环糊精和杯芳烃的包合特性及其在药物中的应用
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摘要
第一章:本章简要综述了环糊精(CDs)和杯芳烃包合作用的研究新进展,着重阐述了它们在药物载体方面的应用研究,并详述了环糊精(CDs)和杯芳烃在类胡萝卜素中的应用。
第二章:研究了HP-β-CD、SBE-β-CD与吡罗昔康的包合作用。用荧光光谱法测定了包合常数,比较了二种环糊精对吡罗昔康的包合能力,并详细探讨了环糊精浓度和体系介质酸度对包合过程的影响。结果表明:实验条件下,由于静电作用力与疏水作用力的协同作用,使得电荷型环糊精SBE-β-CD的包合能力大于中性环糊精HP-β-CD。
第三章:采用溶液法和研磨法分别制备了β-胡萝卜素与β-环糊精的包合物,紫外-可见吸收光谱研究表明,包合物水溶液的光谱特征不同于β-环糊精水溶液及β-胡萝卜素在N,N-二甲基甲酰胺-水混合溶剂中的光谱特征。包合物的水溶液以及光谱特征的变化证实了包合物的形成。包合物水溶液的最大吸收波长改变,可能是这种包合物的疏水部分(β-胡萝卜素)在水溶液中趋向自聚集,形成大的超分子聚集体所致。
第四章:改进了传统的包合物制备方法,制备了β-胡萝卜素与β-环糊精(β-CD)及其衍生物HP-β-CD和SBE-β-CD的固体包合物,并采用紫外光谱、红外光谱和核磁共振技术对包合物表征。详细考察了几种包合物的溶解度和稳定性,结果表明:β-胡萝卜素的包合物在光、热和氧条件下稳定性改善,溶解度得到提高,尤其是SBE-β-CD使β-胡萝卜素的溶解度提高显著。
第五章:主要采用荧光光谱法研究了杯[4]芳烃与β-胡萝卜素的包合作用,并且辅以核磁共振技术讨论了其作用机理。随着β-胡萝卜素浓度的增加,杯[4]芳烃的荧光强度逐渐降低。根据Stem-Volmer方程求得杯[4]芳烃与β-胡萝卜素形成包合物的结合常数。同时基于β-胡萝卜素对杯[4]芳
Chapter 1: The recent development of cyclodextrins and calixarenes has been reviewed, especially its development in drug delivery system. At the same time, the application of the cyclodextrins and calixarenes on carotenoids was expatiated.Chapter 2: The interaction of Piroxicam with sulfobutylether-β-cyclodextrin (SBE-β-CD) was compared with that of hydroxypropyl-β-cyclodextrin (HP-β-CD). The stability constants of the inclusion complexes were obtained by steady-state fluorescence technique. Experimental conditions including concentrations of the two cyclodextrins and media acidity were investigated for the inclusion formation in detail. The results suggested that the interaction of Piroxicam with charged CD (SBE-β-CD) is much stronger than that with neutral CD (HP-β-CD) at any pH studied, in terms of a synergetic effect of hydrophobic and electrostatic interactions.Chapter 3: Water-soluble inclusion compounds of β-cyclodextrin with β-carotene were prepared by two methods: (1) complexation in solution and (2) complexation by kneading. It was found that UV-Vis absorption spectra of the inclusion compounds in water were different from those of β-carotene in water-miscible organic solvents (DMF) and β-cyclodextrin in water, which confirmed the formation of the inclusion compounds. Specific interaction of β-carotene and β-cyclodextrin caused great changes in absorbance maximum of β-carotene. It is considered that in water the hydrophobic moiety (β-carotene) of such inclusion complexes should tend to self-associate forming large supramolecular aggregates.Chapter 4: Inclusion compounds of β-carotene with CDs including β-CD, HP-β-CD and SBE-β-CD had been prepared by using improved method and
characterized via UV-Vis absorption spectroscopy, IR spectra and 'H NMR technique. The solubilization and stabilization of inclusion compounds were investigated in detail. Experimental results on the stability cyclodextrins complexed P-carotene against light, heat and oxygen proved the benefits. The water solubility of the inclusion compounds was improved. SBE-P-CD was found to be the most potent solubilizing agent for P-carotene.Chapter 5: The formation of the inclusion complex of p-carotene with the calix[4]arene was studied by fluorescence spectroscopy. The related mechanism was discussed by means of "H NMR method. The fluorescence intensities of the calix[4]arene was gradually decreased with increasing of the concentration of P-carotene. The formation constant of complex was obtained by using Stern-Volmer equation. A new selective and sensitive method for the spectrofluorimetric determination of P-carotene was developed. This method is based on the quenching of fluorescence of calix[4]arene due to the formation of calix[4]arene-P-carotene complex.
