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1. WO2020157484 - COMPRIMÉ ORODISPERSIBLE

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

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CLAIMS:

1. A composition in the form of an orodispersible tablet comprising a non-steroidal anti-inflammatory drug (NSAID) and a taste-masking agent wherein the NSAID is uncoated and has an average particle size of less than 100 pm.

2. A composition as claimed in Claim 1 wherein the average particle size of the uncoated NSAID is 40 - 60 pm.

3. A composition as claimed in Claim 2 wherein the average particle size is 50 pm.

4. A composition as claimed in any of the preceding Claims wherein the NSAID is ibuprofen and its pharmaceutically acceptable salts or hydrates.

5. A composition as claimed in any of the preceding Claims wherein the taste- masking agent is selected from the group consisting of ascorbic acid, monosodium citrate, fumaric acid, malic acid, and combinations thereof.

6. A composition as claimed in Claim 5 wherein the taste-masking agent is malic acid.

7. A composition as claimed in Claim 5 or Claim 6 wherein the amount of taste- masking agent is 0.1 - 15% by weight of the composition.

8. A composition as claimed in Claim 7 wherein the amount of malic acid is 5 - 10% by weight.

9. A composition as claimed in Claim 7 or Claim 8 wherein the amount of malic acid is 7 - 9% by weight.

10. A composition as claimed in any of the preceding Claims wherein the ratio by weight of the non-steroidal anti-inflammatory drug (NSAID) and the taste-masking agent in the composition can be from 1:1 - 8:1.

11. A composition as claimed in Claim 10 wherein the ratio of the NSAID and the tastemasking agent is 3:1 - 5:1.

12. A composition as claimed in Claim 11 wherein the ratio of the NSAID and the tastemasking agent is 4:1 by weight.

13. A composition as claimed in any of the preceding Claims wherein the composition includes a blend of a cellulosic binder, a sugar alcohol filler and a disintegrant.

14. A composition as claimed in Claim 13 wherein the cellulosic binder is microcrystalline cellulose, the sugar alcohol is mannitol and the disintegrant is cross-linked polyvinylpyrrolidone (crospovidone).

15. A composition as claimed in any of Claim 13 or Claim 14 wherein the composition contains 2 - 4 parts by weight of cellulosic binder per part by weight of disintegrant, and 8 - 12 parts by weight of sugar alcohol binder per part by weight of disintegrant.

16. A composition as claimed in Claim 15 wherein the composition contains cellulosic binder, sugar alcohol filler and disintegrant in a weight ratio of about of 2 - 3 :11

- 12:1.

17. A composition as claimed in any of the preceding Claims wherein the composition has a friability of up to 2% w/w and a hardness of between 40N and 100N.

18. A composition as claimed in Claim 17 wherein the composition has a friability of less than 1% w/w and a hardness of greater than 50N.

19. A composition as claimed in Claim 17 or Claim 18 wherein the composition has a friability of less than 0.5% w/w and a hardness of greater than 80N.

20. A composition as claimed in any of the preceding Claims wherein the composition comprises an uncoated non-steroidal anti-inflammatory drug (NSAID), a taste- masking agent and a disintegrant wherein the uncoated NSAID has an average particle size of less than 100 pm, the taste-masking agent is selected to be malic acid which is present in an amount of 0.1 - 15% by weight of the composition, and the disintegrant is selected to be cross-linked polyvinylpyrrolidone (crospovidone) which is present in an amount of 1-10% by weight of the composition.

21. A composition as claimed in any Claims 1 - 19 wherein the composition comprises an uncoated non-steroidal anti-inflammatory drug (NSAID), a taste-masking agent and a disintegrant wherein the uncoated NSAID has an average particle size of less than 100 pm, the taste-masking agent is selected to be malic acid which is present in an amount of 0.1 - 15% by weight of the composition, wherein the ratio of the uncoated non-steroidal anti-inflammatory drug (NSAID) to taste-masking agent is 4:1 by weight.

22. A composition as claimed in Claim 19 wherein the composition further comprises a disintegrant which is selected to be cross-linked polyvinylpyrrolidone (crospovidone) and which is present in an amount of 1-10% by weight of the composition.

23. A composition as claimed in any of the preceding Claims wherein the composition comprises ibuprofen, a taste-masking agent and a disintegrant wherein the weight ratio of ibuprofe taste-masking agent:disintegrant is from about 10:5:1 to about 5:1:1.

24. A composition as claimed in Claim 23 wherein the weight ratio of ibuprofe taste- masking agent:disintegrant is from about 8:2:1 to about 7:1:1.

25. A composition as claimed in any of the preceding Claims wherein the composition comprises uncoated ibuprofen, a taste-masking agent and a disintegrant wherein the uncoated ibuprofen has an average particle size of 50 pm, the taste-masking agent is selected to be malic acid which can be present in an amount of 7 - 9% by weight of the composition, wherein the ratio of the uncoated ibuprofen to taste- masking agent is 4:1 by weight and the disintegrant is selected to be cross-linked polyvinylpyrrolidone (crospovidone) which can be present in an amount of 3 - 6% by weight of the composition and wherein the weight ratio of ibuprofe taste- masking agent:disintegrant is from about 8:2:1 to about 7:1:1.

