The invention relates to the use of the disaccharide derivatives 3'-aminosucrose, sucrose-C6-acid and palatinose-C6'-acid and/or of an amide or alkyl ester thereof for the prevention or treatment of hyperglycemias.

DESCRIPTION OF THE INVENTION

The invention relates to drug compositions and food compositions for treating hyperglycemias in the human or animal body and process for inhibiting .alpha.-glucosidases.

The breakdown of carbohydrates in the human or animal body requires the presence of .alpha.-glucosidases, in particular sucrases and maltases. Inhibitors of these two enzymes prove to be advantageous, in particular if an increase in the blood sugar level after meals is to be prevented. EP 0 560 284 A1 discloses .alpha.-glucosidase inhibitors which do not have harmful effects on the patient and in addition are taken by the patient only to a small extent. This publication discloses the use of various pentoses and hexoses such as L-arabinose, L-fucose, L-xylose, D-ribose etc. to inhibit the .alpha.-glucosidase activity in a homogenate comprising maltase and sucrase.

GB 2 011 397 A1 discloses that sugars produced by Streptomyces (Actinomyces A 2396) show a glycosidase-inhibiting action. The sugars disclosed in GB 2 011 397 A1 are oligomeric compounds which are at least trisaccharides.

The technical problem underlying the present invention is to provide a drug composition or food composition comprising an inhibitor for the enzyme activity of sucrase and maltase enzyme activities with simultaneously high physical tolerance.

The technical problem underlying the present invention is solved by providing a drug composition or food composition which comprises disaccharide derivatives, in particular oxidized disaccharides or their derivatives such as amides or alkyl esters of the oxidized disaccharides or amino derivatives of disaccharides and if appropriate a pharmaceutically acceptable excipient. In a particularly preferred embodiment of the invention, the oxidized disaccharide derivatives provided according to the invention are methyl and ethyl esters of the oxidized disaccharide. In a further preferred embodiment, the oxidized disaccharide derivatives provided according to the invention are their amides having the general structure R'--CO--NHR, where R'--CO is the oxidized disaccharide and R=H or R=C.sub.nH.sub.(2n+1) where n=0 5. In particular, the technical problem is solved by such a drug composition or food composition which comprises a monocarboxylic acid of sucrose, in particular the C6'-sucrose monocarboxylic acid, called sucrose-C6-acid hereinafter, and/or an oxidized palatinose (isomaltulose), in particular the palatinose-C6'-acid. The problem is also solved by a food composition or drug composition which in a preferred embodiment comprises an amino sucrose, in particular 3'-aminosucrose.

It has surprisingly been found that the enzyme activities of sucrase and maltase were particularly strongly inhibited by the above-mentioned disaccharide derivatives to be used according to the invention, in particular 3'-aminosucrose, and the oxidized disaccharides or their above-mentioned alkyl esters or amides, in particular the sucrose-C6-acid and the palatinose-C6'-acid. The compounds used according to the invention are therefore suitable for reducing the blood sugar level and accordingly for the prevention and treatment of hyperglycemias.

The invention also relates to a drug composition comprising as active constituent the above-mentioned disaccharide derivatives to be used according to the invention, in particular 3'-aminosucrose, and/or oxidized disaccharides or their above-mentioned alkyl esters or amides, in particular sucrose-C6-acid and/or palatinose-C6'-acid, and a pharmaceutically acceptable excipient or additives for reducing an increased blood sugar level or for the treatment and prevention of hyperglycemias of the animal and human body. The drug composition according to the invention can accordingly be used not only prophylactically but also therapeutically.

The invention also relates to a food composition or what is termed a "functional food", comprising the disaccharide derivatives used according to the invention and if appropriate food-compatible additives which can be used, for example, for the prevention or accompanying treatment of increased blood sugar level and hyperglycemias.

The above-described disaccharide derivatives used according to the invention have the advantage that they have a strongly inhibiting action on the sucrase and maltase activities. In particular, the disaccharide derivatives used according to the invention are therefore suitable for preparing a drug and/or food for the prevention or treatment of hyperglycemias.

The invention also relates to the use of the above-described disaccharide derivatives used according to the invention for preparing the above-mentioned compositions.

Pharmaceutically acceptable and/or food-acceptable excipients or additives which can be used in combination with the disaccharide derivatives used according to the invention are, for example, binders, preservatives, stabilizers, release agents and lubricants, sweeteners, colorings and flavorings or the like.

The compositions of the invention can be present as tablets, powders, pills, compressed preparations or solutions and can be administered, for example, orally or intraperitoneally. The dosage is preferably from 0.2 to 90% by weight.

In food compositions of the invention it is preferably provided to use at least 0.2% by weight, preferably from 2 to 50% by weight (based on the total weight of carbohydrates present in the food) of the inventive disaccharide derivatives.

The invention therefore also relates to a process for inhibiting .alpha.-glucosidases, in particular maltase and sucrase activities, in which the disaccharide derivatives to be used according to the invention, in particular 3'-aminosucrose, the oxidized disaccharides or their alkyl esters or amides, in particular sucrose-C6-acid and/or palatinose-C6'-acid are added to an aqueous solution comprising the glucoamylase/maltase enzyme complex and/or the sucrase/isomaltase enzyme complex and an effective inhibition of the sucrase activity and/or maltases activity is achieved.
 

Claim 1 of 8 Claims

1. A drug composition comprising an active ingredient and a carrier in which said active ingredient is an amide or alkyl ester of an oxidized disaccharide and wherein the oxidized disaccharide is selected from the group consisting of monocarboxylic acids of sucrose and oxidized palatinose.

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