目的研究盐酸帕罗西汀的血浆浓度测定方法及其在人体内的药动学。方法18名健康男性志愿者,单剂量口服盐酸帕罗西汀片,在设计的时间点取静脉血,血药浓度采用液相色谱质谱(HPLCMS)法测定。药动学参数采用3P97程序计算。结果单次服用40 mg盐酸帕罗西汀片后的主要药动学参数Ka,AUC0~96,AUC0~∞,cmax,tmax,CL分别为(0.89±0.28) h-1,(576.2±236.0) ng·h·mL-1,(596.8±234.5) ng·h·mL-1,(26.3±9.6) ng·mL-1,(3.89±2.1) h,(0.09±0.05) L·h-1。结论盐酸帕罗西汀片在中国人体内口服吸收缓慢,约4 h达到血药浓度峰值,平均消除半衰期为19~23 h与国外文献报道相似。
Abstract
OBJECTIVE To study the pharmacokinetics of paroxetine hydrochloride tablets in healthy volunteers with HPLC-MS. METHODS A single oral dose of 40 mg paroxetine hydrochloride was given to 18 healthy volunteers.The concentrations of paroxetine in plasma were assayed by HPLC-MS method.The pharmacokinetic parameters of paroxetine hydrochloride tablets were calculated by program 3P97. RESULTS The pharmacokinetic parameters of paroxetine hydrochloride tablets were as follows:Ka (0.89±0.28) h-1,AUC00~96(576.2±236.0) ng·h·mL-1,AUC00~∞(596.8±234.5) ng·h·mL-1,cmax(26.3±9.6) ng·mL-1,tmax(3.89±2.1) h,CL(0.09±0.05) L·h-1respectively. CONCLUSIONS Paroxetine hydrochloride tablet was absorbed slowly in healthy volunteers.Its peak blood concentration was reached at 4 h after oral administration with t1/219~23h.
关键词
盐酸帕罗西汀 /
液相色谱-质谱 /
药动学
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Key words
paroxetine /
HPLC-MS /
pharmacokinetics
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参考文献
[1]卢海儒.赛乐特[J].中国新药杂志,1997,6(4):260.
[2]Shin JG,Kim KA,Yoon YR, et al. Rapid simple highperformance liquid chromatographic determination of paroxetine in human plasma[J]. J Chromatogr B, 1998,713:452.
[3]Kaye CM, Haddok RE, Langley PF, et al. A review of the metabolism and pharmacokinetics of paroxetine in man[J]. Acta Psychiatr Scand, 80(Suppl 350):60.
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脚注
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