益脑康片人参皂苷Rb_1药动学及生物利用度研究

Study of pharmacokinetics in vivo and relative bioavailability on ginsenoside Rb_1 in Yinaokang tablet

考察复方片剂中人参皂苷Rb1体内药动学特征及相对生物利用度,以获得药动学参数为临床疗效提供参考依据.方法:两组大鼠分别灌服益脑康片剂混悬液及三七西洋参提取物(灌胃剂量均相当给予人参皂苷Rb190 mg/kg)后,于不同时间采集血样,用高效液相色谱仪测定血药质量浓度,通过3p97药动学软件自动拟合数据获得药动学参数.大鼠灌胃给予益脑康片剂粉末(试验制剂)及三七和西洋参提取物(参比制剂)后,人参皂苷Rb1药动学行为均符合一室模型,试验制剂药动学参数为Ka=22.217 4 h-1、t1/2Ka=0.031 1 h、Ke=0.144 5 h-1、t1/2Ke=4.7979 h、AUC=666.1752(μg/mL).h;参比制剂药动学参数为Ka=5.428 9 h-1、t1/2Ka=0.1276 h、Ke=0.134 8 h-1、t1/2Ke=5.1413 h、AUC=622.526 0(μg/mL).h.由药动学参数求得益脑康片人参皂苷Rb1的相对生物利用度为107%.实验结果表明益脑康片剂中人参皂苷Rb1在体内的分布较快而代谢排除的速度较慢.人参皂苷Rb1相对生物利用度很高,预示可有较好的疗效.

This paper discussed ginsenoside Rb1＇s internal pharmacokinetic feature and relative bioavailability in compound tablets so as to acquire pharmacokinetic parameters as a reference for clinical application.Two groups of rats were poured in the Yinaokang tablet injectable suspension and an extract in notoginseng,radix panacis quinquefolii,the blood sample was adopted at different times.Determined plasma concentration with the HPLC,and obtained pharmacokinetic parameters through the 3p97 pharmacokinetic software＇s automatically fitting data.After the rat＇s intragastric administration,filling the stomach with Yinaokang tablet powder and an extract in radix panacis quinquefolii,（the dose equals to ginsenoside Rb190 mg/kg）,ginsenoside Rb1＇s pharmacokinetic behaviors accord with one-compartment model.Pharmacokinetic parameters of the group of rats,which were filled stomachs with Yinaokang tablet,was Ka=22.217 4 h-1,t1/2Ka=0.031 1 h,Ke=0.144 5h-1,t1/2Ke=4.797 9 h,AUC=666.175 2（μg/mL） ·h pharmacokinetic parameters of the group of rats which were filled stomachs with medicinal materials was Ka=5.428 9 h-1,t1/2Ka=0.127 6 h,Ke=0.134 8 h-1,t1/2Ke=5.141 3 h,AUC=622.526 0（μg/mL）·h.107% relative bioavailability of ginsenoside Rb1 in Yinaokang tablets was obtained by pharmacokinetic parameters.Pharmacokinetics and relative bioavailability experiment indicate that ginsenoside Rb1 in Yinaokang tablets can distribute quickly,whereas the speed of metabolism and elimination was relatively slow.Relative bioavailability of glucoside Rb1 was very high.