Ghibellini Giulia, Vasist Lakshmi S, Hill Terence E, Heizer William D, Kowalsky Richard J, Brouwer Kim L R
School of Pharmacy, University of North Carolina at Chapel hill, Chapel Hill, NC, USA.
Br J Clin Pharmacol. 2006 Sep;62(3):304-8. doi: 10.1111/j.1365-2125.2006.02662.x.
To evaluate the applicability of a novel method to determine the biliary excretion of piperacillin.
Healthy volunteers were administered piperacillin i.v. Duodenal aspirates were collected via a custom-made oroenteric catheter; blood and urine also were collected. Gallbladder ejection fraction (EF) was determined by gamma scintigraphy and pharmacokinetic parameters were calculated using noncompartmental analysis.
The fraction of the piperacillin dose excreted unchanged into bile was 1.1 +/- 0.3% (biliary clearance corrected for EF was 0.032 +/- 0.008 ml min(-1) kg(-1)).
This methodology can be used to determine reliably the biliary clearance of drugs that are excreted only marginally into bile. Normalization of biliary clearance for EF significantly reduces intersubject variability of this parameter.
评估一种测定哌拉西林胆汁排泄的新方法的适用性。
对健康志愿者静脉注射哌拉西林。通过定制的口腔肠道导管收集十二指肠抽吸物；同时收集血液和尿液。通过γ闪烁显像法测定胆囊射血分数（EF），并使用非房室分析计算药代动力学参数。
未改变排泄入胆汁的哌拉西林剂量分数为1.1±0.3%（经EF校正的胆汁清除率为0.032±0.008 ml·min⁻¹·kg⁻¹）。
该方法可用于可靠地测定仅少量排泄入胆汁的药物的胆汁清除率。对EF进行胆汁清除率标准化可显著降低该参数在受试者间的变异性。
