Strategies For Accelerating The Development Of Modified Release Oral Forms

Oral modified release (MR) formulations enable control over the rate and location of drug release in the gastro-intestinal (GI) tract, in order to achieve specific therapeutic benefits in comparison to immediate release (IR) formulations, including:

• Maintenance of drug plasma concentrations over a prolonged period to reduce dosing frequency
• Attenuation of peak to trough ratios to reduce the incidence of peak-related adverse events (AEs) and potentially improve efficacy
• Deliver drug to specific, targeted regions of the gastrointestinal (GI) tract to improve absorption or for localized treatment

MR drug delivery can also have commercial benefits and is prevalent as part of product life-cycle management (LCM). Modest reformulation of an already approved drug from an IR to MR format allows both line and patent extension opportunities and continued market exclusivity.

An impressive variety of MR formulation technologies are available eliciting a wide range of control on drug release and delivery. Careful selection of appropriate excipients and delivery technologies is key to the design of MR formulations fulfilling specific performance requirements, from gastro-retention (GR) to sustained or pulsatile release.