RU2595837C2 - Composition and method of producing eye drops - Google Patents

Abstract

FIELD: pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics, particularly to ophthalmology, and invites methods of getting pharmaceutical compositions in the form of eye drops for local treatment of inflammatory eye diseases of microbial genesis and bacterial infections in humans and animals. Methods are characterized by the fact that an aqueous solution of methylcellulose according to method 1 or hydroxypropyl methylcellulose according to method 2 at a temperature of 80-90 °C with further cooling to room temperature. Preparation of a solution of boric acid at a temperature of 75-85 °C with further cooling to 50-60 °C, dissolving fluroquinolone compound and sodium chloride in a solution of boric acid with subsequent cooling to room temperature, introduction of an aqueous solution of methylcellulose, homogenization prepared solution, bringing the solution with sodium hydroxide to pH 6-8, carrying out steps of sterilizing filtration and aseptic filling; as an antibacterial fluroquinolone connection one of quinolone, namely lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacine, or moxifloxacin, or gatifloxacin, or gemifloxacin, or their acceptable salts.

EFFECT: preparing the pharmaceutical compositions.

2 cl, 9 tbl

Description

The invention relates to the field of the pharmaceutical industry, in particular to the production of medicines from fluoroquinolones used for topical treatment of inflammatory eye diseases of microbial origin and bacterial infections in humans or animals.

Fluoroquinolones are one of the drugs most widely used in the treatment of infectious diseases. Activity and a wide spectrum of action, effectiveness and relative safety make them suitable for the treatment of common infections and hospital infections.

Fluoroquinolones (English fluoroquinolones) - a group of drugs with pronounced antimicrobial activity, widely used in medicine as broad-spectrum antibiotics. In terms of the breadth of the spectrum of antimicrobial activity, activity, and indications for use, they are really close to antibiotics, but differ in chemical structure and origin (antibiotics are products of natural origin or close synthetic analogs of those, while quinolones do not have a natural analogue).

Fluoroquinolones are a class of antibacterial drugs that have a pronounced bactericidal effect, inhibiting DNA hydrase and inhibiting DNA synthesis in a microbial cell. They have a wide spectrum of antibacterial action. Active against gram-positive and gram-negative microorganisms: Pseudomonas aeruginosa; Escherichia coli; Enterococcus; Campybacter spp .; Legionella spp .; Mycoplasma spp .; Chlamydia; Mycobacterium spp .; Haemophilus influenze; Shigella spp .; Salmonella spp .; Neisseria meningitidis; N. gonorrhoeae, some strains of Staph, spp. (producing and not producing penicillinase).

Quinolone drugs have been successfully used for 30 years to treat a wide range of bacterial infections of various localization, including the treatment of severe mono-infections, and occupy one of the important places in the series of highly effective chemotherapeutic agents. During all these years, research on the search and development of new quinolones with the aim of increasing the degree of activity, expanding the spectrum of action, optimizing pharmacokinetics, tolerance and safety has been intensively developed.

Of the drugs of the quinolone group, lomefloxacin, ofloxacin, ciprofloxacin, levofloxacin, sparfloxacin and moxifloxacin are included in the list of vital and most important drugs.

Preparations of this group are used to treat infectious diseases of the eyelids, lacrimal organs, conjunctiva (including for the treatment of trachoma and paratrachoma), the cornea, and also for the prevention of infectious complications after eye operations and injuries.

Fluoroquinolones penetrate well through the intact corneal epithelium into various tissues of the eye. The therapeutic concentration is achieved in the cornea and the anterior chamber moisture 10 minutes after topical application and persists for 4-6 hours. When applied topically, fluoroquinolones are partially reabsorbed into the systemic circulation. Their half-life is on average 4-5 hours. Fluoroquinolones are actively metabolized in the liver and excreted in the urine and bile.

For topical treatment and prevention of various ocular infectious diseases, fluoroquinolones can be used as an eye ointment (Ciplox®, Cipla Ltd .; Floxal®, Baush & Lomb), but more often they are used in the form of eye drops containing as active substance: ciprofloxacin (Cipromed ®, Promed Exp .; Ciloxan®, Alcon; Ciprolet®, Dr. Reddy's Lab.), Ofloxacin (Floxal®, Baush &Lomb; Uniflox®, Unimed Pharma; Ocuflox®, Allergan; Tarivid®, Santen Pharmaceutical Co.), norfloxacin (Chibroxin®, MSD BV; Normax®, IPCA Lab .; Norflox®, Cipla), lomefloxacin (Okacin®, Novartis Ophth.), gatifloxacin (Zymar®, Allergan), moxifloxacin (Vigamox®, Alcon) and levofloxacin (Ofth ®, Santen Oy), rel. yaschiysya to third-generation fluoroquinolones.

