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1

Horseradish peroxidase-catalyzed oxidative coupling of 3-methyl 2-benzothiazolinone hydrazone and methoxyphenols  

Microsoft Academic Search

The reaction between o-, m-, and p-methoxyphenols and 3-methyl-2-benzothiazolinone hydrazone (MBTH) is studied in the presence of horseradish peroxidase (HRP) and H2O2 as oxidative agent. The findings indicate that enzyme (H2O2 oxidoreductase; EC 1.11.1.7) catalyzes an oxidative coupling reaction between MBTH and phenols which produces azo dye compounds. On the basis of kinetic parameters and optimum pH values, a mechanism

Leonardo Setti; Sara Scali; Igor Degli Angeli; Pier Giorgio Pifferi

1998-01-01

2

Laccase catalyzed-oxidative coupling of 3-methyl 2-benzothiazolinone hydrazone and methoxyphenols  

Microsoft Academic Search

The reaction between o-, m-, and p-methoxyphenols and 3-methyl-2-benzothiazolinone hydrazone was studied in the presence of laccase from Pyricularia oryzae. The findings show that laccase (benzenediol:oxygen oxidoreductase, EC 1.10.3.2) catalyzes the oxidative coupling reaction between MBTH and phenols producing red colored azo-dye compounds. On the basis of kinetic parameters and optimum pH values, the mechanisms of the oxidative coupling reactions

Leonardo Setti; Silvia Giuliani; Giovanni Spinozzi; Pier Giorgio Pifferi

1999-01-01

3

Photometric assay of methanol and formaldehyde in industrial waste-waters using alcohol oxidase and 3-methyl-2-benzothiazolinone hydrazone  

Microsoft Academic Search

An enzymo-chemical method using alcohol oxidase (AO) and 3-methyl-2-benzothiazolinone hydrazone (MBTH) for the simultaneous analysis of methanol and formaldehyde in mixtures, including industrial waste-waters, is described. The enzyme oxidizes methanol to formaldehyde, while MBTH plays a double role: (1) in the first step of the reaction, it forms a colourless azine adduct with pre-existing and enzymatically formed formaldehyde and prevents

Vladimir A. Sibirny; Mykhailo V. Gonchar; Dorota Grabek-Lejko; Halyna M. Pavlishko; Elisabeth Csöregi; Andriy A. Sibirny

2008-01-01

4

Immobilization of tyrosinase in chitosan film for an optical detection of phenol  

Microsoft Academic Search

An optical biosensor based on the immobilized tyrosinase enzyme in a chitosan film is described for the detection of phenol. The film was prepared by depositing a chitosan solution containing tyrosinase onto a microscope glass slide via spin coating technique. The quinone produced from the enzymatic oxidation of phenol was reacted with 3-methyl-2-benzothiazolinone hydrazone (MBTH) to produce a maroon color

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

2006-01-01

5

A Continuous Spectrophotometric Method for Determining the Monophenolase and Diphenolase Activities of Apple Polyphenol Oxidase  

Microsoft Academic Search

A continuous spectrophotometric method for the determination of the monophenolase and diphenolase activities of apple polyphenol oxidase is described. The method is based on the coupling reaction between 3-methyl-2-benzothiazolinone hydrazone (MBTH) and the quinone product of the oxidation of p-hydroxyphenyl propionic acid and 3,4-dihydroxyphenyl propionic acid in the presence of polyphenol oxidase. The ?max and the molar absorptivity (?) for

J. C. Espin; M. Morales; R. Varon; J. Tudela; F. Garciacanovas

1995-01-01

6

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

Microsoft Academic Search

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

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

2007-01-01

7

Chitosan-based tyrosinase optical phenol biosensor employing hybrid nafion\\/sol–gel silicate for MBTH immobilization  

Microsoft Academic Search

The development of an optical biosensor based on immobilization of 3-methyl-2-benzothiazolinone hydrazone (MBTH) in hybrid nafion\\/sol–gel silicate film and tyrosinase in chitosan film for the detection of phenolic compounds has been described. Tyrosinase was immobilized in chitosan film deposited on the hybrid nafion\\/sol–gel silicate film containing MBTH. The enzymatic oxidation product of phenolic compounds were stabilized through formation of adduct

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

2006-01-01

8

Stacked films immobilization of MBTH in nafion\\/sol-gel silicate and horseradish peroxidase in chitosan for the determination of phenolic compounds  

Microsoft Academic Search

The stacked-film immobilization of 3-methyl-2-benzothiazolinone hydrazone (MBTH) in hybrid nafion\\/sol-gel silicate film and\\u000a horseradish peroxidase (HRP) in chitosan, performed in order to allow the determination of phenolic compounds, was investigated\\u000a via an optical method. The stacked films were deposited onto a microscope glass slide by a spin-coating technique. The quinone\\u000a or free radical product formed by the enzymatic reactions of

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

2006-01-01

9

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 0.89×10(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

10

Therapeutic Potential of Hydrazones as Anti-Inflammatory Agents  

PubMed Central

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

Bala, Suman; Sharma, Neha; Saini, Vipin

2014-01-01

11

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

12

Lucanthone hydrochloride  

PubMed Central

This review of the published work on the treatment of bilharziasis with lucanthone hydrochloride draws attention to the inconclusive nature of many of the trials carried out so far: either the dosage was inadequate or the patients were not followed up for a sufficient length of time. The author stresses the importance of obtaining a high concentration of lucanthone in the body fluids. He suggests that better results might be obtained if the total dose were given in two days or even as a single, massive dose. This method might also reduce the side effects, which do not appear, as a rule, until the second or third day. PMID:13573122

Blair, D. M.

1958-01-01

13

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

Espín, J C; Tudela, J; García-Cánovas, F

1998-05-15

14

Amitriptyline hydrochloride overdose  

MedlinePLUS

Amitriptyline hydrochloride is a type of prescription medicine called a tricyclic antidepressant. Amitriptyline hydrochloride overdose occurs when someone accidentally or intentionally takes more than the normal or recommended amount of this medication. ...

15

Desipramine hydrochloride overdose  

MedlinePLUS

Desipramine hydrochloride is a type of medicine called a tricyclic antidepressant. Desipramine hydrochloride overdose occurs when someone accidentally or intentionally takes more than the normal or recommended amount of this medication. ...

16

Importance of ortho Proton Donors in Catalysis of Hydrazone Formation  

PubMed Central

Anthranilic acids were recently reported as superior catalysts for hydrazone and oxime formation compared to aniline, the classic catalyst for these reactions. Here, alternative proton donors were examined with varied pKa in an effort to enhance activity at biological pH. The experiments show that 2-aminobenzenephosphonic acids are superior to anthranilic acids in catalyzing hydrazone formation with common aldehyde substrates. PMID:23477719

Crisalli, Pete

2013-01-01

17

[Phytotoxicity of hydrazones of aromatic aldehydes].  

PubMed

A series of hydrazones of aromatic aldehydes (B) was prepared and tested for phytotoxicity. These compounds are bioisosters of 1-aryltriazenes (A) which were found to possess interesting phytotoxic properties in a previous research. The substances studied (Tables I leads to III: compounds(I leads to CLXXX)) some of which were previously unrecorded, were prepared by the usual procedures from the required aldehyde and hydrazine derivative. The phytotoxicity of all the compounds was studied using seven representative species in both pre- and post-emergence tests at a dose of 6 kg/ha. It was found that this class of compounds shows phytotoxicity by absorption through the foliage with specificity for Amaranthus retroflexus L. The only exceptions are compounds where the aryl residue is 2,6-dichlorophenyl; these compounds show wide spectrum of phytotoxicity by absorption through the leaves. PMID:1269737

Mazza, M; Montanari, L; Pavanetto, F

1976-05-01

18

Characterization of monophenolase activity of polyphenol oxidase from iceberg lettuce.  

PubMed

Polyphenol oxidase (EC 1.14.18.1), a thylakoid membrane-bound enzyme, was isolated by sonication of osmotically shocked chloroplasts from iceberg lettuce (Lactuca sativa). The enzyme showed monophenolase activity when assayed on (p-hydroxyphenyl)propionic acid with 3-methyl-2-benzothiazolinone hydrazone in a reliable continuous spectrophotometric method, with high sensitivity, accuracy, and precision. The monophenolase activity showed a lag period before the steady-state rate (V(ss)) was reached. Both kinetic parameters, the lag period and the steady-state rate, depended on the pH, the enzyme and substrate concentrations, and the presence of catalytic amounts of o-diphenol. This activity shows inhibition by high substrate concentration. The experimental results correspond with the mechanism previously described for PPO from other sources. Kinetic constants K(m), V(max), and K(i) were determined. PMID:10563992

Chazarra, S; García-Carmona, F; Cabanes, J

1999-04-01

19

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

Code of Federal Regulations, 2011 CFR

...2011-04-01 2011-04-01 false Ketamine hydrochloride with promazine hydrochloride...FORM NEW ANIMAL DRUGS § 522.1222b Ketamine hydrochloride with promazine hydrochloride...injection. (a) Chemical name. Ketamine hydrochloride,...

2011-04-01

20

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

21

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

Code of Federal Regulations, 2013 CFR

...2013-04-01 2013-04-01 false Ketamine hydrochloride with promazine hydrochloride...FORM NEW ANIMAL DRUGS § 522.1222b Ketamine hydrochloride with promazine hydrochloride...injection. (a) Chemical name. Ketamine hydrochloride,...

2013-04-01

22

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

Code of Federal Regulations, 2012 CFR

...2012-04-01 2012-04-01 false Ketamine hydrochloride with promazine hydrochloride...FORM NEW ANIMAL DRUGS § 522.1222b Ketamine hydrochloride with promazine hydrochloride...injection. (a) Chemical name. Ketamine hydrochloride,...

2012-04-01

23

Synthesis and anticancer activity of (E)-2-benzothiazole hydrazones.  

PubMed

Benzothiazole hydrazones have been synthesized and evaluated for their in vitro antiproliferative activity against three human cancer cell lines: HL-60 (leukemia), MDAMB-435 (breast) and HCT-8 (colon). The good cytotoxicity for the three cancer cell lines and theoretical profile of compounds 3o and 3p pointed them as promising lead molecules for anticancer drug design. PMID:25147145

Lindgren, Eric B; de Brito, Monique A; Vasconcelos, Thatyana R A; de Moraes, Manuel O; Montenegro, Raquel C; Yoneda, Julliane D; Leal, Kátia Z

2014-10-30

24

The olefinic aldol reaction. Addition of zincated hydrazone to vinylsilane  

Microsoft Academic Search

A zincated N,N-dimethylhydrazone of a ketone bearing a BuZn(II) countercation undergoes intermolecular addition to a vinysilane to afford the hydrazone of a 2-(2-silylethyl)ketone in good yield, providing a new synthetic route to functionalized carbonyl compounds.

Eiichi Nakamura; Katsumi Kubota

1997-01-01

25

Water-soluble organocatalysts for hydrazone and oxime formation.  

PubMed

The formation of oximes and hydrazones is widely used in chemistry and biology as a molecular conjugation strategy for achieving ligation, attachment, and bioconjugation. However, the relatively slow rate of reaction has hindered its utility. Here, we report that simple, commercially available anthranilic acids and aminobenzoic acids act as superior catalysts for hydrazone and oxime formation, speeding the reaction considerably over the traditional aniline-catalyzed reaction at neutral pH. This efficient nucleophilic catalysis, involving catalyst-imine intermediates, allows rapid hydrazone/oxime formation even with relatively low concentrations of the two reactants. The most efficient catalysts are found to be 5-methoxyanthranilic acid and 3,5-diaminobenzoic acid; we find that they can enhance rates by factors of as much as 1-2 orders of magnitude over the aniline-catalyzed reaction. Evidence based on a range of differently substituted arylamines suggests that the ortho-carboxylate group in the anthranilate catalysts serves to aid in intramolecular proton transfer during imine and hydrazone formation. PMID:23289546

Crisalli, Pete; Kool, Eric T

2013-02-01

26

Water-soluble Organocatalysts for Hydrazone and Oxime Formation  

PubMed Central

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

Crisalli, Pete; Kool, Eric T.

2013-01-01

27

21 CFR 582.5676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2014 CFR

... ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 § 582.5676 Pyridoxine hydrochloride. (a) Product. Pyridoxine hydrochloride. (b)...

2014-04-01

28

21 CFR 582.5676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2012 CFR

... ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 § 582.5676 Pyridoxine hydrochloride. (a) Product. Pyridoxine hydrochloride. (b)...

2012-04-01

29

[In vitro synergisms among hydrazones, ajoeno and posaconazole against Cryptococcus spp].  

PubMed

The aim of this study was to assess the in vitro susceptibility to novel antifungal compounds, the steroidal hydrazones, and to compare their antifungal activity and synergistic effects with other compounds, such as ajoeno and posaconazole on Cryptocococus spp isolates. Three Cryptococcus strains were used for this study (42794, 4050 and 44192) and their antifungal sensitivity and synergistic effects with ajoeno and posaconazole were evaluated according to the CLSI protocol number M27-A2. Candida albicans (ATCC 90028) and Candida parapsilosis (ATCC 22019) were used as controls. A plateau effect with hydrazones (H1, H2, H3, H4) was observed after 10 microM (CMI). However, with H4 only a mild inhibition on the growth was obtained. Combining hydrazone and ajoeno, CMI values between 25 and 50 microM were obtained. The highest inhibitions values were obtained with posaconazole and a CMI value of 6 microM for the strains 42794 and 44192, and a CMI value of 20 microM for the strain 4050. Synergy was observed combining posaconazole with ajoeno, ajoeno with hydrazone 3 and posaconazole with hydrazone 3. Fractional inhibitory concentrations were 0.24, 0.16 and 0.09 respectively, which might indicate a synergistic effect. Important synergistic effects were obtained with posaconazole and ajoeno, ajoeno and hydrazone 3 and posaconazole with hydrazone 3, which would be very useful for clinical trials in the future. PMID:22523841

Vivas, Julio; Alvarado, Primavera; Visbal, Gonzalo; Alvarez-Aular, Alvaro; Ruiz, Egle; Ledezma, Eliades

2011-12-01

30

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

31

Physical and Chemical Stability of Palonosetron Hydrochloride with Topotecan Hydrochloride and Irinotecan Hydrochloride During Simulated Y-Site Administration.  

PubMed

The objective of this study was to evaluate the physical and chemical stabilty of undiluted palonosetron hydrochloride 50 micrograms/mL in combination with topotecan hydrochloride 0.1 mg/mL or irinotecan hydrochloride 1 mg/mL in 5% dextrose injection during simulated Y-site administration. Triplicate test samples were prepared by admixing 5 mL of palonosetron hydrochloride with 5 mL of the topotecan hydrochloride or irinotecan hydrochloride admixture. Physical stabilty was assessed by using a multistep evaluation preocdure that included both turbidimetric and particulate measurement as well as visual inspection. Chemical stability was assessed by using stability-indicating high-performance liquid chromatographic analytical techniques to determine drug concentrations. Evaluations were performed initially upon mixing and again 1 and 4 hour after mixing. The palonosetron hydrochloride-topotecan hydrochloride samples were clear and pale yellow when viewed in normal fluorescent room light. When viewed with a Tyndall beam, the samples had a slight haziness. The palonosetron hydrochloride-irinotecan hydrochloride samples were clear and colorless when viewed in in normal fluorescent room light and with a Tyndall beam. Measured turbidities remained unchanged; particulate contents were low and changed little. High-performance liquid chromatographic analysis found that palonosetron hydrochloride, topotecan hydrochloride, and irinotecan hydrochloride remained stable throughout the 4-hour test. Little drug loss was observed. Palonosetron hydrochloride is physically compatible and chemically stable with topotecan hydrochloride and with irinotecan hydrochloride during Y-site administration. PMID:23924983

Trissel, Lawrence A; Xu, Quanyun A

2005-01-01

32

Pyridinyl hydrazone derivatives of thiacalix[4]arene as selective extractants of transition metal ions  

Microsoft Academic Search

The recognition ability of pyridinyl hydrazone derivatives of cone- and 1,3-alternate tetrathiacalix[4]arenes towards transition and alkali metals has been investigated by picrate extraction method. The stoichiometry\\u000a of complexes and the extraction constants have been determined. It has been found that hydrazones do not extract alkali metal\\u000a ions but show an excellent affinity towards transition and heavy metal cations. The removal

Sergey N. PodyachevNadezda; Nadezda E. Burmakina; Victor V. Syakaev; Svetlana N. Sudakova; Wolf D. Habicher; Alexander I. Konovalov

33

Group X aldehyde dehydrogenases of Pseudomonas aeruginosa PAO1 degrade hydrazones.  

PubMed

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; Takaya, Naoki

2012-03-01

34

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

35

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

36

21 CFR 520.2002 - Propiopromazine hydrochloride.  

Code of Federal Regulations, 2010 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...

2010-04-01

37

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

38

21 CFR 520.2002 - Propiopromazine hydrochloride.  

Code of Federal Regulations, 2011 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...

2011-04-01

39

Radical additions to chiral hydrazones: stereoselectivity and functional group compatibility.  

PubMed

Free radical additions to imino compounds offer increased synthetic accessibility of chiral amines, but lack of general methods for stereocontrol has hindered their development. This review focuses on two asymmetric amine synthesis strategies designed to address this problem, with emphasis on addition of functionalized radicals which may facilitate applications to synthesis of complex targets. First, chiral N-acylhydrazones are acceptors for intermolecular radical additions of a wide range of primary, secondary, and tertiary alkyl halides to the C=N bond, with radicals generated under manganese-, tin-, or boron-mediated conditions. A variety of aldehydes and ketones serve as viable precursors for the chiral hydrazones, and the highly stereoselective reactions tolerate electrophilic functionality in both coupling components. Second, radical precursors may be linked to chiral ?-hydroxyhydrazones via a silicon tether to the hydroxyl group; conformational constraints impart stereocontrol during 5-exo radical cyclization under stannyl- or thiyl-mediated conditions. The silicon tether may later be removed to reveal the formal adducts of hydroxymethyl, vinyl, acetyl, and 2-oxoethyl radicals to the C=N bond. Methodology development and applications to biologically important targets are discussed. PMID:21842359

Friestad, Gregory K

2012-01-01

40

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

NASA Astrophysics Data System (ADS)

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

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

2012-09-01

41

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

42

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

43

Linear copper 'chain' complexes with bulky tritopic hydrazone ligands--structural and magnetic studies.  

PubMed

Tritopic 2,6-picolyl-bis-hydrazone ligands with bulky terminal groups derived from phenyl-pyridyl ketone do not form the expected [3 x 3] grids on reaction with copper(II), but instead form Cu8 'pinwheels', and in the present case linear trinuclear, pentanuclear and chain structures also. Direct bridging between copper ions occurs through micro2-N-N diazine groups, and longer O-C-N hydrazone connections, leading to moderately strong antiferromagnetic exchange between adjacent metal centres. Structural and magnetic properties are discussed in the context of specific orthogonal and non-orthogonal bridges, which can be distinguished and quantified. PMID:17702175

Tandon, Santokh S; Dawe, Louise N; Milway, Victoria A; Collins, Julie L; Thompson, Laurence K

2007-05-21

44

Hydrazone radical promoted vicinal difunctionalization of alkenes and trifunctionalization of allyls: synthesis of pyrazolines and tetrahydropyridazines.  

PubMed

The intramolecular addition of hydrazone radicals to carbon-carbon double bonds was achieved by using TEMPO (2,2,6,6-tetramethyl-1-piperidinyloxy) or DIAD (diisopropyl azodicarboxylate) as the hydrazone radical initiator as well as the carbon radical scavenger. Consequently, alkenes were difunctionalized to afford pyrazolines and tetrahydropyridazines via C-N forming 5-exo-trig and 6-exo-trig cyclizations, respectively, and allyls were trifunctionalized to afford pyrazolines via C-N forming tandem 1,5-H-shift/5-exo-trig cyclizations under metal-free neutral conditions. PMID:24063683

Duan, Xiao-Yong; Yang, Xiu-Long; Fang, Ran; Peng, Xie-Xue; Yu, Wei; Han, Bing

2013-11-01

45

Synthesis and antifungal activity of substituted salicylaldehyde hydrazones, hydrazides and sulfohydrazides.  

PubMed

Efficient synthetic procedures for the preparation of acid hydrazines and hydrazides were developed by converting the corresponding carboxylic acid into the methyl ester catalyzed by Amberlyst-15, followed by a reaction with hydrazine monohydrate. Sulfohydrazides were prepared from the corresponding sulfonyl chlorides and hydrazine monohydrate. Both of these group of compounds were condensed with substituted salicylaldehydes using gradient concentration methods that generated a large library of hydrazone, hydrazide and sulfohydrazide analogs. Antifungal activity of the prepared analogs showed that salicylaldehyde hydrazones and hydrazides are potent inhibitors of fungal growth with little to no mammalian cell toxicity, making these analogs promising new targets for future therapeutic development. PMID:25127462

Backes, Gregory L; Neumann, Donna M; Jursic, Branko S

2014-09-01

46

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

PubMed Central

A series of ?-diketone hydrazone derivatives have been synthesized through condensation of ?-diketone with aromatic aldehydes followed by reaction with phenylhydrazine. The structure of the ligands and intermediates are well defined through elemental and spectroscopic analyses. These hydrazones are potential ligands toward lanthanide metal ions. New complexes of trivalent Scandium, Yttrium, Lanthanum, and Cerium have been synthesized. The composition of these complexes is discussed on the basis of elemental analyses, IR, magnetic moments, and thermal analyses. The prepared complexes were screened for antibacterial and antifungal properties and have exhibited potential activity. PMID:21799665

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

2011-01-01

47

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

PubMed

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

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

2009-01-01

48

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

49

Prevention of postasphyxia electroretinal dysfunction with a pyridoxal hydrazone.  

PubMed

The newborn retina is particularly sensitive and frequently subjected to peroxidative stresses that result in visual sequelae. We compared two iron chelators, deferoxamine and a newer compound, pyridoxal isonicotinoyl hydrazone (PIH), in protecting the retina of newborn pigs (1-3 d old) from asphyxia-reoxygenation insults. Animals were treated IV with either saline, deferoxamine 15.2 mumol/kg (10 mg/kg) or PIH 34.8 mumol/kg (10 mg/kg); n = 10 in each treatment group. Scotopic and photopic electroretinograms (ERG) were recorded before and 40 min after drug treatment as well as 45 min following a 5-min period of asphyxia by interrupting ventilation. In separate animals the indices of peroxidation, malondialdehyde (MDA: TBARS) and hydroperoxides, were measured in retina at the same times. In saline-treated animals, there was a marked increase in MDA and hydroperoxide concentrations in the retina following the asphyxia-reoxygenation period. This was associated with a decrease in the a- (photoreceptor generated) and b-wave (generated by Müller and bipolar cells) amplitudes measured under photopic (cone-mediated response) and scotopic (rod-mediated response) conditions, and an increase in their implicit times. PIH and deferoxamine prevented the postasphyxial increase in MDA and hydroperoxides. However, only PIH prevented the postasphyxial changes in a- and b-wave amplitudes and implicit times, whereas deferoxamine markedly altered the preasphyxial ERG and provided only partial postasphyxial protection simply to the retinal outer segment. Our findings indicate that the iron chelator PIH effectively inhibits peroxidation and retinal electrophysiological alterations secondary to asphyxia-reoxygenation-induced oxidative stresses to newborn animals, whereas deferoxamine adversely affects retinal function; hence, PIH may be a preferred alternative to deferoxamine. PMID:8958125

Bhattacharya, M; Ponka, P; Hardy, P; Hanna, N; Varma, D R; Lachapelle, P; Chemtob, S

1997-01-01

50

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

PubMed Central

Reversible covalent conjugation chemistries that allow site- and condition-specific coupling and uncoupling reactions are attractive components in nanotechnologies, bioconjugation methods, imaging and drug delivery systems. Here, we compare three heterobifunctional crosslinkers, containing both thiol- and amine- reactive chemistry, to form pH-labile hydrazones with hydrazide derivatives of the known and often published water-soluble polymer, poly[N-(2-hydroxypropyl methacrylamide)] (pHPMA), while subsequently coupling thiol-containing molecules to the crosslinker via maleimide addition. Two novel crosslinkers were prepared from the popular heterobifunctional crosslinking agent, succinimidyl-4-(N-maleimidomethyl) cyclohexane-1-carboxylate (SMCC), modified to contain either terminal aldehyde groups (i.e., 1-(N-3-propanal)-4-(N-maleimidomethyl) cyclohexane carboxamide, PMCA) or methylketone groups (i.e., 1-(N-3-butanone)-4-(N-maleimidomethyl) cyclohexane carboxamide, BMCA). A third crosslinking agent was the commercially available N-4-acetylphenyl maleimide (APM). PMCA and BMCA exhibited excellent reactivity towards hydrazide-derivatized pHPMA with essentially complete hydrazone conjugation to polymer reactive sites, while APM coupled only ~ 60% of available reactive sites on the polymer despite a 3-fold molar excess relative to polymer hydrazide groups. All polymer hydrazone conjugates bearing these bifunctional agents were then further reacted with thiol-modified tetramethylrhodamine dye, confirming crosslinker maleimide reactivity after initial hydrazone polymer conjugation. Incubation of dye-labeled polymer conjugates in phosphate buffered saline at 37°C showed that hydrazone coupling resulting from APM exhibited the greatest difference in stability between pH 7.4 and 5.0, with hydrolysis and dye release increased at pH 5.0 over a 24hr incubation period. Polymer conjugates bearing hydrazones formed from crosslinker BMCA exhibited intermediate stability with hydrolysis much greater at pH 5.0 at early time points, but hydrolysis at pH 7.4 was significant after 5 hrs. Hydrazones formed with the PMCA crosslinker showed no difference in release rates at pH 7.4 and 5.0. PMID:20695431

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

2010-01-01

51

Synthesis, characterization and crystal structures of the organotin(IV) compounds with the Schiff base ligands of pyruvic acid thiophene-2-carboxylic hydrazone and salicylaldehyde thiophene-2-carboxylic hydrazone  

Microsoft Academic Search

A series of organotin (IV) compounds of the type [R3SnL]2, R is Me (1), Bu (2), [R2SnL]2, R is Ph (3), Me (4), Bu (5), L is pyruvic acid thiophene-2-carboxylic hydrazone, and R2SnL, R is Me (6), Bu (7), Ph (8), L is salicylaldehyde thiophene-2-carboxylic hydrazone have been synthesized in 1:1 molar ratio. All compounds were characterized by elemental analysis,

Han Dong Yin; Shao Wen Chen; Lin Wei Li; Da Qi Wang

2007-01-01

52

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

53

The use of a versatile o-vanilloyl hydrazone ligand to prepare SMM-like Dy3 molecular cluster pair.  

PubMed

A novel lanthanide molecular cluster pair (MCP), displaying single molecule magnet behaviour, was assembled using the novel o-vanilloyl hydrazone ligand, versatile in terms of denticity, tautomerism and the rotatable C-C bond. PMID:22842673

Xue, Shufang; Zhao, Lang; Guo, Yun-Nan; Zhang, Peng; Tang, Jinkui

2012-09-14

54

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

Microsoft Academic Search

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

L. H. Herbst; C. Packer

55

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

PubMed Central

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

2011-01-01

56

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

Bureš, Jan; Jansová, Hana; Stariat, Ján; Filipský, Tomáš; Mlad?nka, P?emysl; Šim?nek, Tomáš; Ku?era, Radim; Klimeš, Ji?í; Wang, Qin; Franz, Katherine J; Kova?íková, Petra

2015-02-01

57

Flow injection analysis of lactose using covalently immobilized beta-galactosidase, mutarotase, and glucose oxidase/peroxidase on a 2-fluoro-1-methylpyridinium salt-activated Fractogel support.  

PubMed

Milk samples were analyzed for their lactose content using flow injection analysis and incorporating immobilized beta-galactosidase or beta-galactosidase/mutarotase and glucose oxidase/peroxidase bioreactors. These enzymes were immobilized, under mild conditions, on to a 2-fluoro-1-methylpyridinium salt-activated Fractogel support. The use of a phosphate buffer (0.15 M) was found to facilitate the rapid mutarotation of alpha-D-glucose and hence could obviate the need for the more expensive mutarotase. The chromogenic agents of choice for monitoring the reaction were 3-methyl-2-benzothiazolinone hydrazone and 3-dimethylaminobenzoic acid. Linearity was observed over the concentration range 16-160 micrograms/ml using lactose standards (r = 0.996). Between 30 and 40 milk samples/h can be analyzed. Comparisons are made with existing HPLC and alkaline methylamine methods for a range of milk matrices. The FIA method consistently gives the lowest standard deviations and coefficient of variation for the various milk matrices analyzed. PMID:1907811

Narinesingh, D; Stoute, V A; Davis, G; Ngo, T T

1991-04-01

58

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

59

Stacked films immobilization of MBTH in nafion/sol-gel silicate and horseradish peroxidase in chitosan for the determination of phenolic compounds.  

PubMed

The stacked-film immobilization of 3-methyl-2-benzothiazolinone hydrazone (MBTH) in hybrid nafion/sol-gel silicate film and horseradish peroxidase (HRP) in chitosan, performed in order to allow the determination of phenolic compounds, was investigated via an optical method. The stacked films were deposited onto a microscope glass slide by a spin-coating technique. The quinone or free radical product formed by the enzymatic reactions of phenolic compounds interacts with MBTH to form azo-dye products, which can be measured spectrophotometrically at a wavelength of 500 nm. The color intensity of the product was found to increase in proportion to the phenolic concentration after 5 min of exposure. The response of the biosensor was linear over concentration ranges of 0.025-0.500, 0.010-0.070 and 0.050-0.300 mM for guaiacol, resorcinol and o-cresol, respectively, and gave detection limits of 0.010, 0.005 and 0.012 mM. The sensor exhibited good sensitivity and stability for at least two months. PMID:17031625

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

2006-11-01

60

Chitosan-based tyrosinase optical phenol biosensor employing hybrid nafion/sol-gel silicate for MBTH immobilization.  

PubMed

The development of an optical biosensor based on immobilization of 3-methyl-2-benzothiazolinone hydrazone (MBTH) in hybrid nafion/sol-gel silicate film and tyrosinase in chitosan film for the detection of phenolic compounds has been described. Tyrosinase was immobilized in chitosan film deposited on the hybrid nafion/sol-gel silicate film containing MBTH. The enzymatic oxidation product of phenolic compounds were stabilized through formation of adduct with MBTH to produce a maroon color adduct. The color intensity of adduct was found to increase proportionally with the increase of the substrate concentrations after 5min exposure. The linearity of the biosensor towards phenol, catechol and m-cresol were in the respective concentration range of 0.5-7.0, 0.5-10.0 and 1.0-13.0mg/L with detection limit of 0.18, 0.23 and 0.43mg/L, respectively. The biosensor shows a good stability for at least 3 months. PMID:18970803

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

2006-10-15

61

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

62

Copper(II) and zinc(II) complexes with 2-formylpyridine-derived hydrazones  

Microsoft Academic Search

In the present work 2-formylpyridine-para-chloro-phenyl hydrazone (H2FopClPh) and 2-formylpyridine-para-nitro-phenyl hydrazone (H2FopNO2Ph) were obtained, as well as their copper(II) and zinc(II) complexes [Cu(H2FopClPh)Cl2] (1), [Cu(2FopNO2Ph)Cl] (2), [Zn(H2FopClPh)Cl2] (3) and [Zn(H2FopNO2Ph)Cl2] (4). Upon re-crystallization in DMSO:acetone conversion of 2 into [Cu(2FopNO2Ph)Cl(DMSO)] (2a) and of 4 into [Zn(2FopNO2Ph)Cl(DMSO)] (4a) occurred. The crystal structures of 1, 2a, 3 and 4a were determined.

