Boon R J, Beale A S, Sutherland R
J Antimicrob Chemother. 1986 May;17 Suppl C:41-6. doi: 10.1093/jac/17.suppl_c.41.
The therapeutic effects produced by ticarcillin plus clavulanic acid were compared with those of ticarcillin and clavulanic acid separately against infections in the mouse caused by beta-lactamase-producing bacteria. The infections studied included a pneumonia model, a local tissue infection and pyelonephritis. The distribution of ticarcillin and clavulanic acid in infected animals was evaluated by measurement of the concentrations of the substances present at sites of infection. The results showed that both ticarcillin and clavulanic acid were well-distributed in the mouse and at the doses employed were present at the sites of infection at concentrations of the same order as those obtained in man after administration of ticarcillin/clavulanic acid formulations (Timentin). The protection of ticarcillin by clavulanic acid from inactivation by the beta-lactamases produced in vivo by Bacteroides fragilis, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa was demonstrated by the pronounced bactericidal effects produced by the ticarcillin/clavulanic acid combination against the ticarcillin-refractory infections studied.
将替卡西林加克拉维酸产生的治疗效果与替卡西林和克拉维酸单独使用时针对由产β-内酰胺酶细菌引起的小鼠感染的治疗效果进行了比较。所研究的感染包括肺炎模型、局部组织感染和肾盂肾炎。通过测量感染部位存在的物质浓度来评估替卡西林和克拉维酸在感染动物体内的分布。结果表明,替卡西林和克拉维酸在小鼠体内分布良好,在所使用的剂量下,感染部位的浓度与给予替卡西林/克拉维酸制剂(特美汀)后人体中获得的浓度处于同一数量级。替卡西林/克拉维酸组合对所研究的对替卡西林耐药的感染产生了显著的杀菌作用,这证明了克拉维酸对替卡西林具有保护作用,使其免受脆弱拟杆菌、大肠杆菌、肺炎克雷伯菌和铜绿假单胞菌在体内产生的β-内酰胺酶的灭活。