Testosterone-independent down-regulation of Oct2 in the kidney medulla from a uranyl nitrate-induced rat model of acute renal failure: effects on distribution of a model organic cation, tetraethylammonium.

abstract：:The aim of this study was to characterize the in vitro hepatic uptake kinetics of sodium fluorescein (NaFluo) and identify the transporters involved. NaFluo exhibited saturable uptake kinetics in suspended rat and human hepatocytes as reflected by K(m) values of 22.5 and 14.1 µM, and V(max) values of 98.3 and 5.8 pmol...

journal_title：Journal of pharmaceutical sciences

authors： De Bruyn T,Fattah S,Stieger B,Augustijns P,Annaert P

更新日期：2011-11-01 00:00:00

abstract：:The objective of this study was to determine the relative importance of metabolism by cytochrome P450 (CYP) enzymes versus efflux by P-glycoprotein (P-gp) in restricting the intestinal mucosal permeation of cyclic prodrugs (AOA-DADLE, CA-DADLE, OMCA-DADLE) of the opioid peptide DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH). AO...

journal_title：Journal of pharmaceutical sciences

authors： Ouyang H,Chen W,Andersen TE,Steffansen B,Borchardt RT

更新日期：2009-01-01 00:00:00

abstract：:Targeted echogenic liposome dispersions for ultrasonic enhancement of vasoactive and pathological components of endothelium and atherosclerosis have recently been developed. The component lipids required for acoustic and targeting properties include phosphatidylcholine, phosphatidylethanolamine phosphatidylglycerol (P...

journal_title：Journal of pharmaceutical sciences

authors： Huang SL,Hamilton AJ,Nagaraj A,Tiukinhoy SD,Klegerman ME,McPherson DD,Macdonald RC

更新日期：2001-12-01 00:00:00

abstract：:Corneal penetration studies were conducted in unanesthetized albino rabbits using various organic compounds representing both polar and nonpolar species. Very low molecular weight compounds demonstrate rapid uptake into the aqueous humor despite the lipid-like barrier imposed by the corneal epithelium. Evidence that t...

journal_title：Journal of pharmaceutical sciences

authors： Grass GM,Robinson JR

更新日期：1988-01-01 00:00:00

abstract：:The impact of intestinal conjugative metabolism on oral bioavailability was assessed by sequential and simultaneous analyses of the reported data in humans. The data were retrieved from reports on drugs that are metabolized by sulfate conjugation, and the organ availabilities affecting oral bioavailability were differ...

journal_title：Journal of pharmaceutical sciences

authors： Mizuma T,Kawashima K,Sakai S,Sakaguchi S,Hayashi M

更新日期：2005-03-01 00:00:00

abstract：:Alkyl esters (C1--C4) of the four halofumaric acids were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes at pH 5.6 and 7.0 in the absence and presence of 10% beef serum in Sabouraud dextrose agar. The most toxic compound to each organism was: C....

journal_title：Journal of pharmaceutical sciences

authors： Gershon H,Shanks L

更新日期：1978-04-01 00:00:00

abstract：:Curcumin has been investigated as a potential photosensitizer (PS) in antimicrobial photodynamic therapy (aPDT). The phototoxic effect of curcumin is dependent on proper formulations of the compound because of the lipophilic nature of the molecule and the extremely low water solubility at physiological conditions. In ...

journal_title：Journal of pharmaceutical sciences

authors： Hegge AB,Nielsen TT,Larsen KL,Bruzell E,Tønnesen HH

更新日期：2012-04-01 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：: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：:Pelrinone HCl is essentially nonhygroscopic. The pH-solubility profile exhibits a U-shaped curve, while the octanol-water partition coefficient-pH profile shows a bell-shaped curve. Two ionizable functions, with a pKa1 value of 4.71 and a pKa2 value of 8.94, produce the cationic and anionic forms, respectively. A weak...

journal_title：Journal of pharmaceutical sciences

authors： Hajdu J,Adams G,Lee HK

更新日期：1988-11-01 00:00:00

abstract：:The aim was to study a new method of dissolution in vitro, the "Bio-Dis" apparatus, and to compare it with the classical rotating bottle method. Several theophylline controlled-release drug dosage forms were studied. Dissolution testing was performed in increasing pH in standard conditions and after treatment with pea...

