Drug antibacterial action and method thereof

 

(57) Abstract:

The invention relates to the field of medicine and is suitable for treatment of respiratory tract infections, upper respiratory tract, skin and soft tissues. The drug is placed in a capsule and is made in the form of granules. The product contains, by weight. %: azithromycin of 83.4-97, as the target additives, microcrystalline cellulose 1,5-5,0, polyvinylpyrrolidone 3,0-9,0 and calcium stearic acid 0.2 to 1.0. The method of obtaining the drug is carried out by granulation with subsequent kapsulirovaniem granules. Antibacterial drug meets formalparam requirements, provides raspadaemost granules and rapid release of the active substance of azithromycin, as well as maintaining its high activity in the body. 2 S. p. f-crystals.

The invention relates to the pharmaceutical industry, in particular to medicines antibacterial action in the form of capsules containing azithromycin, to treat infections of: respiratory tract, ENT, skin and soft tissues, etc. and to a method of its manufacture.

Azithromycin belongs to the category of "new" macrolide - azalides, a semisynthetic derivative of erythromycin group, otlicials is as antibiotics (see Belousov Y. B. and other Clinical pharmacology and pharmacotherapy. M: Universe publishing, 1997, S. 319-320). Azithromycin was opened independently Brigt, U.S. patent 4474768, and Kobrehel and others, U.S. patent 4517359. In these patents described that azithromycin and some of its derivatives have antimicrobial properties and, accordingly, can be used as antibiotics.

Known dosage form with the contents of this antibiotic on the patent of the Russian Federation 2128998, IPC 6 And 61 To 31/73, publ. 20.04.99 made in the form of tablets, suspensions and powders for suspension.

Well-known medication in the form of a capsule containing azithromycin and pharmaceutically acceptable additives target, made in the form of granules, the patent of the Russian Federation 2130311, IPC 6 And 61 To 31/71, publ. 20.01.99.

This drug is the product of prolonged action. Granules are polymer coatings with controlled permeability for azithromycin in a quantity sufficient to create the desired speed or the nature of the controlled or sustained release up to 6 hours or more in weight of azithromycin from 2-7, the Dosage form may be a capsule containing a dose at one time.

As protodermis as active substances azithromycin in powder form. The pathological process in the body dosage form affects the whole set of properties, not just the active substance. However, information about pharmaceutical composition in the patent and scientific literature is not found.

A method of obtaining a medicinal product, made in the pellets placed in the capsule containing the active substance and additives target (see Ivanov, L. A. Technology of medicines, H. 2, S. 7-25; chief 11). The method comprises mixing the active substance with a filler, the mixing of the powder and the binding agent, wet granulation, drying, dry granulation, the powder granules moving substance and encapsulation.

The present invention is to develop a drug antibacterial action, which corresponds to the pharmacopoeial requirements, rapidly releases the active ingredient azithromycin, and retains its high activity, and how to obtain it.

The problem is solved so that the drug is antibacterial action, placed in a capsule and containing azithromycin and targeted supplements, according to the invention is made in the form of gralli stearic acid in the following ratio of ingredients, wt.%: azithromycin by 83.4-97,0 (preferably 90,2); microcrystalline cellulose 1,5-5,0 (preferably 3,2); polyvinylpyrrolidone 3,0-9,0 (preferably 5,6); calcium stearic acid 0.2 to 1.0 (preferably of 1.0).

The proposed ratio of the active substance and the target additives found experimentally and is optimal, providing a quick release, accuracy of dosage, dissolution, raspadaemost granules, satisfying other pharmacopoeial requirements.

Joint use of a drug in the form of water soluble polyvinylpyrrolidone in the ratio provides a quick release of azithromycin from the pellet into solution. When it is dissolved in 45 minutes on Wednesday dissolution goes 95-100% of the azithromycin. Use as an anti-friction substance calcium stearic acid in the specified proportions allows to achieve a good yield of the pellets provides a uniform mechanical and physical properties in the amount of dosage forms and contributes to the normal process of encapsulation.

The hard gelatine capsule must comply with the requirements of these technical conditions TU RB 03278351.006-97.

