Cooper C E, White A R, Slocombe B
SmithKline Beecham Pharmaceuticals, Betchworth, Surrey, UK.
J Antimicrob Chemother. 1991 Jan;27(1):105-15. doi: 10.1093/jac/27.1.105.
An in-vitro kinetic model was used to demonstrate the bactericidal activity of concentrations of temocillin achieved in extravascular body fluids following a 1 g intravenous dosage in man. Concentrations of temocillin attainable in peripheral lymph were bactericidal for ampicillin-resistant strains of Escherichia coli, Enterobacter cloacae and Klebsiella oxytoca. Likewise, concentrations of temocillin achieved in human blister fluid following a 12-hourly dosage regimen were bactericidal for cultures of Ent. cloacae and K. oxytoca which were resistant, respectively, to simulated blister fluid concentrations of cefotaxime and aztreonam. The bactericidal activity of extravascular concentrations of temocillin against these multiresistant, Gram-negative bacteria was a reflection of the beta-lactamase-stability and good pharmacokinetic properties of temocillin.
采用体外动力学模型来证明在人体静脉注射1g剂量后，血管外体液中所达到的替莫西林浓度的杀菌活性。外周淋巴中可达到的替莫西林浓度对大肠杆菌、阴沟肠杆菌和产酸克雷伯菌的氨苄西林耐药菌株具有杀菌作用。同样，在每12小时给药方案后人体水疱液中所达到的替莫西林浓度，对分别对模拟水疱液浓度的头孢噻肟和氨曲南耐药的阴沟肠杆菌和产酸克雷伯菌培养物具有杀菌作用。替莫西林血管外浓度对这些多重耐药革兰氏阴性菌的杀菌活性反映了替莫西林的β-内酰胺酶稳定性和良好的药代动力学特性。