Angel A. Recio Despaigne; Jeferson G. da Silva; Ana Cerúlia M. do Carmo; Flavio Sives; Oscar E. Piro; Eduardo E. Castellano; Heloisa Beraldo

2009-01-01

63

Spectroscopic and PM5 semiempirical studies of new hydrazone of gossypol with 3,6-dioxaheptylhydrazine  

NASA Astrophysics Data System (ADS)

A new hydrazone of gossypol with 3,6-dioxaheptylhydrazine (GHDO) has been synthesised and its structure has been studied by FT-IR, 1H NMR, 13C NMR as well as PM5 semiempirical methods. All the studies have provided clear evidence of the existence of GHDO in the solution in the N-imine- N-imine tautomeric form. The structure and the spectroscopic behaviour of this tautomer are discussed in details. It is shown the structure of GHDO is strongly stabilised by different types of intramolecular hydrogen bonds. In two of them the oxygen atoms of the oxaalkyl chains are also engaged. The strongest intramolecular hydrogen bond is formed between the O 7H proton and N 16 atom from the hydrazone group.

Bejcar, Grzegorz; Przybylski, Piotr; Fusiara, Joanna; Brzezinski, Bogumil; Bartl, Franz

2005-11-01

64

Design, synthesis and pharmacophoric model building of novel substituted nicotinic acid hydrazones with potential antiproliferative activity.  

PubMed

Novel 6-aryl-2-methylnicotinic acid hydrazides 4a-c and their corresponding hydrazones 5a-c and 6a-i were synthesized. X-ray single crystal diffraction of 6h confirmed the chemical structure of hydrazones 6a-i. Antiproliferative activity of the synthetic compounds was investigated against K562 leukemia cell lines. Variable cell growth inhibitory activities were obtained with IC?? range from 24.99 to 66.78 ?M where the compound 6c exhibited the maximum activity. Structure activity relationship analysis has been performed and a common pharmacophore model for the synthesized derivatives has been obtained by using the pharmacophore elucidation module of the software MOE. The best model obtained is characterized by two projected locations of potential H-bond donors (F 3 and F4) and two Aromatic annotations (F1 and F2). PMID:23054710

Abdel-Aziz, Hatem A; Aboul-Fadl, Tarek; Al-Obaid, Abdul-Rahman M; Ghazzali, Mohamed; Al-Dhfyan, Abdullah; Contini, Alessandro

2012-09-01

65

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

NASA Astrophysics Data System (ADS)

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

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

2014-07-01

66

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

NASA Astrophysics Data System (ADS)

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

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

2012-01-01

67

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

PubMed Central

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

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

2011-01-01

68

The conformation and dynamic behaviour of tetrathiacalix[4]arenes functionalized by hydrazide and hydrazone groups  

NASA Astrophysics Data System (ADS)

The 1H, 13C and 15N NMR data, conformation and dynamic behaviour of the new tetrathiacalix[4]arenes functionalized by hydrazide and hydrazone groups are reported and compared with the result of earlier investigations of 4- tert-butylphenoxyacetylhydrazones. The unusual fact of formation of N, N'-diacetylhydrazine bridge and factors leading to its formation in the cone conformer of calixarene has been discussed. The barriers of rotation of hydrazone fragments of tetrathiacalix[4]arenes were determined by NMR-measurements at various temperatures. The structure of 1,3- alternate conformer of 5,11,17,23-tetra- tert-butyl-25,26,27,28-tetrakis[hydrazinocarbonylmethyl]-2,8,14,20-tetrathiacalix[4]arene in solution is compared with crystal structure obtained by the X-ray analysis.

Syakaev, Victor V.; Podyachev, Sergey N.; Gubaidullin, Aidar T.; Sudakova, Svetlana N.; Konovalov, Alexander I.

2008-08-01

69

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

70

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

Microsoft Academic Search

A macrocyclic hydrazone Schiff base was synthesized by reacting 1,4-dicarbonyl phenyl dihydrazide with 2,6-diformyl-4-methyl phenol and a series of metal complexes with this new Schiff base were synthesized by reaction with Co(II), Ni(II) and Cu(II) metal salts. The Schiff base and its complexes have been characterized by elemental analyses, IR, 1H NMR, UV–vis, FAB mass, ESR spectra, fluorescence, thermal, magnetic

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

2009-01-01

71

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

72

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

NASA Astrophysics Data System (ADS)

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

Anbazhagan, R.; Sankaran, K. R.

2015-01-01

73

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

PubMed

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

Manikandan, R; Viswanathamurthi, P; Muthukumar, M

2011-12-01

74

Thermoanalytical Investigation of Terazosin Hydrochloride  

PubMed Central

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

Attia, Ali Kamal; Mohamed Abdel-Moety, Mona

2013-01-01

75

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

76

Acute Psychotic Symptoms due to Benzydamine Hydrochloride Abuse with Alcohol  

PubMed Central

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

Acar, Yahya Ayhan; Kalkan, Mustafa; Çetin, R?dvan; Çevik, Erdem; Ç?nar, Orhan

2014-01-01

77

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

PubMed

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

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

1994-07-01

78

Spectrophotometric method for analysis of metformin hydrochloride.  

PubMed

A simple and sensitive spectrophotometric method has been developed and validated for the estimation of metformin hydrochloride in bulk and in tablet formulation. The primary amino group of metformin hydrochloride reacts with ninhydrin in alkaline medium to form a violet colour chromogen, which is determined spectrophotometrically at 570 nm. It obeyed Beer's law in the range of 8-18 mug/ml. Percentage recovery of the drug for the proposed method ranged from 97-100% indicating no interference of the tablet excipients. The proposed method was found to be accurate and precise for routine estimation of metformin hydrochloride in bulk and from tablet dosage forms. PMID:20177473

Mubeen, G; Noor, Khalikha

2009-01-01

79

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

PubMed

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

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

2013-01-01

80

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

81

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

82

Hydration and dehydration kinetics of xylazine hydrochloride.  

PubMed

From the experiments where mixture of xylazine hydrochloride hydrate H and anhydrous X were held at constant conditions, the stable form of xylazine hydrochloride can be found out. To determine equilibrium relative humidity, the unstable form of xylazine hydrochloride was inserted in thermostated humidity chamber and its weight was recorded by weighing the sample outside the chamber. The kinetic model and the rate constant for each condition were determined. The rate constants give information regarding the speed of the process at every experimentally used relative humidity. Thus using the data in coordinates k-p for each temperature it is possible to determine the water vapor pressure of the equilibrium. With this method the phase boundary for xylazine hydrochloride was determined and hydration enthalpy was calculated. The hydration rates of xylazine polymorphs A and X were investigated. PMID:19630697

B?rzi?s, Agris; Acti?s, Andris; Kreismanis, Juris P

2009-01-01

83

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

PubMed

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

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

2014-02-01

84

A Highly Efficient Catalyst for Oxime Ligation and Hydrazone-Oxime Exchange Suitable for Bioconjugation  

PubMed Central

Imine-based reactions are useful for a wide range of bioconjugation applications. Although aniline is known to catalyze the oxime ligation reaction under physiological conditions, it suffers from slow reaction kinetics, specifically when a ketone is being used or when hydrazone-oxime exchange is performed. Here, we report on the discovery of a new catalyst that is up to 15 times more efficient than aniline. That catalyst, m-phenylenediamine (mPDA), was initially used to analyze the kinetics of oxime ligation on aldehyde- and ketone-containing small molecules. While mPDA is only modestly more effective than aniline when used in equal concentrations (~ 2-fold), its much greater aqueous solubility relative to aniline allows it to be used at higher concentrations, resulting in significantly more efficient catalysis. In the context of protein labeling, it was first used to site-specifically label an aldehyde-functionalized protein through oxime ligation, and its kinetics were compared to reaction with aniline. Next, a protein was labeled with an aldehyde-containing substrate in crude cell lysate, captured with hydrazide-functionalized beads and then the kinetics of immobilized protein release via hydrazone-oxime exchange were analyzed. Our results show that mPDA can release and label 15 times more protein than aniline can in 3 h. Then, using the new catalyst, ciliary neurotrophic factor, a protein with therapeutic potential, was successfully labeled with a fluorophore in only 5 min. Finally, a protein containing the unnatural amino acid, p-acetyl phenylalanine, a ketone-containing residue, was prepared and PEGylated efficiently via oxime ligation using mPDA. This new catalyst should have a significant impact on the field of bioconjugation, where oxime ligation and hydrazone-oxime exchange are commonly employed. PMID:23425124

Rashidian, Mohammad; Mahmoodi, Mohammad M.; Shah, Rachit; Dozier, Jonathan K.; Wagner, Carston R.; Distefano, Mark D.

2014-01-01

85

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

PubMed

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

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

2014-12-22

86

21 CFR 520.1242 - Levamisole hydrochloride oral dosage forms.  

Code of Federal Regulations, 2010 CFR

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

2010-04-01

87

21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.  

Code of Federal Regulations, 2012 CFR

...Food and Drugs 6 2012-04-01 2012-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section...OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage...

2012-04-01

88

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

89

21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.  

Code of Federal Regulations, 2013 CFR

...Food and Drugs 6 2013-04-01 2013-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section...OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage...

2013-04-01

90

21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.  

Code of Federal Regulations, 2011 CFR

...Food and Drugs 6 2011-04-01 2011-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section...OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage...

2011-04-01

91

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

92

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

93

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

94

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

95

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

96

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

PubMed

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

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

2009-09-01

97

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

PubMed

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

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

2014-11-14

98

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

99

Copper complexes with phosphonium containing hydrazone ligand: topoisomerase inhibition and cytotoxicity study.  

PubMed

Four new copper(II) complexes containing phosphonium substituted hydrazone (L) with the formulations [CuL]Cl(3), [Cu(phen)L]Cl(4), [Cu(bpy)L]Cl(5), [Cu(dbpy)L]Cl(6), (where L = doubly deprotonated hydrazone; phen = 1,10'-phenanthroline; bpy = 2,2'-bipyridine; dbpy = 5,5'-dimethyl-2,2'-bipyridine) have been synthesized. The compounds were characterized by elemental analysis, spectroscopic methods and in the case of crystalline products by X-ray crystallography. The cytotoxicity and topoisomerase I (topo I) inhibition activities of these compounds were studied. It is noteworthy that the addition of N,N-ligands to the copper(II) complex lead to the enhancement in the cytotoxicity of the compounds, especially against human prostate adenocarcinoma cell line (PC-3). Complex 4 exhibits the highest activity against PC-3 with the IC?? value of 3.2 ??. The complexes can also inhibit topo I through the binding to DNA and the enzyme. PMID:24602785

Chew, Shin Thung; Lo, Kong Mun; Lee, Sze Koon; Heng, Mok Piew; Teoh, Wuen Yew; Sim, Kae Shin; Tan, Kong Wai

2014-04-01

100

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...

101

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). ...

102

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

PubMed Central

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

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

2014-01-01

103

Simultaneous Estimation of Metformin Hydrochloride and Pioglitazone Hydrochloride by RPHPLC Method from Combined Tablet Dosage Form.  

PubMed

A high performance reverse phase liquid chromatographic procedure is developed for simultaneous estimation of metformin hydrochloride and pioglitazone hydrochloride in combined tablet dosage form. The mobile phase used was a combination of acetonitrile:water:acetic acid (60:40:0.3) and the pH was adjusted to 5.5 by adding triethylamine. The detection of the combined dosage form was carried out at 230 nm and a flow rate employed was 1 ml/min. Linearity was obtained in the concentration range of 0.015 to 0.120 mug/ml of pioglitazone hydrochloride and 0.5 to 4.0 mug/ml of metformin hydrochloride with a correlation coefficient of 0.9992 and 0.9975. The results of the analysis were validated statistically and recovery studies confirmed the accuracy and precision of the proposed method. PMID:20046754

Sahoo, P K; Sharma, R; Chaturvedi, S C

2008-01-01

104

Determination of nalbuphine hydrochloride, methylparaben, and propylparaben in nalbuphine hydrochloride injection by high performance liquid chromatography  

Microsoft Academic Search

Summary  A stability-indicating liquid chromatographic method has been developed for the determination of nalbuphine hydrochloride,\\u000a methylparaben, and propylparaben in nalbuphine hydrochloride injection. Reversed-phase chromatography was carried out using\\u000a a mobile phase containing 0.05 % trifuoroacetic acid, acetonitrile, and tetrahydrofuran. Quantitation was achieved with UV\\u000a detection at 280 nm. Validation data for linearity, accuracy, precision, specificity, and robustness are presented. The chromatographic

M. A. Quarry; D. S. Sebastian; R. C. Williams

1998-01-01

105

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

106

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

Code of Federal Regulations, 2010 CFR

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

2010-07-01

107

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

Code of Federal Regulations, 2012 CFR

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

2012-07-01

108

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

Code of Federal Regulations, 2011 CFR

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

2011-07-01

109

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

Code of Federal Regulations, 2014 CFR

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

2014-07-01

110

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

Code of Federal Regulations, 2013 CFR

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

2013-07-01

111

Partition coefficients of the iron (III) complexes of pyridoxal isonicotinoyl hydrazone and its analogs and the correlation to iron chelation efficacy. Correction of some reported partition coefficients  

Microsoft Academic Search

Pyridoxal isonicotinoyl hydrazone (PIH), salicylaldehydebenzoyl hydrazone (SBH), and their analogschelate iron(III) and show promise asorally effective drugs for treating diseases of iron overload. Theirbiological activity isrelated to their lipophilicity, as measured by their partition coefficients P betweenn-octanoland water. However, the method of calculating log P described in an article in this journal(Edwardet al. 1995; BioMetals, 8, 209-217) is faulty for

John T Edward

1998-01-01

112

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

113

21 CFR 184.1676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2013 CFR

...5-dihydroxymethy-2-methylpyridine hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications...defined in § 170.3(n)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this...

2013-04-01

114

21 CFR 184.1676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2014 CFR

...5-dihydroxymethy-2-methylpyridine hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications...defined in § 170.3(n)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this...

2014-04-01

115

21 CFR 184.1676 - Pyridoxine hydrochloride.  

Code of Federal Regulations, 2012 CFR

...5-dihydroxymethy-2-methylpyridine hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications...defined in § 170.3(n)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this...

2012-04-01

116

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

PubMed

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

Bunck, David N; Dichtel, William R

2013-10-01

117

Verification of the dispersive charge transport in a hydrazone:polycarbonate molecularly doped polymer  

NASA Astrophysics Data System (ADS)

We report results of specially planned experiments intended to verify the dispersive character of the charge carrier transport in polycarbonate molecularly doped with hydrazone at 30 wt% loading, using for this purpose samples specifically featuring a well-defined plateau on a linear-linear plot. For this purpose we propose a new variant of the time-of-flight technique which allows easy changing of the generation zone width from about 0.5 µm (surface excitation) through intermediate values to full sample thickness (bulk excitation). To achieve this, we use electron pulses of 3-50 keV energy rather than traditional light pulses provided by lasers. Experimental results corroborated by numerical calculations uniquely prove that carrier transport in this molecularly doped polymer is dispersive, with the dispersion parameter equal to 0.75. Nevertheless, the mobility field dependence follows the famous Poole-Frenkel law.

Tyutnev, Andrey P.; Saenko, Vladimir S.; Pozhidaev, Evgenii D.; Kolesnikov, Vladislav A.

2009-03-01

118

Structural studies on zinc(II) complexes with 2-benzoylpyridine-derived hydrazones  

Microsoft Academic Search

2-Benzoylpyridine-phenylhydrazone (H2BzPh), 2-benzoylpyridine-para-chloro-phenylhydrazone (H2BzpClPh), and 2-benzoylpyridine-para-nitro-phenyl (H2BzpNO2Ph) hydrazone were obtained and fully characterized, as well as their zinc(II) complexes [Zn(H2BzPh)Cl2] (1), [Zn(H2BzClPh)Cl2] (2) and [Zn(H2BzpNO2Ph)Cl2] (3). During the syntheses of complex 1 a second product crystallized, which was characterized as [Zn(2BzPh)2] (1a). Upon re-crystallization in 1:9 DMSO:acetone conversion of 2 into [Zn(H2BzpClPh)Cl2]·H2O (2a) and of 3 into [Zn(2BzpNO2Ph)Cl(DMSO)] (3a) occurred.

Angel A. Recio Despaigne; Jeferson G. Da Silva; Ana Cerúlia M. do Carmo; Oscar E. Piro; Eduardo E. Castellano; Heloisa Beraldo

2009-01-01

119

Rapid Oxime and Hydrazone Ligations with Aromatic Aldehydes for Biomolecular Labeling  

PubMed Central

A high yielding and rapid chemoselective ligation approach is presented that uses aniline catalysis to activate aromatic aldehydes towards two amine nucleophiles, namely 6-hydrazinopyridyl and aminooxyacetyl groups. The rates of these ligations are resolved for model reactions with unprotected peptides. The resulting hydrazone and oxime conjugates are attained under ambient conditions with rate constants of 101-103 M-1s-1. These rate constants exceed those of current chemoselective ligation chemistries and enable efficient labeling of peptides and proteins at low ?M concentrations, at neutral pH, without using a large excess of one of the components. The utility of the approach is demonstrated by the p-fluorobenzylation of Human Serum Albumin and by the fluorescent labeling of an unprotected peptide with Alexa Fluor 488. PMID:19053314

Dirksen, Anouk; Dawson, Philip E.

2009-01-01

120

Verification of the dispersive charge transport in a hydrazone:polycarbonate molecularly doped polymer.  

PubMed

We report results of specially planned experiments intended to verify the dispersive character of the charge carrier transport in polycarbonate molecularly doped with hydrazone at 30 wt% loading, using for this purpose samples specifically featuring a well-defined plateau on a linear-linear plot. For this purpose we propose a new variant of the time-of-flight technique which allows easy changing of the generation zone width from about 0.5 µm (surface excitation) through intermediate values to full sample thickness (bulk excitation). To achieve this, we use electron pulses of 3-50 keV energy rather than traditional light pulses provided by lasers. Experimental results corroborated by numerical calculations uniquely prove that carrier transport in this molecularly doped polymer is dispersive, with the dispersion parameter equal to 0.75. Nevertheless, the mobility field dependence follows the famous Poole-Frenkel law. PMID:21693912

Tyutnev, Andrey P; Saenko, Vladimir S; Pozhidaev, Evgenii D; Kolesnikov, Vladislav A

2009-03-18

121

Methyl and ethyl ketone analogs of salicylaldehyde isonicotinoyl hydrazone: novel iron chelators with selective antiproliferative action.  

PubMed

Salicylaldehyde isonicotinoyl hydrazone (SIH) is a lipophilic, orally-active tridentate iron chelator providing both effective protection against various types of oxidative stress-induced cellular injury and anticancer action. However, the major limitation of SIH is represented by its labile hydrazone bond that makes it prone to plasma hydrolysis. Recently, nine new SIH analogues derived from aromatic ketones with improved hydrolytic stability were developed. Here we analyzed their antiproliferative potential in MCF-7 breast adenocarcinoma and HL-60 promyelocytic leukemia cell lines. Seven of the tested substances showed greater selectivity than the parent agent SIH towards the latter cancer cell lines compared to non-cancerous H9c2 cardiomyoblast-derived cells. The tested chelators induced a dose-dependent dissipation of the inner mitochondrial membrane potential, an induction of apoptosis as evidenced by Annexin V positivity or significant increases of activities of caspases 3, 7, 8 and 9 and cell cycle arrest. With the exception of nitro group-bearing NHAPI, the studies of iron complexes of the chelators confirmed the crucial role of iron in the mechanism of their antiproliferative action. Finally, all the assayed chelators inhibited the oxidation of ascorbate by iron ions indicating lack of redox activity of the chelator-iron complexes. In conclusion, this study identified several important design criteria for improvement of the antiproliferative selectivity of the aroylhydrazone iron chelators. Several of the novel compounds--in particular the ethylketone-derived HPPI, NHAPI and acetyl-substituted A2,4DHAPI--merit deeper investigation as promising potent and selective anticancer agents. PMID:22521999

Macková, Eliška; Hrušková, Kate?ina; Bendová, Petra; Vávrová, Anna; Jansová, Hana; Hašková, Pavlína; Kova?íková, Petra; Vávrová, Kate?ina; Sim?nek, Tomáš

2012-05-30

122

Treatment of allergic conjunctivitis with olopatadine hydrochloride eye drops  

PubMed Central

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

Uchio, Eiichi

2008-01-01

123

Treatment of allergic conjunctivitis with olopatadine hydrochloride eye drops.  

PubMed

Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H(1) receptor antagonist action, chemical mediator suppressive action, and eosinophil infiltration suppressive action. Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol((R))) was introduced to the market in Japan in October 2006. In a conjunctival allergen challenge (CAC) test, olopatadine hydrochloride 0.1% ophthalmic solution significantly suppressed ocular itching and hyperemia compared with levocabastine hydrochloride 0.05% ophthalmic solution, and the number of patients who complained of ocular discomfort was lower in the olopatadine group than in the levocabastine group. Conjunctival cell membrane disruption was observed in vitro in the ketotifen fumarate group, epinastine hydrochloride group, and azelastine hydrochloride group, but not in the olopatadine hydrochloride 0.1% ophthalmic solution group, which may potentially explain the lower discomfort felt by patients on instillation. Many other studies in humans have revealed the superiority of olopatadine 0.1% hydrochloride eye drops to several other anti-allergic eye drops. Overseas, olopatadine hydrochloride 0.2% ophthalmic solution for a once-daily regimen has been marketed under the brand name of Pataday((R)). It is expected that olopatadine hydrochloride ophthalmic solutions may be used in patients with a more severe spectrum of allergic conjunctival diseases, such as vernal keratoconjunctivitis or atopic keratoconjunctivitis, in the near future. PMID:19668750

Uchio, Eiichi

2008-09-01

124

Phenylazoindole dyes 3: Determination of azo-hydrazone tautomers of new phenylazoindole dyes in solution and solid state  

NASA Astrophysics Data System (ADS)

A new two series of phenylazo indole dyes was synthesized and the structures of the dyes were confirmed by UV-vis, FT-IR, HRMS and 1H/13C NMR spectroscopic techniques. Five of these dyes (I, I?, II?, III and III?) were also characterized in solid state by using single crystal X-ray diffraction studies besides other spectroscopic techniques. The geometries of the azo and hydrazone tautomeric forms of the dyes were optimized by using Density Functional Theory (DFT). In addition, the effects of the donor and acceptor groups on the azo and hydrazone forms of the dyes were evaluated experimentally and theoretically. The results indicate that the phenylazoindole dyes derived from 2-phenyl indole as coupling component exist as azo form in solution, gas phase and solid state.

Babür, Banu; Sefero?lu, Nurgül; Aktan, Ebru; Hökelek, Tuncer; ?ahin, Ertan; Sefero?lu, Zeynel

2015-02-01

125

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

PubMed

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

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

2014-04-28

126

Fast Hydrazone Reactants: Electronic and Acid/Base Effects Strongly Influence Rate at Biological pH  

PubMed Central

Kinetics studies with structurally varied aldehydes and ketones in aqueous buffer at pH 7.4 reveal that carbonyl compounds with neighboring acid/base groups form hydrazones at accelerated rates. Similarly, tests of a hydrazine with a neighboring carboxylic acid group show that it also reacts at an accelerated rate. Rate constants for the fastest carbonyl/hydrazine combinations are 2–20 M?1sec?1, which is faster than recent strain-promoted cycloaddition reactions. PMID:24224646

Kool, Eric T.; Park, Do-Hyoung; Crisalli, Pete

2013-01-01

127

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

128

IMMOBILIZATION OF WHITE-TAILED DEER WITH XYLAZINE HYDROCHLORIDE AND KETAMINE HYDROCHLORIDE AND ANTAGONISM BY TOLAZOLINE HYDROCHLORIDE  

Microsoft Academic Search

Fourteen penned and 17 free-ranging white-tailed deer (Odocoileus virgtnianus Rafinesque) were singularly or repeatedly immobilized with 100 mg xylazine hydrochloride (HCl) and 300 mg ketamine HCl. The mean times from intravenous injection to ambulation for 1.0, 2.0, and 4.0 mg\\/kg body weight doses of tolazoline HCI were 13.5, 10.5, and 9.2 min. Deer not receiving tolazoline HCl recovered in an

Terry J. Kreeger; Glenn D. Del Giudice; S. SealI; Patrick D. Karns

129

REVERSAL BY TOLAZOLINE HYDROCHLORIDE OF XYLAZINE HYDROCHLORIDE-KETAMINE HYDROCHLORIDE IMMOBILIZATIONS IN FREE-RANGING DESERT MULE DEER  

Microsoft Academic Search

We captured 10 free-ranging desert mule deer (Odocoileus hemionus crooki) (five males and five females) by net-gun from a helicopter and immobilized them with xylazine hydrochloride (HCI) (100 mg) and ketamine HC1 (300 to 400 mg) injected intramuscularly. Arousal and ambulation times were 13.9 ± 4.2 and 14.3 ± 4.2 mm in eight deer injected intravenously with tolazoline HC1 (3.0

Glenn D. DelGiudice; Paul R. Krausman; Elizabeth S. Bellantoni; Richard C. Etchberger; Ulysses S. Seal

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

Study on fluorescence characteristics of duloxetine hydrochloride  

NASA Astrophysics Data System (ADS)

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

Liu, Xiangping; Du, Yingxiang; Wu, Xiulan

2008-12-01

132

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

133

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

134

Qsar study of some substituted 4-quinolinyl and 9-acridinyl hydrazones as antimalarial agents.  

PubMed

The quantitative structure-activity relationship (QSAR) analysis of some synthesized substituted 4-quinolinyl and 9-acridinyl hydrazone derivatives were performed to find out the structural requirements of their antimalarial activities. Various 2D descriptors were calculated and used in the present analysis. The 2D-QSAR studies were performed using three statistical methods: the multiple linear regressions, giving square of correlation coefficient (r(2)) = 0.8456, cross validated squared correlation coefficient (q(2)) = 0.7814 and predictable ability (pred_r(2)) = 0.7443; the partial least squares regression, with r(2) = 0.8402, q(2) = 0.7879 and pred_r(2) = 0.7680; and principle component regression, giving r(2) = 0.8392, q(2) = 0.7979 and pred_r(2) = 0.6440. Best equation was selected on the basis of high r(2), q(2) and pred_r(2). The QSAR model indicated that the T_N_O_3, IdAverage, chiV6chain, Most-vePotential and T_C_N_6 played an important role in determining antimalarial activities. The results of the present study may be useful on the designing of more potent analogues as antimalarial agents. PMID:23285677

Sahu, Nitendra K; Sharma, Mukesh; Mourya, Vishnukanth; Kohli, D V

2012-01-01

135

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

Microsoft Academic Search

The impact of zilpaterol hydrochloride (ZH) on carcass yield, composition, and tenderness was evaluated using 384 beef steers in a randomized com- plete block design. Main effects were the addition of 0 or 8.3 mg\\/kg of ZH for the final 20 d of feeding and each inclusion level was paired with withdrawal periods of 3, 10, 17, or 24 d.

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

2009-01-01

136

The Solvation and Dissociation of 4Benzylaniline Hydrochloride in Chlorobenzene  

E-print Network

The Solvation and Dissociation of 4Benzylaniline Hydrochloride in Chlorobenzene Emma K. Gibson-benzylaniline hydrochloride, using chlorobenzene as a solvent at a temperature of 373 K. Two operational regimes in the presence of chlorobenzene as a solvent.1,2,4,5 Methylene diphenyl diisocya- nate (MDI) is the major

Miller, Alice

137

Psychosedation With Dexmedetomidine Hydrochloride During Minor Oral Surgery  

Microsoft Academic Search

We performed intravenous sedation with dexmedetomidine hydrochloride during minor oral surgery and compared this agent with propofol. Patients were random- ly divided into 2 groups: dexmedetomidine hydrochloride ( D ) and propofol (P) groups. In Group D, systolic blood pressure ( SBP ) increased immediately after the start of initial loading, although no significant differences were noted. Both SBP and

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

2009-01-01

138

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

139

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

PubMed

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

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

2013-07-01

140

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

141

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

142

Synthesis and insecticidal activity of novel hydrazone compounds derived from a naturally occurring lignan podophyllotoxin against Mythimna separata (Walker).  

PubMed

In continuation of our program aimed at the discovery and development of natural-product-based insecticidal agents, a series of novel hydrazone derivatives of podophyllotoxin, which is a naturally occurring aryltetralin lignan and isolated as the main secondary metabolite from the roots and rhizomes of Podophyllum species, were synthesized and evaluated as insecticidal agents against the pre-third-instar larvae of oriental armyworm, Mythimna separata (Walker) in vivo at 1mg/mL. Especially compounds 8i, 8j, 8t, and 8u showed the more potent insecticidal activity with the final mortality rates greater than 60%. PMID:24810569

Wang, Yi; Yu, Xiang; Zhi, Xiaoyan; Xiao, Xiao; Yang, Chun; Xu, Hui

2014-06-15

143

Spectroscopic Investigation of the Interaction Between Copper (II) 2-oxo-propionic Acid Salicyloyl Hydrazone Complex and Bovine Serum Albumin  

Microsoft Academic Search

The interaction between copper (II) 2-oxo-propionic acid salicyloyl hydrazone (CuIIL) and bovine serum albumin (BSA) under physiological conditions was investigated by the methods of fluorescence spectroscopy,\\u000a UV-Vis absorption, and circular dichroism spectroscopy. Fluorescence data showed that the fluorescence quenching of BSA by\\u000a CuIIL was the result of the formation of the BSA–CuIIL complex. The apparent binding constants (K\\u000a a) between

Ping Mei; Ye-Zhong Zhang; Xiao-Ping Zhang; Cheng-Xiang Yan; Hua Zhang; Yi Liu

2008-01-01

144

Mononuclear and three-dimensional metal complexes based on a multidentate hydrazone ligand.  

PubMed

A potentially pentadentate hydrazone ligand, N'-[1-(pyrazin-2-yl)ethylidene]nicotinohydrazide (HL), was prepared from the condensation reaction of nicotinohydrazide and acetylpyrazine. Reactions of HL with MnCl2, Mn(CH3COO)2 and Cd(CH3COO)2 afforded three metal complexes, namely dichlorido{N'-[1-(pyrazin-2-yl-?N(1))ethylidene]nicotinohydrazide-?(2)N',O}manganese(II), [MnCl2(C12H11N5O)], (I), bis{N'-[1-(pyrazin-2-yl-?N(1))ethylidene]nicotinohydrazidato-?(2)N',O]manganese(II), [Mn(C12H10N5O)2], (II), and poly[[(acetato-?(2)O,O'){?3-N'-[1-(pyrazin-2-yl-?(2)N(1):N(4))ethylidene]nicotinohydrazidato-?(3)N',O:N(1)}cadmium(II)] chloroform disolvate], {[Cd(C12H10N5O)(CH3COO)]·2CHCl3}n, (III), respectively. Complex (I) has a mononuclear structure, the Mn(II) centre adopting a distorted square-pyramidal coordination. Complex (II) also has a mononuclear structure, with the Mn(II) centre occupying a special position (C2 symmetry) and adopting a distorted octahedral coordination environment, which is defined by two O atoms and four N atoms from two N'-[1-(pyrazin-2-yl)ethylidene]nicotinohydrazidate (L(-)) ligands related via a crystallographic twofold axis. Complex (III) features a unique three-dimensional network with rectangular channels, and the L(-) ligand also serves as a counter-anion. The coordination geometry of the Cd(II) centre is pentagonal bipyramidal. This study demonstrates that HL, which can act as either a neutral or a mono-anionic ligand, is useful in the construction of interesting metal-organic compounds. PMID:25652278

Liu, Yan Fei; Liu, Ya Ping; Zhang, Ke Ke; Ren, Qing Ling; Qin, Jie

2015-02-01

145

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

PubMed

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

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

2014-01-29

146

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

147

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

PubMed

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

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

1994-10-01

148

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

149

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

150

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

PubMed Central

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

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

2014-01-01

151

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 13a–e. 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

152

Spectroscopy study of ephedrine hydrochloride and papaverine hydrochloride in terahertz range  

NASA Astrophysics Data System (ADS)

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

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

2008-12-01

153

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...

154

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...

