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).

Claims

1. 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.

 

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