摘要
目的评价甘露醇-交联聚维酮复合辅料(Man-Cro)的功能性质量,并研究其在口崩片剂中的应用。方法比较甘露醇-交联聚维酮复合辅料与甘露醇、交联聚维酮及其物理混合物之间的物性表征和粉体学性质,并考察其应用于布洛芬口崩片的体外溶出及体内生物利用度。结果甘露醇-交联聚维酮复合辅料在制备形成新的类球形态,具有良好的流动性、可压性、充填性及崩解性,符合口崩片直接压片需要。利用该复合辅料制备的布洛芬口崩片,经测试体外溶出快速,并与市售布洛芬片在大鼠体内生物等效。结论甘露醇-交联聚维酮复合辅料可采用直接压片工艺制备口崩片。
OBJECTIVE To evaluate the properties of co-processed excipient of mannitol and polyplasdone （Man-Cro） and apply it in direct compression of orally disintegrating tablets. METHODS The physical and micromeritic properties of the co-processed ex- cipient were compared with those of mannitol, polyplasdone, and physical mixture of the two compounds. The interaction between the two components was studied by using FT-IR, SEM, DSC and X-RD. The flowability and compressibility of the Man-Cro co-processed excipient were also compared with the two components by determining the angle of repose, bulk density, tap-density, Carl index and Kawakita＇s equation. The co-processed excipient was applied to prepare ibuprofen orally disintegrating tablets. The in vitro dissolution and bioavailability of the tablets were evaluated. RESULTS The co-processed excipient of mannitol and polyplasdone formed novel aspheric particles after cocrystallization. The excipient showed good flowability, compressibility, filling ability and disintegrability. Compared with commercially available ibuprofen tablets, the ibuprofen orally disintegrating tablets prepared with the co-processed ex- cipient had more rapid in vitro dissolution. And the homemade and commercially available preparations were bioequivalent in rats. CONCLUSION The co-processed excipient is superior to physical mixture as drug carrier and suitable for preparation of orally disin- tegrating tablets by direct compression.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2016年第9期715-722,共8页
Chinese Pharmaceutical Journal
基金
深圳市战略新兴产业发展专项资金资助项目(JCYJ20130402144215892)
关键词
复合辅料
甘露醇
交联聚维酮
功能性
直接压片
口崩片
co-processed excipient
mannitol
polyplasdone
function
direct compression
orally disintegrating tablet
作者简介
鲁艺，男，硕士，副主任药师研究方向：药品质量控制。
通讯作者：王铁杰，女，博士，主任药师研究方向：药品质量控制、药动学和检验技术新应用等Tel：（0755）26031728 E-mail：wangtj88@163．com
