He Wei, Qing Du, Cao De-Ying, Fan Li-Fang, Xiang Bai
Department of Pharmaceutics, School of Pharmaceutical Science, Hebei Medical University, 361, ZhongShan East Road, ShiJiaZhuang, 050017, PR China.
PDA J Pharm Sci Technol. 2008 Jul-Aug;62(4):264-72.
A combination of ethylcellulose and pectin, when applied as a film coat, has a potential value as a colon-specific delivery system. Dispersions of pectin in ethylcellulose were used as the film former for coating of 5-aminosalicylic acid (5-ASA) pellet cores. Drug release behavior was assessed, in vitro, under simulating conditions in term of pH and time in vivo during transit to the colon. Negligible drug release occurred during first 5 h, when the coated pellets were in the simulated gastric and small intestinal conditions. After that, rat cecal contents were added into the pH 6.8 medium to simulate the in vivo condition where there is the digestion of bacteria in the colon. Drug release depended on the composition of the mixed film, as well as the ratio of ethylcellulose to pectin. Drug release profiles seemed to conform to the mechanism involving the osmotically driven release and formation of channels in the film caused by dissolution of pectin. Channel formation was, in most cases, activated by the presence of rat cecal contents, showing that the pectin in the mixed film was subjected to enzymic breakdown. In conclusion, pectin could be used as an additive in ethylcellulose films to control the release of colonic delivery system. In addition, the mechanism of the hydrophilic drug release from pellets coated with ethylcellulose aqueous dispersions containing an aqueous gel-forming polymer (pectin) is also discussed.
乙基纤维素和果胶的组合作为薄膜包衣应用时,具有作为结肠特异性给药系统的潜在价值。将果胶分散在乙基纤维素中用作包衣5-氨基水杨酸(5-ASA)微丸芯的成膜材料。在体外模拟pH值和药物在体内转运至结肠过程中的时间条件下,评估药物释放行为。当包衣微丸处于模拟胃和小肠条件下时,最初5小时内药物释放可忽略不计。在此之后,将大鼠盲肠内容物加入pH 6.8的介质中,以模拟结肠中存在细菌消化的体内条件。药物释放取决于混合膜的组成以及乙基纤维素与果胶的比例。药物释放曲线似乎符合涉及渗透驱动释放和果胶溶解导致膜中形成通道的机制。在大多数情况下,通道形成是由大鼠盲肠内容物的存在激活的,这表明混合膜中的果胶受到酶解作用。总之,果胶可作为乙基纤维素膜中的添加剂用于控制结肠给药系统的释放。此外,还讨论了含有水凝胶形成聚合物(果胶)的乙基纤维素水分散体包衣微丸中亲水性药物的释放机制。