Indeno[1,2-c]pyrazolone acetic acids as semirigid analogues of the nonsteroidal anti-inflammatory drugs.

abstract：:We investigated the effect of cytochrome P450 (CYP) 2C9 polymorphism on the inhibition of methylhydroxylation activity of tolbutamide, a typical CYP2C9 substrate, by triazole antifungal agents, fluconazole and voriconazole. Although the Michaelis constants (Km), maximal velocities (Vmax), and Vmax/Km values for CYP2C9...

journal_title：Journal of pharmaceutical sciences

authors： Niwa T,Hata T

更新日期：2016-03-01 00:00:00

abstract：:A new method for determining a quaternary mixture of vitamins B6, B1, and B12 and uridine 5'-triphosphate (UPT) using second-derivative spectrophotometry is described. Calibration graphs were linear up to 30 micrograms/mL of vitamin B6 at 307 nm (r = 0.9999) and vitamin B1 at 282.7 nm (r = 0.9997) and up to 35 microgr...

journal_title：Journal of pharmaceutical sciences

authors： Morelli B

更新日期：1995-01-01 00:00:00

abstract：:Drug-induced phototoxic skin responses involves photoirritation, photoallergy, and photogenotoxicity. In the present study, we attempted to develop effective analytical tools to predict the photogenotoxic potential of pharmaceutical substances on the basis of their photobiological and DNA-binding properties. Photoclea...

journal_title：Journal of pharmaceutical sciences

authors： Onoue S,Seto Y,Oishi A,Yamada S

更新日期：2009-10-01 00:00:00

abstract：:High-field (300 MHz) 1H NMR spectral analyses are reported for various sodium or calcium heparin products available on the Canadian market. Dermatan sulfate (chondroitin sulfate B) was detected as a contaminant in virtually all of these products. Its content varied among the suppliers from less than 1 to 15%, and also...

journal_title：Journal of pharmaceutical sciences

authors： Neville GA,Mori F,Holme KR,Perlin AS

更新日期：1989-02-01 00:00:00

abstract：:The release through silicone rubber membranes of benzocaine suspended in carbomer hydrogels containing different concentrations of low molecular weight polysols (ethylene glycol, propylene glycol, glycerol, and sorbitol) was studied to establish general principles and procedures for control of the effects on percutane...

journal_title：Journal of pharmaceutical sciences

authors： Di Colo G,Carelli V,Giannaccini B,Serafini MF,Bottari F

更新日期：1980-04-01 00:00:00

abstract：:Alkyl 2-imidazolyl disulfide compounds are novel antitumor agents, one of which is currently being evaluated in Phase I clinical trials. These molecules contain an unsymmetrical disulfide fragment, the lipophilic and electronic contributions of which are still not defined in the literature. Lipophilicity, ionization, ...

journal_title：Journal of pharmaceutical sciences

authors： Hashash A,Kirkpatrick DL,Lazo JS,Block LH

更新日期：2002-07-01 00:00:00

abstract：:Dissolution profiles are classified in accordance with the shape of fractional dissolution rate function. This function is constant in time for the classical first-order model and, in this case, the dissolution is described by a monoexponential function. Therefore, any deviation of the fractional dissolution rate from...

journal_title：Journal of pharmaceutical sciences

authors： Lánský P,Weiss M

更新日期：2003-08-01 00:00:00

abstract：:Fifteen pyrimidine-related compounds were evaluated for their ability to inhibit enzymatic degradation of 5-fluoro-2'-deoxyuridine (FUdR). Acyclothymidine [5-methyl-1-(2'-hydroxyethoxymethyl)uracil] showed the highest inhibitory effect on the phosphorolytic degradation of FUdR in various tissue homogenates derived fro...

journal_title：Journal of pharmaceutical sciences

authors： Kawaguchi T,Saito M,Saneyoshi M

更新日期：1988-11-01 00:00:00

abstract：:Midazolam (MDZ) is a benzodiazepine commonly administered in preanesthesia of children by oral or by sublingual routes. To mask its bitter taste and enhance its aqueous solubility, we already developed a 0.2% (w/v) MDZ oral solution containing γ-cyclodextrin (γ-CD), which proves to be better accepted by children in pe...

journal_title：Journal of pharmaceutical sciences

authors： Mathiron D,Marçon F,Dubaele JM,Cailleu D,Pilard S,Djedaïni-Pilard F

更新日期：2013-07-01 00:00:00

abstract：:A theory of charge, fluid-mass, and solute (including macromolecular) transport through porous media is applied to describe transport phenomena across the external layer of mammalian skin. Linear relationships are derived between transport fluxes and applied fields. These relationships introduce six effective transder...

