Bioequivalence Trial of Two Piracetam 800 Mg ImmediateRelease Oral Tablets in Mexicans: Insights in the Use and Abuse of Nootropics

Abstract

Objective: To share pharmacokinetic data and a bio-analytical method for the conduction of a bioequivalence trial of Piracetam 800-mg immediate release tablets in Mexicans. Methods: Twelve male and 18 female healthy volunteers were administered with a single oral dose of one 800-mg Piracetam tablet under fasting conditions, in a cross-over design study, with blood sampling up to 24 h post-dose. Piracetam was measured by tandem Mass Spectrometry coupled to Ultra-Performance Liquid Chromatography (UPLC-MS/MS) using metronidazole as internal standard. Logarithmic ratios of maximal plasma concentration (Cmax ) and Area Under the Curve (AUC) were used to establish 90% Confidence Intervals [CI] for bioequivalence. Results: Both formulations (Nootropil™ as reference product, and PIRACETAM generic formulation as test product) were safe and well tolerated. The analytical method proved to be linear with accuracy and precision within a range of 1-60 µg/mL; 90% CI for and were [82.62–94.68] and [95.22–102.06]. Cmax was reached at approximately 1 h, and plasma elimination half-life (t1/2) was around 5.1 h for both products. Conclusion: Assayed products met the criteria established by the Mexican regulatory agency (COFEPRIS) to be declared bioequivalent. Mexican population appears to be a high absorber of Piracetam, exhibiting a 300% higher and an ABC0-inf 60% greater than other populations previously reported.