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目的:研究格拉司琼对大鼠体内洛铂药动学的影响。方法:雄性Wistar大鼠随机分为2组(n=10),对照组只给洛铂,给药剂量为10.64 mg.kg-1。实验组给洛铂前30 min给予格拉司琼0.4 mg.kg-1,两组大鼠分别于给药前和给药后0,5,15,30,60,90,120,240,360,480 min取血,HPLC法测定血浆洛铂浓度,用统计矩法计算药动学参数。结果:洛铂检测浓度的线性范围为0.5~80.0μg.mL-1(r=0.999 9),方法回收率为96.62%~107.9%,日内、日间RSD均小于9%。对照组和实验组洛铂的药动学参数分别为:AUC(0-∞):(42.3±13.4)mg.h.L-1,(43.8±9.2)mg.h.L-1;Cmax:(66.8±11.0)mg.L-1,(70.8±9.1)mg.L-1;t1/2z:(2.0±0.6)h,(1.7±0.6)h。各项参数均无统计学差异(P>0.05)。结论:洛铂单独使用及与格拉司琼合用的药物动力学参数之间差异无显著性。
Objective: To investigate the effect of granisetron on the kinetics of Methods: Male Wistar rats were randomly divided into 2 groups (n = 10). The control group was treated with Losoplatin. The dose was 10.64 mg.kg-1. In the experimental group, granisetron 0.4 mg.kg-1 was given 30 min before the rabeprazole, and blood was collected before and at 0, 5, 15, 30, 60, 90, 120, 240, 360 and 480 min after administration, Plasma concentration of lobaplatin, using statistical moment method to calculate pharmacokinetic parameters. Results: The calibration curve was linear within the range of 0.5 ~ 80.0μg.mL-1 (r = 0.999 9). The method recoveries ranged from 96.62% to 107.9%. The intra-day and inter-day RSD were less than 9%. The pharmacokinetic parameters of lobaplatin in the control group and the experimental group were as follows: AUC (0-∞) :( 42.3 ± 13.4) mg.hL-1, (43.8 ± 9.2) mg.hL-1; Cmax: (70.8 ± 9.1) mg.L-1; t1 / 2z: (2.0 ± 0.6) h, (1.7 ± 0.6) h. The parameters were not statistically different (P> 0.05). Conclusion: There is no significant difference in the pharmacokinetic parameters between lobaplatin and granisetron alone or in combination with granisetron.