Pharmaceutical composition containing desloratadine (versions)

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and medicine, namely to manufacturing drug preparations for treating allergic diseases, such as allergic rhinitis and urticaria. According to the first version, the pharmaceutical composition contains an active substance that is desloratadine, and additives, including citric acid, calcium hydrogen phosphate dihydrate, microcrystalline cellulose, starch, lactose, magnesium stearate, and talc. According to the second version, the pharmaceutical composition contains an active substance that is desloratadine, and additives, including Pearlitol 100SD-Mannitol, calcium hydrogen phosphate dihydrate, microcrystalline cellulose, starch, magnesium stearate, and talc. According to the third version, the pharmaceutical composition contains an active substance that is desloratadine, and additives, including sodium carboxymethyl starch, microcrystalline cellulose, colloidal silicone dioxide, and sodium sodium stearyl fumarate. According to the fourth version, the pharmaceutical composition contains an active substance that is desloratadine, and additives, including sodium carboxymethyl starch, microcrystalline cellulose, Pearlitol 100SD-Mannitol, magnesium stearate, and talc. The pharmaceutical composition is presented in the form of a film-coated tablet.

EFFECT: pharmaceutical composition according to the invention is storage-stable and releases the active substance quickly in the gastrointestinal tract.

10 cl, 9 tbl, 20 ex

 

The invention relates to pharmaceutical industry and medicine, in particular to the manufacture of pharmaceutical preparations for the treatment of allergic diseases such as allergic rhinitis, allergic conjunctivitis, allergic asthma, urticaria, symptomatic dermographism, angioedema, allergic reactions to insect bites, itchy dermatitis (contact allergodermatita, chronic eczema), but is not limited to this.

The invention is a pharmaceutical composition comprising the active substance is desloratadine, auxiliary substances and shell, made in the form of tablets, film coated liner.

The primary use of the invention is the treatment of allergic rhinitis and urticaria.

Pharmacotherapy of allergic rhinitis, depending on the severity of the disease carried by the following drugs:

1. Antihistamines (desloratadine, levocetirizine and others) in the form of film coated tablets;

2. Stabilizers fat cell membranes (sodium cromoglycate in the form of a nasal spray);

3. Intranasal corticosteroids (beclomethasone, budesonide, and others);

4. Ipratropium bromide in the form of a nasal spray [1].

When the hives are used antihistamines, cold comp is Essy and soothing itch lotions. In severe cases, sometimes you have to resort to steroids [2].

The disadvantage of the use of levocetirizine is the presence of such side effects as drowsiness, cognitive and psychomotor disturbances [3].

The disadvantage of the use of sodium cromoglycate is the slow development of membrane-stabilizing effect (2-4 weeks) [3].

The disadvantages of the use of intranasal glucocorticosteroids are the slow development of clinical effect (1-3 days), the 4-time applications (beclomethasone dipropionate), the presence of such side effects like itchy nose, sneezing, dryness and burning of the mucous membrane of the nose and throat, which creates a significant inconvenience for patients, ipratropium bromide also has a short duration of action (4-8 hours) [3].

Desloratadine active metabolite loratidine, a well-known selective blocker of H1-histamine receptors of the second generation. Desloratadin has a similar pharmacodynamic properties, but is more active than loratadine (2.5-4 times) and other drugs in this group. In experimental studies it was shown that desloratadine has the greatest affinity for H1-histamine receptors and slow dissociation from them. On the affinity it 200 times picsof is Nadine, 50 times - loratadine and cetirizine, 3 times - levocetirizine [4].

It has been shown that desloratadine has 60 times more affinity to H1-receptors than for H2-muscarinic receptors. The selectivity of the drug is confirmed by the results of placebo-controlled pharmacological and clinical studies, in which desloratadin not anticholinergic symptoms such as dry mouth and visual disturbances [4].

Preclinical studies have shown that desloratadine has a pronounced anti-inflammatory, inhibits many of the mediators involved in the development of systemic allergic inflammation, including cytokines and chemokines, and adhesion molecules [4].

Desloratadin characterized by high speed, maximum plasma concentration and a rapid onset of action (through a 1.25-3 hours). Pharmacokinetics of desloratadine is linear and proportional to the dose. The half-life of the drug is 21-24 h, which allows you to assign it 1 time/day [4].

Food intake has no effect on the rate and extent of absorption of the drug. The drug can be taken after meals and on an empty stomach, which indicates the ease of its application. Therefore, prevents and facilitates development for allergic reactions, has antipruritic and against exsudativum action reduces the permeability of capillaries, prevents the development of tissue edema, spasm of smooth muscles [4].

Known medicines with active substance desloratadine with dosage 5 mg - Arius", "Largestin", "Desloratadin-Teva in the form of tablets, film coated liner.

The closest analogue (prototype) of the present invention is a medicinal product "Desloratadin-Teva". The composition of the drug:

active substance: desloratadine 5 mg;

- excipients tablet core: microcrystalline cellulose 65,800 mg; magnesium oxide 2,250 mg; pregelatinized starch 4,750 mg; lactose 4,500 mg hypromellose - 4 thousand 1,700 mg; zinc stearate 1,000 mg;

- excipients-shell: Opadry blue 03B90819 - 2,975 mg (hypromellose 60,00%, titanium dioxide 27,21%, macrogol 400 - 8,00%, Indigo Carmine 4,79%) [6].

The disadvantage of this structure is the presence of magnesium oxide having absorbent properties, and consequently, reduces the activity of the active substance.

