Stabilised ophthalmic compositions of ketotifen containing preserving agent

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine, in particular to ophthalmology. The invention discloses an ophthalmic composition containing ketotifen and a hydrogen peroxide source supplying hydrogen peroxide in the amount approximately from 0.001 to approximately 0.1% (wt %) with pH making 4 to 5.3. What is also disclosed is a method of treating and preventing allergic conjunctivitis with using said composition.

EFFECT: invention provides minimum adverse side effects in treating and preventing conjunctivitis.

16 cl, 4 tbl, 1 ex

 

The background to the present invention

The present invention relates to ophthalmic compositions comprising ketotifen as a pharmaceutically active agent and a source of hydrogen peroxide as preservative intended for use in the treatment of allergic conjunctivitis. In US patents No. 5725887 (patent '887), 5607698 and in application No. 11/078209, fully incorporated into the present description by reference, are described and claimed methods of storage ophthalmic solutions using stabilized hydrogen peroxide, you get a stable composition. However, hydrogen peroxide is a strong oxidizing agent. Many chemical or medicinal substance is not compatible with hydrogen peroxide, i.e. subject to chemical oxidation with hydrogen peroxide. Ketotifen is a pharmaceutically active agent sensitive to chemical oxidation with hydrogen peroxide. Despite the fact that ketotifen is not compatible with low concentrations of hydrogen peroxide upon receipt of the compositions at a neutral pH, i.e. a pH of approximately 7, it is now established that ketotifen is compatible with low concentrations of hydrogen peroxide, if the compositions have a lower compared to neutral pH values.

Short sloganasustin inventions

One object serves a pharmaceutical composition, which includes:

a) ketotifen salt,

b) a source of hydrogen peroxide, which provides hydrogen peroxide in trace amounts from about 0.001 to about 0.1 wt.%,

in one or more ophthalmologist compatible stabilizers of hydrogen peroxide, the pH of the composition is sufficient to stabilize the ketotifen salt in the conditions of oxidation by hydrogen peroxide.

Another object is proposed a method of treatment and prophylaxis of allergic conjunctivitis, which is that the subject is suffering from allergic conjunctivitis or Prednisolonum to him, introduce local way of an effective amount of the ophthalmic composition, including:

a) ketotifen salt,

b) a source of hydrogen peroxide, which provides hydrogen peroxide in an amount of from about 0.001 to about 0.1 wt.%, and

in one or more ophthalmologist compatible stabilizers of hydrogen peroxide, the pH of the composition is sufficient to stabilize the ketotifen salt in the conditions of oxidation by hydrogen peroxide.

Detailed description of embodiments of the invention

The present invention relates to a stable ophthalmic composition comprising salt ket is tipene, the source of hydrogen peroxide, which provides hydrogen peroxide in an amount of from about 0.001 to about 0.1 wt.%, and one or more ophthalmologist compatible stabilizers of hydrogen peroxide. Ophthalmic compositions are obtained when the pH of which is sufficient to stabilize the ketotifen salt in the conditions of oxidation by hydrogen peroxide, for example at a pH of from about 3.5 to about 6. Thus, the acidic form of ketotifen is more stable compared to the neutral form of ketotifen.

Salt ketotifen is, for example, hydrochloride, ketotifen, hydrobromide ketotifen, pamoat ketotifen, maleate ketotifen, sulfate ketotifen and ketotifen fumarate. Fumarate ketotifen is the preferred salt of ketotifen. The salt concentration of ketotifen in the calculation of the free ketotifen usually has a value of from about 0.01 to about 0.1 wt.%, preferably from about 0.02 to about 0.06 wt.%.

As preservative ophthalmic compositions of the present invention can be used trace amounts of peroxide compounds, stabilized by the stabilizer of hydrogen peroxide, first of all, Diethylenetriamine Penta(methylenephosphonic acid) or 1-hydroxyethylidene-1,1-diphosphonic acid. The source of peroxide is odorata means any peroxide compound, which hydrolyses in water to form hydrogen peroxide. Examples of sources of hydrogen peroxide, which ensure the formation of an effective amount of hydrogen peroxide include perborate sodium tetrahydrate sodium perborate, sodium peroxide and urea peroxide. It is established that peracetic acid, an organic peroxide compound, it is impossible to stabilize the system using the present invention.

