title: Evaluation of rat intestinal absorption data and correlation with human intestinal absorption.
abstract: The absorption of 111 drug and drug-like compounds was evaluated from 111 references based on the ratio of urinary excretion of drugs following oral and intravenous administration to intact rats and biliary excretion of bile duct-cannulated rats. Ninety-eight drug compounds for which both human and rat absorption data were available were selected for correlation analysis between the human and rat absorption. The result shows that the extent of absorption in these two species is similar. For 94% of the drugs the absorption difference between humans and rats is less than 20% and for 98% of drugs the difference is less than 30%. There is only one drug for which human absorption is significantly different from rat absorption. The standard deviation is 11% between human and rat absorption. The linear relationship between human and rat absorption forced through the origin, as determined by least squares regression, is %Absorption (human)=0.997%Absorption (rat) (n=98, SD=11). It is suggested that the absorption in rats could be used as an alternative method to human absorption in pre-clinical oral absorption studies.
authors.affiliation: Department of Chemistry, University College London, 20 Gordon Street, WC1H 0AJ, London, UK.
authors.forename: Yuan H
authors.initials: YH
authors.lastname: Zhao
authors.forename: Michael H
authors.initials: MH
authors.lastname: Abraham
authors.forename: Joelle
authors.initials: J
authors.lastname: Le
authors.forename: Anne
authors.initials: A
authors.lastname: Hersey
authors.forename: Chris N
authors.initials: CN
authors.lastname: Luscombe
authors.forename: Gordon
authors.initials: G
authors.lastname: Beck
authors.forename: Brad
authors.initials: B
authors.lastname: Sherborne
authors.forename: Ian
authors.initials: I
authors.lastname: Cooper
mesh_terms: D000465:Algorithms; D000818:Animals; D001646:Bile / Q000378:metabolism; D001711:Biotransformation; D003627:Data Interpretation, Statistical; D004305:Dose-Response Relationship, Drug; D005243:Feces / Q000737:chemistry; D006801:Humans; D007275:Injections, Intravenous; D007408:Intestinal Absorption / Q000502:physiology*; D004364:Pharmaceutical Preparations / Q000378:metabolism; D051381:Rats; D013045:Species Specificity
chemical_list: D004364:Pharmaceutical Preparations