Rozencweig M, Staquet M, Klastersky J
Clin Pharmacol Ther. 1976 May;19(5 Pt 1):592-7. doi: 10.1002/cpt1976195part1592.
Single equimolar oral doses of bacampicillin and ampicillin were given to 9 healthy subjects on a crossover randomized basis. Data were interpreted in terms of a 3-compartment pharmacokinetic open model. Intestinal absorption of bacampicillin was found to be faster and more complete than that of ampicillin, yielding an increase in bioavailability of 30% to 40% as measured by the area under serum levels curve, the urinary excretion and absorption rate constants. After the administration of bacampicillin, much higher and sharper peaks were achieved in the serum and in the "tissue" water than after the administration of ampicillin. The maximum bactericidal dilution (MBD) of the serum samples taken 1 hr after the administration of the antibiotics against 10 strains of Diplococcus pneumoniae was higher following bacampicillin (p less than 0.01), as was the MBD of the 0 to 2 hr urine specimens against 10 strains of Escherichia coli. Further clinical trials are required to accurately assess the possible greater therapeutic effectiveness of bacampicillin than of ampicillin.
在交叉随机的基础上,给9名健康受试者口服单剂量等摩尔的巴卡西林和氨苄西林。数据根据三室药代动力学开放模型进行解释。发现巴卡西林的肠道吸收比氨苄西林更快且更完全,通过血清水平曲线下面积、尿排泄和吸收速率常数测量,其生物利用度提高了30%至40%。服用巴卡西林后,血清和“组织”水中的峰值比服用氨苄西林后更高且更尖。服用抗生素1小时后采集的血清样本对10株肺炎双球菌的最大杀菌稀释度(MBD),巴卡西林组更高(p小于0.01),0至2小时尿液样本对10株大肠杆菌的MBD也是如此。需要进一步的临床试验来准确评估巴卡西林可能比氨苄西林具有更大的治疗效果。