摘要
健康志愿者6人口服依诺沙星(ENX)400mg,用反相高效液相法测定给药后12小时内血药浓度以研究其药动学特征,同时测定ENX对797株临床分离致病菌的体外抗菌活性。 色谱条件,流动相为甲醇:0.008mol/L磷酸缓冲液:0.5mol/L四丁基溴化铵(25:75:4,V:V:V,pH2.85)。紫外检测波长275nm,0.04AUFS,流速为0.8ml/min,反应STD。本方法线性范围为0.0625～4μg/ml,r=0.9977。 ENX对所试革兰氏阳性和革兰氏阴性细菌均有良好抗菌活性,抑菌率均>65％。 口服ENX400mg后,药物在体内的转运过程符合一级动力学一室开放模型。Tmax,Cmax分别为2.12h和2.47μg/ml,T 1/2Ka、T 1/2Ke分别为1.22和2.35h,Vd为3.07L/Kg,CL为0.86L/h.kg,说明口服后药物吸收迅速,可达较高浓度,且广泛分布于全身多数组织和体液中。
Six healthy volunteers were given 400 mg enoxacin (ENX) by oral administration. The serum drug concentrations within 12 hours were determined by HPLC method to study their pharmacokinetic characteristics. Antimicrobial activities in vitro to 797 strains isolated from patients were also tested. Mobile phase of HPLC consisted of methanol/0.008 mol/L phosphate buffer/0.5 mol/L tetrabutyl ammonium bromide(25:75: 4, v:v:v, pH 2.85). UV detector was used. Wave length was 275 nm with 0.04 AUFS. Flow rate was 0.8 ml/min.Standard response was obtained. The linear range was from 0.0625 to 4 μg/ml(r = 0.9977).ENX had good antimicrobial activities to Gram-positive and Gram-negative organisms. The disposition and fate of ENX after oral administration conformed to the one compartment open model.Tmax and Cmax were 2.12h and 2.47 μg/ml respectively. T11/2ka and T1/2ke were 1.22h and 2.35 h respectively. Vd was 3.07 L/kg. CL was 0.86 L/h.kg. These data showed that the drug was quickly absorbed,reached moderate concentration and distributed well in tissue and body fluid.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
1992年第3期215-218,共4页
Chinese Journal of Antibiotics
关键词
依诺沙星
药动学
体外抗菌活性
Enoxacin
Pharmacokinetics
Antimicrobial activity
