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Preparation of Naringenin Solution for In Vivo Application
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Lack of pharmacokinetic interaction between derazantinib and naringin in rats

Ya-Nan Liu1,2, Jie Chen1,2, Xinhao Xu1,2

  • 1Department of Pharmacy, The First Affiliated Hospital of Wenzhou Medical University, Zhejiang, China.

Pharmaceutical Biology
|March 9, 2023
PubMed
Abstract

Insights

This study validated a new method to measure derazantinib in rat plasma. Co-administering naringin with derazantinib did not significantly alter its pharmacokinetics, suggesting safe concurrent use.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Analytical Chemistry

Background:

  • Derazantinib is an orally bioavailable multikinase inhibitor targeting fibroblast growth factor receptors (FGFRs).
  • It shows preliminary antitumor activity in FGFR2 fusion-positive intrahepatic cholangiocarcinoma (iCCA).
  • Understanding drug-drug interactions is crucial for derazantinib's clinical application.

Purpose of the Study:

  • To validate a sensitive and rapid ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for quantifying derazantinib in rat plasma.
  • To investigate the in vivo drug-drug interaction between derazantinib and naringin.

Main Methods:

  • A novel UPLC-MS/MS method was optimized and validated for derazantinib determination.
  • Pharmacokinetic studies were conducted in Sprague-Dawley rats.
  • Rats received derazantinib (30 mg/kg) with or without oral pretreatment of naringin (50 mg/kg).

Main Results:

  • The UPLC-MS/MS method proved suitable for determining derazantinib concentrations in rat plasma.
  • Naringin pretreatment did not lead to significant alterations in derazantinib's key pharmacokinetic parameters (AUC, t1/2, CLz/F, Cmax).

Conclusions:

  • The developed UPLC-MS/MS method is effective for derazantinib analysis.
  • Concomitant administration of naringin with derazantinib does not significantly affect its pharmacokinetics in rats.
  • This suggests that derazantinib and naringin can be safely co-administered without requiring dose adjustments.
Keywords:
Intrahepatic cholangiocarcinomaUPLC-MS/MSdose adjustmentpharmacokinetics

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