HPLC-MS法测定血浆中的帕罗西汀及人体内药动学研究临床药学

彭文兴 符棘玉 蒋丽丽 李焕德

中国药学杂志 ›› 2003, Vol. 38 ›› Issue (11) : 868-870.

中国药学杂志 ›› 2003, Vol. 38 ›› Issue (11) : 868-870.
临床药学

HPLC-MS法测定血浆中的帕罗西汀及人体内药动学研究临床药学

  • 彭文兴,符棘玉,蒋丽丽,李焕德
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Study on the pharmacokinetics of paroxetine hydrochloride tablets in healthy volunteers with HPLC-MS assay

  • PENG Wen-xing1,FU Ji-yu2,JIANG Li-li2,LI Huan-de1
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摘要

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(HPLCMS)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

Key words

paroxetine / HPLC-MS / pharmacokinetics

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导出引用
彭文兴 符棘玉 蒋丽丽 李焕德. HPLC-MS法测定血浆中的帕罗西汀及人体内药动学研究临床药学[J]. 中国药学杂志, 2003, 38(11): 868-870
PENG Wen-xing;FU Ji-yu;JING Li-li;LI Hun-de. Study on the pharmacokinetics of paroxetine hydrochloride tablets in healthy volunteers with HPLC-MS assay[J]. Chinese Pharmaceutical Journal, 2003, 38(11): 868-870

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 highperformance 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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