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：: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：: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：:The aim of the current investigation was to assess the ability GFJ to modulate the pharmacokinetic profile of paracetamol following single or repeated administrations of GFJ in Sprague-Dawley rats. Diclofenac and carbamazepine were both used as positive controls. Rats received single GFJ or single distilled water dose...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Qinna NA,Ismail OA,Alhussainy TM,Idkaidek NM,Arafat TA

更新日期：2016-04-01 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：: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：: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：:Glutathione S-transferases (GSTs) play an important role in the biotransformation of endogenous compounds and xenobiotics as well as in the metabolic inactivation of pharmacologically active substances, including anticancer drugs. Using cisplatin as the prototype drug, we investigated if any correlation exists between...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Nagar R,Khan AR,Poonia A,Mishra PK,Singh S

更新日期：2015-03-01 00:00:00

abstract：:The effect of silymarin (SMN) on the pharmacokinetics of atorvastatin in diabetic rats was evaluated. Male Wistar rats were assigned into two major groups and then sub-grouped according to the purposes of the study. The first major group was subdivided into three groups (n = 6) including control, non-treated diabetic ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Malekinejad H,Rokhsartalab-Azar S,Hassani-Dizaj S,Alizadeh-Fanalou S,Rezabakhsh A,Amniattalab A

更新日期：2014-12-01 00:00:00

abstract：:The main objective of this study was to investigate the release and pharmacokinetic profiles of ketoprofen (KP) from developed thermosensitive and mucoadhesive liquid suppositories. Thermosensitive liquid suppositories were prepared using KP, poloxamer 407 (P 407), poloxamer 188 (P 188) and various amounts of differen...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Ozgüney I,Kardhiqi A,Yıldız G,Ertan G

更新日期：2014-12-01 00:00:00

abstract：:The transdermally applied dopamine receptor agonist rotigotine is extensively metabolized in the liver. An open-label, parallel-group study was conducted to evaluate the effects of moderate hepatic impairment on the pharmacokinetics, safety and tolerability of rotigotine. Eight subjects with normal hepatic function an...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Cawello W,Fichtner A,Boekens H,Braun M

更新日期：2014-09-01 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：:Danirixin (GSK1325756) is a small, high-affinity, selective and reversible CXCR2 antagonist in development for treatment of chronic obstructive pulmonary disease. The objective of the study was to evaluate the relative bioavailability, including the inter-subject variability, of a conventional immediate-release (IR) f...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Miller BE,Smart K,Mistry S,Ambery CL,Bloomer JC,Connolly P,Sanderson D,Shreeves T,Smith R,Lazaar AL

更新日期：2014-09-01 00:00:00

abstract：:Chinese herbal medicines such as hawthorn, salvia, etc., are frequently combined with statins so as to treat cardiovascular diseases more effectively. Chinese herbal medicines contain many kinds of active components, which may have drug-drug interactions with statins. This study aims to explore the effect and mechanis...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hua WJ,Hua WX,Nan FY,Jiang WA,Yan C

更新日期：2014-09-01 00:00:00

abstract：:For many drugs administered per os, high variability in the concentration-time (C-T) values from first sampling to the phase of distribution may cause difficulty in pharmacokinetic analysis. Therefore, the aim of this study was to propose a method of transformation of C-T data, which would allow significantly reducing...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Grabowski T,Jaroszewski JJ,Piotrowski W,Sasinowska-Motyl M

更新日期：2014-06-01 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：:Astragalus injection (AI) and Astragalus granules (AG) are the two representative clinical preparations from Astragali Radix. In order to investigate the regulation of metabolism, AI and AG were tested for their ability to affect the major enzyme cytochrome P450 3A isoforms in vivo and in vitro. In the study of CYP3A1...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Zhang Y,Huang L,Bi H,Cui Y,Li J,Wang X,Qin X,Chen J,Huang M

更新日期：2013-06-01 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：:Pomegranate juice (PJ) is known to be a potent inhibitor of human cytochrome enzymes. The purpose of this study was to investigate the effect of acute and chronic PJ on the pharmacokinetics of oral nitrendipine (10 mg/kg) in rabbits. Male New Zealand rabbits were pretreated with PJ for 1 week and on the last day, a si...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Voruganti S,Rapolu K,Tota S,Yamsani SK,Yamsani MR

更新日期：2012-06-01 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：:Sertraline potently inhibits cytochrome P450 2B6 (CYP2B6) in vitro. Bupropion is commonly co-prescribed with sertraline and is exclusively metabolized by CYP2B6 to its major active metabolite hydroxybupropion. Putatively the co-administration of bupropion and sertraline could lead to a significant pharmacokinetic drug...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Molnari JC,Hassan HE,Myers AL

