FR2906464A1 - Composition, useful to prevent addiction to absorption of alcoholic beverages by oral cavity, comprises a compound able to react with oral mucous membrane to produce a typical sensation and a water insoluble compound - Google Patents

Abstract

Composition for preventing addiction to the absorption of alcoholic beverages by the oral cavity, where the oral cavity is lined by a mucous membrane significantly humid, comprises: a first compound able to react with oral mucous membrane to produce a typical sensation; and a second compound insoluble in water and soluble in the alcoholic drinks, where the second compound is adapted for coating the first compound for confining in a sealed envelope. Composition for preventing addiction to the absorption of alcoholic beverages by the oral cavity, where the oral cavity being lined by a mucous membrane significantly humid, comprises: a first compound able to react with oral mucous membrane to produce a typical sensation; and a second compound insoluble in water and soluble in the alcoholic drinks, where the second compound is adapted for coating the first compound for confining in a sealed envelope, and the active composition is adapted to be stored in the oral cavity, to provoke the dissolution of the second compound and the release of the first compound in the oral cavity when the alcoholic beverages are absorbed, by which the typical sensation produces a signal representative of the absorption of alcoholic beverages. Independent claims are included for: (1) a mucoadhesive composition comprising incorporating the composition; and (2) a preparation of the composition to prevent addiction to the absorption of alcoholic beverages by the oral cavity, comprising providing the first compound to react with the oral mucous membrane to produce the typical sensation, providing the second water insoluble compound and soluble in alcohol, dissolving the second compound in alcohol to form the alcoholic solution, overlaying the first composition by the alcoholic solution, evaporating the alcohol to form a sealed envelope around the first compound, and recovering the composition able to be stored in oral cavity, where the second compound composed of the sealed envelope being adapted to dissolve itself by releasing the first compound in the oral cavity when the alcoholic beverages are absorbed.

Description

2906464 Active composition to prevent habituation to absorption of

  The present invention relates to an active composition for preventing habituation to the absorption of alcoholic beverages. The treatment of the subjugation of people to drugs, especially alcohol, is often painful. Considering that by substituting a substance which would produce physiological effects of the same nature as those of alcohol, but of course that which would be less harmful to the organism, it has been imagined to be able to wean the victims of this addiction by administering this substance. However, such active substances are never totally without side effects and they too can provide addiction. Moreover, it has been suggested that the phenomenon of habituation of a subject to alcohol, was due to the antigenic properties of the alcohol, thanks to which his organism, to defend itself, would superabundantly produce triene fatty acids. Also, the production of these fatty acids in the body would cause the physical need for alcohol, because the alcohol would then neutralize them. Therefore, the subject thus reached, would tend to consume alcohol to neutralize triene fatty acids while the ingested alcohol would generate new quantities. Also, in order to break this alcohol consuming cycle, it has been imagined to neutralize these triene fatty acids by administering to the subject a therapeutic composition containing organic ethers. In fact, it appears that organic ethers have the ability to form peroxides and thus cause oxidation of these fatty acids. In particular, reference may be made to document FR 2 180 674, which describes the administration of such a treatment. However, this type of treatment leads to superaddition in the body of the subject suffering from addiction, a therapeutic composition which, in the same way as alcohol, then intervenes in the metabolism of said subject.

  Also, a problem that arises and that aims to solve the present invention is to provide an active composition that does not interfere directly in the cycle of metabolism related to the absorption of alcohol and is therefore less toxic. In order to solve this problem, the present invention proposes, according to a first aspect, an active composition for preventing habituation to the absorption of alcoholic beverages by the oral cavity, said oral cavity being lined by a substantially wet oral mucosa. and according to the invention, said active composition comprises: a first compound capable of reacting with the oral mucosa to produce a characteristic sensation; a second compound insoluble in water and soluble in said alcoholic beverages, said second compound being adapted to coat said first compound to trap it in a sealed envelope; and said active composition is adapted to be stored in the oral cavity, so as to cause said second compound to dissolve and release said first compound into the oral cavity when said alcoholic beverages are absorbed; whereby said characteristic sensation produces a signal representative of the absorption of said alcoholic beverages.

