Synthetic resins or natural rubbers -- part of the class 520 ser – Synthetic resins – From phenol – phenol ether – or inorganic phenolate
Patent
1993-12-13
1995-10-31
Seidleck, James J.
Synthetic resins or natural rubbers -- part of the class 520 ser
Synthetic resins
From phenol, phenol ether, or inorganic phenolate
528199, C08G 6400
Patent
active
054630126
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 PCT/EP92/01262 filed Jun. 5, 1992.
The present invention relates to polycarbonates of formula (I) ##STR2## wherein a is an integer from 2 to 300; or alicyclic straight or branched chain having from 2 to 18 carbon atoms, ##STR3## in which R.sup.3 is hydrogen or methyl, n is an integer from 1 to 3 and m is an integer from 1 to 200, ##STR4## wherein x and y are integers from 1 to 50, R.sup.4 and R.sup.5, which can be the same or different, are aliphatic straight or branched hydrocarbon chains having from 1 to 4 carbon atoms, R.sup.6 is an aliphatic or alicyclic straight or branched chain having from 2 to 18 carbon atoms, or a polyoxyalkylene residue of formula (II), being intended that the two groups --R.sup.4 --COO and --R.sup.5 --COO are randomly distributed in the polyester residue, x and y being in any possible ratio from 0 to 100.
When R.sup.1 and/or R.sup.2 are alkylene chains, these preferably have from 2 to 12 carbon atoms.
When R.sup.1 and/or R.sup.2 are polyoxyalkylene residues, these are preferably polyoxyethylene residues of formula (II) wherein R.sup.3 is H, n is 1 and m is an integer from 2 to 100.
Polycarbonates in which R.sup.1 and R.sup.2 are hexylene, decylene, dodecylene, 1,4-cyclohexylene, 2,2-dimethyl-1,3-propylene, 2,5-dimethyl-2,5-hexylene or polyoxyethylene residues are preferred.
Particularly preferred are those polycarbonates in which R.sup.1 and R.sup.2 are selected from 1,4-cyclohexylene, 2,2-dimethyl-1,3-propylene, 2,5-dimethyl-2,5-hexylene or polyoxyethylene residues.
More particularly preferred are those polycarbonates in which R.sup.1 and R.sup.2 are polyester residues.
Most particularly preferred are those polycarbonates in which R.sup.1 and R.sup.2 are polyester residues, wherein R.sup.4 and R.sup.5 are methylene or methyl-methylene.
Groups R.sup.1 and R.sup.2 are preferably different from each other so as to give alternate co-polycarbonates, i.e. having regularly alternated monomeric units.
The invention further relates to a process for the preparation of compounds I and the use thereof for the preparation of pharmaceutical formulations slowly releasing the active principles.
Examples of pharmaceutical formulations in which the drug (active principle) is incorporated in a polymer matrix are well known in literature: See "Biodegradable Polymers as Drug Delivery Systems", ed. by M. Chasin and R. Langer, Marcel Dekker Inc., New York 1990; "Methods in Enzymology, Vol. 112, Drug and Enzyme Targeting, Part A", ed. by K. J. Widder and R. Green, Academic Press, Inc., Orlando, Fla. 1985; "Formes Pharmaceutiques Nouvelles", P. Buri, F. Puisieux, E. Doelker and J. P. Benoit, Technique et Documentation (Lavoisier), Paris 1985; "Biodegradable Polymers for controlled release of peptides and proteins", F. G. Hutchison and B. J. To. Furr, in Drug Carrier Systems, F. H. D. Roerdink and A. M. Kroom eds., John Wiley and Sons, Chichester, 1989; and "Controlled Release of Biologically Active Agents" by Richard Baker, John Wiley and Sons, New York 1987.
Aliphatic polycarbonates are known for example from DE 2546534, JP-62241920, JP-1009225, and they were proposed as plastifiers, intermediates for the preparation of polyurethanes or for special applications, such as the preparation of substrates for optical disks. The polycarbonates of the invention, having intrinsic viscosities in chloroform at 30.degree. C. ranging from 0.05 dl/g to 2 dl/g, preferably from 0.077 to 0.32 dl/g, have biodegradability characteristics which make them useful for the preparation of bioerosible matrices.
Therefore, the invention also relates to pharmaceutical compositions providing a slow release of the active principles from bioerosible matrices comprising polycarbonates of formula (I).
Polymers of formula I are prepared by reacting diols of formula (IV) or (V) 1,1'-carbonyldiimidazole, to give diimidazolyl formates of formula (VI) or (VII) ##STR5## which are in their turn reacted with diols of formula (IV) or (V).
When R.sup.1 and/or R.sup.2 are polyester residues, then the compounds (IV) and
REFERENCES:
patent: 4105641 (1978-08-01), Buysch et al.
patent: 5260367 (1993-11-01), Toda et al.
Bignotti Fabio
Ferruti Paolo
Ranucci Elisabetta
Mediolanum Farmaceutici S.p.A.
Mosley Terressa M.
Seidleck James J.
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