石杉碱甲缓释片多剂量给药健康人体药代动力学研究

目的：评价石杉碱甲缓释片多剂量给药在健康人体药代动力学规律。方法：采用双周期自身随机交叉试验设计。24名健康志愿者多次口服试验药石杉碱甲缓释片或参比制剂,采用LC-MS/MS测定血浆中药物浓度,药动学参数采用DAS软件处理获得。结果：试验制剂石杉碱甲缓释片组与参比制剂石杉碱甲普通片组的Cssmin分别为（0.54±0.21）和（0.79±0.20）ng/mL,Cssmax分别为（1.65±0.45）和（1.83±0.37）ng/mL,Css分别为（1.05±0.28）和（1.22±0.28）ng/mL,tmax分别为（3.5±1.9）和（1.1±0.4）h,AUC0-t（ss）分别为（31±8）和（35±9）ng·mL^-1·h,AUC0-∞（ss）分别为（37±10）和（41±11）ng·mL^-1·h,AUCss分别为（25±7）和（15±3）ng·mL^-1·h;相对于参比制剂,受试制剂的生物利用度Fss0-tn为（88±12）%。受试制剂和参比制剂的AUC0-t和AUC0-∞经对数转换后进行方差分析,两制剂间变化相近（P〉0.05）,受试制剂tmax明显比参比制剂有所延长（P〈0.05）,明显具有缓释的特征。结论：试验制剂石杉碱甲缓释片具有明显的缓释特征。

Pharmacokinetics of Huperzine A substain-release tablets after multiple doses in healthy volunteers

AIM：To evaluate the pharmacokinetics of Huperzine A sustained-release tablets after multiple doses in Chinese healthy volunteers.METHODS：In a randomized crossover trial,24 healthy subjects received multiple oral doses of either Huperzine A sustained-release tablets or a common Huperzine A tablet for 7 days.The plasma concentrations were determined by LC/MS/MS.Pharmacokinetic parameters were obtained using DAS program.RESULTS：The major pharmacokinetic parameters of test and reference Huperzine A tables were as follows：Css min were （0.54±0.21） and （0.79±0.20）ng/mL,Css max were （1.65±0.45）and （1.83±0.37）ng/mL,Css were （1.05±0.28） and （1.22±0.28）ng/mL,tmax were （3.5±1.9） and （1.1±0.4） h,AUC0-t（ss） were （31±8） and （35±9）ng·mL^-1·h,AUC0-∞（ss） were （37±10）and （41±11）ng·mL^-1·h,AUCss were （25±7）and （15±3）ng·mL^-1·h,respectively.The relative bioavailability of test tablet as estimated by AUC0-t（ss） was （88±12） %.There was significant difference in tmax between two tablets.CONCLUSION：The results show that the Huperzine A substain-release tablets clearly have the characteristic of slow releasing properties.