Baier R, Puppel H, Zelder O, Zehner R
Arzneimittelforschung. 1981;31(5):857-61.
9 patients (6 female, 3 male) with either cholelithiasis or choledocholithiasis submitted to cholecystectomy were studied during the postoperative period. Sodium 6-[D-(--)-alpha-(4-ethyl-2,3-dioxo-1-piperazinylcarbonylamino)-alpha-phenyl-ace tamido]penicillinate (piperacillin) was administered in single i.v. doses of 2 and 4 g on the 4th and 6th postoperative days. Serum samples were taken at intervals of 20 min over a period of 3 h post injection and bile was collected via T-tube drainage in 20-min periods also for 180 min. The total urine outputs were collected for the periods 0--6 h, 6--12 h and 12--24 h after administration of the drug. The maximum concentration of piperacillin in the bile was observed 60--120 min post administration. The values in the bile were found to exceed the corresponding serum concentrations 30--40fold. Within 3 h 9.6 (+/- 6.5)% and 13.4 (+/- 5.0)% were eliminated in the bile after 2 and 4 g injections, respectively. The percentage of the administered drug excreted in the urine within 24 h was 56.3% (2 g i.v.) and 66.0% (4 g i.v.).
对9例接受胆囊切除术的胆石症或胆总管结石患者（6例女性，3例男性）进行了术后研究。在术后第4天和第6天，静脉注射单剂量2克和4克的6-[D-(-)-α-(4-乙基-2,3-二氧代-1-哌嗪基羰基氨基)-α-苯基-乙酰氨基]青霉素钠（哌拉西林）。注射后3小时内每隔20分钟采集血清样本，并通过T型管引流在20分钟时间段内收集胆汁，持续180分钟。给药后0至6小时、6至12小时和12至24小时收集总尿量。给药后60至120分钟观察到胆汁中哌拉西林的最大浓度。发现胆汁中的值超过相应血清浓度30至40倍。注射2克和4克后，3小时内分别有9.6（±6.5）%和13.4（±5.0）%在胆汁中被清除。24小时内尿液中排泄的给药药物百分比分别为56.3%（静脉注射2克）和66.0%（静脉注射4克）。
