国产盐酸米多君片在健康人体的生物等效性研究

目的:比较国产与进口盐酸米多君片在健康人体的生物等效性.方法:20名健康男性受试者随机交叉单剂量口服国产(受试制剂)或进口盐酸米多君片(参比制剂)5 mg,用液相色谱-串联质谱法测定血浆中盐酸米多君的活性代谢产物脱甘氨酸米多君的浓度,以DAS 2.0软件计算药动学参数,进行生物等效性评价.结果:受试制剂和参比制剂的药动学参数分别为:t1/ 2 (3.19±0.33)和(3.02±0.31)h,tmax(0.6±0.3)和(0.7±0.5)h,Cmax(21.72±6.06)和(21.83±6.24) μg/L,AUC0～t (65.27±8.43)和(65.64±7.08) μg·h·L-1,AUC0～∞(70.08±9.05)和(69.85±7.83) μg·h·L-1.按AUC0～∞计算,国产盐酸米多君片的相对生物利用度为( 100.3±6.8)％.结论:国产与进口盐酸米多君片在健康人体内具有生物等效性.

Bioequivalence of domestic midodrine hydrochloride tablets in healthy volunteers

Objective:To evaluate the bioequivalence of domestic and imported midodrine hydrochloride tablets in healthy volunteers.Methods:A randomized cross-over trial was performed in 20 healthy male volunteers.Each volunteer was randomized to receive a single dose of 5 mg domestic and imported midodrine hydrochloride tablets.Plasma concentrations of desglymidodrine were measured with HPLC-MS/MS method.The pharmacokinetic parameters were calculated with DAS 2.0 software,then bioequivalence of the two preparations was evaluated.Results:The main pharmacokinetic parameters of the domestic and imported preparations were as follows:t1/2(3.19±0.33) vs(3.02±0.31) h,tmax(0.6±0.3) vs(0.7±0.5) h,cmax(21.72±6.06) vs(21.83±6.24) μg/L,AUC0-t(65.27±8.43) vs(65.64±7.08) μg·h·L-1,AUC0-∞(70.08±9.05) vs(69.85±7.83) μg·h·L-1,respectively.Relative bioavailability of the domestic midodrine hydrochloride tablets was(100.3±6.8)%,when calculated according to AUC0-∞.Conclusion:The two preparations of midodrine hydrochloride are bioequivalent in healthy volunteers.