Prediction of absolute bioavailability for drugs using oral and renal clearance following a single oral dose: a critical view.

abstract：:The intestinal absorptive characteristics and the efflux mechanisms of candesartan (CDS), a novel angiotensin II type 1 receptor blocker, were investigated. The Caco-2 cells were used as models of the intestinal mucosa to assess uptake and transport of CDS. The determination of CDS was performed by HPLC-Flu. In the Ca...

journal_title：Biopharmaceutics & drug disposition

authors： Zhou L,Chen X,Gu Y,Liang J

更新日期：2009-07-01 00:00:00

abstract：:Few studies describe the administration of Taxol to rats; however, rats are typically used to study the toxicity of new drugs or novel formulations. A dose finding study was conducted to determine a safe dose of Taxol following intravenous administration in rats. Male Sprague-Dawley rats received a bolus of paclitaxel...

journal_title：Biopharmaceutics & drug disposition

authors： Shord SS,Camp JR

更新日期：2006-05-01 00:00:00

abstract：:In this comparative bioavailability study two sustained release capsule formulations of propranolol, one a clinical trial formulation and the other the U.K. sales formulation ('Inderal' LA), were compared with a conventional 'Inderal' tablet. Twelve healthy adult male volunteers received, on cross-over basis, on three...

journal_title：Biopharmaceutics & drug disposition

authors： McAinsh J,Baber NS,Holmes BF,Young J,Ellis SH

更新日期：1981-01-01 00:00:00

abstract：:This study assessed steady-state azimilide pharmacokinetics and pharmacodynamics in 119 healthy male and female volunteers. Parallel groups of 18-40-year-old subjects received doses of 35, 100, 150 or 200 mg day(-1) for up to 14 days, with 1, 2 or 3 days of loading. Another group of > 55-year-old subjects received 100...

journal_title：Biopharmaceutics & drug disposition

authors： Corey A,Al-Khalidi H,Brezovic C,Marcello S,Parekh N,Taylor K,Karam R

更新日期：1999-03-01 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 pharmacokinetics and pharmacodynamics of furosemide were compared after an oral administration or a direct administration of Lasix into the duodenum in humans (40 mg). Furosemide was absorbed quickly after a direct administration of Lasix into the duodenum; the peak plasma concentration of furosemide was reached w...

journal_title：Biopharmaceutics & drug disposition

authors： Lee WI,Yoon WH,Shin WG,Song IS,Lee MG

更新日期：1997-12-01 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 aim of this investigation was to assess the pharmacokinetic properties of high-dose menadione (VK3), as an anticancer agent, in plasma and red blood cells (RBCs) in rabbits. An extremely high dose of 75 mg menadiol sodium diphosphate (Synkayvite) was intravenously injected. HPLC analysis was applied to measure the...

journal_title：Biopharmaceutics & drug disposition

authors： Hu OY,Wu CY,Chan WK,Wu FY,Whang-Peng J

更新日期：1996-08-01 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：:Guanfacine is used for the treatment of attention-deficit/hyperactivity disorder (ADHD). Using liquid chromatography-tandem mass spectrometry (LC-MS/MS), metabolite profiling of guanfacine was performed in plasma and urine collected from healthy Japanese adults following repeated oral administration of guanfacine exte...

journal_title：Biopharmaceutics & drug disposition

authors： Inoue Y,Morita H,Nozawa K,Kanazu T

更新日期：2019-09-01 00:00:00

abstract：:Stobadin dihydrochloride was administered p.o. to rats at a dose of 1 mg kg-1 once daily for 25 consecutive days. The peak and trough concentrations of the sum of stobadin metabolites, determined from Days 6-16 of treatment, demonstrated a steady-state. The mean daily excretion of 3H-radioactivity during this period w...

journal_title：Biopharmaceutics & drug disposition

authors： Kállay Z,Soltés L,Trnovec T

更新日期：1991-04-01 00:00:00

abstract：AIM:The aim of this study was to build and verify a preliminary physiologically based pharmacokinetic (PBPK) model of Chinese pregnant women. The model was used to predict maternal pharmacokinetics (PK) of 6 predominantly renally cleared drugs. METHOD:Based on SimCYP Caucasian pregnancy population dataset, the prelimi...

