Ophthalmic composition

Abstract

To provide an ophthalmic composition that enables enhancement of wettability.SOLUTION: An ophthalmic composition containing a component (1) and a component (2) and / or a component (3): (1) at least one selected from the group consisting of ectoine, a salt of ectoine, and derivatives thereof; (2) at least one selected from the group consisting of chondroitin sulfate ester and salts thereof; (3) at least one selected from the group consisting of hyaluronic acid and salts thereof; wherein, when the ophthalmic composition contains the component (3), the total content of the component (3) in the ophthalmic composition is 0.05 w / v% or less.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to an ophthalmic composition. [Background technology]

[0002] Various ophthalmic compositions have been developed to relieve eye discomfort. For example, when people experience eye discomfort, they often rub their eyes, but this behavior can cause eye injury. Furthermore, rubbing the eyes while wearing contact lenses increases the risk of eye injury compared to when not wearing contact lenses.

[0003] Ectoine is a known cyclic amino acid obtained from extremophilic microorganisms such as halophiles, and is known to have high water-retaining capacity (Patent Document 1). Patent Document 1 also reports that ectoine is useful for promoting collagen secretion and SEC12 protein expression. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Publication No. 2022-187867 Summary of the Invention [Problem to be solved by the invention]

[0005] The present inventors have focused on wettability in order to alleviate eye discomfort, and the present disclosure provides a new ophthalmic composition that can improve wettability. [Means for solving the problem]

[0006] The present inventor has conducted extensive research and found that when ectoine and chondroitin sulfate are used in combination, wettability can be improved.In addition, the present inventor has found that when ectoine and a specific amount of hyaluronic acid are used in combination, wettability can be improved.The present invention has been completed through further research based on this finding, and the present disclosure includes the following representative inventions. Item 1. An ophthalmic composition comprising the following component (1) and the following component (2) and / or (3): (1) at least one selected from the group consisting of ectoine, ectoine salts, and derivatives thereof; (2) at least one selected from the group consisting of chondroitin sulfate esters and salts thereof; (3) At least one member selected from the group consisting of hyaluronic acid and its salts, wherein when the ophthalmic composition contains component (3), the total content of component (3) in the ophthalmic composition is 0.05 w / v% or less. Item 2. The ophthalmic composition according to Item 1, wherein the total content of component (1) in the ophthalmic composition is 0.05 w / v % or less. Item 3. The ophthalmic composition according to Item 1 or 2, wherein the total content of component (2) in the ophthalmic composition is 0.5 w / v % or less. Item 4. The ophthalmic composition according to any one of Items 1 to 3, wherein the ophthalmic composition is an eyewash. Item 5. The ophthalmic composition according to Item 4, wherein the eyewash is a drop-type eyewash or a cup-type eyewash. Item 6. The ophthalmic composition according to any one of Items 1 to 5, which is an ophthalmic composition for contact lenses. Item 7. Use of a combination of the following component (1) and the following component (2) and / or (3) for the production of an ophthalmic composition: (1) at least one selected from the group consisting of ectoine, ectoine salts, and derivatives thereof; (2) at least one selected from the group consisting of chondroitin sulfate esters and salts thereof; (3) At least one selected from the group consisting of hyaluronic acid and its salts, wherein when component (3) is used, the total content of component (3) in the ophthalmic composition is 0.05 w / v% or less. [Effects of the Invention]

[0007] The ophthalmic composition of the present disclosure can improve wettability, which is useful for preventing or alleviating eye discomfort. [Brief explanation of the drawings]

[0008] [Figure 1] The contact angle θ is shown. [Figure 2] The results of Test Example 1 (Examples 1 to 3 and Comparative Examples 1 to 3 (Group IV)) are shown below. It is shown that when the test liquids of Examples 1 to 3 were used, the wettability was improved. [Figure 3] The results of Test Example 1 (Examples 1 to 3 and Comparative Examples 1 to 3 (Group I)) are shown below. It is shown that when the test liquids of Examples 1 to 3 were used, the wettability was improved. [Figure 4] The results of Test Example 2 (Examples 4 to 6 and Comparative Example 4 (Group IV)) are shown below, which show that when the test liquids of Examples 4 to 6 were used, the wettability was improved. [Figure 5] The results of Test Example 2 (Examples 4 to 6 and Comparative Example 4 (Group I)) are shown below. It is shown that when the test liquids of Examples 4 to 6 were used, the wettability was improved. [Figure 6] The results of Test Example 3 (Examples 7 to 9 (Group IV)) are shown below. It is shown that when the test liquids of Examples 7 to 9 were used, the wettability was improved. [Figure 7] The results of Test Example 3 (Examples 7 to 9 (Group I)) are shown below. It is shown that when the test liquids of Examples 7 to 9 were used, the wettability was improved. DETAILED DESCRIPTION OF THE INVENTION

[0009] Hereinafter, embodiments included in the present disclosure will be described in more detail. In the present disclosure, "comprise" also includes the meaning of "consist essentially of" or "consist of."

