5-氟尿嘧啶分子与β-环糊精包合作用研究  

Formation of inclusion complexes of β-cyclodextrin with 5-fluorouracil in aqueous solution

作　　者：李兆楼 张波 贾少辉 刘莹[2] 徐香玉 

机构地区：[1]济宁医学院基础医学院,济宁272067 [2]济宁医学院,日照276826 [3]济宁医学院科研处,济宁272067

出　　处：《济宁医学院学报》2017年第6期398-401,406,共5页Journal of Jining Medical University

基　　金：济宁医学院博士科研启动基金项目(JY2015BS25);济宁市科技计划(医药卫生)项目(2015-53)

摘　　要：目的验证5-氟尿嘧啶分子与β-环糊精内包含作用,并测定其包合比、表观解离常数,提出包合物的可能结构。方法用紫外分光光度法在极稀浓度下测定5-氟尿嘧啶的吸光度,考察不同β-环糊精浓度对5-氟尿嘧啶吸光度的影响;运用连续变量法及作图法求包合比和表观解离常数。结果 5-氟尿嘧啶的吸光度因β-环糊精浓度的增大而减小,确认β-环糊精对5-氟尿嘧啶分子发生包合作用;Job’s plot表明:β-环糊精的摩尔分数为0.5时,β-环糊精对5-氟尿嘧啶的吸光度变化影响最大,说明二者包合摩尔比为1∶1;包合物的表观解离常数为7.98×10^(-4)。结论抗癌药物5-氟尿嘧啶分子能够全部包合在β-环糊精空腔之中,这揭示了两者构成的药物制剂的内部分子间的微结构关系。Objective The purpose of this investigation is to explore the inclusion of β-cyclodextrin with 5-fluorouracil molecules. The apparent dissociation constant and the inclusion ratio of the β-cyclodextrin complexes are determined,and the structure of the inclusion complexes is speculated. Methods The absorbance of 5-fluorouracil was measured using UV spectrophotometry in extremely dilute solutions,and the absorption intensity change could suggest the generation of the β-cyclodextrin complexes. Utilizing the continuous variation method,the inclusion ratio and the apparent dissociation constant of the β-cyclodextrin complexes could be measured. Results The absorbance of 5-fluorouracil decreased with the increasing of concentration of β-cyclodextrin,suggesting the formation of β-cyclodextrin complexes.The maximal absorbance change of 5-fluorouracil was at the molar fraction of 0. 5 in the job's plot,indicating the 1∶ 1 inclusion ratio in inclusion complexes. The apparent dissociation constants of 7. 98 × 10^(-4) was also calculated. Conclusion One molecule of 5-fluorouracil can entirely be contained into the β-cyclodextrin molecule cavity. This results reveal the microstructure of 5-fluorouracil with β-cyclodextrin molecule in their pharmaceutical preparation.

关 键 词：5-氟尿嘧啶 Β-环糊精 包合比 连续变量法 

分 类 号：O656.9[理学—分析化学]