Tissue-selective uptake of pravastatin in rats: contribution of a specific carrier-mediated uptake system.

abstract：:A chiral gas chromatographic assay previously developed for quantitative analysis of ethosuximide and its major metabolites in rat urine has been adapted for the analysis of the drug in plasma. Ethosuximide, both as a racemic mixture and as the individual enantiomers, was administered to conscious rats by the intraven...

journal_title：Biopharmaceutics & drug disposition

authors： Mifsud J,Collier PS,Millership JS

更新日期：2001-03-01 00:00:00

abstract：:Based on the principle of superposition an expression has been established relating a drug concentration at steady-state to a concentration after a single dose. This relationship applies for drugs with linear pharmacokinetics given at equal dosage intervals and it is independent of the route of administration. The rel...

journal_title：Biopharmaceutics & drug disposition

authors： Love BL,Tsuei SE,Thomas J,Nation RL

更新日期：1982-07-01 00:00:00

abstract：:Aim. To study the pharmacokinetics of dihydroartemisinin (DHA) in Artekin (compound dihydroartemisinin) tablets in Chinese healthy volunteers. Methods. Eighteen healthy volunteers (9 males, 9 females) received Artekin tablets for oral administration. The plasma samples of DHA were analysed by liquid-liquid extraction ...

journal_title：Biopharmaceutics & drug disposition

authors： Hong X,Liu CH,Huang XT,Huang TL,Ye SM,Ou WP,Wang NS,Mi SQ

更新日期：2008-05-01 00:00:00

abstract：:Drugs that are largely restricted to the gastro-intestinal tract (GIT) for their therapeutic efficacy and that are not substantially absorbed into the body are usually inadequately studied in terms of systemic bioavailability. The possibility of systemic effects requires that bioavailabilities be studied to ensure aga...

journal_title：Biopharmaceutics & drug disposition

authors： Fasanmade AA,Akanni AO,Olaniyi AA,Fasanmade AA,Tayo F

更新日期：1994-08-01 00:00:00

abstract：:The usefulness of a limited sampling method (LSM) to determine the bioequivalence of highly variable drugs with long half-lives was investigated. The LSM uses multiple linear regression of observed drug plasma concentrations versus area under the curve (AUC) or C(max) (peak plasma concentration) to obtain a best set o...

journal_title：Biopharmaceutics & drug disposition

authors： Jackson AJ

更新日期：2001-07-01 00:00:00

abstract：:The objective of this study was to investigate the absorption behavior of chikusetsusaponin IVa (CHS-IVa) in the rat intestine using single-pass intestinal perfusion (SPIP) and to classify CHS-IVa into the biopharmaceutics classification system (BCS). The equilibrium solubility of CHS-IVa was determined by the shaker ...

journal_title：Biopharmaceutics & drug disposition

authors： Zhang W,Liu H,Liu C

更新日期：2019-09-01 00:00:00

abstract：:Pharmacokinetics of ragaglitazar (a novel phenoxazine derivative of aryl propanoic acid), a potent insulin sensitizing and lipid-lowering compound was studied in Wistar rats. A single dose of 1, 3 or 10 mg/kg of ragaglitazar was given orally to male rats (n=4 per dose level) to evaluate dose proportionality. In anothe...

journal_title：Biopharmaceutics & drug disposition

authors： Jagannath K,Chaluvadi MR,Mullangi R,Mamidi NV,Srinivas NR

更新日期：2004-10-01 00:00:00

abstract：:Data from sustained-release and enteric-coated oral formulations, and the suppository formulation of diclofenac sodium are fitted simultaneously using NONMEM and the general linear model, ADVAN 5. Absorption and disposition parameters, serum levels, and absorption profiles were determined. The in vivo absorption profi...

journal_title：Biopharmaceutics & drug disposition

authors： Idkaidek NM,Amidon GL,Smith DE,Najib NM,Hassan MM

更新日期：1998-04-01 00:00:00

abstract：:Dolasetron, Anzemet, a 5-hydroxytryptamine receptor antagonist, is under investigation as an antiemetic agent. The keto-reduced metabolite of dolasetron has been identified in human plasma and is probably responsible for the majority of the antiemetic activity. This study evaluated the pharmacokinetics of dolasetron a...

journal_title：Biopharmaceutics & drug disposition

authors： Shah A,Lanman R,Bhargava V,Weir S,Hahne W

更新日期：1995-04-01 00:00:00

abstract：:The biotransformation of thionorphine (N-cyclopropylmethyl-7alpha-[(s)-1-hydroxy-1-methyl-3-(2thiophene)-propyl]-6,14-endo-ethano tetrahydrooripavine), a new analgesic, was in-vestigated in rats. The results of metabolite analysis by liquid chromatography/electrospray ionization tandem mass spectrometry with positive ...

journal_title：Biopharmaceutics & drug disposition

authors： Wei SX,Zhang ZQ,Wang XY,Guo JF

更新日期：2004-04-01 00:00:00

abstract：:Four normal volunteers each received two intravenous doses of PA. The mean low dose was 3.30 mg kg-1 (infused over 20 minutes) while the mean high dose was 12.5 mg kg-1 (infused over 60 minutes). Blood samples were collected for 12 hours and urine was collected for 48 hours after each dose. PA concentrations were dete...

