Pharmacokinetics and pharmacodynamics of ketoprofen plasters

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

doi:10.1002/bdd.587

Pharmacokinetics and pharmacodynamics of ketoprofen plasters

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

Divison of Brain & Cognitive Sciences

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

Ketoprofen plasters of 70 cm² 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 cm² 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 cm² 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.

Original language	English
Pages (from-to)	37-44
Number of pages	8
Journal	Biopharmaceutics and Drug Disposition
Volume	29
Issue number	1
DOIs	https://doi.org/10.1002/bdd.587
State	Published - Jan 2008

Keywords

Analgesic
Anti-inflammation
Ketoprofen
Pharmacodynamics
Pharmacokinetics
Plaster

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10.1002/bdd.587

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@article{558d91e554e04e74bdcd5145950b136e,

title = "Pharmacokinetics and pharmacodynamics of ketoprofen plasters",

abstract = "Ketoprofen plasters of 70 cm2 size using DuroTak{\textregistered} 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 cm2 plaster. AUC0-24h and Cmax 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 cm2 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.",

keywords = "Analgesic, Anti-inflammation, Ketoprofen, Pharmacodynamics, Pharmacokinetics, Plaster",

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

year = "2008",

month = jan,

doi = "10.1002/bdd.587",

language = "English",

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journal = "Biopharmaceutics and Drug Disposition",

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T1 - Pharmacokinetics and pharmacodynamics of ketoprofen plasters

AU - Heo, Sung Koun

AU - Cho, Jeiwon

AU - Cheon, Ji Woong

AU - Choi, Min Koo

AU - Im, Dong Soon

AU - Kim, Jung Ju

AU - Choi, Yang Gyu

AU - Jeon, Do Yong

AU - Chung, Suk Jae

AU - Shim, Chang Koo

AU - Kim, Dae Duk

PY - 2008/1

Y1 - 2008/1

N2 - Ketoprofen plasters of 70 cm2 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 cm2 plaster. AUC0-24h and Cmax 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 cm2 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.

AB - Ketoprofen plasters of 70 cm2 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 cm2 plaster. AUC0-24h and Cmax 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 cm2 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.

KW - Analgesic

KW - Anti-inflammation

KW - Ketoprofen

KW - Pharmacodynamics

KW - Pharmacokinetics

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EP - 44

JO - Biopharmaceutics and Drug Disposition

JF - Biopharmaceutics and Drug Disposition

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ER -

Pharmacokinetics and pharmacodynamics of ketoprofen plasters

Abstract

Keywords

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