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Considerations in the developability of peptides for oral administration when formulated together with transient permeation enhancers
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. AstraZeneca, Pharmaceut Sci, R&D, Adv Drug Delivery, Gothenburg, Sweden.. (Swedish Drug Delivery Center)
AstraZeneca, Clin Pharmacol & Safety Sci, R&D, Clin Pharmacol & Quantitat Pharmacol, Gothenburg, Sweden..
AstraZeneca, Pharmaceut Sci, R&D, Early Chem Dev, Macclesfield, Cheshire, England..
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy. (Swedish Drug Delivery Center)ORCID iD: 0000-0002-8917-2612
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2022 (English)In: International Journal of Pharmaceutics, ISSN 0378-5173, E-ISSN 1873-3476, Vol. 628, article id 122238Article in journal (Refereed) Published
Abstract [en]

This paper reviews many of the properties of a peptide that need to be considered prior to development as an oral dosage form when co-formulated with a permeation enhancer to improve oral bioavailability, including the importance and implications of peptide half-life on variability in pharmacokinetic profiles. Clinical consider-ations in terms of food and drug-drug interactions are also discussed. The paper further gives a brief overview how permeation enhancers overcome barriers that limit oral absorption of peptides and thereby improve their oral bioavailability, albeit bioavailabilities are still low single digit and variability is high.

Place, publisher, year, edition, pages
Elsevier, 2022. Vol. 628, article id 122238
Keywords [en]
Oral peptide delivery, Peptide properties, Permeation enhancer, Bioavailability, Variability, Population pharmacokinetic modelling
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-489724DOI: 10.1016/j.ijpharm.2022.122238ISI: 000882068800006PubMedID: 36174850OAI: oai:DiVA.org:uu-489724DiVA, id: diva2:1716426
Funder
Vinnova, 2019-00048Available from: 2022-12-06 Created: 2022-12-06 Last updated: 2022-12-06Bibliographically approved

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Berg, StaffanBergström, Christel

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