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A rule of unity for human intestinal absorption 3: Application to pharmaceuticals
Author(s) -
Patel Raj B.,
Yalkowsky Samuel H.
Publication year - 2018
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2113
Subject(s) - partition coefficient , absorption (acoustics) , chemistry , absorbed dose , octanol , drug , solubility , aqueous solution , mathematics , pharmacology , chromatography , materials science , dosimetry , medicine , nuclear medicine , composite material
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.