Computational models to predict aqueous drug solubility, permeability and intestinal absorption

Expert Opin Drug Metab Toxicol. 2005 Dec;1(4):613-27. doi: 10.1517/17425255.1.4.613.

Abstract

In the last decade, poor intestinal absorption of candidate drugs intended for oral administration has been identified as a major bottleneck in drug development. Poor intestinal absorption can often be related to poor aqueous solubility and/or poor permeability across the intestinal wall. Other factors, such as poor stability and the metabolism of the compounds, can also decrease the amount of compound absorbed. In an effort to design compounds with enhanced absorption profile, theoretical predictions of solubility and permeability, among other factors, have gained increased interest, and a large number of papers have been published. In this review, the databases and techniques used for the development of in silico absorption models will be discussed. The focus is on aqueous drug solubility, which has become a major problem in drug development.

Publication types

  • Review

MeSH terms

  • Intestinal Absorption*
  • Mathematics
  • Models, Theoretical
  • Permeability
  • Pharmaceutical Preparations / chemistry*
  • Solubility*
  • Solutions

Substances

  • Pharmaceutical Preparations
  • Solutions