5-氨基水杨酸对乙酰氨基酚酯速释微丸制备工艺研究

Study on the preparation of 5-ASA-AAP immediate-release pellets

目的研制新型高效的抗溃疡性结肠炎药物5-ASA对5-ASA-AAP微丸。方法以5-ASA为起始物,首先合成对5-ASA-AAP,然后以溶剂蒸发—沉积法制备5-ASA-AAP固体分散体,最后采用挤出滚圆法制备5-ASA-AAP速释微丸。结果制备的5-ASA-AAP固体分散体在20min内溶出百分率大于60%;粒径在20～40目的微丸收率为83.81%。结论 5-ASA-AAP速释微丸的制备工艺稳定可行。

Objective To prepare 5-Aminosalicyl-Acetaminophen（5-ASA-AAP）immediate-release pellets. Methods 5-ASA was used as starting material to synthesize 5-ASA-AAP. Then by comparing several measures, the solvent evaporation-deposition method was selected to prepare the 5,ASA-AAP solid dispersion. At last, the 5-ASA-AAP pellets were prepared by extrusion-spheronization technology. Results Dissolution studies showed that the accumulated percentage of 5-ASA-AAP dissolved from the optimal solid dispersion in the first 20 minutes was more than 60 %. The weight ratio of pellets between 20mesh and 40mesh was about 83.81%. Conclusion The technique of preparing 5-ASA-AAP pellets is stable and feasible.