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Lingjun Li,Pengcheng Ma,Yuping Cao,Lei Tao,Yue Tao.Journal of Biomedical Research,2011,25(1):56-62
Single-dose and multiple-dose pharmacokinetics of zaltoprofen after oral administration in healthy Chinese volunteers
Received:October 26, 2010  
DOI10.1016/S1674-8301(11)60007-9
Keywordszaltoprofen, nonsteroidal anti-inflammatory drug, pharmacokinetics
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Lingjun Li Department of Pharmacology, Institute of Dermatology, Chinese Academy of Medical Sciences and Peking Union Medical College, Nanjing, Jiangsu , China
Pengcheng Ma Department of Pharmacology, Institute of Dermatology, Chinese Academy of Medical Sciences and Peking Union Medical College, Nanjing, Jiangsu , China
Yuping Cao Department of Pharmacology, Institute of Dermatology, Chinese Academy of Medical Sciences and Peking Union Medical College, Nanjing, Jiangsu , China
Lei Tao Department of Pharmacology, Institute of Dermatology, Chinese Academy of Medical Sciences and Peking Union Medical College, Nanjing, Jiangsu , China
Yue Tao Department of Pharmacology, Institute of Dermatology, Chinese Academy of Medical Sciences and Peking Union Medical College, Nanjing, Jiangsu , China
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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 pharma-cokinetics 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 zal-toprofen 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.
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