Ursocholic acid, a hydrophilic bile acid, fails to improve liver function parameters in primary biliary cirrhosis: comparison with ursodeoxycholic acid.
OBJECTIVE
To compare the effect of short term feeding of ursocholic acid, a hydrophilic bile acid, as the unconjugated acid and the taurine conjugate, on clinical and biochemical features and bile acid metabolism with that of ursodeoxycholic acid in four patients with primary biliary cirrhosis.


METHODS
Four patients with stage II primary biliary cirrhosis were studied. Two were fed ursocholic acid (900 mg/day), and two were given tauroursocholate (900 mg/day) in three divided doses. After 1 month, all patients were given 900 mg/day of ursodeoxycholic acid. Fasting serum, bile, and 24-hour urine levels were measured before and at the end of ursocholic acid and tauroursocholate feeding and after 1 month of ursodeoxycholic acid feeding. Clinical and biochemical symptoms were measured by routine hospital methods, and bile acids were measured by gas-liquid chromatography.


RESULTS
One month of ursocholic acid or tauroursocholate feeding did not improve clinical or biochemical findings in any patient. Approximately 21-25% ursocholic acid was present in the serum and bile, with substantial metabolism to deoxycholic acid. Increased ursocholic acid was excreted in the urine. In comparison, ursodeoxycholic acid improved biochemical parameters and was 45-65% enriched in the serum and bile.


CONCLUSIONS
Ursocholic acid as the free bile acid or as taurine conjugate, although more hydrophilic, is poorly enriched in serum and bile and is ineffective in patients with primary biliary cirrhosis.
Batta
A K
AK
Department of Medicine and Liver Institute, University of Medicine and Dentistry-New Jersey Medical School, Newark, USA.
Salen
G
G
Abroon
J
J
D000410:Alanine Transaminase / Q000097:blood; D000469:Alkaline Phosphatase / Q000097:blood; D001219:Aspartate Aminotransferases / Q000097:blood; D001646:Bile / Q000737:chemistry; D001647:Bile Acids and Salts / Q000378:metabolism; D002793:Cholic Acids / Q000008:administration & dosage / Q000097:blood / Q000627:therapeutic use* / Q000652:urine; D002849:Chromatography, Gas; D003840:Deoxycholic Acid / Q000378:metabolism; D005215:Fasting; D005260:Female; D006801:Humans; D008099:Liver / Q000187:drug effects* / Q000378:metabolism / Q000503:physiopathology; D008105:Liver Cirrhosis, Biliary / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology; D010919:Placebos; D013656:Taurocholic Acid / Q000008:administration & dosage / Q000097:blood / Q000627:therapeutic use / Q000652:urine; D014580:Ursodeoxycholic Acid / Q000008:administration & dosage / Q000097:blood / Q000627:therapeutic use* / Q000652:urine
D001647:Bile Acids and Salts; D002793:Cholic Acids; D010919:Placebos; D003840:Deoxycholic Acid; D013656:Taurocholic Acid; D014580:Ursodeoxycholic Acid; D001219:Aspartate Aminotransferases; D000410:Alanine Transaminase; D000469:Alkaline Phosphatase; C030712:ursocholic acid