Gender differences in pharmacokinetics of lumefantrine and its metabolite desbutyl-lumefantrine in rats.

abstract：:Asialofetuin-labelled liposomes (AF-liposomes) having mean diameters of 0.13 micron ([S]) and 0.35 micron ([L]) were obtained by the subsequent extrusion method in combination with dialysis. Intravenously administered AF-liposomes [S] were rapidly cleared from the systemic circulation. By pre- and post-treatment of th...

journal_title：Biopharmaceutics & drug disposition

authors： Hara T,Aramaki Y,Tsuchiya S,Hosoi K,Okada A

更新日期：1987-07-01 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：:The steady-state pharmacokinetics of an ultralong sustained release formulation of theophylline (Unilong) twice daily (bid) in elderly hospitalized patients suffering from chronic obstructive pulmonary disease (COPD) have been studied in order to establish guidelines for monitoring. The study was carried out in 37 pat...

journal_title：Biopharmaceutics & drug disposition

authors： Armijo JA,Sánchez BM,Peralta FG,González-Ruiz M,Cuadrado A,Verdejo A,Cos MA,Arjona R

更新日期：2003-05-01 00:00:00

abstract：:Biliary clearance (Clb) of sotalol (STL) enantiomers was assessed in anaesthetized Sprague-Dawley rats (419 +/- 9 g, mean +/- SEM, n = 4) following administration of a 10 mg kg-1 i.v. dose of the racemate. Clb for S- and R-STL (0.0675 +/- 0.0090 and 0.0662 +/- 0.0089 mL min-1 kg-1, respectively) represented approximat...

journal_title：Biopharmaceutics & drug disposition

authors： Carr RA,Pasutto FM,Foster RT

更新日期：1996-11-01 00:00:00

abstract：:The effects of gender on the pharmacokinetics of verapamil and its active metabolite, norverapamil, following single oral dose (80 mg, Isoptin) to 12 healthy male (mean age: 25.75+/-2.42 years, mean body weight: 70.59+/-9.94 kg) and 12 healthy female subjects (mean age: 24.08+/-2.84 years, mean body weight: 56.67+/-5....

journal_title：Biopharmaceutics & drug disposition

authors： Dadashzadeh S,Javadian B,Sadeghian S

更新日期：2006-10-01 00:00:00

abstract：:Human organic anion transporter 3 (hOAT3) is localized at the basolateral membrane of renal proximal tubule cells and facilitates the renal secretion of numerous clinical drugs, including anti-HIV therapeutics, anti-tumor drugs, antibiotics, antihypertension drugs and anti-inflammatories. The present study explored th...

journal_title：Biopharmaceutics & drug disposition

authors： Wang H,You G

更新日期：2017-11-01 00:00:00

abstract：:The following results were obtained recently from our laboratories; in rats with 72-h water deprivation (rats with dehydration), the hepatic cytochrome P450 2E1 (CYP2E1) was three-fold induced with an increase in the mRNA. Rehydration of 48-h water-deprived rats for the next 24 h with free access of food (rats with re...

journal_title：Biopharmaceutics & drug disposition

authors： Kim YC,Kim YG,Kim EJ,Cho MK,Kim SG,Lee MG

更新日期：2003-03-01 00:00:00

abstract：:The pharmacokinetics and pharmacodynamics of furosemide were compared after an oral administration or a direct administration of Lasix into the duodenum in humans (40 mg). Furosemide was absorbed quickly after a direct administration of Lasix into the duodenum; the peak plasma concentration of furosemide was reached w...

journal_title：Biopharmaceutics & drug disposition

authors： Lee WI,Yoon WH,Shin WG,Song IS,Lee MG

更新日期：1997-12-01 00:00:00

abstract：:The absorption characteristics of ethiofos were studied using the rat in situ intestine circulating perfusion technique. Slow absorption kinetics were observed for ethiofos with varying rates of absorption and metabolism/degradation in situ as a function of buffer and absorption enhancers. In most cases less than 10 p...

journal_title：Biopharmaceutics & drug disposition

authors： Geary RS,Swynnerton NF,Timmons SF,Mangold DJ

更新日期：1991-05-01 00:00:00

abstract：:The inhibition of rat hepatic mitochondrial aldehyde dehydrogenase (ALDH) isozymes was studied in apparent steady-state conditions after repeated intra-peritoneal cyanamide administration. The low-Km mitochondrial ALDH isozyme was more susceptible to cyanamide-induced inhibition (DI50 = 0.104 mg kg-1) than the high-Km...

