KR930011995B1 - Composition for treatment of cataract - Google Patents

Abstract

The compsn. is compsd. of galangin, and the content of galangin is pref. 0.01-20 W/W %. Tablets and Ointment are made from this compsn. and administered to cataract patients. The compsn. has therapeutic effect for cataract and no side effects.

Description

Cataract Treatment Composition

The present invention relates to a novel cataract treatment composition comprising galangin as an active ingredient.

Cataract is a disease of the eye in which the lens of the lens (cloud) located between the anterior chamber and the vitreous body of the eye becomes cloudy. The lens causes light to focus on the retina, which detects the light and delivers it to the brain in the form of visual impulse. Thus, cataracts are accompanied by deterioration of vision and, in severe cases, blindness.

Until recently, it has generally been thought that the best treatment for cataracts is surgical removal of the lens and implantation of the intraocular lens. Beneficial results during drug treatment include catalin (Nevyas H.J., Ocular Size and Shape, Regulation During Development. (Eds., Hilfer S.R. and Sheffield J.B.), Springer-Verlag, New York, pp. 189-207, 1980]. Aspirin (Hayashi, H. and Nishida, T., The Folia Ophthalmologica Japonica, Vol. 30, No. 4, 1979) has been reported to slow the progression of cataracts. Bendazac, which has high anti-denaturing activity on blood proteins, is also useful for cataract reduction (US Pat. No. 4,451,477). 5-hydroxy bendazac, one of the metabolites of bendazac, can also be used to treat cataracts. Is reported to be high (European Patent 0191520). Other 2- (3,7,11,15-tetramethyl-2,6,10,14-hexadecatetraenyl) -1,3,5-trihydroxybenzene (JP-1226809), (hydroxy Phenyl) thiazoline carboxylic acid (JP-61005015) has been reported as a cataract agent, and recently, isocitric acid and its salts (JP-2062821), and racematol and its derivatives (WO-9013291) are cataracts. It has been reported as a drug.

However, although these drugs have been reported, treatment for cataracts has generally been thought to be the best to surgically remove the lens, implant the intraocular lens and replace its function. Therefore, various efforts are being made to develop new cataracts with higher efficacy.

Recently, attention has been paid to the study that reactive oxygens and free radicals are related to aging. In other words, the oxidative damage of the constituents of the lens is closely related to the formation of cataracts, and antioxidant substances that prevent the oxidative damage are being confirmed dermatologically and clinically. In particular, bend azac and others have been reported to be due to the reaction with the most powerful active oxygen hydroxy radical (Mira, ML, Azevedo, MS and Manso, C., The neutralization of hydroxy radical by silibin, sorbinil, and bendazac , Free Rad.Res. Comms, 4; 125-129, 1987) 5-hydroxybendazak strongly reduces diphenyl picryl hydrazyl (DPPH) free radicals and is very effective in inhibiting butyl peroxide-induced erythrocyte hemolysis (Alison CS Woollard, Simon P. Wolff, and Zainab A.Bascal, Antioxidant characteristics of some potential anticataract agents, Free Radical Biology & Medicine, Vol 9, pp 299-305, 1990).

Therefore, the inventors have found that there may be a useful cataract among the substances showing sulfate action by scavenging free radicals and free radicals. In particular, the present inventors pay attention to flavonoids, which are known as sulfate components of plants. Proceeded.

The present invention relates to a new composition for treating cataracts using galangin, which is a kind of flavonoid component of a plant, as an active ingredient. Flavonoids are plant constituents that vary in type and content depending on the plant. The role of flavonoids in plants is controversial, but sulfated action is known to be one of the most important roles. Among the flavonoids, various physical and chemical properties vary depending on their structure, and many of them show special physiological activities. Among the flavonoids are the singlet oxidants, as well as the high oxidant scavenging hydroxyl radicals (S. Rafat Husain, Josiane Cillard and Pierre Cillard, Hydroxyl radical scavenging activity of flavonoids) , phytochemistry, vol. 26, pp 2489-2491, 2987) and some have high free radical scavenging activity (Wolf Bors and Manfred Saran, Radical Scavenging by flavonoid antioxidants, Free Rad, Res. Comms., vol 2, pp 289-294) (1987) There have been reports of effective defense against erythrocyte hemolysis induced by singlet oxidase (Yasuhiro Sorata, Umeo Takahama and Misutaka Kimura, protective effect of quercetin and rutin on photosensitized lysis of human erythrocytes in the presence of hematoporphyrin , Biochimica et Biophysica Acta, 799 (1984) 313-317).

