The sojourn time and its use in pharmacology.

abstract：:We studied the hepatic handling of bromosulfophthalein in healthy rabbits with hepatic coccidiosis 28 days after an experimental infection with sporulated oocysts of Eimeria stiedai, an experimental model of liver disease histopathologically resembling primary biliary cirrhosis in man. A pharmacokinetic study of the r...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Esteller A,Torres MD,Gomez-Bautista M,Mariño EL,Fernandez-Lastra C,Jimenez R

更新日期：1990-01-01 00:00:00

abstract：:The kinetics of the nootropic drug oxiracetam was studied in 6 elderly female patients (age range 69-96 years) in good physical condition. After a single oral dose (800 mg), serum oxiracetam levels reached a peak (25 +/- 6 micrograms/ml) within 1-3 h and declined thereafter with a half-life of 3 to 6 h. Eighty-four pe...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Perucca E,Parini J,Albrici A,Visconti M,Ferrero E

更新日期：1987-04-01 00:00:00

abstract：:This study developed a physiologically based pharmacokinetic (PBPK) model in intraabdominally infected rats and extrapolated it to humans to predict the levofloxacin pharmacokinetics and penetration into tissues. Twelve male rats with intraabdominal infections induced by Escherichia coli received a single dose of 50 m...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Zhu L,Zhang Y,Yang J,Wang Y,Zhang J,Zhao Y,Dong W

更新日期：2016-08-01 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：:A multicompartmental pharmacokinetic model is presented, which based upon data from a previous study, describes the effects of ethanol (60 mM) on the metabolism of codeine (10 microM) in isolated rat hepatocytes. According to this model, about one third of codeine metabolized was transformed to morphine (13%) and norc...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Bodd E,Green MH,Drevon CA,Mørland J

更新日期：1986-07-01 00:00:00

abstract：:A generic drug product (test product) is bioequivalent to an innovator product (reference product) when their bioavailabilities in the same molar dose are similar. Bioavailability is expressed by pharmacokinetic parameters such as the area under plasma concentration-time curve (AUC), the maximum plasma concentration (...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Zintzaras E

更新日期：2005-01-01 00:00:00

abstract：:The biotransformation of netobimin (NTB) pro-drug by ruminal, abomasal and intestinal fluids of sheep and cattle was investigated under anaerobic conditions in vitro. No metabolic conversion of NTB was observed upon incubation with abomasal fluid or boiled samples of different gastrointestinal fluids. NTB pro-drug was...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Lanusse CE,Nare B,Gascon LH,Prichard RK

更新日期：1992-04-01 00:00:00

abstract：:The pharmacokinetics, biotransformation, protein binding and tissue distribution of mitonafide and pinafide were studied after single i.v. and oral administration of each drug (20 mg/Kg) in female rats. In pregnant rats a study of cross placental-barrier after i.v. administration of the two drugs was also performed. T...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Rivera Cid P,Gonzalez Fernandez E,Martin FR,Braña MF

更新日期：1986-10-01 00:00:00

abstract：:YM466, a novel factor Xa inhibitor, is a hydrophilic compound with a carboxylic acid moiety. Previous studies in rats have shown that YM466 does nor undergo metabolism but is excreted into the bile and urine in unchanged form. Thus, in this study, we investigated in vivo hepatobiliary transport, focusing in particular...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Mano Y,Usui T,Kamimura H

更新日期：2006-04-01 00:00:00

abstract：:Release rates from intramuscular and intra-adipose injection sites are dependent upon several including injection depth. Little is known about the relationship between drug lipophilicity and transport rate of drugs through adipose and muscle tissue. The principal objective of the present study was to investigate to wh...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Kadir F,Zuidema J,Pijpers A,Vulto A,Verheijden JH

更新日期：1991-01-01 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：:IdB 1016 is a complex of silybin (the main active component of silymarin) and phosphatidylcholine, which in animal models shows greater oral bioavailability and therefore greater pharmacological activity compared with pure silybin and silymarin. In order to assess its pharmacokinetic profile in man, plasma silybin lev...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Barzaghi N,Crema F,Gatti G,Pifferi G,Perucca E

更新日期：1990-10-01 00:00:00

abstract：:The pharmacokinetic-pharmacodynamic (PK-PD) relationship of the proton pump inhibitor rabeprazole in healthy Chinese volunteers was characterized via a population approach. Healthy Chinese male volunteers were enrolled in the clinical trial. Subjects were divided into three groups by their CYP2C19 genotype. Serum conc...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Chen ZY,Xie HT,Zheng QS,Sun RY,Hu G

更新日期：2006-01-01 00:00:00

abstract：:Thymoquinone (THQ), the active constituent of Nigella sativa seeds, has demonstrated some potential pharmacological activities. The present study was designed to investigate the pharmacokinetic behavior of THQ following intravenous (IV) and oral (PO) administration using an animal model. THQ was given vascularly (5 mg...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Alkharfy KM,Ahmad A,Khan RM,Al-Shagha WM

更新日期：2015-09-01 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：:The aim of this work was to study the influence of labelling on caffeine metabolism according to the incubation mode. It has been observed that labelling induces an isotopic effect on metabolisation speed: apparent half-lives are systematically increased. Moreover, isotopic effects are in agreement with those previous...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Benchekroun Y,Dautraix S,Desage M,Brazier JL

