Shimamura Tsuyoshi, Miyamae Akiko, Imai Ami, Hirayanagi Kozue, Iwanaga Tomoyuki, Kubota Nobuo, Shibuya Kazutoshi
R&D Laboratories, POLA PHARMA INC.
Med Mycol J. 2016;57(4):J141-J147. doi: 10.3314/mmj.16-00020.
Two topical therapeutic agents were approved in Japan from 2015 to 2016, adding new options for onychomycosis therapy in the clinical field. In order to confirm the differences of formulation properties and nail pharmacokinetics between 5% luliconazole solution and 10% efinaconazole solution, drug concentration and antifungal activity in the nail were measured after topical treatment using human nail plates. In the in vitro permeation study, concentration of each drug was measured in the transversely sliced nail after single treatment with the two topical therapeutic agents. The results showed that concentration of luliconazole is higher than that of efinaconazole at all nail layers, differing by 1.7-8.4 times at each measurement point. Next, we examined antifungal activities of each drug in sliced nail after 14-day topical treatment. Mean rates of formation of inhibition zones for 5% luliconazole solution and 10% efinaconazole solution were 71.0% and 12.6%, respectively, and were statistically different. These results show that the two topical therapeutic agents have different properties, and suggest that 5% luliconazole solution has good nail permeation and retention characteristics. Moreover, luliconazole was found to retain enough antifungal activity in the nail plate against Trichophyton spp. after treatment with the topical agent.
2015年至2016年,日本批准了两种局部治疗药物,为临床领域的甲真菌病治疗增加了新的选择。为了确认5%卢立康唑溶液和10%艾氟康唑溶液在制剂特性和指甲药代动力学方面的差异,使用人指甲板进行局部治疗后,测量了指甲中的药物浓度和抗真菌活性。在体外渗透研究中,用这两种局部治疗药物单次治疗后,测量横向切片指甲中每种药物的浓度。结果表明,在所有指甲层中,卢立康唑的浓度均高于艾氟康唑,每个测量点的差异为1.7至8.4倍。接下来,我们检查了局部治疗14天后切片指甲中每种药物的抗真菌活性。5%卢立康唑溶液和10%艾氟康唑溶液的平均抑菌圈形成率分别为71.0%和12.6%,且具有统计学差异。这些结果表明,这两种局部治疗药物具有不同的特性,并表明5%卢立康唑溶液具有良好的指甲渗透和保留特性。此外,在用局部药物治疗后,发现卢立康唑在指甲板中对毛癣菌属保留了足够的抗真菌活性。