发明名称 Azo containing polyurethanes for drug delivery to the large intestines
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: <IMAGE> A-B <IMAGE> A-C and <IMAGE> A-D 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: <IMAGE> A -aza-, B ZR2Z and C OR3O; D wherein R1 is a skeleton of a diisocyanate and the three R1'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: <IMAGE> (i) <IMAGE> (ii) wherein Y1 and Y2 which can be the same or different, are oxygen, imino(-NH-) or a group of the formula: *R6-O, *R6-NH, O-R6-O, *NHCO-R6-NH or *CONH-R6-NH; wherein R6 is alkylene and an atom or the end of the group, marked by * is bonded to phenyl ring; R4 and R5 each are, independently, hydrogen, halogen, nitro or phenyl; R2 is polyalkylene glycol residue; Z is oxygen or imino and the two Z's are the same; R3 is alkylene or a group of the formula: <IMAGE> wherein R7 and R8 which can be the same or different, are alkylene; and R9 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.
申请公布号 US5225514(A) 申请公布日期 1993.07.06
申请号 US19910812824 申请日期 1991.12.24
申请人 ONO PHARMACEUTICAL CO., LTD. 发明人 KIMURA, YOSHIHARU;KIM, SOONIH;NISHIURA, AKIO
分类号 A61K9/48;A61K9/50;C08G18/38 主分类号 A61K9/48
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