The source of hydrogen peroxide is present in a quantity sufficient to provide from about 0.001 to about 0.1 wt.% of hydrogen peroxide, preferably from about 0.001 to about 0.01 wt.% of hydrogen peroxide. For example, the source of hydrogen peroxide, perborate tetrahydrate, sodium, present in an amount of approximately from 0.005 to about 0.05 wt.%.

Used in this context, the term "stabilizer of hydrogen peroxide" means any of the known stabilizers, peroxide compounds, including phosphonates, phosphates, stannate etc. you Can also use the physiologically compatible salts of phosphonic acids, such as Diethylenetriamine Penta(methylenephosphonic acid) and its physiologically compatible salts, 1-hydroxyethylidene-1,1-diphosphonic acid and its physiologically acceptable salts. Other stabilizers peroxide is soedinenii, suitable for implementing the present invention into practice is described in the patent '887, column 5, line 55 - column 6, line 34.

The above stabilizers can be used for all indications, described below. However, when the contacting of the solution with soft contact lenses based hydrogel should not be used as stabilizers stannate, because they tend to "darken" the lens material.

If the peroxide stabilizer is Diethylenetriamine Penta(methylenephosphonic acid), its content in the composition is from about 0.001 to about 0.02 wt.% or from about 0.002 to about a 0.012 wt.%.

If the peroxide stabilizer is 1-hydroxyethylidene-1,1-diphosphonic acid, its content in the composition is from about 0.002 to about 0.2 wt.%.

Stabilizers other than Diethylenetriamine Penta(methylenephosphonic acid) company Monsanto Company, St. Louis, Mo., trade name DEQUEST 2060, and its physiologically compatible salts, and stabilizers other than 1-hydroxyethylidene-1,1-diphosphonic acid and its physiologically acceptable salts, are used in physiologically-tolerated amounts.

Soluble salts of alkaline-earth metals can be used in ophthalmic compositions in amounts of about is about 0.002 to about 0.2 wt.% based on the solution of the preservative or from about 0.01 to about 0.1 wt.% based on the solution of the preservative. Such salts of alkaline-earth metals include water-soluble salts of magnesium and calcium. Adding these soluble salts of alkaline-earth metals is increased antifungal preservative action of ophthalmic compositions, including as a preservative and a small amount of hydrogen peroxide.

As stated above, the ophthalmic compositions of the present invention are obtained at pH values below neutral, which is sufficient to stabilize the ketotifen salt in the conditions of oxidation by hydrogen peroxide, for example at a pH of from about 3.5 to about 6, preferably at a pH of from about 3.8 to about 5.5 and more preferably at a pH from approximately 4 to approximately 5,3. For example, the ophthalmic composition was prepared at a pH of from 3.5 to 6, preferably at a pH of from 3.8 to 5.5, more preferably at a pH of from 4 to 5.3. The pH, if necessary, adjusted by adding appropriate amounts of acid or base that are physiologically tolerable used in amounts of, for example, hydrochloric acid and sodium hydroxide.

In ophthalmic compositions of the present invention is one or more standard, substantially inert physiologically acceptable agents that increase the osmotic pressure is used. Suitable agents include, for example, mannitol, sorbitol, glycerol, halides of alkali metals, phosphates, phosphate and borate. Preferred are sodium chloride, monobasic sodium phosphate and dibasic sodium phosphate. The action of those agents that increase the osmotic pressure, is to provide approximately physiological osmotic pressure with the introduction of the composition into the eye or in the provision of such osmotic pressure upon dilution if dilution is necessary before contacting eye tissue to dilute the peroxide, as described above.

