Eye drops possessing antiinflammatory and antibacterial action

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to ophthalmology, and aims at treating a wide range of inflammatory ophthalmic diseases: bacterial, allergic, infectious allergic: conjunctivitis, blepharitis, keratitis and others. The eye drops contain a sulphanyl amide preparation, dexamethasone and water. The sulphanyl amide preparation is presented by sodium sulphacyl sodium. Additionally, the drops contain boric acid and hydroxypropyl methyl cellulose in the following proportions, wt %: sodium sulphacyl 8.0-12.0; dexamethasone 0.1-0.01; boric acid 0.4-0.6; hydroxypropyl methyl cellulose 0.4-0.6; water - the rest.

EFFECT: using the invention enables higher therapeutic effectiveness of using the declared eye drops ensured by their prolonged action by prolonging a corneal contact of the preparation.

3 ex

 

The invention relates to medicine, namely to ophthalmology, and can be used to treat a wide range of inflammatory eye diseases: bacterial, allergic, infectious-allergic: conjunctivitis, blepharitis, keratitis, and others.

Analysis of ocular morbidity in Russia estimated number of inflammatory diseases 18 million per year, including conjunctivitis - 12 million Patients with inflammatory diseases of the eye make up 40-60% of outpatient admissions ophthalmologist. Among inflammatory eye diseases share conjunctivitis remains quite high. A fairly common form are combined bacterial and allergic conjunctivitis and blepharoconjunctivitis. They have year-round resistant relapsing course. In these cases, the use of antibiotics often has a therapeutic effect and can cause chronic, persistent drug blepharoconjunctivitis.

Widely known sulfa drugs for the treatment of infectious diseases of the eye, such as conjunctivitis, blepharitis, keratitis, and others.

Known eye drops made in the form of 10-30% aqueous solution of a medicinal product Sulfatsil sodium (Medmaravis "drugs". - M.: Medicine, 1985, Vol.2, s-282.; RU # 2245138 C1, A61K 31/04, 2005).

Closest to the claimed the th invention offer the essence and the achieved result is a drug Alfadex, widely used for chronic (especially allergic) conjunctivitis, containing 10% solution sulfapiridazina sodium and 0.1% solution of dexamethasone (medkarta.com/?cat=article&id=20931).

However, the use of these eye drops as more concentrated solutions causes side effects in the form of tissue irritation and severe tolerability of patients.

The objective of the invention is the creation of eye drops that have powerful anti-inflammatory, antiallergic, antioxidant action, and also to prevent the risk of their side effects and provide good tolerance by patients.

The technical result of the invention is to increase therapeutic efficacy of the claimed eye drops due to their prolonged action by increasing the contact time of the drug with the cornea, providing a reduction in treatment and reduce complications compared with the prototype.

To achieve the technical result of the eye drops with anti-inflammatory and antibacterial effect, containing sulfa drug, dexamethasone and water, according to the invention as sulfa drug they contain sulfanil sodium, and optionally boric acid and hypromellose when the next zootoxin and components in wt.%:

Sulfatsil sodium8,0-12,0
Dexamethasone0,1-0,01
Boric acid0,4-0,6
The hypromellose0,4-0,6
Waterthe rest of it.

Spent an analysis of the prior art, including searching by the patent and scientific and technical information sources and identify sources that contain information about the analogues of the stated eye drops, has allowed to establish that the petitioners have not found a similar, characterized by signs, identical to all the essential features of the claimed eye drops.

The definition from the list of identified unique prototype allowed us to identify a set of essential in relation to perceived technical result of the distinctive features in the claimed eye drops set forth in the claims.

Therefore, the claimed eye drops corresponds to the criterion "novelty".

For verification of the compliance of eye drops applicants conducted an additional search of the known solutions to identify signs, owls is daysie with distinctive features of the prototype features of the claimed invention.

The search results showed that the claimed invention not apparent to the expert in the obvious way from the prior art, certain applicants have identified no impact envisaged the essential features of the claimed eye drops transformations to achieve a technical result.

Therefore, the claimed invention meets the criterion of "inventive step".

The criteria of the invention "industrial applicability" is confirmed by the fact that the alleged eye drops with anti-inflammatory and antibacterial effect with prolonged fixation on the cornea of the eye, contributing to prolonged action of the stated eye drops effects, can be used successfully to treat a wide range of inflammatory eye diseases: bacterial, allergic, infectious-allergic: conjunctivitis, blepharitis, keratitis, and others.

The invention is illustrated in the following examples.

Example 1.

Preparation of eye drops provide a standard method of preparation of eye capelluti mixing all the elemental composition of the components to obtain a homogeneous mass, soluble in water. Received eye drops conform to the requirements of the pharmaceutical agent.

These components of eye drops taken in the following ratio in wt.%:

Sulfatsil sodium10,0
Dexamethasone0,05
Boric acid0,5
The hypromellose0,5
Waterthe rest of it.

Example 2. Carried out analogously to example 1 except the composition of the components, taken in the following ratio in wt.%:

Sulfatsil sodiumto 12.0
Dexamethasone0,1
Boric acid0,6
The hypromellose0,6
Waterthe rest of it.