Fluoroquinolones (PF) have taken a central place in the treatment of eye infections due to the high number of resistant pathogens to antibiotics: gentamicin, tetracycline, chloramphenicol, erythromycin, azithromycin, vancomycin and other drugs. The first report in the local literature on the local application of PF in eye infections was published in 1991. First, ciprofloxacin eye drops 0.3% (Cipromed, Ciprofloxacin-AKOS), ofloxacin 0.3% (Phloxal, Uniflox), norfloxacin 0.3% (Normax), later lomefloxacin 0.3% (Okacin, Lofox) entered our practice. ) In recent years, levofloxacin 0.5% (Oftaquix), Signicef, has been actively involved in the practice. Received permission to use moxifloxacin 0.5% (Vigamox). Gatifloxacin 0.3%, sparfloxacin 0.3%, travofloxacin 0.5%, besifloxacin 0.6% are studied abroad in the form of eye drops.

Trade name of the preparation: UNIFLOX, international nonproprietary name: ofloxacin, dosage form: ear and eye drops.

The composition of a 5 ml solution contains: active substance: ofloxacin 15 mg, excipients: sodium phosphate dodecahydrate, sodium dihydrogen phosphate dihydrate, benzalkonium chloride, purified water up to 5 ml.

Lomefloxacin in the form of eye drops "Okatsin" is considered the first choice in humanitarian ophthalmology.

OKACIN (OKACIN) - Lomefloxacin, manufacturer: USA Vision Ophthalmics.

Composition and form of release - Eye drops 0.3%, 1 ml:

lomefloxacin 3 mg;

other ingredients: disodium EDTA, glycerol, sodium hydroxide, water for injection, preservative: benzalkonium chloride.

Norfloxacin (Normax eye drops), the main active ingredient in Normax eye drops is norfloxacin. 1 ml of the drug contains 3 mg of norfloxacin. The preparation also includes excipients: disodium edetate, sodium chloride, benzalkonium chloride and water for injection.

Oftaquix is a broad-spectrum antimicrobial drug from the group of fluoroquinolones for use in ophthalmology, a 0.5% ophthalmic solution contains 5 mg of levofloxacin, benzalkonium chloride, sodium chloride, hydrochloric acid, sodium hydroxide, and purified water.

There is also the drug Signicef 0.5% eye drops with the active ingredient - levofloxacin hemihydrate, equivalent to levofloxacin 5 mg / ml levofloxacin (in the form of hemihydrate) - 5 mg.

Excipients: benzalkonium chloride, sodium chloride, sodium hydroxide, hydrochloric acid, water d / and.

Dosage regimen Signignef:

Locally, in the affected eye. 1-2 drops into the affected eye (a) every two hours up to 8 times a day during wakefulness for the first 2 days, then four times a day from 3 to 5 days. The duration of the course of treatment is determined by the doctor, usually 5 days. With the simultaneous use of any other topical eye preparations, at least a 15-minute interval between instillations of different drugs is necessary.

Eye drops of 0.5% moxifloxacin are manufactured by Alcon Pharmaceuticals LLC under the trade name Vigamox, eye drops. Composition per 1 ml of the drug.

Active ingredient: moxifloxacin hydrochloride 5.45 mg equivalent to moxifloxacin 5 mg.

Excipients: sodium chloride, boric acid, hydrochloric acid and / or sodium hydroxide to adjust the pH, purified water.

International nonproprietary name: Gatifloxacin (Gatifloxacin).

The dosage form of an eye drop is 0.3%, 5 ml. Ultramed Gatifloxacin (Gatifloxacin) Med-Interplast (India) Pvt. Ltd / AKUMS DRUGS & PHARMACEUTICALS Ltd., India.

The composition of 1 ml of the drug contains: the active substance 3 mg of gatifloxacin; excipients: benzalkonium chloride, mannitol, disodium edetate, hydrochloric acid, sodium hydroxide, water for injection.