[0010] The present disclosure encompasses an ophthalmic composition containing the following component (1) and the following components (2) and / or (3). In the present disclosure, the ophthalmic composition may be referred to as the "ophthalmic composition of the present disclosure." (1) at least one selected from the group consisting of ectoine, ectoine salts, and derivatives thereof; (2) at least one selected from the group consisting of chondroitin sulfate esters and salts thereof; (3) At least one member selected from the group consisting of hyaluronic acid and its salts, wherein when the ophthalmic composition contains component (3), the total content of component (3) in the ophthalmic composition is 0.05 w / v% or less.

[0011] In component (1), ectoine is a cyclic amino acid (CAS number 96702-03-3) obtained from extremophilic microorganisms such as halophiles, and has the molecular formula CH 10 It is represented by N2O2. Examples of ectoine salts include, but are not limited to, alkali metal salts such as sodium salts and potassium salts. Examples of ectoine derivatives include, but are not limited to, homoectoine and hydroxyectoine. Preferred examples of component (1) include ectoine and hydroxyectoine (CAS number 165542-15-4), and more preferred examples include ectoine.

[0012] Component (1) is commercially available, for example, under the trade names RonaCare (registered trademark) Ection and RonaCare (registered trademark) Cyclopeptide-5 (both manufactured by Merck Ltd.), Ectoin natural (manufactured by Bitop AG), and Ectoine (BLOOMAGE BIOTECH (TIANJIN) CO., LTD). Ectoine, ectoine salts, and derivatives thereof may be used alone or in combination of two or more.

[0013] The content of component (1) in the ophthalmic composition of the present disclosure is not limited, but the total content of component (1) is preferably 2 w / v% or less. More preferred examples of the total content of component (1) include 0.001 w / v% to 1.5 w / v%, 0.003 w / v% to 1 w / v%, 0.005 w / v% to 0.5 w / v%, 0.005 w / v% to 0.1 w / v%, and 0.008 w / v% to 0.05 w / v%. Furthermore, even more preferred examples of the total content of component (1) include 0.01 w / v% to 0.04 w / v%, and 0.015 w / v% to 0.035 w / v%.

[0014] In component (2), chondroitin sulfate is a mucopolysaccharide having a structure in which sulfate is ester-bonded to a sugar chain in which disaccharides of D-glucuronic acid and N-acetylgalactosamine are repeated, and is conventionally known. Examples of salts of chondroitin sulfate include, but are not limited to, alkali metal salts such as sodium salt and potassium salt, and alkaline earth metal salts such as magnesium salt and calcium salt. Examples of salts of chondroitin sulfate include, but are not limited to, sodium chondroitin sulfate. Examples of component (2) include, but are not limited to, sodium chondroitin sulfate.

[0015] Although component (2) is not limited thereto, the molecular weight of the chondroitin sulfate ester is preferably, for example, a weight-average molecular weight of about 5,000 to 45,000, more preferably about 10,000 to 40,000, even more preferably about 15,000 to 30,000, and even more preferably about 20,000 to 30,000. The weight-average molecular weight is measured by gel filtration chromatography. Component (2) is commercially available, for example, under the trade name "Extraneous Standard Sodium Chondroitin Sulfate" (Seikagaku Corporation, weight-average molecular weight 20,000). Chondroitin sulfate esters and salts of chondroitin sulfate esters may be used alone or in combination of two or more.

[0016] The content of component (2) in the ophthalmic composition of the present disclosure is not limited as long as the effects of the present disclosure are obtained, but the total content of component (2) is preferably 0.5 w / v% or less, for example. When the composition contains component (2), the total content of component (2) is exemplified as more than 0 w / v% to 0.5 w / v%, more preferably 0.003 w / v% to 0.5 w / v%, even more preferably 0.005 w / v% to 0.3 w / v%, 0.01 w / v% to 0.1 w / v%, 0.05 w / v% to 0.5 w / v%, 0.005 w / v% to 0.05 w / v%, even more preferably 0.01 w / v% to 0.05 w / v%, 0.025 w / v% to 0.05 w / v%, etc.

