Pharmacokinetic Study of 9-O-glucosyl-berberine in Rats

OBJECTIVE:To study the pharmacokinetic parameters of 9-O-glucosyl-berberine(BOG)synthesized by our laboratory. METHODS:Berberine,berberrubine,9-O-octyl-berberine,BOG in rat’s plasma was determinted by HPLC. The determination was performed on PREP-ODS C18(250 mm×4.6 mm,5 μm) column with mobile phase consisted of acetonitrile-acetic acid buffer solution (7.7 gammonium acetate, 12 mL glacial acetic acid, dissolved in 500 mL distilled water)=40 ∶ 60(V/V) at the flow rate of 1 mL·min-1,the column temperature was the room temperature. The detection wavelength was set at 345 nm and injection volume was 20 μL. The pharmacokinetic parameters were calculated by PKSolver software. RESULTS: The components were well-separated from other interference components without interference of impurity. The linear range of berberine was 1.0～75.0 μg·L-1. The bioavailability of 9-O-glucosyl-berberine was increased dramatically, compared with berberine berberrubine and 9-O-octyl-berberine. The Cmax and AUC0～t of 9-O-glucosyl-berberine were 63.438 μg·L-1 and 267.994 μg·h·L-1 respectively, 9.3 and 11.1 times higher than those of berberine. CONCLUSION: The trial indicates that hydrophilic glycosylated modification could increase the bioavailability of berberine.