不同厂家盐酸二甲双胍缓释片体外释放度考察

Release of metformin hydrochloride sustained-release tablets in vitro by different manufacturers

目的对不同厂家的盐酸二甲双胍缓释片进行体外释放度考察,为临床合理用药提供依据。方法根据盐酸二甲双胍缓释片标准(进口药品注册标准JX20010451)及相关参考文献,采用溶出度转篮法的装置进行体外释放实验,以pH 6.8磷酸盐缓冲液1 000 mL为释放介质,转速为100 r·min-1,温度为(37±0.5)℃,用紫外分光光度法进行含量测定。分别对不同厂家的盐酸二甲双胍缓释片,进行体外释放试验,计算累积释放百分率,绘制释放曲线;计算f2相似因子。结果两种进口制剂的相似因子f2为93.54。不同国产制剂与进口制剂的相似因子f2依次为:47.80、48.10、49.67、66.27、47.65、70.53、67.05;各国产制剂与BIOVAIL制剂的相似因子f2依次为:49.21、49.49、51.25、67.00、49.05、68.22、67.21。结论不同国产制剂与进口制剂的体外释药行为存在明显差异。

Objective To study the release rate of metformin hydrochloride sustained-release tablets in vitro by different manufacturers, in order to provide the basis for clinical rational drug use.Methods According to the standard of metformin hydrochloride sustained-release tablets （imported drug registration standard JX2001 0451 ）and related references,the stripping device of rotating basket method was adopted for the release experiment in vitro.Phosphate buffer solution 1 000 mL with pH 6.8 was used as medium,at 1 00 rpm rotation speed,and the temperature was at （37 ±0.5 ）℃.The content was determined by UV spectrophotometry.In vitro release tests of metformin hydrochloride sustained-release tablets of different manufacturers were taken and the cumulative release percentage,drawing stripping curve and f2 similarity factor were calculated.Results The f2 similarity factor of two kinds of imported preparation was 93.54.The f2 similarity factors of the domestic preparation and Bristol-Myers Squibb formulation were 47.80,48.1 0,49.67,66.27, 47.65,70.53,67.05,respectively;and the f2 similarity factors of the domestic preparation and BIOVAIL formulation are 49.21 , 49.49,51 .25,67.00,49.05,68.22,67.21 ,respectively.Conclusions The domestic and imported preparations have significant differences in drug release behavior in vitro.