[0017] When the ophthalmic composition of the present disclosure contains component (2), the content of component (2) is not limited as long as the effects of the present disclosure are obtained. When component (2) is contained, the total content of component (2) in the composition per part by mass of component (1) is preferably 0.01 to 5 parts by mass, more preferably 0.1 to 2.5 parts by mass, even more preferably 0.2 to 2 parts by mass, and particularly preferably 0.25 to 1 part by mass.

[0018] In component (3), hyaluronic acid is conventionally known. Examples of hyaluronic acid salts include alkali metal salts such as sodium salt and potassium salt, and alkaline earth metal salts such as magnesium salt and calcium salt. A preferred example of hyaluronic acid salt is the sodium salt of hyaluronic acid.

[0019] Although component (3) is not limited thereto, the molecular weight of hyaluronic acid or its salts is preferably a viscosity-average molecular weight of approximately 100,000 to 2,000,000, more preferably approximately 300,000 to 1,600,000, and even more preferably approximately 500,000 to 1,200,000. The viscosity-average molecular weight of hyaluronic acid or its salts is determined according to the method described in the "Average Molecular Weight" section of the "Purified Sodium Hyaluronate" section of the 17th Revised Japanese Pharmacopoeia Commentary (editor: Japanese Pharmacopoeia Commentary Editorial Committee, first published July 15, 2016). Component (3) is commercially available, for example, under the trade name Hyaluronic Acid LM (manufactured by NC Corporation), trade name Hyalopure (manufactured by Maruha Nichiro Foods Co., Ltd.), and trade name Hyabest (manufactured by Kewpie Corporation). Hyaluronic acid and hyaluronic acid salts may be used alone or in combination of two or more.

[0020] In the ophthalmic composition of the present disclosure, the total content of component (3) is 0.05 w / v% or less. When the composition contains component (3), the total content of component (3) is not limited as long as it is more than 0 w / v% and 0.05 w / v% or less, and examples of the total content of component (3) include more preferably 0.0003 w / v% or more and 0.05 w / v% or less, even more preferably 0.0005 w / v% or more and 0.02 w / v% or less, 0.0008 w / v% or more and 0.01 w / v% or less, and 0.001 w / v% or more and 0.005 w / v% or less.

[0021] When the ophthalmic composition of the present disclosure contains component (3), the content of component (3) is not limited as long as it is as described above. When component (3) is contained, the total content of component (3) in the composition per part by mass of component (1) is preferably from 0.001 to 0.1 parts by mass, more preferably from 0.005 to 0.05 parts by mass, even more preferably from 0.008 to 0.04 parts by mass, and particularly preferably from 0.008 to 0.02 parts by mass.

[0022] The ophthalmic composition of the present disclosure may further contain any other component acceptable for use in eye drops or eye washes. Examples of such other components include, but are not limited to, buffers, stabilizers, isotonicity agents, solvents (e.g., water), pH adjusters, preservatives, cooling agents, irritants, thickeners, and medicinal ingredients. The other components may be selected appropriately depending on the purpose, etc., as long as they do not interfere with the effects of the present disclosure. They may be used alone or in combination with two or more other components, and the amounts of the other components may be determined appropriately. The components (1) to (3) are also known as medicinal ingredients, etc., depending on the component, but in the present disclosure, the components (1) to (3) are not included in the optional other components.

[0023] Examples of such other components include preservatives, such as quaternary ammonium salt preservatives (benzalkonium chloride, benzethonium chloride, hexadecyltrimethylammonium bromide, etc.), parahydroxybenzoates (parahydroxybenzoates such as methyl parahydroxybenzoate and propyl parahydroxybenzoate, salts of parahydroxybenzoates (alkali metal salts such as sodium salts), etc.), chlorobutanol, and sorbic acids (sorbic acid, salts of sorbic acid (alkali metal salts such as potassium salts), etc.). One type of preservative may be used alone, or two or more types may be used in combination. The ophthalmic composition of the present disclosure can also be prepared without adding a preservative.

