RU2082434C1 - Ocular ointment - Google Patents

Abstract

FIELD: medicine, ophthalmology. SUBSTANCE: ocular ointment is prepared out of karotoline, methyluracil, gentamicin sulfate, methylcellulose, glycerol, emulsifier T-2 and water taken at certain ratio to treat traumatic keratitis, chemical burns, conjunctivitis, cornea and wounding infection, especially. EFFECT: higher efficiency. 1 tbl

Description

 The invention relates to medicine, in particular to ophthalmology, and can be used in the treatment of dystrophy, traumatic erosion of the cornea, various keratitis, chemical burns, conjunctivitis, cornea, and especially with wound infection.

 Known ophthalmic ointment 3% xeroform on a lanolin-vaseline basis, the drawback of which is the appearance of allergic reactions due to the presence of lanolin and petroleum jelly, as well as the insufficient wound healing activity of the drug (Tentsova A.I. Alyushin M.T. Polymers in pharmacy. M. Medicine, 1980, p. 10).

 The closest in technical essence to the claimed technical solution is an eye ointment containing rosehip oil as a medicinal substance, and methyl cellulose glycyrogel, emulsifier t-2 and water as the basis in the following ratio of components, wt.

Rosehip Oil 5-10
Methyl cellulose 1-3
Glycerin 7-15
Emulsifier T-2 0.5-2
Water Else
This ointment is used as a wound healing agent for trophic and burn defects of the cornea and conjunctiva, sluggishly healing wounds of the cornea, traumatic keratitis, skin and mucosal defects. In the course of treatment, the inflammatory reaction, lacrimation and photophobia decrease, and epithelization of damaged surfaces occurs F 9/00 1987 [1]
However, with all its positive properties, an eye ointment with rosehip oil has insufficient regeneration and does not have a bacteriostatic effect against gram-negative and gram-positive microorganisms in wound infections.

 The objective of the invention is the bacteriostatic effect on gram-negative and gram-positive microorganisms in case of wound infection, in reducing the treatment time, increasing the therapeutic effect.

 The problem is solved in that the eye ointment containing medicinal substances and the base methyl cellulose, glycerin, T-2 emulsifier, water, contains carotoline, methyluracil and gentamicin sulfate as medicinal substances in the following ratio of components, wt.

Carotene 2.5-5.0
Methyluracil 0.5-1.0
Gentamicin sulfate 0.08-0.3
Cellulose 1.0-3.0
Glycerin 7.0-15.0
Emulsifier T-2 0.5-2.0
Water Else
The introduction of methyluracil into the ointment significantly accelerates the processes of cell regeneration, accelerates wound healing, and stimulates cellular and humoral defense factors (MD Mashkovsky. Medicines, part II, p. 138, 1987).

 Gentamicin sulfate is one of the main means of combating severe purulent infection. Due to the wide spectrum of action, gentamicin is used for mixed infections, as well as in cases where the pathogen has not yet been established.

 For experimental verification of the claimed composition were prepared 5 compositions of the ingredients, 3 of which showed optimal results (see table).

Medicinal substances
Carotoline (FS 42-24-05-85) is an oil extract of carotenoids from the pulp of rose hips, an oily orange-colored liquid with a characteristic odor. Used in the treatment of trophic ulcers, eczema, atrophic changes in the mucous membranes, some types of erythroderma.

Methyluracil (2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine). Flavourless white crystalline powder. Slightly soluble in water (up to 0.9% at +20 ^o C) and alcohol. By the chemical structure, methyluracil is a pyrimidine derivative. The drug has anabolic and anticatabolic activity. Accelerate the processes of cell regeneration and wound healing. Stimulates cellular and humoral defense factors. Methyluracil is used for sluggishly healing wounds, burns.

 Gentamicin sulfate belongs to the group of aminoglycoside antibiotics. It has a bacteriological effect against many gram-positive and gram-negative microorganisms. It acts on penicillin-resistant staphylococci strains. Gentamicin is used for various infectious diseases caused by microorganisms sensitive to it. Due to the wide spectrum of action, gentamicin is prescribed for mixed infections, as well as when the pathogen is not installed.

