申请人:UNIVERSITY OF FLORIDA
公开号:EP0327766A2
公开(公告)日:1989-08-16
Inclusion complexes of hydroxypropyl, hydroxyethyl, glucosyl, maltosyl or maltotriosyl derivatives of β- or γ-cyclodextrin with the reduced, biooxidizable, blood-brain barrier penetrating, lipoidal forms of dihydropyridine = pyridinium salt redox systems for brain-targeted drug delivery provide a means for stabilizing the redox systems, particularly against oxidation. The redox inclusion complexes also provide a means for decreasing initial drug concentrations in the lungs after administration of the systems, leading to decreased toxicity. In selected instances, complexation results in substantially improved water solubility of the redox systems as well.
β-或γ-环糊精的羟丙基、羟乙基、葡糖基、麦芽糖基或麦芽三糖基衍生物与还原型、可生物氧化、可穿透血脑屏障、类脂形式的二氢吡啶=吡啶鎓盐氧化还原体系的包合物为脑靶向给药提供了一种稳定氧化还原体系,特别是防止氧化的方法。氧化还原包合物还能降低给药后肺部的初始药物浓度,从而降低毒性。在某些情况下,络合物还能大大提高氧化还原体系的水溶性。