申请人:ONO PHARMACEUTICAL CO., LTD.
公开号:EP0398472A2
公开(公告)日:1990-11-22
A polyurethane (I) of 1000 to 100000 in molecular weight, comprising plural segments, which are each structural units of A-B, A-C and A-D of the formulae:
and
the molar proportion of the said segments of A-B, A-C and A-D i.e. x : y : z being 0.01 to 0.8 : 0 to 0.80 : 0 to 0.99, provided that the sum of x, y and z is 1.0; wherein R1 is a skeleton of a diisocyanate, aza is a group of the formula:
or
wherein Y' and Y2, represent oxygen, imino (-NH-) and hydrocarbon derivatives thereof;
R4 and R5 are optional substituents;
R2 is a polyalkylene glycol residue;
Z is oxygen or imino;
R3 is alkylene or the residue of an ether or secondary or tertiary amine. The polurethanes are useful for coating medicaments for release in the large intestine.
分子量为 1000 至 100000 的聚氨酯 (I),由多个区段组成,每个区段都是式中 A-B、A-C 和 A-D 的结构单元:
且
所述 A-B、A-C 和 A-D 段的摩尔比例即 x : y : z 为 0.01 至 0.8 : 0 至 0.80 : 0 至 0.99,条件是 x、y 和 z 之和为 1.0;其中 R1 为二异氰酸酯的骨架,aza 为式中的基团:
或
其中 Y' 和 Y2 代表氧、亚氨基(-NH-)及其烃衍生物;
R4 和 R5 是任选的取代基;
R2 是聚亚烷基二醇残基;
Z 是氧或亚氨基;
R3 是亚烷基或醚或仲胺或叔胺的残基。聚氨酯可用于包覆药物,以便在大肠中释放。