The relative bioavailability of two marketed controlled release diltiazem dosage forms at steady state in healthy volunteers.

abstract：:Vitamin K antagonists (VKAs) remain the oral anticoagulant of choice in venous thromboembolic disease. These drugs are characterized by a large inter-individual variability requiring frequent dose tailoring. Genetic polymorphisms for cytochrome CYP2C9 and VKORC1 explain some of the variability, especially in warfarin ...

journal_title：Biopharmaceutics & drug disposition

authors： Espana B,Couturier S,Prouillac C

更新日期：2017-01-01 00:00:00

abstract：:Twenty-six healthy male volunteers received a single 10 mg dose of diazepam on two occasions in a crossover bioequivalence study comparing the reference product (Valium) and a generic formulation (NeoCalme). Concentrations of diazepam and its metabolite, desmethyldiazepam, were determined during 264h after each dose. ...

journal_title：Biopharmaceutics & drug disposition

authors： Locniskar A,Greenblatt DJ,Harmatz JS,Shader RI

更新日期：1989-11-01 00:00:00

abstract：:The bioavailability of orally administered therapies are often significantly limited in the human intestine by the metabolic activities of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp). Predicting whether candidate compounds induce CYP3A4 and P-gp is a crucial stage in the drug development process, as drug-dr...

journal_title：Biopharmaceutics & drug disposition

authors： Inami K,Sasaki T,Kumagai T,Nagata K

更新日期：2015-04-01 00:00:00

abstract：:Macelignan is a natural phenolic compound that possesses many types of health benefits such as antiinflammation. This study aimed to characterize the metabolism of macelignan via the glucuronidation pathway and to identify the main UGT enzymes involved in macelignan glucuronidation. The rates of glucuronidation were d...

journal_title：Biopharmaceutics & drug disposition

authors： Liu H,Wu Z,Ma Z,Wu B

更新日期：2014-12-01 00:00:00

abstract：:The purpose of this mechanistic drug interaction study was to investigate the effects of ketoconazole on the pharmacokinetics of safinamide. Ketoconazole was applied as a potent prototypic inhibitor of cytochrome CYP3A4, to determine the role of CYP3A4 in the metabolic clearance of safinamide. In an open-label, random...

journal_title：Biopharmaceutics & drug disposition

authors： Krösser S,Marquet A,Gallemann D,Wolna P,Fauchoux N,Hermann R,Johne A

更新日期：2012-12-01 00:00:00

abstract：:The hypothesis that higher molecular weight (MW) quaternary ammoniums (QAs) form lipophilic ion-pair complexes with bile salts in the liver, and are subsequently excreted into bile via a canalicular transporter, P-gp, was re-examined in the present study for its validity. The biliary excretion of tributylmethyl ammoni...

journal_title：Biopharmaceutics & drug disposition

authors： Choi MK,Song IS,Kim DD,Chung SJ,Shim CK

更新日期：2007-12-01 00:00:00

abstract：:Several research groups have reported that in man the oral administration of propranolol with food leads to a marked increase (about 50 per cent) in the area under the plasma concentration-time curve (AUCpo) of this well absorbed and highly metabolized drug. An acute change in hepatic metabolic enzyme activity has bee...

journal_title：Biopharmaceutics & drug disposition

authors： Chow HH,Lalka D

更新日期：1993-04-01 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：:Four experimental controlled-release oral solid dosage formulations were developed and the in vitro dissolution characteristics of theophylline from these formulations were studied in USP apparatus I. Pharmacokinetic evaluation of these formulations was carried out in eight beagle dogs under fasting conditions. Theoph...

journal_title：Biopharmaceutics & drug disposition

authors： Yu Z,Schwartz JB,Sugita ET

更新日期：1996-04-01 00:00:00

abstract：:Affecting the absorption of active ingredients in the intestine serves as one of the important compatibility mechanisms of traditional Chinese medicine. The aim of this study was to investigate the compatibility mechanism of ShengDiHuang Decoction (SDHD) by using the single-pass intestinal perfusion in situ model. The...

