LACK OF EFFECT OF CHOLESTEROL ESTERASE INHIBITOR CVT 1 ON CHOLESTEROL ABSORPTION

。进行了两项临床试验，以检验这一假设 CVT-1是一种有效的胰腺胆固醇酯酶抑制剂，可降低 人体的胆固醇吸收率和低密度脂蛋白。 用氚进行胆固醇吸收的测量。 口服和静脉注射胆固醇示踪剂并在 一种使用负离子质谱学的新技术。学习 1是一项关于CVT-1治疗的随机、双盲平行研究 19名受试者每日剂量分别为0、300、1500和3000 mg。百分比 在基线时测量胆固醇吸收，并在2和6之后再次测量 治疗周无效果，低密度脂蛋白水平不变。 研究II是一项随机开放标签交叉比较 CVT-1每日3次，每次1000 mg，疗程2周，每次187.5 mg 每小时16小时/天，持续2周。胆固醇吸收率和 不同时期的血浆低密度脂蛋白水平无明显差异。我们 结论是胆固醇酯酶是 人体不需要非酯化胆固醇的吸收 研究对象。

. Two clinical trials were performed to test the hypothesis that CVT-1, a potent inhibitor of pancreatic cholesterol esterase, reduces percent cholesterol absorption and LDL cholesterol in humans. Measurements of cholesterol absorption were made with deuterated cholesterol tracers given orally and intravenously and detected in plasma by a new technique using negative ion mass spectrometry. Study 1 was a randomized, double-blind parallel study of CVT-1 treatment at doses of 0, 300, 1500, and 3000 mg/day in 19 subjects. Percent cholesterol absorption measured at baseline and again after 2 and 6 weeks showed no treatment effect and LDL cholesterol was unchanged. Study II was a randomized open-label crossover comparison between CVT-1 given as 1000 mg three times daily for 2 weeks and 187.5 mg hourly 16 hours/day for 2 weeks. Percent cholesterol absorption and plasma LDL cholesterol were not different between periods. We conclude that cholesterol esterase is not requir ed for unesterified cholesterol absorption in human subjects.