石杉碱甲片人体生物等效性研究

 目的建立测定血浆中石杉碱甲浓度的HPLC-MS/MS方法,研究不同厂家生产石杉碱甲片之间的生物等效性。方法采用随机交叉口服2种石杉碱甲片试验设计,对20名健康受试者口服石杉碱甲片受试制剂和参比制剂后36 h内多点抽取静脉血进行血药浓度检测,求算有关药动学参数和受试制剂的相对生物利用度。结果20名健康受试者口服石杉碱甲制剂(相当于石杉碱甲100μg)的药动学参数,参比制剂和受试制剂的t_max分别为(0.80±0.17)和(0.76±0.19)h;ρ_max分别为(0.728±0.16)和(0.728±0.17)μg·L^-1;t_1/2分别为(11.90±1.15)和(12.04±1.38)h;采用梯形法计算,AUC_0-t分别为(7.61±1.22)和(7.47±1.12)μg·h·L^-1,AUC_0-∞分别为(8.63±1.32)和(8.54±1.35)μg·h·L^-1;以AUC_0-t计算,受试制剂的相对生物利用度为(98.6±7.3)%。结论受试制剂与参比制剂生物等效。

Study on Pharmacokintics and Bioequivalence of Two Huperzine A Tablets in Healthy Volunteers

OBJECTIVE To develop a HPLC-MS/MS for evaluating the bioequivalence of huperzine A test tablets and reference tablets in the healthy volunteers.METHODS An oral dose of 100 μg huperzine A test preparation or reference preparation was given to 20 healthy male volunteers in a randomized two-period crossover study.Huperzine A concentrations in plasma were determined by HPLC-MS/MS assay.RESULTS The pharmacokinetic parameters of huperzine A test tablets and reference tablets were shown as follows:t_max(0.80±0.17) and(0.76±0.19)h,ρ_max(0.728±0.16) and(0.728±0.17) μg·L^-1,t_1/2(11.90±1.15) and(12.04±1.38)h,AUC_0-t(7.61±1.22) and(7.47±1.12)μg·h·L^-1,AUC_0-∞(8.63±1.32) and(8.54±1.35) μg·h·L^-1.The relative bioavailability of test preparation was(98.6±7.3)% by AUC_0-t.CONCLUSION The two preparations were bioequivalent according to the statistical analysis.