The diuretic and antihypertensive agent

 

(57) Abstract:

The tool is used in diseases of the cardiovascular system. The product contains as an active ingredient indapamide, as the target auxiliary components - starch and/or modified starch and/or croscarmellose, milk sugar, Aerosil, talc, stearic acid or its salts, low molecular weight polyvinylpyrrolidone. A new tool with a specific combination of components provides optimal physico-chemical and technological properties of the dosage form and high bioavailability of drug substances. 5 C.p. f-crystals.

The invention relates to medicine, in particular to pharmaceutical drugs used in diseases of the cardiovascular system.

One of the famous drugs used in hypertension and chronic heart failure, is indapamide. This drug is disclosed in French patent 2003311, IPC And 61 To 27/00, publication 07.11.1969,

Known dosage form indapamide in the form of coated tablets containing 2.5 mg of the active component and the target auxiliary components (the Background is of indapamide in heavily exposed to moisture and temperature. Therefore, the selection of components, their quantitative composition and technical features of production of medicines containing as an active ingredient indapamide, acquire great importance.

The problem to which the invention is directed, is to obtain a diuretic and antihypertensive drugs, all relevant pharmacopoeial requirements, qualitative and quantitative composition which will provide a high manufacturability of the drug using available components while providing guaranteed raspadaemosti and rapid release of his drugs.

The problem is solved due to the fact that the diuretic and antihypertensive agent containing as an active ingredient indapamide and target accessories, according to the invention as target auxiliary components it contains starch and/or modified starch and/or croscarmellose, milk sugar, Aerosil, talc, stearic acid or its salts and low-molecular polyvinylpyrrolidone in the following ratio of components, wt.%:

indapamide - 1-10

starch, and is to - 0,5-3

stearic acid or its salt is 0.5 - 3

the low-molecular polyvinylpyrrolidone medical - 1-10

this granulate contains starch and/or modified starch and/or croscarmellose, milk sugar, Aerosil and low molecular weight polyvinylpyrrolidone, and apadravya mixture contains indapamide, talc and stearic acid or its salts.

The modified starch mixture contains sodium carboximetilkrahmal, and the number of modified starch and/or croscarmellose may be 1-20% of the raw starch.

The preferred form of diuretic and antihypertensive drugs is a pill or tablet, film coated liner.

In accordance with pharmacopoeial requirements solid dosage form must contain 0.0025 g indapamide.

Selection of components for said solid dosage form was carried out experimentally. It was found that the introduction of apadravya mixture of active substance - indapamide in combination with talc and stearic acid or its salt allows you to avoid the negative effects of moisture and temperature on indapamide. This allows the stability of the drug within the specified shelf life.

The diuretic and antihypertensive agent get on the next technology. In the mixer load sifted powder sugar milk, potato starch and Aerosil, thoroughly stirred for 10-15 min, moistened with a solution of polyvinylpyrrolidone again stirred until a uniform distribution of moisture and granularit.

The granules are dried at a temperature of from 55 to 60oWith a lack of cachemate granules. Dry granules grind, optivault the Indapamid, talc and magnesium stearinovokisly, then stirred to obtain a homogeneous mass. The resulting mixture tabletirujut. Tablets-engine cover film cover.

As example can be mentioned the following composition per tablet Indapamide 0,00250 g, coated:

Name components: Content, g

indapamide - 0,00250

starch and/or modified starch and/or crosscarmellose - 0,01800

milk sugar - 0,09010

Aerosil - 0,00300

talc - 0,00120

magnesium stearinovokisly - 0,00120

the low-molecular polyvinylpyrrolidone medical - 0,00400

The weight of the uncoated tablets 0,12000,

Shell components, g:

methylcellulose - 0,00150

tween-80 - 0,00075 the second composition, with the stated ratio of the components, ensures optimal physico-chemical and technological properties of the dosage form and high bioavailability of the drug.

Received the diuretic and antihypertensive agent used in mild and moderate arterial hypertension, edema in heart failure and nephrotic syndrome.

1. The diuretic and antihypertensive agent containing as an active ingredient indapamide, and the target auxiliary components, wherein the target auxiliary components it contains starch and/or modified starch and/or croscarmellose, milk sugar, Aerosil, talc, stearic acid or its salts and low-molecular polyvinylpyrrolidone in the following ratio, wt. %:

Indapamide - 1-10

Starch and/or modified starch and/or croscarmellose - 5-30

Milk sugar - 30-80

Aerosil - 0,1-3

Talc - 0,5-3

Stearic acid or its salt is 0.5 - 3

The low-molecular polyvinylpyrrolidone medical - 1-10

this granulate contains starch and/or modified starch and/or croscarmellose, milk sugar, aerocity or a salt thereof.

2. The diuretic and antihypertensive agent under item 1, characterized in that it contains as modified starch natrocarbonatite.

3. The diuretic and antihypertensive agent under item 1, characterized in that the amount of modified starch and/or croscarmellose is 1-20% of the raw starch.

4. Diuretic and anti-hypertensive agent for PP.1, 2 or 3, characterized in that it is made in the form of tablets.

5. The diuretic and antihypertensive agent under item 4, characterized in that the tablet is covered with a film cover.

6. The diuretic and antihypertensive agent according to any one of paragraphs.1-5, characterized in that it contains 0.0025 g indapamide.

 

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