Production method of low-water-soluble hard materials based on carboxyl-containing polysaccharides modified with aminosalicylic acid

FIELD: chemistry.

SUBSTANCE: used are films made of glycosaminoglycan conjugates with 4- or 5-aminosalicylic acids or alginate conjugates with 4- or 5-aminosalicylic acids or intermixed conjugates or mixed conjugates and at least one polymer chosen from group including carboxymethyl cellulose, glycosaminoglycan, alginate, gelatine, albumin with salicylate content not less than 50%. Specified mixtures are treated with 2-20% iron (III) chloride solution at room temperature within 1-5 minutes. Surface complex lowers water- and biological liquids solubility of the film.

EFFECT: prolonged of biomaterial activity is provided.

10 ex

 

The invention relates to the field of chemistry, in particular to a method for having low solubility in water films, which can be used in medicine.

To carboxyl-containing polysaccharides include Poliplast both vegetable and animal origin. Acidic glycosaminoglycans (GAGS) from connective tissues of animals and humans (hyaluronic acid, chondroitin sulfates and heparin) are heteropolysaccharides linear structure with different molecular weight and degree of sulfation. On the basis of GAG created a number of Pharmacopoeia drugs, including in the form of a film material. For example, the film "Seprafilm", used as a barrier material to prevent adhesive disease of the peritoneum, are water-soluble mixture of two polysaccharides: carboxymethylcellulose (CMC) and the active substance - hyaluronic acid with reparative-regenerative properties.

Alginic acid (AA) is a linear polysaccharide structure is contained in brown algae and consists of residues β-D-mannurone and α-L-guluronate kislotno the basis of alginic acid or its sodium-calcium salts of the known preparations: "Alginat (in combination with sulfa drug "Mafenide") and "Algipore (in combination with antiseptic furatsilinom) - RA is saillagouse funds with resorptive and regenerating action [PPM Mashkovsky Medicinal product. - M.: New wave. 2005]. From alginate fibers are produced sterile bandages for the treatment of wound surfaces and abundant Department of exudate: "Suprasorb", "Melgisorb and Kaltostat".

Known methods of producing soluble or water-insoluble materials based on carboxyl-containing polysaccharides.

1. The method is based on the formation of complex salts or polyelectrolyte complexes of negatively charged molecules carboxyl-containing polysaccharides and compounds of cationic nature. Usually such complexes obtained by mixing aqueous solutions of electrolytes, the result is the formation of little or insoluble products. Known in such a way that the resulting complexes of hyaluronic acid with proteins (gelatin, casein, collagen, myosin, fibrin) and polysaccharides (chitosan, triethanolammonium). They have a reparative and healing properties and are used for the manufacture of artificial skin, artificial blood vessels and other medical supplies [U.S. Pat. EP 0544259 A1 (1992); Denuziere D., Ferrier A., Damour O., A. Domard // Biomaterials. 1998. V.19. P.1275-1285; Denuziere A., D. Ferrier, A. Domard // Carbohydr. Polym. 1996. V.29. P.317-323; Denuziere A., D. Ferrier, Damour O. // Ann. Pharm. Fr. 2000. V. 58 (1). P.47-53]. Complexes of chondroitin sulfates with chitosan containing 10% of free amino groups proposed in which the quality of drug delivery vehicles, for example prednisolone [Kofuji K., Ito T., Marata Y., Kawashima S. // Biol. Pharm. Bull. 2002. V.25 (2). P.268-271]. Heparin is strongly associated with cellulose, cationizing trimethyl(3-chloro-2-hydroxypropyl)ammoniacloridegas [H. Baumann, R. Keller // J.Membr. Sci. 1991. V.61. P. 253-268], or polimetilvinilovy alcohol, the surface of which is immobilized L-lingerered [Xinghang M., Fazal M.S., Wan for K.S. II]. Colloid Interface Sci. 1991. V.147(1). P.251-261]. These biomaterials innovatory heparin possess anticoagulant activity and can be used as membranes with atrombogenity properties.

Of alginates by interaction with salts of divalent metals [Dhoot N.O., M.A. Wheatley IIJ. Pharm. Sci. 2003. V.92. P.679] or various polyelectrolytes - chitosan [Takeshi G., Matsushima K., Kikuchi Ken-Ichi. // Chemosphere. 2004. V.55 P.135-140], polyethylenimine [H.-J. Park and Y.-H. Khang // Enzyme and Microbial Technol. 1995. V.17. P.408] the obtained water-insoluble gels, which can be used for adsorption of metals as a medium for cultivation of microorganisms, and for encapsulation of drugs.

