熔融挤出法制备阿司匹林肠溶颗粒

Preparation of Aspirin Enteric Granules by Hot Melt Extrusion Technology

目的优化熔融挤出法制备阿司匹林肠溶颗粒的配方和方法。方法以pH值1.2介质中耐酸性与pH值6.8介质中的溶出度为评价指标;以星点设计方法优选肠溶材料与辅料配比。结果以79.8%醋酸羟丙甲纤维素琥珀酸酯为肠溶材料,4.2%十八醇为释药调节剂,3.0%微粉硅胶为润滑剂,于130℃下挤出,过程顺利,颗粒均一;所得载药颗粒在pH值1.2盐酸中2 h溶出(9.1±0.56)%,在pH值6.8缓冲液中45 min溶出(72.42±3.06)%。结论熔融挤出法制备阿司匹林肠溶颗粒简便、可靠。

Objective To optimize the formulation and process of aspirin-loaded enteric granules by hot melt extrusion technology.Methods Using drug dissolution ratio in hydrogen chloride(HCl,pH=1.2)and buffer(pH=6.8)solution as the evaluation index,the central composite design was applied to optimize the formulation.Results HPMCAS(79.8%),octadecyl alcohol(4.2%)and silica gel(3.0%)were used as enteric material,drug release modifier,and lubricant,respectively.Homogeneous granules were extruded smoothly at 130℃;the dissolution ratio of the granules were(9.1±0.56)%at 2 h in HCl(pH=1.2),and(72.42±3.06)%at 45 min in PBS(pH=6.8),respectively.Conclusion Hot melt extrusion technology is suitable and reliable for preparing aspirin enteric granules.