The above examples confirm that at present, based on the proposed quinolones, eye forms have been developed only in the form of eye drops and then only for some quinolones. The disadvantage of eye drops is a short period of therapeutic action. This necessitates their frequent installation, which poses a danger to the eye. The disadvantage is that the ophthalmologist’s arsenal of eye drops with fluoroquinolones is in most cases represented by aqueous solutions that are not able to provide a therapeutic effect, since they are quickly removed from the surface of the eyeball. For example, when treating with eye drops, an aqueous solution of norfloxacin in acute cases is instilled with 1-2 drops into the affected eye from 2 to 4 times per hour, as the symptoms of inflammation subside, the frequency of instillations is reduced to 3-6 times a day. Frequent installations of the aqueous solution wash away the tear fluid containing lysozyme, and thereby create the conditions for infection. As a result, it is not possible to achieve a constant concentration of fluoroquinolone in the eye tissues necessary for therapy. It is necessary to recommend installations up to 6 or more times a day, which is inconvenient for the patient, increases the likelihood of developing a secondary infection by reducing the concentration of natural defense factors, and also increases the likelihood of allergic reactions. The above indicates the need to create viscous eye drops with highly effective fluoroquinolone of a wide spectrum of action, which slow the rapid leaching of drugs from the conjunctival sac.

Similar in technical solution is the patent application No.2015454545 (RU) "PHARMACEUTICAL COMPOSITION CONTAINING A FLUORCHINOLONE ANTIBIOTIC MEDICINE".

An application for an invention discloses an aqueous pharmaceutical composition comprising moxifloxacin and a pharmaceutical carrier for moxifloxacin, wherein the pharmaceutical carrier comprises:

i. sodium chloride in an amount providing a weight / volume ratio of sodium chloride to moxifloxacin in the range from 0.8 to 2.0;

ii. a surfactant that promotes the uniform distribution of moxifloxacin on a pharmaceutical carrier, where the surfactant is a polyether alcohol;

iii. borate / polyol complex antimicrobial agent

iv. xanthan gum.

The disadvantage of this composition of the pharmaceutical composition is the use of xanthan gum. Xanthan gum is a naturally occurring polysaccharide produced by Campestris Xanthomonas from sugar and molasses. It is resistant to enzymes, it is a ballast substance that is not absorbed by the body; possesses high viscosity even at low concentration; has the ability to create a film.

The closest in technical solution is the patent WO No. 0240028 (A1) dated 11.16.2000, "ANTIBACTERIAL GELEOFIC EYE DROPS". The invention discloses antibacterial gel-like eye drops containing levofloxacin, ofloxacin, moxifloxacin or pharmaceutically acceptable salts as the active ingredient, which provide an increased bioavailability of the drug with little chance of side effects. Antibacterial gel-like eye drops contain antibacterial substances and gellan gum, which contains an antibacterial agent, and at least one element selected from the group consisting of levofloxacin, ofloxacin, moxifloxacin and pharmaceutically acceptable salts. In the case of applying eye drops to the eyes, the concentration of antibacterial agents is three times or more higher in the conjunctiva than the concentration of the same preparation, but not containing gellan gum.

The disadvantage of this composition of eye drops is the use of gellan gum. It has a harmful effect on the human body due to the presence of impurities and is not approved for use on the territory of the Russian Federation.

To increase the viscosity of eye drops, oils were previously used (sunflower refined, peach or apricot). However, synthetic hydrophilic macromolecular compounds, such as methyl cellulose (0.5-2%, the amounts necessary to achieve prolonged action of the eye drops), Na - carboxymethyl cellulose salt (0.5-2%), polyvinyl ( 1.5%), microbial PS aubazidan (0.1-0.3%), polyglucin, etc. These substances do not irritate the mucous membrane of the eye, and are also compatible with many medicinal substances and preservatives. Their refractive index is similar to natural tears. They contribute to the restoration, stability and reproduction of the optical characteristics of the tear film.

The authors of this invention set themselves the task of creating pharmaceutical compositions in the form of eye drops with a wider spectrum of antimicrobial activity for the local treatment of inflammatory eye diseases of microbial origin and bacterial infections in humans or animals, including an antibacterial quinolone compound, namely lomefloxacin, or norfloxacin, or pefloxacin or levofloxacin, or sparfloxacin, or moxifloxacin, or gatifloxacin, or hemifloxacin, or their pharmaceutically acceptable salts.

The authors also set themselves the task of obtaining an ophthalmic dosage form, namely, eye drops, which do not irritate the mucous membrane of the eye, do not wash lysozyme from the mucous liquid, and which achieve comfort when using eye drops of the drug.

