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A sensitive high performance liquid chromatography-mass spectrometry (HPLC-MS/MS) method was developed for the determination of repaglinide in human plasma to evaluate the bioequivalence of two repaglinide tablets.The plasma samples of repaglinide were extracted with methyl tertiary-butyl ether and separated by HPLC on a Inertsil ODS-3 column with the mobile phase consisted of 20 mmol·L-1 ammonium formate (included 0.1% formic acid)-acetonitrile (40 ∶ 60,v/v).