非布司他纳米缓释微丸的制备与体外释放度研究

Preparation and in vitro Dissolution of Febuxostat Nanosuspension Sustained-release Pellets

目的:制备非布司他纳米混悬剂,并进一步制备成缓释微丸,考察其体外释放度。方法:采用高压均质法制备非布司他纳米混悬剂,通过流化床底喷包衣技术制备非布司他载药微丸,使用丙烯酸树脂RL30D和丙烯酸树脂RS30D包缓释层衣,制备成非布司他纳米缓释微丸,并评价其释药机制。结果:制备的非布司他纳米混悬剂的平均粒径为(212.5±36.3)nm,多相分散系统(PdI)为(0.193±0.018),Zeta电位为(-12.4±0.3)mV,扫描电镜显示非布司他纳米混悬剂大小分布较均一;制备的非布司他纳米缓释微丸体外释药较为平缓,符合一级释放模型。结论:本研究制备非布司他纳米混悬缓释微丸体外释药平缓,为非布司他临床应用提供全新给药方案。

Objective： To prepare febuxostat nanosuspension and prepare sustained-release pellets,and investigate the in vitro dissolution. Methods： Febuxostat nanosuspension was prepared by a high pressure homogenization method. Febuxostat nanosuspension pellets were prepared by fluidized bed coating technique. Eudragit RL30D and Eudragit RS30D were used to prepare the sustained-release pellets. The dissolution mechanism of febuxostat nanosuspension sustained-release pellets was evaluated. Results： The average particle size of the prepared febuxostat nanosuspension was（ 212. 5 ± 36. 3） nm,PdI was（ 0. 193 ± 0. 018）,zeta potential was（-12. 4 ± 0. 3） mV,and the scanning electron microscopy showed that the particle size distribution of febuxostat nanosuspension was narrow. The in vitro dissolution of febuxostat nanosuspension sustained-release pellets was more stable and conformed to the first-order release model. Conclusion： The in vitro dissolution of febuxostat nanosuspension sustained-release pellets is more stable,and the preparation provides a new choice for febuxostat clinical application.