JPH0386818A - Agent for preventing and treating cataract - Google Patents

Abstract

PURPOSE:To obtain a preventing and treating agent containing disophenol as an active ingredient, capable of safely, effectively and surely treating human and mammalian animal cataract and readily applicable. CONSTITUTION:The objective agent containing disophenol (2,6-diiodo-4- nitrophenol) being a medicine widely used as an excellent for tapeworm of dog as an active ingredient. When the agent is used, administration method by injection is most effective. The production of injection is carried out according to producing method of usual injection and, as necessary, pH controller, isotonic agent, buffer, etc., is added thereto. Disophenol is preferably administered subcutaneously in a dose of about 5-10mg per kg of patient and preferably injected once weekly. Furthermore, the agent is usable internally to mammalian animals.

Description

[Detailed description of the invention] [Industrial application field]

The present invention relates to a drug for preventing or treating cataracts in mammals and a method for preventing or treating cataracts in animals using such a drug.

[Conventional technology]

Cataracts in mammals, including humans, are an eye disease that is particularly common in old age, and if left untreated can lead to blindness.The prevention and treatment of cataracts has long been an important issue in the ophthalmology field, and various solutions have been developed since ancient times. is being considered. There are several types of cataracts, including senile cataracts, traumatic cataracts, combined cataracts, and diabetic cataracts.Moreover, the cause of hepatorenal cataracts has not been specifically clarified, so there is no way to prevent or treat them with drugs. There is no definitive solution, and in severe cases, surgery is performed to remove the crystalline lens, and an artificial crystalline lens,
Currently, there is no other option but to rely on surgical treatment such as inserting a so-called intraocular lens. In addition, mild symptoms are treated with drugs, but because the cause has not been identified, it is currently difficult to expect sufficient effects. Treatments for cataracts include eye drops such as pirenoxine (Catalin■), fucolidine■, and glutathione (Tathion■), and oral administration or injections of tiopronin (Thiola0) and salivary gland hormones (Parotin@). However, it is difficult to say that any of them are definitive. In addition, cataracts are not a disease that only occurs in humans, but are often observed in other mammals, and cataracts in pet animals have become a major problem for veterinary scientists as the number of pet lovers has increased in recent years. ing. Particularly noticeable are cataracts in small animals such as dogs and cats, which are extremely common eye diseases in older dogs and cats. For example, there are reports that over 6% of 7-year-old dogs, just under 60% of 10-year-old dogs, and over 70% of 11-year-old dogs have cataracts. In canine senile cataracts, lubricating opacity or strong milky white opacity under the anterior lens capsule inevitably occurs, and this is accompanied by axial opacity or posterior opacity in the lens cortex. Cataracts in these dogs are similar to those in humans, including traumatic cataracts, concurrent cataracts, and diabetic cataracts. However, the most common type of cataract in dogs is a primary cataract that has no specific cause, and because this symptom is more common in older dogs, it is called canine senile cataract. The frequency of primary cataracts in dogs has been shown to correlate well with the dog's age. Traditionally, this kind of dog cataract has the same symptoms as in humans.
No specific treatment is known, and the drugs used to treat cataracts in humans, such as those mentioned above, have been conveniently used for dogs with cataracts that visit veterinarians. Currently, no clear effects can be expected.

[Problem to be solved]

However, its effectiveness was very limited in both humans, dogs, and cats, and it could not be called a definitive treatment. In addition, several cataract therapeutic agents have been introduced, but none of them are sufficiently effective and have not yet been put to practical use. Therefore, the development of a drug that can accurately prevent and treat cataracts in humans and other mammals has been long-awaited not only in the medical community but also in the veterinary community.

[Means to solve the problem]

