Petit D, Bonnefis M T, Infante R
Pharmacol Res Commun. 1986 Mar;18(3):217-26. doi: 10.1016/0031-6989(86)90120-7.
The relative ability of the resin cholestyramine and sucralfate (disucrose octasulfate) to bind bile acids in the gastro intestinal tract and increase fecal bile acid excretion has been studied in normal rats under standard diet. Plasma and liver cholesterol concentrations and in vitro cholesterol synthesis from 14C-acetate by liver slices, have been determined before and after one and three weeks of drug administration (0.5 or 1.0 g/100 g food). Plasma and liver cholesterol levels were unchanged after one week of treatment, but a moderate decrease in liver cholesterol content was observed after 3 weeks administration of cholestyramine and, to a lesser extent of sucralfate. Both drugs increase fecal bile acid excretion with a definitely higher effect of cholestyramine at either dose or period of administration. However, the resin produced a higher bile acid excretion after one week than after three weeks, whereas sucralfate effect increases with the time of administration. In vitro cholesterogenesis was clearly increased by cholestyramine and moderately by sucralfate although 14C-acetate incorporation into cholesterol was not quantitatively correlated to the amount of bile acid excreted in feces. The potential interest of sucralfate as bile acid sequestrant and hypocholesterolemic agent in man deserves further investigations.
在标准饮食条件下，对正常大鼠研究了树脂消胆胺和硫糖铝（八硫酸蔗糖）在胃肠道结合胆汁酸并增加粪便胆汁酸排泄的相对能力。在给药（0.5或1.0 g/100 g食物）1周和3周前后，测定了血浆和肝脏胆固醇浓度以及肝切片由14C - 乙酸盐进行的体外胆固醇合成。治疗1周后血浆和肝脏胆固醇水平未改变，但在给予消胆胺3周后观察到肝脏胆固醇含量适度降低，硫糖铝的降低程度较小。两种药物均增加粪便胆汁酸排泄，消胆胺在任一剂量或给药期的作用都明显更强。然而，树脂在1周后比3周后产生更高的胆汁酸排泄，而硫糖铝的作用随给药时间增加。消胆胺明显增加体外胆固醇生成，硫糖铝适度增加，尽管14C - 乙酸盐掺入胆固醇的量与粪便中排泄的胆汁酸量没有定量相关性。硫糖铝作为人类胆汁酸螯合剂和降胆固醇药物的潜在价值值得进一步研究。
