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目的探讨急进高原后大鼠体内阿莫西林药代动力学参数的变化。方法 Wistar大鼠于平原地区和急进高原后灌胃给药,分别于给药前(0 h)及给药后0.33、0.66、1、1.5、2、3、4、6、8、12、24 h采血,采用LC-MS/MS方法测定血药浓度,并分别计算蛋白结合率和药代动力学参数。结果急进高原组血浆蛋白结合率(45.00%)与平原组血浆蛋白结合率(36.31%)相比显著升高,药-时曲线下面积从(11 616.40±1071.92)μg·L-1·h增大到(47 879.24±9417.18)μg·L-1·h,急进高原后体内平均驻留时间延长,峰浓度增大,清除率降低。结论统计学分析结果显示急进高原后,阿莫西林在大鼠体内药代动力学参数发生显著变化,为进一步研究人体药代动力学提供实验基础和参考依据。
Objective To investigate the changes of the amoxicillin pharmacokinetic parameters in rats after acute high altitude. Methods Wistar rats were intragastrically administrated in the plain area and the rapid plateau, respectively. Before administration (0 h) and after administration of 0.33, 0.66, 1, 1.5, 2,3,4,6,8,12,24 h, blood concentration was determined by LC-MS / MS and the protein binding rate and pharmacokinetic parameters were calculated respectively. Results The plasma protein binding rate (45.00%) in acute plateau group was significantly higher than that in plain group (36.31%). The area under the drug-time curve increased from (11 616.40 ± 1071.92) μg · L-1 · h (47879.24 ± 9417.18) μg · L-1 · h, the average residence time in the body after lengthening the plateau, the peak concentration increased, the clearance rate decreased. Conclusions The results of statistical analysis show that the pharmacokinetic parameters of amoxicillin are significantly changed in rats after rapid plateau, providing experimental basis and reference for further study of human pharmacokinetics.