MODIFICATION OF CEFIXIME BIOAVAILABILITY BY NIFEDIPINE IN HUMANS - INVOLVEMENT OF THE DIPEPTIDE CARRIER SYSTEM

被引:27
作者
DUVERNE, C
BOUTEN, A
DESLANDES, A
WESTPHAL, JF
TROUVIN, JH
FARINOTTI, R
CARBON, C
机构
[1] HOP BICHAT,DEPT PHARM CLIN & BIOMAT,46 RUE HENRI HUCHARD,F-75877 PARIS 18,FRANCE
[2] HOP BICHAT,INSERM,U13,ETUD INFECT EXPTL & TRAITEMENTS ANTIINFECT LAB,F-75877 PARIS 18,FRANCE
关键词
D O I
10.1128/AAC.36.11.2462
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
We studied the action of nifedipine on the bioavailability of cefixime, a molecule absorbed via the gut wall dipeptide carrier system in the rat, and ou the bioavailability of D-xylose, which is absorbed via a pH (and Na+-)-dependent transporter. Each compound was administered alone or in combination with 20 mg of nifedipine to eight healthy male volunteers. Nifedipine significantly increased the absorption rate of (20.7 +/- 4.3 versus 16 +/- 3.5 mg/h in the absence of nifedipine). The absolute bioavailability of cefixime alone was 31% +/- 6% compared with 53% +/- 1% (P < 0.01) in the presence of nifedipine. ne observed peak concentrations in serum were significantly different (2.5 +/- 0.3 mg/liter without nifedipine and 3.7 +/- 1.1 mg/liter with nifedipine; P < 0.02). In contrast, nifedipine induced no significant differences in the pharmacokinetic profile of xylose following oral administration. We conclude that (i) cefixime is absorbed in humans by an apparently active process which can be enhanced by a calcium channel blocker, in this case, nifedipine; and (ii) nifedipine does not modify the activity of the pentose transporter.
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页码:2462 / 2467
页数:6
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