注射用环糊精包合物研究进展

Research progress of cyclodextrin inclusion complexes for injection

传统注射剂中对于难溶性药物采用的增溶手段多为添加有机助溶剂或表面活性剂,其刺激性易导致疼痛、炎症等多种不良反应。环糊精(cyclodextrin,CD)是一种具有空穴的环状低聚糖,部分天然环糊精及其衍生物具有良好的水溶性和生物相容性,可以通过包合作用增加难溶性药物的溶解度及稳定性,且降低对注射部位的刺激,是注射剂中增溶剂的更优选择。本文对环糊精在已上市注射剂产品中的应用及其发展前景进行综述,为环糊精在注射剂中更广泛的应用发展提供参考。

In order to improve the solubility of poorly water-soluble drugs,the solubilization methods used in conventional injections are mostly the addition of organic cosolvents or surfactants,whose irritation may lead to several adverse effects such as pain and inflammation.Cyclodextrin(CD)is a type of cyclic oligosaccharide with cavity.Partial natural cyclodextrins and their derivatives are water-soluble and biocompatible,making them a more preferable choice of solubilizer in injectable agents.They can increase the solubility and stability of drugs by forming inclusion complexes and the irritation to the injection site can be reduced.This review summarized the application and development prospects of marketed injections with cyclodextrins,and provide references on the wider application of cyclodextrin in injectable products.