摘要
目的:制备和鉴定酮洛芬(KPF)/羟丙基-β-环糊精(HP--βCD)包合物,研究KPF在不同温度、不同浓度HP--βCD水溶液中的溶解度、包合比及包合过程中的热力学参数变化。方法:采用溶液搅拌法制备KPF-HP--βCD包合物,摩尔连续递变法测定包合物的组成比例,相溶解度法测定KPF在25,37,45℃恒温条件下在不同浓度HP--βCD水溶液中的包合稳定常数及相关的热力学常数,差示扫描量热法(DSC)和红外光谱法(IR)对包合物进行鉴定。结果:包合物的摩尔包合比为1∶2,相溶解度曲线为AN型,表观稳定常数Kc随着温度的升高而下降,表征结果表明形成了包合物,KPF与HP--βCD在水溶液中的包合过程可自发进行,且为放热反应。结论:KPF与HP--βCD可以自发形成包合物,且低温有利于包合物的形成和稳定,形成的包合物能够显著地增加药物的溶解度和稳定性。
Aim： To prepare and identify the ketoprofen （KPF）-hydroxypropyl-β-cyclodextrin （HP-β-CD）inclusion complex, and to investigate the complexation of KPF with HP-β-CD in aqueous solutions, inclusion molar ratio of the host to the guest molecules and change of thermodynamic parameters during the complexation process. Methods： The inclusion compound was prepared by the stirring method. The measurements of the inclusion molar ratio of the host to guest molecules, apparent complexation constant, the thermodynamics parameters and the identication of the inclusion complex were carried out by the methods such as continuous variation method, UV absorption spectroscopy, phase solubility diagram, differential scanning calorimeter（DSC） and infrared spectra（IR） methods, respectively. Results： The continuous variation method suggested the formation of a aqueous soluble complex with 1：2 molar ratio. An AN-type phase solubility curve was obtained. The apparent complexation constant Kc decreased when the temperature increased. The change in the thermodynamic parameters suggested that the complexation could proceed spontaneously along with the release of heat and the decrease of entropy. Conclusion： The inclusion complex of KPF-HP-β-CD could be formed spontaneously, and lower temperature is a benefit to the formation and the stability of the inclusion complex. Hence, the solubility and stability of KPF in aqueous solution increase.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2006年第1期37-40,共4页
Journal of China Pharmaceutical University
关键词
酮洛芬
羟丙基-Β-环糊精
包合比
包合常数
热力学参数
ketoprofen
hydroxypropyl-β-cyclodextrin
complexation ratio
apparent complexation constant
thermodynamic parameter
作者简介
通讯作者 Tel：025-83587331 E-mail：lxmnjut@163．com