journal_title：Biopharmaceutics & drug disposition

authors： Song L,Yu Z,Xu Y,Li X,Liu X,Liu D,Zhou T

更新日期：2020-06-01 00:00:00

abstract：:The pharmacokinetics of a non-narcotic analgesic, DA-5018, were compared after single intravenous (i.v.), subcutaneous (s.c.), and oral administrations, and after multiple (seven consecutive days) s.c. administration to rats. After i.v. administration of DA-5018, 1, 2, and 5 mg kg-1, the pharmacokinetic parameters of ...

journal_title：Biopharmaceutics & drug disposition

authors： Lee JJ,Shim HJ,Kim SH,Lee SD,Kim WB,Yang J,Lee MG

更新日期：1998-03-01 00:00:00

abstract：:The oral pharmacokinetics (concentration-time profile) of four proprietary compounds in humans were predicted using the C(vss)-MRT method. The first step was to demonstrate superposition of intravenous (i.v.) pharmacokinetic profiles of preclinical species following mathematical transformation of their respective conc...

journal_title：Biopharmaceutics & drug disposition

authors： Fura A,Vyas V,Humphreys W,Chimalokonda A,Rodrigues D

更新日期：2008-11-01 00:00:00

abstract：:Acyl glucuronidation is the major metabolic conjugation reaction of most carboxylic acid drugs in mammals. The physiological consequences of this biotransformation have been investigated incompletely but include effects on drug metabolism, protein binding, distribution and clearance that impact upon pharmacological an...

journal_title：Biopharmaceutics & drug disposition

authors： Regan SL,Maggs JL,Hammond TG,Lambert C,Williams DP,Park BK

更新日期：2010-10-01 00:00:00

abstract：:The objective was to develop a population pharmacokinetic-pharmacodynamic model of caffeine's psychomotor effects in healthy, non-habitual users of caffeine. Twenty Chinese males each received a single dose of 250 mg of caffeine orally. Plasma concentrations of caffeine were determined at various times within 24 h aft...

journal_title：Biopharmaceutics & drug disposition

authors： Seng KY,Teo WL,Fun CY,Law YL,Lim CL

更新日期：2010-07-01 00:00:00

abstract：:A physiologic model to describe bupivacaine uptake by and elimination from brain and heart was developed. Preliminary validation of the model was accomplished by comparing concentration data predicted by the model with those determined in rabbits. The model was modified to examine similarities and differences followin...

journal_title：Biopharmaceutics & drug disposition

authors： Denson DD,Thompson GA,Coyle DE

更新日期：1986-03-01 00:00:00

abstract：:A new sustained release dosage form of valproic acid (VPA) was developed. The new sustained release dosage form was administered (twice, with and without food) to five dogs in comparison to a standard tablet (Depakine, Labaz) and an i.v. preparation of the drug. Drug level monitoring in the plasma was performed by a G...

journal_title：Biopharmaceutics & drug disposition

authors： Bialer M,Friedman M,Dubrovsky J

更新日期：1984-01-01 00:00:00

abstract：:The study sought to investigate the effect of genetic variants of OCT1 (OCT1-P283L and -P341L) and OCT2 (OCT2-T199I, -T201M and -A270S), which were identified in a Korean population, on the transport of lamivudine in vitro and to compare the substrate dependent effects of OCT1 and OCT2 variants with 1-methyl-4-phenylp...

journal_title：Biopharmaceutics & drug disposition

authors： Choi MK,Song IS

更新日期：2012-04-01 00:00:00

abstract：:A semisolid self-emulsifying system (SES) of itraconazole consisting of oleic acid, polysorbate 80 and coajuvant (citric acid) was prepared by a hot-melt technique and then compared with hydroxypropylmethylcellulose (HPMC) solid dispersion (SD) coated onto inert sugar spheres as a reference formulation for in vitro an...

journal_title：Biopharmaceutics & drug disposition

authors： Park MJ,Ren S,Lee BJ

更新日期：2007-05-01 00:00:00

abstract：PURPOSE:The sonodynamically induced anti-tumor effect of chlorin-e6 (Ce6) was studied in mice bearing hepatoma-22 solid tumors. METHODS:In order to determine the optimum timing of ultrasound exposure after administration of Ce6, the Ce6 concentrations in plasma, skin, muscle and tumor were estimated by measuring the f...

