格列吡嗪胶囊人体药动学的研究

Study on the Pharmacokinetics of Glipizide in Human

目的研究格列吡嗪胶囊人体药物代谢动力学及相对生物利用度。方法用I-IPLC法测定10例受试者单剂量交叉口服5.0 mg格列吡嗪胶囊和片剂后的血药浓度,MC-RKP药动学程序拟合,得药动学参数,计算胶囊剂的相对生物利用度(F)。结果胶囊剂的Cmax为(456±60)ng/mL、Tmax为(2.95±0.6)h、AUC为(2 335±180)ng/(mL.h)。以上参数经双单侧t检验等统计学分析,与片剂比无显著差异。F值为(103±4)%。结论格列吡嗪(2.95±0.6)h血药浓度达高峰,峰浓度为(456±60)ng/mL,且胶囊与片剂为生物等效制剂。

Objective To study the pharmacokinetics and relative bioavailability of glipizide in human. Methods The plasma concentrations of 10 subjects were determined by HPLC after 5.0 mg single dosage glipizide capsules and tablets were taken orally and crossly. The results were fitted with MC - PKP programm to get pharmacokinetie parameters. Then the relative bioavailability of capsule was caculated. Results The phannacokineties parameters of capsule were as fol- lowing, Cmax 456 ng/mL, Tmax, 3.0 h,AUC 2 335 ng/（mL-h）. Alove parameters of two preparations had no significant difference by double single t - test and 1 ～2α confidence in terval analysis. The relative bioavailability of glipizide capsule was （103 ±4）%. Conclusion The plasma concentration of glipizide capsule attach peak in （2.95 ± 0.6）h, its peak concentration might be （456 ± 60）ng/mL. Capsule and tablet of glipizide are bioequivolent preparations.