格列吡嗪胶囊的相对生物利用度和生物等效性

目的:考察格列吡嗪胶囊人体相对生物利用度及生物等效性。方法:20名健康男性志愿者,采用交叉给药方案,分别单剂量口服5.0mg受试格列吡嗪胶囊和参比格列吡嗪胶囊,用液相色谱-串联质谱法测定血浆中格列吡嗪浓度,进行人体相对生物利用度和生物等效性评价。结果:单次口服5.0mg受试格列吡嗪胶囊和参比格列吡嗪胶囊后,达峰时间(Tmax)分别为(2.1±0.5)h和(2.2±1.1)h;峰值血药浓度(Cmax)分别为(298.95±105.66)ng/ml和±281.55±68.84)ng/ml;半衰期(t1/2)分别为(4.14±1.33)h和(3.80±1.28)h;药时曲线下面积采用梯形法计算,AUC0-t分别为(1565.89±659.41)ng·h/ml和(1580.13±465.43)ng·h/ml,AUC0-∞分别为(1649.53±704.58)ng·h/ml和(1644.15±478.92)ng·h/ml。结论:受试格列吡嗪胶囊的相对生物利用度为(98.3±19.3)%,主要参数的双、单侧t检验,结果显示两种制剂为生物等效制剂。

Study on the relative bioavailability and bioequiavailability of Glipizide capsule

Objective To study the relative bioavailability and bioequiavailability of Glipizide capsule. Method A single oral dose (5mg) of test Glipizide capsule and referent Glipizide capsule were given to 20 volunteers in a randomized crossover study. Glipizide concentrations in plasma were determined by LC/MS/MS method. Results Tmax of test Glipizide capsule and referent Glipizide capsule were (2.1±0.5)h and (2.2±1.1)h respectively; Cmax were (298.95±105.66)ng/ml and (281.55±68.84)ng/ml; t1/2 were (4.14±1.33)h and (3.80±1.28)h; AUC0-t were (1565.89±659.41)ng·h/ml and (1580.13±465.43)ng·h/ml; AUC0-∞ were (1649.53±704.58)ng·h/ml and(1644.15±478.92)ng·h/ml. There was no statistically significant difference between the two preparations in AUC values. Conclusion The relative bioavailability of test Glipizide capsule is(98.3±19.3)%, and the results demonstrate that the two preparations were bioequivalent.