And it is also known that it is preferable to use directionspanel with desloratadine excipients, or reactive with desloratadine with good technological properties, such as lactose, proposed in this composition, but together with a pharmaceutically acceptable antioxidant, on the example of the disodium edetate, citric acid [5].

The purpose of the present invention - expanding Arsenal of medicines for the treatment of allergic diseases with pharmaceutical compositions containing as active substances desloratadin. The obtained pharmaceutical composition must meet the requirements of the State Pharmacopoeia, have good strength and raspadaemost to be stable during storage and rapidly releasing the active substance in the gastrointestinal tract.

The goal has been achieved by the development of pharmaceutical compositions comprising the active substance is desloratadine, auxiliary substances and shell. Using one or a combination of the following factors:

a) the introduction of a pharmaceutically acceptable antioxidant in the form of pharmaceutical compositions, for example, citric acid, mainly with the dosage of 1-10 wt. -%, preferably 1 wt. -%;

b) the use in pharmaceutical compositions inert, stable, non-hygroscopic fillers, no reacts with desloratadine: mannitol, preferably mannitol brand Pearlitol 100SD-Mannitol, ready mixes for pressing, such as Prosolv Easytab SP, but not limited to;

b) a coating on the tablet is the core of the spray.

The invention is a FA the pharmaceutical composition, consisting of the active substance is desloratadine, preferably with a dosage of 5 wt. -%, auxiliary substances and shell, made in the form of tablets, film coated liner.

The pharmaceutical composition of the following composition, % wt.:

- active ingredient:

desloratadine - 5

- excipients tablet core:

citric acid - 1-10

calcium hydrogen phosphate dehydrate - 5-10

microcrystalline cellulose - 10-50

starch - 1-20

lactose - 20-70

magnesium stearate and 0.5-1

talc - 1-3

Total - 100% of the mass.

- skin pill - to 7 wt%. including the tablet-kernel.

As filler in this solid dosage form is used lactose because of its good pressuemosti, cheap and pleasant taste. The dosage of lactose - 20-70 wt. -%, but not limited to, the preferred dosage is 40% of the mass.

However, it is known that lactose hygroscopic, can react with desloratadine.

To prevent interaction of desloratadine with lactose in the composition of the pharmaceutical composition is injected pharmaceutically acceptable antioxidant citric acid 1-10% wt., mostly 1-2% of the mass.

In the specified pharmaceutical composition of calcium hydrogen phosphate dehydrate is filler. Dosage of calcium hydrogen phosphate Digue is dratha - 5-10% of the mass. The preferred dosage of calcium hydrogen phosphate dihydrate - 10 wt. -%, but not limited to.

Microcrystalline cellulose acts as a filler and binder, provides a high compressibility and flowability to the composition of desloratadine. Preferably (but not limited to, the use of microcrystalline cellulose MCC brand-102. Dosage microcrystalline cellulose - 10-50 wt. -%, mainly 37,0% of the mass.

Starch, preferably (but not limited to, corn starch pregelatinized, performs the function of disintegrant, that is, substances which improve the raspadaemost tablets. Dosage of starch - 1-20 wt%. but not limited to, preferably 4% of the mass.

To improve fluidity tableting mass., prevent sticking them on the plungers and the walls of the holes of the matrix as the lubricant is magnesium stearate, mainly with dosage of 0.5-1 wt. -%, preferably to 1.0 wt. -%, and as solstudio substances used talc, mainly with a dosage of 1-3 wt. -%, preferably of 2.0% of the mass.

The proposed combination of active substances and excipients was determined experimentally and is optimal. The result is a mixture of substances having good processing properties in the process of tablet is the way, and the resulting tablets have properties that satisfy the requirements of the drug, i.e. have a saleable condition without chips and cracks, have sufficient strength and raspadaemost.

The presence of shell gives pharmaceutical composition, first, the stability of the composition during storage, and secondly, it improves its appearance.

The shell is applied to the tablet cores by spraying suspensions, prepared from ready-mix Opadry Blue (e.g., Opadry II 85F205015 Blue), or VivaCOAT (for example, VivaCoat RA-8P-000), but is not limited to this. The predominant content of the shell in the pharmaceutical composition is up to 7% of the mass. by weight of the tablet core, preferably 5% of the mass. by weight of the tablet core.

The possibility of carrying out the invention is illustrated by examples (but not limited to), are presented in table 1.

Analyzed physico-chemical properties of the samples pharmaceutical compositions of examples 1-4. The compressive strength was determined on the device model TW firm "ERWEKA". Test "Dissolution", characterizing the rate of release of the active substance from the pharmaceutical composition in an environment similar to the environment of the gastrointestinal tract, conducted in accordance with the HEP 42-0003-04. Quantitative determination of desloratadine tablets as well as the content of impurities was determined by HPLC method.

The results obtained are presented in table 2.

Table 2 also presents the normative values in accordance with the draft monograph enterprises (FSE), developed by JSC ğtatkhimpharmpreparatyğ.

This project monograph was developed on the basis of the applicable requirements of the State Pharmacopoeia and the European Pharmacopoeia 8.0.

Thus, the normative value of the index "Dissolution" in the project Fund complies with the normative value specified in the CFC 42-0003-04 "Dissolution" - not less than 75%.

The interval of the quantitative content of desloratadine tablets specified in the project Fund (0,0045 to 0,0055 g), calculated on the basis of the limit value of the deviation of the quantitative content of the active substance in tablets ±10%, set the global Fund XI (volume 2, General articles on dosage forms, tablets).