journal_title：Journal of pharmaceutical sciences

authors： Edwards DA,Langer R

更新日期：1994-09-01 00:00:00

abstract：:The determination of reactive fractal dimension was carried out using two forms of the Noyes-Whitney equation, -dQ/dt = K(Q/Q0)DR/3 and -dQ/dt = K'RDR-3 using the Richardson plot on the basis of previous data obtained by dissolution of an orthoboric acid powder. The correlation of the results provided by the two ways ...

journal_title：Journal of pharmaceutical sciences

authors： Tromelin A,Gnanou JC,Andrès C,Pourcelot Y,Chaillot B

更新日期：1996-09-01 00:00:00

abstract：:Ketoconazole and posaconazole are both Biopharmaceutics Classification System class 2 drugs (highly permeable, poorly soluble), are structurally similar, and are administered at the same doses. Nevertheless, the duodenal concentration profile and the magnitude of the positive food effect observed for these 2 drugs are...

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2016-09-01 00:00:00

abstract：:Crystallization of drugs in metastable, supersaturated adhesive polymeric matrices in transdermal drug delivery devices can be avoided by determination of the solubility of the drug in the adhesive polymer. A novel method is described to determine the solubility of the drug in polymeric matrices. Unlike existing metho...

journal_title：Journal of pharmaceutical sciences

authors： Jasti BR,Berner B,Zhou SL,Li X

更新日期：2004-08-01 00:00:00

abstract：:An interlaboratory comparison of two extraction methods and one thermal desorption test method for the quantification of ethylene oxide (EO) by gas chromatography in two common medical device materials, high density polyethylene (HDPE) and plasticized polyvinyl chloride (PVC), was conducted by 15 laboratories. The thr...

journal_title：Journal of pharmaceutical sciences

authors： Lao NT,Lu HT,Rego A,Kosakowski RH,Burgess DJ,Hume RD

更新日期：1995-05-01 00:00:00

abstract：:Alginate microparticles incorporating hydrocortisone hemisuccinate were produced by aerosolization and homogenization methods to investigate their potential for colonic drug delivery. Microparticle stabilization was achieved by CaCl2 crosslinking solution (0.5 M and 1 M), and drug loading was accomplished by diffusion...

journal_title：Journal of pharmaceutical sciences

authors： Samak YO,El Massik M,Coombes AGA

更新日期：2017-01-01 00:00:00

abstract：:The heat of precipitation of dl-pseudoephedrine was determined by direct calorimetry using a Tronac isoperibolic calorimeter. The precipitation of dl-pseudoephedrine was induced by mixing aqueous solutions of the two enantiomers, namely, d- and l-pseudoephedrine, directly in the calorimeter. The molar heat of precipit...

journal_title：Journal of pharmaceutical sciences

authors： Pudipeddi M,Sokoloski TD,Duddu SP,Carstensen JT

更新日期：1995-10-01 00:00:00

abstract：:The purpose of this study was to develop quantitative structure-activity/pharmacokinetic relationships (QSAR/QSPKR) for 11 selected corticosteroids in man. Multiple linear regression analysis with an automatic forward step-wise inclusion algorithm was used to construct QSAR/QSPKR models from molecular and submolecular...

journal_title：Journal of pharmaceutical sciences

authors： Mager DE,Jusko WJ

更新日期：2002-11-01 00:00:00

abstract：:The aim of this study is to evaluate the effect of peptide cyclization on the blood-brain barrier (BBB) modulatory activity and plasma stability of His-Ala-Val peptides, which are derived from the extracellular 1 domain of human E-cadherin. The activities to modulate the intercellular junctions by linear HAV4 (Ac-SHAV...

journal_title：Journal of pharmaceutical sciences

authors： Alaofi A,On N,Kiptoo P,Williams TD,Miller DW,Siahaan TJ

更新日期：2016-02-01 00:00:00

abstract：:In this study, the effects of structurally related organic impurities on the molecular dynamics of amorphous sulfamethazine were evaluated using thermal analysis. Sulfanilamide (SNA), sulfamerazine (SMR), and sulfadimethoxine were used as virtual impurities of sulfamethazine. The amorphous state was prepared in situ i...

journal_title：Journal of pharmaceutical sciences

authors： Hamada Y,Ono M,Ohara M,Yonemochi E

更新日期：2017-04-01 00:00:00

abstract：:The effects of cyclazocine, a narcotic agonist/antagonist, on the uptake, metabolism, and turnover of norepinephrine in rat brains were studied. Cyclazocine significantly depressed the accumulation of intracisternally administered [3H]norepinephrine and the formation of 3,4-[3H]dihydroxymandelic acid but did not alter...

