The Dispersed States of Medicinal Molecules in Ground Mixtures with α- or β-Cyclodextrin
The Dispersed States of Medicinal Molecules in Ground Mixtures with α- or β-Cyclodextrin
复制标题
α-或β-环糊精研磨混合物中药用分子的分散状态
DOI：
10.1248/cpb.32.685
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发表时间：
1984
期刊：
影响因子：
--
通讯作者：
K. Akimoto
中科院分区：
文献类型：
--
作者：
Y. Nakai;Keiji. Yamamoto;K. Terada;K. Akimoto
阿司匹林、苯甲酸和对羟基苯甲酸均以结晶形式形成分子间氢键二聚体结构，用α-或β-环糊精研磨。除阿司匹林-α-环糊精体系外，包合物均采用共沉淀法制备。通过对羰基拉伸区红外光谱的分析，研究了药物分子的分散状态。说明药物在α-环糊精体系中的分散状态与在β-环糊精体系中的分散状态不同。假设在β-环糊精体系中，阿司匹林分子被包含在环糊精腔中，而在α-环糊精体系中，阿司匹林分子以单分子形式分散在环糊精的氢键网络结构中。用核磁共振方法研究了药物与水溶液中α-或β-环糊精的相互作用。用热重法测定了α-或β-环糊精体系对羟基苯甲酸的升华。研究了环糊精在酸性条件下对阿司匹林水解的影响。
Aspirin, benzoic acid and p-hydroxybenzoic acid, all of which form intermolecularly hydrogen-bonded dimer structures in the crystalline form, were ground with α- or β-cyclodextrin. Inclusion compounds were also prepared by the coprecipitation method, except in the case of the aspirin-α-cyclodextrin system. The dispersed state of the medicinal molecules were investigated by analysis of the infrared spectra in the carbonyl stretching regions. It was suggested that the dispersed state of medicinals in the α-cyclodextrin system was different from that in the β-cyclodextrin system. It was assumed that, by grinding, aspirin molecules were included in the cyclodextrin cavity in the β-cyclodextrin system, but were dispersed monomolecularly in the hydrogen-bonded network structure of cyclodextrin in the α-cyclodextrin system. Interaction between medicinals and α- or β-cyclodextrin in aqueous solution was investigated by means of nuclear magnetic resonance studies. The sublimation of p-hydroxybenzoic acid from the ground mixtures or inclusion compounds with α- or β-cyclodextrin systems was determined by thermogravimetry. The effects of cyclodextrin on the hydrolysis of aspirin under acidic conditions were investigated as well.