盐酸文拉法辛缓释微丸的制备及体外释放度试验

目的制备盐酸文拉法辛缓释微丸,并对其体外释药行为进行研究。方法先用文拉法辛溶液对空白微丸进行上药,通过EC包衣制得速释微丸,然后用速释微丸为丸芯,用EudragitEudragitNE30D,水分散体为包衣材料制备缓释微丸,再将速释微丸和缓释微丸以1:2的比例混合得到最后的缓释微丸。并分别考察了包衣增重对体外释药行为的影响。结果对制备过程中不同阶段的微丸进行了体外释放研究,表明增重20%,速释微丸和缓释微丸以1:2的比例配比结果最为理想。结论盐酸文拉法辛缓释微丸具有较好的释药性能及良好的缓释效果。

Preparation of Venlafaxine Hydrochloride Sustained Release Pellets and Its Release Test in Vitro

OBJECTIVE To characterize venlafaxine's release behavior in vitro following the preparation of venlafaxine hydrochloride sustained-release pellets.METHODS At first,the drug substance was microencapsulated into an EC solution to prepare fast-release pellets by a centrifugal granulator;then,the fast-release pellets was used as the core and microencapsulated into aqueous dispersed coating materials made of Eudragit NE 30D to prepare sustained-release pellets;next,the fast-release pelltes and sustained-release pellets were mixed with a ratio of 1:2 to make the final sustained-release pellets.The effects of coating thicknesses on the sustained-release parameters were analyzed.RESULTS The optimal sustained release behavior in vitro of the sustained-release pellets mixed from fast-release pellets and sustained-release pellets with a ratio of 1:2 was selected when the amount of coating materials was 20% of total weight.CONCLUSION The venlafaxine hydrochloride sustained-release pellets provided a rather good sustained-release efficiency.