泛昔洛韦缓释微丸的研制

Preparation of Famciclovir Sustained-release Pellets

以Eudragit RSPO和RLPO为缓释材料,采用流化床包衣技术制备了泛昔洛韦缓释微丸。采用单因素试验筛选了增塑剂种类及用量、抗黏剂粒度、Eudragit RSPO和RLPO的配比及老化时间。所得优化参数为两种包衣材料配比19∶1,增塑剂为10%聚乙二醇6000,抗黏剂为20%滑石粉(1 250目),包衣增重25%,老化12 h。所制缓释微丸在1.5 h(0.1 mol/L盐酸)、3 h和8 h(pH 6.8磷酸盐缓冲液)的累积释放度分别为10%～30%、30%～70%和70%以上。药动学研究表明,本品与泛昔洛韦普通片相比具有明显的缓释特征。

The famciclovir sustained-release pellets were prepared by fluidized bed coating technology with Eudragit RSPO and Eudragit RLPO as coating material. The kind and amount of plasticizer, the mesh of anti-adhesive agent, the proportion of Eudragit RSPO to Eudragit RLPO and the curing time were investigated by single factor experiment. The optimal parameters were as follows： the proportion was 19 ： 1, the plasticizer was 10% polyethylene glycol 6000, the anti-adhesive agent was 20 % talc powder （1 250 mesh）, the coating level was 25 % and the curing time was 12 h. The cumulated release of product at 1.5 h （in 0.1 mol/L hydrochloric acid）, 3 h and 8 h （in pH 6.8 phosphate buffer） were 10%-30%, 30%-70% and over 70%. The pharmacokinetic test showed that the prepared pellets had significant sustained-release behavior compared with famciclovir tablets.