JP2023180710A - vision improver - Google Patents

Abstract

To provide a highly safe vision improver, particularly a vision improver suitable for administration to patients with eye diseases.SOLUTION: A vision improver contains an iodine compound as an active ingredient. The vision improver should preferably contain the iodine compound in an amount of 0.1 mass% or more and 20 mass% or less in terms of iodine. Preferably, the vision improver should contain an alkali metal salt of iodine, and more preferably, sodium iodide and potassium iodide.SELECTED DRAWING: Figure 3

Description

The present invention relates to a vision improving agent, and more particularly to a vision improving agent containing an iodine compound as an active ingredient.

BACKGROUND ART Drugs containing iodine and iodine compounds have been widely used for disinfecting the skin, sterilizing and disinfecting wounds and ulcers, and various improvements have been made. Furthermore, drugs containing iodine compounds are used for the prevention and treatment of various diseases.

For example, Patent Document 1 discloses a sodium iodide-containing preparation consisting of a weakly alkaline solution with a hydrogen ion concentration of 7 to 8 and containing sodium iodide in an amount equivalent to 1.0% to 1.5% by weight as an iodine content. It has been reported that it has preventive and therapeutic effects against cancer and AIDS.

Patent Document 2 describes an alkaline ionized water containing 3% to 5% by weight of organic iodine in terms of hydrogen iodide, 1 to 3% by weight of sodium hydroxide, and the balance containing a trace amount of hydrogen peroxide, A liquid preparation is disclosed, which is a weakly alkaline colloidal solution with a pH of 7 to 8, in which sodium hydroxide is dissolved and organic iodine is colloidally dispersed in alkaline ionized water, and it has preventive and therapeutic effects on cancer and AIDS. It is reported that there is.

Patent Document 3 discloses a liquid preparation in which 1000 ppm or more of liquiritigenin is added to an aqueous solution containing 0.1% to 4% by weight of organic iodine in terms of potassium iodide and/or hydrogen iodide. It is said to be effective as an anticancer and antiviral agent.
The liquid preparation described in Patent Document 3 is said to have extremely low side effects such as iodine poisoning and to have a high synergistic effect in preventing and treating cancer and viral infections by using organic iodine and liquiritigenin in combination.

Patent Document 4 discloses a preparation for treating bedsores, skin ulcers, and wounds that contains gelatin, saccharides, and iodophor as essential ingredients, and such a preparation is said to be particularly effective for treating bedsores.

US Pat. No. 5,001,201 discloses a composition for the therapeutic treatment of iodine deficiency diseases in human patients, comprising a pure aqueous solution of a specific amount of elemental iodine (I ₂ ), such formulations being used to treat breast cancer, intrauterine cancer, etc. It is said to be effective in preventing and treating membranous disease and premenstrual syndrome.

Patent Document 6 discloses an aqueous disinfectant for vaginal and oral mucosa characterized by containing a specific amount of simple iodine or/and an alkali metal salt of iodine. It is said to have excellent safety against viruses and sufficient virucidal effects.

Patent Document 7 discloses a sterilizing disinfectant composition that is an aqueous or alcoholic aqueous solution containing hydroxypropylcellulose, iodine, and iodide.
In the disinfectant composition of Patent Document 7, the amounts of hydroxypropylcellulose and iodide added can be changed within a relatively wide range, so the amount or concentration of free iodine and bound iodine in the product can be adjusted. It can be set at an appropriate value depending on the application, and can be formulated as a gargle, eye drops, nasal drops, shampoo, etc., and is said to have a wide range of applications.

Patent Document 8 discloses a composition for treating pressure ulcers and skin ulcers, which comprises a non-reducing sugar, povidone-iodine, water, a solubilizing agent, a shape preservation agent selected from polysaccharides, glycerin, and other additives.
The composition of Patent Document 8 is said to have excellent extensibility, no foreign body feeling, and excellent feeling in use.

Non-Patent Document 1 discusses the various medicinal effects of iodine, stating that triiodide ion (I ₃ ^- ), which is generated when iodine is hydrated, acts as an excellent antioxidant within cells and acts as an antioxidant around cell membranes. A theory has been proposed that it removes hydroxyl radicals.

As described above, iodine and iodine compounds are used for various purposes, and their safety has also been thoroughly studied. It is desired to take advantage of the advantages of iodine and iodine compounds and use them more effectively.

Japanese Patent Application Publication No. 2004-315470 Japanese Patent Application Publication No. 2008-143808 Japanese Patent Application Publication No. 2010-265209 Japanese Patent Application Publication No. 2001-122790 Special Publication No. 4-503949 Japanese Patent Application Publication No. 6-172192 Japanese Unexamined Patent Publication No. 4-182431 Japanese Patent Application Publication No. 9-40563

Shozo Yanagida Production and Technology Vol.69, No.3, pp.32-39(2017)

The present invention has been made in view of the above-mentioned background art, and its object is to provide a highly safe vision improving agent.

