pH 敏感性薄膜包衣高分子的合成及萘普生包衣微丸的溶出度

SYNTHESIS OF pH SENSITIVE ENTERIC COATING POLYMERS AND THE DISSOLUTION OF NAPROXEN PELLETS COATED WITH THEM

目的合成聚甲基丙烯酸甲酯－ｃｏ－甲基丙烯酸共聚物（ＰＭＭＡ－ｃｏ－ＭＡＡ）并研究其ｐＨ敏感性。方法采用自由基溶液共聚合合成共聚物；将合成物用作萘普生微丸的包衣材料进行包衣，测定萘普生包衣微丸在不同ｐＨ缓冲溶液中的溶出度。结果成功合成３种具有不同酸值的丙烯酸树脂，该树脂具有高度的ｐＨ敏感性。结论酸值不同的树脂具有不同的ｐＨ敏感值，它们分别可用作小肠和结肠给药的包衣材料。

URPOSE To synthesize pH sensitive enteric coating polymers and evaluate their pH sensitivity and site-targeting as coatings.METHODS The polymers were prepared and characterized by radical solution copolymerization and acid-base titration; the effect of pH on the dissolution of naproxen pellets coated with the synthesized polymers was done by dissolution test.RESULTS Three kinds of pH sensitive acrylic copolymers with different carboxylic group contents were successfully prepared. The synthesized substances were highly pH sensitive and the ones with lower carboxylic group contents had larger pH values.CONCLUSIONS The synthesized copolymers with different carboxylic group contents have different pH sensitive values and can potentially be used as coating for small intestine and colon targeted durg delivery.