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Pharmaceutical cocrystals: from serendipity to design to application
Drug Discovery Today ( IF 6.5 ) Pub Date : 2018-12-03 , DOI: 10.1016/j.drudis.2018.11.023
Oisin N. Kavanagh , Denise M. Croker , Gavin M. Walker , Michael J. Zaworotko

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.



中文翻译:

药用共晶体:从偶然性到设计到应用

药物共晶体的领域已经达到了临界点,特别是因为共晶体可以改善药物的理化性质而不会损害其治疗效果。文献中有关共晶体研究的记载始于2003年,随后紧接着提出了专利申请。两者的频率都在稳步提高,这表明人们对共晶的设计,特征和制造有了更深入的了解,并且引起了业界的极大关注。实际上,从2014年到2017年,已有四项新产品批准,还有更多正在审批中。在这里,我们审查是基于制药共晶药物物质的所有上市药品的产品,从第一个记录例如β-氯碱® 1963年,特别强调了它们的发现,使用原理和市场影响力。

更新日期:2018-12-03
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