JPH08133968A - Ophthalmic preparation for repairing corneal damage - Google Patents

Abstract

PURPOSE: To obtain an ophthalmic preparation high in the effect on repairing the corneal damage and safe when continuously used. CONSTITUTION: This ophthalmic preparation for repairing corneal damage contains (a) sodium chloride, potassium chloride and sodium bicarbonate and (b) 0.5-3wt.% of taurine, and has a pH of 5.5-8.0 and a osmotic pressure of 250-450mOsm.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an ophthalmic solution containing a specific inorganic salt and taurine for the purpose of repairing corneal disorders.

[0002]

2. Description of the Related Art Corneal disorders are caused by wearing contact lenses, ultraviolet rays, dry eyes, etc. In the past, in repairing such corneal disorders, artificial tear fluid composed of boric acid, sodium chloride, potassium chloride, calcium chloride, etc. Was used.

[0003]

However, in the conventional techniques, the effect of repairing corneal disorders is not sufficient or there is a problem in safety. An object of the present invention is to provide an eye drop which has a high effect of repairing a corneal disorder and is safe even when continuously applied.

[0004]

As a result of intensive studies, the present inventors have found that sodium bicarbonate and taurine synergistically enhance the corneal lesion repairing effect in eye drops containing certain specific inorganic salts and taurine. Then, the present invention was completed. That is, the present invention provides (a) sodium chloride,
It contains potassium chloride and sodium hydrogen carbonate, and (b) taurine 0.5 to 3% by weight, and has a pH of 5.5 to 8.0.
And an osmotic pressure of 250 to 450 mOsm for repairing corneal disorders. In the present invention, the effect of the present invention cannot be obtained with an ophthalmic solution from which either the component (a) or the component (b) has been removed, and the same applies to an ophthalmic solution having a pH or osmotic pressure outside the above range. Is.

Further, it is preferable to blend glucose in addition to the above components (a) and (b) in order to further enhance the effects of the present invention. pH 6.5-7.5, osmotic pressure 2
It is preferably in the range of 50 to 350 mOsm, and p
Most preferred is H7.4, osmotic pressure 286 mOsm.

In the eye drop of the present invention, the inorganic salt containing the component (a), the component (b) and preferably glucose are dissolved in sterile purified water in an amount such that the osmotic pressure is 250 to 450 mOsm, and the pH is adjusted. PH with agents (eg borax, citric acid, sodium citrate, hydrochloric acid, sodium hydroxide, etc.)
It can be easily prepared by adjusting it to 5.5 to 8.0.

In the present invention, in addition to the above essential components, if necessary, anti-inflammatory agents (eg dipotassium glycyrrhizinate, epsilon aminocaproic acid, allantoin, berberine chloride, berberine sulfate, sodium azulene sulfonate, zinc sulfate, zinc lactate). , Lysozyme chloride, etc.),
Antihistamines (eg diphenhydramine hydrochloride, chlorpheniramine maleate, etc.), decongestants (naphazoline hydrochloride, tetrahydrozoline hydrochloride, phenylephrine hydrochloride, etc.), various vitamins [eg active vitamin B
₂ (flavin adenine dinucleotide sodium),
Vitamin B ₆ (pyridoxine hydrochloride), Vitamin B ₁₂ (cyanocobalamin), Vitamin A acetate (retinol acetate), Vitamin E acetate (tocopherol acetate), panthenol, calcium pantothenate, sodium pantothenate, etc.], amino acids (L- Magnesium magnesium aspartate, potassium L-aspartate, magnesium L-aspartate, sodium chondroitin sulfate, etc., a cooling agent (eg menthol,
Borneol, camphor, peppermint oil, etc.), polymer additives (eg polyhydric alcohol, polyvinyl alcohol, polyvinylpyrrolidone, methylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose etc.), stabilizers (eg ethylenediaminetetraacetate etc.), preservatives (Bensalkonium chloride, methylparaben, sorbic acid, etc.), various components usually used for the preparation of eye drops such as sulfa and other active ingredients can be added within a range that does not impair the effects of the present invention.

[0008]

INDUSTRIAL APPLICABILITY The ophthalmic solution of the present invention acts synergistically on the damaged cornea of sodium bicarbonate and taurine. Moreover, since no eye irritating component such as boric acid is used, it is safe to instill continuously. Therefore, the present invention makes it possible to provide an eye drop useful for repairing corneal disorders.

Hereinafter, the superiority of the present invention will be specifically shown with reference to test examples. Test Example It has been reported that measuring the amount of LDH in tears is effective in determining the degree of corneal damage (Chem. Pharm.
Bull., Volume 41 (2), pp. 335-338, 1993). (Test method) Ultraviolet irradiation of rabbit cornea Eight rabbits (Japanese white rabbit, male, 5 months old, weight 2.4 to 3.0 kg) were fixed, and the cornea was irradiated with ultraviolet rays (UV-B) for 10 minutes ( 75
0 to 800 μW / cm ² ). The ophthalmic solution prepared in Example 2 was applied to the right eye for 5 days (3 drops a day, 4 times a day). The left eye was non-instilled. Measurement of lactate dehydrogenase (LDH) LDH leakage was measured before, immediately after, and 1 to 5 days after irradiation of ultraviolet rays. The measurement is normal saline 250
μl eye drop, pool for 1 minute, then 50 μl
Sampling the
zer, manufactured by HITACHI).

