Eye drop-type eye-wash 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-washing cup (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-washing 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 has a problem that an eye-washing cup is essential and it lacks portability.

[0003] Further, as an eye-washing method different from the above method, a method of directly instilling 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-washing cup, it is excellent in portability. However, in this method, compared with the above method, the amount of the eye-washing solution applied to the eye is reduced, 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 present inventors conducted intensive studies and found that by incorporating at least one selected from the group consisting of chondroitin sulfate and its salts into an eye-drop type eye-washing composition, the foreign substance removal effect in the eye-drop type eye-washing 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-washing composition containing at least one selected from the group consisting of chondroitin sulfate and its salts. Item 2. The eye-drop type eye-washing 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-washing composition according to Item 1 or 2, which does not contain 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-washing composition according to any one of Items 1 to 3, wherein 3 to 8 drops are instilled into one eye at a time. Item 5. A method for improving the foreign substance removal effect of an eye-drop type eye-washing composition, which comprises incorporating at least one selected from the group consisting of chondroitin sulfate and its salts into the eye-drop type eye-washing composition.

Effects of the Invention

[0007] According to the present invention, an eye-drop type eye-washing composition capable of effectively removing foreign substances can be provided, and the foreign substance removal effect in the eye-drop type eye-washing 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-washing composition containing at least one selected from the group consisting of chondroitin sulfate and its salts.

[0010] 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. Chondroitin sulfate is a mucopolysaccharide having a structure in which sulfuric acid is ester-bonded to a sugar chain in which disaccharides of D-glucuronic acid and N-acetylgalactosamine are repeated, 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, preferably, the weight average molecular weight is about 0.5 to 45,000, more preferably about 10,000 to 40,000, and still more preferably about 15,000 to 30,000. The weight average molecular weight is measured by gel filtration chromatography. Chondroitin sulfate and its salts are commercially available, for example, sold under the trade name Kyowa Chondroitin Sulfate Sodium (manufactured by Kyowa Chemical Industry Co., Ltd., weight average molecular weight 20,000).

[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-washing 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. However, 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. However, 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 that are 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, cooling 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 appropriately determined.

[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 and may be used in combination.

[0018] When the eye-drop type eye-washing 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, 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, and preferably amino acid analogs such as taurine are exemplified. These may be used alone or in combination of two or more. In addition, the eye-drop type eye-washing 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 glycyrrhizinate, etc.) are exemplified. These may be used alone or in combination of two or more. Although it does not limit the present invention, the eye-drop type eye-washing 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, but the eye-drop type eye-washing composition of the present invention can be prepared without blending hyaluronic acid and / or its salts.

[0022] When the eye-drop type 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 by 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 eye-drop type 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 eye-drop type 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. In the composition, it can be appropriately selected from the range of 0.3 to 2 w / v% so that the osmotic pressure ratio (to physiological saline) of the composition is in the range of 0.6 to 1.6 as described later.

[0025] When the eye-drop type 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

[0026] As one embodiment of the present invention, although not limiting the present invention, 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.

[0027] Also, as one embodiment of the present invention, although not limiting the present invention, 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, and boric acid and / or borax.

[0028] Also, as one embodiment of the present invention, although not limiting the present invention, the eye-drop type eye-wash 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-wash 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, although not limiting the present invention, the eye-drop type eye-wash 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, although not limiting the present invention, examples of the eye-drop type eye-wash 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 agent.

[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. 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 is usually liquid at room temperature.

[0035] As described below, the eye-drop type eye-wash composition of the present invention is usually contained in an eye-drop container and instilled. Therefore, the viscosity of the composition is not limited as long as it is within the range that allows instillation, 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 −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 −1, and the viscosity is measured. Measurement is performed for 100 seconds, one-point data is acquired every 2 seconds, and the average value is calculated from 5 data points at the 45th to 49th points, which 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 is within the range that can be used as an eye drop or an eye-washing agent. For example, the osmotic pressure ratio is exemplified as 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 physiological saline (0.9 w / v% sodium chloride aqueous solution) and taking the measured value of physiological saline as 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 drops. From the viewpoint of good usability, etc., the composition is usually contained in an eye-drop container and used.

[0039] The eye-drop container is not limited as long as it can contain the composition and be used for eye drops. 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 as 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 instilling 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 substance removal effect, the composition is preferably instilled with 4 to 8 drops per eye, and more preferably 4 to 6 drops per eye.

[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 instilling the composition, foreign substances 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] From this, it can be said that the present invention also provides a method for improving the foreign substance 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. From this, it can also be said that the present invention provides a method for improving the foreign substance 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-Washing Composition According to the mixing ratios shown in Table 1 below, each component was mixed 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). As the sodium chondroitin sulfate, topical-grade sodium chondroitin sulfate (manufactured by Seikagaku Corporation, weight-average molecular weight 20,000) was used.

[0050] 2. Foreign Substance Removal Evaluation Four panelists were made to wash their eyes according to the instructions by the eye-washing method using an eye cup (commercially available Eye Bon Mild (manufactured by Kobayashi Pharmaceutical Co., Ltd.)). Six hours after the eye-washing, the perimeters of both eyes of these four panelists were 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 one time.

[0051] Except that the composition of Example 2 was used 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] While transferring the total composition collected three times in each eye cup into one eye cup, it was made up to 5 mL with physiological saline (containing 0.9 w / v% sodium chloride) using a graduated cylinder, and the par 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 defined 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, with the average number of foreign substances in the composition of Comparative Example 1 taken as 100, the average number of foreign substances when the compositions of Examples 1 and 2 were used 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 the compositions of Examples 1 and 2 further containing sodium chondroitin sulfate were used, a higher foreign substance removal effect was obtained than when the composition of Comparative Example 1 not containing sodium chondroitin sulfate was used.

[0056] From this, it was found that in the eye-drop type eye wash composition, by blending sodium chondroitin sulfate, the foreign substance removal effect of the eye-drop type eye wash composition can be enhanced. Also, regarding sodium chondroitin sulfate, in the eye-drop type eye wash composition prepared in the same manner as in 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 substance removal effect of the eye could be further enhanced as compared with the compositions having the same composition except that they do not contain sodium chondroitin sulfate (replaced with water).

[0058] [Table 2]

Claims

【Claim 1】 An eye-drop type eye-washing composition containing at least one selected from the group consisting of chondroitin sulfate and its salts.

Images