155

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, 1630–1635]. In the crystal, the cations and chloride anions are linked into a helical chain propagating parallel to the b-axis direction by N—H?Cl and O—H?Cl hydrogen bonds. The title salt and the morphine monohydrate [Bye (1976 ?) Acta Chem. Scand. 30, 549–554] display very similar one-dimensional packing modes of their morphine components. PMID:23476193

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

2012-01-01

156

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

157

40 CFR 180.499 - Propamocarb hydrochloride, tolerances for residues.  

Code of Federal Regulations, 2010 CFR

...for residues. (a) General. Tolerances are established for the residues of propyl[3-(dimethylamino)propyl]carbamate monohydrochloride also known as propamocarb hydrochloride in or on the following raw agricultural commodity:...

2010-07-01

158

40 CFR 180.499 - Propamocarb hydrochloride, tolerances for residues.  

Code of Federal Regulations, 2011 CFR

...for residues. (a) General. Tolerances are established for the residues of propyl[3-(dimethylamino)propyl]carbamate monohydrochloride also known as propamocarb hydrochloride in or on the following raw agricultural commodity:...

2011-07-01

159

40 CFR 180.499 - Propamocarb hydrochloride, tolerances for residues.  

Code of Federal Regulations, 2012 CFR

...for residues. (a) General. Tolerances are established for the residues of propyl[3-(dimethylamino)propyl]carbamate monohydrochloride also known as propamocarb hydrochloride in or on the following raw agricultural commodity:...

2012-07-01

160

21 CFR 522.1642 - Oxymorphone hydrochloride injection.  

Code of Federal Regulations, 2011 CFR

... 0.75-1.5 (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...

2011-04-01

161

21 CFR 522.1642 - Oxymorphone hydrochloride injection.  

Code of Federal Regulations, 2010 CFR

... 0.75-1.5 (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...

2010-04-01

162

21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.  

Code of Federal Regulations, 2010 CFR

...a) Specifications. The drug is an aqueous solution containing 0.5 percent proparacaine hydrochloride, 2.45 percent glycerin as a stabilizer, and 0.2 percent chlorobutanol (choral derivative) and 1:10,000 benzalkonium chloride as...

2010-04-01

163

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

164

21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.  

Code of Federal Regulations, 2011 CFR

...DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1982 Proparacaine hydrochloride...percent chlorobutanol (choral derivative) and 1:10,000 benzalkonium chloride as preservatives. (b) Sponsor. See No....

2011-04-01

165

21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.  

Code of Federal Regulations, 2013 CFR

...DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1982 Proparacaine hydrochloride...percent chlorobutanol (choral derivative) and 1:10,000 benzalkonium chloride as preservatives. (b) Sponsor. See No....

2013-04-01

166

21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.  

Code of Federal Regulations, 2012 CFR

...DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1982 Proparacaine hydrochloride...percent chlorobutanol (choral derivative) and 1:10,000 benzalkonium chloride as preservatives. (b) Sponsor. See No....

2012-04-01

167

Substrate stabilization of lysozyme to thermal and guanidine hydrochloride denaturation  

E-print Network

SUBSTRATE STABILIZATION OF I YSOZYNE TO THERNAL AND GUANIDINE HYDROCHLORIDE DENATURATION A Thesis Timothy NcGrath Submitted to the Graduate College of Texas ABH University in partial fulf illment of the requirement for the degree of NASTER... OF SCIENCE August %977 Na jor Sub j ect: Biochemistry SUBSTRATE STABILE IZATION OF LYSOZYME TO THERMAL AND GUAM IDINE HYDROCHLORIDE DENATURATION A Thesis Timothy NcGrath Approved as to style and content by: Chairman of Commi t tee (Head of De artment...

McGrath, Timothy

1977-01-01

168

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

169

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

170

Second-Derivative Synchronous Fluorescence Spectroscopy for the Simultaneous Determination of Fluphenazine Hydrochloride and Nortriptyline Hydrochloride in Pharmaceutical Preparations  

Microsoft Academic Search

A rapid, simple, and highly sensitive second-derivative synchronous fluorimetric (SDSF) method has been developed for the\\u000a simultaneous analysis of binary mixtures of fluphenazine hydrochloride (FLZ) and nortriptyline hydrochloride (NTP) in their\\u000a co-formulated tablets. The method is based upon measurement of the native fluorescence of these drugs at constant wavelength\\u000a difference (??)?=?120 nm in acetic acid. The different experimental parameters affecting the

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

2009-01-01

171

Effect of ractopamine hydrochloride and zilpaterol hydrochloride on growth, diet digestibility, intake and carcass characteristics of feedlot lambs  

Microsoft Academic Search

The effects of the ?-adrenergic agonists ractopamine hydrochloride (RH; 0.35, 0.70 and 1.05mgkg?1 of BWd?1) and zilpaterol hydrochloride (ZH; 0.10, 0.20 and 0.30mgkg?1 of BWd?1) on growth performance and carcass characteristics were determined in 84 Dorper×Katahdin lambs (12 lambs per treatment), that were randomly assigned to a complete block design during a 42-day feeding trial. Lambs were fed a corn

M. A. López-Carlos; R. G. Ramírez; J. I. Aguilera-Soto; C. F. Aréchiga; F. Méndez-Llorente; H. Rodríguez; J. M. Silva

2010-01-01

172

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

173

Rhodamine hydrazone derivatives as Hg2+ selective fluorescent and colorimetric chemosensors and their applications to bioimaging and microfluidic system.  

PubMed

In this paper, we report new rhodamine hydrazone derivatives bearing thiol and carboxylic acid groups as selective fluorescent and colorimetric chemosensors for Hg(2+). The ring-opening process of spirolactam enables the large fluorescent enhancement and colorimetric change upon the addition of Hg(2+). The sample containing Hg(2+) was mixed with one of the chemosensors in a microchannel where the sensor was examined using confocal laser scanning microscopy. A plot of the fluorescent intensities of both chemosensors versus the log concentration of Hg(2+) exhibited a linear response (r(2)=0.95) in the range of 1 nM-1 ?M, and the detection limits were 1 nM and 4.2 nM, respectively. Both chemosensors also enable the visualization of Hg(2+) accumulated in the nematode Caenorhabditis elegans previously exposed to nanomolar concentrations of Hg(2+). PMID:21240424

Kim, Ha Na; Nam, Seong-Won; Swamy, K M K; Jin, Yan; Chen, Xiaoqiang; Kim, Yonugmee; Kim, Sung-Jin; Park, Sungsu; Yoon, Juyoung

2011-04-01

174

Spectroscopic and physicochemical studies on nickel(II) complexes of isatin-3,2'-quinolyl-hydrazones and their adducts  

NASA Astrophysics Data System (ADS)

Nickel(II) complexes of isatin-3,2'-quinolyl-hydrazones of the type [Ni(L)X] (where X = Cl -, Br -, NO 3-, CH 3COO - and ClO 4-] and their adducts Ni(L)X·2Y [where Y = pyridine or dioxane and X = Cl -, Br -, NO 3- and ClO 4-] have been synthesized under controlled experimental conditions and characterized by using the modern spectroscopic and physicochemical techniques viz. mass, 1H NMR, IR, electronic, elemental analysis, magnetic moment susceptibility measurements and molar conductance, etc. On the basis of spectral studies a four coordinated tetrahedral geometry is assigned for Ni(L)X type complexes whereas the adducts (Ni(L)X·2Y) were found to have a six coordinated distorted octahedral geometry.

Gupta, Lokesh Kumar; Bansal, Usha; Chandra, Sulekh

2007-04-01

175

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

Federal Register 2010, 2011, 2012, 2013, 2014

...DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and...Levomethadyl Acetate Hydrochloride) Oral Solution, 10 Milligrams/Milliliter...acetate hydrochloride (HCl)) oral solution, 10 milligrams (mg...for levomethadyl acetate HCl oral solution, 10 mg/mL, if...

2011-06-06

176

21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.  

Code of Federal Regulations, 2010 CFR

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

2010-04-01

177

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

Federal Register 2010, 2011, 2012, 2013, 2014

...Palonosetron Hydrochloride) Capsules, 0.5 Milligram (Base), Were Not Withdrawn...palonosetron hydrochloride (HCl)) Capsules, 0.5 milligram (mg) (base), were not...ANDAs) for palonosetron HCl capsules, 0.5 mg (base), if all other legal...

2012-09-04

178

Methylphenidate Hydrochloride Extended Release Tablets (Generic Concerta) Made by Mallinckrodt and Kudco  

MedlinePLUS

... Drug Supply Chain Integrity Methylphenidate Hydrochloride Extended Release Tablets (generic Concerta) made by Mallinckrodt and Kudco [11- ... therapeutic equivalence with two generic versions of Concerta tablets (methylphenidate hydrochloride extended-release) Based on an analysis ...

179

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

Federal Register 2010, 2011, 2012, 2013, 2014

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

2011-08-30

180

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

Code of Federal Regulations, 2012 CFR

...Oxytetracycline hydrochloride ophthalmic and topical dosage forms. 524.1662 Section...AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524...Oxytetracycline hydrochloride ophthalmic and topical dosage...

2012-04-01

181

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

Code of Federal Regulations, 2010 CFR

...Oxytetracycline hydrochloride ophthalmic and topical dosage forms. 524.1662 Section...AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524...Oxytetracycline hydrochloride ophthalmic and topical dosage...

2010-04-01

182

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

Code of Federal Regulations, 2011 CFR

...Oxytetracycline hydrochloride ophthalmic and topical dosage forms. 524.1662 Section...AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524...Oxytetracycline hydrochloride ophthalmic and topical dosage...

2011-04-01

183

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

Code of Federal Regulations, 2013 CFR

...Oxytetracycline hydrochloride ophthalmic and topical dosage forms. 524.1662 Section...AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524...Oxytetracycline hydrochloride ophthalmic and topical dosage...

2013-04-01

184

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

185

Sevelamer hydrochloride exacerbates metabolic acidosis in hemodialysis patients, depending on the dosage.  

PubMed

Sevelamer hydrochloride, as a phosphate binder that contains neither aluminum nor calcium, is expected to improve the prognosis of dialysis patients. However, sevelamer hydrochloride has been reported to lower the serum bicarbonate level. In the present study, we performed a retrospective study on the potential influences of sevelamer hydrochloride on metabolic acidosis in hemodialysis patients. The subjects were 72 patients who underwent hemodialysis at our hospital. Thirty-six patients taking sevelamer hydrochloride and 36 patients matched for sex, diabetes mellitus, age and duration of dialysis who were not taking sevelamer hydrochloride were studied. We assigned the 36 patients who had been taking sevelamer hydrochloride to the 'sevelamer group', and the 36 patients not taking sevelamer hydrochloride were the control group. Statistical significance was evaluated by a t-test and Pearson's correlation coefficient. In the sevelamer group, the mean levels of bicarbonate, base excess and pH decreased significantly after administration, compared with the values before administration, but in the control group, aggravation of acidosis was not seen. The levels of bicarbonate, base excess and pH after the medication of sevelamer hydrochloride were found to be significantly and negatively correlated with the daily dose of sevelamer hydrochloride. The levels were also found to be significantly and negatively correlated with the cumulative dose of sevelamer hydrochloride; however, the value of the mean levels of chlorine and the anion gap did not increase with sevelamer hydrochloride. Sevelamer hydrochloride caused metabolic acidosis in a dose-dependent manner in hemodialysis patients without hyperchloremia. PMID:17381531

Oka, Yoshinari; Miyazaki, Masashi; Takatsu, Shigeko; Kunitomo, Kei-ichi; Uno, Futoshi; Maruyama, Masanobu; Matsuda, Hiroaki

2007-04-01

186

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

187

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

188

Measurement of pseudoephedrine hydrochloride dissolution using chloride-ion electrode.  

PubMed

Experiments were performed to determine the suitability of using a chloride-ion electrode for the measurement of pseudoephedrine hydrochloride dissolution from commercially available compressed tablets. Dissolution experiments were carried out in 500 ml of distilled water using the USP paddle method at 100 rpm. Both chloride ion and pseudoephedrine (UV spectrophotometry) were measured at six different sampling times. Percent dissolved versus time values were linearized on a log-normal probability basis. The slopes of individual lines obtained from the chloride and pseudoephedrine measurements were compared using a Student t test and did not differ significantly (t = 0.415, df = 5, p greater than 0.05). In addition to providing an efficient, inexpensive, and simple method for measuring pseudoephedrine hydrochloride dissolution rates, the chloride-ion electrode could be used in the measurement of dissolution rates for a wide variety of drugs available as hydrochloride salts. PMID:7299681

Chen, S T; Thompson, R C; Poust, R I

1981-11-01

189

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

PubMed

Azo dyes, 1,3-dimethyl-5-(arylazo)-6-aminouracil (aryl=-C6H5 (1), -p-CH3C6H4 (2), -p-ClC6H4 (3), -p-NO2C6H4 (4)) were prepared and characterized by UV-vis, FT-IR, (1)H NMR, (13)C NMR spectroscopic techniques and single crystal X-ray crystallographic analysis. In the light of spectroscopic analysis it evidences that of the tautomeric forms, the azo-enamine-keto (A) form is the predominant form in the solid state whereas in different solvents it is the hydrazone-imine-keto (B) form. The study also reveals that the hydrazone-imine-keto (B) form exists in an equilibrium mixture with its anionic form in various organic solvents. The solvatochromic and photophysical properties of the dyes in various solvents with different hydrogen bonding parameter were investigated. The dyes exhibit positive solvatochromic property on moving from polar protic to polar aprotic solvents. They are fluorescent active molecules and exhibit high intense fluorescent peak in some solvents like DMSO and DMF. It has been demonstrated that the anionic form of the hydrazone-imine form is responsible for the high intense fluorescent peak. In addition, the acid-base equilibrium in between neutral and anionic form of hydrazone-imine form in buffer solution of varying pH was investigated and evaluated the pKa values of the dyes by making the use of UV-vis spectroscopic methods. The determined acid dissociation constant (pKa) values increase according to the sequence of 2>1>3>4. PMID:25594208

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

2015-04-01

190

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

NASA Astrophysics Data System (ADS)

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.

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

2013-12-01

191

Protection against hydrogen peroxide-mediated cytotoxicity in Friedreich's ataxia fibroblasts using novel iron chelators of the 2-pyridylcarboxaldehyde isonicotinoyl hydrazone class.  

PubMed

Iron-loading diseases remain an important problem because of the toxicity of iron-catalyzed redox reactions. Iron loading occurs in the mitochondria of Friedreich's ataxia (FA) patients and may play a role in its pathogenesis. This suggests that iron chelation therapy could be useful. We developed previously the lipophilic iron chelators known as the 2-pyridylcarboxaldehyde isonicotinoyl hydrazone (PCIH) ligands and identified 2-pyridylcarboxaldehyde 2-thiophenecarboxyl hydrazone (PCTH) as the most promising analog. Hence, this study assessed the efficacy of PCTH and other PCIH analogs compared with various chelators, including deferiprone and desferrioxamine (DFO). Age- and sex-matched control and FA fibroblasts were preincubated with iron chelators and subsequently challenged with 50 microM H2O2 for up to 24 h. The current study demonstrates an interesting structure-activity relationship among the closely related PCIH series of ligands, with only PCTH being highly effective at preventing H2O2-induced cytotoxicity. PCTH increased FA fibroblast cell viability by up to 70%, whereas DFO rescued viability by 1 to 5% only. Hence, PCTH, which was well tolerated by cells was far more effective than DFO at preventing oxidative stress. It is noteworthy that kinetic studies demonstrated PCTH to rapidly penetrate cells to induce 59Fe efflux, whereas DFO, PCIH, 2-pyridylcarboxaldehyde benzoyl hydrazone, and 2-pyridylcarboxaldehyde m-bromobenzoyl hydrazone were far slower, indicating it is the rate of chelator permeation that is crucial for protection against H2O2. In addition, PCTH was found to be as effective as or more effective than conventional radical scavengers or the antioxidant idebenone (which has undergone clinical trials) at protecting cells against H2O2-mediated cytotoxicity. These findings further indicate the potential of PCTH for treatment of iron overload. PMID:18424550

Lim, C K; Kalinowski, D S; Richardson, D R

2008-07-01

192

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

193

Medium effects on fluorescence of ciprofloxacin hydrochloride  

NASA Astrophysics Data System (ADS)

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

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

2003-10-01

194

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

PubMed

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

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

2014-01-01

195

Estimation of pioglitazone hydrochloride and metformin hydrochloride in tablets by derivative spectrophotometry and liquid chromatographic methods.  

PubMed

Two simple and accurate methods of analysis to determine pioglitazone hydrochloride (PIO) and mefformin hydrochloride (MET) in combined dosage forms were developed using second-derivative spectrophotometry and reversed-phase liquid chromatography (LC). PIO and MET in combined preparations (tablets) were quantified using the second-derivative responses at 227.55 nm for PIO and 257.25 nm for MET in spectra of their solutions in a mixture of methanol and acetonitrile (30 + 70). The calibration curves were linear [correlation coefficient (r) = 0.9984 for PIO and 0.9986 for MET] in the concentration range of 8-40 microg/mL for PIO and 4-12 microg/mL for MET. In the LC method, analysis was performed on a Hypersil ODS-C18 column with 5 microm particle size using the mobile phase acetonitrile-water-acetic acid (75 + 25 + 0.3), adjusted to pH 5.5 with liquor ammonia, at a flow rate of 0.5 mL/min. Measurement was made at a wavelength of 230 nm. Both the drugs were well resolved on the stationary phase, and the retention times were 8.5 min for PIO and 16.0 min for MET. The calibration curves were linear (r = 0.9933 for PIO and 0.9958 for MET) in the concentration range of 4-20 microg/mL for PIO and MET. Both methods were validated, and the results were compared statistically. They were found to be accurate, precise, and specific. The methods were successfully applied to the estimation of PIO and MET in combined tablet formulations. PMID:16152937

Shankar, Madhira B; Modi, Vaibhav D; Shah, Dimal A; Bhatt, Kashyap K; Mehta, Rajendra S; Geetha, Madhira; Patel, Binita J

2005-01-01

196

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

PubMed

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

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

2011-09-01

197

Recrystallization of erlotinib hydrochloride and fulvestrant using supercritical antisolvent process  

Microsoft Academic Search

Recrystallization of two anti-cancer active pharmaceutical ingredients (APIs), erlotinib hydrochloride (erlotinib HCl) and fulvestrant, using supercritical antisolvent (SAS) process was investigated in this study. The most commonly used supercritical carbon dioxide was employed as the antisolvent. Effect of three process parameters including the operating temperature, pressure and solution flow rate have been studied. Analyses of the recrystallized erlotinib HCl and

Yao-Chun Tien; Chie-Shaan Su; Ling-Hsiao Lien; Yan-Ping Chen

2010-01-01

198

Stability of midazolam hydrochloride in extemporaneously prepared flavored gelatin.  

PubMed

The stability of midazolam hydrochloride in flavored gelatin was evaluated after storage at 4 degrees C for 14 days and at -20 degrees C for 28 days. A flavored liquid gelatin mixture was prepared and mixed with midazolam hydrochloride injection in final concentrations of midazolam 1 and 2 mg/mL. Gelatin cups containing 5 and 15 mg of midazolam were prepared by measuring appropriate volumes of the gelatin stock solutions and were stored in a refrigerator at 4 degrees C or in a freezer at -20 degrees C. Immediately after preparation and at 7 and 14 days, three refrigerated and three frozen gelatin samples of each midazolam concentration were visually inspected, tested for pH, and assayed for midazolam concentration by high-performance liquid chromatography. The frozen gelatin samples were also evaluated at 21 and 28 days; three whole and three partial gelatin samples were assayed for midazolam content to determine the uniformity of drug distribution within each sample. All samples maintained greater than 96% of the initial midazolam concentration throughout the study. There was no appreciable change in color, odor, or pH. The midazolam content of the gelatin in the cups was uniform. An extemporaneously compounded preparation of midazolam hydrochloride in flavored gelatin was stable when stored for 14 days at 4 degrees C and for 28 days at -20 degrees C. Distribution of midazolam hydrochloride in the gelatin was uniform. PMID:8442465

Bhatt-Mehta, V; Johnson, C E; Kostoff, L; Rosen, D A

1993-03-01

199

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

200

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

201

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

PubMed

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

202

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

PubMed

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

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

2014-01-01

203

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

PubMed

The antitumor property of iron chelators and aromatic nitrogen mustard derivatives has been well documented. Combination of the two pharmacophores in one molecule in drug designation is worth to be explored. We reported previously the syntheses and preliminary cytotoxicity evaluation of benzaldehyde nitrogen mustard pyridine carboxyl acid hydrazones (BNMPH) as extended study, more tumor cell lines (IC50 for HepG2: 26.1 ± 3.5 ?M, HCT-116: 57.5 ± 5.3 ?M, K562: 48.2 ± 4.0 ?M, and PC-12: 19.4 ± 2.2 ?M) were used to investigate its cytotoxicity and potential mechanism. In vitro experimental data showed that the BNMPH chelating Fe(2+) caused a large number of ROS formations which led to DNA cleavage, and this was further supported by comet assay, implying that ROS might be involved in the cytotoxicity of BNMPH. The ROS induced changes of apoptosis related genes, but the TFR1 and NDRG1 metastatic genes were not obviously regulated, prompting that BNMPH might not be able to deprive Fe(2+) of ribonucleotide reductase. The BNMPH induced S phase arrest was different from that of iron chelators (G1) and alkylating agents (G2). BNMPH also exhibited its inhibition of human topoisomerase II?. Those revealed that the cytotoxic mechanism of the BNMPH could stem from both the topoisomerase II inhibition, ROS generation and DNA alkylation. PMID:24995306

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

2014-01-01

204

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

PubMed Central

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

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

2012-01-01

205

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

206

Isoniazid is not a lead compound for its pyridyl ring derivatives, isonicotinoyl amides, hydrazides, and hydrazones: a critical review.  

PubMed

The relationships between structure, disintegration and antituberculotic in vitro activity were studied for over 200 derivatives of isonicotinic acid hydrazide (isoniazid, INH). Conclusive evidence reflects that many compounds do not withstand the in vitro conditions. A pH dependant partial hydrolysis to INH occurs in the case of hydrazones, in analogy to well-known benzoic acid esters. Hydrazides and amides are cleaved into isonicotinic acid. In general, antimycobacterial potencies drop against INH except for two outliers probably with additional unspecific toxicity of their residues. Analyzing the complexity and heterogeneity of molecular events, trends linked to hydrolysis are found when structural features are clustered. Hammett sigma constants correlate to pK(a) values possessing a twofold descriptive meaning: (i) the cardinal increase of partial positive charge of the reaction center towards nucleophilic water attack and (ii) the ionization crucial for mycobacterial cell permeation through porins or lipid barriers. We review the literature concluding that many so-called "novel leads" are nothing else than precursors of an INH-based scaffold. In addition, INH ring-substitution or analogous backbones never achieve the efficiency of INH, itself a prodrug, which accumulates in Mycobacterium tuberculosis in form of its intrabacterial active principle(s) to which it is an optimal transport vehicle, evidencing that INH is not a promising lead compound at all. PMID:16918349

Scior, T; Garcés-Eisele, S J

2006-01-01

207

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

208

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) Å, b=9.1540(2) Å, c=10.87500(10) Å and V=797.88(3) Å(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

209

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

210

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

PubMed

The impact of zilpaterol hydrochloride (ZH) on carcass yield, composition, and tenderness was evaluated using 384 beef steers in a randomized complete block design. Main effects were the addition of 0 or 8.3 mg/kg of ZH for the final 20 d of feeding and each inclusion level was paired with withdrawal periods of 3, 10, 17, or 24 d. The 2 animals with BW closest to the pen average were selected for carcass fabrication to determine carcass yield, composition, and tenderness. The carcasses from animals fed ZH had greater (P = 0.008) individual side weights. Carcass fat determinations were unchanged (P = 0.70) by ZH. Weights of the strip loin (P = 0.01), peeled tenderloin (P = 0.02), and top sirloin butt (P < 0.001) were all improved with ZH. When expressed as a proportion of carcass weight, ZH increased percentage of carcass in the top sirloin butt (P = 0.006), bottom sirloin tri-tip (P = 0.02), top inside round (P = 0.002), bottom round flat (P = 0.001), and flank steak (P = 0.02). A longer withdrawal time (WT) increased (P < 0.001) carcass weights. Shoulder clod weights were greatest (P < 0.001) with 17-d WT from ZH, whereas chuck roll weights were greatest (P = 0.02) at 17 and 24 d of WT. Peeled tenderloins, top sirloin butts, and eye of rounds responded to WT, with increased (P < 0.001) weights seen at 10 d of WT as compared with all other WT. Shear force values were greater at each of the 3 aging times, 7 d (P < 0.001), 14 d (P < 0.001), and 21 d (P = 0.003), in steaks from ZH-fed steers compared with control steers. Protein percentages were greater in ZH steaks (P = 0.03) and ZH ground beef trim (P < 0.001). Percent moisture was increased (P < 0.001) in strip loin steaks at 3 and 10 d WT. Ground beef trim had an increase (P = 0.04) in percent moisture and a decrease (P = 0.01) in percent fat at 10 d WT. Carcass weights and yields were improved with ZH feeding and may continue to improve even up to 10 d after withdrawal of the supplement. Tenderness was slightly reduced with ZH supplementation but was unaffected by WT. Zilpaterol hydrochloride can be a valuable supplement to finishing beef steers to improve carcass lean yields and composition. PMID:19684279

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

2009-11-01

211

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

Microsoft Academic Search

Literature data related to the Biopharmaceutics Classification System (BCS) are presented on verapamil hydrochloride, propranolol hydrochloride, and atenolol in the form of BCS-monographs. Data on the qualitative composition of immediate release (IR) tablets containing these active substances with a Marketing Authorization (MA) in the Netherlands (NL) are also provided; in view of these MA's the assumptionwasmadethatthesetabletswerebioequivalenttotheinnovatorproduct.The

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

2004-01-01

212

1H, 13C, NH, HH, CH COSY, HH NOESY NMR and UV-vis studies of Solophenyl red 3BL dye azo-hydrazone tautomerism in various solvents.  

PubMed

Azo-hydrazone tautomeric behavior of polyazo Solophenyl red 3BL (C.I. Direct 80) dye in different solvents (water, methanol and DMSO) was investigated using 1H, 13C, NH, HH, CH COSY, HH NOESY NMR techniques and UV-vis spectroscopy. Two-dimensional NMR experiments were used to assign 1H, 13C and 15N NMR lines unambiguously. Results showed that the hydrazone-form proton NMR signal appeared in the weakest field with respect to tetramethylsilane, in comparison with the amide and phenolic proton NMR signals. UV-vis absorption spectroscopic evidences showed that azo-hydrazone mixture exists in water and DMSO solvents, but in methanol, only azo tautomer was dominant, which was in a good agreement with NMR spectroscopic results. PMID:16406789

Hassanzadeh, A; Zeini-Isfahani, A; Habibi, M H; Heravi, M R A Poor; Abdollahi-Alibeik, M

2006-02-01

213

Chemical stabilities of famotidine and ranitidine hydrochloride in intravenous admixtures.  

PubMed

The chemical stabilities of famotidine and ranitidine hydrochloride solutions in 5% dextrose and 0.9% sodium chloride injections have been studied using high-performance liquid chromatographic methods (HPLC). Both the drugs were stable for at least 15 days (loss in potency of less than 10%) at 25 degrees C and 63 days at 5 degrees C. Both drugs were comparatively less stable in 5% dextrose injection than in 0.9% sodium chloride injection. The loss in the potency of phenol, which is added as a preservative to ranitidine hydrochloride injection, was significant in both the vehicles. However, the addition of preservative in a single dose vial is not considered necessary. PMID:3230097

Das Gupta, V; Parasrampuria, J; Bethea, C

1988-10-01

214

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

PubMed

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

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

2008-09-01

215

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

PubMed

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

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

2013-12-01

216

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

NASA Astrophysics Data System (ADS)

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

Ferreira, Ivania R.; Ando, Rômulo A.

2012-01-01

217

Psychosedation with dexmedetomidine hydrochloride during minor oral surgery.  

PubMed

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

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

2009-01-01

218

Optic nerve vasomotor effects of topical apraclonidine hydrochloride.  

PubMed Central

AIMS: To examine, in vivo, the anterior optic nerve vasomotor effects of chronic apraclonidine hydrochloride in rabbits. METHODS: After local treatment in one randomly chosen eye with apraclonidine hydrochloride 0.5% over 21 days, the microvasculature of the optic nerve was examined in five rabbits using an intraluminal microvascular corrosion casting technique. The investigators were masked as to which eye was treated. The vasoconstriction near the branching point of arterioles supplying the optic nerve was calculated as a percentage of the downstream vessel calibre. An average constriction was calculated and compared between the treated and the contralateral, untreated, eyes by means of a two tailed t test for paired variables. Constriction values of a total of 72 arterioles supplying the optic nerve were obtained for the five rabbits. RESULTS: The average constriction in the treated and the control eyes was comparable (p = 0.96). CONCLUSION: Chronic administration of apraclonidine hydrochloride 0.5% produces no observable optic nerve vasomotor effects in the rabbit eye. Images PMID:8664240

Orgül, S; Bacon, D R; Van Buskirk, E M; Cioffi, G A

1996-01-01

219

Torsionally responsive C3-symmetric azo dyes: azo-hydrazone tautomerism, conformational switching, and application for chemical sensing.  

PubMed

An efficient triple azo coupling reaction between anilines and phloroglucinol furnished a series of C(3)-symmetric molecules 7-9 supporting multiple conjugation pathways that converge at the molecular core. A combination of (1)H/(13)C NMR spectroscopy, X-ray crystallography, and density functional theory computational studies provided a coherent picture of the [n,pi]-conjugated molecular core, which is best described as the tris(hydrazone) [rather than tris(azo)] tautomer stabilized by resonance-assisted hydrogen bonding. For a homologous series of compounds, an increase in the torsional angles between the planar molecular core and the peripheral aryl groups results in a systematic blue shift in the low-energy electronic transitions (7, 523 nm; 8, 505 nm; 9, 445 nm in CHCl(3)) that qualitatively correlates with the shrinkage of effective conjugation through structural distortion. Similar spectral shifts could also be induced by amine substrates that interact with the intramolecular hydrogen-bonding network to trigger bond-twisting motions. Specifically, a brief exposure of a thin film of 7 to vapor samples of butyl-, hexyl-, diethyl-, and diisopropylamine resulted in a rapid and reversible color change from pink to dark-orange. Under similar conditions, however, triethylamine did not elicit any detectable color change, despite the fact that it has a significantly higher vapor pressure than n-hexylamine. These findings implicate that the hydrogen-bonding donor ability is a key requirement for the binding-induced conformational switching, which allows for direct naked-eye detection of volatile amines under ambient conditions. PMID:20698548

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

2010-09-01

220

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

Microsoft Academic Search

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

Nicholas J. Gales; Harry R. Burton

221

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

Code of Federal Regulations, 2011 CFR

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

2011-07-01

222

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

223

Formulation of a new polymeric film of Propranolol hydrochloride using Psyllium as a natural polymer  

Microsoft Academic Search

Objective: Propranolol hydrochloride is a widely used beta blocker agent which is administered 3 times daily due to its short half life. The aim of this study was to design and evaluate polymeric film of propranolol hydrochloride using psyllium seed's mucilage as a natural occurring substance in order to deliver the active agent in a controlled manner. Methods: In this

224

76 FR 20685 - Determination That NOVANTRONE (Mitoxantrone Hydrochloride) Injection, Equivalent to 25 Milligrams...  

Federal Register 2010, 2011, 2012, 2013, 2014

...hydrochloride) Injection, equivalent to (EQ) 25 milligrams (mg) base/12.5 milliliters (mL) and EQ 30 mg base/15 mL, was not withdrawn from...mitoxantrone hydrochloride) Injection, EQ 25 mg base/ 12.5 mL and EQ 30 mg...