The normative value of the content of an impurity - N-formelbasierten not specified, no GF, neither in the European Pharmacopoeia. In this regard, in the project Fund prescribed standard value no more than 1%, as specified by the scientific and technical literature on the development of drugs with the active substance desloratadine.

The normative value of the content amounts of unidentified impurities installed in the Fund is not more than 0.5%, meets the requirements of the European Pharmacopoeia 8. (also not more than 0.5%).

Table 2
Name of indicator and unit of measureExample 1Example 2Example 3Example 4Requirements of the Fund
123456
Compressive strength, kgf6-78-10156-7Not regulated
Test "Dissolution", % mass. (average of 12 values)91,39100,1586,78102,86At least 75%

As can be seen from table 2, the technical result of the invention is achieved

- all examples of the invention, 1-4 on key physical and chemical properties comply with the requirements of the draft monograph of the company.

Collectively, the physical and the Ko-chemical parameters the best example is example 2 - pharmaceutical composition in the form of tablets, coated film-coated, weighing 105 mg, containing components in the following ratios, wt. -%:

- active ingredient:

desloratadine - 5,0

- excipients tablet core:

citric acid - 1,0

calcium hydrogen phosphate dehydrate - 10,0

microcrystalline cellulose (MCC 102) is 37.0

the pregelatinized corn starch (Starch 1500) - 4,0

lactose monohydrate (tablettose 80) - 40,0

magnesium stearate - 1,0

talc - 2,0

Total - 100% of the mass.

- skin pill:

Opadry II 85F205015 Blue to 5.0.

A method of obtaining a pharmaceutical composition includes mixing of desloratadine in the tank with citric acid, adding calcium hydrogen phosphate dihydrate, mixing, adding microcrystalline cellulose, mixing, adding lactose monohydrate and corn starch, mixing, passing through a sieve, add magnesium stearate and talc, tableting, cooking covering suspension, coating the obtained tablets-shell nuclei.

Developed pharmaceutical composition containing the active substance - desloratadin, pharmaceutically acceptable excipients, and a shell made in the form of tablets, coated film-coated, characterized in that it contains the following components, wt. -%:

desloratadine - 5

- excipients tablet core:

mannitol - 20-70

calcium hydrogen phosphate dehydrate - 5-10

microcrystalline cellulose - 15-50

starch - 1-20

magnesium stearate and 0.5-1

talc - 1-3

Total - 100% of the mass.

- skin pill - to 7 wt%. including the tablet-kernel

Mannitol is used as a filler in the composition, the choice of excipients is due to the fact that he is not hygroscopic and can be used for tabletting moisture-sensitive substances (in particular, desloratadine). Dosage of mannitol - 20-70 wt. -%, preferably 40.0% of mass., but is not limited to this.

Microcrystalline cellulose acts as a filler and binder. Dosage microcrystalline cellulose - 15-50 wt. -%, preferably 38,0% of the mass.

Calcium hydrogen phosphate dehydrate acts as a filler. Dosage is 5-10 wt. -%, preferably 10.0% of the mass.

Starch, mainly (but not limited to, corn starch pregelatinized, performs the function of a binder and disintegrant. Dosage of starch - 1-20 wt. -%, preferably 4.0% wt.

Magnesium stearate is a lubricant. Dosage of magnesium stearate and 0.5 to 1.0 wt. -%, preferably of 1.0% of the mass.

Talc - moving substance, dosage of 1-3 wt. -%, preferably the I dosage of 2.0 wt. -%, but is not limited to this.

The possibility of carrying out the invention is illustrated by examples 5-10 are presented in table 3, but are not limited to.

The studied physico-chemical properties of examples 5-10 on the above analysis methods, the results are presented in table 4.

As can be seen from table 4, the technical result of the invention is achieved

- all examples of the invention, the 5-10 key physico-chemical properties comply with the requirements of the project Fund.

On set of physico-chemical parameters are presented in table 4, the best example is the example 6 is a pharmaceutical composition in the form of tablets, coated film-coated, weighing 105 mg, containing components in the following ratios, wt. -%:

- active ingredient:

desloratadine - 5,0

- excipients tablet core:

mannitol (Pearlitol 100SD-Mannitol) - 40,0

calcium hydrogen phosphate dehydrate - 10,0

microcrystalline cellulose (MCC 102) - 38,0

the pregelatinized corn starch (Starch 1500) - 4,0

magnesium stearate - 1,0

talc - 2,0

Total - 100% of the mass.

- skin pill:

Viva COAT PA-8P-000 - 5,0.

In this part of the proposed mannitol "Pearltol 100SD-Mannitol" - the second generation of mannitol obtained by spray drying. He is the best technological properties: has a finely porous structure of the particles and low density. This brand mannitol has an excellent compressibility, excellent flowability, chemical stability and non-hygroscopic [7].

The method of obtaining the pharmaceutical composition includes a preliminary preparation of active substances and excipients by sieving through a sieve, mixing of desloratadine and corn starch pregelatinization, adding mannitol, mixing, adding microcrystalline cellulose, mixing, adding talc and magnesium stearate, tableting, cooking covering suspension, coating tablets-shell nuclei.

Developed pharmaceutical composition containing the active substance - desloratadin, pharmaceutically acceptable excipients, and a shell made in the form of tablets, coated film-coated, characterized in that it contains the following components, wt. -%:

- active ingredient:

desloratadine - 5

- excipients tablet core:

carboximetilkrahmal sodium - 0,9-6

microcrystalline cellulose - 80-92

colloidal silicon dioxide is 1.5-10

stearyl fumarate sodium - 0,4-1

Total - 100% of the mass.

