格列吡嗪胶囊的相对生物利用度和生物等效性

Study on the relative bioavailability and bioequiavailability of Glipizide capsule

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。

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 0.80±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 rehtive bioavailability of test Glipizide capsule is （98.3±19.3）%, and the results demonstrate that the two preparations were bioequivalent.