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 acyl (lauroyl and palmitoyl) carnitines on the influx and efflux of lucifer yellow and fluorescein isothiocyanate dextran 4,000, which have characteristic vectorial transport, were examined in Caco-2 cell monolayers. Lauroylcarnitine and palmitoylcarnitine increased influx and decreased efflux of these substrates, in a manner dependent on their concentration and acyl chain lengths by increasing influx and inhibiting efflux of the substrates. The results indicated that both the acyl moiety and long acyl chains play important roles in the modification of influx and efflux transport. Because no marked changes in the levels of P-gp protein or the leakage of LDH were observed at 1 h after the application of acylcarnitines, it was concluded that these acylcarnitines had an effect on modulation of the function of P-gp or other efflux transporters without cytotoxicity.
journal_name
Eur J Drug Metab Pharmacokinetjournal_title
European journal of drug metabolism and pharmacokineticsauthors
Tomita M,Doi N,Hayashi Mdoi
10.1007/s13318-010-0001-1subject
Has Abstractpub_date
2010-09-01 00:00:00pages
1-7issue
1-2eissn
0378-7966issn
2107-0180journal_volume
35pub_type
杂志文章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
pub_type： 杂志文章
doi：10.1007/BF03188812
更新日期：1993-07-01 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
pub_type： 杂志文章
doi：10.1007/BF03190639
更新日期：2006-01-01 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
pub_type： 杂志文章
doi：10.1007/s13318-018-0485-7
更新日期：2018-12-01 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
pub_type： 杂志文章,随机对照试验
doi：10.1007/s13318-015-0316-z
更新日期：2017-02-01 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
pub_type： 杂志文章
doi：10.1007/BF03189852
更新日期：1986-07-01 00:00:00
abstract：:The disposition of the gonadotropin-releasing hormone (GnRH) agonist buserelin was studied in male rats under conditions of long-term administration. Rats were continuously infused with about 30 pmole [3H]-buserelin/24 h subcutaneously by osmotic minipumps for 4-7 days. After killing the rats, the 3H-activity of the t...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189737
更新日期：1996-10-01 00:00:00
abstract：BACKGROUND AND OBJECTIVE:Ginseng is usually consumed as a dietary supplement for health care in the normal state or prescribed as a herbal medicine in pathologic conditions. Although metabolic studies of ginseng are commonly performed on healthy organisms, the metabolic characteristics in pathologic organisms remain un...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-020-00645-1
更新日期：2021-01-01 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
pub_type： 杂志文章
doi：10.1007/BF03189669
更新日期：1995-07-01 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
pub_type： 杂志文章
doi：10.1007/BF03189110
更新日期：1986-10-01 00:00:00
abstract：:This paper deals with press-coated modified release tablets in which the drug dose is situated in the core or is divided between the core and the coat. The coat contains polymer (sodium alginate or hydroxypropylmethyl cellulose, HPMC) to control drug release. The main objective was to investigate how the pharmacokinet...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/BF03189338
更新日期：1998-04-01 00:00:00
abstract：:Microcomputers have been used in pharmacokinetics for several years, but their use in the area of formulation is a new application. By using appropriate data on the drug, the dosage form required and its mechanism of absorption and clearance, microcomputers can systematize and speed-up formulation, simplify manufactur...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/BF03189611
更新日期：1984-04-01 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
pub_type： 杂志文章
doi：10.1007/BF03191128
更新日期：2006-04-01 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
pub_type： 杂志文章
doi：10.1007/BF03188855
更新日期：1994-10-01 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
pub_type： 杂志文章
doi：10.1007/s13318-014-0187-8
更新日期：2014-09-01 00:00:00
abstract：:Parenteral phenytoin solution (Dilantin) was given rectally three times a day for three days to two beagle dogs. This was well tolerated, with no evidence of mucosal irritation noted either on endoscopic nor on rectal mucosal biopsy. When given in this manner, phenytoin is absorbed to a limited degree in canines. Pare...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190088
更新日期：1988-10-01 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
pub_type： 杂志文章
doi：10.1007/s13318-012-0086-9
更新日期：2012-09-01 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
pub_type： 杂志文章
doi：10.1007/s13318-018-00538-4
更新日期：2019-08-01 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
pub_type： 杂志文章
doi：10.1007/BF03189616
更新日期：1984-04-01 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
pub_type： 杂志文章
doi：10.1007/s13318-013-0121-5
更新日期：2013-12-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Mast cell-mediated allergic diseases are a significant global health problem. Nitric oxide (NO) produced by acute type 1 allergies greatly suppresses hepatic cytochrome P450 (CYP) metabolism. A recent in vitro study demonstrated that repeated FcεRI-mediated activation intrinsically modulates m...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-018-0527-1
更新日期：2019-06-01 00:00:00
abstract：:Relative bioavailability of cisapride was investigated after oral administration of a test versus a reference formulation of immediate release tablets of cisapride, both with 10 mg per unit. The study was conducted in a two-way cross-over design, as a single dose open-label randomised trial. The two formulations were ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/BF03192297
更新日期：1998-07-01 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
pub_type： 杂志文章
doi：10.1007/BF03189844
更新日期：1986-07-01 00:00:00
abstract：:The pharmacokinetics of lisuride hydrogen maleate (LHM) were investigated in rat, rabbit and rhesus monkey. Experiments were designed to meet not only the requirements of drug registration but also to serve other preclinical disciplines (toxicology, pharmacology). LHM is absorbed almost completely at a dose level of 1...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189490
更新日期：1981-01-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:UPARANT has emerged as a novel therapeutic agent with the potential to treat ocular diseases as assessed by studies in animal models. Since limited information is available on the pharmacokinetics of UPARANT, the aim of this study is to evaluate its pharmacokinetics after single and multiple a...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-020-00654-0
更新日期：2021-01-01 00:00:00
abstract：:The liver first pass effect of pinazepam in four anaesthetized rabbits was determined by measuring the concentrations of this compound and those of its metabolite N-desmethyldiazepam in the plasma from the portal and hepatic veins. Anaesthesia was induced with an i.p. injection of urethane (1.5 g/kg). Portal and hepat...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03188728
更新日期：1982-01-01 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
pub_type： 杂志文章
doi：10.1007/BF03191385
更新日期：2009-01-01 00:00:00
abstract：:The hypoxic cell radiosensitizing drug, misonidazole (Miso) (Ro 07-0582) and its demethylated metabolite were administered to Wistar rats at different dose levels to examine their renal elimination. The data were consistent with a model in which Miso is eliminated mainly after biotransformation into desmethylmisonidaz...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189740
更新日期：1985-07-01 00:00:00
abstract：:The pharmacokinetics of tolbutamide (TB) have been studied in endotoxin pretreated rats with the aim of evaluating TB as a marker for endotoxin effects. Endotoxin dose of 10 mg/kg resulted in a 50% rate of mortality. TB was i.v. administered 24 h. after endotoxin dosing. Clearance (Cl) decreased by approximately 2/3 o...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190205
更新日期：1990-07-01 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
pub_type： 杂志文章
doi：
更新日期：1991-01-01 00:00:00
abstract：:Apomorphine was administered subcutaneously and intranasally to 7 patients suffering from Parkinsonism with 'on-off' problems. This comparative pharmacokinetic study showed that the two routes of administration are comparable with respect to absorption kinetics. Apomorphine is rapidly absorbed when administered intran...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章
doi：10.1007/BF03192285
更新日期：1995-01-01 00:00:00
