申请人:Mochida Pharmaceutical Co., Ltd.
公开号:EP3770180A1
公开(公告)日:2021-01-27
Provided is water-soluble compound that can be used in a sustained-release preparation and is capable of stably releasing a fixed amount of an active ingredient in vivo by using the novel potential base material option of alginic acid as the base material. The present invention relates to an alginic acid derivative having a structure which is obtained by covalently bonding a nonsteroidal anti-inflammatory compound and alginic acid or a salt thereof via a linker, and preferably relates to an alginic acid derivative represented by formula (1) (in the formula: (A) represents one residue derived from alginic acid or a salt thereof and having the C(=O)- group from either L-guluronic acid or D-mannuronic acid, the monosaccharides that constitute alginic acid; (D) represents one residue from a nonsteroidal anti-inflammatory compound; and -L- represents a linker having a functional group which is capable of bonding to (A) by means of an amide bond and having a functional group which is capable of bonding to (D) by means of an ester bond).
(D)-L-(A) (1)
本发明提供了一种可用于缓释制剂的水溶性化合物,通过使用藻酸作为新型潜在的基础材料选择,该化合物能够在体内稳定释放固定量的活性成分。本发明涉及一种藻酸衍生物,其结构是由非甾体抗炎化合物和藻酸或其盐通过连接剂共价键合而成,优选涉及由式(1)表示的藻酸衍生物(式中,:(A)代表来自藻酸或其盐的一个残基,其 C(=O)-基团来自构成藻酸的单糖 L-谷氨酰胺酸或 D-甘露糖酸;(D)代表来自非甾体抗炎化合物的一个残基;以及-L-代表连接体,其官能团可通过酰胺键与(A)结合,其官能团可通过酯键与(D)结合)。
(D)-L-(A) (1)