Study on bioequivalence of beraprost in healthy volunteers by liquid chromatography with tandem mass spectrometry

Abstract

Beraprost sodium is an oral prostacyclin analog that was first approved in 1992 (Japan) for the treatment of peripheral vascular disorders. It is administered orally as a tablet available in strength 20 μg. In this paper, we described a liquid chromatography tandem mass spectrometry method that was developed for the quantification of beraprost in human plasma with high sensitivity at picogram per milliliter concentration. The method had been validated in terms of selectivity, sensitivity, accuracy and precision, matrix effect, linearity, recovery and carry-over according to the Guideline on Bioanalytical Validation from the European Medicines Agency. The standard calibration curve for beraprost was 9.5-1419 pg/mL. This method has been applied successfully to a bioequivalence study with 60 μg of beraprost (three tablets) in 29 healthy volunteers.The results showed that the two formulations of beraprost are bioequivalent.

What is the role of current mass spectrometry in pharmaceutical analysis?

“…The highly sensitive detection has been recently demonstrated by UHPLC/HPLC‐QqQ methods used for the bioequivalence study of dabigatran, which is the active metabolite of the prodrug dabigatran etexilate mesylate (Abd Allah et al, 2022), triamterene and hydrochlorothiazide (Margaryan et al, 2019), sumatriptan (Wichitnithad et al, 2020), and beraprost sodium (Prasaja et al, 2019). MS is also needed when the API does not contain chromophores for UV‐VIS detection, for example, bioequivalence study of isosorbide‐5‐mononitrate (Zhou et al, 2020) or the total amount of the drug in plasma and the unbound fractions are required, for example, bioequivalence study of paclitaxel protein‐bound particles for injectable suspension (Li et al, 2019).…”