Plaisance K I, Drusano G L, Forrest A, Weir M R, Standiford H C
University of Maryland School of Pharmacy, Baltimore 21201.
Antimicrob Agents Chemother. 1990 Jun;34(6):1031-4. doi: 10.1128/AAC.34.6.1031.
The effect of renal function on the bioavailability of ciprofloxacin was studied in 21 subjects with measured creatinine clearances ranging from 0 to 8.99 liters/h per 1.73 m2. Each subject received ciprofloxacin, 200 mg intravenously and 750 mg orally, separated by at least 1 week. Serial (12 to 15) blood samples were obtained over 24 to 48 h. Concentrations in serum were assayed by high-pressure liquid chromatography. Area under the curve was calculated by the trapezoidal rule with extrapolation to infinity. Bioavailability was calculated as the ratio between the dose-normalized area under the curve of oral and intravenous administrations. The overall mean (standard deviation) bioavailability observed was 63.4% (14.6%), similar to that observed in those with normal renal function (69.0% [15.7%]). The mean bioavailability in the subgroup of subjects with renal insufficiency was 59.9% (13.3%). The observed range in bioavailability was 33.9 to 91.4%. Linear regression did not reveal a correlation between creatinine clearance and bioavailability. Renal insufficiency does not appear to affect ciprofloxacin bioavailability.
在21名肌酐清除率测定值为每1.73平方米0至8.99升/小时的受试者中，研究了肾功能对环丙沙星生物利用度的影响。每位受试者接受200毫克环丙沙星静脉注射和750毫克口服，给药间隔至少1周。在24至48小时内采集系列（12至15份）血样。血清浓度通过高压液相色谱法测定。曲线下面积通过梯形法则计算并外推至无穷大。生物利用度通过口服和静脉给药的剂量标准化曲线下面积之比计算。观察到的总体平均（标准差）生物利用度为63.4%（14.6%），与肾功能正常者观察到的生物利用度（69.0%[15.7%]）相似。肾功能不全受试者亚组的平均生物利用度为59.9%（13.3%）。观察到的生物利用度范围为33.9%至91.4%。线性回归未显示肌酐清除率与生物利用度之间存在相关性。肾功能不全似乎不影响环丙沙星的生物利用度。
