SGK1/Nedd4-2 signaling pathway regulates the activity of human organic anion transporters 3.

abstract：:Dihydroergotoxine is a mixture of semi-synthetic ergot alkaloids mainly used for age-related cognitive impairment. In this study, dihydroergotoxine (30 microM) was added to incubates of rat and bovine liver microsomes, and the resulting major metabolites were identified as hydroxy-dihydroergocornine, hydroxy-dihydroer...

journal_title：Biopharmaceutics & drug disposition

authors： Bicalho B,Giolo JM,Lilla S,De Nucci G

更新日期：2008-01-01 00:00:00

abstract：:The determination of therapeutic levels of glyceryl trinitrate (GTN), isosorbide dinitrate (ISDN), pentaerythritol tetranitrate (PETN), and their metabolites in human plasma was conducted using the TEA Analyzer interfaced to a high-performance liquid chromatograph (HPLC-TEA). Chromatographic separation of these compou...

journal_title：Biopharmaceutics & drug disposition

authors： Yu WC,Goff EU

更新日期：1983-10-01 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 antimalarial drug, halofantrine, is chiral and is administered clinically as the racemate. In order to define the pharmacokinetic properties of halofantrine enantiomers in the rat, male Sprague-Dawley rats (264-311 g) were given halofantrine HCl orally (n = 5; 14 mg/kg) or intravenously (i.v.) (n = 5; 2 mg/kg). Pl...

journal_title：Biopharmaceutics & drug disposition

authors： Brocks DR,Toni JW

更新日期：1999-04-01 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：: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：:Crystalline solid dispersion of lurasidone hydrochloride (LH) was made with various polar and non-polar small molecules to overcome the poor aqueous solubility issue. LH-Glutathione (GSH) solid dispersion in 1:1 ratio was prepared by co-grinding method and characterized by using differential scanning calorimetry (DSC)...

journal_title：Biopharmaceutics & drug disposition

authors： Pardhi VP,Flora S

更新日期：2020-11-01 00:00:00

abstract：:Acute viral infection has long been recognized to down-regulate cytochrome P-450 enzymes and subsequently to result in changes in the pharmacological and toxicological responses to xenobiotics. In our previous research, chronic retrovirus infection induced by inoculating a susceptible strain of mice with LP-BM5 murine...

journal_title：Biopharmaceutics & drug disposition

authors： Chow HH,Tang Y,Li P,Brookshier G,Liang B,Watson R

更新日期：1998-01-01 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：:The lipophilic weak base amodiaquine is an antimalarial drug that has been in use for over 40 years. Little is known of amodiaquine's mechanism of transport across membranes. Transport experiments of amodiaquine in Caco-2 cells showed a low recovery of 30% and rapid disappearance from the apical chamber. Compounds str...

journal_title：Biopharmaceutics & drug disposition

authors： Hayeshi R,Masimirembwa C,Mukanganyama S,Ungell AL

更新日期：2008-09-01 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 purpose of this study was to formulate a drug-in-adhesive (DIA) transdermal patch containing letrozole, a third generation aromatase inhibitor for the treatment of breast cancer, using pressure-sensitive-adhesives (PSAs) and to evaluate the percutaneous penetration and pharmacokinetics of letrozole after transderm...

journal_title：Biopharmaceutics & drug disposition

authors： Li L,Fang L,Xu X,Liu Y,Sun Y,He Z

更新日期：2010-03-01 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：:CYP2C9 is a human microsomal cytochrome P450c (CYP). Much variation in CYP2C9 levels and activity can be attributed to polymorphisms of this gene. Wild-type CYP2C9 and ten mutants were co-expressed with NADPH-cytochrome P450 reductase in Escherichia coli. The hydroxylase activities toward steroids were examined. CYP2C...

