Pharmaceutical composition in form of eye drops for preventing and treating allergic eye diseases

FIELD: medicine.

SUBSTANCE: invention represents a composition for preventing and treating allergic conjunctivitis and keratoconjunctivitis, containing cromoglicic acid, boric acid and water-soluble polymers specified in a group of: carbomer, hypromellose, macrogol and polyvinylpyrrolidone with the components of the composition taken in specific relations, g in 1 ml of the mixture.

EFFECT: invention provides the better reduction of the inflammatory process and symptoms of the disease; there are also ensured ease of use with a smaller frequency of administration, prolonged action and no side effects.

5 ex

 

Pharmaceutical composition in the form of drops for the prevention and treatment of allergic diseases of the eye

The invention relates to medicine, in particular to ophthalmology, and is intended for the prevention and treatment of allergic diseases of the eye, namely, allergic conjunctivitis and keratoconjunctivitis.

Currently there has been a noticeable increase in the number of allergic diseases occurring with lesions of the eye. These include allergic conjunctivitis and allergic keratoconjunctivitis (a combination of symptoms of conjunctivitis and keratitis).

Widely known eye drops for the treatment of allergic diseases, including allergic conjunctivitis and keratoconjunctivitis by reducing and eliminating these allergic manifestations of the eyes like: redness, tearing, itching, pronounced "glassy" edema of the mucosa of the eyes, photophobia: azelastine - Allergodil, olopatadine - Patanol, tetryzoline - Octile, levocabastine - vizin, naphazoline, Sanorin - Analergin, cromoglicate acid - Lekrolin, (hi-Chrome, Bromohexyl), ketotifen and other (Michuk Y. F. Allergic eye disease. M., 1983, p. 223; Michuk F. Y. Topical issues of ophthalmology. M., 1996, CH 11. p. 58-63; Michuk Y. F., Yakushin L. N. New drugs, 1994, No. 11, pp. 3-5; A. E. Egorov Clinical ophthalmology. 200, No. 2, p. 57; Michuk Y. F., K. N. Haitov., Grishakova M. B. New drugs. 1998, No. 10, pp. 26-28; EN 2193403 C1, AC 31/415, 2002; RU 2281086 C1, AK 9/20, 2006; RU 2214228 C2, AC 9/08, 2003; RU 2493823 C1, AC 9/00, 2012 ).

These eye drops have a number of disadvantages: not effective due to short-term pharmacological action or have limited application due to the included in its composition of toxic preservative benzalkonium chloride, irritate the cornea of the eye, or can cause erosion of the cornea due to toxic effects on the mucosa of the eye and cornea, or are difficult to obtain because of the multicomponent nature of the drug; or cause complications during treatment.

The closest solution to the technical essence and the achieved result are eye drops Lekrolin containing cromoglicate acid, preservative benzalkonium chloride, disodium edetate, boric acid and purified water as consistentarea bases in a specific ratio. Used Lekrolin for the prevention and treatment of allergic conjunctivitis and keratoconjunctivitis (http://eyeshelp.ru/drugs/Lekrolin/.

These eye drops are multi-component and include in the overall composition is very toxic to the eye the preservative benzalkonium chloride. Prolonged use of Lekrolin involves the risk of a side effect. Awlays� cause toxic effects on the mucosa of the eye and cornea, they cause drug conjunctivitis or corneal erosion.

The object of the invention is the obtaining of effective medicines for the prevention and treatment of allergic conjunctivitis and keratoconjunctivitis based on the polymer having the ease of design and to avoid the risk of side effects, including toxic effects when in contact with the cornea of the eye, and provide good tolerability in patients.

The technical result for the solution of which directed this invention is to improve therapeutic efficacy of the claimed eye drops for fast relief of allergic conjunctivitis and keratoconjunctivitis and prolonged action of the drug on the cornea of the eye, providing an exception to the recurrence of diseases and complications in comparison with the prototype.

To achieve the said technical result pharmaceutical composition for the prevention and treatment of allergic conjunctivitis and keratoconjunctivitis in the form of drops containing cromoglicate acid, boric acid and consistantness basis, according to the invention, as consistentarea basis, it contains polymers selected from the group: carbomer, polymer, macrogol and polyvinylpyrrolidone at next �at a rate of g per 1 ml of the mixture:

Cromoglicic acid0,00001-0,5
Boric acid0,00001-0,5
Consistentarea basiselse

When creating a droplet, the task was to preserve the effectiveness of the active ingredients of lekrolin if you exclude side effects of the drug associated with toxic benzalkonium chloride, and create a framework that would improve the properties of the drops. This was chosen base polymer polyvinylpyrrolidone (PVP) used as a stabilizer and a complexing agent, and polymers selected from the group: carbomer, polymer, macrogol.

The present invention is illustrated with specific examples of performance, to assess the achievement of the above technical result.

Example 1. Preparation of eye drops perform a standard method of preparation of eye drops by mixing all of their constituent components to obtain a homogeneous mass. Received eye drops meet the requirements of the pharmaceutical composition. As the basis for the use of carbomer and PVP.

These components of eye drops taken in the following ratio in g per 1 ml of a mixture of:/p>

Example 2. Carried out analogously to example 1, except that as a basis for using the polymer of the polymer and PVP.

These components of eye drops taken in the following ratio in g per 1 ml of the mixture:

Example 3. Carried out analogously to example 1, except that used as the basis polymer is macrogol and PVP.

