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作 者:郭丽娟[1] 元永波[1] 李慧[1] 刘利军[1]
出 处:《中国实验方剂学杂志》2012年第2期18-21,共4页Chinese Journal of Experimental Traditional Medical Formulae
基 金:宁夏科技攻关项目(10GG018)
摘 要:目的:筛选制备异甘草素-β-环糊精(β-CD)包合物的最佳制备条件,以达到提高药物水溶性的目的。方法:采用正交设计试验以包合率和收率为指标优化最佳工艺条件,利用计算机模拟实验比较了不同包合方式和包合比的能量变化,通过IR和XRD对包合物进行表征,荧光光度法验证包合比。结果:采用饱和水溶液法制备包合物,最佳包合条件为异甘草素和β-CD的摩尔比1∶2,包合时间5 h,温度60℃。包合率>98%,可能的包合方式为异甘草素的A环进入β-CD的大口端,B环进入β-CD的小口端。结论:异甘草素制成β-CD包合物可以达到提高药物水溶性的目的。Objective:Selected optimum preparation condition of isoliquiritigenin β-cyclodextrin(β-CD) inclusion,in order to improve solubility of water-soluble drugs.Method:Preparation technology was optimized by orthogonal test with inclusion ratio and yield as indexes,energy change of different inclusion mode and inclusion ratio was compared by computer simulation experiment,inclusion was identified by IR and XRD power diffraction,and inclusion ratio was tested by fluorometry.Result:Inclusion was prepared by saturated aqueous solution method.Optimum inclusion condition was:molar ratio of isoliquiritigenin to β-CD 1∶2,inclusion time 5 h,temperature 60 ℃.Incusion efficiency could exceed 98%,possible inclusion approach was:A ring of isoliquiritigenin was external to 1arger side of β-CD,B ring of isoliquiritigenin was external to smaller side of β-CD.Conclusion:This result showed that water solubility was obviously increased of inclusion.
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