OBJECTIVE: To compare the safety and therapeutic efficacy of ursodeoxycholic acid (UDCA) and tauroursodeoxycholic acid (TUDCA) for cholesterol gallstone. METHODS: 74 patients with cholesterol gallstone were randomly divided into 2 groups. Patients were given UDCA (250 mg, tid) or TUDCA (250 mg, tid) for 6 months. The dissolution of cholesterol gallstone was compared by B-ultrasonography at the end of 3rd month and 6th month. RESULTS: After 3 months of treatment, the effective rate was 37.8% in the UDCA group and 56.8% in the TUDCA group, but the effective rate was 75.7%(28/37) in the UDCA group and 78.4%(29/37) in the TUDCA group at the end of 6th month. At the end of 3rd month, TUDCA was more effective than UDCA (P0.01). At the end of 6th month, the difference was not statistically significant. CONCLUSION: Cholesterol gallstone can be dissolved by both UDCA and TUDCA, and the difference of efficacy is not statistically significant. But the dissolution occur more rapidly with TUDCA.