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国产注射用甲磺酸帕珠沙星在健康人体的药代动力学研究

Pharmacokinetics of Pazufloxacin Mesilate Sodium Chloride in healthy Chinese volunteers after intravenous injection
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摘要 评价多个剂量的氟喹诺酮类抗菌药物—甲磺酸帕珠沙星在健康人体单次静脉滴注后的药代动力学参数及其在健康人体中的代谢特点。本文采用随机、开放、平行的试验设计,根据入排标准筛选30名健康受试者,随机分成3组,每组10人,分别静脉滴注低(150mg)、中(300mg)、高(600mg)三个浓度的甲磺酸甲磺酸帕珠沙星,30分钟内完成。采集不同时间点血液样本,收集0–24小时尿液。采用反向高效液相色谱法(RP-HPLC)测定血药浓度及尿药浓度,用DAS1.0软件计算药代动力学参数。结果发现,低、中、高三个剂量组药代动力学参数均符合二室模型。三个剂量组中曲线下面积(AUC0→∞)分别为:3.24±1.2,5.89±1.51和13.32±2.35mg·h·mL–1;峰浓度(Cmax)分别为2.37±0.89,4.27±0.74以及10.74±4.06 mg·mL–1;此外,达峰时间(Tmax)分别为0.48±0.08, 0.50±0.00 and 0.53±0.08 h。低、中、高三个剂量组清除率分别为(8.29±4.06 L/h),(10.96±4.42 L/h),(9.14±1.72 L/h)。分别将AUC0→∞、Cmax与剂量进行相关性分析发现,甲磺酸帕珠沙星药物浓度与给药剂量呈线性关系。数据表明,低、中、高三个剂量组均符合药代动力学二室模型。在150–600mg剂量范围内,甲磺酸帕珠沙星药物浓度与给药剂量呈线性关系。三个剂量组甲磺酸帕珠沙星药物代谢率均在90%以上,其代谢特点与国外文献报道基本一致。 In the present study,we aimed to investigate the pharmacokinetics and dosage proportionality for a single,intravenous utilization of Pazufloxacin Mesilate Sodium Chloride,an injectable synthetic fluoroquinolone antibacterial agent,in healthy Chinese volunteers.In this open-labeled,three-dosage parallel study,subjects were randomized to receive a single dose of Pazufloxacin Mesilate at 150,300 or 600 mg(n=10,10 and 10,respectively)administered as a 30-min intravenous infusion.Blood and urine samples were serially collected from 0 to 24 h after drug administration.Moreover,the sample’s drug concentrations were analyzed via validated RP-HPLC method.Subjects receiving a single dose of Pazufloxacin Mesilate 150,300 or 600 mg were in accordance with the two compartment model.The Cmax for each dosage group was 2.37±0.89,4.27±0.74 and 10.74±4.06 mg·mL(–1),respectively;and the AUC0→∞was 3.24±1.2,5.89±1.51 and 13.32±2.35 mg·h·mL–1,respectively.In addition,Tmax for groups treated with 150,300 and 600 mg was 0.48±0.08,0.50±0.00 and 0.53±0.08 h,respectively.The correlation analysis for AUC0→∞,Cmax and dosage suggested that pazufolxacin mesilate displayed dose proportion at the dose ranging from 150 to 600 mg.The data suggested that all three different dosage regimens fit with the two compartment model.Meanwhile,it presented a linear correlation between AUC0→∞,Cmax and dosage over the range of 150–600 mg.
作者 欧阳文鹃 张亚兰 徐平声 戴智勇 马虹英 秦群 Wenjuan OuYang;Yalan Zhang;Pingsheng Xu;Zhiyong Dai;Hongying Ma;Qun Qin(National Institution of Drug Clinical Trial,XiangYa Hospital,Central South University,Hunan,410008,China;Department of Pharmacy,XiangYa Hospital,Central South University,Hunan,410008,China)
出处 《中国药学:英文版》 CAS CSCD 2019年第1期40-48,共9页 Journal of Chinese Pharmaceutical Sciences
基金 the support of Laboratory of National Institution of Drug Clinical Trial,Xiangya Hospital,Central South University.
关键词 甲磺酸甲磺酸帕珠沙星 反向高效液相色谱 RP-HPLC 药代动力学 Pazufloxacin Mesilate Accumulative urine excretion rate RP-HPLC Pharmacokinetics
作者简介 Corresponding author:Qun Qin,Tel.:+86-0731-84327918,E-mail:qinqun8087@hotmail.com
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