吉非替尼微丸胶囊的研制

Preparation of Capsules Filled with Gefitinib Pellets

利用流化床包衣技术,在空白丸芯上依次包主药层和包衣层,制成吉非替尼微丸后装填胶囊,并采用正交设计优化包衣工艺参数。考察了自制品及原研品(易瑞沙)在pH 1盐酸和pH 6.8磷酸盐缓冲液(PBS)中的溶出度。结果两种剂型在盐酸中30 min的溶出率均高于90%,而在PBS中则低于20%。通过破坏性试验和影响因素试验初步评价了自制品的稳定性。结果表明,经强酸、强碱、氧化或光照破坏后,测得的有关物质均小于0.6%;在高温、强光及高湿条件下放置10 d,性状、含量、有关物质及溶出度无明显改变。

The blank pill core was sequentially coated on the active ingredient layer and inactive ingredients layer by fluidized bed coating method to obtain the gefitinib pellets. The prepared pellets were filled into the capsules. The parameters of the coating process were optimized by orthogonal design. The in vitro dissolution behaviors in pH 1 hydrochloric acid and pH 6.8 phosphate buffer （PBS） of the product and the original preparation （Iressa） were investigated. The results showed that the dissolution at 30 rain of both preparations were over 90 % in hydrochloric acid while in PBS were below 20 %. The destructive test and influencing factor test were carried out to evaluate the preliminary stability of the product. The results showed that the related substances of the product after destruction by acid, alkali, oxidation or light were less than 0.6 %. After storing the pellets under high temperature, light or high humidity condition for 10 d, the appearance, content, related substances and dissolution had no significant changes.