Physiological model for distribution of sulfathiazole in swine.

abstract：:Dendrimers have emerged as a promising drug delivery system due to their well defined size, tailorability, and multifunctional nature. However, their application in brain delivery is relatively a new area of research. The present study was aimed at evaluating the uptake and permeation of polyether-copolyester (PEPE) d...

journal_title：Journal of pharmaceutical sciences

authors： Dhanikula RS,Hammady T,Hildgen P

更新日期：2009-10-01 00:00:00

abstract：:Twenty-two neutral, lipid-soluble 99mTc complexes have been synthesized from diamine dithiol (DADT) ligands which vary in alkyl substitution pattern on nitrogen and carbon. The logarithm of the partition coefficients (log PC), as well as the capacity factor k', of the purified complexes increased linearly with molecul...

journal_title：Journal of pharmaceutical sciences

authors： Lever SZ,Sun SY,Scheffel UA,Kaltovich FA,Baidoo KE,Goldfarb H,Wagner HN Jr

更新日期：1994-06-01 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：:3D cultures of primary human hepatocytes (PHH) are emerging as a more in vivo-like culture system than previously available hepatic models. This work describes the characterisation of drug metabolism in 3D PHH spheroids. Spheroids were formed from three different donors of PHH and the expression and activities of impo...

journal_title：Journal of pharmaceutical sciences

authors： Kanebratt KP,Janefeldt A,Vilén L,Vildhede A,Samuelsson K,Milton L,Björkbom A,Persson M,Leandersson C,Andersson TB,Hilgendorf C

更新日期：2021-01-01 00:00:00

abstract：:The aim of this study was to synthetize cocrystals of nateglinide, an antidiabetic agent of biopharmaceutics classification system Class IIa, as a strategy to improve both the solubility and the dissolution rate of the drug. Benzamide was selected by a screening procedure as a suitable coformer, and binary mixtures wi...

journal_title：Journal of pharmaceutical sciences

authors： Bruni G,Maggi L,Mustarelli P,Sakaj M,Friuli V,Ferrara C,Berbenni V,Girella A,Milanese C,Marini A

更新日期：2019-04-01 00:00:00

abstract：:A physically based method for arriving at topological indexes is described. The derived indexes correlate with molecular surface areas and with the molecular connectivity index. The newly derived index seems to account better for the expected distinctions among primary, secondary, and tertiary alcohol aqueous solubili...

journal_title：Journal of pharmaceutical sciences

authors： Cammarata A

更新日期：1979-07-01 00:00:00

abstract：:An exsorption technique which can assess the transport of a drug from blood to the intestinal lumen was used to study the effects of glucose and to determine the presence of segmental differences in drug transport across the rat small intestinal membrane following intravenous drug administration. The drugs used in the...

journal_title：Journal of pharmaceutical sciences

authors： Johno I,Kitazawa S

更新日期：1985-03-01 00:00:00

abstract：:The goal was to evaluate the effects of acidity, expressed as the Hammett acidity function, on chemical reactivity in freeze-dried materials (lyophiles). Dextran-sucrose-citrate and polyvinyl pyrrolidone (PVP)-sucrose-citrate aqueous solutions, adjusted to pH values of 2.6, 2.8, and 3.0 were freeze dried, and characte...

journal_title：Journal of pharmaceutical sciences

authors： Chatterjee K,Shalaev EY,Suryanarayanan R,Govindarajan R

更新日期：2008-01-01 00:00:00

abstract：:The absorption of the model drug carbenoxolone was reevaluated using an in situ rat intestinal perfusion technique in which disappearance from the intestinal lumen, binding to the perfused jejunal segment, and appearance in the mesenteric (jejunal) vein were measured. The effect of the degree of ionization on these pr...

journal_title：Journal of pharmaceutical sciences

authors： Blanchard J,Tang LM,Earle ME

更新日期：1990-05-01 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：:This work investigates the use of spray freeze-drying (SFD) to produce protein loaded particles suitable for epidermal delivery. In the first part of the study, the effects of formulation and process conditions on particle properties are examined. Aqueous solutions of trehalose produce SFD particles in the size range ...

