Abstract：
:The effect of the concomitant administration of the antifungal drugs ketoconazole (KTC) and itraconazole (ITC) on the pharmacokinetics of ciprofloxacin (CIP) following short- and long-term administration in mice was investigated. Animals received either a dose of CIP (20 mg/kg, i.p.), CIP (20 mg/kg, i.p.) together with KTC (50 mg/kg, p.o.) or CIP (20 mg/kg, i.p.) and ITC (30 mg/kg, p.o.). The same treatments were repeated for 7 days. Blood samples were collected up to 4 h following drug administration and two urine samples were collected at 2 h and 4 h after drug administration. CIP plasma concentrations were significantly higher in KTC- and ITC-treated groups compared with the corresponding control groups. The concomitant administration of KTC or ITC with CIP also significantly (p<0.05) increased C(max), t(1/2), MRT and AUC(0-infinity) with no change in T(max). CIP clearance was significantly reduced by both agents. KTC and ITC reduced CIP urinary excretion. This study suggests that an important pharmacokinetic interaction between CIP and KTC or ITC is likely to occur when either of the two antifungal drugs is administered concomitantly with CIP. The results may suggest possible reductions in total clearance of CIP, owing to inhibition of its renal tubular excretion by KTC and ITC.
journal_name
Biopharm Drug Disposjournal_title
Biopharmaceutics & drug dispositionauthors
Abou-Auda HS,Mustafa AA,Al-Humayyd MSdoi
10.1002/bdd.586subject
Has Abstractpub_date
2008-01-01 00:00:00pages
29-35issue
1eissn
0142-2782issn
1099-081Xjournal_volume
29pub_type
杂志文章abstract：:A relative bioavailability study of conventional tablet of propranolol hydrochloride was conducted in a group of 18 healthy volunteers employing the innovator's product as the reference tablet formation. Based on plasma levels of propranolol for the 24 h following administration of 2 x 40 mg oral propranolol hydrochlo...
journal_title：Biopharmaceutics & drug disposition
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1002/bdd.2510030204
更新日期：1982-04-01 00:00:00
abstract：:The bioavailability of the thiazide diuretic bemetizide from a tablet containing 25 mg of this drug and 50 mg of the chemically unrelated diuretic triamterene was lower than, and significantly different (p less than 0.01) from that from a tablet containing 25 mg bemetizide alone. The mean peak plasma level of bemetizi...
journal_title：Biopharmaceutics & drug disposition
pub_type： 临床试验,杂志文章
doi：10.1002/bdd.2510030409
更新日期：1982-10-01 00:00:00
abstract：:SYL-927, a novel and selective S1P1 agonist, is transferred to its active phosphate for the regulation of lymphocyte recirculation. This in vitro metabolism study is to elucidate the P450-mediated oxidation pathway of SYL-927 in human liver microsomes (HLMs). The results demonstrated that the ω-1 hydroxylated metaboli...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2161
更新日期：2018-11-01 00:00:00
abstract：:MDL 26479 is a new drug undergoing clinical evaluation for the treatment of depression and for memory loss associated with Alzheimer's disease. As part of a dose tolerance trial, the single- (SD) and multiple-dose (MD) pharmacokinetics of MDL 26479 were evaluated in healthy male volunteers. SDs ranging from 2 to 465 m...
journal_title：Biopharmaceutics & drug disposition
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1002/(sici)1099-081x(199705)18:4<325::aid-bdd21
更新日期：1997-05-01 00:00:00
abstract：:Methotrexate (MTX) is an anchor drug used to treat rheumatoid arthritis (RA), but responsiveness is variable in effectiveness and toxicity. Methotrexate and its polyglutamate conjugates (MTXPG(n)) in red blood cells (RBC) have been associated with patient response. In the current study, 13 collagen-induced arthritic (...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.1838
更新日期：2013-05-01 00:00:00
abstract：:A physiologic model to describe bupivacaine uptake by and elimination from brain and heart was developed. Preliminary validation of the model was accomplished by comparing concentration data predicted by the model with those determined in rabbits. The model was modified to examine similarities and differences followin...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2510070204
更新日期：1986-03-01 00:00:00
abstract：:In situ intestinal absorption of baclofen in the rat in the presence of beta-alanine has been investigated. Through the perfusion of 0.50 mM baclofen solutions containing variable concentrations of the aminoacid (from 5 to 100 mM), a partially competitive inhibition of baclofen absorption was characterized: absorption...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2510120903
更新日期：1991-12-01 00:00:00
abstract：:Oral doses of amygdalin and intraperitoneal (i.p.) doses of potassium cyanide (KCN) in the near-lethal range were administered to CD2F1 female mice. Blood cyanide levels were then measured as a function of time. The maximum cyanide level after amygdalin administration was reached at about 11/2 to 2 h and was within th...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2510010409
更新日期：1980-04-01 00:00:00
abstract：:In this comparative bioavailability study in 12 healthy volunteers the blood level profiles of both propranolol and bendrofluazide were studied following the multiple oral administration of the drugs as a fixed combination (Inderetic) and as a free combination at doses of 80 mg propranolol twice daily and 2.5 mg bendr...
