酒石酸美托洛尔缓释微丸的制备及处方因素考察

目的：选用Eudragit RS 30 D与Eudragil RL30D两种包衣材料，制备日服2次的酒石酸美托洛尔缓释徽丸，并对其处方因素进行考察。方法：采用Glatt流化床底喷溶液上药法制备载药微丸，考察缓释聚合物Eudragit RS 30D与Eudragit RL 30D的不同质量配比（2：3，7：3和9：1）、聚合物包衣增重（10％，20％和30％）以及增塑利嗣量（10％，20％和40％）和放置时间对药物释放的影响。结果：当Eudragit RS 30D与Eudragit RL 30D的质量比为9：1，聚合物包衣增重为20％，增塑剂用量为20％时，药物的释放行为符合中国药典对缓释制剂释放度的相关规定。结论：通过调整Eudragit RS 30D与Eudragit RL 30D之间的比例，或提高聚合物包衣增重等手段，能使酒石酸美托洛尔载药徽丸具备较理想的缓释效果。

Preparation of metoprolol tartrate sustained-release pellets

Objective:To optimize the formulation of metoproiol tartrate sustained release pellets coated with mixed Eudragit RS 30D and Eudragit RL 30D.Methods:Metoprolol tartrate pellets were prepared by Glatt fluid bed technique.The ratio of Eudragit RS 30D to Eudragit RL 30D(2:3,7:3 and 9:1,w/w)in the formulation was optimized.The factors to influence the drug release behaviors,such as loading weight of copolymers Eudragit RS 30D and Eudragit RL 30D(10%,20% and 30%,w/w), plasticizer concentration(10%,20% and 40%)and storage time,were evaluated.Results:The opti- mal drug sustained-release was shown at the ratio of Eudragit RS 30D to Eudragit RL 30D of 9:1,the loading weight of copolymers of 20% and the plasticizer concentration of 20%.Conclusion:The optimal sustained release of the metoprolol tartrate pellets is featured by adjusting the ratio of Eudragit RS 30D to Eudragit RL 30D.