ArticleJournal of pharmacokinetics and biopharmaceutics1991
Pharmacokinetics and bioavailability of diclofenac in the rat.
Article in Journal of pharmacokinetics and biopharmaceutics, 1991. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 76 citations in OpenAlex.
- Gut Microbiota in NSAID Enteropathy: Current Evidence and Future Perspectives for Therapeutic Strategies.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Impact of Species and Tissue Differences on In Vitro Glucuronidation of Diclofenac.Molecules (Basel, Switzerland) · 2024Article
- Examination of Urinary Excretion of Unchanged Drug in Humans and Preclinical Animal Models: Increasing the Predictability of Poor Metabolism in Humans.Pharmaceutical research · 2021Review
- Gut Microbiota in NSAID Enteropathy: New Insights From Inside.Frontiers in cellular and infection microbiology · 2021Review
- Antinociceptive Interaction and Pharmacokinetics of the Combination Treatments of Methyleugenol Plus Diclofenac or Ketorolac.Molecules (Basel, Switzerland) · 2020Article
- Sciatic nerve injury following analgesic drug injection in rats: A histopathological examination.Northern clinics of Istanbul · 2018Article
- Role of non-steroidal anti-inflammatory drugs on intestinal permeability and nonalcoholic fatty liver disease.World journal of gastroenterology · 2017Review
- Pharmacokinetics Studies of 12 Alkaloids in Rat Plasma after Oral Administration of Zuojin and Fan-Zuojin Formulas.Molecules (Basel, Switzerland) · 2017Article
- Ciprofloxacin blocked enterohepatic circulation of diclofenac and alleviated NSAID-induced enteropathy in rats partly by inhibiting intestinal β-glucuronidase activity.Acta pharmacologica Sinica · 2016Article
- Oral pharmacokinetics of the acidic drugs, diclofenac and sulfamonomethoxine in male Shiba goats.The Journal of veterinary medical science · 2015Article
- Duel-acting subcutaneous microemulsion formulation for improved migraine treatment with zolmitriptan and diclofenac: formulation and in vitro-in vivo characterization.The AAPS journal · 2014Article
- Multiple NSAID-induced hits injure the small intestine: underlying mechanisms and novel strategies.Toxicological sciences : an official journal of the Society of Toxicology · 2013Review
- Appearance of double peaks in plasma concentration-time profile after oral administration depends on gastric emptying profile and weight function.Pharmaceutical research · 2008Article
- Population pharmacokinetic modelling of the enterohepatic recirculation of diclofenac and rofecoxib in rats.British journal of pharmacology · 2008Article
- Effect of betamethasone and diclofenac sodium on serum and tissue concentration of amoxicillin. In vivo study in rats.Journal of applied oral science : revista FOB · 2006Article
- 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
- Regional drug delivery II: relationship between drug targeting index and pharmacokinetic parameters for three non-steroidal anti-inflammatory drugs using the rat air pouch model of inflammation.Pharmaceutical research · 1995Article
- Evaluation of intestinal absorption into the portal system in enterohepatic circulation by measuring the difference in portal-venous blood concentrations of diclofenac.Pharmaceutical research · 1995Article
- Low bioavailability of amoxicillin in rats as a consequence of presystemic degradation in the intestine.Antimicrobial agents and chemotherapy · 1994Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Diclofenac sodium is a widely used drug with interesting absorption and disposition features when administered to laboratory animals. The present study was undertaken to assess the pharmacokinetics of the drug after iv and gastrointestinal dosing to rats. Renal excretion of unchanged drug was negligible, but biliary excretion of the drug (unchanged and conjugated) was detected in bile duct-cannulated rats; it accounted for 27.2 and 31.2% of the total dose following iv and intraduodenal administration, respectively. Most of the drug excreted in the bile was conjugated diclofenac; unchanged drug accounted for only 4.7 and 5.4% of total diclofenac excreted in the bile after iv and intraduodenal dosing, respectively. In normal animals, intestinal absorption of the drug excreted in the bile resulted in higher drug concentrations in plasma than those obtained in bile duct-cannulated rats, but only after 60 min of dosing. When administered directly into the duodenum, diclofenac absorption was extremely fast and the maximum plasma diclofenac concentration was reached within 2 min. After oral dosing, an early peak was also observed, but it was lower than that obtained after intraduodenal dosing: 71% diclofenac bioavailability was found in bile duct-cannulated rats intraduodenally dosed, whereas in normal animals dosed by mouth a bioavailability of 79% was obtained. In normal animals intraduodenally dosed, an apparent bioavailability of 106% was observed. All of these features, particularly the influence of enterohepatic circulation on drug bioavailability, are discussed.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.