第二章:研究了HP-β-CD、SBE-β-CD与吡罗昔康的包合作用。用荧光光谱法测定了包合常数,比较了二种环糊精对吡罗昔康的包合能力,并详细探讨了环糊精浓度和体系介质酸度对包合过程的影响。结果表明:实验条件下,由于静电作用力与疏水作用力的协同作用,使得电荷型环糊精SBE-β-CD的包合能力大于中性环糊精HP-β-CD。
第三章:采用溶液法和研磨法分别制备了β-胡萝卜素与β-环糊精的包合物,紫外-可见吸收光谱研究表明,包合物水溶液的光谱特征不同于β-环糊精水溶液及β-胡萝卜素在N,N-二甲基甲酰胺-水混合溶剂中的光谱特征。包合物的水溶液以及光谱特征的变化证实了包合物的形成。包合物水溶液的最大吸收波长改变,可能是这种包合物的疏水部分(β-胡萝卜素)在水溶液中趋向自聚集,形成大的超分子聚集体所致。
第四章:改进了传统的包合物制备方法,制备了β-胡萝卜素与β-环糊精(β-CD)及其衍生物HP-β-CD和SBE-β-CD的固体包合物,并采用紫外光谱、红外光谱和核磁共振技术对包合物表征。详细考察了几种包合物的溶解度和稳定性,结果表明:β-胡萝卜素的包合物在光、热和氧条件下稳定性改善,溶解度得到提高,尤其是SBE-β-CD使β-胡萝卜素的溶解度提高显著。
第五章:主要采用荧光光谱法研究了杯[4]芳烃与β-胡萝卜素的包合作用,并且辅以核磁共振技术讨论了其作用机理。随着β-胡萝卜素浓度的增加,杯[4]芳烃的荧光强度逐渐降低。根据Stem-Volmer方程求得杯[4]芳烃与β-胡萝卜素形成包合物的结合常数。同时基于β-胡萝卜素对杯[4]芳
Chapter 1: The recent development of cyclodextrins and calixarenes has been reviewed, especially its development in drug delivery system. At the same time, the application of the cyclodextrins and calixarenes on carotenoids was expatiated.Chapter 2: The interaction of Piroxicam with sulfobutylether-β-cyclodextrin (SBE-β-CD) was compared with that of hydroxypropyl-β-cyclodextrin (HP-β-CD). The stability constants of the inclusion complexes were obtained by steady-state fluorescence technique. Experimental conditions including concentrations of the two cyclodextrins and media acidity were investigated for the inclusion formation in detail. The results suggested that the interaction of Piroxicam with charged CD (SBE-β-CD) is much stronger than that with neutral CD (HP-β-CD) at any pH studied, in terms of a synergetic effect of hydrophobic and electrostatic interactions.Chapter 3: Water-soluble inclusion compounds of β-cyclodextrin with β-carotene were prepared by two methods: (1) complexation in solution and (2) complexation by kneading. It was found that UV-Vis absorption spectra of the inclusion compounds in water were different from those of β-carotene in water-miscible organic solvents (DMF) and β-cyclodextrin in water, which confirmed the formation of the inclusion compounds. Specific interaction of β-carotene and β-cyclodextrin caused great changes in absorbance maximum of β-carotene. It is considered that in water the hydrophobic moiety (β-carotene) of such inclusion complexes should tend to self-associate forming large supramolecular aggregates.Chapter 4: Inclusion compounds of β-carotene with CDs including β-CD, HP-β-CD and SBE-β-CD had been prepared by using improved method and
characterized via UV-Vis absorption spectroscopy, IR spectra and 'H NMR technique. The solubilization and stabilization of inclusion compounds were investigated in detail. Experimental results on the stability cyclodextrins complexed P-carotene against light, heat and oxygen proved the benefits. The water solubility of the inclusion compounds was improved. SBE-P-CD was found to be the most potent solubilizing agent for P-carotene.Chapter 5: The formation of the inclusion complex of p-carotene with the calix[4]arene was studied by fluorescence spectroscopy. The related mechanism was discussed by means of "H NMR method. The fluorescence intensities of the calix[4]arene was gradually decreased with increasing of the concentration of P-carotene. The formation constant of complex was obtained by using Stern-Volmer equation. A new selective and sensitive method for the spectrofluorimetric determination of P-carotene was developed. This method is based on the quenching of fluorescence of calix[4]arene due to the formation of calix[4]arene-P-carotene complex.
引文
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