JP2807535B2 - Cataract treatment - Google Patents

Description

The present invention relates to a useful cataract treatment agent. More specifically, the present invention relates to a useful cataract remedy comprising cysteinol (chemical name: R-2-amino-3-mercaptopropanol) or a pharmacologically acceptable salt thereof as an active ingredient.

[Prior Art] Cataract is a disease in which the lens becomes opaque for various reasons. For example, senile cataract and cataract caused by drugs such as steroids are known.

In addition, when a person has suffered from diabetes for a long period of time without improving his general condition, he often develops diabetic cataract, which is one of the typical complications. In the worst case, cataracts can lead to blindness and require cataract surgery to restore vision.

Conventionally, therapeutic agents for cataracts due to various causes such as senile cataract and diabetic cataract have been known, but at present, there is no drug which is sufficiently satisfactory in terms of its effects and the like.

[Problems to be solved by the invention]

Therefore, the present inventors have intensively searched for a compound having an excellent anticataract activity, and found that cysteinol or a pharmacologically acceptable salt thereof has an unexpectedly useful anticataract activity. Based on this new finding, the present invention has been completed.

[Means for solving the problem]

That is, the present invention relates to a useful cataract therapeutic agent comprising cysteinol or a pharmacologically acceptable salt thereof as an active ingredient.

The present compound used as an active ingredient for anti-cataract of the present invention is already known to have an anti-inflammatory effect, but its use as a therapeutic agent for cataract is not yet known.

The active ingredient of the present invention, cysteinol, is represented by the following formula.

HSCH ₂ CH (NH ₂ ) CH ₂ OH This compound can be prepared, for example, using Helvetica Chimica Acta Vol.
XLIV, III (1961) 706-709 or the like, or can be suitably synthesized according to the method.

The compound used as an active ingredient of the present invention may be a free compound or a pharmacologically acceptable salt. Examples of the salt include a hydrochloride, a sulfate, an oxalate, a citrate, a tartrate, a lactate, and the like, which can be used as appropriate according to the dosage form.

As already mentioned, senile cataract and diabetic cataract are known as cataracts, but the preparation of the present invention can be used orally or parenterally as appropriate for the treatment of those cataracts. . The form of the preparation can be appropriately prepared by any known method such as a solid preparation such as tablets, granules, powders and capsules or a liquid preparation such as syrups, elixirs, eye drops and injections. . These preparations generally include bulking agents, binders, wetting agents, disintegrating agents, lubricants, dispersants, flavoring agents, buffers, surfactants, solubilizing agents, preservatives, isotonic agents, and stabilizing agents. Excipients such as agents and pH adjusters may be used as appropriate.

The dose of the active ingredient varies depending on the age, body weight, dosage form, indications, etc. of the patient.For example, in the case of eye drops, several times a day for an adult, the dose is about 0.005 to 2.5 mg.
It is advisable to administer a daily dose of about 10 to 5000 mg for adults in several divided doses.

The drug of the present invention may appropriately contain other anti-cataract components and components having other types of medicinal effects, as long as the object of the present invention is not violated.

Hereinafter, the present invention will be described in detail with reference to Examples and Formulation Examples.

First, the effects of cysteinol on streptozotocin cataract, a representative model of cataract, are shown below.

[Example 1] Pharmacological test by oral administration of cysteinol for cataract Test substance: cysteinol hydrochloride A solution obtained by dissolving the bulk powder in pure water to 10% was used.

Experimental method: 4 weeks old SD rats were treated with 2 mM citrate buffer (pH 4.5).
Streptozotocin dissolved to 3.5% weight 1
0.2ml per 100g (Streptozotocin amount 70mg / k
g) was administered via the tail vein. The test substance was orally administered at a dose of 0.2 ml / 100 g twice a day from the day of streptozotocin administration (400 mg / kg / day). The control group was orally administered with pure water in the same manner.

Lens observation is performed every 7 days after the start of administration with mydriin P (Santen Pharmaceutical Co., Ltd.) and then with a slit lamp. The progress of cataract is evaluated according to the following scoring criteria.
The test was performed by test.

0 No opacity is observed in the lens.

I The lens surface is slightly opaque or small vacuoles appear at the equator.

II The number of vacuoles increases and spreads to the cortex while fusing.

III Vacuoles that have spread to much of the cortex begin to disappear.

IV Most of the vacuoles disappear and the entire cortex becomes translucent and turbid.

V The nucleoplasm becomes turbid.

VI The entire lens becomes cloudy (mature cataract).

Experimental Results: The frequency of cataract stage occurrence at each observation time point is shown in FIG.

At 7, 21, 28, 35 and 49 days after the start of administration, the cysteinol-administered group showed a significant cataract-retarding effect as compared to the control group.

[Formulation Example 1] Oral tablets Cysteinol hydrochloride 100 mg Lactose 80 mg Corn starch 20 mg Magnesium stearate 3 mg or more One tablet was molded by a conventional method.

[Formulation Example 2] Granules Cysteinol hydrochloride 100mg Polyvinylpyrrolidone 30mg Lactose 300mg [Formulation Example 3] Capsules Cysteinol hydrochloride 100mg Crystalline cellulose 50mg Lactose 50mg Talc 5mg More than 1 capsule material is mixed and filled in the usual way as a capsule material did.

[Formulation Example 4] Eye drops Cysteinol hydrochloride 100 mg Sodium chloride 800 mg Hydrochloric acid Appropriate amount Sodium hydroxide Appropriate amount Sterile purified water Appropriate amount Total amount 100 ml [Effect of the Invention] The preparation of the present invention effectively suppresses the progression of cataract, Useful as a therapeutic. In addition, the present preparation can be particularly advantageously used for diabetic cataract.

[Brief description of the drawings]

FIG. 1 shows the frequency of occurrence of the cataract stage. The left side of the bar graph shows the control group, and the right side shows the cysteinol hydrochloride group. The numbers in parentheses indicate%.

Claims (3)

(57) [Claims] 1. A cataract remedy comprising cysteinol or a pharmacologically acceptable salt thereof as an active ingredient. 2. The method for treating cataract according to claim 1, wherein the pharmacologically acceptable salt is a hydrochloride. 3. The method according to claim 1, wherein the administration route is oral.
Item 3. The cataract treatment agent according to item 2 or 2.