RU2245137C1 - Pharmaceutical composition for threatment of viral inflammations in eyeball - Google Patents

Abstract

FIELD: medicine, in particular ophthalmology.

SUBSTANCE: claimed composition contains (mass %): antiviral drug 0.001-5; vegetable and/or animal phospholipids 0.001-2; sodium chloride 0.8-0.9; sodium hydrophosphate 0.001-0.2; sodium dihydrophosphate 0.001-0.2; and balance: distilled water.

EFFECT: composition with prolonged and effective action.

3 ex

Description

The invention relates to medicine, namely to ophthalmology, and is a drug for the treatment of inflammatory processes of viral etiology in the eyeball.

The well-known drug “Remantadine”, which is a derivative of adamantane and inhibits the release of the viral genome (Kharkevich D. A. “Pharmacology” M. Medicine, 1999, p. 548).

However, this drug has a number of significant disadvantages. The drug, dissolved in a 0.9% sodium chloride solution, is quickly washed out of the cavity of the posterior segment of the eye, and also does not have sufficient buffer capacity, which leads to a decrease in the therapeutic effect of the drug itself and the possible occurrence of local edema of the retinal cells due to the lack of balance of the solution.

The technical result of the present invention is a prolonged anti-inflammatory effect by maintaining the average therapeutic concentration of the drug in the eyeball due to the presence of phospholipids in the composition of the drug.

The technical result is achieved by the fact that the pharmaceutical composition (FC) for the treatment of inflammatory diseases of the viral etiology of the eyeball includes an antiviral drug, plant and / or animal phospholipids, sodium chloride, monosubstituted sodium phosphate, disubstituted sodium phosphate and purified water in the following ratio of components in wt. %:

antiviral drug 0.001-5

plant and / or animal phospholipids 0.001-2

sodium chloride 0.8-0.9

monosubstituted sodium phosphate 0.001-0.2

disubstituted sodium phosphate 0.001-0.2

purified water the rest

FC may contain:

antiviral drug 0.001-5

plant phospholides 0.001-2

sodium chloride 0.8-0.9

monosubstituted sodium phosphate 0.001-0.2

disubstituted sodium phosphate 0.001-0.2

purified water the rest

FC may contain

antiviral drug 0.001-5

animal and plant phospholides 0.001-2

sodium chloride 0.8-0.9

monosubstituted sodium phosphate 0.001-0.2

disubstituted sodium phosphate 0.001-0.2

purified water the rest

FC may contain

antiviral drug; 0.001-5

animal phospholides 0.001-2

sodium chloride 0.8-0.9

monosubstituted sodium phosphate 0.001-0.2

disubstituted sodium phosphate 0.001-0.2

purified water the rest

FC may contain various antiviral drugs, depending on the family of viruses that caused the inflammatory process in the eyeball, for example:

1. Acyclovir is an analogue of purine nucleosides that has an inhibitory effect on the DNA polymerase of the virus, which inhibits the replication of herpetic DNA.

2. Ganciclovir - a synthetic analogue of 2-deoxyguanosine nucleoside, inhibiting the synthesis of cytomegalovirus DNA.

3. Oxolin - tetraoxotetrahydronaphthalene dihydrate, a drug with virucidal activity against adenovirus.

4. Interferons - low molecular weight glycoproteins produced by body cells when exposed to viruses and increasing the resistance of cells to damage by their virus. They are characterized by a wide antiviral spectrum.

Phospholipids have a membrane stabilizing, prolonging effect and are inhibitors of retinal cell edema. Their concentration cannot be less than 0.001% due to a sharp decrease in the decongestant and prolonging effect and cannot be more than 2% due to the fact that at this concentration an undesirable macrophage reaction can be caused.

The concentration of sodium chloride, monosubstituted sodium phosphate and disubstituted sodium phosphate correspond to a solution of a normal osmolarity of 300-310 mOsm, the phosphate concentration cannot be less than 0.001% due to the hypoosmolar effect and cannot be more than 0.2% due to the hyperosmolar effect.