Example 3. Carried out analogously to example 1 except the composition of the components, taken in the following ratio in wt.%:

Sulfatsil sodium11,0
Dexamethas is n 0,01
Boric acid0,6
The hypromellose0,6
Waterthe rest of it.

Received eye drops are kind of transparent liquid.

The resulting compositions were controlled by a number of characteristics that reflect the purity and effectiveness. This pH, transparency, optical refraction, moisturizing effect, surface tension, dynamic viscosity, no irritating to the cornea, and the duration of retention on the cornea.

The pH values of the developed formulations eye drops were subjected to minor changes and were lying in the range of 6.8 to 7.6.

Researched solutions eye drops on a black background and scattered light was not different from water transparency.

Measurement of the known methods of surface tension of the compositions of eye drops showed that all the compounds have surface activity and, therefore, well spread across the cornea.

The refractive index of the developed formulations of eye drops is small, does not cause a hazy look, and close to tears (1,334).

The retention time of the stated eye drops horns on the TSE was determined in rabbits. The results showed a 2-3 times greater prolonging the ability of the claimed compositions eye drops due to the increased penetration in the tissue of the eye, increased their enveloping action, high viscosity and high selectivity relative to the surface of the eye compared to the prototype.

Irritating and toxic effects of compounds of the eye drops was studied on rabbits when introducing them into the conjunctival SAC 5-8 times a day 1-2 drops for 2 weeks. The study found no redness, swelling or other changes of the conjunctiva. No reported deaths of animals or acute poisoning.

In the lung model, non-infectious inflammation of the conjunctiva of the eye was reduced during the treatment of inflammatory lesions of the conjunctiva of the eye when applying eye drops declared.

The effectiveness of eye drops made on the presented examples, was studied in 4 groups of patients, 5 people in each suffering from dry eye disease AAH or dry keratoconjunctivitis, occurs at the height of inflammation of the conjunctiva.

The first group of patients (control), with diagnosis of AAH with phenomena keratopathy and infiltrata cornea after herpetic stromal keratitis with confirmed or suspected bacterial the Noah infection in one eye, treated the prototype with concurrent antibiotic therapy. After 20 days there was an improvement in the health of patients. Eyes completely calmed down. Restore the corneal surface and decrease the transparency of the cornea in both eyes came a month after the start of treatment.

The second group of patients. Diagnosis: - AAH events keratopathy and infiltrata cornea after herpetic stromal keratitis in one eye with proven or suspected bacterial infection. Treatment eye drops declared, made according to example 1, 2 drops 4 times a day for two weeks. As a result of treatment in patients on day 3 marked signs of improvement: decreased lacrimation and photophobia. After a week, the eye became more calm, state the corneal surface has improved, infiltrates in the corneal stroma decreased. Eyes completely calmed down. To 16 days after the start of treatment eyes completely calmed down, there was complete recovery of the corneal surface, decreased turbidity of the cornea.

The third group of patients. The diagnosis of epidemic adenoviral keratoconjunctivitis, acute unbalanced flow with sharp hyperemia of the conjunctiva, swelling of the mucous both eyes, copious eruption of subepithelial infiltrates, micro - what macroparasite of the cornea. Along with conventional antiviral treatment antibiotic treatment eye drops declared, made according to example 2, 2 drops 3-4 times a day for two weeks. On the fourth day there was a positive effect: decreased hyperemia, photophobia, pain in the eyes. Two weeks eyes calmed down, came the partial resorption of corneal opacities and complete epithelialization of the corneal surface. In the study of patients after 6 months of recurrent erosion of the cornea is not marked.

The fourth group of patients. The diagnosis of adenoviral conjunctivitis. Ongoing antiviral therapy scheduled installation of levomycetin and claimed eye drops according to example 3. On day 5 there has been a marked improvement: reducing photophobia, epithelialization of microrate, resorption of epithelial infiltrates. On day 14 after the start of treatment eyes completely calmed down. The cornea was completely transparent.

Analysis of the results of treatment offered eye drops showed a positive therapeutic result in 2, 3 and 4 groups of patients, manifested in the lack of side effects and allergic reactions on the background of the application stated eye drops.

Feature selection of eye drops and their quantitative values gave an opportunity to gain new technical result is royalene good anti-inflammatory effect, prevention of pathological changes in the epithelial layer of the conjunctiva and cornea, which can cause damage to the corneal stroma and the occurrence of erosions, ulcers and perforations.

Thus, the stated eye drops have a high therapeutic efficacy in the treatment of a wide range of inflammatory eye diseases: bacterial, allergic, infectious-allergic: conjunctivitis, blepharitis, keratitis, and others.

Eye drops containing sulfa drug, dexamethasone and water, characterized in that as a sulfa drug they contain sulfanil sodium, and optionally boric acid and hypromellose in the following ratio of components in wt.%:

Sulfatsil sodium8,0-12,0
Dexamethasoneof 0.01-0.1
Boric acid0,4-0,6
The hypromellose0,4-0,6
Waterthe rest of it.



 

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