Eye-drop type eye-washing composition

Abstract

To provide an eye drop-type eye-wash composition capable of effectively removing a foreign substance, and to provide a method for improving an effect of removing a foreign substance.SOLUTION: Provided is an eye drop-type eye-wash composition comprising at least one selected from the group consisting of chondroitin sulfate and a salt thereof. Also provided is a method for improving an effect of removing a foreign substance shown by an eye drop-type eye-wash composition, the method comprising blending at least one selected from the group consisting of chondroitin sulfate and a salt thereof into the eye drop-type eye-wash composition.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to an eye-drop type eye-washing composition.

Background Art

[0002] Conventionally, an eye-washing method using an eye cup has been known. As an example of the method, an appropriate amount (for example, about 5 mL) of an eye-washing solution is poured into the eye cup, and then the cup is pressed against the periphery of one eye to bring the eye-washing solution in the cup into contact with the eye, and the eye is washed by blinking several times. However, this method requires an eye cup and has a problem of lack of portability.

[0003] Further, as an eye-washing method different from the above method, a method of directly dropping an eye-washing solution into the eye for eye-washing is known (for example, Patent Document 1). Since this method does not require an eye cup, it is excellent in portability. However, in this method, the amount of the eye-washing solution applied to the eye is less than that of the above method, and there is a possibility that the eye-washing effect may be insufficient.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] Therefore, an object of the present invention is to provide an eye-drop type eye-washing composition capable of effectively removing foreign substances, and also to provide a method for improving the foreign substance removal effect.

Means for Solving the Problems

[0006] In view of the above problems, the inventors conducted intensive studies and found that by incorporating at least one selected from the group consisting of chondroitin sulfate and its salts into the eye-drop type eye wash composition, the foreign matter removal effect in the eye-drop type eye wash composition can be improved. The present invention was completed as a result of further studies based on this finding, and is as follows. Item 1. An eye-drop type eye wash composition containing at least one selected from the group consisting of chondroitin sulfate and its salts. Item 2. The eye-drop type eye wash composition according to Item 1, further containing at least one selected from the group consisting of boric acid and borax. Item 3. The eye-drop type eye wash composition according to Item 1 or 2, not containing at least one selected from the group consisting of a thickening agent, a preservative, and an antihistamine agent. Item 4. The eye-drop type eye wash composition according to any one of Items 1 to 3, wherein 3 to 8 drops are instilled per eye at a time. Item 5. A method for improving the foreign matter removal effect of an eye-drop type eye wash composition, wherein at least one selected from the group consisting of chondroitin sulfate and its salts is incorporated into the eye-drop type eye wash composition.

Effects of the Invention

[0007] According to the present invention, an eye-drop type eye wash composition capable of effectively removing foreign matter can be provided, and the foreign matter removal effect in the eye-drop type eye wash composition can be improved.

Modes for Carrying Out the Invention

[0008] Hereinafter, the present invention will be described in more detail.

[0009] The present invention provides an eye-drop type eye wash composition containing at least one selected from the group consisting of chondroitin sulfate and its salts.

[0010] The eye-drop type eye-wash composition of the present invention contains at least one selected from the group consisting of chondroitin sulfate and its salts. Chondroitin sulfate is a mucopolysaccharide having a structure in which sulfuric acid is ester-bonded to a sugar chain in which a disaccharide of D-glucuronic acid and N-acetylgalactosamine repeats, and is a known substance.

[0011] Examples of the salts of chondroitin sulfate include, but are not limited to, alkali metal salts such as sodium salts and potassium salts, and alkaline earth metal salts such as magnesium salts and calcium salts. Examples of the salts of chondroitin sulfate preferably include sodium chondroitin sulfate, etc., although not limiting the present invention.

