Cited by 418Pharmacogenetics and Drug MetabolismDiabetes Treatment and ManagementMetabolism, Diabetes, and Cancer

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Accumulation of metformin by tissues of the normal and diabetic mouse

Wilcock, C., Bailey, C. J.·1994·Xenobiotica

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Abstract

1. Tissue accumulation of the antihyperglycaemic agent metformin (dimethylbiguanide) was examined after oral administration to the normal and streptozotocin (STZ) diabetic mouse. 2. Metformin (50 mg/kg body weight containing 14C-metformin 25 microCi/kg body weight), which is stable and not metabolized, resulted in maximum plasma concentrations at 0.5 h which declined to < 5% of maximum by 24 h. Maximum plasma concentrations (mumol/l, mean +/- SE) in the hepatic portal vein (normal 51.7 +/- 5.4, STZ 61.5 +/- 8.0) were higher than in the inferior vena cava (normal 29.0 +/- 2.8, STZ 35.4 +/- 5.9). 3. The greatest accumulation of metformin occurred in tissues of the small intestine, where maximum concentrations were > 1000 mumol/kg wet weight at 0.5-2 h, but declined to < 2% of maximum by 24 h. 4. Stomach, colon, salivary gland, kidney and liver accumulated metformin more than two-fold, and concentrations of the drug in heart and skeletal (gastrocnemius) muscle were greater than plasma concentrations on some occasions up to 8 h. 5. In a separate study, i.v.-administered metformin was selectively accumulated by tissues of the small intestine. Thus, retention of metformin by tissues of the small intestine may represent a deep compartment for the drug.

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Authors: Wilcock, C., & Bailey, C. J.
Affiliations: Aston University (GB)
ORCID: Bailey, C. J.
Venue: Xenobiotica
Publisher: Informa UK Limited
Published: 1994-01
Volume: 24
Issue: 1
Pages: 49-57
ISSN: 0049-8254 (ISSN-L)
1366-5928
DOI: 10.3109/00498259409043220
OpenAlex: W2136667764
Cited by: 418
References: 23
Citations by year: 2026: 6 · 2025: 14 · 2024: 20 · 2023: 23 · 2022: 22 · 2021: 23 · 2020: 21 · 2019: 24 · 2018: 30 · 2017: 31 · 2016: 26 · 2015: 31 · 2014: 30 · 2013: 19 · 2012: 12
FWCI: 2.92
Type: journal article
Language: en
Open access: closed
Locations: Xenobiotica (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
Keywords: metformin, tissue accumulation, streptozotocin-induced diabetes, small intestine, drug retention, plasma concentration, oral administration, antidiabetic drugs, drug distribution
MeSH terms: Administration, Oral, Animals, Diabetes Mellitus, Experimental, Digestive System, Injections, Intravenous, Male, Metformin, Mice, Inbred Strains, Tissue Distribution, Mice

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Accumulation of metformin by tissues of the normal and diabetic mouse

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