Brogard J M, Arnaud J P, Dauchel J, Pinget M, Lavillaureix J
Pathol Biol (Paris). 1979 Sep;27(7):403-10.
Biliary excretion of penicillin G was studied experimentally by perfusion of isolated rabbit liver. Under these conditions, bile recovery accounted for 5% of the amount of penicillin G added to the perfusing blood (10 mg); peak biliary level averaged 135.3 micrograms/ml. In man after intravenous administration of a 599 mg dose of penicillin G (1 MU) to patients provided with T-tube drainage (n = 10), the maximum biliary concentration averaged 18.0 +/- 8.0 micrograms/ml at 2 hours; biliary recovery of penicillin G accounts for 0.12% of the administered dose. The excretion of penicillin G in the juice collected through duodenal tubing in normal subjects averaged 0.07% of the administered dose (599 mg IV). Per-operative assays showed that the concentration determined at 1 hour after intravenous administration of the drug (599 mg) in the gallbladder bile (45.7 +/- 16.7 micrograms/ml) and common duct bile (93.5 +/- 16.3 micrograms/ml) were definitely higher (4.5--9 times) than the serum levels measured simultaneously. The biliary excretion of penicillin G is compared with the biliary elimination of a certain number of beta-lactam derivatives studied under the same conditions (ampicillin, metampicillin, carbenicillin, cefalothin, cefaloridine, cefacetrile, cefalexin, cefazolin).
通过对离体兔肝进行灌注，对青霉素G的胆汁排泄进行了实验研究。在这些条件下，胆汁回收率占灌注血液中添加的青霉素G量（10毫克）的5%；胆汁峰值水平平均为135.3微克/毫升。在对10例置有T形管引流的患者静脉注射599毫克剂量的青霉素G（1MU）后，2小时时胆汁最大浓度平均为18.0±8.0微克/毫升；青霉素G的胆汁回收率占给药剂量的0.12%。正常受试者通过十二指肠管收集的汁液中青霉素G的排泄量平均占给药剂量（静脉注射599毫克）的0.07%。术中检测显示，静脉注射药物（599毫克）1小时后胆囊胆汁（45.7±16.7微克/毫升）和胆总管胆汁（93.5±16.3微克/毫升）中的浓度明显高于（4.5至9倍）同时测量的血清水平。将青霉素G的胆汁排泄与在相同条件下研究的一定数量的β-内酰胺衍生物（氨苄西林、甲氨苄西林、羧苄西林、头孢噻吩、头孢噻啶、头孢乙腈、头孢氨苄、头孢唑林）的胆汁清除情况进行了比较。