Microcrystalline cellulose acts as a filler and binder. It is preferable to use microcrystalline cellulose MCC brand-102 with dosage 80-92% of the mass, but not limited to.

Carboximetilkrahmal sodium - superdisintegrants improving raspadaemost tablets used for tabletting of poorly soluble active ingredients. Use even in small quantities (1-2%) allows to achieve the best raspadaemosti tablets, and as a result their future better dissolution in biological fluids. In addition, carboximetilkrahmal sodium is well pressed and mixed with other ingredients. The preferred dosage of carboximetilkrahmal sodium - 0.9 to 1.0 wt. -%, but is not limited to this.

Colloidal silicon dioxide performs the function solstudio substances, the preferred dosage is 1.9 to 2.0 wt. -%, but is not limited to this.

Stearyl fumarate sodium performs the function of the lubricant, the preferred dosage of 0.4-0.5 wt. -%, but is not limited to this.

Stearyl fumarate sodium has a high melting point, therefore, is a good lubricant for direct compression, it does not have an unpleasant metallic taste is a relatively inert substance is.

The possibility of carrying out the invention is illustrated by examples 11-16 are presented in table 5, but are not limited to.

The resulting samples (examples 11-16) were analyzed physico-chemical properties. The results of the analyses are presented in table 6.

As can be seen from table 6, the technical result of the invention is achieved

- all examples of the invention, the 11-16 on key physical and chemical properties comply with the requirements of the project Fund.

On set of physico-chemical parameters are presented in table 6, the best example is the example 12 is a pharmaceutical composition in the form of tablets, coated film-coated, weighing 105 mg, containing components in the following ratios, wt. -%:

- active ingredient:

desloratadine - 5,0

- excipients tablet core:

carboximetilkrahmal sodium - 0,9

microcrystalline cellulose (MCC 102) - 91,8

colloidal silicon dioxide (Aerosil) - 1,9

stearyl fumarate sodium - 0,4

Total - 100% of the mass.

- skin pill:

Viva COAT PA-8P-000 - 5,0.

It should be noted that as microcrystalline cellulose, carboximetilkrahmal sodium, silicon dioxide to toidnogo (Aerosil), stearyl fumarata sodium can be used ready mix “Prosolv Easytab SP”. The composition of the mixture: microcrystalline cellulose (MCC 102) to 96.5 wt. -%, carboximetilkrahmal sodium to 1.0 wt. -%, colloidal silicon dioxide (Aerosil) to 2.0 wt. -%, fumarate sodium - 0.5% mass.

The use of this mixture in the composition of desloratadine eliminates the introduction of other auxiliary substances, which simplifies and accelerates the production process, as well as to provide a high flowability and compressibility tableting mixture at zero flowability and poor pressuemosti substance of desloratadine.

Example 16 is a pharmaceutical composition in the form of tablets, coated film-coated, weighing 105 mg, containing components in the following ratios, wt. -%:

- active ingredient:

desloratadine - 5,0

- excipients tablet core:

Prosolv Easytab SP - 95,0

Total - 100% of the mass.

- skin pill:

Viva COAT PA-8P-000 - 5,0.

The method of obtaining the pharmaceutical composition includes a preliminary preparation of active substances and excipients by sieving through a sieve, mixing of desloratadine and mixtures "Prosolv Easytab SP", tableting, cooking covering suspension, coating tablets-shell nuclei.

Developed pharmaceutical composition containing the active substance - desloratadin and pharmaceutically acceptable what s auxiliary substances and shell, made in the form of tablets, coated film-coated, characterized in that it contains the following components, wt. -%:

- active ingredient:

desloratadine - 5,0

- excipients tablet core:

carboximetilkrahmal sodium - 0,5-4

microcrystalline cellulose - 10-80

mannitol - 10-80

magnesium stearate and 0.5-1

talc - 1-3

Total - 100% of the mass.

- skin pill - to 7 wt%. including the tablet-kernel

The preferred dosing excipients: mannitol - 22 wt. -%, microcrystalline cellulose - 68,0% wt., carboximetilkrahmal sodium to 2.0 wt. -%, magnesium stearate and 1.0 wt. -%, talc - 2,0% of the mass.

The possibility of carrying out the invention is illustrated by examples 17-20 are presented in table 7, but are not limited to.

Table 7
Component nameThe range of dosages component, % of the mass.The content of component, % of the mass.
Example 17Example 18Example 19Example 20
123 456
Active ingredient:
Desloratadine55,05,05,05,0
Excipients tablet core:
Carboximetilkrahmal sodium0,5-44,02,01,53,5
Microcrystalline cellulose10-8050,068,080,010,0
mannitol10-8037,022,010,080,0
magnesium stearate 0,5-11,01,01,00,5
talc1-33,02,02,51,0
Total-100% of the mass.

The resulting samples (examples 17-20) were analyzed physico-chemical properties. The results of the analyses are presented in table 8.

As can be seen from table 8, the technical result of the invention is achieved

- all examples of the invention, 17-20 on key physical and chemical properties comply with the requirements of the project Fund.

On set of physico-chemical parameters are presented in table 8, the best example is the example of 18 - pharmaceutical composition in the form of tablets, coated film-coated, weighing 105 mg, containing components in the following ratios, wt. -%:

- active ingredient:

desloratadine - 5,0

- excipients tablet core:

carboximetilkrahmal sodium (primogel) - 2,0

microcrystalline cellulose (MCC 102) - 68,0

mannitol (Pearlitol 100SD-Mannitol) - 22,0

magnesium stearate - 1,0

talc - 2,0

Total - 100% of the mass.

