The treatment for eye disease with metronidazole

 

The invention relates to medicine, namely to the pharmacy and is used for treatment of keratitis and conjunctivitis. We offer gel contains metronidazole as the active substance, a buffer solution consisting of sodium tetrabromo-acid, gel base, which consists of a copolymer of styrene with maleic anhydride and purified water in the following ratio, wt.%: metronidazole is 0.5; sodium Teterboro acid 0,018; a copolymer of styrene with maleic anhydride and 1.0; purified water up to 100.0. The offered gel is extended and has antiviral, anti-inflammatory and antibacterial action, convenient and hygienic to use. 3 Il., 1 PL.

The present invention relates to medicine, namely to the pharmacy and the development of a medicine containing metronidazole, and can be used for the treatment of eye diseases, including keratitis (acanthopanax and herpes) and conjunctivitis.

Known drug with antiviral action, "for the treatment of herpetic keratitis”, which contains a copolymer of styrene with maleic anhydride (SMA) and purified water /1 the d of the present invention to the technical essence and the achieved result.

However, the known drug, containing 1% aqueous solution of SMA, has the following disadvantages. Therapeutic effect of SMA has an antiviral effect in the eye tissues, but has no activity against protozoa and obligate anaerobic bacteria and has no anti-inflammatory action.

Object of the invention is the creation of new medicinal products domestic production in the form of a gel containing metronidazole, buffer solution and the gel base, which has anti-inflammatory, antibacterial action and is effective against protozoa with good fixation and a uniform distribution in the tissues of the eye through a gel base, ease of use, expressed in the prolonged action of the drug.

The technical result - the reduction of terms of treatment of patients in the treatment of eye diseases, including keratitis (acanthopanax and herpes) and conjunctivitis due to the possibility of a good fixation on the eye tissues, prolonged action, as well as the convenience and hygiene applications.

This object is achieved in that the gel for the treatment of eye diseases, including keratitis (acanthopanax, gerpeticheskoy simple, antimicrobial and anti-inflammatory action; a buffer solution containing sodium Teterboro acid and purified water, providing the necessary pH value of from 6.2 to 7.0, suitable for ophthalmic dosage forms; gel base, which includes a copolymer of styrene with maleic anhydride and water treated with antiviral action and providing prolonged drug action due to the surface-active properties in the following ratio, wt.%:

Metronidazole 0,5

Sodium tetraborates 0,018

The copolymer of styrene

with maleic anhydride 1

Purified water To 100

All components included in the composition of the gel is allowed for medical use. Metronidazole (FS 42-2283-93). A copolymer of styrene with maleic anhydride (SMA) or modified stromal “Plastigel” redkosty swollen polymer (“agent for the treatment of herpetic keratitis”, patent No. 2135187, 1999, IPC AND 61 TO 31/765), (TU 6-01-02274010913-01) is the product of copolymerization of styrene with maleic anhydride modified with ammonia, is a white powder. The appearance of a 1% solution of a copolymer of styrene in water - clear or slightly cloudy liquid-gel. Rastvorimii was established, that 1% gel base provides reliable fixation of the drug to the eye tissues, contributes to better dissolution of metronidazole in the base, thin, smooth and continuous smear, gel-based has a prolonged action and increases the bioavailability of metronidazole through the surface-active properties, and buffer solution helps to maintain the required pH. Giving drug forms gel provides convenience and hygiene applications, the drug forms a fixed thin raspolzalsya film, the storage stability.

In addition to the manifestations of the known properties of each component in the inventive composition in combination enhances its effect, because, obviously, their synergism.

Example 1. The composition 100,0 eye gel: metronidazole is 0.5; sodium Teterboro acid 0,018; SSMA 1,0; purified water up to 100.0. Get eye gel as follows. In a beaker in a water bath in water treated (FS 42-2619-97) at a temperature of 100°C. dissolve the sodium Teterboro acid (GOST 8429-77), metronidazole (FS 42-2283-93) and stirred until dissolved, then add a copolymer of styrene with maleic anhydride, stirred by the stirrer and leave to swell for 60 min rodny transparent gel, density 1.0 g/cm3pH gel 6,2, refractive index n=1,3348 that ensures no reduction in visual acuity at the time of introduction of gel due to refraction. The resulting gel has a normal consistency, it is easy to spread on the conjunctiva of the eye to form a thin smooth continuous stroke, the gel due to the texture and physico-chemical properties of the gel base is firmly held on the mucosal surface (conjunctiva) of the eye and at the expense of those surface-active substances has a prolonged action of metronidazole, as well as convenient and hygienic to use, because the proposed composition of the ingredients.

Example 2. The composition 100,0 eye gel: metronidazole 1,0; sodium Teterboro acid 0,018; SSMA 1,0; purified water up to 100.0. Make the gel in the same way. The resulting gel has a normal consistency, but during storage after 5 days, the gel becomes opaque and formed white flakes microscopy, which confirms the presence of hexagonal crystals of metronidazole, which is unacceptable in ocular dosage form.

