首页|人参茎叶总皂苷脂质体与水溶液在大鼠体内的血药浓度及药代动力学参数对比分析

人参茎叶总皂苷脂质体与水溶液在大鼠体内的血药浓度及药代动力学参数对比分析

扫码查看
该试验探讨人参茎叶总皂苷脂质体与水溶液在大鼠体内的血药浓度及药代动力学参数对比差异.通过大鼠静脉注射人参茎叶总皂苷水溶液和脂质体后,用高效液相色谱法检测血浆不同时间点的9种主要人参皂苷单体Rg1,Re,Rf,Rb1,Rg2,Rc,Rb2,Rb3,Rd的血药浓度,通过3p97软件拟合数据.大鼠静脉给药后,血浆中可测得9种目标皂苷.水溶液的达峰时间一般在0.05~0.083 3 h;脂质体的达峰时间一般在0.5 h之后.经软件拟合后,人参皂苷Rg1,Re,Rf,Rg2,Rc,Rd,Rb3的水溶液均为二室模型,脂质体为一室模型;人参皂苷Rb1的水溶液和脂质体为三室模型;Rb2的水溶液为三室模型,脂质体为一室模型.9种皂苷脂质体的药-时曲线下面积(AUC)均大于水溶液的曲线下面积,而且脂质体在体内停留时间较长,清除率较水溶液的清除率慢,半衰期一般也较水溶液长.研究结果显示通过静脉注射给药方式,对2种剂型的药动学参数进行对比,人参茎叶总皂苷脂质体与水溶液在大鼠体内的药动学显著不同,脂质体使药物在体内的浓度维持较长时间,降低了药物体内消除速度,提高药物疗效.人参茎叶总皂苷脂质体与传统剂型相比,提高了药物的缓释长效,为今后研发人参皂苷新剂型起到了重要意义.
Analysis of parameters of serum concentration and pharmacokinetic of liposome and aqueous solution of toatal ginsenoside of ginseng stems and leaves in rats
The experiment was aimed to investigate the difference of plasma concentration and pharmacokinetic parameters between liposome and aqueous solution of toatal ginsenoside of ginseng stems and leaves in rats,such as ginsenosides Rg1,Re,Rf,Rb1,Rg2,Rc,Rb2,Rb3,Rd. After intravenous injection of liposome and aqueous solution in rats,the blood was taken from the femoral vein to detect the plasma concentration of the above 9 ginsenoside monomers in different time points by using HPLC. The concentration-time curve was obtained and 3p97 pharmacokinetic software was used to get the pharmacokinetic parameters. After the intravenous injection of ginsenosides to rats,nine ginsenosides were detected in plasma. In general,among these ginsenosides,the peak time of the aqueous solution was between 0.05 to 0.083 3 h,and the serum concentration peak of liposome usually appeared after 0.5 h. After software fitting,the aqueous solution of ginsenoside monomers Rg1,Re,Rf,Rg2,Rc,Rd,Rb3 was two-compartment model,and the liposomes were one-compartment model;aqueous solution and liposome of ginsenoside monomers Rb1 were three-compartment model;aqueous solution of ginsenoside monomers Rb2 was three-compartment model,and its liposome was one-compartment model. Area under the drug time curve(AUC)of these 9 kinds of saponin liposomes was larger than that of aqueous solution,and the retention time of the liposomes was longer than that of the aqueous solution;the removal rate was slower than that of the aqueous solution,and the half-life was longer than that of the water solution. The results from the experiment showed that by intravenous administration,the pharmacokinetic parameters of two formulations were significantly different from each other;the liposomes could not only remain the drug for a longer time in vivo,but also reduce the elimination rate and increase the treatment efficacy. As compared with the traditional dosage forms,the total ginsenoside of ginseng stems and leaves can improve the sustained release of the drug,which is of great significance for the research and development of new dosage forms of ginsenosides in the future.

toatal ginsenoside of ginseng stems and leavespharmacokineticliposomesolutionintravenous injection

查琳、赵岩、祝洪艳、蔡恩博、刘双利、杨鹤、赵英、郜玉钢、张连学

展开 >

吉林农业大学 中药材学院,吉林 长春 130118

人参茎叶总皂苷 药代动力学 脂质体 水溶液 静脉注射

国家重点研发计划项目国家公益性行业科研专项吉林省科技发展计划项目吉林省科技发展计划项目

2016YFC050030320130311120160307005YY20150307012YY

2017

中国中药杂志
中国药学会

中国中药杂志

CSTPCDCSCD北大核心
影响因子:1.718
ISSN:1001-5302
年,卷(期):2017.42(10)
  • 5
  • 13