Dermal absorption of fluprednidene-21-acetate and miconazole from a new topical preparation in pigs.
The dermal absorption of fluprednidene-21-acetate (CAS 1255-35-2) and miconazole nitrate (CAS 22832-87-7) of a new combination cream (Decoderm tri) was studied in pigs after application of 0.5 g cream/kg body weight under occlusive dressing for 5 h. 3H-labelled fluprednidene-21-acetate and 14C-labelled miconazole nitrate were introduced into the base cream as single components or in combination. The three resulting creams were tested in groups of 3 pigs each. To obtain a basis for the assessment of the data after dermal application the two labelled drugs were also examined after intravenous injection. Based on the comparison of the AUC of the radioactive labels an absorption of 4.4% for fluprednidene-21-acetate was calculated when administered alone and 2.4% when administered in the combination cream. For miconazole a smaller absorbed fraction of the dermal dose of 0.5 and 0.8%, resp., was found. Since the differences between single and combined administration were not significant, it follows that there is no relevant reciprocal influence of the two compounds on their dermal absorption.
E. Merck, Institute for Pharmacokinetics and Metabolism, Grafing near Munich, Fed. Rep. of Germany.
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Garbe
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Rogalla
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Faro
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Kunert
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004338:Drug Combinations; D005260:Female; D005938:Glucocorticoids; D007275:Injections, Intravenous; D008825:Miconazole / Q000008:administration & dosage / Q000493:pharmacokinetics*; D011246:Pregnadienetriols / Q000008:administration & dosage / Q000493:pharmacokinetics*; D012869:Skin Absorption / Q000502:physiology*; D013552:Swine
D000893:Anti-Inflammatory Agents; D004338:Drug Combinations; D005938:Glucocorticoids; D011246:Pregnadienetriols; D008825:Miconazole; C100064:fluprednidene acetate