In view of the current situation, the present inventors have repeatedly investigated a number of drugs in order to develop effective and accurate preventive and therapeutic agents for cataracts. We have found that disophenol, which has been used for a long time, is extremely effective in preventing and treating cataracts. Disophenol is said to cause temporary cataracts when administered to dogs, but according to research by the present inventors, such a phenomenon may be observed in young dogs. , in dogs old enough to develop cataracts.
On the contrary, it was found that it has a preventive and therapeutic effect on cataracts, and can be called a surprising new finding that overturns conventional knowledge. Moreover, it was found that this effect is effective not only in dogs, but also in small animals such as cats, and even in the prevention and treatment of cataracts in humans, and that it can be used appropriately. The present invention has been completed based on this new finding, and the present invention is directed to a cataract preventive and therapeutic agent containing disophenol as an active ingredient, and a preventive treatment for cataract in animals characterized by administering zinphenol. It is the law. As mentioned above, disophenol is a drug that is widely used as a hookworm repellent for dogs.It has the chemical structure of 2,6-diiodo-4-ditrophenol, and is commercially available under the trade name Ancyrol■. ing. The method of the present invention can be used therapeutically to treat patients suffering from cataracts (including non-human animals, the same applies hereinafter), and prophylactically to patients who have not developed cataracts but are suffering from systemic symptoms or due to age. Disophenol is administered to patients who are expected to develop cataracts. Disophenol may be administered systemically by injection or locally by means such as eye drops. In some cases, oral administration may also show prophylactic and therapeutic effects, but generally the most effective method of administration is injection. When disophenol is administered by injection, it is best to use it as a sterile aqueous solution containing about 1 to 100 mg per ml, preferably about 1 to 70 mg per ml.
Most preferably, an injection solution with a concentration of about 5 to 50 mg per ml is prepared and used. Such injections are manufactured according to normal injection manufacturing methods,
If necessary, it may contain a pH adjuster, a tonicity agent, a buffer, etc., or may contain other medicinal substances as long as it does not impair the purpose of the present invention. The dose of injectable disophenol depends on the animal species (human, canine,
It varies depending on whether it is a cat or other mammal), prevention or treatment, age of the patient, medical condition, etc., but usually about 5 to 10 m of disophenol per IKg of patient's body weight.
It is best to administer the drug subcutaneously, preferably once a week. If disophenol is administered by eye drops, 1 ml
0 inside. It is best to prepare and use eye drops containing 1 to 10 mg of ginphenol, preferably 0.1 to 6 mg, and the amount used should be increased or decreased depending on the species, medical condition, age, etc. of the animal. However, such eye drops are usually administered by dropping them onto the corneal surface once or several times a day. When preparing eye drops, an isotonizing agent, a bactericidal agent, a chelating agent, etc. may be appropriately included in the same manner as in ordinary eye drops. Examples of tonicity agents include sorbitol, glycerin, polyethylene glycol, propylene glycol, glucose, and sodium chloride. Examples of disinfectants include benzalkonium chloride, chlorohexidine salt, benzethonium chloride, and paraoxybenzoic acid. Esters, benzyl alcohol, parachlormethaxylenol, chlorcresol, phenethyl alcohol, sorbic acid or its salts, thimerosal,
Examples include chlorobutanol. Examples of the chelating agent include sodium edetate, sodium citrate, and condensed sodium phosphate. The cataract preventive and therapeutic agent of the present invention can also be prepared and used in the form of an eye ointment. Examples of ointment bases used when preparing eye ointments include petrolatum, macrogol,
Sodium carboxymethyl cellulose and the like can be used as appropriate. The concentration of disophenol in the eye ointment is about 0.001% to 10%, preferably about 0.01 to 5%.
It is recommended that the solution be prepared at a certain concentration and applied to the corneal surface one to several times per day. Even in this case, it goes without saying that the dosage and frequency of administration should be increased or decreased or selected as appropriate depending on the species of animal, its age, medical condition, etc. In the present invention, disophenol can also be administered internally for the purpose of preventing or treating cataracts in mammals. In this case, capsules, tablets, granules, etc. are conveniently used as dosage forms, and in the case of animals other than humans, etc.
It can also be administered as a mixture in the diet. These internal preparations can be formulated according to conventional methods. In the case of oral administration, the dose usually varies depending on the species, medical condition, age, etc. of the animal, but it is usually 10 mg to 500 mg per day.
It is preferable to separate approximately 1.0 mg into one or several times.

【Example】

1. Injection disophenol-1・・・・・・・・・・・・
・・・・・・・・・4.5g Sterile distilled water for injection・・・・・・
......-100 ml of the above is mixed and dissolved, filled into ampoules of 1 ml each, and sterilized by heating to form a preparation. 2. Eye drops Zinphenol・・・・・・−0,05X Sodium Chloride・・・・・・・・・・・・・−・・−・・−
...-0,25X sodium edetate...-
---0,02X benzalkonium chloride...
・・・－・・・・・・－・0.005X Borisorbate---・・・・・・・・・・・・・・・・・・・・・・・・ 0.3x Dissolve the above in purified water to a total volume of 100ml Then, sterilize by filtration and dispense into eye drop bottles to make the product. 3. Eye ointment disophenol・・・・・・・・・・・・・・・・・・・・・・
・・−・−0,0IX carboxymethylcellulose・・
- Mix an appropriate amount of the above in a conventional manner to make an eye ointment.

[Clinical trial results]

The subjects of the experiment were dogs suffering from senile cataracts. All dogs were subjected to internal examinations, biochemical tests, and blood image tests, and dogs with abnormalities other than cataracts were excluded from the study, and 15 dogs were used in the experiment. In addition, all dogs considered to be suffering from congenital cataracts, traumatic cataracts, combined cataracts, etc. are also excluded from the list based on past medical conditions and ophthalmological findings. An injection solution containing 45 mg of disophenol in 1 ml was prepared, and 6.5 mg to 7.011 g of disophenol was injected subcutaneously once a week per I kg of dog body weight.
Administration continued for an average of 10 weeks. Internal medical tests, biochemical tests, blood imaging tests, etc. were conducted before and after administration to investigate the presence or absence of side effects. In 8 of the 15 test animals, the warming opacity immediately below the anterior capsule began to become transparent one week after administration, and once weekly administration was repeated, the opacity immediately below the anterior capsule gradually became transparent, and the opacity immediately below the anterior capsule began to become transparent. The turbidity has also begun to become clearer. In some cases of excellent response, the opacity directly under the capsule was almost completely cleared. In cases where cataracts were severe before disophenol administration and drug administration showed a significant effect, there were many cases in which changes in the dog's behavior clearly suggested improvement in visual acuity. In this experiment, the drug was administered a maximum of 10 times, and
Although the animals were observed for more than 0 weeks, no weight loss was observed, and no findings suggestive of side effects due to drug administration were found in internal examinations, biochemical examinations, or blood image examinations. The results obtained in this test are shown in the table below.

【Effect of the invention】

The cataract preventive and therapeutic agent of the present invention can be used to extremely safely and effectively treat cataracts in humans and other mammals, for which preventive treatment has been difficult until now, making it easy to apply. It is possible to provide a reliable method for preventing and treating cataracts.

Claims (2)

[Claims] (1) A cataract preventive and therapeutic agent containing disophenol as an active ingredient. (2) A method for preventing and treating cataracts in animals, which comprises administering disophenol to animals.