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Intestinal absorption-modifying excipients: A current update on preclinical in vivo evaluations
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.ORCID iD: 0000-0002-5586-2906
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Neuroscience, Sjöblom/Nylander: Gastrointestinal Physiology.ORCID iD: 0000-0002-1406-9389
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
2019 (English)In: European journal of pharmaceutics and biopharmaceutics, ISSN 0939-6411, E-ISSN 1873-3441, Vol. 142, p. 411-420Article in journal (Refereed) Published
Abstract [en]

Pharmaceutical excipients in drug products are defined as pharmacologically inactive and are integral constituents of all types of oral dosage forms. However, some excipients may increase drug absorption by interacting with the mucosal membrane. If the strategy is to use an excipient with a potential to affect the processes determining the rate and/or extent of the intestinal drug absorption, it is defined as an absorption-modifying excipients (AME). These pharmaceutical excipients may act as AMEs, depending on the amounts applied, and accordingly influence bioequivalence assessment of innovative and generic drug products, as well as enable oral delivery of peptides and oligonucleotides. This review discusses the mechanisms by which AMEs increase drug absorption, and especially permeation step. The focus is on the most recent data regarding how AMEs can be evaluated in preclinical models, with an emphasis on in situ and in vivo intestinal absorption models. The in vivo predictive value of these models is reviewed for five factors of clinical relevance for the intestinal absorption performance: (a) effect and response rate of AMEs, (b) mucosal exposure time and intestinal transit of AMEs, (c) intraluminal AME dilution and prandial state, (d) mucosa] recovery and safety, and (e) variability in the effects of the AMEs. We argue that any preclinical investigations of AMEs that fail to consider these processes will ultimately be of limited clinical value and add little to our understanding of how excipients affect intestinal drug absorption.

Place, publisher, year, edition, pages
2019. Vol. 142, p. 411-420
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-396544DOI: 10.1016/j.ejpb.2019.07.013ISI: 000488654000043PubMedID: 31306749OAI: oai:DiVA.org:uu-396544DiVA, id: diva2:1368564
Funder
EU, FP7, Seventh Framework ProgrammeAvailable from: 2019-11-07 Created: 2019-11-07 Last updated: 2019-11-07Bibliographically approved

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Dahlgren, DavidSjöblom, MarkusLennernäs, Hans

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