Conducted patent studies have not found a similar technical solutions that allows to draw a conclusion about the novelty and inventive step, because this decision is not clear from the current level of technology.

The domestic industry has all the resources (materials, equipment) required to obtain the proposed drug and its use to treat a number of infections.

The essence of the proposed technical solution is illustrated by description of a specific implementation of a medicinal product and method of its production.

We offer drug antibacterial action., placed in the capsule and containing azithromycin and targeted supplements, made in the form of granules, at the same time as the target additives applied polyvinylpyrrolidone, microcrystalline cellulose, calcium stearic acid in the following ratio of ingredients, wt.%: azithromycin by 83.4-97,0 (preferably 90,2); polyvinylpyrrolidone 3,0-9,0 (preferably 5,6); microcrystalline cellulose 1,0-5,0 (preference is radiated on the chemical-pharmaceutical plant: vibrating screens, mixers, granulators vane-type sieves for wiping wet mass, dry granulating mixers for drying and dusting, automatic capsule filling machine, packaging machine.

The method of obtaining the proposed drug product includes the operations used in pharmacology: sifting components, mixing azithromycin with microcrystalline cellulose, preparation of the humidifier, humidification of the mixed mass humidifier, wet granulation, drying of the granulate, dry granulation, the introduction of the moving substance for dusting granules, analysis of granules, encapsulation dosed granules into hard capsules.

When this operation is performed as follows.

1. Sifting ingredients: polyvinylpyrrolidone, calcium, stearic acid and microcrystalline cellulose sift through a sieve.

2. Mixing ingredients: azithromycin mixed with microcrystalline cellulose in a mixer in the following ratio, wt.%: azithromycin by 83.4-97,0; microcrystalline cellulose of 1.5 to 5.0. The mixture is stirred for 20-30 min until a homogeneous mass.

3. Preparation humidifier - 13% aqueous solution of polyvinylpyrrolidone. Use the second hydration and to obtain a homogenous mass by pushing through a sieve. The increase in the concentration of the humidifier leads to hardening of the granules, and thus deterioration of "dissolution".

4. Hydration of mixed ingredients in a moisturizer.

5. The wet granulation through a sieve with the hole diameter of 2.0 mm

6. Drying of the granulate for 40-45o.

The optimum residual moisture content of the pellets after drying is 5%. Higher humidity causes adhesion of granules, deteriorating the fluidity of the mass.

7. The dry granulation through a sieve with a diameter of 1.0 m

8. Introduction calcium stearic acid 0.2 to 1.0 wt.% for dusting granules in the mixer.

In the analysis of granular control over specific average mass, uniformity of dosage dissolution.

9. The encapsulation. Gelatin capsules filled with the obtained pellet machine for filling capsules. The contents of the capsule - 0,311 g, the weight of the capsule content is 0.38,

Capsules with the drug are packaged in jars of yellow glass, contour or other packaging.

In the specific example of obtaining drug use: 902 g of azithromycin, 10 g of calcium stearic acid, 56 g of polyvinylpyrrolidone and 32 g of cellulose microcrystals tool. Dissolving granules capsules for 45 minutes is 95-100%.

Capsules have a good appearance and are easily ingested, can quickly swell and dissolve: guarantee at least 90% of active substance.

Released azithromycin is rapidly and completely absorbed from the gastrointestinal tract, widely distributed in organs and tissues, where it attains bactericidal concentrations (in tissues of the lung, bronchial secretion, sinuses and other).

1. Drug antibacterial action, placed in a capsule and containing azithromycin and target additives, characterized in that it is made in the form of granules, at the same time as the target additives applied polyvinylpyrrolidone, microcrystalline cellulose and calcium stearic acid in the following ratio of ingredients, wt. %: azithromycin - of 83.4-97, microcrystalline cellulose 1,5-5,0, polyvinylpyrrolidone 3,0-9,0, calcium, stearic acid 0.2 to 1.0.

2. A method of obtaining a drug described under item 1, which comprises mixing azithromycin with microcrystalline cellulose, wetting of the mass 13% aqueous solution of the polyvinylpyrrolidone, the moist, granulirovanie the

 

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