Evaluation of 2-azabicyclo[2.2..2]octane analogs of 4-anilidopiperidine analgesics.

abstract：:The combined clearance of endogenous 6β-hydroxycortisol and 6β-hydroxycortisone is suggested biomarker for in vivo cytochrome P450 3A (CYP3A) activity. We aimed to determine whether the combined clearance of these two markers together with information of biopharmaceutics classification system (BCS) of drugs could be u...

journal_title：Journal of pharmaceutical sciences

authors： Luo X,Zheng L,Cai N,Liu Q,Yang S,He X,Cheng Z

更新日期：2015-10-01 00:00:00

abstract：:Antibody therapeutics with poor solubility in the subcutaneous matrix may carry unintended risks when administered to patients. The objective of this work was to estimate the risk of antibodies that precipitate in vitro at neutral pH by determining the impact of poor solubility on distribution of the drug from the inj...

journal_title：Journal of pharmaceutical sciences

authors： Kinderman F,Yerby B,Jawa V,Joubert MK,Joh NH,Malella J,Herskovitz J,Xie J,Ferbas J,McBride HJ

更新日期：2019-06-01 00:00:00

abstract：:Microparticles are of considerable interest for drug delivery, vaccination and diagnostic imaging. In order to obtain microparticles with long circulation times, or to provide the prerequisite for tissue specific targeting through decoration with suitable ligands, their surfaces need to be modified such that they beco...

journal_title：Journal of pharmaceutical sciences

authors： Wattendorf U,Merkle HP

更新日期：2008-11-01 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhi...

journal_title：Journal of pharmaceutical sciences

authors： Verbeeck RK,Kanfer I,Löbenberg R,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Polli JE,Parr A,Shah VP,Mehta M,Dressman JB

更新日期：2017-08-01 00:00:00

abstract：:A GLC method for determining theophylline, hydroxyethyltheophylline, and diphenylpyraline hydrochloride is presented. The method permits the separation and quantitative determination of the therapeutically active ingredients with a single injection in an overall time of approximately 2.5 hr. ...

journal_title：Journal of pharmaceutical sciences

authors： de Fabrizio F

更新日期：1979-04-01 00:00:00

abstract：:The aim of this study was to determine the sensitivity of transgenic immune tolerant mice for the type and level of aggregation of recombinant human interferon alpha2b (rhIFNalpha2b). RhIFNalpha2b was aggregated by metal-catalyzed oxidation or by incubation at elevated temperature and various pHs. Native rhIFNalpha2b ...

journal_title：Journal of pharmaceutical sciences

authors： Hermeling S,Schellekens H,Maas C,Gebbink MF,Crommelin DJ,Jiskoot W

更新日期：2006-05-01 00:00:00

abstract：:The area under the plasma concentration-time curve (AUC) was measured after an intravenous injection of sodium salicylate and after intragastric administration of aspirin, using either an intermittent sampling and the trapezoid rule (AUC-trapezoid) or the recently introduced constant blood withdrawal method (AUC-integ...

journal_title：Journal of pharmaceutical sciences

authors： Kowarski CR,Kowarski AA

更新日期：1978-06-01 00:00:00

abstract：:Cellulose derivatives are commonly used as gelling agents in topical and ophthalmic drug formulations. During the course of manufacturing, cellulose derivatives are believed to generate free radicals. These free radicals may degrade the gelling agent, leading to lower viscosity. Free radicals also may react with the a...

journal_title：Journal of pharmaceutical sciences

authors： Basumallick L,Ji JA,Naber N,Wang YJ

更新日期：2009-07-01 00:00:00

abstract：:An on-line, high-performance frontal analysis (HPFA)-high-performance liquid chromatographic system was developed for the enantioselective determination of a low level of unbound ketoprofen (KP) that is in equilibrium with KP that is bound to protein. The system consists of three subsystems (HPFA system, preconcentrat...

journal_title：Journal of pharmaceutical sciences

authors： Shibukawa A,Terakita A,He JY,Nakagawa T

更新日期：1992-07-01 00:00:00

abstract：:Water evaporation rates were measured from thin samples of a model layered structure of stratum corneum lipids with 32% water. A model with only free fatty acids present gave the lowest evaporation rates, while a model with only oleic acid gave values approximately 50% higher. Using the total lipid spectrum of stratum...

journal_title：Journal of pharmaceutical sciences

authors： Friberg SE,Kayali I

更新日期：1989-08-01 00:00:00

abstract：:Some coated aspirin tablet formulations were evaluated by relating their properties to disintegrating force development patterns. The treatment of disintegrating force-time curves was effected using the Weibull distribution as proposed for dissolution. Such parameters as the maximum disintegrating force developed, the...

journal_title：Journal of pharmaceutical sciences

authors： Colombo P,Conte U,Caramella C,Geddo M,La Manna A

更新日期：1984-05-01 00:00:00

abstract：:Correlations between the bioavailability parameters for erythromycin stearate tablets from five manufacturers and in vitro tests of these tablets were examined using forward (stepwise), multiple linear regression analysis. Bioavailability parameters were determined in clinical studies employing a balanced, incomplete ...

journal_title：Journal of pharmaceutical sciences

authors： Stavchansky S,Doluisio JT,Martin A,Martin C,Cabana B,Dighe S,Loper A

更新日期：1980-11-01 00:00:00

abstract：:Surface adsorption of two monoclonal antibodies (mAb1 and mAb2), with widely different hydrophobicity and self-association behavior in solution, was examined by quartz crystal microbalance with dissipation monitoring to understand how adsorption and protein self-interactions near the surface are impacted by their intr...

