Eye instillation with decongestant effect
Technical Field
Present technical solution relates to eye instillation with decongestant effect, based on a sympathomimetic, a substance for decongestion of the front eye segment, combined with a bioflavonoid.
Background Art
In ophthalmological practice, several individual as well as combined preparations based on a sympathomimetic or a sympathomimetic with synergically acting substances are used: Visin (tetrahydrozoline), Nasopos Ν (tetrahydrozoline), Oculosan Ν (naphazoline, zinc sulfate).
Preparations based on a sympathomimetic combined with a bioflavonoid, substances supporting the correct functioning of capillaries, have not been known yet.
Description of Technical Solution
The group of known ophthalmological preparations showing vasoconstrictive effect is now complemented with an eye instillation according to the present technical solution, the nature of which consists in that it contains from 0.001 % to 1 % by weight of tetrahydrozoline hydrochloride (vasoconstrictor, decongestant) and from 0.001 % to 1 % by weight of rutin trihydrate (bioflavonoid) or possibly its sulfate salt with sulfuric acid, further from 0.0005 to 0.1 % by weight of a preserving additive, from 0.01 to 2 % by weight of auxiliary substances which help to keep the pH value of the medium within a range from 5 to 8.0, from 0.01 to 5 % by weight of auxiliary substances which keep viscosity of the medium within a range of 5 to 25 mPa.s, and the rest to 100 % by weight consists of distilled water.
The auxiliary substances which keep the pH value of the medium within a range from 5 to 8.0, include sodium acetate, sodium chloride, boric acid, borax, disodium edetate, sodium hydrogen phosphate or sodium dihydrogen phosphate, alone or in a mixture.
The auxiliary substances which keep viscosity of the medium within a range of 5 to 25 mPa.s, include hydroxypropylmethylcellulose and polyoxyethylenesorbitan monooleate, alone or in a mixture.
The preserving additive is benzalkonium chloride, carbetopendecinium bromide, thimerosal, chlorohexidine or chlorobutanol.
The active substance tetrahydrozoline hydrochloride is an alpha- sympathomimetic which is a derivative of adrenergens of the imidazoline group. The second active substance of the preparation is rutin trihydrate. Rutin is a bioflavonoid which is important for normal functioning of capillaries.
After an application of the instillation according to the present solution to the pacients conjunctival sac an increased anti-inflammatory and anti-oedematous effect arises as a result of modification of an increased refraction and increased permeability of capillaries in an interaction with vessel vasoconstriction. Generally, microcirculation is improved and subjective compliants are diminished.
The preparation shows also a moderate antiallergenic effect. It diminishes allergic manifestations of the eye caused by allergens.
An advantage of the instillation according to the present solution is an increased efficiency in treating oedematous and hyperaemic conditions of conjunctiva, caused by smoking, dust, wind, chlorinated water, sun, neon light, electrical welding, cosmetic preparations or contact lens, as well as elimination of allergic itises such as nasal allergy and hypersensitiveness to pollen. It affects secondarily the local signs of bleeding at diabetic retinopathy.
Examples of embodiments
Example 1
Weighed amounts of components (according to the production batch size) are dissolved in sterilized distilled water under aseptic conditions. After having dissolved them sterilized distilled water is added to the solution up to the specified volume. The resulting, solution is sterilized by filtration through a membrane filter with 0.2 μm
mesh and immediately dosed into sterile vials under aseptic conditions and sealed with sterile seals. The sealed vials are labeled and packed into specified packages.
The amounts of components of a production batch are a linear function of the amounts per one package, i. e. 10 ml.
a) Composition for one package: tetrahydrozoline hydrochloride 0.00010 g rutin trihydrate 0.00010 g sodium chloride 0.00100 g boric acid 0.00100 g borax 0.00100 g disodium edetate 0.00100 g benzalkonium chloride 0.00005 g sterilized distilled water ad 10 ml
b) Composition for one package: tetrahydrozoline hydrochloride 0.00010 g rutin trihydrate 0.00010 g sodium acetate 0.01000 g boric acid 0.01000 g disodium edetate 0.00010 g tween 80 0.00100 g hypromellose 0.00100 g thimerosal 0.00005 g sterilized distilled water ad 10 ml
c) Composition for one package: tetrahydrozoline hydrochloride 0.00010 g rutin trihydrate 0.00010 g sodium chloride 0.00100 g chlorohexidine 0.00005 g sterilized distilled water ad 10 ml
d) Composition for one package: tetrahydrozoline hydrochloride 0.00010 g rutin trihydrate 0.00010 g sodium hydrogen phosphate 0.01000 g sodium dihydrogen phosphate 0.01000 g hypromellose 0.00100 g chlorobutanol 0.00005 g sterilized distilled water ad 10 ml
e) Composition for one package: tetrahydrozoline hydrochloride 0.00010 g rutin trihydrate 0.00010 g boric acid 0.01000 g disodium edetate 0.00010 g carbetopendecinium bromide 0.00005 g sterilized distilled water ad 10 ml
f) Composition for one package: tetrahydrozoline hydrochloride 0.00010 g rutin trihydrate 0.00010 g sodium hydrogen phosphate 0.01000 g benzalkonium chloride 0.00005 g sterilized distilled water ad 10 ml
Example 2
Weighed amounts of components (according to the production batch size) are dissolved in sterilized distilled water under aseptic conditions. After having dissolved them sterilized distilled water is added to the solution up to the specified volume. The resulting solution is sterilized by filtration through a membrane filter with 0.2 μm mesh and immediately dosed into sterile vials under aseptic conditions and sealed with sterile seals. The sealed vials are labeled and packed into specified packages.
The amounts of components of a production batch are a linear function of the amounts per one package, i. e. 10 ml.
a) Composition for one package: tetrahydrozoline hydrochloride 0.10000 g rutin trihydrate 0.10000 g sodium chloride 0.20000 g boric acid 0.20000 g borax 0.20000 g disodium edetate 0.20000 g benzalkonium chloride 0.01000 g sterilized distilled water ad 10 ml
b) Composition for one package: tetrahydrozoline hydrochloride 0.10000 g rutin trihydrate 0.10000 g sodium acetate 0.20000 g boric acid 0.20000 g disodium edetate 0.20000 g tween 80 0.50000 g hypromellose 0.50000 g thimerosal 0.01000 g sterilized distilled water ad 10 ml
c) Composition for one package: tetrahydrozoline hydrochloride 0.10000 g rutin trihydrate 0.10000 g disodium chloride 0.20000 g chlorohexidine 0.01000 g sterilized distilled water ad 10 ml
d) Composition for one package: tetrahydrozoline hydrochloride 0.10000 g rutin trihydrate 0.10000 g sodium hydrogen phosphate 0.20000 g sodium dihydrogen phosphate 0.20000 g hypromellose 0.50000 g chlorobutanol 0.01000 g sterilized distilled water ad 10 ml
e) Composition for one package: tetrahydrozoline hydrochloride 0.10000 g rutin trihydrate 0.10000 g boric acid 0.20000 g disodium edetate 0.20000 g carbetopendecinium bromide 0.01000 g sterilized distilled water ad 10 ml
f) Composition for one package: tetrahydrozoline hydrochloride 0.10000 g rutin trihydrate 0.10000 g sodium hydrogen phosphate 0.20000 g benzalkonium chloride 0.01000 g sterilized distilled water ad 10 ml
Industrial applicability
The eye instillation according to the present technical solution can be utilized in ophthalmology in treating oedematous and hyperaemic conditions of conjunctiva, secondarily to affect the local signs of bleeding at diabetic retinopathy.