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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。
Objective To evaluate the bioequivalence of huperzine A sustained release tablets in healthy volunteers. Methods Twelve healthy male subjects were randomly divided into 4 dose groups, 4 crossover and 4-week single oral dose of huperzine A sustained-release tablets or control drugs, the plasma concentration of drug was determined by LC-MS / MS, Kinetic parameters using DAS2.0 software processing. Results The C max values of the 200 μg group and 200 μg of the control group were (0.75 ± 0.25) and (1.57 ± 0.44) ng.mL-1, and the Tmax were 5.77 ± 3.60 and 1.27 ± 0.98 h, respectively. The AUC0-t (14.4 ± 5.81) and (15.1 ± 5.66) ng.h.mL-1 respectively, and the AUC0-∞ were (17.1 ± 7.29) and (16.7 ± 6.77) ng.h.mL- The bioavailability of the test drug F0-tn was (97.2 ± 24.4)%. The AUC0-t and AUC0-∞ of the test drug and the control drug were logarithmically transformed for analysis of variance. There was no significant difference between the two preparations (P> 0.05). 2 preparations, Cmax and Tmax were significantly different (P <0.05), Cmax of test drug was lower than that of control drug, but Tmax was prolonged. Conclusion The two huperzine tablets have bioequivalence and the drug has obvious sustained release characteristics.