RU2410088C2 - Syrup pharmaceutical composition and method for producing thereof - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to manufacturing drugs in the liquid dosage forms, namely in the syrup dosage form containing propylene glycol, sodium benzoate, sodium citrate, pentosesquihydrate, riboflavin, citric acid monohydrate, edible sorbite, aromatiser and purified water. An active substance can be presented with paracetamol exhibiting analgetic and antipyretic action, promoting elimination of such symptoms, as a moderate pain and high temperature, as well as ambroxol exhibiting expectorative and mucolytic action.

EFFECT: higher efficacy of the composition.

2 cl, 2 ex

Description

The invention relates to the pharmaceutical industry, in particular to medical preparations made in the form of liquid dosage forms, namely in the form of syrups.

As an active substance can be used with a painkiller and antipyretic effect, contributing to the elimination of symptoms such as moderate pain and fever, in particular paracetamol; as well as expectorant and mucolytic substances, namely ambroxol [1, 3].

A known composition (suspension) for symptomatic therapy in pediatric practice, containing paracetamol as an active substance, and sugar syrup, food sorbitol (70% solution), glycerin, gum, methyl parahydroxybenzoate, carmoisine E 122, purified water and flavoring as an auxiliary substance strawberry [2].

The disadvantage of this composition is the presence of sugar (in the form of sugar syrup), the presence of which in children's dosage forms is extremely undesirable, especially with regard to the use of sugar-containing drugs by children with diabetes.

Also, the disadvantage of this composition is a thick consistency, which can cause inconvenience in use, especially in children and in people with particularly sensitive emetic reflexes.

Known drug expectorant action "Halixol", which consists of Ambroxol hydrochloride, sodium trisubstituted citrate, sodium benzoate, sodium cyclomat, banana flavor, citric acid, polyvidone, food sorbite, distilled water, taken in therapeutic doses [3].

Close to the claimed composition is a pharmaceutical composition containing ambroxol as an active substance, and sodium benzoate, food sorbitol, propylene glycol, citric acid, sodium citrate, ethyl alcohol, flavoring agent, distilled water as an auxiliary substance [4].

The main disadvantage of this composition is the content of ethyl alcohol in it.

Closest to the claimed composition and the method for its preparation is a pharmaceutical composition for symptomatic therapy in children’s practice (syrup), containing paracetamol as an active substance, and sodium benzoate, sugar, food sorbitol, citric acid, trisodium citrate as an auxiliary substance, propylene glycol, ethyl alcohol, riboflavin, aromatic food essences, purified water (prototype) [5]. A method of obtaining the specified composition includes the preparation of raw materials - the preparation of sugar syrup. Food sorbitol is added to the resulting sugar syrup, then sodium benzoate, citric acid, trisodium citrate, riboflavin are successively dissolved. Then a solution of paracetamol in propylene glycol is added, ethyl alcohol and aromatic food essence are introduced. Mix to obtain a homogeneous syrupy mass and, if necessary, bring the volume of the syrup with water to 100 ml.

The main disadvantage of the prototype is paracetamol syrup (2.4%) of known composition is the ethyl alcohol content.

In accordance with the Order of the Federal Service for Supervision of Health and Social Development of 04.17.2006 No. 888-Pr / 06 "On the cancellation of state registration of alcohol-containing paracetamol drugs", due to the risk of irreversible liver damage in children and adults while taking paracetamol and ethanol, in order to improve the safety and effectiveness of treatment for citizens of the Russian Federation, the state registration of alcohol-containing paracetamol drugs, including and paracetamol syrup 2.4%.

The disadvantages of the prototype can also include the content of sugar in it.

The technical effect of the invention is the creation of an effective drug in the form of a syrup based on paracetamol or ambroxol, which has the necessary, including organoleptic properties for its use in pediatric practice, as well as for patients of other age groups.

The aim of this invention is to develop a composition and method for producing a liquid homogeneous dosage form in the form of a syrup without alcohol, sugar, which has antimicrobial stability.

This goal is achieved by the fact that ethyl alcohol and sugar are excluded from the previous composition of the dosage form, and optimal ratios of propylene glycol and other auxiliary substances are established that ensure that in the absence of alcohol ethyl homogeneous liquid dosage forms are obtained. Propylene glycol and sorbitol serve as thickeners for syrup, in addition, sorbitol acts as a sweetener. The introduction of an additional amount of saccharin and sorbitol corrected the bitter taste of paracetamol and ambroxol. The formulations developed have a pleasant smell and a sweet taste.

