JP2671353B2 - Eye drops - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION [Field of Industrial Application] The present invention relates to an eye drop containing sodium chondroitin sulfate, and more specifically to a system in which a quaternary ammonium cationic surfactant is mixed with sodium chondroitin sulfate. The present invention relates to an eye drop that has eliminated the cloudiness that occurs.

[Prior Art] Conventionally, sodium chondroitin sulfate has been widely used in eye drops as a medicinal component having a corneal protective action, a tissue repair action, a viscous (moisturizing) action, and the like, and quaternary ammonium such as benzalkonium chloride. The cationic cationic surfactant is often used as an effective preservative. But,
When these two components coexist, a clouding phenomenon occurs.

Generally, when such white turbidity occurs, a solubilizing agent such as a nonionic surfactant (for example, polyoxyethylene sorbitan fatty acid ester) is added to eliminate the white turbidity.

[Problems to be Solved by the Invention] However, in recent years, there has been a tendency to blend a cooling agent such as menthol, borneol, or camphor for the reason of improvement in eye drop feeling. When these cooling agents are added to the above-mentioned two-component system, the clouding phenomenon becomes more prominent, so a larger amount of solubilizing agent must be added.

However, a nonionic surfactant used as a solubilizing agent is generally a substance having excellent solubilizing ability, but when it is continuously used, side effects such as hemolytic action and mucous membrane stimulating action are feared. Furthermore, there is a problem that the antibacterial activity of the quaternary ammonium cationic surfactant which is a preservative is lowered or inactivated. Therefore, there has been a demand for eye drops in which the amount of the nonionic surfactant blended is kept as small as possible.

[Means for Solving the Problems] The present inventors have found that sodium chondroitin sulfate and the fourth
Focusing on the white turbidity phenomenon generated by a quaternary ammonium-type cationic surfactant and the reaction system with a nonionic surfactant that clarifies this, as a result of intensive studies, by adding glycyrrhizic acid or its salts, They have found that their solubilizing action increases synergistically and completed the present invention.

That is, the present invention is characterized by adding a nonionic surfactant and glycyrrhizic acid or a nonionic surfactant and glycyrrhizinate to a system containing sodium chondroitin sulfate and a quaternary ammonium cationic surfactant. And eye drops.

 Hereinafter, the present invention will be described in detail.

Glycyrrhizic acid or a salt thereof used in the present invention is added in an amount of 0.01 to 0.30% by weight, preferably 0.02 to 0.15% by weight, based on the total length of the eye drop.

The addition amount of the nonionic surfactant used as a solubilizing agent is 0.02 to 0.10% by weight, which is 1/10 to 1/2 of the conventional amount.

Examples of the type of the nonionic surfactant include polyoxyethylene sorbitan fatty acid esters such as polysorbate 80, and polyoxyethylene hydrogenated castor oil.

As the quaternary ammonium cationic surfactant,
Besides benzalkonium chloride, benzethonium chloride, cetylpyridinium chloride and the like can be mentioned.

Examples of glycyrrhizinic acid or salts thereof include glycyrrhizinic acid, dipotassium glycyrrhizinate, disodium glycyrrhizinate, monoammonium glycyrrhizinate, and the like.

In the eye drop of the present invention, the pH of the eye drop is from the stability of the content components.
5.8 or less is desirable.

In the present invention, in addition to the above-mentioned essential components, various components usually used for the preparation of eye drops can be added in the amounts usually used.

For example, as an active ingredient, sulfa drug, diphenhydramine hydrochloride, aspartate, aminoethyl sulfonic acid,
Lysozyme chloride, epsilon aminocaproic acid, chlorpheniramine maleate, neostigmine methylsulfate,
Various vitamins (eg active vitamin B ₂ [flavin adenine dinucleotide sodium], vitamin B ₆ [pyridoxine hydrochloride], vitamin B ₁₂ [cyanocobalamin], vitamin A acetate [retinol acetate], vitamin E acetate [tocopherol acetate] ] Etc.) can be blended.

If necessary, a cooling agent (eg menthol, borneol, camphor, peppermint oil etc.), an isotonicity agent (eg sodium chloride, potassium chloride etc.), a polymer additive (eg polyhydric alcohol, polyvinyl alcohol, polyvinyl) Pyrrolidone, hydroxyethylcellulose, hydroxypropylmethylcellulose, etc.), stabilizers (eg ethylenediaminetetraacetate etc.), buffers (eg boric acid, borax etc.) and the like can be added.

Glycyrrhizic acid or a salt thereof used in the present invention,
Originally, it is an ingredient that has an anti-inflammatory effect and is also described in the Ministry of Health, Labor and Welfare ophthalmological drug approval standard and has almost no side effects even after continuous application, and is known as a highly safe ingredient.

[Advantages of the Invention] According to the present invention, the addition amount of the nonionic surfactant is reduced to 1/10 of the conventional one.
It has become possible to provide a clear eye drop with improved safety and improved eye drop feeling.

[Examples] Examples of the present invention will be shown below, but the present invention is not limited thereto.

(Example 1) An eye drop was prepared according to the following formulation.

 [Ingredient name] [Mixing amount mg / 100ml] Chlorpheniramine maleate 20 Sodium chondroitin sulfate 100 Pyridoxine hydrochloride 100 Benzalkonium chloride 15 Polysorbate 80 50 Boric acid 800 Borax 50 Sodium chloride 50 Glycyrrhizic acid 20 Sterilized purified water 100 ml total (Example 2) [Ingredient name] [Blending amount mg / 100 ml] Neostigmine methylsulfate 2 Sodium chondroitin sulfate 100 Benzethonium chloride 20 Polysorbate 80 100 Boric acid 1000 Borax 40 Menthol 30 Borneol 5 Dipotassium glycyrrhizinate 150 Sterile purified water All 100 ml (Example 3) [Ingredient name] [Mixing amount mg / 100 ml] Cyanocobalamin 10 Sodium chondroitin sulfate 100 Cetylpyridinium chloride 5 Polysorbate 80 20 Boric acid 1000 Borax 90 Dipotassium glycyrrhizinate 50 Sterilized purified water Total 100 ml

Claims (1)

(57) [Claims] 1. A nonionic surfactant and glycyrrhizic acid or a nonionic surfactant and glycyrrhizinate are added to a system containing sodium chondroitin sulfate and a quaternary ammonium cationic surfactant. Eye drops to do.