The process, equipment, and technology for developing and manufacturing oral solid-dosage forms are well defined. Nonetheless, designing a drug product formulation that achieves the desired properties of the target profile both in magnitude and robustness is a multi-dimensional, and generally, constrained optimization problem, observes Aaron Goodwin, principal investigator, Research and Development, Capsugel. The ultimate goal in formulation development is to deliver the drug to the right place, at the right time, in the right concentration so that a beneficial therapeutic effect is achieved, John McDermott, executive director, Drug Product Optimization, Quotient, explains.
“Historically, the focus of formulation optimization has been placed upon the manufacturing process because molecules and drug-delivery requirements were arguably more straightforward,” says McDermott. He points out that most new chemical entities (NCEs) entering the development pipeline, however, often have complex physicochemical properties that require enabled formulation technologies to overcome solubility and/or permeability challenges, or a modified-release technology to achieve a suitable treatment regime or protect patients from adverse events associated with peak plasma concentrations. “In all of these cases, optimization of the formulation composition is essential to ensure successful and consistent drug delivery without compromising other criteria, such as dosage form size, or wasting valuable drug,” he says.