口服洛美沙星的人体药物动力学

Pharmacokinetics of orally administered lomefloxacin

目的:研究健康志愿者单剂po国产洛美沙星400mg后的药物动力学特征.方法;采用HPCL法测定血清和尿中药物浓度.结果:该药在人体内的转运过程符合二室开放模型,C_(max)为 4.88 mg/L,T_(1/2β)为 7.19 h,Vd和AUC分别为 1.51L/kg和51.03(mg·h)/L,CL为 2.47 d/(min·kg),48h尿药排泄率为75.7%.洛美沙星的人血清蛋白结合率为16.3%.结论:洛美沙星400mg单剂po后血和尿中可迅速达到有效抗菌浓度且持续时间较长.

AIM: To study Pharmacokinetics of lomefloxacin after a single 400 mg oral dose was given to 8 male volunteers. METHODS: Concentrations in sera and urine were as-sayed by high performance liquid chromatography. RESULTS: Lomefloxacin concentration time profile comformed to an open two compartment model. The mean serum peak level was 4. 88 mg/L. The mean serum elimination half-life was 7. 19 h. The apparent volume of dis-trabution and AUC were 1.51 L/kg and 51.03 (mg · h)/L, respectively. The total body clearance averaged 2. 47 ml/(min · kg). The mean recovery of lomefloxacin from urine over 48 h was 75. 7%. About 16.3% lomefloxacin was protein bound in serum. CONCLUSION: Concentrations in sera and urine are high. The mean serum elimination half-life is long.