- skin pill:

Viva COAT RA-8P-000 - 5,0

The method of obtaining the pharmaceutical composition includes a preliminary preparation of active substances and excipients by sieving through a sieve, mixing of desloratadine and carboximetilkrahmal sodium, the addition of mannitol, mixing, adding microcrystalline cellulose, mixing, adding talc and magnesium stearate, tableting, cooking covering suspension, coating tablets-shell nuclei.

The experimental studies were conducted to compare the physico-chemical properties of the invention (the best examples 2, 6, 12, 16, 18) with drugs "Desloratadin-Teva" and "Arius" with the same dosage of desloratadine - 5% of the mass. For reliability studies were performed in the same conditions - analyzed tablet, aged for 1 year at 25°C.

The results of the analyses are presented in table 9.

It should be noted that in tables 2, 4, 6, 8 shows the results of the analysis of the test Dissolve after the manufacture of tablets, while table 9 presents the results of the analysis conducted 1 year after storage at a temperature of +25°C, so the values are different.

It should also be noted that in tables 2, 4, 6, 8 shows the results with the holding of N-formelbasierten and the total content of individual unidentified impurities in the samples, aged for 7 months at +40°C and relative humidity of 75%. Table 9 analyses the content of these impurities was performed in samples aged for 1 year at a temperature of +25°C.

From table 9 it follows that developed in the pharmaceutical compositions, the total content of individual unidentified impurities lower than that of drugs "Arius and Desloratadine-Teva". The content of N-formelbasierten developed in the compositions is slightly higher than the Comparators, however, the obtained values of the content of N-formelbasierten are within normal limits (no more than 1% according to the project Fund and the European Pharmacopoeia 8.0), moreover, is below 0.5%, which is indicative of high quality products.

Experimental studies allow us to conclude that the developed pharmaceutical compositions correspond to European standards for medicines containing as an active ingredient, desloratadine made in the form of tablets, film coated liner. Developed pharmaceutical compositions allow to expand the Arsenal of drugs for the treatment of allergic diseases.

The list of references

1. Allergic rhinitis: problems, diagnosis, care is [Electronic resource]. - L. C. Luss, doctor of medical Sciences, Institute of immunology MZ the Russian Federation. - Mode of access: http://www.lvrach.ru/2002/04/4529344/

2. Kolher P. C. Urticaria, angiotech. - M.: Practical medicine, 2012. - 363 S.

3. Turov, A. B. Allergic rhinitis. Diagnosis and treatment / A. B. Turovsky, M. A. Miroshnichenko, Y. S. Kudryavtseva // Russian medical journal. - 2011. No. 6. - senior 409.

4. Goryachkin, L. A. the Role of desloratadine (ERISA) in the treatment of allergic diseases / L. A. Goryachkin, S. C. Moses // Consilium provisorum. - 2002. - №2. - [Electronic resource]. - Mode of access: http://old.consilium-medicum.com/media/provisor/02_03/25.shtml

5. RF patent 2209627 "does Not contain lactose, non-hygroscopic and anhydrous pharmaceutical preparations descarboethoxyloratadine" / Redman Martin P., Balter Hal T., Wald, Stephen A., Rubin, Paul D.

6. Instructions for use of the drug, Desloratadin-Teva".

7. Mannitol Pearlitol [Electronic resource]. - Mode of access: http://www.witec.com.ua

1. The pharmaceutical composition containing the active substance - desloratadin, pharmaceutically acceptable excipients, and a shell made in the form of tablets, coated film-coated, characterized in that it contains the following components, wt%:
active substance:
desloratadine - 5
- excipients tablet core:
citric acid - 1-10
calcium hydrogen phosphate dehydrate - 5-10
micro is kristallicheskaja cellulose - 10-50
starch - 1-20
lactose - 20-70
magnesium stearate and 0.5-1
talc - 1-3
Total - 100 wt.%:.
- skin pill - to 7 wt.%:. including the tablet-kernel.

2. The pharmaceutical composition under item 1, characterized in that it contains components in the following dosages, wt.%:
active substance:
desloratadine - 5,0
- excipients tablet core:
citric acid - 1,0
calcium hydrogen phosphate dehydrate - 10,0
microcrystalline cellulose is 37.0
starch is pregelatinized corn - 4,0
lactose - 40,0
magnesium stearate - 1,0
talc - 2,0
Total - 100 wt.%
- skin pill, wt.% from tablet kernel:
Opadry Blue To 5.0.

3. The pharmaceutical composition containing the active substance - desloratadin, pharmaceutically acceptable excipients, and a shell made in the form of tablets, coated film-coated, characterized in that it contains the following components, wt%:
active substance:
desloratadine - 5
- excipients tablet core:
mannitol brand "Pearlitol 100SD-Mannitol" - 20-70
calcium hydrogen phosphate dehydrate - 5-10
microcrystalline cellulose - 15-50
starch - 1-20
magnesium stearate and 0.5-1
talc - 1-3
Total - 100 wt.%
- skin pill - to 7 wt.% including the tablet-kernel.

4. The pharmaceutical composition according to p. 3, distinguishing the I, that contains components in the following dosages, wt.%:
active substance:
desloratadine - 5,0
- excipients tablet core:
mannitol brand "Pearlitol 100SD-Mannitol" - 40,0
calcium hydrogen phosphate dehydrate - 10,0
microcrystalline cellulose - 38,0
starch is pregelatinized corn - 4,0
magnesium stearate - 1,0
talc - 2,0
Total - 100 wt.%
- skin pill, wt.% from tablet kernel:
VivaCOAT to 5.0.

