目的 制备漆黄素（fisetin，FIT）与β-环糊精衍生物的包合物，并对其包合行为和包合物的水溶性、稳定性进行研究。方法 通过超声法制备了漆黄素与2-羟丙基-β-环糊精［（2-hydroxypropyl）-β-cyclodextrin，HP-β-CD］、2，6-二甲基-β-环糊精［（2，6-di-O-methyl）-β-cyclodextrin，DM-β-CD］和磺丁基醚-β-环糊精（sulfobutyl ether-β-cyclodextrin，SBE-β-CD）的包合物；采用核磁共振氢谱（¹H-NMR和²D-NMR）、X射线粉末衍射（X-ray powder diffraction，XRD）、差示扫描量热法（differential scanning calorimetry，DSC）、扫描电子显微镜（scanning electron microscope，SEM）、紫外-可见光谱法（ultraviolet-visible spectrometry，UV）、Job曲线法对包合物进行表征；测定了包合物的水溶性，在模拟人体胃液和肠液环境下进行了稳定性的测试。结果 核磁共振（¹H-NMR和²D-NMR）分析表明，漆黄素从小口端进入HP-β-CD空腔，从大口端进入DM-β-CD和SBE-β-CD空腔。漆黄素与HP-β-CD、DM-β-CD和SBE-β-CD形成包合物后，其溶解度从0.05 mg/mL分别提高到了3.45、3.70、4.60 mg/mL。结论 漆黄素与β-环糊精衍生物形成包合物后，其溶解度、热稳定性及生物环境稳定性得到明显提高。

Objective To prepare fisetin (FIT) and β-cyclodextrin (β-CD) derivatives inclusion complexes[hydroxypropyl-β-cyclodextrin (HP-β-CD), dimethyl-β-cyclodextrin (DM-β-CD), sulfobutyl ether-β-cyclodextrin (SBE-β-CD)] and explore their inclusion behavior and the water solubility and stability of inclusion complexes. Methods The inclusion complexes of FIT with HP-β-CD, DM-β-CD and SBE-β-CD were prepared by ultrasonic method. Optimize the best inclusion process with drug loading as an index. Inclusion complexes was characterized by ¹H-NMR and ²D-NMR, X-ray powder diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscope (SEM), ultraviolet-visible spectrometry (UV-Vis), and Job curve methods; The water solubility of the inclusion complexes was measured and the stability test was conducted in the simulated human gastric juice and intestinal fluid environment. Results Nuclear magnetic resonance (¹H-NMR and ²D-NMR) analysis showed that FIT entered the HP-β-CD cavity from the small mouth end, and entered the DM-β-CD and SBE-β-CD cavity from the big mouth end. The solubility of FIT was increased from 0.05 mg/mL to 3.45, 3.70, 4.60 mg/mL for HP-β-CD, DM-β-CD and SBE-β-CD, respectively. Conclusion The solubility, thermal stability and biological environment stability had been significantly improved after the formation of inclusion complex.

R283.6

国家自然科学基金资助项目（U1602271）；云南省科技计划项目（2018ZE001）；云南省科技计划项目（202002AB080001）