利福喷丁软胶囊的药动学和相对生物利用度

 目的：研究利福喷丁软胶囊在正常中国人体内的药物动力学，并对其生物等效性进行评价。方法：10名健康志愿者随机交叉口服单剂量(450 mg)利福喷丁软胶囊或硬胶囊。采用HPLC测定血浆中的血药浓度。结果：血浆中药物浓度分别在4.67±0.93 h和6.13±1.77 h达到峰值5.11±1.8 μg/ml和5.07±1.9 μg/ml。两种制剂的消除半衰期分别为16.3±1.2 h和15.6±1.1 h,血药浓度曲线下面积分别为143.2±52.0和149.6±58.9 (μg·h)/ml。药时曲线符合一级吸收的单室模型；利福喷丁软胶囊的相对生物利用度为97.6%±12.3%。结论：经统计分析，利福喷丁软胶囊和硬胶囊在正常人体内的药动学性质相似，两者具有生物等效性。

Pharmacokinetics and relative bioavailability of rifapentine

OBJECTIVE:To study the pharmacokinetics of rifapentine soft capsule in normal volunteers and to assess the bioequivalence.METHODS:The pharmacokinetics of rifapentine was determined following a single oral dose of 450 mg was given to 10 volunteers in an open randomized crossover study.Drug concentration in plasma was assayed by HPLC method.RESULTS:The peak levels in plasma averaged 5.11±1.8 and 5.07±1.9 μg/ml at 4.67±0.93 and 6.13±1.77 h,the terminal elimination half lives were 16.3±1.2 and 15.6±1.1 h for soft and hard capsule respectively,and the areas under the drug concentration-time curves were 143.2±52.0 and 149.6±58.9 (μg·h)/ml for the two formulations.The concentration-time courses after medication conformed to a 1-compartment open model with a first order absorption.CONCLUSION:The pharmacokinetics of the two formulations of rifapentine was similar and the result of statistical analysis showed that the two formulations were bioequivalent.