Fromm H, Roat J W, Gonzalez V, Sarva R P, Farivar S
Gastroenterology. 1983 Dec;85(6):1257-64.
In a double-blind controlled study of ursodeoxycholic acid (400 and 800 mg/day) and chenodeoxycholic acid (375 and 750 mg/day), in comparison with placebo, ursodeoxycholic acid was significantly more effective than chenodeoxycholic acid in dissolving gallstones after 12 mo of treatment. Although there continued to be better dissolution during ursodeoxycholic acid treatment (dissolution complete in 30% and partial in another 30% of the patients) than during chenodeoxycholic acid treatment (dissolution complete in 7% and partial in 40%) at 24 mo, this difference between the treatment groups was no longer statistically significant. The incidence of floating stones was significantly higher in the patients who dissolved their stones than in those who did not (p less than 0.001). The three failures of dissolution of floating stones during bile acid treatment were associated with chenodeoxycholic acid therapy--two of them with the 750-mg and the third with the 375-mg doses. Gallstone dissolution with ursodeoxycholic acid occurred in spite of a rise in biliary cholesterol saturation, which was consistent with a nonmicellar mechanism of cholelitholysis. Furthermore, more than threefold serum elevations of L-alanine aminotransferase were observed only during chenodeoxycholic acid therapy. They occurred in 2 patients treated with 375 and 750 mg/day, respectively. The enzyme levels normalized after discontinuation of chenodeoxycholic acid and have remained normal for 13 and 8 mo, respectively, after the institution of treatment with 800 mg/day of ursodeoxycholic acid. There was no correlation between the liver tests and biliary levels of lithocholic acid. Of all the symptoms studied, only constipation showed changes that approached statistical significance (p = 0.0681). There was a significant improvement of constipation in the combined chenodeoxycholic acid groups when they were compared with the combined ursodeoxycholic acid groups. The total bile acid pool expanded significantly in both the chenodeoxycholic acid and in the 800-mg ursodeoxycholic acid treatment groups. The marked increases of biliary ursodeoxycholic acid and chenodeoxycholic acid, respectively, indicated compliance with the treatment in all but 1 bile acid-treated patient. Neither serum triglycerides nor serum cholesterol showed significant changes in any of the treatment groups. The study shows that ursodeoxycholic acid dissolves gallstones faster and with fewer side effects than chenodeoxycholic acid. The results of the study are also consistent with the view that ursodeoxycholic acid is cholelitholytic at a lower dose than is chenodeoxycholic acid.
在一项关于熊去氧胆酸（400毫克/天和800毫克/天）和鹅去氧胆酸（375毫克/天和750毫克/天）的双盲对照研究中，与安慰剂相比，治疗12个月后，熊去氧胆酸在溶解胆结石方面比鹅去氧胆酸显著更有效。尽管在24个月时，熊去氧胆酸治疗期间的溶解情况（30%的患者结石完全溶解，另外30%部分溶解）仍比鹅去氧胆酸治疗期间（7%的患者结石完全溶解，40%部分溶解）更好，但治疗组之间的这种差异不再具有统计学意义。结石溶解的患者中漂浮结石的发生率显著高于未溶解结石的患者（p<0.001）。胆汁酸治疗期间，三颗漂浮结石溶解失败均与鹅去氧胆酸治疗有关——其中两颗与750毫克剂量有关，第三颗与375毫克剂量有关。尽管胆汁胆固醇饱和度升高，但熊去氧胆酸仍能溶解胆结石，这与非微胶粒溶石机制一致。此外，仅在鹅去氧胆酸治疗期间观察到L-丙氨酸转氨酶血清水平升高超过三倍。分别发生在接受375毫克/天和750毫克/天治疗的2例患者中。停用鹅去氧胆酸后酶水平恢复正常，在用800毫克/天熊去氧胆酸治疗后分别保持正常13个月和8个月。肝功能检查与石胆酸的胆汁水平之间无相关性。在所有研究的症状中，只有便秘的变化接近统计学意义（p = 0.0681）。与联合熊去氧胆酸组相比，联合鹅去氧胆酸组的便秘有显著改善。鹅去氧胆酸和800毫克熊去氧胆酸治疗组的总胆汁酸池均显著扩大。胆汁中熊去氧胆酸和鹅去氧胆酸的显著增加分别表明，除1例胆汁酸治疗患者外，所有患者均依从治疗。任何治疗组的血清甘油三酯和血清胆固醇均未显示出显著变化。该研究表明，熊去氧胆酸比鹅去氧胆酸溶解胆结石更快且副作用更少。研究结果也与以下观点一致，即熊去氧胆酸在比鹅去氧胆酸更低的剂量下具有溶石作用。
