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1. WO2020114714 - PROCESS FOR PREPARING POLYMERIC PARTICLES

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[ EN ]

Claims

1. Process for preparing polymeric particles, comprising polymerized units of methacrylic acid and further monomers, with an overall monomer composition by weight comprising polymerized units of 5 to 25 % by weight methacrylic acid and 75 to 95 % by weight of further monomers, wherein the further monomers are selected from C1- to C4-alkylesters of methacrylic acid and/or C1- to C4-alkylesters of acrylic acid, by stepwise or gradient emulsion polymerization, wherein the ratio by weight of polymerized units of methacrylic acid to further monomers is increasing stepwise or in a gradient from the center to the surface of the particles and wherein the polymeric particles are obtained in the form of an aqueous dispersion.

Process according to Claim 1 , wherein the polymeric particles are polymeric particles with an overall monomer composition by weight comprising polymerized units of 10 to 30% by weight methyl methacrylate, 50 to 70% by weight methyl acrylate and 5 to 15 % by weight methacrylic acid.

3. Process according to Claims 1 or 2, wherein the process is a stepwise emulsion

polymerization comprising at least a first and a second step, wherein in the first step polymeric core particles are polymerized, wherein the ratio by weight of methacrylic acid to the further monomers is lower compared to the overall monomer composition by weight of methacrylic acid and the further monomers and wherein in the second step a polymeric shell is polymerized onto the polymeric core wherein the ratio by weight of methacrylic acid to the further monomers is higher compared to the overall monomer composition by weight of methacrylic acid and the further monomers.

4. Process according to any of Claims 1 to 3, wherein the process is a stepwise emulsion polymerization with two steps, wherein in the first step the further monomers, preferably methyl methacrylate and methyl acrylate, are polymerized as polymeric core particles and wherein in the second step the methacrylic acid is added and polymerized as polymeric shell onto the polymeric core particles.

5. Process according to Claim 1 or 2, wherein the process is a gradient emulsion

polymerization, wherein the monomers are polymerized in a continuous process, wherein the ratio by weight of the methacrylic acid to the further monomers is continuously increased during the polymerization process.

6. Process according to any of Claims 1 to 5, wherein the polymeric particles are converted from the aqueous dispersion to a dry form, preferably to a powder or a granulate, by spray drying, freeze drying, spray granulation or extrusion of the aqueous dispersion.

7. Polymeric particle, obtainable in a process according to any of Claims 1 to 6, comprising polymerized units of 10 to 30% by weight methyl methacrylate, 50 to 70% by weight methyl acrylate and 5 to 15% by weight methacrylic acid with a stepwise or continuous increase of the polymerized methacrylic acid units from the center to the surface.

8. Polymeric particle according to Claim 7, wherein the average particle size is in the range from about 50 to 500 nm, preferably from about 80 to 300 nm.

9. Polymeric particle according to Claim 7 or 8, wherein the increasing concentration of

polymerized units of methacrylic acid from the center to the surface of the particle results in an accelerated dissolution speed compared to a polymeric particle, polymerized by an emulsion polymerization in one step.

10. Polymeric particle according to any of Claims 7 to 9, wherein the increasing concentration of polymerized units of methacrylic acid from the center to the surface of the particles results in a lowered active ingredient release pH of an active ingredient containing coated composition or an active ingredient containing polymeric matrix composition with a polymeric coating or a matrix derived from the polymeric particle, compared to a coating composition or a polymeric matrix composition derived from a polymeric particle of the same monomer composition polymerized in a one step emulsion polymerization process.

1 1. The polymeric particle according to any of Claims 7 to 10, wherein the concentration of polymerized units of methacrylic acid by weight at the surface is increased by a factor of

1.2 to 5, preferably 1.5 to 4.5 compared to the of methacrylic acid content by weight in the allover monomer composition by weight of the polymeric particle.

12. Use of a polymeric particle according to any of Claims 7 to 1 1 as a coating or binding agent in a pharmaceutical or nutraceutical dosage form.

13. Aqueous dispersion comprising water and polymeric particles according to one or more Claims 7 to 1 1.

14. Aqueous dispersion according to Claim 13, comprising 10 to 50 % by weight of the

polymeric particles.

15. Dosage form, comprising a pharmaceutical or nutraceutical active ingredient and a polymeric coating or a polymeric matrix, wherein the polymeric coating or the polymeric matrix is derived from the polymeric particles according to one or more Claims 7 to 1 1.