CS217686B1 - Preparation for decreasing the acidity of the sparing contents - Google Patents

Abstract

invention the relates to cause of preparation solid Medicines forms with determination on the reduction aci Dita gastric juice. It the about combination dried colloidal phosphate aluminum with xanthan polysaccharide and you gave me after powerful substances. Stated Medicines form the prepares by straight tabletting with use of xanthan polysaccharide and than auxiliary substances.

Description

The invention relates to a composition and a process for the preparation of a novel formulation for reducing the acidity of gastric contents. The composition is in tablet form and comprises a dry aluminum phosphate gel with a polysaccharide that forms a colloidal gel in a fluid containing medium. It's easy to make.

German Patent 2 201 752 (Stable Aluminum Phosphate Gel and Process for its Preparation) states that to prepare 2.25 tons of Agar-agar gel, 7501 water must be heated to 100 ° C, Agar-agar added and allow to boil for 30 minutes with stirring. An additional amount of water (700 L) should be heated to 65 ° C, pectin added, mixed for 15 minutes and added to the previous mixture.

The apparatus is then rinsed with 50 liters of hot water and added to the previously prepared mixtures in one vessel. Then calcium sulfate is added and stirred for 15 minutes. Cool the entire amount to ambient temperature. Agar-agar gel preparation takes place in two plants. A third apparatus is used to prepare the final gel formed by mixing the agar-agar gel and the aluminum phosphate gel. Further examples in the patent refer to the preparation described above.

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 higher number of devices (three) increases the risk of microbial contamination of the product. To prepare an Agar-agar gel, it is necessary (as described) to mix the solution using a turbine. Even the actual choice of Agar-agar is not satisfactory because the substance is highly sensitive to bacteria and fungi. Another disadvantage is the considerable variation in batches in terms of color, viscosity and gel forming properties (Idson, B., Bechynsky, MO: Natural 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 mixed with water and swells at pH 8-9 below the antacid levels (Bulletin G-10 "Agar" by Fymeer Corp., USA).

I in MS. AO 204670 (A composition for reducing gastric acidity and a process for its preparation), which discloses achieving a colloidal protective effect by combining pectin and a substance obtained by industrial microbial fermentation of glucose-xanthan polysaccharide. The decrease in acidity of the gastric content is achieved by aluminum phosphate as a colloidal solution, which reacts with the gastric acid with partial dissolution and stops reaching the pH of 3 in the stomach.

The method of preparation of this preparation (according to AO 204670) is substantially technologically simpler and less energy-intensive than in the described patent specification NSR 2201752, but here too it is necessary to use at least 2 containers for homogenization and especially due to the high risk of microbial defect. a relatively large number of excipients should be used. Also, due to recontamination, this product should be packed in a single-dose container.

The object of the present invention removes part of the above-mentioned drawbacks in that the colloidal protective effect is achieved by xanthan polysaccharide in the dry state and the reduction of the acidity of the stomach contents is achieved by dried colloidal aluminum phosphate.

The method of preparation is as follows: After adjusting the particle size of the dried colloidal aluminum phosphate, xanthan polysaccharide and other excipients, all components are homogenized in a suitable homogenizer. The xanthan polysaccharide in a mixture with dried colloidal aluminum phosphate also helps the technological processing of the mixture with the substance! into a tablet form.

From the point of view of our invention, it is important that the xanthan polysaccharide can be processed in the dry state together with other substances, and that the hydrocolloid is only formed in contact with the liquid. For example, gastric juice. The fact that the solution xant. The polysaccharide is stable to the effects of pH in the range of pH 0.5 to 12.5 pH, both chemically and physically chemically, is of particular importance in the antacid preparation.

The microbial safety of the product can be ensured by the use of raw materials complying with the provisions of our Pharmacopoeia (CSL 3) and by maintaining common hygienic principles during production.

In the following, the invention is illustrated in three examples without being limited thereto.

Example # 1

Dried aluminum phosphate Xanthan polysaccharide Aminoacetic acid Talc

Calcium stearate Maize starch wt. 4 wt.

% wt. 2 wt.

0.5 wt. up to 100 wt.

Example # 1 - Method of preparation

The dried aluminum phosphate, xanthan polysaccharide, aminoacetic acid) talc, calcium stearate and corn starch are ground and sieved. They are perfectly homogenized in a homogenized machine. On a rotary tabletting machine with punches of 13 mm diameter, it is tabletted by direct tabletting using a forced filling device. The weight of one tablet is 550 mg.

