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Pharmacokinetics and pharmacodynamics of ketoprofen plasters

2007; Wiley; Volume: 29; Issue: 1 Linguagem: Inglês

10.1002/bdd.587

1099-081X

Sung‐Koun Heo, Jeiwon Cho, Ji‐Woong Cheon, Min‐Koo Choi, Dong‐Soon Im, Jung Ju Kim, Yang Gyu Choi, Do Yong Jeon, Suk‐Jae Chung, Chang‐Koo Shim, Dae‐Duk Kim,

Pain Mechanisms and Treatments

Abstract Ketoprofen plasters of 70 cm 2 size using DuroTak ® acrylic adhesive polymers were developed either containing 30 mg (Ketotop‐L) or 60 mg drug (Ketotop‐P). The in vitro skin permeation profile was obtained in hairless mouse skin and showed the permeation rate of Ketotop‐P to be twice that of Ketotop‐L. The plasma concentration profile of ketoprofen was determined in Sprague‐Dawley rats after applying a 3 × 3 cm 2 plaster. AUC 0−24h and C max of Ketotop‐P were 260.92 µg·h/ml and 25.09 µg/ml, respectively, which were about twice the values of Ketotop‐L. The hind paw edema induced by carrageenan injection was measured for 6 h after applying a 2 × 2 cm 2 plaster, and the area under the time‐response curve ( AUR ) value was significantly lower in Ketotop‐P attached rats (180.70%·h) than in those with the Ketotop‐L (298.65%·h) and the control (407.04%·h) groups, indicating a stronger anti‐inflammatory action of Ketotop‐P. However, the analgesic effect of the two formulations did not show a statistically significant difference. In conclusion, Ketotop‐P was able to achieve higher plasma concentration of ketoprofen, thereby exhibiting higher and more constant anti‐inflammatory effect compared with Ketotop‐L. Copyright © 2007 John Wiley & Sons, Ltd.