Example 3. The composition 100,0 eye gel: metronidazole is 0.5; sodium Teterboro acid 0,018; SSMA 2,5; purified water up to 100.0. Make gel similar obrazom conjunctive surface, smear uneven, discomfort, decreased visual acuity due to refraction.

Example 4. The composition 100,0 eye gel: metronidazole is 0.5; sodium Teterboro acid 0,05; SSMA 1,0; purified water up to 100.0. Make the gel in the same way. The resulting gel has a normal consistency, but there are phenomena discomfort, burning, tearing, due to a high pH value of 8.5-9.0 in.

Example 5. The composition 100,0 eye gel: metronidazole is 0.5; sodium Teterboro acid 0,018; SSMA 1,0; purified water up to 100.0. Make the gel without heating in a water bath at room temperature in the same way. The obtained gel cloudy white color. Visible particles of undissolved drug. Observed phenomena discomfort, decreased visual acuity due to refraction.

Example 6. The composition 100,0 eye gel: metronidazole is 0.5; sodium Teterboro acid 0,018; SSMA 1,0; purified water up to 100.0. Make the gel in the same way. The resulting gel has a liquid consistency, which is explained by the low content of the underlying CSMA, and has reduced antiviral activity.

The given examples show that the optimal from the point of view of consistency, ease of use, effectiveness of treatment is part of the cornea in rats. Study of wound healing activity of the gel with metronidazole was conducted on Mature white rats without regard to gender weighing 180-220 g, were divided into three groups. In the first group of 6 animals, and in the rest of the group 4 experimental animals in each. Under ether anesthesia (with exposure time of 2-3 min) produced by excision of the superficial layers of the cornea of the left eye of rats microsurgical blade (under microscopic control), at a depth of 1/2 of the thickness of the cornea in the Central part of the area up to 1/3 of the area of the cornea. In two cases there was perforation of the cornea. These animals were not included in the overall statistics. In the postoperative period every day, 2 times a day produced applying eye ointment gel 1% (first group), gel metronidazole 0,5% (the second group), baselinevaloe basis (the third group). The removal of animals from the experiment made on the 3rd, 7th and 14th day. When performing experimental and morphological studies on the first term breeding animals of the experiment (3 days) in all three groups were observed complete epithelialization of the defect of the cornea. In this regard, the analysis of the morphological data was performed to normalize the structure of the epithelium. The thickness of the epithelium was assessed by cm parameters; the presence of “+”, no “-”; differentiation of layers of epithelium-point system: one point - no, two ball - weak, three ball - full (table). When performing experimental and morphological studies for a third term breeding animals of the experiment (14 days) in the first group (gel 1%) observed reduction of blood capillaries, the epithelium uniform, under the epithelium typical of the basal membrane is not formed. In stroma evenly distributed keratoplasty, which corresponds to the norm, and the thickness of the stroma is 100 μm (Fig.1). Next, during injection of the experiment (14 days) in the second group (gel metronidazole) structure of all layers of the cornea restored, with stroma thickness of 90 μm. The thickness of the epithelium 20-25 μm, consists of 5 layers of cells, which clearly differentiates uniformly distributed keratoplasty, restored the basal membrane. Cells of the basal layer of the epithelium have rounded nuclei, which gradually flattened to the surface layers. Not broken and the structural integrity of endothelial cells, i.e., is a full restoration of the epithelium (Fig.2). In the third group (veselinova base) obviously deceleration regeneration, thinning of the stroma and nevosstrebovannosti epithelium during defect, the thickness of the stroma is 60 μm (Fig.3).

In the early stages of healing on the day 3 is determined by the formation of a complete epithelium in the control series is also determined formed epithelial cover, but there are no signs of its structural organization. Thus, on the basis of morphological studies of the inventive gel with metronidazole for the treatment of diseases of the eye accelerates regeneration and differentiation.

Monitoring patients showed a positive effect eye gel, and the amount of damage of the drug at a given ratio of components is the same. This allows the doctor in practical medicine, depending on the form and severity of the disease to recommend to patients applying eye gel on the conjunctiva independently, which makes the inventive gel promising dosage form ophthalmic practice. After conducting a full-scale clinical trials for the treatment of diseases of the eye - keratitis (acanthopanax, herpes), conjunctivitis and development of quality control methods planned design monograph.

Sources of information

1. Cure for herpes Coeur is etenia

For the treatment of eye diseases, including keratitis, acanthopanax, herpes and conjunctivitis, containing a copolymer of styrene with maleic anhydride and purified water as a gel base, characterized in that it additionally contains metronidazole and sodium tetraborates in the following ratio, wt.%:

Metronidazole 0,5

Sodium tetraborates 0,018

The copolymer of styrene

with maleic anhydride 1,0

Purified water Up to 100.0

 

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