Walker S, Rudolph G, Raedsch R, Stiehl A
Department of Gastroenterology, Robert-Bosch-Krankenhaus, Stuttgart, Germany.
Gastroenterology. 1992 Mar;102(3):810-5. doi: 10.1016/0016-5085(92)90162-r.
Ursodeoxycholic acid (UDCA) dissolves cholesterol gallstones and improves liver function test results in patients with cholestatic liver diseases. Its absorption was studied in patients who had complete extrahepatic biliary obstruction caused by pancreatic carcinoma but no intestinal or liver disease. Six patients received 500 mg chenodeoxycholic acid (CDCA) or 250-2000 mg UDCA in capsules in single oral doses in random order, with an interval of 2 days between the different treatment regimens. In the control period the patients excreted into bile 382.3 +/- 108.0 mumol CDCA (mean +/- SD) and 1866.7 +/- 172.6 mumol cholic acid per 24 hours. After administration of 1273.6 mumol (500 mg) CDCA, biliary excretion of this bile acid increased to 1370.9 +/- 185.7 mumol/24 h, indicating an intestinal absorption rate of 77.6% +/- 9.8%. After oral administration of 636.8 mumol (250 mg), 1273.6 mumol (500 mg), 2547.2 mumol (1000 mg), and 5094.4 mumol (2000 mg) of UDCA, the respective absorption rates were 60.3% +/- 7.4%, 47.7% +/- 9.0%, 30.7% +/- 7.5%, and 20.8% +/- 3.9%, and whereas in the control period no UDCA was detected in the bile, the UDCA percentages measured were 14.6% +/- 8.2%, 19.6% +/- 9.1%, 23.1% +/- 11.3%, and 27.4% +/- 12.1%. The coadministration of CDCA did not enhance the absorption of UDCA. The data indicate that absorption of orally administered CDCA is almost complete, whereas UDCA absorption is incomplete. With increasing doses UDCA absorption decreases. To achieve absorption of adequate amounts of UDCA, high and/or multiple doses are needed.
熊去氧胆酸（UDCA）可溶解胆固醇性胆结石，并改善胆汁淤积性肝病患者的肝功能检查结果。在因胰腺癌导致完全性肝外胆管梗阻但无肠道或肝脏疾病的患者中研究了其吸收情况。6名患者以随机顺序单次口服胶囊形式给予500毫克鹅去氧胆酸（CDCA）或250 - 2000毫克UDCA，不同治疗方案之间间隔2天。在对照期，患者每24小时胆汁中排泄382.3±108.0微摩尔CDCA（平均值±标准差）和1866.7±172.6微摩尔胆酸。给予1273.6微摩尔（500毫克）CDCA后，该胆汁酸的胆汁排泄量增加至1370.9±185.7微摩尔/24小时，表明肠道吸收率为77.6%±9.8%。口服636.8微摩尔（250毫克）、1273.6微摩尔（500毫克）、2547.2微摩尔（1000毫克）和5094.4微摩尔（2000毫克）UDCA后，各自的吸收率分别为60.3%±7.4%、47.7%±9.0%、30.7%±7.5%和20.8%±3.9%，并且在对照期胆汁中未检测到UDCA，而测得的UDCA百分比分别为14.6%±8.2%、19.6%±9.1%、23.1%±11.3%和27.4%±12.1%。同时给予CDCA并未增强UDCA的吸收。数据表明口服CDCA的吸收几乎是完全的，而UDCA的吸收是不完全的。随着剂量增加，UDCA的吸收减少。为了实现足够量UDCA的吸收，需要高剂量和/或多次给药。
