TOPICAL FORMULATIONS AND USES THEREOF

• US 20170065611A1
• Filed: 11/17/2016
• Published: 03/09/2017
• Est. Priority Date: 05/23/2014
• Status: Abandoned Application

• Current Assignee: Sun Pharma Global Fze (Sun Pharmaceutical Industries Limited)
• Original Assignee: Ocular Technologies SARL (Sun Pharmaceutical Industries Limited)
• Inventors: WEISS, Sidney L.
• Application Number:
  US15/354,568
• Publication Number:
  US 20170065611A1
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61K 31/498 Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
• CPC Class Codes: A61K 31/506 not condensed and containing further heterocyclic rings
• CPC Class Codes: A61K 31/542 ortho- or peri-condensed with heterocyclic ring systems
• CPC Class Codes: A61K 31/5575 having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
• 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 9/08 Solutions composition of solutions A61K47/00
• 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

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:

at least one active agent selected from the group consisting of brinzolamide, latanoprost, brimonidine, and bosentan,

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 wt % 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 wt % 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 wt % 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 wt % 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 wt % of the formulation.

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

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

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

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

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

the active agent is present in an amount between 0.05 and 5 wt % 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 wt % of the formulation;

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

the active agent is present in an amount between 0.05 and 0.2 wt % of the formulation.

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

19. The ophthalmic formulation of claim 1, wherein said active agent is brinzolamide.

20. The ophthalmic formulation of claim 1, wherein said active agent is bosentan.

21. The ophthalmic formulation of claim 1, wherein said active agent is latanoprost.

22. The ophthalmic formulation of claim 1, wherein said active agent is brimonidine.

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

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