FR3142665A1 - EFFERVESCENT COMPOSITION - Google Patents

Abstract

EFFERVESCENT COMPOSITION The invention relates to an effervescent composition in contact with water, the composition of which comprises: at least one electrolyte, N-acetyl-L-cysteine, vitamin B6. Figure for abstract: Fig. 1

Description

EFFERVESCENT COMPOSITION Field of the invention

The invention relates to an effervescent composition, in particular for the relief of symptoms and the treatment of veisalgia.

State of the art

During excessive consumption of alcoholic beverages, a subject may experience an uncomfortable sensation. This sensation appears 6 to 8 hours after alcohol consumption, when the subject's blood alcohol level decreases and reaches a maximum when the blood alcohol level becomes zero. The intensity of symptoms increases with the amount of alcohol consumed. This sensation is also known as “veisalgia” or by the more familiar name “hangover”.

Manifestations of this sensation include dry mouth, discomfort and nausea as well as a feeling of weakness, fatigue, difficulty concentrating, digestive discomfort and headaches. A significant decline in alertness and memory may also be observed. It is particularly known that through its diuretic action, alcohol causes an imbalance which induces dehydration.

It is known, in similar cases, to take paracetamol or ibuprofen. The disadvantage of paracetamol is that its hepatotoxicity can be enhanced by alcohol metabolism. A disadvantage of ibuprofen is that it is capable of worsening gastritis. Taking aspirin, for its part, suddenly increases the alcohol level in the blood and therefore its toxicity and irritates the walls of the stomach.

Today, it is recommended to drink a large quantity of water to counterbalance the dehydration induced by the inhibition of vasopressin (also known by the English acronym “ADH” for “AntiDiuretic Hormone”) by alcohol, and the feeling of dry mouth.

However, this solution does not alleviate most of the other manifestations of veisalgia.

The invention therefore aims to provide a composition, in particular an effervescent composition making it possible to alleviate these symptoms and manifestations while reducing toxicity for the subject.

Summary

The invention relates to one comprising at least one electrolyte, N-acetyl-L-cysteine and vitamin B6. Preferably, the composition is in the form of a solid tablet that effervescently on contact with water.

In one embodiment, the composition includes proanthocyanid. Preferably, the composition comprises grape seed extract.

In one embodiment, the composition comprises at least one antioxidant such as OPC.

In one embodiment, the composition comprises vitamin E.

In one embodiment, the composition comprises ginger extract and/or ginseng extract.

In one embodiment, the composition comprises vitamin C, preferably synthetic vitamin C.

In one embodiment, the composition does not include magnesium. In one embodiment, the composition does not include sucrose.

In one embodiment, the composition comprises at least 2% m of N-acetyl-L-cysteine.

In one embodiment, the composition comprises at least 1% m of ginseng extract.

In one embodiment, the composition comprises at least 1% m of lemon balm extract.

In one embodiment, the composition comprises at least 1% m of cysteine, preferably L-cysteine.

In one embodiment, the composition comprises at least 0.5% m of rhodiola extract.

In one embodiment, the composition comprises at least 0.2% m of vitamin C.

In one embodiment, the composition comprises at least 0.2% m of ginger extract.

In one embodiment, the composition comprises 0.1% m of grape seed extract.

In one embodiment, the composition comprises 0.05% m vitamin B6.

In one embodiment, the composition comprises vitamin E.

In one embodiment, the composition comprises at least one electrolyte from chloride, potassium and sodium or a combination of these three electrolytes.

In one embodiment, the composition comprises at least 5% m of electrolytes. Preferably the composition comprises at least 1% m potassium. Preferably, the composition comprises at least 1% m chloride. Preferably, the composition comprises at least 3% m sodium.

In one embodiment, the composition is a medicinal composition for use in the treatment of symptoms of veisalgia, particularly in mammals or in humans.

In one embodiment, the administration schedule for said effervescent composition comprises a first administration of one or two tablets dissolved in water in the evening after excessive alcohol consumption and a second administration of one or two dissolved tablets in water upon waking up, the day after the first administration.

Preferably, each pellet has a mass of between 1000 mg and 7000 mg, more preferably between 3500 mg and 5000 mg, more preferably between 4000 mg and 4400 mg.

In one embodiment, the composition comprises a carbonic acid such as citric acid to generate effervescence when the composition, in the form of a solid tablet, is immersed in an aqueous solution.

