| 周静,李兆楼,陈昌琳,刘莹,李琳琳.β-环糊精对甲氨蝶呤的包合作用[J].济宁医学院学报,2016,39(5):357-361 |
| β-环糊精对甲氨蝶呤的包合作用 |
| Inclusion complexes of β-cyclodextrin with methotrexate |
| 投稿时间：2016-07-15 |
| DOI：10.3969/j.issn.1000-9760.2016.05.015 |
| 中文关键词: 甲氨蝶呤;β-环糊精;连续变量法;包合摩尔比 |
| 英文关键词: Methotrexate;β-Cyclodextrin;Continuous variation method;Inclusion molar ratio |
| 基金项目:济宁医学院大学生科研项目（2015-06）；济宁市科技计划（医药卫生）项目（2015-53） |
| 作者 | 单位 | E-mail | | 周静 | 济宁医学院, 济宁 272067 | | | 李兆楼 | 济宁医学院基础医学院, 济宁 272067 | jnzhaolou@mail.jnmc.edu.cn | | 陈昌琳 | 济宁医学院, 济宁 272067 | | | 刘莹 | 济宁医学院, 济宁 272067 | | | 李琳琳 | 济宁医学院, 济宁 272067 | |
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| 中文摘要: |
| 目的 研究β-环糊精大环分子对甲氨蝶呤分子的包合作用，测定其化学组成包合比、表观解离常数，并提出包合物可能的结构模型。方法 利用紫外分光光度法测定甲氨蝶呤稀溶液吸光度，根据吸收强度变化来确定包合物形成。利用连续变量法（Job's plot）测定其摩尔包合比、表观解离常数等。结果 研究表明，甲氨蝶呤的吸光度随着β-环糊精浓度的增大而增大，二者能够形成包合物；Job's plot也表明，甲氨蝶呤最大的吸光度变化值对应的β-环糊精摩尔分数为0.5，故甲氨蝶呤能够与β-环糊精形成组成为1∶1的包合物，包合物的表观解离常数为1.30×10-5。结论 抗癌药物甲氨蝶呤可与大环分子β-环糊精发生包合作用，甲氨蝶呤分子的一部分可被包合在环糊精分子空腔中。对于进一步研究以β-环糊精为辅料的甲氨蝶呤药物制剂的内部微结构和性质、性能具有意义。 |
| 英文摘要: |
| Objective The goal of present study is to confirm the formation of the inclusion complexes of ββ-cyclodextrin with methotrexate molecules.The inclusion molar ratio and the apparent dissociation constant of the β-cyclodextrin complexes are explored,and the possible structure of the inclusion complexes is proposed.Methods The UV absorbances of methotrexate were measured by spectrophotometry in dilute concentrations,and the formation of the β-cyclodextrin complexes was determined according to the absorption intensity change.The inclusion molar ratio and the apparent dissociation constant of the β-cyclodextrin complexes were obtained using the continuous variation method (Job's plot).Results The absorbance of methotrexate increased with the addition of β-cyclodextrin.This result suggests formation of the inclusion complexes.The maximum absorbance changes existed at the point of β-cyclodextrinmolar fraction of 0.5 on job's plot,indicating that β-cyclodextrin complexes was formed in inclusion molar ratio of 1:1.The apparent dissociation constants of the conclusion complexes was 1.30×10-5.Conclusion A methotrexate molecule can partly be contained into the cavity of β-cyclodextrin macrocylic molecule in the inclusion complexes.These results showed the significance for further studying the microstructure and properties of pharmaceutical preparations constructed by β-cyclodextrin and methotrexate molecules. |
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