Salts of Therapeutic Agents: Chemical, Physicochemical, and Biological Considerations

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Deepak GuptaSheeba Varghese Gupta

Abstract

The physicochemical and biological properties of active pharmaceutical ingredients (APIs) are greatly affected by their salt forms. The choice of a particular salt formulation is based on numerous factors such as API chemistry, intended dosage form, pharmacokinetics, and pharmacodynamics. The appropriate salt can improve the overall therapeutic and pharmaceutical effects of an API. However, the incorrect salt form can have the opposite effect, and can be quite detrimental for overall drug development. This review summarizes several criteria for choosing the appropriate salt forms, along with the effects of salt forms on the pharmaceutical properties of APIs. In addition to a comprehensive review of the selection criteria, this review also gives a brief historic perspective of the salt selection processes.

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Citations

Jul 4, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Aurel TăbăcaruRodica Mihaela Dinică
Feb 20, 2020·International Journal of Molecular Sciences·Nuno H C S SilvaCarmen S R Freire
Jun 21, 2020·Antibiotics·Muhammad IdreesAyesha Rahman
Jul 16, 2020·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Sophie BouMayeul Collot
Oct 2, 2019·Pharmaceutics·Sawittree SahakijpijarnRobert O Williams
Apr 30, 2020·MedChemComm·Helga Ruebsamen-Schaeff, Helmut Buschmann
Aug 23, 2020·International Journal of Molecular Sciences·Julia L Shamshina, Robin D Rogers
Oct 24, 2020·Pharmaceutics·Manali Banerjee, Blair Brettmann
Feb 13, 2021·Drug Development and Industrial Pharmacy·Bhupendra Raj GiriDong Wuk Kim
Mar 4, 2021·Pharmaceutical Development and Technology·Afrooz HamidehMansoor A Khan
Jun 4, 2021·European Journal of Medicinal Chemistry·Yulia L VolodinaAlexander A Shtil
Dec 22, 2020·ACS Omega·Alexander M SherwoodKelsey Lenoch
Sep 22, 2021·Drug Discovery Today·Elisa PasquaChris Hurley

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Methods Mentioned

BETA
differential scanning calorimetry
X-ray
nuclear magnetic resonance

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