Production method of low-water-soluble hard materials based on carboxyl-containing polysaccharides modified with aminosalicylic acid
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.
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:
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
FIELD: molecular biology, bio-organic chemistry, possible use for producing cellular microchips.
SUBSTANCE: in accordance to suggested method for forming alginate gel with its simultaneous holding on the surface of solid phase, alginate gel is formed on the surface of solid phase which contains metal oxide with free valences, in presence of polyamine connection. Current method is used in the method for producing a cellular microchip. Cellular microchip is produced by forming and holding micro-cells of gel, containing immobilized cells, on the surface of the solid phase.
EFFECT: possible production of alginate gel, reliably held on the surface of solid phase.
3 cl, 1 tbl, ex
FIELD: organic chemistry, pharmacology.
SUBSTANCE: claimed method includes reaction of alginic acid with amine-containing compound (RNH2) in presence of condensing agent 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide in aqueous medium at room temperature and pH 4.7-4.8. As amine-containing compounds some pharmacologically value amines are used such as n- and o-aminophenols, 5- and 4-amino salicylic acids, anthranilic acid, and n-aminobenzoic acid, n-aminobenzoic acid ethyl ester (anaesthezine), n-aminobenzoic acid β-diethylaminoethyl ester (novocaine), nicotinic acid 1-phenyl-2,3-dimethyl-4-aminopyrazolone-5-(4-aminopyrine) hydrazide (isoniaside), 2-amino'thansulfonic acid (taurin), 7-aminocephalosporinic acid, as well as sulfanylamide preparations such as n-aminobenzenesulfacetamide (streptocide), sodium n-aminobenzenesulfacetamide (sodium sulfacyl).
EFFECT: new alginic acid derivatives useful in medicine and pharmacology.
1 cl, 14 ex, 1 tbl
FIELD: medicine; pharmacology.
SUBSTANCE: invention can be used at treatment of pyoinflammatory diseases and trophic ulcers, and also in gynecology - at a cervical pathology. After secondary crushing pectin is dissolved in water in the ratio accordingly 0.09÷0.1:1.0; then the colloidal solution in thickness of 2.0÷2.5 mm is applied on a fluoroplastic surface, dried and the pectinaceous film obtained for the medical purposes in tight packing is sterilised a method of ultra-violet radiation within not less than 15 minutes.
EFFECT: reduction of terms of healing wounds at the expense of their reliable isolation from an environment, reduction of terms of mediko-social rehabilitation of patients at the expense of creation of favorable conditions for tissue regeneration.
5 dwg, 2 tbl, 2 ex
SUBSTANCE: invention can be used for production human and mammal body absorbable surgical suture materials and absorbable wound textiles. Milled chitin-containing natural raw materials (for example, crab shells) are processed many times at 4-10°C, preferable at 4-5°C using aqueous solutions of hydrochloric acid and alkali, then rinsed with water, aqueous solution of weak acid, water, acetone. Produced dry product is dissolved in dimethylacetamide containing lithium chloride 4.56-10.0 wt % to produce chitin solution 2.4-4.0 wt %. Produced solution is extruded at room temperature to alcoholic setting bath, passed through aqueous stretch and rinsing baths; thus alcoholic setting bath is water-soluble aliphatic alcohols C1-C3, preferably C2 and C3.
EFFECT: sufficient elongation and durability especially for surgical suture material.
1 tbl, 1 dwg, 13 ex
SUBSTANCE: the present innovation deals with binding material out of alginate foamy composition which should be manufactured at applying or without applying a foundation. The suggested foamy binding material is of unique property to include soluble or insoluble medicinal preparations as the part of alginate foamy composition being not characteristic of alginate binding materials manufactured due to formation of fiber. Such binding materials, also, exclude the necessity to apply adhesives and secondary bandages for keeping alginate bandage in wound area.
EFFECT: higher efficiency.