journal_title：Biopharmaceutics & drug disposition
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1002/bdd.2510020209
更新日期：1981-04-01 00:00:00
abstract：:Four experimental controlled-release oral solid dosage formulations were developed and the in vitro dissolution characteristics of theophylline from these formulations were studied in USP apparatus I. Pharmacokinetic evaluation of these formulations was carried out in eight beagle dogs under fasting conditions. Theoph...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/(SICI)1099-081X(199604)17:3<259::AID-BDD95
更新日期：1996-04-01 00:00:00
abstract：:Fexofenadine hydrochloride is a non-sedating antihistamine that is used in the treatment of symptoms associated with seasonal allergic rhinitis and chronic idiopathic urticaria. A pooled analysis of pharmacokinetic data from children 6 months to 12 years of age and adults was conducted to identify the dose(s) in child...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.425
更新日期：2004-12-01 00:00:00
abstract：:The comparative bioavailability and steady state fluctuations resulting from the administration of Tegretol 200 mg commercial tablets and carbamazepine OROS controlled delivery tablets were investigated in 22 adult and 12 pediatric epileptic patients. Tegretol commercial tablets were dosed according to previously esta...
journal_title：Biopharmaceutics & drug disposition
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1002/bdd.2510130802
更新日期：1992-11-01 00:00:00
abstract：:The objective of this study was to assess the effect of dietary fibers on the transport of losartan, an angiotensin II type 1 receptor blocker, in small intestinal cells. Using Caco-2 cells in vitro, losartan uptake and transport were evaluated in the presence of various fibers (cellulose, chitosan, sodium alginate an...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2004
更新日期：2016-05-01 00:00:00
abstract：:EXP631, 4-(3-thienyl)-alpha, alpha,1-trimethyl-4-piperidine-methanol hemi-fumarate salt (I), is a centrally acting non-opioid analgesic compound with monoamine uptake blocking properties. EXP631 has analgesic effects in several animal models. It is intended to be used for the treatment of moderate to moderately severe...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2510140608
更新日期：1993-08-01 00:00:00
abstract：:The present study aimed to examine the potential pharmacokinetic drug interaction between valsartan and gemfibrozil. Compared with the control given valsartan (10 mg/kg) alone, the concurrent use of gemfibrozil (10 mg/kg) significantly (p < 0.05) increased the oral exposure of valsartan in rats. In the presence of gem...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2001
更新日期：2016-07-01 00:00:00
abstract：:This study compared the relative ocular bioavailability in rabbits of the antibiotic/steroid combination of 0.3 per cent tobramycin and 0.1 per cent fluorometholone acetate to each of the two single-entity products. Two separate studies were conducted, one measuring fluorometholone acetate in cornea and aqueous humour...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2510080605
更新日期：1987-11-01 00:00:00
abstract：:Regional pharmacokinetics is the study of the drug concentrations in specific regions of the body. It allows greater insight into the mechanisms of drug disposition than the study of systemic blood concentrations. Experimental methods in regional pharmacokinetics and their applications and limitations are reviewed. Po...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章,评审
doi：10.1002/bdd.2510110902
更新日期：1990-12-01 00:00:00
abstract：:The study sought to investigate the effect of genetic variants of OCT1 (OCT1-P283L and -P341L) and OCT2 (OCT2-T199I, -T201M and -A270S), which were identified in a Korean population, on the transport of lamivudine in vitro and to compare the substrate dependent effects of OCT1 and OCT2 variants with 1-methyl-4-phenylp...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.1783
更新日期：2012-04-01 00:00:00
abstract：:When drug-protein binding data are evaluated thermodynamically standard free energy (delta G0), standard enthalpy (delta H0) and standard entropy (delta S0) are usually estimated from association constants (Ka) derived from binding data obtained at only two temperatures. Estimation of delta H0 involves the assumption ...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2510020304
更新日期：1981-07-01 00:00:00
