Document Detail


Solubility parameter and oral absorption.
MedLine Citation:
PMID:  10612038     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
L G Martini; P Avontuur; A George; R J Willson; P J Crowley
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V     Volume:  48     ISSN:  0939-6411     ISO Abbreviation:  Eur J Pharm Biopharm     Publication Date:  1999 Nov 
Date Detail:
Created Date:  2000-01-20     Completed Date:  2000-01-20     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9109778     Medline TA:  Eur J Pharm Biopharm     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  259-63     Citation Subset:  IM    
Affiliation:
SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK. luigi_g_martini@sbphrd.com
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MeSH Terms
Descriptor/Qualifier:
Absorption
Animals
Chemistry, Pharmaceutical
Humans
Mice
Mouth Mucosa / metabolism*
Pharmacokinetics*
Ranidae
Rats
Solubility
Structure-Activity Relationship
Swine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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