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口服伊曲康唑在足癣角质层水平的药代动力学研究。

Pharmacokinetic investigation of oral itraconazole in stratum corneum level of tinea pedis.

作者信息

Morimoto K, Tanuma H, Kikuchi I, Kusunoki T, Kawana S

机构信息

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

出版信息

Mycoses. 2004 Apr;47(3-4):104-14. doi: 10.1046/j.1439-0507.2003.00952.x.

Abstract

In the present study, the authors administered 100 mg itraconazole (ITCZ) twice daily for a period of 1 week to six patients with hyperkeratotic type tinea pedis, and examined its efficacy, safety profile, and usefulness. ITCZ concentration in stratum corneum was also measured to examine the mobility of the drug into the affected site of planta pedis. ITCZ concentration in the stratum corneum of the affected part was first detected at 1 week after the completion of administration, gradually increased over time, and peaked at 3 weeks, with the sum of ITCZ and hydroxyitraconazole (OH-ITCZ) amounting to 163.7 ng g(-1) on a average. It then gradually decreased to a total sum of 10.3 ng g(-1) on average at 8 weeks following the completion of administration. When compared with the geometric mean minimum inhibitory concentration (MIC) of ITCZ against fresh clinical isolates of dermatophytes (Trichophyton rubrum) (0.06 microg ml(-1)), the stratum corneum ITCZ concentration in this study was 2.1-fold of the geometric mean MIC at 2 weeks following the completion of administration, and 2.4-fold at 4 weeks. Although ITCZ does not produce therapeutic effectiveness (fungistasis) during the period of administration, it starts appearing at 2 weeks after the completion of administration, and after it peaks out at 3-4 weeks, clinical symptoms started improving. These results suggest that satisfying effects can be achieved in a short-term oral ITCZ at a dose of 100 mg twice daily for a period of 1 week in cases of hyperkeratotic type tinea pedis.

摘要

在本研究中,作者对6例角化过度型足癣患者每日两次给予100mg伊曲康唑(ITCZ),持续1周,并检测其疗效、安全性和实用性。还测量了角质层中的ITCZ浓度,以研究药物向足跖受累部位的移动情况。给药结束后1周首次在受累部位角质层中检测到ITCZ浓度,其随时间逐渐升高,并在3周时达到峰值,ITCZ和羟基伊曲康唑(OH-ITCZ)的总量平均为163.7ng g(-1)。然后在给药结束后8周逐渐降至平均总量10.3ng g(-1)。与ITCZ对皮肤癣菌(红色毛癣菌)新鲜临床分离株的几何平均最低抑菌浓度(MIC)(0.06μg ml(-1))相比,本研究中角质层ITCZ浓度在给药结束后2周时为几何平均MIC的2.1倍,4周时为2.4倍。虽然ITCZ在给药期间未产生治疗效果(抑菌作用),但在给药结束后2周开始显现,在3 - 4周达到峰值后,临床症状开始改善。这些结果表明,对于角化过度型足癣病例,每日两次口服100mg ITCZ,持续1周,可在短期内取得满意疗效。

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