含甘草酸效应组分微丸的制备及其性质考察

Preparation and properties of sustained-release pellets of glycyrrhizin effective components

目的:应用挤出滚圆法制备含甘草酸效应组分速释微丸,采用Eudragit RS 100与Eudragi RL 1002种包衣材料,制备含甘草酸效应组分缓释微丸。方法:采用Mini Glatt流化床底喷包衣法制备缓释微丸,对其包衣工艺及处方进行单因素考察,评价微丸的粉体学性质和体外释放行为。结果:当Eudragit RS 100与Eudragit RL 100的质量比为4∶l,聚合物包衣增重为5%,增塑剂用量为15%时,药物具有明显的缓释作用,体外释放曲线符合Pep-pas和Higuchi方程。结论:通过调整Eudragit RS 100与Eudragit RL 100的比例,或提高聚合物包衣增重等手段,能使含甘草酸效应组分缓释微丸具备较理想的缓释效果。

Objective： To prepare the glycyrrhizin pellets by extrusion-spheronization, and optimize the formulation of sustained release pellets of glycyrrhizin effective components coated with mixed Eudragit RS 100 and Eudragit RL100. Method： The sustained-release pellets of glycyrrhizin were prepared by Glatt fluid bed technique. The ratio of Eudragit RS 100 to Eudragit RL 100 in the formulation was optimized. The factors that influence the drug release behaviors and their properties were evaluated. Result： The optimal coat for drug sustained-release was shown at the ratio of Eudragit RS 100 to Eudragit RL 100 of 4： 1, the loading weight of copolymers of 5% and the plasticizer concentration of 15%. The curves of cumulative drug release were fit for Peppas and Higuchi equation. Conclusion： The optimal sustained release of the glycyrrhizin effective component pellets is featured by adjusting the ratio of Eudragit RS 100 to Eudragit RL100 and the loading weight of copolymers.