Study On Serum Pharmacochemistry And Pharinacokinetics Of Coreopsis Tinctoria

Objective:1.We make rats as the research object,make Coreopsis tinctoria serum drug chemistry research.2.To examine the Coreopsis tinctoria main ingredients in human liver microsomal degradation.3.To study Coreopsis tinctoria Pharinacokinetics and Tissue Distribution in mice.Methods:1.On the basis of establishment of a dichromatic coreopsis high performance liquid(HPLC)fingerprint,we compare the Coreopsis tinctoria alcohol extract,blank serum and drug—containing serum of HPLC fingerprint,to determine the composition of the transition in Coreopsis tinctoria blood.2.The liver microsomes control,ethanol extract of Coreopsis tinctoria,inactivated liver microsomes and ethanol extract of Coreopsis tinctoria and liver microsomes plus Coreopsis tinctoria alcohol extract were incubated in vitro,using high performance liquid chromatography(HPLC)and Ultra Performance Liquid Chromatography-Tan dem Mass Spectrometry(UPLC-MS/MS)method,by comparing the chromatographic peak,clarify Coreopsis Tinctoria in vitro liver microsomal metabolism regulation.3.To establish HPLC determination of Flavanomarein、Marein of rats serum and tissue concentration method,on the basis of mice by gastric gavage of 11.56 g/kg of Coreopsis tinctoria alcohol extract,use HPLC to detect serum and tissue drug concentration in each time point,and drug pharmacokinetics program PK solution 2.0 TM(Summit Research Services,USA)is analyzed.Results:1.In the Coreopsis Tinctoria drug-containing serum there was 7 kinds of blood components found,including six kinds of composition,1 kind of metabolites.2.The liver microsomes control,ethanol extract of Coreopsis tinctoria,inactivated liver microsomes and ethanol extract of Coreopsis tinctoria and liver microsomes plus Coreopsis tinctoria alcohol extract were incubated in vitro,using high-performance liquid The metabolites of Chrysanthemum indicum in liver microsomes were elucidated by comparing the chromatographic peaks.3.Coreopsis tinctoria alcohol extract were infused to stomach of mice,main pharmacokinetic parameters of Flavanomarein: Tmax,Cmax,T1/2,AUC,CL were5.667 h 、 223.648μg/m L 、 4.309 h 、 2293.727μg-hr/m L 、49218.246mL/hr/kg;main pharmacokinetic parameters of Flavanomarein: Tmax,Cmax,T1/2,AUC,CL were5.000 h 、 112.683μg/m L 、 4.419 h 、 1350.050μg-hr/mL 、82957.857mL/hr/kg.Conclusion:1.Seven into the blood components may be Coreopsis tinctoria direct role in the body material,further research helps to explore its efficacy material basis and mechanism of action.2.The Coreopsis tinctoria alcohol extract in human liver microsomes under the action of drug metabolic enzymes,each component content is reduced,four kinds of material metabolism and is checked out,Flavanokanin respectively,3,4 ’,5,6-pentahydroxyflavanone,Maritimein,Marein,Okanin.3.To obtain pharmacokinetic parameters of Flavanomarein and Marein,mainly distributed in liver and kidney tissue.