Summary: Dr. Vanessa Zann is featured in Drug Development & Delivery, discussing strategies for transitioning from immediate-release to modified-release formulation. She highlights how challenges like poor solubility, permeability, and fluctuating drug concentrations can be addressed through modified-release approaches to enhance compliance, maintain therapeutic levels, and reduce side effects.
Simple, immediate release and once-a-day (QD) formulations are desired not only by the patient for rapid onset and improved compliance, but also by the pharmaceutical industry due to ease of development and cost benefits.
However, many small molecules in today’s pipelines have sub-optimal properties for QD immediate-release formulations. Challenges, including poor solubility or permeability, can lead to reduced absorption (input in the body) or high clearance (output from the body) that causes a short duration of therapeutic effect. This results in more frequent dosing regimens, which may not be suitable for patient compliance.
Another challenge comes from the significant peaks and troughs in circulating drug concentrations. Using immediate-release formulations, the drug immediately enters the bloodstream, and if dosing is not optimized, this could lead to side effects for the patient and variation in therapeutic efficacy.
For immediate-release formulations that require more than once-a-day dosing, a modified release formulation, which delivers the drug to the lower GI tract over a sustained period, can be a better choice to achieve the desired therapeutic effects.
The following article discusses opportunities and challenges when transitioning from an immediate-release to modified release formulation, therapeutic benefits and challenges associated with modified release formulations, considerations related to GI physiology environments and API physicochemical properties, and modified release technology choices to help drug developers achieve translation success.
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