SBE-β-CD是磺基丁基醚β-cyclodextrin衍生物，其用作赋形剂或配制剂以增加难溶性药物的溶解度。
CAS：182410-00-0
分子式：C50H84Na2O41S2
分子量：1451.29
纯度：98%
存储：Store at -20°C

Background:

SBE-β-CD is a sulfobutylether β-cyclodextrin derivative used as an excipient or a formulating agent to increase the solubility of poorly soluble drugs.

SBE-β-CD is a chemically modified β-CD that is a cyclic hydrophilic oligosaccharide which is negatively charged in aqueous media. β-CD functioned is a solubilizer only at low concentrations, whereas SBE7-β-CD exhibits strong solubilizing effects over a wide concentration range[1].

SBE-β-CD is a derivatized form of β-cyclodextrin that has been developed as a safe and effective solubilizing agent for drugs being administered by parenteral and other routes (including oral). SBE-β-CD is a cyclic carbohydrate comprised of seven glucose molecules; the resulting truncated cone-like structure being further derivatized with an average of seven sulfobutyl ether groups[2]. The calorimetric data for the Compound 1/SBE-β-CD complex indicates an extremely strong interaction, with an association constant of 2.3±(0.2)×106M-1 at 25°C and 1.6±(0.2)×106M-1 at 37°C[3]. SBE-β-CD alone evokes a mild cardio-depressant effect independent of cocaine treatment (p=0.0001 compared to baseline) but attenuates further cocaine-induced decreases in RPP, dP/dtmax, and dP/dtmaxabs at high cocaine concentrations. No significant effect is seen on line pressure SBE-β-CD alleviates the most pronounced cardiac depression for RPP, dP/dtmax, and dP/dtmaxabs. This differential effect of SBE-β-CD at low and high concentrations produces an interaction effect in the two-way ANOVA for RPP (p<0.0001), dP/dtmax (p=0.0001), and dP/dtmaxabs (p=0.0015), and prevents any overall treatment effect. Infusing SBE-β-CD also attenuates the cardiac depression associated with cocaethylene toxicity for RPP and dP/dtmax. No differences are observed between ethanol-treated controls and cocaethylene plus SBE-β-CD groups[4].

参考文献
[1]. Fukuda M, et al.Influence of sulfobutyl ether beta-cyclodextrin (Captisol) on the dissolution properties of a poorly soluble drug from extrudates prepared by hot-melt extrusion.Int J Pharm. 2008 Feb 28;350(1-2):188-196
[2]. Lockwood SF, et al. Improved aqueous solubility of crystalline astaxanthin (3,3’-dihydroxy-beta, beta-carotene-4,4’-dione) by Captisol (sulfobutyl ether beta-cyclodextrin). J Pharm Sci. 2003 Apr;92(4):922-926.
[3]. Charman SA, et al. Alteration of the intravenous pharmacokinetics of a synthetic ozonide antimalarial in the presence of a modified cyclodextrin. J Pharm Sci. 2006 Feb;95(2):256-67
[4]. Fettiplace MR, et al. Cardiac depression induced by cocaine or cocaethylene is alleviated by lipid emulsion more effectively than by sulfobutylether-β-cyclodextrin. Acad Emerg Med. 2015 May;22(5):508-17