Thus, a characteristic of the invention lies in the implementation of a signal perceptible by a subject, or individual, ingesting an alcoholic drink, a signal which not only does not come into play at all in the related metabolic cycle. to alcohol, and that is also totally harmless to the subject. Indeed, a problem that 30 alcoholic subjects encounter and which leads them to absorb alcoholic beverages regularly and too frequently, lies essentially in the lack of awareness by the subject himself, which he absorbs well. an alcoholic beverage as it goes into action. It is also striking to check that most of the alcoholic subjects questioned, consider that they absorb only a very small amount of alcohol during the day.

According to a particularly advantageous embodiment of the invention, the characteristic flavor is a bitter taste, for example denatonium benzoate (marketed under the name Bitrex), and is therefore without any risk for the organism. According to an advantageous embodiment, the first compound comprises io quassia amara wood, for example finely ground. According to another alternative, the first compound produces a characteristic acidic flavor which is another characteristic flavor perceptible by the oral mucosa and in particular by the taste buds. This flavor is brought closer to the pungent effect that is felt in the mouth, for example when lemon juice is absorbed. According to another characteristic of the invention which is particularly advantageous, said second compound comprises vegetable proteins, which have the particular feature of forming relatively impervious films under the conditions of implementation which will be explained hereinafter. In addition, these vegetable proteins are food and therefore completely harmless to the body. Advantageously, the second compound will comprise gliadin, a protein extracted for example from wheat or else zein, a protein extracted from corn. According to another aspect, the present invention provides a mucoadhesive preparation incorporating an active composition of the aforementioned type and which then makes it possible to fix said active composition in the oral cavity, for example against the gum or more generally between the inner wall of the cheek and the maxillary. In this way, when an alcoholic beverage is ingested by the subject carrying the mucoadhesive preparation, it flows at least partially against said mucoadhesive preparation and dissolves said second compound of the active composition to release the first compound producing the characteristic sensation. In yet another aspect, the present invention provides a method of producing an active composition for preventing habituation to absorption of alcoholic beverages by the oral cavity. The method comprises the following steps in order: a) providing a first compound capable of reacting with the oral mucosa to produce a characteristic sensation; b) providing a second water insoluble compound soluble in alcohol; c) solubilizing said second compound in alcohol to form an alcoholic solution; d) covering said first compound with said alcoholic solution; e) evaporating the alcohol to form a sealed envelope around said first compound; and, f) recovering an active composition adapted to be stored in the oral cavity, said second compound of said sealant being adapted to dissolve by releasing said first compound into the oral cavity when said alcoholic beverages are absorbed. Thus, a characteristic of the process lies in the implementation of said second compound via an alcoholic solution which makes it possible to coat the first compound first with a layer of said alcoholic solution so as to obtain then, after evaporation of the alcohol, a tight film around the first compound. According to a particularly advantageous embodiment of the invention, said first compound is supplied in a pulverulent form and the particles of the first compound are then coated with the alcoholic solution and then, after evaporation of the alcohol, form a film tight around each of the particles. In this way, the first compound thus coated is impervious to the outside of the film, and moreover, the film or envelope is soluble only in the alcohol and not in the water or saliva which is present in the oral cavity. Advantageously, a first bitter characteristic flavor compound is thus coated, for example denatonium benzoate or Bitrex, or else quassia amara. Moreover, the alcoholic solution is advantageously made from vegetable proteins, for example gliadin or else zein; zein being available on the market in a relatively pure form at a reasonable cost. Other features and advantages of the invention will become apparent on reading the description given below of particular embodiments of the invention, given for information but not limiting. The present invention relates not only to an active composition capable of causing a characteristic sensation in the oral cavity of a subject when absorbing alcohol, but also to a method of producing said composition as well as to a mucoadhesive preparation allowing the implementation of said composition.