[0024] Examples of such other components include buffers, such as boric acid and borax. A single buffer may be used, or two or more buffers may be used in combination. When the ophthalmic composition of the present disclosure contains boric acid, the content of boric acid is not limited as long as it does not impair the effects of the present disclosure, and is preferably 0.1 w / v% to 2.5 w / v% in the composition, and more preferably 0.5 w / v% to 2 w / v% in the composition. When the composition contains borax, the content of borax is not limited as long as it does not impair the effects of the present disclosure, and is preferably 0.005 w / v% to 0.5 w / v% in the composition, and more preferably 0.005 w / v% to 0.05 w / v% in the composition. The composition may or may not contain a buffer other than boric acid or borax.

[0025] Examples of such other components include stabilizers, such as polysorbates (polysorbate 80, polysorbate 60, etc.), polyoxyethylene (POE) hydrogenated castor oil (POE(80) hydrogenated castor oil, POE(60) hydrogenated castor oil, etc.; the number in parentheses indicates the average number of moles of ethylene oxide added), POE polyoxypropylene glycol, and sodium edetate (including hydrate). A single stabilizer may be used, or two or more may be used in combination. When the composition contains a stabilizer, the content of the stabilizer is not limited as long as it does not impair the effects of the present disclosure. The content of the stabilizer in the composition is preferably 0.01 w / v% or more and 0.5 w / v% or less, and more preferably 0.05 w / v% or more and 0.5 w / v% or less.

[0026] Examples of such other components include medicinal components such as amino acids, anti-inflammatory agents (anti-phlogistic agents), antihistamines, vitamins, corneal surface protective agents, etc. The medicinal components may be used singly or in combination of two or more.

[0027] Although not limiting the present disclosure, examples of amino acids include amino acids and salts thereof, such as glutamic acid and its salts (e.g., monosodium glutamate); and amino acid analogs such as taurine. In the present disclosure, an amino acid refers to an amino acid that has both an amino group and a carboxyl group and can be a structural unit of a protein, and includes, for example, L-aspartic acid. The amino acids may be used alone or in combination of two or more.

[0028] Although not limiting the present disclosure, examples of anti-inflammatory agents include zinc sulfate, zinc lactate, epsilon-aminocaproic acid, allantoin, glycyrrhizic acid and its salts (dipotassium glycyrrhizinate, etc.), berberine chloride (berberine chloride hydrate, etc.), etc. Anti-inflammatory agents may be used singly or in combination of two or more.

[0029] When the ophthalmic composition of the present disclosure contains epsilon-aminocaproic acid, the content of epsilon-aminocaproic acid in the composition may be appropriately determined. The content of epsilon-aminocaproic acid in the composition is preferably 0.05 w / v% to 0.5 w / v%, more preferably 0.1 w / v% to 0.4 w / v%, and even more preferably 0.2 w / v% to 0.4 w / v%. Furthermore, without limiting the present disclosure, the content of epsilon-aminocaproic acid in the composition per part by mass of component (1) is preferably 1 part by mass to 20 parts by mass, more preferably 4 parts by mass to 15 parts by mass, and even more preferably 8 parts by mass to 12 parts by mass.

[0030] Although not limiting the present disclosure, examples of antihistamines include diphenhydramine and its salts (diphenhydramine hydrochloride, etc.), chlorpheniramine and its salts (chlorpheniramine maleate, etc.), etc. Antihistamines may be used singly or in combination of two or more.

[0031] Although not limiting to the present disclosure, examples of vitamins include water-soluble or fat-soluble vitamins such as vitamin A, vitamin B, vitamin C, and vitamin E. Vitamins may be used singly or in combination of two or more. Examples of vitamin A include retinol palmitate, retinol acetate, retinol, retinal, and retinoic acid. Examples of vitamin B include flavin adenine dinucleotide, cyanocobalamin, and pyridoxine hydrochloride (vitamin B6), and examples of vitamin E include tocopherol acetate (d-α-tocopherol acetate).

[0032] When the ophthalmic composition of the present disclosure contains a medicinal ingredient, the content of the medicinal ingredient is not limited as long as it does not impair the effects of the present disclosure. The content of the medicinal ingredient in the composition is preferably 0.01 w / v% or more and 5 w / v% or less, more preferably 0.025 w / v% or more and 4 w / v% or less, and even more preferably 0.1 w / v% or more and 2 w / v% or less, for example.

[0033] Examples of the other component include a cooling agent, such as menthol, camphor, borneol, etc. The cooling agent may be used alone or in combination of two or more.

