RU2237475C1 - Combined preparation to remove symptoms of catarrhal diseases and grippe (variants) - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: the suggested preparation contains acetylsalicylic acid, component chosen out of the group: metamysol, paracetamol, ibuprofen, antihistaminic preparation chosen out of the group: prometasine, pheniramine, terphenadine, astemysol, acryvastine, loratadine, phexophenadine and, also, phenylephrine and ascorbic acid, and, also, combined preparation to remove symptoms of catarrhal diseases and grippe containing metamysol, paracetamol or ibuprofen, antihistaminic preparation chosen out of the group: prometasine, pheniramine, terphenadine, astermysol, acryvastine, loratadine, phexophenadine and, also, phenylephrine and ascorbic acid.

EFFECT: higher efficiency of therapy.

11 cl, 12 ex, 2 tbl

Description

The invention relates to medicine and relates to means for the prevention and treatment of colds and flu.

Cold illnesses include a variety of acute infectious diseases and an exacerbation of chronic diseases, especially the upper respiratory tract.

The names of colds correspond to anatomical formations, starting from top to bottom: nasal cavity, pharynx, larynx, trachea and bronchi. Accordingly, the names of the diseases occur: rhinitis, pharyngitis, laryngitis, tracheitis, bronchitis.

Previously, they were united in a group of acute respiratory infections (ARI), now medical scientists believe the more accurate name for acute respiratory viral infections (ARVI).

Influenza and SARS take the first place in the frequency and number of cases in the world and make up 95% of all infectious diseases. Repeatedly repeating, influenza and SARS carry out throughout our lives for a total of about 1 year. A person spends these months inactive, suffering from fever, general fatigue, headache, poisoning of the body with poisonous viral proteins.

The term "acute respiratory infection" (ARVI) covers a large number of diseases that are largely similar to each other. Their main similarity is that they are all caused by viruses that enter the body along with the inhaled air through the mouth and nasopharynx, and that they are all characterized by the same set of symptoms. The patient has several days fever, sore throat, cough, headache. The most common disease is acute rhinitis (runny nose), which is caused by a number of related viruses, known as rhinoviruses. Upon recovery, all these symptoms disappear and do not leave any traces. There are bacterial and mycoplasma forms of the disease. Streptococci, staphylococci, pneumococci and many other bacteria or mycoplasmas cause them. Such diseases often do not occur on their own, but join a viral (ARVI), or occur against a background of chronic respiratory diseases. Influenza is caused directly by the influenza virus (Myxovirus influenzae), which belongs to the family of orthomyxoviruses.

Influenza and acute respiratory viral infections gradually undermine the cardiovascular system, reducing the average life span of a person by several years. In severe influenza, irreversible damage to the cardiovascular system, respiratory organs, central nervous system, provoking diseases of the heart and blood vessels, pneumonia, tracheobronchitis, and meningoencephalitis often occur.

The main actions in the treatment of influenza and acute respiratory viral infections are aimed at reducing severe symptoms. In the acute phase of the disease, bed rest, rest, heavy drinking are recommended.

With increasing temperature, various antipyretic drugs are used (paracetamol, ibuprofen, aspirin).

To reduce nasal congestion, vasoconstrictive drops are used (naphthyzin, galazolin, xymelin, etc.). Also, according to indications, antihistamines are used.

Vitamins such as vitamin C (ascorbic acid) and vitamin A are used to increase the body's resistance.

Also, interferon-based drugs are used to treat the flu. There are a number of anti-influenza drugs that do not act in general on the body, but directly on the influenza virus. These are well-known drugs such as amantadine and remantadine. These medicines have a number of contraindications. When attaching a bacterial infection, as well as with concomitant chronic respiratory diseases, antimicrobials are used (including antibiotics).

The polyetiological nature of this group of diseases makes it impossible to solve the problem of reducing the incidence only due to vaccine prophylaxis, and therefore the role of both chemotherapeutic agents that increase the resistance of the human body and various symptomatic agents does not weaken.

Recently, researchers in this field of medicine have given preference to the creation of combined preparations of complex action. The most famous of the drugs in this group are the following:

- Coldrex Hotrem, Glaxo Smith Kline, based on paracetamol, phenylephrine hydrochloride and ascorbic acid in the form of a powder for solution preparation;

- Fervex UPSA preparation containing pheniramine maleate, paracetamol, ascorbic acid;

- pentaflucin in capsules containing aspirin, vitamin C, rutin, calcium lactate and diphenhydramine (RU 2173555 C1);

- Naturproduct antigrippin in tablets containing paracetamol, ascorbic acid and chlorphenamine;

- antigrippin in granules containing aspirin, vitamin C, diphenhydramine, rutin, calcium gluconate (RU 99102949 A1)

- antigrippin-ANVI in the form of a set of capsules. 1 capsule stained with food coloring (yellow or another color) contains acetylsalicylic acid, ascorbic acid, rutin. 1 white capsule contains metamizole sodium, diphenhydramine, calcium gluconate.

