Ipratropium bromide solution

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine and pharmaceutical industry and concerns a solution of a high-efficacy pharmaceutical substance and excipients allowing to form a fine particle aerosol to penetrate into the bronchi and pulmonary alveoli. As an active ingredient, the solution for producing the preparation for inhalation contains ipratropium bromide monohydrate; and as excipients - sodium benzoate, edible organic acid, purified water in the following proportions provided pH is 3.2-3.5.

EFFECT: solution has high respirabile fractions.

5 cl, 4 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 and chronic is eskay obstructive pulmonary disease.

In practice, the treatment of diseases of the respiratory tract are three main methods of forming aerosols. This is the so-called drugs 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 consequently the delivery of drugs other two methods. 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, use the s the energy of compressed air, ultrasound or actuated mechanical devices. The most widely compressor nebulizers. A General requirement for all types of nebulizers - generation aerosol cloud with a particle size of from 0.5 μm to 10 μm, preferably from 0.5 μm to 5.0 μm, preferably from 0.5 μm to 3.0 μm. Such narrow respirable fraction can 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 "included" in the impactor.

The composition of the solutions for nebularia, in addition to the active pharmaceutical ingredients and solvents, can be added substances to ensure 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 fluids such as water, alcohols, glycols, etc. Preferred solvent is water.

Known liquid pharmaceutical composition in the form of an aerosol containing high-quality active substances ipratropium bromide, at least one organic solvent, at least one partially fluorinated hydrocarbons as propellant, at least one inorganic or organic acid (RF patent 2126248). These solutions contain a propellant, therefore not suitable for use in nebulizers.

Known solutions inhalation compositions containing sulfo-alkilany ether cyclodextrin, ipratropium bromide in combination with a corticosteroid. This composition adapted for administration to a subject by spraying using a spray gun. Mentioned sodium benzoate as a preservative, which is injected optional. There is no information about its effect on respirable f the action.

As the closest analogue of the claimed drug can be called a solution for inhalation Atrovent (Boehringer Ingelheim Pharma GmbH ), having the structure:

Ipratropium bromide monohydrate 0,261 mg/ml (corresponding to 0.25 mg/ml ipratropium bromide);

Benzalkonium chloride 0.1 mg/ml;

Disodium of edetate dehydrate 0.5 mg/ml;

Sodium chloride was 8.8 mg/ml;

Hydrochloric acid 1N 0,659 mg/ml;

Purified water to 1.0 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.

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

This task is solved by a new solution to obtain the drug for inhalation, containing as active substance ipratropium bromide, 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:

<>
Ipratropium bromide monohydrate0,1-0,5
Sodium benzoate0,2-2,0
Organic acid1,3-1,9
Purified waterrest
provided that the pH is3,2-3,5

As the pH Adjuster may be used sodium hydroxide.

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

As an active substance in the composition of a new dosage form in the form of a solution is ipratropium bromide (endo,SYN)-(±)-3-(3-Hydroxy-1-oxo-2-phenylpropoxy)-8-methyl-8-(1-methylethyl)-8-azoniabicyclo[3.2.1]-octane bromide. Pharmacological action - m-holinoblokirutm, bronchodilators. Field of application: chronic obstructive pulmonary disease (chronic obstructive bronchitis, emphysema), asthma (mild and moderate), especially with concomitant diseases of the cardiovascular system; hypersecretion of bronchial glands, bronchospasm on the background of colds, when surgically the operations; samples on reversibility of bronchoobstructive; for the preparation of the respiratory tract before the introduction of aerosol antibiotics and mucolytic drugs, glucocorticoids, kromoglicieva acid.

As a rule, in inhalation formulations as preservatives use benzalkonium chloride. However, there is evidence that benzalkonium chloride may cause allergic reactions, especially in children. Therefore, we have proposed a composition containing as the preservative sodium benzoate at concentrations from 0.2 mg 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. However, we have unexpectedly found that sodium benzoate is not only exhibits antimicrobial and antifungal properties, but also significantly affects the respirable fraction of the active agent, increasing the effectiveness of inhalation of the composition. The stability testing showed that the solution ipratropium bromide stable at pH values of 3.2 to 3.5; preferably the pH of 3.3 and 3.4. As acidity regulator, we propose to use an organic acid, preferably biologically active lemon. Tests showed that the required amount of citric acid to achieve the desired pH value is about 1,5mg/ml

As a special case of carrying out the invention may be a composition by adding to the solution of complexing agents, preferably atlandia-montereysalinas acid in the form of dihydrate disodium 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 mg/ml to 1.0 mg/ml Organoleptic testing of this solution confirmed the absence of cough effect.

Preparation of the solution of ipratropium bromide was as follows:

In the vessel in the water for injection is dissolved calculated amount of sodium benzoate, and complexing agents (if it is included in the recipe). The solution is brought to a pH of 3.2 to 3.5, adding 1% solution of citric acid in purified water. Under stirring the solution enter the required number of ipratropium bromide monohydrate. 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 0,0261% solution (0,025% ipratropiyu). After complete dissolution, again counter leraut pH and if necessary adjust. 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.

Ipratropium bromide monohydrate- 0,614 g
Benzalkonium chloride0.1 g
Sodium benzoate- 1,179 g
Citric acid- 3,912 g
Water for injectionup to 2350 ml
pH- 3,30

Example 2.

Ipratropium bromide monohydrate- 0,614 g
Sodium benzoate- 1,179 g
Citric acid- 3,912 g
Water for injectionup to 2350 ml
pH- 3,30

Example 3.

Ipratropium bromide monohydrate- 0,614 g/td>
Sodium benzoate- 1,178 g
EDTA- is 1.175 g
Citric acid- 3,906 g
Water for injectionup to 2350 ml
pH- 3,30

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

Example 4 determination of the respirable fraction

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, known as 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 allows more under the window to investigate 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 specific 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 75 to 90%. That is significantly higher than that of the prototype.

Analytical determination of ipratropium bromide gave the deviation lower than the average standards. Thus, the uniformity of the emitted dose is very high.

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

1. Solution to obtain the drug for inhalation, containing as active substance ipratropium bromide monohydrate, 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, mg/ml:

Ipratropium bromide monohydrate0,1-0,5
Sodium benzoate 0,2-2,0
Organic acid1,3-1,9
Purified waterrest

provided that the pH is 3.2 to 3.5.

2. The solution according to claim 1, characterized in that as an edible 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 3.3 and 3.4.

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 to 1.0 mg per 1 ml solution.



 

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