Formulation and Evaluation of Ethylene–Vinyl Acetate Copolymer Matrix Patches Containing Formoterol Fumarate

The skin permeability and stability of formoterol fumarate (FF) in matrix patches containing l-menthol as an enhancer and N-methyl-2-pyrrolidone (NMP) as the solvent were investigated. Using a total of 28 matrix patches having a similar composition, containing ethylene–vinyl acetate (EVA) as the for...

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Bibliographic Details
Published in:Biological & Pharmaceutical Bulletin 2006, Vol.29(3), pp.513-516
Main Authors: Kakubari, Ikuhiro, Shinkai, Norihiro, Kawakami, Junji, Uruno, Akemi, Takayasu, Toshiyuki, Yamauchi, Hitoshi, Takayama, Satoshi, Takayama, Kozo
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Animals
Anti-Asthmatic Agents - administration & dosage
Anti-Asthmatic Agents - chemistry
Anti-Asthmatic Agents - pharmacokinetics
Bronchoconstriction - drug effects
Chemistry, Pharmaceutical
Chromatography, High Pressure Liquid
efficacy
Electrochemistry
Ethanolamines - administration & dosage
Ethanolamines - chemistry
Ethanolamines - pharmacokinetics
Excipients
formoterol
Formoterol Fumarate
Hemodynamics - drug effects
Histamine - pharmacology
l-menthol
Male
Mass Spectrometry
Menthol - chemistry
N-methyl-2-pyrrolidone
Polyvinyls - chemistry
Pyrrolidinones - chemistry
Rats
Rats, Wistar
Skin Absorption
skin permeation
stability
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Summary:The skin permeability and stability of formoterol fumarate (FF) in matrix patches containing l-menthol as an enhancer and N-methyl-2-pyrrolidone (NMP) as the solvent were investigated. Using a total of 28 matrix patches having a similar composition, containing ethylene–vinyl acetate (EVA) as the forming polymer and hydrogenated rosin glycerol ester (Ester Gum H) as the adhesive, the skin permeation of FF was found to increase with increasing l-menthol and NMP contents. FF in the matrix patches containing NMP in the range of 4.8—7.2% was stable, but stability decreased at higher values. With a standard matrix patch containing FF, the Cmax and AUC0—24 values were found to be 1.93 ng/ml after 4 h percutaneous application to rats and 25.6 ng·h/ml. The bioavailability after percutaneous exposure was equivalent to 15.2% of the AUC0—24 after intravenous administration. Percutaneous application proved efficacious with regard to control of simulated asthma at dose levels lower than those with which side effects occurred. Thus an optimized matrix patch containing FF was prepared with potential advantages for control of asthma.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.29.513