65 cl, 8 ex
SUBSTANCE: single-layer coating is film or gel produced from rubber latex taken in the amount of 25-98% by mass and at least one water-soluble vegetable origin polysaccharide treated with ethyl alcohol, taken in the amount of 2-75% by mass. Coating material is produced by mixing rubber latex and aqueous solution of vegetable polysaccharide treated with ethyl alcohol during 5-50 min. The obtained mass is distributed over flat surface and dried to gel or film state.
EFFECT: improved adhesive properties; easily detachable from wound surface with its epithelialization in progress; applicability for transferring skin fibroblasts to wound surface or culturing thereof.
14 cl, 2 tbl
FIELD: medicine, chemical-pharmaceutical industry, pharmacy.
SUBSTANCE: invention proposes a preparation used in healing wounds and for prevention sticking a bandage to wound. The preparation comprises hyaluronic acid sodium or potassium salt of molecular mass from 200000 to 2500000 Da, iodine, potassium iodide and water. The preparation is made in form of sterile aqueous solution or gel. The preparation possesses high effectiveness in infected and chronic wounds.
EFFECT: enhanced effectiveness of preparation.
4 cl, 16 dwg, 11 ex
FIELD: medicine, in particular gynecology.
SUBSTANCE: claimed filler contains 1 % hydrogel of chitosan with molecular mass of 300-700 kDa and deacetylation ratio of at least 89 %, as well as metronidazole and dioxydine; and 1 l of composition contains (g): dry chitosan chlorohydrate 10; metronidazole 1.250-1.665; dioxydine 2.5; and balance: distilled water. Method for filler production includes stirring of 10 g dry chitosan chlorohydrate in 300 ml of distilled water heated up to 50°C for 20-30 min until full dissolution. Then gradually under intense agitation 250-333 ml of metronidazole for intravenous injection is added, mixture is thoroughly stirred for 5 min, further gradually under intense agitation 250 ml of 1% dioxydine solution is added, mixture is thoroughly stirred for 10 min and packed in container made of dark glass or plastics for storage. Methods for treatment of female genitals diseases by using absorbent articles containing filler of present invention also are disclosed.
EFFECT: non-toxic filler with prolonged antiinflammation and antibacterial effects.
3 cl, 3 tbl
FIELD: medicine, obstetrics, gynecology.
SUBSTANCE: the present innovation deals with hygienic products applied for preventing inflammatory diseases of genital organs and could be used as antibacterial filler for female hygienic panty shield and/or tampon for daily usage. The suggested innovation has the tendency to solve the problem in developing efficient filler for female hygienic panty shield and/or tampon for daily usage to prevent inflammatory diseases of genital organs being of the following advantages: absolute intoxicity, prophylactic action in case of potential development of inflammatory process in female genital tract, antibacterial effect, selective action upon microflora of female genital organs at keeping the number of viable useful lactobacilli, steady action upon mucosa and skin of genital organs due to viscosity and high fluidity of gel composition, form-resistance of gel composition along with its transparency and absence of fragrance, no formation of antibioticoresistant strains of microorganisms at daily applications of panty shields or tampons. The purpose mentioned should be achieved due to the fact that the filler in the composition of panty shield or tampon contains about 0.5-1%-chitosan hydrochloride aqueous solution for medicinal indication ("M" mark) at molecular weight ranged 300-700 kDa, at degree of deacetylation being 89-98% at the following ratio of components/1000 ml composition: dry chitosan hydrochloride 5-10 g, distilled water - the rest. For normalizing vaginal biocenosis 10 applications will be sufficient.
EFFECT: higher efficiency of prophylaxis.
1 ex, 1 tbl
SUBSTANCE: composition has hydrophilic gel produced from chitosan and hydrophilic poly(N-vinyl lactame) having kinematic viscosity index less than 60. When deposited on cracks, the gel absorbs exudate undergoing no structural transformations.
EFFECT: improved skin compatibility properties.
FIELD: hygienic items, in particular sanitary towels.
