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扎托洛芬在中国健康志愿者口服给药后的单剂量和多剂量药代动力学

Single-dose and multiple-dose pharmacokinetics of zaltoprofen after oral administration in healthy Chinese volunteers.

作者信息

Li Lingjun, Ma Pengcheng, Cao Yuping, Tao Lei, Tao Yue

机构信息

Department of Pharmacology, Institute of Dermatology, Chinese Academy of Medical Sciences and Peking Union Medical College, Nanjing, Jiangsu 210042, China.

出版信息

J Biomed Res. 2011 Jan;25(1):56-62. doi: 10.1016/S1674-8301(11)60007-9.

Abstract

Zaltoprofen, a propionic acid derivative of non-steroidal anti-inflammatory drugs, has strong inhibitory effects on actue and chronic inflammation. A randomized, dose-escalating study was conducted to evaluate the pharmacokinetics of single and multiple oral doses of zaltoprofen in 12 healthy Chinese volunteers. Pharmacokinetics was determined from serial blood samples obtained up to 24 h after administration of a single dose of zaltoprofen at 80, 160 or 240 mg and after multiple doses of zaltqorofen at 80 mg 3 times daily. The Cmax and AUC0-24 of zaltoprofen were found to be proportional to drug dose. Zaltoprofen was rapidly absorbed (tmax =1.46±0.83 h) and cleared (t1/2 =4.96±2.97 h). Pharmacokinetic parameters after multiple doses were similar to those after single doses. Zaltoprofen was well tolerated. These results support a tid regimen of zaltoprofen for the management of acute and chronic inflammation.

摘要

扎托洛芬是一种非甾体抗炎药的丙酸衍生物,对急性和慢性炎症具有强烈的抑制作用。一项随机、剂量递增研究在12名健康中国志愿者中开展,以评估单次和多次口服扎托洛芬的药代动力学。在单次服用80、160或240mg扎托洛芬后以及多次每日3次服用80mg扎托洛芬后,通过采集给药后长达24小时的系列血样来测定药代动力学。发现扎托洛芬的Cmax和AUC0-24与药物剂量成正比。扎托洛芬吸收迅速(tmax =1.46±0.83小时)且清除较快(t1/2 =4.96±2.97小时)。多次给药后的药代动力学参数与单次给药后相似。扎托洛芬耐受性良好。这些结果支持采用扎托洛芬每日3次的给药方案来治疗急慢性炎症。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6200/3596677/f4c7507379ef/jbr-25-01-056-g001.jpg

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