Eye drops

FIELD: medicine.

SUBSTANCE: invention refers to pharmaceutical industry, namely to drugs presented in the form of a solution and applicable for therapeutic purposes, particularly treating eye diseases. Eye drops for inflammatory eye diseases characterised by the fact that they contain benzalkonium chloride, sodium hydrogen phosphate dodecahydrate, disodium edetate, sodium chloride, sodium hyaluronate, potassium dihydrogen phosphate, Polysorbate, linden blossom infusion, camomile blossom infusion, water for injections in certain proportions and pH 4.5-11.4.

EFFECT: eye drops provide deposition, uniform absorption of the active ingredients over a period of time between installations, eye tissue tolerance and finally substantially expanded possibility of therapeutic application; besides, prolonged action of an antihistaminic preparation and a vasoconstrictive agent and availability of a hypoallergic preservative are ensured.

3 ex

 

The invention relates to the pharmaceutical industry, namely to medicines, made in the form of a solution and is intended for therapeutic purposes, in particular the treatment of eye diseases.

Known antiseptic ophthalmic solution according to the patent of Russian Federation №2317810, A61K 9/06, 2003 on the basis of benzalkonium chloride.

The disadvantages of the known solutions are the low efficiency in the treatment of inflammatory processes of the eye, as well as the risk of negative side effects long term use.

The task of the invention is the creation of an original national eye drops in the form of a combined preparation with as hypotensive and reparative action that prolong contact of the drug with the cornea to reduce the number of instillations, with a fairly long shelf life after opening the package.

The technical result is the creation of a pharmaceutical composition antiallergic eye drops that provide Deposit, uniform absorption of the active components over the time interval between installations, tolerance to eye tissues and, ultimately, greatly enhancing the possibility of their therapeutic applications. In addition, achieved prolonged action antihistamine preparation of the TA and the vasoconstrictor and use hypoallergenic preservative.

The introduction of the means of herbal ingredients increases efficiency while reducing the risk of side effects.

The specified result is a tool that is used as eye drops and have anti-inflammatory and disinfectant action, representing a sterile solution containing benzalkonium chloride is a Quaternary ammonium compound (alkyldimethyl (phenylmethyl) ammonium chloride (as hydrobromide); sodium hyaluronate is a biopolymer, which represents a polysaccharide consisting of repeating disaccharide glycosides of chains connected by glycosidic bridges; sodium hydrogen phosphate dodecahydrate (sodium phosphate disubstituted 12-water), potassium dihydrophosphate, of disodium edetate (Trilon B); sodium chloride; infusion of lime flowers and infusion of chamomile flowers.

The pH value of 4.5-11,4,

in the following ratio of components:

benzalkonium chloride 0.1-1.0 mg,

sodium hydrogen phosphate of dodecahydrate - 10.0 to 50.0 mg,

disodium of edetate 0.05 to 1.0 mg,

sodium chloride is 1.0-3.0 mg,

hyaluronate sodium is 0.1-3 mg,

potassium dihydrophosphate - 10,0-20,0 mg,

Polysorbate-80, and 0.1 - 2.0 mg,

infusion of lime flowers (1:10) - 20-70 mg,

infusion of chamomile flowers (1:10) - 20-70 mg,

water for injection to 1 ml

Eye drops are obtained as follows. In chemically pure sterile Cup is h, containing about 50 ml of water for injection, contribute separately (until dissolved) in the proposed doses benzalkonium chloride, sodium hydrogen phosphate of dodecahydrate, of disodium edetate, sodium chloride, sodium hyaluronate, potassium dihydrophosphate, Polysorbate-80, infusion of Linden flowers (1:10), infusion of chamomile (1:10). The volume content of the flask was adjusted with water to 100 ml and Then produce the first sterile filtration of the solution through the filters Millipore" 0.22 μm) in sterile Boxing in laminar flow. The filling solution is performed in a sterile 10 ml vials through the secondary filtering through Millipore a nozzle with a pore diameter of 0.22 μm. Vials sealed with a rubber stopper and compresses aluminum caps. Etecetera and stored at a temperature not exceeding 25°.

Example 1.

Preclinical research tools on the model of cell cultures, experimental animals have shown that it is non-toxic, non-pyrogenic, has no effect, retains the anti-inflammatory activity in full.

