头孢丙烯掩味微丸的制备及其丸芯的处方工艺优化

Preparation of Cefprozil Bitter-masked Pellets and Optimization of Formulation and Technology of Its Pellet Core

目的:制备头孢丙烯掩味微丸,优化其丸芯处方工艺。方法:采用粉末层积离心造粒法载药制备头孢丙烯丸芯,以黏合剂浓度、喷浆转速和供粉速度为因素,以粒径分布、收率、脆碎度、休止角和平面临界角的综合评分为指标,采用正交试验优化头孢丙烯丸芯的处方与工艺;所得丸芯以滑石粉、聚丙烯酸树脂和甜橙香精行掩味包衣,评价口感和累积溶出度。结果:头孢丙烯丸芯的最优处方工艺为黏合剂浓度3%、喷浆转速15 r/min、供粉速度30 r/min;所制头孢丙烯丸芯40~50目粒径分布94.0%,收率(92.1±2.9)%,脆碎度(1.1±0.1)%,休止角(23.2±0.4)°,平面临界角(6.5±0.4)°(n=3)。包衣后头孢丙烯掩味微丸无苦感,在45 min内的头孢丙烯累积溶出度超过85%。结论:成功制得头孢丙烯掩味微丸,其中头孢丙烯丸芯优化后处方合理。

OBJECTIVE:To prepare Cefprozil bitter-masked pellets,and optimize its pellet core.METHODS:Pellet core of cefprozil were prepared by powder layering with centrifugal granulation,using adhesive concentration,guniting rotation speed and supplying powder speed as factors,comprehensive score of particle size distribution,yield,friability,repose angle and plane critical angle as indexes,the orthogonal test was used to optimize the formulation and technology of pellet core of cefprozil.Then the bitter of pellet core was masked by coating with talcum powder,polyacrylic acid resin and orange essence.The texture and accumulative dissolution rate was evaluated.RESULTS:The optimal formulation and technology of pellet core of cefprozil were adhesive concentration of 3%,guniting rotation speed of 15 r/min and supplying powder speed of 30 r/min.The prepared pellet core of cefprozil with 40-50 meshes were particle size of 94.0%,yield of(92.1±2.9)%,friability of(1.1±0.1)%,angle of repose of(23.2±0.4)°,plane critical angle of(6.5±0.4)°(n=3).After coating,Cefprozil bitter-masked pellets were bitterless,and accumulative dissolution rate of cefprozil was more than 85%within 45 min.CONCLUSIONS:Cefprozil bitter-masked pellets are prepared successfully,and the optimized formulation of pellet core of cefprozil are rational.