环丙沙星药代动力学和体外抗菌活性研究

PHARMACOKINETICS AND IN VITRO ANTIBACTERIAL ACTIVITY OF CIPROFLOXACIN

本文报道环丙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名健康志愿者环丙沙星400mg口服后,体内过程符合一室开放模型。血峰浓度于2小时到达,为2.52±0.82μg/ml。表现分布容积为2.47L/kg,AUC为14.10μg·h/ml,消除半衰期为2.93小时。体外抗菌活性研究结果表明,本品抗菌谱广,抗菌活性强。对金葡菌、大肠杆菌、肺炎杆菌、痢疾杆菌、伤寒杆菌MIC90分别为0.125、0.5,0.06、<0.03和0.25μg/ml。对绿脓杆菌抑苗率达87％。上述资料表明,环丙沙星口服400mg后,峰浓度明显高于多种细菌的MIC90值,预期临床可取得较好疗效。

The pharmacokinetics of ciprofloxacin, after adiministr-ation of single oral dose of 400mg, was determined in 6 healthy volunteers. Serum concentration were determined by HPLC. The drug concentration-time profile comformed to the one-compartment model. The peak serum concentration, which was reached in 2 hours after oral adiministr-ation, was 2.52 ± 0.82μg/ml. The apparent volume of distribution and the areas under the serum concentration curve were 2.47 L/kg and 14.10μg·h/mlrespectively. The elimination half-life was 2.39 hours.The in vitro antibacterial activity test showed that ciprofloxacin wasa broad-spectrum and powerful bactericide. The MIC90s for S. aureus, E. coli, K. pneumoniea, Shigella spp., and S. typhi were 0.125, 0.25,0.06, 0.03 and 0.25 μg/ml respectively. 87% of strains of P. aeruginosa tested were sensitivity to this agent.The peak concentration of ciprofloxacin after oral adiministration 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.