Pharmaceutical Salts: Properties, Selection, and UseUpplaga 1

An estimated half of all drug molecules used in medicine are administered as salts, 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, however, the scientific literature on this topic is rather limited and scattered throughout numerous journals and patents. The majority of medicinal chemists in pharmaceutical industry whose primary focus is the design and synthesis of novel compounds as future drug entities are organic chemists for whom salt formation is often a marginal activity restricted to the short-term objective of obtaining crystalline material. Because a comprehensive resource addressing the preparation, selection, and use of salts has not been available, medicinal chemists may have missed opportunities to increase efficacy and improve drug delivery through selection of an optimal salt. To fill this gap in the pharmaceutical bibliography, and international tem of seventeen authors from academia and pharmaceutical industry provide, in their contributions to this volume, the necessary theoretical foundations as well as a wealth of detailed practical experience in the formation and characterization of drug salts and all the issues regarding the final selection of the salt form for drugs and drug candidate.