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正常人口服氨酚待因片的扑热息痛药代动力学研究

A PHARMACOKINETIC STUDY ON ACETAMINOPHEN IN HEALTHY VOLUNTEERS BEING GIVEN ORAL ACETAMINOPHEN-CODEINE-PHOSPHATE TABLET

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【作者】 王文铃许光炘刘静雯蔡志基

【Author】 WANG Wen-Ling, XU Guang-Xin;LIU Jing-Wen;CAI Zhi-ji Institute of Clinical Pharmacology, Beijing Medical University, Beijing

【机构】 北京医科大学临床药理研究所北京医科大学临床药理研究所 北京北京北京

【摘要】 采用HPLC测定人血浆和尿标本中扑热息痛浓度的方法学研究表明,该法分离度、灵敏度、精密度和线性关系均良好,适用于药代动力学研究。正常人口服两片氨酚待因的扑热息痛药代动力学符合二室开放式模型;动力学方程为Ct=12.74e-0.2760t-tL +106.39e-1.6201t-tL—119.08e-2.9125t-tL。口服后扑热息痛吸收较快,达峰浓度时间为0.78±0.32小时(0.43—1.31小时)。峰血浆浓度为18.04±7.71mg/1(12.86—31.73mg/l)。消除半衰期为2.62±0.61小时(1.90—3.54小时)。给药后24小时尿中排出的原型扑热息痛为给药剂量的3.3%。肾清除率和非肾清除率分别为0.59±0.19L/h(0.37—0.87L/h)和17.97±3.81L/h(13.45—21.99L/h)。

【Abstract】 The concentrations of acetaminophen in human body fluids were determined by high-performance liquid chromatography, and thepharmacokinetics of acetaminophen in normal volunteers after oral doseof 2 tablets of acetaminophen-codeine phosphate (500 mg+4 8. 4 mg/tablet)was studied. The results showed that the pharmacokinetics of acetamino-phen in the healthy fitted a two-compartment open model with an equa-tion:Ct=12. 74e-0. 2760(t-t1+106. 39e-1.6201(t-t1-119.08e<sub>-2.8125(t-t1)The average elimination half-life was 2. 62±0. 61 hrs, and the averagepeak concentration of acetaminophen in plasma, 18.04±7. 71 mg/l at 0. 78±0. 32 hours after administration. The recovery in urine during 24hour period after administration was 3. 3% of the dose, and the renalclearance and the non-renal clearance, 0. 59±0. 19 l/h and 18. 61±3. 81 l/h,respectively.

  • 【文献出处】 中国临床药理学杂志 ,The Chinese Journal of Clinical Pharmacology , 编辑部邮箱 ,1987年04期
  • 【被引频次】7
  • 【下载频次】117
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