Eye Instillation Based on Iodine Anions
Technical Field
The solution relates to eye instillation based on iodine anions.
State of the Art
In the thirties of the 20* century, Iodine found its application in ophtalmology in the treatment of both infectious and non-infectious (degenerative) diseases, including prophylaxis of the cataract. The application of the iodine anion and of organic iodine compounds in an experiment has confirmed an inhibitory effect upon arteriosclerosis and, at the same time, it has been proved that iodine anions facilitate the solvability of colloids, due to which the viscosity of blood decreases.
Also the manifestations of ageing - arteriosclerosis - are related first of all with the decrease in colloid dispersity. Dysfunction, which is due to sclerotic changes of the blood vessels in the eye, can be affected favourably by means of potassium iodide. It is probable that the salts of iodine, by inliibiting this process, mitigate the development of arteriosclerosis. On the basis of this it is believed that they affect also the cell membranes, which brmgs about an improvement of the metabolic processes.
In the treatment of the aforementioned diseases, therapeutic practice has long used an iodine instillation with potassium iodide and an eye instillation with potassium and sodium iodides containing tiomersal as a conservation agent. These substance, however, have not proved to be sufficiently stable. Since tiomersal is incompatible with iodine ions, it decomposes rapidly due to which its content in the final substance can not be determined. In addition, gradual increase in the acidity of the substance takes place.
The Background of the Technical Solution
The essence of the submitted solution of eye instillation is that it contains from 0.01 to 5 weight percent of potassium iodide as an active substance, from 0.0005 to 0.1 weight percent of a conservation agent, further from 0.001 to 2 weight percent of ancillary substances maintaining pH of the solution in the range from 5 to 8.0, and the rest to 100 weight percent is sterilized distilled water. Thus, the essence of the submitted solution is an eye instillation
based on iodine ions as an active substance with a content of suitable conservation agent and of ancillary substances ensuring the required stability of the medicine.
The eye instillation may contain also an addition of another active substance of sodium iodide in content from 0.01 to 5 weight percent and possibly also substances maintaining the viscosity of the solution in the range from 1 to 50 mPa.s, their content ranging from 0.01 to 5 weight percent individually or in mixture.
The conservation agent in the instillation is chlorhexidine acetate or chlorhexidine gluconate, chlorbutanol or carbentho pendetinium bromide, which are substances compatible with iodine ions.
The substances maintaining pH in the range from 5 to 8.0 are sodium chloride, boric acid, sodium tetraborate, sodium acetate, sodium edetate, sodium hydrogen phosphate, sodium dihydrogen phosphate, sodium tiosulphate, sodium citrate, citric acid individually or in mixture.
The instillation may contain also substances maintaining the viscosity of the solution in the range from 1 to 50 mPa.s, such as hydroxypropylmethylcellulose, polyvinyl alcohol, monooleate polyoxyethylenesorbitan or carboxyvinyl polymer individually or in mixture.
The eye instillation pursuant to the submitted solution exhibits good physical and chemical stability. Since chlorhexidine is not incompatible with iodine ions, the content of this conservation agent can be determined in the whole range of its antimicrobial activity. Stable topical acidity of the solution has been verified, which allows to utilize these prescriptions in the conditions of mass production.
Figures in Drawings
Figure 1 represents a chromatographic scan of chlorhexidine detection in an eye instillation containing 2 weight percent of KI.
