3种不同厂家环孢素A胶囊在健康人体的药动学和生物等效性

 目的研究3种环孢素A胶囊在健康中国人体内的药动学和生物等效性。方法健康志愿者18名,采用简化三交叉试验设计,单剂量口服试验或参比制剂200mg;于服药后48h内,抽取静脉血;用高效液相色谱法测定全血中环孢素A的含量;用DAS软件计算药动学参数并评价3种制剂的生物等效性。结果参比制剂新山地明及两种试验制剂因普兰他和田可的主要药动学参数:ρ_max分别为(947.161±174.985),(758.869±193.539)和(938.711±202.379)μg·L^-1;t_max分别为(1.694±0.645),(2.472±0.581)和(1.861±0.564)h;t_1/2分别为(25.014±17.692),(28.032±14.602)和(28.056±22.927)h;AUC_0-48h分别为(6563.683±1342.601),(6152.483±1066.901)和(6594.165±927.042)μg·h·L^-1;AUC_0-∞分别为(7113.479±1655.657),(6771.877±1240.034)和(7253.950±1228.181)μg·h·L^-1。结论经统计学分析,3种制剂具有生物等效性。

Phannacokinetics and Bioequivalence of Three Preparations of Cyclosporine A in Chinese Healthy Volunteers

OBJECTIVE To study the pharmacokinetics and bioequivalence of cyclosporin A capsules in Chinese healthy volunteers.METHODS Eighteen Chinese healthy male volunteers were involved in the study.Each subject received a single dose of 200 mg cyclosporin A test or reference preparation.Blood sampling was conducted consequently within 48 h.The whole blood concentration were determined by HPLC.The pharmacokinetic parameters were caculated and bioequivalence of three preparations were evaluated by DAS software.RESULTS The main pharmacokinetic parameters were as follows:ρmax were(947.161±174.985),(758.869±193.539) and(938.711±202.379) μg·L^-1;t_max were(1.694±0.645),(2.472±0.581) and(1.861±0.564) h;t_1/2 were(25.014±17.692),(28.032±14.602) and(28.056±22.927) h;AUC_0-48h were(6 563.683±1 342.601),(6 152.483±1 066.901) and(6 594.165±927.042) μg·h·L^-1;AUC_0-∞ were(7 113.479 ±1 655.657),(6 771.877±1 240.034) and(7 253.950±1 228.181) μg·h·L^-1 for Sandimmun,Implanta and Tianke capsules,respectively.CONCLUSION The result of statistical analysis shows that the three preparations are bioequivalent.