Schmitt H J, Andrade J, Edwards F, Niki Y, Bernard E, Armstrong D
Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, New York.
Eur J Clin Microbiol Infect Dis. 1990 Nov;9(11):832-5. doi: 10.1007/BF01967386.
In a model of bronchopulmonary aspergillosis terbinafine did not improve survival of experimental animals in doses up to 80 mg/kg/day despite adequate lung concentrations. Pretreatment and aerosolization of the compound were also ineffective. Terbinafine was markedly less active in vitro when serum was used instead of Yeast-Nitrogen-Glucose-broth. It is concluded that a lack of bioavailability in the presence of serum may explain the lack of activity of terbinafine in experimental aspergillosis.
在支气管肺曲霉病模型中,尽管肺组织中有足够的药物浓度,但高达80毫克/千克/天剂量的特比萘芬并不能提高实验动物的生存率。该化合物的预处理和气雾给药同样无效。当使用血清而非酵母氮葡萄糖肉汤时,特比萘芬在体外的活性明显降低。由此得出结论,在有血清存在的情况下生物利用度不足可能解释了特比萘芬在实验性曲霉病中缺乏活性的原因。