RU2121825C1 - Eye drops - Google Patents

Abstract

FIELD: medicine, ophthalmology. SUBSTANCE: eye drops containing sodium succinate hexahydrate, sodium citrate 5.5-hydrate, sodium chloride, sorbitol, glutamic acid, benzalkonium chloride, riboflavin mononucleotide phosphate and distilled water have additionally glucose and chondroitin sulfate A at the following ratio of components, wt.-%: sodium succinate hexahydrate, 1.91; sodium citrate 5.5-hydrate, 0.40; sorbitol, 0.80; sodium chloride, 0.31; L-glutamic acid, 0.015; riboflavin mononucleotide phosphate, 0.02; benzalkonium chloride, 0.015; glucose, 0.30; chondroitin sulfate A, 0.20; and distilled water for injection, the balance. Invention can be used for pharmaceutical protection of transplant after keratoplasty, treatment of patients with keratitis, deep erosions and cornea ulcers. EFFECT: enhanced metabolism in cornea cells, blockade of immunocompetent cells, stimulated synthesis of collagen and glycoseaminoglycans by cornea keratoblasts. 1 cl, 3 ex

Description

 The invention relates to medicine, namely to ophthalmology, and can be used for pharmacological protection of the transplant after keratoplasty, treatment of keratitis, deep erosion and corneal ulcers.

Known eye drops "Keratonic" containing sodium succinate, sodium citrate, sorbitol, sodium chloride, benzalkonium chloride, glutamic acid, riboflavin mononucleotide phosphate and distilled water (Patent N 2056821)
The disadvantage of these drops is the slow flow of energy reactions in the epithelial cells and the lack of a stimulating effect on the regeneration of the corneal stroma.

 The objective of the invention is the development of multicomponent eye drops to improve energy metabolism in the cells of the anterior and posterior epithelium of the cornea, keratoblast, immunological protection and stimulate stroma regeneration during corneal transplants, keratitis of various origins and dystrophic processes.

 The technical result is the acceleration of energy reactions in the cycle of tricarboxylic acids in the cells of the anterior and posterior corneal epithelium, keratoblasts, blockade of immunocompetent cells and stimulation of the synthesis of collagen and glycosaminoglycans by keratoblasts of the cornea.

The technical result is achieved by the fact that known eye drops containing sodium succinate hexahydrate, sodium citrate 5.5-aqueous, sodium chloride, sorbitol, glutamic acid, benzalkonium chloride, riboflavin mononucleotide phosphate and distilled water according to the invention additionally contain glucose and chondroitin sulfate A in the following the ratio of components, wt.%:
Sodium succinate, six-water - 1.91
Sodium Citrate 5.5-Aq - 0.40
Sorbitol - 0.80
Sodium chloride - 0.31
L-Glutamic acid - 0.015
Riboflavin Mononucleotide Phosphate - 0.02
Benzalkonium chloride - 0.015
Glucose - 0.30
Chondroitin Sulfate A - 0.20
Distilled Water for Injection - Other
Eye drops are prepared as follows. In a clean sterile beaker containing about 50 ml of water for injection, make separately (until completely dissolved) in the proposed doses, sodium succinate, hexahydrate, sodium citrate, 5.5-aqueous, sorbitol, sodium chloride, L-glutamic acid, riboflavin mononucleotide phosphate, benzalkonium chloride, glucose and chondroitin sulfate A. L-glutamic acid is dissolved separately in a small amount of water for injection at a temperature of 70 ^o C, followed by cooling to room temperature, and riboflavin mononucleotide phosphate in a darkened room when dispersed Oh light. Then the dissolved components are poured into a sterile chemical volumetric flask. The volume of the flask was adjusted with distilled water to 100 ml. Then the first sterile filtration of the solution is carried out (through 0.22 μm Millipor filters) in a sterile box in a laminar cabinet, subject to all the rules of thermolabile preparations for parenteral use. The solution is bottled in sterile vials (drunk flasks) of 10 ml each by secondary filtration through a millipore nozzle with a pore diameter of 0.22 μm. The flasks are sealed with a plastic and silicone stopper and an aluminum cap for hard running. Label and store in accordance with the requirements of the State Pharmacopoeia X-XI.

 Example 1. Patient S., 33 years old. The diagnosis is a condition after end-to-end subtotal keratoplasty of the right eye (3 days after surgery). Clinically pronounced corneal syndrome, edema of all layers of the native corneal transplant, lack of epithelization for 14 days after keratoplasty.

 The patient was prescribed Intertonic 6 times a day, 2 drops in the operated eye (against the background of immunosuppressive therapy with dexamethasone and sandimmun).

 By the end of 1 day from the beginning of the instillation of the drug, a moderate severity of the corneal syndrome, a significant enlightenment of the corneal stroma was achieved. The eye is calm. The patient was discharged for outpatient treatment. At the control examination after 3 months, the eye is calm, the corneal transplant is completely transparent and covered with epithelium.

 Example 2. Patient M., 67 years old. The diagnosis is dry eye syndrome (Sjögren's syndrome), the state after extracapsular cataract extraction, artifact of the right eye, a deep corneal ulcer in the center up to 4 mm in diameter. Clinically, the anterior epithelium is swollen, absent in the ulcer area, the stroma is moderately swollen, in the center there is complete destruction of the main substance to the descemet membrane, the endothelial layer in the optical section is difficult to see.

 The patient was prescribed the proposed drug "Intertonic" in the form of instillations 6 times a day, 2 drops for 14-20 days (until a pronounced clinical effect is obtained). After 17 days, stroma regeneration and corneal epithelization were achieved, after which the patient continued to receive Intertonic in a maintenance dose of 2 drops 4 times a day for 30 days. At the indicated observation period, recurrence of corneal erosion was not observed.

 Example 3. Patient B., 36 years old. The diagnosis is a condition after end-to-end subtotal keratoplasty of the right eye (4 days after surgery). Clinically expressed corneal syndrome, edema of all layers of the native corneal transplant due to insufficient adaptation of the edges in the area of the trepanation ring. The patient was prescribed Intertonic 6 times a day, 2 drops in the operated eye.

 By the end of 1 day from the beginning of instillation of the drug, moderate relief of the corneal syndrome, significant clarification of the cornea was achieved, and after 4 days, edema of all layers of the cornea and in the area of the trepanation ring was completely eliminated. The eye is calm. The patient was discharged for outpatient treatment on day 8. As a maintenance therapy, the drug was recommended for 3 months 4 times a day, 2 drops. At the control examination after 3 months, the eye is calm, the corneal transplant is completely transparent, the fibrous ring has formed transparent.

 Thus, the use of Intertonic eye drops can effectively stop various forms of keratopathy associated with inadequate epithelial-endothelial function and stromal defects of the cornea.

 Long-term use of the drug "Neokeratonic" in our observations did not reveal its side effects and toxico-allergic reactions.

Claims (1)

Eye drops including sodium succinate hexahydrate, sodium citrate 5.5-aqueous, sodium chloride, sorbitol, L-glutamic acid, riboflavin mononucleotide phosphate, benzalkonium chloride, distilled water for injection, characterized in that they additionally contain glucose and chondroitin sulfonate A in the following the ratio of components, wt.%:
Sodium succinate, six-water - 1.91
Sodium Citrate 5.5-Aq - 0.40
Sorbitol - 0.80
Sodium chloride - 0.31
L-Glutamic acid - 0.015
Riboflavin Mononucleotide Phosphate - 0.02
Benzalkonium chloride - 0.015
Glucose - 0.30
Chondroitin Sulfate A - 0.20
Distilled Water for Injection - Rest