CHAPTER 22. Pharmaceutical Properties—the Importance of Solid Form Selection

Abstract

The selection of the solid form for development is a milestone in the conversion of a new chemical entity into a drug product. An understanding of the materials science of a new active pharmaceutical is crucial at the interface of medicinal chemistry and pharmaceutical development. The physical and chemical properties of a new chemical entity that impact product performance and product robustness are strongly influenced by the solid state structure of the active pharmaceutical ingredient. The formation of different solid state structures (salt, co-crystal and polymorph) provides the medicinal chemist and pharmaceutical scientist an opportunity to eliminate undesirable properties thus enabling a rapid and successful development program. Product performance can only be assured when the new chemical entity is delivered to the patient in a chemically and physically stable solid form. In this chapter we will attempt to link new cutting edge academic progress to the best current industrial practices that medicinal chemists and pharmaceutical scientists can apply in selecting the optimal solid form, along with the related pharmaceutical properties that enable the rapid advancement of a new molecules to medicines.