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药用盐:从基础化学到美国食品药品监督管理局批准的全面洞察(2019 - 2023年)

Pharmaceutical Salts: Comprehensive Insights From Fundamental Chemistry to FDA Approvals (2019-2023).

作者信息

Dhaval Mori, Dudhat Kiran, Gadoya Aastha, Shah Sunny, Pethani Trupesh, Jambukiya Nilesh, Patel Ajay, Kalsariya Chintan, Ansari Jainabparvin, Borkhataria Chetan

机构信息

B.K. Mody Government Pharmacy College, Polytechnic Campus, Near Ajidam, Rajkot, Gujarat-360005, India.

R.K. School of Pharmacy, R.K. University, Rajkot, Gujarat, India.

出版信息

AAPS PharmSciTech. 2025 Jan 16;26(1):36. doi: 10.1208/s12249-024-03020-4.


DOI:10.1208/s12249-024-03020-4
PMID:39821716
Abstract

Pharmaceutical salts are a cornerstone in drug development, offering a robust, economical, and industry-friendly option for improving the crucial physicochemical properties of drugs, particularly solubility and dissolution. This review article explores all critical aspects of salt formation, including its importance, the basic chemistry involved, the principles governing counterion selection, the range of counterions used, and the methods for preparing salts along with their advantages and limitations. Additionally, it explores analytical techniques for confirming salt formation and the different approaches various countries adopt in considering new salts as intellectual property. Furthermore, the review sheds light on US FDA-approved salts from 2019 to 2023, providing a unique perspective by analyzing trends in counterion selection observed in FDA-approved salts during this period. Despite the extensive literature on pharmaceutical salts, a comprehensive review addressing all these critical aspects in a single article with a focus on current trends and particularly on US FDA-approved salts from 2019 to 2023 is lacking. This review bridges this gap by thoroughly exploring all mentioned facets of pharmaceutical salts and providing an up-to-date overview.

摘要

药用盐是药物研发的基石,为改善药物的关键物理化学性质,尤其是溶解度和溶出度,提供了一种强大、经济且对行业友好的选择。这篇综述文章探讨了盐形成的所有关键方面,包括其重要性、涉及的基础化学、反离子选择的指导原则、使用的反离子范围、制备盐的方法及其优缺点。此外,还探讨了确认盐形成的分析技术以及各国在将新盐视为知识产权方面采取的不同方法。此外,该综述还揭示了2019年至2023年美国食品药品监督管理局(FDA)批准的盐,通过分析在此期间FDA批准的盐中反离子选择的趋势提供了独特的视角。尽管有大量关于药用盐的文献,但缺乏一篇在一篇文章中全面涵盖所有这些关键方面、关注当前趋势且特别关注2019年至2023年美国FDA批准的盐的综述。本综述通过全面探讨药用盐的所有上述方面并提供最新概述来弥补这一差距。

相似文献

[1]
Pharmaceutical Salts: Comprehensive Insights From Fundamental Chemistry to FDA Approvals (2019-2023).

AAPS PharmSciTech. 2025-1-16

[2]
Recent developments in pharmaceutical salts: FDA approvals from 2015 to 2019.

Drug Discov Today. 2021-2

[3]
Carboxylic Acid Counterions in FDA-Approved Pharmaceutical Salts.

Pharm Res. 2021-8

[4]
Trends in active pharmaceutical ingredient salt selection based on analysis of the Orange Book database.

J Med Chem. 2007-12-27

[5]
Impact of the counterion on the solubility and physicochemical properties of salts of carboxylic acid drugs.

Drug Dev Ind Pharm. 2012-1

[6]
Modulation of biopharmaceutical properties of acidic drugs using cationic counterions: A critical analysis of FDA-approved pharmaceutical salts.

Int J Pharm. 2021-9-25

[7]
Measurement and Accurate Interpretation of the Solubility of Pharmaceutical Salts.

J Pharm Sci. 2017-5

[8]
An investigation into the influence of counterion on the properties of some amorphous organic salts.

Mol Pharm. 2008

[9]
An evaluation of salt screening methodologies.

J Pharm Pharmacol. 2015-6

[10]
Recent advancements in mechanical reduction methods: particulate systems.

Drug Dev Ind Pharm. 2013-8-30

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[1]
Development and Characterization of a New Oral Antileishmanial Bis(pyridine-2-Carboxamidine) Drug Through Innovative Dissolution Testing in Biorelevant Media Combined with Pharmacokinetic Studies.

Pharmaceutics. 2025-6-26

本文引用的文献

[1]
Identification of DprE1 inhibitors for tuberculosis through integrated in-silico approaches.

Sci Rep. 2024-5-17

[2]
Continuous Synthesis of Cinnarizine Salt with Malic Acid by Applying Green Chemistry Using Water-Assisted Twin Screw Extrusion.

Mol Pharm. 2023-10-2

[3]
Epik: p and Protonation State Prediction through Machine Learning.

J Chem Theory Comput. 2023-4-25

[4]
Virtual Screening, Structural Analysis, and Formation Thermodynamics of Carbamazepine Cocrystals.

Pharmaceutics. 2023-3-3

[5]
Challenges and Strategies for Solubility Measurements and Dissolution Method Development for Amorphous Solid Dispersion Formulations.

AAPS J. 2022-12-13

[6]
Crystal Engineering of Pharmaceutical Cocrystals in the Discovery and Development of Improved Drugs.

Chem Rev. 2022-7-13

[7]
In acid-aminopyrimidine continuum: experimental and computational studies of furan tetracarboxylate-2-aminopyrimidinium salt.

RSC Adv. 2021-6-17

[8]
The role of solvation in proton transfer reactions: implications for predicting salt/co-crystal formation using the Δp rule.

Faraday Discuss. 2022-7-14

[9]
Perspectives in solubility measurement and interpretation.

ADMET DMPK. 2019-4-5

[10]
Recent advances in drug polymorphs: Aspects of pharmaceutical properties and selective crystallization.

Int J Pharm. 2022-1-5

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