石杉碱甲缓释片在健康人体的生物等效性

目的评价石杉碱甲缓释片在健康人体的生物等效性。方法入选的12名健康男性受试者随机分成4个剂量组,4交叉、4周期单剂量口服石杉碱甲缓释片或对照药物,用LC-MS/MS测定血浆中药物浓度,药代动力学参数用DAS2.0软件处理获得。结果试验药物200μg组与对照药物200μg组的Cmax分别为(0.75±0.25)和(1.57±0.44)ng.mL-1,Tmax分别为(5.77±3.60)和(1.27±0.98)h,AUC0-t分别为(14.4±5.81)和(15.1±5.66)ng.h.mL-1,AUC0-∞分别为(17.1±7.29)和(16.7±6.77)ng.h.mL-1;相对于对照药物,试验药物的生物利用度F0-tn为(97.2±24.4)%。试验药物和对照药物的AUC0-t和AUC0-∞经对数转换后进行方差分析,2制剂间无显著性差异(P>0.05)。2制剂间,Cmax和Tmax有显著差异(P<0.05),试验药物的Cmax比对照药物有所降低,而Tmax有所延长。结论 2种石杉碱甲片具有生物等效性,同时试验药物具有明显的缓释特征。

Bioequivalence of huperzine A sustain- release tablets in healthy volunteer

Objective To study the bioavailability of the tested and reference huperzine A sustain-release tablets in healthy male volunteers.Methods According to the four-crossing design,each volunteer was orally given huperzine A sustain-release tablets or huperzine A.The plasma concentrations were determined by LC-MS/MS.Pharmacokinetic parameters were obtained using DAS 2.0 program.Results The main pharmacokinetic parameters of huperzine A tablets test and reference were as follows: Cmax were(0.75±0.25),(1.57±0.44)ng·mL-1,Tmax were(5.77±3.60),(1.27±0.98)h,AUC0–t were(14.4±5.81),(15.1±5.66)ng·h·mL-1,AUC0-∞ were(17.1±7.29),(16.7±6.77)ng·h·mL-1,in 200 μg groups respectively.The relative bioavailability was(97.2± 24.4)%.The data of the reference and tested drugs were not different as shown by F test.Conclusion The result shows that the two huperzine A tablets made in two different preparations are bioequivalent.Huperzine A sustain-release tablets clearly have the characteristic of slow releasing properties.