5. The pharmaceutical composition containing the active substance - desloratadin, pharmaceutically acceptable excipients, and a shell made to the form of tablets, coated film-coated, characterized in that it contains the following components, wt%:
active substance:
desloratadine - 5
- excipients tablet core:
carboximetilkrahmal sodium - 0,9-6
microcrystalline cellulose - 80-92
colloidal silicon dioxide is 1.5-10
stearyl fumarate sodium - 0,4-1
Total - 100 wt.%
- skin pill - to 7 wt.% including the tablet-kernel.

6. The pharmaceutical composition according to p. 5, characterized in that it contains components in the following dosages, wt.%:
active substance:
desloratadine - 5,0
- excipients tablet core:
carboximetilkrahmal sodium - 0,9
microcrystalline cellulose - 91,8
silicon dioxide number is oigny - 1,9
stearyl fumarate sodium - 0,4
Total - 100 wt.%
- skin pill, wt.% from tablet kernel:
VivaCOAT to 5.0.

7. The pharmaceutical composition according to p. 6, characterized in that as microcrystalline cellulose, carboximetilkrahmal sodium, silicon dioxide colloidal, stearic fumarata sodium uses a mixture of "Prosolv Easytab SP".

8. The pharmaceutical composition according to p. 7, characterized in that it contains components in the following dosages, wt.%:
active substance:
desloratadine - 5,0
- excipients tablet core:
Prosolv Easytab SP - 95,0
Total - 100 wt.%
- skin pill, wt.% from tablet kernel:
VivaCOAT to 5.0.

9. The pharmaceutical composition containing the active substance - desloratadin, pharmaceutically acceptable excipients, and a shell made in the form of tablets, coated film-coated, characterized in that it contains the following components, wt%:
active substance:
desloratadine - 5
- excipients tablet core:
carboximetilkrahmal sodium - 0,5-4
microcrystalline cellulose - 10-80
mannitol brand "Pearlitol 100SD-Mannitol" - 10-80
magnesium stearate and 0.5-1
talc - 1-3
Total - 100 wt.%
- skin pill - to 7 wt.% including the tablet-kernel.

10. The pharmaceutical composition according to p. 9, characterized in that it contains the components is, for example, in the following dosage, wt.%:
active substance:
desloratadine - 5,0
- excipients tablet core:
carboximetilkrahmal sodium - 2,0
microcrystalline cellulose - 68,0
mannitol brand "Pearlitol 100SD-Mannitol" - 22,0
magnesium stearate - 1,0
talc - 2,0
Total - 100 wt.%
- skin pill, wt.% from tablet kernel:
VivaCOAT to 5.0.



 

Same patents:

FIELD: food industry.

SUBSTANCE: invention relates to nutritional compositions based on a natural extract. One proposes the application of an apple extract containing polyphenols for the manufacture of a complete nutritional composition for the reduction of symptoms of allergy caused by food in patients suffering from allergy caused by food allergens. The apple extract is enriched with polyphenols by at least 1.5 times relative to the unpurified apple extract. The composition contains 0.1% - 1 wt % of the apple extract.

EFFECT: proposed composition has no effect on the patients` sensitisation to the said allergens.

13 cl, 6 dwg

FIELD: biotechnology.

SUBSTANCE: invention is a composition having antibacterial, immunostimulating, anti-allergic and anti-inflammatory action, containing bacterial waste products useful for human body, in the form of exometabolites and fermentolysis products, characterised in that it is a culture medium of lactic acid bacteria, containing laxarane in an amount of 5-10 g/ml, caseicyne, isracydine or their mixture and lectins in an amount of 0.05-2.5 mol/l, histamine in an amount of 0.8-2.0 mmol/l and monocarboxylic fatty acid with an unbranched chain, namely, acetic acid, propionic acid, butyric acid and valeric acid - in an amount of 10-20 mg/ml.

EFFECT: expanding the range of agents having complementary antibacterial, immunomodulating, anti-allergic and anti-inflammatory action.

4 cl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to the field of cosmetology. Described is a stable and safe antioxidant composition, which can be applied daily. In particular, described is the antioxidant composition, which contains one or more compounds, selected from the group, which consists of D-aspartic acid, its derivatives and/or its salts. The composition can be applied with the purpose of suppressing and/or relief of a skin condition. Conditions of skin can include, but are not limited by them, small wrinkles, rough skin, dry skin, skin cancer, skin allergy, skin inflammation, and light-sensitive dermatosis. The composition can be applied as a medication for the external application on the skin.

EFFECT: invention ensures an increase of the antioxidant effect of the composition.

4 cl, 5 dwg, 31 ex

FIELD: medicine.

SUBSTANCE: enterosorbent is administered in the morning in an S daily dose on an empty stomach daily for 1-3 months 2-3 hours before meals. Colonising the intestinal flora with a normal flora is ensured by daily 4-week roal administration of the liquid biocomplex Normoflorin 3 times a day in age doses; the first and second intakes involve the preparation Normoflorin L, and the third one - Normoflorin B.

EFFECT: effective treatment of allergic diseases by eliminating endogenous and exogenous toxic substances of various nature and reducing thereby body sensibilisation, providing extensive cleansing of the bowels from fermentation and putrifaction products, pathogenic and opportunistic flora, and ensuring natural immunity stimulation.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and deals with application of extract of above-ground part/parts of oats, excluding grains, containing from 2 to 15% of flavonoids and from 0.2 to 2% of A and B avenacosides, for preparation of cosmetic and dermatological composition.

