Nishimura T, Tabuki K, Takashima T, Takagi M
Jpn J Antibiot. 1983 Apr;36(4):838-48.
The authors have carried out the laboratory and clinical studies of T-1982 (cefbuperazone). The results were as follows: The sensitivity was estimated by the plate dilution method on 28 strains of S. aureus 26 strains of E. coli, 27 strains of K. pneumoniae, 25 strains of S. marcescens and 14 strains of Proteus sp. isolated from patients. The distribution of susceptibility of S. aureus was 1.25-25 micrograms/ml and the peak of distribution was 12.5 micrograms/ml. The strains of 84.6% of E. coli were inhibited at concentration of less than 0.39 micrograms/ml. The strains of 77.8% of K. pneumoniae were inhibited at concentration of less than 0.2 microgram/ml. The strains of 96% of S. marcescens was inhibited at concentration of less than 3.13 micrograms/ml. The distribution of susceptibility of Proteus sp. was 0.39-25 micrograms/ml. T-1982 was given to intravenous administration for 5 minutes and drip infusion for 30 minutes a single dose of 20 mg/kg of T-1982 to 2 and 2 children respectively. After intravenous administration of T-1982, the mean serum level was peak 88.4 +/- 8.7 micrograms/ml at 15 minutes, 52.5 +/- 2.7 micrograms/ml at 1 hour, 4.6 +/- 0.15 micrograms/ml at 6 hours respectively. Half-life was 89 minutes. And after drip infusion of T-1982, the mean serum level was 75.5 +/- 3.5 micrograms/ml at 30 minutes and 3.1 +/- 0.6 micrograms/ml at 6.5 hours respectively. Half-life was 82 minutes. The mean urinary excretion rate was 94.7%, 57.4 +/- 11.0% up to 6 hours after intravenous administration and drip infusion respectively. T-1982 was effective in 13 cases out of 13 cases with bacterial infections. No side effects were observed except for 1 case with elevation of serum GOT, 1 case with elevation of serum GPT and 2 cases with eosinophilia.
作者进行了T - 1982(头孢布宗)的实验室和临床研究。结果如下:采用平板稀释法对从患者分离出的28株金黄色葡萄球菌、26株大肠杆菌、27株肺炎克雷伯菌、25株粘质沙雷氏菌和14株变形杆菌进行敏感性评估。金黄色葡萄球菌的药敏分布为1.25 - 25微克/毫升,分布峰值为12.5微克/毫升。84.6%的大肠杆菌菌株在浓度低于0.39微克/毫升时受到抑制。77.8%的肺炎克雷伯菌菌株在浓度低于0.2微克/毫升时受到抑制。96%的粘质沙雷氏菌菌株在浓度低于3.13微克/毫升时受到抑制。变形杆菌的药敏分布为0.39 - 25微克/毫升。分别对2名儿童和2名儿童静脉注射T - 1982 5分钟,然后滴注30分钟,单剂量为20毫克/千克T - 1982。静脉注射T - 1982后,平均血清水平在15分钟时达到峰值88.4±8.7微克/毫升,1小时时为52.5±2.7微克/毫升,6小时时为4.6±0.15微克/毫升。半衰期为89分钟。滴注T - 1982后,平均血清水平在30分钟时为75.5±3.5微克/毫升,6.5小时时为3.1±0.6微克/毫升。半衰期为82分钟。静脉注射和滴注后至6小时的平均尿排泄率分别为94.7%、57.4±11.0%。13例细菌感染患者中,T - 1982治疗有效13例。除1例血清谷草转氨酶升高、1例血清谷丙转氨酶升高和2例嗜酸性粒细胞增多外,未观察到副作用。