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 mmx150 mm, 5 µm), 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 (Cmax) 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. Keywords: Double-peak, Fargesin, HPLC, oral administration, pharmacokinetics, tissue distribution.