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Non-Clinical vs Clinical: Risks & Considerations When Developing Modified Release Dosage Forms

1 September 2022

Learn about specialized modified release formulation technologies that are available in the drug development “toolbox” to achieve an optimal target product profile.

In this webinar, Dr. Vanessa Zann, Senior Drug Development Consultant at Quotient Sciences, uses case studies to describe the specialized formulation technologies that are available to achieve an optimal target product profile and how adaptive clinical programs can use human PK data to optimize modified release formulation compositions in real-time.

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Summary

Oral modified release drug products remain highly prevalent in drug development pipelines. These dosage forms tailor the in vivo drug release profile to achieve improved therapeutic outcomes for drugs intended for both local (gastrointestinal) action and systemic delivery. Patients with chronic and acute conditions benefit from the use of modified release dosage forms given that they offer greater compliance and less frequent dosing regimens, coupled with potentially greater efficacy and fewer side effects in comparison to immediate release delivery systems.

Many modified release technologies are available to drug developers, each designed to fulfil very specific performance requirements, such as gastro-retention or sustained-, pulsatile-, or delayed- release formats. The design and development of an effective modified release formulation is however an inherently complex process, presenting many challenges for the development team. Human gastrointestinal anatomy and physiology strongly influences drug release and performance of modified release dosage forms given regional variations in pH, fluid volumes and compositions, surface area, metabolizing enzymes and membrane transporters. Challenges are exacerbated by an over-reliance on in vitro and preclinical test results to inform formulation prototype selection, despite evidence that these data often correlate poorly with pharmacokinetic (PK) performance in humans.

Key discussion points:

  • What challenges exist when developing and manufacturing modified release formulations
  • What drives the need and what are the benefits when going from immediate release to modified release
  • Which approaches to deploy in modified release formulation, such as matrix vs. multiparticulates
  • What relationships exist between formulation parameters, in vitro data and in vivo performance  
  • How gamma scintigraphy can be used to understand bioavailability
  • How to evaluate and optimize formulation performance in real-time using clinical data and design spaces