Pharmacokinetics and Tissue Distribution of Fargesin After Oral Administration in Rats by High Performance Liquid Chromatography

Background: Flos Magnoliae is a frequently-used Chinese herbal medicine, from which Fargesin is isolated with extensive pharmacological activities. Objective: To develop a reliable high performance liquid chromatography (HPLC) method of fargesin and explore pharmacokinetics and tissue distribution profile of fargesin in Sprague Dawley rats after oral administration of 50 mg/kg. Methods and Results: The chromatographic analysis was conducted on a Shimadzu 2010-ODS-3 C18 column (4.6 mm x 150 mm, 5 mu m), and the mobile phase consisted of methanol and water (58:42 v/v) with a flow rate of 1.0 mL/min. Linearity of fargesin in all biological samples was good (R>0.9990) within the corresponding concentration range and the method was verified to be sensitive, accuracy and precision. The pharmacokinetic results of fargesin after oral administration (50 mg/kg) in rats showed that two absorption peaks were observed in rat plasma at 60min and 290 min, with the highest plasma concentration (C-max) being 464.38 +/- 32.75 ng/mL at 290 min. The tissue distribution results showed that the main tissue depots for fargesin were heart, liver, kidney and lung. Conclusion: This study established a sensitive and reliable HPLC method for the content determinations of fargesin. The pharmacokinetics and tissue distribution results may provide practical information for further study of pharmacological actions and clinical application.