| β-环糊精-表柔比星包合物的合成和性质研究 |
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| 引用本文： | 董明南,张友玉,姚守拙.β-环糊精-表柔比星包合物的合成和性质研究[J].湖南师范大学自然科学学报,2012,35(2):58-62. |
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| 作者姓名： | 董明南 张友玉 姚守拙 |
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| 作者单位： | 湖南师范大学化学化工学院,化学生物学及中药分析教育部重点实验室,中国 长沙 410081 |
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| 基金项目： | 国家自然科学基金资助项目 |
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| 摘 要： | 首次采用荧光光谱法研究了水溶液体系中β-环糊精(β-CD)与表柔比星(EPI)的超分子包合行为.考察并讨论了温度,时间和β-CD浓度对包合反应的影响.研究结果表明,EPI与β-CD形成1∶2的超分子包合物后,包合物荧光强度相对于EPI增大近一倍.在36℃,pH=7.4时,包合常数K=8.14×103(L/mol)2.最后通过改变pH值考察了表柔比星从β-CD空腔中的释放速率,当pH分别为5和7.4时,5h内EPI的累积释放率分别达到了36.1％和26.1％,该研究结果对于表柔比星的缓释临床应用提供了很好的参考和依据.
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| 关 键 词： | 环糊精 表柔比星 包合 荧光光谱法 |
Studies on Synthesis and Properties of Supramolecular Inclusion of β-Cyclodextrin and Epirubicin |
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| DONG Ming-nan
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ZHANG You-yu
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YAO Shou-zhuo.Studies on Synthesis and Properties of Supramolecular Inclusion of β-Cyclodextrin and Epirubicin[J].Journal of Natural Science of Hunan Normal University,2012,35(2):58-62. |
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| Authors: | DONG Ming-nan ZHANG You-yu YAO Shou-zhuo |
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| Institution: | (Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research,Ministry of Education; College of Chemistry and Chemical Engineering,Hunan Normal University,Changsha 410081,China) |
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| Abstract: | The supermolecular inclusion of epirubicin(EPI) with β-cyclodextrin(β-CD) was firstly studied in aqueous solution by fluorescence spectroscopy.The effects of reaction temperature,reaction time and concentration of β-CD on the inclusion efficiency of EPI were investigated.The results show that fluorescence intensity of EPI was enhanced about two times after formation of 1∶ 2 inclusion complexes with β-CD.At 36 ℃ and pH 7.4,the inclusion constant was 8.14×103(L/mol)2.The releasing of EPI from β-CD cavity is controlled by varying pH.When the pH was 5 and 7.4,after 5 h EPI cumulative releasing rate reaches 36.1% and 26.1%,respectively.The result provides a good reference for its clinical application. |
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| Keywords: | cyclodextrin epirubicin inclusion fluorescence spectrometry |
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