The pharmacokinetics, bioavailability and excretion of bergapten after oral and intravenous administration in rats using high performance liquid chromatography with fluorescence detection

Abstract

A sensitive, specific, reproducible and optimized high performance liquid chromatography with fluorescence detection (HPLC-FLD) method for the determination of bergapten in rat plasma was established and applied to the pharmacokinetic and bioavailability study in rat after oral and intravenous administration of bergapten. The method was also successfully applied to the excretion study of bergapten after an oral administration of bergapten at a dose of 15 mg kg−1 to rats. The sample preparation was achieved using liquid–liquid extraction. Isoimperatorin was used as the internal standard (IS). The analytes were detected by using fluorescence detection at an excitation and emission wavelength of 288 and 478 nm, respectively. Using aqueous formic acid (0.1 %, v/v) and acetonitrile as the mobile phase, the chromatographic separation was achieved on a Hedera™ ODS column at a flow rate of 1 mL min−1. The lower limit of quantitation (LLOQ) of bergapten was 2 ng mL−1. The HPLC-FLD method was successfully applied to the pharmacokinetic, bioavailability and excretion study of bergapten in rats.Graphical abstractAn high performance liquid chromatography with fluorescence detection (HPLC-FLD) method for the pharmacokinetic and bioavailability study in rat after administration of bergapten.

Pharmacokinetics, Pharmacodynamics and Dermal Distribution of 5-Methoxypsoralen Based on a Physiologically Based Pharmacokinetic Model to Support Phytotherapy Using Brosimum gaudichaudii

“…The half-life of 5-MOP found in our studies was 9-fold lower than values reported previously [17]. Yu et al reported a half-life of 52.2 ± 42.8 h after oral administration of Radix Angelicae Pubescentis extract [17]. The reason for this discrepancy could be due to the interaction between 5-MOP and other compounds in the extract matrix, the involvement of CYP enzymes or transporters [18], or due to drug precipitation in the GI tract.…”

“…Those findings showed that a dosing interval of 48 h had a good in vitro response. The half-life of 5-MOP found in our studies was 9-fold lower than values reported previously [17]. Yu et al reported a half-life of 52.2 ± 42.8 h after oral administration of Radix Angelicae Pubescentis extract [17].…”

Pharmacological Properties of Bergapten: Mechanistic and Therapeutic Aspects

“…Likewise, duplication of the plasma concentration was noted when comparing the samples of the group administered with the low and medium concentrations. However, the same behavior was not observed for the medium and high administrations, suggesting a saturable first-pass effect [ 9 ].…”

“…The combined anti-inflammatory and proresolution activities suggest that BP may be particularly valuable for the treatment of chronic inflammatory diseases [ 7 ]. In addition, it has also been evidenced to act as an analgesic (Teye [ 8 ]) (Teye Azietaku, 2016 #50) and anticoagulant [ 9 ] and has hepatoprotective properties [ 10 ] and anticonvulsant effects [ 11 ]. Moreover, various studies revealed that BP has inhibitory effects on 5-lipoxygenase (5-LOX), cyclooxygenase (COX), and topoisomerase 1 (Teye [ 8 , 12 ]).…”

Dietary Coumarins

“…The bioavailability and metabolism of bergapten (27), a well-known anti-inflammatory and antitumour natural furanocoumarin, was studied after oral administration (15 mg/kg) in a rat model (Yu et al 2016). The absolute oral bioavailability (F) were 80.1 AE 29.6%, 94.0 AE 40.3%, and 69.5 AE 44.2% for low, medium, and high concentrations using the formula F = (AUC oral/AUC intravenous) Â 100%, based on the AUC(0-1) obtained after i.v.…”