西洛他唑与羟丙基-β-环糊精包合的热力学研究

Studies on Thermodynamics Between Cilostazol and HP-β-CD Forming Inclusion Complex

目的:研究西洛他唑(CLTZ)与羟丙基-β-环糊精(HP-β-CD)在混合溶液中的包合作用及其包合过程中热力学参数的变化。方法:运用RP-HPLC法测定CLTZ与HP-β-CD在混合溶液中包合的平衡常数(Kf),计算与分析其热力学的参数变化。结果:CLTZ与HP-β-CD可形成mol∶mol(1∶1)包合物,包合过程可自发进行(ΔG<0),且为放热反应(ΔH<0),也是熵减过程(ΔS<0)。结论:CLTZ与HP-β-CD可形成mol∶mol(1∶1)可溶性包合物,从而增加其溶解度,且较低的温度有利于包合物的形成和稳定。

Objective：To study the process of forming inclusion complex between cilostazol and HP-β-CD in mixed solution. Methods： The study of the process of forming inclusion complex between cilostazol and HP-β-CD was observed by RP-HPLC. Results： The results suggested the formation of a soluble complex is the ratio of 1：1（mol：mol）. The change in the thermodynamic parameters suggested that the complexation could proceed spontaneously（ΔG〈0）along with the releasing of heat（ΔH〈0） and the decrease of entropy（ΔS〈0）. Conclusion： Cilostazol formed a soluble complex of 1：1（mol：mol） ratio with HP-β-CD and the solubility of cilostazol in mixed solution increased. Appropriate temperature probably profits the progress of complexation procedure.