β-环糊精及其聚合物包合布洛芬的热力学研究  

Thermodynamic study on inclusions of ibuprofen by β-cyclodextrin and β-cyclodextrin polymer

作　　者：王齐放[1] 王中彦[1] 赵喆[1] 卢方正[1] 王家骏[2] 李三鸣[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016 [2]沈阳医学院公共卫生学院,沈阳110034

出　　处：《中国新药杂志》2007年第24期2057-2061,共5页Chinese Journal of New Drugs

摘　　要：目的:从热力学的观点出发,阐述以β-环糊精(β-Cyclodextrin,β-CD)及β-环糊精聚合物(β-Cyclodex-trin Polymer,β-CDP)作为包合载体时,包合反应的热力学函数变化。通过Kc,△H0,△S0及△G0,探讨β-CD及β-CDP与客体包合作用的驱动力。方法:以布洛芬(Ibuprofen,IBU)为模型药物,采用共沉淀法制备了药物与β-CD及β-CDP的包合物,用粉末X-射线衍射及差热扫描验证包合物的形成,通过紫外含量分析确定包合物中的药量。结果:在X-射线衍射及差热扫描图谱中药物的特征衍射峰及吸收峰均消失,说明药物与载体形成了包合物。相同条件下β-CDP的包封率高于β-CD。β-CD与β-CDP包合反应的△H0均为负值(放热反应),Kc均随温度的升高而降低。IBU/β-CDP的包合平衡常数大于IBU/β-CD。IBU/β-CDP包合反应的△H0,△S0的绝对值均高于IBU/β-CD。结论:通过包合反应热力学函数的分析比较得出,与β-CD相比以β-CDP作为药物载体,包封率高,包合平衡常数大,包合反应更易进行。Objective：To illustrate the thermodynamic parameters of the inclusion reaction,which use β-cyclodextrin （β-CD） and β-cyclodextrin polymer （β-CDP） as inclusion carriers. Through the in-clusion equilibrium constants （Kc） and the thermodynamic parameters of △ H^0 , △So and △ G^0 , the driving powers of drug between β-CD and β-CDP were predicted. Methods：Ibuprofen （IBU） was used as a model drug,and the inclusion complexes of drugs and β-CD/β-CDP were prepared by using co-precipita-tion method. The formation of the inclusion complexes were confirmed by powder X-ray diffraction and difference scanning calorimetry （DSC） , and the amounts of drug loaded were determined by the UV-spectrophotometer. Results：In the spectra of X-ray diffraction and DSC, the characteristic diffraction peaks and absorption peaks of IBU all disappeared,which demonstrated the formation of the inclusion complexes between the drugs and their carriers. The inclusion reactions of the drug with β-CD and β-CDP were both exothermic reactions,and the Kc was decreased while the temperature was increased. Other things being equal, the drug included in β-CDP were higher than that of β-CD, and the equilibrium constant of IBU/β-CDP was larger than that of IBU/β-CD. The scores of △H^0, △S^0 of IBU with β-CDP were higher than IBU with β-CD in the inclusion reaction. Conclusion： Compared with β-CD,when β-CDP was used as a drug carrier, equilibrium constant of inclusion reaction was larger, and it was easier to realize inclusion reaction.

关 键 词：Β-环糊精 Β-环糊精聚合物 布洛芬 包合物 热力学函数 

分 类 号：R943.4[医药卫生—药剂学] R971.1[医药卫生—药学]