[0012] The chondroitin sulfate and its salts used in the present invention are not limited as such, but from the viewpoint of further improving the foreign substance removal effect, the weight average molecular weight is preferably about 0.5×10⁴ to 4.5×10⁴, more preferably about 1×10⁴ to 4×10⁴, and still more preferably about 1.5×10⁴ to 3×10⁴. The weight average molecular weight is measured by gel filtration chromatography. Chondroitin sulfate and its salts are commercially available. For example, it is sold under the trade name Kyowa Chondroitin Sulfate Sodium (manufactured by Kyowa Chemical Industry Co., Ltd., weight average molecular weight 20000).

[0013] The content of at least one selected from the group consisting of chondroitin sulfate and its salts is not limited as long as the effects of the present invention can be obtained, but from the viewpoint of further improving the foreign substance removal effect, in the eye-drop type eye-wash composition of the present invention, 0.005 to 0.5 w / v% is exemplified, preferably 0.005 to 0.4 w / v%, more preferably 0.006 to 0.3 w / v%, still more preferably 0.007 to 0.1 w / v%, and particularly preferably 0.008 to 0.08 w / v%.

[0014] The eye-drop type eye-wash composition of the present invention may contain boric acid. The content of boric acid is not limited as long as it does not interfere with the effects of the present invention. From the viewpoint of further improving the foreign substance removal effect, in the eye-drop type eye-wash composition of the present invention, 0.2 to 2.5 w / v% is exemplified, preferably 0.5 to 2.2 w / v%, more preferably 1 to 2 w / v%, still more preferably 1.2 to 2 w / v%, and particularly preferably 1.4 to 1.8 w / v%.

[0015] The eye-drop type eye-wash composition of the present invention may contain borax. The content of borax is not limited as long as it does not interfere with the effects of the present invention. From the viewpoint of further improving the foreign substance removal effect, in the eye-drop type eye-wash composition of the present invention, 0.001 to 0.6 w / v% is exemplified, preferably 0.002 to 0.1 w / v%, more preferably 0.003 to 0.05 w / v%, still more preferably 0.005 to 0.025 w / v%, and particularly preferably 0.01 to 0.02 w / v%.

[0016] The eye-drop type eye-wash composition of the present invention may further contain any other components acceptable for use in eye drops and eye washes. Examples of such other components include, but are not limited to, medicinal components, stabilizers, isotonic agents, refreshing agents, solvents, pH adjusters, thickeners, preservatives, etc. These other components may be appropriately selected according to the purpose, etc., and may be used alone or in combination of two or more, and the blending amount may also be determined appropriately.

[0017] Without limiting the present invention to this extent, examples of medicinal components as an example of other components include amino acids, vitamins, anti-inflammatory agents, corneal surface protectants, antihistamines, etc. These may be used alone or in combination of two or more.

[0018] When the ophthalmic eye wash composition of the present invention contains a medicinal ingredient, although it does not limit the present invention, preferably, it is exemplified that it contains at least one selected from the group consisting of amino acids, vitamins, anti-inflammatory agents (anti-inflammatory drugs), corneal surface protectants, and antihistamines. More preferably, it is exemplified that it contains 1 to 5 kinds selected from the group. Even more preferably, it is exemplified that it contains 2 to 4 kinds or 2 to 3 kinds selected from the group.

[0019] Although it does not limit the present invention, for example, as amino acids, amino acids and their salts such as glutamic acid and its salts (sodium glutamate, etc.); amino acid analogs such as taurine, etc. are exemplified. Preferably, amino acid analogs such as taurine are exemplified. These may be used alone or in combination of two or more. In addition, the ophthalmic eye wash composition of the present invention can be prepared without blending amino acids and / or their salts. The amino acids referred to here mean amino acids that can be constituent units of proteins having both functional groups of an amino group and a carboxyl group, and include, for example, L-aspartic acid, etc.