journal_title：Journal of pharmaceutical sciences

authors： Sonner C,Maa YF,Lee G

更新日期：2002-10-01 00:00:00

abstract：:L-3-(3-Hydroxy-4-pivaloyloxyphenyl)alanine (1, NB-355) is a novel L-dopa prodrug. After oral administration with carbidopa in rats, 1 demonstrated 2.3 times longer duration (MRT) and 1.4 times larger bioavailability (AUC) on plasma L-dopa concentrations than those of L-dopa itself. Similar results were obtained in dog...

journal_title：Journal of pharmaceutical sciences

authors： Ihara M,Tsuchiya Y,Sawasaki Y,Hisaka A,Takehana H,Tomimoto K,Yano M

更新日期：1989-07-01 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：:Contraceptive natural steroids, such as progesterone and estradiol, are ineffective when administered orally because of extensive metabolism in the gastrointestinal (GI) tract during absorption and first-pass metabolism. Consequently, highly potent and potentially harmful synthetic steroids are now being used in oral...

journal_title：Journal of pharmaceutical sciences

authors： Hussain AA,Hirai S,Bawarshi R

更新日期：1981-04-01 00:00:00

abstract：:Microbicide intravaginal rings (IVRs) are a promising woman-controlled strategy for preventing sexual transmission of human immunodeficiency virus (HIV). An IVR was prepared and developed from polyether urethane (PU) elastomers for the sustained delivery of UC781, a highly potent nonnucleoside reverse transcriptase in...

journal_title：Journal of pharmaceutical sciences

authors： Clark MR,Johnson TJ,McCabe RT,Clark JT,Tuitupou A,Elgendy H,Friend DR,Kiser PF

更新日期：2012-02-01 00:00:00

abstract：:Adsorption of proteins to solid-fluid interfaces is often empirically found to promote formation of soluble aggregates and larger, subvisible, and visible particles, but key stages in this process are often difficult to probe directly. Aggregation mediated by adsorption to water-silicon oxide (SiOx) interfaces, akin t...

journal_title：Journal of pharmaceutical sciences

authors： Perevozchikova T,Nanda H,Nesta DP,Roberts CJ

更新日期：2015-06-01 00:00:00

abstract：:Oxidative-reductive interconversion of the methylthiomethyl ester of aspirin and the corresponding sulfoxide and sulfone derivatives can be detected in rat liver homogenate, in addition to the extremely facile hydrolysis of these esters. The methylthiomethyl and methylsulfinylmethyl 2-acetoxybenzoates penetrate freshl...

journal_title：Journal of pharmaceutical sciences

authors： Loftsson T,Bodor N

更新日期：1981-07-01 00:00:00

abstract：:The described simple, accurate, and precise reversed-phase high-pressure liquid chromatographic procedure is in excellent agreement with 1-octanol shake-flask partition or distribution coefficients over a 3.5 log range. A chemically bonded octadecylsilane support is persilated and coated with 1-octanol. With 1-octanol...

journal_title：Journal of pharmaceutical sciences

authors： Unger SH,Cook JR,Hollenberg JS

更新日期：1978-10-01 00:00:00

abstract：:One manifestation of cystic fibrosis (CF) is the presence of a viscid mucus secretion in the lungs. The clearance of this mucus is significantly slower than in "normals" due to uncoordinated beating of the cilia and the increased viscosity of the mucus. In these studies, the permeabilities of p-aminosalicylic acid, is...

journal_title：Journal of pharmaceutical sciences

authors： Bhat PG,Flanagan DR,Donovan MD

更新日期：1996-06-01 00:00:00

abstract：:The permeability coefficient, Kp, of pure unbranched alkanoic acids (C2-C7) applied to isolated porcine skin, reached a maximum in the solubility parameter (delta 2) range of 9.7-10 cal1 /2/cm3/2. When these and other penetrants were delivered from a solvent vehicle, the following linear relationships could be demonst...

journal_title：Journal of pharmaceutical sciences

authors： Liron Z,Cohen S

更新日期：1984-04-01 00:00:00

abstract：:The physicochemical properties of ricobendazole (RBZ) were characterized using conventional methods. Solubility in some pharmaceutical solvents, pH-solubility, ionization properties, and lipophilicity are described. The solubility of RBZ in water is 62 mug/mL and very poor in common pharmaceutical solvents, for exampl...

