Skin Pharmacology and Physiology
Original Research Article
Percutaneous Absorption of Methylprednisolone Aceponate following Topical Application of Advantan® Lotion on Intact, Inflamed and Stripped Skin of Male VolunteersGünther C.a · Kecskes A.b · Staks T.b · Täuber U.ca Institute of Pharmacokinetics, b Institute of Clinical Pharmacology, and c Centre of Dermatology, Schering AG, Berlin, Germany
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Article / Publication Details
Published online: April 01, 1998
Issue release date: January – February
Number of Print Pages: 8
Number of Figures: 2
Number of Tables: 2
ISSN: 1660-5527 (Print)
eISSN: 1660-5535 (Online)
For additional information: https://www.karger.com/SPP
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.
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References
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Zaumseil R-P, Kecskes A, Täuber U, Töpert M: Methylprednisolone aceponate (MPA) – a new therapeutic for eczema: A pharmacological overview. J Dermatol Treat 1992;3(suppl):3–7.
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Zaumseil R-P, Fuhrmann H, Kecskes A, Täuber U, Töpert M: Methylprednisolonaceponat (AdvantanR): Eine effektive und nebenwirkungsarme topische Kortikoidtherapie; in Macher E, Kolde G, Bröcker EB (eds): Jahrbuch der Dermatologie. Zülpich, Biermann, 1992/93, pp 243–263.
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Täuber U: Dermatocorticosteroids: Structure, activity, pharmacokinetics. Eur J Dermatol 1994;6:3–13.
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Täuber U: Skin pharmacokinetics of a new topical glucocorticosteroid MPA; in Scott RC, Guy RH, Hadgraft J (eds): Prediction of Percutaneous Penetration. London, IBC Technical Services, 1990, pp 37–48.
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Täuber U: Pharmacokinetics and bioactivation of MPA. J Eur Acad Dermatol Venereol 1994;3(suppl 1):523–531.
Article / Publication Details
Published online: April 01, 1998
Issue release date: January – February
Number of Print Pages: 8
Number of Figures: 2
Number of Tables: 2
ISSN: 1660-5527 (Print)
eISSN: 1660-5535 (Online)
For additional information: https://www.karger.com/SPP
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