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目的:研究单剂量和多剂量口服给予普卢利沙星胶囊的药动学。方法:12名健康成年受试者按3×3拉丁方随机分组,分别单次口服132、264、528mg普卢利沙星胶囊,多次口服264mg普卢利沙星胶囊,连续6d。采用高效液相色谱法测定给药后不同时间普卢利沙星代谢产物NM394的血药浓度。应用DASver1·0软件进行模拟拟合及参数计算。结果:12名受试者全部完成单次给药试验,试验期间未发生任何药品不良反应。各受试者血样中检测不到普卢利沙星,只能测定其代谢产物NM394。高、中、低3个剂量组均符合二室模型,在人体内的药动学过程符合一级动力学,无性别差异。多次给药未见蓄积现象和药动学参数的改变,表明本品无自身酶抑制或诱导作用。结论:本方法灵敏、准确、可靠、特异性强,可满足普卢利沙星临床药动学试验要求,其参数与国外文献报道一致,在我国成人中无性别差异。
OBJECTIVE: To study the pharmacokinetics of prulifloxacin capsules administered orally and in multiple doses. Methods: Twelve healthy adult subjects were randomized into groups of 3 × 3 Latin square. Each group received 132,264,528 mg of prulifloxacin capsules orally, and 264 mg of prulifloxacin capsules orally for 6 days. Plasma concentrations of promethazine metabolite NM394 at different times after administration were determined by high performance liquid chromatography. Application software DASver1.0 simulation and parameter calculation. Results: All the 12 subjects completed the single-dose test. No adverse drug reactions occurred during the experiment. No prulifloxacin was detected in the blood samples of all the subjects, and only its metabolite NM394 was assayed. The three high, middle and low dose groups all fit the two-compartment model. The pharmacokinetics in the human body are in accordance with the first-order kinetics without gender differences. Multiple administration showed no accumulation phenomenon and pharmacokinetic parameters change, indicating that the goods without their own enzyme inhibition or induction. Conclusion: The method is sensitive, accurate, reliable and specific. It can meet the clinical pharmacokinetic test requirements of prulifloxacin. Its parameters are consistent with those reported in foreign literature. There is no gender difference among adults in our country.