Trial reportEuropean journal of clinical pharmacology2014
Effects of one-time apple juice ingestion on the pharmacokinetics of fexofenadine enantiomers.
Trial report in European journal of clinical pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 35 citations in OpenAlex.
- Food Additives Inhibit Intestinal Drug Transporters but Have Limited Effect on In Vitro Drug Permeability.Molecular pharmaceutics · 2025Article
- Flavonoids and Furanocoumarins Involved in Drug Interactions.Molecules (Basel, Switzerland) · 2025Review
- Clinical Pharmacokinetics of Fexofenadine: A Systematic Review.Pharmaceutics · 2024Review
- Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Chiral Discrimination of P-glycoprotein in Parturient Women: Effect of Fluoxetine on Maternal-Fetal Fexofenadine Pharmacokinetics.Pharmaceutical research · 2020Article
- Role of Oatp2b1 in Drug Absorption and Drug-Drug Interactions.Drug metabolism and disposition: the biological fate of chemicals · 2020Article
- Stimulatory effect on the transport mediated by organic anion transporting polypeptide 2B1.Asian journal of pharmaceutical sciences · 2020Review
- Enantioselective Drug Recognition by Drug Transporters.Molecules (Basel, Switzerland) · 2018Review
- Food-drug interactions precipitated by fruit juices other than grapefruit juice: An update review.Journal of food and drug analysis · 2018Review
- The influence of piperine on the pharmacokinetics of fexofenadine, a P-glycoprotein substrate, in healthy volunteers.European journal of clinical pharmacology · 2017Article
Corrections and comments
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Authors and funding
9 authors at 6 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeWe examined the effect of a single apple juice intake on the pharmacokinetics of fexofenadine enantiomers in healthy Japanese subjects.
methodsIn a randomized two phase, open-label crossover study, 14 subjects received 60 mg of racemic fexofenadine simultaneously with water or apple juice. For the uptake studies, oocytes expressing organic anion-transporting polypeptide 2B1 (OATP2B1) were incubated with 100 μM (R)- and (S)-fexofenadine in the presence or absence of 10 % apple juice.
resultsOne-time ingestion of apple juice significantly decreased the area under the plasma concentration-time curve (AUC0-24) for (R)- and (S)-fexofenadine by 49 and 59 %, respectively, and prolonged the time to reach the maximum plasma concentration (t max) of both enantiomers (P < 0.001). Although apple juice greatly reduced the amount of (R)- and (S)-fexofenadine excretion into urine (Ae0-24) by 54 and 58 %, respectively, the renal clearances of both enantiomers were unchanged between the control and apple juice phases. For in vitro uptake studies, the uptake of both fexofenadine enantiomers into OATP2B1 complementary RNA (cRNA)-injected oocytes was significantly higher than that into water-injected oocytes, and this effect was greater for (R)-fexofenadine. In addition, apple juice significantly decreased the uptake of both enantiomers into OATP2B1 cRNA-injected oocytes.
conclusionsThese results suggest that OATP2B1 plays an important role in the stereoselective pharmacokinetics of fexofenadine and that one-time apple juice ingestion probably inhibits intestinal OATP2B1-mediated transport of both enantiomers. In addition, this study demonstrates that the OATP2B1 inhibition effect does not require repeated ingestion or a large volume of apple juice.
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