Challenges of controlled release formulations

The most crucial factor when creating effective modified release formulations during drug product development is that they must be able to control the release rate of the active pharmaceutical ingredient (API). Excipients that can help facilitate this controlled release effectively are often those that can form thin films as well as tablet matrices. These excipients can control API release meticulously by limiting drug dissolution/diffusion. However, due to the integration of multiple excipient polymers as well as multiple doses of the drug, the final product succeeding dosage form development is commonly large in the case of delayed release tablets or capsules, which in turn can adversely affect patient compliance.

The most important development in the excipient space must be the discovery of new properties belonging to existing molecules.

Other challenges also exist when developing controlled release drugs, such as difficulty in targeting release to the lower intestine, especially when in oral solid dosage form. Although excipients used within controlled release drugs are typically pre-established excipients, new excipients are being explored to enable targeted release in the lower intestine.

In an article with Pharm Tech, our Senior Director Technology Officer & Strategic Investments, Torkel Gren and Senior Director, Formulation Development, Philippe Gorria, elaborate on the challenges faced when developing successful controlled-release formulations as well as how to overcome these challenges. They also discuss approaches that can be taken once a suitable prototype is devised.