琥珀酸去甲文拉法辛膜控与骨架结合型缓释微丸的制备及释放特性研究

Study on the preparation and release behavior of membrane-controlled and skeletal sustained release Desvenlafaxine succinate pellets

摘要：目的制备以乙基纤维素水分散体（Surelease^（R））为包衣材料的琥珀酸去甲文拉法辛（DVS）缓释微丸，并评价其体外释药特性。方法在单因素考察的基础上进行正交试验，确定挤出滚圆法制备载药丸芯的工艺参数。在含药丸芯的基础上，以Surelease^（R）为缓释材料进行流化床包衣。以原研缓释片为参比，评价微丸的体外释放，并将释放数据用常用模型拟合，探讨释放机制。结果载药微丸的最佳制备工艺为：软材与润湿剂为8：3．2、挤出速度55r·min^-1、滚圆速度1．0×10^3r·min^-1、滚圆时间2min。优选工艺的重复性好，微丸的收率高，当包衣增重47．50％时，可达到与原研片相似的释放效果。结论制备的琥珀酸去甲文拉法辛缓释微丸具备较理想的缓释效果。

OBJECTIVE To prepare sustained - release Desvenlafaxine succinate （DVS） pellets coated with aqueous ethylcellulose dispersion（ Surelease^（R）） and to investigate their drug release behavior. METHODS Orthogonal test was carried out on the results of single factor study to determine the process parameters of the preparation of pellets by extrusion roll method. The drug - containing pellets were coated with a Surelease ^（R） slow release material by fluidized bed. The in vitro release of the pellets was evaluated by comparing the original sustained release tablets, and the release data was fitted with a common model to explore its release mechanism. RESULTS The optimum process for the preparation of the drug - loaded pellets was a 8 ： 3.2 ratio of the material to the wetting agent,the extrusion speed of 55 r＂ min-1 ,the rolling speed of 1.0 x 103 r＂ min-~ and the spheronization time of 2 rain. The process also had good reproducibility and high yield. When the coating weight was 47.50% , the similar results with the original tablets could he achieved. CONCLUSION The preparation of DVS sustained release pellets has a desirable sustained release effect.