去氧氟尿苷结肠靶向双层包衣片的制备及其体外释放度  

Preparation and in vitro Release of Colon-specifi c Double-coated Tablets Loaded with Doxifl uidine

作　　者：刘源[1] 李毅 尹罡[1] 任静[1] 

机构地区：[1]成都学院(成都大学)四川抗菌素工业研究所,四川成都610052

出　　处：《中国医药工业杂志》2016年第1期53-55,共3页Chinese Journal of Pharmaceuticals

基　　金：成都大学校青年基金资助项目(2014XQCKS13);药食同源植物资源开发四川省高校重点实验室开放基金项目(10Y201505)给予资助

摘　　要：先采用湿法制粒压片法制备去氧氟尿苷（1）片芯;再以果胶和海藻酸钠（2∶1）为内层衣主要材料（增重5%-10%）、Eudragit S100为外层衣主要材料（增重12%-15%）依次包衣,得到1口服结肠靶向双层包衣片。采用桨法测定所得制品在不同p H值介质中的溶出度。结果表明,制品在人工胃液（稀盐酸）中不释药,在人工小肠液（p H 6.8磷酸盐缓冲液）中不溶出或少溶出,但在人工结肠液（p H 7.8磷酸盐缓冲液）中能快速释药（2 h释出85%以上）,提示所得制品具有结肠靶向作用。The cores of the title tablets loaded with doxifluidine （1） were prepared by wet granule compression technique. Then the inner layer with pectin and sodium alginate （2 ： 1） as main materials and weight gain of 5 %-10% and the outer layer with Eudragit S100 as the material and weight gain of 12%--15 % were coated over the surface of the above cores in sequence to obtain the title tablets. The in vitro release profiles of 1 from the tablets in media with different pH values were investigated by paddle method. The results showed that 1 did not release in artificial gastric fluid （dilute hydrochloric acid） and none or a little released in artificial intestinal fluid [phosphate buffer （PBS）, pH 6.81, while more than 85 % of 1 could release from the tablets within 2 h in artificial colonic fluid （PBS, pH7.8）. It indicated that the product had a colon targeting property.

关 键 词：去氧氟尿苷 结肠靶向 双层包衣片 体外释放 

分 类 号：R944.4[医药卫生—药剂学]