Leicester School of Pharmacy, De Montfort University, The Gateway, LE1 9BH Leicester, United Kingdom.
Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW Cambridge, United Kingdom.
Adv Drug Deliv Rev. 2017 Aug 1;117:147-161. doi: 10.1016/j.addr.2017.05.001. Epub 2017 May 3.
Within the pharmaceutical industry, and elsewhere, the screening for new solid forms is a mandatory exercise for both existing and new chemical entities. This contribution focuses on mechanochemistry as a versatile approach for discovering new and alternative solid forms. Whilst a series of recently published extensive reviews exist which focus on mechanistic aspects and potential areas of development, in this review we focus on particular practical aspects of mechanochemistry in order to allow full optimisation of the approach in searches for new solid forms including polymorphs, salts and cocrystals as well as their solvated/hydrated analogues. As a consequence of the apparent experimental simplicity of the method (compared to more traditional protocols e.g. solvent-based methods), the high efficiency and range of conditions available in a mechanochemical screen, mechanochemistry should not be considered simply as an alternative method when other screening methods are not successful, but rather as a key strategy in any fully effective solid form screen providing reduced effort and time as well as the potential of requiring reduced amounts of material.
在制药行业及其他领域，对于现有和新的化学实体，筛选新的固体形式是一项强制性的工作。本研究集中于机械化学，将其作为发现新的和替代的固体形式的通用方法。虽然已经发表了一系列广泛的综述，重点关注机械化学的机制方面和潜在的发展领域，但在本次综述中，我们重点关注机械化学的特定实际方面，以便在寻找新的固体形式（包括多晶型物、盐和共晶以及它们的溶剂化物/水合物类似物）时，对该方法进行全面优化。由于该方法（与更传统的方法相比，例如基于溶剂的方法）在实验上具有明显的简单性，在机械化学筛选中可获得高效率和广泛的条件范围，因此，机械化学不应仅被视为其他筛选方法不成功时的替代方法，而应被视为任何全面有效的固体形式筛选的关键策略，从而减少工作量和时间，并有可能减少所需的材料量。
