The pharmacokinetics of ethosuximide enantiomers in the rat.

abstract：:We synthesized 14C-warfarin hexadecyl ether (14C-WHE) by addition of a palmityl moiety to the hydroxyl group at the 4-position of 14C-warfarin, a compound known to bind to serum albumin. 14C-WHE preferentially bound to the lipoproteins, low-density lipoprotein (LDL) and high-density lipoprotein (HDL), in mouse plasma ...

journal_title：Biopharmaceutics & drug disposition

authors： Tokui T,Kuroiwa C,Muramatsu S,Tokui Y,Sasagawa K,Ikeda T,Komai T

更新日期：1995-03-01 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 utility of pyrazinamide (PZA) in the short-course antituberculous treatment is well established. All available data support the idea that the PZA metabolite pyrazinoic acid (PA) is the active compound against M. tuberculosis. This situation warranted a deeper investigation of possible interactions with respect to ...

journal_title：Biopharmaceutics & drug disposition

authors： Mehmedagic A,Verite P,Menager S,Tharasse C,Chabenat C,Andre D,Lafont O

更新日期：2002-07-01 00:00:00

abstract：:We report here the effect of histamine on amylase secretion in isolated lobules from the rat pancreas. Different concentrations of histamine increased amylase secretion, while the stimulatory effect was reduced by cimetidine although not by chlorpheniramine. These findings suggest that pancreatic lobules have H2 recep...

journal_title：Biopharmaceutics & drug disposition

authors： Jiménez Murillo L,Torre-Cisneros J,Blanco-Molina A,López-Miranda J,Fernández de la Puebla RA,Pérez-Jiménez F

更新日期：1992-07-01 00:00:00

abstract：:Many marketed drugs are chiral and are administered as the racemate, a 50:50 combination of two enantiomers. Pharmacodynamic and pharmacokinetic differences between enantiomers are well documented. Because of enantioselectivity in pharmacokinetics, results of in vitro pharmacodynamic studies involving enantiomers may ...

journal_title：Biopharmaceutics & drug disposition

authors： Brocks DR

更新日期：2006-11-01 00:00:00

abstract：:The objective of this study was to assess the effect of food on the pharmacokinetics of nefazodone (NEF). A group of 24 healthy adult male volunteers received a single 200 mg dose of NEF under fasting conditions as well as 5 min after a high-fat breakfast. There was a 1 week washout between treatments. Serial blood sa...

journal_title：Biopharmaceutics & drug disposition

authors： Dockens RC,Greene DS,Barbhaiya RH

更新日期：1996-03-01 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 plasma protein binding of celecoxib was determined for animals and humans using in vitro and ex vivo methods. Eight, healthy, human volunteers (three male, five female, 20-39 years) received celecoxib (600 mg) BID for 7 days, blood samples were collected and concentrations of bound and unbound celecoxib determined...

journal_title：Biopharmaceutics & drug disposition

authors： Paulson SK,Kaprak TA,Gresk CJ,Fast DM,Baratta MT,Burton EG,Breau AP,Karim A

更新日期：1999-09-01 00:00:00

abstract：:The systemic availability of a solid dispersion (coevaporate) of clofazimine (CLF) in poly(vinyl methyl ether maleic anhydride) copolymer (PVM/MA) was tested in the pig. Single 100 mg oral doses of the coevaporate and the commercial product, Lamprene (Ciba-Geigy) were administered on separate occasions (separated by a...

journal_title：Biopharmaceutics & drug disposition

authors： Krishnan TR,Abraham I

更新日期：1994-05-01 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：BACKGROUND:Mycophenolic acid (MPA) is used widely to prevent graft rejection in kidney-transplant patients. Therapeutic drug monitoring (TDM) in plasma requires an invasive procedure that is inconvenient, especially in pediatric patients. TDM in saliva is a more convenient non-invasive alternative compared with plasma....

journal_title：Biopharmaceutics & drug disposition

authors： Alsmadi MM,Alfarah MQ,Albderat J,Alsalaita G,AlMardini R,Hamadi S,Al-Ghazawi A,Abu-Duhair O,Idkaidek N

更新日期：2019-11-01 00:00:00

abstract：:The pharmacokinetics of the cardioselective beta-adrenoreceptor blocking agent atenolol have been determined following intravenous and oral dosing to the dog. After intravenous administration at 200 mg the blood levels of parent drug were found to decay tri-exponentially with a final elimination phase half-life of abo...

journal_title：Biopharmaceutics & drug disposition

authors： McAinsh J,Holmes BF

更新日期：1983-07-01 00:00:00

abstract：:The comparative bioavailability and steady state fluctuations resulting from the administration of Tegretol 200 mg commercial tablets and carbamazepine OROS controlled delivery tablets were investigated in 22 adult and 12 pediatric epileptic patients. Tegretol commercial tablets were dosed according to previously esta...

