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口服特比萘芬治疗角化过度型足癣的有效性及药代动力学研究

Usefulness and pharmacokinetic study of oral terbinafine for hyperkeratotic type tinea pedis.

作者信息

Kikuchi Izumi, Tanuma Hiroyuki, Morimoto Kensuke, Kawana Seiji

机构信息

Department of Dermatology, Nippon Medical School, Tokyo, Japan.

出版信息

Mycoses. 2008 Jan;51(1):7-13. doi: 10.1111/j.1439-0507.2007.01438.x.

Abstract

To study and establish an optimal administration method of oral antifungal, terbinafine (TBF), for hyperkeratotic type tinea pedis, from the pharmacokinetic point of view, 20 patients with hyperkeratotic type tinea pedis were given TBF 125 mg once daily for 4 weeks and observed over time for improvement in dermatological symptoms and mycological efficacy. Targeting five of the patients, TBF concentration in the stratum corneum was measured using the liquid chromatography/tandem mass spectrometry (LC-MS/MS) method. TBF was detected in the stratum corneum of the sole 1 week after beginning the treatment in some cases and reached its peak 1 week after the completion of the treatment with a concentration of 247.8 ng g(-1), which was approximately more than 50 times higher than its minimal inhibitory concentration against dermatophytes. TBF was not detected at 8 weeks post-treatment, although its concentration was 50.73 ng g(-1) at 6 weeks post-treatment. Its effectiveness rate (effective + markedly effective) was 95% (19/20) with no adverse reactions, including abnormal changes in the laboratory test values, in any patient. These results suggest that TBF is a useful drug to treat hyperkeratotic tinea pedis from the pharmacokinetic point of view.

摘要

为了从药代动力学角度研究并建立治疗角化过度型足癣的口服抗真菌药物特比萘芬(TBF)的最佳给药方法,20例角化过度型足癣患者每日一次服用125mg TBF,持续4周,并随时间观察皮肤症状改善情况及真菌学疗效。选取其中5例患者,采用液相色谱/串联质谱(LC-MS/MS)法测定角质层中的TBF浓度。部分病例在开始治疗1周后在足底角质层中检测到TBF,治疗结束1周后达到峰值,浓度为247.8 ng g(-1),约为其对皮肤癣菌最小抑菌浓度的50倍以上。治疗后8周未检测到TBF,尽管治疗后6周时其浓度为50.73 ng g(-1)。其有效率(显效+有效)为95%(19/20),所有患者均未出现不良反应,包括实验室检查值的异常变化。这些结果表明,从药代动力学角度来看,TBF是治疗角化过度型足癣的有效药物。

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