Intravenous verapamil kinetics in rats: marked arteriovenous concentration difference and comparison with humans.

abstract：:The pharmacokinetic behavior of glycyrrhizin in four patients with acute hepatitis (hepatitis group) and six patients with liver cirrhosis (cirrhosis group) receiving chronically an IV administration of a 120 mg dose once a day or once every other day of glycyrrhizin was investigated. The plasma concentration of glycy...

journal_title：Biopharmaceutics & drug disposition

authors： Yamamura Y,Tanaka N,Santa T,Kotaki H,Aikawa T,Uchino K,Osuga T,Sawada Y,Iga T

更新日期：1995-01-01 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：: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：:The pharmacokinetics and the dose proportionality of a new anticonvulsant compound, HEPP (D,L-3-hydroxy-3-ethyl-3-phenylpropionamide) was studied in healthy male volunteers as part of the pharmacological evaluation for new drugs. Study was performed administering doses of 250, 375, 500 and 625 mg of HEPP to six male v...

journal_title：Biopharmaceutics & drug disposition

authors： González-Esquivel DF,Rubio-Donnadieu F,Carvajal-Sandoval G,Jung HC

更新日期：1998-12-01 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：: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：:The effect of the combination of a new anticonvulsant drug HEPP and carbamazepine (CBZ) on the pharmacokinetics of HEPP and CBZ was investigated using rabbits as an animal model. The study was performed in 18 male New Zealand white rabbits which were randomly divided into three groups, according to a balanced incomple...

journal_title：Biopharmaceutics & drug disposition

authors： García AL,Medina RL,Pérez MR,Jung CH

更新日期：2003-07-01 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：: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：: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：:This review offers a detailed discussion of the interaction between pharmaceutical compounds and vehicles using the affinity capillary electrophoresis and the microemulsion electrokinetic chromatography. Partition coefficients of drugs were calculated between a micelle and an aqueous phases from the measurement of the...

journal_title：Biopharmaceutics & drug disposition

authors： Reinhard N,Mrestani Y

更新日期：2001-10-01 00:00:00

abstract：:Ritalin, an immediate release form of racemic methylphenidate hydrochloride, has been available in the USA since 1955 and is used for the treatment of ADHD. The objective of this study was to evaluate the pharmacokinetics of modified-release methylphenidate (highest single dose), Ritalin LA, when administered under fa...

journal_title：Biopharmaceutics & drug disposition

authors： Lee L,Kepple J,Wang Y,Freestone S,Bakhtiar R,Wang Y,Hossain M

更新日期：2003-09-01 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：: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：: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：:The pharmacokinetics of didanosine and ciprofloxacin were evaluated following the administration of multiple oral doses of each drug as a single agent or in combination. Didanosine was dosed as the Videx chewable/dispersible tablet, which contains the antacids dihydroxyaluminum sodium carbonate and magnesium hydroxide...

journal_title：Biopharmaceutics & drug disposition

authors： Knupp CA,Barbhaiya RH

更新日期：1997-01-01 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 purpose of this project was to develop and validate a pharmacokinetic model and to quantify the rate and extent of distribution between plasma and skin of two beta-lactam antibiotics, amoxicillin (AMX) and cefuroxime (CFX), which are frequently administered systemically to treat skin and skin structure infections....

journal_title：Biopharmaceutics & drug disposition

authors： Shukla C,Patel V,Juluru R,Stagni G

更新日期：2009-09-01 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：: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：:A relative bioavailability study of conventional tablet of propranolol hydrochloride was conducted in a group of 18 healthy volunteers employing the innovator's product as the reference tablet formation. Based on plasma levels of propranolol for the 24 h following administration of 2 x 40 mg oral propranolol hydrochlo...

journal_title：Biopharmaceutics & drug disposition

authors： Roscoe R,Cooper J,Wilson TW,Joshi NN,Midha KK

更新日期：1982-04-01 00:00:00

abstract：:Effects of concomitant colestipol administration on plasma concentrations of diltiazem and desacetyldiltiazem from immediate-release (IR) and sustained-release (SR) formulations were assessed in two studies. In the first study, 12 subjects received 120-mg diltiazem hydrochloride (diltiazem) SR capsules or 120-mg dilti...

journal_title：Biopharmaceutics & drug disposition

authors： Turner SW,Jungbluth GL,Knuth DW

更新日期：2002-12-01 00:00:00

abstract：:In this study, a quantitative threshold was determined for the high/low extent of urinary excretion (UE) of compounds in humans, using a straightforward but robust statistical method known as receiver operating characteristic curve (ROC) analysis, and also 18 potential physicochemical determinants of UE were evaluated...

journal_title：Biopharmaceutics & drug disposition

authors： Dave RA,Morris ME

更新日期：2016-07-01 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：:Pharmacokinetics in rabbits following intravenous administration and in vitro protein binding were studied for two new salts of erythromycin (erythromycin maltobionate and erythromycin fumarate). Serum erythromycin levels following intravenous injection were described by two compartment model kinetics, and values for ...

journal_title：Biopharmaceutics & drug disposition

authors： Basu SK,Manna PK,Goswami BB

更新日期：1992-08-01 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：:In situ intestinal absorption of baclofen in the rat in the presence of beta-alanine has been investigated. Through the perfusion of 0.50 mM baclofen solutions containing variable concentrations of the aminoacid (from 5 to 100 mM), a partially competitive inhibition of baclofen absorption was characterized: absorption...

journal_title：Biopharmaceutics & drug disposition

authors： Polache A,Plá-Delfina JM,Merino M

更新日期：1991-12-01 00:00:00

abstract：:The mechanism of intestinal transport of valacyclovir (VACV), the L-valyl ester prodrug of acyclovir, was investigated in rats using an in situ intestinal perfusion technique. VACV demonstrates an oral bioavailability that is three to five time greater than acyclovir, concentration dependent, and saturable in humans. ...

journal_title：Biopharmaceutics & drug disposition

authors： Sinko PJ,Balimane PV

更新日期：1998-05-01 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：:A method for calculating the mean residence times of metabolites in the body, systemic circulation, and peripheral tissue is described. The calculations require the AUC, AUMC, and derivatives of the plasma concentration versus time curves of the metabolite and its precursor. The method is applicable to metabolites wit...

journal_title：Biopharmaceutics & drug disposition

authors： Cheng HY

更新日期：1991-07-01 00:00:00