Development and validation of a sensitive UHPLC–MS/MS method for quantitative analysis of farrerol in rat plasma: Application to pharmacokinetic and bioavailability studies

Abstract

Farrerol is a 2,3-dihydro-flavonoid isolated from rhododendron. In this study, a sensitive and selective ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed for the determination of farrerol in rat plasma. Liquid-liquid extraction by ethyl ether was used for sample preparation. Chromatographic separation was achieved on an Agilent UHPLC XDB-C column (2.1 × 100 mm, 1.8 μm) with water and methanol (30:70, v/v) as the mobile phase. An electrospray source was applied and operated in negative ion mode; selection reaction monitoring was used for quantification using target fragment ions m/z 299 → 179 for farrerol and m/z 267 → 252 for internal standard. Calibration plots were linear in the range of 2.88-1440 ng/mL for farrerol in rat plasma. Intra- and inter-day precisions were <11.6%, and the accuracy ranged from -13.9 to 11.9%. The UHPLC-MS/MS method was successfully applied in pharmacokinetics and bioavailability studies of farrerol in rats.

Farrerol ameliorate adjuvant‐induced ankle injury via alteration of PPAR‐γ signal pathway

“…UHPLC-MS/MS model for the estimation of farrerol in rat plasma using 50 μl of plasma over the 2-88-1440 ng/ml range has been developed and validated (Piao et al, 2017).…”

A Complete Study of Farrerol Metabolites Produced In Vivo and In Vitro

“…Likewise, glucuronide metabolites were also detected in urine by UHPLC-MS in the present work. With respect to pharmacokinetic and bioavailability studies of farrerol, a sensitive LC-MS method developed and validated for the quantitation of farrerol in rat plasma revealed that farrerol is rapidly absorbed and slowly eliminated in rats when administered orally, but is quickly eliminated when administered intravenously [34]. These results provide a theoretical foundation for the study of farrerol metabolites in plasma.…”

“…The 18 rats were divided into six groups (groups 1, 3, 5: blood experimental group, bile experimental group, urine and feces experimental group; groups 2, 4, 6: blood blank group, bile blank group and urine and feces blank group) and fasted for 12 h before operation. Farrerol powder was suspended in 0.5 wt% aqueous carboxymethyl cellulose sodium (CMC-Na) and intragastrically administered to experimental groups at a dose of 20 mg/kg [34], while an equivalent dose of CMC-Na solution was given to blank groups. All experiments complied with the Guide for the Care and Use of Laboratory Animals of the U.S. National Institutes of Health.…”

“…For plasma sampling, blood (~200 μL) was collected from the orbital vein at 0.083, 0.25, 1, 2, 3, 5, 7, 9, 12, and 24 h after administration [34]. The specimens were centrifuged at 4,500 rpm for 5 min to obtain plasma samples, which were subsequently mixed and stored at −80 °C.…”