黄芪注射液多剂量给药对雷替曲塞在大鼠体内药动学行为影响

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该研究揭示了黄芪注射液多次给药对雷替曲塞大鼠体内药动学行为影响。12只SD大鼠分为多剂量组和对照组,多剂量组每天早晨8点尾静脉注射黄芪注射液,连续给药7 d。第8天早注射黄芪注射5 min后,注射雷替曲塞溶液;对照组前7天不做处理,第8天与多剂量组同时注射雷替曲塞溶液。分别于大鼠雷替曲塞给药后不同时间点采血,处理后经HPLC进样分析,并计算药动学参数。从大鼠血浆药时曲线中可以看出,多剂量组与对照组相比,各时间点浓度均较低,AUC和t1/2均值分别由56 080μg·min·L-1和15.07 min减小到35 834μg·min·L-1和8.95 min,CL则由0.51 mL·h-1提高至0.83mL·h-1,推测黄芪注射液多次给药后可影响大鼠对雷替曲塞的糖代谢和肾排泄功能,进而使其药动学行为发生变化。 The study revealed the Astragalus injection repeated administration of raltitrexed rat pharmacokinetic behavior. Twelve SD rats were divided into multi-dose group and control group. The multi-dose group was given intravenous injection of Astragalus at 8 o’clock in the morning for consecutive 7 days. On the 8th day after injection of Radix Astragali for 5 minutes, the solution of raltitrexed was injected. In the control group, no treatment was done for the first 7 days. On the 8th day, the raltitrexed solution was injected simultaneously with the multi-dose group. Blood samples were collected at different time points after administration of raltitrexed in rats. The samples were analyzed by HPLC after injection and the pharmacokinetic parameters were calculated. It can be seen from the curve of rat plasma drug time that the concentrations of AUC and t1 / 2 were decreased from 56 080 μg · min · L-1 and 15.07 min in the multi-dose group compared with the control group at each time point To 35 834μg · min · L-1 and 8.95 min, CL increased from 0.51 mL · h-1 to 0.83mL · h-1, suggesting that Astragalus injection after repeated administration may affect rat’s response to raltethedoxin Glucose metabolism and renal excretion function, and thus make its pharmacokinetic behavior change.
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