Loftsson Thorsteinn, Másson Már, Brewster Marcus E
Faculty of Pharmacy, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Iceland.
J Pharm Sci. 2004 May;93(5):1091-9. doi: 10.1002/jps.20047.
Cyclodextrins are useful functional excipients, which are being used in an ever-increasing way to camouflage undesirable pharmaceutical characteristics, especially poor aqueous solubility. It has generally been assumed that the mechanism whereby cyclodextrins exert their effects, especially their augmentation of solubility, is via the formation of noncovalent, dynamic inclusion complexes. This is a model, which regards drug-cyclodextrin interactions as a discrete phenomenon and ignores the possible interaction of these complexes with one another. It is becoming increasingly apparent that such assumptions may not be universally applicable or all encompassing. Specifically, there is a growing body of evidence that supports the important contribution of non-inclusion-based aspects for drug solubilization by cyclodextrins including surfactant-like effects and molecular aggregation. This short review attempts to assess the available literature for areas in which such non-inclusion mechanisms are apparent and tries to interpret these in the context of a broader working theory as to how cyclodextrins exert their beneficial effects.
环糊精是有用的功能性辅料，其使用方式不断增加，用于掩盖不良的药物特性，尤其是水溶性差的问题。一般认为，环糊精发挥作用的机制，尤其是其溶解度增强的机制，是通过形成非共价的动态包合物。这是一个将药物 - 环糊精相互作用视为离散现象的模型，忽略了这些复合物之间可能的相互作用。越来越明显的是，这样的假设可能并非普遍适用或涵盖所有情况。具体而言，越来越多的证据支持环糊精增溶药物的基于非包合作用的重要方面，包括表面活性剂样效应和分子聚集。这篇简短的综述试图评估在哪些领域这种非包合机制明显的现有文献，并尝试在关于环糊精如何发挥其有益作用的更广泛工作理论背景下对这些文献进行解读。
