Theexcretionofurinaryandplasmametabolitesofsalbutamolwasstudiedusingultrahigh performance liquid chromatography electrospray time-of-flight mass spectrometry, after a single intragastric gavaged dose administration with salbutamol. The software of Agilent MassHunter Metabolite ID was employed to find and identify the chemical structure of metabolites of salbutamol. Five metabolites from salbutamol were identified. Metabolites identified in swine urine included glucuronide conjugate salbutamol, N-oxide-salbutamol, hydroxyl-salbutamol, methoxyl-salbutamol and dehydrated hydroxyl-salbutamol. Whereas, only the parent drug, glucuronide conjugate salbutamol and dehydrated hydroxyl-salbutamol were observed in swine plasma.