journal_title：Biopharmaceutics & drug disposition

authors： Shi H,Liu Q,Qin X,Wang P,Wang X

更新日期：2011-09-01 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：:A three-way crossover study in 18 healthy male volunteers was conducted to evaluate the bioequivalence of three different 200 mg anhydrous theophylline immediate-release (IR) capsules. The products had not been rated as therapeutically equivalent by the US Food and Drug Administration (FDA) owing to a lack of bioequiv...

journal_title：Biopharmaceutics & drug disposition

authors： Meyer MC,Jarvi EJ,Straughn AB,Pelsor FR,Williams RL,Shah VP

更新日期：1999-12-01 00:00:00

abstract：:Biliary clearance (Clb) of sotalol (STL) enantiomers was assessed in anaesthetized Sprague-Dawley rats (419 +/- 9 g, mean +/- SEM, n = 4) following administration of a 10 mg kg-1 i.v. dose of the racemate. Clb for S- and R-STL (0.0675 +/- 0.0090 and 0.0662 +/- 0.0089 mL min-1 kg-1, respectively) represented approximat...

journal_title：Biopharmaceutics & drug disposition

authors： Carr RA,Pasutto FM,Foster RT

更新日期：1996-11-01 00:00:00

abstract：:A high-performance liquid chromatographic method was developed to determine stobadin pharmacokinetics in dog and man. The relative bioavailability of stobadin dipalmitate compared with dihydrochloride was 46.4 per cent in dog. In man peak serum concentrations ranged from 12 to 289 ng ml-1 after a single oral dose of s...

journal_title：Biopharmaceutics & drug disposition

authors： Soltés L,Kállay Z,Bezek S,Fedelesová V

更新日期：1991-01-01 00:00:00

abstract：:The pharmacokinetics of methylprednisolone and methylprednisolone phosphate were investigated after intravenous administration of methylprednisolone phosphate to six healthy subjects at seven different doses between 16 and 1000 mg. Plasma, urine, and saliva were analyzed for methylprednisolone and methylprednisolone p...

journal_title：Biopharmaceutics & drug disposition

authors： Möllmann H,Rohdewald P,Barth J,Verho M,Derendorf H

更新日期：1989-09-01 00:00:00

abstract：:The influence of caffeine (60 mg) was studied on the pharmacokinetic characteristics of acetaminophen (500 mg single dose) in ten healthy male human volunteers in a complete cross-over design. A high-performance liquid chromatography (HPLC) method was used to analyse serum drug concentrations. Caffeine caused a highly...

journal_title：Biopharmaceutics & drug disposition

authors： Iqbal N,Ahmad B,Janbaz KH,Gilani AU,Niazi SK

更新日期：1995-08-01 00:00:00

abstract：:Mivacurium, a non-depolarizing neuromuscular blocking agent, consists of three isomers; trans-trans (57%), cis-trans (36%) and cis-cis (7%). The purpose of this study was to characterize the pharmacokinetics and pharmacodynamics of mivacurium after various inputs. Four beagle dogs weighing between 7.95 and 9.89 kg wer...

journal_title：Biopharmaceutics & drug disposition

authors： Lugo SI,Liang Z,Eddington ND

更新日期：1998-11-01 00:00:00

abstract：:Although nifedipine has been characterized in terms of its general vasodilatory effects, this dihydropyridine must still be regarded as investigational with regard to available pharmacokinetic and pharmacodynamic data. Although limited studies are available, it is clear that the pharmacokinetic and pharmacodynamic dat...

journal_title：Biopharmaceutics & drug disposition

authors： Hamann SR,Piascik MT,McAllister RG Jr

更新日期：1986-01-01 00:00:00

abstract：:The absorption characteristics of ethiofos were studied using the rat in situ intestine circulating perfusion technique. Slow absorption kinetics were observed for ethiofos with varying rates of absorption and metabolism/degradation in situ as a function of buffer and absorption enhancers. In most cases less than 10 p...

journal_title：Biopharmaceutics & drug disposition

authors： Geary RS,Swynnerton NF,Timmons SF,Mangold DJ

更新日期：1991-05-01 00:00:00