HK1143956B - Clay-based aromatised therapeutic composition - Google Patents

Description

This application concerns a pharmaceutical formulation containing smectite as an active substance.

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The present invention therefore concerns an aromatised therapeutic composition containing clay as the active ingredient and characterised by the following: The clay is a dioctahedral smectite; and the aroma is encapsulated.

A composition according to the present invention may be used for the prevention and/or treatment of certain conditions such as symptomatic treatment of pain associated with oesogastroduodenal and colic conditions, acute and chronic diarrhoea, celiac disease.

Smetites represent a particular family of clays in which dioctahedral species such as montmorillonite and beidellite are found, and trioctahedral species such as hectorite and saponite.

The clay used according to the invention is a dioctahedral smectite. Preferably, the dioctahedral smectite is a montmorillonite or a beidellite or a crystallographic structure intermediate between the two crystallochemical poles montmorillonite and beidellite. This intermediate crystallographic structure can be close to the montmorillonite pole and even very close to the montmorillonite pole; it can also be close to the beidellite pole and even very close to the beidellite pole. Preferably, a smectite according to the invention is a montmorillonite or an intermediate structure close to the montmorillonite pole, and very preferably very close to the montmorillonite pole.

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Specific examples of such compounds can be found in the literature, such as in Fenaroli's Handbook of Flavor Ingredients, 1975, CRC Press; Synthetic Food adjuncts, 1947, M. B. Jacobs, edited by Van Nostrand; or Perfume and Flavor Chemicals, 1969, S. Arctander, Montclair, New Jersey (USA).

These compounds are well known to the professional in the field of flavoured or scented consumer products, i.e. traditionally flavoured consumer products which have been given a fragrance, aroma or taste, or consumer products whose taste has been altered.

Preferably, the aroma is a hydrophobic liquid, soluble in organic solvents but only very slightly soluble in water.

The water incompatibility of most aromas and flavors can in fact be expressed through the Hildebrand solubility parameter which is generally less than 25 MPa1/2 whereas the same parameter for water is 48 MPa1/2 and for alkanes 15-16 MPa1/2. This parameter provides a useful polarity scale correlated to a coercive energy density of the molecules. For a spontaneous mixture to occur, the solubility difference of the molecules to be mixed must be maintained at the minimum. The Handbook of Solubility Parameters (Hand of Solubility Parameters, F.C. Barton, A.C. Barton, M.C. Bocca, 1991) also provides a large list of recommended methods for calculating complex chemical structures, but also allows for a large number of recommended methods for producing complex chemical products.

Preferably also, the aroma is in liquid, volatile or unstable form, with a log P in the range -2 to 7, and very preferably 2 to 6.

Preferably, a composition according to the present invention also includes, as flavoring, natural extracts, essential oils or a mixture thereof.

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Preferably, a composition according to the invention includes at least one encapsulated flavour different from vanilla.

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The flavour is preferably chosen from the flavour of vanilla/caramel/chocolate and citrus extracts and very preferably vanilla/caramel/chocolate and orange, lemon, grapefruit or clementine.

Preferably also, the aroma is a blend of aromas, and very preferably a blend of vanilla and orange aromas.

The flavour may be mixed with solvents, adjuvants, additives and/or other ingredients, e.g. those commonly used in the flavour and/or food industry.

The flavor according to the present invention is preferably encapsulated in a vitreous matrix (encapsulation matrix) of carbon hydrates.

As constituents of the encapsulation matrix, any sugar or sugar derivative which can be processed by extrusion techniques to form a dry extruded solid may be used. Particular examples of suitable constituents may be selected from the following products: sucrose, glucose, lactose, levulose, fructose, maltose, ribose, dextrose, isomalt, sorbitol, mannitol, xenylitol, lactitol, maltitol, pentatol, arabinose, pentatol, xylose, galactose, hydrolysates of starch, maltodextrine, Stabilite (trade name: Polycarbonate of origin USA), agar-agar, carrageenan, other polymers, and the derivatives and mixtures thereof.

