Oral Bioavailability of Peptide and Peptidomimetic Drugs: Amino Acids, Peptides and Proteins in Organic Chemistry: Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis, Volume 4

Arik Dahan, Yasuhiro Tsume, Jing Sun, Jonathan M. Miller, Gordon L. Amidon

    Research output: Chapter in Book/Report/Conference proceedingChapter

    1 Scopus citations

    Abstract

    Peptide oral drug delivery has long been a challenging interest. Remarkable advances in recombinant DNA technology and synthetic chemistry, together with the development of receptor-based screening procedures, allow for the large-scale production of structurally diverse peptides exhibiting a broad spectrum of pharmacological effects. However, the development of these peptides/peptide-like compounds into effective drugs, and especially orally administered drugs, has been restricted due to various limitations, such as transport barriers, intestinal and hepatic metabolism, chemical instability, and hepatic elimination mechanisms. Development of an effective oral delivery system for this class of compounds requires a thorough understanding of the various physicochemical, physiological, and dosage formrelated factors governing the rate and extent of absorption following oral administration. In this chapter, we review the various factors influencing the oral systemic availability of peptide and peptidomimetic compounds, the barriers that compromise their systemic absorption, and the different approaches that have been utilized to overcome these barriers.
    Original languageEnglish
    Title of host publicationAmino Acids, Peptides and Proteins in Organic Chemistry
    EditorsAndrew B. Hughes
    PublisherWiley-VCH
    Chapter8
    Pages277-292
    Number of pages16
    Volume4
    ISBN (Print)9783527321032
    DOIs
    StatePublished - 7 Apr 2011

    Keywords

    • Dosage form
    • Oral drug delivery
    • Peptide
    • Peptidomimetic
    • Systemic availability

    ASJC Scopus subject areas

    • Chemistry (all)

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