journal_title：Journal of pharmaceutical sciences

authors： Wu Z,Razzak M,Tucker IG,Medlicott NJ

更新日期：2005-05-01 00:00:00

abstract：:DB844 (CPD-594-12), N-methoxy-6-{5-[4-(N-methoxyamidino)phenyl]-furan-2-yl}-nicotinamidine, is an oral prodrug that has shown promising efficacy in both mouse and monkey models of second stage human African trypanosomiasis. However, gastrointestinal (GI) toxicity was observed with high doses in a vervet monkey safety ...

journal_title：Journal of pharmaceutical sciences

authors： Ju W,Yang S,Ansede JH,Stephens CE,Bridges AS,Voyksner RD,Ismail MA,Boykin DW,Tidwell RR,Hall JE,Wang MZ

更新日期：2014-01-01 00:00:00

abstract：:Metronidazole (MTZ) is a drug of choice for protozoal infections such as luminal amoebiasis. We designed and synthesized N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine (NMG) as a colon-specific prodrug of MTZ. The synthetic yield of NMG was about 34%. The apparent partition coefficient of MTZ w...

journal_title：Journal of pharmaceutical sciences

authors： Kim D,Hong S,Jung S,Jung Y,Kim YM

更新日期：2009-11-01 00:00:00

abstract：:Phenytoin (DPH) was delivered to the brain by a dihydropyridine in equilibrium pyridinium salt redox system, which was evaluated for anticonvulsant activity. Following iv injection of the lipophilic delivery system of DPH (2) to rats, concentrations of DPH were lower but sustained and, after 30 min, essentially the sa...

journal_title：Journal of pharmaceutical sciences

authors： Shek E,Murakami T,Nath C,Pop E,Bodor NS

更新日期：1989-10-01 00:00:00

abstract：:A difference spectrophotometric analytical method was developed for the selective determination of p-hydroxybenzoic acid in the presence of its alkyl esters without prior separation. Based on the spectral shift to a shorter wavelength accompanyint carboxyl dissociation, the procedure measures as little as 2% of this a...

journal_title：Journal of pharmaceutical sciences

authors： Fink DW,Fink HC,Tolan JW,Blodinger J

更新日期：1978-06-01 00:00:00

abstract：:The objective of this study was to determine if a high Tg polymer (Eudragit(®) S100) could be used to stabilize amorphous domains of polyethylene oxide (PEO) and hence improve the stability of binary polymer systems containing celecoxib (CX). We propose a novel method of stabilizing the amorphous PEO solid dispersion ...

journal_title：Journal of pharmaceutical sciences

authors： Jones DS,Tian Y,Li S,Yu T,Abu-Diak OA,Andrews GP

更新日期：2016-10-01 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：:Complexation of ferrous cytochrome P450 by metabolic intermediates formed during NADPH-catalyzed metabolism of compounds structurally related to orphenadrine was studied. This so-called metabolic intermediate complexation was determined in rat liver microsomes, obtained from phenobarbital-pretreated rats, at 455 nm us...

journal_title：Journal of pharmaceutical sciences

authors： Bast A,Savenije-Chapel EM,Noordhoek J

更新日期：1984-07-01 00:00:00

abstract：:The objective of this study was to generate a water-soluble thiolated chitosan to enable the permeation-enhancing effect of chitosan at pH of at least 5.5 without losing the advantages of improved mucoadhesive properties. Therefore, the thiol-bearing polyoxyethylene ligand {O-(3-carboxylpropyl)-O'-[2-[3-mercaptopropio...

journal_title：Journal of pharmaceutical sciences

authors： Hauptstein S,Bonengel S,Griessinger J,Bernkop-Schnürch A

更新日期：2014-02-01 00:00:00

abstract：:Central-nervous-system, physiologically based pharmacokinetic (PBPK) models predict exposure profiles in the brain, that is, the rate and extent of distribution. The current work develops one such model and presents improved methods for determining key input parameters. A simple linear regression statistical model est...

journal_title：Journal of pharmaceutical sciences

authors： Trapa PE,Belova E,Liras JL,Scott DO,Steyn SJ

更新日期：2016-02-01 00:00:00