journal_title：Biopharmaceutics & drug disposition

authors： Uno T,Nakano R,Kitagawa R,Okada M,Kanamaru K,Takenaka S,Uno Y,Imaishi H

更新日期：2018-09-01 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：: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：:The pharmacokinetics and tolerability of a new putative non-benzodiazepine type anxiolytic compound deramciclane was studied in two consecutive studies. An open dose-escalation design was used to study doses from 0.2 to 50 mg in 18 healthy male volunteers. In the second study doses from 50 to 150 mg were investigated ...

journal_title：Biopharmaceutics & drug disposition

authors： Kanerva H,Kilkku O,Heinonen E,Helminen A,Rouru J,Tarpila S,Scheinin M,Huupponen R,Klebovich I,Drabant S,Urtti A

更新日期：1999-10-01 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：:The oral pharmacokinetics (concentration-time profile) of four proprietary compounds in humans were predicted using the C(vss)-MRT method. The first step was to demonstrate superposition of intravenous (i.v.) pharmacokinetic profiles of preclinical species following mathematical transformation of their respective conc...

journal_title：Biopharmaceutics & drug disposition

authors： Fura A,Vyas V,Humphreys W,Chimalokonda A,Rodrigues D

更新日期：2008-11-01 00:00:00

abstract：:Gastrointestinal distress resulting from drug intake is often remedied by administering the drug with antacids. However, antacids have been shown to modify the absorption and excretion of many drugs. This study was designed to delineate the effects of aluminium and magnesium hydroxide antacid suspension (Maalox) on th...

journal_title：Biopharmaceutics & drug disposition

authors： Caillé G,du Souich P,Vézina M,Pollock SR,Stalker DJ

更新日期：1989-11-01 00:00:00

abstract：:The present study aimed to investigate the effect of atorvastatin on the intravenous and oral pharmacokinetics of verapamil in rats. The pharmacokinetic parameters of verapamil were measured after an oral (9 mg/kg) or intravenous (3 mg/kg) administration of verapamil to rats in the presence and absence of atorvastatin...

journal_title：Biopharmaceutics & drug disposition

authors： Choi DH,Chang KS,Hong SP,Choi JS,Han HK

更新日期：2008-01-01 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：: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：:The pharmacokinetics of methylprednisolone and methylprednisolone phosphate were investigated after intravenous administration of methylprednisolone phosphate to six healthy subjects at seven different doses between 16 and 1000 mg. Plasma, urine, and saliva were analyzed for methylprednisolone and methylprednisolone p...

journal_title：Biopharmaceutics & drug disposition

authors： Möllmann H,Rohdewald P,Barth J,Verho M,Derendorf H

更新日期：1989-09-01 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：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 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：:The bioequivalence of three oral forms of nifedipine was assessed in a triple crossover study on 12 healthy volunteers. Single 10 mg dose was given and ten blood samples were drawn during the first 8 h after administration. Highly sensitive gas chromatographic method was used for the nifedipine assay. Pharmacokinetic ...

journal_title：Biopharmaceutics & drug disposition

authors： Kozjek F,Primozic S,Mrhar A,Karba R,Raemsch KD,Janezic A

更新日期：1987-01-01 00:00:00

abstract：:The bioavailability of the thiazide diuretic bemetizide from a tablet containing 25 mg of this drug and 50 mg of the chemically unrelated diuretic triamterene was lower than, and significantly different (p less than 0.01) from that from a tablet containing 25 mg bemetizide alone. The mean peak plasma level of bemetizi...

journal_title：Biopharmaceutics & drug disposition

authors： Brodie RR,Chasseaud LF,Darragh A,Taylor T,Walmsley LM

更新日期：1982-10-01 00:00:00

abstract：:The pharmacokinetics of a series of novel cyclic, non-peptide inhibitors of HIV protease were studied in rats or dogs after intravenous and oral administration. Six symmetrically substituted cyclic urea compounds (XK234, XM311, XM320, XM321, XM323, and XM412), which effectively inhibited HIV virus replication, with IC...

journal_title：Biopharmaceutics & drug disposition

authors： Wong YN,Burcham DL,Saxton PL,Erickson-Viitanen S,Grubb MF,Quon CY,Huang SM

更新日期：1994-10-01 00:00:00