Absorption prediction from physicochemical parameters

Authors
Citation
Sd. Kramer, Absorption prediction from physicochemical parameters, PHARM SCI T, 2(9), 1999, pp. 373-380
Citations number
44
Categorie Soggetti
Pharmacology & Toxicology
Journal title
PHARMACEUTICAL SCIENCE & TECHNOLOGY TODAY
ISSN journal
14615347 → ACNP
Volume
2
Issue
9
Year of publication
1999
Pages
373 - 380
Database
ISI
SICI code
1461-5347(199909)2:9<373:APFPP>2.0.ZU;2-L
Abstract
Modern drug design not only focuses on the pharmacological activity of a co mpound but also considers its ability to be absorbed and to reach its site of action. The prediction of in vivo barrier permeabilities, particularly i ntestinal absorption and blood-brain barrier passage, are substantial conce rns in the development of new drug compounds. For several decades, n-octano l-water partition coefficients dominated absorption prediction, In recent y ears, the basic physicochemical parameters describing both membrane permeab ility and lipophilicity have been established. This review provides an outl ine of some selected absorption-prediction models with emphasis on intestin al absorption.