The solid state of pharmaceuticals
The solid state of pharmaceuticals
复制标题
药物的固态
DOI：
10.1039/c9ce90044f
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发表时间：
2019
期刊：
影响因子：
3.1
通讯作者：
Edkins K
中科院分区：
文献类型：
--
作者：
Edkins K
几十年来，不同晶体形态的出现一直吸引着研究人员的兴趣，在任何领域，尤其是在制药材料领域。1-3由于对患者安全的影响以及药物配方中使用的所有材料的相关严格规定，对药物实体的物理形式的探索自然比对其他化学品所需的更详尽。多晶型、1水合物2和盐类3是明确寻找和探索的常见形式，实验方法通常得到计算方法4和结构信息学方法的支持。在多晶型筛选或结晶方法的设计中，溶剂型化合物经常出现为不需要的产品。虽然在游戏中也有一段时间了，但7，8最近才引起了人们对药物输送的更广泛兴趣，这引发了一些关于法规的问题。9在这些丰富的固体形式中，人们仍在寻求对最终推动固体形式在特定条件下成核、生长和出现的基本原理的理解。这一主题的问题结合了23篇涉及药物固体的各种重要问题的文章。从冒险进入非环境实验空间时发现著名药物化合物的新多晶型，到开发新的结晶方法或通过计算预测形式，该集合展示了该领域与制药行业仍作为标准执行的现象晶体形式筛选的演变程度，从而预示了制药固态的未来。抗病毒药物阿昔洛韦的卡罗尔·纳托夫斯基、雅罗斯拉夫·希米亚克及其同事(DOI：10.1039/c8ce01814f)令人印象深刻地展示了药物水晶景观的复杂性。作者研究了该体系中水合物的形成、脱水行为和溶剂诱导的相变，以揭示实验条件微小变化的复杂途径和重大影响。Aurora Cruz-Cabeza，Roger Davey等人(DOI：10.1039/c8ce01890a)提出了这一主题，他们审查了模型化合物4-氨基苯甲酸的多态体系，该体系已被广泛用于研究结晶行为、成核速度和溶剂影响。在他们的姊妹论文中，Martin Ward，Iain Oswald和他的同事(DOI：10.1039/c8ce01882k)收集了报道的PABA酸的预测数据，并实现了
The appearance of different crystal forms has intrigued researchers for decades, and in no field more so than in pharmaceutical materials. 1–3 Due to the implications to patients' safety and the connected tight regulations of all materials used in pharmaceutical formulation, the physical forms of drug entities are naturally more exhaustively explored than is necessary for other chemicals. Polymorphs, 1 hydrates2 and salts3 are usual forms explicitly sought and explored with experimental methods often supported by computational methods4 and structural informatics approaches. 5 Solvates often appear as unwanted products in polymorph screenings or during the design of crystallisation methods. 6 Cocrystals, although also in the game for a while, 7, 8 have only recently attracted a wider interest for drug delivery that has raised some questions with regards to regulations. 9 In this abundance of solid forms, much understanding is still sought in the fundamentals that ultimately drive nucleation, growth and the appearance of solid forms under a specific set of conditions.This themed issue combines 23 articles touching upon various important issues for the solid state of pharmaceuticals. From the discovery of new polymorphs of well-known drug compounds upon venturing into the nonambient experimental space to the development of novel crystallisation approaches or the prediction of forms computationally, this collection showcases how far the field has evolved from the phenomenological crystal form screening still performed as standard in pharmaceutical industry and thus indicates where the future of pharmaceutical solid-state might be. The complex nature of crystal landscapes of pharmaceuticals is impressively shown by Karol Nartowski, Yaroslav Khimyak and coworkers (DOI: 10.1039/c8ce01814f) for the antiviral drug acyclovir. The authors investigate the hydrate formation, dehydration behaviour and solvent induced phase transition within this system to reveal the intricate pathways and significant impact of minute changes to experimental conditions. This theme is picked up by Aurora Cruz-Cabeza, Roger Davey et al.(DOI: 10.1039/c8ce01890a), who review the polymorphic system of the model compound 4-aminobenzoic acid (pABA), which has been widely used to investigate crystallisation behaviour, nucleation rates and solvent impact. In their sister paper, Martin Ward, Iain Oswald and coworkers (DOI: 10. 1039/c8ce01882k) pick up the reported prediction data of pABA acid and realise a