Brogard J M, Kopferschmitt J, Arnaud J P, Dorner M, La Villaureix J
Antimicrob Agents Chemother. 1980 Jul;18(1):69-76. doi: 10.1128/AAC.18.1.69.
The biliary elimination of mezlocillin, a new semisynthetic penicillin of the acyl-ureido-penicillin group, was investigated in vitro in rabbit liver preparations and in vivo in humans. Experimentally, mezlocillin recovery in the bile during perfusion of isolted rabbit liver (3 h; n = 5) averaged 20.3% of the administrered dose (10 mg). The mean peak concentration in the bile (758 +/- 129.3 micrograms/ml) was reached between 0.5 and 1 h. Biliary clearance was 169 ml/h. In healthy subjects (n = 5), the concentrations of antibiotic measured in the duodenal fluid during a period of 4 h after intravenous administration of 5 g of mezlocillin ranged between 440 and 637 micrograms/ml. In 10 cholecystectomized patients provided with a T-tube, intramuscular injection of 1 g of mezlocillin resulted in a biliary peak concentration of 295.7 +/- 58.1 micrograms/ml. Mean total amount of antibiotic eliminated in the bile over 12 h corresponded to 2.6% of the administered dose. Assays performed during surgery after intravenous administration of 2 g of mezlocillin (n = 10) showed antibiotic activity of 895 +/- 196 micrograms/ml in the common duct bile and 402 +/- 133 micrograms/ml in the gallbladder bile. These data were compared with the values determined for 11 other beta-lactamines studied under identical conditions.
对新型半合成青霉素酰脲基青霉素类中的美洛西林经兔肝制剂进行体外研究以及在人体进行体内研究，以考察其经胆汁排泄情况。实验中，在离体兔肝灌注期间（3小时；n = 5）胆汁中美洛西林的回收率平均为给药剂量（10毫克）的20.3%。胆汁中的平均峰值浓度（758±129.3微克/毫升）在0.5至1小时之间达到。胆汁清除率为169毫升/小时。在健康受试者（n = 5）中，静脉注射5克美洛西林后4小时内十二指肠液中测得的抗生素浓度在440至637微克/毫升之间。在10例有T形管的胆囊切除患者中，肌肉注射1克美洛西林导致胆汁峰值浓度为295.7±58.1微克/毫升。12小时内经胆汁排泄的抗生素总量平均相当于给药剂量的2.6%。在静脉注射2克美洛西林后手术期间进行的检测（n = 10）显示，胆总管胆汁中的抗生素活性为895±196微克/毫升，胆囊胆汁中的抗生素活性为402±133微克/毫升。将这些数据与在相同条件下研究的其他11种β-内酰胺类药物所确定的值进行了比较。
