Synthesis and Solid State Pharmaceutical Centre (SSPC), Bernal Institute, University of Limerick, Limerick, Ireland.
Synthesis and Solid State Pharmaceutical Centre (SSPC), Bernal Institute, University of Limerick, Limerick, Ireland.
Drug Discov Today. 2019 Mar;24(3):796-804. doi: 10.1016/j.drudis.2018.11.023. Epub 2018 Dec 3.
The field of pharmaceutical cocrystals has reached a tipping point, particularly because cocrystals can improve the physicochemical properties of drugs without compromising their therapeutic benefit. Accounts of cocrystal investigations in the literature started in earnest in 2003 and patent applications soon followed. The frequency of both has steadily accelerated, demonstrating an enhanced understanding of the design, characterisation, and manufacture of cocrystals and heightened interest from industry. Indeed, there were four new product approvals from 2014 to 2017 and more are in the pipeline. Here, we review all marketed drug products that are based upon pharmaceutical cocrystal drug substances, starting with the first recorded example, Beta-Chlor in 1963, with a particular emphasis on their discovery, rationale for use, and market impact.
药物共晶领域已经达到了一个临界点，特别是因为共晶可以改善药物的物理化学性质，而不会影响其治疗效果。文献中对共晶研究的报道始于 2003 年，随后不久就有了专利申请。这两者的频率都在稳步加速，表明人们对共晶的设计、特性和制造有了更深入的了解，并且行业的兴趣也在增加。事实上，2014 年至 2017 年期间有四种新药获得批准，还有更多的正在研发中。在这里，我们回顾了所有基于药物共晶药物物质的上市药物产品，从 1963 年第一个有记录的例子——Beta-Chlor 开始，特别强调了它们的发现、使用原理和市场影响。
