Pharmacokinetics of Picamilon Tablet in Healthy Volunteers

OBJECTIVE To study the pharmacokinetics of picamilon tablet in 12 healthy volunteers. METHODS Picamilon tablets were administrated to healthy volunteers,and plasma concentrations were determined by LC-MS. The pharmacokinetic parameters were calculated. RESULTS The oral dose of 50,100 and 200 mg were administrated to volunteers. The pharmacokineitc parameters were as follows:tmax (0.73±0.41),(0.67±0.33) and (0.67±0.31)h,t1/2 (0.68±0.22),(0.89±0.41) and (0.91±0.21)h,ρmax (1 328.75±552.33),(2 460.83±571.19) and (4 415.00±1 077.45) μg·L-1,AUC0-tn (1 617.37±575.48),(3 117.08±620.93) and (5 987.01±1 365.57) μg·h·L-1,AUC0-∞ (1 697.45±584.78),(3 227.39±641.54) and (6 192.36±1 388.59) μg·h·L-1,respectively. The plasma concentration-time curves were described by a two compartment open model. CONCLUSION AUC and ρmax could be increased with the increased dose. No gender effect on pharmacokinetic parameters was found.