Wu Guolan, Wu Lihua, Hu Xingjiang, Zhou Huili, Liu Jian, Zhu Meixiang, Zheng Yunliang, Zhai You, Shentu Jianzhong
Int J Clin Pharmacol Ther. 2014 Dec;52(12):1037-44. doi: 10.5414/CP202147.
Sitafloxacin is a new fluoroquinolone with a broad spectrum of antibacterial activity, including grampositive and gram-negative bacteria. This study was to evaluate the pharmacokinetic characteristics of a single dose of sitafloxacin in healthy Chinese volunteers.
This was a single-center, open-label, randomized-sequence study conducted in 12 subjects. Subjects were randomly assigned to receive single doses of 50, 100, and 200 mg of sitafloxacin in a 3-way crossover design with a 7-day washout period between administrations. Quantification was carried out using a validated high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method. Pharmacokinetic parameters were calculated and analyzed statistically. Safety assessments were conducted throughout the study.
After administration of single doses of 50, 100, and 200 mg, geometric mean estimate for sitafloxacin Cmax were 0.72, 1.62, and 2.73 μg/mL and the mean of AUClast were 3.97, 8.71, and 18.03 μg x h/mL, respectively. Sitafloxacin was rapidly absorbed, reaching Cmax ranged from 0.85 to 1.21 hours. The terminal half-life ranged from 5.19 to 6.28 hours. The Cmax and AUC last were proportional to the doses. The mean clearance, the half-life, and the volume of distribution were constant, irrespective of the dose.
In healthy Chinese subjects, single dosing of sitafloxacin resulted in linear plasma pharmacokinetics.
西他沙星是一种新型氟喹诺酮类药物，具有广谱抗菌活性，包括革兰氏阳性菌和革兰氏阴性菌。本研究旨在评估单剂量西他沙星在健康中国志愿者体内的药代动力学特征。
这是一项在12名受试者中进行的单中心、开放标签、随机序列研究。受试者按3种剂量水平（50、100和200mg）随机分配，采用3交叉设计给药，给药间隔7天洗脱期。采用经过验证的高效液相色谱-串联质谱（HPLC-MS/MS）方法进行定量分析。计算药代动力学参数并进行统计学分析。在整个研究过程中进行安全性评估。
单次给予50、100和200mg剂量后，西他沙星的Cmax几何均值估计值分别为0.72、1.62和2.73μg/mL，AUClast均值分别为3.97、8.71和18.03μg·h/mL。西他沙星吸收迅速，达峰时间为0.85至1.21小时。末端半衰期为5.19至6.28小时。Cmax和AUClast与剂量成正比。平均清除率、半衰期和分布容积不受剂量影响，保持恒定。
在健康中国受试者中，单剂量西他沙星呈现线性血浆药代动力学特征。
