【作者】 奚泉； 金方；

【Author】 Xiquan Jinfang (Shanghai Institute of Pharmaceutical Industry ShangHai 200437)

【机构】 上海医药工业研究院；

【摘要】 目的制备左旋沙丁胺醇时控脉冲缓释片,考察衣膜固化条件,微丸可压性等工艺因素及体内外相关性。方法采用流化床包衣法制得缓释微丸,将微丸压片后包衣制得时控脉冲缓释片。考察了不同温度、湿度条件下衣膜的愈合情况,对片芯硬度和衣膜破损程度的关系进行了研究。结果温度湿度都能加速衣膜的愈合。片子释药速度随硬度增大而增大。缓释片为一级释药模式。体内外相关系数r=0.9967。结论采用Eudragit NE 30D,辅料乙基纤维素为主要控释材料,制得了于3～4h后起效,并维持药效达8h的时控脉冲缓释片,具良好的体内外相关性。更多还原

【Abstract】 OBJECTIVE To prepare Levalbuterol pulsatile-sustained tablet,and investigate the condition of curing , compressibility of pellets, and in vivo/in vitro co-relationship. METHODS To prepare sustained release pellets using fluid bed, then to get pulsatile-sustained tablet after tabletting and coating. To investigate the degree of curing in different temperature and humidity and the relationship between hardness of tablet and damage of film. RESULTS Temperature and humidity also can speed up the curing of film. As the hardness increasing the tablet release faster. Sustained release tablet release as first order model.. Coefficeent of in vivo/in vitro co-relationship is equal to 0.9967 CONCLUSION successfully prepared pulsatile-sustained tablets using Eudragit NE 30D and ethyl cellulose as major accessories for control release, which can act after 3~4 hours of administration and maintain effect for 8h. Data indicated that pulsatile-sustained tablet have a good in vivo/in vitro co-relationship.更多还原