舒胸脉冲控释滴丸的研制

Preparation of Shuxiong Pulsatile Controlled-release Dropping Pill

目的:制备舒胸脉冲控释滴丸并考察体外释放影响因素。方法:取合适大小(10～15 mg)的舒胸滴丸分别以溶胀层(含交联羧甲基纤维素钠)和控释层(含乙基纤维素水分散体)顺序包衣制备舒胸脉冲控释滴丸,通过考察不同溶胀层材料及溶胀层与控释层的不同包衣增重对药物释放的影响来优选工艺,并进行处方验证试验。结果:各考察因素均对药物的释放影响显著。优选工艺为:溶胀层材料采用交联羧甲基纤维素钠,溶胀层和控释层包衣增重分别为15%、7%。以此制备的脉冲控释滴丸时滞时间为4 h左右,时滞后4 h内累积释药百分率达到80%。结论:该优选工艺所制备的舒胸脉冲控释滴丸具有体外脉冲控释作用。

Objective：To prepare Shuxiong pulsatile controlled-release dropping pill and study the influencing factors in vitro. Methods：Dropping pills with suitable size（ 10 - 15rag）were coated with swelling layer containing croscarmellose sodium and controlled- release layer containing ethyleellulos aqueous dispersion respectively to prepare Shuxiong pulsatile controlled-release dropping pill. The effects of the materials of swelling layer, the weight of swelling layer and controlled-release layer on the release of drugs were investigated to optimize the process technology and validate formula. Results：The release behavior was influenced strikingly by the types and weight of coating layer. The optimal formula was as follows ： Shuxiong pulsatile controlled-release dropping pills were prepared using croscarmellose sodium as inner layer with 15% （weight）coating level and ethylcellulose aqueous dispersion （Surelease）as outer controlled-release layer with 7% （weight）coating level. The lag time of prepared pulsatile controlled-release dropping pills was about 4 h and accumulative release rate reached 80% within 4 h. Conclusion ：The drug release of Shuxiong pulsatile controlled-release dropping pill is shown in pulsatile way in vitro.