喷雾干燥法制备对乙酰氨基酚缓释微球

目的 利用喷雾干燥法制备对乙酰氨基酚缓释微球,并考察其释放度.方法 以对乙酰氨基酚为模型药、乙基纤维素为载体材料、95 %乙醇为溶剂进行喷雾干燥而制备.结果 所制微球外观为圆整球形,粒度分布均匀,其体外释放度1 h时不少于15 %,2 h不超过40 %,12 h在90 %以上;在pH6.8的磷酸盐缓冲液中可缓慢并稳定地释放.经大鼠体内药物动力学研究表明,微球具有明显的缓释效果.结论 所制微球具有很好的缓释作用,操作方便,工艺稳定,有利于工业化生产.

Preparation of paracetamol sustained-released microspheres by spray drying

OBJECTIVE To prepare paracetamol sustained-released microspheres by spray drying,and to investigate the dissolution of the sustained-released preparation.METHODS The sustained-released microspheres were prepared spray drying,using paracetamol as model drug,ethylcellulose as carrying agent materials,and 95 % ethyl alcohol as dissolvent.RESULTS The morphology of paracetamol sustained-released microspheres was spherical and well distributed.The release property of microspheres in vitro was slow and stable,and the release rate was less than 15% in 1 h,not exceecded 40% in 2 h,while over 90% in 12 h in the pH6.8 phosphate buffer.The in vivo research of pharmacokinetics in rat demonstrated the microspheres have good sustained-released characteristics.CONCLUSION The microspheres sustained released well in vitro and in vivo and its convenient preparation is suitable for industrialization and production.