Department of Pharmaceutical Chemistry, The University of Kansas, Lawrence, KS 66047, USA.
Department of Pharmaceutical Chemistry, The University of Kansas, Lawrence, KS 66047, USA.
Int J Pharm. 2020 Jun 15;583:119396. doi: 10.1016/j.ijpharm.2020.119396. Epub 2020 May 4.
This review presents the early history, the motivation, the research and some of the backstories behind the discovery and development of sulfobutylether-β-cyclodextrin as a novel parenterally safe solubilizer and stabilizer. A specific sulfobutylether-β-cyclodextrin with an average degree of 6.5 sulfobutyl-groups variably substituted on the 2-, 3- and 6-hydroxyls of the seven glucopyranose (dextrose) units of β-cyclodextrin, is known by its commercial name, Captisol®. Today it is in 13 FDA approved injectables and numerous clinical candidates. It is also an example of a novel product discovered and initially preclinically developed at an academic institution.
本文综述了磺丁基醚-β-环糊精作为新型安全可注射增溶剂和稳定剂的发现和发展背后的早期历史、动机、研究和一些背景故事。其中一个特定的磺丁基醚-β-环糊精,其平均有 6.5 个磺丁基基团取代在β-环糊精的七个葡萄糖吡喃糖(葡萄糖)单元的 2-、3-和 6-羟基上,其商品名为 Captisol®。如今,它已在 13 种获得 FDA 批准的注射剂和众多临床候选药物中得到应用。它也是在学术机构发现并初步进行临床前开发的新型产品的一个范例。