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Claims for Patent: 5,968,961

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Claims for Patent: 5,968,961

Title: Pharmaceutical compositions of tizoxanide and nitazoxanide
Abstract:The present invention relates to a pharmaceutical composition containing as active agent, solid particles of a compound selected from the group consisting of: compound of formula I ##STR1## and mixtures thereof, said particles having a particle size smaller than 200 .mu.m, the mean particle size of the said active solid particles being greater than 10 .mu.m. It also relates to a pharmaceutical composition which contains at least one pharmaceutically acceptable acid.
Inventor(s): Rossignol; Jean-Fran.cedilla.ois (Clearwater, FL)
Assignee: Romark Laboratories, L.C. (Tampa, FL)
Application Number:08/852,447
Patent Claims: 1. A pharmaceutical composition for oral administration containing as active agent, an effective amount of solid particles having a particle size smaller than 200 .mu.m of a compound of formula II ##STR5## in which the mean particle size of the said active solid particles is greater than 10 .mu.m.

2. The composition of claim 1, in which the mean particle size of the said active solid particles is between 10 and 100 .mu.m.

3. The composition of claim 1, in which the mean particle size of the said active solid particles is between 20 and 50 .mu.m.

4. The composition of claim 1, in which less than 10% of the said active solid particles has a particle size larger than 100 .mu.m.

5. The composition of claim 1, in which at least 50% of the said active solid particles has a particle size smaller than 50 .mu.m.

6. The composition of claim 1, in which less than 10% of the said active solid particles has a particle size smaller than 5 .mu.m.

7. The composition of claim 1 in which the distribution factor of the said active solid particles is between 0.8 and 2, said distribution factor being calculated by the following formula:

in which

F.sub.90% is the distribution factor at 90%;

.O slashed..sub.90% is the maximum particle size of the fraction of particles corresponding to 90% of the said active solid particles, and

.O slashed..sub.10% is the maximum particle size of the fraction of particles corresponding to 10% of the said active solid particles.

8. The composition of claim 1, in which the distribution factor of the said active solid particles is between 1.1 and 1.9, said distribution factor being calculated by the following formula

in which

F.sub.90% is the distribution factor at 90%

.O slashed..sub.90% is the maximum particle size of the fraction of particles corresponding to 90% of the said active solid particles, and

.O slashed..sub.10% is the maximum particle size of the fraction of particles corresponding to 10% of the said active solid particles.

9. The composition of claim 1, which comprises at least one pharmaceutically acceptable acid.

10. The composition of claim 1, which comprises at least one pharmaceutically acceptable acid selected from the group consisting of citric acid, glutamic acid, succinic acid, ethanesulfonic acid, acetic acid, tartric acid, ascorbic acid, methanesulfonic acid, fumaric acid, adipic acid, malic acid and mixtures thereof.

11. The composition of claim 10, in which the ratio of the weight of pharmaceutically acceptable acid/the weight of said active solid particles is between 0.01 and 0.5

12. The composition of claim 10, in which the ratio of the weight of pharmaceutically acceptable acid/the weight of said active solid particles is between 0.03 and 0.2.

13. A pharmaceutical composition for oral administration containing:

as active agent, an effective amount of solid particles having a particle size smaller than 200 .mu.m of a compound of formula II ##STR6## in which the mean particle size of the said active solid particles is greater than 10 .mu.m; and

at least one granulating agent.

14. The composition of claim 13, in which the mean particle size of the said active solid particles is comprised between 10 and 100 .mu.m.

15. The composition of claim 13, in which the mean particle size of the said active solid particles is comprised between 20 and 50.mu.m.

16. The composition of claim 13, in which less than 10% of the said active solid particles has a particle size larger than 100 .mu.m.

17. The composition of claim 13, in which at least 50% of the said active solid particles has a particle size smaller than 50 .mu.m.

18. The composition of claim 13, in which less than 10% of the said active solid particles has a particle size smaller than 5 .mu.m.

19. The composition of claim 13, in which the granulated active solid particles contains from 2 to 99.97% by weight of the said active compound and from 0.03 to 10% by weight of a granulating agent.

20. The composition of claim 19, in which the granulating agent is selected from the group consisting of polyvinylpyrrolidone, water, alcohol, sucrose hydroxyl cellulose and mixture thereof.

21. The composition of claim 13, in which the granulated active solid particles contain at least one pharmaceutically acceptable acid.

22. The composition of claim 13, in which the granulated active solid particles contain at least one pharmaceutically acceptable acid selected from the group consisting of citric acid, glutamic acid, succinic acid, ethanesulfonic acid, acetic acid, tartric acid, ascorbic acid, methanesulfonic acid, fumaric acid, adipic acid, malic acid and mixtures thereof.

23. The composition of claim 22, in which, for the granulated active solid particles, the ratio of the weight of pharmaceutically acceptable acid/the weight of said active agent is between 0.01 and 0.5.

