摘要
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（４５０ｍｇ）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±０．９３ｈ和６．１３±１．７７ｈ达到峰值５．１１±１．８μｇ／ｍｌ和５．０７±１．９μｇ／ｍｌ。两种制剂的消除半衰期分别为１６．３±１．２ｈ和１５．６±１．１ｈ，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。
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 1 0 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± 1.9μg/ml at 4. 67±0. 93 and6. 13±1. 77 h,the terminal elimination half lives were 16.3±1.2 and 15.6±1.1hfor 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.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1996年第5期291-294,共4页
Chinese Pharmaceutical Journal
