| Objective:In this paper,selecting the clinical commonly used slices of gardenia fruit(GF)(raw GF,praeparatus GF,carbonized GF)as the research object,from the perspective of pharmacokinetic discusses the pharmacokinetic differences of three kinds of processed products of GF in normal and fever model rats,the study will reveal the variation and the effect material group of three kinds of processed products of GF in two different models and will provide basic experimental data and references for the investigation of the processing mechanism of GF.Methods:(1)The change patterns of the main iridoids in three kinds of decoction pieces of gardenia fruit(GF)(raw GF,praeparatus GF,carbonized GF)were investigated by using HPLC method.Simultaneous determination of the contents of 8kinds of iridoids(shanzhiside,geniposidic acid,6-alpha-Hydroxygeniposide,gardenoside,scandoside methyl ester,genipin-1-O-β-D-gentiobioside,geniposide,6"-Coumaroyl-Geniplano Glycoside)of the decoction pieces of gardenia fruit(GF)(raw GF,praeparatus GF,carbonized GF)and their extracts were carried out by HPLC.(2)A method for the simultaneous determination of 9 iridoids,namely shanzhiside,Geniposidic acid,6-alpha-Hydroxygeniposide,gardenoside,scandoside methyl ester,genipin-1-O-β-D-gentiobioside,chlorogenic acid,Geniposide,6"-Coumaroyl-Geniplano Glycoside and 1 metabolite(Genipin),in rat plasma by HPLC-MS/MS was established so as to compare the pharmacokinetics differences of iridoids in plasma of febrile rats after intragastrical administration different gardenia decoction pieces.(3)A fever model induced by 15% dry yeast was prepared and aspirin was used as the positive drug.The change of rectal temperature in rats was applied as the drug efficacy index to evaluate the antipyretic effect of different decoction pieces of gardenia on febrile rats.A method for the simultaneous determination of 9 iridoids in rat plasma by HPLC-MS/MS was established so as to compare the pharmacokinetics differences of iridoids in plasma of febrile rats after intragastrical administration different gardenia decoction pieces.Results:(1)Under 254 nm,9 types of peaks were identified for the three types of decoction pieces,namely,shanzhiside,Geniposidic acid,6-alpha-Hydroxygeniposide,gardenoside,scandoside methyl ester,genipin-1-O-β-D-gentiobioside,chlorogenic acid,Geniposide and 6 "-Coumaroyl-Geniplano Glycoside.Compare charred gardenia,gardenia charcoal with raw GF,their main peaks were basically the same,and some of the peak heights were significantly reduced.Based on this,8 kinds of iridoids(shanzhiside,Geniposidic acid,6-alpha-Hydroxygeniposide,gardenoside,Scandoside methyl ester,genipin-1-O-β-D-gentiobioside,chlorogenic,geniposide,Geniposide and6"-Coumaroyl-Geniplano Glycoside)from three kinds of gardenia decoction pieces and their extracts were measured at the same time.The contents of Geniposidic acid were carbonized GF > praeparatus GF > raw GF.The contents of the rest were generally raw GF > praeparatus GF > carbonized GF.As the roasting deepens,the destruction of most components was exacerbated,and the overall content of the 8 components was reduced.(2)A multi-component integrated pharmacokinetic evaluation was used to evaluate the differences in pharmacokinetics of different Gardenia decoction pieces in normal rats.9 components were detected in total,of which 6 components(Geniposidic acid,6-alpha-Hydroxygeniposide,gardenoside,genipin-1-O-β-D-gentiobioside,chlorogenic,geniposide,geniposide)had reached the quantitative limit.The research found that after administrating different gardenia decoction pieces to normal rats,the peak concentration of iridoids steroids in the praeparatus GF administration group was higher,followed by carbonized GF,then the raw GF.The area under the curve during the administration of the three materials were praeparatus GF > raw GF > carbonized GF.The iridoids were more easily absorbed into the blood at a certain processing temperature,but when the processing was intense,the rate of decomposition of the glycosides in vitro was faster than the rate of blood entering the body.(3)Through the comparative research on the antipyretic effects of a 15% dry yeast-induced fever model in rats,it was found that the antipyretic effect of raw GF was the strongest.After being roasted,the antipyretic effects of praeparatus GF and carbonized GF were weakened.Integrated pharmacokinetics was used to evaluate the pharmacokinetics of 6 iridoids in febrile rats and the results showed that under the pathological model,the concentration peak of iridoids in the febrile rats group after administrating raw GF was the highest,the antipyretic effect was the strongest,but the retention time was the shortest,followed by the praeparatus GF administration group,and the carbonized GF administration group which the duration of action was long but the antipyretic effect was weak.Conclusion : By analyzing the content of 8 components in different pieces of gardenia decoction pieces,the change patterns of the content of 8 components in preparing gardenia decoction pieces were preliminarily explained,and the trend of roasting gardenia makes the conversion of glycosides to aglycone.The in vivo dynamic changes of the archetypal components and metabolites of the three kinds of gardenia decoction pieces after intragastric administration in the rat plasma were measured by LC/MS,and by considering the different antipyretic effects of three pieces of gardenia decoction,the pharmacokinetics actions of different pieces of gardenia decoction in fever rats are further researched.Compared with the normal administration rat group,the concentration peak of iridoids in the febrile rat group after administrating raw GF was increased,the absorption was accelerated,the elimination was slowed and the activity of pharmacokinetics was significantly changed.It was speculated that the heat metabolism may change the liver metabolism,renal excretion and gastrointestinal transport status in rats,which may affect the pharmacokinetic parameters.From the perspective of pharmacokinetics,this article investigated the rationality of the preparation of gardenia decoction pieces so as to lay the foundation for exploring the processing mechanism of gardenia decoction pieces. |
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