Two-layer separation-type eye drop containing squalane

• US 9,907,750 B2
• Filed: 03/18/2014
• Issued: 03/06/2018
• Est. Priority Date: 03/19/2013
• Status: Active Grant

• Current Assignee: Senju Pharmaceutical Company Limited
• Original Assignee: Senju Pharmaceutical Company Limited
• Inventors: Sawa, Shirou
• Primary Examiner(s): Jiang, Shaojia A
• Assistant Examiner(s): Miller, Dale R
• Application Number:
  US14/778,359
• Publication Number:
  US 20160067181A1
• Time in Patent Office: 1,449 Days
• Field of Search: None
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/01 Hydrocarbons
• CPC Class Codes: A61K 31/728 Hyaluronic acid
• 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 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The purpose of the present invention is to provide a technique for formulating a two-layer separation-type ophthalmic solution in which, during storage, an aqueous layer and an oil-containing layer containing squalane are separated from each other, wherein it is possible to homogeneously disperse the oil-containing layer in the aqueous layer while suppressing foaming by shaking the ophthalmic solution before administration, and the homogeneous dispersed state is maintained in a stable manner at least until administration. A two-layer separation-type ophthalmic solution containing squalane and water, wherein hyaluronic acid and/or a salt thereof and polyvinyl alcohol are contained in the ophthalmic solution and the polyvinyl alcohol content is set to 0.025 to 0.1 w/v %, whereby it is possible to homogeneously disperse the oil-containing layer in the aqueous layer while suppressing foaming by shaking the ophthalmic solution before administration, and to maintain the homogeneous dispersed state in a stable manner at least until administration.

Claims

1. A two-layer separation-type ophthalmic solution comprising an oil-containing layer and an aqueous layer, wherein

when statically stored, an upper layer consisting of the oil-containing layer and a lower layer consisting of the aqueous layer are formed, the oil-containing layer contains squalane,

the aqueous layer contains hyaluronic acid and/or its salt and polyvinyl alcohol, with 0.3 to 0.4 w/v % of hyaluronic acid and/or its salt and 0.025 to 0.1 w/v % of polyvinyl alcohol being present in the ophthalmic solution.

2. The two-layer separation-type ophthalmic solution according to claim 1, comprising 1 to 10 w/v % of squalane.

3. The two-layer separation-type ophthalmic solution according to claim 1 wherein the ophthalmic solution is for non-human mammals.

4. The two-layer separation-type ophthalmic solution according to claim 1, comprising 0.2 to 10 parts by weight of polyvinyl alcohol per 100 parts by weight of squalane.

5. The two-layer separation-type ophthalmic solution according to claim 1, wherein the ophthalmic solution is for treatment of dry eye.

6. The two-layer separation-type ophthalmic solution according to claim 1 wherein the ophthalmic solution is for protecting cornea.

7. A method of treating dry eye, comprising a step of administering the two-layer separation-type ophthalmic solution according to claim 1 to mammalian eyes suffering from dry eye.

8. A method of protecting the cornea, comprising a step of administering the two-layer separation-type ophthalmic solution according to claim 1 to mammalian eyes requiring corneal protection.