目的制备复方丹参速释微丸,使理化性质差异较大的各成分达到同步释放。方法采用挤出滚圆法制备复方丹参速释微丸,以丹酚酸B、三七总皂苷和冰片为体外溶出考察的指标性成分,对微丸中加入的崩解剂种类、用量,黏合剂和表面活性剂的用量进行了筛选,并采用正交试验设计对处方进行了优化。结果在处方中加入20%泡腾崩解剂、5%羧甲基淀粉钠(CMS-Na)和2%十二烷基硫酸钠(SDS)后,复方丹参速释微丸中冰片的溶出效率增加,且3种指标成分基本达到了同步快速释放。结论通过加入复合崩解剂,可以使采用挤出滚圆法制备的微丸迅速崩解,从而使复方中药中理化性质差异较大的各成分达到同步释放。

Objective To prepare compound Danshen immediate-release pellets and obtain the synchronous release rate of components with significant difference of physicochemical properties.Methods Compound Danshen immediate-release pellets were prepared by extrusion-spheronization method and the type and amount of the disintegrating agents,adhesive agent,and SDS used in the pellets were screened by regarding salvianolic acid B,PNS,and Borneolum as the three index components of release in vitro.Then the preparation formula was optimized by using orthogonal design.Results The dissolution efficiency(DE)of Borneolum in compound Danshen immediate-release pellets was increased,and the three index components were released synchronistically through adding in 20% effervescent disintegrating agents,5% CMS-Na,and 2% SDS.Conclusion The result shows that the same release rate in immediate-release of the three index components with very different physico-chemical properties of compound Danshen pellets which were prepared by extrusion-spheronization is obtained through adding complex disintegrating agents.

国家自然科学基金资助项目(30200363)