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Regional Intestinal Permeability in Rats: A Comparison of Methods.

Molecular pharmaceutics (2017-09-19)
Carl Roos, David Dahlgren, Erik Sjögren, Christer Tannergren, Bertil Abrahamsson, Hans Lennernäs
RÉSUMÉ

Currently, the screening of new drug candidates for intestinal permeation is typically based on in vitro models which give no information regarding regional differences along the gut. When evaluation of intestinal permeability by region is undertaken, two preclinical rat models are commonly used, the Ussing chamber method and single-pass intestinal perfusion (SPIP). To investigate the robustness of in vivo predictions of human intestinal permeability, a set of four model compounds was systematically investigated in both these models, using tissue specimens and segments from the jejunum, ileum, and colon of rats from the same genetic strain. The influence of luminal pH was also determined at two pH levels. Ketoprofen had high and enalaprilat had low effective (P

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Sodium fumarate dibasic, ≥99%