Inhibitory effect of valsartan on the intestinal absorption and renal excretion of bestatin in rats.

abstract：:The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

journal_title：Journal of pharmaceutical sciences

authors： Cabrera MA,Bermejo M,Pérez M,Ramos R

更新日期：2004-07-01 00:00:00

abstract：:Ethyl, n-dodecyl, and n-hexadecyl esters of urocanic acid (4-imidazoleacrylic acid) were prepared from 4-imidazolecarboxaldehyde in satisfactory yields via the Wittig reaction. ...

journal_title：Journal of pharmaceutical sciences

authors： Honda K,Nishijima Y

更新日期：1981-01-01 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：:Allopurinol exhibits good bioavailability (78-90%) after administration of oral dosage forms to humans and rabbits; however, it is not absorbed rectally from any of the dosage forms to any significant extent. Oral administration of allopurinol in a polyethylene glycol suspension, to which allopurinol may be reversibly...

journal_title：Journal of pharmaceutical sciences

authors： Patel VS,Kramer WG

更新日期：1986-03-01 00:00:00

abstract：:An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...

journal_title：Journal of pharmaceutical sciences

authors： Schieffer GW,Palermo PJ,Pollard-Walker S

更新日期：1984-01-01 00:00:00

abstract：:Even though gelatin is the most widely used polymeric excipient in pharmaceutical products, scant attention has been paid to its interaction with small organic molecules. The present work deals with the interaction of gelatin and four monosulfonated or monocarboxylated azo dyes having hydrocarbon moieties of different...

journal_title：Journal of pharmaceutical sciences

authors： Gautam J,Schott H

更新日期：1994-07-01 00:00:00

abstract：:Nipecotic acid (1), one of the most potent in vitro inhibitors of neuronal and glial gamma-amino butyric acid (GABA) uptake, is inactive as an anticonvulsant when administered systemically. To obtain in vivo active prodrugs of (1), we synthesized four new nipecotic acid esters (3-6), which were obtained by chemical co...

journal_title：Journal of pharmaceutical sciences

authors： Bonina FP,Arenare L,Palagiano F,Saija A,Nava F,Trombetta D,de Caprariis P

更新日期：1999-05-01 00:00:00

abstract：:Condensations of carbon disulfide were carried out with amino, chloro, and diamino heterocycles to give condensed ring thiazoline-2-thiones and imidazoline-2-thiones, with cyanomethyl heterocycles to give dithio acid derivatives, and with heterocyclic sulfonamides to give sulfonyldithiocarbamates. Of several examples ...

journal_title：Journal of pharmaceutical sciences

authors： Foye WO,Kauffman JM,Lanzillo JJ,LaSala EF

更新日期：1975-08-01 00:00:00

abstract：:The absorption, protein binding, blood-to-plasma ratio, renal excretion, and pharmacokinetics of the dopamine-2 agonists (D2-agonists) 4-(2-di-n-propylaminoethyl)-7-hydroxy-2-(3H)-indolone (1), N-(2'-hydroxy-5'-[N,N-di-n-propylaminoethylphenyl])methanesulfonamide (2), and 4-(2-di-n-propylaminoethyl)-2-(3H)-indolone (3...

journal_title：Journal of pharmaceutical sciences

authors： Swagzdis JE,Wittendorf RW,DeMarinis RM,Mico BA

更新日期：1986-10-01 00:00:00

abstract：:Comparability studies used to assess a proposed manufacturing change for a biological product include sensitive analytical studies to confirm there are no significant differences in structural or functional attributes that may contribute to clinically meaningful changes in efficacy or safety. When a proposed change is...

journal_title：Journal of pharmaceutical sciences

authors： Grampp G,McElroy PL,Camblin G,Pollock A

更新日期：2018-06-01 00:00:00

abstract：:A representative series of hydroxy-5 beta-cholanyl-24-amines were tested both in vitro and in vivo with respect to their activity against the intestinal bacteria responsible for bile acid metabolism. For the in vitro studies, radiolabeled [14C]cholic acid was incubated with human stools both in aerobic and anaerobic c...

