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标题：Effects of Ethylcellulose and 2-Octyldodecanol Additives on Skin Permeation and Irritation with Ethylene–Vinyl Acetate Copolymer Matrix Patches Containing Formoterol Fumarate
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作者：Ikuhiro Kakubari ; Hiroyuki Sasaki ; Toshiyuki Takayasu 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2006
卷号：29
期号：8
页码：1717-1722
DOI：10.1248/bpb.29.1717
出版社：The Pharmaceutical Society of Japan
摘要：Skin permeation of formoterol fumarate (FF) and irritation with ethylene–vinyl acetate (EVA) copolymer matrix patches was investigated using rat and human skin in vitro and different species of experimental animal, respectively. Skin permeation of FF increased remarkably without addition of ethylcellulose (EC) and was remarkably enhanced by incorporation of 2-octyldodecanol (OD) instead of hydrogenated rosin glycerol ester (Ester Gum H). Effects on skin permeation of FF with EVA matrix patches were similar in rat and human skin, but rat skin was 1000 times more permeable than human skin after 24 h. The primary irritation indices for matrix patches without EC and with EC (OD-0), EC and 0.5 mg OD per square centimeter (OD-0.5), and EC and 1.0 mg OD per square centimeter (OD-1) were 1.46, 1.13,1.29 and 1.38. The results suggested that the irritation induced by these patches was rather mild, but significantly greater than the 0.21 observed with the control. No significant effects were noted for either EC or OD alone. Skin irritation intensity with EVA matrix patches was observed to be in the order of rabbits, guinea pigs, rats and miniature swine.
关键词：skin;permeation;irritation;formoterol