盐酸文拉法辛缓释胶囊的制备及体外释放试验

Preparation of Venlafaxine Hydrochloride Sustained-release Capsules and Drug Release Test in vitro

目的研究盐酸文拉法辛缓释微丸的制备方法，并对其体外释药行为进行考察。方法用挤出滚圆造粒机制备盐酸文拉法辛微丸，用流化床进行微丸包衣，再填装胶囊；采用紫外分光光度法测定盐酸文拉法辛缓释胶囊的释放度。单因素试验考察包衣增重及致孔剂的量对缓释微丸释药行为的影响。结果采用挤出滚圆法制备的盐酸文拉法辛微丸，圆整度好，颗粒均匀。标准曲线方程△A=0．0044C＋0．0015，r=0．9998，盐酸文拉法辛的浓度在7～98μg·mL范围内呈良好的线性关系。包衣增重为12．5％～16．5％时，自制3批盐酸文拉法辛缓释胶囊的释放行为与原研产品一致，f2凶子分别为89．1、87．9、90．4。结论挤出滚圆法制备盐酸文拉法辛微丸工艺简便易行，制得的微丸重复性好，收率高。

Objective To study the preparation method of venlafaxine hydroehloride sustained-release pel- lets and to investigate their drug release behavior in vitro. Methods Venlafaxine hydrochloride pellets were prepared by extrusion-spheronization technology coated by the fluidized bed and filled into capsules. Ultraviolet spectrophoto- metricy was used to determine the release of venlafaxine hydroehloride sustained-release capsules. Single factor experiments were conducted to investigate the effect of coating weight and the amount of the porogen on sustained- release of the pellets. Results The venlafaxine hydroehloride sustained-release pellets, prepared by extrusion-spher- onization technology,were round and uniform. The standard curve equation was A = 0. 0044 C ＋ 0. 0015, r = 0. 9998. There was a good linear relationship the concentration of venlafaxine hydroehloride ranged from 7 to 98 μg ·m1-1. When the coating weight was between 12.5% - 16.5%, the in vitro release behavior of homemade ven- lafaxine hydroehloride sustained-release capsules was consistent with that of the original research product, f2 factor was 89.1,87.9,90.4, respectively. Conclusion The preparation technology of venlafaxine hydrochloride pellets using extrusion-spheronization method is simple and productive.