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

作　　者：张尹萌 马强 金学平[2,3] 祝宏 ZHANG Yin-meng;MA Qiang;JIN Xue-ping;ZHU Hong(School of Chemical Engineering and Pharmacy,Wuhan Institute of Technology,Hubei Key Laboratory of Novel Reactor and Green Chemical Technology,Wuhan 430205;Wuhan Vocational College of Software and Engineering,Wuhan 430205;Wuhan Research Center for Drug Solubilization and Delivery Technology,Wuhan 430205)

机构地区：[1]武汉工程大学化工与制药学院新型反应器与绿色化学工艺湖北省重点实验室,武汉430205 [2]武汉软件工程职业学院,武汉430205 [3]武汉市药物增溶工程技术研究中心,武汉430205

出　　处：《中南药学》2023年第2期375-379,共5页Central South Pharmacy

摘　　要：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.

关 键 词：Β-CD 磷霉素氨基葡萄糖盐 包合物 工艺优化 

分 类 号：R944[医药卫生—药剂学]