Study On Degradation Of Jujuboside A In Rat's Gastrointestinal Tract And The Effect Of Sedative-hypnotic

Semen ziziphi Spinosae is the dried ripe seed of Ziziphus jujuba Mill.var.spinosa Hu ex H.F.Chou.The genuine medicinal material is grown in the Yanshan mountains and Jinxian County of Tianjin.It can nourish the liver,calm the mind and nervous system,arrest sweating,regenerate body fluid,and oppose excitement which is originated by caffeine.Contrast to the western medicine,it is effective and innocuous in sedation and hypnogenesis.This paper has studied on the absorption and metabolism of jujuboside A(Ju A)from the gastrointestinal tract of rat in vitro and in vivo respectively.It focus on the absorption of Ju A in rat's gastrointestinal tract system and the configuration of metabolites,investigate the possible metabolic pathway of Ju A in vivo.Using HPLC-MS/MS method,content of Ju A and the configuration of the metabolites which are dissociation from the reaction solutions detected.The HPLC-MS/MS method has been selected to detecte the content of Ju A and the configuration of the metabolites which are dissociation from the reaction solutions.The results are as follows:(1)In the vitro simulative environment of rat's gastrointestinal tract,the degradation of Ju A is notablely in gastric juice.The clearance speed of Ju A in rat's gastrointestinal tract is listed in the fowllowing sequence: stomach > duodenum > colon > ileum > jejunum.(2)In the culture solution of rat's enterobacteria,enzymatic reactions of Ju A began rapidly,and the curves are similar to the first dynamic process.(3)As study on the pharmacokinetics of Ju A via oral administration in rats,the biological availability of Ju A is only 1.319%.(4)In the vivo intestinal absorption experiment,ligation of rat's choledochus has significant influence to the rate of absorption,but little influence on the percent absorption..(5)In the vivo intestinal absorption experiment,the highest position of absorption rate is duodenum,and it is the optimal absorption position.The absorb effective of Ju A in rat's gastrointestinal tract is listed in the fowllowing sequence: colon > ileum > jejunum.(6)Some kinds of metabolites have been detected in rat's stomach contents and culture solution of rat's enterobacteria,including Ju B and the metabolites which have m/z of 911.5,765.4,and 471.2.Conclusion: JuA is not the main absorb modality in rat's internal after oral administration.The real potency component is the sapogenin of Ju A,which is the metabolites of rat's gastrointestinal tract.