Pharmacokinetics of baicalein, baicalin and wogonin after oral administration of a standardized extract of Scutellaria baicalensis, PF-2405 in rats.
The pharmacokinetics of active components such as baicalein, wogonin and oroxylin A were evaluated after oral administration of a purified extract of Scutellaria baicalensis GEORGI (PF-2405) containing the high contents of baicalein, wogonin and oroxylin A to rats. Following oral administration of PF-2405 at 10, 20 and 40 mg/kg dose (equivalent to 4.5, 9.0 and 18 mg/kg baicalein), a major constituent baicalein and its active metabolite baicalin showed dose-linear pharmacokinetics as evidenced by unaltered dose-normalized AUC, dose-normalized Cmax, Ae(0-30h) and GI(30h) values. Following oral administration of PF-2405 at three doses (equivalent to 0.4, 0.8 and 1.6 mg/kg wogonin), dose-normalized Cmax and dose-normalized AUC were comparable between the 20 and 40 mg/kg PF2405 doses, but plasma concentrations of wogonin at 10 mg/kg of PF-2405 were not measurable as they were below limit of quantitation (LOQ; 18 pmol/mL). Following oral administration of PF-2405 at the three doses (equivalent to 1.5, 3.0 and 6.0 mg/kg oroxylin A), the concentrations of oroxylin A in plasma, urine and gastrointestine samples were below the assay LOQ (18 pmol/mL). Significant differences in AUCs, Ae(0-30h) and GI(30h) values for baicalein and baicalin were observed after oral administration of pure baicalein (18 mg/kg) and PF-2405 (40 mg/kg). The increases in AUCs of baicalein and baicalin after oral administration of PF-2405 may have been due to the significant decrease in GO(30h) values for baicalein.
Kim
Young Hoon
YH
College of Pharmacy, Wonkwang University, Iksan 570-749, Korea.
Jeong
Dong Won
DW
Kim
Yoon-Cheol
YC
Sohn
Dong Hwan
DH
Park
Eun-Seok
ES
Lee
Hye Suk
HS
D000284:Administration, Oral; D000818:Animals; D002853:Chromatography, Liquid; D044950:Flavanones / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics*; D005419:Flavonoids / Q000032:analysis / Q000097:blood* / Q000652:urine; D041981:Gastrointestinal Tract / Q000378:metabolism; D008297:Male; D010936:Plant Extracts / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D031364:Scutellaria baicalensis / Q000737:chemistry; D053719:Tandem Mass Spectrometry
D044950:Flavanones; D005419:Flavonoids; C000605640:PF-2405; D010936:Plant Extracts; C499814:Scutellaria baicalensis extract; C038044:baicalin; C006680:baicalein; C080669:5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one; C085514:wogonin