ArticlePharmaceutical research1995
Evaluation of intestinal absorption into the portal system in enterohepatic circulation by measuring the difference in portal-venous blood concentrations of diclofenac.
Article in Pharmaceutical research, 1995. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 43 citations in OpenAlex.
- Impact of Species and Tissue Differences on In Vitro Glucuronidation of Diclofenac.Molecules (Basel, Switzerland) · 2024Article
- Characterization of P-Glycoprotein Inhibitors for Evaluating the Effect of P-Glycoprotein on the Intestinal Absorption of Drugs.Pharmaceutics · 2021Article
- Assessment of contribution of BCRP to intestinal absorption of various drugs using portal-systemic blood concentration difference model in mice.Pharmacology research & perspectives · 2020Article
- Impact of P-Glycoprotein on Intestinal Absorption of an Inhibitor of Apoptosis Protein Antagonist in Rats: Mechanisms of Nonlinear Pharmacokinetics and Food Effects.Pharmaceutical research · 2018Article
- Ciprofloxacin blocked enterohepatic circulation of diclofenac and alleviated NSAID-induced enteropathy in rats partly by inhibiting intestinal β-glucuronidase activity.Acta pharmacologica Sinica · 2016Article
- Investigating the barriers to bioavailability of macrolide antibiotics in the rat.European journal of drug metabolism and pharmacokinetics · 2012Article
- Population pharmacokinetic modelling of the enterohepatic recirculation of diclofenac and rofecoxib in rats.British journal of pharmacology · 2008Article
- Advanced pharmacokinetic models based on organ clearance, circulatory, and fractal concepts.The AAPS journal · 2007Review
- Effect of drug release rate on therapeutic outcomes: formulation dependence of gastrointestinal toxicity of diclofenac in the rat.Inflammopharmacology · 2004Article
- A recirculatory model with enterohepatic circulation by measuring portal and systemic blood concentration difference.Journal of pharmacokinetics and pharmacodynamics · 2003Article
- Evaluation of capacity-limited first-pass effect through liver by three-points sampling in portal and hepatic veins and systemic artery.Pharmaceutical research · 2002Article
- Possible mechanism by which the carbapenem antibiotic panipenem decreases the concentration of valproic acid in plasma in rats.Antimicrobial agents and chemotherapy · 1998Article
- Effect of coadministered uridine on intestinal first-pass metabolism of 5'-deoxy-5-fluorouridine in conscious rats--an evaluation by method of portal-systemic concentration difference.Pharmaceutical research · 1998Article
- Local absorption kinetics of levofloxacin from intestinal tract into portal vein in conscious rat using portal-venous concentration difference.Pharmaceutical research · 1996Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeWe evaluated the first-pass effects in vivo by the intestine and liver during enterophepatic circulation (EHC) by simultaneously measuring the portal and venous plasma concentrations of the rat.
methodsThe venous and upper portal blood vessels were cannulated through the jugular and the pyloric veins, respectively, to obtain simultaneously blood samples from both sites. After diclofenac was injected as a bolus through the jugular vein, the concentrations of diclofenac in the portal and jugular veins were measured at time intervals. The absorption rate from the intestinal tract into the portal system was determined using the portal-venous difference in plasma concentrations of diclofenac, considering 40% partitioning of diclofenac into erythrocytes.
resultsAfter one hour, the plasma concentration in the portal vein was always higher than that in the jugular vein in awakening rats with intact EHC (portal-venous blood concentration difference). No portal-venous difference was observed in awakening rats with bile-duct cannulation. Therefore, it was concluded that this portal-venous concentration difference was not due to the hepatic clearance but to diclofenac reabsorption from the intestinal tract.
conclusionsApproximately 40% of the dose of diclofenac was reabsorbed over 8 hours from the intestinal tract into the portal system. By comparing the reabsorbed amounts in the portal system and in the systemic circulation, the hepatic extraction ratio in vivo (FH) of diclofenac was estimated to be 63%.
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