Maltodextrin or mixtures of maltodextrin and at least one product chosen from: sucrose, glucose, lactose, levulose, maltose, fructose, isomalt, sorbitol, mannitol, xylitol, lactitol, maltitol and hydrogenated starch hydrolysates are used preferably.

Preferably, maltodextrin has a dextrose equivalent (DE) above 5 and below 20.

An emulsifier such as lecithin, and/or a plasticizer, typically water, may be added to the mixture if necessary.

The product or composition flavoured according to the invention, which is extruded, can be prepared by any standard method. For example, the processes described in US Patents 4,610,890 and 4,707,367, the contents of which are incorporated by reference, are suitable for providing encapsulated flavourings as used in the present invention.

Preferably, the aroma is present at a rate of at least 10% by weight in dry matter, in relation to the total weight (in dry matter) of the encapsulation matrix, and preferably at a rate between 15% and 35%.

A composition according to the invention preferably contains 70 to 90% by weight of active substance, and very preferably 75 to 85% by weight of the total composition.

Preferably, a composition of the invention also contains 0.1 to 3% by weight of encapsulated flavour in relation to the total weight of the composition, and very preferably 0.3 to 2.5% by weight.

A therapeutic composition according to the present invention may be in various solid forms such as powders, granules, tablets or capsules.

In a therapeutic composition according to the present invention, other additives such as colorants, sweeteners, lubricants, glides may also be found.

The colorant (s) used according to the present invention may be any type of colorant commonly used in food and/or pharmaceuticals.Sweeteners include, for example, saccharin, aspartame, maltodextrin, monosaccharides such as fructose or glucose, disaccharides such as sucrose.Lubricants include, for example, talc.Sweeteners include sucrose.

Mineral input may consist, for example, of the addition of metal salts such as aluminium salts or magnesium salts such as aluminium hydroxide, magnesium carbonate.

The method of administration of a composition according to the invention will be chosen, inter alia, according to its galenic form and the pathology to be treated.

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Unless otherwise defined, all technical and scientific terms used herein have the same meaning as is commonly understood by an ordinary specialist in the field to which this invention relates.

The experimental part Example 1: Preparation of an encapsulated orange flavouring (oil)

A syrup is prepared from maltodextrin, sucrose, water and flavoring. The mixture is then heated to 123°C to reduce the moisture level of the syrup. Then the emulsifier is mixed with the concentrated syrup under strong shear conditions to form a uniform melted mass. The melted mass is then extruded under 2x105 Pa pressure through an extrusion matrix plate with 0.8 mm diameter holes in a cold solvent to cool and break the extruded.

Maltodextrin 18DE	1505	44,55
Sucrose	1505	44,55
Huile orange Valence pressée à froid	350	10,36
18	0,54
Eau	400	-
Total		100,00

Example 2: Preparation of a vanilla flavouring encapsulated

Example 1 is reproduced using vanilla extract (ex Firmenich) instead of the orange flavour.

Example 3: Preparation of a caramel flavouring encapsulated

Example 1 is reproduced using a caramel flavour (ex Firmenich) instead of the orange flavour.

Example 4: Preparation of a flavoured therapeutic composition

The following formulae are prepared by mixing together, gently, all the ingredients in the proportions indicated, until they are dispersed evenly. - What?

Ingrédients	Exemple 4a	Exemple 4b	Exemple 4c
Diosmectite	3000	3000	3000
	-	-	10
	50	50	50
	10	-	-
Saccharine soluble + glucose hydraté	700	710	700
Eau	100	100	100

Example 5 - Stability of a composition according to the invention

Since clay is by its nature a stable product, the stability of a composition according to the invention is measured both in terms of the organoleptic characteristics of the aroma and its inertia with respect to clay.

The stability of the organoleptic characteristics of the flavour is established by testers (panel of 7 experts) on the basis of many criteria (sweet, fruity, acid, bitter, etc.) for a period of at least 6 months.

It is also found that the aroma does not deteriorate in the presence of clay for the same period.

