摘要
目的研究制备盐酸拉贝洛尔时控缓释微丸。方法采用挤出滚圆法制备载药丸芯,通过流化床包衣法分别覆上交联羧甲基纤维素钠作为溶胀层、乙基纤维素和羟丙甲纤维素作为控释层制备时控缓释微丸,通过单因素考察筛选溶胀层、控释层的处方组成对体外释药性能的影响。结果以微晶纤维素、羧甲基淀粉钠和乳糖为添加剂可制得性能良好的高载药微丸。随着溶胀层厚度的增加,药物释放时滞变短,速率显著增加;随着控释层包衣厚度的增加,时滞延长,释药减慢;控释层中羟丙甲纤维素用量增加,时滞缩短;控释层中增塑剂用量增加,时滞延长。结论所得包衣微丸具有良好的释药性能,有广阔的应用前景。
Objective To develop a novel time-controlled pellets for labetalol hydrochloride with sustained-release behavior. Methods The labetalol-loaded pellets cores were prepared by extrusion-spheronization, then were coated with croscarmellose sodium as swelling layer, followed by the mixture of ethyl cellulose and hydroxypropyl methyl cel- lulose as controlled release layer via the fluid bed coating equipment. The effects of swelling layer and controlled re- lease membrane on the profile of drug release in vitro were investigated by single factor test. Results The high la- betalol-loaded pellet cores made of microcellulose, sodium carboxymethyl starch and lactose showed satisfactory char- acters. With the thickness of the swelling layer increasing, the lag time of drug release was prolonged and the release rate increased. With the increase of HPMC ratio in the controlled release layer, the lag time increased. The lag time was also prolonged with the addition of plasticizer. Conlusion The obtained pellets display good drug release behavior, which suggests a great potential in clinic application.
出处
《中国医药导报》
CAS
2016年第19期26-30,共5页
China Medical Herald
基金
浙江省药品监督管理局计划项目(2014012)
关键词
盐酸拉贝洛尔
时控缓释微丸
溶胀层
控释层
Labetalol hydrochloride
Sustained-release pellets of time-controlled
Swelling layer
Controlled-release layer
