一种合成药物罗格列酮与天然药物小檗碱的新共晶：制备、晶体结构和溶解。
A New Co-Crystal of Synthetic Drug Rosiglitazone with Natural Medicine Berberine: Preparation, Crystal Structures, and Dissolution.
机构信息
Department of Medicinal Chemistry, School of Pharmacy, Chongqing Medical University, Chongqing 400016, China.
College of Environment and Resources, Chongqing Technology and Business University, Chongqing 400016, China.
出版信息
Molecules. 2020 Sep 18;25(18):4288. doi: 10.3390/molecules25184288.
A co-crystal of rosiglitazone (Rsg) with berberine (Bbr), Rsg-Bbr, was prepared by the solvent evaporation method and characterized. The results showed that the electrostatic attraction existed between the nitrogen anion of rosiglitazone and the quaternary ammonium cation of berberine, and C-H···O hydrogen bonds were formed between Rsg and Bbr. In the crystal structure, rosiglitazone molecules stack into a supramolecular layer through π-π interactions while π-π interactions between berberine cations also result in a similar layer. The co-crystal presented a low moisture adsorption curve in the range of 0-95% relative humidity values at 25 °C. The improved dissolution rate of rosiglitazone in pH = 6.8 buffer solution could be achieved after forming co-crystal.
罗格列酮（Rsg）与小檗碱（Bbr）共晶 Rsg-Bbr 通过溶剂蒸发法制备并进行了表征。结果表明，罗格列酮的氮阴离子与小檗碱的季铵阳离子之间存在静电吸引力，并且在 Rsg 和 Bbr 之间形成了 C-H···O 氢键。在晶体结构中，罗格列酮分子通过 π-π 相互作用堆积成超分子层，而小檗碱阳离子之间的 π-π 相互作用也导致形成类似的层。共晶在 25°C 时在 0-95%相对湿度范围内呈现出低的水分吸附曲线。形成共晶后，可以提高罗格列酮在 pH = 6.8 缓冲溶液中的溶解速率。
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