Cyclosporine-containing non-irritative nanoemulsion ophthalmic composition

• US 9,320,801 B2
• Filed: 01/22/2013
• Issued: 04/26/2016
• Est. Priority Date: 04/30/2012
• Status: Active Grant

• Current Assignee: Huons Co., Ltd.
• Original Assignee: Huons Co., Ltd.
• Inventors: Wang, Sung Joon, Cha, Kwang Ho, Kang, Han, Sun, Bo Kyung
• Primary Examiner(s): Ha, Julie
• Assistant Examiner(s): KOMATSU, LI N
• Application Number:
  US14/398,012
• Publication Number:
  US 20150125494A1
• Time in Patent Office: 1,190 Days
• US Class Current: 1/1
• 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 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• 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

Abstract

Provided is an ophthalmic composition containing cyclosporine as an active ingredient and including polyethoxylated castor oil or polyethoxylated hydrogenated castor oil, and a method of preparing the same. Particularly, the ophthalmic composition is prepared as a nanoemulsion having a particle diameter of 100 nm or less simply by mixing and stirring an oil phase and an aqueous phase without using a high speed stirring or shearing machine, so that it is very physiochemically stable and storable for a long time. In addition, the ophthalmic composition causes no irritation to eyes.

Claims

1. A nanoemulsion ophthalmic composition, comprising:

0.01 to 1 wt % of cyclosporine;

0.5 to 9.79 wt % of polyethoxylated castor oil or polyethoxylated hydrogenated castor oil; and

90 to 99.29 wt % of phosphate buffer, wherein the composition does not contain any other type of oil or emulsifier.

2. The composition according to claim 1, wherein the nanoemulsion has an average particle size of 100 nm or less.

3. The composition according to claim 2, wherein the nanoemulsion has an average particle size of 50 nm or less.

4. The composition according to claim 1, wherein the cyclosporine is cyclosporine A.

5. The composition according to claim 1, further comprising a thickening agent.

6. The composition according to claim 5, wherein the thickening agent is at least one selected from the group consisting of hyaluronic acid or a salt thereof, chitosan, hydroxypropylmethylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, polyvinyl pyrrolidone, carboxymethylcellulose, a carbomer, glycerin, and polyethyleneoxide.

7. The composition according to claim 6, wherein the thickening agent is hyaluronic acid or a salt thereof.

8. The composition according to claim 5, wherein the thickening agent is included at 0.1 to 5 wt % of the entire ophthalmic composition.

9. The composition according to claim 1, further comprising ethanol.

10. The composition according to claim 9, wherein the ethanol is included at 0.1 to 3 wt % of the entire ophthalmic composition.