Abstract Objective: The aim of study was to develop a highly selective LC-MS/MS method using a tandem quadrupole mass spectrometer detector for rapid screening, identification and quantification of 12 antidiabetic agents added in the traditional Chinese medicine preparations. Methods: Glipizide, gliclazide, glyburide, glimepiride, gliquidone, repaglinide, nateglinide, pioglitazone, rosiglitazone, metformin, phenformin and tolbutamide added in the blank ground samples were extracted with 80% methanol and were separated from an ACQUITY UPLC DBH C18 column with a gradient mobile phase of acetonitrile (B) - 0.2 % formic acid water solution (A). A tandem quadrupole mass spectrometer equipped with electrospray ionization source was used in positive ion mode, multiple reaction monitoring (MRM) was performed to quantify above mentioned compounds. Results: Eleven linear calibration curves were obtained in the concentration range of 0.0025 - 0.5 μg﹒mL-1 with r≥0.9959 except that metformin calibration curve were narrow range. Accuracy and recovery were determined at three concentration (0.005, 0.01, 5.0 mg﹒g-1), RSD（n=6）was 1.7 - 11.4 % in accuracy and 93.2 - 109.7 % in recovery. The lowest limits of quantification (LLOQ) were defined as the lowest concentration giving the signal-to-noise ≥10:1, the data were from 0.005 μg﹒g-1 to 0.2 μg﹒g-1. Conclusion: The results indicate that the method can be used in quantificational measure of antidiabetic agents added in traditional Chinese medicine preparations.
