国产与进口二甲双胍片剂人体生物等效性

Bioequivalence of domestic metformin tablets in healthy male volunteers

目的 :评价国产和进口盐酸二甲双胍片剂的生物等效性。方法 :采用随机交叉试验方法 ,用HPLC法对国产和进口盐酸二甲双胍片在 2 0名中国健康男性受试者中的血药浓度进行了测定。药动学参数用 3P97程序进行模型拟合。结果 :国产与进口盐酸二甲双胍片的AUC0→t,AUC0→∞ ,cmax,tmax,T1/ 2 分别是 :(10 189± 2 743) ,(10 436± 30 0 4)h·ng·mL-1;(112 6 9± 30 77) ,(11486± 32 38)h·ng·mL-1;(16 5 0± 493) ,(16 2 4± 46 9)ng·mL-1;2 2 5 (1 5～ 3 0 ) ,2 0 (1 5～ 3 0 )h ;(4 34± 1 2 3) ,(4 70±1 0 8)h。国产盐酸二甲双胍片的相对生物利用度是 98 4 2 %。国产和进口盐酸二甲双胍片的主要药动学参数经统计学 (SPSS10 0软件的ANOVA)处理均无显著性差异 (P >0 0 5 )。AUC对数转换后的双单侧t检验结果表明无显著差别。结论 :国产和进口盐酸二甲双胍片具有生物等效性。

AIM: To evaluate bioequivalence of metformin in 20 healthy male volunteer after a single oral dose of 850 mg. METHODS: The plasma levels of metformin were determined by high performance liquid chromatography with ultraviolet detection. The oral administration pharmacokinetic model was described as a one-compartment model. RESULTS: The pharmacokinetic parameters of domestic metformin (test) were: AUC: (11 269± 3 077) h·ng·mL -1, c max: (1 650±493) ng·mL -1, t max: 2.25 (1.5-3.0) h, T 1/2: (4.34±1.23) h; The pharmacokinetic parameters of metformin (France) were: AUC: (11 486± 3 238) h·ng·mL -1, c max: (1 624±469) ng·mL -1, t max: 2.0 (1.5-3.0) h, T 1/2: (4.70±1.08) h. There were no significant differences in all pharmacokinetic parameters between 2 tablets (P>0.05). CONCLUSION: The results of two one-side test show that 2 preparations are bioequivalent.