Hidaka K, Yamamoto H, Harada S, Katano M, Fujiwara H, Mizoguchi T, Hisatsugu T, Yamaoka K, Kisu T
Department of Surgery, Saga Medical School.
Jpn J Antibiot. 1988 Sep;41(9):1295-303.
Biliary and urinary concentrations and recoveries of 3 different antibiotics (piperacillin (PIPC), cefbuperazone (CBPZ) and cefoperazone (CPZ], after intravenous bolus injection were studied using the crossover method with external cholecystostomies done in order to treat obstructive jaundice due to complete obstruction of the lower biliary tract; the concentrations of antibiotics in bile and urine were determined by means of a high performance liquid chromatography method. Drug concentrations and recoveries in the bile after intravenous injection of these antibiotics were at levels in the order of CPZ greater than CBPZ greater than PIPC. Since our patients were inflicted with various malignancies which made them impaired in terms of biliary excretion of antibiotics, the concentrations of those drugs in the bile were lower than those previously reported by several investigators. However, CBPZ and CPZ showed sufficient levels of excretion into the bile and their amounts were high enough when compared to the value of MIC 80% reported recently against Escherichia coli and Klebsiella pneumoniae, which are known to be main pathogens of biliary system infections. The excretion of CPZ into the bile was invariably found to be 2 times or more as high as the other 2 drugs tested. Concentrations and recoveries of the 3 antibiotics excreted into urine were similar to the cefotaxime excretion, of which into urine had been reported to be excellent. Thus, CBPZ and CPZ appeared to be effective against biliary system infections, even with blockage of antibiotics excretion into the bile.
采用交叉试验方法，对3种不同抗生素（哌拉西林（PIPC）、头孢哌酮舒巴坦（CBPZ）和头孢哌酮（CPZ））在静脉推注后的胆汁和尿液浓度及回收率进行了研究。为治疗因低位胆道完全梗阻所致的梗阻性黄疸，进行了体外胆囊造口术。采用高效液相色谱法测定胆汁和尿液中的抗生素浓度。静脉注射这些抗生素后，胆汁中的药物浓度和回收率依次为CPZ＞CBPZ＞PIPC。由于我们的患者患有各种恶性肿瘤，导致他们的抗生素胆汁排泄功能受损，因此这些药物在胆汁中的浓度低于此前几位研究者报告的浓度。然而，CBPZ和CPZ在胆汁中的排泄水平足够，与最近报道的针对已知为胆道系统感染主要病原体的大肠杆菌和肺炎克雷伯菌的80% MIC值相比，其含量足够高。CPZ在胆汁中的排泄量始终是其他两种受试药物的2倍或更多。3种抗生素在尿液中的浓度和回收率与头孢噻肟的排泄情况相似，据报道头孢噻肟在尿液中的排泄情况良好。因此，即使存在抗生素胆汁排泄受阻的情况，CBPZ和CPZ似乎对胆道系统感染仍有效。
