Eye drops and method for their obtaining

FIELD: pharmaceutics.

SUBSTANCE: the present innovation deals with medicinal preparations designed as solution and indicated for therapeutic needs. Eye drops contain ciprofloxacin hydrochloride monohydrate being equivalent to 0.3% free foundation, a buffer system that keeps pH within 3.5-5.5 interval, as a conserving agent - benzalconium chloride and a s a stabilizer - the salt of disodium ethylenediamine tetraacetic acid, moreover, their range of osmolality values correspond to 150-450 mM/kg H2O. Eye drops should be obtained by preparing buffer system in which mannitol should be dissolved followed by the salt of disodium ethylenediamine tetraacetic acid, benzalconium chloride, ciprofloxacin hydrochloride. Then one should perform the control for the quality of obtained solution to be then filtered by applying sterilizing elements and packed. This innovation provides treatment of eyes at creating the pressure in an eye and at certain desired osmolality.

EFFECT: higher efficiency of therapy.

4 cl, 1 ex

 

The invention relates to the pharmaceutical industry, namely to medicines, made in the form of a solution and is intended for therapeutic purposes, in particular the treatment of eye diseases.

Known eye drops "Ciprolet"that contain ciprofloxacin in an amount of 3 mg per milliliter, made in the form of infusion solution and eye drops (on the main page. Drugs in Russia: a Handbook. M: Attraversare, 2001, SB-691).

Known eye drops "Cipromed"that contain ciprofloxacin in an amount of 3 mg per milliliter (encyclopedia of drugs. The seventh edition revised and expanded. M: RLS. - 2000. - S).

Known aqueous compositions containing ciprofloxacin and the following components in the amounts specified hereinafter and expressed in % (wt./volume) (g/100 ml): (I) 0.12 to 0.6% ciprofloxacin hydrochloride monohydrate (equivalent to 0.1-0.5% of free base); (II) 0,5-3,0% buffer system capable of maintaining a pH in the range from 4 to 5; (III) 0,05-0,3% naanovo surfactant; (IV) water to 100 ml, which includes the following stages: a) the dispersion of a thickening agent in water at a temperature in the range from 20-90°to complete hydration of the thickener; (b) dissolving the surface naanovo-the active substance in water, adding obrazowej the solution to the solution of a thickener, obtained in the previous phase, and the subsequent addition of acetic acid corresponding to the buffer: acetic acid - sodium acetate, and other optional components; (C) dissolving sodium acetate, corresponding to the buffer: acetic acid - sodium acetate in water, and adding ciprofloxacin hydrochloride monohydrate, stirring until dissolved; (e) adding water while maintaining the pH in the range from 4.5 to 4.9 (RF Application 97107154/14. Aqueous compositions containing ciprofloxacin, their use and method of receipt. Publ. 20.05.1999).

Composition for treatment of inflammation of the middle ear with a perforation, including ciprofloxacin, further comprises a buffer system to maintain a pH of 4.0 to 5.0, naenae surfactant, thickener and water in a ratio of components, wt.%/about. (g/100 ml): ciprofloxacin hydrochloride monohydrate (equivalent to 0.1-0.5% of free base) - 0,12-0,6, a buffer system capable of maintaining a pH in the range from 4.0 to 5.0 - 0.5 to 3.0V, naenae surfactant is 0.05 to 0.3, the thickening agent is 0.5 to 2.0, water up to 100 ml (RF Patent 2165755. Publ. 27.04.2001).

However, the known composition intended for the treatment of otitis of the middle ear with a perforation, so that its composition does not allow to obtain the desired osmollnosti. In addition, it is not intended for the treatment of eye diseases.

C is the summer residence of the present invention is the development of a medicinal product on the basis of ciprofloxacin with the required osmollnosti, designed for treatment of eye diseases.

