Multidose studies in the human metabolism of pentobarbitone.

abstract：:We have studied the metabolism of doxorubicin in rat and mouse liver, heart and hepatocytes. Doxorubicinol was present in all cases at very low levels and 7-deoxyaglycones were present only in extraphysiological conditions: no aglycones were found either in fresh livers or in hearts of animals treated with the drug, b...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Vrignaud P,Londos-Gagliardi D,Robert J

更新日期：1986-04-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Sorafenib is an oral, multikinase inhibitor with established single-agent activity in several tumor types. Sorafenib was moderately transported by P-glycoprotein (P-gp) and more efficiently by breast cancer resistance protein. The constitutive androstane receptor (CAR) is a ligand-activated tra...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Karbownik A,Stanisławiak-Rudowicz J,Stachowiak A,Romański M,Grześkowiak E,Szałek E

更新日期：2020-12-01 00:00:00

abstract：:alpha-D-glucose is a weak inhibitor (Ki = 1.7 mM) of glycogen phosphorylase (GP) and acts as physiological regulator of hepatic glycogen metabolism; it binds to GP at the catalytic site and stabilizes the inactive T state of the enzyme promoting the action of protein phosphatase 1 and stimulating glycogen synthase. Th...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Oikonomakos NG,Kontou M,Zographos SE,Tsitoura HS,Johnson LN,Watson KA,Mitchell EP,Fleet GW,Son JC,Bichard CJ

更新日期：1994-07-01 00:00:00

abstract：:The dissolution kinetics of two solid and oral formulations of bezafibrate have been studied. These preparations are available in the Spanish market. Both of them are tablets, one conventional-release (A) and the other slow-release formulation (C). Dissolution studies have been performed using the system proposed by t...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Cadorniga R,Hernanez MT,Negro S,Burgos ML,Molina IT

更新日期：1991-01-01 00:00:00

abstract：:The detection and the isolation in phenobarbital-induced rat liver microsomal incubation systems of a new metabolite of benzo(a)pyrene are described. The structure of this metabolite and the way in which it is formed are described. ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Lhoëst G

更新日期：1980-01-01 00:00:00

abstract：:The present study was carried out to find the in vivo performance of guar gum-based colon-targeted tablets of metronidazole as compared to an immediate release tablets in human volunteers. Six healthy volunteers participated in the study and a crossover design was used. Blood samples were obtained at different time in...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Krishnaiah YS,Veer Raju P,Dinesh Kumar B,Jayaram B,Rama B,Raju V,Bhaskar P

更新日期：2003-10-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Beraprost sodium (BPS) is a chemically stable and orally active prostacyclin analog that is used in the treatment of chronic arterial occlusive disease since 1992 and primary pulmonary hypertension since 1999 in Japan. Multiple-drug therapy is common in clinical practice, and BPS is co-administ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Oshida K,Shimamura M,Seya K,Ando A,Miyamoto Y

更新日期：2017-02-01 00:00:00

abstract：:The antioxidant potential of a new flavonic derivative named conventionally theophylline-rutoside [TR-1722] was estimated by the measurement of G-6-Pase activity (marker enzyme for the endoplasmic reticulum), catalase activity (enzyme involved in the antioxidant defence process), and total -SH groups from the hepatic ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Paduraru I,Saramet A,Danila G,Nichifor M,Jerca L,Iacobovici A,Ungureanu D,Filip M

更新日期：1996-01-01 00:00:00

abstract：:UDP-glucuronosyltransferase 1A9 (UGT1A9) contributes to the glucuronidation of numerous drugs. Cynomolgus monkeys are regarded as experimental animals similar to humans in studies on safety evaluation and biotransformation for drug development. In this study, the similarities and differences in the enzymatic propertie...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Yamamoto K,Mukai M,Nagaoka K,Hayashi K,Hichiya H,Okada K,Murata M,Shigeyama M,Narimatsu S,Hanioka N

更新日期：2014-09-01 00:00:00

abstract：:The pharmacokinetics of chlordemethyldiazepam--a pharmacologically very active new 1,4-benzodiazepine derivative--in healthy subjects after administration of a single oral dose of 2 mg, was studied. Peak concentrations were reached in 1.2 +/- 0.2 hours. Plasma levels declined with a biphasic pattern, and the eliminati...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Bareggi SR,Pirola R,Leva S,Zecca L

