| 李兆楼,张波,贾少辉,刘莹,徐香玉.5-氟尿嘧啶分子与β-环糊精包合作用研究[J].济宁医学院学报,2017,40(6):398-401,406 |
| 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 |
| 投稿时间：2017-10-09 |
| DOI：10.3969/j.issn.1000-9760.2017.06.003 |
| 中文关键词: 5-氟尿嘧啶;β-环糊精;包合比;连续变量法 |
| 英文关键词: 5-Fluorouracil;β-Cyclodextrin;Inclusion ratio;Continuous variation Method |
| 基金项目: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）。 |
| 作者 | 单位 | | 李兆楼 | 济宁医学院基础医学院, 济宁 272067 | | 张波 | 济宁医学院基础医学院, 济宁 272067 | | 贾少辉 | 济宁医学院基础医学院, 济宁 272067 | | 刘莹 | 济宁医学院 日照 276826 | | 徐香玉 | 济宁医学院科研处, 济宁 272067 |
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| 中文摘要: |
| 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。 |
| 英文摘要: |
| 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. |
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