Brogard J M, Jehl F, Monteil H, Adloff M, Blickle J F, Levy P
Antimicrob Agents Chemother. 1985 Aug;28(2):311-4. doi: 10.1128/AAC.28.2.311.
Serum kinetics and biliary, urinary, and fecal elimination of ciprofloxacin, a new quinolone derivative, were studied in 12 recently cholecystectomized patients provided with T-tube drainage during 24 h after oral administration of a single 500-mg dose of this substance. Drug concentrations were measured by both high-pressure liquid chromatography (HPLC) and microbiological assay. The results were comparable for the concentrations in serum (average of peaks, 2.0 +/- 0.2 micrograms/ml by HPLC and 2.3 +/- 0.3 micrograms/ml by the microbiological method) and urine (0 to 6 h, 267 +/- 74 and 241 +/- 58 micrograms/ml, respectively). This was not the case for biliary values, for which the microbiological assay yielded significantly higher concentrations than did HPLC (average of peak concentrations, 21.2 +/- 2.6 and 16.0 +/- 2.5 micrograms/ml, respectively [P less than 0.02]), nor for total 24-h biliary output (2,167 +/- 288 and 1,587 +/- 222 micrograms, respectively [P less than 0.01]). This suggests hepatic biotransformation of ciprofloxacin into microbiologically active metabolites. The apparent broad antibacterial spectrum of ciprofloxacin and its higher biliary levels than simultaneously determined serum concentrations suggest that this derivative is suitable for the treatment of biliary tract infections.
对12例近期行胆囊切除术并在术后24小时内留置T管引流的患者，在口服单剂量500毫克新喹诺酮衍生物环丙沙星后，研究了其血清动力学以及经胆汁、尿液和粪便的排泄情况。通过高压液相色谱法（HPLC）和微生物学测定法测量药物浓度。血清浓度（峰浓度平均值，HPLC法为2.0±0.2微克/毫升，微生物学法为2.3±0.3微克/毫升）和尿液浓度（0至6小时，分别为267±74和241±58微克/毫升）的结果具有可比性。胆汁浓度的情况并非如此，微生物学测定法得出的浓度显著高于HPLC法（峰浓度平均值分别为21.2±2.6和16.0±2.5微克/毫升[P<0.02]），24小时胆汁总排出量的情况也不同（分别为2167±288和1587±222微克[P<0.01]）。这表明环丙沙星在肝脏中生物转化为具有微生物活性的代谢产物。环丙沙星明显的广谱抗菌活性及其胆汁浓度高于同时测定的血清浓度，表明该衍生物适用于治疗胆道感染。