[0020] Although it does not limit the present invention, for example, as anti-inflammatory agents, zinc sulfate, zinc lactate, epsilon-aminocaproic acid, glycyrrhizic acid and its salts (dipotassium glycyrrhizate, etc.) are exemplified. These may be used alone or in combination of two or more. Although it does not limit the present invention, the ophthalmic eye wash composition of the present invention preferably does not contain zinc sulfate and / or zinc lactate.

[0021] Although it does not limit the present invention, for example, as corneal surface protectants, hyaluronic acid and its salts (sodium hyaluronate, etc.) are exemplified. However, the ophthalmic eye wash composition of the present invention can be prepared without blending hyaluronic acid and / or its salts.

[0022] When the ophthalmic eye wash composition of the present invention contains a medicinal ingredient, the content of the medicinal ingredient is not limited as long as the effects of the present invention are not impaired. In the composition, the content of the medicinal ingredient is exemplified as 0.01 to 1 w / v%, preferably 0.025 to 0.8 w / v%, more preferably 0.05 to 0.5 w / v%, still more preferably 0.1 to 0.4 w / v%, and particularly preferably 0.13 to 0.3 w / v%. Note that chondroitin sulfate and its salts are also known as medicinal ingredients, but these ingredients are not included in the description of the medicinal ingredient here. Therefore, the content of chondroitin sulfate and its salts is not included in the content of the medicinal ingredient.

[0023] When the ophthalmic eye wash composition of the present invention contains a stabilizer, the stabilizer may be used alone or in combination of two or more. Also, the content of the stabilizer is not limited as long as the effects of the present invention are not impaired. In the composition, 0.001 to 0.5 w / v% is exemplified, preferably 0.05 to 0.2 w / v%, and more preferably 0.08 to 0.12 w / v%.

[0024] When the ophthalmic eye wash composition of the present invention contains an isotonic agent, the isotonic agent may be used alone or in combination of two or more. Also, the content of the isotonic agent is not limited as long as the effects of the present invention are not impaired. It can be appropriately selected from the range of 0.3 to 2 w / v% in the composition so that the osmotic pressure ratio (to physiological saline) of the composition is in the range of 0.6 to 1.6 as described below.

[0025] When the ophthalmic eye wash composition of the present invention contains a cooling agent, the cooling agent may be used alone or in combination of two or more. Also, the content of the cooling agent is not limited as long as the effects of the present invention are not impaired. In the composition, 0.0001 to 0.6 w / v% is exemplified, preferably 0.002 to 0.01 w / v%, and more preferably 0.004 to 0.008 w / v%.

[0026] As one embodiment of the present invention, without limiting the present invention, the eye-drop type eye-washing composition of the present invention contains at least one selected from the group consisting of chondroitin sulfate and its salts.

[0027] Also, as one embodiment of the present invention, without limiting the present invention, the eye-drop type eye-washing composition of the present invention contains at least one selected from the group consisting of chondroitin sulfate and its salts, and boric acid and / or borax.

[0028] Also, as one embodiment of the present invention, without limiting the present invention, the eye-drop type eye-washing composition of the present invention contains (1) at least one selected from the group consisting of chondroitin sulfate and its salts, (2) boric acid and / or borax, and (3) at least one selected from the group consisting of a medicinal ingredient, a stabilizer, an isotonic agent, a cooling agent, a solvent, and a pH adjuster, and does not contain a thickening agent and / or a preservative (particularly a quaternary ammonium-based preservative (for example, benzalkonium chloride, benzethonium chloride, etc.)).

[0029] Also, boric acid and borax can be used as a buffer, and the eye-drop type eye-washing composition of the present invention may or may not contain a buffer other than boric acid and borax.

[0030] Also, as one embodiment of the present invention, without limiting the present invention, the eye-drop type eye-washing composition of the present invention consists of (1) at least one selected from the group consisting of chondroitin sulfate and its salts, (2) boric acid and / or borax, and (3) at least one selected from the group consisting of a medicinal ingredient, a stabilizer, an isotonic agent, a cooling agent, a solvent, and a pH adjuster.

