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Related Experiment Videos

Marked decrease of cyclosporin absorption caused by phellamurin in rats.

Hung-Yi Chen1, Tian-Shung Wu, Sheng-Fang Su

  • 1Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan, R.O.C.

Planta Medica
|February 23, 2002
PubMed
Summary
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Phellamurin, found in Phellodendron wilsonii, significantly reduces cyclosporin absorption. This herb-drug interaction may impact cyclosporin efficacy, necessitating avoidance of coadministration.

Area of Science:

  • Pharmacology
  • Natural Products Chemistry
  • Drug Metabolism

Background:

  • Phellamurin is a flavonoid glycoside from Phellodendron wilsonii leaves.
  • Phellamurin inhibits intestinal P-glycoprotein in vitro.
  • P-glycoprotein plays a crucial role in drug absorption and efflux.

Purpose of the Study:

  • To investigate the effect of phellamurin on cyclosporin absorption and disposition in rats.
  • To determine potential herb-drug interactions between phellamurin and cyclosporin.

Main Methods:

  • In vitro everted rat intestine study to assess P-glycoprotein inhibition.
  • In vivo study in rats administering cyclosporin with and without phellamurin.
  • Fluorescence polarization immunoassay to quantify blood cyclosporin concentrations.

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Main Results:

  • Phellamurin inhibited intestinal P-glycoprotein in a dose-dependent manner.
  • Coadministration of phellamurin significantly decreased cyclosporin Cmax by 77%.
  • AUC(0-infinity) of cyclosporin was reduced by 56% with phellamurin coadministration, indicating a serious interaction.

Conclusions:

  • Phellamurin significantly reduces cyclosporin absorption and disposition.
  • A significant herb-drug interaction exists between phellamurin and cyclosporin.
  • Avoid coadministration of phellamurin or Phellodendron wilsonii with cyclosporin to ensure therapeutic efficacy.