欢迎访问《中国临床药理学与治疗学》杂志官方网站,今天是

中国临床药理学与治疗学 ›› 1999, Vol. 4 ›› Issue (1): 25-29.

• • 上一篇    下一篇

盐酸洛美沙星在感染患者的药代动力学

袁成, 周大铮1, 曹晚芝2, 王景祥, 刘华1   

  1. 济南军区总医院药理科,济南 250031;
    1解放军106医院;
    2山东建材学院医院
  • 收稿日期:1998-12-24 出版日期:1999-03-26 发布日期:2020-12-03
  • 作者简介:袁成,36岁,副主任医师,主要从事监床药理学研究。

Pharmacokinetic of lomefloxacin hydrochloride in infected patients

YUAN Cheng, ZHOU Da-Zheng1, CAO Xiao-Zhi, WANG Jing-Xiang, LIU Hua1   

  1. Department of Pharmacology y General Hospital of Jinan Military Region, Jinan 250031;
    1Department of Pharmacy,The 106 th Hospital of PLA,Jinan 250022
  • Received:1998-12-24 Online:1999-03-26 Published:2020-12-03

摘要: 目的 观察感染患者体内盐酸洛美沙星的药代动力学。方法 比较口服和静脉滴注、空腹与进餐、不同剂量、单剂量和多剂量给药时的体内过程和动力学特征,体内药物浓度用高效液相色谱法测定。结果 洛美沙星在体内均表现为一级吸收二室开放模型;空愎和餐后口服洛美沙星200 mg后,显示食物可使该药物吸收过程明显延长,T1/2 ka分别为0.39±0.18和0.47±0.20 h,Tmax分别为1.3±0.3和1.6±0.4 h,但Cmax下降不明显。单剂量空復口服洛美沙星 200, 400 和 600 mg 后,Tmax分别为 9.8±2.9, 10.7±4.0 和 11.2±3.9 h, Cmax分别为1.5±0.4, 2.4±0.8和3.8±0.9 mg·L-1, AUC0-∞与剂量呈比例增加,体内药代动力学与剂量呈线性关系;单剂量静脉滴注药物600 mg后Cmax为3.1±0.9 mg·L-1。与单剂量给药相比,400 mg, bid连续口服7d后的Cmax和AUC0-∞均显著增加,蓄积因子为1.45; 600mg,每天1次连续静脉滴注7d时AUC0-∞比单剂量给药增加不明显,蓄积因子为1.10;其他参数变化不显著。在各种给药条件下,洛美沙星原型药物24 h尿排出率均在50%左右。结论 体内过程呈线性药代动力学。

关键词: 盐酸洛美沙星, 药代动力学, 高效液相色谱法

Abstract: Aim The pharmacokinetics of lomefloxacin hydrochloride administered orally or by dripping in infected patients was studed. Methods The parameters with different dosages, fasting and non-fasting, single and multiple dsoes were compared. A hing performance liquid chromatography was used to determine the concentration of lomefloxacin in serum and urine. Results A first-order absorption and an open dubble compartment pharmacokinetics model were showed after taking the drug. When a single oral dose of 200 mg of lomefloxacin was gaven to the patiens before and after breakfast, the absorption was slightly decreased. The T1/2 ka was 0.39±0.18 and 0.47±0.20 h,the Tmax was 1.3±0.3 and 1.6±0.4 h respectively,but the Cmax had no significant difference between before and after food. After a single oral dose of 200,400, and 600 mg of lomefloxacin, pharma-cokinetic parameters for the drug were T1/2β was 9.8±2.9,10.7±4.0 and 11.2±3.9 h, Cmax was 1.5±0.4, 2.4±0.8 and 3.8±0.9 mg·L-1, respectively. The AUC0-∞ were pro-portional to dose and the pharmacokinetics had a linear relationship with dose. The Cmax was 3.1±0.9 mg·L-1 after a single drip dose of 600 mg of lomefloxacin. Compared with those in the single dose, the Cmax and AUC0-∞ had marked increase with a retaining factor of 1.45 after multiple oraling dose of 400 mg twice daily for 7 days. But the parameter had no significant change with a retaining factor 1.10 after dripping 600 mg once daily for 7 days. The percentage of prototype drug urinary recovery within 24 hours was about 50% in all methods and dosages of taking drug. Conclusion Lomefloxacin is a drug that has a linear pharmacokinetic.

Key words: lomefloxacin, pharmacokinetic, high performance liquid chromatography

中图分类号: