Stable solution of fenoterol hydrobromide

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine and describes a solution for producing an inhalation preparation containing fenoterol hydrobromide as an active agent, purified water and excipients with the excipients presented by sodium benzoate, an acidity regulator representing an organic acid in the following proportions, mg/ml: fenoterol hydrobromide 1.0-1.1; sodium benzoate 0.2-2.0; organic acid 1.4-1.7; purified water the rest provided pH makes 3.2-3.5.

EFFECT: solution has the high value of respirable fractions and high stability.

6 cl, 3 ex

 

The invention relates to medicine and the pharmaceutical industry and relates to the efficient solution of a drug substance and excipients, to form an aerosol of fine particles with the aim of penetrating into the bronchi and alveoli of the lungs.

Bronchial asthma (BA) is one of the most common diseases of the respiratory system among people of all ages. In Russia BA suffers from 5 to 7% of the adult population. Severity of disease: 30% of patients - mild course of the disease, a 50% moderate and 20% severe. BA is the cause of 0.4% of all cases of population for medical care, 1.4 percent of hospitalizations. Chronic obstructive pulmonary disease (COPD) is another common chronic disease of the respiratory system, which is accompanied by chronic relapsing inflammation of the bronchial wall. COPD is characterized by a steady progression, even when outside of an exacerbation occurs increase of bronchial obstruction, the accession of complications, and patients gradually lose their ability to work. According to some reports in Russia more than 11 million people suffer from COPD. Thus, there is a significant demand for drugs effective against respiratory diseases, especially asthma, chronic the Russian obstructive pulmonary disease.

In practice, the treatment of diseases of the respiratory tract are three main methods of forming aerosols. This medication under pressure and sprayed with excipients propellant powders for inhalation activated, usually by inhalation of the patient, and the solution or suspension is sprayed with a special device is a nebulizer. Each method has its own specific properties that make them preferable for use in different groups of patients, the site of application, weather conditions, etc. have in Common these methods drugs should ensure the formation of respirable fraction, i.e. to form an aerosol cloud with a predominant particle size of from 0.5 to 5 microns.

The level of technology

Specific properties therapy using nebulizers is the possibility of helping patients with severe bronchial obstruction and respiratory failure, which leads to the inability of patients to create inspiratory flow and, as a consequence, the delivery of drugs other two methods. Also nebularia may be the only way to treat children. Spray solutions for nebularia have less irritation and reduces cough effect.

In medical practice used nebulizers different designs, using the power of LF is in the air, ultrasound or actuated mechanical devices. The most widely compressor nebulizers. A General requirement for all types of nebulizers - generation aerosol clouds with particle sizes from 0.5 to 10 μm, preferably from 0.5 to 5.0 μm, preferably from 0.5 to 3.0 μm. Such narrow respirable fraction may be obtained only spraying the true solutions of medicinal substances. Dimension respirable fraction in the case of nebulizer drugs as possible using impactors and directly measuring the sizes of particles in the air stream, in particular by laser diffraction. Measurements using impactors allows to get the mass distribution and does not depend on the particle shape.

When measuring the dispersion of the aerosol cloud when nebulaman should be noted that a part of the drug gets into the respiratory system of patients, and dispersed in the atmosphere or deposited in the nebulizer. This is because nebularia happens all the time, and the breath of patients discretely. The use of nebulizers with valves not completely solves this problem. Therefore, when evaluating the effectiveness of drugs using impactors should assess the fraction of small particles compared to the amount of the drug, "logged in" to the impactor.

In status is in solutions for nebularia, in addition to the active pharmaceutical ingredients and solvents, can be added substances, ensuring the stability of the solution during storage - acidity regulators, preservatives and antioxidants. Can be added substances, corrective taste, regulators of the size of aerosol particles and other

Solvents and/or co-solvents are selected from the group of biologically acceptable fluid, such as water, alcohols, glycols, etc. Preferred solvent is water.

For example, the known solutions for inhalation, including for nebularia (application WO 2008102128), containing as active substances beta-agonists, including the above excipients. This source does not discuss or explores the impact of combinations of excipients on the amount of respirable fraction.

Known solutions fenoterola for the treatment of obstructive diseases, without propellants that contain as excipients benzalkonium chloride, complexing agents such as EDTA, pH 3.2 (application WO 9827959). The compositions are aimed at improving solubility for use in nebulizers. However, for this purpose, 70° alcohol, which is undesirable from the point of view of the adverse effects on the patient.

As the closest analogue of the claimed drug can be called a solution for inhalation B is rothek (Boehringer Ingelheim Pharma GmbH) (http://medi.ru/doc/2556.htm), having the structure:

Fenoterol hydrobromide 0.1 g;

Benzalkonium chloride 0.01 g;

Disodium of edetate dehydrate 0.05 g;

Chloride-hydrogen acid 1H 0,0946 g;

Purified water to 100 ml.

Respirable fraction of the active substance measured at the 8-stage Andersen impactor (air flow of 28.5 l/min, discrete introduction 4 l through 5 (C), the product was sprayed on the nebulizer ñ M2000, firms Marcos-Mifur, Italy. Respirable fraction, calculated as the ratio of the mass of small particles to the mass of "included in the impactor is high enough - about 70%, or 30% of ingalirovanna drug.

There is evidence that benzalkonium chloride may cause allergic reactions, especially in children.

The present invention is to develop effective inhalation composition for the treatment of asthma and COPD.

This task is solved by the new composition of the solution to obtain the drug for inhalation, containing as active substance fenoterola hydrobromide, and as excipients sodium benzoate, acidity regulator, which represents an edible organic acid, and purified water, with the following content of components, in mg/ml:

fenoterol hydrobromide 1,0-1,1
sodium benzoate0,2-2,0
organic acid1,4-1,7
purified waterrest

provided that the pH is 3.2 to 3.5.

Technical result: a higher percentage of respirable fraction of the active substance and hence higher efficiency.

As the active substance solution contains fenoterola hydrobromide - 5-[1-hydroxy-2-[[2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-1,3-benzodia hydrobromide.

It is election adrenoagonists beta2-adrenergic receptors and has therefore a stronger, relatively long action bronchospastic conditions with fewer side effects (tachycardia and other disorders of the cardiovascular system). There is evidence that the drug has a bronchodilatory effect and simultaneously enhances the function of ciliated epithelium and accelerates mucociliary transport.

Indications:

- attacks of asthma or other conditions with reversible obstruction of the respiratory tract (including chronic bronchitis, chronic obstructive pulmonary disease);

- prevention of asthma attacks due to the physical is a mini voltage;

as bronchodilating agents prior to inhalation of other drugs (antibiotics, mucolytics are presented, SCS);

- conducting bronchodilatory tests in the study of respiratory function.

The proposed composition contains sodium benzoate at concentrations from 0.2 to 2.0 mg per ml. Sodium benzoate is particularly effective in acidic solutions with pH 4.5 and below, and is particularly effective against fungi, a defeat which often accompanies diseases of the respiratory system. The number of benzalkonium can significantly reduce or even abandon its use. In particular, the solution may contain up to 0.05 mg/ml benzalkonium chloride. The stability testing showed that the solutions fenoterola hydrobromide stable at pH values of 3.2 to 3.5; preferably a pH of 3.2 and 3.3. As acidity regulator, we propose to use edible organic acids such as malic, citric, tartaric, benzoic, salicylic, succinic, particularly preferably citric acid. Tests showed that the amount of acid to achieve the desired pH is preferably about 1.5 mg/ml

It is also possible in the particular case of carrying out the invention the addition of solution of complexing agents, preferably ethylenediaminetetraacetic acid dihydrate form Donat what Ieva salt (EDTA). EDTA is a low-toxic substance with the acceptable daily intake of 2.5 mg per kg of body weight (Methodical recommendations on the safe use of excipients in medicinal products, Federal ncase, Minzdravsocrazvitia the Russian Federation, Moscow, 2004). We have determined the concentration of the effective application of EDTA, 0.1 to 1.0 mg/ml Organoleptic testing of this solution confirmed the absence of cough effect.

Preparation of the solution fenoterola hydrobromide was following.

In the vessel in the water purified dissolving the calculated amount of sodium benzoate and complexing agents (if it goes in the recipe). The solution is brought to a pH of 3.2 to 3.5, adding 1% solution of organic acid in purified water. Under stirring the solution enter the required number of fenoterol hydrobromide. As the solution before therapy is to divorce saline depending on the readings and the chamber dimensions of the nebulizer, the calculation quantity of the active substance lead from the need to obtain a 0.1% solution. After complete dissolution once again in control of the pH and, if necessary, correct. The finished solution is filtered through a sterilizing membrane filter with a pore size of 0.22 μm and poured into sterile glass vials-droppers.

