高效液相色谱法测定盐酸二甲双胍肠溶片在正常人体的药动学及生物利用度

 目的：研究盐酸二甲双胍肠溶片与普通片的药动学和生物利用度。方法：受试者交叉口服单剂量（1000 mg）肠溶片与普通片，用反相高效液相色谱法测定血药浓度。结果：两种片剂的主要药动学参数分别为C_max（2.9±0.7）mg·L^-1和（2.6±0.6）mg·L^-1，T_max为（2.6±0.4）和（2.3±0.5）h ，T_1/2Ka为（0.87±0.26）h和（0.81±0.23）h，T_1/2Ke为（1.6±0.4）h和（1.9±0.6）h，AUC为（12.2±1.1）mg·L^-1·h^-1和（11.9±1.2）mg·L^-1·h^-1。肠溶片相对于普通片的生物利用度F为(103.0±12.0)%。结论：两种剂型的各药动学参数之间差异均无显著性(P>0.05)，经双向单侧t检验，两制剂具有生物等效性。

Relative bioavailability and pharmacokinetics of metformin hydrochloride enteric dissolving tablets by HPLC

OBJECTIVE The pharmacokinetics and bioavailability of metformin hydrochloride enteric dissolve tablets were compared with stomach dissolving tablets.METHODS Plasma levels of metformin were detected by RP-HPLC method.RESULTS The parameters of the two formulations for metformin: Cmax of enteric and stomach dissolving tablets were (2.9±0.7) mg·L^-1 and (2.6±0.6)mg·L^-1，T_max(2.6±0.4) h and(2.3±0.5)h；T_1/2Ka(0.87±0.26) h and (0.81±0.23) h；T_1/2Ke（1.6±0.4）and（1.9±0.6）h, AUC（12.2±1.1）and（11.9±1.2） mg·L^-1·h^-1 respectively.The relative bioavailability of enteric dissolving tablets was (103.0±12.0)%.CONCLUSIONS There was no significant difference in pharmacokinetic parameters. It was demonstrated that the two preparations were bioequivalent by one two-sidest tests.