Degradation kinetics and mechanisms of moricizine hydrochloride in acidic medium.

abstract：:A conventional atomistic approach of estimating molecular hydrophobicity (log P) was improved by taking into account the proximity effect of substituent groups as well as the importance of solute-solvent interaction in the partition phenomena. The new method reassigns atomic parameters when the molecule is fully expos...

journal_title：Journal of pharmaceutical sciences

authors： Masuda T,Jikihara T,Nakamura K,Kimura A,Takagi T,Fujiwara H

更新日期：1997-01-01 00:00:00

abstract：:Ketoconazole (KTZ) has 2 chiral centers with the therapeutically active form being a racemic mixture of 2 cis-enantiomers, namely, (2R,4S)-(+)-KTZ and (2S,4R)-(-)-KTZ. The aims of the present study were to examine the effects of (+)-KTZ, (-)-KTZ, and (±)-KTZ on aryl hydrocarbon receptor activation and subsequently CYP...

journal_title：Journal of pharmaceutical sciences

authors： Anwar-Mohamed A,El-Sherbeni AA,Hamdy DA,Korashy HM,Brocks DR,El-Kadi AO

更新日期：2016-03-01 00:00:00

abstract：:Stability of the 1,3,5-triazine derivative (1), a corticotropin-releasing factor inhibitor, was studied in acidic solutions and in solid formulations. Degradant structures were elucidated using liquid chromatography/mass spectrometry (LC/MS) and nuclear magnetic resonance (NMR). Compound 1 was found to undergo hydroly...

journal_title：Journal of pharmaceutical sciences

authors： Badawy S,Hussain M,Zhao F,Ye Q,Huang Y,Palaniswamy V

更新日期：2009-08-01 00:00:00

abstract：:Using two UV-spectrophotometric methods, the hydrolysis of tinidazole was studied at pH 1.00-8.45 at 80 degrees C. The reaction followed apparent first-order kinetics throughout the studied range. No kinetic salt effect was detected, indicating that at least one of the reacting partners forming the transition state ha...

journal_title：Journal of pharmaceutical sciences

authors： Salo JP,Yli-Kauhaluoma J,Salomies H

更新日期：2003-04-01 00:00:00

abstract：:A multichannel continuous-flow apparatus for dissolution rate measurements is described. Typical data are presented to demonstrate its utility for studies with bulk drug powders as well as with tablets and capsules without any change of setup. Procedures are given for the preparation of powder samples for dissolution ...

journal_title：Journal of pharmaceutical sciences

authors： Cakiryildiz C,Mehta PJ,Rahmen W,Schoenleber D

更新日期：1975-10-01 00:00:00

abstract：:The effects of permeant charge (z) on iontophoretic-enhanced transport were investigated with synthetic Nucleopore membranes and with human epidermal membranes using a four-electrode potentiostat with side-by-side diffusion cells. The modified Nernst-Planck model (Nernst-Planck theory with an additional transport term...

journal_title：Journal of pharmaceutical sciences

authors： Li SK,Ghanem AH,Peck KD,Higuchi WI

更新日期：1997-06-01 00:00:00

abstract：:The present study pursued to profile the intestinal solubility of nine HIV protease inhibitors (PIs) in fasted- and fed-state human intestinal fluids (FaHIF, FeHIF) aspirated from four volunteers. In addition, the ability of fasted- and fed-state simulated intestinal fluids (FaSSIF, FeSSIF) to predict the intestinal s...

journal_title：Journal of pharmaceutical sciences

authors： Wuyts B,Brouwers J,Mols R,Tack J,Annaert P,Augustijns P

更新日期：2013-10-01 00:00:00

abstract：:The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are 7-chloro-5-(1,2-epoxy...

journal_title：Journal of pharmaceutical sciences

authors： Boccardi G,Deleuze C,Gachon M,Palmisano G,Vergnaud JP

更新日期：1992-02-01 00:00:00

abstract：:A simple and sensitive assay for quantitating 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one (1; BMY 26517) in human plasma was developed using high-performance liquid chromatography with fluorescence detection. The method involves precipitation of protein and reversed-phase chromatography. The method i...

journal_title：Journal of pharmaceutical sciences

authors： Cheng H,Pittman KA,Dandekar KA

更新日期：1987-12-01 00:00:00

abstract：:Human papillomavirus (HPV) virus-like-particles (VLPs) produced by recombinant expression systems are promising vaccine candidates for prevention of cervical cancers as well as genital warts. At high protein concentrations, HPV VLPs, comprised of the viral capsid protein L1 and expressed and purified from yeast, are p...

