JPH01224321A - Ophthalmic preparation - Google Patents

Abstract

PURPOSE:To provide a clear ophthalmic preparation having improved instillation touch and safety, by adding a nonionic surfactant and glycyrrhizic acid to a system containing chondroitin sulfuric acid sodium salt and a quaternary ammonium cationic surfactant. CONSTITUTION:A nonionic surfactant and glycyrrhizic acid or a salt thereof are added to a system containing chondroitin sulfuric acid salt and a quaternary ammonium cationic surfactant to provide an ophthalmic preparation. The glycyrrhizic acid or the salt thereof is added in an amount of 0.01-0.30wt.%, preferably 0.02-0.15wt.%, based on the whole amount of the ophthalmic preparation. The nonionic surfactant (e.g., polyoxyethylene sorbitan fatty acid esters such as polysorbate 80 or polyoxyethylene hardened castor oil) used as a dissolution auxiliary is preferably added in an amount of 0.02-0.10wt.%.

Description

Detailed Description of the Invention [Industrial Field of Application] The present invention relates to eye drops containing sodium chondroitin sulfate, and more specifically, to a system in which sodium chondroitin sulfate is blended with a quaternary ammonium cationic surfactant. This invention relates to an eye drop that eliminates the clouding that occurs.

[Prior art] In the past, sodium chondroitin sulfate has been frequently used in eye drops as a medicinal ingredient that has corneal protective effects, tissue repair effects, viscosity (moisturizing) effects, etc., and quaternary ammonium such as benzalkonium chloride Cationic surfactants are widely used as effective preservatives. However, when these two components coexist, a cloudy phenomenon occurs.

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

[Problems to be Solved by the Invention] However, in recent years, there has been a tendency to incorporate cooling agents such as menthol, borneol, or camphor in order to improve and improve the feeling of eye drops. When these cooling agents are blended into the above-mentioned two-component system, the clouding phenomenon becomes more pronounced, so a larger amount of the solubilizing agent must be blended.

However, although nonionic surfactants used as solubilizing agents generally have excellent solubilizing ability,
If used continuously, there are concerns about side effects such as hemolysis and mucosal irritation. Furthermore, it has the disadvantage of reducing the antibacterial activity of the quaternary ammonium cationic surfactant, which is a preservative, or making it inactive. Therefore, there has been a desire for eye drops that contain as little nonionic surfactant as possible.

[Means for Solving the Problems] The present inventors have developed a reaction system between the cloudy phenomenon produced by sodium chondroitin sulfate and a quaternary ammonium cationic surfactant, and a nonionic surfactant that clarifies it. After paying attention to this and conducting extensive studies, we discovered that the solubilizing effect of glycyrrhizic acid or its salts increases synergistically by adding glycyrrhizic acid or its salts, and completed the present invention.

That is, the present invention involves 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. This eye drop is characterized by:

The present invention will be explained in detail below.

The amount of glycyrrhizic acid or its salts used in the present invention is 0.01 to 0.30% by weight, preferably 0.02 to 0.15% by weight, based on the total amount of the eye dropper.

The amount of nonionic surfactant used as a solubilizing agent is 0.02 to 0.10% by weight, which is 18% by weight.

~18%.

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

Examples of the quaternary ammonium cationic surfactant include benzalkonium chloride, benzethonium chloride, cetylpyridinium chloride, and the like.

Examples of glycyrrhizic acid or its salts include glycyrrhizic acid, dipotassium glycyrrhizinate, disodium glycyrrhizinate, and monoammonium glycyrrhizinate.

In the eye drops of the present invention, the pH is preferably 5.8 or less in view of the stability of the contents.

In the present invention, in addition to the above-mentioned essential ingredients, various ingredients commonly used in the preparation of eye drops can be blended in the amounts normally used.

For example, the active ingredients include sulfa drugs, diphenhydramine hydrochloride, aspartate, aminoethyl sulfonic acid, lysozyme chloride, epsilon aminocaproic acid, lorpeniramine maleate, neostigmine methyl sulfate, and various vitamins (such as active vitamin B, [flavin adenine dinucleotide]). Sodium, vitamin B, [
pyridoxine hydrochloride], vitamin B1. [Dianocobalamin], vitamin A acetate [retinol acetate], vitamin E acetate [tofferol acetate, etc.] can be blended.

In addition, if necessary, cooling agents (e.g. menthol, borneol, camphor, peppermint oil, etc.), isotonic agents (e.g. sodium chloride, potassium chloride, etc.), polymer additives (e.g. polyhydric alcohol, polyvinyl alcohol, polyvinyl alcohol, etc.), pyrrolidone, hydroxyethylcellulose, hydroxypropylmethylcellulose, etc.), stabilizers (e.g. ethylenediaminetetraacetate, etc.), buffers (e.g. boric acid,
borax etc.) etc. can be blended.

Glycyrrhizic acid or its salt used in the present invention originally has an anti-inflammatory effect, is an ingredient listed in the Ministry of Health and Welfare's ophthalmological drug approval standards, and has almost no side effects even when used repeatedly.
It is known as a highly safe ingredient.

[Effects of the Invention] According to the present invention, the amount of nonionic surfactant added can be reduced to 18% from the conventional amount. It became possible to reduce the amount to 18 to 18, and it became possible to provide clear eye drops with improved safety and improved eye feel.

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

(Example 1) Eye drops were prepared according to the following formulation.

[Ingredient name] [Blend amount mg/100mJ!
] Chlorpheniramine maleate 20 Sodium chondroitin sulfate 100 Pyridoxine hydrochloride
100 benzalkonium chloride
15 Polysorbate 8050 Boric acid 800 Borax
50 sodium chloride
50 Glycyrrhizic acid 2
0 Sterile purified water total 10011! ! (Example 2) [Amount of ingredients] [Blend amount mg 7100ml!
] Neostigmine methyl sulfate 2 Sodium chondroitin sulfate 100 Benzethonium chloride 20 Polysorbate 80
100 boric acid 10
00 Borax 40 Menthol 30 Borneol
5 Dipotassium glycyrrhizinate
150 Sterilized purified water Total 100 mg (Example 3) [Amount of ingredients [Blend amount mg/100rnl] Dianocobalamin 10 Sodium chondroitin sulfate 100 Cetylpyridinium chloride
5 polysorbate 8020 boric acid ioo.

Claims (1)

[Claims] (1) Eye drops 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. agent.