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洛美沙星和环丙沙星与奥美拉唑的相互作用研究及比较药代动力学

Interaction study of lomefloxacin and ciprofloxacin with omeprazole and comparative pharmacokinetics.

作者信息

Stuht H, Lode H, Koeppe P, Rost K L, Schaberg T

机构信息

Department of Infectious and Chest Diseases, City Hospital Zehlendorf/Heckeshorn, Berlin, Federal Republic of Germany.

出版信息

Antimicrob Agents Chemother. 1995 May;39(5):1045-9. doi: 10.1128/AAC.39.5.1045.

Abstract

To assess whether or not concomitant omeprazole treatment influences the pharmacokinetics of lomefloxacin and ciprofloxacin, a randomized, double-blind four-way-crossover study was performed. Another objective was to compare the pharmacokinetics of lomefloxacin and ciprofloxacin. Twelve healthy volunteers participated. On days 1 to 4 of each study period, each of them took 20 mg of omeprazole or a placebo orally, and on day 4, each took 400 mg of lomefloxacin or 500 mg of ciprofloxacin orally. Blood and urine samples were collected and assayed for the quinolones by high-pressure liquid chromatography. The mean peak concentrations in plasma (Cmax) and the areas under the curves (AUC), respectively, of lomefloxacin and ciprofloxacin, respectively, after prior treatment with placebo were 2.88 +/- 0.73 (mean +/- standard deviation) as against 2.60 +/- 0.76 micrograms/ml and 24.9 +/- 3.13 as against 11.9 +/- 1.89 micrograms.h/ml, and 72.4% +/- 5.10% as against 36.1% +/- 7.50% of the doses of lomefloxacin and ciprofloxacin, respectively, were recovered from the urine. None of the pharmacokinetic parameters differed significantly after prior treatment with omeprazole compared with placebo. The Cmax of lomefloxacin was not significantly higher than that of ciprofloxacin, but lomefloxacin's AUC reached twice that of ciprofloxacin because of its significantly longer half-life in plasma (6.68 +/- 1.94 as against 4.15 +/- 0.92 h, respectively, P < or = 0.01). Concomitant therapy with omeprazole did not alter the pharmacokinetics of lomefloxacin or ciprofloxacin in these single-dose studies.

摘要

为评估奥美拉唑联合治疗是否会影响洛美沙星和环丙沙星的药代动力学,进行了一项随机、双盲、四交叉研究。另一个目的是比较洛美沙星和环丙沙星的药代动力学。12名健康志愿者参与了研究。在每个研究周期的第1至4天,他们每人口服20mg奥美拉唑或安慰剂,在第4天,每人再口服400mg洛美沙星或500mg环丙沙星。采集血样和尿样,采用高压液相色谱法测定喹诺酮类药物含量。安慰剂预处理后,洛美沙星和环丙沙星的血浆平均峰浓度(Cmax)及曲线下面积(AUC)分别为2.88±0.73(平均值±标准差)与2.60±0.76μg/ml,以及24.9±3.13与11.9±1.89μg·h/ml,洛美沙星和环丙沙星分别有72.4%±5.10%和36.1%±7.50%的剂量从尿中回收。与安慰剂相比,奥美拉唑预处理后的药代动力学参数均无显著差异。洛美沙星的Cmax并不显著高于环丙沙星,但洛美沙星的AUC是环丙沙星的两倍,因为其血浆半衰期显著更长(分别为6.68±1.94与4.15±0.92小时,P≤0.01)。在这些单剂量研究中,奥美拉唑联合治疗未改变洛美沙星或环丙沙星的药代动力学。

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