Example # 2

Dried aluminum phosphate 65% wt.

Xanthan polysaccharide 4 wt.

2,6-diaminohexanecarboxylic acid 18 wt.

Talc 2% wt.

Aluminum stearate 0.5 wt.

Microcrystalline cellulose up to 100 wt.

Example # 2 - Preparation Method Aluminum phosphate, dried, xanthan polysaccharide, 2,6-diaminohexanecarboxylic acid, talc, aluminum stearate and microcrystalline cellulose are milled and sieved. In a homogenizer, they are perfectly homogenized. On a rotary tabletting machine with punches of 13 mm diameter, it is tabletted by direct tabletting using a forced filling device. The weight of one tablet is 550 mg.

Example # 3

Dried aluminum phosphate 65% wt.

Xanthan polysaccharide 4 wt.

Talc 2 wt.

Magnesium stearate 0.5 wt.

Silica, colloidal, up to 100% w / w

Example # 3 - Preparation Method Dried aluminum phosphate, xanthan polysaccharide, talc, magnesium stearate and colloidal silica are ground and sieved. In a homogenizer for dust homogenization, they are perfectly homogenized. On a rotary tabletting machine with punches of 13 mm diameter, it is tabletted by direct tabletting using a forced filling device. The weight of one tablet is 550 mg.

Xanthan polysaccharide (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 high molecular weight polysaccharide - 2,000,000, but also 13,000,000-5,000,000 (Dintzis, FF, Babcock, GE, and Tobin R., 1970. Carbohyd. Res. 13: 257-67) . It is produced by fermenting glucose in a suitable medium with Xanthomonas campestris (Jeanes, A.R., Pittsley, J.E., and Senti, F.R. 1961. J. Appl. Polymer. Sci. 5: 519-).

Claims (2)

A preparation for reducing the acidity of gastric contents having a colloidal protective effect on the gastric mucosa, comprising a combination of an aluminum phosphate powder in an amount of 1% by weight. 18 to 70% by weight, direct tabletting agents in an amount of 8 to 30% by weight, in particular aminoacetic acid, talc, stearic acid and its salts in an amount of 0.5 to 9% by weight, substances modifying the physical properties of the tablet in an amount of 5 526). Its molecule consists of three different monosaccharides - mannose, glucose, and glucuric acid (Sloneker, J.H., and Jeanes, A.R. 1962. Can. J. Chem. 40: 2066-71) · It is characterized by: - excellent chemical stability in solutions, - viscosity independent of temperature up to 100 ° C, even in the presence of an electrolyte in, - the viscosity is pH independent, it is possible to dissolve the xanthan polysaccharide directly in a 10% hydrochloric acid solution and withstand, without damage, a potassium hydroxide solution up to a concentration of 20%, soluble in hot and cold water, - the solution is frost-stable, - high viscosity of the solution is achieved even at low concentrations of xanthan polysaccharide. Dried colloidal aluminum phosphate - a substance that reduces gastric acidity by direct reaction with the hydrochloric acid present in the stomach, complies with the requirements of "Dried Aluminum Phosphate Gel", British Pharmacopoea 1973, London, England, t. j. the antacid capacity of our preparation is also in the range of 2.0 to 2.5. The composition according to our invention can be used primarily to reduce the acidity of the stomach contents, but also to other diseases associated with increased secretion of hydrochloric acid in the stomach such as gastritis, duodenitis, gastric dispepsia and gastric and duodenal ulcer. It could also be used in diseases of the esophagus (esophagitis), peptic ulcer, pyrosis. It is used in intestinal diseases - postoperative ulcer, enterocolitis, colitis, irritable colon, diverticulitis, sigmoitis, proctitis. In the case of injuries of medicinal origin (gastric and intestinal mucosa is damaged by antituberculotics, corticosteroids, non-steroidal anti-rheumatic drugs, cytostatics) the antacid and colloidal protective effect of this preparation is also applied. BACKGROUND OF THE INVENTION up to 10 percent by weight, in particular corn starch, microcrystalline cellulose, colloidal silica and, optionally, tablet buffer enhancers in an amount of 9 to 30 percent by weight, in particular aminoacetic acid in an amount of 5 to 18 percent by weight, characterized in that it contains xanthan polysaccharide in the dry state in an amount of 0.1 to 20 weight percent.