journal_title：Biopharmaceutics & drug disposition

authors： Coyle JD,Boudoulas H,Mackichan JJ,Lima JJ

更新日期：1985-04-01 00:00:00

abstract：:Comparative in vivo studies of aqueous solution, multiple w/o/w, and w/o emulsions showed that formulating 5-fluorouracil in emulsion systems significantly sustained the release of the drug from intramuscular injection sites in the rat. Intramuscular injection of the drug in both w/o and w/o/w emulsion systems produce...

journal_title：Biopharmaceutics & drug disposition

authors： Omotosho JA,Whateley TL,Florence AT

更新日期：1989-05-01 00:00:00

abstract：:Circadian variations in disposition have been observed for a variety of agents, including anticonvulsants. Valproic acid (VPA), an anticonvulsant used to control generalized and partial seizures, has exhibited diurnal oscillations in steady-state concentrations during long-term administration to humans and non-human p...

journal_title：Biopharmaceutics & drug disposition

authors： Arens TL,Pollack GM

更新日期：2001-09-01 00:00:00

abstract：:The steady-state pharmacokinetics of an ultralong sustained release formulation of theophylline (Unilong) twice daily (bid) in elderly hospitalized patients suffering from chronic obstructive pulmonary disease (COPD) have been studied in order to establish guidelines for monitoring. The study was carried out in 37 pat...

journal_title：Biopharmaceutics & drug disposition

authors： Armijo JA,Sánchez BM,Peralta FG,González-Ruiz M,Cuadrado A,Verdejo A,Cos MA,Arjona R

更新日期：2003-05-01 00:00:00

abstract：:The total body clearance (CL), renal clearance (CLR), and nonrenal clearance (CLNR) of caffeine from plasma were determined following the intravenous administration of caffeine (4 mg kg-1) to ten healthy men (aged 66-86 years) on three separate occasions. Positive correlations were observed between CL and urine flow r...

journal_title：Biopharmaceutics & drug disposition

authors： Trang JM,Blanchard J,Conrad KA,Harrison GG

更新日期：1985-01-01 00:00:00

abstract：:Betahistine, a potent histamine H3 receptor antagonist, is being developed for the treatment of attention deficit hyperactivity disorder (ADHD) that manifests with symptoms such as hyperactivity, impulsivity and inattention. This study describes the pharmacokinetics of betahistine in ADHD subjects at doses higher than...

journal_title：Biopharmaceutics & drug disposition

authors： Moorthy G,Sallee F,Gabbita P,Zemlan F,Sallans L,Desai PB

更新日期：2015-10-01 00:00:00

abstract：:After in vitro incubation of cecal content from CVL or gnotobiotic rats with rhein anthraquinone (1 mg g-1) for 18 h at 37 degrees, the anthraquinone was converted to rhein anthrone for 23.5 (SD +/- 3.4) per cent and 19.4 (+/- 4.7) per cent, respectively. Liquid cultures of some strictly anaerobic fecal bacteria of ma...

journal_title：Biopharmaceutics & drug disposition

authors： de Witte P,Van Hoestenberghe A,Eyssen H

更新日期：1992-05-01 00:00:00

abstract：:CYP2C9 is a human microsomal cytochrome P450c (CYP). Much variation in CYP2C9 levels and activity can be attributed to polymorphisms of this gene. Wild-type CYP2C9 and ten mutants were co-expressed with NADPH-cytochrome P450 reductase in Escherichia coli. The hydroxylase activities toward steroids were examined. CYP2C...

journal_title：Biopharmaceutics & drug disposition

authors： Uno T,Nakano R,Kitagawa R,Okada M,Kanamaru K,Takenaka S,Uno Y,Imaishi H

更新日期：2018-09-01 00:00:00

abstract：:The inhibition potencies of aripiprazole and its active metabolite, dehydroaripiprazole, on the activities of human multidrug resistance protein 1 (MDR1/ABCB1; P-glycoprotein), breast cancer resistance protein (BCRP/ABCG2) and multidrug resistance-associated protein 4 (MRP4/ABCC4), that are drug efflux transporters ex...

journal_title：Biopharmaceutics & drug disposition

authors： Nagasaka Y,Oda K,Iwatsubo T,Kawamura A,Usui T

更新日期：2012-09-01 00:00:00

abstract：:The pharmacokinetic profiles of a sublingual and a conventional oral lorazepam tablet formulation were established following chronic administration to twelve healthy male volunteers. Fitting a multi-dose equation based on a one-compartment model to the observed data, the average elimination half-lives for the sublingu...

journal_title：Biopharmaceutics & drug disposition

authors： Caillé G,Spénard J,Lacasse Y,Brennan J

更新日期：1983-01-01 00:00:00

abstract：:Regional pharmacokinetics is the study of the drug concentrations in specific regions of the body. It allows greater insight into the mechanisms of drug disposition than the study of systemic blood concentrations. Experimental methods in regional pharmacokinetics and their applications and limitations are reviewed. Po...

