Pharmacokinetic behaviors of total flavonoids from Epimedii Folium in osteoporotic rats in vivo / 中成药

ABSTRACT

AIM To investigate the pharmacokinetic behaviors of total flavonoids from Epimedii Folium in osteoporotic rats in vivo.METHODS Twelve rats were divided into model group and sham group,after which the osteoporotic rat model was established by removing bilateral ovaries.After intragastric administration with total flavonoids (500 mg/kg),HPLC-DAD was applied to detecting the plasma concentrations of total flavonoids' prototype glycosides (epimedin A,epimedin B,epimedin C,icariin) and their metabolites (sagittatoside A,sagittatoside B,2-O-rhamnosylicariside Ⅱ,baohuoside Ⅰ,icaritin) at thirteen time points (0.083,0.25,0.5,0.75,1,2,3,4,6,8,12,24 and 48 h),then the plasma concentration-time curves were drawn,followed by the calculation of pharmacokinetic parameters.RESULTS Doubled peaks were observed in the plasma concentration-time curves of total flavonoids' prototype glycosides and their metabolites in both groups.Compared with the sham group,the integrated AUC and Cmax in the model group were significantly decreased (P ＜ 0.01),as well as the prolonged t1/2 (P ＜ 0.01).CONCLUSION The in vivo absorption and metabolism of total flavonoids from Epimedii Folium are much slower in the state of osteoporosis,thus affects the efficacy.