更新日期：1986-07-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:The antitumor activity and toxicity of doxorubicin are potentiated and attenuated by calcitriol, respectively. Potentially, calcitriol can be combined with doxorubicin for clinical benefit in chemotherapy. To gain insight into the interaction between doxorubicin and calcitriol, proposed for com...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Durna Corum D,Uney K

更新日期：2020-10-01 00:00:00

abstract：:Tritiated tetrahydro-tetramethyl-naphthalenyl-propenyl benzoic acid (TTNPB; Ro 13-7410) was administered as a single oral bolus to pregnant hamsters (day 8) to determine the maternal plasma pharmacokinetic profile and peripheral tissue distribution patterns. Blood and tissue, including embryo or fetus, were collected ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Howard WB,Willhite CC,Sharma RP,Omaye ST,Hatori A

更新日期：1989-04-01 00:00:00

abstract：:A remarkably large species difference in cinchonidine oxidation activity catalyzed by aldehyde oxidase (AO) has been known, in particular between rabbit and monkey. As the first step in clarifying the phenomenon from the view point of structures of the active site, we attempted to construct an expression system of rab...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Liu P,Liang S,Wang BJ,Guo RC

更新日期：2009-07-01 00:00:00

abstract：:Guizhi decoction (GZD) is a classic traditional Chinese medicine formula, clinically used for the treatment of influenza, common cold, and other pyretic conditions. A sensitive, specific, and validated liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed to investigate the pharmacokinetic pr...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Chen Y,Gao C,Ma Y,Qiu F

更新日期：2013-12-01 00:00:00

abstract：:Vitexin-4″-O-glucoside (VOG), being a main component in the leaves of Crataegus pinnatifida Bge. var. major, was isolated and then three different doses (20, 40, and 60 mg/kg) of VOG were administered intravenously to rats. To study its pharmacokinetics, a simple and rapid HPLC method was developed using hesperidin as...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Ying XX,Wang F,Cheng ZZ,Zhang WJ,Li HB,Du Y,Liu X,Wang SY,Kang TG

更新日期：2012-06-01 00:00:00

abstract：:The present investigation was designed and undertaken in order to substantiate further contention concerning the universality of the utilization of PEG polymers as matrix carriers. This study could then be considered an attempt to enhance the dissolution rate of triamterene, with the subsequent enhancement in its abso...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Arias MJ,Gines JM,Moyano JR,Perez-Barrales MJ,Vela MT,Rabasco AM

更新日期：1994-10-01 00:00:00

abstract：:The aim of the study was to accelerate the dissolution of the sustained release dosage forms using both elevated temperature and high rpm rates. Teokap(®) SR 200 mg pellets were tested by in vitro sustained and accelerated dissolution studies using USP XXIII rotating paddle method. Sustained dissolution studies were c...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Ertan G,Karasulu E,Ozgüney I,Karasulu Y,Apaydın S,Kantarcı G,Yurdasiper A,Ege MA

更新日期：2011-12-01 00:00:00

abstract：:The effects of potassium ethylxanthogenate (PEX) and 2,3-Dimercaptopropane sulphonate sodium (Unithiol) on the pentobarbital (40 mg/kg, body weight i.v.) (PB) sleeping time, pharmacokinetics, and metabolism, were studied in comparative experiments on male albino mice. It was established that the pretreatment of animal...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Yanev S,Janku I,Stoytchev T,Havlik I,Krebs V

更新日期：1982-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:A clinical trial was conducted to measure and analyse the pharmacokinetic parameters of a lipid formulation of risperidone, VAL401. The VAL401 formulation is designed to repurpose risperidone from an antipsychotic to an adenocarcinoma treatment, with the lipid formulation altering the cellular...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Dilly SJ,Morris GS,Taylor PC,Parmentier F,Williams C,Afshar M

更新日期：2019-08-01 00:00:00

abstract：:The activity of the molybdenum hydroxylase, aldehyde oxidase, was determined in crude homogenates and (NH4)2SO4 fractions prepared from guinea pig liver, lung, kidney, intestine, spleen and heart. Xanthine oxidase was also measured in (NH4)2SO4 fractions. In each case, xanthine oxidase levels were lower than those of ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Beedham C,Bruce SE,Rance DJ

