蒿甲醚结肠定位微丸的制备及体外释放度评价

摘要

〔Abstract〕Objective:To prepare Artemether colon-specific pellets controlled by pH and study the release in vitro. Methods:The cores of pellets were made by extrusion-spheronization. Pellets were prepared using a fluid bed coater , with Eudragit S100 as the out layer, triethyl citrate added to the dispersion as the plasticizer. Results:Artemether was not detected in solution of pH 1.2 for 2 h. The accumulative release in pH 6.8 phosphate buffer for 4 h was smaller than 5%. While the accumulative release in the pH 7.6 phosphate buffer for 3 h was more than 90%. Conclusion:Colon-specificpellets prepared in this way can well perform colon-specific delivery.%目的：拟制备蒿甲醚pH依赖型结肠定位微丸，并对其体外释放度进行考察。方法：采用挤出滚圆法制备丸芯，采用Eu⁃dragit S100作为包衣材料，柠檬酸三乙酯作为增塑剂，使用流化床包衣设备进行包衣。结果：在pH 1.2溶液2 h中未检测到蒿甲醚；在pH 6.8磷酸盐缓冲液中4 h累积释放度均小于5%；而在pH 7.6磷酸盐缓冲液中，3 h累积释放度均达90%以上。结论：本方法制备的蒿甲醚结肠定位微丸能达到结肠定位释药的目的。