【摘要】：目的:本文考察了齊墩果酸(oleanolic acid,OA)和熊果酸(ursolic acid,UA)這2種難溶性同分異構(gòu)體與羥丙基-β-環(huán)糊精(hydroxypropyl-β-cyclodextrin,HP-β-CD)包合過程的差異。方法:觀察HP-β-CD與OA,UA相互作用時的核磁共振氫譜(~1H-NMR)和紫外吸收圖譜的變化。以包合效率(complexation efficiency,CE)為評價指標(biāo),采用相溶解度法比較OA和UA在不同取代度的HP-β-CD,pH值和溫度時包合過程的差異,并計算在包合過程中出現(xiàn)的熱力學(xué)參數(shù)。通過攪拌法分別制備了OA-HP-β-CD和UA-HP-β-CD包合物,差示掃描熱分析(DSC)和X-射線衍射(X-ray)鑒定包合物。結(jié)果:在紫外、~1H-NMR圖譜中,HP-β-CD與OA和UA相互作用產(chǎn)生氫鍵。在不同取代度的HP-β-CD,pH值和溫度下的包合效率OA高于UA,并且OA和UA的熱力學(xué)參數(shù)表明兩者包合過程存在差異。制備工藝簡單、易行;DSC和X-ray表征OA-HP-β-CD,UA-HP-β-CD包合物形成。結(jié)論:OA和UA可以與HP-β-CD形成包合物,增加藥物溶解度。OA和UA的結(jié)構(gòu)不同,兩者與HP-β-CD的包合過程存在差異。
[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.
【作者單位】： 南京醫(yī)科大學(xué);沈陽藥科大學(xué);無錫市人民醫(yī)院;
【基金】：2014年度江蘇省高等學(xué)校大學(xué)生創(chuàng)新創(chuàng)業(yè)訓(xùn)練計劃省級重點項目(201410312008Z)
【分類號】：R943

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