论文部分内容阅读
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，洛美沙星原型药物
Objective To observe the pharmacokinetics of lomefloxacin hydrochloride in infected patients. Methods The in vivo process and kinetics of oral and IV drip, fasting and meal, different doses, single dose and multiple doses were compared. The in vivo drug concentration was determined by high performance liquid chromatography. Results Lomefloxacin showed first-order absorption two-compartment open model in vivo. After fasting and post-prandial oral administration of 200 mg of lomefloxacin, the absorption of lomefloxacin by food was significantly prolonged (T1 / 2ka = 0.39 ± 0 .18 and 0.47 ± 0.20 h, Tmax were 1.3 ± 0.3 and 1.6 ± 0.4h, respectively, but the decrease of Cmax was not significant. After a single dose of fasting oral doses of lomefloxacin 200, 400 and 600 mg, T1 / 2β vehicles were 9.8 ± 2.9, 10.7 ± 4.0 and 11.2 ± 3.9 h, respectively, with Cmax of 1. 5 ± 0.4,2.4 ± 0.8 and 3.8 ± 0.9 mg · L-1, AUC0-∞ increased in dose-proportionally with a linear relationship between in vivo pharmacokinetics and dose; single-dose intravenous Cmax after instillation of 600 mg of drug was 3.1 ± 0.9 mg · L-1. Compared with single-dose administration, Cmax and AUC0-∞ increased significantly after oral administration of 400 mg twice daily for 7 days, with an accumulation factor of 1.45. Compared with single-dose administration of 600 mg once daily for 7 days, Administration was not obvious, the storage factor was 1.10; other parameters did not change significantly. In a variety of drug delivery conditions, lomefloxacin prototype drugs