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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 enoxaparin (ENX) 400mg, and their pharmacokinetic parameters were determined by RP-HPLC method within 12 hours after administration. The effect of ENX on 797 clinical isolates In vitro antibacterial activity of bacteria. Chromatographic conditions, mobile phase methanol: 0.008mol / L phosphate buffer: 0.5mol / L tetrabutylammonium bromide (25: 75: 4, V: V: V, pH2.85). UV detection wavelength 275nm, 0.04AUFS, flow rate of 0.8ml / min, reaction STD. The linear range of this method is 0.0625 ~ 4μg / ml, r = 0.9977. ENX had good antibacterial activity against both Gram-positive and Gram-negative bacteria tested, with antibacterial rates> 65%. Oral ENX400mg, the drug in vivo transport process in line with the first-order kinetic open-chamber model. Tmax, Cmax were 2.12h and 2.47μg / ml respectively, T 1 / 2Ka and T 1 / 2Ke were 1.22 and 2.35h respectively, Vd was 3.07L / Kg and CL was 0.86L / h.kg, indicating that the drug absorption after oral administration Rapid, up to higher concentrations, and are widely distributed in the body most tissues and body fluids.