Thus, the proposed pharmaceutical composition for the treatment of inflammatory processes in the eyeball is a drug with an effective long-term anti-inflammatory effect.

The pharmaceutical composition is prepared as follows: the starting materials are mixed under aseptic conditions, filtered through a 0.22 μm filter, packaged and sterilized by autoclaving.

The claimed pharmaceutical composition is used in inflammatory processes of viral etiology in the eyeball and is introduced into the anterior chamber by paracentesis, and into the vitreous cavity by injection through pars plana after a previous subtotal vitrectomy.

Examples

EXAMPLE 1: Patient B., 34 years old with a diagnosis, right eye - herpetic keratoconjunctivitis, herpetic iridocyclitis. Upon admission, she complained of severe pain in OD, redness of the eye. About-but: OD - mixed injection, edematous cornea, on the endothelium precipitates, Tyndall phenomenon 3-4 tbsp., The color of the iris is changed, the cavity of the CT and retina with direct ophthalmoscopy is intact. The patient underwent standard local antiviral therapy in the treatment of herpetic keratoconjunctivitis in the form of instillations of drops in the conjunctival sac, and the proposed pharmaceutical composition was introduced into the anterior chamber by paracentesis, of the following composition, wt.%:

acyclovir 0.3

phosphotidylcholine 0.9

sodium chloride 0.9

monosubstituted sodium phosphate 0.2

disubstituted sodium phosphate 0.2

purified water

7 days after the administration of this composition, there were no inflammation in the anterior chamber.

EXAMPLE 2: Patient 3. 27 years old with a diagnosis of right eye: cytomegalovirus retinitis. At admission, the patient did not complain, from the anamnesis: systemic cytomegalovirus infection 6 months ago, with biomicroscopy, no changes in the anterior segment were detected, with direct ophthalmoscopy on OD - at the extreme periphery - merging white foci with hemorrhages. The patient underwent anterior vitrectomy and the claimed pharmaceutical composition was once introduced into the vitreous cavity by injection through pars plana of the following composition, wt.%:

ganciclovir 3.1

phosphotidylcholine and egg phospholipid (50/50) 1.8

sodium chloride 0.9

monosubstituted sodium phosphate 0.2

disubstituted sodium phosphate 0.2

purified water the rest

On the 7th day after the introduction of the proposed pharmaceutical composition with biomicroscopy and indirect ophthalmoscopy, a significant decrease in the size of the foci of inflammation was noted. On the 14th day at the site of foci - areas of depigmentation and hyperpigmentation of the retina.

EXAMPLE 3: Patient K., 51, with a diagnosis of left eye: adenoviral keratoconjunctivitis, adenovirus iridocyclitis. Upon receipt complained of severe pain in the OS, redness of the eye. Objectively: OS - mixed injection, swollen cornea, on endothelium precipitates, Tyndall phenomenon 3-4 tbsp., Iris color is changed, CT cavity and retina with direct ophthalmoscopy are intact. The patient underwent local antiviral therapy in the form of instillations of drops into the conjunctival sac, and also the proposed pharmaceutical composition of the following composition was introduced into the anterior chamber by paracentesis, in wt.%:

oxolin 0.3

phosphotidylcholine 0.9

sodium chloride 0.9

monosubstituted sodium phosphate 0.2

disubstituted sodium phosphate 0.2

purified water the rest

4 days after the introduction of this combination, inflammation in the anterior chamber was absent.

Claims (1)

A pharmaceutical composition for treating inflammatory processes of viral etiology in an eyeball containing an antiviral preparation, characterized in that it further comprises plant and / or animal phospholipids, sodium chloride, monosubstituted sodium phosphate, disubstituted sodium phosphate and purified water in the following ratio of components in wt. %: Antiviral drug 0.001-5 Plant and / or animals phospholipids 0.001-2 Sodium Chloride 0.8-0.9 Monosubstituted sodium phosphate 0.001-0.2 Disubstituted sodium phosphate 0.001-0.2 Purified water Else