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目的评价阿莫曲坦在中国健康志愿者中的单次给药药动学特征。方法采用随机开放双交叉试验设计,12例健康受试者(男女各半)在空腹状态下分别单次口服阿莫曲坦片12.5 mg或25 mg。以高效液相色谱-串联质谱(HPLC-MS/MS)法测定血浆中阿莫曲坦的浓度,采用Win Nonlin软件计算药动学参数。结果单次给药(12.5、25 mg)后阿莫曲坦的主要药动学参数:t_(1/2)分别为(3.85±1.38)和(4.18±2.62)h;t_(max)分别为(2.04±0.09)和(2.33±1.39)h;ρ_(max)分别为(28.98±6.09)和(53.80±14.99)μg·L~(-1);AUC0-t分别为(196.1±52.5)和(390.2±78.9)μg·h·L~(-1);AUC_(0-∞)分别为(229.6±66.3)和(427.1±75.3)μg·h·L~(-1)。结论本研究建立的HPLC-MS/MS法准确快速,灵敏度高,专属性强,适用于临床试验中阿莫曲坦血药浓度测定;单次给药(12.5、25 mg)后,阿莫曲坦的体内过程符合一级线性动力学过程。
Objective To evaluate the single-dose pharmacokinetic profile of almotriptan in Chinese healthy volunteers. Methods A randomized open double-crossover trial was designed. Twelve healthy subjects (half-males and half-females) received 12.5 mg or 25 mg almotriptan tablets in a single oral dose, respectively. The concentration of almotriptan in plasma was determined by HPLC-MS / MS, and the pharmacokinetic parameters were calculated by Win Nonlin software. Results The main pharmacokinetic parameters of almotriptan after single administration (12.5 and 25 mg) were: t 1/2 (3.85 ± 1.38) and (4.18 ± 2.62) h, respectively; t max was (2.04 ± 0.09) and (2.33 ± 1.39) h respectively; ρ max was (28.98 ± 6.09) and (53.80 ± 14.99) μg · L -1; AUC0-t was (390.2 ± 78.9) μg · h · L -1; AUC_ (0-∞) were (229.6 ± 66.3) and (427.1 ± 75.3) μg · h · L -1, respectively. Conclusion The HPLC-MS / MS method established in this study is accurate, rapid, sensitive and specific. It is suitable for the determination of almotriptan in clinical trials. After a single dose of 12.5,25 mg, The in vivo process conforms to the first order linear kinetic process.