Donovan J M, Von Bergmann K, Setchell K D R, Isaacsohn J, Pappu A S, Illingworth D R, Olson T, Burke S K
Genzyme Drug Discovery and Development, Waltham, Massachusetts 02451, USA.
Dig Dis Sci. 2005 Jul;50(7):1232-8. doi: 10.1007/s10620-005-2765-8.
Colesevelam HC1 is a potent bile acid-binding polymer. This study's aim was to determine effects of colesevelam HCl on sterol and bile acid excretion in patients with type IIa hypercholesterolemia. Twenty-four patients (low-density lipoprotein cholesterol, 130 to 220 mg/dL) enrolled in an open-label, parallel-design study, entered an American Heart Association/National Cholesterol Education Program diet for 6 weeks and were randomized to colesevelam HCl, 2.3 or 3.8 g/day for 4 weeks. In an apparent dose-related manner, respective mean serum concentrations HCl of low-density lipoprotein cholesterol decreased by 10% (P < 0.01) and 13% (P = 0.05), mean total cholesterol levels decreased by 4.9% (P = 0.05) and 6.1% (P = 0.09), and total fecal bile acid excretion showed median changes of +324% (P < 0.05) and +316% (P < 0.05). Colesevelam HCl did not affect fecal neutral sterol or fecal fatty acid excretion; however, 24-hr urinary mevalonic acid levels significantly increased in both treatment groups (P < 0.05). The cholesterol-lowering action of colesevelam HCl appears to be mediated through increased bile acid excretion.
考来维仑盐酸盐是一种有效的胆汁酸结合聚合物。本研究的目的是确定考来维仑盐酸盐对IIa型高胆固醇血症患者甾醇和胆汁酸排泄的影响。24名患者（低密度脂蛋白胆固醇水平为130至220mg/dL）参与了一项开放标签、平行设计的研究，先采用美国心脏协会/国家胆固醇教育计划饮食6周，然后随机分为两组，分别服用每日2.3g或3.8g考来维仑盐酸盐，为期4周。以明显的剂量相关方式，低密度脂蛋白胆固醇的平均血清浓度分别下降了10%（P<0.01）和13%（P=0.05），总胆固醇水平分别下降了4.9%（P=0.05）和6.1%（P=0.09），粪便中总胆汁酸排泄量的中位数变化分别为+324%（P<0.05）和+316%（P<0.05）。考来维仑盐酸盐不影响粪便中性甾醇或粪便脂肪酸的排泄；然而，两个治疗组的24小时尿中甲羟戊酸水平均显著升高（P<0.05）。考来维仑盐酸盐的降胆固醇作用似乎是通过增加胆汁酸排泄来介导的。
