This article describes the use of MRI to investigate the performance of pharmaceutical dosage forms both in vitro and in vivo. Various commonly used strategies and excipient materials available for controlling drug release are related to MRI methods that are applied to characterize their behavior in biomimetic and biological environments, and also to those circumstances under which application of MRI can be crucial in a pharmaceutical development process. Examples of MRI used in the study of rapid, controlled, and implanted drug-delivery forms are presented and discussed. These include dosage forms based on shaped, multilayer, and membrane designs, and a range of hydrophobic and hydrophilic excipients. Approaches to more detailed understanding based on measuring solvent penetration and diffusion, matrix erosion and disintegration, and correlation between dosage form behavior and drug release are summarized. A significant increase in the use of MRI for industrial dosage form design, testing, quality assurance, and troubleshooting is anticipated.