for quantification of BSIH and SIH in plasma over the concentration range of 0.06-23 and 0.24-23 ?M, respectively, and applied to stability studies in plasma in vitro as well as analysis of plasma taken after i.v. administration of BSIH to rats. A Zorbax-RP bonus column and mobile phases containing either phosphate buffer with EDTA or ammonium formate and methanol/acetonitrile mixture provided suitable conditions for the LC-UV and LC-MS analysis, respectively. Samples were diluted or precipitated with methanol prior to analysis. These separative analytical techniques establish the first validated protocols to investigate BSIH activation by hydrogen peroxide in multiple matrices, directly compare the stabilities of the prochelator and its chelator in plasma, and provide the first basic pharmacokinetic data of this prochelator. Experiments reveal that BSIH is stable in all media tested and is partially converted to SIH by H2O2. The observed integrity of BSIH in plasma samples from the in vivo study suggests that the concept of prochelation might be a promising strategy for further development of aroylhydrazone cytoprotective agents. PMID:25527982

Bure, Jan; Jansov, Hana; Stariat, Jn; Filipsk, Tom; Mlad?nka, P?emysl; im?nek, Tom; Ku?era, Radim; Klime, Ji?; Wang, Qin; Franz, Katherine J; Kova?kov, Petra

2015-02-01

116

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

PubMed Central

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

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

2011-01-01

117

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 510(-8) to 2.210(-6)mol dm(-3) at a sampling rate of 20h(-1). The relative standard deviations for ten determinations of 2.210(-6) and 210(-7)mol dm(-3) hydrogen peroxide were 1.1% and 3.7%, respectively. The proposed method was successfully applied to the determination of hydrogen peroxide in rainwater samples and the analytical results agreed fairly well with the results obtained by different two reference methods; peroxidase method and hydrogen peroxide electrode method. PMID:22817947

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

2012-07-15

118

Spectrophotometric methods for the determination of omeprazole in bulk form and pharmaceutical formulations.  

PubMed

Four simple and sensitive methods for the assay of omeprazole (OMZ) were developed. These methods are based on the formation of colored species by treating OMZ with 3-methyl-2-benzothiazolinone hydrazone (MBTH) following oxidation with ferric chloride (method A) or m-aminophenol following oxidation with chloramine-T (CAT) (method B) or Folin-Ciocalteau reagent (FC) (method D), or by oxidizing OMZ with excess N-bromosuccinimide (NBS) and determining the consumed NBS with a decrease in color intensity of Celestine blue (CB) (method C). All variables have been optimized. Regression analysis of Beer's plots showed good correlation in the concentration range of 1.0-10, 2.0-32, 0.4-2.4 and 0.8-10 mug ml(-1) for methods A, B, C and D, respectively. No interference was observed for formulation additives and the validity of each method was tested by analysing capsules containing OMZ. Recoveries were 98.7-100.1%. PMID:18966856

Sastry, C S; Naidu, P Y; Murty, S S

1997-07-01

119

An Optical Biosensor based on Immobilization of Laccase and MBTH in Stacked Films for the Detection of Catechol  

PubMed Central

The fabrication of an optical biosensor by using stacked films where 3-methyl-2-benzothiazolinone hydrazone (MBTH) was immobilized in a hybrid nafion/sol-gel silicate film and laccase in a chitosan film for the detection of phenolic compounds was described. Quinone and/or phenoxy radical product from the enzymatic oxidation of phenolic compounds was allowed to couple with MBTH to form a colored azo-dye product for spectrophometric detection. The biosensor demonstrated a linear response to catechol concentration range of 0.5-8.0 mM with detection limit of 0.33 mM and response time of 10 min. The reproducibility of the fabricated biosensor was good with RSD value of 5.3 % (n = 8) and stable for at least 2 months. The use of the hybrid materials of nafion/sol-gel silicate to immobilize laccase has altered the selectivity of the enzyme to various phenolic compounds such as catechol, guaicol, o-cresol and m-cresol when compared to the non-immobilized enzyme. When immobilized in this hybrid film, the biosensor response only to catechol and not other phenolic compounds investigated. Immobilization in this hybrid material has enable the biosensor to be more selective to catechol compared with the non-immobilized enzyme. This shows that by a careful selection of different immobilization matrices, the selectivity of an enzyme can be modified to yield a biosensor with good selectivity towards certain targeted analytes.

Abdullah, Jaafar; Ahmad, Musa; Heng, Lee Yook; Karuppiah, Nadarajah; Sidek, Hamidah

2007-01-01

120

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

PubMed

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

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

2010-11-01

121

Evaluation of the BMC glucose oxidase/peroxidase-4-aminophenazone-phenol procedure for glucose as adapted to the Technicon SMAC.  

PubMed

We evaluated the analytical performance of Trinder's glucose oxidase (EC 1.1.3.4)/peroxidase (EC 1.11.1.7) 4-aminophenazone-phenol method for the quantification of serum glucose as adapted to the Technicon SMAC. Our results correlated well with those by the routine SMAC glucose oxidase/peroxidase 3-methyl-2-benzothiazolinone hydrazone-N,N-dimethylaniline method (y = 1.02x - 49.4; r = 0.99) and the glucose oxidase oxygen-rate method (y = 0.99x + 14; r = 0.99) with the Beckman Glucose Analyzer. Sample-to-sample interaction was less than 1%. Ascorbic acid or uric acid in concentrations as high as 200 mg/L were without demonstrable effect on results for glucose. Intra- and inter-assay precisions (CV) were 1.6 and 2.3%, respectively. The upper limit of linearity was about 5 g/L. Adaptation of the Trinder method for glucose to the SMAC is simple and provides an analytically acceptable and economical alternative to the methods ordinarily used with the SMAC. PMID:476940

Purcell, G V; Behenna, D B; Walsh, P R

1979-10-01

122

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

PubMed

The design, synthesis, characterization and their anion sensing properties of two receptors capable of exhibiting azo-hydrazone tautomerism are reported. The anion sensing properties have been investigated using electronic, fluorescence and nuclear magnetic spectral studies in addition to electrochemical and visual detection experiments. Both the receptors selectively bind fluoride ion with >100 nm red-shift in the electronic spectrum and the color changes from yellow to red. The results of the spectral studies revealed that the sensing mechanism involves fluoride ion induced change of chromophore from C=N (hydrazone form) to N=N (azo form) in these receptors leading to the visible color change. Density Functional Theory calculations were conducted to rationalize the optical response of the receptors. PMID:24704596

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

2014-07-15

123

Synthesis and biological activity evaluation of hydrazone derivatives based on a Trger's base skeleton.  

PubMed

We report the design and synthesis of novel anticancer agents based on bis-hydrazones separated by a rigid Trger's base skeleton. This novel approach combines a biologically active moiety (hydrazone) with this scaffold (Trger's base) to construct DNA intercalators. Evaluation of the anticancer activity of these agents using seven cancer cell lines and two healthy cell lines found that several derivatives had potent anticancer activity and excellent selectivity indexes toward cancer cells. The antimicrobial activities were tested on a set of thirteen bacterial stains, but the prepared compounds were not active. Complexation studies using biologically important metal ions demonstrated that these compounds are able to bind Cu(2+), Fe(3+), Co(2+), Ni(2+) and Zn(2+). DNA intercalation studies showed that the compounds themselves do not interact with DNA, but their metallocomplexes do interact, most likely via intercalation into DNA. PMID:25737088

Kaplnek, Robert; Havlk, Martin; Dolensk, Bohumil; Rak, Jakub; Dubk, Petr; Kone?n, Petr; Hajdch, Marin; Krlov, Jarmila; Krl, Vladimr

2015-04-01

124

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

NASA Astrophysics Data System (ADS)

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

Gonzlez-Bar, Ana C.; Pis-Diez, Reinaldo; Parajn-Costa, Beatriz S.; Rey, Nicols A.

2012-01-01

125

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

PubMed

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

Denmark, Scott E; Chang, Wen-Tau T; Houk, K N; Liu, Peng

2014-12-10

126

Structure-activity relationships of pyrrole hydrazones as new anti-tuberculosis agents.  

PubMed

Preliminary investigations of our research team have shown that some pyrrole hydrazones posses strong inhibitory activity against the tuberculosis bacilli, and thus represent a new perspective for development of anti-tuberculosis agents. In this work the anti-tuberculosis activity of an in-house series of pyrrole hydrazones was investigated by quantitative structure-activity relationships (QSAR) analysis and by pharmacophore modelling. Different constitutional, topological, physicochemical, and quantum-mechanical descriptors of the chemical structure were calculated. The QSAR models included the number of chlorine, fluorine and nitrogen atoms, molecular flexibility and shape indexes, and magnitudes of charged molecular surfaces areas and hydrophobic volumes, suggesting importance of these structural characteristics for the activity. Next, a pharmacophore analysis was applied. A possible pharmacophore responsible for the compound interactions with their biological target in the 3D space consisted of five features, including hydrophobic centres, a potential H-bond acceptor and a potential metal ligator. PMID:22530903

Lessigiarska, Iglika; Pajeva, Ilza; Prodanova, Penka; Georgieva, Maya; Bijev, Atanas

2012-05-01

127

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

PubMed

The general and efficient palladium-catalyzed indium-mediated allylation of chiral hydrazones was accomplished with excellent yield (72-92%) and diastereoselectivity (up to 99:1). The development of this reaction and the substrate scope are described. The conversion was found to be proportional to the phosphine concentration, which provided insight into the mechanism and competing pathways of the redox transmetalation process. PMID:25565466

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

2015-01-16

128

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

PubMed Central

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

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

2012-01-01

129

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

Federal Register 2010, 2011, 2012, 2013, 2014

...That TRANDATE (Labetalol Hydrochloride) Tablets, 300 Milligrams and 400 Milligrams...that TRANDATE (labetalol hydrochloride) tablets, 300 milligrams (mg) and 400 mg, were...TRANDATE (labetalol hydrochloride) tablets, 300 mg and 400 mg, are the...

2010-12-28

130

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

131

77 FR 16036 - Determination That CITANEST (Prilocaine Hydrochloride) Injection, 1%, 2%, and 3%, and CITANEST...  

Federal Register 2010, 2011, 2012, 2013, 2014

...Hydrochloride) Injection, 1%, 2%, and 3%, and CITANEST PLAIN (Prilocaine Hydrochloride...hydrochloride (HCl)) Injection, 1%, 2%, and 3%, and CITANEST PLAIN (prilocaine HCl...prilocaine HCl injection, 1%, 2%, and 3%, and prilocaine HCl injection,...

2012-03-19

132

Enantiomeric purity assay of moxifloxacin hydrochloride by capillary electrophoresis  

Microsoft Academic Search

A capillary electrophoresis method for determining the enantiomeric purity of moxifloxacin hydrochloride in drug substance and ophthalmic\\/otic drug products was developed and validated. Because moxifloxacin hydrochloride has two chiral centers, the existence of four different isomers is possible. The method was capable of separating moxifloxacin hydrochloride, which is the S,S-isomer, from its potential chiral degradation products, which are the R,R-enantiomer,

Lou Ann Cruz; Rex Hall

2005-01-01

133

Mucoadhesive bilayer tablets of propranolol hydrochloride  

Microsoft Academic Search

The purpose of this research was to study mucoadhesive bilayer buccal tablets of propranolol hydrochloride using the bioadhesive\\u000a polymers sodium alginate (Na-alginate) and Carbopol 934P (CP) along with ethyl cellulose as an impermeable backing layer.\\u000a The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, mucoadhesive strength, swelling\\u000a index, in vitro drug release, ex vivo drug permeation, ex

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

2007-01-01

134

Solid-state forms of prilocaine hydrochloride  

Microsoft Academic Search

Two polymorphic forms, a dioxane solvate and the amorphous form of the local anaesthetic drug prilocaine hydrochloride (N-(2-methylphenyl)-2-propylamino\\u000a monohydrochloride, PRCHC) were characterized by thermal analysis (hot stage microscopy, differential scanning calorimetry,\\u000a thermogravimetry), vibrational spectroscopy (FTIR, FT-Raman-spectroscopy), powder X-ray diffractometry and water vapor sorption\\u000a analysis. The formation and thermodynamic stability of the different solid phases is described and presented in a

A. C. Schmidt; V. Niederwanger; U. J. Griesser

2004-01-01

135

Particle size distribution of cocaine hydrochloride  

NASA Astrophysics Data System (ADS)

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

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

1997-02-01

136

4-Aminophenylalanine as a Biocompatible Nucleophilic Catalyst for Hydrazone-Ligations at Low Temperature and Neutral pH  

PubMed Central

Hydrazone formation and similar reactions are highly versatile and specific, but their application to biological systems has been limited by their characteristically slow reaction kinetics at neutral pH. Catalysis of these reactions through imine formation with aromatic amines such as aniline has broadened the applicability of these reactions to biomolecular labeling. High concentrations of the catalyst are necessary, which may be incompatible with the native structure of certain proteins. In this study, we investigated the utility of 4-aminophenylalanine (4a-Phe) as a catalyst for these reactions. We find that 4a-Phe is nearly as effective as aniline in catalyzing hydrazone formation between the reactive amino acid 3-formyltyrosine (3f-Tyr) and hydrazine-containing fluorophores, both free in solution and incorporated into the protein tubulin. The catalyst 4a-Phe maintains ~70% of the catalytic efficacy of aniline and is less detrimental to the native structure of tubulin. Examination of the temperature dependence of imine formation between 3f-Tyr and 4a-Phe shows an increase in imine concentration accompanying a decrease in temperature, confirming the exothermic nature of the equilibrium reaction. Interestingly, decreasing the temperature of the 4a-Phe-catalyzed hydrazone reaction between 3f-Tyr and the fluorophore 7-hydrazinyl-3-methylcoumarin increases the overall rate of the reaction. This result indicates that the temperature dependence of the catalyst-aldehyde equilibrium is greater than the temperature dependence of the rate constant for hydrazone formation from this intermediate, and that the rate of hydrazone formation a direct function of the concentration of the intermediate imine. These results provide a platform for conducting nucleophilic catalysis under conditions that are more compatible with biomolecular targets than previously demonstrated, thereby expanding the utility of hydrazone-ligations in biological systems. PMID:21932849

Blanden, Adam R.; Mukherjee, Kamalika; Dilek, Ozlem; Loew, Maura; Bane, Susan L.

2011-01-01

137

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. PMID:18797497

Friestad, Gregory K.; Mathies, Alex K.

2007-01-01

138

Analysis of the volatile organic compounds in seized cocaine hydrochloride  

Microsoft Academic Search

The volatile organic compounds in seized cocaine hydrochloride were analyzed using Gas Chromatography Mass Spectrometry (GC\\/MS). Two different methods of sampling volatile compounds were investigated. In the first method, 20, 50, and 100 mg samples of seized cocaine hydrochloride were loaded into 2-inch glass tubes. The headspace of each tube was then purged with ultra high purity (UHP) helium and

Lindy E. Dejarme; Sara J. Lawhon; Prasenjit Ray; Michael R. Kuhlman

1997-01-01

139

Impact of four loci on serum tamsulosin hydrochloride concentration.  

PubMed

Tamsulosin hydrochloride is one of the most potent drugs for treatment of benign prostatic hyperplasia (BPH), however, the efficacy of tamsulosin hydrochloride varies among individuals. In this study, we measured the maximum serum concentration (Cmax) of tamsulosin hydrochloride in 182 of BPH patients and found remarkable individual variability. To investigate the genetic factors that regulate pharmacokinetics of tamsulosin hydrochloride, we conducted a genome-wide association study in these 182 BPH patients. As a result, rs16902947 on chromosome 5p13.2, rs7779057 on 7q22.3, rs35681285 on 7p21.2 and rs2122469 on 8p21.3 indicated possible associations with Cmax of tamsulosin hydrochloride (P=1.29 10(-7), 2.15 10(-7), 4.35 10(-7) and 7.03 10(-7), respectively), although these single-nucleotide polymorphisms (SNPs) did not reach the genome-wide significance threshold after Bonferroni correction. As these associated SNPs showed additive effects on serum tamsulosin hydrochloride concentration, we defined the 'Cmax prediction index' based on genotypes of these SNPs. This index clearly associated with Cmax values (P=4.5 10(-6)), indicating the possible roles of these four variants in tamsulosin hydrochloride pharmacokinetics. Our findings would partially explain the variability of the response to the tamsulosin hydrochloride treatment. PMID:23151678

Takata, Ryo; Matsuda, Koichi; Sugimura, Jun; Obara, Wataru; Fujioka, Tomoaki; Okihara, Koji; Takaha, Natsuki; Miki, Tsuneharu; Ashida, Shingo; Inoue, Keiji; Tanikawa, Chizu; Shuin, Taro; Sasaki, Shoichi; Kojima, Yoshiyuki; Kohri, Kenjiro; Kubo, Michiaki; Yamaguchi, Masao; Ohnishi, Yozo; Nakamura, Yusuke

2013-01-01

140

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 (C dbnd N), phenolic (OH) and (NH) groups forming polynuclear structures. The involvement of zeolite oxygen in coordination was postulated in the hybrid materials. The intrazeolitic copper, cobalt and nickel-SAPH complexes have distorted tetrahedral, octahedral and square-pyramidal configurations, respectively. The zeolite encapsulated complexes are thermally stable up to 800 C except Cu(II) sample which is thermally stable up to midpoint 428 C. The assessment of the catalytic activity was performed by the use of the photo-degradation of acid violet-1 dye as a probe reaction in presence of H 2O 2 as an oxidant. Decolorization of acid violet-1 dye was examined under the same conditions whereas the unpromoted zeolite and Cu II, Co II, Ni II-hydrazone complexes supported on zeolite showed 13% and 76%, 53%, 43% color removal, respectively. The results revealed that, the zeolite encapsulated Cu(II) complex generally exhibited better catalytic efficiency (76%) compared with other investigated zeolite encapsulated metal-hydrazone samples.

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

2011-12-01

141

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

PubMed Central

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

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

2014-01-01

142

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

PubMed

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

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

2014-01-01

143

The immobilization of wapiti with etorphine hydrochloride.  

PubMed

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

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

1977-07-01

144

Determination of Certain Antispasmodic Drugs as Single Ingredient, Mebeverine Hydrochloride, and in Two Component Mixtures, Mebeverine HYDROCHLORIDE-SULPIRIDE and Isopropamide IODIDE-TRIFLUOPERAZINE Hydrochloride  

Microsoft Academic Search

Two simple and sensitive methods are described for the quantitative determination of mebeverine hydrochloride as single ingredient. The first method depends on the application of quantitative H-NMR spectroscopy using deuterated chloroform and hexamine as an internal reference standard. The second method is based on measuring the native fluorescence of mebeverine hydrochloride in 0.1N sulphuric acid at 360nm with excitation at

Sonia T. Hassib; Bahia A. Moussa; Hanaa A. Hashim; Asmaa A. El-Zaher

2002-01-01

145

Enantiotropically related polymorphs of gaboxadol hydrochloride.  

PubMed

Gaboxadol hydrochloride, also known as THIP hydrochloride (systematic name: 3-hydroxy-4,5,6,7-tetrahydro-1,2-oxazolo[5,4-c]pyridin-6-ium chloride), C6H9N2O2(+)Cl(-), exists as two enantiotropically related polymorphs. Transformation between the polymorphs occurs in a single-crystal-to-single-crystal manner at 221?K, and the enthalpy of transformation from the high-temperature form to the low-temperature form is -0.7?kJ?mol(-1). Single-crystal structures have been determined at 298 and 220?K. At 298?K, the structure is triclinic (space group P overline 1), with two formula units in the crystallographic asymmetric unit. At 220?K, the structure is monoclinic (space group I2/a), with one formula unit in the asymmetric unit. The structures contain identical hydrogen-bonded layers and the transformation between the polymorphs corresponds to a shift of adjacent layers relative to each other. The transformation is shown to be reversible by differential scanning calorimetry and variable-temperature powder X-ray diffraction. PMID:24192165

Lopez de Diego, Heidi; Koradia, Vishal; Bond, Andrew D

2013-11-01

146

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

PubMed

The monoazo dyes, 4-carboxyl-2, 6-dinitrophenylazohydroxynaphthalenes dyes (AZ-01, AZ-03 and AZ-04), were evaluated as a highly selective colorimetric chemosensor for cyanide ion. The recognition of cyanide ion gave an obvious colour change from light yellow to brownish red and upon dilution with acetone produced a purple to lilac colour. Optimum conditions for the reaction between the azo dyes and cyanide ion were established at 30C for 5 min, and different variables affecting the reaction were carefully studied and optimised. Under the optimum conditions, linear relationships between the CN(-) concentrations and light absorption were established. Using these azo-hydrazone molecular switch entities, excellent selectivity towards the detection of CN(-) in aqueous solution over miscellaneous competitive anions was observed. Such selectivity mainly results from the possibility of nucleophilic attack on the azo-hydrazone chemosensors by cyanide anions in aqueous system, which is not afforded by other competing anions. The cyanide chemosensor method described here should have potential application as a new family probes for detecting cyanide in aqueous solution. PMID:24667418

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

2014-07-15

147

Synthesis, characterization and modeling structures of isatin-3-Girard T (IGT) and P (IGP) hydrazone complexes.  

PubMed

The reactions of isatin Girard's T hydrazone, N,N,N-trimethyl-2-oxo-2[(2z)-2-(2-oxo-1,2-dihydro-3H-indole-3-ylidene)hydrazino]ethan ammonium chloride (IGT) and isatin Girard's P hydrazone, 1-{2-oxo-2-[(2z)(2-oxo-1,2-dihydro-3H-indole-3-ylidene)hydrazine]ethyl} pyridinium chloride (IGP), with Fe(3+), Al(3+), Sb(3+) and Sn(2+) salts afford different types of complexes. The isolated solid complexes were characterized by elemental analyses, molar conductance, spectral (IR, UV-Vis, (1)H NMR, mass), magnetic moment and thermal measurements. The results suggest that all the complexes are conducting in polar solvents (EtOH, H2O and DMF). The IR spectral data suggest that the ligands coordinate in a tridentate manner via the two carbonyl of both isatin and Girard's and the azomethine (C=N) groups. The amounts of solvents inside and outside the coordination sphere were determined using thermal data (TGA) and weight loss method. The octahedral geometry of the complexes is confirmed using DFT method from DMOL(3) calculations. The ligands and their metal complexes were tested against different strains of bacteria and fungi. PMID:24509535

Salah, Sabah; El-Wahab, Zeinab H Abd; Farag, Rabei S; Mostafa, Mohsen M

2014-04-24

148

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

NASA Astrophysics Data System (ADS)

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

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

2014-07-01

149

Variation in the biomolecular interactions of nickel(II) hydrazone complexes upon tuning the hydrazide fragment.  

PubMed

Three new bivalent nickel hydrazone complexes have been synthesised from the reactions of [NiCl(2)(PPh(3))(2)] with H(2)L {L = dianion of the hydrazones derived from the condensation of o-hydroxynaphthaldehyde with furoic acid hydrazide (H(2)L(1)) (1)/thiophene-2-acid hydrazide (H(2)L(2)) (2)/isonicotinic acid hydrazide (H(2)L(3)) (3)} and formulated as [Ni(L(1))(PPh(3))] (4), [Ni(L(2))(PPh(3))] (5) and [Ni(L(3))(PPh(3))] (6). Structural characterization of these compounds 4-6 were accomplished by using various physico-chemical techniques. Single crystal X-ray diffraction data of complexes 4 and 5 proved their distorted square planar geometry. In order to ascertain the potential of the above synthesised compounds towards biomolecular interactions, additional experiments involving interaction with calf thymus DNA (CT DNA) and bovine serum albumin (BSA) were carried out. All the ligands and corresponding nickel(ii) chelates have been screened for their scavenging effect towards O(2)(-), OH and NO radicals. The efficiency of complexes 4-6 to arrest the growth of HeLa, HepG-2 and A431 tumour cell lines has been studied along with the cell viability test against the non-cancerous NIH 3T3 cells under in vitro conditions. PMID:22506273

Krishnamoorthy, Paramasivam; Sathyadevi, Palanisamy; Butorac, Rachel R; Cowley, Alan H; Bhuvanesh, Nattamai S P; Dharmaraj, Nallasamy

2012-06-14

150

Hexa-arm star shaped hydrazone derivatives from hexakis(4-formylphenoxy)-cyclotriphosphazene core  

NASA Astrophysics Data System (ADS)

A series of novel hexasubstituted cyclophosphazene hydrazones [N 3P 3( sbnd OC 6H 4sbnd psbnd CH dbnd N sbnd NH sbnd C(O) sbnd C 6H 4sbnd psbnd X) 6] (X = H, Br, Cl, F, OH, OCH 3, CH 3, NO 2, NH 2) were prepared by a sixfold condensation reaction of [N 3P 3( sbnd OC 6H 4sbnd psbnd CHO) 6] with para-substituted benzoic hydrazides [NH 2sbnd NH sbnd C(O) sbnd C 6H 4sbnd psbnd X] with excellent yields (91-98%). The structures of the compounds were confirmed by elemental analysis, FT-IR, 1H, 13C, 31P, 2D-HSQC NMR and mass spectrometry (MALDI-TOF). All the synthesized cyclophosphazene hydrazones exhibit high thermal stability. The crystal structure of a homogeneously substituted hexakis(4-formylphenoxy)-cyclotriphosphazene was determined by X-ray diffraction analysis. The compound crystallizes in the monoclinic system, space group P2 1/n with a = 16.558(3) , b = 10.250(2) , c = 23.429(5) , ? = ? = 90.00, ? = 90.461(4), V = 3976.5(14) 3 and Z = 4. The R value is 0.0823 for 4290 observed reflections. The conformations of the 4-formylphenoxy-groups are different at the three phosphorus atoms.

Patil, Basavaraj R.; Machakanur, Shrinath S.; Badiger, Dayananda S.; Hunoor, Rekha S.; Gudasi, Kalagouda B.; Nethaji, Munirathinam; Annie Bligh, S. W.

2011-09-01

151

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...

152

Convenient Method for Reduction of CN Double Bonds in Oximes, Imines, and Hydrazones Using Sodium BorohydrideRaney Ni System  

Microsoft Academic Search

A practical method has been developed for reduction of C-N double bond in oximes, imines, and hydrazones with sodium borohydride catalyzed by Raney Ni. The reactions were carried out in basic aqueous solution, and the desired products were obtained in moderate yields after a simple procedure. This method can be applied to synthesize simpler aliphatic or aromatic amines and its

Yihua Yang; Shouxin Liu; Junzhang Li; Xia Tian; Xiaoli Zhen; Jianrong Han

2012-01-01

153

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). ...

154

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; Beltrn, J F; de Villafae, G; Moreno, S

1994-10-01

155

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

PubMed

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

Belant, J L

1991-04-01

156

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

PubMed Central

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

Pot??kov, Elika; Hrukov, Kate?ina; Bure, Jan; Kova?kov, Petra; pirkov, Iva A.; Pravdkov, Kate?ina; Kolbabov, Lucie; Hergeselov, Tereza; Hakov, Pavlna; Jansov, Hana; Mach?ek, Miloslav; Jirkovsk, Anna; Richardson, Vera; Lane, Darius J. R.; Kalinowski, Danuta S.; Richardson, Des R.; Vvrov, Kate?ina; im?nek, Tom

2014-01-01

157

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

Microsoft Academic Search

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

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

2006-01-01

158

Isolation and characterization of some potential impurities in ropinirole hydrochloride  

Microsoft Academic Search

Three impurities in ropinirole hydrochloride drug substance at levels ?0.060.15% were detected by reverse-phase high performance liquid chromatography (HPLC). These impurities were isolated from the drug substance. These impurities were analyzed using reverse-phase HPLC. Based on the spectral data (IR, NMR and MS), structures of these impurities were characterized as 4-[2-(propylamino) ethyl]-1,3-dihydro-2H-indol-2-one hydrochloride (impurity-A), 5-[2-(diropylamino) ethyl]-1,4-dihydro-3H-benzoxazin-3-one hydrochloride (impurity-B) and 4-[2-(diropylamino)

B. Sahasrabuddhey; R. Nautiyal; H. Acharya; S. Khyade; P. K. Luthra; P. B. Deshpande

2007-01-01

159

Environmental fate and chemistry of raloxifene hydrochloride.  

PubMed

Raloxifene hydrochloride is a selective estrogen receptor modulator (SERM) used for the prevention and treatment of osteoporosis in women. Excretion of raloxifene occurs through the feces of patients. Raloxifene has the potential to be discharged into waste treatment systems after therapeutic use. Raloxifene hydrochloride was investigated using a battery of studies designed to describe its physical/chemical characteristics and define its fate in the environment. The mean measured solubility of raloxifene hydrochloride (+/- standard deviation) was 345.2 +/- 15.6 microg/ml, 13.3 +/- 0.6 microg/ml, 0.9224 +/- 0.015 microg/ml, and 627.4 +/- 132.0 microg/ml in aqueous buffers at pH 5, 7, and 9 and in unbuffered water, respectively. Raloxifene exhibited a mean molar absorptivity of 34,000 and a wavelength absorbance maximum at 287 nm for pH 5 and 7 aqueous buffer solutions and 297 nm at pH 9. Mean measured Kow values were 516 +/- 17, 1,323 +/- 91, and 1,556 +/- 135 at pH 5, 7, and 9, respectively. After 5 d at 50 degrees C, raloxifene hydrolyzed 8.02, 10.61, and 23.81% in pH 5, 7, and 9 aqueous buffers, respectively. In a 28-d hydrolysis study at 25 degrees C, the calculated first-order hydrolysis rates were 6.92 x 10(-4), 1.70 x 10(-3), and 7.66 x 10(-3)/d, and the corresponding half-lives were 1,001, 410, and 90 d in pH 5, 7, and 9 aqueous buffers, respectively. Raloxifene sorbed significantly to sewage treatment solids with Freundlich isotherm adsorption coefficients K between 2,000 and 3,000. Raloxifene degraded rapidly in the presence of sewage solids. In a system containing 0.470 g/L sludge solids, the raloxifene biodegradation rate and half-life were 0.0966/h and 7.17 h, respectively. In a 28-d aerobic-aquatic biodegradation study containing 30 mg/L sludge solids, the raloxifene biodegradation rate and half-life were 0.0188/d and 37 d, respectively. Given the fate and behavior of raloxifene in these studies, it is anticipated that raloxifene would rapidly dissipate in the environment. PMID:11951945

Teeter, Jerold Scott; Meyerhoff, Roger D

2002-04-01

160

A novel formulation for mebeverine hydrochloride.  

