二甲基亚砜和甘油对三七总皂苷在大鼠体内生物利用度的影响

Influence of Glycerol/Dimethylsulfoxide Homogeneous Solution on PNS Bioavailability in rats

目的考察不同比例的甘油、二甲基亚砜溶液对三七总皂苷在大鼠体内的药物动力学参数和生物利用度的影响。方法以人参皂苷Rg1作为检测指标,分别以静脉注射（iv）和灌胃（ig）为给药方式,采用HPLC测定大鼠血浆中人参皂苷Rg1的血药浓度,根据血浆样品中人参皂苷Rg1的经时曲线过程,计算相应的药代动力学参数及绝对生物利用度。结果大鼠分别灌胃给予100%、80%、60%、40%、20%甘油/DMSO三七总皂苷溶液及三七总皂苷水溶液后,人参皂苷Rg1的达峰时间分别为（0.25±0.00）、（0.25±0.00）、（0.25±0.00）、（0.88±0.25）、（1.00±0.00）、（0.167±0.00）h,AUC（0~t）分别为（17.72±0.65）、（12.90±0.24）、（14.50±0.45）、（23.81±2.23）、（29.99±0.80）、（5.59±0.06）μg/（min·m L）,其绝对生物利用度分别为1.17%、0.85%、0.96%、1.58%、1.99%、0.37%。结论各比例甘油/二甲基亚砜溶液及100%甘油溶液均能显著提高三七总皂苷中人参皂苷Rg1的绝对生物利用度。

OBJECTIVE To study the effect of different proportion of glycerol-DMSO solution to the pharmacokinetic parameters and the bioavailability of Ginsenosides Rg1 in rats. METHODS Using in vivo rat modle,with Ginsenosides Rg1 as detection index; intravenous（ iv） and intragastric（ ig） administration were used. Ginsenosides Rg1 blood concentration was determined by HPLC in blood plasma. The PK parameters and the absolute bioavailability were calculated based on time concentration curve of Ginse-nosides Rg1 in samples. RESULTS After i. g. administration of（ 100%,80%,60%,40%,20%） Glycerol-DMSO solutions and PNS aqueous solution in rats,the peak times were（ 0. 25 ± 0. 00）,（ 0. 25 ± 0. 00）,（ 0. 25 ± 0. 00）,（ 0. 88 ± 0. 25）,（ 1. 00 ± 0. 00） and（ 0. 167± 0. 00） h,respectively; AUC（ 0 ~ t） s were（ 17. 72 ± 0. 65）,（ 12. 90 ± 0. 24）,（ 14. 50 ± 0. 45）,（ 23. 81 ± 2. 23）,（ 29. 99 ± 0. 80）,（ 5. 59 ± 0. 06） μg /（ min·m L）,respectively; the absolute bioavailability were 1. 17%,0. 85%,0. 96%,1. 58%,1. 99% and 0. 37%,respectively. CONCLUSION It was proved that at each proportion of glycerol-DMSO solutions and 100% glycerol solution can all significantly improve absolute bioavailability of Ginsenosides Rg1.