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Cited by 617Drug Solubulity and Delivery SystemsPharmacogenetics and Drug MetabolismDrug Transport and Resistance Mechanisms

Physicochemical and Physiological Mechanisms for the Effects of Food on Drug Absorption: The Role of Lipids and pH

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Charman, William N., Porter, Christopher J.H., Mithani, Sabena, Dressman, Jennifer B.·1997·Journal of Pharmaceutical Sciences
DOI 10.1021/js960085v
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Abstract

Drugs are absorbed after oral administration as a consequence of a complex array of interactions between the drug, its formulation, and the gastrointestinal (GI) tract. The presence of food within the GI tract impacts significantly on transit profiles, pH, and its solubilization capacity. Consequently, food would be expected to affect the absorption of co-administered drugs when their physicochemical properties are sensitive to these changes. The physicochemical basis by which ingested food/lipids induce changes in the GI tract and influence drug absorption are reviewed. The process of lipid digestion is briefly reviewed and considered in the context of the absorption of poorly water-soluble drugs. The effect of food on GI pH is reviewed in terms of location (stomach, upper and lower small intestine) and the temporal relationship between pH and drug absorption. Case studies are presented in which postprandial changes in bioavailability are rationalized in terms of the sensitivity of the physicochemical properties of the administered drug to the altered GI environment.

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  • Fasting/feeding cycles can influence drug efficiency.

    “Indeed, it is well known that fasting/feeding cycles can influence drug efficiency 172; however, the mechanism behind this observation remains mostly unknown.”

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Authors
Charman, W. N., Porter, C. J. H., Mithani, S., & Dressman, J. B.
Affiliations
  • Monash University (AU)
  • University of Michigan (US)
  • Goethe University Frankfurt (DE)
Corresponding author
Charman, William N.
ORCID
Venue
Journal of Pharmaceutical Sciences
Publisher
American Geophysical Union (AGU)
Published
1997-03
Volume
86
Issue
3
Pages
269-282
ISSN
0022-3549 (ISSN-L)
DOI
10.1021/js960085v
OpenAlex
W1972553581
Cited by
617
References
237
Citations by year
2026: 11 · 2025: 10 · 2024: 12 · 2023: 16 · 2022: 19 · 2021: 26 · 2020: 17 · 2019: 26 · 2018: 25 · 2017: 29 · 2016: 41 · 2015: 34 · 2014: 32 · 2013: 22 · 2012: 33
FWCI
1.75
Type
journal article
Language
en
Open access
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • Journal of Pharmaceutical Sciences (publishedVersion)
  • PubMed (publishedVersion)
  • Deep Blue (University of Michigan) (submittedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
  • Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Keywords
food-drug interactions, drug absorption, gastrointestinal pH, dietary fat, lipid digestion, poorly water-soluble drugs, gastrointestinal transit, oral administration, drug solubilization
MeSH terms
Bile, Biological Availability, Clinical Trials as Topic, Dietary Fats, Pharmaceutical Preparations, Gastric Mucosa, Gastrointestinal Transit, Humans, Hydrogen-Ion Concentration, Intestinal Absorption, Lymphatic System, Permeability, Stomach, Food-Drug Interactions, Postprandial Period

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