ArticleWorld journal of gastroenterology2006
Intestinal permeability of metformin using single-pass intestinal perfusion in rats.
Article in World journal of gastroenterology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 94 citations in OpenAlex.
- Trial
- Targeting Permeability Barriers By Strategic Selection of Thiol Containing Coformer for Novel Cocrystals of Metformin.AAPS PharmSciTech · 2026Article
- Multi-Segmental Evaluation of Intestinal Permeability of Amlodipine at Two Dose Levels.Current pharmaceutical design · 2026Article
- Pluronics® F68 and D-α-tocopheryl polyethylene glycol succinate 1000 tailored self-assembled mixed micelles to improve oral bioavailability of oleanolic acid: in vitro and in vivo characterization.Drug delivery and translational research · 2025Article
- LC-ESI-HRMS-Based Evaluation of Antioxidants as Additives to Inhibit Genotoxic Nitrosamine Formation in Metformin Hydrochloride Tablets.AAPS PharmSciTech · 2025Article
- Region-Specific Effects of Metformin on Gut Microbiome and Metabolome in High-Fat Diet-Induced Type 2 Diabetes Mouse Model.International journal of molecular sciences · 2024Article
- Goldenseal-Mediated Inhibition of Intestinal Uptake Transporters Decreases Metformin Systemic Exposure in Mice.Drug metabolism and disposition: the biological fate of chemicals · 2023Article
- A Novel Oral Drugs Delivery System for Borneol Based on HiCapAAPS PharmSciTech · 2023Article
- Challenges in Permeability Assessment for Oral Drug Product Development.Pharmaceutics · 2023Review
- Biomimetic Dispersive Solid-Phase Microextraction: A Novel Concept for High-Throughput Estimation of Human Oral Absorption of Organic Compounds.Analytical chemistry · 2023Article
- Optimized In Silico Modeling of Drug Absorption after Gastric Bypass: The Case of Metformin.Pharmaceutics · 2021Article
- Physicochemical Characterization and Biopharmaceutical Evaluation of ZWF: A Novel Anticancer Drug for the Treatment of Non-small Cell Lung Cancer.AAPS PharmSciTech · 2021Article
- Meta-Assessment of Metformin Absorption and Disposition Pharmacokinetics in Nine Species.Pharmaceuticals (Basel, Switzerland) · 2021Article
- In vitro pH dependent passive transport of ketoprofen and metformin.ADMET & DMPK · 2021Article
- Article
- Article
- Improving the biopharmaceutical attributes of mangiferin using vitamin E-TPGS co-loaded self-assembled phosholipidic nano-mixed micellar systems.Drug delivery and translational research · 2018Article
- Anti-inflammatory Effects of Fungal Metabolites in Mouse Intestine as Revealed byFrontiers in physiology · 2017Article
- Article
- Blockade of P-Glycoprotein Decreased the Disposition of Phenformin and Increased Plasma Lactate Level.Biomolecules & therapeutics · 2016Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTo characterize the intestinal transport and mechanism of metformin in rats and to investigate whether or not metformin is a substrate for P-glycoprotein (P-gp).
methodsThe effective intestinal permeability of metformin was investigated using single-pass intestinal perfusion (SPIP) technique in male Waster rats. SPIP was performed in three isolated intestinal segments (duodenum, jejunum and ileum) at the same concentration of metformin (50 microg/mL) to test if the intestinal transport of metformin exhibited site-dependent changes, and in a same isolated intestinal segment (duodenal segment) at three different concentrations of metformin (10, 50, 200 microg/mL) to test if the intestinal transport of metformin exhibited concentration-dependent changes. Besides, P-gp inhibitor verapamil (400 microg/mL) was co-perfused with metformin (50 microg/mL) in the duodenum segment to find out if the intestinal absorption of metformin was affected by P-gp exiting along the gastrointestinal track. Stability studies were conducted to ensure that the loss of metformin could be attributed to intestinal absorption.
resultsThe effective permeability values (P(eff)) of metformin in the jejunum and ileum at 50 microg/mL were significantly lower than those in the duodenum at the same concentration. Besides, P(eff) values in the duodenum at high concentration (200 microg/mL) were found to be significantly lower than those at low and medium concentrations (10 and 50 microg/mL). Moreover the co-perfusion with verapamil did not increase the P(eff) value of metformin at 50 microg/mL in the duodenum.
conclusionMetformin could be absorbed from the whole intestine, with the main absorption site at duodenum. This concentration-dependent permeability behavior in the duodenum indicates that metformin is transported by both passive and active carrier-mediated saturable mechanism. The P(eff) value can not be increased by co-perfusion with verapamil, indicating that absorption of metformin is not efficiently transported by P-gp in the gut wall. Furthermore metformin is neither a substrate nor an inducer of P-gp. Based on the P(eff) values obtained in the present study and using established relationships, the human fraction dose absorbed for metformin is estimated to be 74%-90% along human intestine.
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