Saano V, Raatikainen O, Paronen P, Komulainen H
Department of Pharmacology and Toxicology, University of Kuopio, Finland.
Int J Clin Pharmacol Res. 1989;9(4):247-54.
The pharmacokinetics and acute adverse effects of nifedipine were studied in a cross-over, single dose (20 mg) study on ten healthy young volunteers. From the liquid-filled capsules, nifedipine was absorbed rapidly (tmax at 30-40 min). From tablets, the peak concentration was 79-88% lower and occurred 74-133 min after ingestion; also the bioavailability was lower, as indicated by on average 39% lower area under curve values after tablets. All the volunteers experienced side-effects: the most common (nine out of the ten) and the most intense was headache. One volunteer withdrew because of unbearable vomiting and headache. Also others felt nauseous (six out of nine who continued) and four of them vomited. After tablets, the dizziness was markedly less than after capsules, but the more slowly-appearing symptoms such as headache and nausea were similar after both types of drug products. By using slow-release tablets instead of capsules it seems possible to avoid some side-effects of nifedipine, but this benefit is gained at the expense of bioavailability.
在一项针对10名健康年轻志愿者的交叉单剂量（20毫克）研究中，对硝苯地平的药代动力学和急性不良反应进行了研究。从软胶囊中，硝苯地平吸收迅速（达峰时间为30 - 40分钟）。从片剂中，峰值浓度低79 - 88%，在摄入后74 - 133分钟出现；片剂后的曲线下面积值平均低39%，这也表明其生物利用度较低。所有志愿者都出现了副作用：最常见的（十人中九人）且最严重的是头痛。一名志愿者因无法忍受的呕吐和头痛退出。其他一些人感到恶心（继续参与的九人中六人），其中四人呕吐。服用片剂后，头晕明显少于服用胶囊后，但两种剂型药物后出现较慢的症状如头痛和恶心相似。通过使用缓释片剂而非胶囊，似乎有可能避免硝苯地平的一些副作用，但这种益处是以生物利用度为代价获得的。
