盐酸洛美沙星在感染患者的药代动力学

Pharmacokinetic of lomefloxacin hydrochloride in infected patients

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；空腹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，Ｔ１／２ｋａ分别为 ０．３９± ０．１８和０．４７±０．２０ ｈ，Ｔｍａｘ分别为１．３±０．３和１．６±０．４ｈ，但Ｃｍａｘ下降不明显。单剂量空腹口服洛美沙星２００，４００和６００ ｍｇ后，Ｔ１／２β车分别为９．８±２．９，１０．７±４．０和１１．２±３．９ｈ，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。

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 k.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, pharmacokinetic 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 AUCo-∞ were proportional 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.