盐酸洛美沙星在感染患者的药代动力学

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,T_{1/2 ka}分别为0.39±0.18和0.47±0.20 h,T_max分别为1.3±0.3和1.6±0.4 h,但C_max下降不明显。单剂量空復口服洛美沙星 200, 400 和 600 mg 后,T_max分别为 9.8±2.9, 10.7±4.0 和 11.2±3.9 h, C_max分别为1.5±0.4, 2.4±0.8和3.8±0.9 mg·L^-1, AUC_0-∞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C_max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C_max和AUC_0-∞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AUC_0-∞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。

Pharmacokinetic of lomefloxacin hydrochloride in infected patients

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 T_{1/2 ka} was 0.39±0.18 and 0.47±0.20 h,the T_max was 1.3±0.3 and 1.6±0.4 h respectively,but the C_max 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 T_1/2β was 9.8±2.9,10.7±4.0 and 11.2±3.9 h, C_max was 1.5±0.4, 2.4±0.8 and 3.8±0.9 mg·L^-1, respectively. The AUC_0-∞ were pro-portional to dose and the pharmacokinetics had a linear relationship with dose. The C_max 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 C_max and AUC_0-∞ 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.