journal_title：Biopharmaceutics & drug disposition

authors： Yang H,Hao Q,Cheng J,Wang M,Zou J,Zhang X,Guo D

更新日期：2020-02-01 00:00:00

abstract：:Non-steroidal anti-inflammatory drugs (NSAIDs) are used widely to relieve pain and to decrease inflammation. Several clinical studies have reported that NSAIDs inhibit uridine 5'-diphospho-glucuronosyltransferase (UGT) enzymes. Therefore, the study evaluated the inhibitory potential of 15 NSAIDs on the activities of s...

journal_title：Biopharmaceutics & drug disposition

authors： Joo J,Kim YW,Wu Z,Shin JH,Lee B,Shon JC,Lee EY,Phuc NM,Liu KH

更新日期：2015-05-01 00:00:00

abstract：:Previous studies have shown that 1α,25-dihydroxyvitamin D3 (1,25(OH)2D3) treatment (2.56 nmol/kg i.p. daily×4) increased PepT1, Mrp2, Mrp4, Asbt, but not Mdr1/P-gp in the rat small intestine. In this study, the intestinal everted sac technique, together with various select probes: mannitol (paracellular transport), gl...

journal_title：Biopharmaceutics & drug disposition

authors： Maeng HJ,Durk MR,Chow EC,Ghoneim R,Pang KS

更新日期：2011-03-01 00:00:00

abstract：:Bevirimat is the first drug in the class of maturation inhibitors, which treat HIV infection by disrupting the activity of HIV protease enzyme with a mechanism of action distinct from that of conventional protease inhibitors. The absorption, distribution, metabolism and elimination characteristics of single intravenou...

journal_title：Biopharmaceutics & drug disposition

authors： Bullock P,Larsen D,Press R,Wehrman T,Martin DE

更新日期：2008-10-01 00:00:00

abstract：:The aim of this study was to determine whether the dose influences the distribution kinetics of ciprofloxacin and ofloxacin in muscle- bone- and skin-tissues included in the isolated hindlimb of the rat. Experiments were carried out in the isolated perfused hindlimb of the rat, administering a single dose of 45, 450 o...

journal_title：Biopharmaceutics & drug disposition

authors： Casquero-Dorado AC,Colino CI,Martínez MS,Sánchez-Navarro A

更新日期：2000-11-01 00:00:00

abstract：:The inhibitory effect of the essential alpha-aminoacid L-leucine on the intestinal absorption of the antispastic drug baclofen was examined by means of an in situ rat gut perfusion technique. When 0.5 mM baclofen solutions were perfused in the presence of increasing concentrations of the aminoacid (5-100 mM), the appa...

journal_title：Biopharmaceutics & drug disposition

authors： Cercós-Fortea T,Polache A,Nácher A,Cejudo-Ferragud E,Casabó VG,Merino M

更新日期：1995-10-01 00:00:00

abstract：:The first day test dose versus steady-state relationship for predicting drug doses was evaluated for the situation where metabolites are produced. An organ clearance model incorporated into a digital computer program simulated drug and metabolite disposition. When the terminal elimination rate for metabolite was simil...

journal_title：Biopharmaceutics & drug disposition

authors： Devane CL,Jusko WJ

更新日期：1983-01-01 00:00:00

abstract：:Methotrexate (MTX) is an anchor drug used to treat rheumatoid arthritis (RA), but responsiveness is variable in effectiveness and toxicity. Methotrexate and its polyglutamate conjugates (MTXPG(n)) in red blood cells (RBC) have been associated with patient response. In the current study, 13 collagen-induced arthritic (...

journal_title：Biopharmaceutics & drug disposition

authors： Liu DY,Lon HK,Wang YL,DuBois DC,Almon RR,Jusko WJ

更新日期：2013-05-01 00:00:00

abstract：:In order to determine the absolute bioavailability, both oral and intravenous administrations of a drug are often used. Recently a new method has been proposed to determine absolute bioavailability in the absence of intravenous dose. Following a single oral dose, this method requires oral and renal clearance data from...

