A survey of solid form landscape: Trends in occurrence and distribution of various solid forms and challenges in solid form selection.

IF 3.7 3区 医学 Q2 CHEMISTRY, MEDICINAL
Z Jane Li, Yue Lu, Ruiping Wang, Xiaomei Dong, Pengyuan Chen, Jie Duan, Meiting Shi, Liyu Wang, Yuan Liu
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引用次数: 0

Abstract

This survey provides a comprehensive analysis of solid form screens for 476 new chemical entities (NCEs) conducted at Pharmaron from 2016 to 2023. The findings from this survey reveal notable trends in polymorphism, salt formation, crystallization behavior and molecular weight (MW) distribution of the NCEs evaluated. Most solid form screens were conducted to select the preferred solid form for Investigational New Drug (IND) enabling projects, others were for candidate selection or late-stage development. Comparison to published historical data was made to show changes in occurrence of counterions/co-formers for salts/co-crystals, polymorphs, and the distribution of MWs over time. Increased complexity in the solid-form landscape and selection of the development form are discussed, including challenges in crystallization and selection of lead forms. The distribution of types of crystal forms and the observation of emerging and disappearing polymorphs are presented. These results highlight the evolving challenges and considerations in solid form screening and form selection and offer insights for future pharmaceutical development and crystallization strategies.

固体形式现状调查:各种固体形态的出现和分布趋势以及固体形态选择方面的挑战。
本调查全面分析了Pharmaron从2016年到2023年对476种新化学实体(NCE)进行的固型筛选。调查结果揭示了所评估的新化学实体在多态性、成盐性、结晶行为和分子量(MW)分布方面的显著趋势。大多数固态筛选是为新药研究 (IND) 启动项目选择首选固态,其他则用于候选药物选择或后期开发。通过与已公布的历史数据进行比较,可以看出随着时间的推移,盐类/共晶体、多晶型的反离子/共形物发生的变化以及截留分子量的分布。讨论了固态形式的复杂性增加和开发形式的选择,包括结晶和铅形式选择方面的挑战。介绍了晶体形态类型的分布以及对新出现和消失的多晶型的观察。这些结果突显了在固态形式筛选和形式选择方面不断变化的挑战和考虑因素,并为未来的药物开发和结晶策略提供了启示。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
7.30
自引率
13.20%
发文量
367
审稿时长
33 days
期刊介绍: The Journal of Pharmaceutical Sciences will publish original research papers, original research notes, invited topical reviews (including Minireviews), and editorial commentary and news. The area of focus shall be concepts in basic pharmaceutical science and such topics as chemical processing of pharmaceuticals, including crystallization, lyophilization, chemical stability of drugs, pharmacokinetics, biopharmaceutics, pharmacodynamics, pro-drug developments, metabolic disposition of bioactive agents, dosage form design, protein-peptide chemistry and biotechnology specifically as these relate to pharmaceutical technology, and targeted drug delivery.
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