阿奇霉素缓释微粒的制备及其体外评价  

Development and in vitro Evaluation of Azithromycin Sustained-release Microparticles

作　　者：武晓荣 唐星[2] WU Xiao-rong;TANG Xing(Department of Pharmacy,Hebei General Hospital of Armed Police Force,Shijiazhuang 050086,China;School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]武警河北总队医院药剂科,河北石家庄050086 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《海峡药学》2022年第12期10-16,共7页Strait Pharmaceutical Journal

摘　　要：目的制备一种大剂量单次给药的阿奇霉素缓释微粒,并对其进行体外评价。方法运用热熔挤出和流化床包衣制备阿奇霉素缓释微粒,X射线粉末衍射、偏光显微镜和扫描电子显微镜对制剂进行表征,运用数学模型探讨药物释放机制,影响因素实验考察制剂稳定性。结果成功制备了以山嵛酸甘油酯为骨架的阿奇霉素缓释微粒,载药量为20%,加入5%的泊洛沙姆188作为致孔剂,粒径为180~250μm,以Eudragit■E PO为包衣材料,包衣增重为5%。药物以无定型形态存在于载体中,其释放更符合一级动力学过程,高湿对药物释放有较大影响。结论所得制剂释放曲线与市售制剂相似,药物分散均匀,具有一定的应用价值和发展前景。OBJECTIVE To prepare a high-dose,single-dose sustained-release microparticle of azithromycin,and evaluate it in vitro.METHODS Azithromycin sustained-release microparticles were prepared by Hot melt extrusion(HME)and coating in fluidized bed.Powder X-ray diffraction,polarized light microscopy and scanning electron microscopy were used to characterize the preparation.The mathematical models were used to discuss the drug release mechanism.The test of influencing factors was conducted to investigate the stability of the formulations.RESULTS Azithromycin sustained-release microparticles with glyceryl behenate as skeleton were successfully prepared.The drug loading was 20%.5%of poloxamer 188 was added as hole-maker,and the particle size was controlled at 180-250μm.Eudragit■ E PO was the coating material,and the coating weight gain was 5%.The drug existed in amorphous form in the carrier,and its release was more in line with the first-order kinetic process.High humidity has a great impact on the drug release.CONCLUSION The obtained azithromycin sustained-release microparticles have similar release curve to that of the commercial preparation and uniform drug dispersion,which indicate certain development prospects and application value.

关 键 词：阿奇霉素 缓释 微粒 热熔挤出 包衣 

分 类 号：R94[医药卫生—药剂学]