环孢素A胶囊人体生物利用度及生物等效性研究  

Bioavailability and Bioequivalence of Cyclosporin A Capsules in Human

作　　者：道毅俊[1] 仲珑瑾[1] 李中东[1] 施孝金[1] 钟明康[1] 

机构地区：[1]复旦大学附属华山医院临床药学研究室,上海200040

出　　处：《中国医药工业杂志》2006年第11期749-752,共4页Chinese Journal of Pharmaceuticals

摘　　要：采用两阶段双交叉实验设计,研究了19名健康志愿者单剂量口服环孢素A胶囊(受试制剂)和环孢素A软胶囊(参比制剂)的人体生物利用度及生物等效性。采用HPLC法测定全血中的药物浓度。受试制剂和参比制剂的药动学参数分别为AUC0→24h(7993.0±2535.1)和(8295.6±2295.9)ng·h·ml-1、AUC0→∞(8851.7±2815.0)和(9258.0±2523.7)ng·h·ml-1、Cmax(1500.3±348.8)和(1742.9±361.3)ng/ml、Tmax(2.63±0.55)和(1.39±0.49)h、T1/2(7.11±3.24)和(7.04±2.47)h。经统计分析,前三者药动学参数无显著性差异(P>0.05),两种制剂生物等效,而Tmax则差异较大。According two-stage and two-way crossover design, 19 healthy volunteers were orally administrated by single dose of cyclosporine A capsules （T） and soft capsules （R）, respectively. The bioavailability and bioequivalence of two preparations were discussed. The concentration of cyclosporin A in human whole blood was determined by HPLC. The pharmacokinetic parameters of T and R were AUC0-24h（7993.0±2535.1）and（8295.6±2295.9）ng·h·ml^-1、AUC0-∞（8851.7±2815.0）and（9258.0±2523.7）ng·h·ml^-1、Cmax（1500.3±348.8）and（1742.9±361.3）ng/ml、Tmax（2.63±0.55）和（1.39±0.49）h、T1/2（7.11±3.24）and（7.04±2.47）h, respectively. The statistical analysis results showed that AUC0→24h, AUC0→∞ and Cmax of two preparations were bioequivalent, but there was a significant difference in Tmax.

关 键 词：环孢素A 生物利用度 生物等效性 高效液相色谱 

分 类 号：R969.1[医药卫生—药理学]