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环糊精在药物递送中的应用。

Cyclodextrins in drug delivery.

作者信息

Loftsson Thorsteinn, Jarho Pekka, Másson Már, Järvinen Tomi

机构信息

University of Iceland, Faculty of Pharmacy, Hagi, Reykjavik.

出版信息

Expert Opin Drug Deliv. 2005 Mar;2(2):335-51. doi: 10.1517/17425247.2.1.335.

Abstract

Cyclodextrins are a family of cyclic oligosaccharides with a hydrophilic outer surface and a lipophilic central cavity. Cyclodextrin molecules are relatively large with a number of hydrogen donors and acceptors and, thus, in general they do not permeate lipophilic membranes. In the pharmaceutical industry cyclodextrins have mainly been used as complexing agents to increase aqueous solubility of poorly soluble drugs, and to increase their bioavailability and stability. Studies in both humans and animals have shown that cyclodextrins can be used to improve drug delivery from almost any type of drug formulation. However, the addition of cyclodextrins to existing formulations without further optimisation will seldom result in acceptable outcome. Currently there are approximately 30 different pharmaceutical products worldwide containing drug/cyclodextrin complexes on the market.

摘要

环糊精是一类环状寡糖,具有亲水性的外表面和疏水性的中心腔。环糊精分子相对较大,有许多氢供体和受体,因此,一般来说它们不能透过亲脂性膜。在制药工业中,环糊精主要用作络合剂,以增加难溶性药物的水溶性,并提高其生物利用度和稳定性。对人类和动物的研究表明,环糊精可用于改善几乎任何类型药物制剂的药物递送。然而,在没有进一步优化的情况下,将环糊精添加到现有制剂中很少会产生可接受的结果。目前全球市场上约有30种不同的含有药物/环糊精复合物的药品。

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