[0031] Also, as one embodiment of the present invention, without limiting the present invention, examples of the eye-drop type eye-washing composition of the present invention in each of the above embodiments include those that do not contain an amino acid and its salt, and those that do not contain an antihistamine.

[0032] The eye-drop type eye-wash composition of the present invention can be produced by mixing at least one selected from the group consisting of chondroitin sulfate and its salts, boric acid and / or borax as required, and the other components as required.

[0033] The pH of the eye-drop type eye-wash composition of the present invention is not limited as long as it is within the range usable as an eye-drop or eye-wash. However, examples include pH 5 to 8, preferably pH 5.5 to 7.5, and more preferably pH 6 to 7.5 at room temperature (24°C). The pH is measured using a desktop pH meter F-52 (manufactured by Horiba, Ltd.).

[0034] The form of the eye-drop type eye-wash composition of the present invention is not limited, and it is usually liquid at room temperature.

[0035] As described below, the eye-drop type eye-wash composition of the present invention is usually housed in an eye-drop container and instilled. Therefore, the viscosity of the composition is not limited as long as it is within the range where it can be instilled, but examples include 0.9 to 2.5 mPa·s, more preferably 0.9 to 1.6 mPa·s, and even more preferably 0.9 to 1.2 mPa·s at room temperature. The viscosity is measured using a cone-plate viscometer (Rheometer MCR302, manufactured by Anton Paar) at a shear rate of 100 s -1 , and a measurement temperature of 25°C. More specifically, 5 mL of the composition is added to the sample plate of the rheometer, a cone-plate sensor with a radius of 50 mm and a cone angle of 1° is set, and at 25°C, the sensor is rotated so that the shear rate is 100 s -1 , and the viscosity is measured. The measurement is carried out for 100 seconds, one data point is acquired every 2 seconds, and the average value is calculated from 5 data points at the 45th to 49th points, and this is taken as the viscosity.

[0036] The osmotic pressure of the eye-drop type eye-washing composition of the present invention is not limited as long as it can be used as an eye-drop or an eye-washing agent. For example, the osmotic pressure ratio is exemplified by 0.6 to 1.6, preferably 0.7 to 1.3, and more preferably 0.8 to 1.2. The osmotic pressure ratio is a value measured and calculated using an automatic osmotic pressure analyzer (Osmo Station OM-6060, manufactured by Arkray, Inc.) and conforms to the 17th revised Japanese Pharmacopoeia 2.47 Osmotic Pressure Measurement Method (Osmol Concentration Measurement Method). It is a value obtained by measuring the osmol concentration of the composition and a physiological saline solution (0.9 w / v% aqueous sodium chloride solution) and setting the measured value of the physiological saline solution to 1.

[0037] The eye-drop type eye-washing composition of the present invention may be used with contact lenses worn or without contact lenses worn. The contact lenses may be either hard contact lenses or soft contact lenses.

[0038] The eye-drop type eye-washing composition of the present invention is not limited as long as it can be used by eye-dropping. From the viewpoint of good usability, etc., the composition is usually used by being contained in an eye-drop container.

[0039] The eye-drop container is not limited as long as it can contain the composition and be used for eye-dropping. For example, eye-drop containers (including, for example, a container body, an inner stopper (nozzle), and a cap) used in conventionally known eye-drops and eye-drop type eye-washing agents are exemplified. The eye-drop container may be of any type, such as a type in which the container body, the inner stopper (nozzle), and the cap are each independent, a type in which at least two of the container body, the inner stopper (nozzle), and the cap are integrated, a type in which a hole is provided in the inner stopper (nozzle), or a type in which no hole is provided in the inner stopper (nozzle) and a hole is opened in the inner stopper (nozzle) by tightening the cap during use.

[0040] The capacity of the eye-drop container is not limited. From the viewpoint of good usability, etc., the capacity is exemplified by 8 to 20 mL, preferably 10 to 15 mL, and more preferably 12 to 14 mL. The capacity may be appropriately determined in consideration of whether it is a multi-dose type or a unit-dose type.