2011-04-13

225

Controlled release of lidocaine hydrochloride from the surfactant-doped hybrid xerogels  

Microsoft Academic Search

We investigate the controlled release of lidocaine hydrochloride from the doped silica-based xerogels. In the xerogel preparation, tetraethoxysilane (TEOS), methyltriethoxysilane (MTES), and propyltriethoxysilane (PTES) are used as precursors, and a nonionic surfactant Igepal CO 720 is used as a dopant. The experimental results suggest that the release of lidocaine hydrochloride can be easily controlled by partially substituting TEOS with the

Zhijian Wu; Hyeonwoo Joo; Tai Gyu Lee; Kangtaek Lee

2005-01-01

226

[Comparative in vitro antibacterial activity of polyhexamethylene guanidine hydrochloride and polyhexamethylene guanidine succinate].  

PubMed

Eye infection is one of the temporary invalidity causes that can lead to blindness. The former antibacterial components of eye drops were polyhexamethylene guanidine hydrochloride and polyhexamethylene guanidine phosphate. Polyhexamethylene guanidine in the form of form of succinate with preserved activity and lover toxicity is described. The antibacterial activity spectra of polyhexamethylene guanidine succinate and polyhexamethylene guanidine hydrochloride were comparatively estimated. PMID:24640138

Kha, Kam An'; Grammatikova, N É; Vasilinko, I A; Kedik, S A

2013-01-01

227

Sustained release of verapamil hydrochloride from sodium alginate microcapsules.  

PubMed

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

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

2010-04-01

228

Porphyria-like cutaneous changes induced by tetracycline hydrochloride photosensitization.  

PubMed

Five patients manifested cutaneous changes indistinguishable from those noted in some porphyric disorders, consisting of fragility, denudation, and blister formation of sun-exposed skin. Microscopical examination showed subepidermal bulla formation and the desposition of PAS-positive, diastase-resistant material and IgG in or around the upper dermal blood vessel walls. There was also electron microscopical evidence of vascular basal lamina reduplication and the deposition of a fine fibrillar material in and around these vessels. However, no abnormal porphyrin formation was noted. All five patients had been receiving 250 mg of tetracycline hydrochloride twice a day for at least six months and had had extensive sun exposure prior to the onset of the condition. For four patients, discontinuing the medication led to complete remission, despite subsequent sun exposure; the fifth patient was much improved, but her skin was still somewhat fragile seven months later. We concluded that these cutaneous changes resulted from a low-grade photosensitization by tetracycline hydrochloride. PMID:132139

Epstein, J H; Tuffanelli, D L; Seibert, J S; Epstein, W L

1976-05-01

229

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride.  

PubMed

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

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

2011-06-01

230

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

231

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

PubMed Central

Evaluation of monoclonal antibody (MAb) fragments (e.g. Fab?, Fab or engineered fragments) as cancer-targeting reagents for therapy with the ?-particle emitting radionuclide astatine-211 (211At) has been hampered by low in vivo stability of the label and a propensity of these proteins localize to kidneys. Fortunately, our group has shown that the low stability of the 211At label, generally a meta- or para-[211At]astatobenzoyl conjugate, on MAb Fab? fragments can be dramatically improved by use of closo-decaborate(2-) conjugates. However, the higher stability of radiolabeled MAb Fab? conjugates appears to result in retention of the radioactivity in kidneys. This investigation was conducted to evaluate whether the retention of radioactivity in kidney might be decreased by the use of acid-cleavable hydrazone between the Fab? and the radiolabeled closo-decaborate(2-) moiety. Five conjugation reagents containing sulfhydryl-reactive maleimide groups, a hydrazone functionality and a closo-decaborate(2-) moiety were prepared. In four of the five conjugation reagents, a discrete polyethylene glycol (PEG) linker was used, and one substituent adjacent to the hydrazone was varied (phenyl, benzoate, anisole or methyl) to provide varying acid-sensitivity. In the initial studies, the five maleimido-closo-decaborate(2-) conjugation reagents were radioiodinated (125I or 131I), then conjugated with an anti-PSMA Fab? (107-1A4 Fab?). Biodistributions of the five radioiodinated Fab? conjugates were obtained in nude mice at 1, 4 and 24 h post injection (pi). In contrast to closo-decaborate(2-) conjugated to 107-1A4 Fab? through a non-cleavable linker, two conjugates containing either a benzoate or a methyl substituent on the hydrazone functionality displayed clearance rates from kidney, liver and spleen that were similar to those obtained with directly radioiodinated Fab? (i.e. no conjugate). The maleimido-closo-decaborate(2-) conjugation reagent containing a benzoate substituent on the hydrazone was chosen for study with 211At. That reagent was conjugated with 107-1A4 Fab?, then labeled (separately) with 125I and 211At. The radiolabeled Fab? conjugates were coinjected into nude mice bearing LNCaP human tumor xenografts, and biodistribution data was obtained at 1, 4 and 24 h pi. Tumor targeting was achieved with both 125I- and 211At-labeled Fab?, but the 211At-labeled Fab? reached a higher concentration (25.56 ± 11.20 vs. 11.97 ± 1.31 %ID/g). Surprisingly, while the 125I-labeled Fab? was cleared from kidney similar to earlier studies, the 211At-labeled Fab? was not (i.e. kidney conc. for 125I vs. 211At; 4h: 13.14 ± 2.03 ID/g vs. 42.28 ± 16.38 %D/g, 24h: 4.23 ± 1.57 ID/g vs. 39.52 ± 15.87 %ID/g). Since the Fab? conjugate is identical in both cases except for the radionuclide, it seems likely that the difference in tissue clearance seen is due to an effect that 211At has on either the hydrazone cleavage or on the retention of a metabolite. Results from other studies in our laboratory suggest that the latter case is most likely. The hydrazone linkers tested do not provide the tissue clearance sought for 211At, so additional hydrazones linkers will be evaluated. However, the results support the use of hydrazone linkers when Fab? conjugated with closo-decaborate(2-) reagents are radioiodinated. PMID:21513347

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

2011-01-01

232

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

233

Spectroscopic approach in the characterization of the copper(II) complexes of isatin-3,2'-quinolyl-hydrazones and their adducts  

NASA Astrophysics Data System (ADS)

Copper(II) complexes of isatin-3,2'-quinolyl-hydrazones of the type [Cu(L)X] (where X = Cl -, Br -, NO 3-, CH 3COO - and ClO 4-] and their adducts Cu(L)X.2Y [where Y = pyridine or dioxane and X = Cl -, Br -, NO 3- and ClO 4-] have been synthesized under controlled experimental conditions and characterized by using the modern spectroscopic and physicochemical techniques viz. IR, electronic, EPR, elemental analysis, magnetic moment susceptibility measurements and molar conductance, etc. On the basis of spectral studies a four coordinated square planer geometry is assigned for Cu(L)X type complexes whereas the adducts (Cu(L)X.2Y were found to have a six coordinated octahedral geometry.

Gupta, Lokesh Kumar; Bansal, Usha; Chandra, Sulekh

2006-10-01

234

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

PubMed

Simple, rapid, sensitive, precise and accurate spectrophotometeric methods for the determination of ephedrine hydrochloride (E-HCl) and bromhexine hydrochloride (Br-HCl) in bulk samples, dosage form and in spiked urine samples were investigated. The methods are based on the formation of a yellow colored ion-associates due to the interaction between the examined drugs with picric acid (PA), chlorophyllin coppered trisodium salt (CLPH), alizarin red (AR) and ammonium reineckate (Rk) reagents. A buffer solution had been used and the extraction was carried out using organic solvent, the ion associates exhibit absorption maxima at 410, 410, 430 and 530 nm of (Br-HCl)with PA, CLPH, AR and Rk respectively; 410, 410, 435 and 530 of (E-HCl) with PA, CLPH, AR and Rk respectively. (E-HCl) and (Br-HCl) could be determined up to 13, 121, 120 and 160; 25, 200, 92 and 206 ?g mL(-1), using PA, CLPH, AR and Rk respectively. The optimum reaction conditions for quantitative analysis were investigated. In addition, the molar absorptivity, Sandell sensitivity were determined for the investigated drug. The correlation coefficient was ?0.995 (n=6) with a relative standard deviation (RSD) ?1.15 for five selected concentrations of the reagents. Therefore the concentration of Br-HCl and E-HCl drugs in their pharmaceutical formulations and spiked urine samples had been determined successfully. PMID:23624039

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

2013-07-01

235

Anti-influenza A virus activity of amantadine hydrochloride and rimantadine hydrochloride in ferret tracheal ciliated epithelium.  

PubMed Central

The activities and toxicities of amantadine hydrochloride and rimantadine hydrochloride against influenza A/Alaska/6/77 (H3N2) and A/Bangkok/1/79 (H3N2) viruses were compared in organ cultures and ferret tracheal ciliated epithelium. Pretreatment of cultures with concentrations (0.5 and 1 micrograms/ml) comparable to those found in human serum after oral administration of amantadine revealed that rimantadine produced significantly longer protection than amantadine against virus-induced cytopathic effects. Correspondingly, rimantadine produced a comparable protective effect at four- to eight-fold-lower concentrations than amantadine. Both drugs produced increasing and similar effects at higher concentrations, which were comparable to those reported in nasal washings after aerosol administration of amantadine. At the concentrations tested, amantadine was nontoxic. However, at concentrations of 16 and 32 micrograms/ml, rimantadine was toxic to the ciliated epithelium after 10 to 21 days of continuous exposure. When the drugs were added 24 h or more after infection, protection against cytopathic effects decreased markedly. Both drugs moderately suppressed virus production at concentrations of 0.5 to 16 micrograms/ml. However, no dose response or difference between the drugs was observed. Because of comparable antiviral activity at lower concentrations and greater activity at similar concentrations, rimantadine may be more useful than amantadine for oral prophylaxis and therapy of influenza. PMID:7103458

Burlington, D B; Meiklejohn, G; Mostow, S R

1982-01-01

236

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

NASA Astrophysics Data System (ADS)

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

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

2013-07-01

237

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

PubMed

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

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

2010-01-01

238

Polymer conjugates of doxorubicin bound through an amide and hydrazone bond: Impact of the carrier structure onto synergistic action in the treatment of solid tumours.  

PubMed

In this study, we describe the synthesis, physico-chemical characterisation and results of the in vitro and in vivo evaluation of the biological behaviour of N-(2-hydroxypropyl)methacrylamide-based (HPMA) copolymer conjugates bearing doxorubicin (DOX) partly bound via a pH-sensitive hydrazone and partly via enzymatically degradable amide bonds, each contributing to a different anti-tumour mechanism of action of the polymer-doxorubicin conjugate. The following two types of HPMA copolymer drug carriers designed for passive tumour targeting were synthesised and compared: the linear non-degradable copolymer and the biodegradable high-molecular-weight (HMW) diblock copolymer. The HMW diblock copolymer carrier containing a degradable disulphide bond between the polymer blocks showed a rapid degradation in a buffer containing glutathione within the first few hours of incubation. In contrast to the conjugate with the amide bond-bound DOX requiring the presence of lysosomal enzymes to release DOX, the polymer-drug conjugate with the DOX bound via a hydrazone bond released DOX by pH-sensitive hydrolysis, which was significantly faster in a buffer of pH 5.0 (intracellular pH) than pH 7.4, mimicking the conditions in the bloodstream. The significant and comparable in vivo anti-tumour activity of the diblock HMW conjugate and an equimolar mixture of the conjugates differing in the DOX attachment method along with the development of cancer resistance during treatment with these conjugates demonstrated the high potential of these compounds in the development of new nanomedicines suitable for the treatment of solid tumours. PMID:24632485

Etrych, Tomáš; Subr, Vladimír; Laga, Richard; Ríhová, Blanka; Ulbrich, Karel

2014-07-16

239

[Pharmacological effects of nalfurafine hydrochloride, a kappa-opioid receptor agonist].  

PubMed

Nalfurafine hydrochloride, a kappa-opioid receptor agonist, was approved in January 2009 and released to the market on March 2009 for the indication of "Improvement of pruritus in hemodialysis patients (only for cases resistant to conventional treatments)" in Japan (Brand Name: REMITCH CAPSULES 2.5 microg, Marketing Authorization Holder: Toray Industries, Inc., Distributed by Torii Pharmaceutical Co., Ltd., Co-developed by Japan Tobacco Inc.). In addition to antipruritic effect, nalfurafine hydrochloride showed ameliorating effects on pain, neuropathic pain, drug dependence, schizophrenia and dyskinesia in non-clinical studies. Therefore, nalfurafine hydrochloride may become a useful therapeutic agent for their diseases. PMID:21226314

Nakao, Kaoru; Hasebe, Ko; Yoshikawa, Satoru; Ikeda, Ken; Hirakata, Mikito; Miyamoto, Yohei; Mochizuki, Hidenori

2010-11-01

240

Determination of impurities in medical products containing metformin hydrochloride.  

PubMed

The object of this study was to present a high-performance liquid chromatography (HPLC) method allowing to identify and quantify the impurities in medical products in which the only active substance is metformin hydrochloride. Metformin (dimethylbiguanide) is a biguanide derivative active after oral administration. It reduces the basic and postprandial blood glucose levels in patients with type II diabetes (insulin-independent), with partially maintained insulin secretion. The separation of the impurities was performed using a PARTISPHER SCX column and a spectrophotometric detector (lambda = 218 nm). The mobile phase was 1.7% (w/v) ammonium dihydrogen phosphate water solution, with pH adjusted to 3.1 using 85% orthophosphoric acid. The proposed method is rapid, sensitive and selective, and it can be used to evaluate those medical products for which the impurity tests are not currently performed, as well as those for which only cyanoguanidine or cyanoguanidine and melamine assays are performed. PMID:21229873

K?aczkow, Gabriela; Anuszewska, Elzbieta L

2010-01-01

241

Rosiglitazone maleate + metformin hydrochloride extend: review of an emerging compound.  

PubMed

Clinical practice guidelines from around the world have continued to highlight the importance of glycemic control in the prevention of diabetes complications. Despite the many tools available to achieve these targets, it remains a constant challenge for healthcare providers and patients alike. Rosiglitazone maleate + metformin hydrochloride extend is a new compound that has the advantage of the clinical experience and knowledge about the current version and the added benefit of being a once daily, single pill option. The existing version of rosiglitazone + metformin has been shown to effectively lower hemoglobin A1C, improve insulin sensitivity and minimize weight gain. It is expected that the new compound will also have similar features, with the added benefit of improved patient adherence given its once daily formulation. PMID:19642952

Cheng, Alice Yy; Josse, Robert G

2009-09-01

242

[Thermosensitive in situ gel of boanmycin hydrochloride for injection].  

PubMed

Poloxamer F127, poloxamer F68 and hydroxypropyl methylcellulose K4M were used to prepare the thermosensitive in situ gel of boanmycin hydrochloride for injection. Its gelation temperature, rheological behavior, texture characteristics, scanning electron microscopy, in vitro and in vivo drug release were evaluated. These results showed that the formulation was a fluid solution at room temperature, which could become semisolid at the temperature of 37 degrees C, and the thermally induced sol-gel transition allowed to be injectable and in situ setting. The formulation was constructed into a tridimensional network at gelation temperature. The drug release was controlled by the diffusion of the drug and the erosion of the gelmatrix. The pharmacokinetics indicated that the drug could be released slowly for up to 48 hours after subcutaneous administration in rats. PMID:21882536

Ding, Wei-Ming; Li, Mei; Li, Gui-Ling; Xu, Hong-Zhang; Chen, Ru-Xian

2011-06-01

243

Polymer based solutions of bupranolol hydrochloride for intranasal systemic delivery.  

PubMed

The present study was aimed at developing intranasal polymer based solutions as alternative route for systemic delivery of Bupranolol hydrochloride (BPH). It is a potent ?-blocker drug which upon oral administration undergoes extremely high hepatic first-pass metabolism (>90% in humans). The polymeric solutions were prepared using varying concentrations of polymers like sodium alginate, chitosan, sodium carboxymethylcellulose, methylcellulose (MC), polyvinyl alcohol, carbopol, hydroxypropyl MC, and hydroxypropyl cellulose. The prepared formulations were evaluated in terms of pH of the solution, angular viscosity, drug content, gel strength, gelation temperature, in vitro drug release, in vivo pharmacodynamic studies, histopathological, and stability studies. Except MC based solutions, a biphasic pattern of drug release was obtained in all other cases. Nasal administration of selected batches of polymeric solutions were found to be nontoxic and were able to improve drug bioavailability when compared to oral, nasal, and intravenous solution administrations of BPH. PMID:20550434

Mishra, Brahmeshwar; Sankar, C; Mishra, Madhusmita

2011-04-01

244

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

245

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

246

A phosphate binding assay for sevelamer hydrochloride by ion chromatography.  

PubMed

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

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

1999-05-01

247

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

248

Prolonged and multiple immobilizations of the southern elephant seal using ketamine hydrochloride-xylazine hydrochloride or ketamine hydrochloride-diazepam combinations.  

PubMed

Thirty seven southern elephant seals (Mirounga leonina) were singularly or repeatedly immobilized with combinations of ketamine hydrochloride (HCl) and xylazine HCl or ketamine HCl and diazepam. Atropine sulphate was included in the drug combinations. To permit experimental procedures the seals were immobilized for periods of 30-330 min. The mean induction dose of ketamine HCl was 8.71 +/- 0.25 mg/kg (mean +/- SE). The mean induction time was 16.02 +/- 2.62 min. For the elephant seals immobilized for periods in excess of 180 min, the mean dose of ketamine HCl used per hr was 3.31 +/- 0.13 mg/kg/hr and the mean dose of ketamine HCl used per hr postinduction was 1.31 +/- 0.15 mg/kg/hr. The mean dose of diazepam used was 0.09 +/- 0.01 mg/kg and the mean dose of xylazine HCl was 0.41 +/- 0.01 mg/kg. Elephant seals were weighed on 20 occasions (weight range: 897-1,932 kg) and the relationship between standard length and weight was found to be: Weight = 9.98 length - 2,317.63 (r2 = 0.724). Adverse reactions to seals immobilized only once or twice were not observed. Two seals immobilized on three occasions developed abscesses at the site of injection. PMID:3682087

Gales, N J; Burton, H R

1987-10-01

249

Formulation and evaluation of verapamil hydrochloride loaded solid lipid microparticles.  

PubMed

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

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

2011-01-01

250

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

Code of Federal Regulations, 2013 CFR

...form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The resin sample being analyzed must contain enough...hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of the polymeric...

2013-07-01

251

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

Code of Federal Regulations, 2012 CFR

...form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The resin sample being analyzed must contain enough...hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of the polymeric...

2012-07-01

252

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

Code of Federal Regulations, 2014 CFR

...form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The resin sample being analyzed must contain enough...hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of the polymeric...

2014-07-01

253

Doxapram Hydrochloride Aggravates Adrenaline-Induced Arrhythmias Accompanied by Bidirectional Ventricular Tachycardia  

PubMed Central

Objectives. Doxapram hydrochloride is a respiratory stimulant that has an inhibitory effect on myocardial IK1 potassium channels and is thought to increase membrane instability and excitability in myocardial cells. We examined the arrhythmogenic effects of doxapram hydrochloride in a rat model of halothane adrenaline-induced arrhythmia. Methods. Thirteen female Wistar rats (12–14 weeks old) were used in the study. Animals were anesthetized with inhalation of halothane to permit observation of the effects of doxapram hydrochloride on halothane adrenaline-induced arrhythmia. Time-dependent changes in ECG repolarization characteristics (QT, QTc, JTp, JT, and Tp-e intervals) were studied. Results. Doxapram hydrochloride itself did not induce arrhythmia but did induce bidirectional ventricular tachycardia after addition of adrenaline. Conclusion. Drug-induced impairment of intracellular Ca2+ regulation caused BVT in the absence of genetic abnormalities in proteins in the sarcoplasmic reticulum. PMID:24527224

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

2014-01-01

254

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

Federal Register 2010, 2011, 2012, 2013, 2014

...GlaxoSmithKline, and 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...

2012-02-21

255

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

PubMed

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

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

2013-03-01

256

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

257

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

Federal Register 2010, 2011, 2012, 2013, 2014

...Prilocaine Hydrochloride) Injection, 4%, Were Not Withdrawn From Sale for Reasons...CITANEST PLAIN (prilocaine HCl) Injection, 4%, were not withdrawn from sale for reasons...and 3%, and prilocaine HCl injection, 4%, if all legal and regulatory...

2012-03-19

258

21 CFR 524.1662a - Oxytetracycline hydrochloride and hydrocortisone spray.  

Code of Federal Regulations, 2013 CFR

...ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1662a Oxytetracycline hydrochloride and hydrocortisone spray. (a)...

2013-04-01

259

21 CFR 524.1662a - Oxytetracycline hydrochloride and hydrocortisone spray.  

Code of Federal Regulations, 2012 CFR

...ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS § 524.1662a Oxytetracycline hydrochloride and hydrocortisone spray. (a)...

2012-04-01

260

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

NASA Astrophysics Data System (ADS)

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

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

2008-03-01

261

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

PubMed

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

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

2008-03-01

262

Design and evaluation of 1- and 3-layer matrices of verapamil hydrochloride for sustaining its release  

Microsoft Academic Search

The present study was performed to design oral controlled delivery systems for the water-soluble drug, verapamil hydrochloride,\\u000a using natural and semisynthetic polymers as carriers in the forms of 1- and 3-layer matrix tablets. Verapamil hydrochloride\\u000a 1-layer matrix tablets containing hydroxypropylmethylcellulose, tragacanth, and acacia either alone or mixed were prepared\\u000a by direct compression technique. 3-layer matrix tablets were prepared by compressing

Mohammad Reza Siahi; Mohammad Barzegar-Jalali; Farnaz Monajjemzadeh; Fatemeh Ghaffari; Shirzad Azarmi

2005-01-01

263

Influence of Zilpaterol Hydrochloride on Growth and Carcass Characteristics of Pelibuey Lambs  

Microsoft Academic Search

Salinas-Chavira, J., Ramirez, R.G., Domínguez-Muñoz, M., Palomo-Cruz, R. and López-Acuña, V.H. 2004. Influence of zilpaterol hydrochloride on growth and. carcass characteristics of lambs. J. Appl. Anim. Res., 26: 13–16.To evaluate the effect of different doses of the feed additive ?-agonist, zilpaterol hydrochloride (ZH) on performance and carcass characteristics of lambs, twelve intact male Pelibuey lambs (28.7±2.7 kg) were kept in

J. Salinas-Chavira; R. G. Ramirez; M. Domínguez-Muñoz; R. Palomo-Cruz; V. H. López-Acuña

2004-01-01

264

Antitumor activity and cross-resistance of carmethizole hydrochloride in preclinical models in mice  

Microsoft Academic Search

Carmethizole hydrochloride [1-methyl-2-methylthio-4,5-bis(hydroxymethyl)imidazole-4',5'-bis(N-methylcarbamate)hydrochloride, NSC 602 668; hereafter called carmethizole] is a new antitumor drug that has shown relatively broad activity in initial evaluations against several murine tumors and human tumor xenografts in vivo. The present studies were designed to address questions about carmethizole's activity against established disease, its activity on different treatment schedules, and the extent of its cross-resistance with

William R. Waud; Jacqueline Plowman; Steadman D. Harrison; Donald J. Dykes; Wayne K. Anderson; Daniel P. Griswold

1992-01-01

265

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

E-print Network

of the requirements for the degree of NASTER OF SCIENCE August 1962 Na]or Sub)ect: Chemistry A STUDY OF THE REACTION BETMEEN ANTINONY (V) CHLORIDE AND ORGANIC ANINE HYDROCHLORIDES A Thesis by Harold Dean Bier Approved as to style and content by& (Chairm.... Isopropylammonibmhexachloroantimonate (v) INTRODUCTION A literature review indicates that comparatively few compounds have been made by reacting an amine hydrochloride with antimony (V) in concentrated hydrochloric acid solution. Weinland ' ' and co-authors have published a series...

Bier, Harold Dean

1962-01-01

266

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

E-print Network

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

Linder, Donald Ernst

1964-01-01

267

An analytical chemical study of pilocarpine hydrochloride and its hydrolysis products  

E-print Network

of the requirements i' or the degree of MASTER OF SCIENCE August, 1956 Major Su'bject: Chemilstry AK AEALYTICAL CHEMICAL STUDY GF PILOCARPINE HYDROCHLORIDE AND ITS HYDROLYSIS PRODUCTS EDWARD R, IBERT APPROVED AS TO STYLE AED CONTEND BY: Chairman of Committee...'e. . . . . . ~ ~ . 20 22 lII. ? Hydrolysis of commercial preparations versus shelf life in months. o ~ ~ ~ 25 Chapter I Introduction Pilocarpine is a medicinal alkaloid. . Pilocarpine hydrochloride is an official entry in the U. S. P. (United States Pharmacopeia...

Ibert, Edward R

1956-01-01

268

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

SciTech Connect

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

Not Available

1980-01-01

269

STRESS DEGRADATION STUDIES ON MEBEVERINE HYDROCHLORIDE AND DEVELOPMENT OF A VALIDATED STABILITY INDICATING UPLC METHOD  

Microsoft Academic Search

A simple, economic, and time-efficient stability-indicating, reverse-phase ultra-performance liquid chromatographic (RP-UPLC) method has been developed for analysis of mebeverine hydrochloride in the presence of both impurities and degradation products generated by forced degradation. When mebeverine hydrochloride was subjected to acid hydrolytic, oxidative, base hydrolysis, photolytic, and thermal stress, degradation was observed only in base hydrolysis. The drug was found to

V. Srinivasan; H. Sivaramakrishnan; B. Karthikeyan; T. S. Balaji; S. Vijayabaskar

2011-01-01

270

Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation  

PubMed Central

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

Eassa, Bayoumy I; El-Shazly, Mohamed A

2013-01-01

271

Use of p-dimethylaminobenzalhyde as a colored reagent for determination of procaine hydrochloride by spectrophotometry.  

PubMed

Spectrophotometric determination of procaine hydrochloride is described. The procaine hydrochloride reacts with p-dimethylaminobenzalhyde in glacial acetic acid to form an Schiff base which is a yellow compound, and its maximum absorption wavelength is at 455nm, epsilon(455)=3.46x10(4). The absorbance for procaine hydrochloride from 0.2 to 15 mug ml(-1) obeys Beer's law. The linear regression equation of the calibration graph is C=5.866A-0.02, with a linear regression correlative coefficient is 0.9994 and relative standard deviation (RSD) of 1.7%; the detection limit is 0.1 mug ml(-1); recovery is from 92.0 to 110.0%. Effects of reaction medium, temperature, gentamycin, beneylpenicillin, kanamycin, streptomycin, foreign ions, and stand for time on the determination of procaine hydrochloride have been examined. The results obtained by this method agreed with those by the official method (dead-stop titration). This method is rapid and simple, and can be used for the determination of procaine hydrochloride in injection solution of procaine hydrochloride. PMID:18968059

Liu, L D; Liu, Y; Wang, H Y; Sun, Y; Ma, L; Tang, B

2000-09-01

272

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

273

Comparative effects of ractopamine hydrochloride and zilpaterol hydrochloride on growth performance, carcass traits, and longissimus tenderness of finishing steers.  

PubMed

Ractopamine hydrochloride (RAC) and zilpaterol hydrochloride (ZH) are beta-adrenergic agonists that improve growth performance and affect carcass characteristics. The objective of this study was to evaluate the comparative effects of RAC and ZH when fed to beef steers during the last 33 d of the finishing period. Three hundred crossbred beef steers (516 +/- 8 kg) were grouped by BW, BCS, and breed type and randomly assigned to 1 of 3 treatments (10 steers per pen; 10 pens per treatment). Treatments were control (no beta-agonists added), RAC (200 mg of ractopaminexhdx(-1)d(-1), for 33 d), or ZH (75 mg of zilpaterolxanimalx(-1)d(-1), for 30 d, removed 3 d for required withdrawal period). Steers were slaughtered, carcass characteristics were evaluated, and cut-out yields were determined. Both RAC and ZH increased final BW, ADG, feed efficiency (G:F), and HCW compared with controls (P < 0.05). Compared with RAC, ZH decreased ADG, ADFI, and final BW, but increased HCW and dressing percentage (P < 0.05). Carcass yield was not affected by RAC in this experiment, whereas ZH decreased adjusted fat thickness and KPH, increased ribeye area, improved yield grade, and increased cut-out yields, when compared with controls (P < 0.05). Marbling, lean maturity, and skeletal maturity were not different between treatments (P > 0.05). Steaks from RAC steers had greater (P < 0.05) Warner-Bratzler shear force (WBSF) values than steaks from control steers at 3 and 7 d of aging, but did not differ from controls after 14 d of aging. Steaks from ZH steers had greater WBSF values (P < 0.05) than steaks from controls and RAC steaks throughout the 21-d postmortem aging period. Although both beta-adrenergic agonists were effective at improving feedlot performance, RAC showed no negative effect on WBSF after 14 d, whereas WBSF values for ZH steaks were significantly greater than controls after 21 d. PMID:20042550

Scramlin, S M; Platter, W J; Gomez, R A; Choat, W T; McKeith, F K; Killefer, J

2010-05-01

274

Cardiovascular effects of dopamine hydrochloride and phenylephrine hydrochloride in healthy isoflurane-anesthetized New Zealand White rabbits (Oryctolagus cuniculus).  

PubMed

OBJECTIVE To determine the cardiopulmonary effects of progressively increasing infusion rates of dopamine hydrochloride and phenylephrine hydrochloride in healthy adult New Zealand White rabbits anesthetized with isoflurane. ANIMALS 6 New Zealand White rabbits. (Oryctolagus cuniculus). PROCEDURES Each rabbit was anesthetized on 2 occasions (? 2 weeks apart) with isoflurane in oxygen at 1.5 times the published isoflurane minimum alveolar concentration of 2.07%. Carotid artery and pulmonary artery catheters were placed. During each anesthetic episode, each rabbit received 5 progressively increasing doses of either dopamine (5, 10, 15, 20, or 30 ?g/kg/min) or phenylephrine (0.125, 0.25, 0.5, 1.0, and 2.0 ?g/kg/min). Blood gas and cardiopulmonary measurements were obtained after a 20-minute equilibration period prior to administration of the first drug dose (baseline) and after each subsequent dose administration. RESULTS Dopamine increased stroke index at the highest infusion rate of 30 ?g/kg/min; however, cardiac output and mean arterial blood pressure remained unchanged from baseline values. Administration of phenylephrine at a rate of 2 ?g/kg/min increased mean arterial blood pressure to 62 mm Hg from the baseline value of 45 mm Hg. This was a result of an increase in systemic vascular resistance with a concomitant decrease in heart rate and no change in cardiac output. Blood lactate concentration increased with time when rabbits received either treatment. CONCLUSIONS AND CLINICAL RELEVANCE Within the dose range of 5 to 30 ?g/kg/min, dopamine was not an effective treatment for isoflurane-induced hypotension in rabbits and phenylephrine was only minimally effective at a dose of 2 ?g/kg/min. PMID:25629908

Gosliga, Jaclyn M; Barter, Linda S

2015-02-01

275

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

276

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

PubMed

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. PMID:23680512

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

2013-08-01

277

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 37°C temperature with a water circulation jacket. The diffusion area of the skin was 1.77cm(2). The donor compartment was loaded with 1ml of the solution containing 2.5mg/ml of amlodipine besylate. The donor chamber was covered with parafilm to avoid evaporation. Passive diffusion across untreated porcine skin served as control. Aliquots were taken every 2h for 12h and analyzed by liquid chromatography-mass spectrometry. Transcutaneous flux of verapamil increased significantly from 8.75?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

278

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

279

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

PubMed Central

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

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

2011-01-01

280

Conformation and interactions of dopamine hydrochloride in solution  

NASA Astrophysics Data System (ADS)

The aqueous solution of dopamine hydrochloride has been investigated using neutron and X-ray total scattering data together with Monte-Carlo based modelling using Empirical Potential Structure Refinement. The conformation of the protonated dopamine molecule is presented and the results compared to the conformations found in crystal structures, dopamine-complexed protein crystal structures and predicted from theoretical calculations and pharmacophoric models. It is found that protonated dopamine adopts a range of conformations in solution, highlighting the low rotational energy barrier between different conformations, with the preferred conformation being trans-perpendicular. The interactions between each of the species present (protonated dopamine molecules, water molecules, and chloride anions) have been determined and are discussed with reference to interactions observed in similar systems both in the liquid and crystalline state, and predicted from theoretical calculations. The expected strong hydrogen bonds between the strong hydrogen bond donors and acceptors are observed, together with evidence of weaker CH hydrogen bonds and ? interactions also playing a significant role in determining the arrangement of adjacent molecules.