EFFECT: invention represents dermatological and cosmetic composition, containing such extract and possessing hypoallergenic properties.

8 cl, 2 ex, 2 tbl, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry and represents application of a composition, containing Bifidobacterium breve CNCM I-3865 (NCC2950) for preparation of a composition for prevention of allergic diarrhoea.

EFFECT: invention provides extension of an arsenal of means for prevention of allergic diarrhea.

7 cl, 1 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry, particularly to method of treatment of dermatological allergic state. Proposed method comprises injection of efficient amount of [4-(5-aminomethyl-2-fluorophenyl)piperidine-1-silt][7-fluorine-1-(2-metoxyethyl)-4-trifluorometoxy-1H-indol-3-il]methanon or its appropriate N-oxide, pharmaceutically acceptable salt or solvate.

EFFECT: higher efficiency.

5 cl, 1 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to an agent for preventing and/or treating an allergic disease selected from pollinosis, allergic rhinitis, allergic conjunctivitis, atopic dermatitis and asthma, which is a low-molecular polysulphated hyaluronic acid derivative.

EFFECT: obtaining a low-molecular polysulphated hyaluronic acid derivative.

15 cl, 103 dwg, 17 tbl, 55 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and medicine and concerns preparing a fast-acting effective and safe agent for treating rhinitis. Solving the problem provides the agent for treating rhinitis, particularly allergi rhinitis containing C-type natriuretic peptide (CNP) and/or B-type natriuretic peptide (BNP) as an active ingredient.

EFFECT: invention provides the notable health improvement in rhinitis, particularly in allergic rhinitis, and besides, the therapeutic effect, ensures fast and prolonged action, and gives no local side effects.

21 cl, 7 ex, 7 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is using a composition containing galactooligosaccharide, fructooligosaccharide and uronic acid oligosaccharide in preparing a composition for oral administration into an infant for preventing the local administration of corticosteroids and/or preventing the administration of a calcineurin inhibitor into the above infant, wherein uronic acid oligosaccharide represents a pectin degradation product and/or an alginate degradation product, and wherein using the corticosteroids and/or administering the calcineurin inhibitor is applicable for treating eczema, infantile eczema, atopic dermatitis, dermatitis herpetiformis, contact dermatitis, seborrheic dermatitis, neurodermatitis, psoriasis and intertrigo. Particularly, the composition is a nutritional composition.

EFFECT: what is shown is reducing probability of the local administration of corticosteroids and dermatological preparations to be required for the purpose of preventing the above skin diseases, or reducing the length of using the corticosteroids.

5 cl, 2 ex

FIELD: medicine.

SUBSTANCE: method involves the endoscopically controlled introduction of Coletex-D gel into a fistulous passage from the oesophagus until filled completely. The following exposure to a laser light at wavelength 0.66 mcm, output power 15-45 mWt/cm2 covers a fistulous passage mouth for 5-7 minutes to be repeated in the same mode every second day. The course of the laser light exposure makes 8-10 procedures.

EFFECT: method provides the adequate therapy requiring no abdominal surgeries and the lower risk of chest and abdominal injuries, the shorter rehabilitation period by improved sealing of the fistulous passage, fistula healing, reduced inflammatory process.

2 ex

FIELD: medicine.

SUBSTANCE: group of inventions relates to therapy, namely to pulmonology, and can be used for suppressing bacteria Pseudomonas aeruginosa, growing in anaerobic conditions, as well as for the treatment of the pulmonary bacterial infection, caused by them. For this purpose an effective quantity of an aerosol of a fluoroquinolone antibiotic, selected from the group, consisting of levofloxacin and ofloxacin, in a concentration of 0.125-0.128 mg/l is introduced.

EFFECT: application of the claimed inventions makes it possible to influence the said bacteria with the quantity of the fluoroquinolone antibiotic, effective of their growth suppression.

22 cl, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is a group of inventions involving: using poractant alfa in a dose of 100 to 200 mg/kg in a combination with beclomethasone dipropionate in a dose of 0.6 to 0.8 mg/kg for preventing bronchopulmonary dysplasia (BPD) (versions) for producing a therapeutic agent for preventing BPD, a respective pharmaceutical composition and a kit for the same application.

EFFECT: reducing the levels of pulmonary oxidative stress markers, but is also combined with improving the external pulmonary mechanics: a synergetic reduction of MAP (mean airway pressure) has been shown.

14 cl, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described new compounds of formula I or their pharmaceutically acceptable salts, wherein R1 means phenyl once or twice substituted by C1-6 alkyl, C1-6 alkoxy, halogen or 5-6-merous heteroaryl; R2 is phenyl once or twice substituted by C1-6 alkyl, C1-6 alkoxy, halogen, halogen-C1-6alkyl, halogen-C1-6alkoxy, C1-6 alkylsulphonyl, nitrile, etc. R3 means H or C1-6 alkyl; X - -O-, -NRa-,-S(O)m- or CRbRc, wherein Ra - H, C1-6 alkyl or C1-6 alkylcarbonyl; Rb and Rc mean H or together with the atom to which they are attached, form 5-merous cycle additionally containing 2 oxygen atoms; m is equal to 0-2; Y means -NRc-, wherein Rc - H or C1-6 alkyl.

EFFECT: compounds can find application in medicine for treating autoimmune and inflammatory diseases related to P2X7 purinoceptor.