[0034] The ophthalmic composition of the present disclosure can be produced by mixing component (1), component (2) and / or (3), and, if necessary, any other component(s) described above. The mixing method is not limited as long as the components can be mixed, and the components may be mixed according to a conventional procedure.

[0035] The pH of the ophthalmic composition of the present disclosure is not limited as long as it is within a range that allows use as an eye drop or eyewash, and examples thereof include a pH of 5 to 8, preferably 5.5 to 7, and more preferably 5.5 to 6.5 at room temperature (25° C.). The pH is measured using a tabletop pH meter F-52 (manufactured by Horiba, Ltd.).

[0036] The viscosity of the ophthalmic composition of the present disclosure is not limited as long as it is within a range that allows it to be used as an eye drop or eyewash, and is preferably 0.01 mPa·s or more and 2.5 mPa·s or less at room temperature, more preferably 0.05 mPa·s or more and 2 mPa·s or less, even more preferably 0.1 mPa·s or more and 1.5 mPa·s or less, and even more preferably 0.1 mPa·s or more and 1 mPa·s or less. The viscosity is measured at a shear rate of 100 s using a cone-plate viscometer (Rheometer MCR302, manufactured by Anton Paar). -1 The measurement is performed at a measurement temperature of 25°C. More specifically, 5 mL of the ophthalmic composition is added to the sample plate of the rheometer, and a cone-plate sensor with a radius of 50 mm and a cone angle of 1° is set. At 25°C, the shear rate is 100 s -1 The sensor is rotated so that the viscosity is measured. Measurement is continued for 100 seconds, with one data point being acquired every two seconds. The average value of the five data points (45th to 49th data points) is calculated and used as the viscosity. As described above, the viscosity of the ophthalmic composition of the present disclosure is not limited, but a preferred example is one in which the viscosity is as low as that of common eye drops or eyewashes. Therefore, the ophthalmic composition of the present disclosure can be advantageous in that it can improve wettability despite its low viscosity.

[0037] The ophthalmic composition of the present disclosure is liquid at room temperature and can be preferably used as an eyewash, eye drops, contact lens wetting solution, etc. When used as an eyewash, it is typically used for eyewashing by eye drops or by using an eyecup. The ophthalmic composition of the present disclosure can be used both when contact lenses are not being worn and when contact lenses are being worn. The contact lenses can be either hard or soft. Soft contact lenses can be broadly classified into four types based on their water content: ionic, nonionic, high water content (water content of 50% or more), and low water content (water content of less than 50%), but any type is acceptable. Therefore, the soft contact lenses can be either silicone hydrogel contact lenses or non-silicone hydrogel contact lenses.

[0038] The ophthalmic composition of the present disclosure is not limited as long as it can be used as described above. However, when used as an eye drop, the composition is usually contained in an eye drop container for ease of use. The eye drop container is not limited as long as it can contain the composition and be used to administer the composition to the eye. Examples of the eye drop container include containers used for conventionally known eye drops and eye drops-type eyewashes (e.g., containers in which the container body, inner stopper, and cap are each independent, containers in which at least two of the container body, inner stopper, and cap are integrated, containers with a hole in the inner stopper, etc.). The volume of the container is also not limited, but from the perspective of ease of use, a volume of 3 to 20 mL is exemplified.

[0039] When used as an eye drop, the eye drop can be administered according to the usual method, by administering 1 to 4 drops of the ophthalmic composition of the present disclosure per eye at a time. When used as an eye wash, the eye drop can be administered according to the usual method, by administering 4 to 6 drops of the ophthalmic composition of the present disclosure per eye at a time. The amount of each drop is not particularly limited, but a preferred amount is 35 to 40 μL per drop. The number of times the composition is administered per day is also not particularly limited, and examples of such amounts include 2 to 8 times per day per eye. The eye can be cleansed in this manner using a drop-type eye wash.

[0040] When the ophthalmic composition of the present disclosure is used with an eyewash cup, it may be generally stored in a conventionally known container (e.g., including the container body and cap). The volume of the container is not limited, but from the viewpoint of ease of use, the volume is preferably, for example, 450 to 550 mL.

