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ABSTRACT OBJECTIVE：To study the metabolic transformation of total glycosides of Cistanche deserticola in artificial gastric and intestinal juice，and to speculate its metabolic transformation pathway in vivo. METHODS：UPLC/Q-TOF-MS was adopted. The determination was performed on ACQUITY UPLC BEH column with mobile phase consisted of 0.2％ formic acid water-acetonitrile（gradient elution）at the flow rate of 0.2 mL/min. The detection wavelength was set at 330 nm，and column temperature was 25 ℃. The ion source was electrospray ion source，and mass to charge ratio（m/z）was 50→1 000. In the positive and negative ion mode，the metabolic components of the total glycosides of C. deserticola in artificial gastric and intestinal juice were identified analysis，and combined with the literature，the metabolic pathway of total glycosides of C. deserticola in artificial gastric and intestinal juice was speculated. RESULTS：After the total glycosides of C. deserticola were metabolized by artificial gastric juice，and a total of 69 components were estimated，including 14 prototype components （such as Mustard aldehyde glucoside，daucosstorol） and 55 metabolic components （such as Methyl-O-Kankanoside J，Methyl-O-Kankanoside E），it is speculated that its metabolic pathways were methylation，demethylation，hydroxylation，methoxylation，acetylation，sulfation，and glucuronidation. After the total glycosides of C. deserticola were metabolized by artificial intestinal juice，a total of 90 components were estimated，including 4 prototype components（such as Kankanoside M，Kankanoside L）and 86 metabolic components（such as Methyl-O-Kankanoside， Methyl-O-Kankanoside E）. It was speculated that its metabolic pathways were methylation， demethylation，hydroxylation，dehydroxylation，methoxylation，acetylation，sulfation and glucuronidation. CONCLUSIONS：This study preliminarily speculates that the total glycosides of C. deserticola may be metabolized by methylation，demethylation， hydroxylation and other metabolic pathway in artificial gastrointestinal juice，which may provide reference for the in vivo metabolic transformation of total glycosides of C. deserticola.
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Objective: To study the biotransformation of saikosaponin A in vitro and analyze its metabolites. Methods: Saikosaponin A was incubated in artificial gastric juice and intestinal contents of rats in anaerobic conditions, respectively, and the metabolites were analyzed and identified by HPLC-DAD-MSn. Results: By incubation of saikosaponin A in artificial gastric juice, saikosaponin b1 and g were detected in the reaction mixture. By the anaerobic incubation of saikosaponin A with intestinal flora, prosaikogenin F was soon detected, but it was further converted to saikogenin F. Conclusion: Saikosaponin A can be transformed to secondary glycosides and glycosides in artificial gastrointestinal environment. And the products can be identified by HPLC-DAD-MSn. The distribution and concentration of saikosaponin A in vivo can not reflect its fate fully, and the metabolites should be considered simutaneously.
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Objective:To study the effect of artificial gastric juice on the dissolution of schizandrin A to provide the parameters for the best extraction method of Schisandra chinensis. Methods:Schisandra chinensis was respectively extracted by artificial gastric juice and water. Schizandrin A in the extracts was determined by HPLC, and the dissolution of schizandrin A in artificial gastric juice and water was studied and compared. Results:At 60 min, schizandrin A dissolution was 0. 483% in artificial gastric juice, and 0. 362%in water. Conclusion:The dissolution of schizandrin A in artificial gastric juice is 33. 4% higher than that in water, suggesting artifi-cial gastric juice can significantly improve the dissolution of schisandrin A.
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OBJECTIVE:To study the ex vivo adsorption of montmorillonite powder to ofloxacin.METHODS:Different dosages of ofloxacin and montmorillonite powder were mixed with artificial gastric juice and artificial intestinal juice,respec?tively,which were filtrated after warmed at(37?0.5)℃in water bath for1hour,the content changes of ofloxacin were de?termined by ultraviolet spectrometry.RESULTS:The adsorption rates of montmorillonite powder to ofloxacin in artificial gastric juice and in artificial intestinal juice were(99.76?0.01)%and(99.55?0.02)%,respectively.CONCLUSIONS:Montmorillonite powder has strong adsorption to ofloxacin in both artificial gastric juice and artificial intestinal juice,there?fore,which should not be administered simultaneously in the clinic.
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This paper is to study the stability of recombinant human epidermal growth factor (rhEGF) in artificial intestinal juice and gastric juice,providing references for its clinical application in intestinal and stomach injury.RhEGF was added into artificial intestinal juice and gastric juice respectively, and the content of rhEGF was determined with RIA at preset time points. The content of rhEGF in artificial gastric juice (pH 2) and intestinal juice (pH 6.8) had a tendency to decrease as time went by,reaching 43.46% and 21.91% from their baselines 1 h later respectively. But the decrease of rhEGF reached 89.62% and 79.52% 1 h after the presence of peptic enzymes respectively. The rhEGF in the artificial intestinal juice and gastric juice was relatively stable but the process of its inactivation could be greatly expedited in the presence of peptic enzymes.