Drusano G L, Plaisance K I, Forrest A, Standiford H C
Antimicrob Agents Chemother. 1986 Sep;30(3):440-3. doi: 10.1128/AAC.30.3.440.
We evaluated the pharmacokinetics of 100- and 200-mg doses of ciprofloxacin, with the 200-mg dose administered either as a 30-min infusion or as a 100-mg loading dose followed by a 4-h constant infusion of 25 mg/h in six normal volunteers. No significant differences were seen in the dose-normalized area under the curve when the 100- and 200-mg 30-min administrations were compared. Differences that approached statistical significance were seen when data from either of these trials were compared with data from the constant-infusion arm. Serum clearances averaged 23.0 +/- 9.1 liters/h per 1.73 m2 for the 100-mg dose and 23.7 +/- 5.1 liters/h per 1.73 m2 for the 200-mg dose. Renal clearance accounted for approximately two-thirds of the serum clearance in each instance. Half-lives were slightly longer than 4 h. For the constant-infusion arm, serum clearance was 28.9 +/- 2.7 liters/h per 1.73 m2, with renal clearance accounting for 58% of serum clearance. Although no nonlinearities were apparent in the 100- to 200-mg dose range, larger doses, particularly in the multiple-dosing situation, may uncover nonlinearity in the disposition of ciprofloxacin.
我们评估了100毫克和200毫克剂量环丙沙星的药代动力学,在六名正常志愿者中,200毫克剂量以30分钟输注的方式给药,或者先给予100毫克负荷剂量,然后以25毫克/小时的速率持续输注4小时。当比较100毫克和200毫克30分钟给药方式时,剂量标准化曲线下面积未见显著差异。当将这两个试验中的任何一个数据与持续输注组的数据进行比较时,发现差异接近统计学显著性。100毫克剂量的血清清除率平均为每1.73平方米23.0±9.1升/小时,200毫克剂量的血清清除率平均为每1.73平方米23.7±5.1升/小时。在每种情况下,肾清除率约占血清清除率的三分之二。半衰期略长于4小时。对于持续输注组,血清清除率为每1.73平方米28.9±2.7升/小时,肾清除率占血清清除率的58%。尽管在100至200毫克剂量范围内未发现明显的非线性,但更大剂量,尤其是在多次给药情况下,可能会揭示环丙沙星处置中的非线性。