[0041] The eye-drop type eye-washing composition of the present invention is used by dropping 3 to 8 drops per eye once. Although not limited as long as this is the case, from the viewpoint of obtaining a more efficient foreign matter removal effect, preferably 4 to 8 drops, and more preferably 4 to 6 drops are dropped per eye once.

[0042] The dropping amount per drop of the composition is not limited as long as the effects of the present invention can be obtained. For example, 30 to 50 μL per drop is exemplified, preferably 35 to 40 μL, and more preferably 35 to 37 μL.

[0043] The number of times of use per day of the composition is not particularly limited, and for example, it may be any of 1 to 12 times, 2 to 8 times, 3 to 6 times, etc. per eye per day.

[0044] In this way, according to the eye-drop type eye-washing composition of the present invention, the eyes can be washed. In particular, since the composition contains at least one selected from the group consisting of chondroitin sulfate and its salts, by dropping the composition into the eyes, foreign matters such as dust, pollen, protein stains, and cosmetics present on the surface of the eyes can be removed more effectively, thereby enhancing the eye-washing effect. Further, when the composition further contains the above-mentioned medicinal components, useful effects based on the medicinal components can also be provided.

[0045] Therefore, it can be said that the present invention also provides a method for improving the foreign matter removal effect of an eye-drop type eye-washing composition by blending at least one selected from the group consisting of chondroitin sulfate and its salts into the eye-drop type eye-washing composition.

[0046] In this method, boric acid and / or borax may be further blended into the eye-drop type eye-washing composition, and the above-mentioned other components may be blended as necessary. Therefore, it can also be said that the present invention provides a method for improving the foreign matter removal effect of the eye-drop type eye-washing composition by blending at least one selected from the group consisting of chondroitin sulfate and its salts into the eye-drop type eye-washing composition containing boric acid and / or borax.

[0047] In these methods, at least one selected from the group consisting of eye-drop type eye-washing compositions, chondroitin sulfate and its salts, boric acid, borax, other components, and the contents of these components are explained in the same manner as described above.

Examples

[0048] Hereinafter, the present invention will be described in more detail with reference to examples, but the present invention is not limited thereto.

[0049] Test Example 1. Preparation of Ophthalmic Eye Wash Composition Each component was mixed according to the mixing ratios shown in Table 1 below to prepare each composition, and 13 mL of the composition was filled into a general eye-drop container (capacity 15 mL, made of polyethylene terephthalate resin, multi-dose type, manufactured by Shin-Ko Chemical Co., Ltd.) (Examples 1 and 2 and Comparative Example 1). Sodium chondroitin sulfate was prepared using topical sodium chondroitin sulfate (manufactured by Seikagaku Corporation, weight average molecular weight 20,000).

[0050] 2. Foreign Substance Removal Evaluation Four panelists were asked to wash their eyes according to the instructions using an eye-washing method with an eye cup (commercially available Eye Bon Mild (manufactured by Kobayashi Pharmaceutical Co., Ltd.)). Six hours after the eye wash, the area around both eyes of these four panelists was wiped clean with a cleaning cotton, and the composition of Comparative Example 1 was dropped into the left eye, and the composition of Example 1 was dropped into the right eye, two drops each (35 μL per drop) while looking upward, and dropped from the eye-drop container so that the composition did not overflow outside the eye. Then, while still looking upward, an eye cup was applied to the periphery of each eye, and by looking downward while the eye cup was applied, the composition dropped into the eye was collected into the eye cup. By repeating the process from dropping the composition into the eye to collecting it three times in total, the composition at the time of a total of 6 drops per eye was collected. One eye cup was used for each eye per time.

[0051] Except for using the composition of Example 2 instead of the composition of Example 1, the composition of Example 2 was also collected at the time of a total of 6 drops per eye in the same manner as described above.