Callear, Samantha K.; Johnston, Andrew; McLain, Sylvia E.; Imberti, Silvia

2015-01-01

281

Controlled release tamsulosin hydrochloride from alginate beads with waxy materials.  

PubMed

The objective of this study was to develop oral controlled release delivery systems for tamsulosin hydrochloride (TSH) using alginate beads with various waxy materials, such as Compritol 888 ATO, Precirol ATO 5 and Gelucires. The beads were prepared from sodium alginate-waxy material-TSH slurry dropped onto calcium chloride to form spherical beads. The effects of the addition of various waxy materials to alginate beads on the drug encapsulation efficiency, bead size and morphology were investigated. The drug encapsulation efficiency significantly increased with the addition of waxy materials. The TSH-loaded alginate beads with and without waxy materials were almost spherical particles with an average diameter of 1.44 and 1.22 mm, respectively. In dissolution study, the TSH-loaded alginate beads with waxy materials exhibited controlled release behaviour over a 6-h period, while beads without waxy materials showed release of 100% TSH within 2 h. These results may be attributed to the formation of a more rigid alginate matrix structure due to incorporated waxy materials. From the Dunnett's t-test and the f2 factor, the release of TSH from alginate beads, a similar dissolution pattern to that of the marketed product (Harunal capsules) could be achieved by adding Gelucire 50/13 into TSH-loaded alginate beads. From these results, oral controlled release of TSH could be achieved with loading in alginate beads with waxy materials, such as Compritol 888 ATO, Precirol ATO 5 and Gelucires. PMID:16354396

Kim, Min-Soo; Park, Gyeong-Deuk; Jun, Seoung-Wook; Lee, Sibeum; Park, Jeong-Sook; Hwang, Sung-Joo

2005-12-01

282

Physical characteristics and chemical degradation of amorphous quinapril hydrochloride.  

PubMed

This study was designed to investigate the relationships between the solid-state chemical instability and physical characteristics of a model drug, quinapril hydrochloride (QHCl), in the amorphous state. Amorphous QHCl samples were prepared by rapid evaporation from dichloromethane solution and by grinding and subsequent heating of the crystalline form. Physical characteristics, including the glass transition temperature and molecular mobility, were determined using differential scanning calorimetry, thermogravimetric analysis, powder x-ray diffractometry, polarizing microscopy, scanning electron microscopy, and infrared spectroscopy. The amorphous form of QHCl, produced by both methods, has a T(g) of 91 degrees C. Isothermal degradation studies showed that cyclization of QHCl occurred at the same rate for amorphous samples prepared by the two methods. The activation energy was determined to be 30 to 35 kcal/mol. The rate of the reaction was shown to be affected by sample weight, dilution through mixing with another solid, and by altering the pressure above the sample. The temperature dependence for chemical reactivity below T(g) correlated very closely with the temperature dependence of molecular mobility. Above T(g), however, the reaction was considerably slower than predicted from molecular mobility. From an analysis of all data, it appears that agglomeration and sintering of particles caused by softening of the solid, particularly above T(g), and a resulting reduction of the particle surface/volume ratio play a major role in affecting the reaction rate by decreasing the rate of removal of the gaseous HCl product. PMID:10664545

Guo, Y; Byrn, S R; Zografi, G

2000-01-01

283

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

284

Spectrophotometric estimation of tamsulosin hydrochloride by acid-dye method.  

PubMed

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

285

Conformation and interactions of dopamine hydrochloride in solution.  

PubMed

The aqueous solution of dopamine hydrochloride has been investigated using neutron and X-ray total scattering data together with Monte-Carlo based modelling using Empirical Potential Structure Refinement. The conformation of the protonated dopamine molecule is presented and the results compared to the conformations found in crystal structures, dopamine-complexed protein crystal structures and predicted from theoretical calculations and pharmacophoric models. It is found that protonated dopamine adopts a range of conformations in solution, highlighting the low rotational energy barrier between different conformations, with the preferred conformation being trans-perpendicular. The interactions between each of the species present (protonated dopamine molecules, water molecules, and chloride anions) have been determined and are discussed with reference to interactions observed in similar systems both in the liquid and crystalline state, and predicted from theoretical calculations. The expected strong hydrogen bonds between the strong hydrogen bond donors and acceptors are observed, together with evidence of weaker CH hydrogen bonds and ? interactions also playing a significant role in determining the arrangement of adjacent molecules. PMID:25573567

Callear, Samantha K; Johnston, Andrew; McLain, Sylvia E; Imberti, Silvia

2015-01-01

286

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

PubMed

Effect of ractopamine hydrochloride (RH) and zilpaterol hydrochloride (ZH) on LM shear force and sensory attributes was determined using pens (n = 40) British × Continental crossbred steers randomly allocated to one of the following treatments: control; RH fed at 200 (RH 200) or 300 mg • steer(-1) • d(-1) (RH 300), or 400 mg • steer(-1) • d(-1) (RH 400) top-dressed for the final 30 d of feeding; or ZH fed at 7.5 mg/kg, beginning 23 d before slaughter with a 3-d withdrawal. Two replicates (pens) per treatment were represented in four blocks. Eighteen carcasses per pen were randomly selected and one 5-cm LM sample was removed from both carcass sides to be used for shear force and sensory evaluation. Samples were aged for 14 d, frozen at -28.8 °C, and cut into 2.5-cm steaks. All steaks were cooked to an internal temperature of 71.1 °C before being evaluated for Warner-Bratzler shear force (WBSF), slice shear force (SSF), or being fed to trained sensory panelists. Increasing dose and potency of ?-agonist increased WBSF by 4 to 17% and SSF by 5 to 24% (P < 0.05). Steaks from steers fed ZH had higher WBSF and SSF values compared with all other treatments (P < 0.05), whereas steaks from controls and steers fed RH 200 were not different (P > 0.05). Probability of steaks failing to meet shear force standards to be certified tender (WBSF <4.4 kg, SSF < 20 kg) was increased from an initial probability of <0.06 in steaks from steers in the control treatment to 0.10 to 0.20 in steers fed RH 400 or ZH (P < 0.05). No difference was detected in panel ratings for overall tenderness of steaks from steers fed RH 200 compared with controls (P > 0.05). Steaks from steers fed RH 300 and RH 400 were comparable for all sensory attributes; however, both RH 300 and RH 400 were rated lower for overall tenderness than controls (P < 0.05). Panelists failed to detect differences in overall tenderness of steaks from steers fed RH 400 and ZH (P < 0.05). Panelists detected no difference in flavor profile or juiciness among treatments (P > 0.05). Results from this study indicated ?-agonists negatively affected beef tenderness and these effects may be more noticeable in steers supplemented with ZH and higher doses of RH. PMID:24166996

Arp, T S; Howard, S T; Woerner, D R; Scanga, J A; McKenna, D R; Kolath, W H; Chapman, P L; Tatum, J D; Belk, K E

2013-12-01

287

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

PubMed

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

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

2014-01-01

288

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

PubMed Central

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

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

2014-01-01

289

A new RP-HPLC method for analysis of mebeverine hydrochloride in raw materials and tablets.  

PubMed

A simple, sensitive, selective, reliable, least time consuming and rapid high-performance liquid chromatographic method for the determination and quantification of mebeverine hydrochloride using hyoscine butylbromide as internal standard has been developed. The chromatographic system consisted of a Shimadzu LC-10 AT VP pump, SPD-10 AV VP UV visible detector, and a CBM-102 Bus Module integrator. Separation was achieved on the micro Bondapak 125 a C18 10microm column at room temperature. The samples were introduced through an injector valve with a 10 microl sample loop. Acetonitrile-water (1:1 v/v) was used as mobile phase, with flow rate 1.7 ml/minutes. pH was adjusted to 2.9 with phosphoric acid. U.V detection was performed at 205 nm. The results obtained showed a good agreement with the declared content. Recovery values of mebeverine hydrochloride were from 99.80% to 100.13%. The proposed method is rapid, accurate, and selective and may be used for the quantitative analysis of mebeverine hydrochloride. The method was found to be specific, accurate, precise and reliable for the determination and quantification of mebeverine hydrochloride in form of raw materials, in bulk drugs and formulation. It was possible to determine all of them in the concentration range of 5-30 nano grams. The detection limit of mebeverine hydrochloride was 0.4-nano gram. PMID:16431391

Arayne, M Saeed; Sultana, Najma; Siddiqui, Farhan Ahmed

2005-04-01

290

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

SciTech Connect

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

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

2012-10-11

291

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

NASA Astrophysics Data System (ADS)

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

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

2008-12-01

292

Gas chromatographic quantification of aliphatic aldehydes in freshly distilled Calvados and Cognac using 3-methylbenzothiazolin-2-one hydrazone as derivative agent.  

PubMed

A new precise and sensitive method was used for the quantification of aliphatic aldehydes from C5 to C11 in highly ethanolic beverages such as freshly distilled spirits. Carbonyl compounds were derivatized using 3-methylbenzothiazolin-2-one hydrazone (MBTH) and then separated and detected by gas chromatography-mass spectrometry (GC-MS). Selective mass spectrometric detection of molecular ions of derivatives was performed to obtain a good sensibility (0.2-1.2 microg l(-1)) and a good selectivity. For a concentration of 20 microg l(-1), relative standard deviations were lower than 10% except for heaviest compounds (decanal and undecanal) where RSD were between 11 and 13%. The concentrations of aliphatic aldehydes were determined in nine samples of freshly distilled Calvados and two samples of freshly distilled Cognac with highest concentrations reported for 3-methylbutanal (from 170 to 1220 microg l(-1) in Calvados and from 1540 to 5500 microg l(-1) in Cognac). 3-Methylbutanal and hexanal, due to their low detection thresholds, could be important olfactive markers of these two products. Less than 1h30 is required to quantify the nine studied aliphatic aldehydes in freshly distilled spirits. PMID:16545391

Ledauphin, Jérôme; Barillier, Daniel; Beljean-Leymarie, Martine

2006-05-19

293

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

PubMed

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

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

2011-01-01

294

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

295

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

Microsoft Academic Search

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

G. Duyckaerts; J. Fuger; W. Mueller

1963-01-01

296

Control of impurities in diphenhydramine hydrochloride by an ion-pairing, reverse liquid chromatography method.  

PubMed

A precise, sensitive, repeatable and robust reverse-phase liquid chromatographic method has been developed for the control of seven possible impurities of diphenhydramine hydrochloride. The robustness of the method was examined by varying, in turn, each of four mobile-phase parameters (acetonitrile content, buffer salt concentration, ion-pair reagent concentration and pH). The method was linear in the range 0-0.14 mg mL(-1) for diphenhydramine hydrochloride with an acceptable precision and accuracy, and a limit of detection of 0.17 microg mL(-1). Five samples of diphenhydramine hydrochloride from two sources were analysed with the developed liquid chromatographic method. PMID:11291747

Henderson, L; Miller, J H; Skellern, G G

2001-03-01

297

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

PubMed

To avoid the undesired deprotonation during the addition of organolithium and organomagnesium reagents to ketones, the thioiminium salts, easily prepared from lactams and amides are converted into 2,2-disubstituted and 2-monosubstituted amines by reaction with simple nucleophiles such as organocerium and organocopper reagents. The reaction of thioiminium iodides with organocerium reagents derived by transmetalation of corresponding lithium reagents with anhydrous cerium(III) chloride has been investigated. These thioiminium iodides act as good electrophiles and accept alkylceriums towards bisaddition. The newly synthesized amines have been characterized by 1H and 13C NMR, IR and mass spectra. The amines have been converted into their hydrochlorides and characterized by COSY. These hydrochlorides have been subjected to antimicrobial screening with clinically isolated microorganisms, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella typhi and Candida albicans. The hydrochlorides show quite good activity against these bacteria and fungus. PMID:24211808

Britto, Sebastian; Renaud, Philippe; Nallu, Maruthai

2014-01-01

298

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

299

Spectrophotometric microdetermination of nefopam, mebevrine and phenylpropanolamine hydrochloride in pharmaceutical formulations using alizarins.  

PubMed

Simple and rapid spectrophotometric procedures have been established for quantitation of nefopam hydrochloride (NF) mebevrine hydrochloride (MB) and phenylpropanolamine hydrochloride (PP). The procedures are based on the reaction between the examined drugs (NF, MB and PP) and alizarin (I), alizarin red S (II), alizarin yellow G (III) and quinalizarin (IV) producing ion-pair complexes which can be measured at the optimum wavelength. The optimization of the reaction conditions is investigated. Beer's law is obeyed in the concentration ranges 0.5-30.0 microg ml(-1). The molar absorptivity, Sandell sensitivity, detection and quantification limits are also calculated. The correlation coefficient was > or =0.9988 (n=6) with a relative standard deviation (R.S.D.) of < or =1.3, for six determinations of 20 microg ml(-1). The methods are successfully applied to the determination of NF, MB and PP in their pharmaceutical formulations. PMID:15248949

Shama, S A; Amin, A S

2004-07-01

300

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

PubMed Central

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

Badr, Jihan M.

2013-01-01

301

Pharmacokinetic and pharmacodynamic evaluation of floating microspheres of metformin hydrochloride.  

PubMed

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

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

2013-01-01

302

Neuroendocrine effects of raloxifene hydrochloride in postmenopausal women.  

PubMed

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

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

2001-10-01

303

A preliminary safety evaluation of polyhexamethylene guanidine hydrochloride.  

PubMed

Polyhexamethylene guanidine hydrochloride (PHMGH) is used worldwide as an antimicrobial agent with broad spectra of activity and also for treating pool water. This non-GLP preliminary study aims at investigating in a subchronic toxicity study possible effects at supra-optimal doses of this biocide. Both acute and subchronic toxicity studies were conducted. LD50 for PHMGH was estimated to be 600 mg/kg (ie LC50 2 ml of 7.5% solution) when administered as a single dose by gavage via a stomach tube in accordance with the expected route of administration. The acute studies showed that the median lethal dose (LD50) of 600 mg/kg was accompanied by signs of neurotoxicity. Haematological and biochemical parameters of subchronic toxicity studies were non-significant. Subchronic doses of 0.006 mg/kg, 0.012 mg/kg and 0.036 mg/kg were administered. 20% of the animals at a dose of 0.006 mg/kg and 0.036 mg/kg showed mild degrees of hydropic changes in proximal tubules while 10% of animals at all the doses had their liver tissues showing local areas of mild pericentral hepatocytes degeneration. PHMGH did not produce any major organ defect with regard to the kidney, heart, and liver. The LD50 was much higher than the recommended dosage by a factor of about 50,000. The recommended residual concentration is far less than the median lethal dose using rats as test subjects. These results could serve as a basis for investigating the full toxicological profile if it is to be used for the treatment of raw water to make it potable. PMID:25359731

Asiedu-Gyekye, Isaac Julius; Mahmood, Seidu Abdulai; Awortwe, Charles; Nyarko, Alexander Kwadwo

2014-11-01

304

Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.  

PubMed

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

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

2012-06-01

305

HPLC method for estimation of metformin hydrochloride in formulated microspheres and tablet dosage form.  

PubMed

A simple, accurate, economical and reproducible HPLC method has been developed for quantitative estimation of metformin hydrochloride from tablet dosage form and formulated microspheres. The developed HPLC method is a reverse phase chromatographic method using phenomenex C(18) column and acetonitrile:phosphate buffer (65:35) pH adjusted to 5.75 with o-phosphoric acid as mobile phase and glipizide as internal standard. The linearity was observed in concentration range of 0-25 mug/ml for metformin hydrochloride. Results of analysis were validated statistically and by recovery studies. PMID:20490303

Kar, Mousumi; Choudhury, P K

2009-05-01

306

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

307

Synthesis and analgesic activity of hydrochlorides and quaternary ammoniums of epibatidine incorporated with amino acid ester.  

PubMed

Hydrochloride derivatives 5a-c and quaternary ammonium derivatives 6a-c of epibatidine incorporated with amino acid ester were synthesized and evaluated for their in vivo analgesic activity and toxicity. Among all tested compounds, compound 6c has the most potent analgesic activity. The quaternary ammonium salts 6a and 6c showed better analgesic activity than the corresponding hydrochlorides 5a and 5c. Both 5a-c and 6a-c showed significantly lower toxicity than epibatidine itself. PMID:14643319

Dong, Jing-Chao; Wang, Xin; Li, Run-Tao; Zhang, Hong-Mei; Cheng, Tie-Ming; Li, Chang-Ling

2003-12-15

308

High performance thin layer chromatographic method for simultaneous estimation of Ibuprofen and pseudoephedrine hydrochloride.  

PubMed

High performance thin layer chromatographic method is developed for simultaneous estimation of ibuprofen and pseudoephedrine hydrochloride in tablets. Silica gel 60F(254) plates were used as stationary phase and t.butanol: ethyl acetate: glacial acetic acid: water (7:4:2:2 v/v) as mobile phase. Wavelength selected for analysis was 254 nm. Percent estimation of ibuprofen and pseudoephedrine hydrochloride was found to be 99.56% and 98.77%, respectively. Percent recovery for both the drugs was found in the range of 98.27% to 100.91%, respectively. PMID:20046759

Chitlange, S S; Sakarkar, D M; Wankhede, S B; Wadodkar, S G

2008-01-01

309

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

PubMed

Holstein steers (n = 2,275) were assigned to 1 of 3 treatments: 1) a control diet containing no ?-agonists, 2) a diet that contained zilpaterol hydrochloride (ZH; 8.3 mg/kg [100% DM basis]) for 20 d with a 3-d withdrawal period before harvest, and 3) a diet that contained ractopamine hydrochloride (RH; 30.1 mg/kg [100% DM basis]) for 28 d before harvest. No differences (P ? 0.18) were detected between treatments for initial BW, BW at d 28, or DMI. Final BW, BW gain for the last 28 d, total BW gain, ADG for the last 28 d, and overall ADG were greater (P < 0.05) for steers fed ZH or RH than for steers fed the control diet. Additionally, G:F for the last 28 d and G:F for the entire trial was increased (P < 0.02) for steers fed ZH (0.147, 0.147) or RH (0.153, 0.151) compared to steers fed the control diet (0.134, 0.143), respectively. Steers fed ZH or RH had HCW that were 15.5 and 8.2 kg heavier (P ? 0.01) and LM areas that were 7.1 and 2.3 cm(2) larger (P < 0.01) than control cattle. Steers fed ZH also had dressed carcass yields that were 1.3% to 1.5% greater and USDA calculated yield grades that were decreased 0.16 to 0.23 units compared to RH and control steers. No differences (P ? 0.39) were found between treatments for marbling score, fat thickness, and percentage KPH. Steers fed ZH had an increased (P ? 0.04) percentage of yield grade 1 and 2 carcasses (15.1, 55.0) and a reduced (P ? 0.02) percentage of yield grade 3 carcasses (27.1) compared with those fed RH (10.5, 49.1, 36.1) or the control diet (9.0, 47.4, 36.4), respectively. Additionally, ZH-fed steers had a decreased (P ? 0.04) percentage of yield grade 4 and 5 carcasses (2.8) compared with steers fed the control diet (6.9). Steers fed ZH had an increased (P ? 0.01) percentage of USDA Select grading carcass (31.0%) and a decreased (P ? 0.01) percentage of USDA Choice grading carcasses (65.0%) compared with steers fed RH (25.8%, 70.2%) and no ?-agonist (24.8%, 72.0%), respectively. Feeding either ?-agonist to calf-fed Holstein steers increased live performance through increased BW, BW gain, and ADG. Furthermore, supplementing calf-fed Holstein steers with ZH provides greater improvements in HCW, LM area, and yield grade components, with a slight decrease in quality grade when compared to calf-fed Holstein steers supplemented with RH. PMID:25006068

Brown, T R; Sexten, A K; Lawrence, T E; Miller, M F; Thomas, C L; Yates, D A; Hutcheson, J P; Hodgen, J M; Brooks, J C

2014-09-01

310

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) Å. Furthermore, the supramolecular structure analysis show that there are two types of supramolecular infrastructures, 1D chain or 2D network, which are formed by intermolecular O-H···N or C-H⋯X (X = O, N or F) hydrogen bonds.

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

2011-03-01

311

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

PubMed

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

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

2014-05-21

312

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 ¹H NMR, ¹³C NMR, HRMS, ESI-MS, and mp. Their nematicidal activity was evaluated against that of the pine wood nematode, Bursaphelenchus xylophilus in vivo. Among all of the derivatives, especially V-12 and V-39 displayed the best promising nematicidal activity with LC?? values of 1.0969 and 1.2632 mg/L, respectively. This suggested that introduction of R¹ and R² together as the electron-withdrawing substituents, R³ as the methyl group, and 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 (R²(training set)), the leave-one-out cross-validation correlation coefficient (Q²(LOO)), and the 7-fold cross-validation correlation coefficient (Q²(7-fold)) were 0.791, 0.701, and 0.715, respectively. The external cross-validation correlation coefficient (Q²ext) and the root-mean-square error for the test set (RMSE(test set)) were 0.774 and 3.412, respectively. This study will pave the way for future design, structural modification, and development of indole derivatives as nematicidal agents. PMID:23738496

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

2013-06-19

313

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

314

Simultaneous HPTLC Determination of Rabeprazole and Itopride Hydrochloride From Their Combined Dosage Form  

PubMed Central

A simple, precise, sensitive, rapid and reproducible HPTLC method for the simultaneous estimation of the rabeprazole and itopride hydrochloride in tablets was developed and validated. This method involves separation of the components by TLC on precoated silica gel G60F254 plate with solvent system of n-butanol, toluene and ammonia (8.5:0.5:1 v/v/v) and detection was carried out densitometrically using a UV detector at 288 nm in absorbance mode. This system was found to give compact spots for rabeprazole (Rf value of 0.23 0.02) and for itopride hydrochloride (Rf value of 0.75±0.02). Linearity was found to be in the range of 40-200 ng/spot and 300-1500 ng/spot for rabeprazole and itopride hydrochloride. The limit of detection and limit of quantification for rabeprazole were 10 and 20 ng/spot and for itopride hydrochloride were 50 and 100 ng/spot, respectively. The method was found to be beneficial for the routine analysis of combined dosage form. PMID:20046748

Suganthi, A.; John, Sofiya; Ravi, T. K.

2008-01-01

315

Simultaneous HPTLC Determination of Rabeprazole and Itopride Hydrochloride From Their Combined Dosage Form.  

PubMed

A simple, precise, sensitive, rapid and reproducible HPTLC method for the simultaneous estimation of the rabeprazole and itopride hydrochloride in tablets was developed and validated. This method involves separation of the components by TLC on precoated silica gel G60F254 plate with solvent system of n-butanol, toluene and ammonia (8.5:0.5:1 v/v/v) and detection was carried out densitometrically using a UV detector at 288 nm in absorbance mode. This system was found to give compact spots for rabeprazole (Rf value of 0.23 0.02) and for itopride hydrochloride (Rf value of 0.75+/-0.02). Linearity was found to be in the range of 40-200 ng/spot and 300-1500 ng/spot for rabeprazole and itopride hydrochloride. The limit of detection and limit of quantification for rabeprazole were 10 and 20 ng/spot and for itopride hydrochloride were 50 and 100 ng/spot, respectively. The method was found to be beneficial for the routine analysis of combined dosage form. PMID:20046748

Suganthi, A; John, Sofiya; Ravi, T K

2008-01-01

316

Adsorption of pharmaceutical excipients onto microcrystals of siramesine hydrochloride: Effects on physicochemical properties  

Microsoft Academic Search

A common challenge in the development of new drug substances is poor dissolution characteristics caused by low aqueous solubility. In this study, microcrystals with optimized physicochemical properties were prepared by precipitation in the presence of excipients, which adsorbed to the particle surface and altered particle size, morphology, and dissolution rate. The poorly water-soluble drug siramesine hydrochloride was precipitated by the

Anne Zimmermann; Anna Millqvist-Fureby; Michiel Ringkjøbing Elema; Tue Hansen; Anette Müllertz; Lars Hovgaard

2009-01-01

317

HEALTH AND ENVIRONMENTAL EFFECTS PROFILE FOR 2,4-DIMETHYLANILINE AND 2,4-DIMETHYLANILINE HYDROCHLORIDE  

EPA Science Inventory

The Health and Environmental Effects Profile for 2-4-Dimethylaniline and 2,4-Dimethylaniline Hydrochloride was prepared to support listings of hazardous constituents of a wide range of waste streams under Section 3001 of the Resource Conservation and Recovery Act (RCRA) and to pr...

318

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)...

319

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

320

Preparation and comparative evaluation of sustained release metoclopramide hydrochloride matrix tablets  

Microsoft Academic Search

Metoclopramide hydrochloride (MCP) is commonly used for the management of gastrointestinal disorders. Frequent administration and the undesired side effects (extra pyramidal symptoms) of the drug on the central nervous system due to the fluctuations of its plasma concentrations may lead to patient incompliance, and hence, improper therapy. Therefore, the present work will be devoted to formulate the drug in sustained

Sayed I. Abdel-Rahman; Gamal M. Mahrous; Mahmoud El-Badry

2009-01-01

321

Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.  

PubMed

Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates. The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked. During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmacopeial test for similarity of dissolution profiles ( f2 equation), previously proposed by Moore and Flanner. Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response. PMID:17848158

Uzunovi?, Alija; Vrani?, Edina

2007-08-01

322

Dietary zilpaterol hydrochloride. I. Feedlot performance and carcass traits of steers and heifers  

Microsoft Academic Search

Experiments were conducted at 3 US locations (CA, ID, and TX) to determine the effects of dietary zilpaterol hydrochloride (Zilmax, Intervet Inc., Millsboro, DE) and duration of zilpaterol feeding on performance and carcass merit of finishing steers and heifers. At each site, 160 steers and 160 heifers were stratified within sex by initial BW (study d ?1) and as- signed

J. L. Montgomery; C. R. Krehbiel; J. J. Cranston; D. A. Yates; J. P. Hutcheson; W. T. Nichols; M. N. Streeter; D. T. Bechtol; E. Johnson; T. TerHune; T. H. Montgomery

2009-01-01

323

The effect of zilpaterol hydrochloride on meat quality of calf-fed Holstein steers  

Microsoft Academic Search

The objective of these studies was to evaluate the effects of zilpaterol hydrochloride (ZH), fed for 0, 20, or 30 d, on meat quality attributes of calf- fed Holstein steers. Steers were slaughtered at a com- mercial facility, and carcasses were selected by HCW to represent the pen mean. Further carcass selection was based on quality grade (Choice and Select)

S. F. Holmer; D. M. Fernández-Dueñas; S. M. Scramlin; C. M. Souza; D. D. Boler; F. K. McKeith; J. Killefer; R. J. Delmore; J. L. Beckett; T. E. Lawrence; D. L. VanOverbeke; G. G. Hilton; M. E. Dikeman; J. C. Brooks; R. A. Zinn; M. N. Streeter; J. P. Hutcheson; W. T. Nichols; D. M. Allen; D. A. Yates

2010-01-01

324

Effect of extended withdrawal of zilpaterol hydrochloride on performance and carcass traits in finishing beef steers  

Microsoft Academic Search

The objective was to evaluate the ef- fects of an extended withdrawal period after feeding the ?-adrenergic agonist zilpaterol hydrochloride (ZH) for 20 d at the end of the feeding period. Three hundred eighty-four crossbred beef steers were blocked by BW and randomly allocated into 64 pens (6 steers\\/pen). Pens were assigned to treatments in a 2 × 4 factorial

B. P. Holland; C. R. Krehbiel; G. G. Hilton; M. N. Streeter; D. L. VanOverbeke; J. N. Shook; D. L. Step; L. O. Burciaga-Robles; D. R. Stein; D. A. Yates; J. P. Hutcheson; W. T. Nichols; J. L. Montgomery

2010-01-01

325

Dietary zilpaterol hydrochloride. II. Carcass composition and meat palatability of beef cattle  

Microsoft Academic Search

Experiments were conducted at 3 US locations (California, Idaho, and Texas) to determine the effects of dietary zilpaterol hydrochloride and dura- tion of zilpaterol feeding on carcass composition and beef palatability. At each site, 160 steers and 160 heif- ers were stratified within sex by initial BW (study d ?1) and assigned randomly within BW strata to 1 of 4

J. M. Leheska; J. L. Montgomery; C. R. Krehbiel; D. A. Yates; W. T. Nichols; M. Streeter; J. R. Blanton; M. F. Miller

2010-01-01

326

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

Technology Transfer Automated Retrieval System (TEKTRAN)

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

327

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

328

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

PubMed

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

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

1977-10-01

329

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

330

Stability profiles of nepenthesin in urea and guanidine hydrochloride: comparison with porcine pepsin A.  

PubMed

Nepenthesin, an aspartic endopeptidase from the pitcher fluid of Nepenthes, was found to be markedly less stable than porcine pepsin A when treated with urea or guanidine hydrochloride. This is in sharp contrast with its remarkably high pH/temperature stability as compared with porcine pepsin A. No protein with such a stability profile has been reported to date. PMID:21071863

Kubota, Keiko; Metoki, Yuya; Athauda, Senarath B P; Shibata, Chiaki; Takahashi, Kenji

2010-01-01

331

Interactions of biocidal guanidine hydrochloride polymer analogs with model membranes: a comparative biophysical study.  

PubMed

Four synthesized biocidal guanidine hydrochloride polymers with different alkyl chain length, including polyhexamethylene guanidine hydrochloride and its three new analogs, were used to investigate their interactions with phospholipids vesicles mimicking bacterial membrane. Characterization was conducted by using fluorescence dye leakage, isothermal titration calorimetry, and differential scanning calorimetry. The results showed that the gradually lengthened alkyl chain of the polymer increased the biocidal activity, accompanied with the increased dye leakage rate and the increased binding constant and energy change value of polymer-membrane interaction. The polymer-membrane interaction induced the change of pretransition and main phase transition (decreased temperature and increased width) of phospholipids vesicles, suggesting the conformational change in the phospholipids headgroups and disordering in the hydrophobic regions of lipid membranes. The above information revealed that the membrane disruption actions of guanidine hydrochloride polymers are the results of the polymer's strong binding to the phospholipids membrane and the subsequent perturbations of the polar headgroups and hydrophobic core region of the phospholipids membrane. The alkyl chain structure significantly affects the binding constant and energy change value of the polymer-membrane interactions and the perturbation extent of the phospholipids membrane, which lead to the different biocidal activity of the polymer analogs. This work provides important information about the membrane disruption action mechanism of biocidal guanidine hydrochloride polymers. PMID:21807631

Zhou, Zhongxin; Zheng, Anna; Zhong, Jianjiang

2011-09-01

332

Nalfurafine hydrochloride: a new drug for the treatment of uremic pruritus in hemodialysis patients.  

PubMed

Uremic pruritus in hemodialysis patients is intractable and no effective treatments have been established yet. Although the precise mechanism of the pruritus is still unclear, accumulating evidence suggests that activation of the micro-opioid receptors may induce pruritus in hemodialysis patients. On the other hand, activation of kappa-opioid receptors is known to control or inhibit the signals activated through micro-opioid receptors; therefore, it was expected that kappa-opioid receptor agonists would be able to reduce pruritus in patients undergoing hemodialysis. Nalfurafine hydrochloride is a novel derivative of the opioid receptor antagonist naltrexone. Nalfurafine hydrochloride is a selective kappa-opioid receptor agonist and has a potent antipruritic effect on various types of pruritus through central kappa-opioid receptor activation in non-clinical pharmacological studies. Moreover, clinical studies have demonstrated that nalfurafine hydrochloride possesses efficacy and safety in hemodialysis patients with uremic pruritus. In this review, we provide a detailed description of the activity of nalfurafine hydrochloride using published data of in vitro, in vivo nonclinical pharmacological and clinical studies in hemodialysis patients with uremic pruritus. PMID:19584962

Nakao, Kaoru; Mochizuki, Hidenori

2009-05-01

333

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

334

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...

