Solubility parameter and oral absorption

Eur J Pharm Biopharm. 1999 Nov;48(3):259-63. doi: 10.1016/s0939-6411(99)00055-7.

Abstract

The solubility parameter (delta) for a series of structurally diverse compounds was determined using a group contribution method devised by Fedors, and then related to the degree of oral absorption. Solubility parameter values around 22.5 MPa1/2 were shown to be associated with compounds that were well absorbed, whereas, compounds with a high delta (30-40 MPa1/2) showed poor absorption. A correlation was also evident between the number of H-bonding acceptor groups in a compound and the extent of oral absorption. Surprisingly, when C Log P values were used in comparison, no obvious correlation existed. The conclusion from this work is that the solubility parameter may be a more reasonable predictor of absorption than using C Log P values.

Publication types

  • Comparative Study

MeSH terms

  • Absorption
  • Animals
  • Chemistry, Pharmaceutical
  • Humans
  • Mice
  • Mouth Mucosa / metabolism*
  • Pharmacokinetics*
  • Ranidae
  • Rats
  • Solubility
  • Structure-Activity Relationship
  • Swine