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Pharmacokinetics and pharmacodynamics of ketoprofen plasters
Author(s) -
Heo SungKoun,
Cho Jeiwon,
Cheon JiWoong,
Choi MinKoo,
Im DongSoon,
Kim Jung Ju,
Choi Yang Gyu,
Jeon Do Yong,
Chung SukJae,
Shim ChangKoo,
Kim DaeDuk
Publication year - 2008
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.587
Subject(s) - ketoprofen , chemistry , pharmacodynamics , pharmacokinetics , pharmacology , analgesic , carrageenan , hairless , chromatography , dose , permeation , medicine , biochemistry , membrane
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.