高通量结晶：药物固体的多晶型物、盐、共晶体和溶剂化物
High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids.
作者信息
Morissette Sherry L, Almarsson Orn, Peterson Matthew L, Remenar Julius F, Read Michael J, Lemmo Anthony V, Ellis Steve, Cima Michael J, Gardner Colin R
机构信息
TransForm Pharmaceuticals, Inc., 29 Hartwell Avenue, Lexington, MA 02421, USA.
出版信息
Adv Drug Deliv Rev. 2004 Feb 23;56(3):275-300. doi: 10.1016/j.addr.2003.10.020.
The concepts of high-throughput (HT) screening and combinatorial synthesis have been integrated into the pharmaceutical discovery process, but are not yet commonplace in the pharmaceutical development arena. Emerging strategies to speed pharmaceutical development and capture solid form diversity of pharmaceutical substances have resulted in the emergence of HT crystallization technologies. The primary type of diversity often refers to polymorphs, which are different crystal forms of the same chemical composition. However, diverse salt forms, co-crystals, hydrates and solvates are also amenable to study in HT crystallization systems. The impact of form diversity encompasses issues of stability and bioavailability, as well as development considerations such as process definition, formulation design, patent protection and regulatory control. This review highlights the opportunities and challenges of HT crystallization technologies as they apply to pharmaceutical research and development.
高通量（HT）筛选和组合合成的概念已被整合到药物发现过程中，但在药物开发领域尚未普及。加速药物开发并获取药物实体固态形式多样性的新兴策略导致了高通量结晶技术的出现。多样性的主要类型通常指多晶型物，即相同化学成分的不同晶体形式。然而，不同的盐形式、共晶体、水合物和溶剂化物也适用于高通量结晶系统的研究。形式多样性的影响包括稳定性和生物利用度问题，以及诸如工艺定义、制剂设计、专利保护和监管控制等开发方面的考虑。本综述重点介绍了高通量结晶技术在药物研发应用中的机遇和挑战。
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