New microspheres based polymethylacrylate, a method of receiving and containing pharmaceutical compositions
The subject invention are microspheres used in the pharmaceutical field as vectors of particles intended for the transport of biologically active substances, in particular hydrophilic substances (peptides and proteins), for oral administration. Microspheres formed by a continuous grid of polymeric material carrier based polymethylacrylate. In the base material can be dispersed biologically active substance. Continuous mesh polymer is dense or may include distributed therein globules with an aqueous phase. Microspheres according to the invention, obtained by means of double emulsification. Microspheres are characterized by progressive and modular decomposition kinetics, allow efficiently encapsulate hydrophilic substances of biological origin and ensure the delivery of specified substances to the desired area of the body. 3 S. and 11 C.p. f-crystals. Description text in facsimile form (see graphic part).
Claims1. Microspheres formed by a continuous grid of polymeric material carrier, which can be dispersed prophetic is broken off recurring units, meet the following General formula (I):in which R1means an alkyl group with 1-6 carbon atoms or the group (CH2)m-R3in which m denotes an integer from 1 to 5 and R3means an alkyl group with 1-6 carbon atoms;R2means an alkyl group with 1-6 carbon atoms;n means an integer from 1 to 5,thus a continuous mesh of polymer is dense or may include globules with an aqueous phase dispersed in a continuous polymer mesh.2. Microspheres under item 1, characterized in that the above-mentioned homopolymer formed of repeating units corresponding to General formula (I) in which R1means an alkyl group with 1-6 carbon atoms, R2means an alkyl group with 1-6 carbon atoms and n denotes a number equal to 1.3. Microspheres under item 1, characterized in that the above-mentioned homopolymer formed of repeating units corresponding to General formula (I) in which R1and R2mean group SN2-CH3.4. Microspheres according to any one of paragraphs.1-3, characterized in that the above-mentioned carrier material contains 90-99,5 wt.% homopolymer specified in paras.1, 2 or 3, and 0.5-10 wt.% copolymer, Klum character, moreover, the above fragment with hydrophobic character includes at least one repeating unit, and meet the General formula (I).5. Microspheres under item 4, wherein the fragment with hydrophilic character of the above copolymer is selected from polyethylene oxide, polyvinyl alcohol, polyvinylpyrrolidone, poly(N-2-hydroxypropylmethacrylamide), polyhydroxyethylmethacrylate, hydrophilic polyaminoamide, such as polylysine, polysaccharide.6. Microspheres under item 4 or 5, characterized in that the above copolymer has a block structure, preferably double or triple, or grafted structure.7. Microspheres according to any one of paragraphs.1-6, characterized in that the substance is dispersed in an effective amount in the above-mentioned base material, and the above-mentioned substance, if necessary, is biologically active.8. Microspheres according to any one of paragraphs.1-7, characterized in that the above-mentioned dispersed substance is a peptide.9. Microspheres according to any one of paragraphs.1-8, characterized in that the above-mentioned dispersed substance is a protein.10. A method of producing microspheres according to any one of paragraphs.1-9, containing the grid, including globules with an aqueous phase,the material carrier, in a volatile organic solvent containing, if necessary, a surfactant, b) preparing a second aqueous solution is not miscible with the solution obtained in paragraph (a) containing, if necessary, the above dispersible substance and, if necessary, a surfactant, b) preparation of the primary emulsion by dispersing the second solution into the first solution and the continuous phase is formed by a solution of one or more polymers, g) preparation of secondary emulsion or by dispersion while mixing the primary emulsion obtained in paragraph (b) in the dispersion medium, not miscible with the primary emulsion and the above-mentioned dispersion medium contains, if necessary, a stabilizer, or by pouring when mixing the primary emulsion of a solution formed by the environment, is not miscible with the primary emulsion and the above environment contains, if necessary, a stabilizer, e) evaporating the organic solvent under stirring.11. The method according to p. 10, characterized in that it further includes (e) allocation of microspheres by centrifugation, W) one or more posidonas PP.10-11, characterized in that the surfactant used to prepare the primary emulsion, choose among poloxamers, polysorbates, polyvinyl alcohols and copolymers, such as those described in any of paragraphs.4-6.13. The method according to any of paragraphs.10-12, characterized in that the above-mentioned stabilizer, used to prepare the secondary emulsion is a polyvinyl alcohol.14. The pharmaceutical composition intended for oral administration, characterized in that it contains microspheres described in any of paragraphs.1-9 or obtained by the method according to any one of paragraphs.10-13.
The polymerization method of immobilization of biological macromolecules and composition for its implementation // 2216547
The invention relates to a composition of composition TO=ANDand+b+with+Dd+Ee+Ffwhere the composition; And - acrylamide, methacrylamide, N-[Tris(hydroxymethyl)methyl]acrylamide, 2-hydroxyethylmethacrylate, methyl methacrylate or other monomer based on the derivatives of acrylic, methacrylic, cinnamic, crotonic, vinylbenzoic or other unsaturated acids; N,N'-methylenebisacrylamide, N,N'-(1,2-dihydroxyethylene)bisacrylamide, polietilenglikolmonostearat, their mixture, or other symmetrical or asymmetrical cross-linking agent based on the derivatives of acrylic, methacrylic, cinnamic, crotonic, vinylbenzoic or other unsaturated acids; S - oligonucleotide, nucleic acid, protein or other molecule that carries the active group, including amino - or sulfhydryl group; D - components of the environment for the polymerization immobilization, namely glycerol, sucrose, polyalcohol; E - water, N,N-dimethylformamide, dimethyl sulfoxide and other polar and non-polar solvents; F - ammonium persulfate, potassium persulfate, methylene blue, fluorescein, N,N, N', N'-tetramethylethylenediamine, hydrogen peroxide, 4-(N, N-dimethylamino)pyridine, triethylamine, acetone or any initiator for chemical or фотоинp://www.fips.ru/chr/8226.gif" ALIGN="ABSMIDDLE">100% solids or X= v/v100% for liquid substances), 3<a+b<40%; 0<c<10%; 0<d<95%; 0<e<95%; 0<f<90%; polymerization immobilization of different molecules comprising linear or three-dimensional porous polymer, including oligonucleotides, proteins and nucleic acids containing in its structure the active group, including aliphatic amino - and/or sulfhydryl groups under the reaction conditions of the merger or substitution (radical, nucleophilic, electrophilic and t
Composition for immobilization of biological macromolecules in the hydrogels, the method of preparation of the composition, the biochip, the method of carrying out pcr on the biochip // 2206575
The invention relates to compositions (K) for polymerization immobilization of biological macromolecules in the hydrogels in the formation of biochips TO=andA+b+withC+dD+eE, including the a - monomer based on the derivatives of acrylic and methacrylic acids; water-soluble crosslinking agent; With modified biological macromolecule containing unsaturated group, D is a water - soluble compound as the component environment for copolymerization; E - water, where a, b, C, d, e - the percentage (X) of each component in the composition (X= m/v100% solids and X=v/v100% for liquid substances), in which the total content of monomer and crosslinking agent lies in the range of 3-40% (3(a+b)(40), the ratio of monomer and cross-linking agent is within 97: 3-60:40, and the percentage of components C, D and E is in the range of 0.0001%10%; 0%d90%; 5%E.
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The invention relates to pharmaceutical industry
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The invention relates to pharmaceutical
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Drugs with a slow release // 2214244
Antiviral agent // 2190402
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