title: Pharmacokinetics and oral bioavailability of epimedin C after oral administration of epimedin C and Herba Epimedii extract in rats.
abstract: Epimedin C, an ingredient of Herba Epimedii, has potential for treatment of cardiovascular disease and bone loss. However, there is still no sensitive analytical method to monitor epimedin C in biological samples. The goal of this study was to develop a sensitive and reliable method based on a LC-MS/MS for evaluating the pharmacokinetics of epimedin C after administration of Herba Epimedii in rat. Electrospray ionization in positive-ion mode and multiple reaction monitoring were used to identify and quantitate active components. Analytes were separated by a reverse-phase C18 column. Liquid-liquid extraction using ethyl acetate, evaporation and reconstitution was used to plasma sample preparation. Mass transition of precursor ion → product ion pairs were monitored at m/z 823.4 → 313.1 for epimedin C and m/z 237.1 → 178.9 for carbamazepine (internal standard). A calibration curve gave good linearity (r > 0.999) over the concentration range 2.5-500 ng/mL. Pharmacokinetic data demonstrated that there was rapid distribution and slow elimination after epimedin C administration (1 mg/kg, i.v.). Oral bioavailabilities of epimedin C in the pure compound and in the Herba Epimedii were around 0.58% and 0.13%, respectively. The result suggests that other herbal ingredients of Herba Epimedii may suppress the oral bioavailability of epimedin C.
authors.affiliation: Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, Taipei, Taiwan; Department of Education and Research, Taipei City Hospital, Taipei, Taiwan.
authors.forename: Chia-Jung
authors.initials: CJ
authors.lastname: Lee
authors.forename: Yu-Tse
authors.initials: YT
authors.lastname: Wu
authors.forename: Thomas Y
authors.initials: TY
authors.lastname: Hsueh
authors.forename: Lie-Chwen
authors.initials: LC
authors.lastname: Lin
authors.forename: Tung-Hu
authors.initials: TH
authors.lastname: Tsai
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D005419:Flavonoids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D053719:Tandem Mass Spectrometry / Q000379:methods*
chemical_list: D004365:Drugs, Chinese Herbal; D005419:Flavonoids; C046314:epimedii flavone; C106054:epimedin C
keywords: Epimedium davidii Franch; bioavailability; epimedin C; herbal medicine; traditional Chinese medicine