Also, the active composition will be described below through its production process. The active composition essentially comprises two compounds which confer on it its properties; a first compound capable of reacting with the oral mucosa and in particular with the taste buds to trigger a signal perceptible by said subject; a second compound capable of trapping the first compound in a sealed envelope, sealed envelope which can degrade on the oral mucosa only when the subject absorbs alcohol. With regard to the first compound used, an alcohol-denaturing substance having organoleptic properties perceptible to the taste organ has been sought so as to cause a reflex of rejection or disgust by an unexpected sensation at the level of the taste system. Thus, compounds whose flavors were similar to two basic flavors such as bitter and acid and which were active at very low doses were searched for. Denatonium benzoate, marketed under the name Bitrex, and whose formula is, according to the 11th edition of the Merck Index: N- [2 - [(2,6-dimethylphenyl) amino] -2-oxoethyl] -N N-diethylbenzenemethanaminium benzoate is presented in the form of a white crystalline powder having an intense bitter flavor. Moreover, this bitter perception is not excessively persistent and it fades relatively quickly. With regard to the second compound, in addition to the basic characteristics of alcohol solubility and water insolubility, it must also form a sufficiently tight envelope around the first compound to the latter does not spread in the oral cavity until the second compound has been destructured by alcohol. Moreover, it is understood that such a compound must also be of a food nature in the same way as the first compound. Also, the choice fell on plant-based proteins and in particular on grass proteins. Zein, which is a protein extracted industrially from corn, is soluble in alcohol and is capable of forming relatively impervious films. And the film thus formed is insoluble in water. In addition, it is available on the market with a degree of purity quite acceptable and compatible with the intended application. Thus, grains of denatonium benzoate powder were coated with a zein film. To do this, the technique used was that known as: fluidized air bed by means of an installation as described for example in patent EP1624959. It is actually a matter of maintaining the powder grains with a mean diameter of, for example, between 50 and 100 μm, in suspension in the air and simultaneously spraying an alcoholic solution incorporating zein on these particles so as to they are completely covered with a film of said alcoholic solution. As will be explained below, the thickness of the film can be adjusted by spraying more or less alcoholic solution onto the suspended particles. Then, after the coating phase, a drying phase makes it possible to evaporate the alcohol and form a dry film around the particles. Thus, a granular composition is obtained comprising granules with a mean diameter of between 200 and 600 μm, for example 350 μm, and each consisting of a denatonium benzoate grain coated with a dry film of zein.

Experiment No. 1 Active compositions were thus made, a first in which the proportion by weight of zein relative to denatonium benzoate was 20%, and a second in which it was 40%. Thus, the zein film of the granules of the first composition is thinner than that of the second composition. A quantity of 100 mg of each of these compositions was incorporated and mixed in 30 ml of water on the one hand and in 30 ml of alcoholic water with 10% alcohol. Thus, five minutes after mixing, the water alone of the first and second active compositions had no particular flavor, while the alcoholic water had a very distinctly bitter flavor, more sustained for the alcoholic water of the water. first active composition than for that of the second. In addition, after 15 minutes while the water alone of the two active compositions still had no particular flavor, the alcoholic water had a bitter flavor even more intense but still more marked for that of the first active composition. As a result, the thinner film granules release denatonium benzoate faster than the thicker film granules. In fact, the rate of dissolution of the zein of the films in the alcohol is substantially constant, and the sealed envelope formed by the films around clenatonium benzoate grains is dissolved more rapidly than it is thin. Experiment No. 2 Another active composition was made using the first compound of Quassia Amara wood powder. This powder was sieved and calibrated to obtain particles smaller than 500 μm. The second compound used was still zein, 2906464, which was dissolved in isopropanol. The Quassia Amara particles were wrapped in the zein film according to the aforementioned technique, with a film thickness corresponding to 35% by weight of zein relative to the wood powder. A test identical to that of Experiment No. 1 was carried out both in water alone and in 10% alcoholic water. Water alone incorporating the active composition showed no flavor either after five minutes or after 15 minutes, while the alcoholic water had an unexpected bitter taste and especially less intense than that of denatonium benzoate. Thus, mucoadhesive preparations are made with the aforementioned active compositions. For this, use is made of mucoadhesive polymers, either of the anionic type, for example sodium carboxymethyl cellulose (SCMC) or of cationic type, for example hydroxypropylmethyl cellulose (HPMC), within which these active composition are embedded. . Different types of mucoadhesive preparations are then made so as to adapt to the largest number of possible cases. Thus, not all subjects have the same perception of the flavors, in particular because of their eating habits or because of their age. Also, a first mucoadhesive, so-called strong preparation was carried out with the active composition obtained according to experiment No. 1 with 20% zein, and it is intended for subjects with a lower perception of flavors. In this way, denatonium benzoate having a very clearly bitter taste, the signal emitted into the oral cavity will be well perceived by these subjects. A second mucoadhesive, so-called mild preparation was made with the active composition obtained according to experiment No. 2 for subjects or individuals, having a greater perception of flavors; Quassia Amara wood having a bitter flavor less intense than that of denatonium benzoate. On the other hand, a third mucoadhesive, so-called prolonged-action preparation was carried out taking into account the teaching of experiment No. 1. Thus, active compositions made in accordance with experiment No. 1, with proportions of zein weight of 20% and 40% respectively have been included in a mucoadhesive polymer, so that, thanks to this mucoadhesive preparation, the subject who will be carrying it will perceive, after the absorption of a first quantity of alcoholic beverage, a the first signal corresponding to the dissolution of the zein films of the granules containing 20%, and after the absorption of a second quantity of alcoholic beverage, a second signal corresponding to the dissolution of the zein films of the granules containing 40%. Other combinations are also possible, for example by mixing granules of an active composition of Quassia Amara particles coated with 20% zein and granules. ules of an active composition of denatonium benzoate particles coated with 40% zein. In this way the first signal perceived by the subject, after a first absorption of alcoholic beverage, would be of less importance compared to the signal perceived by the subject after a second absorption of alcoholic beverage. 10

