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目的采用乙基纤维素水分散体(Surelease~)为包衣材料制备琥珀酸去甲文拉法辛(DVS)缓释微丸,并评价其体外释药性能。方法采用溶液上药法,在蔗糖空白丸芯的基础上旋转锅包衣法上药,通过正交筛选优化上药工艺,再以Surelease~为缓释材料进行包衣,以原研缓释片为参比对微丸的体外释放进行评价,并将释放数据用常用模型拟合,探讨其释放机制。结果所得缓释微丸的载药量和上药率均较高,含量均匀,当聚合物包衣增重32.4%时可达到与原研缓释片一致的释放特性,在pH1.2、pH4.5、水、pH6.8的释放介质中两者的相似因子分别为86.65、69.94、67.47、67.97,体外释放曲线符合一级方程。结论制备的DVS缓释微丸具有较理想的缓释效果。
OBJECTIVE To prepare desvenlafaxine succinate (DVS) sustained-release pellets with ethylcellulose aqueous dispersion (Surelease ~ ) as coating material and to evaluate its in vitro drug release properties. Methods The method of solution on the basis of sucrose blank pellets on the basis of rotary pan coating method on drugs, through the orthogonal screen to optimize the drug process, then Surelease ~ for sustained-release material coating, In order to evaluate the in vitro release of pellets, the release data were fitted with the common model to investigate the release mechanism. Results The sustained-release pellets had higher drug loading rate and higher drug loading rate, with uniform content. When the weight gain of the polymer coating was 32.4%, the sustained release pellets could reach the same release characteristics as the original release tablets at pH 1.2 and pH 4. 5, water, pH6.8 release medium similarity between the two were 86.65,69.94,67.47,67.97, in vitro release curve in line with the first-order equation. Conclusion The prepared DVS sustained-release pellets have an ideal sustained-release effect.