Preferably, agents that increase the osmotic pressure, add in ophthalmic composition for providing substantially isotonicity specified composition or to decomposition or dilution in presence of hydrogen peroxide obtained composition was largely retained the osmotic pressure, for example, was characterized by an osmotic pressure substantially equivalent to 0.9 wt.% aqueous solution of sodium chloride. Preferably, the amount of agent that increases the osmotic pressure that is present in the ophthalmic composition is from about 0.01 to about 1 wt.%.

Ophthalmic compositions of the present invention including the Ute one or more thickeners. Examples of thickeners include, without limitation, ethers of cellulose, such as hypromellose (receiver array), hydroxyethylcellulose (NES) and metilgidroxiatilzelllozu, polyacrylic acid, polyvinyl alcohol, polyvinylpyrrolidone, alginates, carrageenan, guar gum, Karyu, agarose, the fruit of the carob and xanthan gum.

For example, the ophthalmic composition of the present invention includes from about 0,0138 to approximately was 0.138 wt.% fumarata ketotifen and from approximately 0.005 to approximately 0.5 wt.% perborate sodium, from about 0.001 to about 0.01 wt.% Diethylenetriamine Penta(methylenephosphonic acid) and its physiologically compatible salts, or from about 0.002 to about 0.2 wt.% 1-hydroxyethylidene-1,1-diphosphonic acid and its physiologically acceptable salts, and the composition is characterized by a pH from about 3.5 to about 6. The total amount of the composition adjusted to 100% by addition of purified water.

Ophthalmic compositions of the present invention are characterized by extremely high stability even under conditions of rapid decomposition, for example by heating the solution at 100°C for 24 hours Thereby extending the shelf life of these compositions. Moreover, the composition is according to the present invention are characterized by physiological tolerance due to the decomposition of hydrogen peroxide.

Another advantage of the use of hydrogen peroxide in ophthalmic compositions is that the trace amount of hydrogen peroxide decomposes in contact with eye tissue. For example, catalase is present in ocular tissues, causing the decomposition of hydrogen peroxide to water and oxygen. As a result, when the introduction of the ophthalmic composition does not contain a preservative, which greatly minimizes the negative side effects and no problems with other preservatives, such as the inability to decomposition with the formation of harmless compounds.

Ophthalmic compositions of the present invention receive any standard method. For example, all components except hydrogen peroxide and water, is placed in the container and when mixing, add fresh, preferably concentrated hydrogen peroxide. In another embodiment, the dry ingredients triturated with a small portion of liquid stabilizer, then add the remaining quantity of the stabilizer, then hydrogen peroxide and the remainder water. Then add other components, such as agents for regulating the osmotic pressure and thickeners, or the resulting composition is added to these agents. The specialist in this area known for numerous is the variants of the method of producing compositions of the present invention.

Another object of the present invention relates to a method for treatment and prevention of allergic conjunctivitis. This method is that the subject is suffering from allergic conjunctivitis or Prednisolonum to him, introducing an effective amount of the above ophthalmic composition.

In one embodiment, this method ophthalmic compositions can enter the local way in the eye, preferably in the form of eye drops for the treatment and reduction of itching in the eyes allergic conjunctivitis, as well as for treatment and reduce the intensity of symptoms of seasonal allergic conjunctivitis. Dosage ophthalmic compositions depends on the severity of allergic conjunctivitis and the salt concentration of ketotifen in the composition and is determined by the person skilled in the art. Usually, when using the compositions of the present invention once imposed from 1 to 10 drops, or from 1 to 5 drops, or from 1 to 3 drops.

In yet another embodiment, the above method ophthalmic compositions are suitable for use in solutions for the care of contact lenses, for example in solutions for hydrating contact lenses, storage, lubrication, cleaning, disinfection and cosmetic solutions. Ophtalmologic the ski compositions of the present invention placed in any pharmaceutically acceptable packaging however, it should be packaged in flexible plastic containers with multiple dose, such as bottles with dropper. These bottles get, for example, of polyethylene or polypropylene or mixtures thereof. Usually, in a bottle with dropper in the drop contains from about 12 μl to about 50 μl. If you want to "neutralize" the activity of the peroxide, it is possible to use any known method, such as washing, contacting the solution with platinum, catalase, or any other compound which, as is well known, decomposes hydrogen peroxide. Additional physiologically compatible agents, neutralizing peroxide include reducing agents such as pyruvic acid and suitable salts such as the sodium salt.