PubMed

The antispasmodic drug mebeverine hydrochloride was formulated into a film-forming gel to be used as a topical local anesthetic. A mixture of cellulose derivatives was used as a base. Additives were used to enhance the release as well as the residence time. Formulations were characterized in terms of drug release, mucoadhesion and rheology. Clinically, the selected formula has shown faster onset (p = 0.0156), longer duration (p = 0.0313), better film residence (p = 0.0313), and no foreign body sensation (p = 0.0313) in comparison to Solcoseryl dental paste. Histopathological examination showed no change in inflammatory cells count, concluding that this topical anesthetic is efficacious and safe orally. PMID:17882731

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

2007-10-01

161

Morphine hydrochloride anhydrate1  

PubMed Central

In the title molecular salt [systematic name: (5?,6?)-7,8-didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol hydrochloride], C17H20NO3 +Cl?, the conformation of the morphinium ion is in agreement with the characteristics of the previously reported morphine forms [for example, Gylbert (1973 ?). Acta Cryst. B29, 16301635]. In the crystal, the cations and chloride anions are linked into a helical chain propagating parallel to the b-axis direction by NH?Cl and OH?Cl hydrogen bonds. The title salt and the morphine monohydrate [Bye (1976 ?) Acta Chem. Scand. 30, 549554] display very similar one-dimensional packing modes of their morphine components. PMID:23476193

Gelbrich, Thomas; Braun, Doris E.; Griesser, Ulrich J.

2012-01-01

162

Isolation and characterization of some potential impurities in ropinirole hydrochloride.  

PubMed

Three impurities in ropinirole hydrochloride drug substance at levels approximately 0.06-0.15% were detected by reverse-phase high performance liquid chromatography (HPLC). These impurities were isolated from the drug substance. These impurities were analyzed using reverse-phase HPLC. Based on the spectral data (IR, NMR and MS), structures of these impurities were characterized as 4-[2-(propylamino) ethyl]-1,3-dihydro-2H-indol-2-one hydrochloride (impurity-A), 5-[2-(diropylamino) ethyl]-1,4-dihydro-3H-benzoxazin-3-one hydrochloride (impurity-B) and 4-[2-(diropylamino) ethyl]-1H-indol-2,3-dione hydrochloride (impurity-C). Synthesis of these impurities is discussed. PMID:17207602

Sahasrabuddhey, B; Nautiyal, R; Acharya, H; Khyade, S; Luthra, P K; Deshpande, P B

2007-03-12

163

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

Sol, Magali; Brandt, Wolfgang; Arnold, Ulrich

2013-03-18

164

21 CFR 520.2345a - Tetracycline hydrochloride capsules.  

Code of Federal Regulations, 2012 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...

2012-04-01

165

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

166

21 CFR 520.2345a - Tetracycline hydrochloride capsules.  

Code of Federal Regulations, 2011 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...

2011-04-01

167

21 CFR 520.2345a - Tetracycline hydrochloride capsules.  

Code of Federal Regulations, 2010 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...

2010-04-01

168

21 CFR 520.2345a - Tetracycline hydrochloride capsules.  

Code of Federal Regulations, 2014 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 licensed...

2014-04-01

169

21 CFR 522.1642 - Oxymorphone hydrochloride injection.  

Code of Federal Regulations, 2012 CFR

...75-1.5 (2) Do not mix with a barbiturate in the same syringe to preclude precipitation. (3) It tends to depress respiration. Naloxone hydrochloride and other narcotic antagonists are used to counter over-dosing. (4) Federal law...

2012-04-01

170

21 CFR 522.1642 - Oxymorphone hydrochloride injection.  

Code of Federal Regulations, 2011 CFR

...75-1.5 (2) Do not mix with a barbiturate in the same syringe to preclude precipitation. (3) It tends to depress respiration. Naloxone hydrochloride and other narcotic antagonists are used to counter over-dosing. (4) Federal law...

2011-04-01

171

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

PubMed Central

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

Nicolle, Simon M; Moody, Christopher J

2014-01-01

172

Characterization of the Subcritical Water Extraction of Fluoxetine-Hydrochloride.  

PubMed

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

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

2012-08-10

173

Canine olfactory sensitivity to cocaine hydrochloride and methyl benzoate  

NASA Astrophysics Data System (ADS)

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

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

1997-02-01

174

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.

zmen, mmhan zdemir; Olgun, Glin

2008-08-01

175

Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents.  

PubMed

New hydrazone derivatives were synthesized via the nucleophilic addition-elimination reaction of 2-[(1-methyl-1H-tetrazol-5-yl)thio)]acetohydrazide with aromatic aldehydes/ketones. The compounds were tested in vitro against various Candida species and compared with ketoconazole. Genotoxicity of the most effective anticandidal compounds was evaluated by umuC and Ames assays. All compounds were also investigated for their cytotoxic effects on NIH3T3 and A549 cell lines. Compound 8 was the most effective antifungal derivative against C. albicans (ATCC-90028) with a MIC value of 0.05 mg/mL. Compound 5 can be identified as the most promising anticancer agent against A549 cancer cell lines due to its inhibitory effect on A549 cell lines and low toxicity to NIH3T3 cells. PMID:23142671

Alt?ntop, Mehlika Dilek; zdemir, Ahmet; Turan-Zitouni, Glhan; Ilg?n, Sinem; Atl?, zlem; ??can, Gkalp; Kaplanc?kl?, Zafer As?m

2012-12-01

176

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

Federal Register 2010, 2011, 2012, 2013, 2014

...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

177

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

ERIC Educational Resources Information Center

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

Weiss, Margaret; Wasdell, Michael; Patin, John

2004-01-01

178

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(sbnd OC6H4-p-CHdbnd Nsbnd NHsbnd C(O)sbnd 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 [NH2sbnd NHsbnd C(O)sbnd 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

179

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

Microsoft Academic Search

Azohydrazone 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, solutesolvent interactions and the structure of the dye molecule itself. The 4-carboxyl-2,6-dinitrophenylazohydroxynaphthalenes, previously

Olajire A. Adegoke

2011-01-01

180

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

NASA Astrophysics Data System (ADS)

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

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

2014-11-01

181

New organocatalyst scaffolds with high activity in promoting hydrazone and oxime formation at neutral pH.  

PubMed

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

Larsen, Dennis; Pittelkow, Michael; Karmakar, Saswata; Kool, Eric T

2015-01-16

182

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

Code of Federal Regulations, 2012 CFR

...hydrocortisone acetate, tetracaine hydrochloride ear ointment. 524.1484d Section 524...hydrocortisone acetate, tetracaine hydrochloride ear ointment. (a) Specifications...externa in dogs and cats. In treatment of ear canker and other inflammatory...

2012-04-01

183

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

Code of Federal Regulations, 2010 CFR

...hydrocortisone acetate, tetracaine hydrochloride ear ointment. 524.1484d Section 524...hydrocortisone acetate, tetracaine hydrochloride ear ointment. (a) Specifications...externa in dogs and cats. In treatment of ear canker and other inflammatory...

2010-04-01

184

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

Federal Register 2010, 2011, 2012, 2013, 2014

...Bupropion Hydrochloride Extended-Release Tablets, 300 Milligrams AGENCY: Food and Drug...Hydrochloride (HCl) Extended-Release Tablets, 300 Milligrams (mg) (Bupropion HCl Extended-Release Tablets 300 mg), under Abbreviated New...

2013-03-18

185

76 FR 45267 - Determination That INVERSINE (Mecamylamine Hydrochloride) Tablet and Six Other Drug Products Were...  

Federal Register 2010, 2011, 2012, 2013, 2014

...INVERSINE (Mecamylamine Hydrochloride) Tablet and Six Other Drug Products Were Not Withdrawn...hydrochloride 300, Winston Salem, (HCl)) Tablet, 2.5 NC 27101-4165 milligrams (mg...sodium) Delayed- Pharmaceuticals Release Tablet, 75 Corp., One Health mg....

2011-07-28

186

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

Code of Federal Regulations, 2011 CFR

...hydrocortisone acetate, tetracaine hydrochloride ear ointment. 524.1484d Section 524...hydrocortisone acetate, tetracaine hydrochloride ear ointment. (a) Specifications...externa in dogs and cats. In treatment of ear canker and other inflammatory...

2011-04-01

187

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

Code of Federal Regulations, 2013 CFR

...hydrocortisone acetate, tetracaine hydrochloride ear ointment. 524.1484d Section 524...hydrocortisone acetate, tetracaine hydrochloride ear ointment. (a) Specifications...externa in dogs and cats. In treatment of ear canker and other inflammatory...

2013-04-01

188

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

Code of Federal Regulations, 2010 CFR

...2010-07-01 2010-07-01 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,...

2010-07-01

189

21 CFR 524.1484f - Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride eardrops.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 false Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride... 524.1484f Neomycin sulfate, prednisolone acetate, tetracaine hydrochloride...neomycin base, 2.5 milligrams of prednisolone acetate, and 5 milligrams of...

2010-04-01

190

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

Federal Register 2010, 2011, 2012, 2013, 2014

...Determination That METADATE ER (Methylphenidate Hydrochloride) Extended-Release...has determined that METADATE ER (methylphenidate hydrochloride (HCl)) extended-release...new drug applications (ANDAs) for methylphenidate HCl extended-release tablet,...

2013-07-05

191

Simultaneous estimation of metformin hydrochloride, pioglitazone hydrochloride, and glimepiride by RP-HPLC in tablet formulation.  

PubMed

A simple, precise, rapid, and reproducible reversed-phase high-performance liquid chromatography method is developed for the simultaneous estimation of metformin hydrochloride (MET), pioglitazone hydrochloride (PIO), and glimepiride (GLP) present in multicomponent dosage forms. Chromatography is carried out isocratically at 25 degrees C +/- 0.5 degrees C on an Inertsil-ODS-3 (C-18) Column (250 x 4.60 mm, 5 microm) with a mobile phase composed of methanol-phosphate buffer (pH 4.3) in the ratio of 75:25 v/v at a flow rate of 1 mL/min. Detection is carried out using a UV-PDA detector at 258 nm. Parameters such as linearity, precision, accuracy, recovery, specificity, and ruggedness are studied as reported in the International Conference on Harmonization guidelines. The retention times for MET, PIO, and GLP are 2.66 + 0.5 min, 7.12 + 0.5 min, and 10.17 + 0.5 min, respectively. The linearity range and percentage recoveries for MET, PIO, and GLP are 10-5000, 10-150, and 1-10 microg/mL and 100.4%, 100.06%, and 100.2%, respectively. The correlation coefficients for all components are close to 1. The relative standard deviations for three replicate measurements in three concentrations of samples in tablets are always less than 2%. PMID:18647470

Jain, Deepti; Jain, Surendra; Jain, Deepak; Amin, Maulik

2008-07-01

192

Biting deterrence and insecticidal activity of hydrazidehydrazones 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 hydrazidehydrazones (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...

193

Field application of Telazol (tiletamine hydrochloride and zolazepam hydrochloride) to immobilize wild red howler monkeys (Alouatta seniculus) in Venezuela.  

PubMed

Telazol (TEL) (tiletamine hydrochloride and zolazepam hydrochloride combination) was used to immobilize 50 wild red howler monkeys (Alouatta seniculus) in Venezuela between October 1989 and February 1991. The mean (+/- SD) dosages of TEL used for adult males and adult females were 22.4 (+/- 7.3) mg/kg and 22.5 (+/- 5.0) mg/kg, respectively. Juveniles of both sexes received a mean dose of 30.5 (+/- 5.6) mg/kg. The induction time for TEL ranged from 1 to 6.2 min. Thirteen animals were given an additional dosage of ketamine hydrochloride manually when they recovered from the first injection of TEL. Total recovery times ranged from 39 to 308 min. There were no apparent side effects to the fetuses of two pregnant females. PMID:7933286

Agoramoorthy, G; Rudran, R

1994-07-01

194

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

PubMed Central

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

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

2014-01-01

195

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

PubMed Central

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

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

2014-01-01

196

Design and synthesis of phenolic hydrazide hydrazones as potent poly(ADP-ribose) glycohydrolase (PARG) inhibitors.  

PubMed

Poly(ADP-ribose) polymerase (PARP) and poly(ADP-ribose) glycohydrolase (PARG) are enzymes responsible for catalyzing the formation and degradation of poly(ADP-ribose) (PAR) polymers, respectively. Activation of PARP has been shown to be involved in cell death induced by genotoxic stimuli. On the other hand, genetic disruption of PARG also leads to increased level of cell death by accumulation of PAR. Unlike PARP, where significant medicinal effort has been expended to identify potent inhibitors, PARG has been insufficiently investigated as a molecular therapeutic target. In this study, we report the design, synthesis, and biological evaluation of phenolic hydrazide hydrazones as potent PARG inhibitors. Compounds 3d, 3e, 5d, 5e, 8a, 8b and 8c showed their ability to inhibit the catalytic activity of PARG in vitro with IC50 values of 1.0, 2.1, 3.1, 3.2, 3.1, 2.8 and 1.6 ?M, respectively. PMID:25042255

Islam, Rafiqul; Koizumi, Fumiaki; Kodera, Yasuo; Inoue, Kengo; Okawara, Tadashi; Masutani, Mitsuko

2014-08-15

197

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

PubMed Central

A ketal-containing trithiocarbonyl compound has been synthesized and characterized as a chain transfer agent (CTA) in Reversible Addition Fragmentation Transfer (RAFT) polymerization. The ketal functionality does not interfere with RAFT polymerization of acrylate monomers, which proceeds as previously reported to yield macro-CTA polymers and block co-polymers. Post-polymerization ketal cleavage revealed ketone functionality at the polar terminus of an amphiphilic block co-polymer. Hydrazone-formation was facile in both organic solution as well as in aqueous buffer where polymer nanoparticle assemblies were formed, indicating a conjugation/end-functionalization yield of 4050%. Conjugation was verified with fluorescein, biotin and Gd-DOTA derivatives, and though the trithiocarbonate linkage is hydrolytically labile, we observed stable conjugation for several days at pH 7.4. and 37C. As expected, streptavidin binding to biotinylated polymer micelles was observed, and size-change based relaxivity increases were observed when Gd-DOTA hydrazide was conjugated to polymer micelles. Cell-uptake of fluorescently labeled polymer micelles was also readily tracked by FACS and fluorescence microscopy. These polymer derivatives demonstrate a range of potential theranostic/biotechnological applications for this conveniently accessible keto-CTA, which include ligand-based nanoparticle targeting and fluorescent/MR nanoparticle contrast agents. PMID:23148126

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

2012-01-01

198

Radiation induced conductivity of polycarbonate doped with different concentrations of aromatic hydrazone DEH  

NASA Astrophysics Data System (ADS)

Radiation induced conductivity (RIC) of polymers widely used on present-day spacecraft plays is an important factor affecting their charging by the hot plasma of the Earths magnetosphere. As a result, researchers pay special attention to laboratory investigations of RIC in polymers excited by 10 -100 keV electrons prevailing in the hot magnetospheric plasma, including auroral radiation. Due to fluctuating fluxes of plasma electrons and especially of auroral electrons, it is very important to know how RIC depends on time. In our report we present RIC results observed in polycarbonate (PC) molecularly doped with aromatic hydrazone DEH (10 to 30 mas. percent) under continuous irradiation with 50 keV electrons. It has been found that RIC behavior in this material differs markedly from what we observed earlier in most of the polymers. After beginning of the stepwise irradiation, the RIC of PC+DEH rises fast to the quasistationary level but unlike common polymers, does not fall by an order of magnitude, instead it starts to increase further thus causing the accumulating space charge to decrease. This fact combined with the confirmed high radiation and temperature tolerance allows us to recommend this material for application on the spacecraft outer surface and specifically, as a thermal blanket.

Vladimir, Saenko; Novikov, Lev; Tyutnev, Andrey

199

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

200

Cancer stem cell therapy using doxorubicin conjugated to gold nanoparticles via hydrazone bonds.  

PubMed

Nanoparticle-mediated delivery of chemotherapies has demonstrated enhanced anti-cancer efficacy, mainly through the mechanisms of both passive and active targeting. Herein, we report other than these well-elucidated mechanisms, rationally designed nanoparticles can efficiently deliver drugs to cancer stem cells (CSCs), which in turn contributes significantly to the improved anti-cancer efficacy. We demonstrate that doxorubicin-tethered gold nanoparticles via a poly(ethylene glycol) spacer and an acid-labile hydrazone bond mediate potent doxorubicin delivery to breast CSCs, which reduces their mammosphere formation capacity and their cancer initiation activity, eliciting marked enhancement in tumor growth inhibition in murine models. The drug delivery mediated by the nanoparticles also markedly attenuates tumor growth during off-therapy stage by reducing breast CSCs in tumors, while the therapy with doxorubicin alone conversely evokes an enrichment of breast CSCs. Our findings suggest that with well-designed drug delivery system, the conventional chemotherapeutic agents are promising for cancer stem cell therapy. PMID:24144908

Sun, Tian-Meng; Wang, Yu-Cai; Wang, Feng; Du, Jin-Zhi; Mao, Cheng-Qiong; Sun, Chun-Yang; Tang, Rui-Zhi; Liu, Yang; Zhu, Jing; Zhu, Yan-Hua; Yang, Xian-Zhu; Wang, Jun

2014-01-01

201

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

NASA Astrophysics Data System (ADS)

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

Cukurovali, Alaaddin; Yilmaz, Engin

2014-10-01

202

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

PubMed

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

Nolan, Louise C; O'Connor, Kevin E

2005-09-15

203

Interference by ascorbic acid in test systems involving peroxidase. II. Redox-coupled indicator systems.  

PubMed

Ascorbic acid hampers some test systems based on use of peroxidase (EC 1.11.1.7) and redox indicators, by producing a lag time in color development. With reversible indicators, no color development occurs during the ascorbic acid lag time. With oxidatively coupled indicator systems, such as 3-methyl-2-benzothiazolinone hydrazone (MBTH) and a suitable coupler such as chromotropic acid (CTA; 4,5-dihydroxynaphthalene-2,7-disulfonic acid), ascorbic acid diminishes the rate of color development, but does not abolish it. The effect of ascorbic acid strongly depends on the reaction pH as well as the nature of the coupler used. The ascorbate-elicited reduction (or lag) in color development was inversely proportional to the concentrations of MBTH and virtually unaffected by changes in CTA coupler concentration. The rate of color development following the lag was directly proportional to the concentration of MBTH but unaffected by the CTA. These observations suggest that peroxidase with H2O2 catalyzes the oxidation and activation of MBTH to an oxidized species (MBTHox). This species is reduced by ascorbic acid and at the same time couples oxidatively with CTA. Thus, the activity during the ascorbate-induced lag time reflects this competition of ascorbic acid and coupler for MBTHox. This study of peroxidase/ascorbate lag time with the redox coupled indicator system has led to the selection of fast couplers that are highly resistant to interference by ascorbic acid. Suitable resistant couplers (e.g., chromotropic acid, Chicago acid, and H acid) appear to be aromatic ring systems with highly activating substituents and directing toward electrophilic aromatic substitution at the ortho and para positions. PMID:7074825

White-Stevens, R H; Stover, L R

1982-04-01

204

Spectrophotometric stability-indicating methods for the determination of leflunomide in the presence of its degradates.  

PubMed

Five simple and sensitive methods were developed for the determination of leflunomide (I) in the presence of its degradates 4-trifluoromethyl aniline (II) and 3-methyl-4-carboxy isoxazole (III). Method A was based on differential derivative spectrophotometry by measuring the delta(1)D value at 279.5 nm. Beer's law was obeyed in the concentration range of 2.00-20.00 microg/mL with mean percentage accuracy of 100.07 +/- 1.32. Method B depended on first-derivative spectrophotometry and measuring the amplitude at 253.4 nm. Beer's law was obeyed in the concentration range of 2.00-16.00 microg/mL with mean percentage accuracy of 98.42 +/- 1.61. Method C was based on the reaction of degradate (II) with 2,6-dichloroquinone-4-chloroimide (Gibbs reagent). The colored product was measured at 469 nm. Method D depended on the reaction of degradate (II) with para-dimethyl aminocinnamaldehyde (p-DAC). The absorbance of the colored product was measured at 533.4 nm. Method E utilized 3-methyl-2-benzothiazolinone hydrazone in the presence of cerric ammonium sulfate with degradate (II). The green colored product was measured at 605.5 nm. The linearity range was 40.00-280.00, 2.40-24.00, and 30-250 microg/mL with mean percentage accuracy of 100.75 +/- 1.21, 100.13 +/- 1.45, and 99.74 +/- 1.39 for Methods C-E, respectively. All variables were studied to optimize the reaction conditions. The proposed methods have been successfully applied to the analysis of leflunomide in pharmaceutical dosage forms and the results were statistically compared with that previously reported. PMID:17225597

Abbas, Samah S; Bebawy, Lories I; Fattah, Laila A; Refaat, Heba H

2006-01-01

205

A new enzymo-chemical method for simultaneous assay of methanol and formaldehyde.  

PubMed

A new enzymo-chemical method for the simultaneous assay of methanol and formaldehyde in mixtures is described which exploits alcohol oxidase (AO) and aldehyde-selective reagent, 3-methyl-2-benzothiazolinone hydrazone (MBTH). The enzyme is used for methanol oxidation to formaldehyde and MBTH plays a double role: 1) at the first step of reaction, it forms a colorless azine adduct with pre-existing and enzymatically formed formaldehyde and masks it from oxidation by AO; 2) at the second step of reaction, non-enzymatic oxidation of azine product to cyanine dye occurs in the presence of ferric ions in acid medium. Pre-existing formaldehyde content is assayed by colorimetric reaction with MBTH without treating samples by AO, and methanol content is determined by a gain in a colored product due to methanol-oxidising reaction. Possibility of differential assay of methanol and formaldehyde by the proposed method has been proved for model solutions as well as for real samples of industrial waste and technical formaline. A threshold sensitivity of the assay method for both analytes is near 1 microM that responds to 30-32 ng analyte in 1 ml of reaction mixture and is 3.2-fold higher when compared to the chemical method with the use of permanganate and chromotropic acid. Linearity of the calibration curve is reliable (p < 0.0001) and standard deviation for parallel measurements for real samples does not exceed 7%. The proposed method, in contrast to the standard chemical approach, does not need the use of aggressive chemicals (concentrated sulfuric, phosphoric, chromotropic acids, permanganate), it is more simple in fulfillment and can be used for industrial wastes control and certification of formaline-contained stuffs. PMID:16566143

Gonchar, M V; Grabek, D; Oklejewich, B; Pavlishko, H M; Shamlian, O V; Sybirny, V A; Kotylak, Z; Rudke, K; Csregi, E; Sibirny, A A

2005-01-01

206

Quantitative analysis of N-sulfated, N-acetylated, and unsubstituted glucosamine amino groups in heparin and related polysaccharides.  

PubMed

A colorimetric procedure for quantitative determination of free and substituted glucosamine amino groups in heparin and related polysaccharides has been developed. The total content of hexosamine amino groups is determined by a modification of the method of Tsuji et al. (1969, Chem. Pharm. Bull. 17, 1505-1510); this method involves acid hydrolysis under conditions effecting complete removal of N-acetyl and N-sulfate groups, deaminative cleavage with nitrous acid, and colorimetric analysis of the resultant anhydromannose residues by reaction with 3-methyl-2-benzothiazolinone hydrazone (MBTH). N-sulfated glucosamine residues are cleaved selectively by treatment with nitrous acid at pH approximately 1.5 (J. E. Shively, and H.E. Conrad, 1976, Biochemistry 15, 3932-3942) and quantitated by the MBTH reaction. Under carefully controlled conditions, deamination at pH approximately 1.5 is highly specific for N-sulfated glucosamine residues, but an excess of reagent causes some cleavage of residues with unsubstituted amino groups as well. Deaminative cleavage at pH approximately 4.5 results in preferential degradation of unsubstituted glucosamine residues, but some cleavage (5-8%) of N-sulfated residues also occurs. However, analysis of the content of N-sulfated residues by the specific pH 1.5 procedure allows appropriate corrections to be made. From the value for total hexosamine content and the sum of N-sulfated and unsubstituted residues, the content of N-acetylated residues is calculated by difference. The modified deamination procedures, in combination with product analysis by the MBTH reaction, have been applied to several problems commonly encountered in the analysis and characterization of heparin. PMID:2221389

Riesenfeld, J; Rodn, L

1990-08-01

207

Spectrophotometric, spectrofluorimetric, and densitometric methods for the determination of indapamide.  

PubMed

Three sensitive spectrophotometric, spectrofluorimetric, and densitometric methods are described for the determination of indapamide. The first and second methods are based on the oxidative coupling reaction of indapamide with 3-methyl-2-benzothiazolinone hydrazone HCl (MBTH) in the presence of cerium(IV) ammonium sulfate in an acidic medium. The absorbance of the reaction product is measured at the lambdamax, 601 nm. With the same reaction, indapamide is determined by its quenching effect on the fluorescence of excess cerous ions at the emission lambdamax, 350 nm, and the excitation at lambdamax, 300 nm. The reaction conditions were optimized, and Beer's law was obeyed for indapamide at 1.2-9.6 microg/mL with mean recoveries of 99.92 +/- 0.83 and 99.97 +/- 1.11%, respectively. The third method, a stability-indicating densitometric assay, was developed for the determination of indapamide, using toluene-ethyl acetate-glacial acetic acid (69 + 30 + 1, v/v/v) as the developing system and scanning at the lambdamax, 242 nm, in the presence of the degradation product and related substance; for the indapamide concentration range of 0.6-6 microg/spot, the mean recovery was 99.73 +/- 0.71%. The proposed methods were successfully applied to the determination of indapamide in bulk powder and commercial tablets, and the results of the analysis agreed statistically with those obtained with the official method. Furthermore, the methods were validated according to the guidelines of the U.S. Pharmacopeia and also assessed by applying the standard additions technique. PMID:14632394

Youssef, Nadia F

2003-01-01

208

Olopatadine Hydrochloride Inhibits Capsaicin-Induced Flare Response in Humans  

Microsoft Academic Search

Capsaicin, a vanilloid, has the potential for releasing substance P (SP) from sensory nerves. Topical application of capsaicin induces a flare response in the skin. However, it has not been clarified whether the release of SP is involved in the process of flare response or not. A potent antihistamine drug, olopatadine hydrochloride, is known to have inhibitory action against the

Masahisa Shindo; Yuichi Yoshida; Osamu Yamamoto

2011-01-01

209

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

PubMed

A life cycle analysis on the cradle-to-gate production of vancomycin hydrochloride, which begins at natural resource extraction and spans through factory (gate) production, not only shows all inputs, outputs, and energy usage to manufacture the product and all related supply chain chemicals, but can highlight where process changes would have the greatest impact on raw material and energy consumption and emissions. Vancomycin hydrochloride is produced by a low-yield fermentation process that accounts for 47% of the total cradle-to-gate energy. The fermentation step consumes the most raw materials and energy cradle-to-gate. Over 75% of the total cradle-to-gate energy consumption is due to steam use; sterilization within fermentation is the largest user of steam. Aeration and agitation in the fermentation vessels use 65% of the cradle-to-gate electrical energy. To reduce raw materials, energy consumption, and the associated environmental footprint of producing vancomycin hydrochloride, other sterilization methods, fermentation media, nutrient sources, or synthetic manufacture should be investigated. The reported vancomycin hydrochloride life cycle inventory is a part of a larger life cycle study of the environmental consequences of the introduction of biocide-coated medical textiles for the prevention of MRSA (methicillin-resistant Staphylococcus aureus) nosocomial infections. PMID:19942254

Ponder, Celia; Overcash, Michael

2010-02-15

210

40 CFR 180.276 - Formetanate hydrochloride; tolerances for residues.  

Code of Federal Regulations, 2010 CFR

...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 1.5 Peach 0.40...

2010-07-01

211

The Solvation and Dissociation of 4Benzylaniline Hydrochloride in Chlorobenzene  

E-print Network

of the decomposition of the hydrochloride salt (the back reaction of eq 3) is appropriate and could lead ABSTRACT: A reaction scheme is proposed to account for the liberation of 4-benzylaniline from 4 are explored: "closed" reaction conditions correspond to the retention of evolved hydrogen chloride gas within

Miller, Alice

212

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

213

Swelling Behavior of Hyaluronic Acid/Polyallylamine Hydrochloride Multilayer Films  

E-print Network

of the polyelectrolytes in the multilayer assemblies, measured by the potential, on colloidal particles. The films were multilayer thin films is based upon the fact that the adsorption of the polyelectrolyte chains leadsSwelling Behavior of Hyaluronic Acid/Polyallylamine Hydrochloride Multilayer Films Susan E. Burke

Barrett, Christopher

214

Stability of the tranquilizer drug propionylpromazine hydrochloride in formulated products  

Microsoft Academic Search

An analytical method to evaluate propionylpromazine hydrochloride (PPZHCl) in tranquilizer formulations was developed using high-performance liquid chromatography (HPLC). During analysis of aged quality-control samples, a previously unreported chromatographic response was observed at a shorter retention time than PPZHCl. Further investigation of formulations stored in trap tap devices at temperatures ranging from 5 to 40 ?C during field trials at four

Thomas M Primus; Bruce A Kimball; Jerome Hurley; John J Johnston; Sherm Blom; Peter J Savarie

2005-01-01

215

Analysis of the volatile organic compounds in seized cocaine hydrochloride  

NASA Astrophysics Data System (ADS)

The volatile organic compounds in seized cocaine hydrochloride were analyzed using Gas Chromatography Mass Spectrometry (GC/MS). Two different methods of sampling volatile compounds were investigated. In the first method, 20, 50, and 100 mg samples of seized cocaine hydrochloride were loaded into 2-inch glass tubes. The headspace of each tube was then purged with ultra high purity (UHP) helium and the gas exiting the tube was directed through a cryogenic loop filled with glass beads and maintained at liquid nitrogen temperature. The volatile organic compounds were collected onto the glass beads while the helium gas was vented. The organic compounds were subsequently thermally desorbed onto the column and analyzed by GC/MS. In the second method, 10 mg and 100 mg samples of seized cocaine hydrochloride were loaded into glass tubes fitted with glass frits at one end. UHP helium was purged through each sample and the purge gas containing organic compounds was collected onto a sorbent tube packed with Tenax TA. The concentrated organic compounds were then thermally desorbed onto a 4 m section of a split GC capillary column maintained at -70 degrees C with flow rates of 20-28 ml/min. Flow was returned to 2.8 ml/min during analysis. By sampling the seized samples of cocaine hydrochloride using a cryogenic loop, methanol, methyl ethyl ketone, acetic acid, 2,2,4-trimethyl pentane, 2-methyl pentane, dichloromethane, 2-propanol, and 2-propanol, and 2-propane (acetone) were found in three different seized cocaine hydrochloride samples. The observed quantities of these volatile organic compounds were different for each of the three seized cocaine hydrochloride samples. THe observed quantities of these volatile organic compounds were different for each of the three seized samples labeled A, B, and C. By sampling the seized samples of cocaine hydrochloride using sorbent tubes, cocaine was consistently observed. Although volatile components other than cocaine were observed, the number and amount of volatile components were not consistent with the cryogenic loop results.

