非诺贝特与2种β-环糊精水溶性衍生物在水溶液中包合作用研究  

Complexation of fenofibrate with 2 water-soluble β-CD derivatives in aqueous solution

作　　者：谷福根[1] 高源源[1,2] 吴春芝[1] 韩洪波[2] 

机构地区：[1]内蒙古医科大学附属医院,呼和浩特010050 [2]内蒙古医科大学药学院,呼和浩特010110

出　　处：《中南药学》2013年第4期258-261,共4页Central South Pharmacy

基　　金：内蒙古医科大学附属医院博士启动金项目(编号:NYFYBQ2010018)

摘　　要：目的研究羟丙基-β-环糊精(HP-β-CD)及磺丁基醚-β-环糊精(SBE-β-CD)在水溶液中对非诺贝特(fenofibrate,FNB)的包合作用。方法分别采用紫外吸收光谱法、相溶解度法研究HP-β-CD及SBE-β-CD在水溶液中对FNB的包合作用、增溶作用及包合过程中热力学参数的变化。结果 FNB与2种β-CD水溶性衍生物在水溶液中均存在明显的分子间相互作用。FNB的溶解度随着2种β-CD水溶性衍生物浓度的增加而呈线性增加,相溶解度图呈AL-型。包合过程中的热力学参数变化包括吉布斯自由能变化(ΔG)、焓变(ΔH)、熵变(ΔS)均为负值。结论 FNB与HP-β-CD及SBE-β-CD在水溶液中均可自发形成1:1克分子比可溶性包合物,从而增加其溶解度。同时,包合过程均为焓驱动过程,且为放热反应(ΔH<0),熵减过程(ΔS<0)。适当降低温度将有利于包合过程的进行。Objective To investigate the complexation of fenofibrate （FNB） with 2 water-soluble β-CD derivatives in- cluding hydroxypropyl-β-cyclodextrin （HP-β-CD） and sulfobutylether-β-Cyclodextrin （SBE-β-CD） in aqueous solution. Methods The intermolecular action between the host and guest molecules, the solubilizing effect of each CD derivative on FNB in aqueous solution and the changes of thermodynamic parameters in the complexation were studied by UV absorp- tion spectra, and phase solubility method. Results Significant interaction between the host and guest molecules in aqueous solution was confirmed. The solubilities of FNB in aqueous solutions increased linearly with the increasing concentration of each CD derivative, showing a typical AL-type phase solubility diagram. The values of 3 thermodynamic parameters, name- ly AG, AH and AS in the formation of each inclusion complex were all negative. Conclusion A 1 ： 1 molar ratio inclusion complex of FNB with each CD derivative forms spontaneously at all experimental temperatures and thus the solubility of FNB in the aqueous solution is obviously increased. All the complexation processes are enthalpically driven and are exother- mic. Therefore, appropriately low temperature can probably contribute to the progress of complexation.

关 键 词：非诺贝特 羟丙基-Β-环糊精 磺丁基醚-Β-环糊精 溶解度 热力学参数 

分 类 号：R944.9[医药卫生—药剂学]