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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Rg_1,Re,Rf,Rb_1,Rg_2,Rc,Rb_2,Rb_3,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 3h;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Rg_1,Re,Rf,Rg_2,Rc,Rd,Rb_3的水溶液均为二室模型,脂质体为一室模型;人参皂苷Rb_1的水溶液和脂质体为三室模型;Rb_2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。
The experiment to explore ginseng stem and leaf total saponin liposomes and aqueous solution in rats plasma concentrations and pharmacokinetic parameters of the difference. After intravenous injection of total ginsenosides and liposomes in rat ginseng, Rg_1, Re, Rf, Rb_1, Rg_2, Rc, Rb_2 and Rg_2 of nine main ginsenosides in plasma at different time points were detected by high performance liquid chromatography Rb_3, Rd blood concentration, by 3p97 software fitting data. After intravenous administration to rats, 9 target saponins can be measured in plasma. Aqueous solution peak time is generally 0.05 ~ 0.083 3h; liposome peak time is generally 0.5 h after. After fitting by software, the aqueous solution of ginsenosides Rg_1, Re, Rf, Rg_2, Rc, Rd, Rb_3 were two compartment model and the liposomes were one compartment model. The aqueous solution and liposome of ginsenoside Rb_1 were three compartment model. The aqueous solution of Rb_2 is a three-compartment model and the liposome is a one-compartment model. The AUC of the nine saponin liposomes was larger than the area under the curve of the aqueous solution, and the liposomes stayed longer in vivo with a slower clearance rate and a longer half-life than the aqueous solution . The results showed that pharmacokinetic parameters of the two formulations were compared by intravenous administration, the pharmacokinetics of total saponin liposomes and aqueous solution of ginseng stem and leaf were significantly different in rats, liposomes in vivo The concentration maintained for a long time, reducing the speed of drug elimination in vivo and improve drug efficacy. Compared with traditional dosage forms, ginseng stem-leaf total saponin liposomes improve the long-term drug release and play a significant role in the development of new dosage forms of ginsenoside in the future.