Solubilization Comparison between Sulfonated Butyl Ether-β-cyclodextrin and Hydroxypropyl-β-cyclodextrin for Voriconazole by Phase Solubility
- VernacularTitle:磺丁基醚-β-环糊精及羟丙基-β-环糊精对伏立康唑的增溶作用比较
- Author:
Zhihui YAN
;
Jiji ZHANG
;
Yongjun HU
;
Ling SONG
- Keywords:
Phase solubility;
Sulfonated butyl ether-β-cyclodextrin;
Hydroxypropyl β-cyclodextrin;
Voriconazole;
Solubilization
- From:
China Pharmacist
2017;20(7):1296-1298
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To study the solubilization of sulfonated butyl ether-β-cyclodextrin (SBE-β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) for voriconazole (VCZ) to lay basis for the preparation of inclusion compounds of VCZ.Methods: The phase-solubility method was used, and the solubilization of SBE-β-CD and HP-β-CD at different concentrations for VCZ was studied at various temperatures and the inclusion constant (K) and such inclusion parameters as ΔG, ΔH and ΔS were calculated.Results: Both SBE-β-CD and HP-β-CD could improve the solubility of VCZ in water, while the solubilization of SBE-β-CD was more significant than that of HP-β-CD at the same concentration under the same temperature.The equilibrium phase-solubility diagram of SBE-β-CD vs VCZ was AN type, and that of HP-β-CD vs VCZ was AL type.With the increase of temperature, K of both β-CD decreased.ΔG, ΔH and ΔS were all negative for the inclusion process.Conclusion: Compared with that of HP-β-CD, the solubilization of SBE-β-CD for VCZ is better.The inclusion is spontaneously formed with exothermic process, and the main acting force is Van der Waals'' force.
