Sustained release pharmaceutical compositions comprising an antibacterial agent
The present invention relates to carrier systems useful for pharmaceutical compositions. These carriers comprise an emulsifier, and also in further embodiments a polymeric dissolution aid. These carriers are useful for delivering pharmaceutical actives such as antimicrobial agents.
1. A pharmaceutical composition comprising an antimicrobial agent, a pharmaceutical carrier, an emulsifier, and a polymeric dissolution aid, wherein said antimicrobial agent is
(S)—N-((3-(4′-((((1H-1,2,3-triazol-5-yl)methyl)amino)methyl)-2-fluoro-[1,1′-biphenyl]-4-yl)-2-oxooxazolidin-5-yl)methyl)acetamide,
or a pharmaceutically acceptable salt or tautomer thereof.
2. The pharmaceutical composition according to claim 1 wherein said emulsifier is a polyglycolized glyceride.
3. The pharmaceutical composition according to claim 2 wherein said emulsifier is selected from the group consisting of Labrafil, Labrosol, and Gelucire.
4. The pharmaceutical composition according to claim 3 wherein said emulsifier is selected from the group consisting of Gelucire 50/13, Gelucire 44/14, and mixtures thereof.
5. The pharmaceutical composition according to claim 1 wherein said polymeric dissolution aid is selected from the group consisting of polymers of 1-ethenyl-2-pyrrolidinone; polyamine N-oxide polymers; copolymers of N-vinylpyrrolidone and N-vinylimidazole; polyvinyloxazolidones and polyvinylimidazoles or mixtures thereof.
6. The pharmaceutical composition according to claim 5 wherein said polymeric dissolution aid is a polymer of 1-ethenyl-2-pyrrolidinone.
7. The pharmaceutical composition according to claim 5 wherein said polymeric dissolution aid is polyvinylpyrrolidone.
8. The pharmaceutical composition according to claim 1 further comprising a binder, filler, dispersant or wetting agent, disintegrant, or lubricant.
9. The pharmaceutical composition according to claim 1 further comprising one or more components selected from the group consisting of water, a nonaqueous solvent, a coating, a capsule shell, a colorant, a flavoring, a preservative, an antioxidant, a flavor enhancer, a compression aid, and a surfactant.
10. The pharmaceutical composition according to claim 1 in the form of a tablet.
11. The pharmaceutical composition according to claim 1 in the form of a capsule.
12. A method of treating or reducing the risk of a microbial infection in a patient comprising administering a pharmaceutically effective amount of a pharmaceutical composition according to claim 1 .
13. The method of claim 12 wherein the patient is a mammal or a domestic animal.
14. The method according to claim 12 wherein the composition, compared to a control composition, provides at least a 5% improvement in dissolution in a two step dissolution testing system.
15. The method according to claim 14 wherein the two step dissolution system comprises measuring the dissolution in a first step in a simulated gastric environment of about pH 4 for up to 30 minutes followed by measuring the dissolution in a second step in a simulated gastric environment of about pH 5.4 to about 6.5 for up to about 60 minutes.