Eye ointment

 

(57) Abstract:

The invention relates to medicine, in particular to ophthalmology, and can be used in the treatment of traumatic keratitis, chemical burns, conjunctivitis, corneal, and especially when wound infection. The inventive prepare eye ointment of cartolina, methyluracil, gentamicin sulfate, methyl cellulose, glycerine, emulsifier T-2, taken in a certain ratio and water. table 1.

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

Known eye ointment 3% xeroderma on lanolin, vaseline basis, the lack of which is the appearance of allergic reactions due to the presence of lanolin and vaseline, and poor wound healing activity of medicinal substances (ANCOVA A. I. Alushin MT Polymers in pharmacy. M. Medicine, 1980, S. 10).

Closest to the technical nature of the claimed technical solution is an eye ointment containing the medicinal substance oil is komponentov, wt.

Rosehip oil 5-10

The methylcellulose 1-3

Glycerin 7-15

Emulsifier T-2 0,5-2

Water the Rest

This ointment is used as a wound healing agent when food and burn defects of the cornea and conjunctiva, slowly healing wounds of the cornea, traumatic keratitis, defects of the skin and mucosa. In the course of treatment reduced inflammatory response, lacrimation and photophobia, comes epithelialization damaged surfaces F 9/00 1987 [1]

However, with all its positive qualities, eye ointment with rosehip oil does not have a sufficiently high regeneration and not bacteriostatic action against gram-negative and gram-positive microorganisms in wound infections.

The objective of the invention is a bacteriostatic effect on gram-negative and gram-positive microorganisms in wound infections, reduction of treatment time, increase therapeutic effect.

The task is solved in that eye ointment containing medicinal substances and the basis of methylcellulose, glycerine, emulsifier T-2, water as a medicinal substances contains Kartalin, methyluracil and genomic gentamicin sulfate 0,08-0,3

The methylcellulose 1,0-3,0

Glycerin 7,0-15,0

Emulsifier T-2 0,5-2,0

Water the Rest

Introduction in the composition of ointments methyluracil greatly accelerates the processes of cell regeneration, accelerates wound healing, stimulates cellular and humoral defense factors (M. D. Mashkovsky. Drugs, part II, S. 138, 1987).

Gentamicin sulfate is one of the main means of combating severe purulent infection. In connection with a broad spectrum of action gentamicin used in mixed infections, as well as in cases where the pathogen has not yet been installed.

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

Pharmaceutical substances

Kartalin (FS 42-24-05-85) is an oil extract carotenoids from fruit pulp rose hips, orange oily liquid color with a characteristic smell. Used in the treatment of trophic ulcers, eczema, atrophic changes of the mucous membranes, certain types of eritrodermii.

Methyluracil (2,4-Dioxo-6-methyl-1,2,3,4-tetrahydropyrimidin). White crystalline powder, odorless. It is soluble in water (up 0.9% at +20< the anabolic and antimetabolites activity. Accelerate the processes of cell regeneration and wound healing. Stimulates cellular and humoral defense factors. Apply methyluracil weak healing wounds, burns.

Gentamicin sulfate belongs to a group of aminoglycoside antibiotics. Has the bactericidal action against many gram-positive and gram-negative microorganisms. There are strains of staphylococci resistant to penicillin. Gentamicin applied in a variety of infectious diseases caused by sensitive microorganisms. In connection with a broad spectrum of action gentamicin appointed to a mixed infection, and when the causative agent is not installed.

Main components: the water-soluble methylcellulose (TU 6-01-71772) is a methyl ether of cellulose containing 26-33% metaxylene groups. Fibrous material white with a yellowish or grayish tint. At room temperature it forms in water transparent, viscous solutions. Aqueous solutions of methylcellulose have a high binding, emulsifying, dispersing, wetting, and adhesion power.

Glycerin (FS 42-698-73). Derived from glycerol distilled dynamite, higher first and the ugly taste, without smell. 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 certain drugs. Glycerin is part of a series of official ointments.

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

Example 1. Eye ointment with components, which are taken in the following ratio, wt.

Kartalin 2,5

Methyluracil 0,5

Gentamicin sulfate 0,08

The methylcellulose 1,0

Glycerin 7,0

Emulsifier T-2 0,5

Purified water Rest

The method of obtaining ointment next.

One gram of methyl cellulose pour 50 ml of hot purified water. 38, 42 ml of purified water dissolve 0.2 methyluracil and 0.08 gentamicin sulfate. After swelling methylcellulose mesilat. Basis with methyluracil and gentamicin sulfate is subjected to a sterilization fluid vapor at 100oC 30 minutes or in an autoclave at 120oC 8-10 minutes In a sterile mortar is placed 2.5 cartolina, then add in parts sterile bed and everything was thoroughly homogenized by pestle until a homogeneous mass.

