US EPA

4850183 

Journal Article 

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

Gupta, D; Bhatia, D; Dave, V; Sutariya, V; Sheeba Varghese Gupta 

2018 

1 

Molecules
ISSN: 1420-3049 

MDPI AG 

23 

7 (2018) 

1719 

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. 

Organic chemistry; Pharmacokinetics; Chemical compounds; Salts; Pharmaceuticals; Pharmacology; Biological properties; Pharmacodynamics; Drug development; Reviews