Comparison of the pharmacokinetic characteristics of icariin and icarisideIIafter administration of icariin monomer and Epimedium flavonoids in Wistar rats

OBJECTIVE To compare the pharmacokinetics of icariin and icarisideⅡin Wistar rats after administration of icariin monomer and Epimedium flavonoids.METHODS 16 Wistar rats were divided into two groups randomly and received an intragastric administration of 50 mg·kg-1 icariin monomer(5 mL·kg-1) and 0.2 g Epimedium flavonoids(containing 50 mg icariin) kg-1 body weight,respectively.The plasma samples were collected as scheduled,and icariin and icarisideⅡwere analyzed by HPLC-MS/MS.The pharmacokinetic parameters of icariin and icarisideⅡwere calculated and evaluated by non-compartment model.RESULTS The plasma concentration of icariin and icarisideⅡafter administration of icariin monomer were all higher than that after Epimedium flavonoids.The main parameters of icariin after icariin monomer and Epimedium flavonoids were shown as follows:t1/2(3.6±1.1)h and(6.0±3.4)h,tmax(1.0±0.7)h and(1.2±1.1)h,Cmax(21.0±9.1)ng·mL-1and(14.9±4.5)ng·mL-1,AUC0-12(78.5±42.6)ng·mL-1·h and(42.5±13.8)ng·mL-1·h,AUC0-∞(87.0±45.4)ng·mL-1 ·h and(51.2±13.0)ng·mL-1·h.The main parameters of icarisideⅡafter icariin monomer and Epimedium flavonoids were shown as follows: t1/2(3.0±1.4)h and(17.2±10.2)h,tmax(3.9±2.3)h and(0.9±0.5)h,Cmax(20.9±8.6)ng·mL-1 and(5.4±2.4)ng·mL-1,AUC0-12(87.1±24.8)ng·mL-1·h and(18.8±10.2)ng·mL-1·h,AUC0-∞(96.3±22.9)ng·mL-1 ·h and(35.2±8.4)ng·mL-1·h.CONCLUSION The plasma concentration of icariin and icarisideⅡafter administration of icariin monomer were all higher than that after Epimedium flavonoids.Statistical analysis of main pharmacokinetic parameters of icariin showed that AUC0-12 and AUC0-∞ have statistical significance,while all of the main pharmacokinetic parameters of icarisideⅡhave statistical significance.