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

Kartalin 3,5

Methyluracil 0,7

Gentamicin sulfate 0.1 to

The methylcellulose 2,0

Glycerin 11,0

Emulsifier T-2 1,5

Purified water Rest

Example 3. Eye ointment is prepared analogously to example 2, but the components are taken in the following ratio, wt.

Kartalin 5,0

Methyluracil 1,0

Gentamicin sulfate 0.3 to

The methylcellulose 3,0

Glycerin 15,0

Emulsifier T-2 2,0

Purified water Rest

The choice of optimal parameters of the components are presented in the table.

From the above experiment we can conclude that the ointment prepared from the components in the following interval, wt. meets all requirements of the State Pharmacopoeia X-XI edition (uniformity, stability, and well put on porage 1,0-3,0

Glycerin 7,0-15,0

Emulsifier T-2 0,5-2,0

Purified water 88,42 of 73.7

If you increase or decrease the number of components from the given interval ointment exfoliates and does not meet the requirements of the GF-X-XI edition. When reducing components ointment does not show a therapeutic effect in the increase of the components of therapeutic effect does not increase.

Ready ointment of yellow color, with a characteristic pleasant smell, homogeneous consistency. The ointment should be stored in a cool, dark place.

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

In the treatment offered by the ointment therapeutic effect was observed on the second day of treatment. Complete epithelialization and recovery occurred at 5-6 days of treatment with the formation of gentle blackvideo scar.

In the control eyes, the treatment time was 10-11 days, corneal opacity was significantly intense.

The experiment was carried primena">

Example 1. Patient K., 28, received a chemical burn of cornea and conjunctiva of both eyes of the I-II century When irritated eyes, photophobia, blepharospasm, conjunctival hyperemia of the lower arch, desquamation of the epithelium in the lower half of the diffuse corneal edema, muddy areas Kumanovo epithelium. Visual acuity in both eyes 0,3, not also corrected. Appointed local treatment offered by the ointment. By the end of the day the patient was subjectively noted significant improvement. Decreased pain in the eyes, watery eyes. Epithelialization of the cornea defects noted after 48 hours full cure is achieved after 7 days of treatment. The cornea is a transparent, visual acuity of 1.0 in both eyes.

Example 2. Patient A. 24 years, Turner, when working on a lathe injured right eye. An ophthalmologist turned through the day. After removal of the foreign body of the cornea (metal shavings) the patient was hospitalized with the diagnosis: right eye: traumatic keratitis, visual acuity of 0.1 not also corrected. The left eye is healthy, the visual acuity of 1.0.

Upon entering the cornea is determined by the infiltration of 3 mm in diameter, gray in the center of the corneal epithelial defect, rapidly increased fluorescein. In Auteuil treatment: sulfacetamide 30% 4 times and offer ointment 4 times a day. After 2 days of treatment marked clinical improvement. Decreased irritation phenomena infiltration in the cornea was clear, reduced in diameter, began epithelization on the periphery. Complete epithelialization occurred on day 5 of treatment, infiltration resorbed completely on the 7th day of treatment. Formed gentle blackvideo turbidity with a diameter of 2 mm visual Acuity recovered to 0.8. Cytological study of the co content of the oral pathogenic not found.

Example 3. Patient D., 51 years old, was admitted to the hospital UFRII eye disease diagnosis: marginal keratitis in the right eye, the left eye is healthy. Visual acuity at admission: right eye 0,8, not the interviewer. the left eye of 1.0. When entering the right eye is irritated, pericorneal injection at the periphery of the cornea at the limbus at the Meridian of 5 hours three-point infiltrate gray, painted by fluorescein. After 48 hours. after 4 times, the local treatment of the proposed ointment observed decrease photophobia, watery eyes, pericorneal injection, decreased intensity of staining infiltrates. Infiltrates apostiles decreased in size. Complete resorption of infiltrates was observed on the 6th day of treatment the mini-tests allow us to conclude that the proposed ointment has a high therapeutic effect in the keratitis of different etiology and burns, due to the optimal allocation of components ointment with bactericidal, regenerating, anti-inflammatory action. Compared to the prototype (cream with rosehip oil) timing of recovery decreased by 7-14 days.

Eye ointment containing medicinal substances and the basis - methylcellulose, glycerine, emulsifier T-2, water, characterized in that it as a medicinal substances contains Kartalin, methyluracil and gentamicin sulfate in the following ratio, wt.

Kartalin 2,5 5,0

Methyluracil 0,5 1,0

Gentamicin sulfate 0,08 0,3

The methylcellulose 1 3

Glycerin 7 15

Emulsifier T-2 0,5 2,0

Water Ostalnoe

 

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where B is one of the divalent residues and) g)

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X, l, m, n and R1R7have the following meanings:

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R3and R4the same or the difference is,

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