Kinetic study of the percutaneous absorption of 1,2,4-3H-labelled flupamesone.
Two different creams containing 4,4'-methylene bis-[(9 alpha-fluor-11 beta,21-dihydroxy-16alpha,17alpha-isopropylidenedioxy-1,4-pregnadiene-3,20-dione)-3-methoxy-2-naphthoate] (flupamesone) and triamcinolone-acetonide, both labelled with tritium, were prepared in order to study their absorption kinetics. Results were compared in order to find structure-activity relations following Malkinson's hypothesis. The radioactivity was measured in samples of skin taken at various intervals of time after the application of the cream. The results showed a reservoir of corticoids at 400--700 mu depth and that flupamesone remains longer in skin than does triamcinolone-acetonide.
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000378:metabolism*; D005938:Glucocorticoids; D011244:Pregnadienediols / Q000378:metabolism*; D012869:Skin Absorption; D013329:Structure-Activity Relationship; D013552:Swine; D013997:Time Factors; D014222:Triamcinolone Acetonide / Q000378:metabolism; D014316:Tritium
D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D011244:Pregnadienediols; D014316:Tritium; C010960:flupamesone; D014222:Triamcinolone Acetonide