Loftsson T, Brewster M E
Department of Pharmacy, University of Iceland, Reykjavik, Iceland.
J Pharm Sci. 1996 Oct;85(10):1017-25. doi: 10.1021/js950534b.
Cyclodextrins are cyclic oligosaccharides which have recently been recognized as useful pharmaceutical excipients. The molecular structure of these glucose derivatives, which approximates a truncated cone or torus, generates a hydrophilic exterior surface and a nonpolar cavity interior. As such, cyclodextrins can interact with appropriately sized molecules to result in the formation of inclusion complexes. These noncovalent complexes offer a variety of physicochemical advantages over the unmanipulated drugs including the possibility for increased water solubility and solution stability. Further, chemical modification to the parent cyclodextrin can result in an increase in the extent of drug complexation and interaction. In this short review, the effects of substitution on various cyclodextrin properties and the forces involved in the drug-cyclodextrin complex formation are discussed. Some general observations are made predicting drug solubilization by cyclodextrins. In addition, methods which are useful in the optimization of complexation efficacy are reviewed. Finally, the stabilizing/destabilizing effects of cyclodextrins on chemically labile drugs are evaluated.
环糊精是一类环状寡糖，最近被认为是有用的药用辅料。这些葡萄糖衍生物的分子结构近似截顶圆锥体或圆环面，具有亲水性的外表面和非极性的内腔。因此，环糊精能够与大小合适的分子相互作用，形成包合物。与未处理的药物相比，这些非共价复合物具有多种物理化学优势，包括增加水溶性和溶液稳定性的可能性。此外，对母体环糊精进行化学修饰可导致药物络合和相互作用程度的增加。在这篇简短的综述中，讨论了取代对各种环糊精性质的影响以及药物 - 环糊精复合物形成过程中涉及的作用力。做出了一些关于环糊精增溶药物的一般性观察。此外，还综述了有助于优化络合效果的方法。最后，评估了环糊精对化学不稳定药物的稳定/去稳定作用。
