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US 8,785,497 B2Granted
Aqueous ophthalmic compositions containing anionic therapeutic agents
AssigneeAlcon Research, Ltd.
InventorBhagwati P. Kabra
Life of this patent
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Abstract
The present invention is directed to the provision of multi-dose, ophthalmic compositions. The compositions possess sufficient antimicrobial activity to satisfy USP preservative efficacy requirements, as well as similar preservative standards (e.g., EP and JP). The compositions include a balance of ingredients that allow for the formation of ophthalmic compositions that include an anionic drug and exhibit desired characteristics such as stability, preservation efficacy, desired pH, desired osmolality, combinations thereof or the like.
Claims24
An aqueous ophthalmic composition, comprising:
- an anionic therapeutic agent;
- mannitol at a concentration that is at least 0.05 w/v % but is no greater than 1.5 w/v %;
- borate at a concentration that is at least 0.1 w/v % but is no greater than 0.5 w/v %;
- sodium chloride a concentration that is at least 85 mmol wherein the sodium chloride enhances the physical stability or clarity of the composition;
- a positively charged antimicrobial agent that is a polymeric quaternary ammonium compound;
- and
- water, wherein the osmolality of the ophthalmic composition is in the range of 240 to 360 mOsm/kg and wherein the composition is an aqueous solution having a turbidity of less than 2 NTU.
4 more elements
An aqueous ophthalmic composition, comprising:
- an anionic therapeutic agent wherein the concentration of the therapeutic agent is at least 0.01 w/v % and no greater than 0.5 w/v %;
- mannitol at a concentration that is at least 0.05 w/v % but is no greater than 1.5 w/v %;
- borate at a concentration that is at least 0.1 w/v % but is no greater than 0.5 w/v %;
- a positively charged antimicrobial agent that is a polymeric quaternary compound wherein the positively charged antimicrobial agent is present in the composition in a concentration that is at least 0.0001 w/v % but is no greater than 0.0012 w/v %;
- osmolality enhancing agent wherein the osmolality enhancing agent raises the osmolality of the ophthalmic composition at least 160 mOsm/Kg relative to a control composition that includes the exact same ingredients as the ophthalmic composition with the exception that the osmolality enhancing agent is replaced with water and pH is brought to the same value as that of the ophthalmic composition by using sodium hydroxide or hydrogen chloride if necessary and wherein the osmolality enhancing agent is present in the composition at a concentration that is at least 110 mmol but no greater than no greater than 200 mmol and wherein the osmolality enhancing agent also enhances the physical stability or clarity of the composition;
- and
- water;
- wherein the osmolality of the ophthalmic composition is in the range of 240 to 360 mOsm/kg and wherein the composition is substantially free of any benzalkonium chloride and wherein the osmolality enhancing agent is sodium chloride and wherein the composition is an aqueous solution having a turbidity of less than 2 NTU.
5 more elements
An aqueous ophthalmic composition, comprising:
- an anionic therapeutic agent wherein the concentration of the therapeutic agent is at least 0.01 w/v % and no greater than 0.5 w/v %;
- mannitol at a concentration that is at least 0.05 w/v % but is no greater than 1.5 w/v %;
- borate at a concentration that is at least 0.1 w/v % but is no greater than 0.5 w/v %;
- a positively charged antimicrobial agent that is a polymeric quaternary ammonium compound wherein the positively charged antimicrobial agent is present in the composition in a concentration that is at least 0.0001 w/v % but is no greater than 0.0012 w/v %;
- osmolality enhancing agent that is entirely or substantially entirely sodium chloride wherein the osmolality enhancing agent is present in the composition at a concentration that is at least 110 mmol but no greater than no greater than 200 mmol and wherein the osmolality enhancing agent also enhances the physical stability or clarity of the composition;
- and
- water;
- wherein the osmolality of the ophthalmic composition is in the range of 240 to 360 mOsm/kg and wherein the composition is substantially free of any benzalkonium chloride and wherein the osmolality enhancing agent is sodium chloride and wherein the composition is an aqueous solution having a turbidity of less than 2 NTU.
5 more elements
Dependencies are inferred from the claim text.