离心法制备硝酸异山梨酯缓释微丸包衣处方及工艺优化

Preparation of isosorbide dinitrate sustained-release pellets by centrifugal granulation method and optimization it's prescription and process

采用离心法制备硝酸异山梨酯缓释微丸,以微丸的体外释放度为考察指标,探讨包衣处方、工艺因素对缓释微丸的释药特征的影响。结果表明,以丙烯酸树脂Eudragit RLPO为包衣材料,包衣增重为8%,增塑剂与抗粘剂分别占包衣聚合物量的15%,40%。在体外释放度实验中,微丸中药物累积释放百分率0.5 h为20%,2 h为55%,8 h为84%。该方法制备的硝酸异山梨酯缓释微丸包衣均匀,操作简便,质量稳定可靠,适合工业化生产。

Sustained-release pellets of isosorbide dinitrate were prepared by centrifugal granulation method,the pellets in vitro release was used as an indexes.The effect of coating formulation and technology effect on pellets release were investigated.The coating formula was composed of Eudragit RLPO and coating level of 8％,plasticizers occupied 15％ and 40％ of anti adhesive respectively.The accumulation dissolution percentage in vitro of ISDN from the sustained-release pellets was 20％ at 0.5 h,55％ at 2 h,84％ at 8 h.The ISDN membrane controlled release pellets prepared by centrifugal granulation methods are uniformly coated,easy to be operated,which has a reliable quality,and suitable for industrialized production.