盐酸二甲双胍混合材料骨架缓释片的研制

将两种规格的卡波姆与不溶性材料乙基纤维素合用作为骨架材料制备盐酸二甲双胍缓释片。以体外释放度为指标,考察了卡波姆规格及用量、填充剂种类及用量和润滑剂用量对释放度的影响,并通过正交试验筛选得最佳处方。对比了自制缓释片和参比制剂(Glucophage XR)的体外释放行为和兔体内药动学特征。结果表明,本品与参比制剂在pH 6.8磷酸盐缓冲液中的释放曲线相似。兔体内试验表明,本品的相对生物利用度为99%。体内外相关性考察表明,本品的体外释放与体内吸收具有良好的相关性。

Preparation of Metformin Hydrochloride Sustained-release Mixed Matrix Tablets

The metformin hydrochloride sustained-release tablets were prepared with two types of Carbopol and insoluble material ethylcellulose as matrix material.The influences of the type and amount of Carbopol and diluent as well as the amount of lubricant on in vitro release were investigated,and the preparation was further optimized by orthogonal design.The in vitro release and in vivo pharmacokinetics in rabbits of the prepared tablets(test preparation) and Glucophage XR(reference preparation) were compared.The results showed that the release curves in pH 6.8 phosphate buffer of the two preparations were similar.The relative bioavailability of the test preparation was 99% and the in vitro release had a good correlation with in vivo absorption.