Retention of amorolfine in the skin tissue as measured by prevention of the development of experimental dermatophytosis in guinea pigs
Uchida, K.; Yamaguchi, H.
Japanese Journal of Antibiotics 44(9): 1032-1041
1991
ISSN/ISBN: 0368-2781 PMID: 1960853 Document Number: 369506
In order to assess the extent of dermal retention of amorolfine (MT-861), a new morpholine antifungal agent, cream preparations of MT-861 were applied to the skin on the back of guinea pigs and the protective effect was determined regarding the topical treatment on the development of infection induced by subsequent inoculation with conidia of Trichophyton mentagrophytes. One per cent bifonazole (BFZ) cream was used as the reference drug. The results are summarized as follows. 1. Pretreatment with 0.125, 0.25 or 0.5% MT-861 preparation 1 to 3 days before infection significantly reduced the extent of lesion developed compared to the untreated control at post-infection day-12 and day-19 measurements. 2. Cultures of specimens taken from the skin lesion performed on postinfection day-19 showed that pretreatment with 0.125, 0.25 or 0.5% MT-861 cream 1 day before infection significantly lowered the number of culture-positive skin lesions compared to that of untreated control. 3. No significant difference was observed among the 3 experimental groups of animals pretreated with MT-861 preparations 1 to 3 days before infection in extent to lesions developed, though the mycological protective effect of the drug appeared to decrease with increasing time intervals between drug-pretreatment and fungal challenge. 4. A 0.5% MT-861 preparation had an equal or superior infection-preventive effect to 1% BFZ preparation as far as severity of lesion and recovery of fungi were concerned. 5. The potent and prolonged protective action by MT-861 preparations against the development of fungal infection strongly suggests that MT-861 retains in the skin tissue in an active form for substantially long periods of time.