Parmacokinetics of bacalin and berberine Gonglao Quhuo tablets in rats

OBJECTIVE To establish a method for simultaneous determination of baicalin and berberine in plasma,which as major index components in Gonglao Quhuo tablets,study of baicalin and berberine in rats in vivo to discuss the effect on pharmacokinetic.METHODS After intragastic administration of Gonglao Quhuo tablets,the plasma was collected at different times from untreated to treated groups for 24 h,and then baicalin and berberine concentration in rat plasma were determined.The data were calculated with 3p97 software,and then compared with pertinent literature.RESULTS The liner range of baicalin and berberine were 0.061-3.91 μg·ml-1(r=0.9997)and 0.017-1.06 μg·ml-1(r=0.9999),respectively.The lower limit of quantitation(LLOQ)of baicalin and berberine were 0.061 μg·ml-1 and 0.017 μg·ml-1,with accuracy and precision conformed to the requirement of biological specimen analysis.The distribution of bacailin and berberine in rats were conformed to be a two-compartment model and one-compartment model,respectively.The important pharmacokinetic parameters of baicalin:K21 was 0.740±0.30 1/h,K10 was 0.143±0.035 1/h,K12 was 1.26±0.8 1/h,t1/2β and t1/2α were 13.5±1.0 h and 0.40±0.18 h,Tmax was 0.352±0.086 h,Cmax was 0.940±0.18 μg·ml-1,respectively.The important pharmacokinetic parameters of berberine:t1/2(Ke)was 3.65±0.69 h,t1/2(Ka)was 0.073±0.019 h,t1/2(Km)was 0.076±0.022 h,Tmax was 0.605±0.12 h,Cmax was 0.254±059 μg·ml-1,respectively.CONCLUSION The established method was simple and suitable for determination of plasma concentration of baicalin and berberine.Their pharmacokinetics were influened by the medication form and the components of the TCM.