三七三醇皂苷两种制剂在比格犬体内的药物动力学研究

Study on pharmacokinetic behavior of two preparations about protoparaxotriol saponins in Beagle dog

目的研究三七三醇皂苷的三七通舒胶囊和三七通舒胶囊(肠溶微丸)在比格犬体内的药动学特征。方法采用双周期交叉试验设计,6只比格犬分别单剂量口服14粒三七通舒胶囊、10粒肠溶微丸,测定血浆样品中三七皂苷R1(R1)、人参皂苷Rg1(Rg1)、人参皂苷Re(Re)的含量,数据经3P87药动学软件处理。结果三七通舒胶囊、肠溶微丸中的R1、Rg1、Re在比格犬体内的药动学过程符合二室模型,三七通舒胶囊在比格犬体内的药动学特征以R1、Rg1、Re计,AUC0→t分别为10.230、10.898、6.816μg.h.mL-1,t1/2α分别为1.759、1.383、1.019 h-1,t1/2β分别为5.159、3.687、7.177 h;肠溶微丸的AUC0→t分别为10.058、13.218、6.703μg.h.mL-1,t1/2α分别为2.074、1.652、0.887 h,t1/2β分别为6.032、3.922、6.292 h。结论两制剂中3种成分的AUC0-t值无显著性差异,表明两制剂指标成分的体内过程相似,生物利用度接近。

OBJECTIVE To investigate the pharmacokinetic behavior of Sanqi Tongshu and Sanqi Tongshu capsule（enteric pellets）in beagle dogs.METHODS The cross-over design（two-periods） was employed.Six Beagle dogs were orally administrated a single dosage of 14 Sanqi Tongshu capsules and 10 Sanqi Tongshu capsule（enteric pellets）,respectively.The concentration of Notoginsenoside-R1,ginsenoside-Rg1 and ginsenoside-Re in plasma of 6 dogs at different sampling time were detemined by HPLC.The phamacokinetic parameters were calculated by 3P87 program and compared by statistic analysis.RESULTS The mean concentration-curve of Notoginsenoside-R1,ginsenoside-Rg1 and ginsenoside-Re in Sanqi Tongshu capsules and Sanqi Tongshu capsule（enteric pellets）were both fitted to two-compariment model with the main pharmacokinetic parameters as follows：AUC0→t were 10.230,10.898,6.816 μg·h·mL-1 and 10.058,13.218,6.703 μg·h·mL-1,respectively;t1/2α were 1.759,1.383,1.019 h and 2.074,1.652,0.887 h,respectively;t1/2β were 5.159,3.687,7.177 h and 6.032,3.922,6.292 h,respectively.CONCLUSION The AUC0→t of R1,Rg1 and Re in two preparations were no significant difference.Two preparations has the similar bioavailability.