[0052] The total amount of the composition collected three times in each eye cup was transferred to one eye cup and made up to 5 mL with physiological saline (containing 0.9 w / v% sodium chloride) using a graduated cylinder, and the number of particles was measured using a particle counter (model number APSS - 2000, manufactured by Particle Measuring Systems). The number of particles with a particle size of 2 to 125 μm was regarded as the number of foreign substances, and the average value of the number of foreign substances (average number of foreign substances) of four persons was determined. Next, taking the average number of foreign substances in the composition of Comparative Example 1 as 100, the average number of foreign substances when using the compositions of Examples 1 and 2 was rounded to the first decimal place and relatively compared.

[0053] 3. Results The results are shown in Table 1.

[0054]

Table 1

[0055] As shown in Table 1, when using the compositions of Examples 1 and 2 in which sodium chondroitin sulfate was further blended, a higher foreign substance removal effect was obtained than when using the composition of Comparative Example 1 that did not contain sodium chondroitin sulfate.

[0056] From this, it was found that in the eye-drop type eye-washing composition, by blending sodium chondroitin sulfate, the foreign substance removal effect of the eye-drop type eye-washing composition can be enhanced. Also, regarding sodium chondroitin sulfate, even in the eye-drop type eye-washing composition prepared in the same manner as Example 1 except that the weight-average molecular weight was changed to 10,000 or 40,000, the foreign substance removal effect was higher than that of Comparative Example 1, but Example 1 using sodium chondroitin sulfate with a weight-average molecular weight of 20,000 had a particularly excellent foreign substance removal effect.

[0057] Formulation Example Formulation examples are shown below. According to the compositions containing sodium chondroitin sulfate shown in Formulation Examples 1 to 10, the foreign body removal effect of the eyes could be further enhanced as compared with the compositions having the same composition except that they do not contain (replaced with water) sodium chondroitin sulfate.

[0058] [Table 2]

Claims

1. An eye-drop type eye-wash composition for removing foreign substances, containing at least one selected from the group consisting of chondroitin sulfate having a weight-average molecular weight of 15,000 to 30,000 and salts thereof as an active ingredient for the foreign substance removing action. Here, in the eye-drop type eye-wash composition, the total content of at least one selected from the group consisting of chondroitin sulfate and salts thereof is 0.01 to 0.05 w / v%. The eye-drop type eye-wash composition is an eye-drop type eye-wash composition recovered from the eye after eye-drop. (However, excluding the compositions of the following (1) to (4)) (1) An eye-drop type eye-wash composition containing potassium L-aspartate (2) An eye-drop type eye-wash composition containing chlorpheniramine maleate (3) An eye-drop type eye-wash composition containing alginic acid and / or a salt thereof (4) An eye-drop type eye-wash composition containing pyridoxine and / or a salt thereof).

2. The eye-drop type eye-wash composition according to Claim 1, further containing at least one selected from the group consisting of boric acid and borax.

3. A method for improving the foreign substance removing effect in an eye-drop type eye-wash composition, wherein at least one selected from the group consisting of chondroitin sulfate having a weight-average molecular weight of 15,000 to 30,000 and salts thereof is blended so that the total amount becomes 0.01 to 0.05 w / v%. Here, the eye-drop type eye-wash composition containing at least one selected from the group consisting of chondroitin sulfate and salts thereof is an eye-drop type eye-wash composition for removing foreign substances and is an eye-drop type eye-wash composition recovered from the eye after eye-drop. (However, excluding the compositions of the following (1) to (4) as the eye-drop type eye-wash composition) (1) An eye-drop type eye-wash composition containing potassium L-aspartate (2) An eye-drop type eye-wash composition containing chlorpheniramine maleate (3) An ophthalmic eye wash composition containing alginic acid and / or a salt thereof (4) An ophthalmic eye wash composition containing pyridoxine and / or a salt thereof).

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