Description of the invention

The composition is preferably in the form of an effervescent tablet or an effervescent tablet 1 as illustrated in the .

In this description, the symbol “%m” must be understood as a mass percentage. The mass percentage of a compound is equal to the mass of said compound in the composition divided by the mass of the total composition.

In one embodiment, the composition comprises N-acetyl-L-cysteine (also called “NAC” in the remainder of the description) and optionally L-cysteine.

Acetaldehyde is formed during the alcohol elimination process. Acetaldehyde is a toxic metabolite of ethanol, harmful to our body and particularly to the liver. In order to eliminate this compound, the body uses aldehyde dehydrogenase and glutathione. This metabolic cascade is efficient, but quickly saturated due to lack of glutathione, the reserves of which are limited. When this system is saturated, our ability to metabolize acetaldehyde is affected, leading to many adverse effects.

NAC is a precursor of L-cysteine. L-cysteine, combined with glycine and glutamate, helps promote glutathione biosynthesis.

The intake of NAC thus advantageously accelerates the metabolism of alcohol in the body.

In one embodiment, the composition comprises a concentration of NAC of between 1%m and 15%m, preferably between 6%m and 3%m, very preferably between 4%m and 5%m.

In one embodiment, the composition includes L-cysteine. In one embodiment, the concentration of L-cysteine is between 1%m and 5%m, preferably between 1.5%m and 2.5%m. In another alternative embodiment, the composition does not include L-cysteine, but only NAC.

The combined presence of NAC and L-cysteine advantageously makes it possible on the one hand to provide the body with an immediate supply of L-cysteine to improve the metabolism of ethanol, and on the other hand, to provide the body with a precursor of said L-cysteine which is better absorbed by the body and allows better efficiency in the metabolism of ethanol over a longer period of time.

In one embodiment, the composition comprises vitamin E.

Vitamin E is a powerful antioxidant that scavenges free radicals in vivo. In particular, in association with vitamin C, there is a synergy of actions aimed at inhibiting the oxidation of low density lipoproteins (“LDL”).

In one embodiment, the composition comprises proanthocyanidins, in particular oligo-proanthocyanides (designated in the rest of the description by the acronym OPC").

Indeed, the metabolization of acetaldehyde includes the generation of acetaldehyde-Glutathione on the one hand and free radicals on the other.

The antioxidant properties of vitamin E and OPCs advantageously reduce oxidative stress. Oxidative stress is an imbalance between excessive free radicals and antioxidants. The metabolization of acetaldehyde generates a surplus of free radicals responsible for such an imbalance. This imbalance notably promotes cellular aging and can cause inflammation.

The intake of vitamin E and/or OPCs advantageously improves the supply of antioxidants in the body to compensate for this imbalance.

In one embodiment, the composition comprises grape extract or grape seed extract. The benefit of OPC from grape seeds is an additional protective effect against ethanol-induced toxicity in brain cells.

In one embodiment, the composition comprises between 0.01 and 0.1% m of vitamin E, preferably between 0.02 and 0.04% m of vitamin E.

In one embodiment, the composition comprises between 0.2 and 0.5% m of OPC. In one embodiment, the composition comprises between 0.2 and 0.5% m of grape extract or grape seed extract.

In one embodiment, the composition includes vitamin B6. In one embodiment, the composition includes vitamin C (also known as ascorbic acid). Vitamin B6 and vitamin C contribute advantageously to reducing the subject's fatigue. In addition, vitamin B6 helps reduce nausea and digestive discomfort caused by veisalgia.

In one embodiment, the composition comprises between 0.05%m and 0.5%m of vitamin B6, preferably between 0.1%m and 0.2%m.

In one embodiment, the composition comprises acerola, a fruit rich in vitamin C. An advantage is that vitamin C from acerola is better absorbed by the human body than synthetic vitamin C. Vitamin C advantageously helps fight oxidative stress thanks to its antioxidant properties.

In an alternative embodiment, the composition includes synthetic vitamin C.

The advantage of synthetic vitamin C is to preserve a composition without the sugar of acerola.

In one embodiment, the composition does not include sugar. In one embodiment, the composition does not include acerola or acerola extract.

In one embodiment, the composition includes sweeteners to compensate for the absence of sugar such as sucralose, acesulfame potassium and/or sodium saccharinate. An advantage of these last two examples is to allow the additional contribution of electrolytes (potassium and sodium respectively) in the composition.

