Abstract: | Ondansetron, a 5‐hydroxytryptamine type 3 (5‐HT3) receptor antagonist, is regarded as an excellent candidate to treat chemotherapy‐ and radiotherapy‐induced nausea and vomiting. To better understand the metabolic profiles of ondansetron in human urine, the metabolites were analyzed using liquid chromatography/mass spectrometry (LC/MSn). Urine samples were collected after oral administration of 8 mg ondansetron to healthy volunteers. Then samples were treated by solid‐phase extraction and detected with LC/MSn. Besides ondansetron, in human urine, a total of 19 metabolites including 13 new metabolites were detected and identified via comparing the retention time and product ion spectra with those of reference standards isolated and characterized. The results showed that ondansetron was metabolized via hydroxylation, glucuronidation, sulfation and minor N‐demethylation in human. LC/MSn was demonstrated to be useful and sensitive in the metabolic study of ondansetron. |