The authors also set themselves the task of reducing the frequency of installations of eye drops by 2 times and at the same time achieve the required time of contact with the tissues of the eye without much prolongation.

The mucous membrane of the eye is the most sensitive of all the mucous membranes of the body. She reacts sharply to external stimuli. The tear fluid is a protective barrier for microorganisms due to the presence of lysozyme (the enzyme muromidase) in it.

When using eye drops based on fluoroquinolones, side effects are possible - “dry eye syndrome”, therefore, the authors also set the task to solve this problem. “Dry eye syndrome” is a disease accompanied by characteristic complaints of an unpleasant sensation in the eyes, pain, dryness, a foreign body feeling in the eye and objective signs of decreased tear production, violation of the precorneal lacrimal film, and with the development of the disease - damage to the cornea.

The tasks are solved in that experimentally selected formulations and methods for producing pharmaceutical compositions in the form of eye drops based on active ingredients, namely lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacin, or moxifloxacin, or gatifloxacin, or heme their pharmaceutically acceptable salts. To reduce the frequency of installation of eye drops and to achieve the necessary contact time with eye tissues, as well as to eliminate the side effect - “dry eye syndrome”, work was carried out on the experimental selection of high molecular weight compounds (IUDs), as well as their quantitative ratios. Methyl cellulose and hydroxypropyl methyl cellulose were chosen as IUDs.

The technical result of the invention is expressed in the creation of compositions and methods for producing pharmaceutical compositions in the form of eye drops based on active ingredients, namely lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacin, or moxifloxacin, or gatifloxacin, or gemifloxacin acceptable salts, characterized by higher activity against gram-positive bacteria (primarily pneumococci), intracellular pathogens, anaerobes (Ch lamydia spp., Mycoplasma spp., M. tuberculosis, fast-growing atypical mycobacteria (M. avium, etc.), anaerobic bacteria (moxifloxacin), while activity against gram-negative bacteria is not reduced.

Designations:

MFC - moxifloxacin;

CFC - ciprofloxacin;

OFC - ofloxacin;

LFC - levofloxacin;

LMC - lomefloxacin;

SFC - sparfloxacin;

HFC - gatifloxacin;

MSSA - S. aureus sensitive to methicillin;

MRSA - S. aureus resistant to methicillin;

MS - methicillin sensitive;

MR - resistant to methicillin.

The greatest activity in vitro against gram-positive bacteria is moxifloxacin.

Designations:

MFC - moxifloxacin:

HFC - hemifloxacin;

CFC - ciprofloxacin;

OFC - ofloxacin.

HFC has the highest activity; the activity of MFCs against Staphylococcus aureus, sensitive to CPC, is 2 times higher than the activity of HFCs.

Designations:

MFC - moxifloxacin;

CFC - ciprofloxacin;

OFC - ofloxacin;

LFC - levofloxacin;

LMC - lomefloxacin;

SFC - sparfloxacin;

HFC - gatifloxacin.

The highest in vitro activity among fluoroquinolones with respect to Enterobacteriaceae is possessed by HFC.

Designations:

MFC - moxifloxacin;

CFC - ciprofloxacin;

OFC - ofloxacin;

LFC - levofloxacin;

LMC - lomefloxacin;

SFC - sparfloxacin;

HFC - gatifloxacin.

* Acinetobacter spp.

When working out the compositions, the authors also obtained unexpected effects:

- Eye drops may be contaminated with microorganisms during use. In this regard, there is a need to add preservatives to the eye drops, which inhibit the growth and reproduction of microorganisms and, as a result, a decrease in the activity of the active substance during the entire time of use. In existing eye drops based on fluoroquinolones, benzalkonium chloride is mainly used as a preservative. Benzalkonium chloride, along with its high antimicrobial activity and good solubility in water, is not stable during thermal sterilization, as its aqueous solutions are unstable at elevated temperatures. When testing the compositions, the authors tested some preservatives, in particular benzalkonium chloride, methylparaben (nipagin), a mixture of methylparaben and propylparbene (nipazole). During the experimental work, it was also unexpectedly found that lomefloxacin, norfloxacin, pefloxacin, levofloxacin, or sparfloxacin, or moxifloxacin, or gatifloxacin, or gemifloxacin, or their pharmaceutically acceptable salts, due to their wider spectrum of antimicrobial action, allow to obtain pharmaceutical compositions in the form of eye drops with or without preservatives without reducing the activity of the active substance during use. When conducting experimental work, the authors unexpectedly found that the introduction of preservatives into the pharmaceutical composition leads to the appearance of the irritating effect of eye drops. In accordance with this, compositions have been developed that make it possible to make eye drops based on the above active substances without the use of preservatives.

