Abstract

Deuterium-labeled ursodeoxycholic acid (UDCA-d2) was synthesized from cholic acid by heterogeneous catalytic reduction of the 11, 12-unsaturated bile acid with deuterium gas. A new method for the simultaneous determination of UDCA, UDCA-d2, related bile acids and cholesterol in human bile has been developed by gas chromatography-mass fragmentography of the methyl ester trimethylsilyl ether derivatives. The glycine conjugate of 5β-chol-3-en-24-oic acid was prepared from lithocholic acid and used as an internal standard. Calibration plots gave a good linear relationship over the range of 100-500 ng of each compound, and their recoveries (95-99%) relative to the internal standard suggested that the present method is sufficiently accurate for the practical analysis of these bile acids in human bile. The method was applied to investigate the fate of UDCA-d2 orally administered to a patient with complete bile fistula.

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