335

An unexpected reaction of 2-(cyclopent-2-enyl)aniline hydrochloride with dimethyldioxirane  

Microsoft Academic Search

An unusual direction of the reaction of 2-(cyclopent-2-enyl)aniline hydrochloride with dimethyldioxirane was found: the formation\\u000a of two isomeric products,viz., 3- and 6-chloro-2-(cyclopent-2-enyl)anilines, was observed.

D. I. D'yachenko; A. G. Mustafin; V. V. Shereshovets; N. N. Kabal'nova; V. P. Kazakov; I. B. Abdrakhmanov; G. A. Tolstikov

1998-01-01

336

RADIATION INJURIES IN THE PIG AND THEIR MODIFICATION BY AMINOETHYLISOTHIURONIUM CHLORIDE-HYDROCHLORIDE  

Microsoft Academic Search

Studies were performed to ascertain whether aminoethylisothiuronium ; chloride-hydrochloride (AET-HCl) provides protection against ionizing radiation ; in pigs; 300 pigs were used and x-ray doses of 500 to 1000 r. The LDââââ ; for the 5- to 7-week-old animals was found to be 720 r following unilateral ; irradiation in the dorsoventral direction. Increase in weight was disturbed by ;

W. Braun; J. Staubesand; V. Wolf

1961-01-01

337

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

PubMed

Clinical, bronchoscopic, spirographic, scintigraphic, and chemical analyses were done in 24 children with cystic fibrosis to assess the mucolytic effects of acetylcysteine inhalations versus L-arginine hydrochloride aerosols. The latter drug is less active than acetylcysteine and should not be used to treat children with cystic fibrosis. PMID:1110869

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

1975-01-01

338

A randomized, crossover design study of sevelamer carbonate powder and sevelamer hydrochloride tablets in chronic kidney disease patients on haemodialysis  

PubMed Central

Background. Sevelamer carbonate is an improved, buffered form of sevelamer hydrochloride developed for the treatment of hyperphosphataemia in CKD patients. Sevelamer carbonate formulated as a powder for oral suspension presents a novel, patient-friendly alternative to tablet phosphate binders. This study compared the safety and efficacy of sevelamer carbonate powder with sevelamer hydrochloride tablets in CKD patients on haemodialysis. Methods. This was a multi-centre, open-label, randomized, crossover design study. Thirty-one haemodialysis patients were randomly assigned to either sevelamer carbonate powder or sevelamer hydrochloride tablets for 4 weeks followed by a crossover to the other regimen for an additional 4 weeks. Results. The mean serum phosphorus was 1.6 ± 0.5 mmol/L (5.0 ± 1.5 mg/dL) during sevelamer carbonate powder treatment and 1.7 ± 0.4 mmol/L (5.2 ± 1.1 mg/dL) during sevelamer hydrochloride tablet treatment. Sevelamer carbonate powder and sevelamer hydrochloride tablets are equivalent in controlling serum phosphorus; the geometric least square mean ratio was 0.95 (90% CI 0.87–1.03). No statistically significant or clinically meaningful differences were observed in calcium × phosphorus product and lipid levels between sevelamer carbonate powder and sevelamer hydrochloride tablets. Serum bicarbonate levels increased 2.7 ± 3.7 mmol/L (2.7 ± 3.7 mEq/L) during sevelamer carbonate treatment. No statistically significant change in bicarbonate was observed during sevelamer hydrochloride treatment. Sevelamer carbonate powder and sevelamer hydrochloride were well tolerated during this study. Conclusions. Sevelamer carbonate powder and sevelamer hydrochloride tablets are equivalent in controlling serum phosphorus and well tolerated in CKD patients on haemodialysis. Bicarbonate levels improved only during sevelamer carbonate treatment. Sevelamer carbonate powder should provide a welcomed new option for the treatment of hyperphosphataemia for CKD patients on dialysis. PMID:19666658

Fan, Stanley; Ross, Calum; Mitra, Sandip; Kalra, Philip; Heaton, Jeremy; Hunter, John; Plone, Melissa; Pritchard, Nick

2009-01-01

339

Formulation and Evaluation of Propranolol Hydrochloride-Loaded Carbopol-934P/Ethyl Cellulose Mucoadhesive Microspheres  

PubMed Central

The purpose of this research was to formulate and systemically evaluate in-vitro and in-vivo performances of mucoadhesive propranolol hydrochloride microspheres for its potential use in the treatment of hypertension, myocardial infraction and cardiac arrhythmias. Propranolol hydrochloride mucoadhesive microspheres, containing carbopol-934P as mucoadhesive polymer and ethyl cellulose as carrier polymer, were prepared by an emulsion-solvent evaporation technique. Results of preliminary trials indicated that the quantity of emulsifying agent, time for stirring, drug-to-polymers ratio, and speed of rotation affected various characteristics of microspheres. Microspheres were discrete, spherical, free-flowing and showed a good percentage of drug entrapment efficiency. An in-vitro mucoadhesive test showed that propranolol hydrochloride mucoadhesive microspheres adhered more strongly to the gastric mucous layer and could be retained in the gastrointestinal tract for an extended period of time. A 32 full factorial design was employed to study the effect of independent variables, drug-to-polymer-to-polymer ratio (propranolol hydrochloride-ethyl cellulose-carbopol-934P) (X1), and stirring speed (X2) on dependent variables, i.e. percentage of mucoadhesion, drug entrapment efficiency, particle size and t80. The best batch exhibited a high drug entrapment efficiency of 54 %; 82% mucoadhesion after 1 h and particle size of 110 ?m. A sustained pattern of drug release was obtained for more than 12 h. The drug-to-polymer-to-polymer ratio had a more significant effect on the dependent variables. The morphological characteristics of the mucoadhesive microspheres were studied under a scanning electron microscope. In-vivo evaluation studies on propranolol hydrochloride mucoadhesive microspheres and propranolol hydrochloride powder were performed on normal healthy rabbits. The results showed a sustained anti-hypertensive effect over a longer period of time in case of mucoadhesive microspheres, compared to the powder. In conclusion, the prolonged gastrointestinal residence time and slow release of propranolol hydrochloride resulting from the mucoadhesive microspheres, could contribute to the provision of a sustained anti-hypertensive effect. PMID:24363731

Patel, Jayvadan; Patel, Darshna; Raval, Jignyasha

2010-01-01

340

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

PubMed

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

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

2010-08-01

341

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

Code of Federal Regulations, 2014 CFR

...form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The resin sample being analyzed must contain enough...hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of the polymeric...

2014-07-01

342

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

Code of Federal Regulations, 2013 CFR

...form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The resin sample being analyzed must contain enough...hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of the polymeric...

2013-07-01

343

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

Code of Federal Regulations, 2012 CFR

...form. The hydrolysis of these polymers is catalyzed by hydrogen ions. 2.2The resin sample being analyzed must contain enough...hydroxylamine hydrochloride will produce sufficient hydrogen ions to catalyze the depolymerization of the polymeric...

2012-07-01

344

Effect of Duration of Zilpaterol Hydrochloride Treatment on Carcass Characteristics and Weight Gain in Grazing Pelibuey Lambs  

Microsoft Academic Search

Salinas-Chavira, J., Domínguez-Muñoz, M., Díaz-Martínez, R., Cruz-Bautista, P., Montaño-Gómez, M.F. and Arzola-Alvarez, C. 2006. Effect of duration of zilpaterol hydrochloride treatment on carcass characteristics and weight gain in grazing Pelibuey lambs. J. Appl. Anim. Res., 29: 25–28.The effect of zilpaterol hydrochloride (ZH) supplementation on carcass characteristics and weight gain were studied in grazing Pelibuey lambs. Thirty-six intact male Pelibuey sheep,

J. Salinas-Chavira; M. Domínguez-Muñoz; R. Díaz-Martínez; P. Cruz-Bautista; M. F. Montaño-Gómez; C. Arzola-Alvarez

2006-01-01

345

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

346

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

NASA Astrophysics Data System (ADS)

The reaction between ZnCl 2 and di-2-pyridyl ketone benzoyl hydrazone (dpkbh) in acetonitrile under ultrasonic or reflux conditions gave [ZnCl 2(? 3-N,N,O-dpkbh)] in good yield. The identity of the compound was established from the results of its elemental analysis and a number of spectroscopic measurements. Solid-state infrared spectra of [ZnCl 2(? 3-N,N,O-dpkbh)] reveal the coordination of dpkbh, the presence of the amide proton and binding of the oxygen atom of dpkbh. 1H NMR spectra of [ZnCl 2(? 3-N,N,O-dpkbh)] show sensitivity to solvent and temperature variations and confirm the coordination of dpkbh. The electronic absorption spectra of [ZnCl 2(? 3-N,N,O-dpkbh)] in non-aqueous media show high sensitivity to changes in their surroundings and divulge two interlocked intra-ligand-charge transfer (ILCT) transitions of the donor-acceptor type between 300 and 500 nm. Optical measurements show reversible inter-conversion between two forms of [ZnCl 2(? 3-N,N,O-dpkbh)] that may be due to complex-substrate interactions and thermodynamic analysis gave changes in enthalpy (? H?) of -23.3 and +14.1 kJ mol -1, entropy (? S?) of -51 and +31 J mol -1K -1, and free energy (? G?) of -8.16 and +4.54 kJ mol -1 at 298.15 K in DMF and DMSO, respectively. Substrates in concentrations as low as 10 -5 M can be detected and determined using [ZnCl 2(? 3-N,N,O-dpkbh)] in polar solvents. A provisional model for the binding of substrate to [ZnCl 2(? 3-N,N,O-dpkbh)] is developed and a binding constant in the range 6000-8000 M -1 is obtained in the case of ZnCl 2 in DMSO. Electrochemical measurements on [ZnCl 2(? 3-N,N,O-dpkbh)] in DMF show irreversible metal and ligand-based redox processes, and electrochemical reactions of dpkbh with ZnCl 2 show facile coordination of ZnCl 2 and formation of [ZnCl 2(? 3-N,N,O-dpkbh)]. X-ray structural analysis done on a crystal grown from a DMF solution of [ZnCl 2(? 3-N,N,O-dpkbh)] confirmed the identity of [ZnCl 2(? 3-N,N,O-dpkbh)] and shows an extensive network of non-covalent interactions that connects all molecules.

Bakir, Mohammed; Green, Orville; Mulder, Willem H.

2008-02-01

347

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

PubMed

Endometritis is a common disease in animal production and influences breeding all over the world. Berberine is one of the main alkaloids isolated from Rhizoma coptidis. Previous reports showed that berberine has anti-inflammatory potential. However, there have been a limited number of published reports on the anti-inflammatory effect of berberine hydrochloride on LPS-induced endometritis. The purpose of the present study was to investigate the effects of berberine hydrochloride on LPS-induced mouse endometritis. Berberine hydrochloride was administered intraperitoneally at 1h before and 12h after LPS induction. Then, a biopsy was performed, and uterine myeloperoxidase (MPO) and nitric oxide (NO) concentrations were determined. Tumor necrosis factor-? (TNF-?) and interleukin-1? (IL-1?) levels in the uterus homogenate were measured by ELISA. The extent of I?B-? and P65 phosphorylation was detected by Western blot. The results showed that berberine hydrochloride significantly attenuated neutrophil infiltration, suppressed myeloperoxidase activity and decreased NO, TNF-?and IL-1?production. Furthermore, berberine hydrochloride inhibited the phosphorylation of the NF-?B p65 subunit and the degradation of its inhibitor, I?B?. These findings suggest that berberine hydrochloride exerts potent anti-inflammatory effects on LPS-induced mouse endometritis and might be a potential therapeutic agent for endometritis. PMID:25479718

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

2015-01-01

348

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

PubMed

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

Pillai, S; Singhvi, I

2008-09-01

349

Quantitative Estimation of Itopride Hydrochloride and Rabeprazole Sodium from Capsule Formulation  

PubMed Central

Two simple, accurate, economical and reproducible UV spectrophotometric methods and one HPLC method for simultaneous estimation of two component drug mixture of itopride hydrochloride and rabeprazole sodium from combined capsule dosage form have been developed. First developed method involves formation and solving of simultaneous equations using 265.2 nm and 290.8 nm as two wavelengths. Second method is based on two wavelength calculation, wavelengths selected for estimation of itopride hydrochloride was 278.0 nm and 298.8 nm and for rabeprazole sodium 253.6 nm and 275.2 nm. Developed HPLC method is a reverse phase chromatographic method using phenomenex C18 column and acetonitrile: phosphate buffer (35:65 v/v) pH 7.0 as mobile phase. All developed methods obey Beer's law in concentration range employed for respective methods. Results of analysis were validated statistically and by recovery studies. PMID:21394269

Pillai, S.; Singhvi, I.

2008-01-01

350

Development and validation of an HPLC method for mefloquine hydrochloride determination in tablet dosage form.  

PubMed

A simple HPLC method for determination of mefloquine hydrochloride in tablets was developed and validated. The separation was carried out on an Xterra RP18 (250 x 4.6 mm id, 5 pm particle size) analytical column. The mobile phase was 0.05 M monobasic potassium phosphate buffer (pH 3.5)-methanol (40 + 60, v/v). The flow rate and wavelength were set to 1 mL/min and 283 nm, respectively. The method was specific for mefloquine hydrochloride in the presence of hydrolytic, oxidative, and photolytic degradation products. It was also linear, precise, accurate, and robust, being suitable for routine QC analyses and stability studies. The developed HPLC method was compared to a previously described spectrophotometric method. PMID:21919342

Nogueira, Fernando Henrique Andrade; Goulart, Letícia de Paula Lana; César, Isabela da Costa; de Campos, Lígia Maria Moreira; Pianetti, Gérson Antônio

2011-01-01

351

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

PubMed

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

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

2008-01-01

352

Spectrofluorimetric method for the determination of doxepin hydrochloride in commercial dosage forms.  

PubMed

A novel spectrofluorimetric method has been developed for the determination of doxepin hydrochloride in commercial dosage forms. The method is based on the fluorescent ion pair complex formation of the drug with eosin Y in the presence of sodium acetate-acetic acid buffer solution of pH 4.52 which is extractable in dichloromethane. The extracted complex showed fluorescence intensity at lambdaem=567 nm after excitation at 464 nm. The calibration curve was linear over the working range of 0.1-0.8 microg ml(-1). Under the optimized experimental conditions, present method is validated as per International Conference on Harmonization guidelines. The limit of detection for the developed method is 2.95 ng ml(-1). The method has been successfully applied to the determination of doxepin hydrochloride in commercial dosage forms. The results are compared with the reference spectrofluorimetric method. PMID:19936937

Rahman, Nafisur; Siddiqui, Sana; Azmi, Syed Najmul Hejaz

2009-01-01

353

Complete response to irinotecan hydrochloride and nedaplatin in a patient with advanced ovarian clear cell carcinoma.  

PubMed

A 55-year-old multiparous woman was diagnosed with stage IIIc ovarian clear cell carcinoma. Three years after the first surgery and adjuvant chemotherapy with irinotecan hydrochloride and mitomycin C, she developed common iliac lymph node recurrence. Two cycles of chemotherapy with irinotecan hydrochloride and nedaplatin led to a complete response. Surgical resection revealed pathological complete response. The chemosensitivity of ovarian clear cell carcinoma has been reported to be very poor. No standard chemotherapeutic regimens for this carcinoma have been established. The present study is the first report of a pathological complete response in a patient with advanced ovarian clear cell carcinoma. Future studies are needed to confirm the efficacy of this regimen for this carcinoma. PMID:15549593

Nishida, Masato; Tsunoda, Hajime; Ichikawa, Yoshihito; Yoshikawa, Hiroyuki

2004-10-01

354

Study on a new precolumn derivatization method in the determination of metformin hydrochloride.  

PubMed

Metformin hydrochloride is successfully determined by reversed-phase high-performance liquid chromatography with a new precolumn derivatization method using 9,10-anthraquinone-2-sulfonyl chloride as the derivatization agent. Several derivatization systems are tried to optimize the derivatization conditions, and a new post-derivatization treatment method is established. The derivatization product is analyzed on a Lichrosper C18 column (6.0 mm x 150 mm, 5 microm) at 256 nm with methanol-water (70:30, v/v) as the mobile phase. The calibration curves of the derivatives for the UV detector (0.01-4 mg/L) are linear with respect to peak area. The detection limit (peak area) for the metformin hydrochloride is 0.01 mg/L for a signal-to-noise ratio of 3:1. In human plasma, the detection limit is 0.02 mg/L. This assay is rapid, sensitive, and highly reproducible. PMID:16620517

Jiang, Juan Juan; Feng, Fang; Ma, Ming; Zhang, Zheng Xing

2006-04-01

355

Study on the Interaction of ?-Cyclodextrin and Berberine Hydrochloride and Its Analytical Application  

PubMed Central

The fluorescence enhancement of berberine hydrochloride (BBH) as a result of complex with ?-cyclodextrin (?-CD) is investigated. The mechanism of the inclusion was studied and discussed by spectrofluoremetry and infrared spectrograms. The results showed that a 1?1 (?-CD: BBH) complex was formed with an apparent association constant of 4.23×102 L/mol. Based on the enhancement of the fluorescent intensity of berberine hydrochloride, a new spectrofluorimetric method for the determination of BBH in the presence of ?-CD was developed. The linear range was 1.00?4.00 µg/mL with the detection limit of 5.54 ng/mL. The proposed method was successfully applied to the determination of BBH in tablets. PMID:24810601

Jia, Baoxiu; Li, Yuqin; Wang, Decai; Duan, Rui

2014-01-01

356

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

PubMed Central

The aim of the present study is to prepare and evaluate mucoadhesive nasal gels of venlafaxine hydrochloride. Mucoadhesive nasal gels were prepared using polymers like carbopol 934 and sodium alginate and characterized in terms of viscosity, texture profile analysis, ex vivo drug permeation profiles and histopathological studies. The results show that values of viscosity, hardness and adhesiveness increase while those of cohesiveness decrease with corresponding increase in concentration of the polymers. Ex vivo drug permeation profiles showed that formulation containing 5% sodium alginate provided a better controlled release of the drug than the other formulations over a period of 12 h. Histopathological studies assured that gels containing different polymers did not produce any significant change in the nasal mucosae of goat even after 12 h permeation study. Mucoadhesive nasal gel of venlafaxine hydrochloride is a novel dosage form which delivers the drug directly into systemic circulation and provides controlled release of the drug. PMID:23716871

Basu, Shyamoshree; Maity, S.

2012-01-01

357

Physicochemical stability of papaverine hydrochloride-phentolamine mesylate mixtures used for intracavernous injection: a preliminary evaluation.  

PubMed

Physicochemical stability of intracavernous injections of 30 mg. per ml. papaverine hydrochloride with 0.5 or 1.0 mg. per ml. phentolamine mesylate used to induce erection in patients with impotence was examined. The samples were stored at room temperature, in the refrigerator at 4C and in the freezer at -20C for 6 months. The examination consisted of visual observation for change in color or evidence of precipitation, measurement of pH and thin layer chromatography at different intervals. During the 6 months of storage no change had occurred in pH, color development, precipitation or formation of new moieties. Therefore, the aforementioned injection solutions of papaverine hydrochloride with phentolamine mesylate can be dispensed safely with instruction to patients for adequate storage and manipulation. PMID:2454330

Hadzija, B W; Mattocks, A M; Stahl, G M

1988-07-01

358

[Manufacture of tetracaine hydrochloride tablets using direct compression and moist granulation].  

PubMed

The results of quality testing of lozenges made by direct compression and by wet granulation procedure (Ph. Jug. IV) are presented. The aim was to determine hardness, friability and disintegration of the lozenges. Considering the fact that the produced tetracaine hydrochloride lozenges were not transported, but were made according to the needs of the Clinic of Gastroenterology, Military Medical Academy, time of disintegration, not hardness and friability, was the priority in making a choice of formulation. That is why tetracaine hydrochloride lozenges made with 3.5% solution of carmellose sodium, which have the longest disintegration were chosen, which made possible the longest contact of the local anesthetic with mucous membrane of mouth and throat. PMID:12557620

Gazikalovi?, Emilija; Obrenovi?, Dusan; Nidzovi?, Zivorad; Coli?, Olivera

2002-01-01

359

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

PubMed

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

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

360

Compressed matrix dual-component vaginal drug delivery system containing metoclopramide hydrochloride  

Microsoft Academic Search

The purpose of the present investigation was to produce a quick\\/slow biphasic delivery system for metocloprami- de hydrochloride using the superdisintegrant Ac-di-sol for the fast release layer and hydroxypropyl methylcellulose K100M and Ucarflock 302 to modulate the release of the drug. A dual component tablet made up of a sustained release and an immediate release layer was prepared by direct

GEETA M. PATEL; MADHABHAI M. PATEL

361

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

362

Effects of feed supplementation of zilpaterol hydrochloride on growth performance and carcass traits of finishing lambs  

Microsoft Academic Search

Effects of zilpaterol hydrochloride (ZH) on growth performance trial (30-day period), and carcass traits of finishing lambs were evaluated. Twenty-eight male Rambouillet lambs (32.7±2.6 kg body weight) were randomly assigned to diets with: 0, 5.3, 10.6, and 15.9 mg ZH\\/kg dry matter (DM). Average daily weight gain, hot and chilled carcass dressing, muscle conformation, hindquarters width, major and minor torax

J. Mondragón; I. A. Domínguez-Vara; J. M. Pinos-Rodríguez; M. González; J. L. Bórquez; A. Domínguez; M. L. Mejia

2010-01-01

363

Effect of azelastine hydrochloride on release and production of platelet activating factor in human neutrophils  

Microsoft Academic Search

Effect of azelastine hydrochloride (azelastine) on release and production of platelet-activating factor (PAF) in neutrophils obtained from asthmatic and non-asthmatic patients was investigated. Neutrophils were preincubated with or without azelastine and stimulated with f-Met-Leu-Phe (fMLP, 10 ?M) for 15 min. PAF-like activity was detected by aggregation of washed guinea pig platelets.PAF-like activity released from asthmatic neutrophils without preincubation of azelastine

K. Shindo; M. Fukumura; Y. Hirai; K. Koide

1997-01-01

364

Azelastine hydrochloride inhibits platelet activating factor-like activity in human eosinophils  

Microsoft Academic Search

We investigated the inhibitory effect of azelastine hydrochloride (azelastine), an anti-asthmatic drug, on platelet-activating factor (PAF)-like activity in eosinophils obtained from asthmatic and non-asthmatic patients. Eosinophils were preincubated with or without azelastine and stimulated with f-Met-Leu-Phe (fMLP, 10 ?mol) for 15 min. PAF-like activity was detected by aggregation of washed guinea-pig platelets. PAF-like activity released from asthmatic eosinophils without preincubation

Kunihiko Shindo; Motonori Fukumura

1996-01-01

365

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

Microsoft Academic Search

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

Ekapol Limpongsa; Kraisri Umprayn

2008-01-01

366

Crystal Structure of (?)-Mefloquine Hydrochloride Reveals Consistency of Configuration with Biological Activity  

PubMed Central

The absolute configuration of (?)-mefloquine has been established as 11R,12S by X-ray crystallography of the hydrochloride salt, thus allowing comparison of the configuration of mefloquine's optical isomers to those of quinine and quinidine. (?)-Mefloquine has the same stereochemistry as quinine, and (+)-mefloquine has the same stereochemistry as quinidine. Since (+)-mefloquine is more potent than (?)-mefloquine in vitro against the D6 and W2 strains of Plasmodium falciparum and quinidine is more potent than quinine, a common stereochemical component for antimalarial activity is implicated. The crystal of (?)-mefloquine hydrochloride contained four different conformations which mainly differ in a small rotation of the piperidine ring. These conformations are essentially the same as the crystalline conformations of racemic mefloquine methylsulfonate monohydrate, mefloquine hydrochloride, and mefloquine free base. The crystallographic parameters for (?)-mefloquine hydrochloride hydrate were as follows: C17H17F 6N2O+Cl? · 0.25 H2O; Mr, 419.3; symmetry of unit cell, orthorhombic; space group, P212121; parameters of unit cell, a = 12.6890 ± 0.0006 Å (1 Å = 0.1 nm), b = 18.9720 ± 0.0009 Å, c = 32.189 ± 0.017 Å; volume of unit cell, 7,749 ± 4 Å3; number of molecules per unit cell, 16; calculated density, 1.44 g cm?3; source of radiation, Cu K? (? = 1.54178 Å); ? (absorption coefficient), 2.373 mm?1; room temperature was used; final R1 (residual index), 0.0874 for 3,692 reflections with intensities greater than 2?. All of the hydroxyl and amine hydrogen atoms participate in intermolecular hydrogen bonds with chloride ions. The orientation of the amine and hydroxyl groups in (+)-mefloquine may define the optimal geometry for hydrogen bonding with cellular constituents. PMID:11959592

Karle, Jean M.; Karle, Isabella L.

2002-01-01

367

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

PubMed Central

Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer and osteoporosis in post-menopausal women, shows poor oral bioavailability of 2%. The aim of this study was to develop, statistically optimize, and characterize raloxifene hydrochloride-loaded transfersomes for transdermal delivery, in order to overcome the poor bioavailability issue with the drug. A response surface methodology experimental design was applied for the optimization of transfersomes, using Box-Behnken experimental design. Phospholipon® 90G, sodium deoxycholate, and sonication time, each at three levels, were selected as independent variables, while entrapment efficiency, vesicle size, and transdermal flux were identified as dependent variables. The formulation was characterized by surface morphology and shape, particle size, and zeta potential. Ex vivo transdermal flux was determined using a Hanson diffusion cell assembly, with rat skin as a barrier medium. Transfersomes from the optimized formulation were found to have spherical, unilamellar structures, with a homogeneous distribution and low polydispersity index (0.08). They had a particle size of 134±9 nM, with an entrapment efficiency of 91.00%±4.90%, and transdermal flux of 6.5±1.1 ?g/cm2/hour. Raloxifene hydrochloride-loaded transfersomes proved significantly superior in terms of amount of drug permeated and deposited in the skin, with enhancement ratios of 6.25±1.50 and 9.25±2.40, respectively, when compared with drug-loaded conventional liposomes, and an ethanolic phosphate buffer saline. Differential scanning calorimetry study revealed a greater change in skin structure, compared with a control sample, during the ex vivo drug diffusion study. Further, confocal laser scanning microscopy proved an enhanced permeation of coumarin-6-loaded transfersomes, to a depth of approximately160 ?M, as compared with rigid liposomes. These ex vivo findings proved that a raloxifene hydrochloride-loaded transfersome formulation could be a superior alternative to oral delivery of the drug. PMID:25246789

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

2014-01-01

368

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

Microsoft Academic Search

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

Kanako Honda; Hirofumi Kawazumi; Naotoshi Nakashima; Yasuro Niidome

369

Double-blind evaluation of buprenorphine hydrochloride for post-operative pain  

Microsoft Academic Search

Summary and Conclusions  In a double-blind, random assignment study of four groups of 40 patients, relief of severe pain with buprenorphine hydrochloride\\u000a 0.2 mg or 0.4 mg was evaluated and compared with morphine sulphate 5 or 10 mg. Evaluations included pain intensity, pain relief,\\u000a sedation and other effects for up to 12 hours after drug administration, following recovery of wakefulness from

Allen B. Dobkin; Barbara Esposito; Carole Philbin

1977-01-01

370

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

Microsoft Academic Search

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

Alaa El-Gindy; Samy Emara; Ahmed Mostafa

2005-01-01

371

APPLICATION OF THE REACTION OF PROMAZINE HYDROCHLORIDE WITH CHROMIUM(VI) IN VOLUMETRIC AND SPECTROPHOTOMETRIC ANALYSIS  

Microsoft Academic Search

Promazine hydrochloride (PMH) reacts in acidic medium with K2Cr2O7 forming coloured oxidation product. This property is exploited for using PMH as redox indicator in chromatometry. The spectra of oxidation products of PMH in UV and IR regions were recorded. The optimal conditions for the formation of these products and their electrochemical behaviour are described. K2Cr2O7 precipitates PMH from aqueous solutions

Wieslawa Misiuk; Helena Puzanowska-Tarasiewicz; Ludmila Kuzmicka; Katarzyna Mielech

2002-01-01

372

[Forensic chemical investigation of alcohol-containing liquids contained polyhexamethylene guanidine hydrochloride and diethylphthalate].  

PubMed

Alcoholism remains one of the main causes of premature death in the population of Russia. Hence, the importance of the problem of uncontrolled distribution and consumption of surrogate alcoholic products, such as alcohol-containing liquids of uncertain origin. The objective of the present study was to detect ethyl alcohol, polyhexamethylene guanidine hydrochloride, and diethylphthalate in disinfectant liquids, biological fluids and human tissues and to analyse qualitative and quantitative composition of these materials. PMID:20821990

Tsisanova, E S; Salomatin, E M

2010-01-01

373

Determination of Gastrodin and Ligustrazine Hydrochloride in Plasma and Brain Dialysate by LC–Tandem MS  

Microsoft Academic Search

A gradient liquid chromatography-tandem mass spectrometry method has been developed and validated for the determination of\\u000a gastrodin and ligustrazine hydrochloride in rat plasma and brain dialysates. Zolpidem was used as internal standard. For plasma\\u000a samples, solid-phase extraction was used and the brain dialysates were collected from freely moving rats using brain microdialysis.\\u000a Both were followed by HPLC separation and positive

Yun-Feng Lv; Xin Hu; Wei-Ming Cheng; Ying-Lan Nie; Kai-Shun Bi

2008-01-01

374

Extraction-spectrophotometric determination of amprolium hydrochloride using bromocresol green, bromophenol blue and bromothymol blue  

Microsoft Academic Search

A new procedure for the determination of amprolium hydrochloride by reaction with bromocresol green (BCG), bromophenol blue (BPB) and bromothymol blue (BTB) has been developed. The method consists of extracting the yellow ion-pair formed into chloroform from aqueous medium. The ion-pairs have absorption maxima at 420, 410 and 415 nm with molar absorptivities of 3.64 × 104, 3.12 × 104

Adel F. Shoukry; Mahmoud S. Rizk; Yousry M. Issa; Ehab M. Atia

1997-01-01

375

IMMOBILIZATION OF WILD COLLARED ANTEATERS WITH KETAMINE AND XYLAZINE-HYDROCHLORIDE  

Microsoft Academic Search

d'Etude pour I'Amenagement et Ia Protection de Ia Nature en Guyane), BP 411, 97328 Cayenne cedex, Guyane fran#{231}aise ABSTRACT: Collared anteaters (Tarnandua tetradactyla) were immobilized for clinical procedures as part of a wildlife rescue during the filling of a hydroelectric dam (Petit Saut, French Guiana) from March 1994 to March 1995. Two doses of ketamine hydrochloride (KH) (group I I

Christine Fournier-Chambrillon; Pascal Fournler; Jean-Christophe Vie

1997-01-01

376

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

Microsoft Academic Search

Liposomes or oil-in-water emulsions containing egg yolk phosphatidylcholine (EPC) were combined with aqueous polyhexamethylene biguanide hydrochloride (PHMB). The bactericidal activity of these preparations against Pseudomonas aeruginosa and Staphylococcus aureus as well as their cytotoxicity on cultured murine fibroblasts (L929 cells) was then assayed for either 30min or 60min in the presence of cell culture medium containing 10% fetal bovine serum

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

2011-01-01

377

Simultaneous Determination of Sitagliptin Phosphate Monohydrate and Metformin Hydrochloride in Tablets by a Validated UPLC Method.  

