Tvorogova M G, Lupanov V P, Nuraliev E Iu, Zaĭtseva T M, Kukharchuk V V, Titov V N
Ter Arkh. 1998;70(8):17-21.
Evaluation of effectiveness of hypolipidemic action of probucol in doses 500 and 1000 mg/day and comparison of probucol blood concentrations on the treatment month 3 and 6.
Probucol (Akrikhin, Russia) was given to 41 patients with primary hypercholesterolemia in a dose 500 mg/day. 3 months later the patients were divided into two groups. Group 1 patients exhibited a > 10% decrease in cholesterol levels and continued to take probucol in the dose 500 mg/day. Group 2 patients were crossed over to higher cholesterol dose--up to 1000 mg/day. Lipids levels were measured by enzyme tests, apoproteins--by immunoturbidimetry and immunodiffusion, probucol concentrations--by high-performance liquid chromatography.
After 3 months of treatment, cholesterol lowered by 14.3 and 9.2% in groups 1 and 2, respectively. After 6 months, by 19.7 and 12.9%, respectively. Probucol concentrations in blood were higher after 6 months of treatment than after 3 months in both groups. No significant differences existed between the groups by probucol concentrations in 3 and 6 months.
Hypolipidemic effect of probucol depended on the individual features of lipoproteins metabolic disorders rather than the drug blood concentration. Larger probucol doses fail to reduce cholesterol further.
评估剂量为500毫克/天和1000毫克/天的普罗布考降血脂作用的有效性,并比较治疗第3个月和第6个月时普罗布考的血药浓度。
将普罗布考(俄罗斯阿克里欣公司生产)给予41例原发性高胆固醇血症患者,剂量为500毫克/天。3个月后,将患者分为两组。第1组患者胆固醇水平下降超过10%,继续服用500毫克/天的普罗布考。第2组患者交叉使用更高剂量的普罗布考——高达1000毫克/天。血脂水平通过酶法检测,载脂蛋白通过免疫比浊法和免疫扩散法检测,普罗布考浓度通过高效液相色谱法检测。
治疗3个月后,第1组和第2组的胆固醇分别降低了14.3%和9.2%。6个月后,分别降低了19.7%和12.9%。两组治疗6个月后的血药浓度均高于治疗3个月后的血药浓度。两组在第3个月和第6个月时的普罗布考浓度无显著差异。
普罗布考的降血脂作用取决于脂蛋白代谢紊乱的个体特征,而非药物血药浓度。更大剂量的普罗布考不能进一步降低胆固醇。