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目的:考察β-环糊精(β-CD)及羟丙基-β-环糊精(HP-β-CD)对美沙拉嗪(MSZ)的增溶作用,为其包合物的制备提供理论依据。方法:采用相溶解度法分别考察不同浓度和不同温度下β-CD及HP-β-CD对MSZ的增溶作用,绘制出MSZ的相溶解度曲线,并计算包合常数K及包合动力学参数ΔG、ΔH及ΔS。结果:MSZ在两种环糊精中的相溶解度曲线均为AL型,随着温度的升高,两种环糊精对MSZ的包合常数K值均降低,当环糊精浓度和温度相同时,HP-β-CD的增溶效果明显优于β-CD;包合动力学参数ΔG、ΔH及ΔS均为负值。结论:两种环糊精对MSZ均有较好的增溶作用,HP-β-CD的增溶效果优于β-CD。
OBJECTIVE: To investigate the solubilization of mesalazine (MSZ) by β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) Theoretical basis. Methods: Solubilization of MSZ with β-CD and HP-β-CD at different concentrations and different temperatures was investigated by phase-solubility method. The phase solubility curve of MSZ was plotted and the inclusion constant K and inclusion kinetic parameters ΔG, ΔH and ΔS. Results: The phase solubility curves of MSZ in both cyclodextrins were AL type. As the temperature increased, the inclusion complex constants K of both cyclodextrins and MSZ decreased. When the cyclodextrin concentration and temperature phase At the same time, the solubilization effect of HP-β-CD was obviously better than that of β-CD. The inclusion kinetics parameters ΔG, ΔH and ΔS were negative. Conclusion: Both cyclodextrins have better solubilization effect on MSZ, and the solubilization effect of HP-β-CD is better than that of β-CD.