- When developing pharmaceutical compositions in the form of ophthalmic dosage forms based on lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacin, or moxifloxacin, or gatifloxacin, or hemifloxacin, or their pharmaceutically acceptable salts, it was unexpectedly found to reduce the frequency of installation of eye drops and to achieve the necessary time of contact with the tissues of the eye without much prolongation, 0.1-0.3% methylcellulose solution or 0.05-0.1% rast thief of hydroxypropyl methylcellulose. They are hydrophilic polymers that bind aqueous solutions well.

Soluble methyl cellulose - cellulose ether and methanol. Aqueous solutions of methylcellulose have a high sorption, emulsifying and wetting ability. 0.5-1% aqueous solutions are used in the technology as thickeners and stabilizers, for hydrophilization of hydrophobic bases of ointments and liniments, as an emulsifier and stabilizer in the manufacture of suspensions and emulsions, and also as a prolonging component for eye drops. MC gels are stable over a wide pH range.

Hydroxypropyl methylcellulose (HPMC) is a polymer compound. It is soluble in water in any proportions with the formation of a transparent liquid of various viscosities, depending on the type of HPMC. With increasing temperature or mixing speed, the viscosity reversibly decreases. As a result of the non-ionic structure, HPMC solutions are stable to various pH values in the range from 3 to 11. HPMC is part of artificial tears. Artificial tears are commonly used to treat a disease known as keratoconjunctivitis, or dry eye syndrome.

The introduction of MC or HPMC in the composition of the pharmaceutical composition allows to fill the deficit of the tear fluid, stabilizes and reproduces the optical characteristics of the tear fluid, because the refractive index of solutions of MC and HPMC is similar to natural tears. They contribute to the restoration, stability and reproduction of the optical characteristics of the tear film.

The proposed compositions of the pharmaceutical compositions in the form of eye drops also allow you to evenly distribute the active substance over the mucous membrane.

The antimicrobial activity of the developed eye drops in vitro was determined on strains of microorganisms that most often cause bacterial eye damage. The antimicrobial activity of the developed pharmaceutical compositions was determined by the method of serial dilutions. In the experiment used samples of test strains of microorganisms: Staphylococcus aureus 209P, Ε. coli ATCC 25922, P. aeruginosa ATCC 27853. The studied samples of eye drops showed activity against all test microbes. There were no significant differences between the antimicrobial activity of samples with and without preservatives. The studies conducted allow us to conclude that the developed antimicrobial activity of the developed eye drops in vitro is sufficient for strains of microorganisms that most often cause bacterial eye damage.

The technical solution is the compositions of pharmaceutical compositions based on lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacin, or moxifloxacin, or gatifloxacin, or hemifloxacin, or their pharmaceutically acceptable salts, as an active substance for the preparation of new pharmaceutical forms based on them drops and methods for their preparation.

A pharmaceutical composition is provided in the form of eye drops for topical treatment of inflammatory eye diseases of microbial origin and bacterial infections in humans or animals, including an antibacterial quinolone compound and target additives, characterized in that it does not contain preservatives, and one of the compounds is selected as an antibacterial quinolone compound a number of quinolones, namely: lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacin, or moxifloxacin, or gatiflox qing, or hemifloxacin, or their acceptable salts, wt. %:

A method of obtaining a pharmaceutical composition includes preparing an aqueous solution of methyl cellulose at a temperature of 80-90 ° C, followed by cooling to room temperature, preparing a solution of boric acid at a temperature of 75-85 ° C, followed by cooling the solution to 50-60 ° C, dissolving the fluoroquinolone compound and sodium chloride in a solution of boric acid, followed by cooling to room temperature, the introduction of an aqueous solution of methylcellulose, homogenization of the prepared solution, bringing the solution with sodium hydroxide about pH 6-8, carrying out a step of sterilizing filtration and aseptic filling.

A method of obtaining a pharmaceutical composition includes preparing an aqueous solution of hydroxypropyl methylcellulose at room temperature, preparing a solution of boric acid at a temperature of 75-85 ° C, followed by cooling the solution to 50-60 ° C, dissolving the fluoroquinolone compound and sodium chloride in a solution of boric acid, followed by cooling to room temperature temperature, introducing an aqueous solution of hydroxypropyl methylcellulose, homogenizing the prepared solution, adjusting the solution with sodium hydroxide to a pH of 6-8, e stages of sterilizing filtration and aseptic filling.

