Pharmacokinetics and Bioequivalence Evaluation of Piracetam Tablet: A Randomized, Single-Dose, Two-Period, Crossover Study in Healthy Chinese Participants Under Fasting and Fed Conditions.

BACKGROUND

Piracetam, a nootropic drug, is widely used for treating cognitive impairments. However, pharmacokinetic and bioequivalence data for piracetam formulations in the Chinese population are limited. This study was conducted to evaluate the pharmacokinetics and bioequivalence of a newly developed generic piracetam tablet compared with the reference product (Nootropyl®) in healthy Chinese participants under fasting and fed conditions.

METHODS

A randomized, open-label, single-dose, two-period, two-sequence crossover study was conducted in healthy Chinese participants under fasting and fed conditions. Healthy participants received a single oral dose of piracetam 800 mg as either the test or reference formulation, followed by a 7-day washout period. Plasma piracetam concentrations were determined using a validated high-performance liquid chromatography-tandem mass spectrometry method. Pharmacokinetic parameters, including maximum plasma concentration (Cmax), area under the plasma concentration-time curve from time zero to the last measurable concentration (AUC0-t), and area under the plasma concentration-time curve extrapolated to infinity (AUC0-∞), were calculated using non-compartmental analysis. Bioequivalence was assessed by calculating the 90% confidence intervals (CIs) of the geometric mean ratios (GMRs) for Cmax, AUC0-t, and AUC0-∞.

RESULTS

56 participants were enrolled, with 28 participants completing each study under fasting and fed conditions. Under fasting conditions, the 90% confidence intervals (CIs) of the GMRs for Cmax, AUC0-t, and AUC0-∞ were 98.53%, 98.40%, and 98.49%, respectively. Under fed conditions, the corresponding 90% CIs were 99.31%, 99.03%, and 99.01%. All values were within the predefined bioequivalence acceptance range of 80-125%. Food intake reduced the rate of absorption, as indicated by a lower Cmax and delayed time to maximum concentration (Tmax), without affecting the extent of absorption. Both formulations were well tolerated, and no serious adverse events were reported.

CONCLUSIONS

The test piracetam tablet was demonstrated to be bioequivalent to the reference formulation with respect to the rate and extent of absorption under both fasting and fed conditions in healthy Chinese participants. The comparable safety and tolerability profiles support the clinical interchangeability of the generic and reference piracetam formulations.

CLINICAL TRIAL REGISTRATION: CTR20213027.