Abstract: Aim To establish a new and sensitive HPLC-MS method for the determination of zolmitriptan in human plasma and study the pharmacokinetics of zolmitriptan in healthy volunteers. Methods A single oral dose of 5 mg of zolmitriptan tablet was given to 20 healthy male volunteers. After dosing, blood samples were collected for a period of 24 h, and zolmitriptan concentration in plasma was analyzed by HPLC-MS. Results The plasma concentration-time course fitted well a two-compartment open model with a lag time, giving the following pharmacokinetic parameters: Tmax 1.60±0.24 h, Cmax 9.73±1.43 ng·mL^-1, T1/2α1.72±0.46 h, T1/2β 4.52±0.97 h and AUC0-t 55.59±5.12 ng·mL^-1·h. Conclusion The improved analytical method for zolmitriptan is rapid,sensitive and suitable for application to pharmacokinetic studies and routine determination of numerous samples.

Key words: zolmitriptan, zolmitriptan, pharmacokinetics, pharmacokinetics, HPLC-MS, HPLC-MS