journal_title：Journal of pharmaceutical sciences

authors： Esbelin B,Beyssac E,Aiache JM,Shiu GK,Skelly JP

更新日期：1991-10-01 00:00:00

abstract：:The bioavailability of clofibric acid from formulations containing calcium clofibrate along and mixed with calcium carbonate (1:1 w/w) was compared to that from a standard clofibrate formulation in a crossover study in 12 human subjects. The 95% confidence intervals of bioavailability differences were such that they ...

journal_title：Journal of pharmaceutical sciences

authors： Taylor T,Chasseaud LF

更新日期：1977-11-01 00:00:00

abstract：:Reported estrone pKa and solubility data show wide variation. Improved experimental procedures were designed and used to obtain reproducible results. The pKa values for several estrogens and related compounds also were determined to assess the effects of structural differences on ionization. No evidence was obtained f...

journal_title：Journal of pharmaceutical sciences

authors： Hurwitz AR,Liu ST

更新日期：1977-05-01 00:00:00

abstract：:Cosalane is a potent inhibitor of HIV replication with multiple sites of action. The purposes of this study were to (a) determine the extent and nature of cosalane binding to mucin, alpha(1)-acid glycoprotein (AAG), plasma, and human (HSA) and bovine serum (BSA) albumin, and (b) determine the primary site(s) of cosala...

journal_title：Journal of pharmaceutical sciences

authors： Kuchimanchi KR,Ahmed MS,Johnston TP,Mitra AK

更新日期：2001-05-01 00:00:00

abstract：:Increasing costs of research and development in the pharmaceutical industry has necessitated a growing interest in the early prediction of human pharmacokinetics of drug candidates. Of growing interest is the need to understand oral absorption, the most common route of small molecule drug administration. The fraction ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Liu J,Fan P,Wong H

更新日期：2018-07-01 00:00:00

abstract：:Naltrexone (NTX) is an opioid antagonist used for treatment of narcotic dependence and alcoholism. Transdermal naltrexone delivery is desirable to help improve patient compliance. The purpose of this study was to increase the delivery rate of NTX across human skin by using lipophilic alkyl ester prodrugs. Straight-cha...

journal_title：Journal of pharmaceutical sciences

authors： Stinchcomb AL,Swaan PW,Ekabo O,Harris KK,Browe J,Hammell DC,Cooperman TA,Pearsall M

更新日期：2002-12-01 00:00:00

abstract：:An alumina (Al(2)O(3))-steroid-ethanol model is used for forced degradation testing of corticosteroids to predict chemical stability and degradation products in pressurized metered-dose inhaler (pMDI) solution formulations. The model involves an ethanolic solution of a test steroid with Al(2)O(3), stressed at elevated...

journal_title：Journal of pharmaceutical sciences

authors： Wu ZZ,Thatcher ML,Lundberg JK,Ogawa MK,Jacoby CB,Battiste JL,Ledoux KA

更新日期：2012-06-01 00:00:00

abstract：:The objective of the present study was to investigate the iontophoretic transport behavior across multiple membranes of different barrier properties. Spectra/Por(R) (SP) and Ionac membranes were the synthetic membranes and sclera was the biomembrane in this model study. The barrier properties of SP membranes were dete...

journal_title：Journal of pharmaceutical sciences

authors： Molokhia SA,Zhang Y,Higuchi WI,Li SK

更新日期：2008-01-01 00:00:00

abstract：:The challenge of defining the concentration of unbound drug at the lung target site after inhalation limits the possibility to optimize target exposure by compound design. In this study, a novel rat lung slice methodology has been developed and applied to study drug uptake in lung tissue, and the mechanisms by which t...

journal_title：Journal of pharmaceutical sciences

authors： Bäckström E,Lundqvist A,Boger E,Svanberg P,Ewing P,Hammarlund-Udenaes M,Fridén M

