Pharmacokinetics of riluzole: evidence for glucuronidation as a major metabolic pathway not associated with UGT1A1 genotype.

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

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：:The pharmacokinetics of a non-narcotic analgesic, DA-5018, were compared after single intravenous (i.v.), subcutaneous (s.c.), and oral administrations, and after multiple (seven consecutive days) s.c. administration to rats. After i.v. administration of DA-5018, 1, 2, and 5 mg kg-1, the pharmacokinetic parameters of ...

journal_title：Biopharmaceutics & drug disposition

authors： Lee JJ,Shim HJ,Kim SH,Lee SD,Kim WB,Yang J,Lee MG

更新日期：1998-03-01 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：:Prednisolone (POH) and prednisone (PO) were both administered via seven different intravenous infusions (three POH and four PO) in each of six rabbits to obtain steady state. Bolus doses of POH and PO were also administered to four of the rabbits. Plasma samples of POH and PO were analyzed by normal phase HPLC. Unboun...

journal_title：Biopharmaceutics & drug disposition

authors： Hammarlund-Udenaes M,Benet LZ

更新日期：1991-08-01 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：:Loxoprofen (LX) is a prodrug-type non-steroidal anti-inflammatory drug which is used not only as an oral drug but also as a transdermal formulation. As a pharmacologically active metabolite, the trans-alcohol form of LX (trans-OH form) is generated after oral administration to humans. The objectives of this study were...

journal_title：Biopharmaceutics & drug disposition

authors： Sawamura R,Sakurai H,Wada N,Nishiya Y,Honda T,Kazui M,Kurihara A,Shinagawa A,Izumi T

更新日期：2015-09-01 00:00:00

abstract：:Rifampicin, a poorly soluble drug, has great importance in therapeutics as it is the main drug used to treat tuberculosis. The characterization of its permeability and the factors that influence it represent an important tool for predicting its bioavailability. Caco-2 cell monolayers were used as models of the intesti...

journal_title：Biopharmaceutics & drug disposition

authors： Gonçalves JE,Ballerini Fernandes M,Chiann C,Gai MN,De Souza J,Storpirtis S

更新日期：2012-09-01 00:00:00

abstract：:Regional pharmacokinetics is the study of the drug concentrations in specific regions of the body. It allows greater insight into the mechanisms of drug disposition than the study of systemic blood concentrations. Experimental methods in regional pharmacokinetics and their applications and limitations are reviewed. Po...

journal_title：Biopharmaceutics & drug disposition

authors： Upton RN,Runciman WB,Mather LE

更新日期：1990-12-01 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：: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 biotransformation of thionorphine (N-cyclopropylmethyl-7alpha-[(s)-1-hydroxy-1-methyl-3-(2thiophene)-propyl]-6,14-endo-ethano tetrahydrooripavine), a new analgesic, was in-vestigated in rats. The results of metabolite analysis by liquid chromatography/electrospray ionization tandem mass spectrometry with positive ...

journal_title：Biopharmaceutics & drug disposition

authors： Wei SX,Zhang ZQ,Wang XY,Guo JF

更新日期：2004-04-01 00:00:00

abstract：:The enantioselective pharmacokinetics of a new anxiolytic, pazinaclone (DN-2327), and its active metabolite, M-II, were studied in animals. In rats and dogs given racemic pazinaclone intravenously, the total clearance and volume of distribution of (S)-pazinaclone were lower than those of (R)-pazinaclone, whereas the o...

journal_title：Biopharmaceutics & drug disposition

authors： Kondo T,Yoshida K,Yoshimura Y,Tanayama S

更新日期：1995-12-01 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：:Equilibrative nucleoside transporters (ENTs) 1 and 2 reportedly accept fluorouracil as a substrate. Here, we evaluated ENT1/2 expression at the messenger RNA (mRNA), protein, and functional levels in a panel of four triple-negative breast cancer (TNBC) cell lines, BT-549, Hs578T, MDA-MB-231, and MDA-MB-435, and we exa...

