Ginsburg C M, McCracken G H, Clahsen J, Zweighaft T
Rev Infect Dis. 1981 Jan-Feb;3(1):117-20. doi: 10.1093/clinids/3.1.117.
The pharmacokinetics of ampicillin and two preparations of bacampicillin, Veegum and microcapsules, were studied in 24 infants and children. For bacampicillin, mean peak concentrations of 7.6 and 14.4 micrograms/ml were found in the sera of fasting patients after administration of 27.8 mg of drug/ml in Veegum and microcapsular suspensions, respectively. Bacampicillin (27.8 mg/kg) and ampicillin (25 mg/kg) were compared in crossover fashion in 21 of the 24 children. Although the dosage of bacampicillin was 25% smaller on an equimolar basis than that of ampicillin, drug concentrations in serum were consistently higher with bacampicillin than with ampicillin; the differences were statistically significant 0.5, 1, and 2 hr after administration. The bioavailability of bacampicillin was two-to threefold greater than that of ampicillin. Urinary concentrations of drug were twofold higher with bacampicillin than with ampicillin. The proportion of saliva samples with detectable antimicrobial activity was similar among patients who received bacampicillin (31%) and those who received ampicillin (25%); however, the mean salivary concentrations 2 and 4 hr after administration of bacampicillin were substantially higher than those after ampicillin.
在24名婴幼儿和儿童中研究了氨苄西林以及巴卡西林的两种制剂（硅酸镁铝制剂和微囊制剂）的药代动力学。对于巴卡西林，在空腹患者服用硅酸镁铝制剂和微囊悬浮液中每毫升含27.8毫克药物后，血清中的平均峰值浓度分别为7.6微克/毫升和14.4微克/毫升。在24名儿童中的21名儿童身上以交叉方式比较了巴卡西林（27.8毫克/千克）和氨苄西林（25毫克/千克）。虽然按等摩尔计算巴卡西林的剂量比氨苄西林小25%，但巴卡西林的血清药物浓度始终高于氨苄西林；给药后0.5小时、1小时和2小时，差异具有统计学意义。巴卡西林的生物利用度比氨苄西林高两到三倍。巴卡西林的尿液药物浓度比氨苄西林高两倍。接受巴卡西林的患者（31%）和接受氨苄西林的患者（25%）中具有可检测到抗菌活性的唾液样本比例相似；然而，服用巴卡西林后2小时和4小时的平均唾液浓度明显高于服用氨苄西林后的浓度。
