title: Pharmacokinetics of lithospermic acid B isolated from Salvia miltiorrhiza in rats.
abstract: The absorption and pharmacokinetics of an active component of Salvia miltiorrhiza, lithospermic acid B (LSB), was investigated after intravenous and oral administration of doses of 10 or 50 mg LSB/kg to rats. Concentrations of LSB were determined by a validated liquid chromatography/mass spectrometry (LC/MS/MS) assay method. After intravenous administration of 50 mg/kg, dose-normalized (10 mg/kg) area under the curve (AUC) (993 microg.min/ml) was significantly greater than that at 10 mg/kg (702 microg.min/ml). The slower clearance Cl-at 50 mg/kg could be due to saturable metabolism of LSB in rats, and this could be supported by significantly slower Cl(NR) and significantly greater 24-h urinary excretion of LSB at 50 mg/kg than at 10 mg/kg. Following oral administration of LSB, the extent of LSB recovered from the entire gastrointestinal tract at 24 h ranged from 41.2% to 23.3%. Although LSB was not detected (limit of quantitation 10 ng/ml) in plasma after oral dose of 10 mg/kg, the absolute oral bioavailability at 50 mg/kg was 5%. Since LSB was shown to have low permeability through the Caco-2 cell monolayers, the low bioavailability of LSB could be due to poor absorption and metabolism.
authors.affiliation: College of Pharmacy and Medicinal Resources Research Institute, Wonkwang University, Iksan, Korea.
authors.forename: Hui Hyun
authors.initials: HH
authors.lastname: Kim
authors.forename: John
authors.initials: J
authors.lastname: Kim
authors.forename: Hye Young
authors.initials: HY
authors.lastname: Ji
authors.forename: Yoon Chul
authors.initials: YC
authors.lastname: Kim
authors.forename: Dong Hwan
authors.initials: DH
authors.lastname: Sohn
authors.forename: Byung Mu
authors.initials: BM
authors.lastname: Lee
authors.forename: Hye Suk
authors.initials: HS
authors.lastname: Lee
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001572:Benzofurans / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability; D053630:Depsides; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007275:Injections, Intravenous; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D027561:Salvia miltiorrhiza
chemical_list: D001572:Benzofurans; D053630:Depsides; C076944:salvianolic acid B