Abstract: The study was designed to investigate the effect of compound ursodeoxycholic acid oral liquid(C-UDCA)on acute intrahepatic cholestasis in rats, which was induced by α-naphthylisothiocyanate(ANIT, 150 mg/kg). The effects of C-UDCA were examined by serological determination, histological assessment of liver damage and bile excretion experiments. Results demonstrated that the administration of C-UDCA could significantly ameliorate ANIT-induced bile duct injury, cholestasis and hepatocytic damage. Compared with ursodeoxycholic acid(UDCA), high and mediumdoses of C-UDCA could remarkably reduce the elevated serum levels of alanine aminotransferase(ALT), while greatly enhancing the activity of Na⁺-K⁺-ATPase and SOD in liver tissues. All taken together, our data suggested that C-UDCA exhibited a better hepatoprotective effect against ANIT-induced cholestasis than UDCA.