烟台大学学报(自然科学与工程版)2025,Vol.38Issue(3):291-299,9.DOI:10.13951/j.cnki.37-1213/n.240202
人参皂苷Re磷脂复合物的制备及其体外释放和体内药动学评价
Preparation of Ginsenoside Re Phospholipid Complex and Evaluation of Its in vitro Release and in vivo Pharmacokinetic
摘要
Abstract
The preparation process of ginsenoside Re phospholipid complex(Re-PC)was investigated using the solvent evaporation method and further optimized with the Box-Behnken response surface method based on single-factor experiments.The physicochemical properties of Re-PC prepared under optimal conditions were analyzed by Fourier transform infrared spectroscopy(FT-IR)and oil-water partition coefficient,while the pharmacokinetic properties were evaluated through in vitro digestion and release,and in vivo pharmacokinetics in rats.The results showed that the optimal preparation conditions were as follows:tetrahydrofuran as the reaction solvent,a drug-to-lipid ratio of 1∶2,a reaction time of 2.6 hours,a reaction temperature of 45 ℃,and a ginsenoside Re mass con-centration of 2.8 mg/mL.The recombination rate of ginsenoside Re and phospholipid in the prepared Re-PC was 91.80%.FT-IR analysis indicated that hydrogen bonding occurred between ginsenoside Re and phospholipid com-plex molecules.Compared with ginsenoside Re,the oil-water distribution coefficient of Re-PC increased by 1.29 times,and the bioavailability and cumulative release rate increased from 74.80%and 33.18%to 83.32%and 53.54%,respectively.The pharmacokinetic results showed that Cmax,AUC0-t and AUC0-∞ were significantly in-creased compared with ginsenoside Re,(P<0.01),with the relative oral bioavailability increased by 1.74 times.The established Re-PC preparation process is simple and feasible,and the lipid solubility and oral bioavailability of Re-PC are significantly improved.关键词
人参皂苷Re/磷脂复合物/制备工艺/体外释放/药代动力学Key words
ginsenoside Re/phospholipid complex/preparation process/in vitro release/pharmacokinetics分类
医药卫生引用本文复制引用
赵梦健,任慧娟,周小魏,李梅,何杰,李刚,王振华,马成俊..人参皂苷Re磷脂复合物的制备及其体外释放和体内药动学评价[J].烟台大学学报(自然科学与工程版),2025,38(3):291-299,9.基金项目
山东省自然科学基金资助项目(ZR2020MH38) (ZR2020MH38)
烟台市科技创新发展计划项目(2021XDHZ078). (2021XDHZ078)