Pharmacokinetics and Relative Bioavailability Study of Berberine Hydrochloride Phytosome in Rabbits

OBJECTIVE:To study pharmacokinetics and relative bioavailability of berberine hydrochloride phytosome in rabbits.METHODS:6 rabbits were randomly divided into group A and group B.Two groups were given berberine hydrochloride or berberine hydrochloride phytosomes(50 mg·kg-1 of berberine hydrochloride) respectively.Blood samples of femoral vein were collected before administration and 0.5,1,1.5,2,3,4,6,8,10,12,24 after administration.After one week of treatment,therapy of two groups intercrossed.The concentrations of berberine hydrochloride in plasma were determined by HPLC.The pharmacokinetic parameters and relative bioavailability were calculated.RESULTS:The linear range of berberine hydrochloride was 20.0～640.0 μg·L-1(r=0.999 6).The pharmacokinetic parameters of group A vs.group B were as follows:tmax:(0.24±0.12)h vs.(0.23±0.27)h,t1/2β:(5.01±0.17) h vs.(3.80±0.16) h,cmax:(59.88±6.10) μg·L-1 vs.(194.26±8.60) μg·L-1,AUC0～24 h:(446.98±10.50) μg·h·L-1 vs.(1 110.12±28.40) μg·h·L-1.The relative bioavailability of berberine hydrochloride phytosome was(273.3±3.40)%,compared with raw material.CONCLUSIONS:Compared with raw material,berberine hydrochloride phytosomes significantly increases the plasma concentration of berberine hydrochloride and improves the relative bioavailability of it.