Example 1

Fenoterola hydrobromide- 2,521 g
Benzalkonium chloride0.1 g
Sodium benzoate- 1,179 g
Citric acid- 3,912 g
Water for injectionup to 2350 ml
pH- 3,23

Example 2

Fenoterola hydrobromide- 2,521 g
Sodium benzoate- 1,179 g
Citric acid- 3,912 g
Water for injectionup to 2350 ml
pH- 3,23

Example 3

Fenoterola hydrobromide- 2,521 g
Sodium benzoate- 1,178 g
EDTA- is 1.175 g
Citric acid
Water for injectionup to 2350 ml
pH3.21 - in

The solutions were poured into bottles, dropper glass on 21-22 ml.

Test

The preparation obtained by the above technologies, and control the drug was tested in accordance with requirements established for solutions for inhalation of the European Pharmacopoeia. Of particular importance for inhalation drugs represents the fraction of fine particles of active substances, measured in grams or percentage and determined in the course of aerodynamic testing. The magnitude of this fraction, also called respirable determines the effectiveness of the preparations for inhalation for the treatment of respiratory organs. Determination of the respirable fraction is carried out with the use of devices described in the European and American pharmacopoeias. The most often used vosmiseriyny the Andersen impactor (device D of the European Pharmacopoeia), as it gives the opportunity to explore in more detail the particle size distribution in the range from 0.5 μm to 10 μm and more. The European Pharmacopoeia defines terms analysis - volume pumped air 4 l, the flow rate of 28.3 l/min, although it allows the use of other speed. However, each to skretny model of Andersen impactor designed for a certain flow rate of air and cannot be used on another.

For solutions in the above examples using the Andersen impactor was determined respirable fraction. They ranged from 84 to 91%. That is significantly higher than that of the prototype.

Analytical determination of fenoterol hydrobromide gave Delta value below the prescribed norms of the medium. Thus, the uniformity of the emitted dose is very high.

High stability of the solutions was confirmed in the conditions of accelerated aging.

1. Solution to obtain the drug for inhalation, containing as active substance fenoterola hydrobromide, purified water and excipients, characterized in that as auxiliary substances it contains sodium benzoate, acidity regulator, which represents an edible organic acid, with the following content of components in mg/ml:

fenoterol hydrobromide1,0-1,1
sodium benzoate0,2-2,0
organic acid1,4-1,7
purified waterthe rest,

provided that the pH is 3.2 to 3.5.

2. The solution according to claim 1, characterized in that as PI the eve of the organic acid contains citric acid in the amount of 1.5 mg/ml solution.

3. The solution according to claim 1 or 2, characterized in that the pH is 3.2 and 3.3.

4. The solution according to claim 1 or 2, characterized in that it further comprises complexing agents, preferably ethylenediaminetetraacetic acid dihydrate disodium salt.

5. The solution according to claim 4, characterized in that it contains ethylenediaminetetraacetic acid dihydrate disodium salt in an amount of from 0.1 mg to 1.0 mg per ml of solution.

6. The solution according to claim 1 or 2, characterized in that it further contains benzalkonium chloride in an amount up to 0.05 mg per ml of solution.



 

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FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of medicine, in particular to pharmacological preparations, namely: to medicinal syrups. Essence of the invention lies in the following: claimed is syrup with polydihydroxyphenylenethiosulfonate sodium (hypoxenum) based on xilite with the following component ratio: xilite - 70%, polydihydroxyphenylenethiosulfonate sodium - 5%, multifruit concentrate - 7%, purified water - the remaining part, as well as method of said syrup obtaining, which includes swelling of xilite in water for 30 minutes, heating of mixture to 60-70%, boiling for 10 minutes with removal of formed foam, cooling mixture to 95-97єC, adding polydihydroxyphenylenethiosulfonate sodium and multifruit concentrate, re-boiling syrup for 15 minutes with removal of foam, bringing syrup in weight to 100% with purified water, processing mixture with ultra sound at frequency 25 kHz for 30 seconds by means of waveconductor-concentrator, providing amplitude of fluctuation of radiated medium particles up to 7 mcm, further colation and filtration of final syrup.

EFFECT: claimed syrup possesses antihypoxant properties and can be applied in complex treatment and prevention of chronic diseases, including in pediatrics, as it possesses pleasant sour-sweet taste and fruit fragrance.

2 cl, 3 dwg, 5 tbl, 1 ex

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