Effects of solvents on skin permeation of formoterol fumarate.
Effects of various chemicals applied as penetration enhancers on the permeation of formoterol fumarate (FF) across excised rat skin were investigated. Remarkable enhancement was noted with terpenes, fatty acid esters, and higher alcohols, whereas no significant influence was observed in the case of lower alcohols, pyrrolidones, and amines. At high concentration, a cineole/N-methyl-2-pyrrolidone (NMP) mixed solvent system slightly enhanced the skin permeation of FF compared with cineole alone, and a l-menthol/NMP mixed solvent system caused significant further increase. Maximum skin permeation of FF was seen when the ratio of l-menthol/NMP was 60/40 w/w. From the present results, l-menthol/NMP and isopropyl myristate (IPM)/NMP mixed solvent systems can be considered effective for augmenting skin permeation of FF, with potential applications in transdermal delivery of the drug.
Kakubari
Ikuhiro
I
Research Department, Saitama Daiichi Pharmaceutical Co., Ltd, Saitama, Japan. kabukari@sdsk.co.jp
Nakamura
Noriko
N
Takayasu
Toshiyuki
T
Yamauchi
Hitoshi
H
Takayama
Satoshi
S
Takayama
Kozo
K
D000279:Administration, Cutaneous; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004357:Drug Synergism; D004983:Ethanolamines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005079:Excipients; D000068759:Formoterol Fumarate; D066298:In Vitro Techniques; D008297:Male; D010539:Permeability / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption / Q000187:drug effects*; D012997:Solvents / Q000494:pharmacology
D004983:Ethanolamines; D005079:Excipients; D012997:Solvents; D000068759:Formoterol Fumarate