 Base components: water-soluble methyl cellulose (TU 6-01-71772) is a cellulose methyl ester containing 26-33% methoxy groups. The fibrous material is white with a yellowish or grayish tint. At room temperature, it forms transparent, viscous solutions in water. Aqueous solutions of methylcellulose have a large binding, emulsifying, dispersing, wetting and adhesive ability.

 Glycerin (FS 42-698-73). Obtained from distilled dynamite, premium and first grade glycerol according to GOST 6824-76, diluted with water to a density of 1.223-1.233. A clear, colorless syrupy liquid with a sweet taste, odorless. Hygroscopic. Miscible with water and 95% alcohol in all proportions, very slightly soluble in ether, practically insoluble in fatty oils. Used as a solvent for some medicinal substances. Glycerin is part of a number of official ointments.

Emulsifier T-2 (Tu 18-17 / 05-75). Obtained by esterification of stearic acid with polyglycerol by glycerol polymerization product. Consistency at 20 ^o C solid, wax-like, from yellow to light brown in color, with a smack and smell of stearin and polyglycerol, in the molten state - transparent, without impurities. It is used as a stabilizer, plasticizer and emulsifier in the manufacture of ointments.

 Example 1. Ophthalmic ointment with components that are taken in the following ratio, wt.

Carotolin 2.5
Methyluracil 0.5
Gentamicin Sulfate 0.08
Cellulose 1.0
Glycerin 7.0
Emulsifier T-2 0.5
Purified Water
The method of obtaining the ointment is as follows.

One gram of methyl cellulose is poured with 50 ml of hot purified water. In 38, 42 ml of purified water, dissolve 0.2 methyluracil and 0.08 gentamicin sulfate. After the swelling of methylcellulose, a solution of methyluracil and 7.0 glycerol are added, 0.5 T-2 emulsifier is melted separately in a water bath and mixed. The base with methyluracil and gentamicin sulfate is subjected to steam sterilization at 100 ^° C. for 30 minutes or in an autoclave at 120 ^° C. for 8-10 minutes. 2.5 carotolins are placed in a sterile mortar, then a sterile base is added in parts and everything is thoroughly homogenized with a pestle until a homogeneous mass is formed.

 Example 2. An eye ointment is prepared analogously to example 1, but the components are taken in the following ratio, wt.

Carotolin 3.5
Methyluracil 0.7
Gentamicin sulfate 0.1
Cellulose 2.0
Glycerin 11.0
Emulsifier T-2 1.5
Purified Water
Example 3. An eye ointment is prepared analogously to example 2, but the components are taken in the following ratio, wt.

Carotolin 5.0
Methyluracil 1.0
Gentamicin sulfate 0.3
Cellulose 3.0
Glycerin 15.0
Emulsifier T-2 2.0
Purified Water
The selection of the optimal parameters of the components is presented in the table.

From the above experiment, we can conclude that the ointment prepared from the components included in the following intervals, wt. meets all the requirements of the State Pharmacopoeia of the X-XI edition (uniformity, stability, well applied to affected areas)
Carotoline 2.5-5.0
Methyluracil 0.5-1.0
Gentamicin sulfate 0.08-0.3
Cellulose 1.0-3.0
Glycerin 7.0-15.0
Emulsifier T-2 0.5-2.0
Purified water 88.42-73.7
With an increase or decrease in the number of components from this interval, the ointment exfoliates and does not meet the requirements of the GF-X-XI edition. With a decrease in components, the ointment does not exhibit a therapeutic effect, with an increase in components, the therapeutic effect does not increase.

 The finished ointment is yellow in color, with a characteristic pleasant smell, uniform consistency. The ointment is recommended to be stored in a cool, dark place.

 The proposed ointment was used in an experiment on rabbits (6 eyes) in the treatment of experimental bacterial keratitis. The right eye (main group, 6 eyes) was treated with the proposed ointment, laying on the eyelids 4 times a day. The left eye (control) was treated with ointment with rosehip oil 4 times a day.

