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目的:建立大鼠血浆中京尼平苷和京尼平快速液相色谱-串联质谱(LC-MS/MS)检测方法,考察毒性剂量下,性别差异对京尼平苷在大鼠体内的药代动力学特征的影响。方法:将大鼠分为雌雄两组,分别灌胃给与700 mg/kg的京尼平苷水溶液,收集各时间点的大鼠血浆,采用LC-MS/MS法测定血浆京尼平苷和京尼平浓度,通过DAS 2.1.1软件计算主要药代动力学参数。结果:大鼠灌胃京尼平苷后,体内京尼平苷主要的药代动力学参数为:雄性组AUC(0-t)为(17860±6886)μg·h/L,Cmax为(3059±1499)ng/ml,t1/2为(7.4±3.4)h;雌性组AUC(0-t)为(17197±7576)μg·h/L,Cmax为(3904±1062)ng/ml,t1/2为(5.3±2.9)h。结论:灌胃700mg/kg京尼平苷后,京尼平苷药动学特征不具性别差异,而京尼平的药动学特征可能存在性别差异。
OBJECTIVE: To establish a method for the determination of geniposide and genipin in rat plasma by LC-MS / MS. To investigate the effect of geniposide on the pharmacokinetics of geniposide in rats Effect of kinetic characteristics. Methods: The rats were divided into male and female groups. The rats were administered with 700 mg / kg of geniposide solution by gavage respectively. The plasma of rats at each time point was collected. The levels of plasma geniposidase and Genipin concentrations were calculated using DAS 2.1.1 software for the main pharmacokinetic parameters. Results: The main pharmacokinetic parameters of geniposide in vivo were as follows: male AUC (0-t) was (17860 ± 6886) μg · h / L, Cmax was (3059 ± 1499 ng / ml and t1 / 2 were (7.4 ± 3.4) h, respectively. The AUC of females was (17197 ± 7576) μg · h / L and the Cmax was (3904 ± 1062) ng / / 2 is (5.3 ± 2.9) h. Conclusion: After gavage with 700 mg / kg of geniposide, the pharmacokinetics of geniposide has no gender difference, while there may be gender differences in the pharmacokinetics of genipin.