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    Azo containing polyurethanes for drug delivery to the large intestines
    1.
    发明授权
    Azo containing polyurethanes for drug delivery to the large intestines 失效
    用于药物递送至大肠的含有偶氮的聚氨酯

    公开(公告)号：US5225514A

    公开(公告)日：1993-07-06

    申请号：US812824

    申请日：1991-12-24

    申请人： Yoshiharu Kimura ,  Soonih Kim ,  Akio Nishiura

    发明人： Yoshiharu Kimura ,  Soonih Kim ,  Akio Nishiura

    IPC分类号： A61K9/48 ,  A61K9/50 ,  C08G18/38

    CPC分类号： C08G18/3836 ,  A61K9/4891 ,  A61K9/5031 ,  A61K9/5078 ,  C08G2230/00

    摘要： A polyurethane (I) of 1000 to 100,000 in average molecular weight, comprising plural segments, which are each structural units of A-B, A-C and A-D of the formulae: ##STR1## the proportion of the said segments of A-B, A-C and A-D, i.e. x:y:z is in the molar ratio 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; each segment being produced by combining with repeat units of A, B, C and D of the formulae: ##STR2## wherein R.sup.1 is a skeleton of a diisocyanate and the three R.sup.1 's in each of segments A-B, A-C and A-D can be the same or different; aza is a group of the formula: ##STR3## wherein Y.sup.1 and Y.sup.2 which can be the same or different, are oxygen, imino(--NH--) or a group of the formula:*R.sup.6 --O, *R.sup.6 --NH, O--R.sup.6 --O, *NHCO--R.sup.6 --NH or *CONH--R.sup.6 --NH;whereinR.sup.6 is alkylene and an atom or the end of the group, marked by * is bonded to phenyl ring;R.sup.4 and R.sup.5 each are, independently, hydrogen, halogen, nitro or phenyl;R.sup.2 is polyalkylene glycol residue;Z is oxygen or imino and the two Z's are the same;R.sup.3 is alkylene or a group of the formula: ##STR4## wherein R.sup.7 and R.sup.8 which can be the same or different, are alkylene; andR.sup.9 is alkyl;each segment of the polyurethane being contained in the aforementioned proportion of x, y and z, is combined by block-type, random-type or a combination thereof, is degraded specifically in the large intestine. Therefore, by using the polyurethane as pharmaceutical adjuvants, the medicament can be delivered specifically to the large intestine and at a high concentration with hardly any degradation and absorption in the small intestine, after oral administration.

    摘要翻译： 平均分子量为1000至100,000的聚氨酯（I），包含多个片段，其各自为AB，AC和AD的结构单元，其分子式如下： AB AC和 AD 所述AB，AC和AD的区段，即x：y：z的摩尔比为0.01至0.8:0至0.80:0至0.99，条件是x，y和z的和为1.0; 每个片段通过与下式的A，B，C和D的重复单元组合来产生：A -aza-，BZR2Z和C OR3O; D其中R1是二异氰酸酯的骨架，并且段A-B，A-C和A-D中的每一个中的三个R 1可以相同或不同; 氮杂是下式的基团：其中可以相同或不同的Y1和Y2是氧，亚氨基（-NH-）或下式的基团：R6 -O，* R6-NH，O-R6-O，* NHCO-R6-NH或* CONH-R6-NH; 其中R6是亚烷基，并且由*标记的基团的原子或末端键合到苯环上; R4和R5各自独立地为氢，卤素，硝基或苯基; R2是聚亚烷基二醇残基; Z是氧或亚氨基，两个Z相同; R 3是亚烷基或下式的基团：其中可以相同或不同的R 7和R 8是亚烷基; 并且R 9为烷基; 以上述比例的x，y和z包含的聚氨酯的各段通过嵌段型，无规型或其组合组合在大肠中特异性降解。 因此，通过使用聚氨酯作为药物佐剂，可以在口服给药后，将药物特异性递送至大肠，高浓度，几乎不会在小肠中降解和吸收。