The problem is solved in that eye drops, including ciprofloxacin, a buffer system, a thickener in the form of mannitol, have a range of values of osmolality from 150 to 450 mmol/kg H2O, they contain ciprofloxacin hydrochloride monohydrate, which is equivalent to 0.3% of the free base, a buffer system, keeping pH in the range from 3.5 to 5.5, as preservative benzalkonium chloride, and the stabilizer is a salt, the disodium Ethylenediamine tetraoxane acid in the following ratio, wt.%/about. (g/100 ml):

Ciprofloxacin hydrochloride 0,315-0,385

Salt is the disodium Ethylenediamine tetraoxane acid 0,045-0,055

Mannitol 4,14-5,06

Sodium acetate 0,045-0,055

Benzalkonium chloride 0,009-0,011

Glacial acetic acid is 0.135-0,165

Water for injection to 100 ml

To receive them use the method comprising preparing a buffer system containing acetic acid and sodium acetate, and then in the buffer system dissolve mannitol, salt is the disodium Ethylenediamine tetraoxane acid, benzalkonium chloride, prepared in solution dissolve ciprofloxacin hydrochloride monohydrate and bring the volume of solution water for injection to 100 ml, get a pH in the range from 3.5 to 5.5, perform quality control of the obtained R is the target, then, it is filtered using sterile items, and poured.

It is advisable to simplify the use of sterile solution pour into 5 ml vials polymer cap-drip, which is screwing the cap.

In addition, to preserve the properties of the drug suitable for filling solution use bottles of orange glass and hermetically sealed with rubber stoppers, which compresses the aluminum caps.

The present invention explaining a detailed description and an example implementation.

The method of obtaining eye drops includes preparation of buffer systems, which is prepared from sodium acetate in the amount of 0.5 g and 500 ml of water for injection. Both components are mixed until complete dissolution. If necessary, a pH adjusting solution of acetic acid. In the resulting buffer solution dissolve mannitol in the amount of 46 g and again stirred until complete dissolution.

Then salt disodium Ethylenediamine tetraoxane acid in the amount of 0.5 g was dissolved in 100 ml of water for injection, heated to 50-70°C. the resulting solution was stirred until complete dissolution, cooled to a temperature of 20-25°and small portions poured into the received buffer solution. Benzalkonium chloride in an amount of 0.1 g was dissolved in 100 ml of water for injection. Gently PE amerivault, preventing foaming. The prepared solution benzalkonium chloride gradually poured in small portions into the buffer solution. To this solution add ciprofloxacin in the amount of 3.5 g and mixed until complete dissolution. Then bring the volume of solution water for injection up to 1 liter and stirred for 20-30 minutes.

Quality control is carried out, selecting a sample solution for analysis. In laboratory conditions determine the pH and the amount of ciprofloxacin hydrochloride.

When the discrepancy between the pH of the solution perform the adjustment solution of acetic acid.

The solution, having a range of values of osmolality from 150 to 450 mmol/kg H2Oh, in the following ratio, wt.%/about. (g/100 ml): ciprofloxacin hydrochloride - 0,35, salt disodium Ethylenediamine tetraoxane acid is 0.05, mannitol - 4,6, sodium acetate - 0.05, benzalkonium chloride is 0.01, the solution of acetic acid is 0.15, water for injection to 100 ml, transfer to sterile filtration, which is carried through the filter elements with pore sizes of 0.45 and 0.22 μm, poured into 5 ml vials polymer cap-drip, which is screwing the cap.

In addition, bottling use vials amber glass, hermetically sealed rubber tubes, which compresses the aluminum caps.

Sample prepara is placed 1 l of a solution ciprofloxacina g/x is 0.3%.

Originally prepared acetate buffer. This was dissolved in 500 ml of water for injection sodium acetate in the amount of 0.5 g was Mixed until dissolved. Has adjusted the pH of the resulting solution from 3.5 to 5.5 by adding and mixing a solution of acetic acid. In this same buffer solution was added mannitol in the amount of 46 g and mixed until it dissolved.

