The first edition of this handbook was a tremendous success, collating the scientific literature on this topic that had otherwise been rather limited and scattered throughout numerous journals and patents. The result was a comprehensive resource that addresses the preparation, selection, and use of pharmaceutically active salts, examining the opportunities for increased efficacy and improved drug delivery provided by the selection of an optimal salt. This second, revised edition is designed to meet the continued interest in both the topic and the book.
Altogether, the contributions to this book by international team of authors from academia and pharmaceutical industry reflect the multidisciplinary nature of the science involved in selection of suitable salt forms for new drug products. They present the necessary theoretical foundations as well as a wealth of detailed practical experience in the choice of pharmaceutically active salts, taking great care to address every conceivable aspect of the preparation of pharmaceutical salts.
An introductory chapter presents a concise review of the various objectives in the pursuit of pharmaceutically active salts, followed by the theoretical background of salt formation. There then follow chapters on the practice of salt formation in an industrial R&D environment, as well as regulatory and patent issues. Practical examples for the practitioners at the lab bench are provided, before the book concludes with a comprehensive annotated compilation of the individual salt-forming acids and bases with their relevant properties, followed by an appendix containing tables with the acids and bases sorted alphabetically and by pKa, supplemented with other useful facts and data.
An essential reference for students of medicinal and pharmaceutical chemistry, and an indispensable handbook for R&D chemists, analytical chemists, biologists, development pharmacists, regulatory and patent specialists, and medicinal scientists engaged in preclinical development of drugs. In addition, this comprehensive and up-to-date guide is an instructive companion for all scientists involved in the research and development of drugs and, in particular, of pharmaceutical dosage forms.
P. Heinrich Stahl (Author/Editor) studied PharmaceuticalSciences in Freiburg, Germany, and completed his Ph. D. thesis onthe synthesis of purine heterocycles under the supervision of KurtWalter Merz. This was followed by a postdoctoral fellowship at theSloan-Kettering-Institute for Cancer Research, New York. In 1969,he joined in Basel, Switzerland. At CIBA, Basel, Switzerland, hefocused his attention on pharmaceutical technology and solvedproblems in tablet granulate drying. Subsequent to the merger ofthe Ciba and Geigy companies, he built up the Preformulation Groupfor API characterization at the interface between medicinalchemistry, dosage form development, and analytics. After anassignment to the Summit, N.J., research site of Ciba-Geigy, hereturned to Basel to take over the responsibility for specialformulation topics. Since 1995 he was responsible for the globalcoordination of early compound evaluation. After his retirement in1997, he still continues his research at the Biocenter in Basel,focusing on the in vitro modeling of passive drug transport acrosslipid double-layers. Dr. P. H. Stahl is an IUPAC Fellow and amember of the International Association for PharmaceuticalTechnology, of the Pharmaceutical Society of Germany, and of theSwiss Society of Industrial Pharmacists. He has co-authoredmultiple scientific and technological papers, patents, and bookchapters. He is an active consultant to several pharmaceuticalcompanies. Camille G. Wermuth (Author/Editor) PharmD, PhD, Founder,President and Chief Scientific Officer of Prestwick Chemicalis, aformer Professor of Organic and Medicinal Chemistry at the Facultyof Pharmacy at the Louis Pasteur University in Strasbourg, France.Pr. Wermuth's research combines synthesis and molecular modeling,and concentrates mainly on CNS diseases. He is the author andco-author of over 300 peer-reviewed scientific papers and ofseveral books or book chapters, and holds over 60 patents. Pr.Wermuth has been awarded the Charles Mentzer Prize of theSociete Francaise de Chimie Therapeutique, theLeon Velluz Prize of the French Academy of Science, and thePrix de l'Ordre des Pharmaciens by the French Academy of Pharmacy.He is Corresponding Member of the German Pharmaceutical Society,and was nominated Commandeurs des Palmes Academiques. He hasbeen nominated President of the Division of Chemistry and HumanHealth of the International Union of Pure and Applied Chemistry(IUPAC).