title: The use of complexation with alkanolamines to facilitate skin permeation of mefenamic acid.
abstract: The preparation of mefenamic acid (MH)-alkanolamine [monoethanolamine, diethanolamine, triethanolamine and propanolamine] complexes was attempted to increase the transdermal flux of MH. A lipophilic enhancer system consisting of isopropyl myristate (IPM) and ethanol (9:1; EI system) produced a marked enhancement of MH flux from the alkanolamine complexes through hairless rat skin membrane. Among the alkanolamines examined, the propanolamine complex had the greatest enhancing effect on the permeation of MH. The observed permeation enhancement of MH-alkanolamine complexes by the EI system was explained by an analysis based on a two-layer diffusion model. The stratum corneum immersed in IPM forms a continuous phase of vehicle and stratum corneum and, from the phase, ethanol transport the MH-alkanolamine complexes to the epidermis and dermis, and the complexes, which are more water soluble than MH, exhibit increased partition into the epidermis and dermis, as the flux increases.
authors.affiliation: Faculty of Pharmaceutial Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama 350-0295, Japan.
authors.forename: Liang
authors.initials: L
authors.lastname: Fang
authors.forename: Sachihiko
authors.initials: S
authors.lastname: Numajiri
authors.forename: Daisuke
authors.initials: D
authors.lastname: Kobayashi
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Morimoto
mesh_terms: D020003:1-Octanol / Q000737:chemistry; D000277:Adjuvants, Pharmaceutic / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D004339:Drug Compounding; D019856:Ethanolamine / Q000737:chemistry / Q000493:pharmacokinetics; D004983:Ethanolamines / Q000737:chemistry / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D008297:Male; D008528:Mefenamic Acid / Q000493:pharmacokinetics*; D008954:Models, Biological; D011412:Propanolamines / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D011919:Rats, Inbred Strains; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D014867:Water / Q000737:chemistry
chemical_list: D000277:Adjuvants, Pharmaceutic; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004983:Ethanolamines; D011412:Propanolamines; D014867:Water; D008528:Mefenamic Acid; D019856:Ethanolamine; C009546:triethanolamine; C020283:diethanolamine; D020003:1-Octanol