The following examples are provided to illustrate the present invention do not limit the scope of the present invention and serve to illustrate the stability of the ophthalmic compositions stabilized according to the present invention. All quantities stated in wt.%, if not specified otherwise.

Example 1

Table 1
Composition comprising ketotifen and perborate
Track Fumarate
ketotifen
(mg/ml)
pHNaCl
(mg/ml)
Perborate Na·4H2O (mg/ml)Dequest
(mg/ml)
Boric
acid (mg/ml)
Borat Na
(mg/ml)
10,3456,36,650,270,065,00,05
206,36,650,270,065,00,05
305,36,650,270,065,00,05
40,3455,36,650,20,065,00,05

To assess the stability of the compositions presented is in table 1, the composition was poured into vials and kept the song at 55°C for different periods of time. The results are shown in table 2 below.

Table 2
Concentration fumarata ketotifen (mg/ml) in samples when stored in polypropylene vials at 55°C
TrackInitial concentration1 week at 55°C2 weeks at 55°C4 weeks at 55°C
10,3400,3190,3230,296

TrackInitial concentration1 week at 55°C2 weeks at 55°C4 weeks at 55°C
20,000,000,000,00
30,000,000,00 0,00
40,336of 0.3370,3420,341

The compositions listed in table 2 satisfy the performance criteria for test data storage (USP) in accordance with the requirements of the monitoring Committee food and drug administration (FDA) for storage ophthalmic compositions.

The results are given in table 2, show that ketotifen stable at elevated temperatures, especially in the composition 4, which is obtained at a lower pH compared to the composition 1.

Table 3
Compositions comprising ketotifen and perborate
Composition 1of 0.025% Ketotifen (0,0345% fumarate ketotifen)
2% Propylene glycol
0.3% of the receiver array (EM)
0,006% Dequest 2060
0,028% Perborate sodium
Purified water to allali to the desired volume
the pH was brought to 5,487
The osmotic pressure 296 mOsm/kg
Composition 2United 10 vials drug Zaditor (to 0.025% ketotifen (0,0345% ketotifen fumarate, 2.5 ml), the received sample weight 26,38 g
Dequest 2060, 60 ppm million
0,028% perborate sodium
pH=4,484

The stability of the compositions shown in table 3, was evaluated by heating the composition at 100°C for 24 h the Results are presented in table 4 below.

Table 4
Heating compositions comprising ketotifen and perborate, at 100°C for 24 h
TrackStability perborate sodium stability
heating, %)
Stability ketotifen (%)pH
Before heatingAfter heating
1 79,792,65,494,87
293,3102,74,484,43

The results given in table 4, indicate stability of ketotifen in the above-mentioned conditions of rapid decomposition.

1. Ophthalmic composition including:
a) ketotifen salt, and the salt concentration of ketotifen in the calculation of the free ketotifen is from about 0.01 to about 0.1 wt.%;
b) a source of hydrogen peroxide, which provides hydrogen peroxide in trace amounts from about 0.001 to about 0.1 wt.%; and
in one or more ophthalmologist compatible stabilizers of hydrogen peroxide, where the pH of the composition is from 4 to 5.3.

2. The composition according to claim 1, where the ketotifen salt is fumarate ketotifen.

3. The composition according to claim 1, where the source of hydrogen peroxide selected from the group including perborate sodium tetrahydrate sodium perborate, sodium peroxide and urea peroxide.

4. The composition according to claim 1, where one or more of the stabilizers of hydrogen peroxide selected from the group including Diethylenetriamine Penta(methylenephosphonic acid), 1-hydroxyethylidene-1,1-diphosphonic acid and their physio is logicheskie acceptable salt.

5. The composition according to claim 4, comprising from about 0.001 to about 0.02 wt.% Diethylenetriamine Penta(methylenephosphonic acid) or its physiologically acceptable salt.

