硝苯吡啶控释微丸研究  

STUDIES ON THE CONTROLLED-RELEASE PELLETS OF NIFEDIPINE

作　　者：杨天华[1] 张钧寿[1] 刘国杰[1] 陈刚[2] 

机构地区：[1]中国药科大学 [2]南京军区总医院

出　　处：《药学学报》1989年第8期622-628,共7页Acta Pharmaceutica Sinica

摘　　要：国内至今尚未有硝苯吡啶缓释制剂的报道。本文研制了硝苯吡啶控释微丸,并从体外溶出、家犬及人体试验诸方面进行评价。硝苯吡啶控释微丸体外释药基本符合一级方程(K=0.23h^(-1)),而更符合Higuchi方程(K=37.05h^(-1/2));家犬体内血药浓度较国外报道的缓释微丸更平稳,人体血药浓度也较平稳,10 min左右能达20ng/ml以上,维持在20～70ng/ml的时间约为15h,生物利用度较速释微丸略高。本文还对硝苯吡啶的药动学特性作了初步探讨,硝苯吡啶体内过程符合双室模型(t_(1/2)β为3.5h)。Controlled-release pellets of nifedipine have been prepared and evaluated by in vitro and in vivo (in dogs and human bodies) tests in the study. The pellet-released drug fitted to a first-order process (K=0.23 h^(-1)) as wall as Higuchi's function (K=37.05h^(-1/2)).After administration the concentration of these pellets was more steady than that of sustained-release pellets reported in dogs. It was also found to be steady in human. The concentration reached 20 ng/ml in about 10 minutes and stayed between 20～70ng/ml within from 10 minutes to 15 hours. The bioavailability of the controlled-release pellets is a little higher than that of the conventional pellets. The pharmacokinetic character of nifedipine has primarily been explored in this article,and corresponds with a two-compartment model (t_(1/2β)=3.5h).

关 键 词：硝苯吡啶 控释微丸 

分 类 号：R965.4[医药卫生—药理学]