Identification of Endogenous Biomarkers to Predict the Propensity of Drug Candidates to Cause Hepatic or Renal Transporter-Mediated Drug-Drug Interactions.

abstract：:Repeated acetaminophen (AP) administration modulates intestinal P-glycoprotein (P-gp) expression. Whether AP can modulate P-gp activity in a short-term fashion is unknown. We investigated the acute effect of AP on rat intestinal P-gp activity in vivo and in vitro. In everted intestinal sacs, AP inhibited serosal-mucos...

journal_title：Journal of pharmaceutical sciences

authors： Novak A,Carpini GD,Ruiz ML,Luquita MG,Rubio MC,Mottino AD,Ghanem CI

更新日期：2013-10-01 00:00:00

abstract：:Citric acid anhydrate (CAA) and paracetamol (PARA), prepared as crystalline physical mixtures and as amorphous blends, were studied using (13)C solid-state cross polarization magic angle spinning (CPMAS) NMR. Amorphous blends showed significant line broadening from the conformational distribution as compared to the cr...

journal_title：Journal of pharmaceutical sciences

authors： Schantz S,Hoppu P,Juppo AM

更新日期：2009-05-01 00:00:00

abstract：:Levemopamil was solubilized by varying the concentration of hydroxypropyl-beta-cyclodextrin (HPbetaCD) and by the alteration of pH. The drug molecule has two sites for possible complexation with HPbetaCD, creating the possibility of either 1:1 or 1:2 complexation. The solubility as a function of HPbetaCD concentration...

journal_title：Journal of pharmaceutical sciences

authors： McCandless R,Yalkowsky SH

更新日期：1998-12-01 00:00:00

abstract：:New methods are being applied to distinguish silicone oil droplets from subvisible particles in therapeutic protein formulations. The need to standardize these methods and compare them to established methods is critical to increase the understanding of the risks from protein aggregation and other subvisible particulat...

journal_title：Journal of pharmaceutical sciences

authors： Vandesteeg N,Kilbert C

更新日期：2013-06-01 00:00:00

abstract：:The intense blue color formed in the official assay of menadione injection by treatment of the sample with 2,4-dinitrophenylhydrazine and ammonia is shown by data from visible light spectra and mass spectra and by comparison of the pKa value with that of the corresponding reaction product of acetone to be due to proto...

journal_title：Journal of pharmaceutical sciences

authors： Burns LB,Stedman RJ,Tuckerman MM

更新日期：1978-02-01 00:00:00

abstract：:In vitro studies on the photodecomposition of uric acid in the presence of the monosodium salt of riboflavin 5'-phosphate in buffers at various pH values, in methanol, and in human plasma are reported. The decomposition rate increased with increasing pH and was independent of solvent or buffer species. The mechanism a...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Combs AB,Hsu TF

更新日期：1977-11-01 00:00:00

abstract：:The purpose of this study was to investigate the feasibility of delivering sinomenine hydrochloride (SH) transdermally using composite dissolving microneedles (DM) which integrated with liquid crystals (H2). The fabricated SH-loaded composite DM was evaluated for their appearance, mechanical strength, irritation, and ...

journal_title：Journal of pharmaceutical sciences

authors： Gui Z,Wu X,Wang S,Cao Y,Wan J,Shan Q,Yang Z,Zhang J,Gui S

更新日期：2017-12-01 00:00:00

abstract：:The antifungal activity of amphotericin B (AmB) incorporated in three cholesteryl carbonate esters (CCEs), sodium cholesteryl carbonate, cholesteryl palmityl carbonate, and dicholesteryl carbonate, was examined to assess their potential for use in a dry powder aerosol. Formulations containing dissolved AmB were stable...

journal_title：Journal of pharmaceutical sciences

authors： Chuealee R,Wiedmann TS,Srichana T

更新日期：2011-05-01 00:00:00

abstract：:A modified NF method for the quantitative determination of pentaerythritol tetranitrate is reported. A solution of powder is made directly from the dosage form in glacial acetic acid and is then reacted with phenoldisulfonic acid TS. The proposed method saves approximately 75% of the time required with the NF method. ...

journal_title：Journal of pharmaceutical sciences

authors： Gupta VD

更新日期：1978-05-01 00:00:00

abstract：:New butyrate derivatives were synthesized to investigate the residence time of potent butyric acid in vivo. These derivatives were triglycerides in which one, two, or three butyric acid molecules were bound to glycerol or to mono- and dipalmitic esters of glycerol. Pharmacokinetic studies showed that a constant plasma...

