培氟沙星药代动力学和体外抗菌活性研究

PHARMACOKINETICS AND IN VITRO ANTIBACTERIAL ACTIVITY OF PEFLOXACIN

本文报道培氟沙星体外抗菌活性及药代动力学研究结果。用HPLC法测定血清药物浓度。6名健康志愿者(男女各半)口服400mg培氟沙星后,体内过程符合一室开放模型。血峰浓度于4h达到,为8.20±2.84μg/ml,表观分布容积为3.05L/kg,AUC为163.08μg·h/ml,消除半衰期为13.35h。体外抗菌活性研究表明本品对常见致病菌有较强抗菌活性。对金葡球菌、大肠杆菌、变形杆菌、痢疾杆菌与伤寒杆菌的MIC_(30)(μg/ml)分别为0.25、2、2、0.25和1。上述结果表明,口服400mg培氟沙星后,其血峰浓度远较多种细菌的MIC_(90),预期临床可取得较好结果。

The pharmacokinetics and in vitro antibacterial activity of China-made pefloxacin were reported. Six healthy volunteers ( 3 male and 3 female) participated in this study. Serum concentration of pefloxacin was determined by HPLC. After administration of single oral dose of 400 mg, the drug concentration and time profile comformed to the one-compartment open model. The peak serum concentration,which was reached in 4 hours after oral administration, was 8.20±2.84μg/ml.The apparent volume of distribution and the area under the serum concentration curve were 3.05 L/kg and 163.08μg·h/ml respectively.The elimination half-life was 13.35h. The in vitro antibacterial activity test showed that pefloxacin was a powerful bactericide. The MIC90s (μg/ml) for S. aureus, E. coli, Proteus spp., Shigella spp and S. typhi were 0.25, 2, 2, 0.25 and 1. The peak concentration of pefloxacin, after oral administration of 400mg, is much higher than the MIC90s for most pathogenic bacteria. This ensures its effectiveness in the treatment of various clinical infections caused by sensitive bacteria.