庆大霉素普鲁卡因胃漂浮缓释微丸的制备及质量评价

摘要

采用挤出滚圆法制备含药丸芯,运用流化床包衣技术对丸芯进行多层包衣以控制微丸的漂浮性和药物的释放特性,从而获得性能良好的庆大霉素普鲁卡因胃漂浮缓释微丸；利用紫外分光光度法测定普鲁卡因的含量和累积释放度,考察其体外漂浮和释药等性能.当m(普鲁卡因)∶m(庆大霉素)∶m(微晶纤维素)∶m(十八醇)∶m(NaHCO3)=10∶2∶20∶5∶1,以2％十二烷基硫酸钠为润湿剂时,所得丸芯圆整度较好；微丸包衣材料由内而外依次为尤特奇RS,NaHCO3和尤特奇RL,其增重分别为14.9％,10.2％和16.6％；所得微丸在人工胃液中迅速起漂,8h漂浮百分率超过90％,体外释放行为符合Higuchi扩散模型.结果表明:按本法制备的丸芯质量较好,所得包衣微丸达到了漂浮与缓释的双重要求.%An optimal preparation of gastric floating sustained-release pellets for gentamycin and procaine was attained,with its behaviors of floating and release investigated in vitro.The drugloaded pellet cores were prepared by extrusion-spheronization method and then coated with Eudragit RS,NaHCO3 and Eudragit RL successively by fluid bed coating equipment.A UV method was established to determine the procaine in pellets or in release medium.The optimal pellet cores with good sphericity were obtained when the weight ratio of procaine,gentamycin,MCC,stearyl alcohol and NaHCO3was 10 ∶ 2 ∶ 20 ∶ 5 ∶ 1,with 2％ sodium dodecyl sulfate as wetting agent.When the coating weight gains were 14.9％ for Eudragit RS,10.2％ for NaHCO3 and 16.6％ for Eudragit RL,the pellets could float immediately in simulated gastric fluid and more than 90％ remain floating after 8 h.Procaine was released sustainedly and the release behavior was well fitted to Higuchi equation.All these results showed that the pellets prepared as described in the present paper possessed excellent floating behavior and sustained release characteristics which had met the designed requirement.