Dejarme, Lindy E.; Lawhon, Sara J.; Ray, Prasenjit; Kuhlman, Michael R.

1997-02-01

216

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. PMID:12642383

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

2003-01-01

217

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

PubMed Central

The present study was conducted to define the physiological responses of captive sloth bears immobilized with ketamine hydrochloride and xylazine hydrochloride and to determine and compare the values of hematology and serum biochemical parameters between sexes. A total of 15 sloth bears were immobilized using combination of ketamine hydrochloride and xylazine hydrochloride drugs at the dose rate of 5.0?milligram (mg) per kg body weight and 2.0?mg per kg body weight, respectively. The use of combination of these drugs was found satisfactory for the chemical immobilization of captive sloth bears. There were no significant differences observed in induction time and recovery time and physiological parameters such as heart rate, respiratory rate, and rectal temperature between sexes. Health related parameters comprising hematological values like packed cell volume (PCV), hemoglobin (Hb), red blood cell count (RBC), erythrocyte indices, and so forth and biochemical values like total protein, blood urea nitrogen (BUN), creatinine, alkaline amino-transferase (ALT), aspartate amino-transferase (AST), and so forth were estimated in 11 (5 males and 6 females) apparently healthy bears. Comparison between sexes revealed significant difference in PCV (P < 0.05) and mean corpuscular hemoglobin concentration (MCHC) (P < 0.05). The study might help to evaluate health profiles of sloth bears for appropriate line treatment. PMID:24876990

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

2014-01-01

218

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

PubMed

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

Yazici, Serafettin; Velioglu, Y Sedat

2002-08-01

219

Solid-state characterization of falicaine hydrochloride and isomorphic dyclonine hydrochloride. Part IV. Crystal polymorphism of local anaesthetic drugs.  

PubMed

Two homologous local anaesthetic drugs, falicaine (propipocaine) hydrochloride (1-(4-propoxyphenyl)-3-(1-piperidinyl)-1-propanone hydrochloride, PPCHC) and dyclonine hydrochloride (1-(4-butoxyphenyl)-3-(1-piperidinyl)-1-propanone hydrochloride, DCNHC) were characterized by thermal analysis (hot-stage-microscopy, differential scanning calorimetry, thermogravimetry), vibrational spectroscopic methods (FTIR-, FT-Raman-spectroscopy), powder X-ray diffractometry, solid-state-/solution-NMR and water-vapor sorption analysis. The formation and thermodynamic stability of the two different solid phases of both the compounds is described and presented in a flow chart and energy/temperature-diagram, respectively. Of the two substances investigated, mod. II degrees is the thermodynamically stable form at room temperature. This form is present in commercial products of PPCHC as well as of DCNHC, and it endothermally transforms to the less stable form mod. I, at about 10K prior to the melting points. The stable mod. II degrees crystallizes from all tested solvents. Mod. I crystallizes from the super cooled melt. According to the heat of transition rule, mod. I is the thermodynamically less stable form below the transition temperature (enantiotropism). The transition temperatures as well as the melting points of the stable forms could be experimentally determined. The sorption isotherms show a distinct higher hygroscopicity for the less stable mod. I of PPCHC and DCNHC. Solid-state NMR spectra were used to obtain both structural- and molecular-level mobility information. PMID:15896948

Schmidt, Andrea C

2005-01-01

220

Synthesis and absorption and luminescence spectral properties of 3-formyl and 3-acetyl-7- (diethylamino) coumarin hydrazones  

SciTech Connect

Various substitued coumarins are of interest as organic luminphors, many of which are effective laser dyes for the blue-green region of the spectrum. This paper attempts to extend the range of fluorescent coumarin dyes by synthesizing and investigating substitued hydrazones of 3-formyl- and 3-acetyl-coumarins (III). The absorption and luminescence spectral properties of the coumarins synthesized are discussed. Some lowering of the quantum yield of fluorescence in comparison with known coumarins is explained by the nonradiative degradation of the energy of electron excitation, which competes with the fluorescence.

Komlev, I.V.; Khrolova, O.R.; Mikhailova, T.A.; Tavrizova, M.A.

1985-10-10

221

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

PubMed

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

Alam, Mohammad Sayed; Lee, Dong-Ung

2015-06-15

222

Convenient synthesis, anti-inflammatory, analgesic and ulcerogenic activites of some new bis-hydrazones and pyrazole derivatives.  

PubMed

The reaction of acid hydrazides (1a-c) with 2-chloro-1-(4-chlorophenyl)ethanone (2a) or 2-bromo-1-(4-bromophenyl)ethanone (2b) afforded bis-hydrazones 6a-d, while the reaction of la-c with 2-oxo-N-arylpropanehydrazonoyl chlorides (3a,b) furnished N-(aryl)propanehydrazonoyl chlorides 8a-c. The reaction of the latter chlorides with sodium benzenesulfinate furnished sulfones 11a-c. On the other hand, treatment of benzothiazole-2-carbohydrazide (1c) with the appropriate ketones yielded the corresponding hydrazones 13a,b, while the reaction of 1c with 2-(ethoxymethylene)malononitrile (14) or with 2-[bis(methylthio)methylene]malononitrile (16) afforded pyrazole derivatives 15 and 17, respectively. In acute toxicity study, no mortalities were observed for the tested compounds. All the tested compounds showed significant anti-inflammatory activity, while some of them exhibited potent analgesic activity. In addition, all compounds exhibited lower ulcerogenic effects than the standard ketoprofen. PMID:23757938

Hamdy, Nehal A; Abdel-Aziz, Hatem A; Kamel, Gehan M; Fakhr, Issa M I

2013-01-01

223

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

PubMed

Different types of complexes derived from the reactions of N-methylisatin Girard's T hydrazone, N,N,N-trimethyl-2-[(2z)-2-(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxo-ethan ammonium chloride (MIGT) and N-methylisatin Girard's P hydrazone, 1-{2-(2z)-2-[(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxoethyl}pyridinium chloride (MIGP) with Fe(3+), Al(3+), Sb(3+) and Sn(2+) salts were synthesized. The isolated complexes were characterized by elemental analyses, molar conductivities, spectral (IR, UV-Vis., (1)H NMR, mass), magnetic moments and thermal measurements. The values of conductance suggest that the complexes are conducting in polar solvents (EtOH, H2O and DMF). The IR spectra suggest that the ligands coordinate in a bidentate and/or tridentate manner via the carbonyl groups of both N-methylisatin and Girard's T and/or P and the (CN) group. The solvents inside and outside the coordination sphere were determined by weight loss and TGA methods. The octahedral geometry of the complexes is confirmed using spectral, magnetic and DFT method from DMOL(3) calculations. The ligands and their metal complexes were tested against different strains of bacteria and fungi. PMID:25467685

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

2014-11-01

224

Highly efficient donor-acceptor hydrazone dyes-inorganic Si/TiO2 hybrid solar cells.  

PubMed

We have synthesized the two donor-bridge-acceptor organic dyes (hydrazone dye 1 (HD1) and hydrazone dye 2 (HD2)) with the aim to enhance intra-molecular charge transfer then characterized by FTIR and NMR. The ground state geometries have been optimized at three different levels of theories, i.e., B3LYP/6-31G(?), B3LYP/6-31G(??) and Hartee-Fock HF/6-31G(??). The absorption spectra and oscillator strengths in different solvents have been computed and compared with the experimental data. The vibrational spectral assignments have been performed on the recorded FTIR spectra based on the theoretical predicted wavenumbers at three different levels of theories. The effect of different solvents (CHCl3, CH3CN and C2H5OH) has been studied on the absorption wavelengths. Furthermore, we have computed the ionization potentials, electron affinities and reorganization energies of studied compounds and shed light on the charge transport properties. The hetero-junction solar cell devices were fabricated by organic-inorganic hetero-junction (Si/TiO2/dye) then the efficiency has been measured by applying the incident power 30, 50 and 70mW/cm(2). The maximum efficiency 3.12% has been observed for HD1. PMID:25766477

Al-Sehemi, Abdullah G; Irfan, Ahmad; Al-Melfi, Mohrah Abdullah M

2015-06-15

225

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

NASA Astrophysics Data System (ADS)

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

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

2015-02-01

226

Synthesis and Antimicrobial Evaluation of Some Novel Thiazole, Pyridone, Pyrazole, Chromene, Hydrazone Derivatives Bearing a Biologically Active Sulfonamide Moiety  

PubMed Central

This study aimed for the synthesis of new heterocyclic compounds incorporating sulfamoyl moiety suitable for use as antimicrobial agents via a versatile, readily accessible N-[4-(aminosulfonyl)phenyl]-2-cyanoacetamide (3). The 2-pyridone derivatives were obtained via reaction of cyanoacetamide with acetylacetone or arylidenes malononitrile. Cycloaddition reaction of cyanoacetamide with salicyaldehyde furnished chromene derivatives. Diazotization of 3 with the desired diazonium chloride gave the hydrazone derivatives 13ae. Also, the reactivity of the hydrazone towards hydrazine hydrate to give Pyrazole derivatives was studied. In addition, treatment of 3 with elemental sulfur and phenyl isothiocyanate or malononitrile furnished thiazole and thiophene derivatives respectively. Reaction of 3 with phenyl isothiocyanate and KOH in DMF afforded the intermediate salt 17 which reacted in situ with 3-(2-bromoacetyl)-2H-chromen-2-one and methyl iodide afforded the thiazole and ketene N,S-acetal derivatives respectively. Finally, reaction of 3 with carbon disulfide and 1,3-dibromopropane afforded the N-[4-(aminosulfonyl) phenyl]-2-cyano-2-(1,3-dithian-2-ylidene)acetamide product 22. All newly synthesized compounds were elucidated by considering the data of both elemental and spectral analysis. The compounds were evaluated for both their in vitro antibacterial and antifungal activities and showed promising results. PMID:24445259

Darwish, Elham S.; Abdel Fattah, Azza M.; Attaby, Fawzy A.; Al-Shayea, Oqba N.

2014-01-01

227

Pharmacological evaluation and preparation of nonsteroidal anti-inflammatory drugs containing an N-acyl hydrazone subunit.  

PubMed

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

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

2014-01-01

228

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

PubMed Central

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

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

2014-01-01

229

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

PubMed

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

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

2015-01-01

230

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...

231

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...

232

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

233

Recrystallization of tetracycline hydrochloride using supercritical anti-solvent process  

Microsoft Academic Search

Tetracycline hydrochloride (TTC) was micronized by an Aerosol Solvent Extraction System (ASES) using supercritical CO2. The effects of solvent, pressure and temperature of CO2, solution concentration, and solution feed rate on particle size were investigated. Mean particle sizes of processed TTC\\u000a were 0.160.31 ?m, but the morphologies of processed particles were affected by agglomeration between the primary particles.\\u000a Mean particle

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

2009-01-01

234

Calculation of the vibrational spectra of betaine hydrochloride  

Microsoft Academic Search

The molecular geometries of betaine hydrochloride, BETHCl, and free protonated betaine, BETH+, were calculated with the 631G(d,p) basis set at the SCF, MP2 and DFT levels of theory. At the SCF level, the minimum energy corresponds to the ionic pair, B+Htctdot;A?, however, the equilibrium Otctdot;Cl distance is 0.14 shorter than the X-ray value. Inclusion of the correlation effects, both

Miroslaw Szafran; Jacek Koput

1997-01-01

235

Structure and vibrational spectra of pyridine betaine hydrochloride  

Microsoft Academic Search

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

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

1997-01-01

236

Enhanced Topical Delivery of Terbinafine Hydrochloride with Chitosan Hydrogels  

Microsoft Academic Search

Chitosan-based carriers have important potential applications for the administration of drugs. In the present study, topical\\u000a gel formulations of terbinafine hydrochloride (T-HCl) were prepared using different types of chitosan at different molecular\\u000a weight, and the antifungal inhibitory activity was evaluated to suggest an effective formulation for the treatment of fungal\\u000a infections. The characteristics of gel formulations were determined with viscosity

?pek zcan; zlem Abac?; Alev Haliki Uztan; Buket Aksu; Hayal Boyac?o?lu; Tamer Gneri; zgen zer

2009-01-01

237

Potentiometric Flow Injection Analysis of Drotaverine Hydrochloride in Pharmaceutical Preparations  

Microsoft Academic Search

Five poly (vinyl chloride) (PVC) membrane electrodes for the determination of drotaverine hydrochloride (DvCl) were constructed and fully characterized in terms of composition, life span, response time, usable pH range, working concentration range, and temperature. The membranes of these electrodes consist of drotaverinium?silicotungstate (Dv?ST), silicomolybdate (Dv?SM), phosphotungstate (Dv?PT), phosphomolybdate (Dv?PM), or tetraphenylborate (Dv?TPB) ion associations dispersed in PVC matrix with

Hosny Ibrahim; Yousry M. Issa

2005-01-01

238

Simple Sensitive Spectrophotometric Determination of Isoniazid and Ritodrine Hydrochloride  

Microsoft Academic Search

A novel coupling reagent was used for simple, rapid, and sensitive spectrophotometric determination of isoniazid (1NH) and ritodrine hydrochloride (RTH) in pure form or in pharmaceutical preparations of it. The method is based on the diazotization of 4,4-methylene-bis-m-nitroaniline followed by a coupling reaction with either INH or RTH in hydrochloric acid medium. The resulting colored products have absorption maxima at

G. Krishnamurthy Naidu; K. Suvardhan; K. Suresh Kumar; D. Rekha; B. S. Sastry; P. Chiranjeevi

2005-01-01

239

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

Code of Federal Regulations, 2010 CFR

...2010-07-01 2010-07-01 false Poly(hexamethylenebiguanide) hydrochloride...Exemptions From Tolerances 180.1280 Poly(hexamethylenebiguanide) hydrochloride...from the requirement of a tolerance. Poly(hexamethylenebiguanide)...

2010-07-01

240

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

Code of Federal Regulations, 2011 CFR

...2011-07-01 2011-07-01 false Poly(hexamethylenebiguanide) hydrochloride...Exemptions From Tolerances 180.1280 Poly(hexamethylenebiguanide) hydrochloride...from the requirement of a tolerance. Poly(hexamethylenebiguanide)...

2011-07-01

241

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

242

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

PubMed Central

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

Denmark, Scott E.; Ares, Jeffrey J.

2011-01-01

243

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

Federal Register 2010, 2011, 2012, 2013, 2014

...Clonidine Hydrochloride) Extended- Release Tablets, 0.1 Milligram and 0.2 Milligram...clonidine hydrochloride) Extended-Release Tablets, 0.1 milligram (mg) and 0.2 mg...clonidine hydrochloride extended-release tablets, 0.1 mg and 0.2 mg, if all...

2012-02-13

244

78 FR 38053 - Determination That OPANA ER (Oxymorphone Hydrochloride) Drug Products Covered by New Drug...  

Federal Register 2010, 2011, 2012, 2013, 2014

...hydrochloride (HCl)) Extended-Release Tablet products approved under new drug application...for oxymorphone HCl extended-release tablets if all other legal and regulatory requirements...oxymorphone hydrochloride) Extended-Release Tablets approved under NDA 21-610 were...

2013-06-25

245

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

Federal Register 2010, 2011, 2012, 2013, 2014

...hydrochloride; penicillin G potassium, USP; and tetracycline hydrochloride...200-347 for Penicillin G Potassium, USP, all soluble powders administered...Penicillin V powder. * * * * * 0 8. In Sec. 520.1696d, revise...2012-8322 Filed 4-6-12; 8:45 am] BILLING CODE...

2012-04-09

246

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

247

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

NASA Astrophysics Data System (ADS)

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

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

2006-08-01

248

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

NASA Technical Reports Server (NTRS)

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

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

1973-01-01

249

Effect of landiolol hydrochloride on suxamethonium-induced neuromuscular block  

Microsoft Academic Search

PurposeThe aim of this study was to examine the effect of landiolol hydrochloride, an ultrashort-acting ?1-blocker, on suxamethonium-induced neuromuscular block.\\u000a \\u000a \\u000a \\u000a MethodsThirty patients were randomly allocated to receive a loading dose of landiolol, 0.125 mgkg?1min?1 for 1 min, followed by an infusion at 0.04 mgkg?1min?1, or placebo. Twenty minutes after the infusion of landiolol or placebo, suxamethonium 1 mgkg?1 was administered

Takahiro Suzuki; Mayu Aono; Tomomi Isaka; Eri Miyake; Naoko Fukano; Shigeru Saeki; Setsuro Ogawa

2009-01-01

250

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 1 mg/mL, were 62.1%, 65.5% and 65.5%, respectively, exhibited more pronounced insecticidal activity compared to toosendanin at 1 mg/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

2013-10-15

251

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. PMID:21806053

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

2011-01-01

252

A novel mixed valent Cu(II)-Cu(I) 2D framework made of a hydrazone and ?-SCN bridged metallacyclic loops cross-linked by ?3-SCN chains.  

PubMed

A mixed valent copper complex [Cu(II)Cu(I)(L)(?-SCN)(?(3)-SCN)](n) (LH = N'-((pyridin-2-yl)methylene)acetohydrazide) has been synthesized and characterized. It is a unique example of a 2D mixed valent Cu(II)-Cu(I) interlinked molecular assembly with a very unusual bridging property of the hydrazone ligand. An extraordinary in situ partial Cu(II)? Cu(I) reduction is observed in this system at room temperature. PMID:22930162

Sadhukhan, Dipali; Rizzoli, Corrado; Garribba, Eugenio; Gmez-Garca, Carlos J; Yahia-Ammar, Akram; Charbonnire, Loc J; Mitra, Samiran

2012-10-14

253

Solid-supported hydrazone of 4-(4'-formyl-3'-methoxyphenoxy)butyric acid as a new traceless linker for solid-phase synthesis.  

PubMed

The use of a hydrazine derived from a backbone amide linker as a new hydrazone-based traceless linker for solid-phase organic synthesis is described. The stability of the linker was tested under various conditions, including treatment with acids, bases, and borohydrides. Final compounds can be released by selective cleavage using trimethylsilanolate. To demonstrate the versatility of the linker, the synthesis of a model compound under various reaction conditions was performed with good results. PMID:25536078

Okorochenkov, Sergei; Burglova, Kristyna; Popa, Igor; Hlavac, Jan

2015-01-16

254

Synthesis, crystal structure, antioxidation and DNA-binding properties of the Ln complexes with 1-phenyl-3-methyl-5-hydroxypyrazole-4-carbaldhyde-(benzoyl)hydrazone  

Microsoft Academic Search

Two lanthanide complexes (Ln=La, Pr) with a PMFP Schiff-base, 1-phenyl-3-methyl-5-hydroxypyrazole-4-carbaldhyde-(benzoyl)hydrazone (H2L) were synthesized and characterized. The crystal structure of the La complex was determined by single-crystal X-ray diffraction, the coordination polyhedron is a tricapped trigonal prism configuration with the nine-coordinate atoms composed of three nitrogens and six oxygens from three ligands. The complex crystallized in the monoclinic lattice with a

Hong-Ge Li; Zheng-Yin Yang; Bao-Dui Wang; Jin-Cai Wu

2010-01-01

255

Synthesis, characterization, and DNA-binding properties of the Ln(III) complexes with 6-hydroxy chromone-3-carbaldehyde-(2?-hydroxy) benzoyl hydrazone  

Microsoft Academic Search

A new ligand, 6-hydroxy chromone-3-carbaldehyde-(2?-hydroxy) benzoyl hydrazone (L), was prepared by condensation of 6-hydroxy-3-carbaldehyde chromone (CDC) with 2-hydroxy benzoyl hydrazine. Its four rare earth complexes have been synthesized and characterized on the basis of elemental analyses, molar conductivities, mass spectra, 1H NMR, thermogravimetry\\/differential thermal analysis (TGDTA), UVvis spectra, fluorescence spectra, and IR spectra. The general formula of the complexes is

Bao-dui Wang; Zheng-Yin Yang; Tian-rong Li

2006-01-01

256

Oral administration of diazepam and promazine hydrochloride to immobilize pronghorn.  

PubMed

Oral tranquilizers were mixed with a grain bait and fed to pronghorn (Antilocapra americana) in an attempt to immobilize and thus facilitate their capture. Diazepam, administered at 6 mg/kg body weight immobilized a tame pronghorn fawn within 30 min. Tranquilization was still apparent after 8 h. A minimum dose of 23 mg/kg body weight was necessary to immobilize a wild adult pronghorn. Immobilization occurred after 60 min and tranquilization was apparent 24 h post ingestion. Excitement severely impeded the effect of the drug and although easily captured, the animal struggled wildly when handled. Wild pronghorn fawns showed moderate tranquilization when administered diazepam at 23 mg/kg body weight but were unapproachable. Doses of diazepam between 13 and 23 mg/kg body weight were used to capture tame yearling and adult pronghorn held in a 132 ha enclosure. A dose of 23 mg/kg body weight was excessive in that the animals did not recover for 48 to 54 h post ingestion and had difficulty maintaining a sternal bedding position. Diazepam at 13 mg/kg body weight failed to tranquilize the animals sufficiently for easy capture. Promazine hydrochloride at doses of 2 to 17 mg/kg body weight, given orally to wild pronghorn fawns and an adult, did not produce visible signs of tranquilization. Animals refused to eat bait containing doses of promazine hydrochloride greater than 17 mg/kg body weight. PMID:7097876

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

1982-01-01

257

[A case of anaphylactic shock induced by pirarubicin hydrochloride].  

PubMed

A 75-year-old man was admitted to our hospital for treatment of superficial bladder tumor. Transurethral resection (TUR) was performed and histopathological examination revealed a transitional cell carcinoma (G2). Despite one course of post-TUR bladder instillation therapy using pirarubicin hydrochloride, carcinoma in situ (CIS) was found 4 months later. CIS disappeared after another course of bladder instillation therapy using BCG; but, it recurred a month later. BCG bladder instillation therapy was performed again, and no malignant cells were detected in the urinary tract thereafter. Four months later, lung metastasis was diagnosed and an MVAC regimen (cisplatin, methotrexate, vinblastin adriamycin) was administered. However, anaphylactic shock was induced by intravenous injection of pirarubicin hydrochloride, so this therapy was stopped in the middle of the second course. Even though the lung metastasis disappeared once after the same MVAC treatment, it recurred the following year. At that time, 3 courses of a cisplatin-methotrexate-vinblastin regimen were administered, and a complete response was achieved. PMID:15188619

Mitsuhashi, Makoto; Iwata, Hiroyuki; Kiyota, Atsuhiko; Kamizuru, Masato; Nakatani, Tatsuya

2004-04-01

258

Determination of isoxsuprine hydrochloride by sequential injection visible spectrophotometry.  

PubMed

An automated sequential injection (SI) spectrophotometric method for the determination of isoxsuprine hydrochloride is described. The method is based on the condensation of aminoantipyrine with phenols (isoxsuprine hydrochloride) in the presence of an alkaline oxidizing agent (potassium hexacyanoferrate) to yield a pink colored product, the absorbance of which is monitored at 507 nm. Chemical as well as physical SI parameters that affect the signal response have been optimized in order to get better sensitivity, higher sampling rate and better reagent economy. Using the optimized aforesaid parameters, a linear relationship between the relative peak height and concentration was obtained in the range 1-60 mg l-1. The detection limit (as 3sigma value) was 0.3 mg l-1 and precision was 1.4% and 1.6% at 5 and 10 mg l-1, respectively. As compared to previous reports, wide linear range, low detection limit, and highly economical reagent consumption are the advantages of this automated method. PMID:15935351

Beyene, Negussie W; Van Staden, Jacobus F; Stefan, Raluca-Ioana; Aboul-Enein, Hassan Y

2005-01-01

259

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

NASA Astrophysics Data System (ADS)

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

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

2008-03-01

260

Lanthanide complexes of tritopic bis(hydrazone) ligands: single-molecule magnet behavior in a linear Dy(III)3 complex.  

PubMed

Tritopic pyridinebis(hydrazone)-based ligands typically produce square M(9) [3 3] grid complexes with first-row transition-metal ions (e.g., M = Mn, Fe, Co, Cu, Zn), but with larger lanthanide ions, such coordination motifs are not produced, and instead linear trinuclear complexes appear to be a preferred option. The reaction of 2pomp [derived from pyridine-2,6-bis(hydrazone) and 2-acetylpyridine] with La(III), Gd(III), and Dy(III) salts produces helical linear trinuclear [Ln(3)(2pomp)(2)]-based complexes, where each metal ion occupies one of the three tridentate ligand pockets. Two ligands encompass the three metal ions, and internal connections between metal ions occur through ?-O(hydrazone) bridges. Coligands include benzoate, nitrate, and N,N-dimethylformamide. The linear Dy(III)(3) complex exhibits single-molecule magnet behavior, demonstrated through alternating-current susceptibility measurements. Slow thermal magnetic relaxation was detected in an external field of 1800 Oe, where quantum-tunneling effects were suppressed (U(eff) = 14 K). PMID:22191543

Anwar, Muhammad U; Tandon, Santokh S; Dawe, Louise N; Habib, Fatemah; Murugesu, Muralee; Thompson, Laurence K

2012-01-16

261

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

PubMed Central

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

Yu, Cuicui; Wang, Junke

2013-01-01

262

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

PubMed

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

Amorim da Costa, A; Leite, J E

2001-02-16

263

X-ray crystallographic, electrochemical and spectroscopic properties of 2-pyridinio 2-pyridyl ketone phenyl hydrazone chloride hydrate  

NASA Astrophysics Data System (ADS)

In contrast to the reaction between di-2-pyridyl ketone with a variety of hydrazines or hydrazides in refluxing acidified alcoholic solution to form unprotonated di-2-pyridyl ketone hydrazones (dpkhydrazones), the reaction between di-2-pyridyl ketone and phenyl hydrazine hydrochloric acid under the same conditions gave unprecedented pyridyl protonated 2-pyridinio 2-pyridyl ketone phenyl hydrazone chloride hydrate, dpkphhHCl3H 2O. Crystals of dpkphhHCl3H 2O obtained from an ethanolic solution of dpkphhHCl3H 2O that contains a few drops of HCl are in the centric triclinic space group P-1. Structure analysis reveals non-coplanar dpkphhH + along with a chloride anion and three water molecules. The molecules pack show infinite stacks of anti-parallel dpkphhH + locked to the chloride anion and water molecules via novel fused hydrogen bonded oxygen-chloride four and six-membered cyclic rings propagating between the stacks. Electrochemical measurements on dpkphhHCl3H 2O in non-aqueous solvents show solvent dependence, single and multi-electronic transfers in DMF and in CH 3CN single electronic redox transfers. The reversibility of the second electronic reduction following the first irreversible electronic transfer hints to the stability of electrochemically generated intermediate following the sequential electronic transfers. In contrast to the optical behavior of a variety unprotonated and metal coordinated dpkhydrazones, protonation of one pyridine ring in dpkphhHCl3H 2O decreases the electron density on the pyridine ring ceases the intraligand charge transfer electronic transition and renders the protonated systems (dpkphhHCl3H 2O plus surrounding solvent molecules) insensitivity to their surroundings although the spectra show strong solvent-solute interactions. 1H NMR measurements on dpkphhHCl3H 2O in non-aqueous media reveal sensitivity to solvent and temperature variations that point to strong solvent-solute interactions. The amide and water protons show sensitivity to solvent and temperature variations higher than the aromatic protons consistent with their participation in non-covalent hydrogen bonds.

Bakir, Mohammed; Hassan, Ishmael; Johnson, Toni; Brown, Ordel; Green, Orville; Gyles, Colin; Coley, Michael D.

2004-01-01

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

Crystal structure of bis(pyridine betaine) hydrochloride monohydrate  

NASA Astrophysics Data System (ADS)

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

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

1990-04-01

266

Crystal structure of BIS(Betaine) hydrochloride monohydrate  

NASA Astrophysics Data System (ADS)

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

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

1990-11-01

267

Conductivity scaling and thermoelectric properties of polyaniline hydrochloride  

NASA Astrophysics Data System (ADS)

We report on the thermoelectric properties of the polyaniline hydrochloride as a function of the temperature. In order to stress the influences of both the synthesis and the samples preparation on the thermoelectric efficiency, we have systematically measured the electrical conductivity, the thermopower, and the thermal conductivity. We show that several parameters such as the polymerization temperature and the pressure used to compress powders are crucial in order to optimize the thermoelectric performance. The microscopic origins of the transport coefficients are also discussed. In particular, the overall dataset of the measured electrical conductivity is found to scale onto a master curve involving a unique microscopic length, which coincides with the total bond length of the repeating unit of the polymeric chain. We believe that the drawn conclusions can hold for most of the conducting polymers and are thus potentially generic.

Limelette, P.; Schmaltz, B.; Brault, D.; Gouineau, M.; Autret-Lambert, C.; Roger, S.; Grimal, V.; Tran Van, F.

2014-01-01

268

Residual solvent analysis in hydrochloride salts of active pharmaceutical ingredients.  

