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

Xie-An Yu,Yan-Xu Chang,Mingrui An,John Teye Azietaku,Jin Li,Jia Hao,Jun He,Jun Cao

doi:10.1186/s13065-016-0212-x

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.

Highlights

Bergapten (Fig. 1), is one of coumarins found in many herbal medicines
A simple, selective, sensitive and optimised HPLC-FLD method has been developed for the quantitative determination of bergapten in rat plasma using isoimperatorin as an internal standard (IS)
The results indicated that the assay was reproducible, accurate and reliable

Summary

Introduction

Bergapten (Fig. 1), is one of coumarins found in many herbal medicines. Pharmacological studies showed that bergapten had the analgesic, anti-inflammatory, anticoagulant and anti-cancer activities [1, 2]. Bergapten has been known to counteract the proliferative effect and cause apoptosis of breast cancer cells [3]. Coumarins have been known to be interesting fluorophores, with their fluorescences changing drastically with substituents and their introduced positions [10]. In this present study, a simple, selective, sensitive and optimised HPLC-FLD method has been developed for the quantitative determination of bergapten in rat plasma using isoimperatorin as an internal standard (IS). A simple, selective, sensitive and optimised HPLC-FLD method has been developed for the quantitative determination of bergapten in rat plasma using isoimperatorin as an internal standard (IS) This analytical method has been successfully applied to

Methods

Discussion

Conclusion