Percutaneous absorption of methylprednisolone aceponate following topical application of Advantan lotion on intact, inflamed and stripped skin of male volunteers

Skin Pharmacol Appl Skin Physiol. 1998 Jan-Feb;11(1):35-42. doi: 10.1159/000029806.

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.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial

MeSH terms

  • Adhesives
  • Administration, Topical
  • Aged
  • Anti-Inflammatory Agents / adverse effects
  • Anti-Inflammatory Agents / pharmacokinetics*
  • Dermatitis / drug therapy*
  • Dermatitis / metabolism
  • Dose-Response Relationship, Drug
  • Emulsions
  • Erythema / drug therapy
  • Erythema / metabolism
  • Humans
  • Male
  • Methylprednisolone / adverse effects
  • Methylprednisolone / analogs & derivatives*
  • Methylprednisolone / pharmacokinetics
  • Middle Aged
  • Reference Values
  • Skin Absorption*
  • Sunburn / drug therapy*
  • Sunburn / metabolism
  • Surface Properties
  • Ultraviolet Rays

Substances

  • Adhesives
  • Anti-Inflammatory Agents
  • Emulsions
  • methylprednisolone aceponate
  • Methylprednisolone