Protective coatings for acidic active ingredients

Patent metadata

Field	Value
Publication number	US-9795576-B2
Application number	US-201113246324-A
Country	US
Kind code	B2
Filing date	Sep 27, 2011
Priority date	Sep 27, 2010
Publication date	Oct 24, 2017
Grant date	Oct 24, 2017

Abstract

Dosage forms provided with protective coatings in which a core comprising at least one acidic active ingredient is provided with at least one inner and one outer coating layer, where the outer layer comprises, as component A, a cationic polymer which is an emulsion polymer of N,N-diethylaminoethyl methacrylate and further monomers.

First claim

The invention claimed is:

1. A dosage form provided with protective coatings, in which a core comprising at least one acidic active ingredient is provided with at least one inner and one outer coating layer, where the outer layer comprises, as component A, a cationic polymer which is an emulsion polymer of N,N-diethylaminoethyl methacrylate and further monomers,
wherein the inner coating layer comprises a neutral water-soluble polymer comprising polyvinyl alcohols, polyalkylene glycol—polyvinyl alcohol graft copolymers, polyvinylpyrrolidones, vinylpyrrolidone—vinyl acetate copolymers, alkylated and hydroxyalkylated celluloses or starches or mixtures of such polymers, and
wherein component A of the outer coating layer comprises a polymer obtained by free-radical polymerization of:
a) N,N-diethylaminoethyl methacrylate, and
b) at least one free-radically polymerizable compound selected from esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids with C 1 -C 8 -alkanols; and

wherein component A of the outer coating layer comprises a polymer of 43 to 47% by weight, based on the total weight of the monomers used for the polymerization, of N,N-diethylaminoethyl methacrylate a), and 53 to 57% by weight, based on the total weight of the monomers used for the polymerization, of at least one compound b).

2. The dosage form according to claim 1 , wherein the at least one acidic active ingredient comprises an active ingredient with free carboxyl, sulfonic acid or phosphonic acid groups, acidic hydroxyl groups, acidic N—H groups or acidic C—H groups or mixtures of these active ingredients.

3. The dosage form according to claim 1 , comprising acidic active ingredients with a pKa value between 6.5 and 0.5.

4. The dosage form according to claim 1 , comprising acidic active ingredients with a pKa value between 5.0 and 1.0.

5. The dosage form according to claim 1 , wherein the neutral polymer of the inner coating layer comprises polyvinyl alcohols, polyalkylene glycol—polyvinyl alcohol graft copolymers or mixtures thereof.

6. The dosage form according to claim 1 , wherein component A comprises a polymer obtained with methyl methacrylate as monomer b).

7. The dosage form according to claim 1 , wherein the outer coating layer further comprises, as component B, one or more antioxidants.

8. The dosage form according to claim 1 , wherein the outer coating layer further comprises, as component B, one or more antioxidants selected from the group consisting of phenolic antioxidants, thiolic antioxidants, basic amino acids, alkali metal carbonates and alkali metal bicarbonates.

9. The dosage form according to claim 1 , wherein the outer coating layer further comprises, as component C, one or more plasticizers.

10. The dosage form according to claim 1 , wherein the outer coating layer further comprises, as component C, one or more plasticizers selected from the group consisting of tributyl citrate, acetyltributyl citrate, acetyltriethyl citrate, triacetin, triethyl citrate, diethyl sebacate and dibutyl sebacate.

11. The dosage form according to claim 1 , wherein the outer coating layer further comprises, as component D, one or more pharmaceutical excipients selected from the group consisting of aroma substances, taste-improving substances, sweeteners, glidants, wetting agents, release agents, antiadhesives, stabilizers, pore formers, neutralizing agents, polishes, dyes, pigments, disinfectants or preservatives, and thickeners.

12. The dosage form according to claim 1 , wherein the inner coating layer has a layer thickness of from 1 to 50 μm.

13. The dosage form according to claim 1 , wherein the inner coating layer has a layer thickness of from 2 to 25 μm.

14. The dosage form according to claim 1 , wherein the inner coating layer has a layer thickness of from 5 to 15 μm.

15. The dosage form according to claim 1 , wherein the outer coating layer has a layer thickness of from 5 to 200 μm.

16. The dosage form according to claim 1 , wherein the outer coating layer has a layer thickness of from 10 to 150 μm.

17. The dosage form according to claim 1 , wherein the outer coating layer has a layer thickness of from 20 to 100 μm.

Assignees

• Kolter Karl
• Angel Maximilian
• Basf Se

Inventors

• Kolter Karl
• Angel Maximilian

Classifications

• A61K31/616

  by carboxylic acids, e.g. acetylsalicylic acid · CPC title

• A61K9/5073

  having two or more different coatings optionally including drug-containing subcoatings · CPC title

• A61K31/192 Primary

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title