Faergemann J, Godleski J, Laufen H, Liss R H
University of Gothenburg, Sweden.
Acta Derm Venereol. 1995 Sep;75(5):361-3. doi: 10.2340/000155557575361363.
Fluconazole administered at 150 mg/week for 1-5 weeks is effective orally against dermatophytes and yeast in stratum corneum. Clinical and mycological cure rates approach 90%, but the precise distribution of the drug within various layers of skin is uncertain. We administered fluconazole at 150 mg/week for 2 weeks to 5 volunteers. Distribution of fluconazole in biopsies of skin was imaged by energy dispersive analysis of X-rays (EDX) and transmission electron microscopy, and in cells by electron energy-loss spectroscopy (EELS). Eight hours after a second dose, EDX showed fluconazole highest and homogeneously distributed in stratum corneum, lower in the rest of the epidermis, and lowest in dermis. The highest fluconazole levels detected by EELS were in cytoplasmic inclusions of sweat and sebaceous glands and less in keratinocytes and dermal collagen. We conclude that fluconazole delivered to stratum corneum by direct diffusion from capillaries and in sweat is also in all likelihood transported in sebum.
每周口服150毫克氟康唑，持续1至5周，对角质层中的皮肤癣菌和酵母菌有效。临床和真菌学治愈率接近90%，但该药物在皮肤各层中的具体分布尚不确定。我们对5名志愿者每周给予150毫克氟康唑，持续2周。通过X射线能量色散分析（EDX）和透射电子显微镜对皮肤活检组织中氟康唑的分布进行成像，并通过电子能量损失谱（EELS）对细胞中的氟康唑分布进行成像。第二次给药8小时后，EDX显示氟康唑在角质层中分布最高且均匀，在表皮其余部分较低，在真皮中最低。EELS检测到的氟康唑最高水平存在于汗腺和皮脂腺的细胞质内含物中，在角质形成细胞和真皮胶原蛋白中较少。我们得出结论，通过从毛细血管直接扩散以及汗液输送到角质层的氟康唑，很可能也通过皮脂进行转运。
