磷霉素氨基葡萄糖盐β-CD包合物的制备与研究

Preparation and study of fosfomycin glucosamine salt β-CD inclusion complex

目的 制备磷霉素氨基葡萄糖盐(FA)-β-环糊精(β-CD)包合物,解决磷霉素氨基葡萄糖盐高温不稳定、引湿性强的问题。方法 采用冷冻干燥法制备FA-β-CD包合物,以包合率和收率为评价指标,单因素考察投料质量比、包合时间、包合温度对包合效果的影响;通过红外光谱分析、X-射线衍射法对FA-β-CD包合物进行鉴定;对FA、FA-β-CD包合物以及β-CD进行抗菌活性测试;对FA和FA-β-CD包合物及其溶液在不同温度下进行稳定性考察。结果冷冻干燥法制备FA-β-CD包合物的最佳工艺为m(β-CD)∶m(FA)=1.25∶1,包合时间为2h,包合温度为20℃;抗菌活性测试和稳定性考察结果均表明β-CD能够较好的保护FA。结论冷冻干燥法可以成功制备FA-β-CD包合物,并能提高FA的稳定性。

Objective To prepare fosfomycin glucosamine salt(FA)-β-cyclodextrin(β-CD) inclusion complex, and to solve the problems of instability in high temperature and strong hygroscopicity of fosfomycin glucosamine salt. Methods The FA-β-CD inclusion complex was prepared by freezedrying method, and the inclusion rate and yield were used as evaluation indicators. The inclusion complex was identified by infrared spectroscopy and X-ray diffraction;the antibacterial activity of FA, FA-β-CD inclusion complex and β-CD were tested;the stability of FA and FA-β-CD inclusion complexes was tested at different temperatures, and the changes in the antibacterial activity of the inclusion complex solutions were also measured. Results The optimal process for preparing FA-β-CD inclusion complex by freeze-drying method was m(β-CD) ∶ m(FA) = 1.25∶1, the inclusion time was 2 h, and the inclusion temperature was 20 ℃. The stability test showed that β-CD protected FA well. Conclusion Freeze-drying method can successfully prepare FA-β-CD inclusion complex, and improve the stability of FA.