Relative Bioavailability of Berberine Laurate Following Intestinal Administration

OBJECTIVE To investigate the pharmacokinetic characteristics and relative bioavailability of berberine laurate (BL) following intraperitoneal injection and intestinal administration using berberine sulfate (BS) as a reference. METHODS BL was synthesized by the reaction between BS and potassium laurate. MS and ¹H-NMR were used to confirm the structure. The plasma concentrations in rats were measured by HPLC. RESULTS After intraperitoneal injection, the pharmacokinetics of BL and BS in rats were best described by a two-compartment model. After intestinal administration, the relative bioavailability of BL vs BS was 224.32%. Compared with intraperitoneal injection, the relative bioavailability of BL following intestinal administration was 27.66%. CONCLUSION The oral bioavailability of berberine can be increased by improving its lipophilicity. Fatty acid salts of berberine might be potential candidates for further research.