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目的研究硫酸奈替米星在大鼠体内分布和排泄情况。方法大鼠iv给药后,采用高效液相色谱-间接光度检测(HPLC-IPD)法测定组织和体液中药物浓度,并计算药动学参数。结果血药浓度-时间曲线符合一室开放模型,不同给药剂量时其体内T1/2为3.01~3.62h;组织中药物浓度以肝、脾、肺、肾中最高,脂肪和脑中较低;平均血浆蛋白结合率为6.8%~17.4%;尿、粪和胆汁24h排泄原型药物量占给药量的74.7%,1.70%和4.84%。结论硫酸奈替米星在大鼠体内组织分布具有选择性,蛋白结合率低,主要经肾脏以原型排泄。
Objective To study the distribution and excretion of netilmicin sulfate in rats. Methods After iv administration, the drug concentrations in tissues and body fluids were determined by HPLC-IPD and the pharmacokinetic parameters were calculated. Results The plasma concentration-time curve was in accordance with the open-chamber model. The T1 / 2 in vivo was 3.01-3.62h at different doses. The concentration of the drug in the tissue was highest in liver, spleen, lung and kidney, ; The average plasma protein binding rate was 6.8% ~ 17.4%; urinary, excrement and bile 24h excreted prototype drugs accounted for 74.7%, 1.70% and 4.84% of the dose. CONCLUSION Netilmicin sulfate is selective for tissue distribution in rats. Its protein binding rate is low, mainly excreted by the kidney.