羟丙基-β-环糊精包合甲氧苄啶的研究  

Study on Inclusion of Trimethoprim with Hydroxypropyl-β-cyclodextrin

作　　者：张伟[1] 符华林[1] 陈静[1] 姜彪[1] 舒刚[1] 付强[1] 

机构地区：[1]四川农业大学动物医学院,动物疫病与人类健康四川省重点实验室,四川雅安625014

出　　处：《中国畜牧兽医》2011年第11期66-69,共4页China Animal Husbandry & Veterinary Medicine

基　　金：教育部《长江学者和创新团队发展计划》创新团队项目(IRTO848)

摘　　要：为了研究甲氧苄啶(Trimethoprim,TMP)与羟丙基-β-环糊精(HP-β-CD)在水溶液中的包合作用、包合过程中的热力学参数变化及包合比,试验分别采用相溶解度法、等摩尔系列法、摩尔比率法测定了TMP与HP-β-CD的包合表观常数、包合过程的熵变、焓变、自由能变化及包合比。结果表明,在不同温度下,TMP与HP-β-CD在水溶液中均可形成1∶1摩尔比的包合物,相溶解度图呈AL型;TMP与HP-β-CD的包合过程可自发进行(△G<0),且为放热反应(△H<0),同时也是熵值增大的过程(△S>0);说明TMP与HP-β-CD在水溶液中均可自发形成1∶1摩尔比的包合物,从而增加其溶解度。选择适宜的包合温度将有利于包合过程的进行。To investigate the inclusion of Trimethoprim（TMP） with Hydroxypropyl-β-cyclodextrin（HP-β-CD） in aqueous soliutions,change of thermodynamic parameters during the inclusion process and inclusion molar ratio of the host and guest molecules.The measurements of apparent inclusion constant of TMP with HP-β-CD,the change of entropy,enthalpy and free energy of the reaction,inclusion molar ratio were carried out by the following methods separately were phase solubility method,equimolar series method and molar ratio method,respectively.That all the phase solubility diagrams showed a typical A_L-type in various temperature aqueous solutions,suggested the formation of a inclusion complex of 1∶1 molar ratio.The change in the thermodynamic parameters suggested that the inclusion could proceed spontaneously along with the release of heat and the increase of entropy.An 1∶1 molar ratio inclusion complex of TMP with HP-β-CD could be formed spontaneously and the solubility of TMP in aqueous solution increased.Appropriate temperature probably favor the progress of inclusion procedure.

关 键 词：甲氧苄啶 羟丙基-Β-环糊精 包合常数 热力学参数 包合比 

分 类 号：R94[医药卫生—药剂学]