【作者】 孙英华； 刘晓红； 李磊； 孙进； 何仲贵；

【Author】 Yinghua Sun,Xiaohong Liu,Lei Li,Jin Sun,Zhonggui He

【机构】 沈阳药科大学药学院生物药剂学研究室；

【摘要】 目的:制备苦参素缓释微丸和缓释片,并研究其Beagle犬体内的相对生物利用度。方法:采用离心造粒技术,选用Eudragit RS30D作为包衣材料制成膜控缓释微丸,同时制备了骨架型缓释片,用HPLC法测定Beagle犬口服苦参素缓释微丸和缓释片、市售普通胶囊(参比制剂)后不同时间血浆中的浓度,计算药物动力学参数及相对生物利用度。结果:实验研究表明自制缓释微丸的相对生物利用度103.1%;自制缓释片相对生物利用度117.6%。结论:两种自制缓释制剂与市售胶囊生物等效。更多还原

【Abstract】 OBJECTIVE To prepare kushenin sustained-release pellets and sustained-release tablets,and to study the bioavailability of these two preparations in beagle dogs.METHODS The pellets were prepared and coated using the centrifugation coating & granulating equipment.Eudragit RS30D was used as the coating material.And HPMC was used as the matrix of the sustained-release tablet.HPLC was selected to determine the concentration of the active drug-oxymatrine and its metabolite-matrine in plasma.The pharmacokinetic parameters and relative bioavailability were calculated comparing with conventional capsules.RESULTS The relative bioavailability of oxymatrine in sustained release pellets and sustained release tablets analyzed by non-compartment model theory were 103.1% and 117.6%,respectively.CONCLUSIONS Two formulations are both bioequivalent with the conventional capsules.更多还原