In one embodiment, the composition comprises between 0.5%m and 3%m of vitamin C, preferably between 0.5%m and 1.5%m.

In one embodiment, the composition further comprises ginseng extract.

Ginseng is a stimulant that helps reduce fatigue. Ginseng extract exhibits hepatoprotective effects, attributed to its antioxidant properties, the principle of which has been described previously. Ginseng extract also has anti-inflammatory and cognitive-enhancing properties.

Finally, ginseng extract advantageously improves water intake in the body.

The composition comprises between 1%m and 5%m of ginseng extract, preferably between 2%m and 3%m. In one embodiment, the ginseng extract comprises between 5 and 20% m of ginsenoside, preferably between 08 and 12% m.

In one embodiment, the composition further comprises ginger extract. Ginger advantageously helps reduce the feeling of nausea, headaches and stimulate the blood system. The antioxidant properties of ginger advantageously help reduce oxidative stress as described previously.

The action of ginger on the body also increases the quantity of gluthanion, thus complementing the action of NAC in preventing oxidative stress. Another benefit of ginger extract is reducing nausea as well as having an anti-inflammatory action.

In one embodiment, the composition comprises between 0.2%m and 5%m of ginger extract, preferably between 0.5%m and 1.5%m. in one embodiment,

In one embodiment, the ginger extract comprises between 1%m and 10%m of gingerol, preferably between 3%m and 7%m.

It has been observed that the presence of ginger and vitamin B6 causes a synergy of actions in reducing the symptoms of nausea and vomiting.

In one embodiment, the composition includes electrolytes.

The role of electrolytes is to fight against cellular dehydration, recorded after a significant intake of alcohol. Electrolytes may include sodium, potassium, calcium, bicarbonate, magnesium, chlorine and/or phosphate or a mixture of these compounds.

Alcohol consumption induces an imbalance of these electrolytes. Indeed, the latter are mobilized to eliminate the toxic metabolites of ethanol. Electrolyte deficiency can manifest itself directly through the feeling of intense thirst or headaches. Consumed electrolytes must be reabsorbed to regain vital fluid balance.

Electrolytes are beneficial in reducing headaches.

In one embodiment, the composition comprises between 1%m and 3%m of potassium, preferably approximately 2.2%m of potassium. Another benefit of chloride is to aid digestion and relieve digestive discomfort.

In one embodiment, the composition comprises between 1%m and 3%m Chloride, preferably around 2%m.

In one embodiment, the composition comprises between 3%m and 7%m of sodium, preferably between 5%m and 6%m.

In one embodiment, the composition comprises potassium chloride and/or sodium bicarbonate to guarantee the supply of electrolytes in the composition as previously defined.

In one embodiment, the composition does not include magnesium. Magnesium has the disadvantage of promoting hypermagnesimia to which the subject may be exposed after consuming certain alcoholic beverages.

In one embodiment, the composition includes lemon balm. Lemon balm helps improve the quality of sleep. The composition preferably comprises lemon balm extract.

A first benefit of lemon balm is to reduce insomnia.

A second benefit of lemon balm is to help correct the imbalance induced by alcohol consumption on the GABAergic system.

The GABA type A receptor has a certain affinity for ethanol. When this substance is present in the body following the absorption of alcoholic beverages, it is found, through the blood system, in the central nervous system. The ethanol can then bind to the GABA type A receptor, thereby reducing the subject's cognitive and balance abilities.

In one embodiment, the composition comprises a concentration of lemon balm extract of between 1%m and 5%m, preferably between 2%m and 3%m.

In one embodiment, the composition comprises rhodiola or rhodiola extract (also called "rhodiola"). Rhodiola advantageously helps improve concentration abilities, attention in cognitive function in the event of fatigue, and the subject's mental performance.

Rhodiola extract preferentially comprises salidroside, p-tryosol, rosavin, pyride, rhodiosin and rhodionine which are the active ingredients of the Rhodiola species,

In one embodiment, the concentration of the rhodiola extract in the composition is between 0.5m and 5%m, preferably between 0.5%m and 2%m.

In one embodiment, the rhodiola extract comprises between 1%m and 5%m rosavin, preferably between 2.5%m and 3.5%m

In one embodiment, the rhodiola extract comprises between 0.1% m and 3% m salidroside, preferably between 0.5% m and 1.5% m.

