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Related Experiment Videos

Drug transport and targeting. Intestinal transport.

D M Oh1, H K Han, G L Amidon

  • 1Department of Pharmacokinetics, Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48105, USA.

Pharmaceutical Biotechnology
|April 1, 2000
PubMed
Summary
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Intestinal transporters play a key role in nutrient and drug absorption. Targeting these transporters, like the intestinal peptide transporter, can enhance drug bioavailability and improve oral absorption.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Gastroenterology

Background:

  • Intestinal transporters are crucial for nutrient and drug absorption, located in brush border and basolateral membranes.
  • These transporters exhibit substrate specificity and regional variations along the intestine, influencing physiological and pathological responses.
  • Deficiencies in intestinal transporters can lead to genetic disorders.

Purpose of the Study:

  • To explore the role of intestinal transporters in drug absorption and bioavailability.
  • To highlight strategies for improving oral drug absorption by targeting intestinal transporters.
  • To discuss the potential of molecular-level understanding for drug design.

Main Methods:

  • Review of existing literature on intestinal transporter function and substrate specificity.
Keywords:
Non-programmatic

Related Experiment Videos

  • Analysis of prodrug strategies utilizing intestinal transporters, such as the peptide transporter.
  • Discussion of recent advances in molecular biology for transporter characterization.
  • Main Results:

    • Intestinal transporters significantly impact the absorption of nutrients and drugs.
    • Prodrug strategies targeting transporters, like the intestinal peptide transporter, have successfully improved bioavailability for drugs such as ACE inhibitors and beta-lactam antibiotics.
    • Inhibiting efflux transporters or utilizing absorption transporters can enhance the bioavailability of poorly absorbed drugs.

    Conclusions:

    • Targeting intestinal transporters is a promising strategy for enhancing drug bioavailability and tissue distribution.
    • Molecular characterization of transporters provides a basis for designing drugs with improved pharmacokinetic profiles.
    • Understanding transporter specificity and kinetics is key to developing effective drug delivery systems.