摘要
目的制备酒石酸美托洛尔脉冲控释微丸,并对脉冲控释微丸在Beagle犬体内的药动学进行研究。方法采用挤出-滚圆法制备载药丸芯,以水溶胀性材料CCNa(交联羧甲基纤维素钠)为内包衣溶胀层,以乙基纤维素水分散体Surelease为外包衣控释层制备酒石酸美托洛尔脉冲控释微丸;对6条Beagle犬进行双制剂双周期交叉试验,利用高效液相色谱法测定血浆中的药物浓度,用DAS2.0统计软件计算相关药动学参数。结果所制备的脉冲控释微丸体外释药时滞为4h,时滞后2.1h累积释药量大于80%(w);脉冲控释微丸在Beagle犬体内的时滞为3.2h,达峰时间为5.6h,可起到延迟释药和短程缓释的作用。
Objective To prepare metoprolol tartrate pulsatile controlled-release pellets and study its pharmacokinetics in Beagle dogs.Methods The pellets prepared by extrusion-spheronization technology were coated with CCNa as swelling layer and with ethylcellulose aqueous dispersion as controlled release layer.Drug concentration in the plasma after taking the test and reference samples was determined by HPLC method and pharmacokinetic parameters were calculated by DAS 2.0 software.Results The lag time of drug release in vitro was 4 h and the accumulative drug release was over 80% in 2.1 h after lag time.In contrast,the lag time in vivo was 3.2 h and tmax was 5.6 h.The test formulation was shown to have delayed-release property with extended-release in a short period of time in vivo.
出处
《中国药剂学杂志（网络版）》
2011年第2期30-37,共8页
Chinese Journal of Pharmaceutics：Online Edition
关键词
药剂学
酒石酸美托洛尔
脉冲控释微丸
药动学
高效液相色谱
pharmaceutics
metoprolol tartrate
pulsatile controlled-release pellets
pharmacokinetics
HPLC
