- P-ISSN 1225-0163
- E-ISSN 2288-8985
International Olympic Committee (IOC) prohibits the use of carteolol which is one of <TEX>${\beta}$</TEX>-blockers. To prove whether carteolol product was taken or not, the analytical method in urine using GC/MS was established, and metabolism and excretion study were evaluated. As compared with acid hydrolysis, enzyme hydrolysis method was more efficiency. Coefficients of variation for intra-assay precision was around 10%. Error was less than 5% except the concentration of <TEX>$0.05{\mu}g/m{\ell}$</TEX>. Recovery was 78.5% at <TEX>$2{\mu}g/m{\ell}$</TEX>. Free carteolol, conjugated carteolol, and small amount of p-OH carteolol were found in dosed human urine samples. The conjugated form was being 59.4% of the total carteolol in human urine. The amount of carteolol renal excreted for 72 h after oral dose of 10 mg of carteolol was 49% of the administred dose.