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Recent developments in pharmaceutical salts: FDA approvals from 2015 to 2019
Drug Discovery Today ( IF 7.4 ) Pub Date : 2020-11-19 , DOI: 10.1016/j.drudis.2020.11.016
Sonali S Bharate 1
Affiliation  

Around half of the new molecular entities approved by the US Food and Drug Administration (FDA) are pharmaceutical salts. The pharmaceutical salts have been on a continuous growth trajectory since the approval of the first salt form in 1939. This review aims to provide updates on pharmaceutical salts approved by the FDA between 2015 and 2019. The five-year drug-approval database contains 61 pharmaceutical salts, featuring a diverse range of counterions; however, hydrochlorides are the most abundant. The chemical structures of all pharmaceutical salts in each class are presented here, along with their therapeutic indications and date of approval. The reason behind the selection of a particular counterion and the technical superiority achieved by the salt form over the free active pharmaceutical ingredient base are also discussed.



中文翻译:

药用盐的最新进展:2015 年至 2019 年 FDA 批准情况

美国食品和药物管理局 (FDA) 批准的新分子实体中约有一半是药用盐。自 1939 年批准第一种盐形式以来,药用盐一直处于持续增长的轨道上。本综述旨在提供 FDA 2015 年至 2019 年批准的药用盐的最新信息。五年药物批准数据库包含 61 个药用盐。盐,具有多种抗衡离子;然而,盐酸盐是最丰富的。此处列出了每一类所有药用盐的化学结构,以及它们的治疗适应症和批准日期。还讨论了选择特定抗衡离子的原因以及盐形式相对于游离活性药物成分基质所获得的技术优势。

更新日期:2020-11-19
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