title: Effect of cyclohexanone derivatives on percutaneous absorption of ketoprofen and indomethacin.
abstract: The promoting effect of cyclohexanone derivatives on the percutaneous absorption of ketoprofen and indomethacin from gel ointments was investigated in rats. Drug absorption was markedly enhanced by the addition of 2-tert-butylcyclohexanone. Promoting activities of 2,6-dimethyl and 4-tert-butylcyclohexanone were also observed, but their effects were significantly lower than that of the 2-tert-butyl derivative. The effect of side chain length at the 2-position of the cyclohexanone ring on the percutaneous absorption of these drugs was determined similarly using a series of 2-n-alkylcyclohexanones. Pronounced effects were observed in the case of 2-n-octylcyclohexanone, suggesting that a chain length of eight carbons is an important factor for absorption enhancement in this series. The extent of absorption enhancement was found to be an almost linear function of 2-n-octycyclohexanone concentrations in the range from 0 to 10%.
authors.affiliation: Faculty of Pharmaceutical Science, Hoshi University, Tokyo, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Akitoshi
authors.forename: K
authors.initials: K
authors.lastname: Takayama
authors.forename: Y
authors.initials: Y
authors.lastname: Machida
authors.forename: T
authors.initials: T
authors.lastname: Nagai
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D003512:Cyclohexanones / Q000008:administration & dosage / Q000493:pharmacokinetics; D015195:Drug Design; D007213:Indomethacin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D007660:Ketoprofen / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D007700:Kinetics; D008297:Male; D010666:Phenylpropionates / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains; D012869:Skin Absorption; D013329:Structure-Activity Relationship
chemical_list: D003512:Cyclohexanones; D010666:Phenylpropionates; D007660:Ketoprofen; D007213:Indomethacin