journal_title：Biopharmaceutics & drug disposition

authors： Mahmood I

更新日期：1997-08-01 00:00:00

abstract：:The influence of dose volume on drug absorption following oral administration of a highly and a poorly water soluble drug was examined in male Sprague-Dawley rats. A constant mass of each 14C-labeled compound was given via gavage in dose volumes of 1, 5, 10, and 20 mL kg-1. Blood levels, as well as the quantitative ex...

journal_title：Biopharmaceutics & drug disposition

authors： Nickerson DF,Weaver ML,Tse FL

更新日期：1994-07-01 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：: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：:The pharmacokinetics and pharmacodynamics of furosemide were investigated after intravenous (i.v.), 1 mg/100 g body weight, and oral administration, 2 mg per 100 g body weight, to spontaneously hypertensive rats (SHRs) and deoxycorticosterone acetate-salt-induced hypertensive rats (DOCA-salt rats). After i.v. administ...

journal_title：Biopharmaceutics & drug disposition

authors： Jang SH,Lee MG,Kim ND

更新日期：1994-04-01 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：:Pharmacokinetic studies of riluzole show a large inter-individual variability of the drug's clearance and serum concentrations. Optimizing the individual dosage of riluzole may have the potential to improve the effect of riluzole treatment on survival of patients with amyotrophic lateral sclerosis (ALS). Limited data ...

journal_title：Biopharmaceutics & drug disposition

authors： van Kan HJ,van den Berg LH,Groeneveld GJ,van der Straaten RJ,van Vught PW,Lie-A-Huen L,Guchelaar HJ

更新日期：2008-04-01 00:00:00

abstract：:This study compared the relative ocular bioavailability in rabbits of the antibiotic/steroid combination of 0.3 per cent tobramycin and 0.1 per cent fluorometholone acetate to each of the two single-entity products. Two separate studies were conducted, one measuring fluorometholone acetate in cornea and aqueous humour...

journal_title：Biopharmaceutics & drug disposition

authors： Schoenwald RD,Harris RG,Turner D,Knowles W,Chien DS

更新日期：1987-11-01 00:00:00

abstract：:The plasma levels and tissue penetration of pefloxacin were studied after prophylactic administration to patients undergoing elective biliary surgery. Pefloxacin was administered as a single dose of 800 mg given intravenously as an infusion 1 h before surgery. Over a period of two years, cultures of bile and stone wer...

journal_title：Biopharmaceutics & drug disposition

authors： Gascón AR,Campo E,Olea E,Hernández RM,Calvo B,Errasti J,Pedraz JL

更新日期：2002-10-01 00:00:00

abstract：:The effect of moderate and prolonged exercise on the disposition and metabolism of drugs has not been extensively examined. The present study examined the effect of exercise training on the pharmacokinetics of procainamide and its active metabolite, N-acetylprocainamide. Male Sprague Dawley rats were randomly assigned...

journal_title：Biopharmaceutics & drug disposition

authors： Eddington ND,Adekoya F,Kharidia J

更新日期：1998-07-01 00:00:00

abstract：:The pharmacokinetics of verapamil, a calcium channel blocker, were studied in male Sprague-Dawley rats following i.v. administration at a dose of 1 mg kg-1. Both arterial and venous blood were collected and the plasma drug concentrations were determined by reversed-phase high-performance liquid chromatography. Verapam...

journal_title：Biopharmaceutics & drug disposition

authors： Manitpisitkul P,Chiou WL

更新日期：1993-10-01 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：:Fexofenadine hydrochloride is a non-sedating antihistamine that is used in the treatment of symptoms associated with seasonal allergic rhinitis and chronic idiopathic urticaria. A pooled analysis of pharmacokinetic data from children 6 months to 12 years of age and adults was conducted to identify the dose(s) in child...

journal_title：Biopharmaceutics & drug disposition

authors： Krishna R,Krishnaswami S,Kittner B,Sankoh AJ,Jensen BK

更新日期：2004-12-01 00:00:00