醋氨酚在6例健康志愿者的药代动力学研究

中国临床药理学与治疗学 ›› 2001, Vol. 6 ›› Issue (2): 126-128.

醋氨酚在6例健康志愿者的药代动力学研究

徐斌, 贺平, 陶勇, 许平波, 张国友

第二军医大学东方肝胆外科研究所, 上海 200435

收稿日期:2000-01-19 修回日期:2001-03-08 出版日期:2001-04-26 发布日期:2020-11-25
作者简介:徐斌, 男, 实习研究员。贺平, 男, 42 岁, 博士, 副研究员

Study on the pharmacokinetics of acetaminophen in six healthy volunteers

XU Bin, HE Ping¹, TAO Yong, XU Ping-Bo, ZHANG Guo-You

¹Eastern Institute of Hepatobiliary Surgery, Second Military Medical University, Shanghai 200433

Received:2000-01-19 Revised:2001-03-08 Online:2001-04-26 Published:2020-11-25

摘要/Abstract

摘要： 目的研究结合代谢模型药物醋氨酚(acetaminophen, Ace) 在健康人的药代动力学及其尿液中代谢产物的累积排泄量。方法 6 例健康志愿者空腹口服醋氨酚1.0 g 后, 定时收集唾液及24 h 尿液。采用高效液相色谱法(HPLC), 测定Ace、葡萄糖醛酸-Ace (GA) 和硫酸-Ace (SA) 含量。结果唾液Ace t_1/2 为(2.50 ±0.29) h, CL 为(10.3 ±1.6) L ·h^-1, k 为0.28 ±0.03, AUC 为(98.9 ±16.7) μg·h·ml^-1, V_d 为(44.4 ±16.5) L; 24 h尿液中Ace、GA、SA 的含量及三者累积排泄量分别占给药量的(3.4 ±0.7) %、(37.5 ±10.2) %、(24.5 ±15.5) % 和(70.4 ±7.7) %。结论与国外同类报道比较, Ace t_1/2延长25 %, GA 累积排泄量仅占其50 %。提示肝脏葡萄糖醛酸结合代谢能力低下可能是引起Ace t_1/2延长的主要原因之一。

关键词: 醋氨酚, 葡萄糖醛酸醋氨酚, 硫酸醋氨酚, 高效液相色谱法, 药代动力学

Abstract: Aim To study the pharmacokinetics of acetaminophen (Ace) in healthy volunteers and total recovery of its metabolites in urine. Methods 1.0 g Ace was administrated o rally in 6 fasted healthy males; saliva and 24 h urine were collected regularly for the determination of Ace, glucuronide-Ace (GA) and sulfate-Ace (SA) levels by using HPLC. Results Ace in saliva showed that t_1/2 was (2.50 ± 0.29) h, CL was (10.3 ±1.6) L·h^-1, k was (0.28 ±0.03), AUC was (98.9 ±16.7) μg·h·ml^-1, V_d was (44.4 ±16.5) L; GA and SA in 24 h urine and in total recovery were (3.4 ±0.7) %, (37.5 ± 10.2) %, (24.5 ±15.5) % and (70.4 ±7.7) % respectively. Conclusions Compared with those reported by researchers in western countries, t_1/2 of Ace prolonged 25 % and total elimination was only 50 % of theirs. It seemed that low hepatic glucuronide metabolism might be an important facto r for prolongation of t_1/2 of Ace.

Key words: acetaminaphen, glucuronide-Ace, sulfate-Ace, HPLC, pharmacokinetics

中图分类号:

R969.1

徐斌, 贺平, 陶勇, 许平波, 张国友. 醋氨酚在6例健康志愿者的药代动力学研究[J]. 中国临床药理学与治疗学, 2001, 6(2): 126-128.

XU Bin, HE Ping, TAO Yong, XU Ping-Bo, ZHANG Guo-You. Study on the pharmacokinetics of acetaminophen in six healthy volunteers[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2001, 6(2): 126-128.

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