匹卡米隆片在健康人体的药动学研究

 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。

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.