Brogard J M, Jehl F, Monteil H, Blickle J F, Arnaud J P
Drugs Exp Clin Res. 1987;13(2):105-14.
During a 3-h perfusion of five isolated rabbit liver preparations, 1.4% of 10 mg of ceftazidime added to the circulating blood was eliminated in the bile and 0.9% was metabolized or inactivated in the liver. Five normal subjects were given 2 g of ceftazidime intravenously; antibiotic concentration in the aspirated duodenal fluid rose progressively during the 4 h of the investigational period to a maximal mean level of 21.3 +/- s.e.m. 9.2 micrograms/ml and 0.05% of the dose given was recovered during this period. The same dose was given to 12 cholecystectomized patients fitted with a Kehr drain. An average peak value of 36.3 +/- 4.0 micrograms/ml was reached in the collected bile during the second hour after drug administration. The 12-h biliary recovery was 0.21% of the dose given. Ceftazidime concentrations in choledochal and gallbladder bile sampled peroperatively in 10 patients 1 h after intravenous administration of 2 g of ceftazidime were 78.3 +/- 12.0 and 17.9 +/- 7.5 micrograms/ml respectively. These data compare favourably with the results of the authors' studies on the biliary elimination of 15 other beta-lactams and are consistent with a possible beneficial effect of ceftazidime in the treatment of biliary tract infections.
在对5个离体兔肝标本进行3小时灌注期间,添加到循环血液中的10毫克头孢他啶有1.4%经胆汁排出,0.9%在肝脏中代谢或失活。5名正常受试者静脉注射2克头孢他啶;在研究期的4小时内,抽取的十二指肠液中的抗生素浓度逐渐升高,最高平均水平达到21.3±标准误9.2微克/毫升,在此期间回收的剂量占给药剂量的0.05%。对12名装有凯尔引流管的胆囊切除患者给予相同剂量。给药后第2小时,收集的胆汁中平均峰值达到36.3±4.0微克/毫升。12小时胆汁回收率为给药剂量的0.21%。10名患者静脉注射2克头孢他啶1小时后,术中采集的胆总管和胆囊胆汁中的头孢他啶浓度分别为78.3±12.0和17.9±7.5微克/毫升。这些数据与作者对其他15种β-内酰胺类药物胆汁排泄的研究结果相比很有利,并且与头孢他啶在治疗胆道感染中可能产生的有益作用一致。