TOPICAL FORMULATIONS AND USES THEREOF

• US 20140057854A1
• Filed: 08/23/2013
• Published: 02/27/2014
• Est. Priority Date: 08/24/2012
• Status: Active Grant

• Current Assignee: Sun Pharmaceutical Industries Limited
• Original Assignee: Ocular Technologies SARL (Sun Pharmaceutical Industries Limited)
• Inventors: Mitra, Ashim K., Weiss, Sidney L.
• Granted Patent: US 8,980,839 B2
• Time in Patent Office: Days
• US Class Current: 514/20.5
• CPC Class Codes: A61K 31/202 having three or more double bonds, e.g. linolenic eicosanoids, e.g. leukotrienes A61K31/557
• CPC Class Codes: A61K 38/13 Cyclosporins
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided herein include formulations for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and or a polyalkoxylated alcohol and may include nanomicelles. Also include methods of treating or preventing diseases or conditions, such as ocular diseases or conditions.

Claims

1. An ophthalmic formulation, comprising cyclosporine, a polyoxyl lipid or fatty acid and a polyalkoxylated alcohol.

2. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40, HCO-60, HCO-80, HCO-100, polyoxyl 40 stearate and polyoxyl 35 castor oil.

3. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40, HCO-60 and HCO-80.

4. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises HCO-40.

5. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-60, HCO-80, HCO-100, polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.05-5% of the formulation.

6. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40, HCO-60, HCO-80, HCO-100, polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.5-1.5% of the formulation.

7. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40 HCO-60, and HCO-80, and is present in an amount between 0.5-1.5% of the formulation.

8. The ophthalmic formulation of claim 1, wherein said polyalkoxylated alcohol is Octoxynol-40.

9. The ophthalmic formulation of claim 1, wherein the polyalkoxylated alcohol is Octoxynol-40 and is present in an amount between 0.02 and 4% of the formulation.

10. The ophthalmic formulation of claim 1, wherein the polyalkoxylated alcohol is Octoxynol-40 and is present in an amount between 0.02 and 0.1% of the formulation.

11. The ophthalmic formulation of claim 1, wherein the cyclosporine is present in an amount between 0.05 and 5% of the formulation.

12. The ophthalmic formulation of claim 1, wherein the cyclosporine is present in an amount between 0.05 and 0.2% of the formulation.

13. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40, HCO-60, HCO-80, HCO-100, polyoxyl 40 stearate and polyoxyl 35 castor oil;

and wherein said polyalkoxylated alcohol is Octoxynol-40.

14. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40, HCO-60, HCO-80, HCO-100, polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.5-5% of the formulation;

and said polyalkoxylated alcohol is Octoxynol-40 and is present in an amount between 0.02 and 4% of the formulation.

15. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40, HCO-60, HCO-80, HCO-100, polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.5-1.5% of the formulation;

and said polyalkoxylated alcohol is Octoxynol-40 and is present in an amount between 0.02 and 0.1% of the formulation.

16. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40, HCO-60, HCO-80, HCO-100, polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.5-5% of the formulation;

said polyalkoxylated alcohol is Octoxynol-40 and is present in an amount between 0.02 and 4% of the formulation; and

the cyclosporine is present in an amount between 0.05 and 5% of the formulation.

17. The ophthalmic formulation of claim 1, wherein said polyoxyl lipid comprises one or more selected from the group consisting of HCO-40, HCO-60, HCO-80, HCO-100, polyoxyl 40 stearate and polyoxyl 35 castor oil and is present in an amount between 0.5-1.5% of the formulation;

and said polyalkoxylated alcohol is Octoxynol-40 and is present in an amount between 0.02 and 0.1% of the formulation; and

the cyclosporine is present in an amount between 0.05 and 0.2% of the formulation.

18. The ophthalmic formulation of claim 1, wherein said formulation comprises nanomicelles.

19. A method of treating or preventing an ocular disease or condition, said method comprising topically administering a formulation of claim 1.

20. A method of treating or preventing an ocular disease or condition, said method comprising topically administering a formulation of claim 17.