CS204670B1 - Preparation for decreasing the acidity of the stomach contens and method of preparation thereof - Google Patents

Description

The invention relates to a composition and a process for the preparation of a new medicament for reducing the acidity of gastric contents. The composition is gel-like and contains aluminum phosphate with a colloidal gel of natural or synthetic origin. It can be ingested without danger and is of good taste.

For example, in German Patent Specification No. 2 201752 (a stable gel based on aluminum phosphate and a process for its preparation) it is stated (p. 4) that 750 l of water must be heated to 100 ° C to prepare 2.25 tons of Agar-agar gel , add Agar-agar and allow to stir for 30 minutes with stirring. An additional amount of water (700 L) is required. Heat to 65 ° C, add pectin and stir for 15 minutes. The apparatus is then rinsed with 50 liters of hot water, which is added to the two previous amounts of Agar-agar and pectin water in a single vessel. Calcium sulfate was added and stirred for 15 minutes. The entire amount is then cooled to ambient temperature using a cooling device. The whole preparation of the Agar-agar gel takes place in two facilities. A third apparatus is used to prepare the final gel formed by mixing the Agar-agar gel and the aluminum phosphate gel.

All the other six examples in the patent refer to the preparation described in example no. First

The whole preparation process is technologically and energy intensive. Relatively large amounts of water should be heated up to 100 ° C and then cooled. Also, a greater number of devices (three) increase the risk of microbial contamination of the formulation. In the preparation of an agar-agar gel, it is necessary (according to the description to mix the solution using a turbine. Even the actual selection of the agar is not satisfactory because the substance is very susceptible to bacteria and fungi). Properties (Idson, B., Bechynsky, MO: Naturel raw materials in semi-solid dosage forms. Drug Cosmet. Ind., 122, 38-46,153-155 (1978). Agar is highly sensitive to electrolytes and organic solvents with water and Maximum swelling at pH 8-9, which values are not achieved with antacid preparations of this type (Bulletin G-10 "Agar" Fy. Meer Corporation, USA).

The above-mentioned drawbacks are eliminated in that the colloidal protective effect is achieved by combining the natural pectin substance and the substance obtained by industrial microbial fermentation of glucose-xanthan polymer in an amount of 0.05 to 1 wt. %. The decrease in acidity of the gastric content is achieved by aluminum phosphate, which reacts with the gastric acid to partially dissolve and stops its action when it reaches a pH of 3 in the stomach. it therefore does not cause gastric juice alkalinity.

The microbial safety of the formulation is provided by substances such as, methyl p-hydroxybenzoic acid, propyl p-hydroxybenzoic acid, benzoic acid and its salts and sorbic acid and its salts. The taste is corrected by sweeteners such as sorbitol, saccharin, sucrose and flavoring agents such as vanilla, orange and peppermint essences. The appearance is also color-coded, for example, a lively color. The consistency modifiers are methylcellulose, carboxymethylcellulose, acacia and carboxyvinyl polymer.

In a suitable homogenizer equipped with a planetary stirrer and a colloid mill, aluminum phosphate is homogenized with microbial safety adjuvants and water. A dispersion or gel of pectin, xanthan, consistency modifiers and other excipients is prepared in a separate container. The resulting dispersion or gel is slowly poured into the homogenizer while the machine is running slowly or at rest, but in portions. The entire contents are perfectly homogenized, the other ingredients are added and homogenized again. All oiperations take place: for ^; ambient temperature.

From the technological point of view, the fact that xanthan polymer can be processed in the whole temperature range from 0´C to 100 ° C is significant. Because it is an antacid preparation and the fact that the xanthanum polymer solution is stable to the effects of pH in the range of 0.5 pH to 12.5 pH a. both chemical and physico-chemical. The rheological properties of the xanthan polymer solution allow it to be pumped, even at high viscosity.

In the following, the invention is illustrated by means of four examples, without being limited thereto.

