摘要
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 β-cyclodextrin （I3-CD） and hydroxypropyl β-cyclodextrin （HP-β-CD） for mesalazine （MSZ） to provide theoretical basis for the preparation of inclusion complexes. Methods： The solubilization of β-CD and HP-β-CD at different concentrations for MSZ was studied at various temperatures, and the inclusion constant （K） and inclusion parameters AG, AH and AS were calculated. Results： The phase solubility curves of MSZ with the two cyclodextrins were both AL styles. With the increase of the temperature, K was decreased. The solubilization of HP-β-CD was better than that of β-CD at the same concentration and temperature. The parameters AG, AH and AS were all negative. Conclusion： β-CD and HP-β-CD both show promising solubilization for MSZ and HP-β-CD is better.
出处
《中国药师》
CAS
2016年第1期65-67,共3页
China Pharmacist
