Crosignani A, Battezzati P M, Setchell K D, Camisasca M, Bertolini E, Roda A, Zuin M, Podda M
Department of Internal Medicine, Ospedale S. Paolo, University of Milan, Italy.
Hepatology. 1991 Feb;13(2):339-44.
The effect of ursodeoxycholic acid administration on liver function tests and on bile acid metabolism was investigated in 18 patients with chronic active hepatitis. Three different doses of ursodeoxycholic acid--250 mg, 500 mg and 750 mg--were administered daily to each patient for consecutive 2-mo periods. The order of doses was randomly assigned according to a replicated Latin-square design. A significant decrease in serum transaminases and gamma-glutamyl transpeptidase occurred with the lowest dose of ursodeoxycholic acid, which corresponded to 4 mg/kg body wt/day, and no further significant decrease with the higher doses was seen. Biliary bile acid composition was determined by high-performance liquid chromatography and gas chromatography-mass spectrometry. At entry the relative proportions of major bile acids were similar to those observed in normal individuals. During treatment the mean percentage of ursodeoxycholic acid in bile (22% with the 250 mg dose, 32% with the 500 mg dose and 34% with the 750 mg dose) was lower than values previously reported for patients with gallstones and normal liver function. The major bile acids were cholic, chenodeoxycholic and deoxycholic acids. A number of unusual bile acids were identified by gas chromatography-mass spectrometry, but these accounted for only 3% to 5% of the total and did not change during ursodeoxycholic acid therapy. No correlation between the improvement in liver function tests and the percentage of ursodeoxycholic acid in bile existed. These data suggest that even a slight enrichment of bile with ursodeoxycholic acid, as is attained with 250 mg/day, is effective in improving biochemical markers of liver function in patients with chronic active hepatitis.
在18例慢性活动性肝炎患者中研究了熊去氧胆酸给药对肝功能检查及胆汁酸代谢的影响。对每位患者每日连续给予三种不同剂量的熊去氧胆酸——250毫克、500毫克和750毫克，为期2个月。剂量顺序根据重复拉丁方设计随机分配。最低剂量的熊去氧胆酸（相当于4毫克/千克体重/天）使血清转氨酶和γ-谷氨酰转肽酶显著降低，而较高剂量未观察到进一步显著降低。通过高效液相色谱法和气相色谱-质谱法测定胆汁胆汁酸组成。入组时主要胆汁酸的相对比例与正常个体中观察到的相似。治疗期间胆汁中熊去氧胆酸的平均百分比（250毫克剂量时为22%，500毫克剂量时为32%，750毫克剂量时为34%）低于先前报道的胆结石患者和肝功能正常患者的值。主要胆汁酸为胆酸、鹅去氧胆酸和脱氧胆酸。通过气相色谱-质谱法鉴定出一些不寻常的胆汁酸，但这些仅占总量的3%至5%，且在熊去氧胆酸治疗期间未发生变化。肝功能检查的改善与胆汁中熊去氧胆酸的百分比之间不存在相关性。这些数据表明，即使每日250毫克的剂量使胆汁中熊去氧胆酸略有富集，也能有效改善慢性活动性肝炎患者肝功能的生化指标。
