蒿甲醚结肠定位微丸的制备及体外释放度评价

J4 ›› 2016, Vol. 1 ›› Issue (8): 8-.

蒿甲醚结肠定位微丸的制备及体外释放度评价

发布日期:2016-08-25

Study on the Preparation of Artemether Colon-specific Pellets and the Release in Vitro

Published:2016-08-25

摘要/Abstract

摘要：

［摘要］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。

关键词: ［关键词］蒿甲醚, pH 依赖型, 结肠定位, 体外释放度

Abstract:

〔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.

Key words: 〔Key words〕Artemether, pH controlled, colon-specific, release in vitro

中图分类号:

R944

马寅，张伟，张国丽，张锐武，杨兆祥. 蒿甲醚结肠定位微丸的制备及体外释放度评价[J]. J4, 2016, 1(8): 8-.