2. The method is based on the covalent binding of polysaccharides with compounds with, for example, hydrophobic properties, or compounds of a polymeric nature. For example, conjugation of hyaluronic acid with esters or inorganic salts of natural amino acids (L-leucine, Z-isoleucine, Z-valine, Z-Proline, Z-arginine, L-histidine, L-lysine, phenylalanine, and Z-leucine) in the presence of 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide (CBI) receive the products, insoluble in water [U.S. Pat. US 6610669 (2003)]. Using the same CBI receive conjugates of chondroitin sulfates with collagen [L. Zhang, D. MA, F. Wang, Q.Zang // Artif. Cells Blood Substit. Immobil. Biotechnol. 2002. V.30. P.319] and gelatin [Ch.-H. Chang, H.-C.Liu, C.-C.Lin, C.-H.Chou, F.-H.Lin // Biomaterials. 2003. V.24. P.4853], which can be used as an artificial cartilage tissue. Cross-linked products obtained by the interaction of GAG (hyaluronic acid or chondroitin sulfates) α,ω-dioxopyrimidine, in the form of a film material can be used for wound healing and tissue regeneration [K.R. Kirker, Luo Y., Nielson J.H., Shelby J., Prestwich G.D. // Biomaterials. 2002. V.23 supported (17). P.3661-3671]. The gels obtained from alginate, cross-linked with such polymers such as chitosan [Tau L.-K., Khoh L.-K., Loh, C.-S., Khor E. // Biotechnol. Bioeng. 1993. V.42. P.449], polyacrylic acid [Mano T., Mitsuda, S., Kumazawa, E. and Takeshida Y. // J.Ferment. Bioeng. 1992. V.73. P.486], polyvinyl alcohol [Wu K.-Y. and Wisecarver K.D. // Biotechnol. Bioeng. 1992. V.39. P.447], polyvinyliden [F.F. Wang, C.R. Wu and Wang Y.J. // Biotechnol. Bioeng. 1992. V.40. P.1115], show increased resistance to the destructive action of monovalent cations.

3. Intermolecular and intramolecular cross-linking also reduces the solubility of biomaterials based on polysaccharides. As cross-linking reagents used various bi - and polyfunctional compounds [K.P. Vercruysse, G.D. Prestwich // Therapeutic Drug Carrier Systems. 1998. V.15. No. 5. P.513-555]: POCl3[Pat. WO 9009401 (1990)], e is chlorhydrin [U.S. Pat. EP 0161887 (1985)], water-soluble carbodiimide (for example, the OED) [K. Tomihata, Ikada Y. // J.Biomed. Mater. Res. 1997. V.37 (2). P.243-251], diphenylsulfone, polyaniline, ethylene oxide and other epoxysilane. Modification of polysaccharides leads to lower their Biodegradability under the action of substratespecific lids [K.P. Vercruysse, Marecak D.M., Marecak J.F., G.D. Prestwich // Bioconj. Chem. 1997. V.8 (5). P.686-694], thus can be achieved with the prolongation of drug action on the basis of poliprinolov or drugs encapsulated in a soluble polysaccharide shell.

The task of the invention is to obtain having low solubility in water films on the basis of modified aminosalicylic acids acidic polysaccharides by treating their surfaces with a solution of ferric chloride (FeCl3).

Films made from conjugates of glycosaminoglycans or alginic acid with 4 - or 5-aminosalicylic acid or mixtures of the above conjugates in any proportion to each other, or from mixtures of conjugates and polymer compounds containing covalently linked 4 -, or 5-aminosalicylic acid, and can form a film (carboxymethylcellulose (CMC), glycosaminoglycans, sodium alginate, gelatin, albumin, and others). In the latter case, the fraction of polymer that does not contain residues of 4 - or 5-aminosalicylic the howling acids, should not be more than 50%. When processing the film surface 2-20% solution of FeCl3very quickly formed a complex with the remainder of salicylic acid, the film acquires a purple color and, depending on the exposure time (1-5 min) with FeCl3the film is partially or completely loses solubility in water (or body fluids). Such processing can be performed from one side of the film just before its application, while the other side of the film retains its adhesiveness to the surface of living tissue. It should be noted that FeCl3has a hemostatic effect and is part of the hemostatic "Cuprofen", which can also be used for surface treatment of films.

