Using Biorelevant Flux Measurements for Prediction of Fraction Absorbed for the Drug Products of Poorly Soluble Compounds

It was demonstrated [1] that flux measurements provide more in-depth understanding of supersaturated systems than solute concentration measurements alone. Such measurements were further employed to characterize and explain the differences between brand name and generic drug products that were reported from the bioequivalence studies [2]. The benefits of flux measurements are based on the fact that they capture the complex interplay between effects of formulation ingredients on solubility, dissolution rate and permeability of an active pharmaceutical ingredient (API). From the other hand, there has not been a predictive model that would use flux measurements as an input parameter for calculation of maximum absorbable dose (MAD) or fraction of the API absorbed (Fa) from an oral dosage form. This study demonstrated a feasibility of using flux measurements through gastro-intestinal tract (GIT) mimicking artificial membrane to predict MAD and Fa values in biopharmaceutics modelling for BCS Class 2 drugs.

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