Pharmacokinetics Study On The Main Active Components Of ShenXiong In Intestinal Absorption And Metabolism In Rat Liver Microsomes Kinetics

Objective In vitro studies Caco-2 cells and rat liver microsomes as a model,The main active ingredient in Shenxiong include Danshensu,TMP,Ferulic acid orthogonal compatibility for the study.The study by absorption and metabolism to explore the main active ingredient ShenXiong orthogonal compatibility pharmacokinetic characteristics.Compatibility Law prescriptions for clinical research to provide a reference.Method 1.Establish Caco-2 cell model,MTT assay was used to select the dosing concentration.To transfer the amount for the detection of targets,ShenXiong transport capacity for the detection of target.Experimental samples were analyzed by HPLC.2.Incubated with rat liver microsomes,Cocktail probe study ShenXiong orthogonal main active ingredient compatibility for CYP450 isoforms of the enzyme in vitro inhibition characteristics.Experimental samples were analyzed by HPLC.Results 1.ShenXiong orthogonal main active ingredient compatibility;In 30 min and 60 min AP side,presumably affect concentrations of the active ingredient of the drug transshipment volume:Ferulic acid>Danshensu>TMP.When 90 min,presumably affect concentrations of the active ingredient of the drug transshipment volume:Danshensu>Ferulic acid>TMP.In 30 min and 60 min BL side,presumably affect concentrations of the active ingredient of the drug transshipment volume:Ferulic acid>Danshensu>TMP.Cocktail probe method chosen phenacetin,tolbutamide,chlorzoxazone as a probe substrate.Concentration of Danshensu,low concentration of Ferulic acid and TMP metabolism in concentration after compatibility on CYP]A2 may produce inhibition.Low concentration of Danshensu,high concentration of Ferulic acid,low concentration of TMP on CYP2E1 metabolism after compatibility may inhibit,The concentration of Danshensu and Ferulic acid,The high concentration of Danshensu and TMP concentration offerulic acid on CYP2C9 may have metabolic inibitionConclusion This research through the absorption and metabolism of ShenXiong main effective components compatibility found orthogonal,Absorption of main effective components compatibility of ShenXiong because of concentration is different,in 1 hour transfer amount are Ferulic acid>Danshensu>TMP,Inhibition of P450 enzyme CYP1A2,CYP2E1,CYP2C9 of different concentration for each.Therefore,the need to pay attention to the ratio of clinical medicine.Select the optimal absorption ratio.To avoid an adverse reaction.