[0041] Eye washing using an eyewash cup can be performed according to standard procedures. For example, an appropriate amount of the ophthalmic composition of the present disclosure is poured from the container into the eyewash cup, for example, 4 to 6 mL per eye. The cup is then pressed against the area around one eye to bring the ophthalmic composition in the cup into contact with the eye, and the patient is then blinked several times. The number of times the composition is used per day is not limited, and examples include 1 to 6 times per day per eye. In this manner, the eyes can be washed.

[0042] When used as a contact lens wetting solution, the method of use is not limited. Typically, 1 to 3 drops of the ophthalmic composition of the present disclosure may be applied to the contact lens before wearing it. Alternatively, the ophthalmic composition of the present disclosure may be applied to the naked eye or used as an eyewash before wearing the contact lens. In this way, the ophthalmic composition of the present disclosure can be used even while wearing contact lenses. Therefore, the ophthalmic composition of the present disclosure can also be used as an ophthalmic composition for contact lenses (contact lens eye drops (eye drops that can be used while wearing contact lenses)), contact lens eyewash (eyewash that can be used while wearing contact lenses), contact lens wetting solution, contact lens care preparation (contact lens cleaning solution, contact lens storage solution, etc.).

[0043] According to the ophthalmic composition of the present disclosure, wettability can be improved by using the component (1) in combination with the component (2) and / or (3). In the present disclosure, improved wettability refers to improved water wettability of the surface of the eye or contact lens. As shown in the test examples described below, the smaller the angle (contact angle θ (FIG. 1)) formed between a droplet of the ophthalmic composition of the present disclosure and the surface of the eye or contact lens, the higher the wettability, and the improved wettability can be evaluated. Improved wettability can prevent or suppress eye discomfort. Examples of discomfort include dry eyes, itching, and a gritty feeling in the eyes (foreign body sensation). Furthermore, if the ophthalmic composition of the present disclosure further contains the aforementioned medicinal ingredients, beneficial effects based on the medicinal ingredients can also be obtained. When the ophthalmic composition of the present disclosure is used as an eyewash, it has the advantage of improving wettability in addition to removing eye dirt.

[0044] Furthermore, in recent years, with the widespread use of electronic devices, the number of people experiencing unpleasant symptoms such as dry eyes, eye pain, and a gritty feeling has been increasing. These symptoms are one of the factors that prevent people from wearing contact lenses. Furthermore, contact lenses are said to have the property of absorbing tears, and wearing contact lenses can also cause discomfort such as dry eyes. According to the present disclosure, as shown in the test examples described below, wettability was improved even when contact lenses were used, and therefore, the present disclosure has the advantage of being suitable for use even when contact lenses are worn. [Example]

[0045] Hereinafter, the embodiments of the present disclosure will be described more specifically with reference to examples, but the embodiments of the present disclosure are not limited to the following examples.

[0046] Test Example 1 Testing Procedures Ophthalmic compositions were prepared according to the following procedure, and their wettability was evaluated.

[0047] As ophthalmic compositions, the components were mixed according to Table 1 to prepare test solutions shown in Examples 1 to 3 and Comparative Examples 1 to 3. In Table 1, the viscosity-average molecular weight of sodium hyaluronate is 1,000,000, and the weight-average molecular weight of sodium chondroitin sulfate is 20,000.

[0048] [Table 1]

[0049] In this test example, the test was carried out using contact lenses according to the following procedure. 1) Release of blister solution (contact lens storage solution) The contact lenses were removed from their containers and immersed in saline (0.9 w / v% sodium chloride) for 1 hour to release the blister fluid from the contact lenses. The contact lenses were then removed from the saline, and the saline adhering to the surface of the contact lenses was removed with a Kimwipe. 2) Wettability measurement (initial value measurement) A drop of saline was placed on the convex surface of the contact lens from which the saline solution had been removed in 1) above, and the contact angle of the drop was measured using the drop method (Figure 1). The value of the contact angle at this time was used as the control (initial value). Specifically, for this measurement, a 5 μL drop of saline was placed on the convex surface of the contact lens, and the angle between the drop and the contact lens surface (contact angle θ, Figure 1) was measured. A smaller contact angle indicates a higher wettability (water-wettability) of the surface. 3) Contact with test liquid and measurement of wettability (measurement of wettability after contact with test liquid) The contact lens from which the saline solution had been removed in 1) above was immersed in the test solution for 1 hour. The contact lens was then removed from the test solution, and the test solution adhering to the surface of the contact lens was removed with a Kimwipe in the same manner as in 1) above. After removal, a drop of saline was placed on the convex surface of the contact lens, and the contact angle was measured in the same manner as in 2) above. The value of this contact angle was taken as the contact angle after contact with the test solution. 4) Release of test liquid and measurement of wettability (measurement of wettability after release of test liquid) The contact lens from which the test solution had been removed in 3) above was immersed in physiological saline for 1 hour. The contact lens was then removed from the physiological saline, and the physiological saline adhering to the surface of the contact lens was removed with a Kimwipe in the same manner as in 1) above. After removal, a drop of physiological saline was placed on the convex surface of the contact lens and the contact angle was measured in the same manner as in 2) above. The value of this contact angle was taken as the contact angle after the test solution had been released. 5) Calculating the rate of change The contact angle θ (after contact with the test liquid) obtained in 3) was divided by the contact angle θ (initial value) obtained in 2) to calculate the rate of change in the contact angle after contact relative to the initial value ("after contact" in the figure). In addition, the contact angle θ (after release of the test liquid) obtained in 4) was divided by the contact angle θ obtained in 2) to calculate the rate of change in the contact angle after release of the test liquid relative to the initial value ("after release" in the figure).

