Study on clinical pharmacokinetics of tegaserod hydrogen maleate tablet in healthy Chinese volunteers by LC-MS

AIM:To study the pharmacokineties of Te- gaserod Hydrogen Maleate Tablet in healthy Chinese vol- unteers.METHODS:The volunteers received a single 6,12 or 18 mg dose of tegaserod orally,respectively.Te- gaserod in plasma was determined by LC-MS.RE- SULTS:The pharmacokinetics of tegaserod conformed to a 2-compartment open model after single oral dose(6,12 and 18 nag).The t_(max)was(2.2±1.0),(1.3±0.5), (1.3±0.4)h;C_(max)was(3.4±0.4),(8.5±1.4), (12.0±2.4)ng/mL;t1/2αwas(5.5±6.4),(4.6±5.6),(2.0±2.0)h;t1/2βwas(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);MRTwas(16.3±1.0),(14.8±1.1),(14.6±0.7)h.The C_(max) AUC_(0→48)and AUC_(0→∞)were correlated linearly with dos- age within 6-18 mg.The statistical analysis indicated that the t_(max),t1/2α,t1/2βand MRT had no significant dif- ferences among different groups.The plasma concentration of tegaserod reached steadv state after successive adminis- tration of 3 clays,and the t_(max),C_(ss,max),C_(ss,max),C_(ss,max), DF were(1.5±0.4)h,(8.1±1.3),(2.6±0.7), (4.4±0.8)ng/mL,(126±16)% respectively.The C_(max),AUC_(0→48),AUC_(0→∞)and t1/2βwere apparently more than those reported in other population.CONCLUSION: The pharmacokinetics of tegaserod hydrogen maleate tablet in healthy chinese volunteers can be described by a two compartment model and has a linear dynamics character within the range of 6-18 mg.