McColm A A, Shelley E, Ryan D M, Acred P
J Antimicrob Chemother. 1986 Nov;18(5):599-608. doi: 10.1093/jac/18.5.599.
The activity of ceftazidime was examined in a murine model of Klebsiella pneumoniae pneumonia in which the antibiotic was administered subcutaneously 6 h after intranasal infection and then twice daily for the next three days (i.e. seven doses). In a series of experiments using this test, the dose of ceftazidime giving 50% survival relative to controls (SD50) ranged from 1.0-9.0 mg/kg/dose while the dose required to reduce the log10 cfu/lung by 50% (CD50) ranged from 24-64 mg/kg/dose. Ceftazidime was considerably more effective than cefotiam, amoxycillin-clavulanic acid or kanamycin in the test. Pharmacokinetic studies with ceftazidime showed that no differences in respiratory tract penetration existed between uninfected mice and mice infected for 48 h with K. pneumoniae. The percentage penetration of ceftazidime from serum was 73% for pleural fluid, 44% for tracheal fluid, 27% for tracheal wall tissue and 17% for whole lung tissue after a subcutaneous injection of 100 mg/kg. At this dose, ceftazidime remained at supra-MIC concentrations for 2-3 h in all compartments examined.
在肺炎克雷伯菌肺炎小鼠模型中对头孢他啶的活性进行了研究,在鼻内感染后6小时皮下注射该抗生素,然后在接下来的三天里每天注射两次(即七剂)。在一系列使用该试验的实验中,相对于对照组,使存活率达到50%的头孢他啶剂量(SD50)为1.0 - 9.0毫克/千克/剂量,而使每升肺内菌落形成单位(cfu)的对数减少50%所需的剂量(CD50)为24 - 64毫克/千克/剂量。在该试验中,头孢他啶比头孢替安、阿莫西林 - 克拉维酸或卡那霉素有效得多。头孢他啶的药代动力学研究表明,未感染小鼠与感染肺炎克雷伯菌48小时的小鼠在呼吸道穿透方面没有差异。皮下注射100毫克/千克后,头孢他啶在胸腔积液中的血清穿透率为73%,气管液中为44%,气管壁组织中为27%,全肺组织中为17%。在此剂量下,头孢他啶在所有检测隔室中保持高于最低抑菌浓度(MIC)的浓度达2 - 3小时。