Chemistry of carbon compounds – Miscellaneous organic carbon compounds
Patent
1978-10-31
1980-12-16
Woodberry, Edward M.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
260 9, 424 9, 424 80, 424183, C08L 510
Patent
active
042396646
ABSTRACT:
The present invention relates to a group of novel compounds defined as covalently bound poly-N-vinyl pyrrolidinone (PVP)-heparins. These compounds are synthesized on the basis of a novel concept that heparin molecules can be modified to have new desirable qualities by binding heparin covalently to an appropriate polymer carrier which has the desired characteristics.
Heparin is hydrophilic and thereby insoluble in organic solvent. It has a short half-life in vivo. PVP-heparins, on the other hand, not only retain the anticoagulant activities of heparin, but also have the solubility (in organic solvents) and longer half-life in vivo of PVP.
PVP-heparins are produced either in anhydrous or heterogeneous media wherein PVP is activated by thionyl chloride to produce an imidoyl ion which is subsequently bound to heparin. PVP-heparin produced in anhydrous media is chloroform soluble and has been found useful for coating plastics and similar substances. PVP-heparin produced in heterogeneous media has been found to have twice the half-life in sheep as the native, unmodified heparin.
REFERENCES:
patent: 3453194 (1969-07-01), Bennett et al.
patent: 3457098 (1969-07-01), Leininger et al.
patent: 3673612 (1972-07-01), Merrill et al.
patent: 3846353 (1974-11-01), Grotta
patent: 4087567 (1978-05-01), Sullivan
PVP, Lesser, Drugs and Cosmetic Industry, Jul. 1954: 75,1-pp. 32-37.
Schmer Gottfried
Teng Lin-Nar
Research Corporation
Roberts, Jr. John S.
Woodberry Edward M.
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