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Last Updated: March 28, 2024

Claims for Patent: 8,741,948


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Summary for Patent: 8,741,948
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:13/592,088
Patent Claims: 1. A controlled release oral pharmaceutical composition comprising: (1) a tablet core comprising a homogeneous structure comprising (a) rifamycin SV, (b) a hydrophilic substance, (c) a lipophilic substance, and (d) an amphiphilic substance; and (2) a coating on said tablet core, said coating comprising a gastro-resistant substance, wherein said controlled release oral pharmaceutical composition comprises from about 10% to about 90% by weight of rifamycin SV, and wherein said controlled release oral pharmaceutical composition provides an in vitro release rate of said rifamycin SV in a buffer at pH 7.2 such that less than about 20% of said rifamycin SV is released after about 1 hour and more than about 70% of said rifamycin SV is released after about 8 hours.

2. A controlled release oral pharmaceutical composition according to claim 1, wherein said controlled release oral pharmaceutical composition provides an in vitro release rate of said rifamycin SV in a buffer at pH 7.2 such that less than about 50% of said rifamycin SV is released after about 3 hours.

3. A controlled release oral pharmaceutical composition according to claim 1, wherein said controlled release oral pharmaceutical composition is resistant to dissolution in an acidic environment.

4. A controlled release oral pharmaceutical composition according to claim 1, wherein said controlled release oral pharmaceutical composition is resistant to dissolution for 2 hours in an environment at pH 1.

5. A controlled release oral pharmaceutical composition according to claim 1, wherein said controlled release oral pharmaceutical composition is resistant to dissolution for 1 hour in an environment at pH 6.4.

6. A controlled release oral pharmaceutical composition according to claim 1, wherein said controlled release oral pharmaceutical composition comprises from about 20% to about 60% by weight of rifamycin SV.

7. A controlled release oral pharmaceutical composition according to claim 1, wherein said rifamycin SV is in the form of a sodium salt.

8. A controlled release oral pharmaceutical composition according to claim 1, wherein said lipophilic substance is a lipophilic substance having a melting point less than about 90.degree. C.

9. A controlled release oral pharmaceutical composition according to claim 1, wherein said amphiphilic substance comprises lecithin.

10. A controlled release oral pharmaceutical composition according to claim 1, wherein said hydrophilic substance is chosen from at least one of carboxyvinyl polymers, carboxyvinyl copolymers, hydroxyalkyl celluloses, alkyl celluloses, carboxyalkyl celluloses, polysaccharides, pectins, hyaluronic acid, glucuronic acid and glucosamines.

11. A controlled release oral pharmaceutical composition according to claim 10, wherein said hydrophilic substance is chosen from at least one of carboxyvinyl polymers and carboxyvinyl copolymers.

12. A controlled release oral pharmaceutical composition according to claim 1, wherein said gastro-resistant substance comprises at least one methacrylic acid polymer.

13. A method of treating an infection of the large intestine comprising administering to a patient in need thereof a therapeutically effective amount of a controlled release oral pharmaceutical composition comprising: (1) a tablet core comprising a homogeneous structure comprising (a) rifamycin SV, (b) a hydrophilic substance, (c) a lipophilic substance, and (d) an amphiphilic substance; and (2) a coating on said tablet core, said coating comprising a gastro-resistant substance, wherein said controlled release oral pharmaceutical composition comprises from about 10% to about 90% by weight of rifamycin SV, and wherein said controlled release oral pharmaceutical composition provides an in vitro release rate of said rifamycin SV in a buffer at pH 7.2 such that less than about 20% of said rifamycin SV is released after about 1 hour and more than about 70% of said rifamycin SV is released after about 8 hours.

14. A method of treating an infection of the large intestine according to claim 13, wherein said controlled release oral pharmaceutical composition provides an in vitro release rate of said rifamycin SV in a buffer at pH 7.2 such that less than about 50% of said rifamycin SV is released after about 3 hours.

15. A method of treating an infection of the large intestine according to claim 13, wherein said controlled release oral pharmaceutical composition is resistant to dissolution in an acidic environment.

16. A method of treating an infection of the large intestine according to claim 13, wherein said controlled release oral pharmaceutical composition is resistant to dissolution for 2 hours in an environment at pH 1.

17. A method of treating an infection of the large intestine according to claim 13, wherein said controlled release oral pharmaceutical composition is resistant to dissolution for 1 hour in an environment at pH 6.4.

18. A method of treating an infection of the large intestine according to claim 13, wherein said controlled release oral pharmaceutical composition comprises from about 20% to about 60% by weight of rifamycin SV.

19. A method of treating an infection of the large intestine according to claim 13, wherein said rifamycin SV is in the form of a sodium salt.

20. A method of treating an infection of the large intestine according to claim 13, wherein said lipophilic substance is a lipophilic substance having a melting point less than about 90.degree. C.

21. A method of treating an infection of the large intestine according to claim 13, wherein said amphiphilic substance comprises lecithin.

22. A method of treating an infection of the large intestine according to claim 13, wherein said hydrophilic substance is chosen from at least one of carboxyvinyl polymers, carboxyvinyl copolymers, hydroxyalkyl celluloses, alkyl celluloses, carboxyalkyl celluloses, polysaccharides, pectins, hyaluronic acid, glucuronic acid and glucosamines.

23. A method of treating an infection of the large intestine according to claim 21, wherein said hydrophilic substance is chosen from at least one of carboxyvinyl polymers and carboxyvinyl copolymers.

24. A method of treating an infection of the large intestine according to claim 13, wherein said gastro-resistant substance comprises at least one methacrylic acid polymer.

25. A method of treating an infection of the large intestine according to claim 13, wherein the infection of the large intestine is infectious colitis, bacillary dysentery, pseudomembranous colitis, traveller's diarhoea, diverticular disease or diverticulitis.

26. A method of treating an infection of the large intestine according to claim 13, wherein the infection of the large intestine is traveller's diarhoea.

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