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 200 mg 后的实测平均达峰时间 <> t _max 分别为 (0.73 ± 0.41) ， (0.67 ± 0.33) 和 (0.67 ± 0.31)h ； <> t _1/2 分别为 (0.68 ± 0.22) ， (0.89 ± 0.41) 和 (0.91 ± 0.21)h ；平均 <> ρ _max 分别为 (1 328.75 ± 552.33) ， (2 460.83 ± 571.19) 和 (4 415.00 ± 1 077.45)μg·L^{- 1} ； AUC _{0 -t<>n} 平均值分别为 (1 617.37 ± 575.48) ， (3 117.08 ± 620.93) 和 (5 987.01 ± 1 365.57)μg·h·L^{- 1} ； AUC _{0 - ￥} 平均值分别为 (1 697.45 ± 584.78) ， (3 227.39 ± 641.54) 和 (6 192.36 ± 1 388.59)μg·h·L^{- 1} 。 结论 血浆药物的 <> ρ _max 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-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.