Shimamura Tsuyoshi, Miyamae Akiko, Arai Masakazu, Minemura Aya, Nozawa Akira, Kubota Nobuo
R&D Laboratories, POLA PHARMA INC.
Med Mycol J. 2016;57(1):J19-25. doi: 10.3314/mmj.57.J19.
To clarify the character of luliconazole nail solution we have developed, we investigated luliconazole distribution and antifungal activity in nail plate. An in vitro permeation study which measured luliconazole concentration of sliced nail in the transverse direction after treatment of luliconazole nail solution was conducted to investigate for concentration dependency and the influences of nail thickness and treatment duration. When 0.2, 1, 3, 5, and 7.5% luliconazole nail solutions were used, luliconazole was detected in the all the layers of nail and there was a concentration gradient from the dorsal side to deep nail layers. The luliconazole concentration was almost same after 14-day treatment with 5% luliconazole nail solution when using nails of different thicknesses. And we confirmed that concentration of luliconazole into the nail was increased depending on the treatment duration. In zone of inhibition test after 14-day treatment, 5% luliconazole nail solution showed statistically high formation rate of zones of inhibition compared to 8% ciclopirox nail lacquer. Above all, these data suggested that 5% luliconazole nail solution has the potential to show high therapeutic effect for onychomycosis.
为阐明我们研发的卢立康唑指甲溶液的特性，我们研究了卢立康唑在甲板中的分布及抗真菌活性。进行了一项体外渗透研究，在使用卢立康唑指甲溶液处理后，测量横向切片指甲中卢立康唑的浓度，以研究浓度依赖性以及指甲厚度和处理持续时间的影响。当使用0.2%、1%、3%、5%和7.5%的卢立康唑指甲溶液时，在指甲的所有层中均检测到卢立康唑，并且从背侧到指甲深层存在浓度梯度。当使用不同厚度的指甲时，用5%卢立康唑指甲溶液处理14天后，卢立康唑浓度几乎相同。并且我们证实，卢立康唑进入指甲的浓度随处理持续时间而增加。在14天处理后的抑菌圈试验中，与8%环吡酮指甲漆相比，5%卢立康唑指甲溶液显示出统计学上较高的抑菌圈形成率。最重要的是，这些数据表明5%卢立康唑指甲溶液有可能对甲癣显示出高治疗效果。
