Abstract: AIM: To study the phamnacokinetics of Tegaserod Hydrogen Maleate Tablet in healthy Chinese volunteens, METHODS: The volunteers received a single 6, 12 or 18 mg dose of tegaserod orally, respectively. Te-gasenxl in plasma was detemined by LC-MS.RE-SULTS: The pharmacok inetics of tegaserod confomed toa 2-compartment open moolel after single oral dose (6, 12 and 18 mg). The t_max was (2.2±1.0), (1.3±0.5),(1.3±0.4) h; C_max (3.4±0.4), (8.5±1.4),(12.0±2.4) ng/mL; $t_{\frac{1}{2}α}$ was (5.5 ±6.4), (4.6 ±5.6), (2.0±2.0) h; $t_{\frac{1}{2}β}$ was(16.2±2.4), (15.2±1.8), (14.9±2.0) h; $AUC_{0→48}$ was (53±9), (96±29), (135±54) ng·h·mL^-1; $AUC_{0→∞}$ was (64±12),(108±33), (158±60) ng·h·mL^-1; MRT was (16.3±l.0), (14.8±1.1), (14.6±0.7) h. The C_max、$AUC_{0→48}$ and $AUC_{0→∞}$ were orelated linearly with dosage within 6-18 mg. The satistical unalysis indicated that the t_max, $t_{\frac{1}{2}α}$, $t_{\frac{1}{2}β}$ and MRT had no significant differences among different groups.'The plasma concentration of tegaserod reached steady state after successive adminis-trationof 3 days, and the t_max 、C_ss,max、C_ss,min 、C_ss,avg、,DF were(1.5±0.4) h, (8.1 ± 1.3), (2.6±0.7),(4.4±10.8) ng/mL, (126±16) % respectively. The C_max、$AUC_{0→48}$、$AUC_{0→∞}$ and $t_{\frac{1}{2}β}$ were apparently more than those reported in other population. CONCLUSION: The phamnacokinetics of tegaserod hydrogen maleate tabletin healthy chinese volunteers can he described by a two compartment model and has a linear dlynamics character within the range of 6-18 mg.

Key words: tegaserd, phannack ineticos, liquidchromalographymass spectrometry