title: Pharmacokinetics and pharmacodynamics of ketoprofen plasters.
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 x 3 cm(2) plaster. AUC(0-24h) and C(max) of Ketotop-P were 260.92 microg.h/ml and 25.09 microg/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 x 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.
authors.affiliation: College of Pharmacy, Pusan National University, Busan 609-735, Korea.
authors.forename: Sung-Koun
authors.initials: SK
authors.lastname: Heo
authors.forename: Jeiwon
authors.initials: J
authors.lastname: Cho
authors.forename: Ji-Woong
authors.initials: JW
authors.lastname: Cheon
authors.forename: Min-Koo
authors.initials: MK
authors.lastname: Choi
authors.forename: Dong-Soon
authors.initials: DS
authors.lastname: Im
authors.forename: Jung Ju
authors.initials: JJ
authors.lastname: Kim
authors.forename: Yang Gyu
authors.initials: YG
authors.lastname: Choi
authors.forename: Do Yong
authors.initials: DY
authors.lastname: Jeon
authors.forename: Suk-Jae
authors.initials: SJ
authors.lastname: Chung
authors.forename: Chang-Koo
authors.initials: CK
authors.lastname: Shim
authors.forename: Dae-Duk
authors.initials: DD
authors.lastname: Kim
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000269:Adhesives / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D019540:Area Under Curve; D002351:Carrageenan; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D006614:Hindlimb / Q000378:metabolism; D006358:Hot Temperature / Q000009:adverse effects; D066298:In Vitro Techniques; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control; D007660:Ketoprofen / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D008657:Metabolic Clearance Rate; D051379:Mice; D008812:Mice, Hairless; D010147:Pain Measurement / Q000379:methods; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption
chemical_list: D000180:Acrylic Resins; D000269:Adhesives; D000894:Anti-Inflammatory Agents, Non-Steroidal; D002351:Carrageenan; D007660:Ketoprofen