【摘要】 目的筛选合适的释放介质,用于魔芋胶为载体结肠定位给药系统的体外评价。方法采用压制包衣法制备魔芋胶包衣片;制备含大鼠盲、结肠内容物,内容物降解酶和β-甘露聚糖酶的3种体外释放介质;通过测定不同pH、温度条件下酶的活性,比较魔芋胶包衣片在不同介质中的药物释放及衣膜溶蚀情况,筛选合适的体外释放介质。结果酶的活性研究表明,在体外释放37℃,pH 6.8介质条件下,内容物降解酶和β-甘露聚糖酶可保持较高活性(为最大酶活性的80%~90%);体外药物释放及衣膜溶蚀研究表明,在含酶介质中,魔芋胶包衣片的药物释放及衣膜溶蚀随酶浓度增加而加快(P<0.05),具有结肠定位释放特性;在含0.1 g.L-1(酶活性6.27 U.mL-1)β-甘露聚糖酶1、.0 g.L-1(酶活性7.32 U.mL-1)盲结肠内容物降解酶5、0 g.L-1大鼠盲结肠内容物的3种介质中,包衣片药物释放及衣膜溶蚀情况相似。结论含0.1 g.L-1(酶活性6.27 U.mL-1)β-甘露聚糖酶的pH 6.8磷酸盐缓冲液可有效模拟体内结肠环境,用于魔芋胶为载体结肠定位给药系统的体外评价。更多还原

【Abstract】 OBJECTIVE To select the in vitro release medium for elevating the colon-specific effect of preparations prepared with konjac glucomannan.METHODS Konjac glucomannan coated tablets were prepared by compression coating;three kinds of release medium,composed of rat ceca and colonc content,enzymes from rat cecal and colonic content and β-mannase,were prepared respectively.In vitro release medium was chosen by observing the activity of enzymes in different pH and temperature conditions,and by comparing release of berberine hydrochloride from konjac glucomannan coated tablets and coating film erosion in different release media.RESULTS The activity of enzymes in rat ceca and colon content and β-mannase were 80%～90% maximal activity of enzymes in in vitro release condition of 37 ℃ and pH（6.8）;drug released and coating film erosion were accelerated with the increase of enzyme contents（P<0.05）,konjac glucomannan coated tablets was used as colon-specific drug delivery system;drug released and erosion of film in pH 6.8 PBS with 50 g·L^-1 rat cecal and colonic content、 0.1 g·L^-1 β-mannase(6.27 U·mL^-1) or 1.0 g·L^-1 rat cecal and colonic content enzymes(7.32 U·mL^-1)were similar.CONCLUSION PBS（pH 6.8） with 0.1 g·L^-1 β-mannase(6.27 U·mL^-1)is determined as in vitro release medium to study colon-specific drug delivery system prepared with konjac glucomannan.更多还原