(Results) The results are shown in Table 1. A decrease in the amount of LDH leakage was observed by instilling the eye drop prepared in Example 2 2 and 4 days after the ultraviolet irradiation. That is, when the ophthalmic solution prepared in Example 2 was applied, the total LDH immediately after the ultraviolet irradiation to 5 days after the ultraviolet irradiation was reached.
The leakage was significantly reduced. This confirmed the effect of the eye drops of the present invention for repairing corneal disorders.

[0011]

[Table 1]

[0012]

EXAMPLES The present invention will be described in more detail with reference to examples. (Example 1) Taurine 1000 mg, sodium chloride 5
57 mg, potassium chloride 106 mg, calcium chloride 1
1 mg, magnesium sulfate 15 mg, sterile purified water 90 m
After dissolving in 1 and adjusting the pH to 7.4 with borax, sterile purified water was added to bring the total volume to 100 ml to prepare an eye drop. The osmotic pressure of this ophthalmic solution was measured and found to be 286 mOsm.
Met.

(Example 2) 1000 mg of taurine, 480 mg of sodium chloride, 91 mg of potassium chloride and 151 mg of sodium hydrogen carbonate were dissolved in 90 ml of sterile purified water, and the pH was adjusted to 7.4 with hydrochloric acid, and then sterile purified water was added. The total amount was 100 ml and an eye drop was prepared. As a result of the measurement, the osmotic pressure of this ophthalmic solution was 286 mOsm.

(Example 3) 1000 mg of taurine, 542 mg of sodium chloride, 103 mg of potassium chloride, 11 mg of calcium chloride, 14 mg of magnesium sulfate and 100 mg of glucose were dissolved in 90 ml of sterile purified water, and the pH was adjusted to 7.4 with borax. Then, sterile purified water was added to bring the total volume to 100 ml to prepare an eye drop. As a result of the measurement, the osmotic pressure of this ophthalmic solution was 286 mOsm.

(Example 4) 1000 mg of taurine, 467 mg of sodium chloride, 89 mg of potassium chloride, 146 mg of sodium hydrogen carbonate and 100 mg of glucose were dissolved in 90 ml of sterilized purified water, and the pH was adjusted to 7.4 with hydrochloric acid, and then sterilized purified water. Was added to bring the total volume to 100 ml to prepare an eye drop. The osmotic pressure of this ophthalmic solution was measured and found to be 28
It was 6 mOsm.

(Example 5) Taurine (1000 mg), sodium chloride (472 mg), potassium chloride (90 mg), calcium chloride (9 mg), magnesium sulfate (12 mg) and sodium hydrogen carbonate (148 mg) were dissolved in sterile purified water (90 ml).
After adjusting the pH to 7.4 with hydrochloric acid, sterile purified water was added to bring the total volume to 100 ml to prepare an eye drop. As a result of the measurement, the osmotic pressure of this ophthalmic solution was 286 mOsm.

(Example 6) 1000 mg of taurine, 459 mg of sodium chloride, 87 mg of potassium chloride, 9 mg of calcium chloride, 12 mg of magnesium sulfate, 144 mg of sodium hydrogen carbonate and 100 mg of glucose were dissolved in 90 ml of sterile purified water, and the pH was adjusted to 7.4 with hydrochloric acid. Then, sterile purified water was added to adjust the total volume to 100 ml to prepare an eye drop. The osmotic pressure of this ophthalmic solution was measured and found to be 286
It was mOsm.

(Example 7) Taurine (1000 mg), sodium chloride (397 mg), potassium chloride (75 mg) and sodium hydrogencarbonate (125 mg) were dissolved in sterile purified water (90 ml), the pH was adjusted to 7.4 with hydrochloric acid, and then sterile purified water was added. The total amount was 100 ml and an eye drop was prepared. The osmotic pressure of this ophthalmic solution was measured and found to be 250 mOsm.

Example 8 Taurine (1000 mg), sodium chloride (860 mg), potassium chloride (163 mg) and sodium hydrogencarbonate (271 mg) were dissolved in sterile purified water (90 ml), the pH was adjusted to 7.4 with hydrochloric acid, and sterile purified water was added. The total amount was 100 ml and an eye drop was prepared. As a result of the measurement, the osmotic pressure of this eye drop was 450 mOsm.

Claims (2)

[Claims] 1. (a) Sodium chloride, potassium chloride and sodium hydrogen carbonate, and (b) Taurine 0.5 to 3
An ophthalmic solution for repairing corneal disorders, which contains the weight% and has a pH of 5.5 to 8.0 and an osmotic pressure of 250 to 450 mOsm. 2. (a) Sodium chloride, potassium chloride and "one or more inorganic salts selected from the group consisting of sodium hydrogen carbonate, magnesium sulfate and calcium chloride", (b) Taurine 0.5 to 3 An ophthalmic solution for repairing a corneal disorder, which contains wt% and (c) glucose and has a pH of 5.5 to 8.0 and an osmotic pressure of 250 to 450 mOsm.