Example # 1

Aluminum phosphate 7 to 8% by weight

Pectin 2% by weight

Xanthan polymer max. up to 1% by weight

Methylcellulose 2% by weight

Propylene glycol. 5% by weight

Sucrose 27% by weight

Benzoic acid 0,2% w / w

Orange essence 0.2% by weight

Water up to 100% by weight

Example # 1- Preparation method

An aluminum phosphate, sucrose and water are charged into a homogenizer equipped with a planetary stirrer and a colloid mill. The contents are thermogenised using a collagen mill. In a separate vessel, benzoic acid and benzoic acid are dissolved in the propylene glycol, and pectin, methylcellulose and xanthan polymer are included in this solution. The resulting dispersion is slowly poured into the homogenizer, either under slow agitation or at rest, but in portions. The contents thoroughly effilý zhomogenfehje ¹ through a colloid mill ,, In asymptomatic pomarahdtová- the flavor and homogenized again? All operations are carried out at room temperature.

Example # 2

phosphate aluminum 7 to 8% of the hibernation pectin 2% and xanthan polymer max. 1% at Carboxyvinylpolymer 0,15% when Sodium benzoate = 0,04% (( saccharin 0,04% (( sucrose 12% at glycerin 4% at essence peppermint. 0.2% at Water up to 100% at

Example; no. 2 '- Method of preparation

Aluminum phosphate, behzoan sodium, saccharin, sucrose and water are charged into a homogenizer equipped with a planetary stirrer and a colloid mill. Contents ¹ were well homogenized using a colloidal ¹ mill. In a more particular container: a dispersion is prepared in glycerine; of pectin. carboxy vinyl polymer and xanthanum. The resulting ¹ dispersion is slowly poured; a homogenizer; either while the machine is running slowly or at rest but after a while. Then, the entire content is perfectly homogenized through. colloid mill, the essence of peppermint is added and is again homogenized. All operations are carried out at room temperature.

Example # 3

phosphate

aluminum 7 to 8% by weight pectin 2% (( xanthan polymer max. 1% « Arabic gum 6% (( sucrose 27% at Potassium sorbate 0.2% « Rye dye 0.1% U Mandarin essence 0,2% « Water to 100% (s

Example # 3 - Method of preparation

An aluminum phosphate, sucrose, dye and half the total amount of water are charged into a homogenizer equipped with a planetary stirrer and a colloid mill. The contents are well homogenized using a colloid mill. In a separate container, pectin, gum arabic and xanthan polymer are swollen in the other half of the water. After swelling, add the contents of the container to the homogenizer in the machine but in portions. The entire contents are perfectly homogenized via colloidal ml-yn. Finally, add the mandarin essence and potassium sorbate. Homogenize again. All operations take place ₄ at room temperature.

Example # 4 Aluminum phosphate 7 to 8% by weight

Pékfín 2%

Xanthan polymer max. 1% "

P-hydroxybenzoic acid methyl ester 0,08% '

P-hydroxybenzoic acid propyl ester 0,02% '

Potassium sorbate 0,2% '

Sorbitol 36%

Ethyl alcohol 3%

Vanilla aroma 0,1% '

Dye 0,1% '.

Water up to 100%

Example # 4 - Method of preparation

An aluminum phosphate, sorbitol and 2/3 of the total amount of water are charged into a homogenizer equipped with a planetary stirrer and a colloid mill. The contents are well homogenized using a colloid mill. In a separate vessel, dissolve p-hydroxybenzoic acid methyl ester and propyl ester in ethyl alcohol and then disperse pectin, xanthan polymer and colorant in this solution. Add enough water to the dispersions to form a gel. The resulting gel is added to the homogenizer and the whole content is perfectly homogenized. Add the aroma and make up the rest of the water to a total of 100% by weight. This gives a gel-like suspension of good chemical, physicochemical, microbial stability and pleasant taste correction.

