黄芩素-烟酰胺共晶结晶过程的热力学研究

发布时间：2018-08-17 14:56

【摘要】：以黄芩素-烟酰胺共晶为模型药物,研究共晶形成的热力学。通过测定不同温度下黄芩素在不同浓度烟酰胺溶液中的溶解度,探讨黄芩素-烟酰胺共晶的络合形式,计算相关热力学参数,并绘制不同温度下的黄芩素-烟酰胺-乙酸乙酯三元相图。结果表明,黄芩素-烟酰胺共晶在乙酸乙酯中符合物质的量比1∶1溶液络合模型,共晶形成反应为热力学自发反应(ΔG°0),随着温度升高,Ksp逐渐增大,K11逐渐减小,反应自发程度减弱,三元相图中共晶区域减小,当温度达到T*=315 K后,ΔG°=0(ΔH°=-6.314×10-2k J/mol,ΔS°=-0.200 5 J/mol·K),自发反应不再进行,证明低温有利于共晶的形成。根据三元相图的非对称特点,设计了3种不以物质的量比1∶1为出发点制备共晶的方法,DSC结果表明,3种方法制备得到的黄芩素-烟酰胺共晶均为熔点单一的纯共晶。
[Abstract]:The thermodynamics of eutectic formation was studied using baicalin-nicotinamide eutectic as model drug. By measuring the solubility of baicalin in nicotinamide solution with different concentrations at different temperatures, the complexation of baicalein-nicotinamide eutectic was discussed, and the thermodynamic parameters were calculated. The ternary phase diagrams of baicalein-nicotinamide-ethyl acetate were drawn at different temperatures. The results showed that baicalein-nicotinamide eutectic was in accordance with the 1:1 solution complexation model in ethyl acetate. The eutectic reaction was thermodynamic spontaneous reaction (螖 G 掳0), and gradually decreased with the increase of temperature. The spontaneous reaction decreased and the eutectic region of ternary phase diagram decreased. When the temperature reached 315K, 螖 G 掳O (螖 H 掳-6.314 脳 10-2k J / mol, 螖 S 掳-0.200 5 J/mol K),) no longer occurred. It is shown that low temperature is favorable to eutectic formation. According to the asymmetric characteristics of ternary phase diagram, three kinds of eutectic methods were designed to prepare eutectic without the 1:1 mass ratio of substance. The DSC results showed that baicalein-nicotinamide eutectic was pure eutectic with a single melting point.
【作者单位】：中国药科大学药剂学教研室;中国药科大学中药制剂学教研室;
【基金】：江苏省自然科学基金资助项目(No.BK20141351) 江苏高校优势学科建设工程资助项目江苏省高校“青蓝工程”资助项目~~
【分类号】：R914

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