- Pliva pivalgine of the company in the form of tablets containing paracetamol, propiphenazone, caffeine, phenobarbital, codeine.

Known drugs have a good analgesic, antipyretic effect. However, they do not sufficiently effectively reduce the risk of complications from influenza, which, as noted above, arise quite often and are very dangerous. In addition, many of these drugs do not have a sufficient shelf life.

The objective of the present invention is to expand the range of cold and flu remedies by creating new combination drugs that quickly eliminate the symptoms of colds and reduce the risk of complications after flu with high efficiency.

The problem is solved by the creation of new combined preparations. One of the options is a preparation based on a pharmaceutical composition containing acetylsalicylic acid, a component selected from the group: metamizole, paracetamol, ibuprofen, an antihistamine selected from the group: promethazine, pheniramine, terfenadine, astemizole, acrivastine, loratadine, fexofenadine, and phenylephrine and ascorbic acid. The drug may additionally contain caffeine. If necessary, it may contain excipients.

Another option according to the invention is a drug recommended for patients for whom acetylsalicylic acid is contraindicated, for example, suffering from gastrointestinal disorders. It is based on a pharmaceutical composition containing metamizole, paracetamol or ibuprofen, an antihistamine selected from the group: promethazine, pheniramine, terfenadine, astemizole, acrivastine, loratadine, fexofenadine, as well as phenylephrine and ascorbic acid. The drug may additionally contain caffeine. If necessary, it may contain excipients.

It was found that the combined introduction of NSAIDs and an analgesic-antipyretic or two NSAIDs into the drug leads to a significant increase in antipyretic, anti-inflammatory and analgesic effects.

The choice of antihistamine depends on the patient's condition and time of day. Considering the peculiarities of the action of antihistamines, a combined preparation was developed in the form of a kit to eliminate the symptoms of colds and flu, characterized in that it contains three drugs intended for use in the morning, afternoon and evening hours, and for administration in the evening it contains the drug comprising acetylsalicylic acid, a component selected from the group: metamizole, paracetamol, ibuprofen, as well as promethazine, phenylephrine and ascorbic acid, or a drug comprising metamizole, parace tamol or ibuprofen, promethazine, phenylephrine and ascorbic acid, for daytime use, it contains a drug including acetylsalicylic acid, a component selected from the group: metamizole, paracetamol, ibuprofen, as well as pheniramine or acrivastine, phenylephrine and ascorbic acid, including metamizole, paracetamol or ibuprofen, pheniramine or acrivastin, phenylephrine and ascorbic acid, and for administration in the morning, it contains a preparation comprising acetylsalicylic acid, a component selected from the group: metamizo l, paracetamol, ibuprofen, an antihistamine selected from the group: terfenadine, astemizole, loratadine, fexofenadine, as well as phenylephrine and ascorbic acid or a drug that includes metamizole, paracetamol or ibuprofen, an antihistamine selected from the group: terfedinden, asth fexofenadine, as well as phenylephrine and ascorbic acid.

The preparations according to the invention can be in the form of powders, granules or other acceptable dosage forms, for example tablets, capsules, syrups, solutions or suspensions for oral administration.

Pharmaceutically acceptable excipients are used depending on the desired form of administration. Most preferably, water, glycerin, microcrystalline cellulose, cellulose derivatives, PVP, starch and its modifications, sugars such as lactose and glucose, dusting, gliding, flavoring and the like are used.

Improving the bioavailability and effectiveness of the compositions can be achieved by introducing as auxiliary substances malic, succinic or isocitric acids, glycine from 10 to 100 mg.

To obtain drugs using methods generally accepted in pharmacy.

Doses of the administered ingredients may vary depending on the severity of the disease, gender, age, the presence of concomitant diseases and the nature of the substances used. Preferably, the doses of acetylsalicylic acid, paracetamol, ibuprofen are from 20 to 500 mg, analgin from 5 to 500 mg, antihistamines from 1 to 50 mg, phenylephrine from 25 to 100, ascorbic acid (vitamin C) from 5 to 700 mg. The drug exhibits analgesic, antipyretic, anti-inflammatory, antiviral, antihistamine, significant angioprotective, antioxidant, anti-edematous effects. A practically new drug is a universal remedy for acute respiratory viral infections, influenza, and other febrile conditions. The components are administered in therapeutically effective amounts.

The individual unit forms can be granules, tablets, capsules containing powder or granules, sachets.

The possibility of carrying out the invention can be confirmed by the following examples, which serve to illustrate, but do not limit the scope of the invention:

Examples 1-5.

The compositions of the tablets of the composition according to the invention are given in table. 1.

Example 6

Syrup containing the following components, mg:

Paracetamol 250

Metamizole 50

Loratadine 20

Phenylephrine 50

Ascorbic acid 100

Sugar 500

Sodium Benzoate 50

Citric Acid 50

Propylene glycol 2 ml

Water Up to 100 ml

Example 7-11 Capsules of the composition according to the invention (table. 2).

Capsules contain powders or granules.

The drug can be made in the form of powders or granules placed in separate sachets.