PubMed

GMP conditions commands to control adequately the quality of APIs by checking the levels of residual solvents. Organic solvents such as acetone, ethyl acetate, isopropyl alcohol, methanol, tetrahydrofuran and toluene frequently used in pharmaceutical industry for the manufacturing of Active Pharmaceutical ingredients (APIs). A selective Gas Chromatographic (GC) method has been developed and validated as per ICH guidelines for residual solvent analysis in 10 different hydro chloride salts of APIs. Residual solvents in APIs were monitored using gas chromatography (GC) with Flame Ionisation detector (FID). The separation was carried out on BP 624 column (30 mx0.53 mm i.d.x0.25 m coating thickness), using GC 17 A shimadzu, with nitrogen as carrier gas in the split mode by direct injection method. The method described is simple, sensitive, rugged, reliable and reproducible for the quantitation of acetone, ethyl acetate, isopropyl alcohol, methanol, tetrahydrofuran and toluene at residual level from hydrochloride chloride salts of APIs. PMID:19783521

Puranik, S B; Pawar, Varun R; Lalitha, N; Pai, P N Sanjay; Rao, G K

2009-10-01

269

Determination of tetracycline hydrochloride by terahertz spectroscopy with PLSR model.  

PubMed

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

Qin, Jianyuan; Xie, Lijuan; Ying, Yibin

2015-03-01

270

Coated hydralazine hydrochloride beads for sustained release after oral administration.  

PubMed

Hydralazine hydrochloride is an antihypertensive used alone or in combination with isosorbide nitrate for the treatment of congestive heart failure. Since control of blood pressure should be continuous, sustained release delivery of this drug is considered therapeutically beneficial. Core beads for oral administration of this drug were prepared by extrusion-spheronization. Using experimental design to define the coat that was applied, the core beads were coated using a fluid bed coater to different coat thickness with combinations of two commercially available products dissolved in a hydroalcoholic solvent. The coat is a film with a combination of ethylcellulose and hydroxypropylcellulose that can provide desirable release profiles. Visually spherical and rugged bead products were obtained. Two products were identified that exhibited essentially a zero order release profile following a 2-h lag time with release of greater than 70% of the drug over the next 10?h in simulated intestinal fluid. PMID:23057650

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

2013-09-01

271

Sustained release microspheres of ropinirole hydrochloride: effect of process parameters.  

PubMed

An emulsion solvent evaporation method was employed to prepare microspheres of ropinirole hydrochloride, a highly water soluble drug, by using ethylcellulose and PEG with the help of 32 full factorial design. The microspheres were made by incorporating the drug in a polar organic solvent, which was emulsified using liquid paraffin as an external oil phase. Effects of various process parameters such as viscosity of the external phase, selection of the internal phase, surfactant selection and selection of stirring speed were studied. Microspheres were evaluated for product yield, encapsulation efficiency and particle size. Various drug/ethylcellulose ratios and PEG concentrations were assayed. In vitro dissolution profiles showed that ethylcellulose microspheres were able to control release of the drug for a period of 12 h. PMID:22202196

Avachat, Amelia M; Bornare, Pralhad N; Dash, Rakesh R

2011-12-01

272

Multilayer Films and Capsules of Sodium Carboxymethylcellulose and Polyhexamethylenguanidine Hydrochloride  

NASA Astrophysics Data System (ADS)

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

Guzenko, Nataliia; Gabchak, Oleksandra; Pakhlov, Evgenij

273

Potentiometric batch and flow injection analysis of betaine hydrochloride.  

PubMed

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

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

2007-01-01

274

Instability of the hydrochloride salts of cathinone derivatives in air.  

PubMed

We observed the decomposition of the hydrochloride salt of ?-pyrrolidinoheptanophenone (?-PHPP-HCl), a newly distributed pyrrolidine-type cathinone derivative when 2.5ng of this substance was placed in glass test tubes and stored in a refrigerator for 3 days. To further investigate this phenomenon, we studied the (i) time course of the residual ratios of ?-PHPP-HCl when a small amount (10?g) of ?-PHPP-HCl was stored in glass vials in air at room temperature; (ii) identification of the decomposition products of ?-PHPP-HCl; (iii) effect of air on the decomposition process; (iv) effect of the added amounts of ?-PHPP-HCl on its decomposition; and (v) comparison of the stability between various cathinone derivatives and their decomposition products. The decomposition of ?-PHPP-HCl occurred in air and increased with time. Two possible decomposition products, ?-(2?-oxopyrrolidino)heptanophenone and ?-PHPP-N-oxide, were identified. These products were formed by oxygen in air because the yield significantly decreased by storing them in a vacuum desiccator. With the decrease in the amount of ?-PHPP-HCl, the residual ratios decreased and amount of the decomposition products increased. This indicates that the decomposition of ?-PHPP-HCl occurred on the upper surface of the samples. The hydrochloride salts of other cathinone derivatives were also unstable in air, and the residual ratios observed were different depending on the compounds. The pyrrolidine-type cathinone derivatives afforded two types of decomposition products, which were presumed to be 2?-oxo and N-oxide derivatives, similar to ?-PHPP-HCl. In contrast, secondary amine-type cathinone derivatives showed different decomposition patterns, possibly including the dealkylated derivative. These findings may be very useful for the future toxicological analysis of cathinone derivatives. PMID:25594691

Tsujikawa, Kenji; Yamamuro, Tadashi; Kuwayama, Kenji; Kanamori, Tatsuyuki; Iwata, Yuko T; Inoue, Hiroyuki

2015-03-01

275

Sinomenine hydrochloride protects against polymicrobial sepsis via autophagy.  

PubMed

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

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

2015-01-01

276

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

PubMed

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

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

2002-06-01

277

Formulation Optimization of Propranolol Hydrochloride Microcapsules Employing Central Composite Design  

PubMed Central

A central composite design was employed to produce microcapsules of propranolol hydrochloride by o/o emulsion solvent evaporation technique using a mixture of cellulose acetate butyrate as coat material and span-80 as an emulsifier. The effect of formulation variables namely levels of cellulose acetate butyrate (X1) and percentage of Span-80 (X2) on encapsulation efficiency (Y1), drug release at the end of 1.5 h (Y2), 4 h (Y3), 8 h (Y4), 14 h (Y5), and 24 h (Y6) were evaluated using the F test. Mathematical models containing only the significant terms were generated for each response parameter using multiple linear regression analysis and analysis of variance. Both the formulation variables exerted a significant influence (P <0.05) on Y1 whereas the cellulose acetate butyrate level emerged as the lone factor which significantly influenced the other response parameters. Numerical optimization using desirability approach was employed to develop an optimized formulation by setting constraints on the dependent and independent variables. The experimental values of Y1, Y2, Y3, Y4, Y5, and Y6 for the optimized formulation was found to be 92.861.56% w/w, 29.581.22%, 48.562.56%, 60.852.35%, 76.233.16% and 95.122.41%, respectively which were in close agreement with those predicted by the mathematical models. The drug release from microcapsules followed first order kinetics and was characterized by Higuchi diffusion model. The optimized microcapsule formulation developed was found to comply with the USP drug release test-1 for extended release propranolol hydrochloride capsules. PMID:20046763

Shivakumar, H. N.; Patel, R.; Desai, B. G.

2008-01-01

278

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

Code of Federal Regulations, 2013 CFR

...greater the concentration of free formaldehyde in a resin, the more of that formaldehyde will be in the polymeric form...analyzed must contain enough free formaldehyde so that the...hydroxylamine hydrochloride will produce sufficient...

2013-07-01

279

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

Code of Federal Regulations, 2012 CFR

...greater the concentration of free formaldehyde in a resin, the more of that formaldehyde will be in the polymeric form...analyzed must contain enough free formaldehyde so that the...hydroxylamine hydrochloride will produce sufficient...

2012-07-01

280

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

Code of Federal Regulations, 2014 CFR

...greater the concentration of free formaldehyde in a resin, the more of that formaldehyde will be in the polymeric form...analyzed must contain enough free formaldehyde so that the...hydroxylamine hydrochloride will produce sufficient...

2014-07-01

281

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

Code of Federal Regulations, 2011 CFR

...greater the concentration of free formaldehyde in a resin, the more of that formaldehyde will be in the polymeric form...analyzed must contain enough free formaldehyde so that the...hydroxylamine hydrochloride will produce sufficient...

2011-07-01

282

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

Federal Register 2010, 2011, 2012, 2013, 2014

...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

283

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

Federal Register 2010, 2011, 2012, 2013, 2014

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

2012-02-21

284

77 FR 41411 - Determination That TOPOTECAN INJECTION (Topotecan Hydrochloride) 1 Milligram (Base)/1 Milliliter...  

Federal Register 2010, 2011, 2012, 2013, 2014

...Determination That TOPOTECAN INJECTION (Topotecan Hydrochloride) 1 Milligram (Base)/1 Milliliter, 3 Milligram (Base)/3 Milliliter, 4 Milligram (Base)/4 Milliliter, Was Not Withdrawn From Sale for Reasons of Safety or...

2012-07-13

285

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

Microsoft Academic Search

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

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

2005-01-01

286

Bioavailability of doxycycline monohydrate. A comparison with equivalent doses of doxycycline hydrochloride.  

PubMed

Two derivatives of doxycycline, the monohydrate-free base and the hydrochloride salt were given orally to 12 volunteers in a crossover study. There was no difference in absorption and bioavailability between the two preparations. Secondary plasma peaks indicating reabsorption were noticed for both derivatives. Doxycycline monohydrate, proven to have a lower risk of inducing esophageal lesions, is a good alternative to the hydrochloride salt in oral treatment. PMID:6697815

Malmborg, A S

1984-01-01

287

Experimental studies on the long-term effects of methylphenidate hydrochloride  

Microsoft Academic Search

Toxicology and carcinogenesis studies of methylphenidate hydrochloride, a drug used in the treatment of attention-deficient disorders, were performed in F344 rats and B6C3F1 mice. In these studies, methylphenidate hydrochloride was administered for 2 years at doses of 0, 100, 500 or 1000 ppm in the feed to rats and at doses of 0, 50, 250, 500 ppm to mice in

June K. Dunnick; James R. Hailey

1995-01-01

288

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

Microsoft Academic Search

Raman vibrational spectroscopy, at 298 K, has been used to study the hydration of betaine hydrochloride and betaine in the concentration range 0.52 M. The observed changes in the internal vibrations of the solutes, namely, in the C?O, COO? and CH stretchings, and in the components of the OH stretching band are consonant with anionic waterbetaine and betaine hydrochloride dimeric

Antnio Amorim da Costa; Joana E. S. Leite

2001-01-01

289

Comparison of Anesthetic Potency of Benzocaine Hydrochloride and MS222 in Two Freshwater Fish Species  

Microsoft Academic Search

The hydrochloride of ethyl p-aminobenzoate was synthesized and its anesthetic potency compared with that of MS-222 at concentrations of 50,80, and 100 mg\\/L. The free compound of these agents in fish blood was also determined. The results indicate that benzocaine hydrochloride is a more effective anesthetic than MS-222 at the concentrations applied. It must be pointed out, however, that benzocaine

J. T. Ferreira; G. L. Smit; H. J. Schoonbee; C. W. Holzapfel

1979-01-01

290

An analytical chemical study of pilocarpine hydrochloride and its hydrolysis products  

E-print Network

. . cept ? . hc optical rotation is appli- cable when the drug is handled and stored in aqueous solution. Pre- sent pharmaceutical practice calls f' or handling and storing pilocar- pine hydrochloride in aqueous solution. It is used as an opthalmic... Present commercial pharmaceutical practice in the preparation of pilocarpine hydrochloride solutions vary somewhat with different phar~m~ceutical companies. In general the solutions are prepared in commercial laboratories, sealed in sterile containers...

Ibert, Edward R

1956-01-01

291

Voltammetric assay of anti-vertigo drug betahistine hydrochloride in sodium lauryl sulphate  

Microsoft Academic Search

Assay and electrochemical behaviour of betahistine hydrochloride in BrittonRobinsons (BR) buffer of pH range 2.512.0 at a glassy carbon electrode have been investigated. Addition of anionic surfactant (sodium lauryl sulphate) to the betahistine hydrochloride solution containing electrolyte enhanced the reduction current signal while neutral surfactant (Tween-20) and cationic surfactant cetyl trimethylammonium bromide (CTAB) showed an opposite effect. Voltammograms of betahistine

Rajeev Jain; Rajeev Kumar Yadav; Jahangir Ahmad Rather

2010-01-01

292

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

293

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

294

Solid state characterization of hydroxyprocaine hydrochloride. Crystal polymorphism of local anaesthetic drugs, part VIII  

Microsoft Academic Search

Two polymorphic and a pseudopolymorphic crystal form of the local anaesthetic drug hydroxyprocaine hydrochloride (4-Butylamino-2-hydroxybenzoic acid 2-dimethylaminoethyl ester hydrochloride, HPCHC) are characterized by thermal analysis (hot stage microscopy, differential scanning calorimetry, thermogravimetry), spectroscopy (FTIR-, FT-Raman-, SSNMR-spectroscopy), powder X-ray diffractometry and water vapor sorption analysis. The formation and thermodynamic stability of the different solid phases is described and presented in a

A. C. Schmidt; I. Schwarz

2005-01-01

295

In vitro effects of artemisinin ether, cycloguanil hydrochloride (alone and in combination with sulfadiazine), quinine sulfate, mefloquine, primaquine phosphate, trifluoperazine hydrochloride, and verapamil on Toxoplasma gondii.  

PubMed

The in vitro effect of the following antimicrobial agents on Toxoplasma gondii tachyzoites were studied: artemisinin ether (arteether), cycloguanil hydrochloride (cycloguanil), mefloquine, primaquine phosphate, and quinine sulfate, as well as the calcium channel blocker verapamil and the calmodulin inhibitor trifluoperazine hydrochloride. Arteether at > or = 0.5 micrograms/ml and cycloguanil at > or = 1.0 micrograms/ml inhibited T. gondii in vitro. Cycloguanil (2.5 micrograms/ml) combined with a noninhibitory concentration of sulfadiazine (25 micrograms/ml) inhibited T. gondii more than cycloguanil alone. Neither primaquine phosphate, mefloquine, nor quinine sulfate had an inhibitory effect on intracellular T. gondii. Verapamil and trifluoperazine hydrochloride were not inhibitor at lower physiologic concentrations, but higher physiologic concentrations were toxic to cell cultures in vitro and therefore our assay could not be used to assess their effects. PMID:8092843

Holfels, E; McAuley, J; Mack, D; Milhous, W K; McLeod, R

1994-06-01

296

In vitro effects of artemisinin ether, cycloguanil hydrochloride (alone and in combination with sulfadiazine), quinine sulfate, mefloquine, primaquine phosphate, trifluoperazine hydrochloride, and verapamil on Toxoplasma gondii.  

PubMed Central

The in vitro effect of the following antimicrobial agents on Toxoplasma gondii tachyzoites were studied: artemisinin ether (arteether), cycloguanil hydrochloride (cycloguanil), mefloquine, primaquine phosphate, and quinine sulfate, as well as the calcium channel blocker verapamil and the calmodulin inhibitor trifluoperazine hydrochloride. Arteether at > or = 0.5 micrograms/ml and cycloguanil at > or = 1.0 micrograms/ml inhibited T. gondii in vitro. Cycloguanil (2.5 micrograms/ml) combined with a noninhibitory concentration of sulfadiazine (25 micrograms/ml) inhibited T. gondii more than cycloguanil alone. Neither primaquine phosphate, mefloquine, nor quinine sulfate had an inhibitory effect on intracellular T. gondii. Verapamil and trifluoperazine hydrochloride were not inhibitor at lower physiologic concentrations, but higher physiologic concentrations were toxic to cell cultures in vitro and therefore our assay could not be used to assess their effects. PMID:8092843

Holfels, E; McAuley, J; Mack, D; Milhous, W K; McLeod, R

1994-01-01

297

Structure investigation of three hydrazones Schiff's bases by spectroscopic, thermal and molecular orbital calculations and their biological activities  

NASA Astrophysics Data System (ADS)

Three Schiff's bases AI (2(1-hydrazonoethyl)phenol), AII (2, 4-dibromo 6-(hydrazonomethyl)phenol) and AIII (2(hydrazonomethyl)phenol) were prepared as new hydrazone compounds via condensation reactions with molar ratio (1:1) of reactants. Firstly by reaction of 2-hydroxy acetophenone solution and hydrazine hydrate; it gives AI. Secondly condensation between 3,5-dibromo-salicylaldehyde and hydrazine hydrate gives AII. Thirdly condensation between salicylaldehyde and hydrazine hydrate gives AIII. The structures of AI-AIII were characterized by elemental analysis (EA), mass (MS), FT-IR and 1H NMR spectra, and thermal analyses (TG, DTG, and DTA). The activation thermodynamic parameters, such as, ?E?, ?H?, ?S? and ?G? were calculated from the TG curves using Coats-Redfern method. It is important to investigate their molecular structures to know the active groups and weak bond responsible for their biological activities. Consequently in the present work, the obtained thermal (TA) and mass (MS) practical results are confirmed by semi-empirical MO-calculations (MOCS) using PM3 procedure. Their biological activities have been tested in vitro against Escherichia coli, Proteus vulgaris, Bacillissubtilies and Staphylococcus aurous bacteria in order to assess their anti-microbial potential.

Belal, Arafa A. M.; Zayed, M. A.; El-Desawy, M.; Rakha, Sh. M. A. H.

2015-03-01

298

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

PubMed

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

Mohammed, Khaled O; Nissan, Yassin M

2014-10-01

299

Structure investigation of three hydrazones Schiff's bases by spectroscopic, thermal and molecular orbital calculations and their biological activities.  

PubMed

Three Schiff's bases AI (2(1-hydrazonoethyl)phenol), AII (2, 4-dibromo 6-(hydrazonomethyl)phenol) and AIII (2(hydrazonomethyl)phenol) were prepared as new hydrazone compounds via condensation reactions with molar ratio (1:1) of reactants. Firstly by reaction of 2-hydroxy acetophenone solution and hydrazine hydrate; it gives AI. Secondly condensation between 3,5-dibromo-salicylaldehyde and hydrazine hydrate gives AII. Thirdly condensation between salicylaldehyde and hydrazine hydrate gives AIII. The structures of AI-AIII were characterized by elemental analysis (EA), mass (MS), FT-IR and (1)H NMR spectra, and thermal analyses (TG, DTG, and DTA). The activation thermodynamic parameters, such as, ?E(?), ?H(?), ?S(?) and ?G(?) were calculated from the TG curves using Coats-Redfern method. It is important to investigate their molecular structures to know the active groups and weak bond responsible for their biological activities. Consequently in the present work, the obtained thermal (TA) and mass (MS) practical results are confirmed by semi-empirical MO-calculations (MOCS) using PM3 procedure. Their biological activities have been tested in vitro against Escherichia coli, Proteus vulgaris, Bacillissubtilies and Staphylococcus aurous bacteria in order to assess their anti-microbial potential. PMID:25437844

Belal, Arafa A M; Zayed, M A; El-Desawy, M; Rakha, Sh M A H

2015-03-01

300

Synthesis, structure, spectral, thermal and first-order molecular hyperpolarizability of 4-benzoylpyridine isonicotinyl hydrazone monohydrate single crystals.  

PubMed

Single crystals of 4-benzoylpyridine isonicotinyl hydrazone monohydrate were grown by slow evaporation solution growth technique from ethanol at room temperature. It belongs to triclinic system with space group P1 and the cell parameters are, a=8.9250(2) , b=9.1540(2) , c=10.87500(10) and V=797.88(3) (3). Powder XRD closely resembles with that of simulated pattern from single crystal XRD. The characteristic functional groups present in the molecule are confirmed by FT-IR and FT-Raman analyses. The crystal is transparent in the visible region having a lower optical cut-off at ?420 nm and the band gap energies are estimated by the application of Kubelka-Munk algorithm. Thermal analysis by TG/DTA indicates the stability of the material. The scanning electron microscopy studies reveal the surface morphology of the as-grown crystal. Mass spectrometry provides information pertaining to the structure and molecular weight of the compound. Theoretical calculations were performed using Hartree-Fock method with 6-31G(d,p) as the basis set for to derive the optimized geometry, dipole moment and first-order molecular hyperpolarizality (?) values. PMID:24508881

Meenatchi, V; Muthu, K; Rajasekar, M; Meenakshisundaram, S P

2014-04-24

301

Coordination diversity of new mononuclear ONS hydrazone with transition metals: Synthesis, characterization, molecular modeling and antimicrobial studies  

NASA Astrophysics Data System (ADS)

The mononuclear hydrazone ligand, H2L, a condensation product of 4-amino-6-methyl-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one with 2-hydroxy-1-naphthaldehyde and its metal chelates of Cu(II), Ni(II), Co(II), Zn(II), Cd(II), VO(IV) and UO2(VI) ions were synthesized and characterized using elemental analyses, spectral, magnetic and molar conductance studies as well as thermal gravimetric analysis (TGA). The physico-chemical studies support that the ligand acts as mono- or dibasic tridentate ONS donor toward metal ions forming a mononuclear square planar, tetrahedral, square pyramidal and octahedral geometrical arrangements except UO2(VI) complex in which the metal ion is octa-coordinated. The ligand field parameters, Dq, B and ? values, in the case of the cobalt and nickel complexes are calculated. The kinetics of the thermal decomposition for some metal complexes studied and their thermodynamic parameters were reported. Structural parameters of the ligand and its metal chelates have been calculated and correlated with the experimental data. The ligand and its metal chelates were screened for their antimicrobial activity against Staphylococcus aureus and Bacillus subtilis as Gram-positive bacteria, Escherichia coli and Salmonella typhimurium as Gram-negative bacteria and Candida albicans as fungus strain.

Adly, Omima M. I.; Taha, A.

2013-04-01

302

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

303

Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation  

PubMed Central

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

Eassa, Bayoumy I; El-Shazly, Mohamed A

2013-01-01

304

Formation of methyl benzoate from cocaine hydrochloride under different temperatures and humidities  

NASA Astrophysics Data System (ADS)

It is of interest for drug enforcement agencies to know the fate of cocaine hydrochloride when in storage. Reported here are results obtained on vapor samples collected from cocaine hydrochloride stored under several combinations of temperature and humidity. The storage conditions were varied from ambient temperature to 40 degrees C and from zero humidification to 80 percent relative humidity. Cocaine hydrochloride samples were coated onto glass beads and loaded into a glass reactor which was in turn placed inside a heated metal chamber. Ultra-zero air, conditioned to the desired humidification, was purged into the glass container, through the glass frit, over the coated beads, and the exit gas was collected onto a sorbent tube packed with Tenax TA. Any chemical product arising from the interaction between cocaine hydrochloride and the flowing air was effectively collected onto the sorbent tube, which was analyzed using a split column GC/MS technique. The results of these storage experiments showed that methyl benzoate is a predominant volatile product, even at zero percent humidification. The average formation of methyl benzoate was found to range from 1.89 ng/min with ambient/dry conditions after one hour to 62 ng.min at 40 degrees C/80 percent RH upon introduction of flowing air. These results indicate that cocaine hydrochloride exposed to any realistic humidity level in the environment will produce methyl benzoate, a volatile organic material which can be much more readily detected than cocaine hydrochloride itself.

Dejarme, Lindy E.; Gooding, Rachel E.; Lawhon, Sara J.; Ray, Prasenjit; Kuhlman, Michael R.

1997-02-01

305

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. PMID:24082344

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

2013-01-01

306

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

307

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 Antnio Sodr; Rey, Nicols A

2013-12-01

308

Synthesis and spectroscopic characterization of nickel(II) complexes of 1-benzotriazol-1-yl-[( p-X-phenyl)hydrazone]propan-2-one  

Microsoft Academic Search

The reaction of NiCl2H2O with 1-benzotriazol-1-yl-[(p-X-phenyl)hydrazone]propan-2-one, X=H (HL1), X=Cl (HL2), X=Br (HL3) and X=Me (HL4), gave the complexes [(HL)NiCl2]nH2O and [LNi(OH)]2, where L is the monobasic anion of HL2 or HL3. The nature of the products is solvent and ligand dependent. The complexes are characterized by elemental analyses, molar conductivity, magnetic moments and spectroscopic (IR and UV\\/vis) measurements. The IR

Nouria Al-Awadi; Nadia M. Shuaib; Ali El-Dissouky

2006-01-01

309

Microneedle-assisted delivery of verapamil hydrochloride and amlodipine besylate.  

PubMed

The aim of this project was to study the effect of stainless steel solid microneedles and microneedle rollers on percutaneous penetration of verapamil hydrochloride and amlodipine besylate. Verapamil, 2-(3,4-dimethooxyphenyl)-5-[2-(3,4 dimethoxyphenyl)ethyl-methyl-amino]-2-propan-2-yl-pentanenitrile is a calcium channel blocker agent that regulates high blood pressure by decreasing myocardial contractilty, heart rate and impulse conduction. Amlodipine, (R, S)-2-[(2-aminoethoxy) methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1, 4-dihydropyridine, is a calcium channel blocker that is used for the management of hypertension and ischemic heart disease. Passive penetration of verapamil and amlodipine across the skin is low. In vitro studies were performed with microneedle-treated porcine ear skin using vertical static Franz diffusion cells (PermeGear, Hellertown, PA, USA). The receiver chamber contained 5ml of PBS (pH7.4) and was constantly maintained at 37C temperature with a water circulation jacket. The diffusion area of the skin was 1.77cm(2). The donor compartment was loaded with 1ml of the solution containing 2.5mg/ml of amlodipine besylate. The donor chamber was covered with parafilm to avoid evaporation. Passive diffusion across untreated porcine skin served as control. Aliquots were taken every 2h for 12h and analyzed by liquid chromatography-mass spectrometry. Transcutaneous flux of verapamil increased significantly from 8.75?g/cm(2)/h to 49.96?g/cm(2)/h across microneedle-roller treated porcine skin. Percutaneous flux of amlodipine besylate following the use of stainless steel microneedles was 22.39?g/cm(2)/h. Passive flux for the drug was 1.57?g/cm(2)/h. This enhancement of amlodipine flux was statistically significant. Transdermal flux of amlodipine with microneedle roller was 1.05?g/cm(2)/h in comparison with passive diffusion flux of 0.19?g/cm(2)/h. The difference in flux values was also statistically significant. Stainless steel solid microneedles and microneedle rollers increased percutaneous penetration of verapamil hydrochloride and amlodipine besylate. It may be feasible to develop transdermal microneedle patches for these drugs. PMID:24176676

Kaur, Monika; Ita, Kevin B; Popova, Inna E; Parikh, Sanjai J; Bair, Daniel A

2014-02-01

310

A Double-Blind, Placebo-Controlled Trial of Dexmethylphenidate Hydrochloride and D,l-Threo-Methylphenidate Hydrochloride in Children with Attention-Deficit-Hyperactivity Disorder  

ERIC Educational Resources Information Center

Objective: To evaluate the efficacy and safety of dexmethylphenidate hydrochloride (d-MPH, Focalin[TM]) for the treatment of attention-deficit/hyperactivity disorder (ADHD) and to test an a priori hypothesis that d-MPH would have a longer duration of action than d,l-threo-methylphenidate (d,l-MPH). Method: This was a randomized, double-blind study

Wigal, Sharon; Swanson, James M.; Feifel, David; Sangal, R. Bart; Elia, Josephine; Casat, Charles D.; Zeldis, Jerome B.; Conners, C. Keith

2004-01-01

311

Flow injection chemiluminescence determination of naphazoline hydrochloride in pharmaceuticals.  

PubMed

A simple and sensitive flow injection chemiluminescence (FI-CL) method was developed for the determination of naphazoline hydrochloride (NPZ). The method is based on the enhancing effect of NPZ on the weak CL signal from the reaction of KIO4 with H2 O2 . Experimental parameters that affected the CL signal, including the pH of the KIO4 solution, concentrations of KIO4 , H2 O2 and disodium-EDTA and flow rate were optimized. Under the optimum conditions, the increment of CL intensity was linearly proportional to the concentration of NPZ in the range 5.0 10(-6) to 70 10(-6) mol/L. The detection limit was 1.0 10(-6) mol/L and the relative standard deviation for 50 10(-6) mol/L NPZ solution was 2.8% (n = 11). In addition, a high throughput of 120 samples/h was achieved. The utility of this method was demonstrated by determining NPZ in pharmaceuticals. PMID:23463582

Iranifam, Mortaza; Sorouraddin, Mohammad H

2014-02-01

312

Novel chewable sustained-release tablet containing verapamil hydrochloride.  

PubMed

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

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

2004-01-01

313

Aqueous core nanocapsules: a new solution for encapsulating doxorubicin hydrochloride.  

PubMed

In this study, we propose a new solution for the nanoencapsulation of hydrophilic anticancer drug, doxorubicin hydrochloride (DOX). The drug molecules are solubilized in the core of aqueous nanoreservoirs, so-called aqueous core nanocapsules (ACN) recently developed by our team, and dispersed in aqueous bulk media. Since it is well acknowledged that the nanoencapsulation of DOX has many advantages, like reducing the sides effects (e.g. cardiac toxicity), we propose through the present study a novel formulation solution for this purpose. After focusing on the formulation process for optimizing the drug encapsulation yield, the DOX-release profiles were followed up and analyzed. Different physicochemical and in vitro characterization were performed, and complement activation experiments. ACN were shown efficient to encapsulate DOX reaching yields as high as 80%, followed by a sustained release governed by a diffusion-controlled mechanism. The loaded nanocarriers showed low levels of complement activation, compatible with stealth properties. To summarize, this study brings out a new tool for the nanoencapsulation of hydrophilic anticancers and could open new doors for the administration of this particular class of drugs. PMID:23289391

Vrignaud, Sandy; Anton, Nicolas; Passirani, Catherine; Benoit, Jean-Pierre; Saulnier, Patrick

2013-11-01

314

Structure and vibrational spectra of pyridine betaine hydrochloride  

NASA Astrophysics Data System (ADS)

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

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

1997-12-01

315

Calculation of the vibrational spectra of betaine hydrochloride  

NASA Astrophysics Data System (ADS)

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

Szafran, Miroslaw; Koput, Jacek

1997-02-01

316

Preliminary Toxicological Report of Metformin Hydrochloride Loaded Polymeric Nanoparticles  

PubMed Central

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

2012-01-01

317

Release Kinetics of Papaverine Hydrochloride from Tablets with Different Excipients  

PubMed Central

Abstract The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, (3-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release.

Kasperek, Regina; Polski, Andrzej; Zimmer, ?ukasz; Poleszak, Ewa

2014-01-01

318

Trans-ungual delivery of itraconazole hydrochloride by iontophoresis.  

