摘要
目的:选用Eudragit RS 30 D与Eudragit RL 30 D两种包衣材料,制备日服2次的酒石酸美托洛尔缓释微丸,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Eud- ragit 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%)以及增塑剂用量(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微丸具备较理想的缓释效果。
Objective： To optimize the formulation of metoprolol 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 RI, 30D （10% , 20% arid 30% , w/w） , plasticizer concentration （10% , 20% and 40% ） and storage time, were evaluated. Results： The optimal drug sustained-release was shown at the ratio of Eudragit RS 30D to Eudragit RL 301） 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 301） to Eudragit RL 30D.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2006年第14期1172-1176,共5页
Chinese Journal of New Drugs
