• 약학회지
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• 제42권1호
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• pp.25-30
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• 1998

This study was designed to compare the absorption fraction and extent of ketoprofen gels and a matrix typed ketoprofen plaster patch. 3g (90mg as ketoprofen) of the two gels whi ch has oleohydrogel or hydrogel as a base, respectively, and 3 pieces of plaster patches (90mg as ketoprofen) were, applied in the area of 210$cm^2$ on forearm in 12 volunteers by cross over design. Blood samples were collected serially up to 24 hours and the plasma concentrations of ketoprofen were analyzed by HPLC using flurbiprofen as an internal standard. The detection limit of the assay was 1ng/ml of ketoprofen in plasma. The pharmacokinetic parameters (e.g. $AUC_{24hr}$, $AUMC_{24hr}$, MRT, Fraction Absorbed) were calculated from the plasma concentrations time data of each volunteer. The oleo-hydrogel showed significantly higher absorption fraction and extent of ketoprofen than the current hydrogel. The mean plasma concentrations of the oleo-hydrogel were increased to 98.46${\pm}$23.15ng/ml by 6 hour after application, and increased futher to 100.61${\pm}$18.65ng/ml at 24 hour. On the other hand, those of the hydrogel were increased 17.61${\pm}$18.65ng/ml at 5 hour to 34.68${\pm}$9.65ng/ml at 24 hour gradually. Therefore the plasma concentrations of oleo-hydrogel at each measured time were 3~7 times greater than those of the hydrogel with statistical significance. The $AUC_{24hr}$ (1797.26${\pm}$52.09ng.h/ml) of the oleo-hydrogel was 3.5 times greater (P<0.05) than that (516.17${\pm}$104.52ng.h/ml) of the hydrogel. The plaster patches showed higher bioavailability ($AUC_{24hr}$ 2877.37${\pm}$578.27ng.h/ml) than the olea-hydrogel ($AUC_{24hr}$ 1797.26${\pm}$52.09ng.h/ml) without statistical significance. But the absorption fraction of the oleo-hydrogel was rather higher than that of the plaster patches during the first 6 hours after administration. These results suggest that newly developed ketoprofen gel which is used oleo-hydrogel as a base would show excellent skin permeation on topical application for the corresponding clinical indications and could be absorbed as well as plaster patches.

• 한국임상수의학회지
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• 제31권3호
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• pp.220-222
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• 2014

14년령의 Shih-Tzu 개가 이물섭취 및 구토를 주 증으로 본원에 내원하였다. 구토물은 인의에서 사용되는 부착형 제제인 ketoprofen plaster 였다. 대증치료로 위장관 보호제 투여와 수액요법을 실시하였다. 하지만 임상증상은 점점 악화되어 빈혈 및 흑색변, 백혈구 증가증, 고지혈증이 관찰되었다. 환자는 위장관 출혈이 있는 것으로 평가되었고, 수혈 및 위장관 보호제로 바륨제제를 도포하였다. 바륨제제를 위장관 보호제로 사용한 후 임상증상의 개선이 확인 되었다.

• Biomolecules & Therapeutics
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• 제9권4호
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• pp.298-306
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• 2001

To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of vehicle composition and drug loading dose on the skin permeation property were investigated. And in vivo skin absorption property studied by analysing the $C_{max}$ and AUC was investigated after applying the developed plaster systems on rabbit back skin. Addition of isopropyl myristate (IPM) and IPM-diethylene glycol monoethyl ether (DGME) cosolvent in the plaster showed higher permeation rates than those from propylene glycol laurate-DGME cosolvent systems. As the concentration of LP in the plaster increased from 0.56 mg/$\textrm{cm}^2$ to 1.19 mg/$\textrm{cm}^2$, the drug release and skin permeation rates increased linearly. At loading dose of 1.19 mg/$\textrm{cm}^2$, the flux reached 35.6 $\mu$g/$\textrm{cm}^2$/hr. New LP plasters showed a good adhesive property onto skin, and showed no crystal formation. The AU $C_{0-24hr}$ and $C_{max}$ after dermal application of LP plaster (60 mg/70 $\textrm{cm}^2$) were found to be 6951$\pm$230 ng.hr/ml and 400$\pm$44 ng/ml, respectively. And the plasma concentration maintained above 300 ng/ml up to 24 hr period. In the carrageenan-induced rat paw edema test, LP plaster showed similar inhibition rate with marketed ketoprofen (Ketoto $p^{R}$) plaster.aster.r.

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.237.1-237.1
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• 2001