As a result of intensive studies to solve the above-mentioned problems, the inventors of the present invention have found that a drug containing an iodine compound as an active ingredient not only has conventional effects such as disinfection and sterilization, but also has a visual improvement effect. The present invention was completed based on this discovery.

That is, the present invention provides a visual improvement agent characterized by containing an iodine compound as an active ingredient.

The vision improving agent of the present invention contains as an active ingredient an iodine compound that has been conventionally used for disinfection, sterilization, etc., and is highly safe and has few side effects. Therefore, the vision improving agent of the present invention has a wide range of applications.

In particular, the vision improving agent of the present invention contains an iodine compound that has disinfecting and bactericidal properties, so it is useful for patients with eye diseases such as dry eyes, glaucoma, age-related macular degeneration, allergic conjunctivitis, and cataracts. By administering it, it can be used to disinfect and sterilize as well as improve vision.

This is the contrast sensitivity of both eyes of the subject in Example 1 (7 days after the start of administration of the vision improving agent). This is the contrast sensitivity of both eyes of the subject in Example 1 (33 days after the start of administration of the vision improving agent). This is the contrast sensitivity of both eyes of the subject in Example 1 (76 days after the start of administration of the vision improving agent).

The present invention will be described below, but the present invention is not limited to the following embodiments and can be implemented with arbitrary modifications.

The vision improving agent of the present invention contains an iodine compound as an active ingredient.

"Visual improvement agent" refers to an agent that has the effect of improving the vision of the subject (patient, etc.) to whom it is administered. "Visual vision" improved by the vision improving agent of the present invention includes visual acuity, contrast sensitivity, color vision, glare, and the like.
Further, "visual acuity" includes static visual acuity, dynamic visual acuity, depth visual acuity, central visual acuity, non-central visual acuity, and the like.

"Improving" vision by the vision improving agent of the present invention may mean improving vision that has deteriorated due to aging, disease, etc. to its original state (or in a direction approaching its original state); It may be to further improve the original state.
The vision improving agent of the present invention contains an iodine compound that has disinfecting and bactericidal properties, so it can be administered to patients suffering from eye diseases such as dry eye, glaucoma, age-related macular degeneration, allergic conjunctivitis, and cataracts. This makes it particularly suitable for administration to patients with eye diseases, as it can disinfect and sterilize while improving vision at the same time.

The iodine compound contained in the vision improving agent of the present invention is not particularly limited, but includes alkali metal salts such as sodium iodide, potassium iodide, and lithium iodide; glycerin, polyvinyl alcohol, povidone (polyvinylpyrrolidone), lecithin, and cod liver oil. Examples include iodine compounds that are derivatives of , draconic, creosote, and the like.
These iodine compounds may be used alone or in combination of two or more.

The vision improving agent of the present invention desirably contains an alkali metal salt of iodine.
In this case, it is particularly desirable to contain only an alkali metal salt of iodine as the iodine compound, although the case where other iodine compounds are contained is not excluded.

Moreover, it is preferable that the vision improving agent of the present invention contains both sodium iodide and potassium iodide among the alkali metal salts of iodine.
In this case, it is particularly desirable that the visual improvement agent of the present invention contains only sodium iodide and potassium iodide as the iodine compound, although it is not excluded that it contains other alkali metal salts of iodine.

When the iodine compound as the active ingredient in the vision improving agent of the present invention is an alkali metal salt of iodine, especially when it is sodium iodide and potassium iodide, even if the iodine content in the vision improving agent is increased, the iodine It can be made into a highly safe drug that is less likely to cause toxicity and exhibits a sufficient visual improvement effect.

When the vision improving agent of the present invention contains both sodium iodide and potassium iodide, the content of sodium iodide per 1 part by mass of potassium iodide is preferably 0.5 parts by mass or more, and 1 part by mass. It is more preferably at least 2 parts by mass, particularly preferably at least 2 parts by mass. Moreover, it is preferably 30 parts by mass or less, more preferably 20 parts by mass or less, and particularly preferably 10 parts by mass.
When sodium iodide and potassium iodide are contained in the above ratio, toxicity is unlikely to occur even if the iodine content is high, and the visual improvement effect is likely to be sufficiently exhibited.

The content of the iodine compound in the vision improving agent of the present invention is preferably 0.1% by mass or more as iodine, more preferably 0.5% by mass or more, and particularly preferably 1% by mass or more. preferable. Moreover, it is preferably 20% by mass or less, more preferably 15% by mass or less, and particularly preferably 10% by mass or less.
When the content of the iodine compound as iodine is at least the above-mentioned lower limit, the visual improvement effect is sufficiently exhibited. Moreover, when the content is below the above upper limit, safety can be ensured and costs can be easily suppressed.

