tcsc0731 SBE-β-CD

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

In Vitro: 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].

In Vivo: 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/dtmax_abs 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/dtmax_abs. 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/dtmax_abs (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].