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Oral Delivery

Tech Session VI: Oral Delivery III

Increasing Efficacy - Decreasing Toxicity for a Given Dose Via Controlled Delivery

Thursday, July 17, 2025
6:19 PM – 6:30 PM EDT
Introduction: It is believed that pharmacodynamic (PD) measures, efficacy and toxicity, following oral drug delivery are a function of pharmacokinetic (PK) exposure (AUC, Cmax and Cmin). It is recognized that controlled drug delivery could decrease toxicity due to Cmax. However, it is a basic concept of PK and clinical medicine that controlled drug delivery for a given dose cannot increase efficacy.  Here we show that this is not correct, consistent with a number of studies demonstrating unexplained significant increases in efficacy for extended release (ER) vs immediate release (IR) formulations.

Learning Objectives:

At the completion of this activity, participants will know
  • Participants will understand why drug AUC can be function of clearance from the delivery site.
  • Define why drug input can increase AUC & PD effects, allowing the formulator to control clearance.
  • Use slow clearance from a delivery site relative to iv bolus clearance to increase PD for low doses.