Salicylates glycosaminoglycans and alginic acid are produced in a known manner by the reaction of polysaccharides with a 4 - or 5-aminosalicylic acid in the presence of a condensing reagent CBI [Peredelkino YOU, Odinokov V.N., Vakhrusheva Y.S., Golikova M.L., Khalilov L.M., Dzhemilev sea level // Bioorg. chemistry. 2005 T. No. 1. S-95; Peredelkino YOU, Odinokov V.N., Lukin Y.S., Temkina T.V., Khalilov L.M., Dzhemilev sea level II Bioorg. chemistry. 2006. 32. No. 5. S-529; U.S. Pat. Of the Russian Federation No. 2283848].

Examples of hyaluronic acid and alginate shows the scheme of the synthesis of conjugates with aminosalicylic acid:

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To obtain sparingly soluble or insoluble in water film material cast from aqueous solutions and air-dried films based on modified aminosalicylic acid carboxyl-containing polysaccharides are treated as follows.

Example 1. On one or both sides of a film made of a conjugate of hyaluronic acid, 4-aminosalicylic acid (as sodium salt), brush put 2%solution of ferric chloride (FeCl3or immerse the film in a solution of FeCl3), incubated at 20°2-5 min until a purple color, then the excess solution is removed by soaking filter paper. Get film material, sparingly soluble in water.

Example 2. On one or both sides of a film made of a conjugate of hyaluronic acid, 4-aminosalicylic acid (as sodium salt), brush put 20%solution of ferric chloride (FeCl3or immerse the film in a solution of FeCl3), incubated at 20°With 1-2 minutes until violet color, then the excess solution is removed by soaking filter paper. Get film material, insoluble in water.

Example 3. The film, made of a conjugate of hyaluronic acid with 5-aminosalicylic acid (in the form of nutrie the Oh salt), treated with a solution of ferric chloride (FeCl3) analogously to example 1 or example 2.

Example 4. The film, made of a conjugate of alginate with 4-aminosalicylic acid (as sodium salt), is treated with a solution of ferric chloride (FeCl3) analogously to example 1 or example 2.

Example 5. The film, made of a conjugate of alginate with 5-aminosalicylic acid (as sodium salt), is treated with a solution of ferric chloride (FeCl3) analogously to example 1 or example 2.

Example 6. The film, made of a conjugate of chondroitin sulfates (natural mixtures of chondroitin-6-sulfate/dermatologit from the umbilical cord of newborns or chondroitin-4-sulfate/chondroitin-6-sulfate of cartilage) with 4-aminosalicylic acid (as sodium salt), is treated with a solution of ferric chloride (FeCl3) analogously to example 1 or example 2.

Example 7. The film, made of a conjugate of chondroitin sulfates (natural mixtures of chondroitin-6-sulfate/dermatologit from the umbilical cord of newborns or chondroitin-4-sulfate/chondroitin-6-sulfate of cartilage) with 5-aminosalicylic acid (as sodium salt), is treated with a solution of ferric chloride (FeCl3) analogously to example 1 or example 2.

Primer. The film, made of a conjugate of heparin with 4-aminosalicylic acid (as sodium salt), is treated with a solution of ferric chloride (FeCl3) analogously to example 1 or example 2.

Example 9, 10. Film containing 50 wt.% carboxymethyl cellulose and 50 wt.% conjugate of hyaluronic acid with 4 - or 5-aminosalicylic acid, cast from water and treated with a solution of ferric chloride (FeCl3) analogously to example 1 or example 2.

Other mixed composition based on polymer salicylates with the introduction of the mixture is not more than 50 wt.% one polymer selected from the group consisting of glycosaminoglycan, alginate, gelatin and albumin, prepared similarly and treated with a solution of ferric chloride (FeCl3as described in example 1 or example 2.

The method of obtaining having low water solubility of the film material on the basis of modified glycosaminoglycans, and alginate, namely, that film made of conjugates of glycosaminoglycans with a 4 - or 5-aminosalicylic acid or conjugates of alginate with a 4 - or 5-aminosalicylate acids or mixtures of conjugates of each other in any ratio, or mixtures of conjugates of at least one polymer selected from the group comprising carboxymethyl cellulose, glycosome is aglican, alginate, gelatin, albumin, containing a mixture of polymer musk at least 50%, process 2-20%solution of ferric chloride (III) at room temperature for 1-5 minutes



 

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