β-环糊精及其衍生物对灯盏花乙素增溶作用的研究

Study on β-cyclodextrin and Its Derivative as the Solubilizer of Scutellarin

采用相溶解度法研究了β-环糊精(β-CD),及其衍生物羟丙基-β-环糊精(HP-β-CD)、磺丁基醚-β-环糊精(SBE-β-CD)、单6-脱氧-氨基-β-环糊精(NH2-β-CD)和单6-脱氧-乙二胺-β-环糊精(en-β-CD)对灯盏花乙素的增溶作用,并测定了主-客体分子形成包合物的平衡常数。结果表明,当灯盏花乙素与上述5种环糊精形成可溶性包合物时,对应的相溶解度曲线均为AL型,说明其与环糊精的包合比均为1∶1;多种弱相互作用力协同作用于环糊精的包结配位过程,环糊精衍生物的取代基影响了主-客体配位能力。5种环糊精主体化合物对灯盏花乙素客体分子的增溶能力的大小为:en-β-CD>NH2-β-CD>HP-β-CD>SBE-β-CD>β-CD。

A phase solubility method was adopted to investigate solubilization of scutellarin with β-cyclodextrin （β--CD）, hydroxypropyl-β-cyclodextrin （HP-β-CD）, sulfobutylether-β-cyclodextrin （ SBE-β- CD）, mono （ 6-amino -6-deoxy）-β-cyelodextrin （NH2-β-CD） and mono （ 6-ethylene-diamino-6-deoxy）-β- cyclodextrin（en-β-CD）. The apparent stability constants of their inclusion complexes were determined. The results indicated that the phase solubility curves of scutellarin/CDs complexes were classified as AL style and the inclusion ratio of scutellarin versus cyclodextrins was 1 ： 1. Several weak interactions cooperatively contributed to the inclusion complexation ofβ-CD and its derivatives, and the substituent of theβ-cyclodextrin derivatives changed its original binding ability. The solubilization ability of eyclodex- trin hosts on scutellarin guest was in the order：en-β-CD〉NH2-β-CD〉HP-β-CD〉SBE-β-CD〉β-CD