journal_title：Biopharmaceutics & drug disposition

authors： Thakker KM,Mangat S,Garnett WR,Levy RH,Kochak GM

更新日期：1992-11-01 00:00:00

abstract：:The pharmacokinetics of mexiletine and its metabolite hydroxy-methyl-mexiletine have been investigated following single-dose and during multiple-dose administration of a sustained-release form of mexiletine to six post-myocardial infarct patients. Comparison of single-dose and washout pharmacokinetics, after short-ter...

journal_title：Biopharmaceutics & drug disposition

authors： Bruno R,Santoni Y,Iliadis A,Djiane P,Serradimigni A,Cano JP

更新日期：1992-10-01 00:00:00

abstract：:Zopiclone is a new sedative showing a rapid onset of hypnotic effect and a relatively short duration of action. The goal of this study was to assess the kinetic parameters of zopiclone and its interaction with trimipramine when administered concomitantly. Ten normal subjects each received doses of zopiclone (7.5 mg), ...

journal_title：Biopharmaceutics & drug disposition

authors： Caille G,du Souich P,Spenard J,Lacasse Y,Vezina M

更新日期：1984-04-01 00:00:00

abstract：:In order to evaluate the influence of food and time of administration on the absorption of diethylamine chromocarbe, a bioavailability study was performed in 8 volunteers by using a new method of plasmatic drug evaluation. The results obtained indicate that lunch has little effect on diethylamine chromocarbe absorptio...

journal_title：Biopharmaceutics & drug disposition

authors： Aiache JM,Faurie M,Sibaud Y,Kaftelip JP,Aiache S

更新日期：1986-05-01 00:00:00

abstract：:Cardizem SR and Bi-Tildiem were both approved in their respective countries on the basis of clinical trials demonstrating efficacy and safety in the treatment of angina pectoris. In this cross-over randomized study, we assessed whether these two sustained-release formulations of diltiazem have equivalent pharmacokinet...

journal_title：Biopharmaceutics & drug disposition

authors： Guimont S,Landriault H,Klischer K,Grace M,Lambert C,Caillé G,Gossard D,Russell A,Raymond M,Hutchings E

更新日期：1993-12-01 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：:In a double-blind, placebo-controlled, single-dose ascending pharmacokinetics and tolerance study, we evaluated the bispyridinium oxime HI-6 dichloride monohydrate (62.5, 125, 250, and 500 mg), administered intramuscularly with atropine sulphate, 2 mg, in 24 healthy male volunteers. The plasma HI-6 peak concentration ...

journal_title：Biopharmaceutics & drug disposition

authors： Clement JG,Bailey DG,Madill HD,Tran LT,Spence JD

更新日期：1995-07-01 00:00:00

abstract：:Reducing the maximum plasma concentration whilst maintaining the exposure was shown to ameliorate adverse events following the oral administration of 6-hydroxybuspirone. This observation, along with a desire to provide for once daily dosing of this compound, provided the basis for the development of an extended releas...

journal_title：Biopharmaceutics & drug disposition

authors： Nicholson SJ,Timmins P,Dockens RC,Connor A,Croop R,Ferrie P,Zeng J,Dennis AB,Wilding I

更新日期：2012-12-01 00:00:00

abstract：:Prednisolone (POH) and prednisone (PO) were both administered via seven different intravenous infusions (three POH and four PO) in each of six rabbits to obtain steady state. Bolus doses of POH and PO were also administered to four of the rabbits. Plasma samples of POH and PO were analyzed by normal phase HPLC. Unboun...

journal_title：Biopharmaceutics & drug disposition

authors： Hammarlund-Udenaes M,Benet LZ

更新日期：1991-08-01 00:00:00

abstract：:Glucocorticoids have diverse effects on various components of the immune system and assessment of such activities in vivo often involves complex techniques and numerous animals. We developed a whole blood technique for determining proliferation rate of lymphocytes in minute amounts of rat blood (5 microL as opposed to...

journal_title：Biopharmaceutics & drug disposition

authors： Fasanmade AA,Jusko WJ

更新日期：1999-07-01 00:00:00

abstract：:Niosomes (non-ionic surfactant vesicles) prepared from C16G2 (a hexadecyl-diglycerol ether), and loaded with doxorubicin, were administered intraperitoneally to male AKR mice at dose levels of 0, 2.5, 5.0, and 10.0 mg kg-1. Free drug was given at 10.0 mg kg-1 by the intraperitoneal route. At a dose level of 10.0 mg kg...

journal_title：Biopharmaceutics & drug disposition

authors： Uchegbu IF,Turton JA,Double JA,Florence AT

更新日期：1994-11-01 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：:Twenty-four healthy volunteers, aged 21-59 years, received single 30 mg oral doses of the benzodiazepine hypnotic temazepam. Levels of intact temazepam were determined in multiple plasma samples drawn during 48 h after dosage. Intact temazepam, its direct glucuronide conjugate, and the conjugate of its demethylated (o...

journal_title：Biopharmaceutics & drug disposition

authors： Locniskar A,Greenblatt DJ

更新日期：1990-08-01 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 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：: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：: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：: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