Hunter P A, Rolinson G N, Witting D A
Antimicrob Agents Chemother. 1973 Sep;4(3):285-93. doi: 10.1128/AAC.4.3.285.
Against experimental infections in mice with strains of Escherichia coli and with Proteus mirabilis, amoxycillin was found to be more active than ampicillin both by the oral and the subcutaneous routes of administration. With the bacteria used in these experiments, ampicillin and amoxycillin showed the same minimal inhibitory concentrations and, after subcutaneous administration, the levels of ampicillin and amoxycillin in the plasma and tissue homogenate were also similar. However, counts of the number of viable bacteria present in the infected tissue showed that amoxycillin exerted a more rapid and a more marked bactericidal effect than did ampicillin, and this could be correlated with the difference in therapeutic effect. When given by mouth, amoxycillin was more completely absorbed than ampicillin and gave rise to higher levels of antibiotic in the plasma. This may have accounted in part for the difference in therapeutic activity seen when these penicillins were given by the oral route. However, when appropriate oral dosages of ampicillin and amoxycillin were used so as to achieve similar levels of antibiotic in the plasma and tissue homogenate, amoxycillin was again found to exert a more marked bactericidal effect than did ampicillin, and this was accompanied by greater therapeutic activity. In experiments in vitro, amoxycillin also showed a more rapid bactericidal effect than did ampicillin against the bacteria which were used to produce the experimental infections.
在针对小鼠进行的大肠杆菌菌株和奇异变形杆菌的实验性感染中,发现阿莫西林无论是经口服还是皮下给药,其活性均高于氨苄西林。对于这些实验中所使用的细菌,氨苄西林和阿莫西林显示出相同的最低抑菌浓度,并且在皮下给药后,血浆和组织匀浆中的氨苄西林和阿莫西林水平也相似。然而,对感染组织中活菌数量的计数表明,阿莫西林比氨苄西林发挥出更快速且更显著的杀菌作用,这与治疗效果的差异相关。口服时,阿莫西林比氨苄西林吸收更完全,在血浆中产生更高的抗生素水平。这可能部分解释了这些青霉素经口服给药时所观察到的治疗活性差异。然而,当使用适当的口服剂量的氨苄西林和阿莫西林以在血浆和组织匀浆中达到相似的抗生素水平时,再次发现阿莫西林比氨苄西林发挥出更显著的杀菌作用,并且伴随着更大的治疗活性。在体外实验中,对于用于产生实验性感染的细菌,阿莫西林也比氨苄西林显示出更快速的杀菌作用。