盐酸二甲双胍缓释片与国外上市品的药动学比较及体内外相关性研究

目的研究并比较盐酸二甲双胍缓释片与进口片的药代动力学性质及体内外相关性。方法分别单剂量和多剂量口服两种制剂后测定血药浓度并计算出它们的药动学参数。将体外释放度数据与用Wagner—Nelson方法计算的药物体内吸收百分数进行线形回归来进行体内外相关性研究。结果研制品与进口品的药动学特性非常近似。结论研制片与进口片具有生物等效性并且它们的体内外相关性良好。

Pharmacokinetics and in vitro-in vivo correlation of sustained-release metformin in healthy volunteers

Objective The single-dose and multi-dose pharmacokinetics of two sustained-release tablet formulations of metformin hydrochloride in fed, 40 healthy volunteers were compared, and their in vitro-in vivo correlations were evaluated. Methods Self-made and imported (Glucophage XP) sustained-release tablets of metformin hydrochloride were administered orally in a single-dose, 1000 mg/d for two times with a 6-day interval, or the multi-dose regimen of 1000 mg/d for two blocks of five-consecutive days with a 14-day interval. The plasma concentrations and pharmacokinetics of metformin hydrochloride were analyzed after administration. The in vivo drug release rate was compared with in vivo Absorption percentage calculated from Wagner-Nelson method for getting the in vitro-in vivo correlation. Result and Conclusion The two formulations have similar phamarcokinetics and bioequivalent, and their in vitro-in vivo correlations are good.