The proposed compositions of pharmaceutical compositions, the ranges of ratios of the ingredients used and the sequence of their dissolution are optimal, found experimentally and allow to obtain a high-quality and stable dosage form in the following ratio of components, g

Paracetamol 2.2-2.6 or ambroxol 0.25-0.35 Propylene glycol 15.0-35.0 Sorbitol 20.0-45.0 Riboflavin 0.00200-0.00275 Sodium Benzoate 0.4-0.1 Sodium Citrate Pentose Squigidrate 0.15-0.30 Citric Acid Monohydrate 0.05-0.1 Saccharin 0-0.2 Flavoring 0.05-0.2 Purified water up to 100 ml

A method for producing pharmaceutical compositions includes preparing purified water, preparing active and auxiliary substances, preparing a solution of sorbitol, introducing a solution of the active substance and riboflavin in propylene glycol, sequentially dissolving sodium benzoate, saccharin, sodium citrate pentosesesquhydrate, citric acid monohydrate, flavor and thoroughly mixing the resulting composition.

To illustrate, we give specific examples.

Example 1:

We dissolve 35 g of sorbitol in 45 ml of purified water, we introduce a solution of 2.4 g of paracetamol and 0.0025 g of riboflavin in 30 g of propylene glycol, then 0.5 g of sodium benzoate, 0.15 g of saccharin are successively added; 0.2 g of sodium citrate pentosesquihydrate; 0.07 g of citric acid monohydrate acid, 0.2 g of flavoring. Stir until a homogeneous syrupy mass is obtained, bring the volume of the syrup with water to 100 ml and mix thoroughly again.

Example 2:

We dissolve 40 g of sorbitol in 50 ml of purified water, introduce a solution of 0.002 g of riboflavin in 20 g of propylene glycol, then successively dissolve 1.0 g of sodium benzoate, 0.3 g of ambroxol with thorough stirring; 0.17 g of sodium citrate pentosesquihydrate; 0.075 g of citric acid monohydrate acid, 0.1 g of flavor. Stir until a homogeneous syrupy mass is obtained, bring the volume of the syrup with water to 100 ml and mix thoroughly again.

INFORMATION SOURCES

1. VFS 22 53 - 99 "Paracetamol syrup 2.4%."

2. Kalpol (suspension for oral administration for children). Register of medicines of Russia. Radar Encyclopedia of drugs. - 14th issue / Gl.red. G.L. Vyshkovsky. - M .: RLS-2006, 2005. - p. 1392 (620 p.), Www.rlsnet.ru, http://www.rlsnet.ru/opisdrug/PrepDescr.php3?prid=2292

3. Mashkovsky M.D. Medicines: Pharmacotherapy Manual for Doctors / MD Mashkovsky - M .: New Wave Publishing House LLC, 2000 - T 1-2. - 14th edition rev., Rev. and add. T.1, p. 161.

4. Patent No. 2169557 (RU), 2000.04.03. "Ambroxol Syrup for the treatment of bronchopulmonary diseases."

5. Patent No. 2206322 (RU), 2002.02.18. "A drug with analgesic and antipyretic effects."

Claims (2)

1. A pharmaceutical composition in the form of a syrup containing the active substance: paracetamol 2.2-2.6 g or ambroxol 0.25-0.35 g, as well as excipients: propylene glycol, sodium benzoate, sodium citrate pentosesesquigidrate, riboflavin, citric acid monohydrate, food sorbitol, flavor and purified water, characterized in that it does not contain ethyl alcohol and sugar and the homogeneity of the liquid dosage form is ensured by the required amount of propylene glycol, and sorbate is introduced to correct the bitter taste of the active substance t food and saccharin at
optimal ratios of components, g:
active substance:
paracetamol 2.2-2.6 ambroxol 0.25-0.35 propylene glycol 15.0-35.0 sorbitol 20.0-45.0 riboflavin 0.00200-0.00275 sodium benzoate 0.4-1.0 sodium citrate pentosesquihydrate 0.15-0.30 citric acid monohydrate 0.05-0.1 saccharin 0-0.2 flavor 0.05-0.2 purified water up to 100 ml 2. The method of obtaining the pharmaceutical composition according to claim 1, comprising obtaining purified water, preparing medicinal and auxiliary substances, characterized in that the solution of sorbitol is initially prepared, then a solution of the active substance and riboflavin in propylene glycol is introduced and sodium benzoate, saccharin are successively dissolved with thorough stirring. , sodium citrate pentosesquihydrate, citric acid monohydrate and flavor.