journal_title：Journal of pharmaceutical sciences

authors： Planchon P,Pouillart P,Ronco G,Villa P,Pieri F

更新日期：1993-10-01 00:00:00

abstract：:Thiamine hydrochloride (Vitamin B(1), THCl) can exist as a nonstoichiometric hydrate (NSH) and as a hemihydrate (HH). NSH can contain up to approximately 1 molar equivalent of water and be dehydrated to an isomorphic desolvate (ID) with minimal change in lattice structure. Crystallographic and spectroscopic techniques...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Berendt RT,Munson EJ,Young VG Jr,Govindarajan R,Suryanarayanan R

更新日期：2010-02-01 00:00:00

abstract：:A procedure for the quantitative determination of adinazolam in plasma was developed. The drug, an N-demethylated metabolite, and an internal standard were extracted from basified plasma into ethyl acetate. After evaporation, the residue was dissolved in toluene which was washed with sodium hydroxide. The toluene was ...

journal_title：Journal of pharmaceutical sciences

authors： Peng GW

更新日期：1984-08-01 00:00:00

abstract：:The pharmacokinetics and tissue distribution of methotrexate (MTX) were investigated following intra-articular injection of either MTX solution or controlled release MTX loaded microspheres in healthy rabbit joints. MTX solution or MTX loaded microspheres (size 30-100 mum) (10 mg MTX) was injected into the right knee ...

journal_title：Journal of pharmaceutical sciences

authors： Liang LS,Wong W,Burt HM

更新日期：2005-06-01 00:00:00

abstract：:The viscosity and surface tension of systems containing small amounts of salicylic acid in aqueous solutions of cetrimide were determined. An abrupt increase in viscosity was observed, and the molar ratio of salicylic acid to certrimide at which this viscosity increase occurred was 1:2. The surface tension of these sy...

journal_title：Journal of pharmaceutical sciences

authors： Wan LS

更新日期：1977-12-01 00:00:00

abstract：:A simple solution model that has lead to successful predictive equations for the partial molar excess properties of a solute in simple binary solvent mixtures containing only nonspecific interactions is extended to include association between the solute and one of the solvent components. An expression is derived and t...

journal_title：Journal of pharmaceutical sciences

authors： Acree WE Jr,McHan DR,Rytting JH

更新日期：1983-08-01 00:00:00

abstract：:A revised classification system for oral drugs was developed using the biopharmaceutics classification system (BCS) as a starting point. The revised system is designed to have a greater focus on drug developability. Intestinal solubility, the compensatory nature of solubility and permeability in the small intestine an...

journal_title：Journal of pharmaceutical sciences

authors： Butler JM,Dressman JB

更新日期：2010-12-01 00:00:00

abstract：:Aqueous wet massing of stable anhydrous theophylline (A) with polyvinylpyrrolidone (PVP) resulted in its complete transformation to theophylline monohydrate (M). Drying at 45 degrees C, resulted in the formation of metastable anhydrous theophylline (A*) which then transformed to A. PVP, a known crystallization inhibit...

journal_title：Journal of pharmaceutical sciences

authors： Tantry JS,Tank J,Suryanarayanan R

更新日期：2007-05-01 00:00:00

abstract：:The bioavailability of three different brands and three different dosage forms of doxycycline was studied in normal subjects. Single doses, equivalent to 200 mg of doxycycline, were administered to six subjects in a crossover design as the innovator's intravenous solution given orally (Treatment A), the innovator's ca...

journal_title：Journal of pharmaceutical sciences

authors： Antal EJ,Jaffe JM,Poust RI,Colaizzi JL

更新日期：1975-12-01 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：:At low protein concentrations (c2), non-native protein aggregation rates are known to be sensitive to changes in conformational stability and "weak" or "colloidal" protein-protein interactions. Protein-protein interactions are also known to be strong functions of c2. In the present work, protein-protein interactions a...

journal_title：Journal of pharmaceutical sciences

authors： Ghosh R,Calero-Rubio C,Saluja A,Roberts CJ

更新日期：2016-03-01 00:00:00

abstract：:An electron-capture GLC method was developed for measuring pindolol in human plasma and urine. The unchanged drug was extracted with benzene from alkalinized plasma or urine using propranolol as the internal standard. Both compounds subsequently were back-extracted into 0.1 M HCl and then into benzene. After evaporati...

