4-Hydroxy-5-oxo-4,5-dihydrobenzo(a)pyrene, a new metabolite of benzo(a)pyrene.

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：:Tectorigenin (Te) is a main active component in the flowers of Pueraria thomsonii Benth. and the rhizomes of Belamcanda chinensis (L.) DC. Previously, we have reported the pharmacokinetic properties of Te in rat plasma. The purpose of this study was to investigate the urinary excretion of Te after oral administration ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Shi Z,Zhang G,Zhao L,Wang S,Kano Y,Yuan D

更新日期：2015-09-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Fufang Danshen formula, a famous Chinese patent medicine containing Salvia miltiorrhiza, Panax notoginseng and borneol, has been widely used in the treatment of coronary heart disease. The application is restricted by low bioavailability partly due to Panax notoginseng saponins (PNS) instabilit...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Chen XN,Li DQ,Zhao MD,Yu GY,Du SY,Lu Y,Bai J,Li PY,Wu YL,Tian ZH,Zeng YY

更新日期：2018-04-01 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 purpose of this study was to determine the distribution of cyclosporin A (CsA) in various ocular fluids and tissues in the rabbit by two routes of administration. CsA was administered to two groups of two rabbits either by intramuscular route at a dose of 25 mg/kg/day or by local route using eyedrops, at a dose of...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Vernillet L,Lundh RL,Acezat-Mispelter F,Goizel C,Humbert H,Pouliquen Y

更新日期：1991-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Maximum plasma concentration of biopharmaceuticals sometimes occurs long after completion of intravenous infusion. The objective of this research was to study the hypothetical adsorption of biopharmaceuticals to endothelium and infusion material, which may theoretically explain this phenomenon...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Reijers JAA,Dane MJC,van Zonneveld AJ,Burggraaf J,Moerland M

更新日期：2018-02-01 00:00:00

abstract：:The metabolic fate of anti-inflammatory agent 2-(5-ethylpyridin-2-yl)benzimidazole (KB-1043) was studied in rats after oral administration. An average of 12.2 +/- 1.5% of the dose was excreted in the urine in the course of 0-48 h; 56.7 +/- 2.6% with feces. Two metabolites were also detected in the urine and isolated b...

journal_title：European journal of drug metabolism and pharmacokinetics

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

更新日期：1989-10-01 00:00:00

abstract：:The metabolism of (-)-(S)-nicotine has been investigated following intratracheal administration to the recirculating perfused rabbit lung model. The metabolic products present in the perfusate were identified by co-chromatography (HPLC and GC) with authentic standards and quantified by HPLC. After the 180 min perfusio...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Aislaitner G,Bello A,Tan SC,Hutt AJ,Marriott C,Gorrod JW

更新日期：1997-10-01 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：: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：BACKGROUND AND OBJECTIVES:Acetaminophen (APAP, paracetamol) is currently the principal cause of acute liver failure in both the USA and the UK. However, relatively little is known about the influence of genes and race/ethnicity on the disposition of APAP and the extent to which genetic variation and ethnicity may predi...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Zurlinden TJ,Reisfeld B

更新日期：2017-02-01 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 disposition kinetics of the N-oxide of picobenzide were studied after administration to rabbits at a bolus dose of 30 mg/kg of picobenzide intravenously. The biotransformation process fits a first-order kinetic process, and the metabolite shows good access capacity to the peripheral compartment. The N-oxide of pic...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Santos Buelga D,Mariño EL,Domínguez-Gil A

更新日期：1989-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Polyethylene glycol-modified canine uricase (PEG-UHC) prepared with a lower-molecular-weight (5 kDa) PEG is used to treat gout. This study investigated the comparative pharmacokinetics of single and multiple doses of PEG-UHC administered intravenously and a single dose of uricase (UHC) administ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Li H,Huo J,Sun D,Jiang L,Hu C,Bai Y,Ma X,Zhang H,Shi X,Zhao Z,Zhou J,Lu Y,Zhang C

更新日期：2020-08-01 00:00:00

abstract：:Recent evidences suggest that genetic CYP2C19 polymorphism plays a role in the development of treatment resistance for clopidogrel's antiplatelet therapy. This short communication puts forward some strategies that could be potentially used to overcome the genetic polymorphism associated hurdles. While there is some es...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Srinivas NR

更新日期：2009-07-01 00:00:00

abstract：:This study investigated the effect of a commercial preparation of stevioside and a synthetic compound, sodium salt of monketocholic acid (MKC), administered per os (p.o.) and also adminstered via an osmotic pump, on glycemia in normoglycemic and diabetic Wistar rats. Diabetes was induced with alloxan, 100 mg/kg, i.p. ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Rasković A,Mikov M,Skrbić R,Jakovljević V,Vasović V,Posa M,Kuhajda K,Kevresan S,Tomic Z,Siladji D

更新日期：2008-01-01 00:00:00

abstract：:SC-46264 is an antagonist of the alpha 2-adrenergic receptor. Distribution and excretion of [14C]-SC-46264 were studied after single and repeated daily oral administrations to the Cynomolgus monkey at a 1.5 mg/kg dose. After a single oral administration, more than 95% of the administered dose was recovered within 48 h...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Jacqmin P,Hérin M,Cavalier R,Lesne M

