A rule of unity for human intestinal absorption 3: Application to pharmaceuticals.

Biopharm Drug Dispos

Department of Pharmaceutical Sciences, College of Pharmacy, The University of Arizona, Tucson, Arizona, USA.

Published: February 2018

The rule of unity is based on a simple absorption parameter, Π, that can accurately predict whether or not an orally administered drug will be well absorbed or poorly absorbed. The intrinsic aqueous solubility and octanol-water partition coefficient, along with the drug dose are used to calculate Π. We show that a single delineator value for Π exist that can distinguish whether a drug is likely to be well absorbed (FA ≥ 0.5) or poorly absorbed (FA < 0.5) at any specified dose. The model is shown to give 82.5% correct predictions for over 938 pharmaceuticals. The maximum well-absorbed dose (i.e. the maximum dose that will be more than 50% absorbed) calculated using this model can be utilized as a guideline for drug design and synthesis.

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http://dx.doi.org/10.1002/bdd.2113DOI Listing

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