Pharmacokinetic profile of [14C]flutrimazole following single topical application in normal and scarified skin of healthy volunteers.
14C-labelled 1-[(2-fluorophenyl)(4-fluorophenyl)phenylmethyl]-1H- imidazole (flutrimazole, UR-4056, CAS 119006-77-8) was administered topically (dermally) in three male volunteers to normal skin and scarified skin, respectively. Blood, urine and faeces were collected and radioassayed by liquid scintillation counting techniques. After topical application to healthy skin area, less than 1% of flutrimazole was absorbed percutaneously from a 1% cream and the amount absorbed was excreted with the urine. Following administration of the drug to scarified skin, the proportions absorbed were very similar to those measured after application to normal skin. About 0.5% of the administered dose is recovered in urine. The absorbed amount of drug leads to very low concentrations in the circulation, lower than a few ng/ml.
Duchène
P
P
Adme Bioanalyses, Parc Haute Technologie, Mougins, France.
Papalexiou
P
P
Ramis
J
J
Izquierdo
I
I
Houin
G
G
D000287:Administration, Topical; D000328:Adult; D000935:Antifungal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002921:Cicatrix / Q000378:metabolism*; D003022:Clotrimazole / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D005243:Feces / Q000737:chemistry; D006801:Humans; D008297:Male; D012869:Skin Absorption; D012879:Skin Physiological Phenomena
D000935:Antifungal Agents; C076986:flutrimazole; D003022:Clotrimazole