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Claims for Patent: 6,117,894

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Claims for Patent: 6,117,894

Title: Acid stabilized 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## compound of formula II: ##STR2## 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. (DE)
Application Number:09/073,436
Patent Claims: 1. A pharmaceutical composition containing as active agent, the

compound of formula (II): ##STR7## and further containing a stability improving amount of a pharmaceutically acceptable acid.

2. A pharmaceutical composition containing as active agent, at least one compound selected from the group consisting of:

a compound of formula (I): ##STR8## and a compound of formula (II): ##STR9## and further containing a stability improving amount of a pharmaceutically acceptable acid, wherein said pharmaceutically acceptable acid is 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.

3. The composition of claim 1, wherein said pharmaceutically acceptable acid is citric acid.

4. The composition of claim 1, wherein said pharmaceutically acceptable acid is ascorbic acid.

5. A pharmaceutical composition containing as active agent, a compound of formula (II): ##STR10## and further containing a pharmaceutically acceptable acid in an amount sufficient to render the pH of said pharmaceutical composition between 2 and 6 when said pharmaceutical composition is contacted with water, wherein the weight ratio of the pharmaceutically acceptable acid to the pharmaceutical composition is between 0.01 and 0.5.

6. The composition of claim 5, wherein the weight ratio of the pharmaceutically acceptable acid to the pharmaceutical composition is between 0.03 and 0.2.

7. A pharmaceutical composition containing as active agent, at least one compound selected from the group consisting of:

a compound of formula (I): ##STR11## and a compound of formula (II): ##STR12## and further containing a pharmaceutically acceptable acid in an amount sufficient to render the pH of said pharmaceutical composition between 2 and 6 when said pharmaceutical composition is contacted with water, wherein said composition is in a solid dosage form, and wherein active particles of said composition are granulated in the presence of at least a granulating agent to form granulated active solid particles.

8. The composition of claim 7, wherein said granulating agent is selected from the group consisting of polyvinylpyrrolidone, water, alcohol, sucrose, hydroxyl cellulose and mixture thereof.

9. The composition of claim 7, wherein said pharmaceutically acceptable acid is 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.

10. A pharmaceutical composition containing as active agent, at least one compound selected from the group consisting of:

a compound of formula (I): ##STR13## and a compound of formula (II): ##STR14## and further containing a pharmaceutically acceptable acid in an amount sufficient to render the pH of said pharmaceutical composition between 2 and 6 when said pharmaceutical composition is contacted with water, wherein said composition is in the form of a suspension of solid particles of at least one compound of formula I and formula II in a liquid, and wherein said active particles prior to forming said suspension are granulated in the presence of at least a granulating agent to form granulated active solid particles.

11. The composition of claim 10, wherein said liquid is water.

12. A pharmaceutical composition containing as active agent, the compound of formula (II): ##STR15## and further containing a stability improving amount of a pharmaceutically acceptable acid, wherein said composition is in the form of a suspension of solid particles of the compound of formula II in a liquid, and wherein the pH of said suspension is between 2 and 6.

13. The composition of claim 12, wherein the pH of said suspension is between 3 and 5.

14. A pharmaceutical composition containing as active agent, at least one compound selected from the group consisting of:

a compound of formula (I): ##STR16## and a compound of formula (II): ##STR17## and further containing a pharmaceutically acceptable acid in an amount sufficient to render the pH of said pharmaceutical composition between 2 and 6 when said pharmaceutical composition is contacted with water, wherein said composition is in the form of a paste comprising active particles of at least one compound of formula (I) and formula (II), a wetting agent, and a thickener.

15. The composition of claim 14, wherein said pharmaceutically acceptable acid is 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.

16. The composition of claim 7, wherein said active agent is a compound of formula (I): ##STR18## and wherein said active particles prior to granulating have a particle size smaller than 200 .mu.m and a mean particle size greater than 10 .mu.m.

17. The composition of claim 16, wherein said mean particle size of said active particles is between 10 and 100 .mu.m.

18. The composition of claim 7, wherein said active agent is a compound of formula (I): ##STR19## and wherein said granulated active solid particles comprise from 2 to 99.97% by weight of said active compound and from 0.03 to 10% by weight of said granulating agent.

19. The composition of claim 7, wherein said active agent is a compound of formula (I): ##STR20## and wherein in granulated active solid particles the ratio by weight of pharmaceutically acceptable acid/weight of active agent is between 0.01 and 0.5.

20. The composition of claim 14, wherein said active agent is a compound of formula (I): ##STR21## and wherein said active particles have a particle size smaller than 200 .mu.m, less than 10% of said particles have a size larger than 100 .mu.m, less than 50% of said particles have a size larger than 50 .mu.m and less than 10% of said particles having a size less than 5 .mu.m.

21. A stabilized pharmaceutical suspension, said suspension containing:

(a) as active agent, at least one compound selected from the group consisting of:

a compound of formula I: ##STR22## and a compound of formula II: ##STR23## (b) a liquid, and (c) a pharmaceutically acceptable acid in an amount sufficient to provide a stabilizing pH for said suspension in the range of from 2.0 to 6.0.

22. A stabilized pharmaceutical suspension, said suspension containing:

(a) as active agent, at least one compound selected from the group consisting of:

a compound of formula I: ##STR24## and a compound of formula II: ##STR25## (d) water, and (e) a pharmaceutically acceptable acid in an amount sufficient to provide a stabilizing pH for said suspension in the range of from 2.0 to 6.0.

23. A stabilized pharmaceutical suspension, said suspension containing:

(a) as active agent, a compound of formula II: ##STR26## (b) a liquid, and (c) a pharmaceutically acceptable acid in an amount sufficient to provide a stabilizing pH for said suspension in the range of from 2.0 to 6.0.

24. The process as in claim 7, wherein at least one pharmaceutically acceptable acid is added during said granulation process.
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