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目的:考察磺丁基醚-β-环糊精(SBE-β-CD)及羟丙基-β-环糊精(HP-β-CD)对伏立康唑(VCZ)的增溶作用,为其包合物的研制奠定基础。方法:用相溶解度法考察不同浓度的SBE-β-CD及HP-β-CD在不同温度下对VCZ的增溶作用,计算包合常数K及包合动力学参数ΔG、ΔH及ΔS。结果:两种包合材料均能明显提高VCZ的水溶性,而在相同用量及相同温度时,SBE-β-CD的增溶作用较HP-β-CD明显;SBE-β-CD对VCZ的平衡相溶解图为A_N型,而HP-β-CD对VCZ的平衡相溶解图为AL型;温度升高,两种包合材料对VCZ的K值逐渐降低;包合动力学参数ΔG、ΔH及ΔS均为负值。结论:相较于HP-β-CD,SBE-β-CD对VCZ的增溶效果更好,包合为自发形成的放热过程,作用力主要为分子间范德华力。
OBJECTIVE: To investigate the solubilization of voriconazole (VCZ) by sulfobutyl ether-β-cyclodextrin (SBE-β-CD) and hydroxypropyl-β-cyclodextrin Preparation of the compound laid the foundation. Methods: The solubilization of VCZ by different concentrations of SBE-β-CD and HP-β-CD at different temperatures was investigated by phase-solubility method. Inclusion constants K and inclusion kinetics parameters ΔG, ΔH and ΔS were calculated. Results: The solubilization of SBE-β-CD was more obvious than that of HP-β-CD at the same dosage and the same temperature for both of the two inclusion compounds. The effect of SBE-β-CD on VCZ The equilibrium phase diagram shows A_N type, while the HP-β-CD phase equilibrium solution of VCZ shows the AL type. The K value of VCZ decreases with the increase of temperature. The inclusion kinetic parameters ΔG and ΔH And ΔS are negative. CONCLUSIONS: Compared with HP-β-CD, SBE-β-CD has a better effect on the solubilization of VCZ, which is a spontaneous exothermic process. The main interaction force is intermolecular van der Waals forces.