国产与进口盐酸多奈哌齐片在健康人体的生物等效性

Bioequivalence of domestic and imported donepezil hydrochloride tablets in healthy volunteers

目的研究国产与进口盐酸多奈哌齐片在健康人体的生物等效性。方法 20名男性健康志愿者随机交叉给药,分别单剂量口服国产(受试制剂)与进口盐酸多奈哌齐片(参比制剂),用高效液相飞行时间质谱(HPLC/TOF/MS)联用技术,测定人血浆中多奈哌齐的浓度,计算2者的药代动力学参数及相对生物利用度,并评价2制剂的生物等效性。结果口服国产及进口盐酸多奈哌齐片5mg的主要药代动力学参数:t1/2分别为(62.56±9.76),(65.70±12.80)h;tmax分别为(3.15±0.67),(3.10±0.55)h;Cmax分别为(10.42±2.52),(10.06±2.02)ng·mL-1;AUC0-192分别为(489.37±154.32),(484.76±150.13)ng.h.mL-1;AUC0-∞分别为(566.52±193.84),(564.38±176.10)ng.h.mL-1。用AUC0-192、AUC0-∞估算多奈哌齐供试片的相对生物利用度分别为(100.7±9.2)%,(99.2±11.9)%。结论 2种盐酸多奈哌齐片为生物等效制剂。

Objective To study the bioequivalence of domestic and im- ported donepezil hydrochloride tablets in healthy volunteers. Methods Twenty healthy males volunteers were orally administered with a randomized and single crossover dose of domestic and imported donepezil hydrochloride tablets 5mg. The plasma concentration of donepezil was determined by high pressure liquid chromatography timeofflight mass spectrometry. The pharmaeokinetie parameters and relative bioavalibility were calculated to evaluate the bioequivalenee of two preparations. Results The main pharmacokinetic parameters of test （domestic）and refer- ence（ imported ） sample were as follows： t1/2 were （ 62. 56 ± 9. 76 ） h and （ 65. 70 ±12. 80）h;tmax were （3. 15 ±0.67） h and （3. 10 ±0.55） h;Cmax were（10. 42 ±2.52） ng · mL^-1 and （10.06 ±2.02） ng· mL^-1 ;AUC0-192 were （489.37 ±154.32） ng·h · mL^-1 and （484.76 ±150. 13） ng·h · mL^-1 ;AUC0-192 were （566. 52 ± 193.84） ng · h· mL-1 and （564. 38 ± 176. 10 ） ng ·h · mL^-1. The mean bioavalibility values of AUC0-192 and AUC0-192 were （100.7±9.2）% and （99.2±11.9）%. Conclusion The two kinds of donepezil hydroehloride tablets were bioequivalent.