大环糊精包埋制霉菌素的研究

大环糊精（LR-CD）具有优于普通环糊精（α-环糊精、β-环糊精、γ-环糊精）的高水溶性、低粘度、不回生等特性,但目前关于大环糊精的应用研究非常少。本文以共轭四烯类大环内酯抗生素制霉菌素为客体,探讨了大环糊精对制霉菌素的包埋能力,结果表明,LR-CD的相溶解曲线为AL型,计算得到LR-CD包埋制霉菌素的包合常数为1.577L/mmol,远远大于β-环糊精和γ-环糊精对制霉菌素的包埋常数（0.375L/mmol和0.539L/mmol）;预测饱和环糊精溶液对制霉菌素的增溶倍数为2958.87倍;红外光谱鉴定表明制霉菌素的酯键及二烯部分进入到环糊精的空腔,而共轭四烯部分及羧基、氨基部分在环糊精腔体表面。 

Study on the inclusion behavior between LR-CD and nystatin

Large ring cyclodextrin (LR-CD) had properties of high solubility, low viscosity, anti-retrogradation and so on, which was superior to the common cyclodextrins (α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin) , however, there was very little reports are about the application of LR-CD.In this text, nystatin was as guest molecules, the inclusion properties of large ring-cyclodextrin on nystatin was investigated.Results showed that the phase solubility curve for LR-CD was AL type, and the embedding constant was 1.577L/mmol for LR-CD, it was much larger than that of α-cyclodextrin, β-cyclodextrin andγ-cyclodextrin (0.375L/mmol and 0.539L/mmol) , the solubility enhanced by saturated large ring-cyclodextrins was predicted as 2958.87 folds, the identification by infrared spectrum (IR) indicated that the ester linkage and diene were included in the cavity of cyclodextrin, while conjugate arachidonic, carboxyl and amino group were left outside of cyclodextrins.