Claims (28)

1. Flavoured therapeutic composition containing a clay as active ingredient, and characterized in that

   - the clay is a dioctahedral smectite; and

   - the flavour is encapsulated.
2. Composition according to claim 1, characterized in that the dioctahedral smectite is a montmorillonite or a beidellite or an intermediate crystallographic structure between the two crystal-chemical poles: montmorillonite and beidellite.
3. Composition according to one of the previous claims, characterized in that the dioctahedral smectite is a montmorillonite or an intermediate crystallographic structure close to the montmorillonite pole.
4. Composition according to one of the previous claims, characterized in that the dioctahedral smectite is a montmorillonite or an intermediate crystallographic structure very close to the montmorillonite pole.
5. Composition according to one of the previous claims, characterized in that the dioctahedral smectite is the smectite known as "diosmectite".
6. Composition according to one of the previous claims, characterized in that the flavour is a hydrophobic liquid.
7. Composition according to one of the previous claims, characterized in that the flavour has a Hildebrand solubility parameter less than 30 MPa^1/2.
8. Composition according to one of claims 1 to 5, characterized in that the flavour is in liquid form with a log P comprised within the range -2 to 7.
9. Composition according to the previous claim, characterized in that the flavour has a log P comprised within the range 2 to 6.
10. Composition according to one of the previous claims, characterized in that the flavour is a natural extract, an essential oil or a mixture thereof.
11. Composition according to one of the previous claims, characterized in that it comprises at least one encapsulated flavour different from vanilla.
12. Composition according to one of the previous claims, characterized in that the flavour is chosen from the following flavours: liquorice, exotic fruits, red fruits, extracts of citrus fruits, vanilla, caramel, chocolate, coca, green tea, crème brêlée (caramel custard).
13. Composition according to one of the previous claims, characterized in that the flavour is chosen from the following flavours: vanilla, caramel, chocolate and extracts of citrus fruits.
14. Composition according to one of the previous claims, characterized in that the flavour is chosen from the following flavours: vanilla, caramel, chocolate, orange, lemon, grapefruit and clementine.
15. Composition according to one of the previous claims, characterized in that the flavour is a mixture of flavours.
16. Composition according to the previous claim, characterized in that the flavour is a mixture of vanilla and orange flavours.
17. Composition according to one of the previous claims, characterized in that the flavour is encapsulated in a glassy matrix of carbohydrates.
18. Composition according to the previous claim, characterized in that the matrix is constituted by maltodextrin or a mixture of maltodextrin and at least one product chosen from: sucrose, glucose, lactose, levulose, maltose, fructose, isomalt, sorbitol, mannitol, xylitol, lactitol, maltitol and hydrogenated starch hydrolysates.
19. Composition according to one of claims 17 to 18, characterized in that the matrix is constituted by maltodextrin or a mixture of maltodextrin and at least one product chosen from: sucrose, maltose, isomalt, maltitol and hydrogenated starch hydrolysate.
20. Composition according to one of claims 17 to 19, characterized in that the matrix is constituted by maltodextrin and sucrose.
21. Composition according to one of claims 18 to 20, characterized in that the maltodextrin has a dextrose equivalent greater than 5 and less than 20.
22. Composition according to one of the previous claims, characterized in that the flavour is present in a proportion of at least 10% by weight expressed as dry matter, with respect to the total weight (expressed as dry matter) of the encapsulation matrix.
23. Composition according to one of the previous claims, characterized in that the flavour is present in a proportion comprised between 15 and 35% by weight expressed as dry matter, with respect to the total weight (expressed as dry matter) of the encapsulation matrix.
24. Composition according to one of the previous claims, characterized in that it comprises from 70 to 90% by weight of active ingredient.
25. Composition according to one of the previous claims, characterized in that it comprises from 75 to 85% by weight of active ingredient.
26. Composition according to one of the previous claims, characterized in that it comprises from 0.1 to 3% by weight of encapsulated flavour.
27. Composition according to one of the previous claims, characterized in that it comprises from 0.3 to 2.5% by weight of encapsulated flavour.
28. Composition according to one of the previous claims, characterized in that it comprises from 0.5 to 2% by weight of encapsulated flavour.