journal_title：Biopharmaceutics & drug disposition

authors： Pruñonosa Piera J,Obach R,Sagristá ML,Bozal J

更新日期：1993-07-01 00:00:00

abstract：PURPOSE:Amifostine is a prodrug in which selectivity is largely determined by the preferential formation and uptake of its cytoprotective metabolite, WR-1065, in normal tissues as a result of differences in membrane-bound alkaline phosphatase activity. It was hypothesized that amifostine may be a good candidate for reg...

journal_title：Biopharmaceutics & drug disposition

authors： Levi M,DeRemer SJ,Dou C,Ensminger WD,Smith DE

更新日期：2004-01-01 00:00:00

abstract：:The present study aimed to examine the potential pharmacokinetic drug interaction between valsartan and gemfibrozil. Compared with the control given valsartan (10 mg/kg) alone, the concurrent use of gemfibrozil (10 mg/kg) significantly (p < 0.05) increased the oral exposure of valsartan in rats. In the presence of gem...

journal_title：Biopharmaceutics & drug disposition

authors： Yang SJ,Kim BJ,Mo L,Han HK

更新日期：2016-07-01 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：: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：: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：: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：: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：: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：: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：: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：: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 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 objective of this study was to assess the effect of dietary fibers on the transport of losartan, an angiotensin II type 1 receptor blocker, in small intestinal cells. Using Caco-2 cells in vitro, losartan uptake and transport were evaluated in the presence of various fibers (cellulose, chitosan, sodium alginate an...

journal_title：Biopharmaceutics & drug disposition

authors： Iwazaki A,Takahashi N,Miyake R,Hiroshima Y,Abe M,Yasui A,Imai K

更新日期：2016-05-01 00:00:00

abstract：:It was shown previously that the anticancerous cytotoxic oxygenated triterpenes, cucurbitacin E (Cuc E) and its deacetylated form, cucurbitacin I (Cuc I), interacted differently with human serum albumin. In this study, the biochemical stability of Cuc E was investigated in vitro by reverse-phase high performance liqui...

journal_title：Biopharmaceutics & drug disposition

authors： Saade M,Magdalou J,Ouaini N,Greige-Gerges H

更新日期：2009-10-01 00:00:00

abstract：:The intestinal lymphatic absorption of cyclosporin A (CyA) following oral administration of 6.5 +/- 0.6 and 25.2 +/- 1.4 mg kg-1 doses of the drug dissolved in an olive oil solution was studied using a thoracic duct-cannulated rat model. Cumulative lymph samples were collected for up to 114 h post-dosing and assayed b...

journal_title：Biopharmaceutics & drug disposition

authors： Ueda CT,Lemaire M,Gsell G,Nussbaumer K

更新日期：1983-04-01 00:00:00

abstract：:Telaprevir, a chronic hepatitis C virus (HCV) protease inhibitor, is known to be a cytochrome P450 (CYP) 3A4/5 substrate and inhibitor. In the present study, the in vitro inhibitory effect of telaprevir on the metabolism of tacrolimus in human liver microsomes was investigated using 13-O-demethyltacrolimus (M-I) as a ...

journal_title：Biopharmaceutics & drug disposition

authors： Oda K,Yamano K

更新日期：2014-12-01 00:00:00

abstract：:Potential differences in pharmacokinetics (PK) between healthy subjects and patients with cancer were investigated using a physiologically based pharmacokinetic approach integrating demographic and physiological data from patients with cancer. Demographic data such as age, sex and body weight, and clinical laboratory ...

journal_title：Biopharmaceutics & drug disposition

authors： Cheeti S,Budha NR,Rajan S,Dresser MJ,Jin JY

更新日期：2013-04-01 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：:Sulfotransferase (SULT) 1A1 and SULT1A3 play important roles in the presystemic inactivation of beta(2) agonists in the liver and intestine, respectively. The study aimed to investigate the inhibitory effects of grapefruit juice, orange juice, green tea, black tea and oolong tea and their constituents on the activitie...

journal_title：Biopharmaceutics & drug disposition

authors： Nishimuta H,Ohtani H,Tsujimoto M,Ogura K,Hiratsuka A,Sawada Y

更新日期：2007-12-01 00:00:00