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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: To screen the best preparation conditions of the inclusion compound of isoliquiritigenin-β-cyclodextrin (β-CD) in order to improve the water-solubility of the drug. Methods: Orthogonal design was used to optimize the optimum technological conditions with the inclusion rate and the yield as the indexes. The energy changes of different inclusion methods and inclusion ratios were compared by computer simulation. The inclusion complex was characterized by IR and XRD , Fluorescence spectrophotometry to verify inclusion ratio. Results: The inclusion complex was prepared by saturated aqueous solution. The optimal inclusion conditions were isoliquiritigenin and β-CD molar ratio of 1: 2, inclusion time of 5 h and temperature of 60 ℃. Inclusion rate> 98%. The possible inclusion way is that the A ring of isoliquiritigenin enters the large mouth of β-CD, and the B ring enters the small mouth of β-CD. Conclusion: β-CD inclusion of isoliquiritigenin can improve the water-solubility of drugs.