The vision improving agent of the present invention may contain hydrogen peroxide (H ₂ O ₂ ).
The content of hydrogen peroxide in the vision improving agent of the present invention is preferably 1 x 10 ^-9 mass % or more, more preferably 1 x 10 ^-8 mass % or more, and 1 x 10 ^-7 mass %. % or more is particularly preferable. Moreover, it is preferably 1×10 ⁻⁴ mass % or less, more preferably 1×10 ⁻⁵ mass % or less, and particularly preferably 1×10 ⁻⁶ mass % or less.
When the content of hydrogen peroxide is within the above range, the iodine compound tends to be in a colloidally dispersed state, and the visual improver is less likely to cause toxicity.

The vision improving agent of the present invention may contain hydrogen.
The hydrogen content in the vision improving agent of the present invention is preferably 1 ppb or more, more preferably 10 ppb or more, particularly preferably 100 ppb or more. Moreover, it is preferably 1.5 ppm or less, more preferably 1.3 ppm or less, and particularly preferably 1 ppm or less.

There is no particular limitation on the method of administering the vision improving agent of the present invention, and examples include eye drops, injection, inhalation, oral administration, and application, but eye drops are preferred as the method of administration is more likely to exhibit the effects of the present invention.

The vision improving agent of the present invention is preferably in a liquid form such as a solution or suspension.
The solvent of the solution and the dispersion medium of the suspension desirably contain water, and it is particularly desirable that water be the main component. The solvent and the dispersion medium may contain ethanol, 1-propanol, 2-propanol, etc. in addition to water.

The content of water in the solvent or the dispersion medium is preferably 50% by mass or more, more preferably 70% by mass or more, and particularly preferably 90% by mass or more. Moreover, it is preferably 100% by mass or less, more preferably 99% by mass or less, and particularly preferably 98% by mass or less.

The vision improving agent of the present invention is preferably alkaline. Specifically, the vision improving agent of the present invention preferably has a pH of 8 or higher, more preferably 9 or higher, and particularly preferably 10 or higher. Further, it is preferably 13 or less, more preferably 12.5 or less, and particularly preferably 12 or less.
Since the vision improving agent of the present invention is alkaline, it tends to have good storage stability. In particular, when the pH is above the above lower limit and below the above upper limit, this effect tends to be more pronounced.

By using a pH adjuster, the pH of the vision improving agent of the present invention can be adjusted within the above range. Examples of pH adjusting agents for lowering the pH include hydrochloric acid, acetic acid, and sulfuric acid. Examples of pH adjusters for increasing pH include sodium hydroxide, potassium hydroxide, and the like.

When the vision improving agent of the present invention is an eye drop, as mentioned above, even if the pH is alkaline, the pH will be around 7 (neutral) at the moment it enters the eye due to the buffering properties of tear fluid. becomes.

The visual improvement agent of the present invention may contain additives such as isotonic agents, cooling agents, thickeners, preservatives, stabilizers, buffers, surfactants, etc., to the extent that the effects of the present invention are not impaired. It can be added as appropriate.

Examples of the tonicity agent include sodium chloride, potassium chloride, glycerin, propylene glycol, and the like. These may be used alone or in combination of two or more.

Examples of the cooling agent include menthol, borneol, camphor, and the like. These may be used alone or in combination of two or more.

Examples of the thickener include polyvinyl alcohol, methylcellulose, hydroxypropylmethylcellulose, hydroxyethylcellulose, polyvinylpyrrolidone, sodium chondroitin sulfate, alginic acid, and carboxyvinyl polymer. These may be used alone or in combination of two or more.

Examples of preservatives include benzalkonium chloride, benzethonium chloride, methyl paraoxybenzoate, chlorobutanol, and sorbic acid. These may be used alone or in combination of two or more.

Examples of the stabilizer include citric acid, sodium sulfite, sodium edetate, polyvinylpyrrolidone, and polysorbate 80. These may be used alone or in combination of two or more.

Examples of the buffer include boric acid, phosphoric acid, citric acid, acetic acid, aspartic acid, and salts thereof. These may be used alone or in combination of two or more.

Surfactants include polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, alkyldiaminoethylglycine, lauryldimethylaminoacetic acid betaine, alkyl sulfate, polyoxyethylene alkyl ether phosphate, polyoxyethylene alkyl ether sulfate. Examples include salts, alkylpyridinium salts, and alkylamine salts. These may be used alone or in combination of two or more.

The dosage of the vision improving agent of the present invention is not particularly limited and can be appropriately selected depending on the age, body weight, degree of desired effect, etc. of the individual to be administered.
For example, the daily dosage for adults is preferably 1 μg or more, more preferably 10 μg or more, particularly preferably 100 μg or more. Further, the amount is preferably 20 mg or less, more preferably 5 mg or less, and particularly preferably 1 mg or less.

