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目的:制备阿奇霉素壳聚糖-海藻酸钠肠溶微球,并评价各因素对微球性质的影响。方法:以壳聚糖-海藻酸钠为基质材料,采用复凝聚法制备阿奇霉素壳聚糖-海藻酸钠肠溶微球。通过单因素考察研究对粒径、收率和包封率影响较大的因素,以包封率和释放度为指标进行正交设计优化最佳处方。结果:海藻酸钠浓度为3%、氯化钙浓度为2.5%、壳聚糖浓度为0.25%,和投药量为20%为最佳处方。该处方制得的微球形态圆整,粒径分布合理,包封率和收率均较高。体外溶出试验表明,该条件制得的微球在酸中的释放量小于10%,可减少阿奇霉素的胃肠道不良反应;在pH 6.8的缓冲液中快速释放,能迅速达到最小抑菌浓度(MIC)。结论:阿奇霉素壳聚糖-海藻酸钠肠溶微球能有效避免药物在酸性环境中释放。
OBJECTIVE: To prepare azithromycin chitosan-alginate enteric-coated microspheres and evaluate the effect of various factors on the properties of microspheres. Methods: Chitosan - sodium alginate as matrix material, the use of complex coacervation Azithromycin chitosan - alginate enteric microspheres. Through single factor study to study the factors that affect the particle size, yield and entrapment efficiency, the optimal prescription was optimized by orthogonal design using the entrapment efficiency and release rate as the indexes. Results: Sodium alginate concentration of 3%, calcium chloride concentration of 2.5%, chitosan concentration of 0.25%, and the dosage of 20% is the best prescription. The microsphere prepared by this prescription has the advantages of round shape, reasonable particle size distribution and high entrapment efficiency and yield. In vitro dissolution tests showed that the release of the microspheres in this condition was less than 10% in the acid can reduce the side effects of azithromycin gastrointestinal tract; in pH 6.8 buffer quickly released, can quickly reach the minimum inhibitory concentration ( MIC). Conclusion: Azithromycin chitosan-alginate enteric-coated microspheres can effectively prevent drug release in acidic environment.