SK7314Y1 - Ophthalmological preparation based on iodine anion for the treatment of virus diseases of the eye - Google Patents

Abstract

The preparation having antivirus effects contains 0.01 to 5 % by weight of potassium iodide, 0.01 to 5 % by weight of sodium iodide, 0.001 to 2 % by weight of auxiliary agents having antioxidant effect, 0.5 to 10 % by weight of non-ionic surface active agent and water for injection.

Description

Technical field

The solution relates to eye drops based on iodine anion.

BACKGROUND OF THE INVENTION

Iodine has been used in ophthalmology in the 1930s for the treatment of infectious and non-infectious (degenerative) conditions, including prophylaxis of cataract. The application of iodine anion and organic iodine compounds in the experiment confirmed the braking effect on arteriosclerosis and at the same time it was shown that iodine anions facilitate the solubility of cholesterol in blood serum. Iodine anions strongly increase the dispersity of colloids, resulting in a decrease in blood viscosity.

The manifestations of aging - arteriosclerosis - are also related primarily to a decrease in colloid dispersity. Functional disorders associated with sclerotic vascular changes in the eye can be favorably affected by potassium iodide. It is likely that iodine salts hampering this process to alleviate the development of arteriosclerosis. On this basis, it is considered that it also affects cell membranes with the consequent improvement of metabolic processes.

Utility model SK3313 describes an iodine-based ophthalmic instillation for use in supporting the resorption processes in the eye, in particular exudates, vitreous opacities of various etiology, athero and arteriosclerotic changes in retinal and choriodeal vessels, retinal degenerative processes, incipient cataracts, fungal conjunctivitis.

In the treatment of the above-mentioned conditions, eye instillation with potassium iodide and eye instillation with potassium iodide and sodium containing thiomersal as a preservative have long been used in therapeutic practice. However, these formulations have not shown sufficient stability. Since thiomersal is incompatible with iodine ions, it is rapidly decomposed, making it impossible to determine its content in the finished formulation. In addition, there is a gradual increase in the actual acidity of such a formulation.

The essence of the technical solution

The present invention is characterized in that the iodine anionic ophthalmic preparation for the treatment of viral diseases of the eye contains 0.01 to 5 wt. % potassium iodide and 0.01 to 5 wt. % sodium iodide, 0.001 to 2 wt. % of adjuvants with antioxidant effect, 0.5 to 10 wt. nonionic surfactant and water for injection.

The nonionic surfactant is selected from the group of polyoxyethylene sorbitan monooleate, polyoxyl 35 castor oil, polyethylene glycol individually or in admixture.

A suitable antioxidant adjuvant is one selected from the group consisting of vitamin E, sodium thiosulfate or sodium edetate individually or in admixture.

For adjusting the viscosity of the medium in the range of 1 to 50 mPa.s, an excipient in an amount of 0.001 to 3% by weight may be added to maintain the viscosity of the medium selected from hydroxypropylmethylcellulose, polyvinyl alcohol, sodium hyaluronate and carboxyvinyl polymer individually or in admixture.

The ophthalmic formulation of the present invention may contain an adjuvant to adjust the pH of the solution in the range of 5 to 8 selected from boric acid, sodium tertaborate, sodium acetate, sodium hydrogen phosphate, sodium dihydrogen phosphate, sodium citrate, citric acid, tartaric acid, sodium tartrate, trometamol , sulfuric acid, hydrochloric acid, sodium hydroxide individually or in a mixture.

The iodine anionic ophthalmic formulation of the present invention is suitable for the treatment of viral eye diseases.

The advantage of this ophthalmic composition is that it does not need to contain a preservative because it is sufficiently stable.

BRIEF DESCRIPTION OF THE DRAWINGS

In the accompanying figure, inhibition of HSV-1 herpes virus replication K17 strain in the presence of the tested products is potassium iodide 2% and potassium iodide 2% at various times after the infection phase. The abbreviation PFU in the attached figure means plaque forming units.

SK 7314 Υ1

EXAMPLES

Example 1

The weighed amounts of the components (depending on the size of the production batch) are dissolved under aseptic conditions in injection water. After dissolution, the solution is made up to volume with injection water. The resulting solution is sterilized by filtration through a 0.2 µm membrane filter and immediately aseptically filled into sterile vials and sealed with sterile caps. The closed bottles are labeled and packaged in the prescribed containers.

The amounts of the components of the production batch are a linear dependence of the quantities per package, i. j. 10 ml.

