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Planta Med 2002; 68(2): 138-141
DOI: 10.1055/s-2002-20244
Original Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

Marked Decrease of Cyclosporin Absorption Caused by Phellamurin in Rats

Hung-Yi Chen1 , Tian-Shung Wu2 , Sheng-Fang Su3 , Sheng-Chu Kuo1 , Pei-Dawn Lee Chao4
  • 1Graduate Institute of Pharmaceutical Chemistry, China Medical College, Taichung, Taiwan, R.O.C.
  • 2Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, R.O.C.
  • 3Department of Clinical Pharmacy, National Cheng Kung University, Tainan, Taiwan, R.O.C.
  • 4Department of Pharmacy, China Medical College, Taichung, Taiwan, R.O.C.
Further Information

Publication History

February 23, 2001

May 24, 2001

Publication Date:
22 February 2002 (online)

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Abstract

Phellamurin is a flavonoid glycoside that is abundant in the leaves of Phellodendron wilsonii Hayata et Kanehira (Rutaceae). In vitro everted rat intestine study indicated that phellamurin inhibited intestinal P-glycoprotein in a dose-dependent manner. In order to investigate the effect of phellamurin on cyclosporin absorption and disposition, rats were given cyclosporin (5 mg/kg) with or without phellamurin in a parallel design. Fluorescence polarization immunoassay was used to determine the blood concentration of cyclosporin. Unanticipatedly, our results indicated that the coadministration of phellamurin significantly decreased the Cmax of cyclosporin by 77 % and reduced the AUC0-∞ of cyclosporin by 56 %. This indicated that a serious interaction occurred between phellamurin with cyclosporin. To ensure the efficacy of cyclosporin, we suggest that the coadministration of phellamurin or Phellodendron wilsonii with cyclosporin should be avoided.

Key words

Phellamurin - cyclosporin - pharmacokinetic interaction - Phellodendron wilsonii - Rutaceae - flavonoid

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Prof. Pei-Dawn Lee Chao

Dept. of Pharmacy

China Medical College

Taichung

Taiwan 404

R. O. C

Fax: +886-4-22031028

Email: pdlee@mail.cmc.edu.tw

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