申请人:MOCHIDA PHARMACEUTICAL CO., LTD.
公开号:US20210000968A1
公开(公告)日:2021-01-07
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)
提供的是一种水溶性化合物,可以用于持续释放制剂,并能够稳定地通过使用新型潜在基材料选项海藻酸作为基材料在体内释放固定量的活性成分。本发明涉及一种通过连接剂以共价键结合非甾体类抗炎化合物和海藻酸或其盐而获得的结构的海藻酸衍生物,优选涉及由式(1)所表示的海藻酸衍生物(在该式中:(A)表示从海藻酸或其盐中派生的一个残基,并且具有构成海藻酸的L-古洛糖酸或D-甘露糖酸中的C(═O)基团的单糖;(D)表示来自非甾体类抗炎化合物的一个残基;以及-L-表示具有能够通过酰胺键与(A)结合的功能基团,并且具有能够通过酯键与(D)结合的功能基团的连接剂)。(D)-L-(A) (1)