The compositions of the pharmaceutical compositions in the form of eye drops are shown in Appendix 1 (see table 1).

A few specific options for the composition of eye drops based on moxifloxacin:

As an active substance, it is possible to use any of the claimed fluoroquinolone compounds in these compositions.

The claimed composition and method of obtaining a pharmaceutical composition in the form of eye drops make it possible to obtain a dosage form in the form of eye drops that do not irritate the mucous membrane of the eye; with a refractive index that does not affect the quality of vision; halving the frequency of installation of eye drops; allowing to achieve the necessary contact time with the tissues of the eye without much prolongation, as well as eliminating the side effect - “dry eye syndrome”.

Also, the proposed compositions of the pharmaceutical composition allowed us to solve other problems: obtaining an ophthalmic dosage form that does not wash lysozyme from the mucous membrane, which allows to achieve comfort during use, as well as preserving the quality of the drug during storage.

The claimed ratio of components allows you to get eye drops that preserve the activity of the active substance (fluoroquinolone) during the shelf life (2 years). The results of the analyzes of some pharmaceutical compositions during storage during the expiration date are given in the Appendix (tables 2-3).

References

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4. The State Pharmacopoeia of the USSR. XI ed., Vol. 2. - M .: Medicine, 1990.

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9.http: //www.eyemed.ru.

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Known eye drops containing 0.5% levofloxacin (Signetsef®, Oftaquix®, L-Optic Rompharm®), 0.3% levofloxacin (Lofox®, Okatsin®), 0.3% norfloxacin (Normax®), but the technical result The formulations of eye drops of fluoroquinoles developed by us differ favorably from the above formulations, because our formulations possess viscous properties that allow achieving optimal duration of contact with eye tissues, which leads to a reduction in the frequency of instillation of eye drops, do not affect the quality of vision, eliminate the side effect of “dry eye syndrome”, have high stability during storage and use and high antimicrobial activity.

Claims (2)

1. A method of obtaining a pharmaceutical composition in the form of eye drops for topical treatment of inflammatory eye diseases of microbial origin and bacterial infections in humans or animals, comprising preparing an aqueous solution of methylcellulose at a temperature of 80-90 ° C, followed by cooling to room temperature, preparing a solution of boric acid at a temperature of 75-85 ° C, followed by cooling the solution to 50-60 ° C, dissolving the fluoroquinolone compound and sodium chloride in a solution of boric acid, followed by cooling to omnatnoy temperature, the introduction of an aqueous methylcellulose solution, homogenizing the prepared solution, sodium hydroxide, adjusting the solution to pH 6-8, conducting step sterile filtration and aseptic filling;
and at the same time contains as an antibacterial fluoroquinolone compound one of the compounds of a number of quinolones, namely lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacin, or moxifloxacin, or gatifloxacin, or gemifloxacin, or their acceptable salts, in the following ratio, .%: fluoroquinolone compound - 0.1-0.9; sodium chloride - 0.12-1.16; boric acid - 0.06-0.54; methyl cellulose - 0.1-0.3; sodium hydroxide to bring to a pH of 6-8; purified water - up to 100. 2. A method of obtaining a pharmaceutical composition in the form of eye drops for topical treatment of inflammatory eye diseases of microbial origin and bacterial infections in humans or animals, comprising preparing an aqueous solution of hydroxypropyl methylcellulose at room temperature, preparing a solution of boric acid at a temperature of 75-85 ° C, followed by cooling of the solution up to 50-60 ° C, dissolving the fluoroquinolone compound and sodium chloride in a solution of boric acid, followed by cooling to room temperature, introduction an aqueous solution of hydroxypropyl methylcellulose, homogenizing the prepared solution, adjusting the solution with sodium hydroxide to a pH of 6-8, performing a sterilizing filtration and aseptic filling step;
and at the same time contains as an antibacterial fluoroquinolone compound one of the compounds of a number of quinolones, namely lomefloxacin, or norfloxacin, or pefloxacin, or levofloxacin, or sparfloxacin, or moxifloxacin, or gatifloxacin, or gemifloxacin, or their acceptable salts, in the following ratio, .%: fluoroquinolone compound - 0.1-0.9; sodium chloride - 0.12-1.16; boric acid - 0.06-0.54; hydroxypropyl methylcellulose - 0.05-0.1; sodium hydroxide to bring to a pH of 6-8; purified water - up to 100.