CS254358B1 - Antitussive-expectorant - Google Patents

Abstract

Antitussive-expectorant preparation for use in human medicine, especially in pediatrics. The invention provides a composition of a preparation with antitussive and expectorant effects, which are achieved by combining butamirate citrate, licorice extract and guaifenesin using conventional pharmaceutical excipients.

Description

(54) Anti-tussive expectorant

Antitussive-expectorant preparation for use in human medicine, especially in pediatrics. The present invention solves the composition of an antitussive and expectorant-effect formulation obtained by combining citrate butyrate, liquorice extract and guaiphenesin using conventional pharmaceutical excipients.

The present invention relates to a novel antitussive composition having an expectorant action.

It is in the form of a solution to be used as drops. Dosing is provided by a drip insert.

Contains butyrate citrate, licorice extract, guaiphenesin and pharmaceutical excipients.

There is a large number of antitussive resp. expectorant formulations which state the composition and / or method of preparation and are well illuminated by the mechanism of action.

One of the antitussive agents used in current pharmacotherapy is the citrate-butyrate-based formulation, but exhibits little expectorant activity. For this reason, it is not suitable for some indications. First of all, it is a therapy of dry irritating, difficult to cough cough in viral infections of the upper and lower airways.

The aforementioned drawbacks and problems are overcome by the fact that the agents according to the invention work with substances strictly used in pharmacy and that they are based on their precisely defined properties, which makes it possible to predict with certainty the resulting effect of the preparation, this has been confirmed by extensive clinical testing.

The composition comprises a combination of citrate butyrate 0.05 to 0.5% by weight, guaiphenesin 1.0 to 10.0% by weight, liquorice extract 0.1 to 2% by weight. and substances providing stability by chemical, microbiological and acceptable taste correction.

The invention is further illustrated by two examples, without being limited thereto.

Example 1

Butyrate citrate 0.40 % wt Guaiphenesin 10.00 % wt Liquorice extract 0.30 % wt Aroma (alpine flowers) 0.20 % wt Polysorbate 80 0.10 % wt Alcohol 95% 30,00 % wt Water dest. 0 70 % wt Propylene glycol do 100,00 % wt

Example 1 - Preparation Method

Alcohol and propylene glycol are charged into the homogenizer at ordinary temperature, citrate butyrate, guaiphenesin and liquorice extract are added sequentially, followed by the addition of a preformed mixture of aroma, polysorbate and water. Everything is perfectly homogenized, filtered and filled.

Example 2

Butyrate citrate 0.20 % wt. Guaiphenesin 5.00 % wt. Emetine dihydrochloride 0.15 % wt. Liquorice extract 0.20 % wt. Aroma (cough drops) 0.25 % wt. Polysorbate 20 0.50 % wt. Alcohol 95% 15.00 % ňmot. Glycerine 20,00 % wt. Propylene glycol 20,00 % wt. Water dest. d® 100.00 % wt.

Example 2 - Preparation Method

The homogenizer is charged at ordinary temperature, with alcohol, glycerin, half the amount of water, propylene glycol and gradually added butyrate citrate, guaiphenesin, liquorice extract and emetine dihydrochloride. A pre-prepared mixture of flavor, polysorbate and the other half of water are then added. Everything is perfectly homogenized, filtered and filled.

Pharmacology of the preparation according to the invention

Acute toxicity tests were performed with favorable results. Prolonged administration of subacute toxicity was also performed followed by histological examination. This test also had a favorable result.

Clinical experience with the formulation of the invention

It has been tested in leading clinics in a total of 241 pediatric patients and 31 adults. As a comparative product, a one-component purely antitussive preparation was used containing citrate butyrate of the same active substance concentration. It was tested on 50% of patients defined by sex. The product was applied in the following diseases - acute nasopharyngitis, acute pharyngitis, acute laryngitis, acute bronchitis, acute bronchitis, lung and bronchitis, hyperreactivity in bronchitis and chronic bronchitis and other airway diseases.

Parameters were evaluated - cough frequency, cough intensity and expectoration. The focus of the evaluation of expectoration parameters was in the clinical trial in connection with the history.

Further, the viscosity of sputum was monitored and the results show that the composition according to the invention has a good secretomotor and mucokinetic effect, manifested by large and easy expectoration. Pulmonary ventilation was also positively influenced - the improvement of its basic parameters.

This is explained by the mucus cleansing of the bronchial tree and the bronchospasmolytic and activity-enhancing activity of the guaiacolglycerin ether substance. The main advantage and benefit should be considered excellent action in influenza, ie. For example, in the case of viral respiratory infections associated with dry cough, which after a short period of use is converted to a moist form by the preparation according to the invention, expectoration and good expectoration occur. The preparation was well tolerated by all patients. It did not show any side / side effects.

Claims (1)

SUBJECT OF THE INVENTION Antitussive-expectorant preparation in the form of a solution containing a combination of 0.05 to 0.5% by weight of citrate butyrate, liquorice extract 0.1 to 0.2% by weight, flavoring, propanediol, ethanol, solubilizer and water, characterized by % by weight of guaiphenesin in an amount of 1 to 10 wt.