journal_title：Biopharmaceutics & drug disposition

authors： Noguchi S,Takagi A,Tanaka T,Takahashi Y,Pan X,Kibayashi Y,Mizokami R,Nishimura T,Tomi M

更新日期：2021-01-10 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：:A new sustained release dosage form of valproic acid (VPA) was developed. The new sustained release dosage form was administered (twice, with and without food) to five dogs in comparison to a standard tablet (Depakine, Labaz) and an i.v. preparation of the drug. Drug level monitoring in the plasma was performed by a G...

journal_title：Biopharmaceutics & drug disposition

authors： Bialer M,Friedman M,Dubrovsky J

更新日期：1984-01-01 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 effect of the combination of a new anticonvulsant drug HEPP and carbamazepine (CBZ) on the pharmacokinetics of HEPP and CBZ was investigated using rabbits as an animal model. The study was performed in 18 male New Zealand white rabbits which were randomly divided into three groups, according to a balanced incomple...

journal_title：Biopharmaceutics & drug disposition

authors： García AL,Medina RL,Pérez MR,Jung CH

更新日期：2003-07-01 00:00:00

abstract：:Zopiclone is a new sedative showing a rapid onset of hypnotic effect and a relatively short duration of action. The goal of this study was to assess the kinetic parameters of zopiclone and its interaction with trimipramine when administered concomitantly. Ten normal subjects each received doses of zopiclone (7.5 mg), ...

journal_title：Biopharmaceutics & drug disposition

authors： Caille G,du Souich P,Spenard J,Lacasse Y,Vezina M

更新日期：1984-04-01 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：:Although nifedipine has been characterized in terms of its general vasodilatory effects, this dihydropyridine must still be regarded as investigational with regard to available pharmacokinetic and pharmacodynamic data. Although limited studies are available, it is clear that the pharmacokinetic and pharmacodynamic dat...

journal_title：Biopharmaceutics & drug disposition

authors： Hamann SR,Piascik MT,McAllister RG Jr

更新日期：1986-01-01 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：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：:Data from sustained-release and enteric-coated oral formulations, and the suppository formulation of diclofenac sodium are fitted simultaneously using NONMEM and the general linear model, ADVAN 5. Absorption and disposition parameters, serum levels, and absorption profiles were determined. The in vivo absorption profi...

journal_title：Biopharmaceutics & drug disposition

authors： Idkaidek NM,Amidon GL,Smith DE,Najib NM,Hassan MM

更新日期：1998-04-01 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：:This study compared the relative ocular bioavailability in rabbits of the antibiotic/steroid combination of 0.3 per cent tobramycin and 0.1 per cent fluorometholone acetate to each of the two single-entity products. Two separate studies were conducted, one measuring fluorometholone acetate in cornea and aqueous humour...

journal_title：Biopharmaceutics & drug disposition

authors： Schoenwald RD,Harris RG,Turner D,Knowles W,Chien DS

更新日期：1987-11-01 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 pharmacokinetics of fluvoxamine after single oral administration of 25, 50, and 100 mg fluvoxamine maleate was studied in a three-way cross-over study in 12 healthy male subjects. Fluvoxamine was administered orally in a solution. For dose-proportionality, AUC, and Cmax-dose relationships were evaluated by linear ...

journal_title：Biopharmaceutics & drug disposition

authors： De Vries MH,Van Harten J,Van Bemmel P,Raghoebar M

更新日期：1993-05-01 00:00:00

abstract：:The effect of the concomitant administration of the antifungal drugs ketoconazole (KTC) and itraconazole (ITC) on the pharmacokinetics of ciprofloxacin (CIP) following short- and long-term administration in mice was investigated. Animals received either a dose of CIP (20 mg/kg, i.p.), CIP (20 mg/kg, i.p.) together wit...

journal_title：Biopharmaceutics & drug disposition

authors： Abou-Auda HS,Mustafa AA,Al-Humayyd MS

更新日期：2008-01-01 00:00:00