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临床使用配方中的拉托康唑对豚鼠实验性皮肤癣菌病的治疗效果。

Therapeutic efficacy of latoconazole in formulations of clinical use on experimental dermatophytosis in guinea pigs.

作者信息

Oka H, Niwano Y, Ohmi T, Tanaka T, Uchida M, Yamaguchi H

机构信息

Pharmaceutical Research Institute, Nihon Nohyaku Co., Ltd., Osaka, Japan.

出版信息

Arzneimittelforschung. 1992 Mar;42(3):345-9.

PMID:1497697
Abstract

Therapeutic efficacy of clinical dosage forms of latoconazole (NND-318, CAS 101530-10-3), related compound of ketene dithioacetals with an imidazole ring, was examined on two experimental tinea models: a recently developed tinea pedis model and a conventional tinea corporis model in guinea pigs. The efficacy of the dosage forms was estimated on the basis of the rate of fungus-positive skin cultures and/or the score of skin lesions, and was compared to the other antifungal agents, bifonazole, clotrimazole and tolnaftate. While these reference agents exhibited curative effect on the tinea corporis model, the tinea pedis model was considerably resistant to the therapeutic treatment of the agents. The cream preparation and solution of lactoconazole at concentrations of more than 0.25% were highly effective in either tinea models, and at concentrations of more than 1%, lactoconazole achieved complete mycological cure. These results suggest that 1% of lactonazole is an optimal concentration for clinical use.

摘要

拉考康唑(NND - 318,CAS 101530 - 10 - 3)是一种具有咪唑环的烯酮二硫代缩醛类相关化合物,其临床剂型在两种实验性癣病模型上进行了治疗效果研究:一种是最近开发的足癣模型,另一种是豚鼠传统体癣模型。基于真菌阳性皮肤培养率和/或皮肤损伤评分来评估剂型的疗效,并与其他抗真菌药物联苯苄唑、克霉唑和特比萘芬进行比较。虽然这些参比药物在体癣模型上显示出治疗效果,但足癣模型对这些药物的治疗相当耐药。浓度超过0.25%的拉考康唑乳膏制剂和溶液在两种癣病模型中均具有高效性,浓度超过1%时,拉考康唑实现了完全真菌学治愈。这些结果表明,1%的拉考康唑是临床使用的最佳浓度。

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