[0050] In this test, two types of soft contact lenses were used: Group I (non-ionic, low-water content lenses) and Group IV (ionic, high-water content lenses). Soft contact lenses are generally divided into four types (Groups I to IV). Group I is non-ionic, low-water content (less than 50% water content) lenses. Group II is non-ionic, high-water content (more than 50% water content) lenses. Group III is ionic, low-water content lenses. Group IV is ionic, high-water content lenses. High-water content lenses contain a lot of water, making them soft and comfortable to wear, but they tend to evaporate easily and feel dry. Low-water content lenses have less water, making them less likely to evaporate and feel dry, but because they are naturally low in water content, they tend to feel less comfortable to wear than high-water content lenses. Ionic lenses, made of ionic materials, have higher oxygen permeability and a better fit than non-ionic materials, but they tend to be more susceptible to soiling and less durable than non-ionic materials. Non-ionic lenses tend to be less susceptible to staining and more durable than ionic lenses, but they tend to be less comfortable to wear because they have lower oxygen permeability than ionic lenses.

[0051] ·result The results are shown in Figures 2 and 3. Figure 2 shows the results using contact lenses from Group IV, and Figure 3 shows the results using contact lenses from Group I.

[0052] As shown in FIG. 2, when the test liquid (EC) of Comparative Example 1 was used, the contact angle was smaller after contact with the test liquid compared to the initial value, i.e., improved wettability was observed. However, after the test liquid was released, the contact angle was larger than the initial value, i.e., wettability was decreased. When the test liquid (HA) of Comparative Example 2 was used, the contact angle was smaller after contact with the test liquid compared to the initial value, indicating improved wettability, but after the test liquid was released, the contact angle was similar to the initial value, indicating no improvement in wettability. When the test liquid (CSS) of Comparative Example 3 was used, as in Comparative Example 1, improved wettability was observed after contact with the test liquid compared to the initial value, but after the test liquid was released, wettability was actually lower than the initial value.

[0053] In contrast, as shown in Figure 2, when the test liquid of Example 1 (EC+HA) was used, the contact angle was smaller than the initial value both after contact with the test liquid and after release of the test liquid, demonstrating improved wettability. When the test liquid of Example 2 (EC+CSS) or the test liquid of Example 3 (EC+HA+CSS) was used, improved wettability was also observed both after contact with the test liquid and after release of the test liquid, compared to the initial value. From these results, it was confirmed that the test liquids of Examples 1 to 3 can improve wettability.

[0054] A similar trend was observed in Figure 3. Specifically, when the test liquid (EC) of Comparative Example 1, the test liquid (HA) of Comparative Example 2, or the test liquid (CSS) of Comparative Example 3 was used, an improvement in wettability was observed after contact with the test liquid compared to the initial value. However, with all of the test liquids of Comparative Examples 1 to 3, the wettability after release of the test liquid either decreased from the initial value or remained at the same level as the initial value.

[0055] In contrast, as shown in Figure 3, when the test solution of Example 1 (EC+HA) was used, improvements in wettability were observed both after contact with the test solution and after release of the test solution, compared to the initial value. When the test solution of Example 2 (EC+CSS) or Example 3 (EC+HA+CSS) was used as the test solution, improvements in wettability were also observed both after contact with the test solution and after release of the test solution, compared to the initial value. These findings demonstrate that the test solutions of Examples 1 to 3 can improve the wettability of both Group IV and Group I contact lenses. Furthermore, it was found that the test solutions of Examples 1 to 3 can effectively improve wettability despite their low viscosity.

