依达拉奉与环糊精包合物的制备及验证

Preparation and Characterization of the Edaravone and Cyclodextrin Inclusion Complex

关键词:  依达拉奉  环糊精  包合常数  溶解度  稳定性

Key words:  edaravone  cyclodextrin  equilibrium constant  solubility  stability

摘要:

目的 利用包合技术改进依达拉奉理化性质，为研制新型制剂提供依据。方法 光谱法测定依达拉奉-环糊精包合常数，研磨法和溶液法制备包合物；热分析(DTA和TGA)及谱学分析(1H-NMR和XRD)验证包合物；光度法测定依达拉奉含量并考察其稳定性。结果 依达拉奉与环糊精可形成稳定包合物(包合常数Ka为146~4 285 L·mol ^-1)，包合技术能增加依达拉奉溶解度，提高稳定性。结论 环糊精能显著改善依达拉奉理化性质，依达拉奉包合技术具有应用价值。

Abstract:

OBJECTIVE To improve the physicochemical property of edaravone by inclusion technology. METHODS The inclusion constant of edaravone and cyclodextrin was determined by spectroscopic methodology and the inclusion complexes were prepared by levigation and solution method, characterized by the thermal analysis (DTA and TGA) methods, nuclear magnetic resonance method (1H-NMR) and X-ray diffractometry (XRD) techniques. The solubility and stability of edaravone were also measured. RESULTS Edaravone formed an optimal inclusion complex with cyclodextrin with the equilibrium constant of 146-4 285 L·mol ^-1. The inclusion complex increased the solubility and improved the stability of edaravone. CONCLUSION The solubility and stability of edaravone were significantly improved with cyclodextrin and this technique may have medical values for the development of edaravone preparation.