In-vitro permeability of the human nail and of a keratin membrane from bovine hooves: Prediction of the penetration rate of antimycotics through the nail plate and their efficacy
In-vitro permeability of the human nail and of a keratin membrane from bovine hooves: Prediction of the penetration rate of antimycotics through the nail plate and their efficacy
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DOI：
10.1111/j.2042-7158.1997.tb06127.x
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发表时间：
1997-09-01
影响因子：
3.3
通讯作者：
Lippold, BC
中科院分区：
文献类型：
--
作者：
Mertin, D;Lippold, BC
与辛醇/水的分配系数相反，渗透性药物的分子大小对人指甲盖和牛蹄角蛋白膜的渗透性有明显的影响。渗透率和分子量之间的关系是建立在完善的理论基础上的。甲板的渗透性与蹄膜的渗透性之间的相关性允许在确定药物透过蹄膜后预测甲渗透性。（阿莫罗芬，联苯苄唑，环吡酮，克霉唑，益康唑，灰黄霉素，酮唑，萘替芬，制霉菌素和托萘酯）通过指甲板的渗透率是基于它们通过蹄膜的渗透率和它们的水溶解度来预测的。根据最大通量和最小抑菌浓度计算了对甲真菌病的有效性系数，因此，阿莫罗芬、环吡酮、益康唑和萘替芬预计对皮肤真菌特别有效，而在仅感染酵母菌的情况下，阿莫罗芬和环吡酮是有希望的。
In contrast to the partition coefficient octanol/water the molecular size of penetrating drugs has a noticeable influence on the permeability of the human nail plate and a keratin membrane from bovine hooves. The relationship between permeability and molecular weight is founded on well-established theories. The correlation between the permeability of the nail plate and that of the hoof membrane allows a prediction of the nail permeability after determination of the drug penetration through the hoof membrane.The maximum flux of ten antimycotics (amorolfine, bifonazole, ciclopirox, clotrimazole, econazole, griseofulvin, ketaconazole, naftifine, nystatin and tolnaftate) through the nail plate was predicted on the basis of their penetration rates through the hoof membrane and their water solubilities. An efficacy coefficient against onychomycoses was calculated from the maximum flux and the minimum inhibitory concentration.Accordingly, amorolfine, ciclopirox, econazole and naftifine are expected to be especially effective against dermatophytes, whereas in the case of an infection with yeasts only, amorolfine and ciclopirox are promising.