Role of Mechanochemistry in Solid Form Selection and Identification of the Drug Praziquantel,Crystal Growth & Design

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Role of Mechanochemistry in Solid Form Selection and Identification of the Drug Praziquantel
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2021-09-27 , DOI: 10.1021/acs.cgd.1c00736
Basanta Saikia ₁ , Andreas Seidel-Morgenstern ₁ , Heike Lorenz ₁

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Identification of all possible polymorphs for a pharmaceutical compound is vital for the better formulation of medicine with desired properties. This study demonstrates the application of a mechanochemical approach to reveal new polymorphs of a drug and the potential of variable amounts of solvent in liquid-assisted grinding for solid form screening. Without solvent and by varying the amount of solvent added, we found two new polymorphs and an amorphous form, which were not reported previously. The finding portrays the advantage of the mechanochemical approach as a means of the polymorph screening strategy. While the focus here was on praziquantel, a similar approach is applicable to other pharmaceutical systems. This study also contributed to reinvestigate the solid-state behavior of the chiral praziquantel system, including the melt phase diagram and the role of experimental conditions on its phase behavior.

中文翻译：

机械化学在药物吡喹酮的固体形式选择和鉴定中的作用

鉴定药物化合物的所有可能的多晶型物对于更好地配制具有所需特性的药物至关重要。这项研究证明了机械化学方法的应用，以揭示药物的新多晶型物以及在液体辅助研磨中使用不同量的溶剂进行固体形式筛选的潜力。在没有溶剂的情况下，通过改变添加的溶剂量，我们发现了两种新的多晶型物和一种无定形形式，这是以前没有报道过的。该发现描绘了机械化学方法作为多晶型筛选策略手段的优势。虽然这里的重点是吡喹酮，但类似的方法也适用于其他制药系统。这项研究还有助于重新研究手性吡喹酮系统的固态行为，

更新日期：2021-10-06

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