羟丙基-β-环糊精对齐墩果酸与熊果酸包合作用的研究
发布时间：2019-01-30 14:09
【摘要】：目的:本文考察了齐墩果酸(oleanolic acid,OA)和熊果酸(ursolic acid,UA)这2种难溶性同分异构体与羟丙基-β-环糊精(hydroxypropyl-β-cyclodextrin,HP-β-CD)包合过程的差异。方法:观察HP-β-CD与OA,UA相互作用时的核磁共振氢谱(~1H-NMR)和紫外吸收图谱的变化。以包合效率(complexation efficiency,CE)为评价指标,采用相溶解度法比较OA和UA在不同取代度的HP-β-CD,pH值和温度时包合过程的差异,并计算在包合过程中出现的热力学参数。通过搅拌法分别制备了OA-HP-β-CD和UA-HP-β-CD包合物,差示扫描热分析(DSC)和X-射线衍射(X-ray)鉴定包合物。结果:在紫外、~1H-NMR图谱中,HP-β-CD与OA和UA相互作用产生氢键。在不同取代度的HP-β-CD,pH值和温度下的包合效率OA高于UA,并且OA和UA的热力学参数表明两者包合过程存在差异。制备工艺简单、易行;DSC和X-ray表征OA-HP-β-CD,UA-HP-β-CD包合物形成。结论:OA和UA可以与HP-β-CD形成包合物,增加药物溶解度。OA和UA的结构不同,两者与HP-β-CD的包合过程存在差异。
[Abstract]:Aim: to investigate the inclusion process of oleanolic acid (oleanolic acid,OA) and ursolic acid (ursolic acid,UA) with hydroxypropyl 尾 -cyclodextrin (hydroxypropyl- 尾-cyclodextrin,HP- 尾-CD). Methods: the changes of nuclear magnetic resonance (1H-NMR) and UV absorption spectra of HP- 尾-CD interacting with OA,UA were observed. With the inclusion efficiency (complexation efficiency,CE) as the evaluation index, the phase solubility method was used to compare the differences between OA and UA in the inclusion process at different HP- 尾-CD,pH values and temperatures, and the thermodynamic parameters in the inclusion process were calculated. The inclusion complexes of OA-HP- 尾-CD and UA-HP- 尾-CD were prepared by stirring method. The inclusion complexes were identified by differential scanning calorimetry (DSC) and X-ray diffraction (X-ray). Results: in UV, ~ 1H-NMR spectra, HP- 尾-CD interacted with OA and UA to form hydrogen bonds. The inclusion efficiency (OA) of HP- 尾-CD,pH at different degree of substitution and temperature is higher than that of UA, and the thermodynamic parameters of OA and UA show that there are differences in the inclusion process between them. DSC and X-ray were used to characterize the formation of OA-HP- 尾-CD,UA-HP- 尾-CD inclusion complex. Conclusion: OA and UA can form inclusion complexes with HP- 尾-CD and increase their solubility. The structures of OA and UA are different from those of HP- 尾-CD.
【作者单位】： 南京医科大学;沈阳药科大学;无锡市人民医院;
【基金】：2014年度江苏省高等学校大学生创新创业训练计划省级重点项目(201410312008Z)
【分类号】：R943
[Abstract]:Aim: to investigate the inclusion process of oleanolic acid (oleanolic acid,OA) and ursolic acid (ursolic acid,UA) with hydroxypropyl 尾 -cyclodextrin (hydroxypropyl- 尾-cyclodextrin,HP- 尾-CD). Methods: the changes of nuclear magnetic resonance (1H-NMR) and UV absorption spectra of HP- 尾-CD interacting with OA,UA were observed. With the inclusion efficiency (complexation efficiency,CE) as the evaluation index, the phase solubility method was used to compare the differences between OA and UA in the inclusion process at different HP- 尾-CD,pH values and temperatures, and the thermodynamic parameters in the inclusion process were calculated. The inclusion complexes of OA-HP- 尾-CD and UA-HP- 尾-CD were prepared by stirring method. The inclusion complexes were identified by differential scanning calorimetry (DSC) and X-ray diffraction (X-ray). Results: in UV, ~ 1H-NMR spectra, HP- 尾-CD interacted with OA and UA to form hydrogen bonds. The inclusion efficiency (OA) of HP- 尾-CD,pH at different degree of substitution and temperature is higher than that of UA, and the thermodynamic parameters of OA and UA show that there are differences in the inclusion process between them. DSC and X-ray were used to characterize the formation of OA-HP- 尾-CD,UA-HP- 尾-CD inclusion complex. Conclusion: OA and UA can form inclusion complexes with HP- 尾-CD and increase their solubility. The structures of OA and UA are different from those of HP- 尾-CD.
【作者单位】： 南京医科大学;沈阳药科大学;无锡市人民医院;
【基金】：2014年度江苏省高等学校大学生创新创业训练计划省级重点项目(201410312008Z)
【分类号】：R943
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