The gastrointestinal microbiota as a site for the biotransformation of drugs

Sousa, Tiago; Paterson, Ronnie; Moore, Vanessa; Carlsson, Anders; Abrahamsson, Bertil; Basit, Abdul W.

doi:10.1016/j.ijpharm.2008.07.009

Cited by 618Pharmacogenetics and Drug MetabolismGut microbiota and healthAdvanced Drug Delivery Systems

The gastrointestinal microbiota as a site for the biotransformation of drugs

Sousa, Tiago, Paterson, Ronnie, Moore, Vanessa, Carlsson, Anders, Abrahamsson, Bertil, Basit, Abdul W.·2008·International Journal of Pharmaceutics

DOI 10.1016/j.ijpharm.2008.07.009

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Abstract

There are 100 trillion microbes in the human gastrointestinal tract with numbers increasing distally. These microbiota secrete a diverse array of enzymes (primarily for carbohydrate and protein fermentation) giving them substantial metabolic potential which can have major implications for drug stability. At least thirty drugs which are, or have been, available commercially, were subsequently shown to be substrates for these bacterial enzymes, and with increasing numbers of new and existing drugs having the potential for contact with the distal gut (through modified release systems or poor solubility/permeability), many more are expected to be discovered. The major concern with bacterial drug degradation is the behaviour of the metabolite; is it more or less active than the parent compound, or has toxicity resulted? For example, there were eighteen deaths in 1993 due to a drug interaction in which a toxic drug metabolite was produced by bacterial fermentation. Thus, the objective of this review is the provision of a comprehensive overview of this area; the gastrointestinal microbiota, their drug substrates and metabolic mechanisms, and approaches to studying this further are discussed.

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24,25-DIHYDROXYVITAMIN D3: NOT SUCH AN “INACTIVE” METABOLITE AFTER ALL
Lancaster, S. T., Mansell, J. P., & Blom, A. W. (2018) · Orthopaedic Proceedings

Authors: Sousa, T., Paterson, R., Moore, V., Carlsson, A., Abrahamsson, B., & Basit, A. W.
Affiliations: University of London (GB)
AstraZeneca (United Kingdom) (GB)
AstraZeneca (Sweden) (SE)
Corresponding author: Basit, Abdul W.
ORCID: Sousa, Tiago
Abrahamsson, Bertil
Basit, Abdul W.
Venue: International Journal of Pharmaceutics
Publisher: Elsevier BV
Published: 2008-11
Volume: 363
Issue: 1-2
Pages: 1-25
ISSN: 0378-5173 (ISSN-L)
DOI: 10.1016/j.ijpharm.2008.07.009
OpenAlex: W2059272234
Cited by: 618
References: 140
Citations by year: 2026: 19 · 2025: 21 · 2024: 26 · 2023: 34 · 2022: 44 · 2021: 48 · 2020: 53 · 2019: 57 · 2018: 31 · 2017: 41 · 2016: 36 · 2015: 39 · 2014: 42 · 2013: 42 · 2012: 34
FWCI: 2.41
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: International Journal of Pharmaceutics (publishedVersion)
PubMed (publishedVersion)
UCL Discovery (University College London) (submittedVersion)
Topics: Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Gut microbiota and health
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
Keywords: gut microbiota, bacterial enzymes, drug-microbe interactions, drug metabolites, drug toxicity, modified-release formulation, drug solubility and permeability
MeSH terms: Administration, Oral, Animals, Bacteria, Bacterial Proteins, Biological Availability, Biotransformation, Drug Interactions, Drug Stability, Pharmaceutical Preparations, Humans, Intestinal Absorption, Substrate Specificity, Gastrointestinal Tract, Drug-Related Side Effects and Adverse Reactions

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The gastrointestinal microbiota as a site for the biotransformation of drugs

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