近年来药物盐的发展:2015 年至 2019 年 FDA 的批准情况。
Recent developments in pharmaceutical salts: FDA approvals from 2015 to 2019.
机构信息
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai 400056, India.
出版信息
Drug Discov Today. 2021 Feb;26(2):384-398. doi: 10.1016/j.drudis.2020.11.016. Epub 2020 Nov 19.
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.
约一半的由美国食品药品监督管理局(FDA)批准的新分子实体是药物盐。自 1939 年批准首个盐形式以来,药物盐一直呈持续增长趋势。本综述旨在提供 2015 年至 2019 年期间 FDA 批准的药物盐的最新信息。五年药物批准数据库包含 61 种药物盐,具有多种抗衡离子;然而,盐酸盐是最丰富的。这里展示了每个类别中所有药物盐的化学结构,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的技术优势。