Ketotifen transdermal delivery systems were prepared using polyisobutylene, liquid paraffin, and fatty acid. In vitro skin penetration studies were conducted in Franz diffusion cells using excised porcine skin to determine the skin permeation rates of ketotifen patches. A trend of increased skin penetration of ketotifen was observed as the amount of liquid paraffin in the patch was increased. In addition, we found that 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 anaphylactic 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 produced higher survival rates. The pharmacokinetics of the ketotifen patch were determined by applying the skin patch to the dorsal skin of rabbits. The plasma levels were maintained constant (42.5-36.4 ng/ml) from 9 to 30 hr. From our study, the prepared ketotifen patch may further be developed for the treatment or prevention of allergic asthma.