Claims (16)

  1. Active composition for preventing habituation to the absorption of alcoholic beverages by the oral cavity, said oral cavity being lined by a substantially moist oral mucosa, characterized in that it comprises: a first compound capable of reacting with the oral mucosa to produce a characteristic sensation; a second compound insoluble in water and soluble in said alcoholic beverages, said second compound being adapted to coat said first compound in order to trap it in a sealed envelope; and in that said active composition is adapted to be stored in the oral cavity, so as to cause the dissolution of said second compound and the release of said first compound into the oral cavity when said alcoholic beverages are absorbed; whereby said characteristic sensation produces a signal representative of the absorption of said alcoholic beverages.   2. Active composition according to claim 1, characterized in that said first compound produces a bitter characteristic flavor. 20   3. Active composition according to claim 2, characterized in that said first compound comprises N- [2 - [(2,6-dimethylphenyl) amino] -2-oxoethyl] -N, N-diethylbenzenemethanaminium benzoate.   4. Active composition according to claim 2, characterized in that said first compound comprises quassia amara. 25   5. Active composition according to claim 1, characterized in that said first compound produces a characteristic acidic flavor.   6. Active composition according to any one of claims 1 to 5, characterized in that said second compound comprises vegetable proteins. 30   7. Active composition according to claim 6, characterized in that said second compound comprises gliadin. 11 2906464   8. Active composition according to claim 6, characterized in that said second compound comprises zein.   Mucoadhesive preparation incorporating an active composition according to any one of claims 1 to 8.   10. A method of producing an active composition for preventing habituation to absorption of alcoholic beverages by the oral cavity, characterized in that it comprises, in order, the following steps: a) providing a first compound capable of reacting with the oral mucosa to produce a characteristic sensation; b) providing a second water insoluble compound soluble in alcohol; c) solubilizing said second compound in alcohol to form an alcoholic solution; D) covering said first compound with said alcoholic solution; e) evaporating the alcohol to form a sealed envelope around said first compound; and, f) recovering an active composition adapted to be stored in the oral cavity, said second compound of said sealant being adapted to dissolve by releasing said first compound into the oral cavity when said alcoholic beverages are absorbed.   11. The production method according to claim 10, characterized in that in step a) said first compound is provided in a powder form.   12. Production process according to claim 10 or 11, characterized in that said first compound produces a bitter characteristic flavor.   13. The production method according to claim 12, characterized in that said first compound comprises N- [2 - [(2,6-dimethylphenyl) amino] -2-oxoethyl] -N, N-diethylbenzenemethanaminium benzoate. 12 2906464   14. Production method according to claim 12, characterized in that said first compound comprises quassia amara.   15. Production method according to any one of claims 10 to 14, characterized in that in step b) a second compound comprising vegetable proteins is provided.   16. The production method according to claim 15, characterized in that said second compound comprises zein. i0