TOPICAL FORMULATIONS AND USES THEREOF

• US 20150165048A1
• Filed: 02/24/2015
• Published: 06/18/2015
• Est. Priority Date: 08/24/2012
• Status: Abandoned Application

• Current Assignee: Sun Pharma Global Fze (Sun Pharmaceutical Industries Limited)
• Original Assignee: Ocular Technologies SARL (Sun Pharmaceutical Industries Limited)
• Inventors: MITRA, Ashim K., WEISS, Sidney L., MCNALLY, Eugene J.
• Application Number:
  US14/629,883
• Publication Number:
  US 20150165048A1
• Time in Patent Office: Days
• US Class Current: 1/1
• 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 an active agent, a polyoxyl lipid or fatty acid and a polyalkoxylated alcohol.

6. The ophthalmic formulation of any of the preceding claims, wherein said active agent is one or more selected from the group consisting of calcineurin inhibitors, mTOR inhibitors, peptides, eicosanoids (e.g. prostacyclins and prostaglandins), anti-inflammatory drugs (such as NSAIDS), autonomic drugs (e.g. beta-blockers, alpha-blockers, beta-agonists, and alpha-agonists), biologics, gene therapy agents (e.g. viral vectors), anti-infectives (e.g. antifungals, antibiotics, and antivirals), retinoids, RNAi, photo sensitizers, steroids (e.g., estrogens and derivatives thereof, and corticosteroids), mixture drugs, immuno-modulators, chemotherapeutic agents, G-coupled protein receptor antagonists, receptor tyrosine kinase (RTK) inhibitors, growth hormone inhibitors, integrin inhibitors, Sdf1/CXCR4 pathway inhibitors, and nACh receptor antagonists, resolvins (or resolvin-like compounds), lipoxins, and oxylipins.

7. The ophthalmic formulation of any of the preceding claims, wherein said active agent is a resolvin.

8. The ophthalmic formulation of any of the preceding claims, wherein said active agent is compound 1001.

9. The ophthalmic formulation of any of the preceding claims, wherein said active agent is one or more selected from the group consisting of cyclosporine A, voclosporin, ascomycin, tacrolimus, pimecrolimus, an analog thereof, or a pharmaceutically acceptable salt thereof.

10. The ophthalmic formulation of any of the preceding claims, wherein said active agent is cyclosporine A

11. A method of treating or preventing an ocular disease or condition, said method comprising topically administering a formulation of any of the preceding claims.

2. An ophthalmic formulation, comprising an active agent, and an ≧

40 polyoxyl lipid or fatty acid.

3. An ophthalmic formulation, comprising an active ingredient and a polyoxyl lipid or fatty acid;

wherein said polyoxyl lipid or fatty acid is present in an amount equal to greater than 1% of said formulation.

4. An ophthalmic formulation, comprising an active agent and a polyoxyl lipid or fatty acid;

wherein said formulation comprises nanomicelles.

5. An ophthalmic formulation, comprising an active agent, 0.05-5% of 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 about 0.01-0.1% octoxynol-40.

12. A method of manufacturing an ophthalmic formulation comprising liquefying/melting and mixing (a) a polyoxyl lipid or fatty acid, (b) a polyalkoxylated alcohol and (c) an active agent and subsequently adding a buffer and a saline.