6. The composition according to claim 4, comprising from about 0.002 to about 0.2 wt.% 1-hydroxyethylidene-1,1-diphosphonic acid or its physiologically acceptable salt.

7. The composition according to claim 1, additionally comprising an agent that increases the osmotic pressure.

8. The composition according to claim 1, including:
a) from about 0.02 to about 0.06 wt.% salt ketotifen in the calculation of the free ketotifen,
b) from about 0.001 to about 0.01 wt.% of hydrogen peroxide and
in one or more ophthalmologist compatible stabilizers of hydrogen peroxide, where the pH of the composition is sufficient to stabilize the ketotifen salt in the conditions of oxidation by hydrogen peroxide, at the same time, the pH of the composition is from 4 to 5.3.

9. Method for the treatment and prevention of allergic conjunctivitis, which is that the subject is suffering from allergic conjunctivitis or Prednisolonum to him, introduce local way of an effective amount of the ophthalmic composition, including:
a) ketotifen salt, and the salt concentration of ketotifen as ketotifen is from about 0.01 to about 0.1 wt.%;
B. a source of hydrogen peroxide, providing hydrogen peroxide in trace amounts from about 0.001 to about 0.1 wt.%; and
in one or more ophthalmologist compatible stabilizers of hydrogen peroxide, where the pH of the composition is from 4 to 5.3.

10. The method according to claim 9, where the ketotifen salt is fumarate ketotifen.

11. The method according to claim 9, where the source of hydrogen peroxide selected from the group comprising hydrogen peroxide, perborate sodium, sodium peroxide and urea peroxide.

12. The method according to claim 9, where one or more of the stabilizers of hydrogen peroxide selected from the group including Diethylenetriamine Penta(methylenephosphonic acid), 1-hydroxyethylidene-1,1-diphosphonic acid and their physiologically acceptable salts.

13. The method according to item 12, where the composition includes from about 0.001 to about 0.02 wt.% Diethylenetriamine Penta(methylenephosphonic acid) or its physiologically acceptable salt.

14. The method according to item 12, where the composition includes from about 0.002 to about 0.2 wt.% 1-hydroxyethylidene-1,1-diphosphonic acid or its physiologically acceptable salt.

15. The method according to claim 9, where the composition also includes an agent that increases the osmotic pressure.

16. The use of a composition according to claim 1 for the treatment and prevention of allergic conjunctivitis.



 

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3 cl, 8 ex, 3 tbl, 1 dwg

FIELD: medicine.

SUBSTANCE: group of inventions refers in particular to solutions for mouth rinsing. The water based composition possessing antimicrobic activity consists of: a) from 0,001 to 10 % of weight octenidin dihydrochlorid b) from 0,05 to 30 % of weight of not ionic surface-active substance - derivative fat acids, c) from 0,01 to 10 % of weight poliol, chosen from 1,2-propylene glycol, 1,3 propylene glycol, butane-1,4-diol, sorbite (hexa-1,2,3,4,5,6-hexole) and glycerin or their mix, d) from 0,05 to 10 % of weight of fruit acid and-or its salt chosen from lemon acid, dairy acid, apple acid, wine acid, glycogenic acids, fumaric and amber acid or their mix, e) from 0,025 to 10 % of weight of flavour and-or sweetener, chosen from alitam, aspartame, dulcin, neohesperidin DC, stevioside, sucralose, suosane and thaumatinor their mixtures with water - up to 100 %. The composition is applied as a solution for mouth rinsing and controlling S. Aureus and/or E. faecalis resistant to methicillin.

EFFECT: invention provides efficiency of application as the solution for mouth rinsing awhich is characterized by pleasant taste and a small tendency to foaming.

