Pollak Richard A, Siu William J Jo, Tatsumi Yoshiyuki, Pillai Radhakrishnan
San Antonio Podiatry Associates, San Antonio, TX 78229, USA.
Dow Pharmaceutical Sciences, a Division of Valeant Pharmaceuticals North America LLC, Petaluma, CA 94954, USA.
J Fungi (Basel). 2015 Jul 3;1(2):107-114. doi: 10.3390/jof1020107.
To provide an adequate therapeutic effect against onychomycosis, it has been suggested that topical drugs should have two properties: drug permeability through the nail plate and into the nail bed, and retention of their antifungal activity in the disease-affected areas. Only recently has the importance of other delivery routes (such as subungual) been discussed. Efinaconazole has been shown to have a more potent antifungal activity than the most commonly used onychomycosis treatments. The low keratin affinity of efinaconazole contributes to its effective delivery through the nail plate and retention of its antifungal activity. Its unique low surface tension formulation provides good wetting properties affording drug delivery both through and under the nail. High antifungal drug concentrations have been demonstrated in the nail of onychomycosis patients, and effectiveness of efinaconazole topical solution, 10% confirmed in two large well-controlled multicenter Phase 3 clinical studies in patients with mild-to-moderate disease.
为了提供足够的治疗甲真菌病的效果,有人提出局部用药应具备两个特性:药物透过甲板进入甲床的通透性,以及在患病区域保持其抗真菌活性。直到最近才开始讨论其他给药途径(如甲下给药)的重要性。已证明艾氟康唑比最常用的甲真菌病治疗药物具有更强的抗真菌活性。艾氟康唑对角蛋白的低亲和力有助于其有效透过甲板并保持抗真菌活性。其独特的低表面张力配方具有良好的湿润特性,可使药物透过指甲并在指甲下方传递。在甲真菌病患者的指甲中已证明有高浓度的抗真菌药物,在两项针对轻至中度疾病患者的大型、严格对照的多中心3期临床研究中证实了10%的艾氟康唑外用溶液的有效性。