JPS61233622A - Eye lotion composition - Google Patents

Abstract

PURPOSE:To provide an eye lotion composition effective to prevent the degradation of acid mucopolysaccharide an useful for the remedy of cataract, etc., by compounding a group composed of an acid mucopolysaccharide, ascorbic acid and their salt and a group composed of tryptophan, histidine, uric acid, etc. CONSTITUTION:The objective composition contains (A) 0.01-5 wt% one or more compounds selected from acid mucopolysaccharide, ascorbic acid and their salts and (B) 0.001-1 wt% one or more compounds selected form tryptophan, histidine, uric acid and their salts. The depolymerization of acid mucopolysaccharide can be prevented even in the presence of a depolymerization acceleration factor such as ascorbic acid, metallic ion, etc., by the use of tryptophan, histidine, uric acid and their salts. Accordingly, the composition is effective for the remedy and prevention of eye diseases (e.g. catalact, glaucoma, etc.) caused by the chemical change in the acid mucopolysaccharide in the lens. It can be applied also as a preservation liquid for surgical operation of eye diseases.

Description

Detailed Description of the Invention [Industrial Application Field] The present invention provides a novel ophthalmic composition, more specifically, a novel ophthalmic composition containing one or two of acidic mucopolysaccharides, ascorbic acid, or salts thereof.
The present invention relates to an eye drug composition containing one or more of tryptophan, distyrene, uric acid, or salts thereof.

[Prior art and its problems] The mammalian eye lens contains acidic polysaccharides such as hyaluronic acid, chondroitin sulfate, and chondroitin, which play a role in maintaining the shape of the lens and forming a transparent vitreous body. However, it is known that ascorbic acid is present along with these acidic mucopolysaccharides. In addition, recent research has shown that senile eye diseases are thought to be caused by chemical changes in acidic mucopolysaccharides, and are closely related to aging phenomena, but there are currently few methods for preventing them.

Although this is an in-VitrO study, it has been confirmed that acidic mucopolysaccharides are significantly reduced in molecular weight by metal ions such as iron and copper present in living tissues (FFBSLETTER8).
96, 2, 238, 1978) Furthermore, the addition of ascorbic acid promotes the reduction of molecular weight (JOIIrnal
of l n0rjlantc B! 0CIIQII
I-istry 4, 135 (1981). However, in a normal crystalline lens, acidic mucopolysaccharide and ascorbic acid coexist, and although it is thought that metal ions are also contained, it is kept very stable.

In other words, the presence of a third component is inferred.

The present invention has been developed based on the fact that eye diseases such as cataracts and glaucoma are caused by acidic mucopolysaccharide, which exists in the eyeball, and ascorbic acid, and in particular, it is a component of the crystalline lens. Acid I11 Mucopolysaccharide hyaluronic acid, [chondroitin]1~[]idecine! is used to stabilize certain acidic mucopolysaccharides and to treat eye diseases and prevent σ, and is also used in eye medicines. IM, dermatan sulfate, l\valine, heparan sulfate, tunoraun sulfate, etc., d-3, etc.) Prevents the oxidative and photo-degradation of alkali metal salts and maintains its strength. 11-Continue / "Eye Function Key 1"
There are some people whose purpose is to have one.

[Means for solving the problem] As a result of examining this topic for the eyes, we found that (r+f-
F C, 1~rib 1 hefan, hisdecine, uric acid or their salts (by containing acid I'U)
: It was discovered that reducing the molecular weight of lx zr polysaccharide can be used for mountain prevention, and the present invention was completed.

The eye A of the present invention also has a composition IJ resistance 1 rim] polyi1J+knowledge, death. A) One or more of these salts and one or more of 1-ributophane, histidine, SR, or their salts (a) (for J-
4f from that.

Acidic mucopolysaccharides as used in the present invention include hyaluronic acid, chondroitin, chondroitin sulfate, dermatan sulfate, heparin, heparan sulfate, gratan sulfate, etc., and these salts, potassium, calcium, ammonium,
Ascorbic acid and its thorium, potassium, calcium salts, etc.) are mixed in an amount of 0.01 to 5% by weight.

If the amount is less than 0.01% by weight, the desired therapeutic or preventive effect cannot be obtained, and if it is more than 5% by weight, it is not necessary from the viewpoint of efficacy and economy.

