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Title:  Sodium ion absorption inhibitors, sodium ion excretion accelerators, and preventive and therapeutic agents for diseases resulting from excessive intake of common salt

United States Patent:  6,369,043

Inventors:  Sato; Takaya (Tokyo, JP); Uehara; Tutomu (Saitama, JP); Yamaoka; Ippei (Tokushima, JP); Asagi; Kozo (Tokushima, JP); Kobayashi; Masaru (Tokushima, JP); Kohri; Hideaki (Tokushima, JP)

Assignee:  Otsuka Pharmaceutical Factory, Inc. (Tokushima, JP)

Appl. No.:  582435

Filed:  June 26, 2000

PCT Filed:  December 24, 1998

PCT NO:  PCT/JP98/05873

371 Date:  June 26, 2000

102(e) Date:  June 26, 2000

PCT PUB.NO.:  WO99/33478

PCT PUB. Date:  July 8, 1999

Foreign Application Priority Data:  Dec 25, 1997[JP] (9-357609)


Abstract

An sodium ion absorption inhibitor, a sodium ion excretion accelerator and an agent for preventing and treating a disease caused by excessive common salt ingestion, each of which comprising a metal salt (excluding sodium salt) of lambda-carrageenan as an active ingredient, can excrete excessively ingested common salt outside the body positively and safely, and particularly have excellent action in excreting the sodium ions into feces.

BEST MODE FOR CARRYING OUT THE INVENTION

The lambda-carrageenan (.lambda.-carrageenan) for use in the present invention is a component contained in carrageenan which is broadly used as stabilizing agents, dispersing agents, and the like, such as gelling agents, cosmetics and the like.

Carrageenan is a sticky polysaccharide obtained from red algae, such as the genus Chondrus, the genus Gigartina, and the like (e.g., Chondrus crispus (Irish moss), Gigartina stellata, G. acicularis, G. pistillata and G. radula, which belong to the order Gigartinaceae, species of Fursellaria, Hypnea, Euchema, and the like), of which a component that precipitates in a gel form from a hot water extract with potassium chloride is kappa-carrageenan (.kappa.-carrageenan), and the unprecipitated supernatant fraction (a component which is soluble in a potassium chloride solution) is .lambda.-carrageenan.

.lambda.-Carrageenan does not contain a. 3,6-anhydro derivative found in the .kappa.-fraction, but is a galactan sulfate which is mainly constituted by a constituting monosaccharide D-galactose (D-Gal), particularly a galactan sulfate formed by the alternate bonding with .beta.-(1,4) and .alpha.-(1,3) bonds. .lambda.-Carrageenan is on the market and is easily available.

The above-described metal salt (but excluding sodium salt) of .lambda.-carrageenan is used in the present invention. Examples of the metal salt include all metal salts, such as alkali metal salts (but excluding sodium salt), alkaline earth metal salts and the like. Potassium salt, calcium salt, magnesium salt and iron salt are particularly preferred.

The above-described red algae is extracted, for example, using hot water of from 60 to 100oC., preferably from 80 to 90oC., for from 30 minutes to 3 hours, preferably about 1 hour, to obtain a hot water extract of carrageenan. The metal salt of .lambda.-carrageenan can be obtained by cooling the hot water extract, adding potassium chloride thereto, removing the thus formed precipitate, adding metal halide, such as calcium chloride or the like, to the resulting supernatant, stirring the mixture to completely dissolve the halide, removing low molecular weight substances by dialysis and then allowing the solution to stand for a predetermined period, generally from 2 hours to 24 hours. Alternatively, commercially available .lambda.-carrageenan may be used instead of the above-described hot water extract of carrageenan.

The thus obtained .lambda.-carrageenan metal salt may be used as such or optionally after further purification by alcohol precipitation, ion exchange resin chromatography, gel filtration chromatography and the like.

Desirable physical properties of the thus obtained .lambda.-carrageenan metal salt are as follows.

        (1)   Weight average molecular     50,000 to 1,000,000
              weight
        (2)   Neutral sugar content            58 to 91%
        (3)   Sulfur content                    4 to 15%
The .lambda.-carrageenan metal salt of the present invention has sodium ion absorption inhibiting ability, and, particularly when it is orally administered, it inhibits absorption of sodium ions in digestive tracts and accelerates their excretion.

Consequently, it is effective as a sodium ion absorption inhibitor and a sodium ion excretion accelerator, and can be contained in various foods and the like. Particularly, it can alleviate common salt restriction for patients suffering from various diseases caused by excessive common salt ingestion, such as hypertension, gastric cancer and stroke, so that it is useful as medicaments for preventing and treating such diseases. Also, since it excretes a large amount of sodium ions into feces, it is particularly useful for excreting sodium ions from patients having reduced renal functions, such as renal disease and the like.

The sodium ion absorption inhibitor, sodium ion excretion accelerator and medicament of the present invention which comprise the metal salt of .lambda.-carrageenan can be produced by processing the .lambda.-carrageenan metal salt obtained by the above-described method into various forms. Their examples include solids form materials, liquid form materials, emulsion form materials, paste form materials and the like.

The sodium ion absorption inhibitor and sodium ion excretion accelerator of the present invention can be applied to foods effectively. Examples of the foods containing these sodium ion absorption inhibitor and sodium ion excretion accelerator include any one of those which can be ingested immediately as such, are ingested after carrying out cooking and the like, and are premixed materials for use in food production. The solids form materials may be any of powder forms, granular forms and solid forms, and examples include various confectionery, such as biscuits, cookies, cakes, snacks, rice crackers, and the like, bread and powder drinks (powder coffee, cocoa, and the like) Examples of the liquid form, emulsion form and paste form materials include various drinks, such as juices, carbonated drinks, lactic acid drinks, and the like.

Examples of the medicament of the present invention include tablets, powders, granules, fine particles, solutions, and the like, and these preparations can be produced by making the hot water extract of the present invention and a pharmaceutically acceptable carrier into desired forms in the conventional way.

The metal salt of .lambda.-carrageenan of the present invention has an ability to excrete and absorb about 1 g of common salt (about 400 mg as sodium ions) based on about 10 g of the salt. Thus, using this ability as a standard, it is preferred to take it in an amount of approximately from 10 to 50 g calculated as the metal salt of .lambda.-carrageenan.

Claim 1 of 9 Claims

What is claimed is:

1. A sodium ion absorption inhibitor comprising a metal salt (excluding sodium salt) of lambda-carrageenan as an active ingredient.


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