辛伐他汀-烟酸双层缓释片的制备及其体外质量评价

目的 制备辛伐他汀(SVT) -烟酸(NA)双层缓释片并进行体外质量评价.方法 分别通过正交实验和单因素实验,筛选NA缓释层与SVT常释层处方,确定最佳处方组成并制备SVT-NA双层缓释片,测定缓释片中NA与SVT的含量.以国内已上市NA缓释片为参比制剂,测定自制双层缓释片中NA的释放度,计算释放度相似因子(f2),并进行方程拟合.按照中国药典2010版中SVT普通片溶出度测定条件,测定自制双层缓释片常释层中SVT的溶出度.结果 自制双层缓释片中NA的释放度与市售NA缓释片相似(f2＞75),其释放行为符合Higuchi方程；常释层中SVT 30 min内的累积溶出度＞98％,符合中国药典有关规定.结论 SVT-NA双层缓释片处方组成合理,制备工艺稳定,重现性良好,有望开发成为新的复方制剂.

Preparation and in vitro evaluation of simvastatin and nicotinic acid double layer sustained release tablets

Objective To prepare simvastatin(SVT)-nicotinic acid(NA) double layer sustained release tablets and evaluate its quality in vitro.Methods The formulation composition of NA sustained release layer and SVT immediate release layer was established by orthogonal experiment and single factor test respectively.The SVT-NA double layer sustained release tablets were then prepared.The relative labeled content of the 2 active drugs in the sustained tablets was determined by HPLC.The release profile of NA in the sustained layer was investigated and the similar factor value(f2) was calculated with the marketed NA sustained tablets as the reference drug.The dissolution of SVT in the immediate release layer was determined according to the related qualifications for SVT tablets in the China Pharmacopoeia Edition(2010).Results The release characteristics of NA in the sustained release layer were similar to those of the marketed NA sustained release tablets and also conformed to the Higuchi equation.The calculated f2 was greater than 75.The cumulative dissolution of SVT in the immediate release layer was above 98% in 30 min and met the requirement of SVT tablets in Chinese Pharmacopoeia.Conclusion The formulation of SVT-NA double layer sustained release tablets is reasonable.The production process is stable and reproducible.The preparation may become a new SVT-NA product.