Fed and Fasting Bioequivalence Study for Two Formulations of Bosentan 125 Mg Tablets in Healthy Colombian People

Abstract

This is a pharmacokinetic study of two formulations containing Bosentan 125 mg, in order to compare the bioavailability between the Test product (Bosentan produced by Tecnoquímicas S.A. laboratory, Colombia) and the Reference product (Tracleer® produced by Actelion Pharmaceuticals) in fasting and fed conditions, in order to state the bioequivalence between them. With this purpose, an open label, four periods, two randomized sequences, crossover, with single pre- and fed 125 mg dose study was performed in 30 healthy volunteers, with an 8-day washout period between each period and a collection of 14 plasma samples between 0 and 24 hours. Identification and evaluation of Bosentan in plasma was carried out by ultra-high-performance liquid chromatography-tandem mass spectrometry UHPLC/MS/MS as analytical method. Based on the European and FDA bioequivalence research guidelines, the Confidence Interval (CI) falls within the allowed ranges for the Bioequivalence and Interchangeability Statement of the Tecnoquímicas S.A. product with the Reference product. Both formulations had similar pharmacokinetic parameters in each studied condition, fed and fasted. Moreover, an increase in the amount of active pharmaceutical ingredient is evident in fed conditions.