Riluzole is an anti-cytokine agent that has several mechanisms of action that affect glutamate neurotransmission. The objective of this work is to obtain the pharmacokinetic parameters necessary for the comparison between the two formulations of Riluzole 50 mg tablet. The study was an open, randomized, two-period, two-group crossover trial (2 × 2). Fifty healthy volunteers of both sexes participated in the study. For the determination of the drug in human plasma, a previously validated analytical method was used with Riluzole-13C,15N2 as an internal standard. The analyte and internal standard were extracted from the human plasma by liquid-liquid extraction and subsequently analyzed by ultra performance liquid chromatography coupled to mass spectrometry (UHPLC-MS/MS), and the linearity range of the method for Riluzole was 2-500 ng/mL and the lowest quantification for Riluzole was 2 ng/mL. The geometric mean values of the parameters Cmax, ASC0-t and ASC0-inf transformed into natural logarithmic were found to be between 80% and 125%, according to the Brazilian legislation; in this way the test formulation was bioequivalent to the formulation available in the market.
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