Abstract: AIM To develop a sensitive, specific and accurate method for quantifying bambuterol in human plasma and to study pharmacokinetics of bambuterol in male healthy Chinese. METHODS Plasma samples were prepared based on a simple liquid liquid extraction. The extracted samples were analyzed on liquid chromatography using a Zorbax SB C₁₈ column interfaced with a triple quadrupole tandem mass spectrometer and detected by use of selected reaction monitoring mode. RESULTS The linear calibration curves were obtained in the concentration range of 0.05-4.0 ng·mL^-1. The limit of quantification was 0.05 ng·mL^-1. The intra- and inter-run precision was measured to be below 7%. The inter-run accuracy was less than 8% for the analyte. After an oral administration of 10 mg bambuterol hydrochloride to 18 healthy Chinese volunteers the main pharmacokinetic parameters of bambuterol were as follows: T_max was (2.3±1.3) h; C_max was (3.95±2.20) ng·mL^-1; T_1/2 was (11.4±6.1) h and AUC_0-t was (26.85±11.77) ng·h·mL^-1. CONCLUSION The method is shown to be accurate, robust and convenient, and suitable for pharmacokinetic studies of bambuterol. It was found that there was marked inter-individual difference in the pharmacokinetics of bambuterol in Chinese volunteers after a single oral dose, which may be attributed to the difference of activity of cholinesterase, an enzyme catalyzing bambuterol metabolism.