更新日期：1997-04-01 00:00:00

abstract：:The in vitro and in vivo metabolism of RWJ-69442, an alpha-1A-adrenergic receptor antagonist, was investigated after incubation with rat, dog, and human hepatic S9 fractions in the presence of NADPH-generating system, and a single oral/iv dose administration to rats (oral: 100 mg/kg; iv: 10 mg/kg). Unchanged RWJ-69442...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Wu WN,McKown LA,Kuo GH

更新日期：2005-01-01 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：:Following i.v. administration of mono-HR to the beagle, plasma levels of both mono-HR and its glucuronide conjugates fell rapidly, neither being detectable 8 h after injection. Following oral administration of 14C-mono-HR, mono-HR-glucuronide was detected in plasma, confirming the absorption of mono-HR, and low levels...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hackett AM,Griffiths LA

更新日期：1979-01-01 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：:10 healthy lactating women were treated orally with the anthelmintic praziquantel (Biltricide), and the resulting timedependent concentrations of the unchanged substance in plasma and milk were determined simultaneously. 5 of the women ("1st trial") received the single dose of 50 mg/kg; the other 5 women ("2nd trial")...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Pütter J,Held F

更新日期：1979-01-01 00:00:00

abstract：:We have investigated the in vitro metabolism of three small antimicrobial β(2,2)-amino acid derivatives (M (w) < 500) that are highly potent against methicillin resistant Staphylococcus aureus, and are among the first compounds designed from small cationic antimicrobial peptides with potential ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hansen T,Moe MK,Anderssen T,Strøm MB

更新日期：2012-09-01 00:00:00

abstract：:The metabolic fate of the anti-Parkinsonian drug budipine was studied in rats after oral administration. The presence of an aromatic hydroxylation product, metabolite M1, and its O-sulphate conjugate was confirmed. Three new minor metabolites, budipine N-oxide, metabolite M1 N-oxide and a secondary metabolite derived ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Caputo O,Grosa G,Ceruti M,Rocco F,Biglino G

更新日期：1991-04-01 00:00:00

abstract：:Influence of two newly synthesized bile acids derivates, namely sodium salt of monoketocholic acid MKH-Na and methyl ester of monoketocholic acid MKH-Me on tramadol (12.5 mg/kg oral and intramuscular) analgesic effect was examined in this research. Analgesic effect was measured by antinociceptive hot plate method. Int...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Vasovic V,Vukmirovic S,Pjevic M,Mikov I,Mikov M,Jakovljevic V

更新日期：2010-09-01 00:00:00

abstract：:BACKGROUND AND OBJECTIVE: Efavirenz is commonly used in Africa and is frequently associated with neurocognitive toxicity, which may compromise clinical outcomes. Older individuals are at increased risk for drug toxicity and clinical outcomes may be worse in older age, particularly among those individuals with cytochro...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Torgersen J,Bellamy SL,Ratshaa B,Han X,Mosepele M,Zuppa AF,Vujkovic M,Steenhoff AP,Bisson GP,Gross R

更新日期：2019-04-01 00:00:00

abstract：:Hepatic distributional volumes were investigated in the in situ perfused rat liver. Perfusion experiments were conducted using Krebs bicarbonate buffer delivered via the portal vein in single-pass mode at a total flow rate of 15 mL/min. A bolus dose of normal erythrocytes (RBC, vascular marker) and Evans blue (EB, ext...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Karabey Y,Sahin S

更新日期：2006-10-01 00:00:00

abstract：:Two positional iodine derivatives of benzoic acid, i.e. ortho- (OIB) and para- (PIB), were used alone and in combination with salicylic acid (SA) to study the effects of plasma binding on their pharmacokinetics. Their lymphatic bioavailability (central lymph), their biotransformation and urinary excretion in rats were...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Lamka J,Láznícek M,Gallová S,Rudisar L,Kvĕtina J

更新日期：1993-07-01 00:00:00

abstract：:Diabetes mellitus is becoming an increasingly prevalent disease that concerns patients and healthcare professionals worldwide. Among many anti-diabetic agents in clinical uses, numerous reports are available on their altered pharmacokinetics because of changes in the expression of drug transporters and metabolic enzym...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Ma L,He L,Wang L,Li L,Lin X,Pan G

更新日期：2016-06-01 00:00:00

abstract：:COR3224 is a new 2-amino-2 oxazoline derivative with antidepressant properties. The distribution, excretion and metabolism of radiochemically labelled 14C-COR3224 has been investigated in the rat after intravenous injection. The compound was widely distributed and rapidly excreted. Hydroxylation and sulphate conjugati...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Neau B,Damaj I,Lambrey B,Akbaraly JP,Roux J,Perrissoud D,Jacquot J

更新日期：1991-01-01 00:00:00

abstract：:Pharmacokinetics of ketoprofen (KTP) enantiomers has been studied in patients with rheumatoid arthritis (RA) following administration of a single oral dose of 100 mg rac-KTP during multidrug therapy taking into consideration the genotype of RA patients Concentrations of (-)-R and (+)-S enantiomers of KTP in plasma, ur...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Główka F,Karaźniewicz-Łada M,Grześkowiak E,Rogozinska D,Romanowski W

更新日期：2011-09-01 00:00:00