26. A composition as claimed in any of the preceding Claims wherein the composition comprises an uncoated non-steroidal anti-inflammatory drug (NSAID), a taste- masking agent, a binder, a disintegrant and a filler wherein the uncoated NSAID has an average particle size of less than 100 pm, the taste-masking agent can be present in an amount of 0.1 - 15% by weight of the composition, wherein the ratio of the NSAID to taste-masking agent is 4:1 by weight and wherein the composition contains 2 - 4 parts by weight of binder per part by weight of disintegrant, and 8 - 12 parts by weight of filler per part by weight of disintegrant.

27. A composition as claimed in Claim 26 wherein the composition is in the form of an orodispersible tablet comprising uncoated ibuprofen, a taste-masking agent, a cellulosic binder, a disintegrant and a sugar alcohol filler wherein the ibuprofen has an average particle size of 50 pm, the taste-masking agent is selected to be malic acid and is present in an amount of 0.1 - 15% by weight of the composition, wherein the ratio of the uncoated ibuprofen to taste-masking agent is 4:1 by weight, the cellulosic binder is selected to be microcrystalline cellulose and is present in an amount of 2 - 25% by weight of the composition, the disintegrant is selected to be cross-linked polyvinylpyrrolidone (crospovidone) and is present in an amount of 1-10% by weight of the composition, the filler is selected to be mannitol and is present in an amount of 20 - 70% by weight of the composition, wherein the composition contains 2 - 4 parts by weight of cellulosic binder per part by weight of disintegrant, and 8 - 12 parts by weight of sugar alcohol filler per part by weight of disintegrant, and wherein the weight ratio of ibuprofe malic acid:cross-linked polyvinylpyrrolidone is from about 10:5:1 to about 5:1:1.

28. A composition as claimed in any of Claims 1 - 19 wherein the composition comprises:

(a) 20 - 35% of an uncoated NSAID having an average particle size of less than 100 pm or a pharmaceutically acceptable salt thereof;

(b) 20 - 70% of a filler;

(c) 0.5 - 5% of a lubricant;

(d) 5 - 10% of a taste-masking agent; and

(e) 1 - 10% of a disintegrant.

29. A composition as claimed in Claim 28 wherein the composition comprises:

(a) 25 - 30% of an uncoated NSAID having an average particle size of less than 100 pm or a pharmaceutically acceptable salt thereof;

(b) 40 - 50% of a filler;

(c) 0.5 - 5% of a lubricant;

(d) 5 - 10% of a taste-masking agent; and

(e) 1 - 10% of a disintegrant.

30. A composition as claimed in Claim 28 or Claim 29 wherein the composition further comprises one or more additional excipients selected from:

(f) 0.1 - 5% of a glidant; and

(g) 2 - 25% of a binder.

31. A composition as claimed on any of Claims 28 - 30 wherein the composition further comprises:

(a) 28 - 30% of an uncoated NSAID having an average particle size of less than 100 pm or a pharmaceutically acceptable salt thereof;

(b) 0.5 - 1.5% of a glidant;

(c) 42 - 47% of a filler;

(d) 0.75 - 1.5% of a lubricant;

(e) 8 - 12% of a binder;

(f) 6 - 8% of a taste-masking agent; and

(g) 3 - 5% of a disintegrant.

32. A composition as claimed on any of Claims 28 - 31 wherein the composition comprises:

(a) 25 - 30% of uncoated ibuprofen having an average particle size of less than 100 pm or a pharmaceutically acceptable salt thereof;

(b) 0.1 - 5% of colloidal silica;

(c) 40 - 50% of mannitol;

(d) 0.5 - 5% of sodium stearyl fumarate;

(e) 5 - 15% of microcrystalline cellulose;

(f) 5 - 10% of malic acid; and

(g) 1 - 10% of crospovidone.

33. A composition as claimed in any of Claims 28 - 32 wherein the composition comprises:

(a) 28 - 30% of uncoated ibuprofen having an average particle size of less than 100 pm or a pharmaceutically acceptable salt thereof;

(b) 0.5 - 1.5% of colloidal silica;

(c) 42 - 47% of mannitol;

(d) 0.75 - 1.5% of sodium stearyl fumarate;

(e) 8 - 12% of microcrystalline cellulose;

(f) 6 - 8% of malic acid; and

(g) 3 - 5% of crospovidone.

34. A composition as claimed in any of Claims 28 - 33 wherein the average particle size of the uncoated ibuprofen is from 40 - 60 pm.

35. Use of malic acid as a taste-masking agent in a composition in the form of an orodispersible tablet that comprises an uncoated ibuprofen particle having an average particle size of 40 - 60 pm.

36. The use as claimed in Claim 35 wherein the average particle size of the uncoated ibuprofen is 50 pm.

37. The use as claimed in either Claim 35 or Claim 36 wherein the ratio by weight of the uncoated ibuprofen particle and the malic acid in the composition is from 1:1 - 8:1.

38. The use as claimed in Claim 37 wherein the ratio by weight of the uncoated ibuprofen particle and the malic acid in the composition is from 3:1 - 5:1.

39. The use as claimed in Claim 38 wherein the ratio by weight of the uncoated ibuprofen particle and the malic acid in the composition is from 4:1.

40. Use of malic acid as a taste-masking agent in a composition in the form of an orodispersible tablet that comprises an uncoated ibuprofen particle having an average particle size of 50 pm wherein the ratio by weight of the uncoated ibuprofen particle and the malic acid is 4:1.