In the present invention, tryptophan, histidine, uric acid, or its salts include tryptophan or its salts, including DL-1, 1--1, 1--1, and their hydrochlorides. , refers to nitrate, acetate, sulfate, and its salts include L-histidine and its hydrochloride, nitrate, vinegar MJi, and sulfate, and uric acid or its salts refers to 1et1, uric acid, uric acid]
・Rium, potassium urate, calcium urate, hydrogen urate±
1-lium, potassium hydrogen urate 1, calci hydrogen urate 1 cum, ammonium hydrogen urate, uric acid amino acid salt, uric acid amine salt, etc., added in an amount of 1110.01 to 1.0% by weight.
If the content is 0.01% by weight or more, the desired effect cannot be obtained, and if it is less than 1.0% by weight, it is unnecessary in terms of solubility and effectiveness.

In some cases, inorganic inorganic substances such as common salt and monolithium phosphate are added to eye drops in order to adjust the penetration level 1-f, but this does not affect the composition of the present invention in any way.

The 11-1 value of the composition of the present invention is preferably 4.0 to 8.0) and 6.0 to 7. It is desirable to maintain it at 0.

On the other hand, when the p l-1 value is less than 4.0 and the p l-1 value is more than 8.0, the irritation caused by the deterioration of the eye tissue is strong enough to make it difficult to use eye medicine. induce inflammation 1
．． 3. The ophthalmic composition of the present invention (1) Treatment of 1R disease induced by changes in intralenticular acid 11 mucopolysaccharide chemical properties such as cataracts and glaucoma; Although the present invention is used in the first stage, it can also be applied as an eye tissue preservation solution or an injection solution for maintaining the shape of eye tissue during eye disease surgery such as corneal transplant surgery.

The pharmaceutical composition of the present invention will be explained below using Examples and Experimental Examples.

Example 1. Cataract prevention eye medicine sodium hyaluronate lx 0.05% by weight
Chondroitin sulfate 1 helium 0, 5 On tryptophan hydrochloride 0.02 Chloride I~
Rium 2. QnSterilized purified water
97.43,.

Example 2. Healthy eye beauty agent Naphazoline hydrochloride 0.1% by weight] Chondroitin sulfate 1 helium i,o.

Sodium urate 0.1.

Salomethyl 0.2 Sodium chloride 2.0. 1 Sterile purified water
96,6, J Example 30 Surgical corneal drying preventive agent Sodium hyaluronate 0.3% by weight Pr1-Rium chloride 5. OI! J talk potassium 2.0!・Phosphoric acid water - Notorium 0,1 n boric acid
0.3 ・11p Shochu Tsuno Riu
11 0,0
3 NoIas] 1-rium lupine acid
0.2/I sterile purified water 92.
1! ! Example 4. =] Eye drops for contact lenses Hif))
[Potassium monophosphate 0.・2 Weight%1
--Histidine hydrochloride 0.111 As]l: 1 cum of dinic acid 0.11Ilp 1~Rium 2,0! ! Sterile purified water! 117.6! l Experimental Example 1 Age 23 - 25 50-year-olds who work in office work and experience eye strain every day or occasionally, including 6 women and 19 men, were given 1 pear of Example 2 1 to 2 times a day. Eye fatigue and hyperemia were investigated using drops before and after using the solution.

The product of the present invention showed remarkable effects on eye fatigue and hyperemia.

Experimental Example 2 Immediately after enucleating rat eyeballs, they were immersed in the aqueous solution prepared in Example 3, and the freshness and color tone of the eyeballs were examined.

The humidity was adjusted to pl-16.7 at 5°C.

Comparative Example 1 is a prepared solution obtained by removing sodium hyaluronate, uric acid, and helium from Example 3.

Comparative Example 2 is a prepared solution obtained by removing uric acid from Example 3.

The numbers in the table represent the number of individuals whose eyeballs had almost the same color tone from run 1 immediately after extraction.

Although the product of the present invention maintained good color tone even after 48 hours, Comparative Example 1 in which mono-lium hyaluronic acid and sodium urate were excluded
And Comparative Example 2 excluding sodium urate was 1! i1f i8
Only time culm could be saved.

Claims (1)

[Claims] 0.01 to 5% by weight of one or more selected from acidic mucopolysaccharides, ascorbic acid, or their salts, and 0.001 to 5% by weight of one or more selected from tryptophan, histidine, uric acid, or their salts. An eye drug composition containing 1% by weight.