Preparation and physicochemical characteristics of the complex of edaravone with hydroxypropyl-β-cyclodextrin
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- 作者：Jian Zeng ; Yong Ren ; Chengliang Zhou ; Shuqin Yu ; Wen-Hua Chen
- 关键词：Edaravone ; Hydroxypropyl-β ; -cyclodextrin ; Inclusion complex ; Phase solubility ; Dissolubility ; Stability
- 刊名：Carbohydrate Polymers
- 出版年：2011
- 出版时间：30 January 2011
- 年：2011
- 卷：83
- 期：3
- 页码：1101-1105
- 全文大小：536 K
文摘
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.