PubMed

A novel approach was used to develop and validate a rapid, specific, accurate and precise reverse phase ultra performance liquid chromatographic (UPLC) method for the simultaneous determination of Sitagliptin phosphate monohydrate and Metformin hydrochloride in pharmaceutical dosage forms. The chromatographic separation was achieved on Aquity UPLC BEH C8 100 × 2.1 mm, 1.7 ?m, column using a buffer consisting of 10 mM potassium dihydrogen phosphate and 2 mM hexane-1-sulfonic acid sodium salt (pH adjusted to 5.50 with diluted phosphoric acid) and acetonitrile as organic solvent in a gradient program. The flow rate was 0.2 mL min(-1) and the detection wavelength was 210 nm. The limit of detection (LOD) for Sitagliptin phosphate monohydrate and Metformin hydrochloride was 0.2 and 0.06 ?g mL(-1), respectively. The limit of quantification (LOQ) for Sitagliptin phosphate monohydrate and Metformin hydrochloride was 0.7 and 0.2 ?g mL(-1), respectively. This method was validated with respect to linearity, accuracy, precision, specificity and robustness. The method was also found to be stability-indicating. PMID:22396910

Malleswararao, Chellu S N; Suryanarayana, Mulukutla V; Mukkanti, Khagga

2012-01-01

378

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

379

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

PubMed

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

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

2014-09-01

380

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

381

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

PubMed Central

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

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

2013-01-01

382

[Preparation and in vitro evaluation of self-assembled beads drug delivery system of berberine hydrochloride].  

PubMed

The purpose of the present work was to investigate the innovative self-assembling system, "beads", prepared by continuously shaking alpha-cyclodextrin and soybean oil without the use of organic solvents and surfactants at room temperature. Berberine hydrochloride previously dissolved in soybean oil was chosen as a model drug to explore the shape, structure, drug loading and in vitro release of beads. The particle size and drug loading of berberine hydrochloride-loaded beads were (2.25 +/- 0.23) mm and (67.02 +/- 0.64) microg x g(-1), respectively. Confocal microscopy showed that the core-shell structure of beads could contain poorly water soluble drugs or lipophilic drugs in the lipid core. The drug release rate and cumulative releases of beads were both higher than those of raw medicine of berberine hydrochloride in simulated intestinal fluid. These results suggested that beads were the novel and potential lipid-based drug delivery system for lipophilic or poorly water soluble traditional Chinese medicine. PMID:24066585

Liu, Chuan; Xu, Yani; Ouyang, Hui; Yi, Tao

2013-06-01

383

Pioglitazone hydrochloride: chemopreventive potential and development of site-specific drug delivery systems.  

PubMed

Abstract The aim of this study was to investigate the potential of pioglitazone hydrochloride as a promising anticancer agent and then to design and evaluate the colon-targeted delivery system. The role of pioglitazone hydrochloride as a promising anticancer agent was evaluated by in vitro cell line studies and in vivo 1,2-dimethylhydrazine-induced colon carcinogenesis in rats. In order to deliver the drug at site of action, i.e. colon, drug embedded in matrices containing a release retarding polymer (HPMC K4M) and a polysaccharide (locust bean gum) were prepared. These matrix systems were further enteric coated with Eudragit®S100 to minimize the premature drug release in the upper segments of the GIT. In vitro dissolution studies were performed in absence and presence of rat caecal contents on selected batches and samples were analyzed using a validated RP-HPLC method. Hence, the studies led to the conclusion that successful site-specific delivery systems of pioglitazone hydrochloride were developed to improve its therapeutic efficacy in the management of colorectal cancer. PMID:24547712

Sinha, Vivek Ranjan; Sethi, Shilpa

2014-02-19

384

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/sq·cm compared to 744.81 ± 125.41??g/sq·cm after modulated alternating current iontophoresis for 2?h. Modulated direct current iontophoresis also enhanced lidocaine delivery by twelvefold compared to passive delivery as 91.27 ± 18.71??g/sq·cm of lidocaine was delivered after passive delivery. Modulated iontophoresis enhanced the delivery of lidocaine hydrochloride across porcine skin compared to the passive delivery. Modulated alternating current iontophoresis for duration of 2?h at frequency of 1?kHz was found to be comparable to the continuous direct current iontophoresis for 1?h. PMID:24959580

Banga, Ajay K.

2014-01-01

385

Liquid chromatographic methods for the determination of vildagliptin in the presence of its synthetic intermediate and the simultaneous determination of pioglitazone hydrochloride and metformin hydrochloride.  

PubMed

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

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

2011-09-01

386

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

387

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

NASA Astrophysics Data System (ADS)

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

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

2010-09-01

388

A new hydrophilic interaction liquid chromatographic (HILIC) procedure for the simultaneous determination of pseudoephedrine hydrochloride (PSH), diphenhydramine hydrochloride (DPH) and dextromethorphan hydrobromide (DXH) in cough-cold formulations.  

PubMed

A new HILIC method has been developed for the simultaneous determination of pseudoephedrine hydrochloride (PSH), diphenhydramine hydrochloride (DPH) and dextromethorphan hydrobromide (DXH) in cough-cold syrup. Mobile phase consists of methanol:water (containing 6.0 g of ammonium acetate and 10 mL of triethylamine per liter, pH adjusted to 5.2 with orthophosphoric acid), 95:5 (v/v). Column containing porous silica particles (Supelcosil LC-Si, 25 cm x 4.6 mm, 5 microm) is used as stationary phase. Detection is carried out using a variable wavelength UV-vis detector at 254 nm for PSH and DPH, and at 280 nm for DXH. Solutions are injected into the chromatograph under isocratic condition at constant flow rate of 1.2 mL/min. Linearity range and percent recoveries for PSH, DPH and DXH were 150-600, 62.5-250, 75-300 microg/mL and 100.7%, 100.1% and 100.8%, respectively. Method is stability indicating and excipients like saccharin sodium, sodium citrate, flavour and sodium benzoate did not interfere in the analysis. Compounds elute in order of increasing ionization degree caused by cation-exchange mechanism in a run time of less than 15 min. Mobile phase pH is manipulated to regulate ionization and ion-exchange interaction and thereby retention of compounds. PMID:16887317

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

2007-01-01

389

Dietary zilpaterol hydrochloride. I. Feedlot performance and carcass traits of steers and heifers.  

PubMed

Experiments were conducted at 3 US locations (CA, ID, and TX) to determine the effects of dietary zilpaterol hydrochloride (Zilmax, Intervet Inc., Millsboro, DE) and duration of zilpaterol feeding on performance and carcass merit of finishing steers and heifers. At each site, 160 steers and 160 heifers were stratified within sex by initial BW (study d -1) and assigned randomly within BW strata to 1 of 4 treatments in a randomized complete block design (4 blocks/treatment for each sex). The 4 treatments were arranged in a 2 (no zilpaterol vs. zilpaterol) x 2 (20 or 40 d duration of zilpaterol feeding) factorial arrangement of treatments. When included in the diet, zilpaterol was supplemented at 8.3 mg/kg of DM. Each pen consisted of 10 animals. Each animal was individually weighed unshrunk on d 1, 21 or 41, and 66 of the experiment. Following d 66, cattle were slaughtered and carcass data collected. Feeding zilpaterol increased (P<0.01) final BW of steers and heifers by 11.6 and 6.7 kg, respectively. In addition, feeding zilpaterol hydrochloride increased (P or= 0.12) and KPH (P >or= 0.70) were not affected by feeding zilpaterol to steers or heifers. Feeding zilpaterol decreased (i.e., improved; P=0.02) calculated yield grade of steer and heifer carcasses. Marbling score (P=0.002) and quality grade (P=0.002) were decreased when zilpaterol hydrochloride was fed to steers, and the decrease in marbling score and quality grade tended to be greater when zilpaterol was fed for 40 compared with 20 d (zilpaterol x duration interaction, P=0.07). For heifers, marbling score tended (P=0.07) to be decreased and quality grade was decreased (P=0.05) when zilpaterol hydrochloride was fed. In general, it appears from these data that zilpaterol hydrochloride fed for 20 to 40 d at the end of the finishing period enhances growth performance and carcass muscle deposition for steers and heifers. PMID:19098247

Montgomery, J L; Krehbiel, C R; Cranston, J J; Yates, D A; Hutcheson, J P; Nichols, W T; Streeter, M N; Bechtol, D T; Johnson, E; TerHune, T; Montgomery, T H

2009-04-01

390

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

PubMed Central

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

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

2013-01-01

391

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

PubMed

A simple, sensitive and specific fluorimetric method has been developed for the determination of thioridazine hydrochloride in human plasma involving solid phase extraction (SPE). In a flow-injection system, thioridazine hydrochloride is on-line oxidized into a strongly fluorescent compound with a lead dioxide solid-phase reactor and the fluorescence intensity is measured with a fluorescence detector (lambda(ex)=349nm, lambda(em)=429nm). A comparison of plasma sample pretreatment between SPE procedure and precipitation method was made and the results showed that SPE procedure was better than precipitation method. Under the optimum conditions, the fluorescence intensity is proportional to the concentration of thioridazine hydrochloride in the range from 0.015 to 2.000microg mL(-1). The detection limit is 5.5ng mL(-1) of thioridazine hydrochloride and the relative standard deviation is 1.06%. This method has been applied to determination of thioridazine hydrochloride in real patients plasma samples with the results compared with those obtained by HPLC method. PMID:19071563

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

2007-03-30

392

Metabonomic study of biochemical changes in the serum of type 2 diabetes mellitus patients after the treatment of metformin hydrochloride.  

PubMed

A metabonomic study on biochemical changes in the serum of type 2 diabetes mellitus patients after the treatment of metformin hydrochloride was performed. (1)H NMR and UPLC/MS were used to generate metabolic fingerprints for the metabonomic analysis of serum samples obtained from 20 type 2 diabetes mellitus patients without any drugs treatment and 15 type 2 diabetes mellitus patients treated with metformin hydrochloride for 3 months. The resulting data were subjected to chemometric analysis (principal component analysis and partial least squares discriminant analysis) to investigate the effect of metformin hydrochloride on serum metabolite profiles of type 2 diabetes mellitus patients. (1)H NMR spectroscopic analysis revealed increased trimethylamine-N-oxide (TMAO), 3-hydroxybutyrate (3-HB) and decreased glucose, N-acetyl glycoprotein (NAC), lipoprotein, lactate, acetoacetate and unsaturated lipids in serum from metformin treated patients compared to untreated ones. UPLC/MS in positive electrospray ionization detected increased tryptophan and decreased lysophosphatidylcholines (C16:0 LPC, C18:0 LPC and C18:2 LPC) as well as phenylalanine in treated group. Both analytical techniques used in this study were able to detect biochemical changes in the serum of type 2 diabetes mellitus patients after the treatment of metformin hydrochloride, which may be helpful to the understanding of action mechanism of metformin hydrochloride. PMID:19249171

Huo, Taoguang; Cai, Shuang; Lu, Xiumei; Sha, Yi; Yu, Mingyang; Li, Famei

2009-05-01

393

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

PubMed

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 standard are separated on a reversed phase cyano column (5 microm ps, 250 mm x 4.6 id) using acetonitrile: water (70:30 v/v) adjusted to pH = 7 as a mobile phase. The drugs were detected at 221 nm over a concentration range of 5-40 microg ml(-1) and 5-60 microg ml(-1) with mean percentage recoveries 99.75% (S.D. 0.910) and 99.99% (S.D. 0.450) for sulpiride and mebeverine hydrochloride respectively. The second method is High Performance Thin Layer Chromatography, where sulpiride and mebeverine hydrochloride are separated on silica gel HPTLC F(254) plates using absolute ethanol:methylene chloride:triethyl amine (7:3:0.2 by volume) as mobile phase and scanning of the separated bands at 221 nm over a concentration range of 0.4-1.4 and 0.2-1.6 microg band(-1) with mean percentage recoveries 101.01% (S.D. 1.991) and 100.40% (S.D. 1.868) for sulpiride and mebeverine hydrochloride respectively. PMID:20538381

Naguib, Ibrahim A; Abdelkawy, Mohammed

2010-09-01

394

Simultaneous determination of metformin hydrochloride and pioglitazone hydrochloride in binary mixture and in their ternary mixture with pioglitazone acid degradate using spectrophotometric and chemometric methods.  

PubMed

In this work two well known oral hypoglycemic drugs that are administered in combination for patients with type-II diabetes were simultaneously determined. Several spectrophotometric methods were developed and validated for the determination of metformin hydrochloride (MET), pioglitazone hydrochloride (PIO) and pioglitazone acid degradate (PIO Deg). Derivative, ratio derivative, isosbestic and chemometric-assisted spectrophotometric methods were developed. The first derivative (D(1)) method was used for the determination of MET in the range of 5-30 microg x mL(-1) and PIO in the range of 10-90 microg x mL(-1) by measuring the peak amplitude at 247 nm and 280 nm, respectively. The concentration of PIO was calculated directly at 268 nm. The first derivative of ratio spectra (DD(1)) method used the peak amplitudes at 238 nm and 248.6 nm for the determination of MET in the range of 5-30 microg x mL(-1). In the isosbestic point method (ISO), the total mixture concentration was calculated by measuring the absorbance at 254.6 nm. Classical least squares (CLS), principal component regression (PCR) and partial least squares (PLS-2) were used for the quantitative determination of MET, PIO and PIO Deg. The methods developed have the advantage of simultaneous determination of the cited components without any pre-treatment. Resolution and quantitative determination of PIO degradate with a minimum concentration of 3 microg x mL(-1) in drug samples was done. The proposed methods were successfully used to determine each drug and the acid degradate in a laboratory-prepared mixture and pharmaceutical preparations. The results were statistically compared using one-way analysis of variance (ANOVA). The methods developed were satisfactorily applied to the analysis of the two drugs in pharmaceutical formulations. PMID:20355212

Hegazy, Maha A; El-Ghobashy, Mohamed R; Yehia, Ali M; Mostafa, Azza A

2009-07-01

395

Pharmacokinetics and in vivo chemosuppressive activity studies on cryptolepine hydrochloride and cryptolepine hydrochloride-loaded gelatine nanoformulation designed for parenteral administration for the treatment of malaria.  

PubMed

The main objective of this investigation was to establish the pharmacokinetics profile and in vivo chemosuppressive activities of cryptolepine hydrochloride-loaded gelatine nanoparticles (CHN) designed for parenteral administration for the treatment of malaria in comparison to the drug free in solution (CHS). Single-dose pharmacokinetics was investigated in Wistar rats by administering CHN or CHS (equivalent to 10 mg/kg of drug) by IV bolus injection via the lateral tail vein. The drug concentration in plasma was monitored over a 24-h period following administration. Chemosuppressive activity was investigated in Wistar rats challenged with P berghei parasites. Animals were given a daily dose of either CHN or CHS, equivalent to 2.5-100 mg/kg by intraperitoneal injection. The level of parasitaemia was determined by light microscopy by examining Giemsa-stained thin blood smears prepared from the tail end on day four of infection. It was found that CHN attained a higher (4.5-folds) area under the curve (AUC (0-24)) compared to CHS. CHS however produced a higher volume of distribution (4-folds). Distribution and elimination rates were higher with CHS which resulted in a lower (11.7 h) elimination half-life compared to that of CHN (21.85 h). The superior pharmacokinetic profile of CHN translated into superior chemosuppressive activity at all dose levels relative to CHS. As a conclusion, loading cryptolepine hydrochloride into gelatine nanoparticles improved both pharmacokinetics and in vivo antiplasmodial activity of the compound with the highest chemosuppression (97.89 ± 3.10) produced by 100 mg/kg of CHN. PMID:23643517

Kuntworbe, N; Ofori, M; Addo, P; Tingle, M; Al-Kassas, R

2013-09-01

396

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 µg/band) and (0.4-2.2 µg/band) with good accuracy for HCZ and BZ, respectively, for the first mixture and in the range of (0.6-1.8 µg/band) and (0.4-2.4 µg/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

397

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

PubMed

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

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

2014-04-01

398

Stability and compatibility of anakinra with intravenous cimetidine hydrochloride or famotidine in 0.9% sodium chloride injection.  

PubMed

We designed a study to evaluate the stability and compatibility of anakinra (recombinant human interleukin-1 receptor antagonist) with cimetidine hydrochloride or famotidine in 0.9% sodium chloride injection during a 4-h period at room temperature (22 degrees C) and light. Anakinra was diluted in 0.9% sodium chloride to concentrations of 4 and 36 mg/ml. At each concentration, anakinra was mixed with 3 mg/ml cimetidine or with 1 mg/ml famotidine, in a 50:50 proportion and stored in plastic culture vials with polypropylene caps. The mean concentrations of anakinra, cimetidine hydrochloride, and famotidine exceeded 95% of initial concentrations throughout the study. No changes were noted in the physical appearance, pH, or the chromatograms during the study period. Thus, anakinra appears to be stable and compatible with cimetidine hydrochloride or famotidine when diluted into 0.9% sodium chloride injection for 4 h at ambient room temperature and light. PMID:7650081

Nahata, M C; Morosco, R S; Sabados, B K; Weber, T R

1995-04-01

399

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

PubMed

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

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

2006-10-01

400

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

PubMed

Metomidate hydrochloride is an imidazole-based, nonbarbiturate hypnotic drug primarily used as an immersion sedation and anesthetic agent in freshwater and marine finfish. To the authors' knowledge, there is no documentation in the literature of its use in amphibians. In this study, 7 male and 4 female leopard frogs (Rana pipiens) were induced with metomidate hydrochloride via immersion bath at a concentration of 30 mg/L for 60 min. The pH of the induction solution ranged from 7.63 to 7.75. Each frog was then removed from the induction solution, rinsed, and recovered in 26.6 degrees C amphibian Ringer's solution. After 210 min in the Ringer's solution, the frogs were transferred to moist paper towels for recovery. Heart rate, gular and abdominal respiration rates, righting reflex, superficial and deep pain withdrawal reflexes, corneal and palpebral reflexes, and escape response were monitored and recorded at defined intervals during both induction and recovery. The average time to loss of righting reflex and escape response was 17.36 min and 17.82 min, respectively. Metomidate produced clinical sedation in all frogs (n = 11). Surgical anesthesia was achieved in only 27% (3/11), with an anesthetic duration that ranged from 9 to 20 min. Recovery times were extremely prolonged and varied, with a range from 313 min to longer than 600 min. The findings of this study indicate that metomidate hydrochloride is unsuitable as a sole anesthetic agent in leopard frogs, and further research is needed to evaluate its suitability in other amphibians. PMID:24712162

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

2014-03-01

401

Cardiovascular effects in man of intravenous prizidilol hydrochloride (SK&F 92657); a new antihypertensive agent.  

PubMed Central

1 Cardiovascular responses to intravenous prizidilol hydrochloride (SK&F 92657) 0.86 mg/kg were studied in eight supine resting healthy volunteers. Five subjects were slow and the remaining three were fast acetylators of sulphamethazine. Compared with pre-infusion values, mean resting systolic and diastolic blood pressures were significantly reduced, while mean resting pulse rate was significantly increased at 30 min after the start of the twenty minute infusion. 2 During the 6 h study period the lowest mean +/- s.e. mean systolic blood pressure (108.8 +/- 1.7) was recorded 30 min after the start of the infusion. This represented a mean reduction of 5.2 mmHg. Reductions in mean diastolic blood pressure were greater and of longer duration, the lowest mean value (44.8 +/- 2.0 mmHg) being recorded 3.5 h after the start of the infusion and representing a reduction of 18.5 mmHg from the pre-dosing value. At 6 h after the start of the infusion mean diastolic blood pressure was still significantly reduced (by 15.3 mmHg). 3 The maximum mean +/- s.e. mean resting pulse rate (79.3 +/- 4.4 beats/min) occurred 3 h after the start of the infusion, an increase of 23.0 beats/min over the pre-infusion value. At the end of the study the pulse rate was still significantly raised (by 17.7 beats/min). 4 The left ventricular ejection fraction, evaluated in five subjects, 45 min after the start of the infusion, was not altered by prizidilol hydrochloride, but the left ventricular area decreased significantly. 5 Intravenous prizidilol hydrochloride decreases resting blood pressure and left ventricular area, increases pulse rate and has virtually no effect on left ventricular ejection fraction. PMID:7295490

Edmonstone, W M; Manghani, K K; Bell, A J; McLeod, M; Milton-Thompson, G J; Burland, W L

1981-01-01

402

Comparative antifungal efficacy of light-activated disinfection and octenidine hydrochloride with contemporary endodontic irrigants.  

PubMed

The aim of this study was to evaluate the antifungal effects of light-activated disinfection (LAD) in comparison with contemporary root canal irrigation solutions: sodium hypochlorite and 2 % chlorhexidine gluconate and a new wound antiseptic, octenidine hydrochloride. Seventy extracted teeth having single root canals were contaminated with Candida albicans for 14 days. The samples were divided into five experimental (n?=?10) and two control (positive and negative) groups (n?=?10): (1) LAD with toluidine blue O, (2) octenidine hydrochloride (OCT), (3) 2.5 % sodium hypochlorite (2.5 % NaOCl), (4) 5.25 % sodium hypochlorite (5.25 % NaOCl) and (5) 2 % chlorhexidine. Five millilitres of each test solution was applied for 3 min, and irradiation time used for LAD was 30 s. After treatment, the dentin chips were collected from inner canal walls into vials containing phosphate buffered saline, vortexed, serially diluted, seeded on Tryptic Soy Agar plates and incubated (37 °C, 48 h). The number of colony-forming units was then counted. Differences between LAD group and positive control group were statistically significant (P?hydrochloride, demonstrated better potential than LAD in elimination of Candida albicans cells and may be a promising alternative to NaOCl and chlorhexidine solutions in future. PMID:23884903

Eldeniz, Ayce Unverdi; Guneser, Mehmet Burak; Akbulut, Makbule Bilge

2015-02-01

403

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

PubMed

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

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

2010-09-01

404

Comparison of two different formulations of mebeverine hydrochloride in irritable bowel syndrome.  

PubMed

A total of 213 patients were recruited to a multicentre, randomised, double-blind, double dummy, general practice study lasting eight weeks. The objectives of the study were (i) to demonstrate therapeutic equivalence of mebeverine hydrochloride 200 mg b.i.d. capsules (Colofac MR) and 135 mg t.i.d. tablets (Colofac) in the treatment of abdominal pain in irritable bowel syndrome (IBS) and (ii) to evaluate safety and physicians' and patients' assessments of therapeutic response. Patients were randomised at day 0 and assessments performed after four and eight weeks. Primary and secondary efficacy endpoints were number of responders (response being defined as 50% or more improvement in global mean visual analogue scale for abdominal pain); patients' and physicians' global assessment of therapeutic response; and physicians' global impression of patient symptoms. Safety was assessed from adverse event reports and routine laboratory tests. Therapeutic equivalence was proven statistically (difference < 18%; p = 0.003), with 65/92 (71%) of the 135 mg t.i.d. group and 64/92 (70%) of the 200 mg b.i.d. group classified as responders. The patients' evaluation of response (week 8) was that 75% of 135 mg t.i.d. and 81% of 200 mg b.i.d. improved; the physicians' assessment of therapeutic response (week 8) was that 64% of 135 mg t.i.d. and 70% of 200 mg b.i.d. had no or mild symptoms. In conclusion, Mebeverine hydrochloride 200 mg b.i.d. (Colofac MR) was shown to be therapeutically equivalent to mebeverine hydrochloride 135 mg t.i.d. (Colofac) in the treatment of abdominal pain in IBS. Results for the secondary efficacy variables were comparable. No safety concerns were identified. PMID:11070572

Gilbody, J S; Fletcher, C P; Hughes, I W; Kidman, S P

2000-09-01

405

Metabolomic Analyses of Blood Plasma after Oral Administration of D-Glucosamine Hydrochloride to Dogs  

PubMed Central

D-Glucosamine hydrochloride (GlcN?HCl) is an endogenous amino monosaccharide synthesized from glucose that is useful in the treatment of joint diseases in both humans and animals. The aim of this study was to examine amino acid metabolism in dogs after oral administration of GlcN?HCl. Accelerated fumarate respiration and elevated plasma levels of lactic acid and alanine were observed after administration. These results suggest that oral administration of GlcN?HCl induces anaerobic respiration and starvation in cells, and we hypothesize that these conditions promote cartilage regeneration. Further studies are required to evaluate the expression of transforming growth factor-beta (TGF-?). PMID:23015778

Osaki, Tomohiro; Azuma, Kazuo; Kurozumi, Seiji; Takamori, Yoshimori; Tsuka, Takeshi; Imagawa, Tomohiro; Okamoto, Yoshiharu; Minami, Saburo

2012-01-01

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

Zilpaterol Hydrochloride on Performance and Sperm Quality of Lambs Fed Wet Brewers Grains  

Microsoft Academic Search

Aguilera-Soto, J.I., Ramirez, R.G., Arechiga, C.F., Mendez-Llorente, F., Lopez-Carlos, M.A., Silva-Ramos, J.M., Rincón-Delgado, R.M. and Duran-Roldan, F.M. 2008. Zilpaterol hydrochloride on performance and sperm quality of lambs fed wet brewers grain. J. Appl. Anim. Res., 34: 17–21.Forty Rambouillet × elibuey male lambs were grouped as light-weight (LW; n =20; 28±1.2 kg BW) and heavy-weight (HW; n = 20; 40.5±1.6 kg

J. I. Aguilera-Soto; R. G. Ramirez; C. F. Arechiga; F. Mendez-Llorente; M. A. Lopez-Carlos; J. M. Silva-Ramos; R. M. Rincon-Delgado; F. M. Duran-Roldan

2008-01-01

408

Liquid chromatographic determination of methylparaben and propylparaben in nortriptyline hydrochloride oil-water microemulsions  

Microsoft Academic Search

Summary  A reversed-phase LC method using UV detection has been developed and validated for the analysis of methylparaben and propylparaben\\u000a in nortriptyline hydrochloride oil-water (o-w) microemulsions. The precision and accuracy of the method was excellent with\\u000a RSD values of 4.53% and 2.13% respectively for methylparaben, and 3.69% and 2.06% respectively for propylparaben. The linearity\\u000a established was 50–150% of theoretical concentrations of

M. A. Moreno; D. Castro; P. Frutos; M. P. Ballesteros; J. L. Lastres

2000-01-01

409

Quantitative Analysis of Propranolol Hydrochloride by High Performance Thin Layer Chromatography  

PubMed Central

A simple, accurate and precise HPTLC method has been developed for estimation of propranolol hydrochloride from bulk drug and tablet formulations. The separation was achieved on TLC plates using appropriate solvent system. The spots so developed were densitometrically scanned at 290 nm. The linearity of the method was found to be within the concentration range of 200–2000 ng/spot. The validation parameters, tested in accordance with the requirements of ICH guidelines, prove the suitability of this method. The method was successively applied for determination of drug in tablets, wherein, no interference from tablet excipients was observed. PMID:20046758

Bhavar, Girija; Chatpalliwar, V. A.

2008-01-01

410

A new commercially viable synthetic route for donepezil hydrochloride: anti-Alzheimer's drug.  

PubMed

An economical new process has been developed for the synthesis of donepezil hydrochloride (1) an anti-Alzheimer's drug. The process involves Darzen reaction of pyridine-4-carboxaldehyde and 2-bromo-5,6-dimethoxy indanone affording epoxide 5,6-dimethoxy-3-(pyridine-4-yl)spiro[indene-2,2'-oxiran]-1(3H)-one (4) as a key intermediate. The one-pot deoxygenation of 4 and hydrogenation of the aryl moiety in high yield improved the overall yield of the process. PMID:20823593

Dubey, Shailendra Kumar; Kharbanda, Manita; Dubey, Sushil Kumar; Mathela, Chandra Shekhar

2010-09-01

411

Assessment of bioavailability of experimental single-unit sustained release tablets of verapamil hydrochloride using the stable isotope technique.  

PubMed

A stable isotope technique has been used to assess the bioavailability of sustained release verapamil products. The test formulations were tablets with a core containing 90 mg of verapamil hydrochloride coated with ethylcellulose film, the permeability of which was controlled using different amounts of hydroxypropyl methylcellulose. A product containing ethylcellulose 75% hydroxypropyl methylcellulose 25% w/w gave a single-unit sustained release tablet of verapamil hydrochloride that allowed a dose interval of 24 h. There was no loss in bioavailability, even though verapamil had extensive first-pass metabolism. PMID:2867156

Marvola, M; Kannikoski, A; Taskinen, J; Ottoila, P

1985-11-01

412

Cerebral perfusion imaging in Alzheimer's disease. Use of single photon emission computed tomography and iofetamine hydrochloride I 123  

SciTech Connect

We used single photon emission computed tomography (SPECT) to study 15 patients with Alzheimer's disease and nine controls. Iofetamine hydrochloride I 123 uptake data were recorded from the entire brain using a rotating gamma camera. Activity ratios were measured for the frontal, posterior parietal, posterior, medial, and lateral cortical temporal regions and striate cortex and were normalized by the activity in the cerebellum. Abnormalities in iofetamine hydrochloride I 123 activity were similar to the abnormalities in glucose metabolism observed with positron emission tomography. Cortical tracer activity was globally depressed in patients with Alzheimer's disease, with the greatest reduction in the posterior parietal cortex.

Johnson, K.A.; Mueller, S.T.; Walshe, T.M.; English, R.J.; Holman, B.L.

1987-02-01

413

Simultaneous determination of the counter ion and possible impurity from the synthetic route in the pharmaceutical substance prasugrel hydrochloride.  

PubMed

A fast and selective capillary electrophoresis method was developed and validated for the simultaneous determination of the hydrochloride and acetic acid content in prasugrel hydrochloride. Because of the poor chromophore, the indirect detection was chosen. Among different compositions studied as the background electrolyte, the pyromellitic acid with diethylamine (DEA) and myristyltrimethylammonium bromide (TTAB) was chosen. During the validation the specificity, linearity, accuracy, precision, range, and stability of the sample solution were confirmed. The results indicate that the method is suitable for the determination of the counter ion and impurity from the synthetic route of the pharmaceutical drug substance in the same assay. PMID:25527979

Maruszak, Wioleta; Cybulski, Marcin

2015-02-01

414

Stimulatory action of itopride hydrochloride on colonic motor activity in vitro and in vivo.  

PubMed

We investigated the effects of itopride hydrochloride (itopride, N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide hydrochloride), a gastroprokinetic agent, on the colonic motor activity in vitro and in vivo, in comparison with benzamides, cisapride hydrate (cisapride), and mosapride citrate (mosapride). Itopride stimulated both peristaltic and segmental motility induced by applying intraluminal pressure to the isolated guinea pig colon. Although cisapride and mosapride enhanced the segmental motility, they markedly reduced the peristaltic motility. In conscious dogs with implanted strain gauge force transducers, itopride stimulated contractile activity in the gastrointestinal tract from the stomach to the colon. Cisapride stimulated contractile activity in the gastric antrum, ileum, and ascending colon. Mosapride stimulated contractile activity only in the gastric antrum and ileum. In guinea pigs and rats, itopride accelerated colonic luminal transit. On the other hand, cisapride and mosapride failed to enhance colonic transit. These results demonstrate that itopride has a stimulatory action on colonic peristalsis, propelling colonic luminal contents, different from that of cisapride and mosapride. Therefore, itopride may be a useful drug for the treatment of functional bowel disorders such as functional constipation. PMID:12724347

Tsubouchi, Tadashi; Saito, Takaharu; Mizutani, Fujie; Yamauchi, Toshie; Iwanaga, Yuji

2003-08-01

415

Efficacy and tolerability of itopride hydrochloride in patients with non-ulcer dyspepsia.  

PubMed

To document the clinical efficacy and tolerability of itopride hydrochloride in patients with non-ulcer dyspepsia an open-label, non-comparative study, was undertaken at the Medical College, Thiruvananthapuram, among patients with endoscopically confirmed diagnosis of non-ulcer dyspepsia or chronic gastritis. Itopride hydrochloride 50 mg (1 tablet) thrice a day for 2 weeks was administered among them. Relief of symptoms at the end of two weeks treatment, assessed as marked/complete, moderate, slight, none or worse; QT interval on ECG; adverse events; haemogram; serum chemistry for hepatic and renal functions. None had QT prolongation on ECG. At the end of 2 weeks' treatment, moderate to complete relief of symptoms was reported by 22 patients (73%), whereas 5 (17%) reproted slight improvement, and 3 (10%) reported no improvement. Clinical tolerability was excellent in 28 patients (93%) and good in 2 (7%). None of the patients had any prolongation of QT on ECG, nor did any patient show any abnormality in haemogram or serum chemistry during the treatment. PMID:14579989

Shenoy, K T; Veenasree; Leena, K B

2003-06-01

416

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

417

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

418

Spectinomycin hydrochloride in the treatment of gonorrhoea: Its effect on associated Chlamydia trachomatis infections.  

