Pharmacokinetics and Bioequivalence Study of Aniracetam after Single-dose Administration in Healthy Chinese Male Volunteers

Abstract

The pharmacokinetics of aniracetam (CAS 72432-10-1) in Chinese healthy male volunteers was investigated for the first time. Twenty male volunteers were enrolled into this open, randomized, single blind two-sequence, two-period crossover study. Under fasting conditions, each subject received a single oral dose of 400 mg (2 × 200 mg/capsule) aniracetam as a test or reference formulation with a 3-day washout period between the two preparations. The plasma concentrations of aniracetam were analyzed by a sensitive liquid chromatography - tandem mass spectrometry (LC-MS/MS) method. The pharmacokinetic parameters of the test and reference formulations were estimated as follows: The maximum plasma concentrations (C_max) were 8.75 ± 7.82 and 8.65 ± 8.70 ng/mL, T_max were 0.4 ± 0.1 and 0.4 ± 0.1 h, and plasma elimination half-lives (t_1/2) were 0.47 ± 0.16 and 0.49 ± 0.24 h, respectively. The AUC_0–t values demonstrated nearly identical bioavailability of aniracetam from the examined formulations. AUC_0–2.5 values were 4.53 ± 6.62 and 4.76 ± 6.65 ng h/mL, the areas under the plasma concentration-time curve (AUC_0–∞) were 4.62 ± 6.66 and 4.85 ± 6.71 ng h/mL for the test and reference formulation, respectively. No statistical differences were observed for C_max and AUC_0–∞ for aniracetam. The 90% confidence limits calculated for AUC and C_max of aniracetam were within the standard bioequivalence range (80%-125% for AUC and C_max). Therefore, the aniracetam test formulation can be regarded as bioequivalent to the aniracetam reference formulation.

Key words

Aniracetam, bioequivalence, pharmacokinetics - CAS 72432-10-1 - Cognition enhancers

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