Accessing Mefenamic Acid Form II through High-Pressure Recrystallisation.
Accessing Mefenamic Acid Form II through High-Pressure Recrystallisation.
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DOI：
10.3390/pharmaceutics9020016
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发表时间：
2017-05-16
期刊：
影响因子：
5.4
通讯作者：
Pulham CR
中科院分区：
文献类型：
--
作者：
Abbas N;Oswald IDH;Pulham CR
高压结晶已成功地用作制备非甾体抗炎药甲芬那酸（MA）的II型的替代技术。通过使用金刚石砧座单元，在0.3GPa下从乙醇溶液中生长形式II的单晶，表示为高压形式II。晶体结构的比较表明，MA分子的结构灵活性使II型分子的有效包装成为可能。对形式I的单晶进行的压缩研究导致晶胞体积降低14%至2.5GPa。在此压力下没有观察到相变。一个重构相变是必需的，以诱导结构中的构象变化，这是证实了在高压下的结晶的结果。
High-pressure crystallisation has been successfully used as an alternative technique to prepare Form II of a non-steroidal anti-inflammatory drug, mefenamic acid (MA). A single crystal of Form II, denoted as high-pressure Form II, was grown at 0.3 GPa from an ethanolic solution by using a diamond anvil cell. A comparison of the crystal structures shows that the efficient packing of molecules in Form II was enabled by the structural flexibility of MA molecules. Compression studies performed on a single crystal of Form I resulted in a 14% decrease of unit cell volume up to 2.5 GPa. No phase transition was observed up to this pressure. A reconstructive phase transition is required to induce conformational changes in the structure, which was confirmed by the results of crystallisation at high pressure.