These components of eye drops taken in the following ratio in g per 1 ml of the mixture:

With all the proposed options the proposed composition clinical studies.

Available today is the result of such studies has demonstrated the best effect of treatment on achievement of specified technical result is the pharmaceutical composition on the basis of PVP used as a stabilizer and a complexing agent, and polymers selected from the group: carbomer, polymer, macrogol.

The study included 38 patients with acute and chronic allergic eye diseases. The best results in terms of speed of relief of inflammation, symptoms of disease, ease of use were obtained in the treatment of drops based on PVP and polymers selected from the group: carbomer, polymer, mA�Rogol.

Side effects were observed. In addition, when the treatment was used less frequency of administration of such drops. If other options offered drops in arresting the pathological process required a 4-5 fold dripping, droplet-based PVP and polymers selected from the group: carbomer, polymer, macrogol, enough was 2-3-times use per day, and further 1-2-fold use. This obviously testified to a prolonged action with preservation of efficiency of action of the active substances in the form of drops. The side effects while using the drops from PVP was absent in patients (10 patients). At the same time, when using drops with macrogoal 5 patients had worsening or stabilization of the symptoms of conjunctivitis (9 patients), when using drops with hypromellose - in 3 cases (9 patients), when using drops with Carbonera - in 4 cases (10 patients). In this regard, in patients with side effects in the further treatment was replaced by drops from PVP. In the end, the treatment time drops from PVP were less than in other groups of patients.

Prevention of allergic diseases of the eye drops suggested also possible. It follows from the use of funds with similar active ingredients composition (Le�rolina). It is known that lekrolin shown and used for the prevention of allergic diseases of the eye.

Our aim was to exclude from the known composition of toxic benzalkonium chloride and add this preservative, which does not worsen, and will improve therapeutic effects of known composition.

According to research, the most suitable basis for of cromoglicic and boric acid was the basis of PVP and polymers selected from the group: carbomer, polymer, macrogol.

In addition, our patients, conducting preventive dripping drops from PVP 1-2 times a day, had no recurrence of the disease during 6-18 months of monitoring. Thus, both theoretically and practically confirmed the possibility of prevention of allergic diseases of the eye drops offered by us.

Example 4. Patient G. 30 years. Diagnosis: chronic allergic conjunctivitis, worsening. Complaints of pain in the eyes moderate, photophobia, slight tearing, at times increasing redness of the eye. The low tolerance of eye drops, especially antibiotics. The examination found slight hyperemia of the conjunctiva, the mucous loosened, lightweight papillary hypertrophy of the conjunctiva of the upper eyelid, slight mucous discharge. In smears from the conjunctiva Staphylococcus zo�testy. When allergological examination revealed hypersensitivity to house dust (+++). Prescribed treatment: the Preparation of example 1, 2 drops 3 times a day. During examination after two days all the phenomena of the disease has decreased, the microflora is not detected. Further improvement observed on day 7 and the eye is completely relaxed to 14 day. Portability is good. There were no complications. Later conducted prophylactic instillation of the drug 1 time per day. After 6 months, recurrence was not found.

Example 5. Patient N. 35. Diagnosis: acute keratoconjunctivitis left eye infectious-allergic Genesis. The patient suffered a long period of time, bacterial conjunctivitis, worsening occurred a week ago, the use of eye drops antibiotics causes eye irritation. At the moment of examination expressed irritation eyes: tearing, photophobia, eyelids are hyperemic, thickened, sharply hyperemic conjunctiva, swollen discharge is negligible. Along the outer edge of the cornea marginal corneal ulcer a width of 1.5 mm, surface is stained with fluorescein. In smears and crops Staphylococcus aureus. Prescribed treatment preparation according to example 2 or example 3 1-2 drops 3 times per day. The phenomena of irritation of the eyes decreased after 3 days of treatment, disappeared after 14 days. Subsequently conducted a successful�e treatment of ulcers. Complaints of drug was not. Complications were observed. Conducted prophylactic instillation of the drug 1 time per day. Relapse at 12 months was not revealed.

The choice of the components stated of the droplets and their quantitative values were given the opportunity to obtain a new technical result is a manifestation of a good anti-allergic effect, prevention of pathological changes in the epithelial cells of the conjunctiva and cornea, which can lead to damage of the corneal stroma and the occurrence of erosions, ulcers and perforations. Drops have good tolerability. Relapses after their application is not detected.

Thus, the inventive eye drops have a high therapeutic efficacy in the treatment of allergic conjunctivitis and keratoconjunctivitis.

Stated drops are easy to perform and allow you to avoid the danger of side effects, including toxic effects when in contact with the cornea of the eye, and provide good tolerability in patients. Increased therapeutic efficacy of the claimed eye drops explained by the high rate of relief of allergic conjunctivitis and keratoconjunctivitis and sustained effect of the drug on the cornea of the eye, providing an exception to the recurrence of diseases and complications comparedwith the prototype. The use of drops 1-2 times a day to prevent recurrence of the disease also provides preventive effect.

Pharmaceutical composition for the prevention and treatment of allergic conjunctivitis and keratoconjunctivitis in the form of drops containing cromoglicate acid, boric acid and consistantness the basis, characterized in that as consistentarea basis, it contains polymers selected from the group: carbomer, polymer, macrogol and polyvinylpyrrolidone in the following ratio in g per 1 ml of the mixture:

Cromoglicic acid0,00001-0,5
Boric acid0,00001-0,5
Consistentarea basisElse



 

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