abstract：:A semisolid self-emulsifying system (SES) of itraconazole consisting of oleic acid, polysorbate 80 and coajuvant (citric acid) was prepared by a hot-melt technique and then compared with hydroxypropylmethylcellulose (HPMC) solid dispersion (SD) coated onto inert sugar spheres as a reference formulation for in vitro an...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.546
更新日期：2007-05-01 00:00:00
abstract：:Pharmacokinetic compartment models were constructed to describe the absorption and metabolism of dopamine (DA) and DA prodrug, N-(N-acetyl-L-methionyl)0,0-bis-eth-oxycarbonyl) dopamine(1). Plasma concentrations of DA, DA-SO4, and DOPAC after oral administration of DA to dogs, were analysed using the pharmacokinetic mo...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2510110207
更新日期：1990-03-01 00:00:00
abstract：:Bevirimat is the first drug in the class of maturation inhibitors, which treat HIV infection by disrupting the activity of HIV protease enzyme with a mechanism of action distinct from that of conventional protease inhibitors. The absorption, distribution, metabolism and elimination characteristics of single intravenou...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.625
更新日期：2008-10-01 00:00:00
abstract：:The systemic availability of a solid dispersion (coevaporate) of clofazimine (CLF) in poly(vinyl methyl ether maleic anhydride) copolymer (PVM/MA) was tested in the pig. Single 100 mg oral doses of the coevaporate and the commercial product, Lamprene (Ciba-Geigy) were administered on separate occasions (separated by a...
journal_title：Biopharmaceutics & drug disposition
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1002/bdd.2510150407
更新日期：1994-05-01 00:00:00
abstract：:Understanding the performance of a drug product in vivo plays a key role in the development of meaningful in vitro drug release methodology. In case of functional chewing gums, the mode and the mechanism of release and the site of application differ significantly from other conventional solid oral dosage forms and req...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.1796
更新日期：2012-10-01 00:00:00
abstract：:The purpose of this mechanistic drug interaction study was to investigate the effects of ketoconazole on the pharmacokinetics of safinamide. Ketoconazole was applied as a potent prototypic inhibitor of cytochrome CYP3A4, to determine the role of CYP3A4 in the metabolic clearance of safinamide. In an open-label, random...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章,随机对照试验
doi：10.1002/bdd.1822
更新日期：2012-12-01 00:00:00
abstract：:The pharmacokinetics of mexiletine and its metabolite hydroxy-methyl-mexiletine have been investigated following single-dose and during multiple-dose administration of a sustained-release form of mexiletine to six post-myocardial infarct patients. Comparison of single-dose and washout pharmacokinetics, after short-ter...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2510130702
更新日期：1992-10-01 00:00:00
abstract：:Twenty-six healthy male volunteers received a single 10 mg dose of diazepam on two occasions in a crossover bioequivalence study comparing the reference product (Valium) and a generic formulation (NeoCalme). Concentrations of diazepam and its metabolite, desmethyldiazepam, were determined during 264h after each dose. ...
journal_title：Biopharmaceutics & drug disposition
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1002/bdd.2510100609
更新日期：1989-11-01 00:00:00
abstract：:The urinary elimination of 4-hydroxyamphetamine (PHA) and a series of homologous 4-alkoxy-substituted amphetamines and their metabolites was examined after single and multiple oral administration to pregnant and non-pregnant mice. The metabolic profile and extent of biotransformation in a series of alkoxy analogues we...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.2510140807
更新日期：1993-11-01 00:00:00
abstract：:A chiral gas chromatographic assay previously developed for quantitative analysis of ethosuximide and its major metabolites in rat urine has been adapted for the analysis of the drug in plasma. Ethosuximide, both as a racemic mixture and as the individual enantiomers, was administered to conscious rats by the intraven...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.266
更新日期：2001-03-01 00:00:00
abstract：:Non-steroidal anti-inflammatory drugs (NSAIDs) are used widely to relieve pain and to decrease inflammation. Several clinical studies have reported that NSAIDs inhibit uridine 5'-diphospho-glucuronosyltransferase (UGT) enzymes. Therefore, the study evaluated the inhibitory potential of 15 NSAIDs on the activities of s...
journal_title：Biopharmaceutics & drug disposition
pub_type： 杂志文章
doi：10.1002/bdd.1933
更新日期：2015-05-01 00:00:00
