| CAS NO: | 182410-00-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| 25g | 电议 |
| 50g | 电议 |
| Molecular Weight (MW) | 1134.98 |
|---|---|
| Formula | C42H70-nO35.nNa.n(C4H8O3S) |
| CAS No. | 182410-00-0 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 6 mg/mL |
| Water: >100 mg/mL | |
| Ethanol: <1 mg/mL | |
| SMILES | [R]O[C@@H]1[C@H](O[R])[C@H](O[C@@H]2[C@H](O[R])C(O[R])[C@H](O3)[C@@H](CO[R])O2)[C@@H](CO[R])O[C@@H]1O[C@H]4[C@H](O[R])[C@@H](O[R])[C@@H](O[C@H]5[C@H](O[R])[C@@H](O[R])[C@@H](O[C@@H]6C(O[R])[C@H](O[R])[C@H](O[C@@H]7[C@@H](O[R])[C@H](O[R])[C@H](O[C@@H]8[C@@H](O[R])[C@H](O[R])[C@H]3O[C@H]8CO[R])O[C@H]7CO[R])O[C@H]6CO[R])O [C@@H]5CO[R])O[C@@H]4CO[R].[R= H 21-m or C4H8SO3-Na+ m , m=6.0-7.1] |
| Synonyms | Sodium sulfobutylether β-cyclodextrin; SBE-β CD; SBE-β-CD; SBE β-CD; SBE β CD; SBE-beta-CD; Sulfobutylether beta-cyclodextrin; Captisol; beta-cyclodextrin sulfobutyl ether sodium salts Chemical Name: beta-cyclodextrin sulfobutyl ether sodium salts |
| In Vitro | In vitro activity: SBE-β-CD, also named as Sulfobutylether beta-cyclodextrin or Captisol, is a highly water-soluble anionic derivative of cyclodextrin that is widely used as an excipient or a formulating agent to increase the solubility of poorly soluble drugs.. The sodium sulfonate salt of it is separated from the lipophilic cavity by a butyl ether spacer moiety, namely the sulfobutylether (SBE). SBE-β-CD can form non-covalent inclusion complexes with drug molecules, by so doing, it can improve drug stability, solubility and safety, reduce toxicity, cover up bad smell, and control drug release rate. As an excipient, SBE-β-CD has been used in various formulation including injection, oral, nasal and eye medication. Modification of the structure by charged functional groups can improve the binding affinity of cyclodextrins for oppositely charged guests, therefore it has a specific affinity for drugs containing nitrogen atoms. Kinase Assay: 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. |
|---|---|
| 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. 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. 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. |
| Animal model | Rats |
| Formulation & Dosage | A 300 g rat is administered with 1 mL of a 0.1 M SBE-β-CD solution containing 5.64 mg of Compound 1, and assuming an extracellular volume of 90 mL, less than 0.1% of the complex would rapidly dissociate due to the initial effects of dilution. This calculation, combined with the changing blood to plasma ratio in the presence of SBE-β-CD, provides a reasonable explanation for the observed differences in the blood and plasma profiles of Compound 1 after intravenous administration in either the cyclodextrin or cyclodextrin-free formulations. After IV administration of the cyclodextrin formulation, Compound 1 would initially be prevented from distributing into erythrocytes thereby resulting in a whole blood to plasma ratio of less than one. Subsequently, clearance of SBE-β-CD from the circulation would lead to changes in the complexation equilibrium such that the unbound fraction of Compound 1 would increase, thereby reestablishing normal blood to plasma partitioning (i.e. in favour of whole blood) and clearance. |
| References | J Pharm Sci. 2006 Feb;95(2):256-67. |
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