进口与国产尼扎替丁制剂在中国健康人体的生物等效性

Bioequivalence of domestic and imported nizatidine formulations in Chinese healthy volunteers

目的研究进口与国产尼扎替丁在健康人体的药代动力学,并评价2种制剂的生物等效性.方法用双交叉试验设计,20名健康志愿者口服国产尼扎替丁片剂和进口胶囊剂,服药后0～8.5 h内间隔取血,用HPLC法测定血药浓度.计算主要药代动力学参数,并以胶囊剂为参比制剂,计算尼扎替丁片剂的相对生物利用度,判断其生物等效性.结果国产片剂和进口胶囊剂的体内药代动力学参数分别为:tmax为(1.49±0.48),(1.38±0.58)h;Cmax为(2319±511),(2408±572)ng·mL-1;MRT为(3.08±0.44),(2.97±0.46)h;t1/2为(1.55±0.33),(1.51±0.21)h;AUC0-t为(6625±964),(6725±1078)ng·h·mL-1;AUC0-∞为(6836±973),(6928±1114)ng·h·mL-1.尼扎替丁片剂的相对生物利用度F0-8.5h为(99.67±13.93)%.结论2种制剂具有生物等效性.

Objective To evaluate the pharmacokinetics and bioequivalence of two nizatidine preparations in Chinese healthy volunteers. Methods According to a randomized cross-over design, a single oral dose of 300 mg of nizatidine test or reference preparation was given to 20 Chinese healthy young volunteers. After dosing, serial blood samples were collected for a period of 8.5 h. Nizatidine concentration in plasma was analyzed by HPLC. Results The main pharmacokinetic parameters of nizatidine preparations were as follow: t max were (1.49±0.48) and (1.38±0.58) h,C max were (2319±511) and (2408±572) ng·mL -1 ,MRT were(3.08±0.44) and (2.97±0.46) h,t 1/2 were (1.55±0.33) and (1.51±0.21) h, AUC 0-t were (6625±964) and (6725± 1078) ng·h ·mL -1 ,AUC 0-∞ were (6836±973) and (6928±1114) ng·h·mL -1 for imported tablets and domestic tablets respectively. The relative bioavailability of nizatidine tablet F 0-8.5h was (99.67±13.93)%.Conclusion The test and reference preparations were bioequivalent.