journal_title：Journal of pharmaceutical sciences

authors： Guerret M,Lavene D,Kiechel JR

更新日期：1980-10-01 00:00:00

abstract：:The estimation of aqueous solubilities of organic nonelectrolytes by the General Solubility Equation (GSE) as proposed by Valvani and Yalkowsky (1980) is used in this study. The data and assumptions on which the GSE are based are reevaluated, and the equation is revised. The revised GSE is validated on a set of 580 ph...

journal_title：Journal of pharmaceutical sciences

authors： Jain N,Yalkowsky SH

更新日期：2001-02-01 00:00:00

abstract：:The phase diagram for the binary system nafcillin sodium-water, was determined using differential scanning calorimetry (DSC) and polarized light microscopy. In the temperature range of -20-30 degrees, three crystalline forms and an amphiphilic liquid crystalline phase were detected. The stable crystalline form of nafc...

journal_title：Journal of pharmaceutical sciences

authors： Bogardus JB

更新日期：1982-01-01 00:00:00

abstract：:Drugs possessing the ability to bind to melanin-rich tissue, such as the eye, are linked with higher ocular exposure, and therefore have the potential to affect the efficacy and safety profiles of therapeutics. A high-throughput melanin chromatographic affinity assay has been developed and validated, which has allowed...

journal_title：Journal of pharmaceutical sciences

authors： Reilly J,Williams SL,Forster CJ,Kansara V,End P,Serrano-Wu MH

更新日期：2015-12-01 00:00:00

abstract：:The biphasic degradation of delta9-tetrahydrocannabinol (I), as monitored by flame-ionization GLC, produced delta8-tetrahydrocannabinol (II), cannabidiol (X), 9-hydroxyhexahydrocannabinol (VI), 9,10-dihydro-9-hydroxyisocannabidiol (VI), and and 6,12-dihydro-6-hydroxycannabidiol (VIII) in acidic solutions. Further iden...

journal_title：Journal of pharmaceutical sciences

authors： Garrett ER,Gouyette AJ,Roseboom H

更新日期：1978-01-01 00:00:00

abstract：:Nadolol was extracted from tablet excipients with an acidic potassium chloride solution. The drug was oxidized with periodic acid, and the resulting aldehyde was reacted with 2,4-dinitrophenylhydrazine to form the corresponding hydrazone. Excess reagent was removed with a cupric chloride solution. The hydrazone was ex...

journal_title：Journal of pharmaceutical sciences

authors： Ivashikiv E

更新日期：1978-07-01 00:00:00

abstract：:A series of mono-, di-, and trimethylated derivatives of 4-chloro- and 4-methoxybenzanilide was synthesized and evaluated for anticonvulsant activity. This series was prepared in the course of studies designed to examine the relationship between anticonvulsant effects and benzamide structure. The compounds were tested...

journal_title：Journal of pharmaceutical sciences

authors： Clark CR,McMillian CL

更新日期：1990-03-01 00:00:00

abstract：:The role of particle size and surface modification on biodistribution of nanocarriers is widely reported. We report for the first time the role of nanoparticle shape on biodistribution. Our study demonstrates that irregular shaped polymer lipid nanoparticles (LIPOMER) evade kupffer cells and localize in the spleen. We...

journal_title：Journal of pharmaceutical sciences

authors： Devarajan PV,Jindal AB,Patil RR,Mulla F,Gaikwad RV,Samad A

更新日期：2010-06-01 00:00:00

abstract：:Sustained-release formulations such as hydroxypropyl methylcellulose (HPMC)-based hydrophilic matrix tablets of poorly water-soluble drugs often result in incomplete release because of the poor solubility and dissolution rate of the drug in the hydrophilic matrix. Sulfobutylether-beta-cyclodextrins ((SBE)(7M)-beta-CDs...

journal_title：Journal of pharmaceutical sciences

authors： Rao VM,Haslam JL,Stella VJ

更新日期：2001-07-01 00:00:00

abstract：:The reaction of chlorthalidone with methanol to give the corresponding methyl ether was investigated. The kinetics are pseudo-first-order in chlorthalidone, but the observed pseudo-first-order rate constants show an unexpected dependence on the initial chlorthalidone concentration, attributable to the presence of trac...

journal_title：Journal of pharmaceutical sciences

authors： Pandit NK,Hinderliter JS

更新日期：1985-08-01 00:00:00