Claims for Patent: 8,529,945

Summary for Patent: 8,529,945

Title:	Oral antimicrobial pharmaceutical compositions
Abstract:	The present invention relates to oral pharmaceutical compositions with controlled and/or programmed release containing at least one active ingredient having antimicrobial and/or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.
Inventor(s):	Ajani; Mauro (Milan, IT), Bozzella; Roberta (Milan, IT), Celasco; Giuseppe (Genoa, IT), Villa; Roberto (Lecco, IT)
Assignee:	Cosmo Technologies Ltd. (Dublin, IE)
Application Number:	13/616,582
Patent Claims:	1. A controlled release oral pharmaceutical composition comprising: (1) a tablet core comprising a homogeneous structure comprising (a) rifamycin SV in an amount effective for the treatment of an infection of the colon, (b) at least one lipophilic substance having a melting point less than about 90.degree. C, (c) at least one amphiphilic substance and (d) at least one hydrophilic substance; and (2) a coating on said tablet core, said coating comprising a gastro-resistant substance, wherein said controlled release oral pharmaceutical composition releases said rifamycin SV substantially in the large intestine. 2. The controlled release oral pharmaceutical composition of claim 1, wherein said controlled release oral pharmaceutical composition releases said rifamycin SV solely in the colon. 3. The controlled release oral pharmaceutical composition of claim 1, wherein said rifamycin SV comprises rifamycin SV or a pharmaceutically acceptable salt thereof. 4. The controlled release oral pharmaceutical composition of claim 1, wherein said controlled release oral pharmaceutical composition is resistant to dissolution for 2 hours in an environment at pH 1. 5. The controlled release oral pharmaceutical composition of claim 1, wherein said controlled release oral pharmaceutical composition is resistant to dissolution for 1 hour in an environment at pH 6.4. 6. The controlled release oral pharmaceutical composition of claim 1, wherein said controlled release oral pharmaceutical composition is resistant to dissolution for 2 hours in an environment at pH 1 and is resistant to dissolution for 1 hour in an environment at pH 6.4. 7. The controlled release oral pharmaceutical composition of claim 1, wherein said gastro-resistant substance comprises at least one methacrylic acid polymer. 8. The controlled release oral pharmaceutical composition of claim 1, wherein said rifamycin SV comprises from about 20% to about 60% by weight of the total weight of said controlled release oral pharmaceutical composition. 9. The controlled release oral pharmaceutical composition of claim 1, wherein said infection of the colon is caused by gram negative bacteria, gram positive bacteria, or a combination of gram negative bacteria and gram positive bacteria. 10. The controlled release oral pharmaceutical composition of claim 1, wherein said infection of the colon is infectious colitis, bacillary dysentery, colitis, or diverticulitis. 11. The controlled release oral pharmaceutical composition of claim 1, wherein said infection of the colon causes diarrhea. 12. The controlled release oral pharmaceutical composition of claim 1, wherein said infection of the colon causes hyperammonaemia. 13. The controlled release oral pharmaceutical composition of claim 1, wherein said hydrophilic substance comprises at least one of a hydroxyalkylcellulose, an alkylcellulose, a carboxyalkylcellulose, a polyvinyl alcohol, a carboxyvinyl polymer, a carboxyvinyl copolymer, a polysaccharide, hyduronic acid, glucoronic acid, a glucosamine, or a pectin. 14. The controlled release oral pharmaceutical composition of claim 1, wherein said amphiphilic substance comprises at least one of a phospholipid, a ceramide, a sphingomyelin, lecithin, an alkyl block copolymer, a salt of a sulphated alkyl acid, a polyoxyethylenealkyl, or sorbitan. 15. The controlled release oral pharmaceutical. composition of claim 14, wherein said amphiphilic substance is lecithin. 16. The controlled release oral pharmaceutical composition of claim 1, wherein said lipophilic substance comprises at least one of beeswax, carnuba wax, stearic acid, or stearin. 17. A controlled release oral pharmaceutical composition according to claim 1, wherein said lipophilic substance comprises from about 1% to about 3.4% by weight of the total weight of the controlled release oral pharmaceutical composition. 18. The controlled release oral pharmaceutical composition of claim 1, wherein said hydrophilic substance comprises from about 8.4% to about 23% by weight of the total weight of the controlled release oral pharmaceutical composition. 19. The controlled release oral pharmaceutical composition of claim 1, wherein said rifamycin SV is in the form of a sodium salt. 20. The controlled release oral pharmaceutical composition of claim 19, wherein said sodium salt of rifamycin SV comprises from about 20% to about 60% by weight of the total weight of said controlled release oral pharmaceutical composition. 21. The controlled release oral pharmaceutical composition of claim 13, wherein said amphiphilic substance comprises at least one of a phospholipid, a ceramide, a sphingomyelin, lecithin, an alkyl block copolymer, a salt of a sulphated alkyl acid, a polyoxyethylenealkyl, or sorbitan. 22. The controlled release oral pharmaceutical composition of claim 21, wherein said amphiphilic substance is lecithin. 23. The controlled release oral pharmaceutical composition of claim 13, wherein said lipophilic substance comprises at least one of beeswax, carnuba wax, stearic acid, or stearin. 24. The controlled release oral pharmaceutical composition of claim 21, wherein said lipophilic substance comprises at least one of beeswax, carnuba wax, stearic acid, or stearin. 25. The controlled release oral pharmaceutical composition of claim 22, wherein said lipophilic substance comprises at least one of beeswax, carnuba wax, stearic acid, or stearin. 26. The controlled release oral pharmaceutical composition of claim 24, wherein said gastro-resistant substance comprises at least one methacrylic acid polymer. 27. The controlled release oral pharmaceutical composition of claim 25, wherein said gastro-resistant substance comprises at least one methacrylic acid polymer.