更新日期：1993-07-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Chalcone constitutes one of the most used molecular frameworks in medicinal chemistry and its derivatives exhibit a broad spectrum of biological activities. Low absolute bioavailability, poor distribution, intensive metabolism and elimination of chalcones are the main problems in designing new...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Okoniewska K,Konieczny MT,Lemke K,Grabowski T

更新日期：2017-02-01 00:00:00

abstract：:Benzo[alpha]pyrene (B[a]P) is a product derived from incomplete combustion of organic material and is considered responsible for chemically-induced cancer in humans. In the present study, the levels of noradrenaline (NA), dopamine (DA), dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA), 5-hydroxytryptamine (...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Stephanou P,Konstandi M,Pappas P,Marselos M

更新日期：1998-10-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Hydronidone is a novel pyridine derivative with therapeutic potential for hepatic fibrosis. The aim of this study was to investigate the safety, tolerability, and pharmacokinetics of hydronidone in healthy subjects. Effects of sex and food on hydronidone pharmacokinetics were also evaluated. ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Liu Y,Wu J,Li Z,Luo Y,Zeng F,Shi S

更新日期：2017-02-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Drug-drug interactions (DDIs) can occur when one drug alters the metabolism of another drug. Drug metabolism mediated by cytochrome P450 enzymes (CYPs) is responsible for the majority of metabolism of known drugs and inhibition of CYP enzymes is a well-known cause of DDIs. In the current study...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Reinen J,Smit M,Wenker M

更新日期：2018-12-01 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

abstract：:The MDR modulator, OC144-093, is a potential candidate for use in cancer therapy and exhibits potent biological activity in vitro and in vivo when combined with anticancer agents such as paclitaxel. Its inhibitory interaction with P-glycoprotein (Pgp), the mdr1 gene product and a mechanistic participant in multidrug r...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Guns ES,Denyssevych T,Dixon R,Bally MB,Mayer L

更新日期：2002-04-01 00:00:00

abstract：BACKGROUND:MTBH, a novel hesperetin derivative, possesses in vivo hepatoprotective effects against carbon tetrachloride (CCl4)-induced acute liver injury in Institute of Cancer Research (ICR) mice. OBJECTIVES:This study investigated the pharmacokinetics and tissue distribution of MTBH and its conjugated metabolites in...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Shen C,Qian Z,Chen R,Meng X,Hu T,Chen Z,Li Y,Huang C,Hu C,Li J

更新日期：2016-12-01 00:00:00

abstract：:Herbal medicinal products have to meet comparable standards concerning the assessment of efficacy, safety and (bio)pharmaceutical quality as chemically defined synthetic drugs. However, these requirements are not fulfilled for many herbal products so far, particularly regarding in vitro dissolution and in vivo bioavai...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Blume HH,Schug BS

更新日期：2000-01-01 00:00:00

abstract：:Penbutolol is a not cardioselective beta-adrenergic blocking drug; it is lipid soluble and differs in its protein binding from the other members of its group because shows linkage to alpha 1-glycoprotein, with no detectable binding to albumin. AAG levels change during pregnancy and so the binding of [3H]-penbutolol wa...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Aquirre C,Rodriguez-Sasiain JM,Navajas P,Calvo R

更新日期：1988-01-01 00:00:00

abstract：:Bioavailability of lansoprazole, a new gastric proton pump inhibitor, was investigated in 12 healthy subjects. Each subject received in random order, lansoprazole (30 mg) alone or associated with standard meal or with antacids (aluminium and magnesium hydroxides) or one hour later than antacids. Lansoprazole and metab...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Delhotal-Landes B,Cournot A,Vermerie N,Dellatolas F,Benoit M,Flouvat B

更新日期：1991-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Methyl 3,4-dihydroxybenzoate (MDHB) has the potential to prevent neurodegenerative diseases (NDDs). The present work aims to reveal the pharmacokinetics and tissue distribution characteristics of MDHB. METHODS:The pharmacokinetics and tissue distribution of MDHB were analyzed using LC-MS/MS a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Wang JH,Hu SH,Su JY,Pan JP,Mi XN,Geng HJ,Zhang W,Cai L,Su CF,Hong AH,Luo HM

更新日期：2019-04-01 00:00:00

abstract：:Carboxylesterases (CESs) play major roles in catalyzing the hydrolysis of a wide range of ester- and amide-containing compounds. CESs dominate both the biotransformation of numerous therapeutic drugs and the detoxification of environmental toxicants, and the activity alteration of CESs may be a determinant reason for ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Xu Y,Zhang C,He W,Liu D

更新日期：2016-08-01 00:00:00

abstract：:A comparative bioavailability study was undertaken between a new formulation of rifampicin 'Famcin' and a standard formulation of rifampicin 'R-cin' in eight healthy male volunteers at two dose levels: 300 mg and 450 mg given orally under both single dose and steady state conditions. Plasma rifampicin was assayed spec...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Garg SK,Chakrabarti A,Panigrahi D,Sharma M,Talwar P,Kumar N,Sharma PL

更新日期：1991-07-01 00:00:00