Identification and human pharmacokinetics of dihydroergotoxine metabolites in man: preliminary results.

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：: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：:BMS-378806 is a prototype of novel HIV attachment inhibitors that block the gp120 and CD4 interaction, the first step of HIV-1 entry into cells. The present work investigated the pharmacokinetics of BMS-378806 in rats, dogs and monkeys and assessed its in vitro permeability and metabolism. BMS-378806 exhibited species...

journal_title：Biopharmaceutics & drug disposition

authors： Yang Z,Zadjura L,D'Arienzo C,Marino A,Santone K,Klunk L,Greene D,Lin PF,Colonno R,Wang T,Meanwell N,Hansel S

更新日期：2005-12-01 00:00:00

abstract：:The definitions of mean residence time of drug molecules in the body (MRT) from the literature are reviewed. A formal definition of MRT, based on excretion of drug molecules and amount of drug, a parameter which is independent of constancy of both clearance and volume of distribution, is introduced and compared to oth...

journal_title：Biopharmaceutics & drug disposition

authors： Kasuya Y,Hirayama H,Kubota N,Pang KS

更新日期：1987-05-01 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：: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：: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：: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：:We present a novel method for performing pharmacokinetic and metabolism studies on macromolecules that offers advantages over the existing techniques of radiolabeling, immunoassay or bioassays. Our strategy uses macromolecules with stable isotopes uniformly distributed throughout the structure. The stable isotope enri...

journal_title：Biopharmaceutics & drug disposition

authors： Osborn BL,Abramson FP

更新日期：1998-10-01 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：: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：:This study aims to characterize the pharmacodynamic properties of denosumab, a RANK ligand inhibitor, and ibandronate, a bisphosphonate, using an integrated bone homeostasis model in postmenopausal women. Mean temporal profiles of denosumab, serum and urine N-telopeptide (sNTX, uNTX), lumbar spine bone mineral density...

journal_title：Biopharmaceutics & drug disposition

authors： Marathe DD,Marathe A,Mager DE

更新日期：2011-11-01 00:00:00

abstract：:Previously we demonstrated that a hydrophilic HMG-CoA reductase inhibitor, pravastatin, was actively taken up by the liver via the 'multispecific anion transporter' using isolated rat hepatocytes (M. Yamazaki, H. Suzuki, M. Hanano, T. Tokui, T. Komai, and Y. Sugiyama, Am. J. Physiol., 264, G36-G44 (1993)). Such a carr...

journal_title：Biopharmaceutics & drug disposition

authors： Yamazaki M,Tokui T,Ishigami M,Sugiyama Y

更新日期：1996-12-01 00:00:00

abstract：:In this comparative bioavailability study in 12 healthy volunteers the blood level profiles of both propranolol and bendrofluazide were studied following the multiple oral administration of the drugs as a fixed combination (Inderetic) and as a free combination at doses of 80 mg propranolol twice daily and 2.5 mg bendr...

journal_title：Biopharmaceutics & drug disposition

authors： McAinsh J,Holmes BF,Baber NS,Young J

更新日期：1981-04-01 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：: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 bioavailability of orally administered therapies are often significantly limited in the human intestine by the metabolic activities of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp). Predicting whether candidate compounds induce CYP3A4 and P-gp is a crucial stage in the drug development process, as drug-dr...

journal_title：Biopharmaceutics & drug disposition

authors： Inami K,Sasaki T,Kumagai T,Nagata K

更新日期：2015-04-01 00:00:00

abstract：:The pharmacokinetic regularity of the murine monoclonal antibody ior EGF/r3 across mammals was studied using allometry. The allometric relationship between the volume of distribution and body weight (W) across mammalian species was characterized by the power equation V(d)=218.8 W(0.84) (r=0.92), and that for clearance...

journal_title：Biopharmaceutics & drug disposition

authors： Ducongé J,Fernández-Sánchez E,Alvarez D

更新日期：2004-05-01 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：: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：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：: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：:The pharmacokinetics of a new selective oestrogen receptor modulator levormeloxifene was investigated in mice, rats, cynomolgus monkeys and humans by compartmental pharmacokinetics. Levormeloxifene was administered as an oral solution in all studies. Allometric scaling was used to predict human pharmacokinetic paramet...

journal_title：Biopharmaceutics & drug disposition

authors： Østerberg O,Kiehr B,Erichsen L,Poulsen HE,Ingwersen SH

更新日期：2003-04-01 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：: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：: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：: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 inhibition potencies of aripiprazole and its active metabolite, dehydroaripiprazole, on the activities of human multidrug resistance protein 1 (MDR1/ABCB1; P-glycoprotein), breast cancer resistance protein (BCRP/ABCG2) and multidrug resistance-associated protein 4 (MRP4/ABCC4), that are drug efflux transporters ex...

journal_title：Biopharmaceutics & drug disposition

authors： Nagasaka Y,Oda K,Iwatsubo T,Kawamura A,Usui T

更新日期：2012-09-01 00:00:00

abstract：:Utilization of nitric oxide (NO) synthase (NOS) inhibitors to probe the role of NO in various central nervous system processes requires use of an inhibitor selective for neuronal NOS, and is facilitated by knowledge of the pharmacokinetics of the inhibitor. The present project was undertaken to elucidate the dispositi...

journal_title：Biopharmaceutics & drug disposition

authors： Bush MA,Pollack GM

更新日期：2000-09-01 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