11 cl, 2 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers namely to dermatology and can be used for prevention and treatment of the pustulous diseases caused by bacterial skin defeats. For this purpose the damaged skin amazed and adjoining areas are worked with the antiseptic of "Likvacid" received with the use of trinol by means of its preliminary dissolution in a dimethyl sulfoxide in the ratio 1 mas.h. to 0,9 mas.h., accordingly, at the temperature not below indoor temperature before dark blue coloring of a mix occurs, and mixture then with a filler based on alcohol with addition of glycerin and further filtration of the received mix, herewith using as a filler of a solution of acid in ethyl spirit with its initial concentration accepted that the end-product has not less than 70 %, and with a choice of all components in the following ratio, mas.: trinitrotoluene- 0,25-1,5, a dimethyl sulfoxide - 1,0-10,0, acid - 0,5-1,0, glycerin - 17,5-23,0, ethyl spirit - the rest. The skin is greased with a wadded tampon with frequency of 2-3 times a day. Thus duration of therapy is not less than 17 days and to epulosisof the damaged surface. Or in case of the second invention grease the damaged skin and adjoining areas are greased with a wadded tampon with frequency of 2-3 times a day. The therapy course is not less and in addition is accepted than 10 days by taking "Likvacid" per oral 2-3 times a day within no more than 10 days. Herewith adults people take 11-16 ml, young men to 18-year-old age - 5-10 ml.

EFFECT: the use of the given inventions allows carrying out effective preventive maintenance and treatment in case of optimum terms of therapy.

2 tbl, 1 dwg

Banking process // 2440131

FIELD: medicine.

SUBSTANCE: present invention refers to chemical-pharmaceutical industry and concerns a banking, perfusion and/or reperfusion solution for an organ, especially heart to be grafted. The solution contains proteinkinase C peptide inhibitor.

EFFECT: method of applying said solution is also described, including banking process for ischemic organ protection against the damage for relieving post-ischemic organ dysfunction for maintaining nitrogen oxide release and/or superoxide release inhibition in an ischemic organ, as well as for organ protection from the damages when isolated from the blood circulatory system.

24 cl, 1 ex, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine, in particular to pharmacy. A composition for injections exhibiting tranquilising action contains the ingredients in the following proportions, wt %: crystalline β-modification of 7-brom-1,3-dihydro-5-(2-chlorphenyl)-2H-1,4-benzodiazepin-2-one - 0.05-0.15, polyvinylpyrrolidone - 0.50-1.20, "Tween-80" - 2.00-10.00, glycerine - 5.00-15.00, sodium pyrosulphite - 0.30-1.20, sodium hydrate solution - to pH 6.0-7.5, water - the rest. A method for preparing the composition consist in the fact that "Tween-80" and glycerine are mixed, heated to 70-90°C, and crystalline β-modification of 7-brom-1,3-dihydro-5-(2-chlorphenyl)-2H-1,4-benzodiazepin-2-one is dissolved. The prepared mixture is poured in the mixed aqueous solution of sodium pyrosulphite and polyvinylpyrrolidone heated to 40-90°C, cooled to room temperature, filtered, reduced to pH 6.0-7.5 with sodium hydrate solution, bottled and sterilised.

EFFECT: presented group of inventions provide a composition exhibiting improved anxiolytic action and decreased sedation in comparison with the composition based on pharmacopoeial phenazepam.

2 cl, 2 tbl, 4 ex

FIELD: ophthalmology.

SUBSTANCE: main composition contains: (a) ketotifen fumarate to the concentration in calculation to free ketotifen from approx. 0.01 mas. % to approx. 0.1 mas.%;(b) source of hydrogen peroxide ensuring presence of hydrogen peroxide with trace quantities amounting from approximately 0.001 to approximately 0.1% (mas./vol.); (c) one or several stabilizers of hydrogen peroxide compatible with eyes; (d) hypromellose to the concentration from approximately 0.005 mas% to approximately 0.5 mas.%; and (e) sodium carboxymethyl cellulose to the concentration from approx. 0.005 mas.% to approx 0.5 mas.%. At this the value of composition pH amounts to approximately from 4.0 to 5.3.

EFFECT: invention is a method of treatment and prevention of allergic conjunctivitis which is ensured with application locally in the effective quantity of the mentioned eye composition to person with allergic conjunctivitis or sensitive to it.

13 cl, 15 tbl, 4 ex

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