【摘要】 目的考察三七总皂苷与Labrafil M1944CS以不同比例混合后对大鼠体内药代动力学参数和生物利用度的影响。方法以人参皂苷Rg1为检测指标,大鼠分别灌胃三七总皂苷水溶液和三七总皂苷-Labrafil M1944CS复合溶液后,采用HPLC测定血药浓度的变化。计算其房室模型药动学参数,根据药-时曲线下面积AUCt和给药剂量,分别计算其绝对生物利用度。结果人参皂苷Rg1血浆样品在0.51~51.00μg·m L-1范围内线性关系良好(r=0.999),高、中、低3个浓度的提取回收率分别为88%、91%、88%。大鼠灌胃给予不同比例的三七总皂苷-Labrafil M1944CS复合溶液(三七总皂苷与Labrafil M1944CS比例分别为1∶0.1、1∶0.5、1∶1、1∶1.5、1∶2)和三七总皂苷水溶液,人参皂苷Rg1的达峰时间分别为0.25h、0.25h、0.5h、0.25h、0.5h、0.25h,AUCt分别为(17.54±2.95)、(11.45±0.40)、(33.22±3.98)、(23.56±0.70)、(37.96±1.12)、(16.45±2.33)μg/(h·m L),其绝对生物利用度分别为0.88%、0.58%、1.67%、1.18%、1.91%、0.83%。结论当三七总皂苷与Labrafil M1944CS比例为1∶1、1∶1.5、1∶2时能显著提高三七总皂苷的绝对生物利用度。更多还原

【Abstract】 OBJECTIVE To investigate the pharmacokinetics and bioavailability of PNS-Labrafil M1944 CS solution with different ratio in rats. METHODS The serum concentrations of ginsenoside Rg1 was detected by HPLC. The pharmacokinetics parameters and absolute bioavailability was calculated after i. g. administration PNS solution and PNS-Labrafil M1944 CS solution. RESULTS The calibration curve of Rg1 was linear at a range of 0. 51 ~51. 00μg·m L- 1(r = 0. 999). The extracted recoveries were 88%,91%,88% at high,middle and low concentrations,respectively. Rats were orally administered the PNS-Labrafil M1944 CS solution(the ratio of PNS and Labrafil M1944 CS was 1∶ 0. 1,1 ∶ 0. 5,1 ∶ 1,1 ∶ 1. 5,1 ∶ 2,respectively) and PNS solution. The peak time of Rg1 were 0. 25 h,0. 25 h,0. 5h,0. 25 h,0. 5h,0. 25 h,respectively. AUCtwere(17. 54 ± 2. 95),(11. 45 ± 0. 40),(33. 22 ± 3. 98),(23. 56 ± 0. 70),(37. 96 ± 1. 12),(16. 45 ± 2. 3) μg /(h·m L),respectively. The absolute bioavailability were0. 88%,0. 58%,1. 67%,1. 18%,1. 91%,0. 83%,respectively. CONCLUSION The PNS-Labrafil M1944 CS solution with the ratio of 1∶ 1,1∶ 1. 5,1∶ 2 can significantly improve the absolute bioavailability of PNS.更多还原