Study on Preparation and Releasing Characteristics in vitro of Weiyoukang Intragastric Floating Tablet / 中国药房

ABSTRACT

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 reg-ulator)and magnesium stearate(lubricant)as excipients. The amounts of HPMC-K15M,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 glyc-yrrhizic 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 com-ponents. RESULTS:The optimized formulation was as follows as HPMC-K15M 40 g,octadecanol 14 g,PVP-K30 2 g for 200 tab-lets. Y2 h,Y4 h and Y8 h of berberine of preparations were 31.94%,55.88%,93.34%(RSDs were 1.2%,1.5% and 1.5%,n=3),re-spectively. T1 and T2 were about 1 min and 13 h. The drug release of four ingredients all fitted Higuchi models,and were synergis-tic 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-re-lease and balanced release of multiple indigents.