THERAPEUTIC EFFECT AND PHARMACOKINETICS OF KETOTIFEN TRANSDERMAL DELIVERY SYSTEM

Ketotifen transdermal delivery systems were prepared using polyisobuty lene, liquid paraffin, and fatty acid. In vitro skin penetration studi es were conducted in Franz diffusion cells using excised porcine skin to determine the skin permeation rates of ketotifen patches. A trend o f increased skin penetration of ketotifen was observed as the amount o f liquid paraffin in the patch was increased. In addition, we found th at lauric acid was a suitable enhancer for percutaneous absorption of ketotifen. Challenge tests were performed in guinea pigs to determine the therapeutic effect of the delivery systems for the inhibition of a naphylactic shock using varied concentrations of chicken ovum albumin as sensitizer. Our results showed that compared with the treatment of intramuscular administration, the skin patch was more effective and pr oduced higher survival rates. The pharmacokinetics of the ketotifen-pa tch were determined by applying the skin patch to the dorsal skin of r abbits. The plasma levels were maintained constant (42.5-36.4 ng/ml) f rom 9 to 30 hr. From our study, the prepared ketotifen patch may furth er be developed for the treatment or prevention of allergic asthma.