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普卢利沙星片人体药代动力学研究

魏春敏**, 王本杰, 李惠云, 郭瑞臣*   

  1. 山东大学齐鲁医院临床药理研究所, 山东 济南 250012
  • 收稿日期:2005-01-17 修回日期:2005-11-10 出版日期:2005-12-15 发布日期:2005-12-15
  • 通讯作者: 魏春敏**, 郭瑞臣*

Pharmacokinetics of Active Metabolite of Prulifloxacin in Healthy Chinese

WEI Chun-min**, WANG Ben-jie, LI Hui-yun, GUO Rui-chen*   

  1. Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan 250012, China2003 Master degree student, School of Pharmacy, Shandong University
  • Received:2005-01-17 Revised:2005-11-10 Online:2005-12-15 Published:2005-12-15
  • Contact: WEI Chun-min**, GUO Rui-chen*

摘要: 目的 进行健康志愿者普卢利沙星片单次和多次口服给药活性代谢物NM394人体药代动力学研究。方法 采用三交叉试验设计, 12名健康志愿者随机分为3, 普卢利沙星片132.1 mg, 264.2 mg 396.3 mg分别单次口服或264.2 mg每日2, 连续7日口服, 采集肘静脉血, HPLC法测定NM394 血浓度, DAS软件计算药动力学参数。结果 普卢利沙星片单次口服给药NM394主要药动学参数Cmax0.64±0.25 μg·mL-1, 1.06±0.35 μg·mL-1 1.45±0.44 μg·mL-1, Tmax 0.94±0.22 h, 1.02±0.17 h 0.98±0.23 h, t1/2 8.37±0.70 h, 7.70±0.82 h7.78±0.77 h, AUC0-24 2.93±0.78 μg·mL-1·h, 4.39±1.05 μg·mL-1·h 5.55±1.32 μg·mL-1·h, AUC0-∞3.32±0.84 μg·mL-1·h, 4.82±1.06 μg·mL-1·h 6.10±1.38 μg·mL-1·h; 连续多次口服给药NM394主要药动学参数Cmax1.20±0.33 μg·mL-1, Tmax 0.67±0.12 h, t1/2 7.38±1.03 h, AUC0-245.58±1.25 μg·mL-1·h AUC0-∞6.09±1.24 μg·mL-1·h结论 普卢利沙星片单次口服给药NM394 Cmax AUC呈良好剂量依赖性; 单次和多次给药NM394药动学特征无明显差异; 多次给药NM394体内无蓄积。

关键词: 普卢利沙星, 普卢利沙星, 普卢利沙星, NM394, NM394, NM394, 高效液相色谱法, 高效液相色谱法, 高效液相色谱法, 药代动力学, 药代动力学, 药代动力学

Abstract: Aim To investigate the pharmacokinetics of NM394 (an active metabolite of prulifloxacin) and evaluate the dose relationship and accumulation characteristics after single and multiple doses of prulifloxacin. Methods Twelve healthy volunteers were given 132.1 mg, 264.2 mg, and 396.3 mg of prulifloxacin tablets in a randomized 3 ×3 crossover design test for single doses trial. With one-week washout period, 264.2 mg of prulifloxacin tablets were given for multiple doses trial. NM394 in plasma was determined by a sensitive HPLC method and its pharmacokinetic parameters were analyzed and evaluated by Drug and Statistics saftware (version 1.0). Results The Cmax, Tmax, t1/2, AUC0-24, and AUC0-∞ of NM394 after single doses of 132.1 mg, 264.2 mg, and 396.3 mg of prulifloxacin tablets were 0.64±0.25 μg·mL-1, 1.06±0.35 μg·mL-1, and 1.45±0.44 μg·mL-1, respectively; Tmax 0.94±0.22 h, 1.02±0.17 h, and 0.98±0.23 h, respectively; t1/2 8.37±0.70 h, 7.70±0.82 h, and 7.78±0.77 h, respectively; AUC0-24 2.93±0.78 μg·mL-1·h, 4.39±1.05 μg·mL-1·h, and 5.55±1.32 μg·mL-1·h, respectively; AUC0-∞ 3.32±0.84 μg·mL-1·h, 4.82±1.06 μg·mL-1·h, and 6.10±1.38 μg·mL-1·h, respectively. And the Cmax,Tmax, t1/2, AUC0-24, and AUC0-∞ after multiple doses of 264.4 mg prulifloxacin tablets were 1.20±0.33 μg·mL-1, 0.67±0.12 h, 7.38±1.03 h, 5.58±1.25 μg·mL-1·h, and 6.09±1.24 μg·mL-1·h, respectively. Conclusion The Cmax and AUC of NM394 are in high correlation with given prulifloxacin doses. There are no differences in pharmacokinetic characteristics of NM394 between single and multiple doses. No accumulation in plasma is observed after multiple doses of 264.2 mg per day for 7 d.

Key words: prulifloxacin, prulifloxacin, NM394, NM394, pharmacokinetics, pharmacokinetics, HPLC, HPLC

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Supporting: *Corresponding author. Tel.: 86-531-82169636.
**2003 Master degree student, School of Pharmacy, Shandong University.