喷雾干燥法制备罗红霉素掩味肠溶缓释微球

Preparation of masked enteric microcapsule of roxithromycin by spray drying

目的采用喷雾干燥法制备罗红霉素肠溶掩味微球,得到最佳掩味工艺。并对微球性质进行考察。方法以包封率为评价指标,对喷雾干燥工艺参数进行正交优化设计,并考察Eudragit L100用量、微球芯材比对微球性能的影响,同时对掩味效果进行考察。结果最优工艺条件为进风温度145℃;进料速度10mL/min;喷雾压力0.3MPa;药物与Eudragit L100材料的质量比1:4;制得的微球外形良好,包封率可达96.38%;药物掩味效果良好;药物在人工肠液中缓慢释放,药物1h释放量不超过30%,24h不低于99%。结论所得制备工艺可行,实验条件制得的微球球形圆整,包封率较高,掩味效果良好,有很好的缓释特征。

Objective To prepare roxithromycin enteric masking microsphere by spray drying and get the optima masking technique and study the characterization of microsphere. Methods Orthogonal designing was applied to investigate and optimize the technique operation of spray drying .Influence of the polymer material Eudragit L100 dosage, the ratio of core and polymer material were studied using embedding ratio（ER）as a standard;also, the masking effect was investigated. Results The optimal condition for spray drying technique is as follows, temperature as 145~C. Spray pressure as 0.35MPa. Feeding rate as 15mL/min, the best ratio of core and polymer material as 1：4, By which, the ratio of embed （ER） could reach 96.38% with good masking effect, the drug released was no more than 30% in lh, not less than 99% in 24h. Conclusion The roxithromycin microspheres prepared by the established method were round and full, with satisfying ER, good masking effect and slow release.