离心造粒法制备利巴韦林缓释微丸

Preparation of ribavirin sustained-release pellets by centrifugal granulation technology

目的研究离心造粒粉末层积法制备利巴韦林缓释微丸。方法采用BZJ-360M离心包衣造粒机制备微晶纤维素空白丸核和利巴韦林含药素丸,并在此基础上进行丙烯酸树脂水分散体(Eudragit○RNE30D)包衣。通过单因素考察筛选包衣水平并对包衣微丸的释药特征进行探讨。结果以水为润湿剂微晶纤维素空白母核32～40目收率为803%;在空白丸核的基础上以3%羟丙甲基纤维素水溶液为黏合剂,以含利巴韦林91%微晶纤维素9%混合物为层积粉料,所得含药微丸20～24目收率为901%,药物含量为725%。利巴韦林缓释微丸的释药机制主要是以膜控为主的扩散作用,释药动力为渗透压驱动力。结论该制备技术操作灵活,包衣均匀,载药量高,可自动化操作。

OBJECTIVE: To prepare ribavirin sustained-release pellets by centrifugal granulation technology. METHODS: Ribavirin pellets were prepared by means of powder layering with the centrifugal granulation equipment. Ribavirin pellets were coated in the same equipment with Eudragit&reg NE30D as coating material. The release mechanism of coated pellets was studied by fitting with different release models. RESULTS: The yield of ribavirin pellets was 90.1% and drug content was 72.5%. The drug release from coated pellets was promoted by osmotic pressure. CONCLUSION: The preparation of technology ribavirin sustained-release pellets can be used in large-scale industrial production.