Ursodeoxycholic acid complexation with 2-hydroxypropyl-beta-cyclodextrin increases ursodeoxycholic acid biliary excretion after single oral administration in rats

Complexation of ursodeoxycholic acid (UDCA) with 2-hydroxypropyl-beta -cycl odextrin (HP beta CD) improves the water solubility and the dissolution rat e of UDCA and may therefore increase its bioavailability. We compared the a mount and the rate of biliary excretion of UDCA and biliary lipid secretion after a single oral administration of UDCA in 3 different pharmaceutical f ormulations [UDCA-HP beta CD ('urso-beta -cyclodextrin'), UDCA suspension a nd UDCA capsule] at 3 different dosages each, in 11 groups (2 control group s) of bile fistula rats. UDCA excretion increased with an increase in dose, biliary UDCA recovery and peak secretion were significantly higher after a dministration of UDCA-HP beta CD than after UDCA in suspension or capsule. This enhancement of biliary excretion may achieve greater UDCA enrichment i n the bile acid pool than conventional pharmaceutical UDCA formulations, th is giving to UDCA-HP beta CD a considerable therapeutical potential, Copyri ght (C) 2001 S. Karger AG, Basel.