Physicochemical Characterization and Oral Dosage Form Design and Selection

Abstract

AbstractIn order to initiate formulation development activities – that is the identification of a “marketable” product – important physical and chemical properties (physicochemical properties) as well as permeability properties need to be determined. Evaluation of these properties early in the discovery process can help discovery teams select which templates to pursue as well as identify the most promising leads. This information is also valuable “downstream” as decisions regarding dosage form design are being made. The focus of this article will be on the physicochemical properties that are most important in the evaluation of discovery leads and that provide the information needed as dosage form development is initiated and progresses. It will become apparent that the most appropriate dosage forms that make sense to consider are dictated by both the physicochemical and biopharmaceutical properties of the drug molecule. Throughout this article, there will be an emphasis on the tools and principles that will help the medicinal chemist during the drug discovery process, with particular emphasis on oral dosage forms.