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Claims for Patent: 6,136,347

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Claims for Patent: 6,136,347

Title: Flavor-masked pharmaceutical compositions
Abstract:The invention relates to flavor-masked pharmaceutical compositions for oral administration, their preparation and their use as medicaments. The new pharmaceutical preparations according to the invention make it possible to administer pharmaceutical active substances having very unpleasant organoleptic properties such as, for example, very bad taste, even in liquid form.
Inventor(s): Pollinger; Norbert (Odenthal, DE), Michaelis; Johannes (Cologne, DE), Benke; Klaus (Kyoto, JP), Rupp; Roland (Leichlingen, DE), Bucheler; Manfred (Overath, DE)
Assignee: Bayer Aktiengesellschaft (Leverkusen, DE)
Application Number:08/653,535
Patent Claims: 1. A pharmaceutical composition comprising microcapsules, said microcapsules comprising an active ingredient microencapsulated within a microcapsule wall, wherein said active ingredient is present in said microcapsules as an anhydrate of its base form, said microcapsule wall comprises a coating of water-insoluble neutral methyl or ethyl ester compounds of polymethacrylic acid or a mixture thereof, or quaternary ammonium compounds of polymethacrylic acid or a mixture thereof, or ethylcellulose, and wherein the microcapsule wall further comprises triethylcitrate and optionally hydroxypropylmethylcellulose, and said microcapsules are free of disintegrants.

2. A pharmaceutical composition according to claim 1, wherein the microcapsule wall comprises a coating comprising a mixture of 100 parts by weight of neutral methyl or ethyl esters of polymethacrylic acid or a mixture thereof and 20 to 50 parts by weight of hydroxypropylmethylcellulose.

3. A pharmaceutical composition according to claim 1, further comprising additional water-soluble polymers, plasticizers and wetting agents.

4. A pharmaceutical composition according to claim 1, wherein the microcapsules have a size of 10 to 800 .mu.m.

5. A pharmaceutical composition according to claim 1, wherein the active ingredient is an antimicrobial active ingredient.

6. A pharmaceutical composition according to claim 1, wherein the active ingredient is a gyrase inhibitor selected from the group consisting of naphthyridone- and quinolone carboxylic acid gyrase inhibitors.

7. A pharmaceutical composition according to claim 1, wherein the active ingredient is ciprofloxacin.

8. A pharmaceutical composition according to claim 1, which is in the form of an oily juice formulation.

9. A pharmaceutical composition according to claim 1, which is in the form of a sachet.

10. A pharmaceutical composition in the form of an oily juice formulation, said pharmaceutical composition comprising microcapsules, said microcapsules comprising an active ingredient microencapsulated within a microcapsule wall, wherein said active ingredient is present in said microcapsules as an anhydrate of its base form, said microcapsule wall comprises a coating of water-insoluble neutral methyl or ethyl ester compounds of polymethacrylic acid or a mixture thereof, or quaternary ammonium compounds of polymethacrylic acid or a mixture thereof, or ethylcellulose, and said microcapsules are free of disintegrants.

11. A pharmaceutical composition according to claim 10, wherein the microcapsule wall further comprises triethylcitrate and optionally hydroxypropylmethylcellulose.

12. A pharmaceutical composition according to claim 10, wherein the microcapsule wall comprises a coating comprising a mixture of 100 parts by weight of neutral methyl or ethyl esters of polymethacrylic acid or a mixture thereof and 20 to 50 parts by weight of hydroxypropylmethylcellulose.

13. A pharmaceutical composition according to claim 10, further comprising additional water-soluble polymers, plasticizers and wetting agents.

14. A pharmaceutical composition according to claim 10, wherein the microcapsules have a size of 10 to 800 .mu.m.

15. A pharmaceutical composition according to claim 10, wherein the active ingredient is an antimicrobial active ingredient.

16. A pharmaceutical composition according to claim 10, wherein the active ingredient is a gyrase inhibitor selected from the group consisting of naphthyridone- and quinolone carboxylic acid gyrase inhibitors.

17. A pharmaceutical composition according to claim 10, wherein the active ingredient is ciprofloxacin.

18. A pharmaceutical composition which is in the form of sachet comprising microcapsules, said microcapsules comprising an active ingredient microencapsulated within a microcapsule wall, wherein said active ingredient is present in said microcapsules as an anhydrate of its base form, said microcapsule wall comprises a coating of water-insoluble neutral methyl or ethyl ester compounds of polymethacrylic acid or a mixture thereof, or quaternary ammonium compounds of polymethacrylic acid or a mixture thereof, or ethylcellulose, and said microcapsules are free of disintegrants.

19. A pharmaceutical composition according to claim 18, wherein the microcapsule wall further comprises triethylcitrate and optionally hydroxypropylmethylcellulose.

20. A pharmaceutical composition according to claim 18, wherein the microcapsule wall comprises a coating comprising a mixture of 100 parts by weight of neutral methyl or ethyl esters of polymethacrylic acid or a mixture thereof and 20 to 50 parts by weight of hydroxypropylmethylcellulose.

21. A pharmaceutical composition according to claim 18, further comprising additional water-soluble polymers, plasticizers and wetting agents.

22. A pharmaceutical composition according to claim 18, wherein the microcapsules have a size of 10 to 800 .mu.m.

23. A pharmaceutical composition according to claim 18, wherein the active ingredient is an antimicrobial active ingredient.

24. A pharmaceutical composition according to claim 18, wherein the active ingredient is a gyrase inhibitor selected from the group consisting of naphthyridone- and quinolone carboxylic acid gyrase inhibitors.

25. A pharmaceutical composition according to claim 18, wherein the active ingredient is ciprofloxacin.

26. In the method of combatting a disease in a patient suffering therefrom, said method comprising administering to such patient an
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