Then prepared in a solution of the stabilizer, which contains disodium salt of ethylene diamine tetraoxane acid. This salt is the disodium Ethylenediamine tetraoxane acid in the amount of 0.5 g was dissolved in 100 ml of water for injection, heated to 50-70°C. Mix the ingredients until dissolved and cooled to a temperature of 20-25°C, the resulting solution of disodium salt of ethylene diamine tetraoxane acid gradually in small portions were injected into the buffer solution.

The solution benzalkonium chloride obtained by dissolving it in 0.1 g in 100 ml of water for injection. Slowly shuffled to prevent foaming. The resulting solution was poured in small portions gradually in buffer solution. In this solution was dissolved ciprofloxacin in the amount of 3.5 g and brought the volume of solution water for injection up to 1 litre. The resulting solution was 20-30 minutes mixed. Thus the range of values of osmolality brought to the interval from 150 to 450 IMO the e/kg N 2O.

Took a sample solution for analysis. When the discrepancy between the pH interval of 3.5 to 5.5 carry out the pH adjustment solution of acetic acid.

After receiving a positive result of the analysis of the solution of ciprofloxacin hydrochloride 0.3% filtered through filter elements with pore sizes of 0.45 and 0.22 μm.

The resulting solution eye drops contains ciprofloxacin hydrochloride monohydrate, which is equivalent to 0.3% of the free base, a buffer system, keeping pH in the range from 3.5 to 5.5, as preservative - benzalkonium chloride, and the stabilizer is a salt, the disodium Ethylenediamine tetraoxane acid in the following ratio, wt.%/about. (g/100 ml): ciprofloxacin hydrochloride - 0,35, salt is the disodium Ethylenediamine tetraoxane acid is 0.05, mannitol - 4,6, sodium acetate - 0.05, benzalkonium chloride - 0.01, glacial acetic acid is 0.15, water for injection up to 100 ml. With its osmollnosti has the range is made from 150 to 450 mmol/kg H2O.

Received sterile solution was poured into 5 ml vials polymer cap-drip, which was replaced colpack.

If necessary, it is poured into vials amber glass and hermetically sealed with rubber stoppers, which compresses the aluminum caps.

We offer eye drops have properties that fitted nymi to the goods of this pharmaceutical group. The retrieval method allows to obtain the drug for the treatment of diseases of the eye, an important property which is created by the pressure in the eye.

1. Eye drops, including ciprofloxacin, salt is the disodium Ethylenediamine tetraoxane acid and water for injection, characterized in that the drops optionally contain a buffer system in the form of sodium acetate and glacial acetic acid, keeping the pH in the range from 3.5 to 5.5, the thickener in the form of mannitol, as a preservative benzalkonium chloride, have a range of values of osmolality from 150 to 450 mmol/kg H2Oh, when this ciprofloxacin as ciprofloxacin hydrochloride monohydrate, which is equivalent to 0.3% of the free base, in the following ratio, wt.%/about. (g/100 ml):

Ciprofloxacin hydrochloride

monohydrate 0,315-0,385

Salt is the disodium Ethylenediamine

tetraoxane acid 0,045-0,055

Mannitol 4,14-5,06

Sodium acetate 0,045-0,055

Benzalkonium chloride 0,009-0,011

Glacial acetic acid is 0.135-0,165

Water for injection To 100 ml

2. The method of obtaining eye drops, including preparation of buffer systems containing glacial acetic acid and sodium acetate, after which the buffer system dissolve mannitol, salt is the disodium Ethylenediamine of tetraoxy the th acid, benzalkonium chloride, prepared in solution dissolve ciprofloxacin hydrochloride monohydrate and bring the volume of solution water for injection to 100 ml, get the pH value in the range from 3.5 to 5.5, perform quality control of the obtained solution, then it is filtered using sterile items, and poured.

3. The method according to claim 2, characterized in that the sterile solution is poured into 5 ml vials polymer cap-drip, which is screwing the cap.

4. The method according to claim 3, characterized in that use bottles of orange glass and hermetically sealed rubber tubes, which compresses aluminum caps.



 

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