Preparation and Characterization of Novel Poly(alkylamine)-Based Hydrogels Designed for Use as Bile Acid Sequestrants

Preparation and Characterization of Novel Poly(alkylamine)-Based Hydrogels Designed for Use as Bile Acid Sequestrants

Preparation of novel poly(alkylamine)-derived hydrogels is described. Polymers are prepared via reaction of various diamines with dihalo compounds or diepoxides. N-substituted polymers are readily prepared by reaction of primary amines with dihalo compounds. The resulting covalently cross-linked pol...

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Bibliographic Details
Published in:Macromolecules Vol. 30; no. 20; pp. 6174 - 6184
Main Authors: Figuly, Garret D, Royce, Susan D, Khasat, Nitya P, Schock, Laurel E, Wu, Shilain D, Davidson, Fredric, Campbell, G. Creston, Keating, Mimi Y, Chen, Harry W, Shimshick, Edward J, Fischer, Robert T, Grimminger, Lisa C, Thomas, Beth E, Smith, Linda H, Gillies, Peter J
Format: Journal Article
Language:English
Published: Washington, DC American Chemical Society 06-10-1997
Subjects:
Applied sciences
Biological and medical sciences
Exact sciences and technology
General and cellular metabolism. Vitamins
Medical sciences
Organic polymers
Pharmacology. Drug treatments
Physicochemistry of polymers
Polymers with particular properties
Preparation, kinetics, thermodynamics, mechanism and catalysts
Diepoxide
Molecular structure
Swelling
Crosslink density
Experimental study
Polyaddition
Alcohol polymer
Colloidal gel
Diamine
Bile acid
Chlorocarbon
Preparation
Sequestering power
Property structure relationship
Quaternary ammonium polymer
Antilipemic agent
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Summary:Preparation of novel poly(alkylamine)-derived hydrogels is described. Polymers are prepared via reaction of various diamines with dihalo compounds or diepoxides. N-substituted polymers are readily prepared by reaction of primary amines with dihalo compounds. The resulting covalently cross-linked polymers exhibit hydrogel behavior (high swell with water) when ionized to polyammonium species at low pH. At high pH, the polymers reside in the free base polyamine form and lose all hydrogel character (they no longer swell in water). Characterization of polymer structure with carbon-13 NMR, thermal analysis, and swell behavior reveals a structure which is highly branched and only loosely cross-linked. In the ionic polyammonium form thermal stability up to ∼300 °C is observed. The polymers exhibit activity as bile acid sequestrants significantly superior to cholestyramine, as evidenced by their ability to efficiently bind quantities of cholate when tested in vitro. This behavior indicates that these hydrogels should be very useful for the treatment of hypercholesterolemia.
Bibliography:istex:8BBA42D2D24CCA7CC5AAB2B86A497B391E9897D8
Abstract published in Advance ACS Abstracts, September 15, 1997.
ark:/67375/TPS-FBC8717T-T
ISSN:0024-9297
1520-5835
DOI:10.1021/ma9702509