In one embodiment, the composition is in the form of an effervescent tablet. The effervescent tablet, on contact with water, will dissolve, producing a release of gas.

For this purpose, the composition comprises an acidifier such as a carbonic acid, for example citric acid. The composition preferably comprises sodium bicarbonate.

An advantage of sodium bicarbonate is, on the one hand, that its reaction with citric acid allows dilution by effervescence of the composition in water accompanied by a production of carbon dioxide, on the other hand, it allows the sodium intake to the body.

In order to produce an effervescent tablet, the quantity of citric acid and/or sodium bicarbonate must generally be high in the composition, for example above 1%m. An advantage is thus to provide additional electrolytes to fight against oxidative stress.

The composition may further comprise one or more dyes such as riboflavin. The composition may further comprise an anti-caking agent such as polyethylene glycol. The anti-caking agent advantageously makes it possible to limit the agglutination of the particles of the composition when it is dissolved in water.

Example

In one example, effervescent tablets of 4200 mg were produced with the composition according to one embodiment of the invention.

The quantity of compounds in this composition are given in Table 1.

Compound Quantity in a 4200 mg tablet (in mg) Sodium 227.64 N-acetyl-L-cysteine 195 Potassium 95 chloride 86.15 Ginseng extract (including ginsenosides) 100 (10.0) Melissa extract 100 Cysteine 75 Rhodiola extract (including rosavins/salidrosides) 50 (1.5/0.5) vitamin C 37.5 Ginger extract (including gingerols) 40 (2.0) Grape seed extract (including proanthocyanidin) 12.63 (12.0) vitamin B6 6.25 Vitamin E 1.25

Results

The composition according to Table 1 was tested on a group called “test group” composed of 49 people.

The test group was subjected to excessive consumption of alcoholic beverages in the evening in order to test the composition in a state of veisalgia. The test group took one effervescent tablet dissolved in water after consuming alcoholic beverages before going to sleep and another effervescent tablet dissolved in water upon waking up.

The test group completed a questionnaire assessing their state of health according to several criteria: headaches, fatigue, difficulty sleeping, nausea, dehydration, difficulty concentrating, anxiety and general discomfort. For each criterion, the target group was asked to give a score between 0 and 10 (0 corresponding to no symptoms felt and 10 to maximum pain) with taking the composition and without taking the composition.

The results are shown in Table 2.

Criteria With plug Without socket Headache 1.9 6.0 Fatigue 3.6 7.2 Difficult sleep 2.6 5.1 Nausea 1.1 3.6 Dehydration 2.3 6.3 Difficulty concentrating 2.1 6.1 Anxiety 2.3 5.6 general unhappiness 1.9 6.0

It is observed that the composition according to the invention advantageously makes it possible to observe an improvement in the state of health and a significant reduction in all the symptoms of veisalgia.

Claims (10)

Composition, in particular intended to be effervescent on contact with an aqueous solution and comprising:

• at least one electrolyte,
• N-acetyl-L-cysteine,
• vitamin B6.

Composition according to claim 1 comprising proanthocyanid such as grape seed extract. Composition according to one of claims 1 or 2 comprising vitamin E. Composition according to one of claims 1 to 3 comprising ginger extract and/or ginseng extract. Composition according to one of claims 1 to 4 comprising synthetic vitamin C. Composition according to one of claims 1 to 5 not comprising magnesium and/or not comprising sucrose. Composition according to one of claims 1 to 6, comprising:

• At least 2%m of N-acetyl-L-cysteine;
• At least 1% m ginseng extract;
• At least 1% m of lemon balm extract;
• At least 1% m cysteine, preferably L-cysteine;
• At least 0.5% m of rhodiola extract;
• At least 0.2%m vitamin C;
• At least 0.2%m of ginger extract;
• At least 0.1%m of grape seed extract;
• At least 0.05%m of vitamin B6, and
• Vitamin E.

Composition according to one of claims 1 to 7 in which the at least one electrolyte comprises at least one compound from sodium, chloride and potassium or a combination of these compounds. Medicinal composition according to one of claims 1 to 8 for use in the treatment of the symptoms of veisalgia in humans. Composition according to claim 9, wherein the administration schedule of said effervescent composition comprises a first administration of one or two lozenges dissolved in water in the evening after excessive alcohol consumption and a second administration of one or two tablets dissolved in water upon waking up, the day after the first administration.