Accordingly, the inventors of the present invention are contemplated that there may be a useful component as a composition for treating cataract among flavonoid components of plants and searched and evaluated the inhibitory ability against singlet oxygen-induced erythrocyte hemolysis of a plurality of flavonoid components. Briefly describing the experimental method, red blood cells were dispersed in a buffer solution (15 million red blood cells / ml), rosebengal was added to a concentration of 1.5 μM, and the fluorescent lamp was split to generate singlet oxygen. Under this condition, the average human erythrocytes were hemilyzed in half within 32 minutes. This appears to be due to the singlet oxytransition promoted peroxidation of cell membrane lipids. However, erythrocytes treated with various flavonoids at a concentration of 50 μM significantly prolonged the time for hemolysis, and found that galangin's singlet oxygen-induced erythrocyte hemolysis was very potent. Galangin had a haemolysis time of 1800 min for red blood cells treated at 50 μM. On the other hand, aspirin had little inhibitory effect on hemolysis even when treated at 100 μM. The inventors predicted that galangin, which is very potent in inhibiting singlet oxygen-induced erythrocyte hemolysis, would be effective for cataracts, and continued research to develop a composition for treating cataracts after undergoing animal and clinical trials. It has led to the development of highly novel cataract treatment compositions.

The present invention relates to a composition for treating cataracts, comprising as an active ingredient, galangin, a vegetable flavonoid component. Galangin is a completely new ingredient that has never been suggested or used as a cataract, and there are no more powerful cataracts. In the composition for treating cataracts of the present invention, the active ingredient galangin is contained in an amount of 0.01 to 20 ((w / w))%, and the composition is formulated in the form of tablets or ointments to be administered orally or parenterally. Can be. The composition for treating cataracts containing the galangin of the present invention shows an excellent effect of cataracts upon oral and parenteral administration, and almost no side effects occur. In the following examples will be described in more detail.

Example 1

Tablet

Galangin 4.0g

1.0 g of sodium citrate

10.0 g powdered lactose

1.0 g of hydroxypropyl cellulose

3.0 g of crystalline cellulose

1.0 g magnesium stearate

20.0 g of total

[quite]

Mix 4 g of galangin and 1 g of sodium citrate. This is kneaded using an aqueous solution of hydroxypropyl cellulose. 200 tablets are prepared by mixing crystalline cellulose and magnesium stearate, followed by compression.

Example 2

Ointment

Galangin 0.01g

Neobee M-5 20.00g

Soft yellow paraffin 79.99g

[quite]

Add 0.01 g of gallangin to 20 g of NeoBi M-5, dissolve by heating at 70 ° C. for 5 minutes, add 79.99 g of light yellow paraffin, mix for 5 more minutes, and cool at room temperature.

Experimental Example

The first 60 patients with cataracts were divided into 2 groups of 30 people, and the first group took tablets (Example 1) once a day for 3 months (active ingredient 20mg gallangin / 1 day), and the second group was an ointment (Example 2) Was administered directly to the eye 100 mg three times a day, each time (active ingredient about 0.03 mg galangin / day). After 3 months, visual acuity and lens transparency were compared. The results are summarized in Table 1. Both tablets and ointments showed excellent cataract improvement and no side effects were observed.

TABLE 1

Claims (2)

A composition for treating cataracts, comprising galangin as an active ingredient. The composition of claim 1, wherein the content of the active ingredient is 0.01 to 20.0 (w / w)%.