Raedsch R, Stiehl A, Götz R, Walker S, Kommerell B
Z Gastroenterol. 1981 Apr;19(4):159-63.
Cheno- and ursodeoxycholic acid feeding are both efficient in conservative gallstone therapy. Urso decreases biliary cholesterol excretion even more than cheno. Glyco-urso becomes dose dependent the predominant bile acid conjugate in bile under urso feeding. We therefore studied the kinetics of cholesterol gallstone dissolution in aqueous solutions of 100 mM glyco-cheno, 100 mM glyco-urso, and mixtures of both consisting of 40 mM glyco-urso plus 60 mM glyco-cheno and 80 mM glyco-urso plus 20 mM glyco-cheno in vitro. The daily dissolution rates of cholesterol achieved by these solutions were for 100 mM glyco-cheno 0.87 +/- 0.1 mg (mean +/- SEM), for 40 mM glyco-urso plus 60 mM glyco-cheno 0.28 +/- 0.003 mg, for 80 mM glyco-urso plus 20 mM glyco-cheno 0.07 +/- 0.002 mg, and for 100 mM glyco-urso 0.07 +/- 0.03 mg. Correspondingly were the weight decreases of the gallstones by 100 mM glyco-cheno 1.2 +/- 0.1 mg/day, by 40 mM glyco-urso plus 60 mM glyco-cheno 0.3 +/- 0.01 mg/day, by 80 mM glyco-urso plus 20 mM glyco-cheno 0.11 +/- 0.02 mg/day, and by 100 mM glyco-urso 0.1 +/- 0.02 mg/day. Complete gallstone dissolution occurred during the observation time of 4 months only by 100 mM glyco-cheno in 12.8 +/- 3.3 weeks. Thus glyco-urso dissolves only little cholesterol and decreases the speed of cholesterol gallstone dissolution. It is concluded that high doses of urso in gallstone therapy which lead to great amounts of glyco-urso in bile may diminish gallstone dissolution rates.
鹅去氧胆酸和熊去氧胆酸给药在保守性胆结石治疗中均有效。熊去氧胆酸比鹅去氧胆酸更能降低胆汁中胆固醇的排泄。在给予熊去氧胆酸时，甘氨熊去氧胆酸成为胆汁中主要的胆汁酸共轭物，且呈剂量依赖性。因此，我们在体外研究了胆固醇胆结石在100 mM甘氨鹅去氧胆酸、100 mM甘氨熊去氧胆酸以及由40 mM甘氨熊去氧胆酸加60 mM甘氨鹅去氧胆酸和80 mM甘氨熊去氧胆酸加20 mM甘氨鹅去氧胆酸组成的两者混合物的水溶液中的溶解动力学。这些溶液实现的胆固醇每日溶解速率分别为：100 mM甘氨鹅去氧胆酸0.87±0.1毫克（平均值±标准误），40 mM甘氨熊去氧胆酸加60 mM甘氨鹅去氧胆酸0.28±0.003毫克，80 mM甘氨熊去氧胆酸加20 mM甘氨鹅去氧胆酸0.07±0.002毫克，以及100 mM甘氨熊去氧胆酸0.07±0.03毫克。相应地，胆结石的重量减轻分别为：100 mM甘氨鹅去氧胆酸1.2±0.1毫克/天，40 mM甘氨熊去氧胆酸加60 mM甘氨鹅去氧胆酸0.3±0.01毫克/天，80 mM甘氨熊去氧胆酸加20 mM甘氨鹅去氧胆酸0.11±0.02毫克/天，以及100 mM甘氨熊去氧胆酸0.1±0.02毫克/天。仅在12.8±3.3周内，100 mM甘氨鹅去氧胆酸在4个月的观察期内实现了胆结石的完全溶解。因此，甘氨熊去氧胆酸仅溶解少量胆固醇并降低胆固醇胆结石的溶解速度。得出的结论是，胆结石治疗中高剂量的熊去氧胆酸导致胆汁中大量甘氨熊去氧胆酸，可能会降低胆结石的溶解速率。
