国产与进口盐酸多奈哌齐片在健康人体的生物等效性

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:t_(1/2)分别为(62.56±9.76),(65.70±12.80)h;t_(max)分别为(3.15±0.67),(3.10±0.55)h;C_(max)分别为(10.42±2.52),(10.06±2.02)ng·mL~(-1);AUC_(0-192)分别为(489.37±154.32),(484.76±150.13)ng·h·mL<-1>;AUC_(0-∞)分别为(566.52±193.84),(564.38±176.10)ng·h·mL~(-1).用AUC_(0-192)、AUC_(0-∞)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.

Bioequivalence of domestic and imported donepezil hydrochloride tablets in healthy volunteers

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 random-ized and single crossover dose of domestic and imported donepezil hydro-chloride tablets 5 mg. The plasma concentration of donepezil was deter-mined 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. Re-sults The main pharmacokinetic parameters of test (domestic)and refer-ence(imported) sample were as follows: t_(1/2) were (62. 56 ± 9. 76) h and (65. 70 ±12. 80)h;t_(max) were (3.15±0.67) h and (3. 10±0.55) h;C_(max)were(10. 42±2. 52) ng· mL~(-1) and (10. 06±2. 02) ng· mL~(-1) ;AUC_(0-192) were (489. 37 ±154. 32) ng·h · mL~(-1) and (484. 76 ±150. 13) ng ·h · mL~(-1);AUC_(0-∞) were (566.52±193.84) ng · h· mL~(-1) and (564.38 ±176. 10) ng ·h ·mL~(-1). The mean bioavalibility values of AUC_(0-192) and AUC_(0-∞) were (100.7±9.2)% and (99.2±11.9)%. Conclusion The two kinds of donepezil hydrochloride tablets were bioequivalent.