Patent EA-002908-B1 (EA)
Title: Pharmaceutical compositions of tozoxanide and nitazoxanide
Inventor: ROSSIGNOL JEAN-FRANCOIS
IPC: A61P31/04
Filed: 1998-05-06
Abstract: 1. A pharmaceutical composition for oral administration containing as active agent at least one compound selected from the group consisting of: compound of formula (I)   and compound of formula (II)   wherein said active agent is in the form of active particles having a particle size smaller than 200 μm and a mean particle size of greater than 5 μm. 2. The composition of Claim 1, wherein the mean particle size of said active particles is between 10 and 100 μm. 3. The composition of Claim 1, wherein the mean particle size of said active particles is between 20 and 50 μm. 4. The composition of Claim 1, wherein less than 10% by weight of said active particles has a particle size larger than 100 μm. 5. The composition of Claim 1, wherein at least 50% by weight of said active particles has a particle size smaller than 50 μm. 6. The composition of Claim 1, wherein less than 10% by weight of said active particles has a particle size smaller than 5 μm. 7. The composition of Claim 1, wherein distribution coefficient of active solid particles is from 0,8 to 2, said distribution coefficient is calculated F90% = (D90% - D10%)/((D90% + D10%)/2) Where in  F90% - distribution coefficient at 90%; D90% - maximal particle size in particle fraction, corresponding 90% of said active solid particles, and D10% - maximal particle size in particle fraction, corresponding 10% of said active solid particles. 9. A pharmaceutical paste for topical administration which comprises as an active ingredient solid particles of at least one compound, selected from the group, consisting of: compound of formula I   and compound of formula II   which have particle size smaller than 200 μm and a mean particle size of greater than 5 μm; at least one thickener; at least one moistening agent; and at least one pharmaceutically acceptable acid, at that pH of the paste has the meaning from 2 to 6. 10. A pharmaceutical paste as in Claim 9, wherein said paste further comprises at least one additive selected from the group consisting of cetylic alcohol, glyceride derivatives, propylene glycol, and mixtures thereof. 11. A pharmaceutical composition for oral administration containing active agent granulated in the presence of a granulating agent, wherein: said active agent is in the form of solid active particles of at least one compound selected from the group consisting of: compound of formula (I)   compound of formula (II)   and wherein said active particles have a particle size smaller than 200 μm and a mean particle size of greater than 10 μm. 12. The composition of Claim 11, wherein said granulating agent is selected from the group consisting of polyvinylpyrrolidone, water, alcohol, sucrose, hydroxyl cellulose and mixture thereof. 13. The composition of Claim 11, wherein said granulated active solid particles contain at least one pharmaceutically acceptable acid. 14. The composition of Claim 13, 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. 15. The composition of Claim 13, wherein the ratio of the weight of pharmaceutically acceptable acid/the weight of said solid particles is between 0.01 and 0.5. 16. A pharmaceutical composition for oral administration containing active agent, a wetting agent and a starch derivative, wherein: said active agent is in the form of solid active particles of at least one compound selected from the group consisting of: compound of formula (I)   compound of formula (II)   and wherein said active particles having a particle size smaller than 200 μm and a mean particle size of greater than 10 μm. 17. The pharmaceutical composition of Claim 16, further comprising at least one pharmaceutically acceptable acid. 18. The pharmaceutical composition of Claim 16, wherein the active particles are granulated in the presence of a granulating agent to form granulated active agent containing from 2 to 99.97% by weight of said active compound and from 0.03 to 10% by weight of a granulating agent. 19. The pharmaceutical composition of Claim 18, wherein said granulating agent is selected among the group consisting of polyvinylpyrrolidone, water, alcohol, sucrose, hydroxyl cellulose and mixtures thereof. 20. A liquid suspension of active agent for oral administration, said suspension containing: as active agent, solid particles of at least one compound selected from the group consisting of: compound of formula (I)   and compound of formula (II)   said particles having a particle size smaller than 200 μm and a mean particle size greater than 10 μm; and at least one pharmaceutically acceptable acid, the pH of the suspension being between 2 and 6. 21. The suspension of Claim 20, wherein the pH of the suspension is between 3 and 5. 22. The suspension of Claim 20, further comprising a granulating agent.