Evaluation of anti-inflammatory effect developed compositions eye drops conducted on three groups of five rabbits of the chinchilla breed (the weight of each rabbit in the range of 2-2,5 kg) with experimental traumatic conjunctivitis according to the following procedure:

The first group of rabbits was buried developed the th composition of eye drops in the following ratio of components:

benzalkonium chloride 0.2 mg

sodium hydrogen phosphate of dodecahydrate and 24.5 mg,

disodium of edetate 0.1 mg,

sodium chloride 1.5 mg,

hyaluronate sodium - 1 mg,

potassium dihydrophosphate - 4.4 mg,

Polysorbate - 80-0,67 mg,

infusion of lime flowers (1:10) - 50 mg,

infusion of chamomile flowers (1:10) - 50 mg,

water for injection to 1 ml

The second group of rabbits was prescribed eye drops for RF patent No. 2317810, A61K 9/06, 2003 on the basis of benzalkonium chloride.

The third control group was buried 0.9% sodium chloride solution.

In the majority of eyes in the control group (the third group), starting with 10 min for an extended period of time (three days), there was a strong hyperemia of the conjunctiva. In the first group on the third day the redness had no or minor (in one case).

In the second group, on the third day the redness was absent in six rabbits, slight hyperemia in four rabbits.

This allows us to conclude that the developed composition of eye drops has a more pronounced protivovospalitelnym and antiseptic effect compared to eye drops based on benzalkonium chloride.

Example 2.

Sick Days due to exposure To foreign object was a slight injury to the mucous membrane of the cornea, accompanied by redness, lacrimation with weakly expressed in the swelling of the eyes. Treatment was conducted in the form of installation of eye drops of the following composition:

benzalkonium chloride 0.5 mg

sodium hydrogen phosphate of dodecahydrate and 24.5 mg,

disodium of edetate 0.1 mg,

sodium chloride 1.5 mg,

hyaluronate sodium - 1 mg,

potassium dihydrophosphate - 4.4 mg,

Polysorbate-80 is 0.67 mg,

infusion of lime flowers (1:10) - 50 mg,

infusion of chamomile flowers (1:10) - 50 mg,

water for injection to 1 ml

A positive treatment effect noted in the first 3-5 minutes after instillation in the conjunctival cavity of the eye. Decreased itching and conjunctival hyperemia. The patient was recommended to continue treatment for 1-2 drops in the affected eye 5-6 times a day. On the third day of treatment, itching and watering of the eyes was absent. Both eyes are calm, when biomicroscopic study indicated a slight redness and swelling of the conjunctiva, which completely disappeared within the next 2 days of treatment.

Example 3.

Patient M In the extended wear contact lenses have a slight injury to the mucous membrane of the cornea, accompanied by redness and slight swelling of the eyes. Treatment was conducted in the form of installation of eye drops of the following composition:

benzalkonium chloride 0.3 mg

sodium hydrogen phosphate of dodecahydrate and 24.5 mg,

disodium of edetate 0.1 mg,

sodium chloride 1.5 mg,

hyaluronate NAT is s - 1 mg,

potassium dihydrophosphate - 4.4 mg,

Polysorbate-80 is 0.67 mg,

infusion of lime flowers (1:10) - 50 mg,

infusion of chamomile flowers (1:10) - 50 mg,

water for injection to 1 ml

A positive treatment effect noted in the first 5-10 min after instillation in the conjunctival cavity of the eye. Decreased itching and conjunctival hyperemia. Contact lenses were worn not earlier than 15 minutes after instillation. The patient was recommended to continue treatment for 1-2 drops in the affected eye 5-6 times a day. On the third day of treatment the redness and swelling was absent.

Clinical trials on human volunteers indicate that the drug is safe, well tolerated, does not cause allergic reactions. The drug is injected into the eye 5-6 times a day in a dose of 1-2 drops before the disappearance of symptoms.

The use of the invention reduces the risk of traumatic injury of the corneal endothelium and other tissues of the eye, provides transparency of fields of vision, has anti-inflammatory and antiseptic action.

Eye drops for the treatment of inflammatory diseases of the eye, characterized in that they contain benzalkonium chloride, sodium hydrogen phosphate dodecahydrate, disodium edetate, sodium chloride, sodium hyaluronate, potassium dihydrophosphate, Polysorbate, infusion of Linden flowers, infusion of chamomile flowers, water for injection in the following the ratio of components mg:

benzalkonium chloride0,1-1,0
sodium hydrogen phosphate dodecahydrateof 10.0 to 50.0
disodium edetate0,05-1,0
sodium chloride1,0-3,0
sodium hyaluronate0,1-3
potassium dihydrophosphate10,0-20,0
Polysorbate-800,1-2,0
infusion of Linden flowers (1:10)20-70
infusion of chamomile flowers (1:10)20-70
water for injectionto 1

at pH values of 4.5 11.4 in.



 

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