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Pharmacokinetics, Bioavailability and Metabolism of Rhaponticin in Rat Plasma by UHPLC-Q-TOF/MS and UHPLC-DAD-MSn

Pharmacokinetics, Bioavailability and Metabolism of Rhaponticin in Rat Plasma by UHPLC-Q-TOF/MS and UHPLC-DAD-MSn

Ying-Yong Zhao, Qi Su, Xian-Long Cheng, Xiao-Jie Tan, Xu Bai, Rui-Chao Lin

Bioanalysis. 2012 Mar;4(6):713-23.

PMID: 22452262

Abstract:

Background:
Rhaponticin (Rheum L.) demonstrates a variety of pharmacological activities, including antitumor, antithrombotic and antioxidant effect. However, there is no information describing the pharmacokinetics, bioavailability and metabolism of rhaponticin after intravenous administration.
Results:
UHPLC-Q-TOF/MS and UHPLC-multistage tandem MS methods were developed for the pharmacokinetics, bioavailability and metabolism of rhaponticin in rats. The metabolite of rhaponticin, rhapontigenin, a potent inhibitor of cytochrome P450, was confirmed by UHPLC-multistage tandem MS. The plasma profile of rhaponticin and rhapontigenin was determined by UHPLC-Q-TOF/MS. The results showed that rhaponticin was rapidly distributed and eliminated from rat plasma. The absolute oral bioavailability of rhaponticin was calculated to be 0.03%. The plasma concentrations of rhapontigenin rapidly increased and gradually eliminated after intravenous administration.
Conclusion:
The present pharmacokinetics, bioavailability and metabolism studies of rhaponticin will provide helpful information for development of suitable dosage forms and clinical references on rational administration.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP155588-A	Rhaponticin		155-58-8	Price

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