Pharmacokinetics, bioavailability, tissue distribution and excretion of tangeretin in rat

W.-L. Hung, W.-S. Chang, W.-C. Lu, G.-J. Wei, Y. Wang, C.-T. Ho, L.S. Hwang

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74 Citations (Scopus)


Tangeretin, 4′,5,6,7,8-pentamethoxyflavone, is one of the major polymethoxyflavones (PMFs) existing in citrus fruits, particularly in the peels of sweet oranges and mandarins. Tangeretin has been reported to possess several beneficial bioactivities including anti-inflammatory, anti-proliferative and neuroprotective effects. To achieve a thorough understanding of the biological actions of tangeretin in vivo, our current study is designed to investigate the pharmacokinetics, bioavailability, distribution and excretion of tangeretin in rats. After oral administration of 50 mg/kg bw tangeretin to rats, the Cmax, Tmax and t1/2 were 0.87 ± 0.33 μg/mL, 340.00 ± 48.99 min and 342.43 ± 71.27 min, respectively. Based on the area under the curves (AUC) of oral and intravenous administration of tangeretin, calculated absolute oral bioavailability was 27.11%. During tissue distribution, maximum concentrations of tangeretin in the vital organs occurred at 4 or 8 h after oral administration. The highest accumulation of tangeretin was found in the kidney, lung and liver, followed by spleen and heart. In the gastrointestinal tract, maximum concentrations of tangeretin in the stomach and small intestine were found at 4 h, while in the cecum, colon and rectum, tangeretin reached the maximum concentrations at 12 h. Tangeretin excreted in the urine and feces was recovered within 48 h after oral administration, concentrations were only 0.0026% and 7.54%, respectively. These results suggest that tangeretin was mainly eliminated as metabolites. In conclusion, our study provides useful information regarding absorption, distribution, as well as excretion of tangeretin, which will provide a good base for studying the mechanism of its biological effects. © 2017
Original languageEnglish
Pages (from-to)849-857
Number of pages9
JournalJournal of Food and Drug Analysis
Issue number2
Publication statusPublished - 2018
Externally publishedYes


  • Excretion
  • Oral bioavailability
  • Pharmacokinetics
  • Tangeretin
  • Tissue distribution
  • drug metabolite
  • tangeretin
  • animal experiment
  • animal tissue
  • area under the curve
  • Article
  • cecum
  • colon
  • controlled study
  • drug absorption
  • drug bioavailability
  • drug elimination
  • drug excretion
  • drug half life
  • feces
  • gastrointestinal tract
  • heart
  • in vivo study
  • kidney
  • limit of detection
  • limit of quantitation
  • liquid chromatography-mass spectrometry
  • liver
  • lung
  • male
  • maximum concentration
  • nonhuman
  • rat
  • rectum
  • small intestine
  • spleen
  • stomach
  • time to maximum plasma concentration
  • tissue distribution
  • urinary excretion


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