Reduction of the acute bioavailability of metformin by the α‐glucosidase inhibitor acarbose in normal man
Abstract
In a double‐blind cross‐over study, we investigated a possible influence of the α‐glucosidase inhibitor acarbose on the bioavailability of the biguanide compound metformin. Each of the six healthy young male volunteers was randomly allocated during two consecutive 7 day periods to either acarbose (days 1–3: 3 times 50mg day−1; days 4–7: 3 times 100 mg day−1) or placebo. At day 7 and 14 of the study, the overnight‐fasted subjects ingested 1000mg metformin with the first bite of a standardized breakfast (500kcal; 60 g carbohydrates) and together with either placebo or 100 mg acarbose. Acarbose significantly (P < 0·05) reduced the meal‐induced increase in blood glucose and plasma insulin levels. Acarbose induced a significant (P < 0·05) reduction in early (90, 120, 180min) serum levels, peak concentrations (Cmax: 1·22 ± 0·14 vs. 1·87 ± 0·60 mgl−1) and area under the curve of metformin (AUC 0–540min: 423±55 vs. 652±55 mg minl−1), but did not diminish its 24 h urinary excretion. In conclusion, acarbose significantly reduces the acute bioavailability of metformin in normal subjects.
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Acarbose reduces the bioavailability of metformin.
“Acarbose reduces the bioavailability of metformin [37].”
From Metformin: An Old But Still the Best Treatment for Type 2 Diabetes (2013) · cites this paper as [37]
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Metformin: An Old But Still the Best Treatment for Type 2 Diabetes
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- Authors
- SCHEEN, A. J., FERREIRA ALVES de MAGALHAES, A. C., SALVATORE, T., & LEFEBVRE, P. J.
- Affiliations
- University of Liège (BE)
- Corresponding author
- SCHEEN, A. J.
- Venue
- European Journal of Clinical Investigation
- Publisher
- Wiley
- Published
- 1994-08
- Volume
- 24
- Issue
- S3
- Pages
- 50-54
- ISSN
- 0014-2972 (ISSN-L)
- 1365-2362
- OpenAlex
- W2073462187
- Cited by
- 42
- References
- 18
- Citations by year
- 2026: 1 · 2025: 1 · 2024: 1 · 2018: 1 · 2017: 1 · 2016: 3 · 2015: 2 · 2014: 2 · 2013: 2 · 2012: 1
- FWCI
- 3.81
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Clinical Investigation (publishedVersion)
- PubMed (publishedVersion)
- Open Repository and Bibliography (University of Liège) (submittedVersion)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
- Keywords
- metformin, acarbose, alpha-glucosidase inhibitors, drug-drug interactions, bioavailability, pharmacokinetics, biguanides, blood glucose, insulin, urinary excretion, healthy volunteers
- MeSH terms
- Adult, Biological Availability, Blood Glucose, Double-Blind Method, Humans, Hypoglycemic Agents, Insulin, Male, Metformin, Reference Values, Trisaccharides, Cross-Over Studies, Acarbose, Glycoside Hydrolase Inhibitors
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