journal_title：Journal of pharmaceutical sciences

authors： Shi L,Sanyal G,Ni A,Luo Z,Doshna S,Wang B,Graham TL,Wang N,Volkin DB

更新日期：2005-07-01 00:00:00

abstract：:The synthesis of some substituted 7-hydroxy-5H-1,3,4-oxadiazolo [3,2-a]pyrimidin-5-ones, a class of bicyclics with unexplored pharmacotoxicological properties, is described. Reacting the 2-phenyl derivative with bis(2,4,5-trichlorophenyl)benzylmalonate afforded a linear pyrano-oxadiazolopyrimidinedione. The assigned s...

journal_title：Journal of pharmaceutical sciences

authors： Soliman FS,Shafik RM,Darwish M

更新日期：1982-02-01 00:00:00

abstract：:Eprosartan mesylate (SKF 108566-J; EM) is an antihypertensive agent approved for marketing in the USA. EM dihydrate was prepared by three methods, one of which included suspending the anhydrous drug in an aqueous solution of 1.0 M methanesulfonic acid to form a slurry, followed by filtration. The dehydration kinetics ...

journal_title：Journal of pharmaceutical sciences

authors： Sheng J,Venkatesh GM,Duddu SP,Grant DJ

更新日期：1999-10-01 00:00:00

abstract：:The growing interest of pharmaceutical companies toward the crystal morphology prediction of active pharmaceutical ingredients is a consequence of the dramatic effect of the crystal habit on the tableting behavior of drugs. In order to help the optimization of the industrial process, molecular mechanics calculations t...

journal_title：Journal of pharmaceutical sciences

authors： Li Destri G,Marrazzo A,Rescifina A,Punzo F

更新日期：2013-01-01 00:00:00

abstract：:It is demonstrated that the fluid-phase thermodynamics theory conductor-like screening model for real solvents (COSMO-RS) as implemented in the COSMOtherm software can be used for accurate and efficient screening of coformers for active pharmaceutical ingredient (API) cocrystallization. The excess enthalpy, H(ex) , be...

journal_title：Journal of pharmaceutical sciences

authors： Abramov YA,Loschen C,Klamt A

更新日期：2012-10-01 00:00:00

abstract：:The pharmacokinetics of tamsulosin (TAM) was investigated using male Sprague-Dawley rats in which plasma alpha(1)-acid glycoprotein (alpha(1)-AGP) levels were elevated by the subcutaneous injection of 0.2 mL/kg of turpentine oil. alpha(1)-AGP levels increased about eight times after turpentine oil treatment, causing a...

journal_title：Journal of pharmaceutical sciences

authors： Matsushima H,Watanabe T,Higuchi S

更新日期：2000-04-01 00:00:00

abstract：:A general spectroscopic method is described that might be applied to validating amino acid sequences in peptides and protein fragments with a view to it becoming a routine procedure with which to characterize biotechnology drug products. The tripeptides are the L-enantiomers of GGA, GGH, GGI, GGL, GGF, GHG, LGG, and Y...

journal_title：Journal of pharmaceutical sciences

authors： Purdie N,Province DW,Johnson EA

更新日期：1999-07-01 00:00:00

abstract：:A simple, sensitive GLC assay was developed for fusaric acid, the active metabolite of bupicomide, to follow the disposition of this investigational antihypertensive agent in patients undergoing therapy. Fusaric acid is efficiently extracted from biological samples, derivatized by on-column methylation, and chromatogr...

journal_title：Journal of pharmaceutical sciences

authors： Fung KK,Koda RT,Maronde RF,Cohen JL

更新日期：1976-04-01 00:00:00

abstract：:Though there is an advantage in using the higher solubility amorphous state in cases where low solubility limits absorption, physical instability poses a significant barrier limiting its use in solid oral dosage forms. Unlike chemical instability, where useful accelerated stability testing protocols are common, no met...

journal_title：Journal of pharmaceutical sciences

authors： Bhugra C,Pikal MJ

更新日期：2008-04-01 00:00:00

abstract：:The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of metabolite and parent drug area under the time-concentration curve ratio (AUCm/AUCp) and their PK profiles in humans using in vitro data when active transport process...

journal_title：Journal of pharmaceutical sciences

authors： Nguyen HQ,Lin J,Kimoto E,Callegari E,Tse S,Obach RS

更新日期：2017-09-01 00:00:00

abstract：:The stereochemistries of geometric isomers of 4-(2-bromo-1,2-diphenylvinyl)phenol, 4-(2-bromo-1,2-diphenylvinyl)anisole, and 2-[p-(2-bromo-1,2-diphenylvinyl)phenoxy]triethylamine were determined by conversion of the phenolic analog to the ethers and subsequent comparison of physical properties with those of 2-[p-(2-ch...

