ACS Comb Sci. 2012 Mar 12;14(3):155-9. doi: 10.1021/co200175e. Epub 2012 Feb 24.
Reported here is a relatively simple technique for polymorph screening of pharmaceutical compounds that are thermally stable. Polymer libraries have previously been used as surfaces to influence, or direct, the crystalline form adopted by an active pharmaceutical ingredient on crystallization from solution. In this current work, we demonstrate the polymorph-directing effect of homopolymer surfaces in the absence of solvent by recrystallization from the supercooled melt. When the nonsteroidal anti-inflammatory drug indomethacin is melted, cooled, and subsequently reheated above its glass transition temperature on an untreated surface, it has a proclivity to crystallize as its δ polymorph. On certain polymer surfaces, however, it preferentially crystallizes as the α polymorph, as a direct result of polymer templating. The method is well-suited to implementation in multiwell plate formats requiring only small amounts of material and enabling multiple experiments to be carried out in parallel with samples readily characterized using X-ray powder diffraction.
本文报道了一种相对简单的热稳定药物化合物多晶筛选技术。聚合物库以前曾被用作表面，以影响或指导活性药物成分在溶液中结晶时采用的晶型。在当前这项工作中，我们通过过冷熔体重结晶证明了均聚物表面在没有溶剂的情况下对多晶型的导向作用。当非甾体抗炎药吲哚美辛在未处理表面上熔融、冷却并随后在玻璃化转变温度以上重新加热时，它倾向于结晶为其 δ 多晶型。然而，在某些聚合物表面上，它优先结晶为 α 多晶型，这是聚合物模板作用的直接结果。该方法非常适合于多孔板格式的实施，只需要少量的材料，并能够同时进行多个实验，使用 X 射线粉末衍射对样品进行快速分析。