The frequency of administration of the vision improving agent of the present invention is also not particularly limited, but it is preferably administered once every three days or more, more preferably once a day or more, and particularly preferably three times or more a day. Further, it is preferably 30 times or less a day, more preferably 20 times or less a day, and particularly preferably 10 times or less a day.

The vision improving agent of the present invention can be applied to improving the vision of healthy individuals as well as patients suffering from eye diseases.
There is no particular restriction on the timing of administration of the vision improving agent of the present invention, and it can be appropriately selected depending on the purpose. When administered to a patient suffering from an eye disease or the like, it may be administered prophylactically or therapeutically.

Although the action and principle by which the vision improving agent of the present invention exhibits the excellent hypoglycemic effect is not clear, the following is presumed. However, the present invention is not limited to the scope of the operation and principle estimated below.

The vision improving agent of the present invention contains an iodine compound as an active ingredient. Although the action and principle by which the vision-improving agent of the present invention exerts the vision-improving effect is not clear, the hydrated iodine compound acts as an antioxidant, removes hydroxyl radicals, and activates intracellular mitochondria. It is believed that this treatment revives dead eye cells and improves vision.

EXAMPLES The present invention will be described in more detail below with reference to Examples and Comparative Examples, but the present invention is not limited to these Examples unless the gist thereof is exceeded.

Example 1
Visual Improving Agent 1 containing the following components was prepared. The pH of Visual Improver 1 was 11.9.

・Water: 97.8 parts by mass ・Sodium iodine: 2.1 parts by mass ・Potassium iodine: 0.8 parts by mass ・pH adjuster and other additives: appropriate amount

Visual Improving Agent 1 was administered to a subject (a 68-year-old male) by instilling several drops into both eyes several times a day (one drop is approximately 0.05 mL).

The visual acuity of the right eye (Vd) and the visual acuity of the left eye (Vs) of the subject measured before the start of administration of Vision Improvement Agent 1 were as follows.
Vd: 0.15 (1.2×-1.00D:cyl-1.50DA×60°)
Vs: 0.09 (1.0×-1.50D:cyl-0.75DA×110°)

On the other hand, the visual acuity of the subjects measured 76 days after the start of administration of Visual Improving Agent 1 was as follows, and it was confirmed that visual acuity was improved by administration of Visual Improving Agent 1.
Vd: 0.4 (1.2×-0.50D:cyl-2.00DA×60°)
Vs: 0.4 (1.2×-1.75D:cyl-0.75DA×120°)

In addition, the contrast sensitivity of both eyes of the subjects was measured using a contrast sensitivity measuring device CSV-1000 (manufactured by Vector Vision) 7 days, 33 days, and 76 days after the start of administration of the vision improving agent 1.
The results are shown in Figure 1 (after 7 days), Figure 2 (after 33 days), and Figure 3 (after 76 days).

In FIGS. 1 to 3, the broken lines indicate the measured contrast sensitivity of the subject, and the dense vertical lines indicate the normal range of contrast sensitivity.
As the number of days of administration of Visual Improving Agent 1 progressed, the contrast sensitivity of the subjects approached the normal range, and improvement in contrast sensitivity was confirmed.

Example 2
Visual Improving Agent 2 having a pH of 8.1 was prepared in the same manner as in Example 1, except that the pH adjuster added to the visual improving agent was changed.

When Visual Improving Agent 2 was continuously administered to the test subjects, improvements were seen in the test subjects' visual acuity and contrast sensitivity as the number of days of administration progressed.

The vision improving agent of the present invention has as an active ingredient an iodine compound that has been conventionally used for disinfection and sterilization, and is highly safe and has few side effects. It can also be applied to improve the vision of patients suffering from eye diseases such as glaucoma, age-related macular degeneration, allergic conjunctivitis, and cataracts.

Claims (8)

A visual improvement agent characterized by containing an iodine compound as an active ingredient. The vision improving agent according to claim 1, which contains the iodine compound in a proportion of 0.1% by mass to 20% by mass as iodine. The vision improving agent according to claim 1, which is alkaline. The visual improvement agent according to claim 3, which has a pH of 8 or more and 13 or less. The vision improving agent according to claim 1, wherein the daily dose for adults is 1 μg or more and 20 mg or less. The vision improving agent according to claim 1, which is administered at a frequency of administration at least once every 3 days and at most 30 times a day. The visual improvement agent according to any one of claims 1 to 6, which contains an alkali metal salt of iodine. The visual improvement agent according to claim 7, which contains sodium iodide and potassium iodide, and has a content of sodium iodide of 0.5 parts by mass or more and 30 parts by mass or less with respect to 1 part by mass of potassium iodide.

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