磺丁基醚-β-环糊精在药物制剂中的应用及安全性研究进展

Application and Safety Study of Sulfobutyl Ether-β-cyclodextrin in Pharmaceutical Preparations

磺丁基醚-β-环糊精(SBECD)是由1,4-丁烷磺内酯在碱性条件下与β-环糊精的2-、3-、6-位碳上的羟基发生取代反应而得到的阴离子型高水溶性环糊精衍生物。与β-环糊精相比,SBECD 的水溶性增强,并具有更高的体内安全性,广泛应用于注射剂、口服制剂、鼻腔给药制剂、滴眼剂等制剂工艺中。本文综述了SBECD 的特点及在制剂工艺中的应用,并重点阐述了其在健康人及肾功能损伤患者体内安全性的研究进展。

Sulfobutyl ether-β-cyclodextrin (SBECD) is an anionic high water-soluble cyclodextrin derivative, which is obtained by substituting by 1,4-butane sulfonate with 2-, 3-, 6-bits of carbon on glucose-β-cyclodextrin glucose unit under basic conditions. Compared with β-cyclodextrin, SBECD has enhanced water solubility and higher in vivo safety, and it is widely used in pharmaceutical preparations such as injections, oral preparations, nasal administration preparations, and eye drops. This paper reviews the characteristics of SBECD and the application in the formulation process, and focuses on the progress of SBECD in safety study in healthy volunteers and patients with renal impairment.