SUBSTANCE: claimed article has multicomponent absorbing structure, containing the first liquid absorbing component which represents bonded flexible matrix including stratified layers made of fibrous material, and the second liquid absorbing component.
EFFECT: article of increased liquid absorbing capability and improved adjoining.
24 cl, 9 dwg, 5 tbl, 4 ex
FIELD: cellulose fibers treated with oil and compacting agent for modifying properties of fibers; methods of production of cellulose fibers.
SUBSTANCE: cellulose sheet includes: cellulose fibers, oil applied on cellulose fibers; oil is present in the amount of about 0.5 to 20 mass-% of mass of dry fibers and modifying agent applied on cellulose fibers; modifying agent is present in the amount of about 0.5 to 20 mass-% of active agents of dry mass of fibers. Method of production of cellulose sheet includes: preparation of cellulose mass, molding cellulose sheet from this mass, application of oil on cellulose sheet; oil is present on fibers in the amount of about 0.5 to 20 mass-% of mass of dry fibers and application of modifying agent on cellulose fibers; modifying agent is present in the amount of about 0.5 to 20 mass-% of active agents of dry mass of fibers. Method of production of compacted cloth of cellulose fibers includes: making cellulose fibers treated with oil and modifying agent which modifies properties of compacting the cellulose fibers; cellulose fibers treated with oil and modifying agent contain about 0.5 to 20 mass-% of active agents of dry mass of cellulose fibers; method includes also separation of cellulose fibers treated with oil and compacting modifying agent, molding separated cellulose fibers treated with oil and modifying agent into cloth and compression of cloth. Method of modifying properties for compacting of cellulose fibers includes treatment of fibers with oil; before treatment of cellulose fibers with oil and after application and removal of compressive load they are compacted to first specific mass; then cellulose fibers are compacted to second specific mass after application and removal of compressive force; first specific mass exceeds second specific mass; this method includes: application of modifying agent on fibers treated with oil; this modifying agent modifies properties of fibers for compacting; it is applied on cellulose fibers in the amount of about 0.5 to 20 mass-% of active agents of dry mass of cellulose fibers; modifying agent is applied on fibers treated with oil in the amount sufficient for compacting the fibers to third specific mass after application and removal of compressive load; third specific mass is more than first specific mass. Article for absorption of aqueous fluid medium includes: super-absorbing materials and oil applied on cellulose fibers in the amount of about 0.5 to 20 mass-% of mass of dry fibers and modifying agent applied on cellulose fibers in the amount sufficient for presence of active agents in the amount of about 0.5 to 20 mass-% of dry mass of cellulose fibers.
EFFECT: possibility of retaining super-absorbing materials in structures.
38 cl, 3 dwg, 1 tbl
SUBSTANCE: agent for prevention and alcoholism treatment contains admixture of amidocyanogen and polylactide in the ratio (wt) from 10:90 till 40:60. The method of prevention and alcoholism treatment consists that to the patient, as a rule, enter intramusculary a solution containing an admixture amidocyanogen and polylactide in a single dose of 0.5-1.5 g once a month.
EFFECT: appreciable effect of delay and slow liberation of the operating beginning.
4 cl, 3 dwg, 2 tbl, 3 ex
SUBSTANCE: agent contains Rifabutin sorbated in polymeric nanoparticles matrix, potassium cholesterylphosphate, or sodium glycocholate, or hexadecyl dihydrogen phosphate, or a-tocopheryl succinate, water-soluble polymeric stabiliser and bulking agents. Polymeric nanoparticles sized 100-800 nm include lactic acid polymer/polymers and/or lactic and glycolic acid copolymer/copolymers at glycolic acid content in specified copolymers up to 50 mole %. Molecular weight of specified polymers and copolymers is 5 to 300 kDa. Molecular weight of water-soluble polymeric stabiliser is no more than 70 kDa and is selected from the group including polyvinyl alcohol, polyvinylpyrrolidone, polysorbate and seralbumin.
