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KMID : 0366919980100010273
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Sungkyun Pharmceutical Journal
1998 Volume.10 No. 1 p.273 ~ p.277
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Pharmacokinetic Properties and Antiinflammatory Activity of Ketoprofen Lotion
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Abstract
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The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5㎎/㎏, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and E-lotion, which is a 3% ketoprofen lotion in the Japanese market, was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, C_max were 316±22.3ng/㎖ and 163±12.2ng/㎖, respectively, at the same T_max of 2 hours postdose, while C_max and T_max after oral administration of the drug were 1,030±89.1ng/㎖ and 0.25 hours, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageenen-induced edema method after 50㎎ of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while E-lotion showed 34.7%. The calculated ED_50 after transdermal application of ID-lotion was 2.5㎎/㎏, while that after oral administration was 7.0 ㎎/㎏. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.
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KEYWORD
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