ArticlePharmaceutical research2009
Concentration-dependent effect of naringin on intestinal absorption of beta(1)-adrenoceptor antagonist talinolol mediated by p-glycoprotein and organic anion transporting polypeptide (Oatp).
Article in Pharmaceutical research, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 86 citations in OpenAlex.
- Effects of one-time apple juice ingestion on the pharmacokinetics of fexofenadine enantiomers.European journal of clinical pharmacology · 2014Trial
- Effect of grapefruit juice on the pharmacokinetics of tolvaptan, a non-peptide arginine vasopressin antagonist, in healthy subjects.European journal of clinical pharmacology · 2012Trial
- Biowaiver monograph for immediate-release solid oral dosage forms: Amlodipine besylate.Journal of pharmaceutical sciences · 2026Review
- Drug Transporters and Metabolizing Enzymes in Antimicrobial Drug Pharmacokinetics: Mechanisms, Drug-Drug Interactions, and Clinical Implications.Biomolecules · 2025Review
- Conversion of Olmesartan to Olmesartan Medoxomil, A Prodrug that Improves Intestinal Absorption, Confers Substrate Recognition by OATP2B1.Pharmaceutical research · 2024Article
- The Use of an Antioxidant Enables Accurate Evaluation of the Interaction of Curcumin on Organic Anion-Transporting Polypeptides 4C1 by Preventing Auto-Oxidation.International journal of molecular sciences · 2024Article
- Endoplasmic reticulum stress in pancreatic β-cell dysfunction: The potential therapeutic role of dietary flavonoids.Current research in pharmacology and drug discovery · 2024Review
- P-glycoprotein: new insights into structure, physiological function, regulation and alterations in disease.Heliyon · 2022Review
- Influence of osmolality on gastrointestinal fluid volume and drug absorption: potential impact on oral salt supplementation.Journal of pharmaceutical health care and sciences · 2021Article
- Effect of Multi Drug Resistance Protein 4 (MRP4) Inhibition on the Pharmacokinetics and Pharmacodynamics of Ciprofloxacin in Normal and Rats with LPS-Induced Inflammation.European journal of drug metabolism and pharmacokinetics · 2016Article
- Substrate- and dose-dependent drug interactions with grapefruit juice caused by multiple binding sites on OATP2B1.Pharmaceutical research · 2014Article
- Intestinal absorption of HMG-CoA reductase inhibitor pravastatin mediated by organic anion transporting polypeptide.Pharmaceutical research · 2010Article
- Interaction of macrolide antibiotics with intestinally expressed human and rat organic anion-transporting polypeptides.Drug metabolism and disposition: the biological fate of chemicals · 2009Article
- The role of transporters in the pharmacokinetics of orally administered drugs.Pharmaceutical research · 2009Review
- Simulations of the nonlinear dose dependence for substrates of influx and efflux transporters in the human intestine.The AAPS journal · 2009Article
- The grapefruit: an old wine in a new glass? Metabolic and cardiovascular perspectives.Cardiovascular journal of AfricaReview
Corrections and comments
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Authors and funding
8 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe purpose of this study is to clarify the impact of P-gp and Oatp on intestinal absorption of the beta(1)-adrenoceptor antagonist talinolol.
methodsP-gp-mediated transport was measured in LLC-PK1/MDR1 cells. Oatp-mediated uptake was evaluated with Xenopus oocytes expressing Oatp1a5. Rat intestinal permeability was measured by the in situ closed loop method. In vivo absorption was pharmacokinetically assessed by measuring plasma concentration after oral administration in rats.
resultsIn LLC-PK1/MDR1 cells, the permeability of talinolol was markedly higher in the secretory direction than in the absorptive one. The uptake of talinolol by Xenopus oocytes expressing Oatp1a5 was significantly increased compared with that by water-injected oocytes. Naringin inhibited talinolol uptake by Oatp1a5 (IC (50) = 12.7 microM). The reported IC (50) value of naringin for P-gp-mediated transport of talinolol is approximately 2,000 microM. Rat intestinal permeability of talinolol was significantly decreased in the presence of 200 microM naringin, but was significantly increased by 2,000 microM naringin. Similar results were obtained in in vivo absorption studies in rats.
conclusionThe absorption behavior of talinolol can be explained by the involvement of both P-gp and Oatp, based on characterization of talinolol transport by Oatp1a5 and P-gp, and the effects of naringin.
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