Zha Lin, Zhao Yan, Zhu Hong-Yan, Cai En-Bo, Liu Shuang-Li, Yang He, Zhao Ying, Gao Yu-Gang, Zhang Lian-Xue
Chinese Medicine Material College of Jilin Agricultural University, Changchun 130118, China.
Zhongguo Zhong Yao Za Zhi. 2017 May;42(10):1957-1963. doi: 10.19540/j.cnki.cjcmm.20170224.003.
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.
本实验旨在研究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差异，如人参皂苷Rg₁、Re、Rf、Rb₁、Rg₂、Rc、Rb₂、Rb₃、Rd。大鼠静脉注射脂质体与水溶液后，从股静脉取血，采用高效液相色谱法检测不同时间点上述9种人参皂苷单体的血药浓度。绘制浓度 - 时间曲线，并用3p97药代动力学软件计算药代动力学参数。大鼠静脉注射人参皂苷后，血浆中检测到9种人参皂苷。总体而言，这些人参皂苷中，水溶液的达峰时间在0.05至0.083 3小时之间，脂质体的血药浓度峰值通常在0.5小时后出现。经软件拟合，人参皂苷单体Rg₁、Re、Rf、Rg₂、Rc、Rd、Rb₃的水溶液为二室模型，脂质体为一室模型；人参皂苷单体Rb₁的水溶液和脂质体均为三室模型；人参皂苷单体Rb₂的水溶液为三室模型，其脂质体为一室模型。这9种皂苷脂质体的药时曲线下面积（AUC）大于水溶液，脂质体的保留时间长于水溶液；清除率低于水溶液，半衰期长于水溶液。实验结果表明，静脉给药时两种制剂的药代动力学参数有显著差异；脂质体不仅能使药物在体内停留更长时间，还能降低消除速率，提高治疗效果。与人参茎叶总皂苷传统剂型相比，其能改善药物的缓释效果，对未来人参皂苷新剂型的研发具有重要意义。