 In the treatment of the proposed ointment, the therapeutic effect is noted on the second day of treatment. Complete epithelization and recovery occurred on the 5-6th day of treatment with the formation of a tender, cloud-like scar.

 In the control eyes, the treatment time was 10-11 days, the clouding of the cornea was significantly intense.

 The results of the experiment made it possible to apply the proposed ointment in the treatment of corneal burns, traumatic and bacterial keratitis in the clinic.

 Example 1. Patient K., 28 years old, received a chemical burn of the cornea and conjunctiva of both eyes, I-II art. Upon receipt, the eyes are irritated, photophobia, blepharospasm, hyperemia of the conjunctiva of the lower vault, desquamation of the epithelium, diffuse edematous, turbid areas of desquamated epithelium in the lower half of the cornea. Visual acuity in both eyes is 0.3, is not corrected. Appointed local treatment of the proposed ointment. By the end of the day of treatment, the patient subjectively noted a significant improvement. Pain in the eyes, lacrimation decreased. Epithelization of corneal defects was noted after 48 hours. A full recovery was achieved after 7 days of treatment. The cornea is transparent, visual acuity 1.0 in both eyes.

 Example 2. Patient A. 24 years old, turner, while working on a lathe received an injury to his right eye. I turned to the ophthalmologist every other day. After removal of the foreign body of the cornea (metal shavings), the patient was hospitalized with a diagnosis of: right eye: traumatic keratitis, visual acuity of 0.1 is not corrected. The left eye is healthy, visual acuity is 1.0.

 Upon admission to the cornea, an infiltrate of 3 mm in diameter of gray color is determined in the center of the cornea with an epithelial defect, which is intensely stained with fluorescein. Staphylococci sensitive to gentamicin were found in the discharge from the conjunctival cavity. Local treatment was prescribed: albucid 30% 4 times and the proposed ointment 4 times a day. After 2 days of treatment, clinical improvement was noted. Irritation phenomena decreased, corneal infiltrate cleared, decreased in diameter, and peripheral epithelialization began. Complete epithelization occurred on the 5th day of treatment, the infiltrate resolved completely on the 7th day of treatment. A gentle cloud-like clouding with a diameter of 2 mm was formed. Visual acuity restored to 0.8. When cytological examination of the contents of the conjunctival cavity of pathogenic microflora was not found.

 Example 3. Patient D. 51 years old, was admitted to the clinic UFNII eye diseases with a diagnosis of marginal keratitis of the right eye, the left eye is healthy. Visual acuity at admission: right eye 0.8, not corr. left eye 1.0. Upon receipt, the right eye is irritated, periocorneal injection, on the periphery of the cornea near the limb on the meridian of 5 hours, a three-point gray infiltrate, stained with fluorescein. After 48 hours. after 4 local treatments with the proposed ointment, a decrease in photophobia, lacrimation, periocorneal injection was noted, the intensity of staining of infiltrates decreased. The infiltrates are flattened, reduced in size. Complete resorption of infiltrates was observed on the 6th day of treatment, there were gentle point opacities. Visual acuity recovered to 1.0.

 Thus, clinical trials allow us to conclude that the proposed ointment has a high therapeutic effect in keratitis of various etiologies and burns, which is due to the optimal compatibility of the components of the ointment with a bactericidal, regenerating, anti-inflammatory effect. Compared with the prototype (ointment with rosehip oil), the healing time was reduced by 7-14 days.

Claims (1)

 An eye ointment containing medicinal substances and a base - methyl cellulose, glycerin, T-2 emulsifier, water, characterized in that it contains carotoline, methyluracil and gentamicin sulfate as medicinal substances in the following ratio of components, wt. Carotoline 2.5 5.0
Methyluracil 0.5 1.0
Gentamicin sulfate 0.08 0.3
Cellulose 1 3
Glycerin 7 15
Emulsifier T-2 0.5 2.0
The rest of the water

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