JPS6126968B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to an anti-ulcer agent, and more particularly to an anti-ulcer agent containing inositol hexasulfate sodium-aluminum salt as an active ingredient. Inositol hexasulfate is a known compound and is usually produced by dehydration condensation of inositol and sulfuric acid. Further, its salts can be produced by neutralizing the produced inositol hexasulfate with a basic substance. Examples of the salts that can be produced include sodium salts, potassium salts, ammonium salts, magnesium salts, calcium salts, aluminum salts, and sodium-aluminum salts, and the present invention relates to the sodium-aluminum salts thereof. be. As a result of conducting research on the pharmacological effects of the above-mentioned salts of inositol hexasulfate, the present inventors discovered that the above-mentioned salts have excellent anti-ulcer effect, antacid effect, and anti-pepsin effect, and completed the present invention. This is what I came to do. All of the above salts of inositol hexasulfate have excellent anti-ulcer effects. Inositol hexasulfate sodium-aluminum salt will be described below. Inositol hexasulfate sodium-aluminum salt is expressed by the following formula (1) (In the formula, R ¹ to ^{R 6} are Al(OH) ₂ or Na,
It cannot be all Al(OH) ₂ or Na. X is an integer from 6 to 12. ) is a compound represented by This compound is a white powder with no clear melting point. This compound is slightly soluble in water, but almost insoluble in organic solvents such as anhydrous ethanol and benzene. When this compound is dried under reduced pressure (1 mmHg) at 80°C for 4 hours, it loses crystal water and becomes anhydrous. In the infrared absorption spectrum, crystal water is present at 2.86μ.
Shows absorption of OH, CH ₉ at 6.13μ and OSO ₃ at 8.00μ. The measurement results of anti-ulcer effect, antacid effect, anti-pepsin effect, acute toxicity, etc. regarding this compound are shown below. (1) Anti-ulcer effect The anti-ulcer effect on various experimental gastric and duodenal ulcers was investigated according to conventional methods. The results are shown in Table 1.

[Table] (2) Effects on gastric acid secretion and pepsin activity Pylorus-ligated rats were prepared, gastric juice was collected 4 hours later, acid secretion was determined by neutralization titration method (0.05N sodium hydroxide solution), and pepsin activity was determined by neutralization titration method (0.05N sodium hydroxide solution). Measured using the Anson method. The results are shown in Table 2.

[Table] (3) Acute toxicity The acute toxicity of this compound was tested using mice and rats using conventional methods. The experimental results are shown in Table 3.

[Table] As is clear from the above experimental examples, this compound exhibits excellent anti-ulcer activity and is useful in the pharmaceutical field. The dosage of this compound when used for adult treatment varies depending on the dosage form or the number of administrations, but is preferably in the range of 500 to 3000 mg per day. The antiulcer agent of the present invention, like other gastrointestinal drugs, can be prepared as an oral drug in a conventional manner.
Appropriate forms for expected medicinal efficacy as a drug for the digestive system include tablets, capsules, granules, dry syrup, and internal liquid preparations, which can be arbitrarily selected and administered depending on the symptoms. When manufacturing tablets, which are often used as oral preparations, one or a combination of excipients used for oral preparations, such as lactose, starch, crystalline cellulose, calcium phosphate, and carboxymethylcellulose calcium, are added to inositol hexasulfate. Add 1 to 10 parts as needed to 10 parts of the ate salts, or add a binder such as gelatin polyvinylpyrrolidone, hydroxypropyl cellulose, etc. as a solution as necessary.
The mixture is granulated by a conventional method, a lubricant such as calcium stearate, talc, silicic anhydride, etc. is added, and tablets are manufactured using a tablet machine. The tablets can be coated with sugar or film by a conventional method. To produce granules, 1 to 10 parts of the above-mentioned excipients, sucrose, mannitol, etc., are added as necessary to 10 parts of the salts of inositol hexasulfate, and the above-mentioned binder is added. The solution is granulated and dried in a conventional manner to form granules. Prescription examples for tablets and granules are as follows: (1) One tablet: 280mg Nakamoto compound 250mg Corn starch 25〃 Hydroxypropylcellulose 2mg Calcium stearate 3〃 (2) Granule 1000mg Nakamoto compound 900mg Corn starch 50〃 Crystalline cellulose 40 [Hydroxypropyl cellulose 10] and the anti-ulcer agent of the present invention, which is manufactured for oral use, is suitable for use as a drug for the digestive system.
Although it is possible to mix it with other active ingredients, it can be blended in a sufficiently stable form. For example, stable mixtures can be prepared by blending with other gastrointestinal drugs, various acid-forming agents, dry aluminum hydroxide gel, magnesium aluminate metasilicate, magnesium silicate, etc.

Claims (1)

[Claims] 1. An antiulcer agent containing inositol hexasulfate sodium aluminum salt as an active ingredient.