Nonstationary disposition of valproic acid during prolonged intravenous infusion: contributions of unbound clearance and protein binding.

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：:Infliximab (IFX) is used as a therapeutic agent for ulcerative colitis (UC) and Crohn's disease (CD). Although the dosage regimen has been established through clinical trial experience, it has yet to be assessed with a pharmacokinetic and pharmacodynamic model. The present study analysed sequential changes of clinical...

journal_title：Biopharmaceutics & drug disposition

authors： Kimura K,Yoshida A,Katagiri F,Takayanagi R,Yamada Y

更新日期：2019-07-01 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：: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：: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：: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 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：: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：: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 study examined the effect of doxorubicin (DOX) on the hepatic expression of CYP2C and its activity for metabolizing tolbutamide (TB), a specific CYP2C substrate, in rats and whether the pharmacokinetics of tolbutamide were altered by doxorubicin exposure. The expression level of hepatic CYP2C11 was depressed 1 day...

journal_title：Biopharmaceutics & drug disposition

authors： Fukuno S,Nagai K,Yamamoto K,Tanimura T,Nabe T,Konishi H

更新日期：2019-07-01 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 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：: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：: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：: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：:EMA401, (the S-enantiomer of 5-(benzyloxy)-2-(2,2-diphenylacetyl)-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid), also known as Olodanrigan, is an orally active selective angiotensin II type 2 receptor (AT2 R) antagonist that is in Phase IIb clinical development as a novel analgesic for the relief of chro...

journal_title：Biopharmaceutics & drug disposition

authors： Murgasova R,Carreras ET,Suetterlin-Hachmann M,da Silva Torrao LR,Kittelmann M,Alexandra V,Fredenhagen A

更新日期：2020-04-01 00:00:00

abstract：:An evaluation of the literature indicated that certain aspects of the disposition kinetics of iothalamate, important to the accurate determination of glomerular filtration rate in dogs and humans, remain to be resolved. The simultaneous clearances of iothalamate and inulin in 5 dogs were determined at three steady-sta...

journal_title：Biopharmaceutics & drug disposition

authors： Prueksaritanont T,Lui CY,Lee MG,Chiou WL

更新日期：1986-07-01 00:00:00

abstract：:MDL 26479 is a new drug undergoing clinical evaluation for the treatment of depression and for memory loss associated with Alzheimer's disease. As part of a dose tolerance trial, the single- (SD) and multiple-dose (MD) pharmacokinetics of MDL 26479 were evaluated in healthy male volunteers. SDs ranging from 2 to 465 m...

journal_title：Biopharmaceutics & drug disposition

authors： Robbins DK,Hutcheson SJ,Miller TD,Green VI,Bhargava VO,Weir SJ

更新日期：1997-05-01 00:00:00

abstract：:This open-label, two-way crossover study was undertaken to determine whether the enteric formulation of didanosine influences the pharmacokinetics of itraconazole or fluconazole, two agents frequently used to treat fungal infections that occur with HIV infection, and whose bioavailability may be influenced by changes ...

journal_title：Biopharmaceutics & drug disposition

authors： Damle B,Hess H,Kaul S,Knupp C

更新日期：2002-03-01 00:00:00

abstract：AIMS:To study the dose-ranging population pharmacokinetics of controlled release verapamil in healthy subjects and patients with angina or hypertension. To characterize the pharmacodynamics of controlled-release verapamil in patients with hypertension. METHODS:Dose-ranging studies were conducted in healthy volunteers ...

journal_title：Biopharmaceutics & drug disposition

authors： Gupta S,Modi NB,Sathyan G,Ho Pl PL,Aarons L

更新日期：2002-01-01 00:00:00

abstract：:Methotrexate (MTX) is an antifolate agent used in the treatment of numerous types of cancer, and eliminated by active tubular secretion via organic anion transporter 3 (OAT3). Gastric antisecretory drugs, such as proton pump inhibitors (PPIs) and histamine H2 receptor antagonists, are widely used among patients with c...

journal_title：Biopharmaceutics & drug disposition

authors： Narumi K,Sato Y,Kobayashi M,Furugen A,Kasashi K,Yamada T,Teshima T,Iseki K

更新日期：2017-12-01 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：:A major component of physiologically based pharmacokinetic (PBPK) models is the prediction of the rate and extent of absorption of orally dosed drugs for which knowledge of effective passive intestinal permeability (Peff ) is essential. Single-pass intestinal perfusion (SPIP) studies are used to establish effective pe...

journal_title：Biopharmaceutics & drug disposition

authors： Pade D,Jamei M,Rostami-Hodjegan A,Turner DB

更新日期：2017-03-01 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：:The tumour uptake as well as the anti-tumour activity of RS-1541 (palmitoyl rhizoxin), a potent antineoplastic agent, were investigated in mice bearing M5076 sarcoma. After intravenous administration, 14C-RS-1541 preferentially bound to the lipoproteins, to which 14C-rhizoxin did not bind. 14C-RS-1541 showed persistin...

journal_title：Biopharmaceutics & drug disposition

authors： Tokui T,Kuroiwa C,Tokui Y,Sasagawa K,Kawai K,Kobayashi T,Ikeda T,Komai T

更新日期：1994-03-01 00:00:00

abstract：:Remogliflozin etabonate (RE) is the prodrug of remogliflozin (R), an inhibitor of renal glucose transport designed to reduce blood glucose concentrations for the treatment of type 2 diabetes. This open-label, randomized, single-dose, four-way crossover study, (with one add-on arm) in eight healthy men evaluated the re...

journal_title：Biopharmaceutics & drug disposition

authors： O'Connor-Semmes RL,Sandefer EP,Hussey EK,Tao W,Doll WJ,Page RC,Dobbins R

更新日期：2013-03-01 00:00:00

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：: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：: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 urinary elimination of 4-hydroxyamphetamine (PHA) and a series of homologous 4-alkoxy-substituted amphetamines and their metabolites was examined after single and multiple oral administration to pregnant and non-pregnant mice. The metabolic profile and extent of biotransformation in a series of alkoxy analogues we...

journal_title：Biopharmaceutics & drug disposition

authors： Foster BC,Litster DL,Buttar HS,Dawson B,Zamecnik J

更新日期：1993-11-01 00:00:00