Phellamurin
Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is 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.
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Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Planta Med. 2002 Feb;68(2):138-41.
Marked decrease of cyclosporin absorption caused by phellamurin in rats.[Pubmed:
11859464]
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.
METHODS AND RESULTS:
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 AUC(0-infinity) of cyclosporin by 56 %.
CONCLUSIONS:
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.
