健康志愿者口服大量剂量利福平的药动学

 目的 研究健康志愿者 po 利福平胶囊(0.6 g)的药动学。方法 高效液相色谱法测定人血清中利福平及其代谢物，薄层色谱分离代谢物，以二极管阵列检测器进行定性。结果 利福平的体内过程符合具有一级吸收的二房室模型，其主要药动学参数t_1/2β,t_max，c_max及AUC分别为(5.17±2.10)h，(1.84±0.68)h，(7.84±4.86)μg·ml^-1，(126.67±34.02)μg·h·ml^-1，利福平体内代谢物主要为21-脱乙酰利福平，血清中21-脱乙酰利福平浓度较长时间维持在4 μg·ml^-1以上。结论 为临床合理用药提供了参考资料。

Pharmacokinetics of rifampin in healthy volunteers after a high oral dose

OBJECTIVE To study the pharmacokinetics of rifampin capsules in healthy volunteers after a high oral dose of 0.6 g. METHODS The serum drug concentration was determined by HPLC.The metabolite of rifampin was separated by TLC and identified by DAD-detector. RESULTS The pharmacokinetics of rifampin was fitted to a two-compartment model with first order absorption.The t_1/2β,t_max，c_maxand AUC of rifampin were (5.17±2.10)h，(1.84±0.68)h，(7.84±4.86)μg·ml^-1，(126.67±34.02)μg·ml^-1·h,respectively.The metabolite of rifampin in human body was 21-desacetylrifampin.Its serum concentration was over 4 μg·ml^-1for a long time. CONCLUSION The study presented some useful information for clinical trails.