【摘要】 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。更多还原

【Abstract】 Objective To study the bioequivalence of domestic and imported 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 5 mg.The plasma concentration of donepezil was determined by high pressure liquid chromatography time-of-flight mass spectrometry.The pharmacokinetic parameters and relative bioavalibility were calculated to evaluate the bioequivalence of two preparations.Results The main pharmacokinetic parameters of test(domestic)and reference(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-∞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-∞ were(100.7±9.2)% and(99.2±11.9)%.Conclusion The two kinds of donepezil hydrochloride tablets were bioequivalent.更多还原