磺丁基醚-β-环糊精对桂利嗪的包合作用

Utilization of sulfobutyl ether-β-cyclodextrin as the solubilizer of cinnarizine

目的通过研究磺丁基醚-β-环糊精对桂利嗪增溶作用,包合物的制备以及包合物光谱学结构确证来研究磺丁基醚-β-环糊精对桂利嗪的包合作用。方法在25℃运用相溶解度法进行实验,采用紫外分光光度法测定桂利嗪在溶液中的浓度;采用冷冻干燥法来制备磺丁基醚-β-环糊精桂利嗪包合物,再使用DSC和X-射线衍射法来进行结构确证。结果随着磺丁基醚-β-环糊精浓度增加和pH值减小,桂利嗪的溶解度显著提高;采用冷冻干燥法制备包合物时,桂利嗪被完全包入磺丁基醚-β-环糊精孔穴内部。结论磺丁基醚-β-环糊精可提高难溶性药物桂利嗪的溶解度并能形成稳定的包合物。

Objective To study the clathration of ether-β-cyclodextrin（SBE-β-CD）with cinnarizine through solution effects,complexes preparation and structure identification by spectrum method.Methods The solubilization experiment was performed by the phase-solubility method at 25 ℃.The concentration of cinnarizine was determined by the UV spectrophotometric method.Freeze drying method was used in the preparation of complexes and the complexes were verified using DSC and X-ray diffraction.Results The apparent solubility of cinnarizine was enhanced obviously with the increase of concentration SBE-β-CD and decrease of pH values.The apparent stability constants were calculated respectively.Conclusions SBE-β-CD is a good solubilizer for cinnarizine and can form stable complexes with it.