杠柳毒苷在模拟消化液中的稳定性研究

Stability of periplocin in the mimetic digestive fluid

[目的]考察杠柳毒苷在模拟人体消化道液中的稳定性。[方法]配制不同pH值的模拟消化液,采用高效液相色谱法,检测杠柳毒苷在各种模拟消化液中的含量变化,并利用薄层鉴别、高效液相色谱-质谱联用法对水解产物进行定性分析。[结果]杠柳毒苷在模拟空腹胃液(pH=1.2)中1 h含量降低22.2%,其水解产物为脱去两分子糖的杠柳苷元;在模拟进食胃液、小肠液、大肠液中0～6 h含量均无变化。[结论]杠柳毒苷在不同pH值的模拟消化液中的稳定性不同,在模拟进食胃液、小肠液、大肠液中稳定,在模拟空腹胃液中不稳定,可被水解为杠柳苷元。模拟消化液的pH值是影响杠柳毒苷稳定性的重要因素,模拟消化液中的胃蛋白酶、胰蛋白酶不影响杠柳毒苷的稳定性。

[Objective] To investigate the stability of Periplocin in mimetic gastrointestinal fluids. [Methods] Different pH values of mimetic gastrointestinal fluids were prepared. High performance liquid chromatography （HPLC） method was used to detect the variation of Periplocin in mimetic gastrointestinal fluids and the hydrolysate was qualified by thin layer chromatography （TLC） and HPLC coupled with mass spectrometry （LC-Ms）. [Results] The content of Periplocin decreased to 22.2% in an hour in mimetic gastric fluid in fasting state （pH=1.2）, the hydrolysate was periplogenin. However, there wasn＇t evident variation up to 6 hours in mimetic gastric fluid, small intestinal fluid and large intestinal fluid in feeding state. [Conclusions] The stability of Periplocin is different in different pH values of mimetic gastrointestinal fluids. It was stable in mimetic gastric fluid, small intestinal fluid and large intestinal fluid in feeding state but not in gastric fluid in fasting state and can be hydrolyzed into periplogenin. The stability of Periplocin in mimetic gastrointestinal fluids was pH-dependent and wasn＇t influenced by pepsin and trypsin.