Xanthan polymer (Xanthan gum, Xanthan Gummi). It is characterized in "Food Chemicals Codex", 2nd Ed. 1972, National Academy of Sciences, Washington, D. C., p. 856. It is essentially a natural polysaccharide with a high molecular weight of 2,000,000, but also 13,000,000 to 50,000,000 (Dintzíis, FF Babcock, GE, and Tobin R., 1970. Carbohyd. Res. 13: 257 -67).

It is produced by fermenting glucose in a suitable medium with Xanthomonas campestrls (Jeans, A.R., Pittsley, J.E., and Senti, F.R. 1961. J. Appl. Polymer. Sci. 5: 519-526). Its molecule consists of three different monosaccharides - mariose, glucose and glucuronic acid (Sloneker, J. H., and Jeanes, A. R. 1962. Can. J. Chem. 40: 2066-71).

It is characterized by:

Excellent chemical stability in solutions, excellent Theological properties - extreme pseudoplastioitosis, ie the low viscosity of the stirrer or the calm, the viscosity of the solution is high and the rapid viscosity is low (Řees, DA 1973. Biophysical Society Winter Meeting, London) , England), (Rees, D.A. 1972. Biocharn. J. 126: 257-273], viscosity independent of temperature up to 100 ° C, even in the presence of electrolytes, viscosity independent of pH, possible directly dissolve the xanthanum polymer in a 10% hydrochloric acid solution and also resists without damage the potassium hydroxide solution up to a concentration of 20%, it is soluble in hot and cold water, the solution is frost-stable, even at low concentrations of xanthanum polymer reaches a high solution viscosity.

The acid-reducing substance in the stomach by direct reaction with the hydrochloric acid present in the gastric juice - aluminum phosphate complies with the requirements of the article "Aluminum phosphate gel", British Pharmacopoea 1973, London, England.

The pectin used in our preparation as a colloidal protection agent for the gastrointestinal walls and, in particular, normalizing the intestinal passage, complies with the specifications in "Food Chemicals Codax", 2nd Ed. 1972, National Academy of Sciences, Washington, DC, and in FAO / WHO: Specifications for Identity and Purity of Food Additives-Part I. Thickening Agent, Stabilizers., Rome 1973. The composition of the present invention is primarily used to reduce gastric acidity. However, it is also used in other diseases associated with increased secretion of hydrochloric acid in the stomach such as gastritis, duodentitis, gastric dispepsia and gastric and duodenal ulcer. It can also be used in diseases of the esophagus, (in esophagitis in peptic ulcer, in pyrosis). it is also damaged by antituberculotics, corticosteroids, non-steroidal antirheumatics, cytostatics) and the antacid and colloidal protective effect of this preparation is also applied. it is secreted from the body by this preparation.

Claims (2)

OBJECT OF THE INVENTION A preparation for reducing the acidity of gastric contents having a colloidal protective effect on the gastric mucosa, comprising a combination of aluminum phosphate in an amount of 7 to 8% by weight, pectin in an amount of 0.5 to 2% by weight, microbial safety agents in an amount of 0, 02 to 0.2% by weight, in particular methyl ester of p-hydroxybenzoic acid, propyl ester of p-hydroxybenzoic acid, benzoic acid and its salts, sorbic acid and its salts, flavoring agents in an amount of 0.04 to 36% by weight, in particular sorbitol, saccharin, sucrose, aromatic substances in an amount of 0.1 to 0.2% by weight, the lowest essence of vanilla, orange, peppermint, appearance modifying agents in an amount of 0.01 to 1% by weight, the lowest colorant, consistency adjusters in an amount of 0 15 to 6% by weight, in particular methylcellulose, carboxymethylcellulose, acacia, carboxyvinyl polymer and water, characterized by: The composition of claim 1, wherein said xanthan polymer comprises from about 0.05% to about 1% by weight. 2. A method according to claim 1, characterized in that the aluminum phosphate is homogeneous with microbial safety agents and water, then a dispersion or gel containing pectin, xanthan polymer, consistency modifiers and other excipients and water formed are separately prepared. the dispersion or gel is added to the aforementioned homogeneous mixture and homogenized together until a gel is formed which is re-homogenized after taste adjustment.