Absolute concentrations of an antimycotic agent, econazole, in the human skin after local application. 1976

H Schaefer, and G Stüttgen

The absolute concentrations of an antimycotic drug, econazole, 1-[2,4-dichloro-beta-(p-chlorobenzyloxy)-phenethyl]-imidazole nitrate, in the different layers of the skin are reported when the agent is applied to human skin in vitro and in vivo. The drug was tritium-labelled and incorporated into an ointment to give a 1% concentration as it is used in the therapy of dermatomycoses. This ointment was applied to the skin surface. After fixed time intervals, the skin was sliced parallel to the surface and the amount in each layer determined by liquid scintillation counting. In the in vivo investigations, the excretion of the drug in the urine was also determined. The results reveal that though up to 90% of the drug remain on the surface, about 20 mug/ml epidermal tissue and 1.5 mug/ml dermal tissue can be achieved. The amount which is excreted in the urine is equivalent to the quantity which enters the skin, i.e., the penetrating drug is absorbed by the circulatory system.

UI MeSH Term Description Entries
D007093 Imidazoles Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
D008297 Male Males
D003881 Dermatomycoses Superficial infections of the skin or its appendages by any of various fungi. Skin Diseases, Fungal,Dermatomycosis,Dermatophyte Infection,Fungal Skin Diseases
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000287 Administration, Topical The application of drug preparations to the surfaces of the body, especially the skin (ADMINISTRATION, CUTANEOUS) or mucous membranes. This method of treatment is used to avoid systemic side effects when high doses are required at a localized area or as an alternative systemic administration route, to avoid hepatic processing for example. Drug Administration, Topical,Administration, Topical Drug,Topical Administration,Topical Drug Administration,Administrations, Topical,Administrations, Topical Drug,Drug Administrations, Topical,Topical Administrations,Topical Drug Administrations
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000368 Aged A person 65 years of age or older. For a person older than 79 years, AGED, 80 AND OVER is available. Elderly
D000935 Antifungal Agents Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues. Anti-Fungal Agents,Antifungal Agent,Fungicides, Therapeutic,Antibiotics, Antifungal,Therapeutic Fungicides,Agent, Antifungal,Anti Fungal Agents,Antifungal Antibiotics
D012869 Skin Absorption Uptake of substances through the SKIN. Absorption, Skin,Intracutaneous Absorption,Intradermal Absorption,Percutaneous Absorption,Transcutaneous Absorption,Transdermal Absorption,Absorption, Intracutaneous,Absorption, Intradermal,Absorption, Percutaneous,Absorption, Transcutaneous,Absorption, Transdermal,Absorptions, Intracutaneous,Absorptions, Intradermal,Absorptions, Percutaneous,Absorptions, Skin,Absorptions, Transcutaneous,Absorptions, Transdermal,Intracutaneous Absorptions,Intradermal Absorptions,Percutaneous Absorptions,Skin Absorptions,Transcutaneous Absorptions,Transdermal Absorptions

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