1-脱氧野尻霉素控释微丸的制备及其性能研究

以1-脱氧野尻霉素为原料，羟丙基甲基纤维素钛酸酯作为控释包衣材料，以微晶纤维素为芯材制备空白丸芯，羟丙基甲基纤维素作为黏合剂进行上药，采用流化床进行包衣制备了载药1-脱氧野尻霉素控释微丸。制备后的微丸装入胶囊中。SEM分析表明，制备的控释微丸呈近圆球状，表面光滑、均匀紧致，横切面丸芯、上药层与控释层清晰可见，厚度均匀一致，说明包衣工艺稳定。控释胶囊中1-脱氧野尻霉素含量均匀度好且杂质符合规定。在体外溶出试验中，分别在pH值1.2、4.5和6.8的溶出介质中，1-脱氧野尻霉素制备控释微丸与1-脱氧野尻霉素速释片溶出曲线有很大的差异，在1~12h呈现零级线性释放，控释效果良好。产品分别在高湿度92.5%、强光照（4500±500） lx和高温条件下存放30d，存放后产品稳定性良好。

Preparation and Properties of 1-Deoxynojirimycin Controlled-release Pellets

Fluidized bed coater was employed to prepare controlled-release pellet core with 1-deoxynojirimycin as raw material and hydroxypropyl methely cellulose phthalate as coating material. Blank pellet core was prepared with microcrystalline cellulose. Hydroxypropyl methyl cellulose was used as adhesives to administer medicines. The prepared pellets were packed into capsule. In the dissolution test, it was found that 1-deoxynojirimycin pellets exhibited controlled release effect. SEM analysis showed that the controlled-release pellets were nearly ball shape,the surface was smooth,uniform and compact,and the pellet core,durg layer and controlled-release layer were clearly and had uniform thichness,which indicated that the coating teachnology was stable.The capsules had the uniform content of 1-deoxynojirimycin and the impurities accorded with the regulation.The drug releases of the 1-deoxynojirimycin controlled-release pellets in medias with pH value of 1.2, 4.5 and 6.8 were studied. Compared controlled-release pellets with immediate-release tablets, there was significant difference in the mean cumulative drug concentration profile in different media evaluation. The results indicated that drug release profiles from 1 to 12 hours showed excellent zero-order release character in vitro.Exposed on the conditions of RH 92.5%, strong light (4500±500)lx and high temperature 60℃, respectively, the product was stable.