扑热息痛缓释微丸的制备

Preparation of sustained-release pellets of paracetamol

目的制备扑热息痛缓释微丸,并对其体外释药情况进行研究。方法采用挤出滚圆法制备扑热息痛素丸,在流化床内采用丙烯酸树脂水分散体对其包衣,制备扑热息痛缓释微丸。用释放度测定法考察影响药物释放的各种因素,对包衣微丸体外释药机理进行研究。结果包衣材料为丙烯酸树脂NE30D(Eudragit NE30D),质量分数增加6%时包衣微丸在pH 6.18的磷酸盐缓冲液中呈现良好的缓释效果,体外释药过程基本符合Higuchi方程:Y=31.213t1/2+0.425(r=0.993 2)。结论采用挤出滚圆法和丙烯酸树脂流化床包衣,成功地制备了扑热息痛缓释微丸,其体外释药缓慢、持续平稳。

Objective To prepare paracetamol sustained-release pellets and investigate the drug release mechanism in vitro. Methods Extrusion-spheronisation method was used to prepare uncoated pellets. Eudragit NE30D dispersions were coated as a sustained-release layer in a fluid-bed equipment. The release mechanism of the drug from the pellets was studied. Results The main factors affecting the release rate were the type and the amount of the coating material applied. Release of the drug from pellets was in accordance with Higuchi equation. Conclusions The method and the formulation are proved to be successful in providing slow and steady release of paracetamol from sustained-release pellets.