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[Pharmacokinetics and metabolites of scutellarin in normal and model rats]
Hui-min Gao1, Zhi-min Wang, Juan Tian
1Institute of China Materia Media, China Academy of Traditional Chinese Medicine, Beijing 100700, China.
Aim:
To investigate the pharmacokinetics and metabolites of scutellarin in normal rats and rats with thrombosis model induced by carrageenan.
Methods:
Scutellarin was assayed by reverse phase high performance liquid chromatography in various plasma samples after a single dose of 36 mg x kg(-1) iv to each rat, the pharmacokinetic parameters were estimated by 3P97 program. The metabolites of scutellarin in blood were chromatographed and identified by HPLC-PDA, LC/MS/MS.
Results:
The calibration curve was linear over the range from 0.625 to 80.0 microg x mL(-1) (r = 0.9995), the limit quantitation was 0.312 microg x mL(-1). The plasma scutellarin concentration-time curve was fitted to the open two-compartment model. In the plasma samples, the main metabolites were deduced as 4',5-dihydroxyflavonon-7-O-beta-D-glucuronopyranosyl ester (M1), scutellarin (M2), 7-methoxy-4',5-dihydroxy-flavonon (M3) and 7-methoxy4,5,6-dihydroxyflavonon (M4).
Conclusion:
The pharmacokinetic parameters of scutellarin were significantly different in normal and model rats. The metabolic pathways of scutellarin was proposed to be dehydroxylation and methylation.
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