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HPLC with electrochemical detection to examine the pharmacokinetics of baicalin and baicalein in rat plasma after oral administration of a Kampo medicine

, : HPLC with electrochemical detection to examine the pharmacokinetics of baicalin and baicalein in rat plasma after oral administration of a Kampo medicine. Analytical Biochemistry 350(1): 99-104

A highly sensitive method for determining baicalin and baicalein in rat plasma was developed using micro HPLC with electrochemical detection ( micro HPLC-ED). Peak heights for baicalin and baicalein were found to be linearly related to the amounts injected, ranging from 2.2 pg to 4.5 ng (r=0.997) and from 1.4 pg to 2.7 ng (r=0.997), respectively. The detection limits (signal/noise ratio=3) of the current method for baicalin and baicalein were 0.89 and 0.54 pg, respectively. The concentrations of baicalin, baicalein, and their conjugates in rat plasma after oral administration of 2.0 mg/kg of Saiko-keishi-to (TJ-10) were determined. The glucuronide and sulfate forms of baicalin and baicalein in plasma were hydrolyzed enzymatically using beta -glucuronidase and sulfatase, respectively, and the hydrolyzed solutions were extracted with a 0.1-mol/L phosphoric acid-ethyl acetate mixture (1:1, v/v). Based on the time courses of the concentrations of the free and conjugated forms of baicalin and baicalein in rat plasma after oral administration of Saiko-keishi-to, the pharmacokinetic parameters of Cmax, tmax, and AUC0-6h were obtained.


PMID: 16434017

DOI: 10.1016/j.ab.2005.11.007

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