NL193607C - Pharmaceutical preparation containing N-acetylcysteine. - Google Patents

Description

1 193607

Pharmaceutical preparation containing N-acetylcysteine

The present invention relates to a pharmaceutical preparation comprising 7-10 wt.% N-acetyl-cysteine, 80-86 wt.% Sucrose and optionally minor amounts of additives customary in pharmacy, which preparation is soluble in a pharmaceutical acceptably dissolute mistake to form a syrup.

Such a pharmaceutical preparation is known from British patent application 2,234,171. Example 3 mentions a granulate containing 2,226 mg sucrose and 200 mg N-acetylcysteine. The known preparation can be dissolved in a pharmaceutically acceptable solvent to form a syrup. The sucrose present is reported to mask the unpleasant taste of N-acetylcysteine.

A drawback of the known preparation is that the good taste of the preparation is lost during storage. The object of the present invention is therefore to provide a preparation containing N-acetylcysteine, which retains its pleasant taste even after storage.

Surprisingly, it has now been found that the stated aim is achieved by also including a specific amount of trisodium citrate in the composition. The invention is therefore characterized in that the preparation mentioned in the preamble also comprises 7-10% by weight of trisodium citrate and is in the form of a powder.

N-Acetylcysteine is a pharmaceutically active substance well known for its beneficial properties in mucilaginization. This substance advantageously liquefies secretions, especially in the case of respiratory diseases and cystic fibrosis. It is part of the group of substances called mucolytics or expectorants.

For its practical use as a mucolytic, the N-acetylcysteine can be taken orally in the form of an aqueous solution obtained by dissolving a granule or effervescent tablet or in the form of a tablet or capsule with water.

However, the organoleptic properties of this active are very unpleasant. To achieve these formulations to be administered orally, numerous studies have been required to mask this disgusting taste of N-acetylcysteine.

The oral recordings just mentioned above must either be taken with water and dissolved within the body or taken up immediately after dissolving. The present pharmaceutical preparation can be stored in a liquid state. It is an advantage that this preparation is stable for a long time in storage, at normal temperature and thereby retains a pleasant taste, since the unpleasant organoleptic properties of the active substance remain masked.

The recipe provided according to the invention is extemporane, that is, it relates to a powder, which at the chosen time must be dissolved in a pharmaceutically compatible solvent, preferably water, to prepare the syrup on its own .

The resulting syrup has a good taste which masks that of the N-acetylcysteine and retains this good taste for the duration of its use. It is stable under normal storage conditions for a time long enough for its use and does not need to be stored under refrigeration conditions.

The powder has the following composition: N-acetylcysteine 7-10% by weight

Trisodium Citrate 7-10 wt% 45 Sucrose 80-86 wt% and optionally minor amounts of additives commonly used in pharmacy.

At the time of use, this powder is dissolved with stirring and the syrup is ready for use.

The syrup can be in the form of unit dose ampoules having an amount of N-acetylcysteine between 100 and 600 mg, preferably between 100 and 200 mg, advantageously 200 mg.

It is advantageously present in the form of a unit volume syrup equal to several posological unit doses. It is then present in a bottle of, for example, 100, 150 or 250 ml of syrup after addition of the solvent. In these vials, the concentration of N-acetylcysteine 55 is such that each administration (e.g. of appropriate measuring cup or teaspoon) contains an amount of active substance from about 100 to about 200 mg, preferably from 100 to 200 mg.

Claims (2)

193607 2 Example I Syrup composition according to the invention. Component Amount of N-acetylcysteine 6.0 g 5. excess (5%) 0.3 g Sodium edetate 0.03 g Trisodium citrate 7.28 g Sodium methyl parahydroxybenzoate 0.18 g Flavor 0.21 g 10 Saccharose (ultrafine quality) 60 g 74 g The whole was made up to 150 ml by adding water. An excess of 5% N-acetylcysteine was added to compensate for the loss during the pot-life of the resulting solution. Example II Process for the preparation of syrup described in example 1. The components were sieved: 20 N-acetylcysteine 710 µm Sodium Edetate 125 µm Trisodium Citrate 315 µm Sodium Methyl Parahydroxybenzoate 125 µm Sucrose 710 µm 25 The appropriate weights of sodium edetate, sodium methyl parahydroxybenzoate, flavoring agent and 10% sucrose were then mixed at 70 rpm for 20 min. The other ingredients were added: trisodium citrate, N-acetylcysteine and 90% sucrose and mixing was continued for 30 min at 65 rpm. 74 g of the powdered mixture was poured into each vial. During the preparation, the relative humidity did not exceed 30%. After diluting the solution by adding water to obtain 150 ml, the pH of the resulting solution was 4.3 ± 0.5. 35 A pharmaceutical composition comprising 7-10 wt.% N-acetylcysteine, 80-86 wt.% Sucrose and optionally minor amounts of pharmaceutically customary additives, which preparation is soluble in a pharmaceutically acceptable solvent to form a syrup, characterized in that the preparation also comprises 7-10% by weight of trisodium citrate and is in the form of a powder. A pharmaceutical preparation which is in the form of a syrup obtained by dissolving a preparation according to claim 1 in said solvent.