journal_title：Journal of pharmaceutical sciences

authors： Roda A,Bellini AM,Mencini E,Minutello A,Fini A,Guarneri M

更新日期：1992-03-01 00:00:00

abstract：:The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were condu...

journal_title：Journal of pharmaceutical sciences

authors： Shaik N,Pan G,Elmquist WF

更新日期：2008-12-01 00:00:00

abstract：:Pepsin adsorbed on gibbsite or boehmite, non-acid-reactive forms of aluminum hydroxide, had a significantly lower activity than pepsin in solution. IR and desorbed pepsin activity studies showed that the reduced activity of adsorbed pepsin was not due to denaturation of pepsin on adsorption. Steric occlusion of the ac...

journal_title：Journal of pharmaceutical sciences

authors： Sepelyak RJ,Feldkamp JR,Regnier FE,White JL,Hem SL

更新日期：1984-11-01 00:00:00

abstract：:The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...

journal_title：Journal of pharmaceutical sciences

authors： Hall IH,Kasai R,Wu RY,Tagahara K,Lee KH

更新日期：1982-11-01 00:00:00

abstract：:The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However...

journal_title：Journal of pharmaceutical sciences

authors： Welling PG,Elliott RL,Pitterle ME,Corrick-West HP,Lyons LL

更新日期：1979-02-01 00:00:00

abstract：:The spherically agglomerated crystals of aminophylline (theophylline-ethylenediamine complex) can be compounded directly into pharmaceutical formulations without further processing, e.g., granulation. Such crystals were prepared by mixing theophylline and ethylenediamine in a partially miscible solvent system, i.e., o...

journal_title：Journal of pharmaceutical sciences

authors： Kawashima Y,Aoki S,Takenaka H,Miyake Y

更新日期：1984-10-01 00:00:00

abstract：:The purpose of the present experiment was to prepare and characterize the aqueous-based pseudolatex system of cellulose acetate butyrate (CAB) for controlled drug delivery. Aqueous pseudolatex systems are advantageous over organic-based coating systems because these systems are devoid of criteria pollutants such as ca...

journal_title：Journal of pharmaceutical sciences

authors： Vaithiyalingam S,Nutan M,Reddy I,Khan M

更新日期：2002-06-01 00:00:00

abstract：:In liver microsomes, selexipag (NS-304; ACT-293987) mainly undergoes hydrolytic removal of the sulfonamide moiety by carboxylesterase 1 (CES1) to yield the pharmacologically active metabolite MRE-269 (ACT-333679). However, it is not known how much CES in the liver and intestine contributes to the hydrolysis of selexip...

journal_title：Journal of pharmaceutical sciences

authors： Imai S,Ichikawa T,Sugiyama C,Nonaka K,Yamada T

更新日期：2019-02-01 00:00:00

abstract：:The assessment of provenance of heparin is becoming a major concern for the pharmaceutical industry and its regulatory bodies. Batch-specific [carbon (δ(13) C), nitrogen (δ(15) N), oxygen (δ(18) O), sulfur (δ(34) S), and hydrogen (δD)] stable isotopic compositions of five different animal-derived heparins were perform...

journal_title：Journal of pharmaceutical sciences

authors： Jasper JP,Zhang F,Poe RB,Linhardt RJ

更新日期：2015-02-01 00:00:00

abstract：:A novel process based on solvent extraction was developed to produce drug-loaded polyanhydride microspheres for controlled-release applications. The technique consists of adding a chloroform solution of polyanhydride and drug into a stirred silicone oil phase containing suspended droplets of surfactant. No chemical re...

journal_title：Journal of pharmaceutical sciences

authors： Bindschaedler C,Leong K,Mathiowitz E,Langer R

更新日期：1988-08-01 00:00:00

abstract：:Avoiding unwanted immunogenicity is of key importance in the development of therapeutic drug proteins. Animal models are of less predictive value because most of the drug proteins are recognized as foreign proteins. However, different methods have been developed to obtain immunotolerant animal models. So far, the immu...

