匹卡米隆片在健康人体的药动学研究

Pharmacokinetics of Picamilon Tablet in Healthy Volunteers

目的探讨匹卡米隆片在健康人体的药动学。方法采用液-质联用法测定12名健康志愿者口服匹卡米隆片后的血药浓度,计算药动学参数。结果受试者单次口服匹卡米隆片50,100和200mg后的实测平均达峰时间tmax分别为(0.73±0.41),(0.67±0.33)和(0.67±0.31)h;t1/2分别为(0.68±0.22),(0.89±0.41)和(0.91±0.21)h;平均ρmax分别为(1328.75±552.33),(2460.83±571.19)和(4415.00±1077.45)μg·L-1;AUC0-tn平均值分别为(1617.37±575.48),(3117.08±620.93)和(5987.01±1365.57)μg·h·L-1;AUC0-∞平均值分别为(1697.45±584.78),(3227.39±641.54)和(6192.36±1388.59)μg·h·L-1。结论血浆药物的ρmax和AUC随剂量的增大而增加,匹卡米隆的体内药代过程无性别差异。

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^-1AUC0-tn （1 617.37±575.48）,（3 117.08±620.93） and （5 987.01±1 365.57） μg·h·L^-1AUC0-∞ （1 697.45±584.78）,（3 227.39±641.54） and （6 192.36±1 388.59） μg·h·L^-1respectively. 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.