环糊精及其衍生物在药学应用中的安全性综述  

Review of safety assessment for cyclodextrin and its derivatives in drug administration

作　　者：卓敏[1] 严忠海[2] 张加慧 ZHUO Min YAN Zhong-Hai ZHANG Jia-Hui(Nanjing Hailing Pharmaceutical Co., Ltd, Yangtze River Phar- maceuticals Group, Nanjing 210049, China Departmem of Medicine, Columbia University, New York 10032, USA Xiuzheng Bio-pharmaceutieal （ Hangzhou ） Research Institute Co., Ltd, Hangzhou 310053, China)

机构地区：[1]扬子江药业集团南京海陵药业有限公司,江苏南京210049 [2]美国哥伦比亚大学医学院,美国纽约10032 [3]修正生物医药(杭州)研究院有限公司,浙江杭州310053

出　　处：《转化医学电子杂志》2017年第6期77-82,共6页E-Journal of Translational Medicine

摘　　要：环糊精(CD)是由6~8个D-吡喃葡萄糖单元通过α-1,4-糖苷键聚合而成的环状低聚糖化物.改性环糊精具有低毒、易修饰等优良性质,并可通过与药物分子形成包合物而提高药物的溶解性、稳定性、安全性和生物利用度等.改性环糊精不仅能够以其本身或修饰CD的形式充当载体,还可通过聚轮烷、阳离子聚合物或纳米粒等形式构建有效的药物载体.作为一种新型的药物赋形剂,改性环糊精广泛应用于口服、静脉注射和皮下给药等多种药物剂型,因此,其在人体内代谢及生物安全性等方面仍需要进一步研究.本文综述了改性环糊精类药物的结构特点、应用领域、吸收代谢以及毒理学性质的研究进展,并对市场上具有代表性的两种CD药物的安全性进行了初步归纳分析,提出了改性环糊精类物质研究的重点与发展方向.Cyclodextrins （CDs） are polysaccharide of six to eight glucose units that are covalently attached end to end via a-l, 4 linkages. The modified CDs present the characteristics of low toxicity and high flexibility of structure modification, and they also can enhance the aqueous solubility, chemical stability, safety and bio- availability of drugs in virtue of their peculiar ability to form CD/ drug inclusion complexes. Not only native and chemically modified CDs were employed as drug carriers, but also sorts of CD-based more sophisticated carrier systems such as polyrotaxanes, polyp- seudorotaxanes, polycations and nanoparticles emerged recently. In the pharmaceutical industry, modified CDs have mainly been used as complexing agents via oral, intravenous and hypodermic injection administration. However, their large-scale commercial u- tilization was prevented mainly due to the concerns regarding their safety. In this review, the structure of natural CDs, applications of modified CDs in drug delivery systems, characteristics features of dif- ferent types of inclusion complexation, safety, absorption and metab- olism, and comparative toxicology of modified CDs, as well as future prospects of research and development of modified CDs are summa- rized.

关 键 词：改性环糊精 水溶性 药物剂型 给药途径 生物安全性 药学应用 

分 类 号：R917[医药卫生—药物分析学]