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Enhancing the Pharmaceutical Properties of Pirfenidone by Mechanochemical Cocrystallization

机译：通过机械化学聚碳化增强Pirfenidone的药物特性

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摘要

Pirfenidone is an important drug molecule used in the treatment of idiopathic lung fibrosis. Although approved by the USFDA in 2014, pirfenidone's aqueous solubility is too high and must be mitigated by additives. In this work, the cocrystallization of pirfenidone is explored as an alternative approach to reducing its solubility. Herein, an anhydrous form of pirfenidone is reported, alongside its first two reported cocrystals. The new crystalline solids are thoroughly characterized by single crystal X-ray diffraction (SCXRD), powder X-ray diffraction analysis (PXRD), Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA). Equilibrium solubility and intrinsic dissolution rates (IDR) are studied for the cocrystals and compared to that of the parent drug. Both cocrystal forms exhibit drastically lower aqueous solubility (by up to 90%) and dissolution rates, rationalized based on both lattice energy calculations and consideration of intermolecular interactions in the solid state. Furthermore, we compare the physicochemical properties of solution-based material with that of material produced mechanochemically. Importantly, no differences are observed between the two production methods. This work demonstrates the strength of crystal engineering strategies to beneficially modify important pharmaceutical properties and highlights the potential of mechanochemistry to facilitate this in an environmentally benign way.
机译：Pirefenidone是用于治疗特发性肺纤维化的重要药物分子。虽然2014年由USFDA批准，Pirfenidone的水溶性太高，必须通过添加剂缓解。在这项工作中，探讨了Pirfenidone的Cocryalization作为降低其溶解度的替代方法。在此，据报道了一种无水形式的吡啶酮，以及其前两个报告的碳酸烯酮。通过单晶X射线衍射（SCXRD），粉末X射线衍射分析（PXRD），傅里叶变换红外（FTIR）光谱，差示扫描量热法（DSC）和热重分析（TGA）进行全面地表征新的结晶固体。对甲基烯的研究并与母体药物相比，研究了平衡溶解度和固有溶解速率（IDR）。双晶体形式均显示出急剧下含水溶解度（高达90％）和溶解速率，基于晶格能量计算合理化，并考虑固态中的分子间相互作用。此外，我们将基于溶液的材料的物理化学性能与机械化学制备的材料进行比较。重要的是，两种生产方法之间没有观察到差异。这项工作展示了晶体工程策略的强度，以便有利地改变重要的药物特性，并强调机械化学的潜力以环境良好的方式促进这种情况。

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