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药物共晶体全知道:十年快速发展的新科学与专利

The A to Z of pharmaceutical cocrystals: a decade of fast-moving new science and patents.

作者信息

Almarsson Örn, Peterson Matthew L, Zaworotko Michael

机构信息

Alkermes, Inc. 852 Winter Street, Waltham, MA 02451, USA.

出版信息

Pharm Pat Anal. 2012 Jul;1(3):313-27. doi: 10.4155/ppa.12.29.

Abstract

From aspirin to zoledronic acid, pharmaceutical cocrystals emerged in the past decade as a promising new weapon in the arsenal of drug development. Resurgence of interest in multicomponent crystal compositions has led to significant advances in the science of cocrystal design and discovery. These advances have built upon crystal engineering, which provides a deep understanding of supramolecular interactions between molecules that govern crystal packing and physicochemical properties of crystalline materials. Concomitantly, the patent landscape of pharmaceutical cocrystals developed rapidly in the last decade. This review presents a broad survey of patents issued in the area of pharmaceutical cocrystals. In addition, the review contains analyses of key patents in the area involving compositions and methodologies. Along the way, the main events of the past decade representing a renaissance of cocrystals of pharmaceutical materials are chronicled. Future directions in the area are discussed in light of key pending patent applications and recent publications of seminal interest.

摘要

从阿司匹林到唑来膦酸,药物共晶体在过去十年中成为药物研发武器库中一种有前景的新手段。对多组分晶体组合物兴趣的复苏推动了共晶体设计与发现科学的重大进展。这些进展建立在晶体工程学基础之上,晶体工程学能深入理解分子间的超分子相互作用,而这种相互作用决定了晶体堆积以及晶体材料的物理化学性质。与此同时,药物共晶体的专利格局在过去十年中迅速发展。本综述对药物共晶体领域发布的专利进行了广泛调查。此外,该综述还包含对该领域涉及组合物和方法的关键专利的分析。在此过程中,记录了过去十年中代表药物材料共晶体复兴的主要事件。根据关键的待决专利申请和近期具有重大影响力的出版物,讨论了该领域的未来发展方向。

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