Graham D J, Dow R J, Hall D J, Alexander O F, Mroszczak E J, Freedman D
Br J Clin Pharmacol. 1985;20 Suppl 1(Suppl 1):23S-28S. doi: 10.1111/j.1365-2125.1985.tb05141.x.
Studies have been carried out to investigate the disposition of nicardipine hydrochloride following intravenous and oral administration to male volunteers. Following oral administration of a radiolabelled dose, nicardipine was shown to be rapidly and extensively metabolised and to be rapidly eliminated from plasma. After intravenous infusion of nicardipine at 5 mg-1 for 3 h, plasma levels declined biexponentially, and clearance values were of the same order as hepatic blood flow. With repeated oral administration, 20 mg three times daily for 28 days, plasma levels rose over the first 3 days of administration and then declined to some extent. Possible reasons for this decline are discussed. Steady-state plasma levels and bioavailability show a nonlinear relationship with doses over the range 10-40 mg three times daily. Food consumption has been shown to reduce the bioavailability of nicardipine when the food is taken before or at the same time as nicardipine administration.
已开展研究以调查盐酸尼卡地平在静脉注射和口服给药后在男性志愿者体内的处置情况。口服放射性标记剂量后，尼卡地平显示出迅速且广泛的代谢，并从血浆中迅速消除。以5毫克/小时的速度静脉输注尼卡地平3小时后，血浆水平呈双指数下降，清除率与肝血流量处于同一水平。重复口服给药，每日三次，每次20毫克，共28天，血浆水平在给药的前3天上升，然后有所下降。讨论了这种下降的可能原因。稳态血浆水平和生物利用度在每日三次10 - 40毫克的剂量范围内与剂量呈非线性关系。已表明在进食前或与尼卡地平同时进食时，食物摄入会降低尼卡地平的生物利用度。
