Quintanar-Guerrero D, Ganem-Quintanar A, Tapia-Olguín P, Kalia Y N, Buri P
FES-Cuautitlan, Universidad Nacional Autónoma de México, Mexico City.
Drug Dev Ind Pharm. 1998 Jul;24(7):685-90. doi: 10.3109/03639049809082373.
The permeability of three imidazole antimycotics (miconazole nitrate, ketoconazole, and itraconazole) through the free edge of healthy human nail was evaluated in vitro using side-by-side diffusion cells. The influence of keratolytic substances (papain, urea, and salicylic acid) on the permeability of the antimycotics was also studied. The results suggested that the nail constituted an impermeable barrier for these antimycotics; it could be considered that the nail behaved as a hydrophilic gel membrane, through which drugs of low solubility could not permeate. The use of ethanol did not promote the passage of any of the antimycotic drugs. Although scanning electron microscopy indicated that the keratolytic substances had a significant effect on the nail surface (papain > salicylic acid > urea), the passage of the three antimycotics was not improved by pretreatment with salicylic acid alone (20% for 10 days), or by the application of the drug in a 40% urea solution. It was found that only the combined effects of papain (15% for 1 day) and salicylic acid (20% for 10 days) were capable of enhancing the permeability of the antimycotic.
使用并列扩散池在体外评估了三种咪唑类抗真菌药（硝酸咪康唑、酮康唑和伊曲康唑）透过健康人指甲游离边缘的渗透性。还研究了角质溶解剂（木瓜蛋白酶、尿素和水杨酸）对抗真菌药渗透性的影响。结果表明，指甲对这些抗真菌药构成了不透性屏障；可以认为指甲表现为亲水性凝胶膜，低溶解度的药物无法透过。使用乙醇并未促进任何一种抗真菌药的透过。尽管扫描电子显微镜显示角质溶解剂对指甲表面有显著影响（木瓜蛋白酶＞水杨酸＞尿素），但单独用水杨酸预处理（20%，10天）或在40%尿素溶液中应用药物，三种抗真菌药的透过并未得到改善。发现只有木瓜蛋白酶（15%，1天）和水杨酸（20%，10天）的联合作用能够增强抗真菌药的渗透性。