PubMed

Sixty-three heterosexual men were successfully treated with a single injection of spectinomycin hydrochloride 2 g for urethral infections with Neisseria gonorrhoeae. Chlamydia trachomatis was recovered from the urethra of 11 of these men both before and after treatment. In six men, the organism was isolated after but not before treatment. No isolates were obtained from the remaining men either before or after treatment. All 17 of the men who yielded C. trachomatis developed post-gonococcal urethritis. Eight of 46 men from whom no isolate was obtained in their cultures developed post-gonococcal urethritis. Seventeen of 50 women successfully treated with spectinomycin for cervical infections with N. gonorrhoeae yielded isolates of C. trachomatis both before and after treatment. The organism was isolated from five women before but not after treatment, and from four women after but not before treatment. In 24 women culture for C. trachomatis was negative both before and after treatment. Spectinomycin hydrochloride in the dosage used rarely eliminated C. trachomatis from the genital tract of either men or women; in this respect it resembled two other drugs commonly used for the treatment of gonorrhoea-pencillin and ampicillin. PMID:144543

Oriel, J D; Ridgway, G L; Tchamouroff, S; Owen, J

1977-08-01

419

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

PubMed Central

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

Bhoyar, PK; Biyani, DM; Umekar, MJ

2010-01-01

420

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

PubMed

The aim of this study was to investigate the effect of benzydamine hydrochloride bioadhesive gel on healing of oral mucosal ulceration in an animal model. For in vivo determination of the effects of the bioadhesive gel, 36 rabbits were separated into three groups: the first group was treated with the gel formulation without active agent, the second group with the gel formulation containing benzydamine, and the third group received no treatment. Clinical healing was established by measuring the area of the ulcer in each test group on days 3, 6, 9 and 12. Histological healing was determined on the same days. Benzydamine containing gel applications resulted in a decrease in the ulcer area in 12 days (p=0.000). Histological evaluation showed that the benzydamine group had a higher mean histological score than the base and the control groups during the whole test period, and the difference between the benzydamine group and the control group was significant (p=0.04). The bioadhesive gel formulation of benzydamine hydrochloride showed a statistically significant increased rate of mucosal repair in this experimental standard mucosal wound animal study. It is a candidate for the topical treatment of oral mucosal ulcerative lesions. PMID:21549562

Karavana Hizarcio?lu, S Y; Sezer, B; Güneri, P; Veral, A; Boyacio?lu, H; Ertan, G; Epstein, J B

2011-09-01

421

Analytical control of process impurities in Pazopanib hydrochloride by impurity fate mapping.  

PubMed

Understanding the origin and fate of organic impurities within the manufacturing process along with a good control strategy is an integral part of the quality control of drug substance. Following the underlying principles of quality by design (QbD), a systematic approach to analytical control of process impurities by impurity fate mapping (IFM) has been developed and applied to the investigation and control of impurities in the manufacturing process of Pazopanib hydrochloride, an anticancer drug approved recently by the U.S. FDA. This approach requires an aggressive chemical and analytical search for potential impurities in the starting materials, intermediates and drug substance, and experimental studies to track their fate through the manufacturing process in order to understand the process capability for rejecting such impurities. Comprehensive IFM can provide elements of control strategies for impurities. This paper highlights the critical roles that analytical sciences play in the IFM process and impurity control. The application of various analytical techniques (HPLC, LC-MS, NMR, etc.) and development of sensitive and selective methods for impurity detection, identification, separation and quantification are highlighted with illustrative examples. As an essential part of the entire control strategy for Pazopanib hydrochloride, analytical control of impurities with 'meaningful' specifications and the 'right' analytical methods is addressed. In particular, IFM provides scientific justification that can allow for control of process impurities up-stream at the starting materials or intermediates whenever possible. PMID:20189340

Li, Yan; Liu, David Q; Yang, Shawn; Sudini, Ravinder; McGuire, Michael A; Bhanushali, Dharmesh S; Kord, Alireza S

2010-08-01

422

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

NASA Astrophysics Data System (ADS)

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

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

2006-09-01

423

Stability-indicating spectrofluorimetric method for determination of itopride hydrochloride in raw material and pharmaceutical formulations.  

PubMed

A simple, sensitive and rapid spectrofluorimetric method for determination of itopride hydrochloride in raw material and tablets has been developed. The proposed method is based on the measurement of the native fluorescence of the drug in water at 363 nm after excitation at 255 nm. The relative fluorescence intensity-concentration plot was rectilinear over the range of 0.1-2 ?g/mL (2.5?×?10(-7)-5.06?×?10(-6) mole/L), with good correlation (r?=?0.9999), limit of detection of 0.015 ?g/mL and a lower limit of quantification of 0.045 ?g/mL. The described method was successfully applied for the determination of itopride hydrochloride in its commercial tablets with average percentage recovery of 100.11?±?0.32 without interference from common excipients. Additionally, the proposed method can be applied for determination of itopride in combined tablets with rabeprazole or pantoprazole without prior separation. The method was extended to stability study of itopride. The drug was exposed to acidic, alkaline, oxidative and photolytic degradation according to ICH guidelines. Moreover, the method was utilized to investigate the kinetics of the alkaline, acidic and oxidative degradation of the drug. A proposal for the degradation pathways was postulated. PMID:23852162

Walash, Mohamed I; Ibrahim, Fawzia; Eid, Manal I; El Abass, Samah Abo

2013-11-01

424

Mediastinal pancreatic pseudocyst caused by obstruction of the pancreatic duct was eliminated by bromhexine hydrochloride.  

PubMed

A 49-year-old man, who had a 30-year history of drinking the equivalent of 80 g of ethanol per day, underwent a detailed medical examination for cough and dyspnea. Chest-abdominal computed tomography and endoscopic retrograde pancreatography led to the diagnosis of a mediastinal pancreatic pseudocyst resulting from obstruction of the pancreatic duct by a protein plug. The pseudocyst rapidly improved with conservative treatment with camostat mesilate, H2-receptor antagonist and digestive enzymes. Although the patient abstained from alcohol for approximately 6 months, he resumed drinking, leading to recurrent attacks of pancreatitis. Bromhexine hydrochloride was then administered for 6 months, with the expectation that it would have a mucolytic effect on the pancreatic juice, resulting in improvement in the clinical symptoms, pancreatic enzymes and pancreatic exocrine function, as well as elimination of the protein plug. Bromhexine hydrochloride may be a new therapy for pathological states, such as alcoholic chronic pancreatitis, in which there is increased viscosity of the pancreatic juice because of elevated protein concentration, leading to protein plug formation and temporary blockage of the pancreatic duct. PMID:15609697

Tsujimoto, Tatsuhiro; Takano, Masato; Tsuruzono, Takuya; Hoppo, Kazushige; Matsumura, Yoshinobu; Yamao, Jyunichi; Kuriyama, Shigeki; Fukui, Hiroshi

2004-11-01

425

Development and Validation of RP-HPLC Method for the Estimation of Ivabradine Hydrochloride in Tablets  

PubMed Central

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, 250×4.6 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 6.55±0.05 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.

2010-01-01

426

Effect of thiamine hydrochloride on the redox reactions of iron at pyrite surface  

SciTech Connect

The present investigation is a part of our studies on the electro chemical aspects of pyrite bioleaching involving Thiobacillus ferrooxidans. Previously (1,2) we have examined the effect of T. ferrooxidans and their metabolic products on the redox reactions of Fe[sup 2+]/Fe[sup 3+] couple at the pyrite surface. Results obtained suggest that beyond 1. 5 days during their growth in a batch fermenter, the bacteria and their metabolic products completely cover the pyrite surface and shut down all electron transfer across the electrode-solution interface. In addition, it has been observed that the bacteria serve as the nucleation site for jarosite formation, which is found detrimental to bioleaching. In the present work we have focussed on the effect of the presence of vitamins on the redox chemistry of iron. Our examination of the effect of the presence of thiamine hydrochloride in the redox behavior of Fe[sup 2+]/Fe[sup 3+] at the pyrite surface has revealed that thiamine hydrochloride does not undergo chemical interaction with ferrous or ferric iron. However, it may adsorb onto the pyrite surface causing polarization of the pyrite electrode.

Pesic, B.; Oliver, D.J.

1990-01-01

427

Thermoreversible nasal in situ gel of venlafaxine hydrochloride: formulation, characterization, and pharmacodynamic evaluation.  

PubMed

In order to improve the bioavailability of the antidepressant drug, venlafaxine hydrochloride, in situ mucoadhesive thermoreversible gel, was formulated using Lutrol F127 (18%) as a thermo gelling polymer. Mucoadhesion was modulated by trying carbopol 934, PVP K30, HPMC K4M, sodium alginate, tamarind seed gum, and carrageenan as mucoadhesive polymers. Results revealed that as the concentration of mucoadhesive polymer increased the mucoadhesive strength increased but gelation temperature decreased. Formulation was optimized on the basis of clarity, pH, gelation temperature, mucoadhesive strength, gel strength, viscosity, drug content, diffusion through sheep nasal mucosa, histopathological evaluation of mucosa, and pharmacodynamic study in rats. Final formulation T5 containing 18% Lutrol F127 and 0.3% PVP K30 was considered as an optimized formulation. T5 released 97.86±0.073% drug in 150 min with a flux of 0.1545 mg?cm(-2)?min(-1) and gelation temperature 31.17±0.30°C. Histopathological evaluation of nasal mucosa revealed that T5 formulation was safe for nasal administration as it caused no damage to nasal epithelium. From the results of pharmacodynamic study, mainly forced swim test (FST), it was concluded that venlafaxine hydrochloride was more effective as an antidepressant by nasal route as in situ gel nasal drops in comparison to oral administration of equivalent dose. PMID:23229381

Bhandwalkar, Mandar J; Avachat, Amelia M

2013-03-01

428

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

PubMed

Labetalol hydrochloride (LBT), 2-hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl) amino] ethyl]-benzamide, a non-selective alpha, beta-adrenoceptor antagonist is used in the treatment of hypertension. It shows variable bioavailability ranging from 10-80% which may be attributed to its minimum solubility in pH range 6 to 10, the pH conditions prevailing at the major site of absorption i.e. small intestine. Also due to its half life of 3 to 6 hrs it is administered twice daily. In the present work non-effervescent sustained release gastroretentive floating tablets of labetalol hydrochloride have been developed using various grades of HPMC and Poloxamer M127 as wetting agent. The tablets were evaluated for in vitro drug release, floating time, floating lag time, swelling studies etc. The tablets formulated with HPMC K4M CR and HPMC K15M CR along with Poloxamer showed negligible floating lag time with a total floating time over 12 hrs with complete release. Formulation was optimized using Stat-Ease Design Expert 7.1 software. Optimized batch was evaluated for the effect of change of osmolarity and pH on drug release, floating and swelling behaviour. PMID:20361305

Garse, Harshal; Vij, Mohit; Yamgar, Manohar; Kadam, Vilasrao; Hirlekar, Rajashree

2010-03-01

429

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], 0–28 025) parasites/µL × hour in patients treated with levamisole and 5489 (IQR, 192–25 848) parasites/µL × 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, 12–30) hours with levamisole vs 28 (IQR, 12–36) 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

430

Synthesis of novel 10-hydroxycamptothecin derivatives utilizing topotecan hydrochloride as ortho-quinonemethide precursor.  

PubMed

A series of 9-(alkylthiomethyl)-10-hydroxycamptothecins and pyrano-fused camptothecin derivatives were synthesized via the reaction of topotecan hydrochloride with various thiols and alkyl vinyl ethers respectively. In the reactions, topotecan hydrochloride was utilized as ortho-quinonemethide (o-QM) precursor. The configuration of 19 was determined by (1)H NMR and NOESY spectra as syn-isomers, suggesting that the cycloaddition of topotecan with alkyl vinyl ethers could undergo a hetero Diels-Alder reaction. All the synthesized compounds were screened on cancer cell lines HepG2, KB, HCT-8 and SGC7901. Some compounds were selected to assess their inhibitory activity against Topo I via Topo I mediated DNA cleavage assays. The results showed that among those tested 9-(alkylthiomethyl)-10-hydroxycamptothecins, the compounds with bulkier hydrophobic side chains at 9-position have better bioactivities. As well as all pyrano-fused camptothecins possess antiproliferative activity against the tested cancer cell lines. Docking studies suggested that there are more interactions between the novel analogues and the binding site of Topo I. PMID:25481395

Tan, Hanyi; Wang, Guolin; Li, Jiajun; Meng, Guangrong; Liu, Zhenfeng; Dong, Mengjie; Li, Yubin; Ju, Dianwen; Zhang, Qian

2015-01-01

431

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

432

Determination of donepezil hydrochloride in human plasma and pharmaceutical formulations by HPLC with fluorescence detection.  

PubMed

A sensitive, isocratic reversed-phase high performance liquid chromatographic method involving fluorescence detection was developed for the determination of donepezil hydrochloride in tablets and in human plasma. Pindolol was used as an internal standard. Good chromatographic separation was achieved by using an analytical column C18. The system operated at room temperature using a mobile phase consisting of methanol, phosphate buffer (0.02 mol L?¹) and triethyl amine (pH 3.5) (55 : 45 : 0.5, V/V/V) at a flow rate 0.9 mL?¹ min. The analyte and internal standard were extracted from human plasma via liquid-liquid extraction. The proposed method was validated for sensitivity, selectivity, linearity, accuracy and precision. The calibration curve was linear over the range of 5-2000 ng mL?¹ of donepezil with detection limit of 1.5 ng mL?¹. Intra- and inter-day relative standard deviations were less than 2.5%. The method was found to be suitable for quality control of donepezil hydrochloride in bulk drug as well as in human plasma. PMID:22202199

Abonassif, Mohammed A; Hefnawy, Mohammed M; Kassem, Mohamed G; Mostafa, Gamal A E

2011-12-01

433

Dietary zilpaterol hydrochloride. II. Carcass composition and meat palatability of beef cattle.  

PubMed

Experiments were conducted at 3 US locations (California, Idaho, and Texas) to determine the effects of dietary zilpaterol hydrochloride and duration of zilpaterol feeding on carcass composition and beef palatability. At each site, 160 steers and 160 heifers were stratified within sex by initial BW (study d -1) and assigned randomly within BW strata to 1 of 4 treatments in a randomized complete block design (4 blocks/treatment for each sex). The 4 treatments were arranged in a 2 (no zilpaterol vs. zilpaterol) x 2 (20- or 40-d duration of zilpaterol feeding) factorial. When included in the diet, zilpaterol was supplemented at 8.3 mg/kg (DM basis). Each pen consisted of 10 animals. After slaughter 2 carcasses per pen (n=64 per trial site) were selected. The entire right side of the selected carcasses was collected for dissection and chemical analysis of the soft tissue. Additionally, the left strip loin was collected for Warner-Bratzler shear force determinations and aged to 28 d postmortem. Sensory analysis was conducted on the Idaho trial site samples only. All data were pooled for analyses. Feeding zilpaterol hydrochloride increased carcass muscle deposition (P<0.01) of both steer and heifer carcasses. However, carcass percentage fat of steers and heifers was not affected (P>0.11) by the zilpaterol treatment. In heifer carcasses, carcass moisture percentage was increased (P=0.04) and bone percentage was decreased (P=0.02), whereas in steer carcasses, carcass moisture and bone percentage were not affected (P>0.10). In heifer carcasses, carcass ash percentage was not affected (P=0.61) by zilpaterol, whereas in steer carcasses, carcass ash percentage tended (P=0.07) to be increased. The protein-to-bone ratio was increased (P<0.001) by zilpaterol hydrochloride treatment in both steers and heifers, whereas the protein-to-fat ratio was not affected (P=0.10). Cooking loss of the LM was not affected (P=0.41) by zilpaterol treatment of steers or heifers. However, LM Warner-Bratzler shear force was increased (P=0.003) on average (3.3 vs. 4.0 kg) due to zilpaterol hydrochloride treatment of both steers and heifers. In both steers and heifers, LM sensory panel scores of overall juiciness (6.2 vs. 6.0), tenderness (6.2 vs. 6.0), and flavor intensity (6.2 vs. 6.0) tended (P=0.06) to be decreased in cattle supplemented with zilpaterol. Zilpaterol hydrochloride is a repartitioning agent that seems to affect carcass composition primarily through protein deposition. However, zilpaterol treatment can adversely affect tenderness and other palatability traits. PMID:18849379

Leheska, J M; Montgomery, J L; Krehbiel, C R; Yates, D A; Hutcheson, J P; Nichols, W T; Streeter, M; Blanton, J R; Miller, M F

2009-04-01

434

Effect of feeding zilpaterol hydrochloride to beef and calf-fed Holstein cattle on consumer palatability ratings  

Microsoft Academic Search

The need to provide consumer data for beef steak tenderness, juiciness, flavor, and overall palatability ratings from zilpaterol hydrochloride (ZH) beef to the processor, retailers, restaurants, and con- sumers is paramount. Consumer palatability responses were studied for 14- and 21-d aged USDA Choice and USDA Select quality grade beef and USDA Choice calf- fed Holstein New York Strip steaks from

J. M. Mehaffey; J. C. Brooks; R. J. Rathmann; E. M. Alsup; J. P. Hutcheson; W. T. Nichols; M. N. Streeter; D. A. Yates; B. J. Johnson; M. F. Miller

2009-01-01

435

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

436

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

Code of Federal Regulations, 2010 CFR

40 ? Protection of Environment ? 23 ? 2010-07-01 ? 2010-07-01 ? false ? N,N-diethyl-2-(4-methylbenz-yloxy)ethylamine hydrochloride; tolerances for residues. ? 180.558 ? Section 180.558 ? Protection of Environment ? ENVIRONMENTAL PROTECTION AGENCY (CONTINUED) ? PESTICIDE PROGRAMS ? TOLERANCES...

2010-07-01

437

The crystal structure and moisture sensitivity of (+)-4-(1-(2,3 dimethylphenyl) ethyl) 1H-imidazole hydrochloride  

Microsoft Academic Search

The preliminar crystal structure determination of dexmedetomidine hydrochloride was carried out. The diffraction data was collected on Rigaku AFC5S diffractometer with graphite monogromated Mo(K sub alpha) radiation at 23 C. The molecular structure and packing in the unit cell was solved by using direct methods. The structure was refined by using the full matrix least squares refinement to an R

E. Laine; R. Rajala; R. Sillanpaa; J. Pirttimaki

1991-01-01

438

Simultaneous determination of diclofenac potassium and drotaverine hydrochloride in human plasma using reversed-phase high-performance liquid chromatography.  

PubMed

A simple high-performance liquid chromatographic method with ultraviolet detection is proposed for the estimation of diclofenac potassium and drotaverine hydrochloride in human plasma. Liquid-liquid extraction was carried out with a mixture of dichloromethane-isopropyl alcohol (80:20, v/v). Chromatographic separation of the analytes and internal standard was achieved on an analytical 250 × 4.6 mm i.d. reversed-phase Thermo BDS Hypersil C8 (5 µm particle size) column using a mobile phase of acetonitrile-0.02M ammonium acetate buffer (53:47, v/v) at pH 3.5. The run time was less than 15 min. Column eluate was monitored at 230 nm. The linearity over the concentration ranges of 25-1500 ng/mL and 32-960 ng/mL was obtained for diclofenac potassium and drotaverine hydrochloride, respectively. The limit of quantification was 25 and 32 ng/mL for diclofenac potassium and drotaverine hydrochloride, respectively. Recoveries of diclofenac potassium and drotaverine hydrochloride from plasma were 97.45% and 98.27%, respectively. PMID:22573800

Dahivelkar, Prasad P; Bhoir, Suvarna I; Bari, Sanjay B; Surana, Sanjay J; Bhagwat, Ashok M

2012-09-01

439

Recovery of cognitive dysfunction in a case of delayed encephalopathy of carbon monoxide poisoning after treatment with donepezil hydrochloride.  

PubMed

Delayed encephalopathy following carbon monoxide poisoning is a serious complication. Here, we report a patient with delayed encephalopathy who suffered from cognitive disorders and urinary incontinence after a temporal normal period of 15 days after acute intoxication, and his cognitive function recovered gradually following donepezil hydrochloride treatment. Now, he can undertake slight farming work. PMID:19770553

Wang, Pin; Zeng, Tao; Chi, Zhao-fu

2009-01-01

440

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

441

Imidazole derivatives. XXVII. Synthesis and radioprotective activity of substituted phenacylthioimidazoline and 3-phenyl-5,6-dihydroimidazo[2,1-B]thiazole hydrochlorides  

SciTech Connect

Previously, we described the synthesis of phenacylthioimidazolines and investigated the biological properties of the corresponding hydrochlorides. It was found that some hydorchlorides exhibited quite significant sympathicolytic and mutagenic activity. Due to the low solubility of substituted phenacylthioimidazoline hydrobromides in water and the fact that they can cyclize into imidazothiazoles it was difficult to convert the hydrobromides to the corresponding hydrochlorides. For this reason the phenacylthioimidazoline hydrochlorides were synthesized in the present work by reacting the phenacyl chlorides with 2-thio-2-imidazoline. 8 refs., 2 figs., 2 tabs.

Iradyan, M.A.; Aroyan, R.A.; Engoyan, A.P. [and others

1995-05-01

442

A validated stability-indicating HPLC method for the simultaneous determination of pheniramine maleate and naphazoline hydrochloride in pharmaceutical formulations  

PubMed Central

Background A simple, rapid, and accurate stability-indicating reverse phase liquid chromatographic method was developed and validated for the simultaneous determination of pheniramine maleate and naphazoline hydrochloride in bulk drugs and pharmaceutical formulations. Results Optimum chromatographic separations among pheniramine maleate, naphazoline hydrochloride and stress-induced degradation products have been achieved within 10 minutes by using an Agilent zorbax eclipse XDB C18 column (150 mm?×?4.6 mm, 5 ?m) as the stationary phase with a mobile phase consisted of 10 mM phosphate buffer pH 2.8 containing 0.5% triethlamine and methanol (68:32, v/v) at a flow rate of 1 mL min-1. Detection was performed at 280 nm using a diode array detector. Theoretical plates for pheniramine maleate and naphazoline hydrochloride were calculated to be 6762 and 6475, respectively. The method was validated in accordance with ICH guidelines with respect to linearity, accuracy, precision, robustness, specificity, limit of detection and quantitation. Regression analysis showed good correlations (R2?>?0.999) for pheniramine maleate in the concentration range of 150–1200 ?g mL-1 and naphazoline hydrochloride in 12.5-100 ?g mL-1. The method results in excellent separation of both the analytes and degradation products. The peak purity factor is ?980 for both analytes after all types of stress, indicating complete separation of both analyte peaks from the stress induced degradation products. Conclusions Overall, the proposed stability-indicating method was suitable for routine quality control and drug analysis of pheniramine maleate and naphazoline hydrochloride in pharmaceutical formulations. PMID:24485011

2014-01-01

443

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 (cow’s 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.; Schröder, Cornelis H.; Willems, Johannes L.; Monnens, Leo A.H.

2013-01-01

444

3D-QSAR and 3D-QSSR studies of thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as CDK4 inhibitors by CoMFA analysis  

PubMed Central

Aim: To investigate the structural basis underlying potency and selectivity of a series of novel analogues of thieno[2,3-d]pyrimidin-4-yl hydrazones as cyclin-dependent kinase 4 (CDK4) inhibitors and to use this information for drug design strategies. Methods: Three-dimensional quantitative structure-activity relationship (3D-QSAR) and three-dimensional quantitative structure-selectivity relationship (3D-QSSR) models using comparative molecular field analysis (CoMFA) were conducted on a training set of 48 compounds. Partial least squares (PLS) analysis was employed. External validation was performed with a test set of 9 compounds. Results: The obtained 3D-QSAR model (q2=0.724, r2=0.965, r2pred=0.945) and 3D-QSSR model (q2=0.742, r2=0.923, r2pred=0.863) were robust and predictive. Contour maps with good compatibility to active binding sites provided insight into the potentially important structural features required to enhance activity and selectivity. The contour maps indicated that bulky groups at R1 position could potentially enhance CDK4 inhibitory activity, whereas bulky groups at R3 position have the opposite effect. Appropriate incorporation of bulky electropositive groups at R4 position is favorable and could improve both potency and selectivity to CDK4. Conclusion: These two models provide useful information to guide drug design strategies aimed at obtaining potent and selective CDK4 inhibitors. PMID:24122012

Cai, Bao-qin; Jin, Hai-xiao; Yan, Xiao-jun; Zhu, Peng; Hu, Gui-xiang

2014-01-01

445

Stimulating Retinal Blood Vessel Protection with Hypoxia-Inducible Factor Stabilization: Identification of Novel Small-Molecule Hydrazones to Inhibit Hypoxia-Inducible Factor Prolyl Hydroxylase (An American Ophthalmological Society Thesis)  

PubMed Central

Purpose To discover novel small molecules that inhibit hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD), a key enzyme that regulates the posttranslational stability and hence activity of HIF. Methods: NIH3T3 cell line stably transfected with firefly luciferase under a HIF-1-inducible promoter was used to screen a Chembridge library of 34,000 small molecules of molecular weight 250 to 550 Da. Positive hits were considered at 4.5-fold higher luminescence than control. Selected compounds were validated in vitro. The most effective dose was then used to treat mice expressing firefly luciferase fused to the oxygen-dependent degradation domain (lucODD) in order to determine the location of the receptor for systemic treatment with small-molecule HIF PHD inhibitors. Results: Twenty-three novel small molecules were discovered, the majority of which were hydrazones and hydrazines. Of the 23 compounds, each had different selectivity for expression of erythropoietin or vascular endothelial growth factor, two angiogenic, HIF-regulated gene products. In addition, each showed different selectivity for hepatocytes or kidney, or both or neither, when injected intraperitoneally in an in vivo reporter gene assay. Conclusion: The discovery of multiple small molecules that inhibit HIF PHD identifies new reagents to develop strategies to prevent the degradation of HIF by its selective PHD. These molecules are novel hypoxia mimetics that may provide new strategies to protect retinovasculature from hyperoxia. PMID:24385673

Sears, Jonathan E.; Hoppe, George

2013-01-01

446

Neutral dioxovanadium(V) complexes of biomimetic hydrazones ONO donor ligands of bioinorganic and medicinal relevance: Synthesis via air oxidation of bis(acetylaceto-nato)oxovanadium(IV), characterization, biological activity and 3D molecular modeling  

NASA Astrophysics Data System (ADS)

The interaction of bis(acetylacetonato)oxovanadium(IV), [VO(acac) 2] with biomimetic hydrazone ONO donor ligands HL in 1:1 mole ratio [where, HL = N-(4'-benzoylidene-3'-methyl-1'-phenyl-2'-pyrazolin-5'-one)-isonicotinic acid hydrazide (bmphp-inH, I), N-(4'-butyrylidene-3'-methyl-1'-phenyl-2'-pyrazolin-5'-one)-isonicotinic acid hydrazide (bumphp-inH, II), N-(4'-acetylidene-3'-methyl-1'-phenyl-2'-pyrazolin-5'-one)-isonicotinic acid hydrazide (amphp-inH, III), N-(3'-methyl-1'-phenyl-4'-propionylidene-2'-pyrazolin-5'-one)-isonicotinic acid hydrazide (mphpp-inH, IV) and N-(4'- iso-butyrylidene-3'-methyl-1'-phenyl-2'-pyrazolin-5'-one)-isonicotinic acid hydrazide ( iso-bumphp-inH, V)] in a mixed solvent (ethanol-methanol, 1:10) via aerial oxidation for 2-3 days yield dioxovanadium(V) complexes of composition [VO 2(L)(H 2O)] · H 2O. The compounds so obtained were characterized on the basis of elemental analyses, thermogravimetry, vanadium determination, IR, Electronic, 51V NMR, 1H NMR and mass spectral studies. The 3D molecular modeling and analysis for bond lengths and bond angles have also been carried out for one of the representative compounds, [VO 2(ampph-in)(H 2O)] ( 3).

Maurya, R. C.; Rajput, S.

2007-05-01

447

Structures of hydrazones, (E)-2-(1,3-benzothiazolyl)-NHsbnd Ndbnd CHsbnd Ar, [Ar = 4-(pyridin-2-yl)phenyl, pyrrol-2-yl, thien-2-yl and furan-2-yl]: Difference in conformations and intermolecular hydrogen bonding  

NASA Astrophysics Data System (ADS)

Structures of hydrazones, (E)-2-(1,3-benzothiazolyl)-NHsbnd Ndbnd CHsbnd Ar(Ar = pyridine-2-yl (1), pyrrol-2-yl (2), thien-2-yl (3) and furan-2-yl (4), prepared from 2-hydrazinyl-1,3-benzothiazole and ArCHO, followed by recrystallisation from alcohol solutions, are reported. No significant intramolecular hydrogen bonds are present in any of the four molecules. Different conformations were found between 2 and 3, on one hand and for 4, on the other. Thus for 4, the oxygen atom of the furanyl ring is on the same side of the molecule as is the sulfur atom of the benzothiazole unit, while in contrast, each of the heteroatoms of the thienyl and pyrrole rings lies on opposite sides to the benzothiazole sulphur atom. In addition to the conformational variations, differences are noted in the connections between molecules. Despite the presence in each case of N(hydrazono)sbnd H---N(benzothiazolo) intermolecular hydrogen bonds, molecules of 4 are linked into spiral chains, while molecules of 2 and 3 (and indeed all compounds having Ar = substituted phenyl) form symmetric dimers. Further intermolecular interactions, albeit weaker ones, are found in 2 [Csbnd H··N and Nsbnd H··?], 3 [Csbnd H··?] and 4 [?··?], while dimers of 1 remain essentially free. Calculations carried out using the DFT(B3LYP)/6-311++G(d,p) method indicated that the conformations determined by crystallography for 2-4 were the more stable.

Lindgren, Eric B.; Yoneda, Julliane D.; Leal, Katia Z.; Nogueira, Antônio F.; Vasconcelos, Thatyana R. A.; Wardell, James L.; Wardell, Solange M. S. V.

2013-03-01

448

Evaluation of anti-GERD activity of gastro retentive drug delivery system of itopride hydrochloride.  

PubMed

The present work describes the formulation and evaluation of the gastroretentive system of Itopride hydrochloride. In this research, we have formulated floating hydrogel-based microspheres employing calcium carbonate (CaCO(3)) as a gas forming agent dispersed in alginate matrix. In vitro characterizations such as drug content, particle size, and drug release were carried out. GI motility was determined by administration of charcoal meal to rats. Results demonstrated that prepared microspheres were spherical in shape with smooth surface, good loading efficiency, and excellent buoyancy. The gastro retentive dosage form of itiopride demonstrated significant antacid, anti-ulcer, and anti-GERD activity after 12 hours in comparison with the conventional dosage form. PMID:20515421

Satapathy, Trilochan; Panda, Prasana K; Goyal, Amit K; Rath, Goutam

2010-08-01

449

Simultaneous determination of a binary mixture of pantoprazole sodium and itopride hydrochloride by four spectrophotometric methods  

NASA Astrophysics Data System (ADS)

Four simple, sensitive, accurate and precise spectrophotometric methods were developed for the simultaneous determination of a binary mixture containing Pantoprazole Sodium Sesquihydrate (PAN) and Itopride Hydrochloride (ITH). Method (A) is the derivative ratio method (1DD), method (B) is the mean centering of ratio spectra method (MCR), method (C) is the ratio difference method (RD) and method (D) is the isoabsorptive point coupled with third derivative method (3D). Linear correlation was obtained in range 8-44 ?g/mL for PAN by the four proposed methods, 8-40 ?g/mL for ITH by methods A, B and C and 10-40 ?g/mL for ITH by method D. The suggested methods were validated according to ICH guidelines. The obtained results were statistically compared with those obtained by the official and a reported method for PAN and ITH, respectively, showing no significant difference with respect to accuracy and precision.

Ramadan, Nesrin K.; El-Ragehy, Nariman A.; Ragab, Mona T.; El-Zeany, Badr A.

2015-02-01

450

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

451

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