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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 investigate the pharmacokinetics of picamilone tablets in healthy volunteers. Methods The blood concentration of 12 healthy volunteers after oral administration of Picamilone tablets was determined by liquid chromatography-mass spectrometry (HPLC-MS / MS). Pharmacokinetic parameters were calculated. Results The mean time to peak tmax in single oral picamilone tablets after oral administration of 50, 100 and 200 mg was (0.73 ± 0.41), (0.67 ± 0.33) and (0.67 ± 0.31) h, respectively; t1 / 2 was 0.68 ± 0.22), (0.89 ± 0.41) and (0.91 ± 0.21) h respectively; mean ρmax were (1328.75 ± 552.33), (2460.83 ± 571.19) and (4415.00 ± 1077.45) μg · L- (1617.37 ± 575.48), (3117.08 ± 620.93) and (5987.01 ± 1365.57) μg · h · L-1, respectively. The average AUC0-∞ values were (1697.45 ± 584.78), (3227.39 ± 641.54) and (6192.36 ± 1388.59 ) μg · h · L-1. Conclusion The ρmax and AUC of plasma drug increased with the increase of dose, and there was no gender difference in the pharmacokinetics of picamilone in vivo.