Department of Pharmaceutical Sciences, University of Pisa, Pisa, Italy.
J Eur Acad Dermatol Venereol. 2013 Feb;27(2):e153-8. doi: 10.1111/j.1468-3083.2012.04529.x. Epub 2012 Mar 26.
In a previous study a new hydrosoluble nail lacquer (P-3051) containing 8% ciclopirox (CPX) showed higher nail penetration compared to a water-insoluble 5% amorolfine (MRF) lacquer. To our knowledge, in vivo human data on a similar topic are not available.
To compare fingernail penetration of P-3051 with that of MRF reference in humans and to evaluate their predicted efficacy against Trichophyton rubrum and Candida parapsilosis.
Single centre, randomized, multiple dose, open label, within subjects study. Test and reference were self-applied to all fingernails of either hand for 28 days. At baseline and after 15 and 25 days, the nail free edge was collected for analysis. Efficiency coefficients were calculated for T. rubrum and C. parapsilosis as ratios of nail concentration/minimum inhibitory concentration. The coefficients were classified as very high, high or poor.
Nail concentrations after 15 days were 2.82 ± 0.58 μg/mg for CPX and 0.64 ± 0.11 μg/mg for MRF. At day 25 there was a non-significant decline (1.85 ± 0.31 μg/mg, P = 0.077) for CPX and a highly significant (0.13 ± 0.03 μg/mg, P = 0.0002) 80% decline for MRF. Efficiency coefficients were very high/high in all subjects treated with P-3051 against both T. rubrum and C. parapsilosis; they were significantly lower for MRF reference against both pathogens at both observation points.
P-3051 exhibited better penetration and higher predicted efficacy after in vivo multiple application to human fingernails when compared to MRF reference. These in vivo data are in good agreement with our previous in vitro study.
在之前的一项研究中,一种新的水溶性指甲漆(P-3051),含有 8%环吡酮(CPX),与不溶于水的 5%阿莫罗芬(MRF)漆相比,显示出更高的指甲穿透力。据我们所知,目前尚无类似主题的人体体内数据。
比较 P-3051 与 MRF 参考制剂在人体指甲中的穿透情况,并评估它们对红色毛癣菌和近平滑念珠菌的预测疗效。
单中心、随机、多剂量、开放性、自身对照研究。试验和参考制剂在 28 天内每天自行涂抹于双手的所有指甲。在基线以及第 15 天和第 25 天,采集指甲游离缘进行分析。针对红色毛癣菌和近平滑念珠菌,计算效率系数作为指甲浓度/最低抑菌浓度的比值。根据比值将系数分为很高、高或差。
第 15 天时 CPX 的指甲浓度为 2.82±0.58μg/mg,MRF 为 0.64±0.11μg/mg。第 25 天时 CPX 呈非显著性下降(1.85±0.31μg/mg,P=0.077),而 MRF 则呈高度显著性下降(0.13±0.03μg/mg,P=0.0002),下降 80%。所有接受 P-3051 治疗的患者,其指甲对红色毛癣菌和近平滑念珠菌的效率系数均很高或很高;而 MRF 参考制剂在两个观察点的所有患者中对这两种病原体的效率系数均显著较低。
与 MRF 参考制剂相比,P-3051 在多次应用于人体指甲后的体内穿透性和预测疗效更好。这些体内数据与我们之前的体外研究结果一致。