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

 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，AUC_0～96，AUC_0～∞，c_max，t_max，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。

Study on the pharmacokinetics of paroxetine hydrochloride tablets in healthy volunteers with HPLC-MS assay

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，AUC0_0～96(576.2±236.0) ng·h·mL-1，AUC0_0～∞(596.8±234.5) ng·h·mL-1，c_max(26.3±9.6) ng·mL-1，t_max(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 t_1/219～23h.}