ArticlePharmaceutical research2000
Pharmacokinetic study of the hepatobiliary transport of indomethacin.
Article in Pharmaceutical research, 2000. 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.
- Characterization of fecal deglucuronidation activity in healthy subjects and in patients treated with fecal microbiota transplantation.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Sex-dependent responses in mice to indomethacin-induced organ injury and gut microbiome-targeted alleviation.Scientific reports · 2025Article
- Physiological Characterization of the Transporter-Mediated Uptake of the Reversible Male Contraceptive H2-Gamendazole Across the Blood-Testis Barrier.The Journal of pharmacology and experimental therapeutics · 2022Article
- Identification of Drug Transporter Genomic Variants and Inhibitors That Protect Against Doxorubicin-Induced Cardiotoxicity.Circulation · 2022Article
- Review
- Towards a Quantitative Mechanistic Understanding of Localized Pulmonary Tissue Retention-A Combined In Vivo/In Silico Approach Based on Four Model Drugs.Pharmaceutics · 2020Article
- Yinchenhao Decoction Alleviates Liver Fibrosis by Regulating Bile Acid Metabolism and TGF-β/Smad/ERK Signalling Pathway.Scientific reports · 2018Article
- Herbal medicine Yinchenhaotang protects against α-naphthylisothiocyanate-induced cholestasis in rats.Scientific reports · 2017Article
- Development of Physiologically Based Pharmacokinetic/Pharmacodynamic Model for Indomethacin Disposition in Pregnancy.PloS one · 2015Article
- Predicting efflux ratios and blood-brain barrier penetration from chemical structure: combining passive permeability with active efflux by P-glycoprotein.ACS chemical neuroscience · 2013Article
- Evaluation of the protective effect of Rhei Radix et Rhizoma against α-naphthylisothiocyanate induced liver injury based on metabolic profile of bile acids.Journal of ethnopharmacology · 2012Article
- CM2 antigen, a potential novel molecule participating in glucuronide transport on rat hepatocyte canalicular membrane.European journal of histochemistry : EJH · 2012Article
- Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.Pharmaceutical research · 2002Article
- Enterohepatic circulation: physiological, pharmacokinetic and clinical implications.Clinical pharmacokinetics · 2002Review
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe biliary excreted amount of indomethacin and its glucuronide is related to the intestinal toxicity of this drug. In the present study, we investigated the hepatobiliary transport of indomethacin.
methodsThe uptake of indomethacin into primary cultured rat hepatocytes and COS-7 cells transfected with cDNA encoding sodium taurocholate co-transporting polypeptide or organic anion transporting polypeptide 1 was examined. Moreover, we compared the biliary excretion of indomethacin and its glucuronide between Sprague-Dawley (SD) rats and Eisai hyperbilirubinemic rats (EHBR) whose canalicular multispecific organic anion transporter/multidrug resistance associated protein 2 (cMOAT/MRP2) function is hereditarily defective.
resultsThe uptake of indomethacin into rat hepatocytes was mediated by Na+-dependent and independent active transport systems. Neither transfectant stimulated the uptake of indomethacin. After intravenous infusion of indomethacin to SD rats, the biliary excretion of indomethacin glucuronide exceeded that of indomethacin. The indomethacin transport clearance across the bile canalicular membrane was comparable between SD rats and EHBR, whereas the corresponding value for indomethacin glucuronide in EHBR was approximately 50% that in SD rats.
conclusionsThese results indicate that another transporter(s) is involved in the hepatic uptake of indomethacin and the canalicular transport of indomethacin glucuronide is mediated by cMOAT/MRP2 whereas that of indomethacin is not mediated by cMOAT/MRP2.
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