Arika T, Hase T, Yokoo M
Central Research Laboratories, Kaken Pharmaceutical Co., Ltd, Kyoto, Japan.
Antimicrob Agents Chemother. 1993 Feb;37(2):363-5. doi: 10.1128/AAC.37.2.363.
We examined anti-Trichophyton mentagrophytes activity, cutaneous penetration, and skin localization of butenafine, a novel benzylamine antifungal agent. The following results were obtained. (i) In the guinea pig dorsal skin trichophytosis model, butenafine produced complete eradication of fungi from infected sites. Clotrimazole was active when animals were infected with 10(4) or 10(5) cells but was almost inactive when the inoculum size was 10(6) cells. (ii) The MICs of butenafine and clotrimazole against arthrospores of T. mentagrophytes KD-04 were 0.025 and 0.39 microgram/ml, respectively. (iii) When 0.2 ml of a 1% 14C-butenafine solution was applied for 23 h/day for 7 days, high radioactivity corresponding to 250 to 500 micrograms of butenafine per g of skin in the epidermis, including the horny layer, was observed. (iv) Butenafine penetrates through transepidermal and transfollicular routes. The excellent therapeutic efficacy of butenafine on experimental dermatophytosis may be attributed to its low MIC and good penetration and distribution in the horny layer and hair follicles, where fungi reside.
我们研究了新型苄胺类抗真菌药布替萘芬对须癣毛癣菌的活性、皮肤渗透性及在皮肤中的定位。结果如下：（i）在豚鼠背部皮肤癣菌病模型中，布替萘芬可使感染部位的真菌完全清除。当动物感染10⁴或10⁵个细胞时，克霉唑有活性，但接种量为10⁶个细胞时，克霉唑几乎无活性。（ii）布替萘芬和克霉唑对须癣毛癣菌KD - 04关节孢子的最低抑菌浓度分别为0.025和0.39微克/毫升。（iii）当每天23小时涂抹0.2毫升1%的¹⁴C - 布替萘芬溶液，持续7天时，在包括角质层在内的表皮中观察到高放射性，相当于每克皮肤中有250至500微克布替萘芬。（iv）布替萘芬通过经表皮和经毛囊途径渗透。布替萘芬对实验性皮肤癣菌病的优异治疗效果可能归因于其低最低抑菌浓度以及在真菌所在的角质层和毛囊中的良好渗透性和分布。
