Quantitative relationship between rat intestinal absorption and Abraham descriptors.
Literature data on the intestinal absorption of 158 drug and drug-like compounds in rats have been collected, and Abraham descriptors for the set of drugs have been calculated using the method of Platts and Abraham et al. Results show that there is a significant relationship between rat intestinal absorption and the Abraham descriptors. In agreement with the human intestinal absorption model, the dominant descriptors in the rat model are the drug hydrogen bond acidity and basicity. In order to compare the absorption models in humans and rats, the absorption model developed from rats was used to predict the absorption in humans. The rat intestinal absorption model is similar to the human absorption model, and data on rats can effectively be used to predict human intestinal absorption.
Zhao
Yuan H
YH
Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, UK.
Abraham
Michael H
MH
Hersey
Anne
A
Luscombe
Chris N
CN
D000818:Animals; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects / Q000502:physiology*; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism*; D011237:Predictive Value of Tests; D051381:Rats; D013329:Structure-Activity Relationship
D004364:Pharmaceutical Preparations