石斛碱/环糊精衍生物包合行为研究

On the Inclusion Behavior of Dendrobine/Cyclodextrin-Derivatives Complexation

为了提高石斛碱的水溶性,用环糊精衍生物制备石斛碱包合物,并探讨其包合行为。采用显微分析法、差示扫描量热法(DSC)和薄层色谱法(TLC)对所制备的包合物进行表征,通过分子对接技术模拟包合行为,通过气相色谱法测定包合物的水溶性。各项表征分析均表明石斛碱可以被成功包合,分子模拟表明羟丙基-β-环糊精能完全包埋石斛碱,且其构象稳定,溶解度试验表明石斛碱被包合后在水中的溶解度提升了约277倍。石斛碱环糊精包合物能提高石斛碱的水溶性,拓展石斛碱在外用剂型中的应用。

To develop a cyclodextrin derivatives inclusion complex(CDIC)of dendrobine for increasing its solubility in aqueous solution,and characterize the inclusion behavior.The physicochemical properties of the inclusion complex were analyzed by microscopic method,differential scanning calorimetry and thin layer chromatography.The model structure of the inclusion complex was simulated using molecular docking technology.The water solubility of the inclusion complex was determined by gas chromatography.The CDIC of dendrobine was prepared successfully and its conformation was stable.Compared with dendrobine,the solubility of the inclusion complex in water increased by 277 times.CDIC of dendrobine can improve the solubility of dendrobine in water,which lays a foundation for expanding the application of dendrobine in external preparation.