更新日期：1987-10-01 00:00:00

abstract：:The disposition of cloflumide (VUFB 15496), 2-chloro-7-fluoro-10 [4-(carbamoylethyl)piperazino]-10,11-dihydrodibenzo [b,f] thiepin methansulfonate, a new neuroleptic agent, following single oral and intravenous dose was studied in the rat using radiotracer techniques. [3H]Cloflumide was almost completely absorbed from...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Lapka R,Franc Z,Smolík S

更新日期：1987-04-01 00:00:00

abstract：:Hepatic transporters and metabolic enzymes affect drug pharmacokinetics. Limited information exists on the alteration in mRNA levels of hepatic transporters and metabolic enzymes with aging. We examined the effects of aging on the mRNA levels of representative hepatic drug transporters and metabolic enzymes by analyzi...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Kawase A,Ito A,Yamada A,Iwaki M

更新日期：2015-06-01 00:00:00

abstract：:Fluvastatin (FV), a new cholesterol-lowering agent, has been studied for its effects on hepatic microsomal drug-metabolizing enzymes in male rats. FV was orally administered in dosages of 1, 5, and 30 mg/kg/day for 7 consecutive days. 3-Hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase activities were markedly decrease...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Ohtawa M,Masuda N,Karasawa Y,Tojo H

更新日期：1995-07-01 00:00:00

abstract：:The kinetics of fenfluramine isomers were studied in the rat following oral doses of racemic fenfluramine. The data, analyzed using an analogue computer, indicate that the d-fenfluramine is metabolised and excreted at a slower rate than the 1-isomer, resulting in higher plasma and brain concentrations. The kinetic par...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Caccia S,Dagnino G,Garattini S,Guiso G,Madonna R,Zanini MG

更新日期：1981-01-01 00:00:00

abstract：:The kinetics of five cisplatin analogs binding to human plasma fractions possessing a molecular weight greater than 50,000 daltons were studied. Each drug solution in plasma ultrafiltrate or phosphate buffer (pH = 7.4, mu = 0.154) was mixed with human plasma and filterable platinum concentrations were measured versus ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Momburg R,Bourdeaux M,Sarrazin M,Roux F,Briand C

更新日期：1985-01-01 00:00:00

abstract：:In this article, the methods of isolation and determination of bile acids are reviewed. Methods for separation of bile acids from cattle and pig bile are given in detail. Isolation of a mixture of cholic acid and deoxycholic acids from cattle bile and their subsequent purification are described. The isolation and puri...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Kandrac J,Kevresan S,Gu JK,Mikov M,Fawcett JP,Kuhajda K

更新日期：2006-07-01 00:00:00

abstract：:The purpose of the study was to investigate the factors upon which the first order rate constant depends in order to assess the impact on the body-drug concentration when it changes throughout a treatment. A reasoning for linking the first order rate constants with several factors in a multiplicative way was proposed ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Fagiolino P

更新日期：2004-01-01 00:00:00

abstract：:The cardioselective beta-adrenergic blocking drug Visacor (ICI 141,292) was dosed to six beagle dogs in a randomized cross-over manner. Five formulations were examined i.e. a 15 mg/kg intravenous solution, a 50 mg/kg oral solution, and 50, 100 and 200 mg/kg oral powder formulations. Whole blood and urine samples were ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： McAinsh J,Smith RP,Ferguson RA

更新日期：1984-04-01 00:00:00

abstract：:Mathematical models that can predict the kinetics of compounds have been increasingly adopted for drug development and risk assessment. Data for these models may be generated from in vitro experimental systems containing enzymes contributing to metabolic clearance, such as subcellular tissue fractions including micros...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Doerksen MJ,Jones RS,Coughtrie MWH,Collier AC

更新日期：2020-12-19 00:00:00

abstract：:Six healthy volunteers received the same oral dose of doxycycline, base (200 mg). Each received two of the three preparations at two-week intervals. Experimental results were interpreted on the basis of one or two-compartment models. The three preparations gave the elimination constants of the same order of magnitude ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Saux MC,Mosser J,Pontagnier H,Leng B

更新日期：1981-01-01 00:00:00