journal_title：Biopharmaceutics & drug disposition

authors： Upton RN,Runciman WB,Mather LE

更新日期：1990-12-01 00:00:00

abstract：:Antiretroviral therapy has been the mainstay of treatment for neonates born to HIV infected mothers. Neonates born prematurely to HIV positive mothers are underdeveloped not only in anatomical terms but also in their physiological systems. Zidovudine, the first antiretroviral drug in clinical therapy for the treatment...

journal_title：Biopharmaceutics & drug disposition

authors： Wei L,Mansoor N,Khan RA,Czejka M,Ahmad T,Ahmed M,Ali M,Yang DH

更新日期：2019-11-01 00:00:00

abstract：:Raltegravir is a human immunodeficiency virus (HIV)-1 integrase strand transfer inhibitor currently marketed at a dose of 400 mg twice-daily (b.i.d.). Raltegravir 1200 mg once-daily (q.d.) (investigational q.d. formulation of 2 × 600 mg tablets; q.d. RAL) was found to be generally well tolerated and non-inferior to th...

journal_title：Biopharmaceutics & drug disposition

authors： Krishna R,East L,Larson P,Valiathan C,Deschamps K,Luk JA,Bethel-Brown C,Manthos H,Brejda J,Gartner M

更新日期：2016-12-01 00:00:00

abstract：:The pharmacokinetics of 3-(decyldimethylsilyl)-N-[2-(4-methylphenyl)-1-phenylethyl]propanamide (DMPP), an inhibitor of acyl-CoA:cholesterol acyltransferase, have been studied in the dog and the rat using 14C and 3H dual-labelled drug. In both species, gastrointestinal absorption of DMPP was slow and incomplete, amount...

journal_title：Biopharmaceutics & drug disposition

authors： Tse FL,Jaffe JM

更新日期：1987-09-01 00:00:00

abstract：:An equation based on the absorption potential concept was developed. This enabled us to establish an approach for the quantitative prediction of the fraction of dose absorbed. Classification of drugs into three broad categories, according to their absorption potential values in relation to the fraction of dose absorbe...

journal_title：Biopharmaceutics & drug disposition

authors： Macheras PE,Symillides MY

更新日期：1989-01-01 00:00:00

abstract：:Two studies are reported that assess the bioequivalence of a new half-strength drug combination containing 25 mg hydrochlorothiazide and 37.5 mg triamterene compared to a full-strength formulation containing 50 mg hydrochlorothiazide and 75 mg triamterene. The first study (I) compared the absorption and disposition of...

journal_title：Biopharmaceutics & drug disposition

authors： Williams RL,Lin ET,Liang-Gee W,Blume CD,Benet LZ

更新日期：1990-04-01 00:00:00

abstract：:'Casodex' (bicalutamide) is an orally active, non-steroidal, pure antiandrogen; it is a racemate with antiandrogenic activity residing predominantly in the (R)-enantiomer. Healthy male volunteers (n = 15) were administered single oral doses of bicalutamide (50 mg) after food and after fasting as part of a three-treatm...

journal_title：Biopharmaceutics & drug disposition

authors： Cockshott ID,Oliver SD,Young JJ,Cooper KJ,DC Jones

更新日期：1997-08-01 00:00:00

abstract：:The citrus flavonoid hesperetin (4'-methoxy-3',5,7-trihydroxyflavanone) is the aglycone of hesperidin, the major flavonoid present in sweet oranges. Hesperetin 7-O-glucuronide (H7G) and hesperetin 3'-O-glucuronide (H3'G) are the two most abundant metabolites of hesperetin in vivo. In this study, their interaction with...

journal_title：Biopharmaceutics & drug disposition

authors： Brand W,Oosterhuis B,Krajcsi P,Barron D,Dionisi F,van Bladeren PJ,Rietjens IM,Williamson G

更新日期：2011-12-01 00:00:00

abstract：:The inhibition of rat hepatic mitochondrial aldehyde dehydrogenase (ALDH) isozymes was studied in apparent steady-state conditions after repeated intra-peritoneal cyanamide administration. The low-Km mitochondrial ALDH isozyme was more susceptible to cyanamide-induced inhibition (DI50 = 0.104 mg kg-1) than the high-Km...

journal_title：Biopharmaceutics & drug disposition

authors： Pruñonosa Piera J,Obach R,Sagristá ML,Bozal J

更新日期：1993-07-01 00:00:00

abstract：:The enantioselective pharmacokinetics of a new anxiolytic, pazinaclone (DN-2327), and its active metabolite, M-II, were studied in animals. In rats and dogs given racemic pazinaclone intravenously, the total clearance and volume of distribution of (S)-pazinaclone were lower than those of (R)-pazinaclone, whereas the o...

journal_title：Biopharmaceutics & drug disposition

authors： Kondo T,Yoshida K,Yoshimura Y,Tanayama S

更新日期：1995-12-01 00:00:00