Example 2

Composition per package

Potassium iodide 0.01000 g sodium iodide 0.01000 g sodium chloride 0.00010 g sodium thiosulphate 0.00010 g polyoxyethylene 0.00100 g edetate sodium 0.00010 g hydroxypropyl 0.00100 g water for injections ad 10 ml

Example 3

Single-pack potassium iodide sodium chloride sodium thiosulfate polyoxyethylene sorbitan monooleate sodium edetate polyvinyl alcohol water for injections

0.01000 g

0.00010 g

0.00010 g

0.00100 g

0.00010 g

0.00100 g and 10 ml

Example 4

Sodium iodide Sodium iodide Sodium tartaric acid Sodium thiosulphate Polyoxyethylene sorbitan monooleate Sodium edetate Polyvinyl alcohol Water for injections

Example 5

Sodium iodide sodium iodide polyetelenglycol tocopherol acetate edetate sodium hydroxypropylmethylcellulose water for injections

Example 6

Sodium iodide Sodium iodide Sodium thiosulfate Sodium edetate Polyoxyethylene sorbitan monooleate Water for injections

0.00100 g

0.00100 g

0.00010 g

0.00010 g

0.00010 g

0,05000 g

0.00010 g

0.00100 g and 10 ml

0,50000 g

0,50000 g

1,00000 g

0,20000 g

0,20000 g

0.30000 g and 10 ml

0,20000 g

0,20000 g

0.00200 g

0.00200 g

0.05000 g and 10 ml

SK 7314 Υ1

table

3 hpi 6 hpi 9 hpi 12 hpi 15 hpi 18 hpi 20 hpi 22 hpi HSV-1 KI 7 POTASSIUM JODIO 2% PF + HSV-1 K17 POTASSIUM AND SODIUM IODIDE 2% PF + HSV-1 KI 7 6xl0 ⁵ 2x10 ⁶ Ο, ΟΙχΙΟ ⁴ 7x10 ⁵ Ο, ΙΟχΙΟ ⁶ 6x10 ² 3.5x10 ⁶ 1.5X10 ⁶ 6x10 ' 1.5x10 '8.5x10 ⁶ 6x10 ² 6,5xl0 6xl0 ^{6 6} 1.5x10 ⁴ 7x10 '2x10' 9.5x10 ⁴ 3x10 '1x10 ⁶ 0,75x10' 5,25x10 ' 1.5x10 ' 0.5x10 '

Mean virus titer values (expressed as CFU / ml) evaluated at 3, 6, 9, 12, 15, 18, 20, and 22 hours after infection.

Results processed in Table no. 1 and the graph in the figure show significant inhibition of HSV-1 K17 replication of herpes virus strain K17 by POTASSIUM AND SODIUM 2% without preservative, where the virus titer was reduced by more than 4 log 10 CFU / ml compared to controls at 20 and 22 1 hour after infection. CFU means colony forming units.

Industrial usability

The iodine anionic ophthalmic formulation of the present invention with the potassium iodide and sodium iodide active ingredient can be used in ophthalmology in a number of indications. They are useful in viral diseases of the eye, in support of resorption processes in the eye, in particular exudates, in vitreous hazards of different etiology, athero- and arteriosclerotic changes of retina and chorioid vessels, in retinal degenerative processes, incipient cataract, fungal and viral conjunctivitis.

Claims (6)

PROTECTION REQUIREMENTS Ophthalmic preparation based on iodine anion for the treatment of viral diseases of the eye, characterized in that it contains from 0.01 to 5% by weight of an ophthalmic preparation. % potassium iodide, 0.01 to 5 wt. % sodium iodide, 0.001 to 2 wt. % of adjuvants with antioxidant effect and 0.5 to 10 wt. nonionic surfactant and water for injection. The iodine anionic ophthalmic preparation of claim 1, wherein the nonionic surfactant is selected from the group of polyoxyethylene sorbitan monooleate, polyoxyl 35 castor oil, polyethylene glycol individually or in admixture. Ophthalmic preparation based on iodine anion according to claim 1, characterized in that the antioxidant adjuvant is a substance selected from the group of vitamin E, sodium thiosulphate or sodium edetane, singly or in a mixture. Ophthalmic preparation based on iodine anion according to claim 1, characterized in that it contains 0.001 to 3 wt. excipients maintaining a viscosity of the environment in the range of 1 to 50 m Pa.s. The iodine-based ophthalmic preparation of claim 4, wherein the excipient maintaining a viscosity of from 1 to 50 mPa.s is selected from the group of hydroxypropylmethylcellulose, polyvinyl alcohol, sodium hyaluronate, and the carboxyvinyl polymer individually or in admixture. An iodine-based ophthalmic preparation according to any one of the preceding claims 1 or 4, characterized in that it further comprises an auxiliary for adjusting the pH of the solution in the range of 5 to 8 selected from boric acid, sodium tertaborate, sodium acetate, sodium hydrogen phosphate, sodium dihydrogen phosphate, sodium citrate, citric acid, tartaric acid, sodium tartrate, trometamol, sulfuric acid, hydrochloric acid, sodium hydroxide individually or in admixture.