EFFECT: new agent provides durable action of Rifabutin; higher bioavailability of Rifabutin and efficiency of bacterial infection treatment.
3 dwg, 1 tbl, 7 ex
SUBSTANCE: invention concerns coordination complex of platinum (II) diaminocyclohexane with block copolymer containing structure of the general formula PEG-block-poly(carbo), where PEG is a poly(ethyleneglycol) segment, and carbo is a repeating chain containing carboxylic group in the side chain, and platinum (II) diaminocyclohexane is immobilised by block copolymer due to linkage between carboxylic carbo residue anion and platinum; as well as method of obtaining the complex and anticancer composition including effective anticancer quantity of coordination complex and pharmaceutically acceptable carrier. In addition, invention concerns coordination complex of platinum (II) diaminocyclohexane and block copolymer with structure of the general formula (1-a) or (2-a) , where R1 is a hydrogen atom or unsubstituted or substituted serial or furcated C1-C12 alkyl group, L1 and L2 are linkage group, R3 is a hydrogen atom, protective group of aminogroup, hydrophobic group or polymerisation-capable group, R4 is hydroxylic group or initiator residue, each of R5 radicals is independently a hydrogen atom, alkali metal ion or protective group of carboxylic group, m is an integer from 5 to 20000, n is an integer from 2 to 5000 if alkali metal ion comprises 50% or more of the number of R5 groups which is n, with platinum (II) diaminocyclohexane immobilised by the said block copolymer due to linkage between carboxylic carbo residue anion and platinum, and equivalent ratio of diaminocyclohexane platinum (Pt) to carboxylic groups of the said block copolymer (Pt/COO-) is 0.3-1. The invention also concerns the method of obtaining this coordination complex and method of tumour treatment involving introduction of effective quantity of combined coordination complex of platinum (II) diaminocyclohexane and coordination complex of cis-platinum to a patient.
EFFECT: increased composition efficiency.
20 cl, 2 ex, 1 tbl
SUBSTANCE: invention concerns aldehyde derivatives and conjugates of di-, oligo- or polysaccharide, of the general formula (I), methods of obtaining them, and pharmaceutical composition based on them and capable of staying in blood flow for prolonged time. , where R is -CH(CHO)CH2OH, -CH2CHO, -CH(CH2NHR1)CH2OH, -CH(CH2NHNHR1)CH2OH, -CH(CH=NNHR1)CH2OH, -CH2CH2NHR1, -CH2CH=N-NHR1, -CH2CH2NHNHR1; R1 is polypeptide or albumen; GlyO is a sialic acid bond; R3 is H; R4 is OH; n is 2 or more.
EFFECT: obtaining pharmaceutical composition based on aldehyde derivatives of sialic acid capable of staying in blood flow for prolonged time.
20 cl, 7 tbl, 22 dwg, 10 ex
SUBSTANCE: present invention refers to medicine and concerns microparticles containing sphere mainly consisting of cross-linked agarose carbohydrate and allergen covalently bonded with sphere, applied for immune system disturbance treatment. Used allergen is produced of plant pollen, specifically of timothy grass pollen. Application of specified microparticles provides effective treatment for patients suffering from allergy, as well as reduces by-effects of parenteral introduction.
EFFECT: development of effective method of allergy treatment and prevention.
9 cl, 4 dwg, 1 tbl, 5 ex
FIELD: medicine; pharmacology.
SUBSTANCE: medicinal agent is mixed with preaerated and irradiated with accelerated electron current or pulse UV-laser radiation 5.0-50.0% polyethylene oxide solution of molecular weight 0.4-20 kilodaltons in presence of 0.01-0.1 M phosphate buffer, pH 6.0-8.0 and containing 0.05-0.3 M sodium chloride. Offered method is easy and multipurpose, and can be applied to increase enteral bioavailability of medicinal agents introduced mainly or solely parenterally due to low resorption by intestine walls.
EFFECT: increased enteral bioavailability of medicinal agents.
4 cl, 3 tbl, 10 ex, 1 dwg