更新日期：2016-02-01 00:00:00

abstract：:The in vitro antifungal activity of a novel series of cis- and trans-5-([aryl or aryloxy (or thio)]methyl)-3-(1H-imidazol-1-ylmethyl)-3- (2-thienyl)-2-methylisoxazolidines (13-24) was evaluated and compared with ketoconazole. The title series of compounds was prepared via a 1,3-dipolar cycloaddition reaction of 1-(2-t...

journal_title：Journal of pharmaceutical sciences

authors： Mullen GB,Mitchell JT,Allen SD,St Georgiev V

更新日期：1988-12-01 00:00:00

abstract：:The kinetic profile for the decomposition of ditiocarb sodium salt in aqueous solution was achieved with UV-visible absorption spectrometry. The kinetic profile indicates that the decomposition reaction is hydrogen ion-catalyzed over the entire 4-10 pH range and enables the determination of the value of the acid-base ...

journal_title：Journal of pharmaceutical sciences

authors： Martens T,Langevin-Bermond D,Fleury MB

更新日期：1993-04-01 00:00:00

abstract：:Glasses were prepared from a number of barbiturates. The viscosities and glass transition temperatures of the glasses were dependent on the structure of the groups present on the C-5 and N-1 atoms. Solid dispersions were prepared from three selected barbiturates formulated with citric acid. The glass transition temper...

journal_title：Journal of pharmaceutical sciences

authors： Summers MP

更新日期：1978-11-01 00:00:00

abstract：:The problem of optimizing ocular bioavailability of topically applied ophthalmic drugs is discussed. A formula for drug concentration in the tear film is derived using well-known pharmacokinetic relationships and a first-order drug decay model for the tear film. The time integral of the tear film concentration is then...

journal_title：Journal of pharmaceutical sciences

authors： Keister JC,Cooper ER,Missel PJ,Lang JC,Hager DF

更新日期：1991-01-01 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：:This study describes the synthesis of a new generation of immunotoxins made by a noncovalent interaction between a monoclonal antibody derivatized with a dichlorotriazinic dye and the ribosomal inhibitor protein gelonin. The scheme of preparation has several advantages with respect to the traditional methods, which us...

journal_title：Journal of pharmaceutical sciences

authors： Dosio F,Brusa P,Delprino L,Grosa G,Ceruti M,Cattel L

更新日期：1994-02-01 00:00:00

abstract：:The p-aminobenzyl analogues (8a and 8b, respectively) of the cardioselective beta-adrenergic receptor antagonists practolol and atenolol were prepared from the corresponding phenoxymethyloxiranes in 30 and 13% yields, respectively. The dissociation constants for the beta-adrenergic receptor were measured in membrane p...

journal_title：Journal of pharmaceutical sciences

authors： Jones GS Jr,Bylund DB,Hanson RN

更新日期：1992-04-01 00:00:00

abstract：:It is hypothesized that ferrocene (FC)-loaded nanocarriers (FC-NCs) are safe label-free contrast agents for cochlear biodistribution study by transmission electron microscopy (TEM). To test this hypothesis, after engineering, the poly(epsilon-caprolactone)/polyglycolide NCs are tested for stability with various types ...

journal_title：Journal of pharmaceutical sciences

authors： Youm I,Musazzi UM,Gratton MA,Murowchick JB,Youan BC

更新日期：2016-10-01 00:00:00

abstract：:An assay is described for the determination of the H2-receptor antagonist, cimetidine, in human plasma and urine. Alkalinized plasma or urine was extracted with methylene chloride, the organic phase was evaporated, and the reconstituted residue was analysed by high-pressure liquid chromatography (HPLC) using a reverse...

journal_title：Journal of pharmaceutical sciences

authors： Mihaly GW,Cockbain S,Jones DB,Hanson RG,Smallwood RA

更新日期：1982-05-01 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：:By using data from a sample of 1767 community pharmacies, a total cost function was estimated by a polynomial regression of total cost on output. The Cobb-Douglas production function was estimated by a multiple linear regression of natural logarithmic transformations of output on natural logarithmic transformation of ...

journal_title：Journal of pharmaceutical sciences

authors： Lohrisch D,Shull SC,Smith MC

更新日期：1976-02-01 00:00:00