Bérubé D, Kirouac D, Croteau D, Bergeron M G, Lebel M
Ecole de Pharmacie, Université Laval, Quebec, Canada.
Antimicrob Agents Chemother. 1988 Aug;32(8):1227-30. doi: 10.1128/AAC.32.8.1227.
In a crossover design study, we compared the plasma bactericidal activities of erythromycin estolate (500 mg) and erythromycin ethylsuccinate (600 mg) after administration of a single oral dose to 12 healthy volunteers. Both erythromycin esters displayed very good plasma bactericidal activities against Streptococcus pneumoniae. The median bactericidal titers produced in plasma against Streptococcus pyogenes and Streptococcus pneumoniae were significantly higher with erythromycin estolate than with the ethylsuccinate ester at both 2 and 8 h after dosing (P less than 0.05 by Student's t test). Both erythromycin esters showed rather weak bactericidal activity against Branhamella catarrhalis; a further look at these results indicated that erythromycin estolate presented 50% of the plasma samples at 2 h with bactericidal titers superior or equal to 1:8, versus 11% for the ethylsuccinate ester. Of the 60 plasma bactericidal activity tests performed against Staphylococcus aureus, only 6 (10%) and 3 (5%) exhibited titers of 1:8 or greater for erythromycin estolate and erythromycin ethylsuccinate, respectively. Clinical trials are warranted in which these products are compared in infections other than Streptococcus pyogenes pharyngitis, for which the clinical superiority of erythromycin estolate has been demonstrated.
在一项交叉设计研究中,我们对12名健康志愿者单次口服给药后无味红霉素(500毫克)和琥乙红霉素(600毫克)的血浆杀菌活性进行了比较。两种红霉素酯对肺炎链球菌均表现出非常好的血浆杀菌活性。给药后2小时和8小时,无味红霉素在血浆中对化脓性链球菌和肺炎链球菌产生的杀菌效价中位数均显著高于琥乙红霉素(经Student t检验,P小于0.05)。两种红霉素酯对卡他莫拉菌的杀菌活性均较弱;进一步观察这些结果表明,无味红霉素在2小时时有50%的血浆样本杀菌效价等于或高于1:8,而琥乙红霉素为11%。在针对金黄色葡萄球菌进行的60次血浆杀菌活性测试中,无味红霉素和琥乙红霉素分别只有6次(10%)和3次(5%)的效价达到或高于1:8。有必要进行临床试验,比较这些产品在除化脓性链球菌咽炎之外的其他感染中的效果,无味红霉素在该疾病中的临床优势已得到证实。