PURPOSE

This chapter focuses on the in vitro and in vivo performance of oral dosage forms and provides an overview of the methodology for characterizing the properties of a drug substance as well as its associated oral dosage form that are critical to establish the relationship to the pharmacokinetic properties of the drug product. Results of in vitro methods are linked with information from in vivo evaluations through an in vitro–in vivo correlation (IVIVC), or, if an IVIVC is not possible, an in vitro–in vivo relationship (IVIVR). Establishing an IVIVC may enable a waiver of in vivo bioequivalence study requirements as well as support scale-up and post-approval changes.