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目的:研究2种不同的5-HT3拮抗剂止吐药格拉司琼和昂丹司琼对大鼠体内多西他赛药动学的影响。方法:Wistar♂大鼠随机分为3组(n=8),给药剂量为5 mg.kg-1。第1组只给多西他赛,第2组给予多西他赛15 min前给予格拉司琼0.4mg.kg-1,第3组给予多西他赛15 min前给予昂丹司琼1 mg.kg-1。3组大鼠分别于给药前和给药后2,15,30,90,240,480,720,1440 min取血用于测定药代动力学。结果:3组的平均消除半衰期分别为(236.4±53.5),(363.1±301.1),(328.2±206.1)min;平均药时曲线下面积(AUC0～t)范围分别为54597.0～88141.9,46932.8～72004.6,51585.6～70958.0μg.min.L-1[平均值±SD:(66664.8±11389.4),(60700.2±7666.6),(60018.4±7545.3)μg.min.L-1];清除率分别为(0.076±0.012),(0.08±0.013),(0.081±0.011)L.min.kg-1。第1组和第2组平均滞留时间没有显著性差异,第1组和第2组、第2组和第3组之间平均滞留时间存在显著差异。结论:多西他赛单独使用的药代动力学参数和与格拉司琼合用的药代动力学参数之间没有显著性差异,与昂丹司琼合用的药代动力学参数除平均滞留时间也没有显著性差异。
Objective: To study the effects of two different 5-HT3 antagonist antiemetics granisetron and ondansetron on docetaxel pharmacokinetics in rats. Methods: Wistar rats were randomly divided into 3 groups (n = 8), and the dose was 5 mg.kg-1. Group 1 received docetaxel only, group 2 received docetaxel granisetron 0.4 mg.kg-1 15 min, and group 3 received docetaxel 15 min prior to ondansetron 1 mg .kg-1.3 groups of rats were taken before and after administration of 2,15,30,90,240,480,720,1440 min blood for the determination of pharmacokinetics. RESULTS: The mean elimination half-lives of the three groups were (236.4 ± 53.5) and (363.1 ± 301.1) and (328.2 ± 206.1) min, respectively. The mean area under the curve of the mean drug time (AUC0 ~ t) was 54597.0 ~ 88141.9 and 46932.8 ~ 72004.6, respectively , Respectively. The clearance rates were (0.076 ± 0.65) μg / L, 0.012), (0.08 ± 0.013), (0.081 ± 0.011) L.min.kg-1. There was no significant difference in mean residence time between Groups 1 and 2, with significant differences in mean residence time between Groups 1 and 2, Groups 2 and 3. CONCLUSIONS: There is no significant difference between the pharmacokinetic parameters of docetaxel alone and the pharmacokinetic parameters used with granisetron. The pharmacokinetic parameters used in combination with ondansetron, in addition to the mean residence time No significant difference.