Mertin D, Lippold B C
Department of Pharmaceutical Technology, Heinrich-Heine-University, Düsseldorf, Germany.
J Pharm Pharmacol. 1997 Sep;49(9):866-72. doi: 10.1111/j.2042-7158.1997.tb06127.x.
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, ketoconazole, 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.
与辛醇/水分配系数不同，穿透性药物的分子大小对人指甲板和牛蹄角质膜的渗透性有显著影响。渗透性与分子量之间的关系基于已确立的理论。指甲板渗透性与蹄膜渗透性之间的相关性使得在测定药物透过蹄膜的渗透率后能够预测指甲渗透率。根据十种抗真菌药（阿莫罗芬、联苯苄唑、环吡酮、克霉唑、益康唑、灰黄霉素、酮康唑、萘替芬、制霉菌素和托萘酯）透过蹄膜的速率及其水溶性，预测了它们透过指甲板的最大通量。根据最大通量和最小抑菌浓度计算了抗甲真菌病的疗效系数。因此，预计阿莫罗芬、环吡酮、益康唑和萘替芬对皮肤癣菌特别有效，而仅在酵母感染的情况下，阿莫罗芬和环吡酮有望有效。
