环孢素国产微乳胶囊与进口微乳胶囊的生物等效性研究

Study on pharmacokinetics and bioavailability of domestic cyclosporin A microemulsion capsule

目的:以进口制剂(Neo)为对照,研究国产环孢素微乳胶囊(NC)在健康人体内的药代动力学及相对生物利用度。方法:选择10例健康志愿者随机交叉口服单剂量国产环孢素微乳胶囊或进口制剂,用荧光偏振免疫分析法测定血药浓度,所得数据采用3P87药代动力学程序拟合。结果:环孢素的药-时曲线符合一级吸收的二室模型,NC和Neo两种制剂的t1／2β分别为(4.89±1.84)、(4.78±1.49)h,tmax分别为(1.89±0.41)、(1.96±0.32)h,cmax分别为(875.26±168.63)、(908.48±167.23)ng·ml-1,国产环孢素微乳胶囊相对于进口制剂的生物利用度为(96.47±8.69)％。结论:2种制剂的药代动力学及生物利用度无显著差异,具有生物等效性。

Objective: To compare the pharmacokinetics and the relative bioavailability of a domestic cyclosporin A (CsA) microemulsion capsule and an imported one. Methods: A single oral dose of New Cyspin (NO capsule or Neoral (Neo) capsule was given to 10 healthy volunteers in a randomized crossover study. Drug concentrations in blood were determined by fluorescence polarization immunoassay. The data were dealt with 3P87 pharmacokinetics program. Results:The concentration-time curve of CsA conformed to first-order absorption and 2 compartment model. The t1/2β, tmax and cmax of NC capsule were (4. 89±1. 84) h,(1. 89 ± 0. 41) h and (875. 26±168. 63) ng · ml-1, respectively, and of Neo capsule were (4. 78± 1. 49) h,(1. 96 ± 0. 32) h and (908. 48±167. 23) ng · ml-1 .respectively. The bioavailability of NC capsule was (96. 47± 8. 69)% of Neo capsule. Conclusion: The pharmacokinetics and bioavailability of NC capsule have no significant differences from those of Neo capsule. NC capsule and Neo capsule are bioequivalent.