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Quantitative and radioautographic studies on the penetration kinetics of 9α-fluoro-16-methylene-prednisolone-21-acetate-7-T in human skin

  • V. K. Hopsu-Havu
  • P. Tuohimaa
Article

Summary

Penetration kinetics of tritium-labeled 9α-fluoro-16-methyleneprednisolone acetate (fluprednylidene-21-acetate, E. Merck AG), applied as 0.1% cream to normal as well as diseased skin were analyzed. Measurements of radioactivity in the epidermal samples obtained by stripping and tangential sectioning of skin revealed a high concentration of steroid in stratum corneum and granulosum, with only minimal amounts in the other epidermal layers. The same finding was verified by radioautography. Only a minimal penetration of labeled steroid from the suction blister roof to the subepidermal blister fluid was found to take place. Serial punch biopsies taken from the area of steroid application revealed that less than 10% of the steroid had been absorbed in three days when covered by an occlusive film. No radioactivity was detected in the urine after the application of a large sample of the steroid on normal skin without occlusion. When using an occlusive film, the peak of radioactivity in urine was detected 24 hours after the application of the steroid on eczematous skin and 48 hours after application on normal skin.

Keywords

Stratum Corneum Blister Fluid Suction Blister Eine Hohe Eczematous Skin 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Zusammenfassung

Die vorliegenden Untersuchungen am Menschen befassen sich mit der Penetrationskinetik des Tritium-markierten 9α-Fluor-16-methylenprednisolon-acetat (Fluprednyliden-21-acetat, E. Merck AG). Die bei den Versuchen angewendete Creme war eine 0,1% ige Öl-Wasser-Emulsion, deren Penetration an der normalen und kranken Haut studiert wurde. Wenn Tesafilm®-Abrisse oder tangentiale Hautschnitte angewandt wurden, zeigte die Radioaktivitätsverteilung in der Epidermis eine hohe Konzentration des Steroids in dem Stratum corneum und granulosum und nur minimale Mengen in den anderen epidermalen Schichten. Radioautographische Ergebnisse zeigten eine hohe Konzentration in den keratinisierten Schichten. Das Steroid wurde nur geringfügig durch die Blasendecke hindurch von der Flüssigkeit der Saugblase aufgenommen. Die Radioaktivitätsmessung von täglichen Hautbiopsien zeigte, daß weniger als 10% des Steroids, das unter einem occlusiven Verband war, innerhalb von 3 Tagen von der Haut absorbiert wurde. Eine Radioaktivität im Urin wurde nach epicutaner Applikation von großen Mengen des Steroids auf die normale Haut ohne einen occlusiven Verband nicht gefunden. Nach Anwendung eines Occlusivverbandes erschien ein Gipfel der Radioaktivität im Urin 24 Std nach der Applikation des Steroids auf die ekzematierte Haut und 48 Std nach der Applikation auf die normale Haut.

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Copyright information

© Springer-Verlag 1970

Authors and Affiliations

  • V. K. Hopsu-Havu
    • 1
    • 2
  • P. Tuohimaa
    • 1
    • 2
  1. 1.Department of AnatomyUniversity of TurkuFinland
  2. 2.Department of DermatologyUniversity of TurkuFinland

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