journal_title：Journal of pharmaceutical sciences

authors： Richardson A Jr,Benson HD,Hite G

更新日期：1976-10-01 00:00:00

abstract：:A carboxymethyl derivative of scleroglucan (Scl-CM) with derivatization degree 300 ± 10 was synthesized and characterized by Fourier transform infrared spectroscopy, potentiometer titration, mucus adhesion studies, and rheological measurements. Rheological measurements showed the ability of the polymer to undergo sol-...

journal_title：Journal of pharmaceutical sciences

authors： Corrente F,Paolicelli P,Matricardi P,Tita B,Vitali F,Casadei MA

更新日期：2012-01-01 00:00:00

abstract：:Emerging 3D printing technologies offer an exciting opportunity to create customized 3D objects additively from a digital design file. 3D printing may be further leveraged for personalized medicine, clinical trial, and controlled release applications. A wide variety of 3D printing methods exists, and many studies focu...

journal_title：Journal of pharmaceutical sciences

authors： Chang SY,Li SW,Kowsari K,Shetty A,Sorrells L,Sen K,Nagapudi K,Chaudhuri B,Ma AWK

更新日期：2020-10-01 00:00:00

abstract：:The mechanism of drug loading in cross-linked polymers was studied by X-ray photoelectron spectroscopy (XPS). This gave the atomic composition of the surface layers of the loaded polymeric particles so that the exact location of the drug molecules could be identified. Three different lots of popcorn crospovidone and a...

journal_title：Journal of pharmaceutical sciences

authors： Carli F,Garbassi F

更新日期：1985-09-01 00:00:00

abstract：:New dihydropyridine in equilibrium pyridinium salt-type redox carrier systems were developed in which the drug is linked via the ring nitrogen atom of nicotinamide. The rate of oxidation of the dihydropyridine forms, and thus the overall and brain-specific distribution of the corresponding 3-carbamoyl-1-carbamoylalkyl...

journal_title：Journal of pharmaceutical sciences

authors： Bodor N,AbdelAlim AM

更新日期：1985-03-01 00:00:00

abstract：:The kinetics and pathways for degradation of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770; 1), a newly developed muscle-relaxing agent, and its analogues were studied in aqueous solution at 50 degrees C, ionic strength 0.5 M, and pH 8.0-12.0. Compound 1 and its four analogues followed ...

journal_title：Journal of pharmaceutical sciences

authors： Nagata O,Terasaki T,Yada E,Sato H,Tamai I,Tsuji A

更新日期：1989-01-01 00:00:00

abstract：:The nanosizing of poorly soluble drugs as a formulation strategy can eventually enhance their dissolution rate and bioavailability. Standard comminution techniques such as high-pressure homogenization (HPH) or wet bead milling have limitations in reaching the desired mean particle size. Combinative methods have been d...

journal_title：Journal of pharmaceutical sciences

authors： Salazar J,Müller RH,Möschwitzer JP

更新日期：2013-05-01 00:00:00

abstract：:We have shown that adsorbability of local anesthetics onto activated carbon, expressed by the partition coefficients at infinite dilution, correlated well with the pharmacological activity. However, there is no parameter that can singly express the tendency to be adsorbed. Adsorbability is a loosely defined term and i...

journal_title：Journal of pharmaceutical sciences

authors： Abe I,Kamaya H,Ueda I

更新日期：1990-04-01 00:00:00

abstract：:The objective of this article was to monitor phase transformation in thiamine hydrochloride, from a nonstoichiometric hydrate (NSH) to a hemihydrate (HH), in stored tablets, prepared both by direct compression and wet granulation, and to relate the storage-induced phase transformation with changes in tablet microstruc...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Suryanarayanan R,Govindarajan R

更新日期：2012-04-01 00:00:00

abstract：:Postabsorptive factors which can affect systemic drug exposure are assumed to be dependent on the active pharmaceutical ingredient (API), and thus independent of formulation. In contrast, preabsorptive factors, for example, hypochlorhydria, might affect systemic exposure in both an API and a formulation-dependent way....

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2017-02-01 00:00:00

abstract：:Knowledge of slip or cleavage planes can facilitate the fundamental understanding of mechanical properties of organic crystals important to pharmaceutical operations, such as tableting and milling. Slip/cleavage planes were frequently assigned based on attachment energy calculation. These crystallographic planes can a...

journal_title：Journal of pharmaceutical sciences

authors： Sun CC,Kiang YH

更新日期：2008-08-01 00:00:00