国产药物辅料磺丁基倍他环糊精钠的注射安全性研究  

Study on the Injection Safety of Domestic Medicinal Excipient Sulfobutyl Beta Cyclodextrin Sodium

作　　者：申健 孙涛 SHEN Jian;SUN Tao(School of Chemistry and Chemical Engineering,Weifang University,Weifang 261061,China;School of Pharmacy,Fudan University,Shanghai 201203,China)

机构地区：[1]潍坊学院化学化工与环境工程学院,山东潍坊261061 [2]复旦大学药学院,上海201203

出　　处：《聊城大学学报（自然科学版）》2021年第5期66-71,共6页Journal of Liaocheng University:Natural Science Edition

基　　金：科技部“科技助力经济2020”重点专项项目(山东省立项列表序号16)资助。

摘　　要：磺丁基倍他环糊精钠(Sulfobutyl beta cyclodextrin sodium,SBCD),作为一种重要的、对多种药物可起包结作用的药用辅料,长期以来受控于国外“Cyclolab”等公司,是我国药物辅料界一款著名的被“卡脖子”的产品。对国产SBCD的注射安全性考察,是重要的破局式研究。分别对国产SBCD的取代度、溶血性、肾上皮细胞毒性,以及其超大剂量静脉注射安全性,进行了系统性研究。相比于原研市售产品,国产SBCD表现出了相当的溶血安全性和肾上皮细胞毒性;且在SD大鼠进行动物水平研究发现,国产SBCD拥有良好的超大剂量静脉注射安全性。研究为国产SBCD突破国外产品封锁和进一步的市场应用提供重要参考依据。Sulfobutyl beta cyclodextrin sodium(SBCD)can be employed as medicinal excipients for many pharmaceuticals via an inclusion model.However,for a long period,the SBCD production was limited by external incorporations such as Cyclolab,which has been always regarded as a famous“bottleneck”pharmaceutical product.The study on the injection safety of domestic SBCD is an important ice-breaking area.In this work,the substitution degree,hemolysis,renal toxicity,safety of supreme large injection doses of domestic SBCD were studied in detail.Compared with the original marketed product,domestic SBCD show comparable hemolysis and renal safety.Based on the in vivo experiments obtained from SD rats,the domestic SBCD possessed favorable biosafety upon supreme large injection doses.This work will provide important reference for breaching the blockade of foreign products and further marked application of the domestic SBCD.

关 键 词：国产辅料 磺丁基倍他环糊精钠 溶血性 肾毒性 超大剂量注射安全性 

分 类 号：R94[医药卫生—药剂学]