氟苯尼考-β-环糊精包合物的制备与结构表征

摘要

目的 为改善氟苯尼考的水溶性,采用β-环糊精包合技术制备氟苯尼考可溶性粉.方法 通过正交试验筛选最佳包合工艺,以包合率和包合物产率为评价指标,以差示扫描量热分析法,傅里叶红外光谱法,电镜扫描对包合物进行结构确证.结果 试验结果表明:最佳包合条件为氟苯尼考与β-环糊精投料摩尔比1:1、包合温度80℃、包合时间2h、搅拌速度500r/min;差示扫描量热分析,傅里叶红外光谱分析和电镜扫描结果证实氟苯尼考-β-环糊精包合物的形成;氟苯尼考-β-环糊精包合物的包合率平均值为91.85％,产率平均值为91.26％,15min溶出率达到100％,为氟苯尼考的5倍.结论 采用饱和水溶液法制备氟苯尼考-β-环糊精包合物的制备工艺方法简单,可提高氟苯尼考水溶性.%Objective To improve the water solubility of florfenicol,water-soluble florfenicol powder was prepared by inclusion technology with β-cyclodextrin.Methods Taking inclusion rate and the yield of inclusion complex as evaluation indexes,the best inclusion process was screened by orthogonal experiments,the inclusion complex was identified by differential scanning calorimetry analysis (DSC),Fourier transform infra-red spectroscopy (FTIR),scanning electron microscopy (SEM).Results The results showed that the optimum preparation conditions were florfenicol:β-cyclodextrin=l:l(mole ratio),the inclusion temperature was 80℃,the inclusion time was two hours and the stirring speed was 500r/min.Differential scanning calorimetry analysis (DSC),Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM) showed that florfenicol-β-cyclodextrin inclusion complex had formed.The inclusion ratio of florfenicol-β-cyclodextrin inclusion complex was 91.85％ and the yield of florfenicol-β-cyclodextrin inclusion complex was 91.26％.The dissolution rate of florfenicol-β-cyclodextrin was 100％ in 15 minutes which was five times as much as florfenicol crude drug.Conclusion The preparation method of florfenicol-β-cyclodextrin inclusion complex with saturated solution method is simple and can improve the water solubility of florfenicol.