RT Journal Article
SR Electronic
T1 Predicting Drug Absorption: How Nature Made It a Difficult Problem
JF Journal of Pharmacology and Experimental Therapeutics
JO J Pharmacol Exp Ther
FD American Society for Pharmacology and Experimental Therapeutics
SP 889
OP 895
DO 10.1124/jpet.102.035006
VO 303
IS 3
A1 Philip S. Burton
A1 Jay T. Goodwin
A1 Thomas J. Vidmar
A1 Benny M. Amore
YR 2002
UL http://jpet.aspetjournals.org/content/303/3/889.abstract
AB Significant recent work has focused on predicting drug absorption from structure. Several misperceptions regarding the nature of absorption seem to be common. Among these is that intestinal absorption, permeability, fraction absorbed, and, in some cases, even bioavailability, are equivalent properties and can be used interchangeably. A second common misperception is that absorption, permeability, etc. are discrete, fundamental properties of the molecule and can be predicted solely from some structural representation of the drug. In reality, drug absorption is a complex process dependent upon drug properties such as solubility and permeability, formulation factors, and physiological variables, including regional permeability differences, pH, lumenal and mucosal enzymology, and intestinal motility, among others. This article will explore the influence of these different variables on drug absorption and the implications with regards to attempting to develop predictive drug absorption algorithms.