[Pharmacokinetics and metabolites of scutellarin in normal and model rats].
OBJECTIVE
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).


CONCLUSIONS
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.
Institute of China Materia Media, China Academy of Traditional Chinese Medicine, Beijing 100700, China.
Hui-min
HM
Gao
Zhi-min
ZM
Wang
Juan
J
Tian
D000818:Animals; D047310:Apigenin / Q000302:isolation & purification / Q000378:metabolism* / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002351:Carrageenan; D005965:Glucuronates / Q000302:isolation & purification / Q000378:metabolism* / Q000493:pharmacokinetics*; D008745:Methylation; D010946:Plants, Medicinal / Q000737:chemistry; D011897:Random Allocation; D051381:Rats; D017208:Rats, Wistar; D031363:Scutellaria / Q000737:chemistry; D013927:Thrombosis / Q000139:chemically induced / Q000378:metabolism*
D005965:Glucuronates; C484876:scutellarin; D047310:Apigenin; D002351:Carrageenan