Hofmann A F
Am J Clin Nutr. 1977 Jun;30(6):993-1000. doi: 10.1093/ajcn/30.6.993.
The feeding of one of the major biliary bile acids, chenodeoxycholic acid, at a dose of 10 to 15 mg/kg per day causes the circulating bile acid pool to become greatly enriched in this bile acid. When chenodeoxycholic acid composes more than 70% of the biliary bile acids, the amount of cholesterol secreted in bile falls, and bile becomes unsaturated in cholesterol. If cholesterol gallstones are present and are exposed to this unsaturated bile, they will dissolve in 4 to 24 months in the majority of patients. Extensive clinical experience indicates that such medical therapy is safe, despite unequivocal toxicity of chenodeoxycholic acid in several nonhuman primates. When therapy is stopped, bile resaturates, and stones may recur. Since cholecystecomy is a rapid, safe, effective, and usually permanent treatment for all gallstones, the value of medical therapy remains uncertain at present, except for patients in whom surgery is inadvisable. Nonetheless, the demonstration that chenodeoxycholic acid ingestion will desaturate bile and induce gallstone dissolution would appear to be an important pharmacological advance.
每天以10至15毫克/千克的剂量投喂主要胆汁酸之一的鹅去氧胆酸，会使循环胆汁酸池在这种胆汁酸中大量富集。当鹅去氧胆酸在胆汁酸中所占比例超过70%时，胆汁中分泌的胆固醇量会下降，胆汁中的胆固醇会变得不饱和。如果存在胆固醇结石并暴露于这种不饱和胆汁中，大多数患者的结石会在4至24个月内溶解。广泛的临床经验表明，尽管鹅去氧胆酸在几种非人类灵长类动物中具有明确的毒性，但这种药物治疗是安全的。当治疗停止时，胆汁会重新饱和，结石可能复发。由于胆囊切除术是对所有胆结石快速、安全、有效且通常是永久性的治疗方法，目前药物治疗的价值仍不确定，除非是不适合手术的患者。尽管如此，摄入鹅去氧胆酸会使胆汁不饱和并诱导胆结石溶解这一发现似乎是一项重要的药理学进展。