PubMed

Abstract Itraconazole (ITR) is a potent antifungal drug. However, poor aqueous solubility limits its permeation ability across the human nail plate. Therefore, in this project, ITR was converted to hydrochloride salt (ITR-HCl) to improve its solubility and to render it amenable to iontophoresis. ITR-HCl was characterized by spectroscopic methods and antifungal efficacy was evaluated in comparison to the base. In vitro and ex vivo transport studies (passive and iontophoresis) were carried out across the porcine hoof membrane and excised human cadaver toe using two different protocols; continuous delivery of drug for 24?h and pulsed delivery of drug for 3 days (8?h/day). The antifungal efficacy of ITR-HCL was comparable to ITR. Iontophoresis was found to be more effective than passive mode of delivery of ITR-HCL. In both iontophoresis as well as passive mode of delivery, the pulsed protocol resulted in more ungual and trans-ungual delivery of drug than continuous protocol. ITR-HCL could be delivered into and across the nail plate by iontophoresis. Human cadaver toe appears to be a good model to investigate the ungual delivery of drugs. PMID:25482587

Kushwaha, Avadhesh; Jacob, Melissa; Shiva Kumar, H N; Hiremath, Shobharani; Aradhya, Sacchidanand; Repka, Michael A; Murthy, S Narasimha

2014-12-01

319

Spectrophotometric estimation of tamsulosin hydrochloride by acid-dye method  

PubMed Central

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

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

2011-01-01

320

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

PubMed

Effects of ractopamine hydrochloride (RH) and zilpaterol hydrochloride (ZH) on saleable yield of carcass sides from calf-fed Holstein steers were evaluated using steers implanted with a progesterone (100 mg) plus estradiol benzoate (10 mg) implant followed by a terminal trenbolone acetate (200 mg) plus estradiol (40 mg) implant. Steers were blocked by weight into pens (n = 32) randomly assigned to one of four treatments: control, RH fed at 300 mgsteer(-1)/d(-1) (RH 300) or RH fed at 400 mgsteer(-1)/d(-1) (RH 400) the final 31 d of finishing, and ZH fed at 60 to 90 mgsteer(-1)/d(-1) (7.56 g/ton on a 100% DM basis) for 21 d with a 5 d withdrawal before harvest. Eight to nine carcass sides were randomly selected from each pen; carcass sides with excessive hide pulls, fat pulls or bruises were avoided. Cutout data were collected within a commercial facility using plant personnel to fabricate sides at a rate of one every 3 to 4 min into items typically merchandised by the facility. All lean, fat and bone were weighed and summed back to total chilled side weight with a sensitivity of 2% to be included in the data set. Compared to controls, ?-agonists increased saleable yield of whole-muscle cuts by 0.61%, 0.86% and 1.95% for RH 300, RH 400 and ZH, respectively (P < 0.05). Percent fat was less in carcasses from the ZH treatment compared to controls (P < 0.05); however, this difference was not observed between RH treatments and controls (P > 0.05). Percent bone was less in the ZH treatment due to increased muscle (P < 0.05). The percent of chilled side weight comprised of trimmings was unchanged between treatments, but on a 100% lean basis, RH 400 and ZH increased trim yields (P < 0.05). Analysis of saleable yield by primal showed a fundamental shift in growth and development. Beta-agonists caused a shift in proportion of saleable yield within individual primals, with a greater portion produced from the hindquarter relative to the forequarter, specifically in those muscles of the round (P < 0.05). Beta-agonists increased saleable yield, but these effects were not constant between all major primals. The cutout value gained by packers as a result of ?-agonist use may be influenced more by reduced fatness and increased absolute weight if musculature is primarily increased in the lower priced cuts of the carcass. PMID:24243909

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

2014-01-01

321

Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and cellular studies.  

PubMed

Recently we described some (thiazol-2-yl)hydrazones as antiprotozoal, antifungal and anti-MAO agents as well as Gcn5 HAT inhibitors. Among these last compounds, CPTH2 and CPTH6 showed HAT inhibition in cells and broad anticancer properties. With the aim to identify HAT inhibitors more potent than the two prototypes, we synthesized several new (thiazol-2-yl)hydrazones including some related thiazolidines and pyrimidin-4(3H)-ones, and we tested the whole library existing in our lab against human p300 and PCAF HAT enzymes. Some compounds (1x, 1c', 1d', 1i' and 2m) were more efficient than CPTH2 and CPTH6 in inhibiting the p300 HAT enzyme. When tested in human leukemia U937 and colon carcinoma HCT116 cells (100 ?M, 30 h), 1x, 1i' and 2m gave higher (U937 cells) or similar (HCT116 cells) apoptosis than CPTH6, and were more potent than CPTH6 in inducing cytodifferentiation (U937 cells). PMID:24835815

Carradori, Simone; Rotili, Dante; De Monte, Celeste; Lenoci, Alessia; D'Ascenzio, Melissa; Rodriguez, Veronica; Filetici, Patrizia; Miceli, Marco; Nebbioso, Angela; Altucci, Lucia; Secci, Daniela; Mai, Antonello

2014-06-10

322

Synthesis of a novel hydrazone derivative and biophysical studies of its interactions with bovine serum albumin by spectroscopic, electrochemical, and molecular docking methods.  

PubMed

Hydrazone derivatives possess potential antitumor activities based on modulation of the iron metabolism in cancer cell. A novel hydrazone, N'-(2,4-dimethoxybenzylidene)-2-hydroxybenzohydrazide (DBH), has been synthesized and characterized, which is an analogue of 311 possessing potent anticancer activity. The interactions between DBH and bovine serum albumin (BSA) have been investigated systematically by fluorescence, molecular docking, circular dichroism (CD), UV-vis absorption, and electrochemical impedance spectroscopy (EIS) methods under physiological conditions. The fluorescence quenching observed is attributed to the formation of a complex between BSA and DBH, and the reverse temperature effect of the fluorescence quenching has been found and discussed. The primary binding pattern is determined by hydrophobic interaction occurring in Sudlow's site I of BSA. DBH could slightly change the secondary structure and induce unfolding of the polypeptides of protein. An average binding distance of ~4.0 nm has been determined on the basis of the Frster resonance energy theory (FRET). The effects of iron on the system of DBH-BSA have also been investigated. It is found that iron could compete against BSA to bind DBH. All of these results are supported by a docking study using a BSA crystal model. It is shown that DBH can efficiently bind with BSA and be transported to the focuses needed. Subsequent antitumor test and detailed anticancer mechanism are undergoing in our lab. PMID:21038894

Tian, Fang-Fang; Jiang, Feng-Lei; Han, Xiao-Le; Xiang, Chen; Ge, Yu-Shu; Li, Jia-Han; Zhang, Yue; Li, Ran; Ding, Xin-Liang; Liu, Yi

2010-11-25

323

Pharmacokinetics of hydromorphone hydrochloride after intravenous and intramuscular administration of a single dose to American kestrels (Falco sparverius)  

USGS Publications Warehouse

Results indicated hydromorphone hydrochloride had high bioavailability and rapid elimination after IM administration, with a short terminal half-life, rapid plasma clearance, and large volume of distribution in American kestrels. Further studies regarding the effects of other doses, other administration routes, constantrate infusions, and slow release formulations on the pharmacokinetics of hydromorphone hydrochloride and its metabolites in American kestrels may be indicated.

Guzman, David Sanchez-Migallon; KuKanich, Butch; Drazenovich, Tracy; Olsen, Glenn H.; Paul-Murphy, Joanne

2014-01-01

324

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

Federal Register 2010, 2011, 2012, 2013, 2014

...Oxymorphone Hydrochloride) Extended- Release Tablets, 7.5 Milligrams and 15 Milligrams...hydrochloride (HCl)) extended-release tablets, 7.5 milligrams (mg) and 15 mg...for oxymorphone HCl extended- release tablets, 7.5 mg and 15 mg, if all other...

2011-08-30

325

Development and validation of stability indicating HPLC and HPTLC methods for determination of sulpiride and mebeverine hydrochloride in combination  

Microsoft Academic Search

Validated sensitive and highly selective stability indicating methods are adopted for simultaneous quantitative determination of sulpiride and mebeverine hydrochloride in presence of their reported impurities and hydrolytic degradates whether in pure forms or in pharmaceutical formulation.The first method is High Performance Liquid Chromatography, where the mixture of sulpiride and mebeverine hydrochloride together with the reported interferents plus metopimazine as internal

Ibrahim A. Naguib; Mohammed Abdelkawy

2010-01-01

326

Photoacoustic imaging to detect rat brain activation after cocaine hydrochloride injection  

NASA Astrophysics Data System (ADS)

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

Jo, Janggun; Yang, Xinmai

2011-03-01

327

Protective effects of glucosamine hydrochloride against free radical-induced erythrocytes damage.  

PubMed

Glucosamine (GlcN) is an important precursor in the biochemical synthesis of glycosylated proteins and lipids in human body. It gains importance because of its contribution to human health and its multiple biological and therapeutic effects. In this study, the in vitro oxidative hemolysis of rat erythrocyte was used as a model to study the potential protective effect of glucosamine hydrochloride against free radical-induced damage of biological membranes. Glucosamine hydrochloride exhibited dose-dependent DPPH antioxidant activity. Oxidative hemolysis and lipid/protein peroxidation of erythrocytes induced by a water-soluble free radical initiator 2,2'-azobis (2-amidinopropane) dihydrochloride (AAPH) were significantly suppressed by GlcN in a time and dose dependent manner. GlcN also prevented the depletion of cytosolic antioxidant glutathione (GSH) in erythrocytes. These results indicated that glucosamine hydrochloride efficiently protected erythrocytes against free radicals and it could be recommended as a pharmaceutical supplement to alleviate oxidative stress. PMID:24959958

Jamialahmadi, Khadijeh; Arasteh, Omid; Matbou Riahi, Maryam; Mehri, Soghra; Riahi-Zanjani, Bamdad; Karimi, Gholamreza

2014-07-01

328

Impurity profiling of methamphetamine hydrochloride drugs seized in the Philippines.  

PubMed

Methamphetamine hydrochloride is one of the most widely used illicit drugs in the Philippines. In this study, we describe the application of cluster analysis of trace impurities in the profiling of the seized methamphetamine drug samples. Thirty milligrams of a homogenized drug sample were dissolved in 1 mL of pH 10.5 buffer solution and extracted with ethyl acetate containing three internal standards. The trace impurities were identified using gas chromatography-mass spectrometry (GC-MS) and quantified by gas chromatography with a flame ionization detector (GC-FID). Following previously reported methodologies, 30 impurity peaks were selected from the GC-FID chromatograms. The peak areas and retention times were referenced to the internal standards. The peak areas of the selected peaks were then grouped for cluster analysis. In order to check for consistency of clustering, two further cluster analyses were performed using 40 and 50 impurity peaks. Changes in clustering were observed in going from 30 to 40 impurity peaks, while analyses using 40 and 50 impurity peaks gave similar results. Thus, for the seized drug samples used in this study, cluster analysis using at least 40 impurity peaks showed better consistency of clustering as compared to analysis using 30 peaks only. Ten of the impurity peaks were identified, of which four were identified for the first time in methamphetamine drug samples. These are p-bromotoluene, N-benzyl amphetamine, N-ethyl amphetamine, and N-ethyl methamphetamine. The presence of phenyl-2-propanone (P2P), N,N-dimethyl amphetamine, and N-formyl amphetamine is indicative that these casework samples were synthesized using the Leuckart method. PMID:15240018

Dayrit, Fabian M; Dumlao, Morphy C

2004-08-11

329

A novel lidocaine hydrochloride ophthalmic gel for topical ocular anesthesia  

PubMed Central

Topical anesthetics play an important role in the practice of ophthalmology, both for procedures in the office and in the operating room. The need for safe, long-acting topical ocular anesthetic agents is ongoing, and has been highlighted by the increase of intravitreal administration of pharmacologic agents. Current practices for ocular anesthesia include subconjunctival injection of 2% aqueous lidocaine, topical 2% lidocaine drops and topical 0.5% tetracaine. Tetracaine is not yet FDA approved, and is associated with corneal epithelial toxicity and delayed epithelial healing after multiple administrations. Lidocaine jelly (2%) preparations have been reported to be beneficial in several systemic procedures, including those of the upper airway, dental, urogenital, and gastrointestinal. It has been theorized, and recent studies support the idea, that gel formulations of lidocaine may enhance anesthetic effect, and therefore be superior to anesthetic solutions for topical cataract surgery. The viscous nature of gel formulations is thought to lengthen contact time, resulting in better anesthesia at lower drug concentrations. Furthermore, several studies suggest that lidocaine is bactericidal and bacteriostatic, and may have a supplementary role in preventing and treating surgical site infections. Akten, lidocaine 3.5% gel (Akorn, Buffalo Grove, IIlinois) was FDA approved for all ophthalmic procedures in October 2008. This gel is a preservative-free, lidocaine-based anesthetic gel consisting of 35 mg/mL of lidocaine hydrochloride. We describe the properties, including chemical structure, indications, evidence of support, use, adverse effects, and precautions, which we believe enable Akten to provide superior anesthesia, while minimizing side effects. PMID:22915870

Shah, HR; Reichel, E; Busbee, BG

2010-01-01

330

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

NASA Astrophysics Data System (ADS)

The terahertz spectrum of ketamine hydrochloride at room temperature, in the range of 0.2-2.6THz, has been measured by terahertz time-domain spectroscopy (TDS). Full-geometry optimizations and frequency calculations using the density functional theory (DFT) are also applied to predict the absorption spectra of ketamine hydrochloride and 3, 4-methylenedioxymethamphetamine (MDMA). The results of the simulation show qualitative agreement with the experimental data especially for MDMA, and the observed spectra features are assigned based on the DFT calculation. The results suggest that use of the terahertz TDS technique can be an effective method for the detection and inspection of illicit drugs.

Wang, Guangqin; Shen, Jingling; Jia, Yan

2007-07-01

331

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

PubMed

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

Stanisz, Beata

2004-01-01

332

Spectrophotometric determination of oxalate in urine and plasma with oxalate oxidase.  

PubMed

In order to establish a standard procedure for the spectrophotometric determination of urinary and plasma oxalate with oxalate oxidase (Laker, M.F., et al. (1980) Clin. Chem. 26, 827-830; Sugiura, M., et al. (1980) Clin. Chim. Acta 105, 393-399) and to define the limitations of the method, the procedures and reactions involved in the assay have been examined. Among the chromogenic hydrogen donors for peroxidase tested, a combination of 3-methyl-2-benzothiazolinone hydrazone (MBTH) and sodium N-sulfopropylaniline (HALPS) was found to be best for the oxalate determination under the conditions used. Urine contained substance(s) which were inhibitory to the measurement of hydrogen peroxide by the peroxidase-catalyzed oxidative condensation of MBTH and HALPS, but they were largely removed by charcoal treatment at pH 5.6 without significant loss of oxalate. Deproteinization of plasma was carried out by ultrafiltration through a membrane cone (Centriflo CF-25) at neutral pH. The plasma oxalate ultrafiltrability under the conditions employed was calculated to be approximately 95%. A standard assay system for oxalate in these urine and plasma samples was then set up based on a series of studies on the reactions involved in the assay. In the case of normal plasma, however, the absorbance change was very small due to the low concentration of oxalate, and in addition, pretreatment of plasma with excess oxalate decarboxylase followed by the ultrafiltration and oxalate determination did not abolish completely the oxalate oxidase-dependent absorbance increase. It was concluded that the enzymic method was useful for the assay of urinary oxalate and in detecting elevated levels of plasma oxalate such as those in hemodialysis patients but was not sensitive enough to determine accurately the normal or decreased level of oxalate in plasma. The apparent concentration of oxalate in normal human plasma was measured in this work as 3.5 +/- 0.8 microM (mean +/- S.D., n = 8), and this result was interpreted to mean that the concentration of plasma oxalate was less than approximately 3.5 microM, as estimated by the present method. PMID:4086485

Ichiyama, A; Nakai, E; Funai, T; Oda, T; Katafuchi, R

1985-11-01

333

Stability indicating methods for assay of mequitazine in presence of its degradate.  

PubMed

Six procedures have been suggested for the determination of the antihistaminic agent, mequitazine, in the presence of its degradate. Mequitazine, having a phenothiazine group, undergoes peroxide oxidation and the corresponding sulphone is produced. Its identity was confirmed by IR and MS. The first procedure is based on determination of mequitazine by HPLC with UV detection at 256 nm. The mobile phase used is acetonitrile, ortho phosphoric acid (50:50) using caffeine as an internal standard. Linearity range is 1.00-9.00 microg/ml. The second determination is a densitometric procedure based on the determination of mequitazine in the presence of its degradate at 256 nm using the mobile phase, chloroform:methanol:ammonia (50:18:3). Linearity range is 1.25-7.50 microg per spot. The third procedure is spectrophotometric, where a mixture of mequitazine and its degradate are resolved by first derivative ratio spectra. Linear calibration graphs of first derivative values at wavelengths 210.2, 247 and 259.8 nm are obtained. On carrying out measurements at the three mentioned wavelengths, the linearity range is found to be 1.00-10.00 microg/ml. The fourth procedure is based on first derivative spectrophotometry, where D(1) measurements are carried out at 290 nm. Linearity range is 1.00-10.00 microg/ml. The fifth procedure is based on the reaction of mequitazine with 3-methyl-2-benzothiazolinone hydrazone (MBTH) in the presence of ferric chloride. A stable violet colored oxidative coupling product is formed, which is measured spectrophotometrically at 685 nm. The optimum experimental parameters for the reaction have been studied and assigned. Linearity range is 1.00-16.00 microg/ml. The sixth procedure is based on the reaction of mequitazine in the presence of its degradate with 2,6-dichloroquinone-4-chloroimide (Gibbs reagent) in aqueous methanolic medium. The reddish-brown colored condensation product is measured at 405 nm. The optimum experimental conditions for the reaction have been studied. Linearity range is 50.00-600.00 microg/ml. The validity of the described procedures was assessed by applying the standard addition technique. Statistical analysis of the results has been carried out revealing high accuracy and good precision. The suggested procedures could be used for the determination of mequitazine, both in pure and dosage forms, as well as in the presence of its degradate. PMID:12062671

El-Ragehy, N A; Badawey, A M; El Khateeb, S Z

2002-06-20

334

A new enzymatic function in the melanogenic pathway. The 5,6-dihydroxyindole-2-carboxylic acid oxidase activity of tyrosinase-related protein-1 (TRP1).  

PubMed

Since the characterization of 5,6-dihydroxyindole-2-carboxylic acid (DHICA) as a major melanogenic intermediate, the fate of this compound and the mechanisms of its incorporation into the melanin polymer have become major issues in the study of melanogenesis. DHICA is a stable dihydroxyindole with a low rate of spontaneous oxidation, suggesting that enzymatic mechanism(s) might contribute to its evolution. The most obvious candidates are the melanosomal tyrosinases. We have recently shown that mouse melanosomes contain two electrophoretically distinct tyrosinase isoenzymes, termed low electrophoretic mobility tyrosinase (LEMT) and high electrophoretic mobility tyrosinase (HEMT), that can be resolved and purified. In this study, we report immunological evidence indicating that LEMT corresponds to the protein encoded by the brown locus (termed tyrosinase-related protein-1, TRP1), while HEMT corresponds to the tyrosinase encoded by the albino locus. We have compared the ability of both isoenzymes to catalyze DHICA evolution as determined by high performance liquid chromatography; although LEMT is a relatively poor tyrosine hydroxylase and DOPA oxidase as compared to HEMT, it was readily able to accelerate DHICA consumption concomitant with the production of a brownish product. However, the DHICA conversion activity of HEMT was barely detectable. The ability of purified LEMT to catalyze DHICA conversion could be almost completely abolished by treatment with heat or trypsin, and was inhibited in a concentration dependent way by the tyrosinase inhibitor 2-phenylthiourea and by L-tyrosine. Moreover, in the presence of low concentration of ascorbate, the DHICA conversion activity of LEMT displayed a lag period which was progressively longer at higher ascorbate concentrations. Based on the relationship between ascorbate added, enzyme activity, and lag period, it is very likely that the DHICA converting activity is indeed a DHICA oxidase activity. This was further proven by the demonstration that the product reacts rapidly and efficiently with the quinone trapping reagent 3-methyl-2-benzothiazolinone hydrazone, yielding a colored adduct similar to the one obtained with DOPAquinone. The DHICA oxidase activity of LEMT displayed a Km for DHICA of about 0.8 mM, as compared to 1.9 mM for L-DOPA and 0.23 nM for L-tyrosine. These results suggest that TRP1, the product of the brown locus, is indeed a tyrosinase with DHICA oxidase activity. However, as opposed to the tyrosinase encoded by the albino locus, TRP1's role in melanogenesis could be more directly related to DHICA metabolism than to the first steps of the pathway. PMID:8027058

Jimnez-Cervantes, C; Solano, F; Kobayashi, T; Urabe, K; Hearing, V J; Lozano, J A; Garca-Borrn, J C

1994-07-01

335

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

PubMed

Celgene has developed a chirally pure form of methylphenidate (Ritalin), called dexmethylphenidate [d-methylphenidate, d-methylphenidate hydrochloride, d-MPH; Focalin]. The drug has been launched in the USA and is undergoing registration in Canada for the treatment of children with attention-deficit hyperactivity disorder (ADHD). Dexmethylphenidate is the single isomer version of racemic methylphenidate (Ritalin), which contains the active d isomer of Ritalin. Dexmethylphenidate acts via the inhibition of reuptake of norepinephrine and dopamine. Research is ongoing to further clarify the mode of therapeutic action in ADHD. Dexmethylphenidate was developed with the aim of reducing drug load, adverse events and drug interactions. Dexmethylphenidate provides effective management of attention-deficit hyperactivity disorder at half the dose of Ritalin. In April 2000, worldwide rights (excluding Canada) to dexmethylphenidate were granted to Novartis. Celgene has also granted Novartis rights to all related intellectual properties and patents. Novartis will fund all remaining development and marketing expenses required for regulatory approval and commercialisation of dexmethylphenidate. Crystaal Corporation, the marketing division of Biovail Corporation International, has exclusive Canadian marketing rights for all formulations of dexmethylphenidate. Novartis launched dexmethylphenidate (Focalin) in the USA during Q1 2002. It is available as a D-shaped tablet (2.5, 5 and 10 mg doses). Novartis had planned to use the tradename Ritadex, however the FDA recommended an alternative name due to potential prescribing errors with Ritalin. The finalized tradename to be used is Focalin. In July 2001, a new drug submission was filed with Canada's Therapeutic Products Programme for dexmethylphenidate in the treatment of attention-deficit disorder and attention-deficit hyperactivity disorder. Novartis is also developing an extended-release version of chirally pure dexmethylphenidate. Dexmethylphenidate has been found to be effective and well tolerated in clinical trials, involving a total of 684 children with ADHD and in 15 healthy adult volunteers. Dexmethylphenidate is a schedule II drug. PMID:12455205

2002-01-01

336

Colon-specific drug delivery for mebeverine hydrochloride.  

PubMed

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

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

2007-12-01

337

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

2011-06-15

338

Development of directly compressible metformin hydrochloride by the spray-drying technique.  

PubMed

Metformin hydrochloride exhibits poor compressibility during compaction, often resulting in weak and unacceptable tablets with a high tendency to cap. The purpose of this study was to develop directly compressible metformin hydrochloride by the spray-drying technique in the presence of polymer. Metformin hydrochloride was dissolved in solutions containing a polymer, namely polyvinylpyrrolidone (PVP K30), in various concentrations ranging from 0-3% (m/V). These solutions were employed for spray-drying. Spray-dried drug was evaluated for yield, flow property and compressibility profile. Metformin hydrochloride spray-dried in the presence of 2% PVP K30 showed an excellent flow property and compressibility profile. From the calculated Heckel's parameter (Py = 2.086), it was demonstrated that the treated drug showed better particle arrangement in the initial compression stage. Kawakita analysis revealed better packability of the treated drug compared to the untreated drug. Differential scanning calorimetry and Fourier transform infrared spectroscopy experiments showed that the spray-dried drug did not undergo any chemical modifications. Tablets made from the spray-dried drug (90%, m/m) were evaluated for crushing strength, friability and disintegration time and the results were found satisfactory. PMID:21134853

Barot, Bhavesh S; Parejiya, Punit B; Patel, Tushar M; Parikh, Rajesh K; Gohel, Mukesh C

2010-06-01

339

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

340

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

Federal Register 2010, 2011, 2012, 2013, 2014

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

2010-10-19

341

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

342

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

Technology Transfer Automated Retrieval System (TEKTRAN)

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

343

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

344

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)...

345

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

346

77 FR 53892 - Determination That ALOXI (Palonosetron Hydrochloride) Capsules, 0.5 Milligram (Base), Were Not...  

Federal Register 2010, 2011, 2012, 2013, 2014

...Hydrochloride) Capsules, 0.5 Milligram (Base), Were Not Withdrawn From Sale for Reasons...Capsules, 0.5 milligram (mg) (base), were not withdrawn from sale for reasons...palonosetron HCl capsules, 0.5 mg (base), if all other legal and regulatory...

2012-09-04

347

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

Microsoft Academic Search

In this paper, the bovine serum albumin (BSA) was selected as a target molecule, the sonodynamic damage to protein in the presence of promethazine hydrochloride (PMT) and its mechanism were studied by the means of absorption, fluorescence and circular dichroism (CD) spectra. The results of hyperchromic effect of absorption spectra and quenching of intrinsic fluorescence spectra indicate that the ultrasound-induced

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

2011-01-01

348

Performance of finishing beef steers in response to anabolic implant and zilpaterol hydrochloride supplementation  

Technology Transfer Automated Retrieval System (TEKTRAN)

Our objectives were to evaluate the dose/payout pattern of trenbolone acetate (TBA) and estradiol-17b (E2) implants and feeding of zilpaterol hydrochloride (ZH) on performance and carcass characteristics of finishing beef steers. A randomized complete block design was used with a 3 2 factorial arr...

349

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

Technology Transfer Automated Retrieval System (TEKTRAN)

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

350

Nano-liposomes of entrapment lidocaine hydrochloride on in vitro permeability of narcotic.  

PubMed

In order to explore two kinds of nano-liposomes in lidocaine hydrochloride nano-liposomes on in vitro permeability of drug, and conduct comparison and analysis, this paper investigates cumulative infiltration situation of lidocaine hydrochloride flexible nano-liposomes and ordinary nano-liposomes by using modified Franz diffusion pool on mice vitro skin. Cumulative osmotic quantity of lidocaine hydrochloride flexible nano-liposomes for 9h was higher than ordinary nano-liposomes.tmax(Maximum osmotic quantity time) of lidocaine hydrochloride flexible nano-liposomes and ordinary nano-liposomes in mice skin was 5 and 60min, the former Cmax (maximum dosage time) was 1.2 times of the latter. Drug was not found in mice plasma of ordinary nano-liposomes group, traces of drugs was detected in 0.5 and 1h in flexible nano-liposomes group, but the concentration was lower than the effective concentration. Compared with the classic skin transparent promoter and ordinary liposome, flexible nano-liposomes have more advantages, but its stability is less than ordinary nano-liposomes because of the addition of surface active substance. Flexible nano-liposomes have great development potential as a carrier of transdermal drug delivery field. PMID:25631510

Sun, Nenghong; Zhu, Yanyan; Yuan, Lei; Lang, Bao

2015-01-01

351

Spectrophotometric methods for the determination of ritodrine hydrochloride and its application to pharmaceutical preparations  

Microsoft Academic Search

Two simple and sensitive spectrophotometric methods are described for the determination of ritodrine hydrochloride (RTH) in both pure and dosage forms. The methods are based on the interaction of diazotised p-nitroaniline (DPNA) and sulphanilic acid (DSNA) with RTH in an alkaline medium. The resulting azo dyes are measured at 480 nm (for the DPNA method) and at 440 nm (for

Hosakere D. Revanasiddappa; Bochhegowda Manju

2001-01-01

352

Spectrophotometric determination of diphenhydramine hydrochloride in pharmaceutical preparations and biological fluids via ion-pair formation  

Microsoft Academic Search

A simple, sensitive and accurate spectrophotometric method has been described for the assay of diphenhydramine hydrochloride (DPH) in raw material and in biological samples. The method is based on extraction of DPH into dichloromethane as ion-pair complexes with patent blue (PB), eriochrome black T (EBT), methyl orange (MO) and bromocresol purple (BCP) in acidic medium. The coloured species exhibited absorption

Akram M. El-Didamony; Moftah A. Moustafa

2010-01-01

353

Sensitive spectrophotometric determination of metoclopramide hydrochloride in dosage forms and spiked human urine using vanillin  

Microsoft Academic Search

A new spectrophotometric method which is simple, sensitive, selective and rapid is described for the determination of metoclopramide hydrochloride (MCP) in bulk drug and in dosage forms using vanillin as the chromogenic agent. The method is based on the condensation reaction between primary aromatic amine group present in MCP with aromatic aldehyde, vanillin to produce an intense yellow colored product.

O. Zenita Devi; K. Basavaiah; K. B. Vinay; H. D. Revanasiddappa

354

Iontophoretic Delivery of Ropinirole Hydrochloride: Effect of Current Density and Vehicle Formulation  

Microsoft Academic Search

Purpose. The objectives of this work were 1) to establish the feasibility of the transdermal iontophoretic delivery of ropinirole hydrochloride; 2) to investigate the possibility of delivering therapeutic doses of this drug; and 3) to determine the key factors that control ropinirole electrotransport.

Asteria Luzardo-Alvarez; M. Begoa Delgado-Charro; Jos Blanco-Mndez

2001-01-01

355

Denaturation behavior of phaseolin in urea, guanidine hydrochloride, and sodium dodecyl sulfate solutions.  