journal_title：Journal of pharmaceutical sciences

authors： Russi GD

更新日期：1985-01-01 00:00:00

abstract：:The interaction between sulfadimethoxine and tolbutamide in sheep involving displacement from protein binding sites was investigated quantitatively. A 52% increase in the unbound plasma concentration of tolbutamide was observed in vitro at 37 degrees after the addition of sulfadimethoxine (100 microgram/ml) to sheep p...

journal_title：Journal of pharmaceutical sciences

authors： Thiessen JJ,Rowland M

更新日期：1977-08-01 00:00:00

abstract：:The equilibrium kinetics of triazolam in aqueous solution was investigated in the pH range of 1-11 at body temperature. The quantitative study indicated that it forms equilibrium mixtures consisting of ring-opened and closed forms with the composition being dependent on pH. The equilibrium constants of the two species...

journal_title：Journal of pharmaceutical sciences

authors： Konishi M,Hirai K,Mori Y

更新日期：1982-12-01 00:00:00

abstract：:Phenylpropanolamine was determined by measuring its fluorescent fluorescamine derivative. The method is rapid, sensitive, and easily automated. Statistics are presented for an effervescent cold product, and recovery data are presented for other commercially available products. ...

journal_title：Journal of pharmaceutical sciences

authors： Shankle LL

更新日期：1978-11-01 00:00:00

abstract：:The purpose of this study was to evaluate the cardiovascular effects of two potential beta-hydroxylase inhibitors, a dithiocarbamate and a thiourea derivative of d-amphetamine, 1 and 2, respectively. These compounds when given intravenously elicited a significant dose-dependent depressor effect in normotensive rats an...

journal_title：Journal of pharmaceutical sciences

authors： Venugopalan CS,Jenkins HJ

更新日期：1985-06-01 00:00:00

abstract：:Multidrug resistance (MDR) mediated by the overexpression of the drug efflux protein P-glycoprotein is one of the major obstacles to successful cancer chemotherapy. The development of safe and effective MDR-reversing agents is an important approach to addressing this problem clinically. In this study, we evaluated the...

journal_title：Journal of pharmaceutical sciences

authors： Liu R,Zhang Y,Chen Y,Qi J,Ren S,Xushi MY,Yang C,Zhu H,Xiong D

更新日期：2010-07-01 00:00:00

abstract：:The interaction of cyclosporin A (CsA) with dimethyl-alpha- and -beta-cyclodextrins (DM-alpha-CyD and DM-beta-CyD) was investigated by the solubility method, electrospray ionization mass spectrometry (ESI-MS) and 1H-nuclear magnetic resonance spectroscopy (1H NMR). The extremely low solubility (1.9 x 10(-5) M at 25 de...

journal_title：Journal of pharmaceutical sciences

authors： Miyake K,Hirayama F,Uekama K

更新日期：1999-01-01 00:00:00

abstract：:The purpose of this study was to examine the external predictability of an in vitro-in vivo correlation (IVIVC) for a metoprolol hydrophilic matrix extended-release formulation, with an acceptable internal predictability, in the presence of a range of formulation/manufacturing changes. In addition, this report evaluat...

journal_title：Journal of pharmaceutical sciences

authors： Mahayni H,Rekhi GS,Uppoor RS,Marroum P,Hussain AS,Augsburger LL,Eddington ND

更新日期：2000-10-01 00:00:00

abstract：:Adsorption isotherms for the diazepam-activated carbon system in simulated intestinal fluid (SIF), without pancreatin, and in SIF with different percentages of ethanol were determined as were the solubilities of diazepam in SIF and in SIF with different percentages of ethanol. The surface area of the activated carbon ...

journal_title：Journal of pharmaceutical sciences

authors： Wurster DE,Alkhamis KA,Matheson LE

更新日期：2003-10-01 00:00:00

abstract：:A swellable matrix tablet is described which is partially coated with cellulose acetate (CA) to obtain a film having the shape of a cup, whose permeability to water and solutes was altered by mixing increasing amounts of poly(ethylene glycol) 400 (PEG). The drug-release mechanism from such systems was assessed by carr...

journal_title：Journal of pharmaceutical sciences

authors： Catellani PL,Colombo P,Peppas NA,Santi P,Bettini R

更新日期：1998-06-01 00:00:00

abstract：:To prepare (+)-tubocurine and O,O-dimethyl-(+)-tubocurine, the commonly used dequaternization procedures with sodium theophenoxide and ethanolamine were investigated. The quaternary compounds were (+)-tubocurarine chloride and the chloride and iodide salts of O,O-dimethyl-(+)-chondocurarine. The results obtained with ...

journal_title：Journal of pharmaceutical sciences

authors： Naghaway JA,Soine TO

更新日期：1978-09-01 00:00:00