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长效心得安是一种新的制剂,它可以恒速地溶入胃肠液中,从而缓慢可控地进入血循环。以往研究表明:长效心得安比常用心得安血药峰值较低,出现峰时间较晚。但这些研究均未报道其代谢物——4-羟基心得安的药代动力学,4-羟基心得安的β-受体阻断作用与母药相当。我们比较了常用和长效心得安从治疗开始到稳态水平时心得安和4-羟基心得安的药代动力学。 10名健康男性受试者,年龄17～25岁(平均20岁),治疗方案Ⅰ给予常用心得安,每12小时160mg片剂,连续4天。在治疗方案Ⅱ中,给予长效心得安,每天一次160mg胶囊2粒,连续4天。每个受试者分二次随机接受上述二种方案,中间至少相隔10天。受试者不允许再给任何其他药物,在研究期间受试者进行正常饮食和保持轻度活动。
Long-acting propranolol is a new preparation that dissolves into the gastrointestinal fluid at a constant rate and slowly and controllably enters the blood circulation. Previous studies have shown that: long-term experience than the commonly used security Ann blood peak value is lower, peak time late. However, none of these studies reported pharmacokinetics of its metabolite, 4-hydroxy-propranolol, and the 4-hydroxy-propranolol β-blocker was comparable to the parent drug. We compared propranolol and propranolol with propranolol and propranolol from the start of treatment to steady-state levels. Ten healthy male subjects, aged 17 to 25 years (mean 20 years). Treatment regimen I was given propranolol at 160 mg tablets every 12 hours for 4 consecutive days. In the treatment program Ⅱ, given long-acting propranolol, once a day 160mg capsules 2, for 4 days. Each subject was randomized to receive either of the above two schedules at least 10 days apart. Subjects were not allowed to give any other medications and subjects were given normal diet and mild activity during the study period.