The effects of three absorption-modifying critical excipients on the in vivo intestinal absorption of six model compounds in rats and dogs

International Journal of Pharmaceutics
David DahlgrenH Lennernäs

Abstract

Pharmaceutical excipients that may affect gastrointestinal (GI) drug absorption are called critical pharmaceutical excipients, or absorption-modifying excipients (AMEs) if they act by altering the integrity of the intestinal epithelial cell membrane. Some of these excipients increase intestinal permeability, and subsequently the absorption and bioavailability of the drug. This could have implications for both the assessment of bioequivalence and the efficacy of the absorption-enhancing drug delivery system. The absorption-enhancing effects of AMEs with different mechanisms (chitosan, sodium caprate, sodium dodecyl sulfate (SDS)) have previously been evaluated in the rat single-pass intestinal perfusion (SPIP) model. However, it remains unclear whether these SPIP data are predictive in a more in vivo like model. The same excipients were in this study evaluated in rat and dog intraintestinal bolus models. SDS and chitosan did exert an absorption-enhancing effect in both bolus models, but the effect was substantially lower than those observed in the rat SPIP model. This illustrates the complexity of the AME effects, and indicates that additional GI physiological factors need to be considered in their evaluation. We therefore recom...Continue Reading

Citations

Mar 19, 2020·Pharmaceutics·David DahlgrenHans Lennernäs
Mar 23, 2019·Nutrients·Ana M PugaGregorio Varela-Moreiras
Aug 28, 2020·Expert Opinion on Drug Delivery·Alejandro Ruiz-PicazoMarta González-Álvarez
Sep 22, 2020·Journal of Pharmaceutical Sciences·Xavier J H PepinSandra Suarez-Sharp
Jul 10, 2019·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·I R DubbelboerH Lennernäs
Jul 16, 2019·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·C RoosH Lennernäs
Aug 8, 2021·Journal of Pharmaceutical Sciences·James Butler, Patrick Augustijns
May 30, 2020·Molecular Pharmaceutics·Alejandro Ruiz-PicazoMarival Bermejo
Aug 22, 2021·Advanced Drug Delivery Reviews·Sam Maher, David J Brayden

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