国产与进口替米沙坦片的人体生物等效性

Bioequivalence of domestic telmisartan tablets in healthy male volunteers

目的 :评价国产和进口替米沙坦片剂的生物等效性。方法 :采用随机交叉试验 ,HPLC荧光法测定 2 0名中国健康男性受试者口服替米沙坦的血药浓度。药动学参数用 3P97程序进行计算。结果 :国产与进口替米沙坦片的主要药动学参数 :AUC0→t分别为 (2 381 2 0± 10 98 5 1)、(2 333 36± 114 5 75 ) μg·h·L-1;AUC0→∞ 为 (2 4 86 4 4± 1135 70 )、(2 4 4 0 35± 1190 37) μg·h·L-1;cmax为 (5 71 99± 36 8 2 7)、(5 30 97± 2 5 6 38) μg·L-1;tmax为 (1 15± 0 6 8)、(1 2 0± 1 6 0 )h ;T1/ 2 为 (19 0 8± 2 91)、(18 99±2 92 )h。国产替米沙坦片的相对生物利用度是 (10 4 2 9± 2 1 17) % (n =2 0 )。国产和进口替米沙坦片主要药动学参数经统计学(ANOVA)处理均无显著性差异 (P >0 0 5 ) ;AUC0→t、cmax经对数转换后的双单侧t检验示无显著性差异。结论

AIM: To evaluate bioequivalence of telmisartan in 20 healthy male volunteers after a single oral dose of 80 mg. METHODS: The plasma levels of telmisartan were determined by HPLC with fluorescence detector.The oral administration pharmacokinetic model was described as a two-compartment model. RESULTS: The pharmacokinetic parameters of domestic telmisartan (test) were:AUC(2 381.20±1 098.51)μg·h·L -1,c max(571.99±368.27)μg·L -1,t max(1.15±0.68)h,T 1/2(19.08±2.91)h. The pharmacokinetic parameters of telmisartan (Germany)were:AUC( 2 333.96±1 145.75)μg·h·L -1,c max(530.97±256.38)μg·L -1,t max(1.20±1.60)h,T 1/2(18.99±2.92)h.There were no significant differences in all pharmacokinetic parameters between 2 tablets(P>0.05). CONCLUSION: The results of 2 one-side test show that 2 preparations are bioequivalent.