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非离子型水溶性造影剂的稳定性:对其设计的影响

Stability of nonionic water-soluble contrast media: implications for their design.

作者信息

Sovak M, Ranganathan R

出版信息

Invest Radiol. 1980 Nov-Dec;15(6 Suppl):S323-8. doi: 10.1097/00004424-198011001-00068.

Abstract

The stability of the nonionic contrast media metrizamide, P-297, iopamidol, and nonionic phenyl ether DS-1-132 was studied by exposing their aqueous solutions to 120 C. Metrizamide showed decomposition of the sugar residue, while in P-297 the sugar substituent was cleaved off the triiodoaniline moiety. Iopamidol and DS-1-132 showed no decomposition. For stability, sugar moieties should be attached either by an ether linkage or as amides, as long as the acylamino group is not on a carbon adjacent to the anomeric carbon. Polyhydroxyalkylamines are less hydrophilic but more stable than sugars.

摘要

通过将非离子型造影剂甲泛葡胺、P - 297、碘帕醇和非离子型苯醚DS - 1 - 132的水溶液加热至120℃,研究了它们的稳定性。甲泛葡胺显示出糖残基的分解,而在P - 297中,糖取代基从三碘苯胺部分断裂下来。碘帕醇和DS - 1 - 132未显示出分解。为了保证稳定性,糖部分应以醚键或酰胺的形式连接,只要酰氨基不在异头碳相邻的碳原子上。聚羟基烷基胺的亲水性比糖小,但比糖更稳定。

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