journal_title：Journal of pharmaceutical sciences

authors： Brenden N,Madeyski-Bengtson K,Martinsson K,Svärd R,Albery-Larsdotter S,Granath B,Lundgren H,Lövgren A

更新日期：2013-03-01 00:00:00

abstract：:Co-amorphous drug-amino acid systems have gained growing interest as an alternative to common amorphous formulations which contain polymers as stabilizers. Several preparation methods have recently been investigated, including vibrational ball milling on a laboratory scale or spray drying in a larger scale. In this st...

journal_title：Journal of pharmaceutical sciences

authors： Lenz E,Löbmann K,Rades T,Knop K,Kleinebudde P

更新日期：2017-01-01 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：:NF-kappaB activation is clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The prominent role of IkappaB kinase-2 (IKK-2) in regulating NF-kappaB signaling in response to proinflammatory stimuli has made IKK-2 a primary anti-inflammation therapeutic target. PHA-408, a potent and ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Kishore NN,Thompson DC

更新日期：2010-03-01 00:00:00

abstract：:Approximately 30% of active pharmaceutical ingredients (APIs) experience agglomeration, granulation, and breakage during agitated drying. Currently, there is no small-scale bench tool to help assess and observe granulation behavior of APIs in the laboratory and subsequently lead to the development of a robust drying m...

journal_title：Journal of pharmaceutical sciences

authors： Zhang S,Lamberto DJ

更新日期：2014-01-01 00:00:00

abstract：:Poly(methyl [1-14C]methacrylate) nanoparticles were injected subcutaneously into rats. Almost all of the radioactivity stayed at the injection site. After an initial urinary and fecal excretion of approximately 1% of the administered dose per day, the rate of elimination dropped to a low level (approximately 0.005%/da...

journal_title：Journal of pharmaceutical sciences

authors： Kreuter J,Nefzger M,Liehl E,Czok R,Voges R

更新日期：1983-10-01 00:00:00

abstract：:Although several mathematical models have been reported for the estimation of human plasma concentration profiles of drug substances after dermal application, the successful cases that can predict human pharmacokinetic profiles are limited. Therefore, the aim of this study is to investigate the prediction of human pla...

journal_title：Journal of pharmaceutical sciences

authors： Yamamoto S,Karashima M,Arai Y,Tohyama K,Amano N

更新日期：2017-09-01 00:00:00

abstract：:Aqueous solutions of several ionizable substances were stored in plastic infusion bags and the sorption of the substances monitored with time. The substances used were p-nitrophenol, p-toluidine, warfarin sodium [3-(alpha-acetonylbenzyl)-4-hydroxycoumarin sodium salt] and trifluoperazine hydrochloride (10-[3-(4-methyl...

journal_title：Journal of pharmaceutical sciences

authors： Kowaluk EA,Roberts MS,Polack AE

更新日期：1986-06-01 00:00:00

abstract：:The quantitative analysis of a new pharmaceutically active amine hydrochloride is described. Samples are extracted with chloroform. A yellow amine-dye complex is formed by buffering a sample-bromthymol blue solution at pH 8.5 +/- 0.1 and subsequently extracted with chloroform. The complex is treated with 0.01 N NaOH t...

journal_title：Journal of pharmaceutical sciences

authors： Chang ZL,Papendick VE

更新日期：1976-10-01 00:00:00

abstract：:Arginine-glycine-aspartate (RGD) has been shown to be essential for the recognition of integrins overexpressed in tumor cells, especially during tumor invasion, angiogenesis, and metasis. In this study, a novel tetrapeptide, RGD-valine (RGDV), was designed and attached to the N position of 1-β-D-arabinofuranosylcytosi...

journal_title：Journal of pharmaceutical sciences

authors： Wang F,Cui C,Ren Z,Wang L,Liu H,Cui G

更新日期：2012-12-01 00:00:00