新型丙烯酸树脂肠溶包衣材料的合成与应用

用自由基溶液共聚合的方法合成了3种有不同羧基含量的pH敏感性甲基丙烯酸甲酯(MMA)和甲基丙烯酸(MAA)二元共聚物以及MMA,MAA与丙烯酸丁酯(BA)三元共聚物;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。结果表明:通过改变反应单体中MAA的含量,可制备有不同酸值的丙烯酸树脂;包衣微丸的萘普生溶出度与溶出介质的pH值和包衣材料的酸值密切相关,萘普生在其用作包衣材料制备的微丸中只有在较高pH值的缓冲介质中才有较高的溶出度和溶出速率;MMA,MAA和BA的三元共聚物本身具有可塑性,在用作包衣时可不再外加增塑剂。

SYNTHESIS AND APPLICATION OF NOVEL ACRYLIC RESIN AS ENTERIC COATING

The pH sensitive two- and three-component acrylic resins were synthesized by radical solution copolymerization of methyl methacrylate (MMA), methacrylic acid (MAA) and/or butyl acrylate (BA) and their acid values were measured by acid-base titration. The dissolution of naproxen pellets coated with the synthesized resins in dissolution medium of different pH value was studied. The results show that the acrylic resin with different acid value can be prepared by adjusting the monomer ratios (MMA:MAA or MMA:MAA:BA). The smaller the acid value of the resin is, the higher pH sensitive value it has. The release of naproxen from pellets coated with these resins is greatly influenced by the pH value of the dissolution medium and the pH sensitive value of the coating resin. The three-component resins are plastic and can be used as coating material without adding plastisizers.