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目的:对人参皂苷Rg1与原人参三醇进行聚乙二醇修饰和表征,并考察PEG修饰前后人参皂苷Rg1在胃中的稳定性,比较修饰前后的变化。方法:选择单甲氧基聚乙二醇2000为原料,经过与丁二酸酐的催化酯化反应活化为单甲氧基聚乙二醇2000-琥珀酸单酯后,再分别与人参皂苷Rg1和原人参三醇分子耦联,并采用核磁共振等方法来表征合成产物;以大鼠为实验动物,采用UPLC方法分析样品,分别考察人参皂苷Rg1与PEG-Rg1在离体胃中的稳定性情况,并对修饰前后的变化进行比较。结果:成功合成了原人参三醇与人参皂苷Rg1的聚乙二醇修饰产物,产率分别为16.2%和17.5%;人参皂苷Rg1在胃中容易降解,2 h时降解73.2%,PEG-Rg1在2 h时仅降解18.2%,稳定性提高。结论:成功合成了人参皂苷Rg1与原人参三醇的聚乙二醇修饰产物。修饰之后可以大大提高人参皂苷Rg1在胃中的稳定性。
OBJECTIVE: To study the modification and characterization of ginsenoside Rg1 and protopanaxatriol by polyethylene glycol, and to study the stability of ginsenoside Rg1 in stomach before and after PEG modification. The changes before and after modification were compared. Methods: Monomethoxypolyethylene glycol 2000 was chosen as the raw material. After the monoester of monomethoxy polyethylene glycol 2000-succinate was catalyzed and esterified with succinic anhydride, it was respectively reacted with ginsenoside Rg1 and The original ginseng triol molecule coupling, and the use of nuclear magnetic resonance and other methods to characterize the synthesis of products; the rats as experimental animals, the UPLC method samples were analyzed, were ginsenoside Rg1 and PEG-Rg1 in isolated gastric stability , And compare the changes before and after modification. Results: Polyethylene glycol modified products of protopanaxatriol and ginsenoside Rg1 were successfully synthesized with yields of 16.2% and 17.5%, respectively. Ginsenoside Rg1 was easily degraded in the stomach and degraded 73.2% at 2 h. PEG-Rg1 At 2 h, only degradation of 18.2%, stability increased. Conclusion: Polyethylene glycol modified products of ginsenoside Rg1 and protopanaxatriol have been successfully synthesized. Modification can greatly improve the stability of ginsenoside Rg1 in the stomach.