Process for the preparation of iodinated biopolymers having disi

Details Process for the preparation of iodinated biopolymers having disi Process for the preparation of iodinated biopolymers having disi

1995-01-03

1996-07-23

Kunz, Gary L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536 20, 536124, C08B 3708, A61K 3170

Patent

active

055389554

DESCRIPTION:

BRIEF SUMMARY
DESCRIPTION

The present invention has as its subject a process for the preparation of complexes of iodine with chitosan or deacetylated, acylated with mono- or polycarboxylic acids, aldyminated, N or O-carboxymethylated or sulphatated derivatives thereof and their salts, the iodinated complexes thus obtainable and the therapeutical compounds containing them as an active principle.
According to a particularly preferred embodiment, the present invention has as its subject complexes of iodine with chitosan and derivatives thereof, containing iodine in a proportion expressed by the general formula X(I.sub.2).sub.n, in which X is the monomeric unit of a polymer chosen from the group comprising chitin, chitosan, N-carboxybutylchitosan, N-acylchitosans, N-carboxymethylchitosan, N-O-carboxymethylchitosan, N-O-chitosan sulphate and n is a number variable from 0.01 to 1.5.
According to a still more particularly preferred embodiment, X is chosen from the group comprising the monomeric units given in the following Table 1.


TABLE 1 ______________________________________ Meanings of X in the general formula X(I.sub.2)n Polysaccharide Type of monomeric unit.degree. ______________________________________ Chitin A B * Chitosan A B * N-carboxybutyl chitosan A B C N-acylchitosans A B D N-carboxymethyl chitosan A B E N--O-carboxymethyl chitosan A B E F N-carboxymethyl chitosan A B G N--O-chitosan sulphate A B H I ______________________________________ (.degree.) Monomeric units: 2amino-2-deoxy-D-glycan (A); 2acetamido-2-deoxy-D-glycan (B); 2N-carboxybutylamino-2-deoxy-D-glycan (C); 2N-acylamino-2-deoxy-D-glycan in which acyl is for example propionyl butyrryl, caproyl, oxalyl, succinyl, phtalyl etc. (D); 2N-carboxymethylamino-2-deoxy-D-glycan (E); 2N-carboxymethylamino-2-deoxy-D-6-O-carboxymethylglycan (F); 2N-dihydroxypropylamino-2-deoxy-D-glycan (G); 2amino-2-deoxy-D-glycan Nsulphate (H); 2amino-2-deoxy-D-glycan Osulphate (I); (*) In chitin the monomeric unit B prevails, whereas in chitosan the gradual increase of monomeric unit A imparts a growing watersolubility to the polymer in an acid environment. ( ) In the polymers given above, whose molecular weight may vary from several thousand to millions of Dalton, the monomeric units are bound together by glycosidic .beta. 1-4 bonds. The ionizable groups, according to their pH, are salified by counterions of organic and inorganic nature.
Iodine in its elementary state exhibits notable germicidal activity, for this reason it is used in alcoholic solutions as a disinfectant for topical use.
The limits to said use are the low stability over a period of time of the iodine solutions, the notable aggressiveness of this halogen on the tissues when applied as a solution, and the persistent stains it leaves on the skin.
More recently, water-soluble forms of iodine with polyvinylpyrrolidone have been commercialized, which only partially mitigate these undesirable negative effects.
There is therefore great interest in the development of "slow release" iodine-based forms which allow application of large quantities of active principle, which are then released gradually but continually, so as to guarantee effective defence from infection by microorganisms over a long period, without damaging the tissues and reducing the number of medications required.
Of particularly great advantage is the possibility of coupling the iodine with compounds capable of stimulating tissue regeneration, so as to aid the healing process as a whole.
From this point of view chitin, chitosan and in general the other derivatives of this polysaccharide, only partially indicated in Table 1, are of particular interest according to the present invention, due to their notable cicatrizing and hemostatic powers.
Chitin, a biopolymer present in a large number of living organisms, such as arthropods, annelids, mollusks, coelenterates and fungi, is a polysaccharide with a molecular weight varying from a few thousand to several million Dalton, formed by molecul

REFERENCES:
patent: 4275194 (1981-06-01), Kato et al.
patent: 4424346 (1984-01-01), Hall et al.
patent: 5051256 (1991-09-01), Barnes
patent: 5336415 (1994-08-01), Deans
Journal Of The Applied Polymer Science. vol. 25, 1980, pp. 731-738. Y. Shno et al. "On the Adsorption of Iodine onto Chitosan".
Database WPI. Week 9232, Derwent Publications Ltd., London, GB; AN 263004 & JP, A, 4 178 329 (Unitika) 25 Jun. 1992. Patent Abstracts Of Japan. vol. 16, No. 485 (C-0993).
Takahashi J. Inclusion Phenomena 1987, 5, 525-534.
Shigeno et al. Angew. Makromolecul. Chem. 1980, 91, 55-67.

Affiliated with

Also associated with

Rating

Process for the preparation of iodinated biopolymers having disi does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Process for the preparation of iodinated biopolymers having disi, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process for the preparation of iodinated biopolymers having disi will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-713104