PubMed

The denaturation behavior of phaseolin in urea, guanidine hydrochloride, and sodium dodecyl sulfate solutions was examined by monitoring changes in the intrinsic fluorescence of tryptophan and tyrosyl residues. Changes in various fluorescence parameters, such as quantum yield, emission maximum, spectral half-width, fluorescence depolarization, and fluorescence quenching by acrylamide, have indicated that while phaseolin is relatively stable up to 8 M urea, it is completely destabilized in 6 M guanidine hydrochloride and 6 mM sodium dodecyl sulfate. Furthermore, while the denaturation of phaseolin in urea solutions followed a two-step process, that in guanidine hydrochloride and sodium dodecyl sulfate followed a single-step process. While the accessibility of tryptophan residues to the nonionic acrylamide quencher is almost 100% in 6 M guanidine hydrochloride and 6 mM sodium dodecyl sulfate, only about 72% was accessible in 8 M urea compared to 52% in native phaseolin. The results presented here suggest that the protomeric structure of phaseolin is quite stable to changes in the environment. This structural stability may be partly responsible for its resistance to proteolysis by various proteinases. PMID:2054055

Deshpande, S S; Damodaran, S

1991-02-01

356

Denaturation behavior of phaseolin in urea, guanidine hydrochloride, and sodium dodecyl sulfate solutions  

Microsoft Academic Search

The denaturation behavior of phaseolin in urea, guanidine hydrochloride, and sodium dodecyl sulfate solutions was examined by monitoring changes in the intrinsic fluorescence of tryptophan and tyrosyl residues. Changes in various fluorescence parameters, such as quantum yield, emission maximum, spectral half-width, fluorescence depolarization, and fluorescence quenching by acrylamide, have indicated that while phaseolin is relatively stable up to 8 M

S. S. Deshpande; Srinivasan Damodaran

1991-01-01

357

The K-band ?max values of the ultraviolet-visible spectra of some hydrazones in ethanol by a TD-DFT/PCM approach  

NASA Astrophysics Data System (ADS)

We presented the time-dependent density functional theory calculated ultraviolet-visible (UV-vis) spectra for derivatives of phenylhydrazones, semicarbazones and pyrrole hydrazones in ethanol. We employed the B3LYP, PBE0, CAM-B3LYP, LC- ?PBE, LC-PBE and ?B97X-D functionals. We gauged the performance of the six hybrid functionals of choice in determination of the K-band ?max values of the UV-vis spectra. The PCM-TD-PBE0/6-311+G(2d,p)//PCM-PBE0/6-311G(d,p) approach provided the smallest error with an average absolute deviation limited to 14 nm. We also investigated the impacts of including explicit solvent molecules and considering vibrational envelope with the Franck-Condon Herzberg-Teller method.

Lu, Shih-I.

2010-07-01

358

A novel preparation of human platelet lipoxygenase. Characteristics and inhibition by a variety of phenyl hydrazones and comparisons with other lipoxygenases.  

PubMed

Acetone-pentane powder preparations of human blood platelets were prepared and the characteristics of the 12L-lipoxygenase were studied using measurements of oxygen consumption. No sharp pH optimum with equal reaction velocities was observed over a range of pH 7.5-8.5 in a variety of buffers. The enzyme could be easily solubilized in 1% deoxycholate, and in this form was moderately stable to heat. Of 10 divalent cations tested at a concentration of 3.7 . 10(-3) M, only zinc and tin were inhibitory. None of he other ions was stimulatory. The products of the oxidation of arachidonate were characterized from both soluble and insoluble enzyme preparations. With the insoluble suspension, 55% of the added arachidonate was recovered as 12-hydroxy-5,8,10,14-eicosatetraenoic acid (12-HETE) and 27% appeared as trihydroxyeicosatetraenoic acid isomers (THETEs). With the soluble preparation, 84% of the arachidonate appeared as 12-HETE and only 5% as THETEs. The Michaelis constants for dihomo-gamma-linolenic aicd, arachidonic acid, and eicosapentaenoic acid substrates are presented. A series of phenyl hydrazone inhibitors of various structural types were discovered to be potent inhibitors of the human platelet lipoxygenase. The sensitivities of this enzyme to these inhibitors were compared to soybean lipoxygenase and sheep seminal vesicular cyclodioxygenase. In general, the soybean enzyme was most sensitive; the sheep seminal vesicular cyclodioxygenase was the least sensitive and the human platelet lipoxygenase was intermediate between the two. The Ki values for two phenyl hydrazone inhibitors with both soybean and human platelet lipoxygenases is presented. PMID:6783111

Wallach, D P; Brown, V R

1981-02-23

359

DEVELOPMENT AND VALIDATION OF REVERSE PHASE HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC AND HIGH PERFORMANCE THIN LAYER CHROMATOGRAPHIC METHODS FOR SIMULTANEOUS ESTIMATION OF MELITRACEN HYDROCHLORIDE AND FLUPENTIXOL HYDROCHLORIDE IN BULK AND COMBINED DOSAGE FORM  

Microsoft Academic Search

Sensitive and reproducible reverse phase high performance liquid chromatographic and high performance thin layer chomatographic methods have been developed for simultaneous estimation of melitracen hydrochloride and flupentixol hydrochloride in bulk and combined tablet dosage form. The methods were validated according to International Conference on Harmonization guidelines. In RP-HPLC method linearity was achieved with a detection range of 50-300g\\/ml (r=0.998) and

Ratna S. Limgavkar; Priti D. Trivedi; Archita J. Patel

2012-01-01

360

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

Code of Federal Regulations, 2011 CFR

...greater the concentration of free formaldehyde in a resin, the more of that formaldehyde will be in the polymeric form...analyzed must contain enough free formaldehyde so that the...hydroxylamine hydrochloride will produce sufficient...

2011-07-01

361

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

Code of Federal Regulations, 2013 CFR

...greater the concentration of free formaldehyde in a resin, the more of that formaldehyde will be in the polymeric form...analyzed must contain enough free formaldehyde so that the...hydroxylamine hydrochloride will produce sufficient...

2013-07-01

362

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

Code of Federal Regulations, 2014 CFR

...greater the concentration of free formaldehyde in a resin, the more of that formaldehyde will be in the polymeric form...analyzed must contain enough free formaldehyde so that the...hydroxylamine hydrochloride will produce sufficient...

2014-07-01

363

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

Code of Federal Regulations, 2012 CFR

...greater the concentration of free formaldehyde in a resin, the more of that formaldehyde will be in the polymeric form...analyzed must contain enough free formaldehyde so that the...hydroxylamine hydrochloride will produce sufficient...

2012-07-01

364

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

Microsoft Academic Search

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

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

2002-01-01

365

Rapid and accurate determination of chlorpheniramine maleate, noscapine hydrochloride and guaiphenesin in binary mixtures by derivative spectrophotometry  

Microsoft Academic Search

Rapid and accurate binary mixture resolution of chlorpheniramine maleate-noscapine hydrochloride and chlorpheniramine maleate-guaiphenesin, was performed. Derivative spectrophotometry, by the zero-crossing measurements, was used due to the drugs closely overlapping absorption spectra. Neither sample pretreatment nor separation were required. Linear calibration graphs of first derivative values at 268.0 and 261.0 nm for chlorpheniramine-maleate-noscapine hydrochloride and at 273.2 and 261.0 nm for

Nora B. Pappano; Yolanda C. De Micalizzi; Nora B. Debattista; Ferdinando H. Ferretti

1997-01-01

366

Spectrophotometric determination of procaine hydrochloride in pharmaceutical products using 1,2-naphthoquinone-4-sulfonic acid as the chromogenic reagent  

NASA Astrophysics Data System (ADS)

Spectrophotometric determination of procaine hydrochloride is described. The procaine hydrochloride reacts with 1,2-naphthoquinone-4-sulfonic acid in pH 3.60 buffer solution to form a salmon pink compound, and its maximum absorption wavelength is at 484 nm, ? 484=5.2210 3.The absorbance for procaine hydrochloride from 0.30 to 100 ?g ml -1 obeys Beer's law. The linear regression equation of the calibration graph is C=19.23A-0.03, with a linear regression correlative coefficient is 0.9996, the detection limit is 0.28 ?g ml -1; recovery is from 98.0 to 105.2%. Effects of pH, surfactant, organic solvent, foreign ions, and standing time on the determination of procaine hydrochloride have been examined. This method is rapid and simple, and can be used for the determination of procaine hydrochloride in injection solution of procaine hydrochloride. The results obtained by this method agreed with those by the official method (dead-stop titration).

Xu, Li Xiao; Shen, Yun Xiu; Wang, Huai You; Jiang, Ji Gang; Xiao, Yan

2003-11-01

367

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

PubMed Central

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

Nair, Rajasree; Moss, Shannon B

2009-01-01

368

Transdermal delivery of betahistine hydrochloride using microemulsions: physical characterization, biophysical assessment, confocal imaging and permeation studies.  

PubMed

Transdermal delivery of betahistine hydrochloride encapsulated in various ethyl oleate, Capryol 90(), Transcutol() and water microemulsion formulations was studied. Two different kinds of phase diagrams were constructed for the investigated microemulsion system. Pseudoplastic flow that is preferable for skin delivery was recorded for the investigated microemulsions. A balanced and bicontinuous microemulsion formulation was suggested and showed the highest permeation flux (0.500.030mgcm(-2)h(-1)). The effect of the investigated microemulsions on the skin electrical resistance was used to explain the high permeation fluxes obtained. Confocal laser scanning microscopy was used to confirm the permeation enhancement and to reveal the penetration pathways. The results obtained suggest that the proposed microemulsion system highlighted in the current work can serve as a promising alternative delivery means for betahistine hydrochloride. PMID:23732802

Hathout, Rania M; Nasr, Maha

2013-10-01

369

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

PubMed

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

Nair, Rajasree; Moss, Shannon B

2009-01-01

370

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

PubMed Central

Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer and osteoporosis in post-menopausal women, shows poor oral bioavailability of 2%. The aim of this study was to develop, statistically optimize, and characterize raloxifene hydrochloride-loaded transfersomes for transdermal delivery, in order to overcome the poor bioavailability issue with the drug. A response surface methodology experimental design was applied for the optimization of transfersomes, using Box-Behnken experimental design. Phospholipon 90G, sodium deoxycholate, and sonication time, each at three levels, were selected as independent variables, while entrapment efficiency, vesicle size, and transdermal flux were identified as dependent variables. The formulation was characterized by surface morphology and shape, particle size, and zeta potential. Ex vivo transdermal flux was determined using a Hanson diffusion cell assembly, with rat skin as a barrier medium. Transfersomes from the optimized formulation were found to have spherical, unilamellar structures, with a homogeneous distribution and low polydispersity index (0.08). They had a particle size of 1349 nM, with an entrapment efficiency of 91.00%4.90%, and transdermal flux of 6.51.1 ?g/cm2/hour. Raloxifene hydrochloride-loaded transfersomes proved significantly superior in terms of amount of drug permeated and deposited in the skin, with enhancement ratios of 6.251.50 and 9.252.40, respectively, when compared with drug-loaded conventional liposomes, and an ethanolic phosphate buffer saline. Differential scanning calorimetry study revealed a greater change in skin structure, compared with a control sample, during the ex vivo drug diffusion study. Further, confocal laser scanning microscopy proved an enhanced permeation of coumarin-6-loaded transfersomes, to a depth of approximately160 ?M, as compared with rigid liposomes. These ex vivo findings proved that a raloxifene hydrochloride-loaded transfersome formulation could be a superior alternative to oral delivery of the drug. PMID:25246789

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

2014-01-01

371

Evaluation of techniques for lignocaine hydrochloride analgesia of the velvet antler of adult stags  

Microsoft Academic Search

Aim: To evaluate the effectiveness of various routes of administration and doses of local anaesthetic (LA) to provide analgesia of the velvet antler of adult stags.Methods: In Experiment 1, antlers from 50 red deer stags, ?2-years-old were allocated to 1 of 4 treatment groups (n = 25 antlers\\/group) to receive injections with 2% lignocaine hydrochloride as follows: High-dose (1 ml\\/cm

P. R. Wilson; K. J. Stafford; D. G. Thomas; D. J. Mellor

2000-01-01

372

Titrimetric and spectrophotometric assay of some antihistamines through the determination of the chloride of their hydrochlorides  

Microsoft Academic Search

Two simple, rapid and reliable methods for the determination of four antihistamines based on the measurement of the chloride of their hydrochlorides are described. In the titrimetric method, the chloride content of each drug is determined by titrating with mercury(II) nitrate using diphenylcarbazonebromothymol blue as indicator. In the spectrophotometric method, to a fixed concentration of mercury(II)diphenylcarbazone complex different amounts of

K Basavaiah; V. S Charan

2002-01-01

373

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

374

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

PubMed Central

Background: Nebivolol hydrochloride is a third generation ?-blocker with highly selective ?1-receptor antagonist with antihypertensive properties having plasma half life of 10 h and 12% oral bioavailability. The aim of the present investigation was to form matrix type transdermal patches containing Nebivolol hydrochloride to avoid its extensive hepatic first pass metabolism, lesser side effect and increase bioavailability of drug. Materials and Methods: Matrix type transdermal patches containing Nebivolol hydrochloride were prepared using EudragitRS100, HPMC K100M (2:8) polymers by solvent evaporation technique. Aluminum foil was used as a backing membrane. Polyethylene glycol (PEG) 400 was used as plasticizer and Dimethyl sulfoxide (DMSO) was used as a penetration enhancer. Drug polymer interactions determined by FTIR and standard calibration curve of Nebivolol hydrochloride were determined by using UV estimation. Result: The systems were evaluated physicochemical parameters and drug present in the patches was determined by scanning electron microscopy. All prepared formulations indicated good physical stability. In vitro drug permeation studies of formulations were performed by using Franz diffusion cells using abdomen skin of Wistar albino rat. Result showed best in vitro skin permeation through rat skin as compared to all other formulations prepared with hydrophilic polymer containing permeation enhancer. Conclusions: It was observed that the formulation containing HPMC: EudragitRS100 (8:2) showed ideal higuchi release kinetics. On the basis of in vitro drug release through skin permeation performance, Formulation F1 was found to be better than other formulations and it was selected as the optimized formulation. PMID:24223377

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

2013-01-01

375

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

NASA Astrophysics Data System (ADS)

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

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

2008-09-01

376

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

Microsoft Academic Search

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

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

2010-01-01

377

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

Microsoft Academic Search

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

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

2008-01-01

378

Copolymers of 2-Deoxy-2-Methacrylamido-D-Glucose with Aminoacrylates and Allylamine Hydrochloride  

Microsoft Academic Search

New polyvinylsaccharides containing primary or tertiary amino groups were synthesized by radical copolymerization of 2-deoxy-2-methacrylamido-D-glucose (MAG) with 2-(dimethylamino)ethyl methacrylate, 2-(diethylamino)ethyl methacrylate (DEAEM), or allylamine hydrochloride. The reactivity ratios of comonomers were determined. The effect of copolymer composition on the conformational properties of macromolecules was detected. For MAG-DEAEM copolymers with DEAEM unit content more than 60 mol-% the increase of degree

Olga V. Nazarova; Elena A. Leontyeva; Tatyana N. Nekrasova; Anatoliy V. Dobrodumov; Yulia I. Zolotova; Alexander V. Slita; Egor N. Sushchenko; Irina I. Malakhova; Natalia N. Zelenko; Evgeny F. Panarin

2009-01-01

379

Normal coordinate analysis and vibrational spectra of 9-?-D-arabinofuranosyladenine hydrochloride (ara-A.HCl)  

Microsoft Academic Search

The vibrational spectra of a synthetic purine nucleoside with known antiviral activity, 9--D-arabino-furanosyladenine hydrochloride (ara-A.HCl) are reported. The Fourier transform infrared (FT-IR) and Fourier transform Raman (FT-Raman) spectra were recorded in the 4000-30 cm-1 spectral region. The harmonic frequencies and potential energy distributions (PED) of the vibrational modes of ara-A.HCI were calculated by two different methods: a classical molecular mechanics

L. E. Bailey; A. Hernanz; R. Navarro; T. Theophanides

1996-01-01

380

The swelling properties of hydroxypropyl methyl cellulose loaded with tetracycline hydrochloride: magnetic resonance imaging study  

Microsoft Academic Search

Magnetic resonance imaging was used to study the behavior of the gel layer thickness in hydroxypropyl methyl cellulose (HPMC) matrices loaded with different amounts of soluble tetracycline hydrochloride. The time dependence of the diffusion front, effective T2, and proton-density analysis clearly indicates a Case II diffusion mechanism in the system composed of water solution of hydrochloric acid (pH=2) and HPMC.

Joanna Kowalczuk; Jadwiga Tritt-Goc; Narcyz Pi?lewski

2004-01-01

381

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

382

Spectrophotometric Determination of Ofloxacin and Lomefloxacin Hydrochloride with Some Sulphonphthalein Dyes  

Microsoft Academic Search

Three spectrophotometric methods for the determination of ofloxacin and lomefloxacin hydrochloride are proposed, which are based on their extraction into chloroform as ion pairs with Bromophenol Blue (BPB), Bromothymol Blue (BTB) and Bromocresol Purple (BCP). The calibration graphs generated were linear over the range 525, 215 and 220 ?g ml of drug in chloroform, using three dyes, respectively. The composition

Y. M. Issa; F. M. Abdel-Gawad; H. M. Hussein

1997-01-01

383

Spectroscopic Investigation on the Synergistic Effects of Ultrasound and Dioxopromethazine Hydrochloride on Protein  

Microsoft Academic Search

The bovine serum albumin (BSA) was selected as a target molecule, the sonodynamic damage to protein in the presence of dioxopromethazine\\u000a hydrochloride (DPZ) and its mechanism were studied by means of absorption and fluorescence spectra. The results of hyperchromic\\u000a effect of absorption spectra and quenching of intrinsic fluorescence spectra indicated that the synergistic effects of ultrasound\\u000a and DPZ could induce

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

384

Spectrophotometric methods for sertraline hydrochloride and\\/or clidinium bromide determination in bulk and pharmaceutical preparations  

Microsoft Academic Search

A spectrophotometric procedure for the determination of sertraline hydrochloride (Sert) and\\/or clidinium bromide (Clid) in\\u000a bulk sample and in dosage forms was developed. The purpose of this work was to develop a rapid, simple, inexpensive, precise,\\u000a and accurate visible spectrophotometric method. The procedure is based on formation of an ion-pair complex by their reaction\\u000a with bromocresol green (BCG), bromophenol blue

Alaa S. Amin; Hassan A. Dessouki; Moustafa M. Moustafa; Mohammed S. Ghoname

2009-01-01

385

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

Microsoft Academic Search

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

Muhammad Akhlaq Mughal; Zafar Iqbal; Steven Henry Neau

2011-01-01

386

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

Microsoft Academic Search

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

Sevgi Takka; Sangita Rajbhandari; Adel Sakr

2001-01-01

387

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

PubMed

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

Tolia, Gaurav; Li, S Kevin

2014-02-01

388

Effects of various excipients on tizanidine hydrochloride tablets prepared by direct compression.  

PubMed

This study was conducted to assess the effects of various excipients in 10 different Tizanidine hydrochloride tablet dosage forms that were prepared by direct compression method (DC). Various excipients are available for DC method; we selected those excipients that are used commonly in tablet manufacturing. The excipients used included lactose anhydrous, di-basic calcium phosphate anhydrous, starch, talc, sodium carboxy methyl cellulose, polyvinyl pyrrolidone (PVP), silicon dioxide (Aerosil), stearic acid, magnesium stearate and microcrystalline cellulose (Avicel). These tablets were then evaluated by performing different pharmacopoeial and non-pharmacopoeial tests (i.e. diameter, hardness, thickness, weight variation, disintegration and assay). It was observed that Formulations B, D and H of Tizanidine hydrochloride gave best results within USP specified limits for the tests employed among all the formulations whereas Formulations F and G showed poor friability, disintegration and dissolution profiles rendering starch in combination of talc and sodium carboxy-methyl cellulose unsuitable for Tizanidine hydrochloride tablet formulations. With the present approach, more studies can be designed using other active ingredients and excipients to get an optimal and cost effective product. PMID:25176379

Khan, Lubna Ghazal; Razvi, Nighat; Anjum, Fakhsheena; Siddiqui, Saeed Ahmed; Ghayas, Sana

2014-09-01

389

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

PubMed

The effect of deprotenizing agents on recovery of donepezil hydrochloride in the development of a simple, rapid, selective and sensitive high performance liquid chromatography method for quantification of donepezil hydrochloride in human plasma was described. The deprotenizing agents were comprised of, perchloric acid, methanol, acetonitrile, chloroform and their mixtures. The chromatographic separation was carried out using reversed phase C18 column (Agilent Eclipse Plus C18) with UV detection at 268 nm. The mobile phase was comprised of 0.01 M potassium dihydrogen phosphate buffer, methanol and acetronitrile (50:30:20, v/v) adjusted to pH 2.7 with phosphoric acid (80%). A combination of perchloric acid and methanol gave a cleaner sample with a good recovery of donepezil hydrochloride of above 96%. The method showed intraday precision and accuracy in the range of 6.82% to 1.5% and 3.13% to 1.12% respectively, while interday precision and accuracy ranged between 1.06% to 4.71% and 13.01% to 6.43% respectively. The standard calibration curve was linear from 30ng/mL to 4000ng/mL, with a correlation coefficient of 0.99650.0034. The retention time of donepezil was 5.9 min with a run time of 7.0 min. The method can be applied to analyze large batch plasma samples in pharmacokinetic studies. PMID:25176366

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

2014-09-01

390

Penehyclidine hydrochloride protects against oxygen and glucose deprivation injury by modulating amino acid neurotransmitters release.  

PubMed

Penehyclidine hydrochloride (PHC) is an anticholinergic agent, with only high degree of selectivity for M1 and M3 receptor subtypes. In this study, we investigated whether PHC could play a protective effect on hippocampal slice against oxygen and glucose deprivation (OGD), as well as related to the change of amino acid neurotransmitters release. Penehyclidine hydrochloride 2, 10, and 50 ?M doses were adopted in the lactate dehydrogenase (LDH) leakage assay and triphenyl tetrazolium chloride (TTC) staining. The spontaneous miniature excitatory postsynaptic currents (mEPSCs) and amino acid neurotransmitters were detected by electrophysiology method and high-performance liquid chromatography (HPLC), respectively. Our study showed that PHC can lessen the LDH leakage ratio and tissue injury values according to TTC staining. Penehyclidine hydrochloride decreased the content of aspartate acid (Asp) and glutamate (Glu), and elevated the content of glycine (Gly) and gamma-aminobutyric acid (GABA). Ischemia increased the amplitude and frequency of the mEPSCs, but PHC obviously decreased the frequency and amplitude of mEPSCs. Thus, the study reveals the fact that PHC protects hippocampus slice against OGD injury by decreasing excitatory amino acids release and increasing inhibitory amino acids release. PMID:23899495

Wang, Yun; Ma, Tengfei; Zhou, Li; Li, Mei; Sun, Xiao-Jing; Wang, Yi-Gang; Gu, Shuling

2013-12-01

391

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

NASA Astrophysics Data System (ADS)

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

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

2014-07-01

392

Sensitive extractive spectrophotometric methods for the determination of nortriptyline hydrochloride in pharmaceutical formulations.  

PubMed

Two simple, sensitive and rapid extractive spectrophotometric methods have been developed for the assay of the antidepressant drug nortriptyline (NOR) hydrochloride in pure form and in different dosage forms. The methods involve the formation of colored ion-pairs between the drug and the complex of niobium(V)-thiocyanate (Nb-SCN) or iron(III)-thiocyanate (Fe-SCN) followed by their extraction with butanol or a mixture of butanol and chloroform and quantitative determination at 360 nm and 490 nm, using Nb-SCN and Fe-SCN, respectively. The experimental conditions were optimized to obtain the maximum colour intensity. The methods permit the determination of nortriptyline over a concentration range of 15-100 microg/ml and 5-24 microg/ml with the detection limit of 0.84 microg/ml and 0.32 microg/ml, using Nb-SCN and Fe-SCN, respectively. The proposed methods are applicable for the assay of the investigated drug in different dosage forms and the results are in good agreement with those obtained by the official and HPLC methods. No interference was observed from common excipients present in pharmaceutical formulations. The proposed procedures were applied to determine the amount of nortriptyline hydrochloride as active ingredient in the presence of its degradation product, dibenzosuberone. The extractive spectrophotometric methods can also be used to determine the amount of nortriptyline hydrochloride in tablets after its solid phase extraction (SPE). PMID:18057736

Misiuk, Wieslawa; Tykocka, Agnieszka

2007-12-01

393

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

2011-07-01

394

Effect of Modulated Alternating and Direct Current Iontophoresis on Transdermal Delivery of Lidocaine Hydrochloride  

PubMed Central

The objective of this study was to investigate the iontophoretic delivery of lidocaine hydrochloride through porcine skin and to compare the effects of modulated alternating and direct current iontophoresis. Continuous and modulated iontophoresis was applied for one hour and two hours (0-1?h and 4-5th?h) using a 1%?w/v solution of lidocaine hydrochloride. Tape stripping was done to quantify the amount of drug permeated into stratum corneum and skin extraction studies were performed to determine the amount of drug in stripped skin. Receptor was sampled and analyzed over predefined time periods. The amount of lidocaine delivered across porcine skin after modulated direct current iontophoresis for 2?h was 1069.87 120.03??g/sqcm compared to 744.81 125.41??g/sqcm after modulated alternating current iontophoresis for 2?h. Modulated direct current iontophoresis also enhanced lidocaine delivery by twelvefold compared to passive delivery as 91.27 18.71??g/sqcm of lidocaine was delivered after passive delivery. Modulated iontophoresis enhanced the delivery of lidocaine hydrochloride across porcine skin compared to the passive delivery. Modulated alternating current iontophoresis for duration of 2?h at frequency of 1?kHz was found to be comparable to the continuous direct current iontophoresis for 1?h. PMID:24959580

Banga, Ajay K.

2014-01-01

395

Controlled delivery of ropinirole hydrochloride through skin using modulated iontophoresis and microneedles.  

PubMed

The objective of this study was to investigate the effect of modulated current application using iontophoresis- and microneedle-mediated delivery on transdermal permeation of ropinirole hydrochloride. AdminPatch microneedles and microchannels formed by them were characterized by scanning electron microscopy, dye staining and confocal microscopy. In vitro permeation studies were carried out using Franz diffusion cells, and skin extraction was used to quantify drug in underlying skin. Effect of microneedle pore density and ions in donor formulation was studied. Active enhancement techniques, continuous iontophoresis (74.13 2.20 g/cm(2)) and microneedles (66.97 10.39 g/cm(2)), significantly increased the permeation of drug with respect to passive delivery (8.25 2.41?g/cm(2)). Modulated iontophoresis could control the amount of drug delivered at a given time point with the highest flux being 5.12 1.70 g/cm(2)/h (5-7 h) and 5.99 0.81 g/cm(2)/h (20-22 h). Combination of modulated iontophoresis and microneedles (46.50 6.46 g/cm(2)) showed significantly higher delivery of ropinirole hydrochloride compared to modulated iontophoresis alone (84.91 9.21 g/cm(2)). Modulated iontophoresis can help in maintaining precise control over ropinirole hydrochloride delivery for dose titration in Parkinson's disease therapy and deliver therapeutic amounts over a suitable patch area and time. PMID:23311703

Singh, Neha D; Banga, Ajay K

2013-05-01

396

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

PubMed

The aim of the present study was to apply design of experiment (DOE) to optimize floating drug delivery of tapentadol hydrochloride. Tapentadol hydrochloride is a synthetic opioid used as a centrally acting analgesic and effective in both experimental and clinical pain. The half-life of the drug is about 4 hours and oral dose is 50 to 250?mg twice a day. For optimization 3(2) full factorial design was employed for formulation of tapentadol hydrochloride tablets. Sodium bicarbonate was incorporated as a gas-generating agent. Combination of polymers Xanthan gum and Locust bean gum was used to achieve controlled release effect. The concentration of polymers was considered as the independent variables and dependent variables were floating lag time and swelling index of the tablets. From the factorial batches, it was observed that formulation containing combination of 20% sodium bicarbonate and 10% citric acid shows optimum floating ability whereas the formulation containing 20% Xanthan gum and 28% Locust bean gum shows optimum sustained drug release pattern with adequate floating. PMID:23878616

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

2013-01-01

397

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. PMID:21886901

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

2011-01-01

398

Polyoxyethylene fatty acid esters as potential promotors of transdermal absorption for morphine hydrochloride and sulphate.  

PubMed

The presence of opioid receptors mu in pathologically changed skin and mucosa justifies application of preparations with morphine salts to obtain topical analgesic activity. Numerous factors associated with the vehicle and therapeutic agent physiochemical properties affect the capability and rate of penetration of a therapeutic substance in the form of a drug into dermis. Promotors of transcutaneous absorption, which weaken the integrity of epidermal corneal layer and thus, increase therapeutic substance penetration play more and more important role. In this study non-ionic macromolecular surface active compounds from Rokacets group were suggested as potential promotors of transdermal absorption for morphine sulphate and hydrochloride. The aim of the study was to work out prescription composition of ointment with morphine salts of optimal rheological and morphological parameters and high pharmaceutical availability of the therapeutic agent (morphine sulphate, hydrochloride). Three model emulsive ointment vehicles were prepared and selected promoters of transdermal absorption were introduced into them. On the basis of the formed vehicles ointments were made with morphine sulphate and hydrochloride. The obtained vehicles and ointment preparations were subjected to rheological tests. Spreadness was determined by extensometric method and viscosity with digital cone-plate rheometer. Morphological parameters of the vehicles and ointments, such as: pH and pharmacopeal density were estimated. Carrying out direct diffusion from the surface of the preparation to acceptor fluid (to water), the amount of the released therapeutic substance in time function was determined by spectrophotometric method. The performed tests demonstrated that the investigated vehicles and ointments are non-Newtonian systems, viscoelastic and highly thixotropic. The kind of morphine salt affects the spreadness and viscosity of model ointments. Preparations with morphine hydrochloride have higher spreadness than viscosity and more alkaline pH. From among the investigated non-ionic surface active compounds Rokacet R-40 appeared to be the most beneficial promotor of transdermal absorption for both pharmacopeal morphine salts. Pharmaceutical availability of morphine sulphate and hydrochloride is the highest from ointments with its content in the vehicle prescription. PMID:17022153

Samczewska, Grazyna; Piechota-Urba?ska, Magdalena; Ko?odziejska, Justyna

2006-01-01

399

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

NASA Astrophysics Data System (ADS)

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

Borisova, T.; Krisanova, N.

