哈巴俄苷在大鼠胃肠道内容物中的稳定性及其入血成分分析

Stability of Harpagoside in Gastrointestinal Contents of Rats and Analysis of Its Constituents Absorbed in Rat Serum After Oral Administration

摘要:

目的：研究哈巴俄苷在生物样品中的稳定性及其大鼠灌胃后的入血成分。方法：利用HPLC测定哈巴俄苷的含量，流动相0.03%磷酸水溶液-乙腈梯度洗脱，检测波长210 nm，计算其在各样品中的剩余率，研究哈巴俄苷在人工胃液、人工肠液、大鼠胃肠内容物及相应pH溶液中的稳定性；利用LC-MS检测大鼠灌胃给药后的血液样品，对哈巴俄苷的入血成分进行定性研究。结果：哈巴俄苷在人工肠液、大鼠小肠内容物、大鼠大肠内容物中较稳定，降解率<10%；在稀酸液、人工胃液、大鼠胃内容物中哈巴俄苷可发生降解，但降解率<15%；大鼠灌胃给予哈巴俄苷后的血液样品中检测到了哈巴俄苷、哈巴苷、肉桂酸。结论：哈巴俄苷在人工胃肠液、大鼠胃肠道内容物及相应pH溶液中较稳定，少部分在酸性环境可分解成肉桂酸及哈巴苷苷元的脱水产物；哈巴俄苷大鼠灌胃给药后主要以原型入血，在体内可代谢为肉桂酸及哈巴苷。

Abstract:

Objective: To investigate stability of harpagoside in biological fluids in vitro and analyze its constituents absorbed in rat serum after oral administration. Method: Harpagoside was dissolved in artificial gastric juice,intestinal juice and gastrointestinal contents of rats,the corresponding pH solution,respectively;then thermostatically maintained at 37℃.HPLC was used to calculate the remaining rate of harpagoside in biological samples by measuring the content of harpagoside at time intervals after degradation.Constituents absorbed in rat serum were detected by LC-MS after oral administration. Result: Harpagoside was relatively stable in artificial intestinal juice and intestinal contents of rats,its degradation rates were less than 10%;however,it could be degraded in diluted acid,artificial gastric juice and gastric contents of rats,its degradation rates were less than 15%.Harpagoside,cinnamic acid and harpagide were detected in rat serum after oral administration of harpagoside. Conclusion: Harpagoside is relatively stable in artificial gastric juice,intestinal juice as well as gastrointestinal contents of rats,and a few of it in the acidic environment can be broken into cinnamic acid and dehydration product of harpagide aglycone.Harpagoside is mainly absorbed by prototype in rat serum after oral administration,and it can be metabolized to cinnamic acid and harpagide in vivo.