Method for producing an immediately decomposing oral form of administration which releases active ingredients

1. A method for producing

a pharmaceutical composition that when placed in the mouth immediately disintegrates releasing active ingredient (a) comprising:

vigorously mixing

(a) an anionic active pharmaceutical ingredient with

(b) a copolymer consisting of free-radical polymerized C 1 to C 4 esters of acrylic or methacrylic acid and further (meth)acrylate monomers which have functional tertiary amino groups, and

(c) 5 to 50% by weight, based on (b), of a C 12 to C 22 carboxylic acid in a melt,

solidifying the mixture,

grinding the mixture to an active ingredient-containing powder with an average particle size of 200 μm or less, and

incorporating the powder into a water-soluble matrix of at least one pharmaceutically acceptable excipient,

with the proviso that not more than 3% by weight, based on the copolymer (b), of emulsifiers having an HLB of at least 14 may be present.

2. The method as claimed in claim 1 , wherein a twin-screw extruder is employed for the purpose of vigorous mixing in the melt.

3. The method as claimed in claim 1 , wherein extrusion takes place at temperatures in the range from 80 to 200° C.

4. The method as claimed in claim 1 , wherein the incorporation of the powder into the water-soluble matrix takes place by compression, casting, granulation or freeze drying.

5. A powder with an average particle size of 200 μm or less, comprising:

(a) an anionic active pharmaceutical ingredient,

(b) a copolymer which consists of free-radical polymerized C 1 to C 4 esters of acrylic or methacrylic acid and further (meth)acrylate monomers which have functional tertiary amino groups, and

(c) 5 to 50% by weight, based on (b), of a C 12 to C 22 carboxylic acid,

with the proviso that less than 3% by weight, based on the copolymer (b), of an emulsifier having an HLB of at least 14 is present,

wherein said powder when placed in the mouth immediately disintegrates and releases active ingredient (a); and

wherein said powder is produced by vigorously mixing

(i) the anionic active pharmaceutical ingredient with

(ii) the copolymer consisting of free-radical polymerized C 1 to C 4 esters of acrylic or methacrylic acid and further (meth)acrylate monomers which have functional tertiary amino groups, and

(iii) 5 to 50% by weight, based on (b), of said C 12 to C 22 carboxylic acid, in a melt, solidifying the mixture, and grinding to an active ingredient-containing powder with an average particle size of 200 μm or less.

6. The powder of claim 5 , wherein (a) comprises an anionic analgesic, an anionic antirheumatic, or an anionic antibiotic.

7. The powder of claim 5 , wherein said anionic active pharmaceutical ingredient (a) has been incorporated into said copolymer (b).

8. The powder of claim 5 , wherein copolymer (b) is a copolymer of methyl methacrylate, butyl methacrylate, and dimethylaminoethyl methacrylate.

9. The powder of claim 5 , wherein carboxylic acid (c) is at least one of selected from the group consisting of lauric acid, myristic acid, palmitic acid, and stearic acid.

10. The powder of claim 5 that contains no emulsifier having an HLB (hydrophilic/lipophilic balance) of 14 or more.

11. The powder of claim 5 that contains from 1 to less than 3% by weight, based on the copolymer, of an emulsifier having an HLB (hydrophilic/lipophilic balance) of 14 or more.

12. The powder of claim 5 that contains from 1-2% of an emulsifier having an HLB (hydrophilic/lipophilic balance) of 14 or more.

13. The powder of claim 5 , which has a bitterness value determined by DAB 1999 method 2.8.N8 below 1,000 for at least 30 seconds after release of the active ingredient (a).

14. A pharmaceutical composition comprising the powder of claim 5 and at least one pharmaceutically acceptable excipient.

15. The pharmaceutical composition of claim 14 , wherein said at least one excipient is a release agent having an HLB between 3 and 8.

16. The pharmaceutical composition of claim 14 , wherein said at least one excipient is a plasticizer having a molecular weight ranging between 100 and 20,000 and which comprises at least one hydrophilic group.

17. The pharmaceutical composition of claim 14 in the form of a compressed tablet, suckable tablet, freeze-dried tablet, cast tablet, pastilles, sachet, chewable tablet, powder for reconstitution, lozenge and/or liquid-filled lozenge.

18. The pharmaceutical composition of claim 14 which is produced by:

vigorously mixing

(a) an anionic active pharmaceutical ingredient with

(b) a copolymer consisting of free-radical polymerized C 1 to C 4 esters of acrylic or methacrylic acid and further (meth)acrylate monomers which have functional tertiary amino groups, and

(c) 5 to 50% by weight, based on (b), of a C 12 to C 22 carboxylic acid in a melt with no emulsifier having an HLB of at least 14,

solidifying the mixture,

grinding to an active ingredient-containing powder with an average particle size of 200 μm or less, and

incorporating the powder into a water-soluble matrix of at least one pharmaceutically acceptable excipient.