400

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

PubMed Central

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

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

2014-01-01

401

Spectroscopic and biological studies of new mononuclear metal complexes of a bidentate NN and NO hydrazone-oxime ligand derived from egonol.  

PubMed

A novel ligand, vicinal dioxime ligand (egonol-hydrazone glyoxime) (LH2) was synthesized and characterized using (1)H NMR, (13)C NMR, MS, AAS, infrared spectroscopy, and magnetic susceptibility measurements. Mononuclear nickel (II), copper (II) and cobalt (II) complexes with a metal:ligand ratio of 1:2 for LH2 were also synthesized. Zn(II) forms complex [Zn(LH)Cl2] with a metal to ligand ratio of 1:1. IR spectrum shows that the ligand act in a bidentate manner and coordinates N4 donor groups of the ligands to Ni(II), Cu(II), Co(II) and Zn(II) ions. The detection of H-bonding (OH?O) in the [M(LH)2] metal complexes by IR spectra supported the square-planar MN4 coordination of Ni(II), Cu(II) and Co(II) complexes. The antimicrobial activities of compounds LH2 and their Ni(II), Cu(II), Co(II) and Zn(II) complexes were evaluated using the disc diffusion method against 16 bacteria and 5 yeasts. The minimal inhibitory concentrations (MICs) against all the bacteria and yeasts were also determined. Among the attempted test compounds, it is showed that all the compounds (L, LH2, [Ni(LH)2], [Cu(LH)2], [Co(LH)2(H2O)2], [Zn(LH)Cl2]) were effective against used test microorganisms. PMID:25686861

Babahan, Ilknur; Emirda?-ztrk, Safiye; Poyrazo?lu-oban, Esin

2015-04-15

402

Simultaneous determination of hydrochlorothiazide and benazepril hydrochloride or amiloride hydrochloride in presence of hydrochlorothiazide impurities: chlorothiazide and salamide by HPTLC method.  

PubMed

Simple, selective and sensitive high-performance thin layer chromatographic (HPTLC) method has been developed and validated for the simultaneous determination of hydrochlorothiazide (HCZ) in the presence of its impurities (chlorothiazide (CT) and salamide (DSA)), in two quaternary mixtures with benazepril hydrochloride (BZ) or amiloride hydrochloride (AM). The separation was carried out on HPTLC silica gel 60 F254 using ethyl acetate-methanol-glacial acetic acid (85:2:0.3 v/v/v) followed by densitometric measurement of bands at 240 nm for the first mixture containing HCZ, CT, DSA, BZ and by using ethyl acetate-methanol-water-ammonia (90:10:5:3 v/v/v) followed by densitometric measurement at 278 nm for the second mixture containing HCZ, CT, DSA, AM. Calibration curves were constructed in the range of (0.2-1.8 g/band) and (0.4-2.2 g/band) with good accuracy for HCZ and BZ, respectively, for the first mixture and in the range of (0.6-1.8 g/band) and (0.4-2.4 g/band) with good accuracy for HCZ and AM, respectively, for the second mixture. The developed method was validated according to ICH guidelines and demonstrated good accuracy and precision. Moreover, the methods were successfully applied for the determination of HCZ and BZ and AM in pure form and pharmaceutical dosage forms. The results were statically compared with the reported methods with no significant difference, indicating the ability of the proposed method to be used for routine analysis of drug product. PMID:24771053

Naguib, Ibrahim A; Abdelaleem, Eglal A; Zaazaa, Hala E; Draz, Mohammed E

2015-01-01

403

Fluorimetric determination of prenalterol hydrochloride in pharmaceuticals and biological fluids based on its oxidation reaction by hexacyanoferrate(III).  

PubMed

A rapid and sensitive fluorimetric method for the determination of prenalterol hydrochloride is presented, based on the oxidation of the analyte with potassium hexacyanoferrate(III) in a slightly alkaline medium (pH 9.23). The different experimental parameters were carefully studied and incorporated into the procedure. The oxidation product exhibits a blue fluorescence with its emission maximum at 427 nm, and excitation maximum at 314 nm. Fluorescence intensity is a linear function of prenalterol hydrochloride concentration over the range of 0.2-3.6 microg/ml(-1) in the solution finally measured. The method was successfully applied to the determination of prenalterol hydrochloride in pharmaceutical formulations and biological fluids. A proposal for the reaction pathway is suggested. PMID:10701414

Aly, F A

1999-11-01

404

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. PMID:23139625

Xiao, Hong-Tao; Liao, Zhi; Tong, Rong-Sheng

2012-01-01

405

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

Microsoft Academic Search

The effect of hydrogen bonding, inter- and intramolecular electrostatic interactions on the structure of 3-hydroxy-pyridine betaine hydrochloride monohydrate (1-carboxymethyl-3-hydroxypyridinium chloride monohydrate), 3-HO-PBHClH2O, has been studied by X-ray diffraction, 1H and 13C NMR and FTIR spectroscopies, and by the B3LYP\\/6-31G(d,p) calculations. In the crystal, the Cl? anion is connected with protonated betaine via the hydrogen bond, OCOH?Cl?=2.993(2) and with neighboring

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

2007-01-01

406

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

NASA Astrophysics Data System (ADS)

The aim of this work was to determine the chemical changes induced in thin films of the dry polypeptide poly-L-arginine hydrochloride and its mixture with calf thymus deoxyribonucleic acid (DNA) during 5 h of soft X-ray exposure. The physical and chemical effects of the soft X-ray irradiation were studied using X-ray Photoelectron Spectroscopy (XPS). Analysis of O1 s, N1 s and C1 s features in XPS spectra reveals the existence of several routes of radiation-induced decomposition and shows quantitative and qualitative changes.

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

2014-11-01

407

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

408

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

PubMed

The compatibility of thermodynamically unstable polymorph of two active pharmaceutical compounds (xylazine hydrochloride form X and zopiclone form C) with different excipients was investigated. The effects of the excipient and its amount in the sample on the thermal properties and possible chemical interactions were studied. The most commonly used excipients in the pharmaceutical industry - calcium carbonate, lactose hydrate, cellulose, magnesium stearate hydrate and calcium stearate hydrate were selected for this study. The dependence of the phase transition rate from an unstable to a more stable polymorph on the excipients and their amounts in the initial sample was analysed at 80C, and the corresponding phase transition rate constants were calculated. PMID:25590944

Kr?kle-B?rzi?a, Krist?ne; Acti?, Andris

2015-03-25

409

[Effect of promethazine hydrochloride (pipolphen) on the stability of R plasmid resistance in Escherichia coli].  

PubMed

The influence of promethazin hydrochloride (pipolphen) on stability of R plasmid inheritance in Escherichia coli strains of various serogroups was studied. The strains were isolated from patients with acute intestinal infection and from healthy persons. It was shown that in subbacteriostatic concentrations (100 to 450 micrograms/ml) pipolphen promoted elimination of the R plasmids. Decreased stability of the R plasmid inheritance was not associated with the pipolphen concentration. No influence of the drug on the biochemical characteristics, antigenic properties and nutritional requirements of the plasmid-free derivatives was detected. The eliminating action of pipolphen and ethidium bromide in some strans of Escherichia coli was shown to be different. PMID:9334148

Evdokimova, O V; Smirnov, I V; Artem'eva, N A; Rozhkova, E A

1997-01-01

410

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

PubMed Central

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

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

2012-01-01

411

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

PubMed

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

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

2012-04-01

412

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

Microsoft Academic Search

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

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

2009-01-01

413

Pediatric oral solutions with propranolol hydrochloride for extemporaneous compounding: the formulation and stability study.  

PubMed

The aim of this study is to formulate an extemporaneous pediatric oral solution of propranolol hydrochloride (PRO) 2 mg/ml for the therapy of infantile haemangioma or hypertension in a target age group of 1 month to school children and to evaluate its stability. A citric acid solution and/or a citrate-phosphate buffer solution, respectively, were used as the vehicles to achieve pH value of about 3, optimal for the stability of PRO. In order to mask the bitter taste of PRO, simple syrup was used as the sweetener. All solutions were stored in tightly closed brown glass bottles at 5 3 C and/or 25 3 C, respectively. The validated HPLC method was used to evaluate the concentration of PRO and a preservative, sodium benzoate, at time intervals of 0-180 days. All preparations were stable at both storage temperatures with pH values in the range of 2.8-3.2. According to pharmacopoeial requirements, the efficacy of sodium benzoate 0.05 % w/v was proved (Ph.Eur., 5.1.3). The preparation formulated with the citrate-phosphate buffer, in our experience, had better palatability than that formulated with the citric acid solution. Keywords: propranolol hydrochloride pediatric preparation extemporaneous preparation solution stability testing HPLC. PMID:23578266

Klovrzov, Sylva; Zahlka, Luk; Matysov, Ludmila; Hork, Petr; Sklubalov, Zdenka

2013-01-01

414

Stability-indicating LC method for the estimation of bendamustine hydrochloride and its related impurities.  

PubMed

A novel, simple, sensitive and stability-indicating high-performance liquid chromatography method was developed and validated for the quantification of impurities (process related and degradants) and the assay determination of Bendamustine hydrochloride. A chromatographic separation of Bendamustine and its impurities was achieved with an Inertsil ODS-2 analytical column, 250 4.6 mm, 5 m, using gradient elution with mobile phase A consisting of a mixture of water and trifluoroacetic acid (1000:1, v/v) and mobile phase B consisting of acetonitrile. The instrumental settings included a flow rate of 1.0 mL/min, column temperature of 27C and a detector wavelength of 233 nm, using a photodiode array detector. The tailing factor for Bendamustine was 1.10. Bendamustine hydrochloride was exposed to thermal, photolytic, hydrolytic and oxidative stress conditions and the stressed samples were analyzed by the proposed method. Peak homogeneity data of Bendamustine were obtained by using a photodiode array detector in the stressed sample chromatograms, which demonstrated the specificity of the method for estimation in the presence of degradants. The developed method was validated for parameters such as precision, accuracy, linearity, limit of detection, limit of quantification, ruggedness and robustness. The stability tests were also performed on drug substances as per International Conference on Harmonization guidelines. PMID:23825351

Kasa, Srinivasulu; Raja Sekhar Reddy, M; Kadaboina, Raja Sekhar; Murki, Veerender; Mulukutla, Venkata Suryanarayana

2014-08-01

415

Solubility-modulated asymmetric membrane tablets of triprolidine hydrochloride: statistical optimization and evaluation.  

PubMed

The aim of the present study was to develop asymmetric membrane (AM) tablets for controlled delivery of highly water-soluble antihistaminic drug triprolidine hydrochloride. The solubility of triprolidine hydrochloride was modulated through the incorporation of coated sodium chloride crystals encapsulated with asymmetric membrane coating polymer, cellulose acetate butyrate. Formulation of AM tablets was based on a 2(3) factorial design to study the effect of formulation variables, namely, polymer concentration, level of pore former, and amount of osmogen on the in vitro release. Core tablets prepared by wet granulation and coated with asymmetric membrane by a dip coating method were evaluated. Statistical analysis was done with the Design Expert Software 8.0.2 (USA), and the polynomial equation generated by Pareto charts was used for validation of the experimental design. The interaction chart and response surface plots deduced the simultaneous effect of independent variables on in vitro drug release. The in vitro drug release was inversely proportional and directly related to the level(s) of polymer and pore former in the membrane, respectively. The level of osmogen not only increased the osmotic pressure but also controlled the drug release due to a common ion effect. The drug release of the optimized formulation (F6) followed zero-order kinetics, which would be capable of reducing the administration, and was stable over 3 months. SEM photographs revealed asymmetry in membrane structure. PMID:22183255

Dev, Rahul; Kumar, Anil; Pathak, Kamla

2012-03-01

416

Randomized Controlled Trial of Levamisole Hydrochloride as Adjunctive Therapy in Severe Falciparum Malaria With High Parasitemia  

PubMed Central

Background.?Cytoadherence and sequestration of erythrocytes containing mature stages of Plasmodium falciparum are central to the pathogenesis of severe malaria. The oral anthelminthic drug levamisole inhibits cytoadherence in vitro and reduces sequestration of late-stage parasites in uncomplicated falciparum malaria treated with quinine. Methods.?Fifty-six adult patients with severe malaria and high parasitemia admitted to a referral hospital in Bangladesh were randomized to receive a single dose of levamisole hydrochloride (150 mg) or no adjuvant to antimalarial treatment with intravenous artesunate. Results.?Circulating late-stage parasites measured as the median area under the parasite clearance curves were 2150 (interquartile range [IQR], 028 025) parasites/L hour in patients treated with levamisole and 5489 (IQR, 19225 848) parasites/L hour in controls (P = .25). The sequestration ratios at 6 and 12 hours for all parasite stages and changes in microvascular blood flow did not differ between treatment groups (all P > .40). The median time to normalization of plasma lactate (<2 mmol/L) was 24 (IQR, 1230) hours with levamisole vs 28 (IQR, 1236) hours without levamisole (P = .15). Conclusions.?There was no benefit of a single-dose of levamisole hydrochloride as adjuvant to intravenous artesunate in the treatment of adults with severe falciparum malaria. Rapid parasite killing by intravenous artesunate might obscure the effects of levamisole. PMID:23943850

Maude, Richard J.; Silamut, Kamolrat; Plewes, Katherine; Charunwatthana, Prakaykaew; Ho, May; Abul Faiz, M.; Rahman, Ridwanur; Hossain, Md Amir; Hassan, Mahtab U.; Bin Yunus, Emran; Hoque, Gofranul; Islam, Faridul; Ghose, Aniruddha; Hanson, Josh; Schlatter, Joel; Lacey, Rachel; Eastaugh, Alison; Tarning, Joel; Lee, Sue J.; White, Nicholas J.; Chotivanich, Kesinee; Day, Nicholas P. J.; Dondorp, Arjen M.

2014-01-01

417

Vascular Normalization Induced by Sinomenine Hydrochloride Results in Suppressed Mammary Tumor Growth and Metastasis  

PubMed Central

Solid tumor vasculature is characterized by structural and functional abnormality and results in a hostile tumor microenvironment that mediates several deleterious aspects of tumor behavior. Sinomenine is an alkaloid extracted from the Chinese medicinal plant, Sinomenium acutum, which has been utilized to treat rheumatism in China for over 2000 years. Though sinomenine has been demonstrated to mediate a wide range of pharmacological actions, few studies have focused on its effect on tumor vasculature. We showed here that intraperitoneally administration of 100?mg/kg sinomenine hydrochloride (SH, the hydrochloride chemical form of sinomenine) in two orthotopic mouse breast cancer models for 14 days, delayed mammary tumor growth and decreased metastasis by inducing vascular maturity and enhancing tumor perfusion, while improving chemotherapy and tumor immunity. The effects of SH on tumor vessels were caused in part by its capability to restore the balance between pro-angiogenic factor (bFGF) and anti-angiogenic factor (PF4). However 200?mg/kg SH didn't exhibit the similar inhibitory effect on tumor progression due to the immunosuppressive microenvironment caused by excessive vessel pruning, G-CSF upregulation, and GM-CSF downregulation. Altogether, our findings suggest that SH induced vasculature normalization contributes to its anti-tumor and anti-metastasis effect on breast cancer at certain dosage. PMID:25749075

Zhang, Huimin; Ren, Yu; Tang, Xiaojiang; Wang, Ke; Liu, Yang; Zhang, Li; Li, Xiao; Liu, Peijun; Zhao, Changqi; He, Jianjun

2015-01-01

418

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, Vctor

2006-09-01

419

Solid state characterization of hydroxyprocaine hydrochloride. Crystal polymorphism of local anaesthetic drugs, part VIII  

NASA Astrophysics Data System (ADS)

Two polymorphic and a pseudopolymorphic crystal form of the local anaesthetic drug hydroxyprocaine hydrochloride (4-Butylamino-2-hydroxybenzoic acid 2-dimethylaminoethyl ester hydrochloride, HPCHC) are characterized by thermal analysis (hot stage microscopy, differential scanning calorimetry, thermogravimetry), spectroscopy (FTIR-, FT-Raman-, SSNMR-spectroscopy), powder X-ray diffractometry and water vapor sorption analysis. The formation and thermodynamic stability of the different solid phases is described and presented in a flow chart and in an energy/temperature diagram, respectively. Mod. II is the thermodynamically stable form at room temperature and present in commercial products mostly contaminated with a hydrated form which is isostructural with the unstable mod. I. The stable mod. II crystallizes from most organic solvents in combination with seeds of the metastable mod. I and from the melt below 130 C. Pure mod. I crystallizes from the melt at temperatures above 130 C and additionally appears on dehydration of the hydrate. According to the heat of fusion rule, mod. I is the thermodynamically less stable form below the transition temperature (enantiotropism). The sorption isotherms show a distinct lower hygroscopicity for the stable mod. II, whereas the unstable mod. I converts to the hydrate under moisture conditions above 0% RH at room temperature.

Schmidt, A. C.; Schwarz, I.

2005-06-01

420

Vascular normalization induced by sinomenine hydrochloride results in suppressed mammary tumor growth and metastasis.  

PubMed

Solid tumor vasculature is characterized by structural and functional abnormality and results in a hostile tumor microenvironment that mediates several deleterious aspects of tumor behavior. Sinomenine is an alkaloid extracted from the Chinese medicinal plant, Sinomenium acutum, which has been utilized to treat rheumatism in China for over 2000 years. Though sinomenine has been demonstrated to mediate a wide range of pharmacological actions, few studies have focused on its effect on tumor vasculature. We showed here that intraperitoneally administration of 100?mg/kg sinomenine hydrochloride (SH, the hydrochloride chemical form of sinomenine) in two orthotopic mouse breast cancer models for 14 days, delayed mammary tumor growth and decreased metastasis by inducing vascular maturity and enhancing tumor perfusion, while improving chemotherapy and tumor immunity. The effects of SH on tumor vessels were caused in part by its capability to restore the balance between pro-angiogenic factor (bFGF) and anti-angiogenic factor (PF4). However 200?mg/kg SH didn't exhibit the similar inhibitory effect on tumor progression due to the immunosuppressive microenvironment caused by excessive vessel pruning, G-CSF upregulation, and GM-CSF downregulation. Altogether, our findings suggest that SH induced vasculature normalization contributes to its anti-tumor and anti-metastasis effect on breast cancer at certain dosage. PMID:25749075

Zhang, Huimin; Ren, Yu; Tang, Xiaojiang; Wang, Ke; Liu, Yang; Zhang, Li; Li, Xiao; Liu, Peijun; Zhao, Changqi; He, Jianjun

2015-01-01

421

Effects of automated external lubrication on tablet properties and the stability of eprazinone hydrochloride.  

PubMed

We investigated the advantages of an external lubrication technique for tableting. A newly developed external lubricating system was applied to tableting in a rotary tablet press using magnesium stearate. The resulting tablets were compared with tablets produced by the conventional internal lubrication method, in which lubricant is blended before tableting. As a model API, we chose eprazinone hydrochloride, because it is easily hydrolyzed by alkaline lubricant. The amount of lubricant required to prevent sticking with external lubrication was only 1/13th of that required with internal lubrication. External lubrication increased tablet crushing strength by 40%, without prolonging tablet disintegration time, and improved the residual ratio of eprazinone hydrochloride in tablets stored under stress conditions for 4 weeks by 10%. The distribution of lubricant on the surface of externally lubricated tablets was observed by scanning electron microscopy after the preparation by focused ion beam milling. The lubricant had formed a layer on the tablet surface. At the central part of the tablet surface, this layer was much thinner than at the edges, and remained extremely thin even when there was excess magnesium stearate. This is the first report to describe the distribution of lubricant on the surface of externally lubricated tablets. PMID:19059327

Yamamura, Takahiro; Ohta, Tomoaki; Taira, Toshinari; Ogawa, Yutaka; Sakai, Yasuyuki; Moribe, Kunikazu; Yamamoto, Keiji

2009-03-31

422

Development and Validation of RP-HPLC Method for the Estimation of Ivabradine Hydrochloride in Tablets.  

PubMed

A simple, sensitive, precise and robust reverse-phase high-performance liquid chromatographic method for analysis of ivabradine hydrochloride in pharmaceutical formulations was developed and validated as per ICH guidelines. The separation was performed on SS Wakosil C18AR, 2504.6 mm, 5 ?m column with methanol:25 mM phosphate buffer (60:40 v/v), adjusted to pH 6.5 with orthophosphoric acid, added drop wise, as mobile phase. A well defined chromatographic peak of Ivabradine hydrochloride was exhibited with a retention time of 6.550.05 min and tailing factor of 1.14 at the flow rate of 0.8 ml/min and at ambient temperature, when monitored at 285 nm. The linear regression analysis data for calibration plots showed good linear relationship with R=0.9998 in the concentration range of 30-210 ?g/ml. The method was validated for precision, recovery and robustness. Intra and Inter-day precision (% relative standard deviation) were always less than 2%. The method showed the mean % recovery of 99.00 and 98.55 % for Ivabrad and Inapure tablets, respectively. The proposed method has been successfully applied to the commercial tablets without any interference of excipients. PMID:21695008

Seerapu, Sunitha; Srinivasan, B P

2010-09-01

423

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 KorsmeyerPeppas 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. PMID:23960766

Koocheki, S.; Madaeni, S.S.; Niroomandi, P.

2011-01-01

424

Effect of guanidine hydrochloride on removal rate selectivity and wafer topography modification in barrier CMP  

NASA Astrophysics Data System (ADS)

We propose an alkaline barrier slurry containing guanidine hydrochloride (GH) and hydrogen peroxide. The slurry does not contain any corrosion inhibitors, such as benzotriazole (BTA). 3-inch samples of tantalum copper and oxide were polished to observe the removal rate. The effect of GH on removal rate selectivity along with hydrogen peroxide was investigated by comparing slurry containing GH and H2O2 with slurry containing only GH. Details about the tantalum polishing mechanism in an alkaline guanidine-based slurry and the electrochemical reactions are discussed. The results show that guanidine hydrochloride can increase the tantalum polishing rate and the selectivity of copper and barrier materials. The variation of the dishing and wire line resistance with the polishing time was measured. The dishing value after a 300 mm pattern wafer polishing suggests that the slurry has an effective performance in topography modification. The result obtained from the copper wire line resistance test reveals that the wire line in the trench has a low copper loss.

Hailong, Li; Jin, Kang; Yuling, Liu; Chenwei, Wang; Hong, Liu; Jiaojiao, Gao

2014-03-01

425

Role of 1-methyl-3-octylimidazolium chloride in the micellization behavior of amphiphilic drug amitriptyline hydrochloride.  

PubMed

The mixed micellization behaviour of amitriptyline hydrochloride (AMT) with ionic liquid (IL) 1-methyl-3-octylimidazolium hydrochloride, [C8mim][Cl], have been investigated using electrical conductivity, at different temperatures. The non-ideal behaviour (i.e., synergistic interaction) of AMT-[C8mim][Cl] binary mixtures, explained by the deviations in critical micelle concentration (cmc) from ideal critical micelle concentration (cmc*) and micellar mole fraction (X(m)) from ideal micellar mole fraction (X(ideal)) values. The values of interaction parameter (?) and activity coefficients (f1 and f2), also confirm the synergistic interaction. The excess free energy (?Gex) for the AMT-[C8mim][Cl] binary mixtures explains, stability of mixed micelles in comparison to micelles of pure, AMT and [C8mim][Cl]. The calculated thermodynamic parameters (viz., the standard Gibbs energy change, ?Gm(?), the standard enthalpy change, ?Hm(?), the standard entropy change, ?Sm(?)), suggest the dehydration of hydrophobic part of the drug at higher temperatures (>313K), not only in case of AMT but also in the presence of [C8mim][Cl]. PMID:24077084

Khan, Abbul Bashar; Ali, Maroof; Malik, Nisar Ahmad; Ali, Anwar; Patel, Rajan

2013-12-01

426

[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

427

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

PubMed Central

The objective of this investigation was the development of chitosan/xanthan polyelectrolyte complex based mucoadhesive nasal insert of promethazine hydrochloride a drug used in the treatment of motion sickness. A 32 factorial design was applied for preparing chitosan/xanthan polyelectrolyte complex and to study the effect of independent variables i.e. concentration of xanthan [X1] and concentration of chitosan [X2] on various responses i.e. viscosity of polyelectrolyte complex solution, water uptake of nasal inserts (at pH 2, 5.5, 7.4), bioadhesion potential of nasal inserts and in-vitro drug release at Q6h through nasal inserts. FTIR and DSC analysis were carried out to confirm complex formation and on loaded and unloaded nasal insert to investigate any drug excipient interaction. The nasal inserts were also characterized by powder X-ray diffractometry (PXRD) and Scanning electron microscopy (SEM) and for ex-vivo permeation studies. The results show that higher amount of xanthan in polyelectrolyte complexes with respect to higher amount of chitosan retarded in-vitro drug release. The water uptake behaviour of nasal insert was strongly influenced by pH of the medium and by polycation/ polyanion concentration. The investigation verifies the formation of polyelectrolyte complexes formation between chitosan and xanthan at pH values in the vicinity of pKa intervals of the two polymers and confirms their potential for the nasal delivery of promethazine hydrochloride. PMID:25276178

G Dehghan, Mohamed Hassan; Marzuka, Marzuka

2014-01-01

428

Spectrophotometric estimation of eflornithine hydrochloride by using ion-pair reagents.  

PubMed

Four newer, cost effective and sensitive ion-pair complex methods were estimated for the determination of eflornithine hydrochloride drug in pharmaceutical formulation. In these methods eflornithine hydrochloride react with bromocresol green (buffer of pH 4), bromophenol blue (buffer pH 4.5), methyl orange (buffer of pH 5.5) and bromothymol blue (buffer of pH 5) respectively. The chloroform was used for extraction of ion-pair complexes. The measurement of complexes was done at 413, 416, 417 and 425 nm respectively. Under the described conditions the proposed methods are linear over the concentration range of 3-18, 4-16, 6-30 and 2-12 ?g/ml and the coefficient of determination were >0.999 (n=6) with a relative standard deviation of <1% (n=6). The average recovery of the target compound is >100% with a limit of quantification (LOQ) of 20, 0.869, 2 and 4.167 ?g/ml and the limit of detection (LOD) 6.6, 0.287, 0.66 and 1.375 ?g/ml. The mechanism of the derivatization reaction is proposed and advantages of the proposed method are discussed. PMID:25730793

Kumar, Amit; Singh, Vijender; Kumar, Praveen

2015-03-01

429

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

430

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

NASA Astrophysics Data System (ADS)

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

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

2011-03-01

431

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.

2011-10-01

432

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 H NMR, 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 LC?? values of 1.0969 and 1.2632 mg/L, respectively. This suggested that introduction of R and R together as the electron-withdrawing substituents, R as the methyl group, and R? 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(training set)), the leave-one-out cross-validation correlation coefficient (Q(LOO)), and the 7-fold cross-validation correlation coefficient (Q(7-fold)) were 0.791, 0.701, and 0.715, respectively. The external cross-validation correlation coefficient (Qext) and the root-mean-square error for the test set (RMSE(test set)) were 0.774 and 3.412, respectively. This study will pave the way for future design, structural modification, and development of indole derivatives as nematicidal agents. PMID:23738496

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

2013-06-19

433

Cytotoxic iron chelators: characterization of the structure, solution chemistry and redox activity of ligands and iron complexes of the di-2-pyridyl ketone isonicotinoyl hydrazone (HPKIH) analogues.  

PubMed

Di-2-pyridyl ketone isonicotinoyl hydrazone (HPKIH) and a range of its analogues comprise a series of monobasic acids that are capable of binding iron (Fe) as tridentate ( N, N, O) ligands. Recently, we have shown that these chelators are highly cytotoxic, but show selective activity against cancer cells. Particularly interesting was the fact that cytotoxicity of theHPKIH analogues is maintained even after complexation with Fe. To understand the potent anti-tumor activity of these compounds, we have fully characterized their chemical properties. This included examination of the solution chemistry and X-ray crystal structures of both the ligands and Fe complexes from this class and the ability of these complexes to mediate redox reactions. Potentiometric titrations demonstrated that all chelators are present predominantly in their charge-neutral form at physiological pH (7.4), allowing access across biological membranes. Keto-enol tautomerism of the ligands was identified, with the tautomers exhibiting distinctly different protonation constants. Interestingly, the chelators form low-spin (diamagnetic) divalent Fe complexes in solution. The chelators form distorted octahedral complexes with Fe(II), with two tridentate ligands arranged in a meridional fashion. Electrochemistry of the Fe complexes in both aqueous and non-aqueous solutions revealed that the complexes are oxidized to their ferric form at relatively high potentials, but this oxidation is coupled to a rapid reaction with water to form a hydrated (carbinolamine) derivative, leading to irreversible electrochemistry. The Fe complexes of theHPKIH analogues caused marked DNA degradation in the presence of hydrogen peroxide. This observation confirms that Fe complexes from theHPKIH series mediate Fenton chemistry and do not repel DNA. Collectively, studies on the solution chemistry and structure of theseHPKIH analogues indicate that they can bind cellular Fe and enhance its redox activity, resulting in oxidative damage to vital biomolecules. PMID:14564555

Bernhardt, Paul V; Caldwell, Lorraine M; Chaston, Timothy B; Chin, Piao; Richardson, Des R

2003-11-01

434

Extractive spectrophotometric methods for the determination of doxepin hydrochloride in pharmaceutical preparations using titanium (IV) and iron (III) thiocyanate complexes  

Microsoft Academic Search

Two simple, precise, and accurate extractive spectrophotometric methods have been developed for the determination of doxepin hydrochloride in pharmaceutical preparations. The methods are based on the formation of ion association complexes of doxepin with titanium (IV) and iron (III) thiocyanate complexes in acidic medium. The produced compounds are insoluble in water but well soluble in some organic solvents. They are

Wies?awa Misiuk

2005-01-01

435

Potentiometric determination of antihistaminic diphenhydramine hydrochloride in pharmaceutical preparations and biological fluids using screen-printed electrode  

Microsoft Academic Search

The performance characteristic of sensitive screen-printed (SPE) and carbon paste (CPE) electrodes was investigated for the determination of diphenhydramine hydrochloride (DPH) drug in pure, pharmaceutical preparations and biological fluids. Different experimental conditions namely types of materials used to prepare the working electrode (plasticizer), titrant, pH, temperature and life time were studied. Under these conditions, the SPE shows the best performance

Eman Y. Z. Frag; Gehad G. Mohamed; Wael G. El-Sayed

2011-01-01

436

Chemical stability of ziconotide-clonidine hydrochloride admixtures with and without morphine sulfate during simulated intrathecal administration.  

