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After oral administration of aniracetam to humans, aniracetam is mainly (ca.70%) biotransformed into 4-p-anisamidobutyric acid (ABA).Therefore, it is essential to develop a specific, sensitive and rapid method for the determination of ABA in human plasma to characterize the pharmacokinetic profile of aniracetam.A selective, sensitive and rapid high performance liquid chromatography-tandem mass spectrometric (HPLC-MS/MS) method was developed and validated for the determination of ABA in human plasma using lisinopril as internal standard (IS).