硫酸奈替米星在大鼠体内的药代动力学

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。

Pharmacokinetics of netilmicin sulfate in rats

AIM To investigate the pharmacokinetic of netilmicin sulfate in rats. METHODS The concentration of netilmicin sulfate was detected by a high performance liquid chromatography indirect photometric determination (HPLC IPD) method. RESULTS After intramuscutar injection netilmicin sulfate, the data obtained were fitted with 3P87 pharmacokinetic program. The dispostion was conformed to a single compartment model with T1/2=301￣362 h at single dose. The binding percentage of the drug to plasma protein was 68%￣174%. There was a highest drug accumulation in liver, lung and kidney, and a lowest in fat and brain. It excreted in urine, feces and bile within 24 h was 747%, 170% and 484%. CONCLUSION Netilmicin sulfate in rats is noted for its characteristic of distributed in tissues selectively, lower binding percentage to protein and excreted with prototype in kidney mainly.