Pharmaceutical Properties – The Importance of Solid Form Selection

Author:

Doherty Cheryl L.1,Robertson Amy L.2,Clear Nicola3,Docherty Robert4

Affiliation:

1. Medicines Research Centre, GlaxoSmithKline Gunnels Wood Road Stevenage Hertfordshire SG1 2NY UK cheryl.x.doherty@gsk.com

2. Chemical Development, Pharmaceutical Technology and Development, Operations, AstraZeneca Macclesfield SK11 2NA UK

3. Pharmaceutical Sciences, Pfizer Global R&D Ramsgate Road Sandwich Kent CT13 9NJ UK

4. School of Chemical and Process Engineering, University of Leeds Leeds, LS2 9JT UK

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 physicochemical properties of a new chemical entity that impact product performance 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 an opportunity to eliminate undesirable properties thus enabling a rapid and successful development program. In this chapter we will link new 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 new molecules to medicines.

Publisher

The Royal Society of Chemistry

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