论文部分内容阅读
目的:探讨氟西汀及其活性代谢产物去甲氟西汀在汉族健康人体的药动学。方法:24名健康男性志愿者单剂量口服盐酸氟西汀分散片20 mg后,采用液相色谱-串联质谱法测定血浆中氟西汀和去甲氟西汀浓度,应用DAS2.0软件计算药动学参数。结果:氟西汀和去甲氟西汀在人体内药-时曲线呈一室模型。除1例慢代谢型受试者外,23名受试者主要药动学参数如下:t1/2分别为(30.8±7.6)和(130.9±42.0)h;tmax分别为(5.5±2.1)和(58.5±31.7)h;Cmax分别为(11.8±3.5)和(14.2±5.0)ng.mL-1;AUC0-t分别为(487.4±190.2)和(3370.9±1175.8)ng.h.mL-1;AUC0-∞分别为(506.5±208.8)和(3537.8±1424.1)ng.h.mL-1。结论:盐酸氟西汀分散片在人体吸收迅速,消除较慢,而其活性代谢产物去甲氟西汀消除更慢;其中1例受试者呈明显慢代谢型。
Objective: To investigate the pharmacokinetics of fluoxetine and its active metabolite norfluoxetine in healthy Han people. Methods: Twenty-four healthy male volunteers received a single oral dose of fluoxetine hydrochloride dispersible tablets (20 mg). The concentrations of fluoxetine and nifacil in plasma were determined by liquid chromatography-tandem mass spectrometry (DAS2.0) Dynamic parameters. Results: Fluoxetine and norfluoxetine in the human body drug-time curve was a model. The main pharmacokinetic parameters of 23 subjects were as follows: t1 / 2 = (30.8 ± 7.6) and (130.9 ± 42.0) h; tmax = (5.5 ± 2.1) and (58.5 ± 31.7) h and Cmax were (11.8 ± 3.5) and (14.2 ± 5.0) ng.mL-1, respectively; AUC0-t was 487.4 ± 190.2 and 3370.9 ± 1175.8 ng · mL- ; AUC0-∞ were (506.5 ± 208.8) and (3537.8 ± 1424.1) ng.h.mL-1, respectively. CONCLUSION: Fluoxetine hydrochloride dispersible tablet absorbs quickly and slowly in human body, and its active metabolite norfluoxetine is eliminated more slowly. One patient showed obvious slow metabolism.