15 cl, 1 tbl, 10 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to a therapy of a bronchoconstrictive condition and can be used for treating allergic rhinitis, asthma and chronic obstructive pulmonary disease (COPD). To this effect, a composition containing pentameric type A procyanidin in the concentration from approximately 55 wt/wt % to approximately 99 wt/wt %, trimeric procyanidin and tetrameric procyanidin, each in the concentration from approximately 0.5 wt/wt % to approximately 35 wt/wt % together with one or more pharmaceutical excipients in the concentration from approximately 0.5% to approximately 99.9% is administered into an individual in need thereof.

EFFECT: invention provides treating the bronchoconstrictive conditions without inducing side effects.

8 cl, 4 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining a polymer conjugate of an indolocarbazole compound of formula (I), where R1, R2, R3, W1 and W2 represent hydrogen, X represents methoxy-polyethyleneglycol. The method includes the interaction of a polymer compound of formula (II) with an indolocarbazole compound of formula (III), where Y stands for a methoxygroup. The nvention also relates to a polymer conjugate of formula (I), a pharmaceutical composition, containing the conjugate of formula (I) as an active ingredient, and to the application of the polymer conjugate of formula (I).

EFFECT: obtaining the polymer conjugate of the formula with a high output, the polymer conjugate of the formula for treatment of skin pathologies and HMGB1-associated pathologies.

48 cl, 7 dwg, 7 tbl, 15 ex

FIELD: medicine.

SUBSTANCE: invention refers to veterinary immunology. A method for the vaccinal prevention of respiratory diseases in calves involves immunising 20-30-day-old clinically healthy calves three times every 10-12 days by subcutaneous injections of animal donor's hyperimmune serum containing anti-parainfluenza virus type 3 hemagglutinin antibodies in titre min. 1:1280, anti-rednose virus hemagglutinin antibodies in titre min. 1:256, anti-viral diarrhoea virus hemagglutinin antibodies in titre min. 1:1024, anti-respiratory syncytial virus hemagglutinin antibodies in titre min. 1:128, anti-rotavirus and anti-coronavirus hemagglutinin antibodies in titre min. 1:128, in a dose of 1 ml/kg of body weight; 15 days after the last injection, the animals are vaccinated by double administration of the inactivated combined vaccine Combovac for rednose, parainfluenza type 3, viral diarrhoea, respiratory syncytial, rota- and coronavirus diseases according to the instructions.

EFFECT: method provides higher postvaccinal immunity and the stimulated antibody production as a result of activating cell and humoral immunity and optimising the natural body resistance.

3 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to anaesthesiology and resuscitation, and can be used in intensive care patients suffering from ventilator-associated pneumonia, or where there is a high risk of development thereof. Stabilising haemodynamics is followed by 8 turns of a patient's body a day. The cycle is started from 08-00: 3 hours on his/her back, 2 hours on his/her side, 2 hours on the other side, 3 hours on his/her back, 6 hours on his/her stomach, 4 hours on his/her back, 2 hours on his/her side, 2 hours on his/her side. The patient's centre of gravity is changed every 2 hours with the patient lying on his/her stomach and back. Propofol is infused at 2-3 mg/kg/hour 20 minutes before the patient is turned on his/her stomach and continued until the patient's position is changed again. A nitroglycerin infusion is started 5 minutes after the patient is turned on his/her back in a dose of 0.5-1.0 mcg/kg/min and continues for 5 hours. An antibacterial preparation is intermittently or microfluid single administered 10 min after the patient is turned on the stomach; observing other rate of administration of the antibacterial preparation, one of the administrations is performed 10 minutes after the patient is turned on the stomach.

EFFECT: method provides effective treatment and/or preventing of ventilator-associated pneumonia by exposing to a gravity factor of regional non-uniform ventilation and pulmonary perfusion, and an excessive hypoxic vasoconstriction.

2 cl, 4 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: what is presented is using neuroleptic spiperone as an agent able to prevent developing disorders in pulmonary tissue caused by cytostatic bleomycin administered.

EFFECT: anti-inflammatory and antifibrotic action of spiperone is presented on simulated reversible and irreversible pulmonary fibrosis caused by bleomycin with reducing a degree of alveocyte desquamation and delaying pulmonary tissue destruction.

2 dwg, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to a novel derivative of N-acylanthranilic acid, represented by the following general formula 1, or to its pharmaceutically acceptable salt, in which R1, R2, R3, X1, X2, X3, X4 and A are determined in the invention formula.

EFFECT: invention relates to an inhibitor of collagen production, a medication for treating diseases, associated with the excessive production of collagen, containing N-acylanthranilic acid derivative Formula 1.

FIELD: medicine, pharmaceutics.

SUBSTANCE: claim describes a standard solid dosage form for oral administration which represents a mini-tablet having a core and an outer coating, wherein the core contains a therapeutically effective amount of aliskiren or its pharmaceutically acceptable salt, while the outer coating represents a film coating containing a taste masking material specified in polyacrylates, and/or a release modifying ingredient of the coating specified in cellulose derivatives and acryl copolymers, and a mixture thereof. The above mini-tablet has a size of 1 mm to 4 mm and contains aliskiren in an amount making 2 mg/tablet to 4 mg/tablet. The oral solid dosage form is preferentially applied in paediatrics.

EFFECT: according to the invention, the dosage form of aliskiren can be dosed and possesses a taste that makes it applicable for children, and maintains a biological availability at a level comparable to that of the available medicinal product for adults.

19 cl, 13 dwg, 5 tbl, 3 ex

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