更新日期：2012-03-01 00:00:00

abstract：:Previous studies have indicated that borneol has double side effects on the central nervous system (CNS), but the mechanism is unknown. The aim of this study was to clarify the relationship between excitation ratio [contents of excitatory amino acids (AAs) versus that of inhibitory] and the content of natural borneol ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Li WR,Chen RY,Yang L,Huang TL,Xu QW,Mi SQ,Wang NS

更新日期：2012-03-01 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 in vivo assessment of percutaneous absorption of molecules is a very important step in the evaluation of any transdermal drug delivery system and a key goal in the design and optimization of transdermal dosage forms lies in understanding the factors that determine a good in vivo performance. The objective of the p...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Swain K,Pattnaik S,Yeasmin N,Mallick S

更新日期：2011-12-01 00:00:00

abstract：:Blood loss during cesarean section was calculated based on post-operative decrement of hemoglobin (Hb) and hematocrit (Hct) level. The model used for pregnant women was previously validated for non-pregnant women who underwent gynecological surgery. 1,068 pregnant women who underwent cesarean section and 517 women who...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Milosevic N,Popovic J,Grujic Z,Rapaic M

更新日期：2011-09-01 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

abstract：:A simple and sensitive HPLC method has been developed and validated for the determination of tyrosol galactoside (TG) in rat plasma. After one-step protein precipitation with methanol, plasma samples were separated on an Ultimate AQ-C18 column (150 mm×4.6 mm, 5 μm) using acetonitrile-water (7:93, v/v) as mobile phase ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Wang Q,Wang Y,Deng Y,Shi T,Liu X,Sun X,Li X,Zhou D

更新日期：2011-01-01 00:00:00

abstract：:This study examined the effects of the absorption enhancers, acylcarnitines, on efflux transporting systems, including P-glycoprotein (P-gp) and other efflux transporters, and elucidated the importance of acyl chain length and the concentration of acylcarnitine on the activity of efflux transport. The effects of two a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Tomita M,Doi N,Hayashi M

更新日期：2010-09-01 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：: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：: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：OBJECTIVE:By using a population pharmacokinetic analysis method, we predicted the efficacy of Ceftriaxone (CTRX) based on the pharmacokinetics of CTRX in Japanese adults and the sensitivity of infective organisms to CTRX in 2004. In addition, we clarified the difference in efficacy between once-a-day administration and...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Iida S,Kinoshita H,Kawanishi T,Hayashi M

更新日期：2009-04-01 00:00:00

abstract：:Torcetrapib was the lead candidate belonging to the class of cholesteryl ester transfer protein (CETP) inhibitor which was being developed for the management of cardiovascular risk factors by raising HDL. The availability of pharmacokinetic parameters (clearance: CL/F, volume of distribution: Vd/F, elimination rate co...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Mullangi R,Ahlawat P,Trivedi RK,Srinivas NR

更新日期：2009-01-01 00:00:00

abstract：:In the last years there appeared many articles about the adverse influence of non-steroidal anti-inflammatory drugs on the liver and heart. This study is concerned with the influence of the duration of treatment with diclofenac and ketoprofen on the macroscopic and microscopic changes in the liver, lungs, heart, and k...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Tomic Z,Milijasevic B,Sabo A,Dusan L,Jakovljevic V,Mikov M,Majda S,Vasovic V

更新日期：2008-10-01 00:00:00

abstract：:Hyaluronic acid (HA), is a high molecular weight (HMW) glucosaminoglycan with significant acitivity, and which influences a number of physiological and pathological processes such as tumorogenesis, arthritis, etc. The aim of this study was to determine the difference in the biodistributional pathways of 111In-labeled ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Svanovsky E,Velebny V,Laznickova A,Laznicek M

更新日期：2008-07-01 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：:The co-administration of lidocaine and propranolol leads to significant drug-drug interactions. Beta-blockers decrease liver perfusion and inhibit the activity of hepatic microsomal lidocaine metabolizing enzymes of the P450_2D subfamily. Hence, there is a resulting reduction in the hepatic breakdown of lidocaine and ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Tesseromatis C,Kotsiou A,Tsagataki M,Tigka E,Vovou J,Alevizou A,Perisanidis C,Saranteas T,Karakitsos D,Karabinis A,Kostopanagiotou G

更新日期：2007-10-01 00:00:00

abstract：:The aim of the present study was to investigate the relative bioavailability and bioequivalence of a new tablet formulation of metformin hydrochloride with reference to a standard product in healthy Chinese adult male volunteers. Two randomized, comparative, two-way crossover studies were therefore conducted. In study...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Li J,Jin Y,Wang TY,Lü XW,Li YH

更新日期：2007-01-01 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：: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