IVIVC in oral absorption for fenofibrate immediate release tablets using a dissolution/permeation system

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery and Formulation
• Pharmacokinetics

Background:

• Predicting in vivo drug performance from in vitro data is crucial for drug development.
• Fenofibrate is a poorly soluble drug whose absorption is significantly affected by food intake.
• Developing reliable in vitro models is essential for efficient drug screening.

Purpose of the Study:

• To evaluate the predictive capability of a dissolution/permeation (D/P) system for fenofibrate solid dosage forms.
• To assess the impact of biorelevant media simulating gastrointestinal conditions on fenofibrate performance.
• To correlate in vitro D/P results with in vivo pharmacokinetic parameters in rats.

Main Methods:

• Utilized a dissolution/permeation (D/P) system with biorelevant dissolution media.
• Simulated both fasted and fed state conditions of the human gastrointestinal tract.
• Correlated in vitro D/P data with in vivo pharmacokinetic parameters (AUC, Cmax) in rat models.

Main Results:

• The in vitro D/P system successfully simulated the effect of food on fenofibrate absorption.
• The amount permeated in the D/P system strongly correlated with in vivo AUC and Cmax of fenofibric acid.
• The D/P system demonstrated good predictability of in vivo performance for fenofibrate.

Conclusions:

• The dissolution/permeation (D/P) system is a valuable tool for predicting the in vivo performance of poorly soluble drugs.
• This in vitro model can aid in the absorption screening of fenofibrate dosage forms.
• The D/P system offers a promising approach for early-stage drug development and formulation optimization.