24. A solid dosage form for oral administration containing:

as active agent, an effective amount of solid particles having a particle size smaller than 200 .mu.m of a compound of formula II ##STR7## in which the mean particle size of the said active solid particles is greater than 10 .mu.m;

at least one wetting agent, and

at least one starch derivative.

25. The dosage form of claim 24, in which the mean particle size of the said active solid particles is between 10 and 100 .mu.m.

26. The dosage form of claim 24, in which the mean particle size of the said active solid particles is between 20 and 50 .mu.m.

27. The dosage form of claim 24, in which less than 10% of the said active solid particles has a particle size larger than 100 .mu.m.

28. The dosage form of claim 24, in which at least 50% of the said active solid particles has a particle size smaller than 50 .mu.m.

29. The dosage form of claim 24, in which less than 10% of the said active solid particles has a particle size smaller than 5 .mu.m.

30. The composition of claim 24, in which the distribution factor of the said active solid particles is between 0.8 and 2, said distribution factor begin calculated by the following formula:

in which

F.sub.90% is the distribution factor at 90%;

.O slashed..sub.90% is the maximum particle size of the fraction of particles corresponding to 90% of the said active solid particles, and

.O slashed..sub.10% is the maximum particle size of the fraction of particles corresponding to 10% of the said active solid particles.

31. The composition of claim 24, in which the distribution factor of the said active solid particles is between 1.1 and 1.9, said distribution factor being calculated by the following formula

in which

F.sub.90% is the distribution factor at 90%;

.O slashed..sub.90% is the maximum particle size of the fraction of particles corresponding to 90% of the said active solid particles, and

.O slashed..sub.10% is the maximum particle size of the fraction of particles corresponding to 10% of the said active solid particles.

32. The dosage form of claim 24, which includes particles of at least one pharmaceutically acceptable acid.

33. The dosage form of claim 24, in which the active particles are granulated, said granulated active agent containing form 2 to 99.97% by weight of the said active compound and from 0.03 to 10% by weight of a granulating agent.

34. The dosage form of claim 33, in which the granulating agent is selected from the group consisting of polyvinylpyrrolidone, water, alcohol, sucrose hydroxyl cellulose and mixture thereof.

35. The dosage form of claim 24, said form comprised of:

solid granulated active particles, said granulated active particles containing from 2 to 90% by weigh of the said active compound, from 0.03 to 10% by weight of a granulating agent, and at least one pharmaceutically acceptable acid;

at least one wetting agent;

at least one starch derivative, and

at least one pharmaceutically acceptable acid.

36. An aqueous or other liquid suspension of solid particles for oral administration, said suspension containing:

as active agent, an effective amount of solid particles having a particle size smaller than 200 .mu.m of a compound of formula II ##STR8## in which the mean particle size of the said active solid particles is greater than 10 .mu.m; and

at least one pharmaceutically acceptable acid, the pH of the suspension being between 2 and 6.

37. The suspension of claim 36, in which the pH of the suspension is between 3 and 5.

38. An aqueous or other liquid suspension of solid particles for oral administration, said suspension containing:

as active agent, an effective amount of solid particles having a particle size smaller than 200 .mu.m of a compound of formula II ##STR9## in which the mean particle size of the said active solid particles is greater than 10 .mu.m;

a granulating agent; and

at least one pharmaceutically acceptable acid, the pH of the suspension being between 2 and 6.

39. The suspension of claim 38, in which the pH of the suspension is between 3 and 5.

40. A pharmaceutical composition for oral administration containing:

as active agent, an effective amount of solid particles having a particle size smaller than 200 .mu.m of a compound of formula II ##STR10## in which the mean particle size of the said active solid particles is greater than 10 .mu.m;

at least one pharmaceutically acceptable acid.

41. A paste for oral administration containing:

as active agent, an effective amount of solid particles having a particle size smaller than 200 .mu.m of a compound of formula II ##STR11## in which the mean particle size of the said active solid particles is greater than 10 .mu.m;

at least one wetting agent;

at least one pharmaceutically acceptable acid, the pH of the paste being between 2 and 6;

at least one thickener.

42. The paste of claim 41, in which the thickener is selected from the group consisting of Xanthan gum, a guar gum, crystalline cellulose, carruba gum, carboxymethylcellulose or a mixture thereof.

43. A paste for topical administration containing:

as active agent, an effective amount of solid particles having a particle size smaller than 200 .mu.m of a compound of formula II ##STR12## in which the mean particle size of the said active solid particles is greater than 10 .mu.m;

at least one wetting agent;

at least one additive selected from the group consisting of cetylic alcohol, glyceride derivatives, propyleneglycol and mixtures thereof;

at least one thickener.

44. A paste for intravaginal administration containing:

as active agent, solid particles having a particle size smaller than 200 .mu.m of a compound of formula II ##STR13## in which the mean particle size of the said active solid particles is greater than 10 .mu.m;

at least one wetting agent;

at least one additive selected from the group consisting of cetylic alcohol, glyceride derivatives, propyleneglycol and mixtures thereof;

at least one thickener.
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