Noguchi Y, Taguchi M, Takasugi M, Sakamoto T, Matsumoto K
Jpn J Antibiot. 1983 Dec;36(12):3405-11.
Serum concentrations of dibekacin (DKB), sisomicin (SISO) and gentamicin (GM) were measured in 3 rabbits after intratracheal administration through the transtracheal teflon tube. The peak serum levels (average) were 106 micrograms/ml (administrated 100 mg DKB for injection), 148 micrograms/ml (administrated 100 mg DKB solution), 166 micrograms/ml (administrated 100 mg SISO solution) and 80 micrograms/ml (administrated 80 mg GM solution). Serum concentrations and urine excretions of DKB were measured in 3 volunteers after aerosol administration using ultrasonic nebulizer. The peak serum levels (average) were 4.6 micrograms/ml (administrated 100 mg DKB for injection) and 3.1 micrograms/ml (administrated 100 mg DKB solution). The urine excretions (average) were 3.7 mg and 4.3 mg respectively during 6 hours. Before and after administration of DKB aerosol the spirogram and flow-volume curve were examined in the volunteers. But the examinations showed no changes. Sputum concentrations were measured in 1 patient with chronic bronchobronchiolitis after administration of DKB aerosols using the ultrasonic nebulizer. The highest sputum concentration was acquired immediately after nebulization and the sputum levels decreased gradually while time passed. Six patients with the lower respiratory tract infections were treated with DKB aerosol therapy and the utility rate was 80%.
通过经气管聚四氟乙烯管对3只兔子进行气管内给药后,测定了双去氧卡那霉素(DKB)、西索米星(SISO)和庆大霉素(GM)的血清浓度。血清峰值水平(平均值)分别为106微克/毫升(注射100毫克DKB)、148微克/毫升(给予100毫克DKB溶液)、166微克/毫升(给予100毫克SISO溶液)和80微克/毫升(给予80毫克GM溶液)。在3名志愿者使用超声雾化器进行气雾剂给药后,测定了DKB的血清浓度和尿排泄量。血清峰值水平(平均值)分别为4.6微克/毫升(注射100毫克DKB)和3.1微克/毫升(给予100毫克DKB溶液)。6小时内尿排泄量(平均值)分别为3.7毫克和4.3毫克。在志愿者吸入DKB气雾剂前后,检查了肺量图和流量-容积曲线。但检查结果未显示有变化。对1例慢性细支气管炎患者使用超声雾化器吸入DKB气雾剂后,测定了痰液浓度。雾化后立即获得最高痰液浓度,随着时间推移,痰液浓度逐渐下降。6例下呼吸道感染患者接受了DKB气雾剂治疗,有效率为80%。