title: Percutaneous absorption of methylprednisolone aceponate following topical application of Advantan lotion on intact, inflamed and stripped skin of male volunteers.
abstract: Six healthy, elderly volunteers received three topical treatments with Advantan lotion containing 0.1% of methylprednisolone aceponate (MPA, CAS 86401-95-8) on intact, inflamed and stripped skin in a consecutive fashion at weekly intervals. The lotion (O/W emulsion) containing 14C-MPA (specific radioactivity 1.8 MBq/mg MPA) was applied in an area dose of 5 mg lotion/cm2 on a marked area of 100 cm2 on the back for 24 h. Inflammation was caused by UV-B irradiation at 3 MED 6 h prior to the treatment with the test preparation. Removal of stratum corneum was performed by 20-fold adhesive tape stripping. The concentration of radioactivity was measured in the plasma and in the urine up to 7 days following each treatment. The concentration of radioactivity in the plasma did not exceed the limit of detection of 1.5 ng MPA Eq/ml at any time point. The percutaneous absorption was assessed from the cumulated excretion of radiolabelled substances in the urine corrected for biliary excretion. Less than 0.5% of the dose was percutaneously absorbed through intact skin and through inflamed skin. After removal of the penetration barrier ('stripping') the percutaneous absorption increased to 15.4 +/- 7.7% of the applied dose.
authors.affiliation: Institute of Pharmacokinetics, Schering AG, Berlin, Germany.
authors.forename: C
authors.initials: C
authors.lastname: Günther
authors.forename: A
authors.initials: A
authors.lastname: Kecskes
authors.forename: T
authors.initials: T
authors.lastname: Staks
authors.forename: U
authors.initials: U
authors.lastname: Täuber
mesh_terms: D000269:Adhesives; D000287:Administration, Topical; D000368:Aged; D000893:Anti-Inflammatory Agents / Q000009:adverse effects / Q000493:pharmacokinetics*; D003872:Dermatitis / Q000188:drug therapy* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004655:Emulsions; D004890:Erythema / Q000188:drug therapy / Q000378:metabolism; D006801:Humans; D008297:Male; D008775:Methylprednisolone / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008875:Middle Aged; D012016:Reference Values; D012869:Skin Absorption; D013471:Sunburn / Q000188:drug therapy* / Q000378:metabolism; D013499:Surface Properties; D014466:Ultraviolet Rays
chemical_list: D000269:Adhesives; D000893:Anti-Inflammatory Agents; D004655:Emulsions; C078007:methylprednisolone aceponate; D008775:Methylprednisolone