The single-point method of dosage prediction: pharmacokinetic basis and method optimization.

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：:The effects of age on hepatic microsomal enzyme induction were studied in male CD-1 mice. Six week old and 1 year old animals were treated with either phenobarbital (80 mg kg-1) or saline once daily for 3d. Twenty-four hours after the last treatment, animals were sacrificed and livers were harvested. Hepatic microsoma...

journal_title：Biopharmaceutics & drug disposition

authors： Charpentier KP,von Moltke LL,Poku JW,Harmatz JS,Shader RI,Greenblatt DJ

更新日期：1997-03-01 00:00:00

abstract：:Beta-adrenoceptor blocking drugs are widely used as effective antihypertensive and antianginal agents. We have determined the effect of beta-blockade in the rat to ascertain whether there are differences between metoprolol (MET) and acebutolol (AC) with respect to regional blood flow (RBF). Both AC and MET were admini...

journal_title：Biopharmaceutics & drug disposition

authors： Mostafavi S,Lewanczuk R,Foster R

更新日期：2000-05-01 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：:The objective of this study was to investigate the absorption behavior of chikusetsusaponin IVa (CHS-IVa) in the rat intestine using single-pass intestinal perfusion (SPIP) and to classify CHS-IVa into the biopharmaceutics classification system (BCS). The equilibrium solubility of CHS-IVa was determined by the shaker ...

journal_title：Biopharmaceutics & drug disposition

authors： Zhang W,Liu H,Liu C

更新日期：2019-09-01 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：: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：: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：: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：:Dolasetron, Anzemet, a 5-hydroxytryptamine receptor antagonist, is under investigation as an antiemetic agent. The keto-reduced metabolite of dolasetron has been identified in human plasma and is probably responsible for the majority of the antiemetic activity. This study evaluated the pharmacokinetics of dolasetron a...

journal_title：Biopharmaceutics & drug disposition

authors： Shah A,Lanman R,Bhargava V,Weir S,Hahne W

更新日期：1995-04-01 00:00:00

abstract：:Flow microcalorimetry was used to estimate primary binding constants for drug-albumin interactions. Measurements of heat of reaction at two temperatures illustrated the danger of extrapolation for pharmacokinetic purposes of measurements made at temperatures other than 37 degrees. The method could be used to predict c...

journal_title：Biopharmaceutics & drug disposition

authors： Hardee GH,Fleitman JS,Otagiri M,Perrin JH

更新日期：1984-10-01 00:00:00

abstract：:In the search for orally available drugs, the prediction of human pharmacokinetics (PK) is essential for successfully selecting compounds that will be clinically useful. This report describes the selection of TAK-272 (SCO-272), a novel orally active renin inhibitor, as a clinical candidate via the detailed investigati...

journal_title：Biopharmaceutics & drug disposition

authors： Ebihara T,Nishihara M,Takahashi J,Jinno F,Tagawa Y

更新日期：2018-03-01 00:00:00

abstract：:The pharmacokinetics and pharmacodynamics of torasemide were evaluated after intravenous administration of the same total dose of torasemide at a dose of 1mg/kg to rabbits with different infusion times, 1 min (treatment I), 30 min (treatment II) and 2 h (treatment III). The loss of water and electrolytes in urine indu...

journal_title：Biopharmaceutics & drug disposition

authors： Kim YC,Lee MG,Ko SH,Kim SH

更新日期：2004-07-01 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：:It was reported that gastric motility was delayed and gastric acid secretion was reduced in vagotomized dogs which mimics a low gastric acidity in humans. A delay in gastric motility causes long residence of amlodipine in the stomach. More unionized fractions of amlodipine could exist in less acidic conditions of gast...

journal_title：Biopharmaceutics & drug disposition

authors： Kwak HH,Kim JO,Chung HK,Choi SM,Kim JH,Kwon JW,Yoo M,Lee JH,Lee MG

更新日期：2006-04-01 00:00:00

abstract：:The bioavailability of an improved formulation of enteric-coated phenylbutazone with faster dissolution, more consistent in vitro rate of drug release and improved stability was compared in 8 normal subjects at doses of 100 and 200 mg with commercially available Butacote. Phenylbutazone was more rapidly absorbed from ...

journal_title：Biopharmaceutics & drug disposition

authors： John VA,Goldsborough S,Morrison PJ,Rogers HJ,Spector RG,Bradbrook ID

更新日期：1982-01-01 00:00:00

abstract：:EXP631, 4-(3-thienyl)-alpha, alpha,1-trimethyl-4-piperidine-methanol hemi-fumarate salt (I), is a centrally acting non-opioid analgesic compound with monoamine uptake blocking properties. EXP631 has analgesic effects in several animal models. It is intended to be used for the treatment of moderate to moderately severe...

journal_title：Biopharmaceutics & drug disposition

authors： Wong YN,Burcham DL,Huang SM,Quon CY

更新日期：1993-08-01 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：: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：:The relative lung and systemic bioavailability of sodium cromoglycate following inhalation by different methods have been determined using a urinary excretion pharmacokinetic method. On three separate randomised study days, 7 days apart, subjects inhaled (i) 4x5 mg from an Intal metered dose inhaler (MDI), (ii) 4x5 mg...

journal_title：Biopharmaceutics & drug disposition

authors： Aswania O,Chrystyn H

更新日期：2002-05-01 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 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：: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：: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：:A pharmacokinetic study of sachets containing nalidixic acid (0.66 g) associated with sodium citrate (3.75 g)--NSC--was carried out in 10 healthy volunteers in order to determine the influence of the urine alcalinization due to sodium citrate on the elimination of nalidixic acid (NA) and its 7-hydroxy (HNA) and 7-carb...

journal_title：Biopharmaceutics & drug disposition

authors： Ferry N,Cuisinaud G,Sassard J,Pozet N,Zech PY

更新日期：1984-07-01 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 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：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：: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：: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