Pharmaceutical Salts: Properties, Selection, and Use

An estimated half of all drug molecules used in medicine are administered as salts, and the formation and the selection of a suitable salt for a drug candidate is recognized as an essential step in the preclinical phase of modern drug development. Surprisingly, the scientific literature on this topic is rather limited and scattered throughout numerous journals and patents. The majority of medicinal chemists in pharmaceutical industry are organic chemists for whom salt formation is often a marginal activity restricted to the short-term objective of obtaining crystalline material, and, because a comprehensive resource that addresses the preparation, selection, and use of pharmaceutically active salts has not been available, may forego the opportunities for increased efficacy and improved drug delivery provided by selection of an optimal salt. To fill this gap, an international team presents the necessary theoretical foundations as well as a wealth of detailed practical experience in the choice of pharmaceutically active salts.