A 'rule of unity' for human intestinal absorption

The ability to predict the passive intestinal absorption of organic compounds can be a valuable tool in drug design. Although Lipinski's 'rule of 5' is commonly used for this purpose, it does not routinely give reliable results. An alternative 'rule of unity' is proposed to...

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Bibliographic Details
Published in:Pharmaceutical research 2006-10, Vol.23 (10), p.2475-2481
Main Authors: YALKOWSKY, S. H, JOHNSON, J. L. H, SANGHVI, T, MACHATHA, S. G
Format: Article
Language:English
Subjects:
Algorithms
Area Under Curve
Bioavailability
Biological and medical sciences
Digestive system
Forecasting
General pharmacology
Humans
Intestinal Absorption
Medical sciences
Molecular Weight
Pharmaceutical technology. Pharmaceutical industry
Pharmacology
Pharmacology. Drug treatments
ROC Curve
Software
Solubility
Sorption
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Summary:The ability to predict the passive intestinal absorption of organic compounds can be a valuable tool in drug design. Although Lipinski's 'rule of 5' is commonly used for this purpose, it does not routinely give reliable results. An alternative 'rule of unity' is proposed to predict the absorption efficiency of orally administered drugs that are passively transported. The rule of unity based upon the theoretical principals that govern passive transport. The 'rule of 5' and the 'rule of unity' are compared using experimentally determined passive human intestinal absorption data for 155 drugs. Absorption values which are >50% of the dose are classified as well absorbed and absorption values which are
ISSN:0724-8741
1573-904X
DOI:10.1007/s11095-006-9000-y