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 througli a membrane filter with 0.2 μm mesh and immediately dosed into sterile vials and sealed with sterile seals under aseptic conditions. 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:
potassium iodide 0,01000 g sodium iodide 0,01000 g sodium chloride 0,00010 g sodium tiosulphate 0,00010 g monooleate polyoxyethylensorbitan 0,00100 g sodium edetate 0,00010 g hydroxypropylmethylcellulose 0,00100 g chlorhexidine acetate 0,00005 g sterilized distilled water ad 10 ml
b) Composition for one package:
potassium iodide 0,01000 g sodium chloride 0,00010 g sodium tiosulphate 0,00010 g monooleate polyoxyethylensorbitan 0,00100 g sodium edetate 0,00010 g polyvinyl alcohol 0,00100 g chlorbutanol 0,00005 g sterilized distilled water ad 10 ml
C) Composition for one package:
potassium iodide 0,01000 g sodium iodide 0,01000 g boric acid 0,00010 g sodium tertaborate 0,00010 g sodium tiosulphate 0,00010 g sodium edetate 0,00010 g carbetho pendetinium bromide 0,00005 g sterilized distilled water ad 10 ml
Composition for one package:
potassium iodide 0,01000 g sodium iodide 0,01000 g sodium hydrogen phosphate 0,00010 g sodium dihydrogen phosphate 0,00010 g sodium tiosulphate 0,00010 g chlorhexidine gluconate 0,00005 g sterilized distilled water ad 10 ml
β) Composition for one package:
potassium iodide 0,01000 g citric acid 0,00010 g sodium citrate 0,00010 g monooleate polyoxyethylensorbitan 0,00100 g hydroxypropylmethylcellulose 0,00100 g chlorhexidine acetate 0,00005 g sterilized distilled water ad 10 ml
) Composition for one package:
potassium iodide 0,01000 g sodium iodide 0,00010 g sodium tiosulphate 0,00010 g sodium edetate 0,00010 g chlorhexidine acetate 0,00005 g sterilized diestilled water ad 10 ml
g) Composition for one package: potassium iodide 0,01000 g sodium iodide 0,01000 g sodium tiosulphate 0,00010 g monooleate polyoxyethylensorbitan 0,00100 g sodium edetate 0,00010 g chlorhexidine gluconate 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 and sealed with sterile seals under aseptic conditions. 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: potassium iodide 0,50000 g sodium iodide 0,50000 g sodium chloride 0,20000 g sodium tiosulphate 0,20000 g monooleate polyoxyethylensorbitan 0,50000 g sodium edetate 0,20000 g hydroxypropylmethylcellulose 0,50000 g chlorhexidine gluconate 0,05000 g sterilized distilled water ad 10 ml
b) Composition for one package: potassium iodide 0,50000 g sodium chloride 0,20000 g sodium tiosulphate 0,20000 g monooleate polyoxyethylensorbitan 0,50000 g sodium edetate 0,20000 g polyvinyl alcohol 0,50000 g chlorbutanol 0,05000 g sterilized distilled water ad 10 ml
c) Composition for one package: potassium iodide 0,50000 g sodium iodide 0,50000 g boric acid 0,20000 g sodium tertaborate 0,20000 g sodium tiosulphate 0,20000 g sodium edetate 0,20000 g carbetho pendetinium bromide 0,05000 g sterilized distilled water ad 10 ml
Φ Composition for one package:
potassium iodide 0,50000 g sodium iodide 0,50000 g sodium hydrogen phosphate 0,20000 g sodium dihydrogen phosphate 0,20000 g sodium tiosulphate 0,20000 g chlorhexidine acetate 0,05000 g sterilized distilled water ad 10 ml
e) Composition for one package:
potassium iodide 0,50000 g citric acid 0,20000 g sodium citrate 0,20000 g monooleate polyoxyetliylensorbitan 0,50000 g hydroxypropylmethylceluulose 0,20000 g chlorhexidine acetate 0,05000 g sterilized distilled water ad 10 ml
f) Composition for one package:
potassium iodide 0,50000 g sodium iodide 0,20000 g sodium tiosulphate 0,20000 g sodium edetate 0,20000 g chlorhexidine glukonate 0,05000 g sterilized distilled water ad 10 ml
g) Composition for one package: potassium iodide 0,50000 g sodium iodide 0,50000 g sodium tiosulphate 0,20000 g monooleate polyoxyethylensorbitan 0,50000 g sodium edetate 0,20000 g chlorhexidine acetate 0,05000 g sterilized distilled water ad 10 ml
industrial Applicability
The eye instillation based on iodine anions pursuant to the submitted solution with iodine anions in the form of potassium iodide or potassium and sodium iodides as an active substance can be utilized in ophtalmology in such indications as the support of resorption processes in the eye, in particular of exudates, cataracts of diverse ethiology, atero- and arteriosclerotic changes of the vessels of the retina and chorioidea, degenerative processes on the retina, beginning cataracts, mucotic conjuntivites and ceratidites.