Tablets containing a sweetening mixture

Details Tablets containing a sweetening mixture Tablets containing a sweetening mixture

1999-05-27

2001-05-01

Spear, James M. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

C424S439000, C424S440000, C424S441000, C424S465000, C514S777000, C514S778000, C514S781000

Reexamination Certificate

active

06224904

ABSTRACT:

DESCRIPTION
The present inventions relates to compressed formulations containing a sweetener mixture which comprises 1-O-&agr;-D-glucopyranosil-D-sorbitol. In particular, the invention relates to compressed formulations containing a sweetener mixture composed of 6-O-&agr;-D-glucopyranosil-D-sorbitol, 1-O-&agr;-D-glucopyranosil-D-sorbitol, and 1-O-&agr;-D-glucopyranosil-D-manitol and to the use of these sweetener mixtures in compressed formulations.
Compressed formulations are fancy foods, drugs or also foodstuffs consisting of compacted components. Compressed formulations therefore in general contain a carrier medium or diluting medium, binders, release agents or lubricating jellies, as well as the active ingredients such as flavourings, drugs or sweeteners. Sucrose, lactose, glucose, starch or mannitol are often used as the carrier medium or diluting medium. The use of these carrier or diluting media has the disadvantage that additional binders are required to ensure adequate compressibility.
EP-B1 0 028 905 describes the use of isomaltulose as a diluting medium in pills. But isomalulose has a conparatively low sweetness.
The industrial problem underlying the present invention is to provide compressed formulations which overcome the aforementioned shortcomings and which have particularly improved sweetness, solubility, and compressibility.
The solution of this industrial problem is based on the compressed formulations and containing 1-O-&agr;-D-glucopyranosil-D-sorbitol (abbreviated as 1,1-GPS in what follows), and particularly on compressed formulations containing a sweetener mixture formed by 6-O-&agr;-D-glucopyranosil-D-sorbitol (abbreviated as 1,6-GPS in what follows), 1-O-&agr;-D-glucopyranosil-D-sorbitol, and 1-O-&agr;-D-glucopyranosil-D-mannitol (abbreviated as 1,1-GPM in what follows). Because of their content of 1,1-GPS, particularly because of their content of the sweetener mixture composed of 1,6-GPS, 1,1-GPS, and 1,1-GPM, the compressed formulations of the invention therefore have improved solubility and sweetening power vis-a-vis conventional compressed formulations containing Isomalt® (equimolar mixture of 1,6-GPS and 1,1-GPM, hydrogenated isomaltulose). The compressed formulations according to the invention have the surprising advantage that they can be produced without using binders and that they have improved compressibility, i.e., for obtaining a certain hardness, a comparatively lower compacting pressure is required. Other advantages, associated with the improved compressibility of the inventive compressed formulations, result from their high hardness which is obtained with a comparatively low principal compacting pressure.
Other advantageous embodiments of the invention can be inferred from the dependent claims.
In a preferred embodiment, the invention relates to compressed formulations containing a sweetener mixture of 10 to 50% by weight of 1,6-GPS, 2 to 20% by weight of 1,1-GPS, and 30 to 70% by weight of 1,1-GPM, based on the weight of the sweetener mixture. In another particularly preferred embodiment, the invention relates to compressed formulations containing a sweetener mixture of 5 to 10% by weight of 1,6-GPS, 30 to 40% by weight of 1,1-GPS, and 45 to 60% by weight of 1,1-GPM, based on the weight of the sweetener mixture. Because of the increased 1,1-GPS and the reduced 1,1-GPM content, the latter sweetener mixture imparts to the compressed formulations a further improved sweetening power and solubility in aqueous solutions.
In a particularly preferred embodiment of the invention, the compressed formulations have 50 to 99% by weight of 1,1-GPS or of the sweetener mixture, based on the weight of the compressed formulations. The compressed formulations can contain, in addition, monosaccharides, disaccharides, monosaccharide alcohols, disaccharide alcohols, starch, derivatives of starch, cellulose, derivatives of cellulose, or inulin. The compressed formulations can contain, specifically, sorbitol, mannitol, hydrogenated or non-hydrogenated oligosaccharides, xylitol or sugars, such as sucrose, glucose, fructose or xylose. But these are advantageously present in amounts of less than 30% by weight, preferably less than 5% by weight, based on the weight of the compressed formulations. In a particularly advantageous embodiment, the compressed formulations according to the invention are free of sugar and therefore have a reduced calorific value and are suitable for diabetics.
In a particularly preferred embodiment of the invention, it is provided that the compressed formulations contain, in addition, intense sweeteners such as acesulfame-K, aspartame, cyclamate, glycyrrhizin, thaumatin, saccharin or similar substances. Advantageously, the inventive compressed formulations contain, in addition, flavourings and aromatics such as lemon flavour or peppermint flavour. The inventive compressed formulations can contain food-compatible acids such ascorbic acid or citric acid and, as lubricants, fatty acids or their salts such as magnesium stearate or sodium stearate. Finally, it can be provided that the inventive compressed formulations contain dyes and/or disintegrants such as bicarbonate or carboxymethyl cellulose.
A particularly preferred embodiment provides to produce compressed formulations which transfer pharmaceutically active ingredients into the mouth and throat region and release them there. In the context of the present invention, pharmaceutically active ingredients are understood as substances which have a desired prophylactic or therapeutic effect on the human or animal organism. These substances therefore serve particularly for the prophylaxis or therapy of deficiencies or syndromes. According to the invention, for example enzymes, coenzymes, minerals, vitamins, antibiotics, microbicidal or fungicidal substances such as nicotine, caffeine, eucalyptol, codeine, phenacetin, acetylsalicylic acid, menthol, or other pharmaceutically active ingredients can be incorporated in the compressed formulations. The pharmaceutically active ingredients are to be provided in an amount such that they render the desired pharmaceutical effect. The gentle digestion of the compressed formulations and their peculiar solubility characteristics make the inventive compressed formulations particularly suitable for transferring pharmaceutically active ingredients into the mouth and throat region. Compressed formulations containing Isomalt® as well as sugar-containing compressed formulations dissolve in a comparatively poorer fashion so that the release of the active ingredients is delayed. The release of active ingredients of inventive compressed formulations advantageously begins soon and lasts for an extended period of time.
In a further embodiment, the invention relates to compressed formulations in the form of lozenges or chewable tablets.
Finally, the invention relates to the use of 1,1-GPS or of a sweetener mixture composed of 1,6-GPS, 1,1-GPM and 1,1-GPS in a powder mixture or the compressed formulations made from it for improving its compressibility.


REFERENCES:
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T. Dörr, et al., “Beurteiling der Auflösekinetic Oralen Pharmazeutischer Darreichungsformen aus Verschiedenen Sacchariden und Zuckeraustauschstoffen”, Bd. 58, Nr. 10, 1996, pp. 947-952.
F.W. Lichtenthalter, et al., “The Preferred Conformations of Glycosylalditols”, Liebig's Annalen der Chemie, 1981, pp. 2372-2383.

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