Example 12

The set consists of three sachets.

The first package is for reception in the morning. It contains powder for solution (oral), mg:

Acetylsalicylic acid 200

Paracetamol 300

Loratadine 10

Phenylephrine 10

Ascorbic acid 60

Caffeine 10

Excipients: sodium starch glycolate, sodium citrate dihydrate, lactose, titanium dioxide, lemon flavor, calcium phosphate.

The second package is for daytime use. It contains powder for solution (oral), mg:

Acetylsalicylic acid 200

Paracetamol 300

Akrivastin 10

Phenylephrine 10

Ascorbic acid 60

Excipients: sodium starch glycolate, sodium citrate dihydrate, lactose, titanium dioxide, lemon flavor, calcium phosphate.

The third package is intended for reception in the evening (night) hours. It contains powder for solution (oral), mg:

Acetylsalicylic acid 200

Paracetamol 300

Promethazine 10

Phenylephrine 10

Ascorbic acid 60

Excipients: sodium starch glycolate, sodium citrate dihydrate, lactose, titanium dioxide, lemon flavor, calcium phosphate.

The kit may also be in the form of tablets or capsules.

The invention was tested in laboratory conditions and in the clinic on volunteers.

The activity of the proposed combination preparations was studied in the laboratory on white outbred mice according to generally accepted tests.

The analgesic effect was studied by tests of “hot plate”, “vinegar cramps”, “pressure on the paw”.

Antipyretic effect was assessed by a decrease in hyperthermia 2 hours after administration of the test substance. A febrile reaction was induced by the administration of a 20% suspension of baker's yeast.

Anti-inflammatory and anti-edematous effect was evaluated on the model of “carrageenin paw edema in rats”. An acute inflammatory reaction (edema) is reproduced by subplanetary administration of 0.1 ml of a 1% solution of carrageenin. The severity of the inflammatory reaction was evaluated 3 hours after the induction of inflammation by the change in paw volume. The test substances are injected into the stomach with a probe 1 hour before carrageenin. The anti-inflammatory effect was evaluated by reducing edema.

The antihistamine effect was studied on a model of bronchospasm caused by aerosol exposure to histamine (1% solution).

Antiviral activity was studied against influenza virus in in vitro experiments in cell culture. For work, a chicken embryo cell culture was used. Evaluation of antiviral activity of drugs was carried out by monitoring the reproduction of the virus.

All tests performed showed satisfactory results of the investigated activities compared with the control.

Research on volunteers. In the group of patients taking the formulations according to example 1 and 2, there was a significant improvement in the condition for 3-4 days. The nasal congestion, headache, chills, pain in the joints and muscles disappeared, and breathing was relieved. The drug was well tolerated, with virtually no side effects.

The studies conducted allow us to conclude that the new combination drugs are highly effective in the treatment of influenza, colds and other febrile conditions with an unknown etiology. The presented drugs can eliminate the adverse symptoms associated with these diseases.

Claims (11)

1. A combined preparation for eliminating the symptoms of colds and flu, characterized in that it contains acetylsalicylic acid, a component selected from the group: metamizole, paracetamol, ibuprofen, an antihistamine selected from the group: promethazine, pheniramine, terfenadine, astemizole, acrivastin, loratadine, fexofenadine, as well as phenylephrine and ascorbic acid in therapeutically effective amounts. 2. The drug according to claim 1, characterized in that it further comprises caffeine. 3. The drug according to claim 1 or 2, characterized in that it further comprises pharmaceutically acceptable excipients. 4. The drug according to claim 3, characterized in that the antihistamine is contained in an amount of from 1 to 50 mg per unit dose. 5. The drug according to claim 3, characterized in that it is made in the form of capsules, tablets, syrup, sachets. 6. A combined preparation for eliminating the symptoms of colds and flu, characterized in that it contains metamizole, paracetamol or ibuprofen, an antihistamine selected from the group: promethazine, pheniramine, terfenadine, astemizole, acrivastin, loratadine, fexofenadine, as well as phenylebenufrin and acid in therapeutically effective amounts. 7. The drug according to claim 6, characterized in that it further comprises caffeine. 8. The drug according to claim 6 or 7, characterized in that it further comprises pharmaceutically acceptable excipients. 9. The drug according to claim 8, characterized in that the antihistamine is contained in an amount of from 1 to 50 mg per unit dose. 10. The drug according to claim 8, characterized in that it is made in the form of capsules, tablets, syrup, sachets. 11. A combined preparation for eliminating the symptoms of colds and flu, characterized in that it is a kit containing three components intended for administration in the morning, afternoon and evening hours, and for administration in the evening hours it contains the preparation according to any one of paragraphs. 1 and 2, in which the antihistamine is promethazine, for daytime use it contains the drug according to any one of claims 1 and 2, in which the antihistamine is pheniramine or acrivastine, and for morning use it contains pre arat according to any one of claims 1 and 2, wherein the antihistaminic agent is one of a terfenadine, astemizole, loratadine, fexofenadine.