Preparation and physicochemical characteristics of the complex of edaravone with hydroxypropyl-β-cyclodextrin
Preparation and physicochemical characteristics of the complex of edaravone with hydroxypropyl-β-cyclodextrin
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DOI：
10.1016/j.carbpol.2010.09.007
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发表时间：
2011-01
影响因子：
11.2
通讯作者：
J. Zeng;Yong Ren;Chengliang Zhou;Shuqin Yu;Wen-Hua Chen
中科院分区：
文献类型：
--
作者：
J. Zeng;Yong Ren;Chengliang Zhou;Shuqin Yu;Wen-Hua Chen
目的：制备新型自由基清除剂依达拉曲与羟丙基-β-环糊精（HP-β-CD）包合物，以提高其表观溶解度、溶出率和稳定性。采用相溶解度法对依达拉奉的溶解度进行了表征，结果表明其溶解度为典型的al型，形成了1:1的化学计量包合物。采用冷冻干燥法制备了包合物，并用DTA、XRD和NMR对其进行了表征。这些结果表明依达拉奉可以与HP-β-CD形成包合物，并被深度包裹在HP-β-CD的空腔中。与依达拉奉相比，包合物的溶出速度和稳定性均有较大提高。这些结果有力地表明，利用HP-β-CD可以改善依达拉奉的理化特性。
The aim of this study was to prepare an inclusion complex of edaravone, a novel free radical scavenger drug, with hydroxypropyl-β-cyclodextrin (HP-β-CD) to improve its apparent solubility, dissolution rate and stability. The solubility of edaravone was evaluated by phase solubility method and the profile displayed a typical AL-type, indicating the formation of 1:1 stoichiometric inclusion complex. The inclusion complex was prepared by freeze-drying method and characterized by DTA, XRD and NMR. These results suggested that edaravone could form inclusion complex with HP-β-CD and was deeply included in the cavity of HP-β-CD. Additionally, the dissolution rate and stability of the inclusion complex were greatly improved compared with that of edaravone. These results strongly showed that the use of HP-β-CD could be a promising approach to improve the physicochemical characteristics of edaravone.