Wakerly Z, Fell J T, Attwood D, Parkins D
Department of Pharmacy, University of Manchester, United Kingdom.
Pharm Res. 1996 Aug;13(8):1210-2. doi: 10.1023/a:1016016404404.
The purpose of the study was to investigate the potential of pectin, ethylcellulose combinations as a practical film coating for colonic delivery.
Combinations of pectin and ethylcellulose, in the form of an aqueous dispersion, were used as coating formulations. Paracetamol cores were used as the substrate. The coatings were assessed by a flow through dissolution system simulating in vivo conditions by changes in pH and residence time. Pectinolytic enzymes were used to simulate the bacterial flora of the colon.
Drug release was controlled by the ratio of ethylcellulose to pectin in the film coat. Increasing the proportion of ethylcellulose and increasing the coat weight reduced drug release in pH1 and pH7.4 media. The addition of pectinolytic enzymes to pH6 media increased the release of drug.
Combinations of ethylcellulose and pectin can provide protection to a drug in the upper g.i. tract while allowing enzymatic breakdown and drug release in the colon.
本研究旨在探究果胶与乙基纤维素组合作为结肠给药实用薄膜包衣的潜力。
以水分散体形式存在的果胶与乙基纤维素组合用作包衣制剂。对乙酰氨基酚片芯用作基质。通过模拟体内条件的流通溶解系统,根据pH值和停留时间的变化来评估包衣。使用果胶酶来模拟结肠的细菌群落。
药物释放受薄膜包衣中乙基纤维素与果胶比例的控制。增加乙基纤维素的比例以及增加包衣重量可降低药物在pH1和pH7.4介质中的释放。向pH6介质中添加果胶酶可增加药物释放。
乙基纤维素与果胶的组合可为药物在上消化道提供保护,同时允许其在结肠中发生酶解并释放药物。