PMID: 9165526May 1, 1997Paper

Intestinal absorption screening of mixtures from combinatorial libraries in the Caco-2 model

Pharmaceutical Research
E W TaylorR A Braeckman

Abstract

Understanding how chemical structures influence transport across the intestinal mucosa will greatly enhance the discovery of orally available drugs. In an attempt to accelerate defining such relationships between structure and transport, six arbitrary mixtures of N-substituted glycine (NSG) peptoids containing 24 physicochemically diverse compounds were evaluated in the Caco-2 model of intestinal absorption. Samples were analyzed by HPLC and the areas of the peaks representing the components of each mixture were summed to measure "aggregate" apparent permeability coefficients (Papp), a score of the influence of the common structural element within each mixture towards absorption. Mass spectrometry was used to identify the chemical structure of Caco-2 permeable compounds. Three linear trimeric mixtures were examined and, for each mixture, none of the components was detected in receiver chambers. It was concluded that the components of these mixtures each had a Papp value less than 0.8 x 10(-6) cm/sec, a permeability less than mannitol. Three dimeric mixtures were examined and they exhibited aggregate P(app) values of 9.2 x 10(-6), 14 x 10(-6) and 6.9 x 10(-6) cm/sec. These transport rates reflected the transport of most of the c...Continue Reading

Citations

Jan 5, 2002·Expert Opinion on Biological Therapy·Imelda Lambkin, Clemencia Pinilla
Aug 21, 2001·Biological & Pharmaceutical Bulletin·T SakaedaM Hashida
Aug 18, 2010·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Adrian S Culf, Rodney J Ouellette
Jun 3, 2000·Annual Review of Pharmacology and Toxicology·R E White
May 5, 1999·Journal of Chromatography. B, Biomedical Sciences and Applications·R D Süssmuth, G Jung
Jun 19, 2001·International Journal of Pharmaceutics·G KrishnaA A Nomeir

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