journal_title：Journal of pharmaceutical sciences

authors： Oom A,Poggi M,Wikström J,Sukumar M

更新日期：2012-02-01 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

abstract：:The oral absorption of drugs has been represented by various concepts such as the absorption potential, the maximum absorbable dose, the biopharmaceutics classification system, and in vitro-in vivo correlation. The aim of this article is to provide an overview of the theoretical relationships between these concepts. I...

journal_title：Journal of pharmaceutical sciences

authors： Sugano K,Terada K

更新日期：2015-09-01 00:00:00

abstract：:N-Acetyl-DL-penicillamine (IIIb), a structural analog of N-acetyl-L-cysteine (IIIa), did not protect mice from lethal doses of acetaminophen (I), whereas IIIa offered protection. This lack of efficacy of IIIb probably is due to the decreased nucleophilicity of its sulfhydryl group compared to that of IIIa, the probabl...

journal_title：Journal of pharmaceutical sciences

authors： Zera RT,Nagasawa HT

更新日期：1980-09-01 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：:The present studies were undertaken to describe the dynamic nature of the degradation and absorption of insulin in the subcutaneous injection site and to develop agents which would stabilize this dosage form. [125I]Insulin with 0.2-U/kg of unlabeled insulin in 10 microliters of aqueous solution was injected subcutaneo...

journal_title：Journal of pharmaceutical sciences

authors： Hori R,Komada F,Okumura K

更新日期：1983-04-01 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：:The usefulness of poly(N-isopropyl acrylamide), PNIPA, for preparing sustained release matrix or photopolymerization-coated cellulosic pellets was evaluated. Theophylline pellets and granules were prepared using powdered cellulose (PC), poly(vinylpyrrolidone) (PVP), and PNIPA of Mw approximately 330 kDa, Mn approximat...

journal_title：Journal of pharmaceutical sciences

authors： Mayo-Pedrosa M,Alvarez-Lorenzo C,Lacík I,Martinez-Pacheco R,Concheiro A

更新日期：2007-01-01 00:00:00

abstract：:Chitosan salts are being investigated as materials for bacterially triggered colonic drug delivery, via the oral route, based on the assumption that they will be degraded by the enzymes produced by the human colonic bacteria. The actual susceptibility of chitosan to these enzymes is, however, unclear. The digestion of...

journal_title：Journal of pharmaceutical sciences

authors： McConnell EL,Murdan S,Basit AW

更新日期：2008-09-01 00:00:00

abstract：:Eleven quinazolinylformamidines and quinazolinediylbisformamidines were synthesized and investigated for antihypertensive activity in spontaneous hypertensive rats. Several compounds showed moderate antihypertensive activity at 100 mg/kg po. The same compounds were not hypotensive in the normotensive dog. ...

journal_title：Journal of pharmaceutical sciences

authors： Warren JD,Lang SA Jr,Chan PS,Marsico JW

更新日期：1978-10-01 00:00:00

abstract：:A Bayesian approach was developed to determine an amikacin dosage regimen to achieve the desired plasma concentrations for each patient. Statistical characteristics of pharmacokinetic parameters were first evaluated in a group of patients (reference population), which when combined with three individual plasma concent...

journal_title：Journal of pharmaceutical sciences

authors： Garraffo R,Iliadis A,Cano JP,Dellamonica P,Lapalus P

更新日期：1989-09-01 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：:Both nonequilibrium and equilibrium models were proposed to explain the optimal biological response to a set of congeners with respect to the oil-water partition coefficient (P). A detailed analysis of the kinetic model proposed by Hansch demonstrates the bilinear form of the model, with the initial slope of the logar...

journal_title：Journal of pharmaceutical sciences

authors： Cooper ER,Berner B,Bruce RD

更新日期：1981-01-01 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：:A commercial dispersive Raman spectrometer operating at 785 nm with a CCD detector was used to acquire spectra of USP reference materials inside amber USP vials. The laser and collection beams were directed through the bottom of the vials, resulting in a 60% loss of signal. The Raman shift was calibrated with a 4-acet...

journal_title：Journal of pharmaceutical sciences

authors： McCreery RL,Horn AJ,Spencer J,Jefferson E

更新日期：1998-01-01 00:00:00

abstract：:2 closely related prostaglandins (PGs), A2 and B2, were separated by ion-exchange liquid chromatography. PGA2 and PGB2 are an isomeric pair of PGs which show little resolution on thin-layer chromatography; the pair can be resolved as gas-liquid chromatography, but use of this method requires protection of the C9-carb...

journal_title：Journal of pharmaceutical sciences

authors： Morozowich W

更新日期：1974-05-01 00:00:00

abstract：:Current drug level predictions in nonlinear pharmacokinetics are based on specific pharmacokinetic models in contrast to the model-independent (structureless), dose-linearity, and superposition principles used in linear pharmacokinetics. Such model-dependent methods may not provide reliable predictions due to their in...

journal_title：Journal of pharmaceutical sciences

authors： Veng-Pedersen P

更新日期：1984-06-01 00:00:00

abstract：:Iontophoretic transdermal delivery of sumatriptan was investigated in vitro. Among the conditions tested, 0.25 mA/cm2 and low ionic strength (NaCl 25 mM) was the best experimental condition to increase its transport across the skin. The flux increased 385-fold respective to passive diffusion, thus resulting in a trans...

journal_title：Journal of pharmaceutical sciences

authors： Femenía-Font A,Balaguer-Fernández C,Merino V,López-Castellano A

更新日期：2005-10-01 00:00:00