反溶剂重结晶法制备阿奇霉素超细粉体

Preparation of ultrafine azithromycin by anti-solvent recrystallization

采用反溶剂重结晶法进行了阿奇霉素微粉化实验研究。系统考察了药物溶液质量浓度、溶剂反溶剂比例、搅拌时间、干燥方式等因素对产品形貌和粒度的影响。得到较优的制备工艺条件为:药物溶液质量浓度0.2 g/mL、溶剂反溶剂体积比1∶20及搅拌时间10 min,可制备出平均粒径为270 nm的药物颗粒,经喷雾干燥可得粒径为2～5μm的阿奇霉素超细粉体。采用扫描电镜、比表面积测试、红外光谱分析和体外溶出实验对原料药及产品性质进行分析表征,分析结果表明,阿奇霉素超细粉体化学结构不变,且比表面积增大8倍,溶解速率明显提高。

Ultrafine azithromycin（AZM） powder has been prepared by anti-solvent recrystallization.The effects of varying the experimental parameters,such as AZM solution concentration,solvent/anti-solvent ratio,stirring time and drying method,on the particle size and morphology,were investigated.The results showed that the optimum conditions were an AZM solution concentration of 0.2g/mL,solvent/anti-solvent ratio of 1∶20 and stirring time of 10 min.Under these conditions,ultrafine AZM particles with a mean particle size of 270 nm could be precipitated.AZM dry powder with a particle size ranging from 2 to 5 μm was subsequently prepared by spray drying.The commercial crude AZM and as-prepared powder were characterized by SEM,BET,FT-IR and dissolution tests.The analyses indicated that the chemical structure of as-prepared ultrafine AZM powder remained unchanged.The specific surface area of the ultrafine AZM powder increased 8 times and it exhibited a significantly improved dissolution rate.