摘要
作者对单剂量口服卡托普利缓释片和市售糖衣片进行了Beagle狗和健康志愿者体内生物利用度研究,动力学特征符合一室模型。缓释片相对于糖衣片的生物利用度为131.6％(狗)和111.0％(人);缓释片的平均体内保留时间为4.52h(狗)和4.28h(人),糖衣片分别为1.96h和2.77h;缓释片的峰浓度为995.9ng/ml(狗)和126.2ng/ml(人),糖衣片为2470.8ng/ml和251.2ng/ml。血浆卡托普利浓度维持在抑制血管紧张素转化酶活性一半以上的时间,缓释片为10h,糖衣片为6h。因而预计卡托普利缓释片2次/d给药能达到糖衣片3次/d的疗效。
Bioavailable studies were performed based on plasma concentrations of captopril in 5 Beagle dogs and 5 male healthy volunteers after a single oral administration of captopril sustained-release tablet and sugar-coated tablet. A one-compartment model was adopted. Relative bioavailability of sustained-release tablet to sugar-coated one was 131.6% for dogs and 111.0% for humans. Their mean residence times (MRTs) were 4.52 h and 1.96 h in dogs, 4.28 h and 2.77 h in humans, respectively. The maximum concentrations were 995.9 ng/ml and 2470.8 ng/ml in dogs, 126.2 ng/ml and 251.2 ng/ml in humans for two kinds of tablets, respectively. The duration time, in which plasma concentration staved above 50% inhibitory concentration of angiotensin converting enzyme activity, was more than 10 h for sustained-release tablets and 6h for sugar-coated tablets at the same dose (37.5 mg). consequently, it could be expected that the sustained-release tablet dosed twice a day should have a greater efficiency than marketed sugar-coated tablet taken 3 times daily.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
1992年第3期258-261,共4页
Academic Journal of Second Military Medical University
关键词
生物学效应
卡托普利
缓释
angioteasin converting enzyme inhibitor
delayed-action preparations
biological availability
human
dogs