[0056] Furthermore, in this test example, when the test solutions of Examples 1 to 3 were used, improved wettability was observed after contact with and release from the contact lenses of both Group I (non-ionic, low-water content lenses) and Group IV (ionic, high-water content lenses). This suggests that the test solutions of Examples 1 to 3 have enhanced affinity for contact lenses compared to the test solutions of Comparative Examples 1 to 3. Furthermore, improved wettability was observed for both non-ionic, low-water content lenses and ionic, high-water content lenses, demonstrating that the test solutions of Examples 1 to 3 can improve the wettability of any contact lenses, regardless of whether they are ionic or non-ionic, or whether they have a low or high water content.

[0057] Test Example 2 Tests were conducted in the same manner as in Test Example 1, except that the test solutions of Comparative Example 4 and Examples 4 to 6 (Table 2) were used, in which the EC content in each of Comparative Example 1 and Examples 1 to 3 was reduced to 0.03 w / v%.

[0058] [Table 2]

[0059] The results are shown in Figure 4 (Group IV lenses) and Figure 5 (Group I lenses). As shown in Figures 4 and 5, when the test solution (EC) of Comparative Example 4 was used, improved wettability was observed after contact with the test solution, but wettability after release of the test solution remained at the same level as the initial value. In contrast, when the test solution of Example 4 (EC+HA) was used, improved wettability was observed both after contact with the test solution and after release of the test solution compared to the initial value. When the test solution of Example 5 (EC+CSS) or Example 6 (EC+HA+CSS) was used, improved wettability was also observed both after contact with the test solution and after release of the test solution compared to the initial value. In Figure 4, when the test solution of Example 5 was used, the degree of improvement in wettability was inferior to that when the test solutions of Examples 4 and 6 were used, but the improvement in wettability was maintained even after release of the test solution, as with the test solutions of Examples 4 and 6. From these results, it was understood that the test solutions of Examples 4 to 6 could also improve wettability.

[0060] Test Example 3 Tests were carried out in the same manner as in Test Example 1, except that the test solutions of Examples 7 to 9 (Table 3), which were prepared by further adding epsilon-aminocaproic acid to each of Examples 4 to 6, were used.

[0061] [Table 3]

[0062] The results are shown in Figure 6 (Group IV lenses) and Figure 7 (Group I lenses). As shown in Figures 6 and 7, when the test solution of Example 7 (EC+HA+ε-Acp) was used, improved wettability was observed after contact with the test solution and after release of the test solution. Furthermore, when the test solution of Example 8 (EC+CSS+ε-Acp) or Example 9 (EC+HA+CSS+ε-Acp) was used, improved wettability was observed both after contact with the test solution and after release of the test solution. From this, it was understood that the test solutions of Examples 7 to 9 could also improve wettability.

[0063] Furthermore, as described above, wettability was improved when the test solutions of Examples 1 to 9 shown in Test Examples 1 to 3 were used. From this, it was understood that wettability can be improved by applying the ophthalmic composition of the present disclosure to the eye with or without a contact lens, and allowing the composition to remain on the eye or contact lens.

Claims

1. An ophthalmic composition comprising the following component (1) and the following components (2) and / or (3): (1) at least one selected from the group consisting of ectoine, ectoine salts, and derivatives thereof; (2) at least one selected from the group consisting of chondroitin sulfate esters and salts thereof; (3) At least one selected from the group consisting of hyaluronic acid and salts thereof, wherein when the ophthalmic composition contains component (3), the total content of component (3) in the ophthalmic composition is 0.05 w / v% or less.

2. The ophthalmic composition according to claim 1, wherein the total content of component (1) in the ophthalmic composition is 0.05 w / v % or less.

3. The ophthalmic composition according to claim 1, wherein the total content of component (2) in the ophthalmic composition is 0.5 w / v % or less.

4. The ophthalmic composition of claim 1 , wherein the ophthalmic composition is an eyewash.

5. The ophthalmic composition according to claim 4, wherein the eyewash is a drop-type eyewash or a cup-type eyewash.

6. The ophthalmic composition of claim 1 , which is an ophthalmic composition for contact lenses.

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