Abstract

Twenty-three patients with gallstones were treated with two dosage levels of ursodeoxycholic acid, 600 mg/day and 150 mg/day. Two to three months after the treatment, the molar percentage of cholesterol in bile significantly decreased (from 7.4 to 4.5 mole % in the 600 mg group and from 7.6 to 4.0 mole % in the 150 mg group), so that bile became unsaturated in most patients in both treatment groups. However, there was no significant difference between the two groups. Biliary ursodeoxycholate increased in proportion to dose, and the sum of ursodeoxycholic acid plus chenodeoxycholic acid in biliary bile acids was over 70%. The was no significant increase in the proportion of lithocholate in bile. The major fecal bile acid of patients receiving ursodeoxycholic acid was lithocholic acid. Serum bile acid concentration rose slightly after 3 months of ursodeoxycholic acid treatment, and the major circulating bile acid became ursodeoxycholic acid. Ursodeoxycholic acid is well absorbed from intestine, undergoes little biotransformation during hepatic passage, and is 7-dehydroxylated by colonic bacteria. The litholytic activity of ursodeoxycholic acid was demonstrated in two patients receiving 450 mg and 150 mg, respectively, of the bile acid per day.

Highlights

  • Twenty-three patients with gallstoneswere treated with two dosage levels of ursodeoxycholic acid, 600 mg/day and 150 mg/day

  • Following the report by Danzinger, et al [1]that chenodeoxycholic acid (CDCA) dissolves cholesterol gallstones in man, the metabolism of CDCA has been studied in detail by many investigators [2,3].In 1975, we reported [4]that the administration of ursodeoxycholic acid (UDCA),the 7-pepimer of CDCA, reduced biliary cholesterol concentrations, and this result suggested the possibility that UDCA could dissolve gallstones [5].little work has been done to study the metabolism of UDCA in man

  • At a dose of 600 mg/day, UDCA predominated so that almost half of the biliary bile acids consisted of UDCA

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Summary

Ursodeoxycholic acid

UDCA was synthesized by Tokyo Tanabe Pharmaceutical Co. (Tokyo, Japan), and was better than 99% pure by gas-liquid chromatography and thinlayer chromatography. UDCA was synthesized by Tokyo Tanabe Pharmaceutical Co. (Tokyo, Japan), and was better than 99% pure by gas-liquid chromatography and thinlayer chromatography. All patients with radiolucent gallstones in radiologically visualizing gallbladders were treated at the Department of Medicine, Hokkaido University Hospital. The control subjects were persons without hepatobiliary diseases selected from the medical staff and nurses of our clinic

Analysis of duodenal bile
Bile acid
Analysis of serum bile acid
Changes of biliary lipid and bile acid composition in bile
Changes in fecal bile acids
Changes of serum bile acid
Mean f SD
LCA DCCAA UDCACDCA

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