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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 inclusion of cilostazol (CLTZ) and hydroxypropyl-β-cyclodextrin (HP-β-CD) in mixed solution and the change of thermodynamic parameters during the inclusion process. Methods: The equilibrium constants (Kf) of CLTZ and HP-β-CD in the mixed solution were determined by RP-HPLC. The thermodynamic parameters were calculated and analyzed. Results: CLTZ and HP-β-CD could form mol: mol (1: 1) inclusion complex. The inclusion process was spontaneous (ΔG <0) and exothermic (ΔH <0) (ΔS <0). CONCLUSION: CLTZ and HP-β-CD form a mol: mol (1: 1) soluble inclusion complex, which increases its solubility and lower temperature is favorable for the formation and stabilization of inclusion complex.