胃幽康胃漂浮片的制备及其体外释药特性研究  

Study on Preparation and Releasing Characteristics in vitro of Weiyoukang Intragastric Floating Tablet

作　　者：杨晨[1] 杨志洁[1] 邱余新[1] 蔡宝昌[2] 李伟东[2] 

机构地区：[1]溧阳市中医院药剂科,江苏溧阳213300 [2]南京中医药大学药学院,南京210023

出　　处：《中国药房》2015年第31期4409-4411,共3页China Pharmacy

基　　金：常州市卫生局科技项目(No.WZ201228)

摘　　要：目的:制备胃幽康胃漂浮片并考察其体外释药特性。方法:以羟丙基甲基纤维素K15M(HPMC-K15M,骨架材料)、十八醇(低密度助漂剂)、碳酸氢钠(发泡剂)、聚乙烯基吡咯烷酮K30(PVP-K30,释放调节剂)、硬脂酸镁(润滑剂)为辅料,采用全粉末压片法制备胃幽康胃漂浮片。以小檗碱2、4、8 h的累积释放度(Y2 h、Y4 h、Y8 h)为指标,起飘时间(T1)和持续漂浮时间(T2)为辅助指标,采用正交试验对HPMC-K15M、十八醇、PVP-K30用量进行优选,并进行验证。以释放模型拟合法、Peppas方程拟合法考察所制制剂中主要臣药黄连、延胡索、黄芩和甘草中有效成分小檗碱、延胡索乙素、黄芩苷和甘草酸的释药规律;并以相似因子(f2)法考察4种有效成分的释药相似性。结果:最优处方为HPMC-K15M 40 g、十八醇14 g、PVP-K30 2 g(200片量)。所制制剂中小檗碱Y2 h、Y4 h、Y8 h分别为31.94%、55.88%、93.34%(RSD为1.2%、1.5%、1.5%,n=3),T1、T2分别在1 min和13 h左右;4种成分释药特性均符合Higuchi模型;均为扩散协同骨架溶蚀作用;f2均大于80,各成分均衡释放。结论:成功制得起飘时间快、持飘时间长,且具有缓释和多成分均衡释药特性的胃幽康胃漂浮片。OBJECTIVE：To prepare Weiyoukang intragastric floating tablet,and to investigate in vitro releasing characteristics of it. METHODS：Weiyoukang intragastric floating tablet was prepared by full powder compression method using HPMC-K15M（framework material）,octadecanol（low density bleaching promoter）,sodium bicarbonate（foaming agent）,PVP-K30（release regulator）and magnesium stearate（lubricant）as excipients. The amounts of HPMC-K15 M,octadecanol and PVP-K30 were optimized by orthogonal test and validated with 2 h,4 h and 8 h accumulative release rate of berberine（Y2 h,Y4 h,Y8 h）as index,start time（T1）and duration（T2）of floating as adjunctive index. The releasing regularity of berberine,tetrahydropalmatine,baicalin and glycyrrhizic acid in Coptis chinensis,Corydalis vanhus,Scatellaria baicalensis and Glycyrrhiza uralensis were measured by release model fitting method and Peppas equarion fitting method. Similar factor（f2）method was used to investigate the similarity of 4 components. RESULTS：The optimized formulation was as follows as HPMC-K15 M 40 g,octadecanol 14 g,PVP-K30 2 g for 200 tablets. Y2 h,Y4 hand Y8 hof berberine of preparations were 31.94%,55.88%,93.34%（RSDs were 1.2%,1.5% and 1.5%,n=3）,respectively. T1 and T2were about 1 min and 13 h. The drug release of four ingredients all fitted Higuchi models,and were synergistic action of diffusion and matrix erode. The f2 were all more than 80,indicating that the release of four ingredients were similar.CONCLUSIONS：Weiyoukang intragastric floating tablet is prepared successfully,showing fast onset,long floating,sustained-release and balanced release of multiple indigents.

关 键 词：胃漂浮片 小檗碱 延胡索乙素 黄芩苷 甘草酸 

分 类 号：R943.1[医药卫生—药剂学]