PubMed

Objective.? To determine the stability of ziconotide-clonidine hydrochloride admixtures with and without morphine sulfate during simulated intrathecal infusion under laboratory conditions at 37. Materials and Methods.? Admixtures of ziconotide (25g/mL) and clonidine hydrochloride (2mg/mL) with and without morphine sulfate (35mg/mL) were stored in Medtronic SynchroMed II pumps at 37. Pumps were sampled immediately after filling and at four additional time points over the course of 28 (ziconotide-clonidine hydrochloride admixture) or 20 (ziconotide-clonidine hydrochloride-morphine sulfate admixture) days. Drug concentrations were determined using high-performance liquid chromatography. Results.? Ziconotide concentration exceeded 97% of initial at all time points when combined with clonidine alone; statistical evaluation indicated that both ziconotide and clonidine concentrations would remain above 90% of initial for more than 60days. When compounded with both clonidine and morphine, ziconotide and clonidine concentrations declined; statistical evaluation indicated that the ziconotide concentration was 70% of initial after 20days, and that clonidine would remain 90% stable for 42days. Morphine was stable in the presence of ziconotide and clonidine. Conclusions.? A ziconotide-clonidine admixture was 90% stable for 60days (extrapolated), and a ziconotide-clonidine-morphine admixture was 70% stable for 20days. PMID:22150946

Shields, David; Montenegro, Rick

2007-10-01

437

Utilization of carbon disulphide for the analytical determination of betahistine hydrochloride and captopril in their pharmaceutical preparations  

Microsoft Academic Search

Spectrophotometric, atomic absorption spectrometric and high performance liquid chromatographic (HPLC) procedures have been developed for the determination of betahistine hydrochloride and captopril. The three procedures are based on the reaction of the drugs with carbon disulphide in alkaline medium with the formation of the dithiocarbamate or the trithiocarbonate derivative of betahistine (BHT) and captopril (CAP), respectively, then subsequent chelation with

A. F. M El Walily; O. A Razak; S. F Belal; R. S Bakry

1999-01-01

438

DETERMINATION OF THE SLEEP AID INGREDIENTS DIPHENHYDRAMINE HYDROCHLORIDE AND DOXYLAMINE SUCCINATE IN PHARMACEUTICAL PRODUCTS BY QUANTITATIVE HPTLC  

Microsoft Academic Search

A quantitative method, using high performance thin layer chromatography (HPTLC) with automated sample application and UV-absorption scanning densitometry, was developed for the determination of diphenhydramine hydrochloride and doxylamine succinate in pharmaceutical sleep aid products. Separation was performed on high performance silica gel plates, and the analytes were detected as fluorescence-quenched zones under 254 nm UV light. Three pharmaceutical products containing

Donna DiGregorio; Joseph Sherma

1999-01-01

439

Determination of ranitidine hydrochloride in pharmaceutical preparations by titrimetry and visible spectrophotometry using bromate and acid dyes  

Microsoft Academic Search

Four new methods using titrimetry and spectrophotometry are described for the determination of ranitidine hydrochloride (RNH) with potassium bromate as the oxidimetric reagent and acid dyes, methyl orange, indigo carmine and metanil yellow. In direct titrimetry (method A), the drug is titrated directly with bromate in acid medium and in the presence of excess of bromide using methyl orange indicator.

K. Basavaiah; P. Nagegowda

2004-01-01

440

Randomized controlled trial of pilocarpine hydrochloride for the moderation of oral mucositis during autologous blood stem cell transplantation  

Microsoft Academic Search

Pilocarpine hydrochloride has been reported to increase salivation and decrease oral mucositis in patients receiving head and neck radiotherapy, but there is only one report of its use in a cancer chemotherapy patient population. This prospective, double-blinded, randomized, placebo-controlled trial was undertaken to determine the efficacy of pilocarpine for the moderation of oral mucositis during autologous blood stem cell transplantation.

P B Lockhart; M T Brennan; M L Kent; C H Packman; H J Norton; P C Fox; G Frenette

2005-01-01

441

Simultaneous spectrophotometric determination of metformin hydrochloride and glibenclamide in binary mixtures using combined discrete and continuous wavelet transforms.  

PubMed

In this work, a combined discrete and continuous wavelet transform analysis was developed for simultaneous spectrophotometric determinations of metformin hydrochloride and glibenclamide, two antidiabetic drugs, in binary mixtures without any chemical pretreatment. Absorption spectra were subjected to the 4-level db4 discrete wavelet transform (DWT) for signal de-noising. Selected continuous wavelet transform (CWT) families (rbio3.1 with scaling factor, a = 80, and gaus2, a = 60) were applied on these de-noised signals. Finally, a zero-crossing technique was used for the construction of calibration curves for both drugs. The proposed method was validated by analyzing synthetic mixtures of the investigated drugs with various concentrations. The amount of metformin hydrochloride and glibenclamide were determined by using CWT amplitudes in zero-crossing points. The mean recovery values of metformin hydrochloride and glibenclamide were found between 98.6-102.0 and 97.9-102.4% for rbio3 and 98.3-101.2 and 97.1-101.4% for gaus2 families, respectively. The obtained results showed that the developed method is a simple, rapid and precise procedure for the simultaneous determination of metformin hydrochloride and glibenclamide in binary mixtures. PMID:21985929

Sohrabi, Mahmoud Reza; Kamali, Naghmeh; Khakpour, Mazyar

2011-01-01

442

Sevelamer hydrochloride dose-dependent increase in prevalence of severe acidosis in hemodialysis patients: analysis of nationwide statistical survey in Japan.  

PubMed

Metabolic acidosis has a negative impact on prognosis of dialysis patients. The aim of this study was to determine the prevalence of severe metabolic acidosis in dialysis patients treated with sevelamer hydrochloride. In 2004, a nationwide survey (101,516 dialysis patients) was conducted by the Japanese Society for Dialysis Therapy. We analyzed 32,686 dialysis patients whose bicarbonate levels were measured in the survey. Sevelamer hydrochloride was prescribed to 9231 dialysis patients while 23,455 dialysis patients were not prescribed sevelamer hydrochloride. In the present study, we defined severe acidosis as bicarbonate <15.8 mmol/L. The mean serum bicarbonate level correlated significantly and negatively with the daily dose of sevelamer hydrochloride (R(2)?= 0.806, P < 0.0001). Logistic regression analysis indicated that the percentage of patients with severe acidosis increased significantly with increased dose of sevelamer hydrochloride (R(2) = 0.885, P < 0.00001). The estimated doses of sevelamer hydrochloride associated with severe acidosis in 10% and 15% of patients were 3.5 g/day (95% confidence interval [95%CI], 2.8-4.4) and 7.7 g/day (95%CI = 5.9-10.9), respectively. Severe acidosis was noted in 4.5% of patients who were not treated with sevelamer hydrochloride and in 16.1% of patients treated with sevelamer hydrochloride at ? 5.25 g/day (P < 0.0001). The results call for careful monitoring of serum bicarbonate level in hemodialysis patients treated with sevelamer hydrochloride. PMID:24499082

Oka, Yoshinari; Miyazaki, Masashi; Matsuda, Hiroaki; Takatsu, Shigeko; Katsube, Ryouichi; Mori, Toshiko; Takehara, Kiyoto; Umeda, Yuzo; Uno, Futoshi

2014-02-01

443

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

PubMed

Metal complexes of copper(II), nickel(II), cobalt(II), oxovanadium(IV), chromium(III) and cadmium(II) with a new bridged ONS dibasic tridentate hydrazone (H2L) derived from 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione with S-methyl dithiocarbazate have been synthesized and characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, spectral (infrared, electronic, mass, 1H NMR and ESR) studies as well as thermal gravimetric analysis (TGA). The synthesized complexes have dimeric structures with the general formula [ML(NO3)m(H2O)x]2nH2OzMeOH, L=dianion of the hydrazone, m=0-1, x=0-2, n=0-4 and z=0-1. The metal complexes exhibited square planar, tetrahedral and octahedral geometrical arrangements, the molar conductivity data indicates that all complexes are neutral. The Coats-Redfern equation was used to calculate the kinetic and thermodynamic parameters for the different thermal decomposition stages of some complexes. Structural parameters of the ligand and its metal complexes have been theoretically computed on the basis of semiempirical PM3 level and the results were correlated with their experimental data. Antibacterial activities of the free ligand and its metal complexes were screened against various organisms. PMID:24810030

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

2014-09-15

444

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

NASA Astrophysics Data System (ADS)

Metal complexes of copper(II), nickel(II), cobalt(II), oxovanadium(IV), chromium(III) and cadmium(II) with a new bridged ONS dibasic tridentate hydrazone (H2L) derived from 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione with S-methyl dithiocarbazate have been synthesized and characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, spectral (infrared, electronic, mass, 1H NMR and ESR) studies as well as thermal gravimetric analysis (TGA). The synthesized complexes have dimeric structures with the general formula [ML(NO3)m(H2O)x]2nH2OzMeOH, L = dianion of the hydrazone, m = 0-1, x = 0-2, n = 0-4 and z = 0-1. The metal complexes exhibited square planar, tetrahedral and octahedral geometrical arrangements, the molar conductivity data indicates that all complexes are neutral. The Coats-Redfern equation was used to calculate the kinetic and thermodynamic parameters for the different thermal decomposition stages of some complexes. Structural parameters of the ligand and its metal complexes have been theoretically computed on the basis of semiempirical PM3 level and the results were correlated with their experimental data. Antibacterial activities of the free ligand and its metal complexes were screened against various organisms.

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

2014-09-01

445

Antazoline phosphate and naphazoline hydrochloride, singly and in combination for the treatment of allergic conjunctivitis-a controlled, double-blind clinical trial.  

PubMed

A controlled, double-blind comparison of naphalzoline hydrochloride 0.05%, antazoline phosphate 0.5%, a combination of both components and a placebo was performed on 51 ragweed sensitive patients presenting allergic conjunctivitis. Evaluation of response at various times after instillation of medication for lacrimation, conjunctival inflammation, pruritus, photophobia and pain showed naphazoline hydrochloride, antazoline phosphate and the combination product superior to placebo. The combination product was statistically significantly superior for conjunctival inflammation and photophobia. The need for post-challenge treatment with epinephrine hydrochloride was significantly less in those eyes treated with the combination product. demonstrating prophylactic efficacy. PMID:1096685

Miller, J; Wolf, E H

1975-08-01

446

Pre-treatment of Dairy and Breast Milk with Sevelamer Hydrochloride and Sevelamer Carbonate to Reduce Phosphate  

PubMed Central

? Introduction: Young children and infants with chronic kidney disease are at increased risk of hyperphosphatemia because of high intake of dairy products. Hyperphosphatemia leads to metastatic calcifications and an increased risk of cardiovascular complications. Sevelamer is an effective phosphate binder, but for children it has important practical disadvantages: it clogs enteral feeding tubes and can cause gastrointestinal complaints. Pre-treatment of dairy products to reduce their phosphate content might solve those problems. ? Methods: Sevelamer hydrochloride and sevelamer carbonate were suspended in various dairy products (cows milk, breast milk, baby formula, and tube-feeding formula). Each product was tested with varying concentrations of sevelamer. After suspension, each sample was stored for 10 minutes, allowing the sevelamer to precipitate. The supernatant was decanted and analyzed for pH and for phosphate, calcium, magnesium, potassium, sodium, and chloride content. ? Results: We observed a significant decrease in the phosphate content of all tested products. With sevelamer hydrochloride, the phosphate reduction was 48% - 91% in the various products, and with sevelamer carbonate, it was 22% - 87%. The highest effectiveness was found in breast milk. A pH increase was found in all products. With sevelamer hydrochloride, a significant increase in chloride occurred. Notably, a significant decrease in calcium content (-75%) was observed in treated breast milk. ? Conclusions: Pretreatment of a variety of dairy products with either sevelamer hydrochloride or sevelamer carbonate effectively reduced their phosphate content and might avoid troublesome ingestion of sevelamer in children. The change in pH with sevelamer hydrochloride was remarkable, reflecting buffering mechanisms. The reduction in the calcium content of breast milk is a potential concern and should be carefully considered and monitored during clinical use of sevelamer. PMID:23636435

Raaijmakers, Renske; Houkes, Lambertus M.W.; Schrder, Cornelis H.; Willems, Johannes L.; Monnens, Leo A.H.

2013-01-01

447

A validated stability-indicating HPLC method for the simultaneous determination of pheniramine maleate and naphazoline hydrochloride in pharmaceutical formulations  

PubMed Central

Background A simple, rapid, and accurate stability-indicating reverse phase liquid chromatographic method was developed and validated for the simultaneous determination of pheniramine maleate and naphazoline hydrochloride in bulk drugs and pharmaceutical formulations. Results Optimum chromatographic separations among pheniramine maleate, naphazoline hydrochloride and stress-induced degradation products have been achieved within 10 minutes by using an Agilent zorbax eclipse XDB C18 column (150mm??4.6mm, 5?m) as the stationary phase with a mobile phase consisted of 10mM phosphate buffer pH2.8 containing 0.5% triethlamine and methanol (68:32, v/v) at a flow rate of 1mLmin-1. Detection was performed at 280nm using a diode array detector. Theoretical plates for pheniramine maleate and naphazoline hydrochloride were calculated to be 6762 and 6475, respectively. The method was validated in accordance with ICH guidelines with respect to linearity, accuracy, precision, robustness, specificity, limit of detection and quantitation. Regression analysis showed good correlations (R2?>?0.999) for pheniramine maleate in the concentration range of 1501200?gmL-1 and naphazoline hydrochloride in 12.5-100?gmL-1. The method results in excellent separation of both the analytes and degradation products. The peak purity factor is ?980 for both analytes after all types of stress, indicating complete separation of both analyte peaks from the stress induced degradation products. Conclusions Overall, the proposed stability-indicating method was suitable for routine quality control and drug analysis of pheniramine maleate and naphazoline hydrochloride in pharmaceutical formulations. PMID:24485011

2014-01-01

448

Vibrational spectra and density functional theoretical calculations on the anti-neurodegenerative drug: Orphenadrine hydrochloride  

NASA Astrophysics Data System (ADS)

Vibrational spectral analysis and quantum chemical computations based on density functional theory have been performed on the anti-neuro-degenerative drug Orphenadrine hydrochloride. The geometry, intermolecular hydrogen bond, and harmonic vibrational frequencies of the title molecule have been investigated with the help of B3LYP method. The calculated molecular geometry has been compared with the experimental data. The various intramolecular interactions have been exposed by natural bond orbital analysis. The distribution of Mulliken atomic charges and bending of natural hybrid orbitals also reflect the presence of intramolecular hydrogen bonding. The analysis of the electron density of HOMO and LUMO gives an idea of the delocalization and low value of energy gap indicates electron transport in the molecule and thereby bioactivity. Effective docking of the drug molecule with NMDA receptor subunit 3A also enhances its bioactive nature.

Edwin, Bismi; Hubert Joe, I.

2012-11-01

449

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

NASA Astrophysics Data System (ADS)

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

Jo, Janggun; Yang, Xinmai

2011-09-01

450

Spectroscopic analyses on interaction of Naphazoline hydrochloride with bovine serum albumin  

NASA Astrophysics Data System (ADS)

The fluorescence and ultraviolet spectroscopy were explored to study the interaction between Naphazoline hydrochloride (Naphcon) and bovine serum albumin (BSA) at three different temperatures (292, 301, and 310 K) under imitated physiological conditions. The quenching mechanism of BSA by Naphacon was interpreted using the Stern-Volmer mechanism, and a combined quenching (dynamic and static quenching). The binding constants, binding sites and the corresponding thermodynamic parameters (?G, ?H, and ?S) of the interaction system were calculated at different temperatures. According to Frster non-radiation energy transfer theory, the binding distance between BSA and Naphcon was found to be 4.71 nm. Synchronous fluorescence spectroscopy showed the conformation of BSA changed in the presence of Naphacon. In addition, the effect of some common metal ions (Mg2+, Ca2+, Ni2+, Cu2+, and Fe2+) on the binding constant between Naphcon and BSA was examined.

Zhu, Shizhong; Liu, Yang

2012-12-01

451

Report: Simultaneous determination of naphazoline hydrochloride, chlorpheniramine maleate and methylene blue in their ternary mixture.  

PubMed

Validated spectrophotometric and chemometric methods were developed for determination of Naphazoline Hydrochloride (NAP), Chlorpheniramine maleate (CLO) and Methylene blue (MB) in their ternary mixture. Method A was a spectrophotometric method, where NAP and MB were determined using second derivative (D) spectrophoto metric method using the peak amplitudes at 299 nm and 337 nm for NAP and MB respectively , while CLO was determined using second derivative ratio (DD) spectrophotometric method using the peak amplitude at 276.6 nm. Method B used the chemometric techniques; principal component regression (PCR) and partial least squares (PLS) for determination of NAP, CLO and MB using the information contained in the absorption spectra of their ternary mixture solutions. The proposed methods have been successfully applied for the analysis of NAP, CLO and MB in their pharmaceutical formulation and the obtained results were statistically compared with the reported methods. PMID:23625443

Ali, Nouruddin Wageih; Hegazy, Maha Ahmad; Abdelkawy, Mohamad; Abdelfatah, Rehab Magdy

2013-05-01

452

Spectroscopic analyses on interaction of Naphazoline hydrochloride with bovine serum albumin.  

PubMed

The fluorescence and ultraviolet spectroscopy were explored to study the interaction between Naphazoline hydrochloride (Naphcon) and bovine serum albumin (BSA) at three different temperatures (292, 301, and 310 K) under imitated physiological conditions. The quenching mechanism of BSA by Naphacon was interpreted using the Stern-Volmer mechanism, and a combined quenching (dynamic and static quenching). The binding constants, binding sites and the corresponding thermodynamic parameters (?G, ?H, and ?S) of the interaction system were calculated at different temperatures. According to Frster non-radiation energy transfer theory, the binding distance between BSA and Naphcon was found to be 4.71 nm. Synchronous fluorescence spectroscopy showed the conformation of BSA changed in the presence of Naphacon. In addition, the effect of some common metal ions (Mg(2+), Ca(2+), Ni(2+), Cu(2+), and Fe(2+)) on the binding constant between Naphcon and BSA was examined. PMID:22995546

Zhu, Shizhong; Liu, Yang

2012-12-01

453

High pressure study of molecular dynamics of protic ionic liquid lidocaine hydrochloride  

NASA Astrophysics Data System (ADS)

In this paper, we investigate the effect of pressure on the molecular dynamics of protic ionic liquid lidocaine hydrochloride, a commonly used pharmaceutical, by means of dielectric spectroscopy and pressure-temperature-volume methods. We observed that near Tg the pressure dependence of conductivity relaxation times reveals a peculiar behavior, which can be treated as a manifestation of decoupling between ion migration and structural relaxation times. Moreover, we discuss the validity of thermodynamic scaling in lidocaine HCl. We also employed the temperature-volume Avramov model to determine the value of pressure coefficient of glass transition temperature, dTg/dP|P = 0.1. Finally, we investigate the role of thermal and density fluctuations in controlling of molecular dynamics of the examined compound.

Swiety-Pospiech, A.; Wojnarowska, Z.; Pionteck, J.; Pawlus, S.; Grzybowski, A.; Hensel-Bielowka, S.; Grzybowska, K.; Szulc, A.; Paluch, M.

2012-06-01

454

Formulation and Evaluation of Extended-Release Solid Dispersion of Metformin Hydrochloride  

PubMed Central

The purpose of this research was to formulate and characterize solid dispersion (SD) of metformin hydrochloride using methocel K100M as the carrier by the solvent evaporation and cogrinding method. The influence of drug polymer ratio on drug release was studied by dissolution tests. Characterization was performed by fourier transform spectroscopy (FTIR), ultraviolet, differential scanning calorimetry and X-ray powder diffractometry. The optimized formulation was subjected to accelerated stability testing as per ICH guidelines. Release data were examined kinetically. SD with 1:4 and 1:5 ratio of drug to polymer obtained by solvent evaporation and cogrinding were selected as the best candidates suitable for prolonged-release oral dosage form of metformin. PMID:21264113

Patil, SA; Kuchekar, BS; Chabukswar, AR; Jagdale, SC

2010-01-01

455

Simultaneous determination of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate in pharmaceutical preparations using multivariate calibration 1  

NASA Astrophysics Data System (ADS)

Resolution of binary mixtures of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate with minimum sample pre-treatment and without analyte separation has been successfully achieved by methods of partial least squares algorithm with one dependent variable, principal component regression and hybrid linear analysis. Data of analysis were obtained from UV-vis spectra of the above compounds. The method of central composite design was used in the ranges of 1-15 mg L -1 for both calibration and validation sets. The models refinement procedure and their validation were performed by cross-validation. Figures of merit such as selectivity, sensitivity, analytical sensitivity and limit of detection were determined for all three compounds. The procedure was successfully applied to simultaneous determination of the above compounds in pharmaceutical tablets.

Samadi-Maybodi, Abdolraouf; Hassani Nejad-Darzi, Seyed Karim

2010-04-01

456

Metallic-like Wilson ratio in the polyaniline hydrochloride conducting polymer  

NASA Astrophysics Data System (ADS)

We report on the calorimetric and magnetic properties of the polyaniline hydrochloride in order to discuss its metallicity. Both the specific heat and the magnetic susceptibility ? have been investigated as a function of temperature from 300 K down to 2 K. The measurements of the specific heat have allowed us to determine the electronic Sommerfeld coefficient ? and the temperature dependence of the susceptibility has revealed a Pauli-like component. By combining ? and ?, the dimensionless Wilson ratio RW??/? demonstrates that the universal free electrons limit is reached above 100 K as a strong check of the metallicity of this conducting polymer. By removing the Pauli component from the measured susceptibility, the resulting contribution displays below 100 K a well-defined Curie-like component in agreement with a few percents of spins localized by disorder at low temperatures. These results are therefore consistent with an electronic itinerancy, namely, a metallic state even in the presence of disorder.

Limelette, P.; Schmaltz, B.; Brault, D.; Tran Van, F.

2015-03-01

457

Enthalpies of solvation for dopamine hydrochloride in water-ethanol solutions  

NASA Astrophysics Data System (ADS)

The enthalpies of dissolution of dopamine hydrochloride (H2Dop HCl) in water-ethanol solvents containing from 0 to 0.8 mole fraction of ethanol are measured by calorimetry at 298.15 K. Standard enthalpies of transfer (?tr H ?) for the molecular (H2Dop) and cationic (H3Dop+) forms of dopamine from water into binary solvents are calculated from the obtained data. The enthalpies of transfer of H3Dop+ cation are determined from the enthalpies of dissolution of H2Dop HCl using the familiar method of separating the molar quantities into ionic contributions (Ph4P+ = BPh{4/-}), and by an original alternative procedure. The effect of the composition of the binary solvent on the solvation of dopamine is considered.

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

2012-10-01

458

[Clinical significance of cevimeline hydrochloride in the treatment of dry mouth in patients with Sjgren's syndrome].  

PubMed

To evaluate the efficacy and safety of cevimeline hydrochloride for the treatment of dry mouth in patients with Sjgren's syndrome (SS), eight SS patients received 30 mg of cevimeline twice or three times daily for 24 weeks. Six out of the eight patients had improvement in dry mouth. Five patients had more than 20% increase in saliva secretion. In the assessment of salivary gland scintigraphy, three patients showed improvement. There was a significant negative correlation between the improvement of saliva secretion and the severity of tissue damage assessed by MR sialography (r= - 0.754, p<0.05). One patient stopped cevimeline at 4 weeks because of headache and nausea. There was no significant change in laboratory data. Cevimeline is safe and effective medicine for dry mouth in patients with SS, in particular, with less severe salivary gland destruction. PMID:15559322

Ogawa, Noriyoshi; Shimoyama, Kumiko; Karasawa, Hiromi; Fukushima, Toshihiro; Masaki, Yasufumi; Wano, Yuji; Hirose, Yuko; Sugai, Susumu

2004-10-01

459

Biogenic gold nanoparticles as fotillas to fire berberine hydrochloride using folic acid as molecular road map.  

PubMed

Use of biologically modified gold nanoparticles (GNPs) as molecular vehicle to ferry potential anti-cancer drug berberine hydrochloride (BHC) using folic acid (FA) as targeting molecule is reported in this work. A tropical fruit peel, Trapa bispinosa is used to fabricate highly monodispersed GNPs, passivated with essential functional groups which were used as linkers to attach FA and BHC via amide linkage. Flocculation Parameter (FP) of biologically synthesized GNPs was calculated under different salt concentrations which were found to be very ideal under a physiological condition. Various statistical models were used to find drug release profile out of which Higuchi was found to be the most ideal. GNP-FA-BHC complexes were found to be active against folic acid expressing HeLa cells. PMID:23910269

Pandey, Sunil; Mewada, Ashmi; Thakur, Mukeshchand; Shah, Ritu; Oza, Goldie; Sharon, Madhuri

2013-10-01

460

Thiocytosine as a radiation energy trap in a single crystal of cytosine hydrochloride.  

PubMed

Single crystals of cytosine hydrochloride with thiocytosine as an impurity were found suitable for the study of a possible new mechanism of long-range migration of energy deposited by ionizing radiation. In a crystal containing thiocytosine, two kinds of chlorine-containing paramagnetic centres are present that are completely absent in the pure cytosine. HCl crystals irradiated under the same condition. The thiocytosine molecules in conjunction with Cl- ions behave as hole traps. The centres have been characterized by EPR spectroscopy. One of the centres is derived from the cationic thiocytosine radical by interaction with a Cl- ion, and the other centre is formed by interaction of Cl. with a thiocytosine molecule. It is suggested that the transfer of an electron-loss site (a hole) in the Cl- network is the actual mechanism of the long-range energy transfer. PMID:8027610

Herak, J N; Sankovic, K; Htterman, J

1994-07-01

461

Metabolism of roxatidine acetate hydrochloride. Liberation of deuterium from the piperidine ring during hydroxylation  

SciTech Connect

The metabolism of roxatidine acetate hydrochloride (RA), a new histamine-2 receptor antagonist, was studied by GC/MS in rats and dogs in vivo. The co-administration of /sup 14/C-RA and RA-d10 labeled with deuterium in the piperidine ring expedited the isolation and identification of 15 urinary metabolites. The major metabolites in both animals were M-1, M-8, M-10, and M-11; M-4 could be found only in the rat. The aromatic and piperidine ring-hydroxylated metabolites were found in small amounts in both species. Following the administration of RA-d10 to rats and dogs, oxygenated metabolites on the piperidine ring, such as M-3 and M-4, were isolated and their analysis indicated the unexpected loss of three or four deuterium atoms from the ring. Also, first and second isotope effects were observed on the conversion rate in vivo and retention time in HPLC, respectively.

Honma, S.; Iwamura, S.; Kobayashi, R.; Kawabe, Y.; Shibata, K.

1987-07-01

462

Bilayer matrix tablets for prolonged actions of metformin hydrochloride and repaglinide.  

PubMed

A combination therapy of metformin hydrochloride (MH) and repaglinide (RG) achieves a perfect glycemic control; however, the combination formulation of immediate release must be taken several times a day, compromising the therapeutic benefits and causing inconveniences to the patients. Herein, a bilayer matrix tablet that aimed at continuously releasing both MH and RG over time was developed, in which the two drugs were formulated into two separated layers. The tablets were prepared by wet granulation method, and the optimized formulation was obtained by evaluating the factors that affected the drug release. The bilayer tablets simultaneously released the two drugs over 12 h; and a better in vivo performance with a steady plasma concentration, markedly lower C max, prolonged T max, and perfect absorption was obtained. Summarily, the bilayer matrix tablets sustained both MH and RG release over time, thereby prolonging the actions for diabetic therapy and producing better health outcomes. PMID:25319054

He, Wei; Huang, Shijing; Zhou, Chunyan; Cao, Lin; Yao, Jing; Zhou, Jianping; Wang, Guangji; Yin, Lifang

2015-04-01

463

Ultrasonic Studies of 4-Aminobutyric Acid in Aqueous Metformin Hydrochloride Solutions at Different Temperatures  

NASA Astrophysics Data System (ADS)

Ultrasonic speeds and density data of 4-aminobutyric acid in 0.05 M, 0.10 M, and 0.15 M aqueous metformin hydrochloride (MFHCl) solutions are measured at 308.15 K, 313.15 K, and 318.15 K. The isentropic compressibility ( k S ), the change in isentropic compressibility (? k S ), the relative change in isentropic compressibility ({? k_S/k_S^0}), the apparent molal compressibility ({k_?}), the limiting apparent molal compressibility ({k_?^0 }), the transfer limiting apparent molal compressibility ({? k_?^0}), the hydration number ( n H), and the pair and triplet interaction parameters ( k AH, k AHH) are estimated. The above parameters are used to interpret the solute-solute and solute-solvent interactions of 4-aminobutyric acid in aqueous MFHCl solutions.

Rajagopal, K.; Jayabalakrishnan, S. S.

2010-12-01

464

UV-prepared salep-based nanoporous hydrogel for controlled release of tetracycline hydrochloride in colon.  

PubMed

A highly swelling nanoporous hydrogel (NPH) was synthesized via UV-irradiation graft copolymerization of acrylic acid (AA) onto salep backbone and its application as a carrier matrix for colonic delivery of tetracycline hydrochloride (TH) was investigated. Optimized synthesis of the hydrogel was performed by the classic method. The swelling behavior of optimum hydrogel was measured in different media. The hydrogel formation was confirmed by Fourier transform infrared spectroscopy (FTIR) and thermo-gravimetric analysis (TGA/DTG/DTA). The study of the surface morphology of hydrogels using SEM showed a nanoporous (average pore size: about 350nm) structure for the sample obtained under optimized conditions. The drug delivery results demonstrated that this NPH could successfully deliver a drug to the colon without losing the drug in the stomach, and could be a good candidate as an orally administrated drug delivery system. PMID:21251847

Bardajee, Ghasem Rezanejade; Pourjavadi, Ali; Ghavami, Somayeh; Soleyman, Rouhollah; Jafarpour, Farnaz

2011-03-01