NL8701744A - N-ACETYLCYSTEINE-CONTAINING WATER-SOLUBLE PHARMACEUTICAL PREPARATION. - Google Patents

Description

VO 9230 N-acetylcysteine-containing water-soluble pharmaceutical preparation.

N-acetylcystelne (hereinafter referred to as NAC) is a drug which has several beneficial properties, including a mucolytic action.

In practical application as a mucolytic, NAC can be taken orally as an aqueous solution, which is obtained by dissolving a granulate or an effervescent tablet. However, the organoleptic properties of the drug can be subjectively perceived as unpleasant. It is therefore necessary to mitigate the typical taste of NAC when taken orally. In the medicines on the market, this is achieved by the addition of sucrose. However, the use of sucrose can have drawbacks, especially for diabetics. In addition, sucrose is a sugar-causing sugar.

It is therefore necessary, as an alternative to existing drugs, to be able to have new pharmaceutical NAC products, which can be taken orally, and also by persons for whom sucrose is harmful.

At first sight, it might seem an easily solved problem to replace sucrose in an NAC-containing drug with an artificial sweetener or a sugar substitute, which does not cause caries. However, the problems are numerous and difficult to solve. For example, it is necessary that the NAC and the sweetener chemically tolerate each other, that the sweetener or the sugar substitute has the ability to effectively soften the typical taste of the NAC, that the taste of the product is perceived as pleasant. and that the sweetener or sugar substitute is suitable for the preparation of the desired form of the drug and for the associated operations.

This problem is now solved by the invention, as can be seen from the following claims.

The object of the invention is a pharmaceutical, NAC-containing preparation in the form of a water-soluble granulate, which is composed as follows (in percent by weight): NAC 10-20 wt.% Aspartame 2-3 wt. % 35 sorbitol 67-78% by weight of flavoring substance 10% by weight 8701744% -2-, the sum of the parts by weight being 100%.

For better consumer acceptance of the drug, it may be required to add the corresponding colorant associated with this flavor when using an flavoring agent. For example, when peppermint flavor is used, the addition of a dye may appear suitable which gives the solution a green color. In such cases, the addition of a dye for pharmaceutical purposes in an amount of 0.5-1.0% by weight in the composition may be useful.

The preparation of the granulate, the subject of the present invention, is carried out in the usual pharmaceutical technical manner. The granulate can be packaged in appropriate papers containing, for example, 1, 1.5 or 2 g of the preparation. Preferably, each paper contains an amount of the preparation corresponding to 100, 150, 200 or 300 mg NAC.

The examples below for a granulate according to the invention relate to a single dose of 1 g: NAC 100 mg apartame 25 mg 20 sorbitol 775 mg lemon flavor 100 mg NAC 100 mg aspartame 25 mg sorbitol 774.2 mg 25 peppermint flavor 100 mg green food coloring 0.8 mg NAC 200 mg aspartame 25 mg sorbitol 675 mg 30 lemon flavor 100 mg NAC 200 mg aspartame 25 mg sorbitol 674.2 mg orange flavoring 100 mg 35 orange food coloring (or β-carotene) 0, 8 mg 8701744 -3- NAC 150 mg aspartame 30 mg sorbitol 720 mg citrus flavor 100 mg 5 The granules according to the invention are easily soluble in water and provide an aqueous NAC solution with a pleasant taste.

A number of examples are given below to further illustrate the invention without, however, limiting it.

EXAMPLE I

A granulate consisting of: NAC 10 kg aspartame 2.5 kg sorbitol 77.42 kg orange flavor 10 kg colorant E-110 0.08 kg is prepared in the following manner:

The powders, except for the colorant, are sieved on a 1.07 mm mesh sieve and mixed for 10 minutes.

The mixture is then granulated in a fluidized bed granulator with an aqueous dye solution. The granulate is then packaged in pressed paper-aluminum-polyethylene papers into individual doses of 1 g (NAC dose per package is 100 mg).

EXAMPLE II

As described in example I, but with a mixture consisting of: NAC 20 kg aspartame 2.5 kg sorbitol 67.42 kg 30 orange flavor 10 kg $ carotene 0.08 kg papers are made with a content of 1 g of the preparation (content of NAC = 200 mg).

870) 744 -4 r -4-

EXAMPLE III

In the manner mentioned in example I, but without adding a coloring agent, a granulate is prepared, consisting of: NAC 15 kg 5 aspartame 3 kg sorbitol 72 kg citrus flavor 10 kg

The granulate is packaged in pressed paper-aluminum-polyethylene papers into individual doses of 2 g (300 mg NAG per 10 individual dose) or alternatively in individual doses of 1 g (150 mg NAC per individual dose).

EXAMPLE IV

The preparation described in Example I can also be prepared by the following alternative method.

NAC, sorbitol and aspartame are sieved on a shaker screen with a mesh size of 1.08 mm and mixed. The mixture is placed in a granulator and granulated with an aqueous solution containing the dye E-110. The resulting granulate is dried in a dryer and granulated in a crank granulator equipped with a 1.0 mm sieve.

The flavoring substance is added to the granulate and the whole is mixed one more time until a homogeneous mixture is formed. The mixture is packaged in pressed paper-aluminum-polyethylene papers in individual doses of 1 g (100 mg NAC per individual dose).

EXAMPLE V

The preparation described in Example II can also be prepared by the following alternative method.

NAC, sorbtitol and aspartame are sieved on a shaker screen with a mesh size of 1.08 mm and mixed. The mixture is placed in a fluidized bed granulator and granulated with a water-alcohol solution (1: 1) containing β-carotene. The dried granulate is regulated with a 1.08 mm mesh sieve and mixed with the orange flavor. The mixture is then packaged in pressed paper-aluminum-polyethylene papers into individual doses of 1 g (200 mg 35 NAC per individual dose).

8701744

Claims (8)

Pharmaceutical preparation containing N-acetylcysteine, in the form of a water-soluble granulate and containing: N-acetylcysteine 10-20 wt.% Aspartame 2-3 wt. % 5 sorbitol 67-78 wt. % flavoring substance 10 wt. % where the sum of the parts by weight is 100%. Pharmaceutical preparation according to claim 1, characterized in that it additionally contains a dye 10 suitable for pharmaceutical purposes. Pharmaceutical preparation according to claim 1, containing per dose of 100, 150, 200 or 300 mg N-acetylcysteine. Pharmaceutical preparation according to claim 1 or 2, consisting of: N-acetylcystelne 10% by weight 15 aspartame 2.5% by weight sorbitol 77.5% by weight aroma substance 10% by weight Pharmaceutical preparation according to claim 1 or 2, consisting of: N-acetylcysteine 20 wt.% 20 aspartame 2.5 wt.% Sorbitol 67.5 wt.% Flavoring 10 wt.% Pharmaceutical preparation according to claim 1 or 2, consisting of: N-acetylcysteine 10 wt.% 25 aspartame 2.5 wt.% Sorbitol 77.42 wt.% Flavoring 10 wt. % dye 0.08 wt% Pharmaceutical preparation according to claim 1 or 2, consisting of: 30 N-acetylcysteine 20 wt% aspartame 2.5 wt% sorbitol 67.42 wt% flavoring 10 wt% dye 0.08 wt% 8701744 -6- * Pharmaceutical preparation according to claim 1 or 2, consisting of: N-acetylcysteine 15% by weight aspartame 3% by weight sorbitol 72% by weight 5 flavoring substance 10% by weight 8701744