Challenor V, Waller D G, Gruchy B S, Renwick A G, George C F, McMurdo E T, McEwen J
Br J Clin Pharmacol. 1986 Nov;22(5):565-70. doi: 10.1111/j.1365-2125.1986.tb02936.x.
The pharmacokinetics of a novel 20 mg biphasic release tablet of nifedipine were compared with the conventional 10 mg capsule and 20 mg sustained release preparations in healthy volunteers. The influence of food and posture on the pharmacokinetics of the biphasic tablet were studied. In the fasting state, the time to peak concentration of nifedipine was not significantly different between the 20 mg biphasic and 20 mg sustained release tablets, but plasma concentrations were higher between 2 and 4 h after the biphasic tablet. The terminal elimination half-lives of the two formulations were similar. In subjects who fed prior to nifedipine administration there was no significant difference between either the peak plasma concentration or terminal half-life of the biphasic tablet and two 10 mg capsules of nifedipine. When the biphasic preparation was given after a standard breakfast, the time to peak plasma concentration was significantly longer and the terminal half-life shorter than when given in the fasting state. The dissolution characteristics of the biphasic tablet were influenced by prior administration of food to an extent which may be of clinical significance during twice daily administration.
在健康志愿者中，对一种新型20毫克硝苯地平双相释放片的药代动力学与传统10毫克胶囊及20毫克缓释制剂进行了比较。研究了食物和体位对双相片药代动力学的影响。在禁食状态下，20毫克双相片和20毫克缓释片的硝苯地平达峰时间无显著差异，但双相片给药后2至4小时的血浆浓度更高。两种制剂的末端消除半衰期相似。在硝苯地平给药前进食的受试者中，双相片的血浆峰浓度或末端半衰期与两粒10毫克硝苯地平胶囊之间均无显著差异。当双相制剂在标准早餐后服用时，血浆达峰时间显著延长，末端半衰期比禁食状态下给药时缩短。双相片的溶出特性在一定程度上受给药前食物的影响，这在每日两次给药时可能具有临床意义。
