Rohwedder R W, Bergan T, Thorsteinsson S B, Scholl H
Pharma Research Center, Bayer AG, Wuppertal, FRG.
Diagn Microbiol Infect Dis. 1990 Mar-Apr;13(2):127-33. doi: 10.1016/0732-8893(90)90095-d.
This study identified the routes of elimination of ciprofloxacin in two groups of five subjects each: one of healthy volunteers; the other of patients with severe renal failure having mean creatinine clearance of 12 ml/min (range, 8-16 ml/min). Each subject received one dose of 200 mg ciprofloxacin infused intravenously (IV) over 30 min. In an effort to recover the total drug administered, all urine and feces were collected for 7 days following dosing. Blood samples were drawn at set intervals. Serum, urine, and feces were assayed for ciprofloxacin and metabolites by high-pressure liquid chromatography. The ciprofloxacin elimination half-life was 3.9 +/- 0.4 hr in the healthy volunteers and 11.2 +/- 2.5 hr in the patients with severe renal failure. The total 7-day recovery of ciprofloxacin and its metabolites in urine and feces ranged from 74.0% to 114.7% of the dose (mean, 96.3 +/- 14.1%) in normal subjects and from 48.5% to 109.1% (mean, 88.1 +/- 20.9%) in patients. The dose of ciprofloxacin recovered in urine was 65.3 +/- 10.7% in healthy subjects and 19.0 +/- 15.9% in impaired patients (reduction factor, 3.4). In contrast, the dose recovered in feces was 11.4 +/- 2.6% in the group of normal subjects and 37.2 +/- 12.5% in the group of patients with impaired renal function in a 3.3-fold increase.(ABSTRACT TRUNCATED AT 250 WORDS)
本研究确定了环丙沙星在两组受试者(每组五名)中的消除途径:一组为健康志愿者;另一组为重度肾衰竭患者,其平均肌酐清除率为12 ml/分钟(范围为8 - 16 ml/分钟)。每位受试者静脉注射(IV)200 mg环丙沙星,输注时间为30分钟。为了回收所给予的全部药物,给药后7天收集所有尿液和粪便。按设定的时间间隔采集血样。采用高压液相色谱法测定血清、尿液和粪便中的环丙沙星及其代谢物。环丙沙星在健康志愿者中的消除半衰期为3.9±0.4小时,在重度肾衰竭患者中为11.2±2.5小时。环丙沙星及其代谢物在尿液和粪便中的7天总回收率,在正常受试者中为剂量的74.0%至114.7%(平均为96.3±14.1%),在患者中为48.5%至109.1%(平均为88.1±20.9%)。环丙沙星在尿液中回收的剂量,健康受试者为65.3±10.7%,肾功能受损患者为19.0±15.9%(降低系数为3.4)。相比之下,粪便中回收的剂量,正常受试者组为11.4±2.6%,肾功能受损患者组为37.2±12.5%,增加了3.3倍。(摘要截断于250字)