FR3002847A1 - ANTIEMETIC COMPOSITION, FOOD SUPPLEMENT COMPRISING THE SAID COMPOSITION AND PROCESS FOR PREPARING THE SAME - Google Patents

Abstract

Antiemetic composition containing, as active ingredients, the mixture of at least one active ingredient based on red fruits, in particular strawberry-based, and at least one cocoa-based active ingredient, said active ingredients being in the form of an extract and / or or powder. Food supplement or fortified food or dietary product comprising said antiemetic composition in weight proportions of between 0.1% and 85%, preferably between 3% and 65%, more preferably between 20 and 60%.

Description

The present invention relates to the field of treatment of nausea in pregnant women. In particular, the present invention relates to an antiemetic composition for and / or treating nausea in pregnant women. The present invention also relates to a food supplement or a fortified food or a dietary product comprising said antiemetic composition. Finally, the present invention also relates to the method of manufacturing said antiemetic composition. STATE OF THE ART Nausea and vomiting are among the most frequent and unpleasant complications of pregnancy. These symptoms usually begin at four to six weeks of pregnancy, but can occur as early as two to three weeks after the onset of the last menstrual period. These typical symptoms are most intense at eight to twelve weeks, and usually stop within three to four months. However, symptoms may persist for fourteen weeks in forty percent of women, sixteen weeks in less than twenty percent, and twenty weeks in less than ten percent. Very few women (less than ten percent) experience these symptoms until the end. Nausea and vomiting are very common symptoms that can be caused, in addition to pregnancy, by transport, drug therapy, chemotherapy and irradiation, surgery, etc. The etiology of nausea and vomiting is complex. , involving both nerve pathways and motor responses. This results in a series of gastrointestinal reactions, including hyposecretion, decreased motility of the small intestine, hypotonia, hypoperistalsis until ejection of the contents of the stomach and small intestine. The use of certain pharmacological agents to relieve the symptoms of pregnancy nausea and vomiting (NVP) during the period of embryonic organogenesis is contraindicated. Vitamin B6 (pyridoxine hydrochloride) and ginger are the two main treatments whose effectiveness and safety are documented and recently recommended by healthcare professionals to reduce the symptoms of NVP. In addition, NVP can be alleviated by eating small portions of food at intervals, increasing sugars and reducing fats, and foods with an unpleasant odor.

The object of the invention is therefore to propose a novel composition having an antiemetic action for preventing and / or treating nausea in pregnant women, at least as effective as those existing on the market at the present time.

DESCRIPTION OF THE INVENTION To this end, the present invention relates to an antiemetic composition containing, as active ingredients, the mixture of at least one active ingredient based on red fruits and at least one cocoa-based active ingredient, said active ingredients being in the form of extract and / or powder.

This antiemetic composition is used to prevent and / or treat nausea in pregnant women, but can also be effective in any other person suffering from nausea related to various causes mentioned above (motion sickness, drug treatment ...). The berries-based active can be made from strawberries, raspberries, blackcurrants, blueberries, cranberries, blackberries, currants, cherries, lingonberries or a mixture of these fruits.The applicant has discovered, surprisingly , that the mixture of the aforementioned active compounds, namely the combination of at least one active derived from red fruits, in particular strawberry, and at least one cocoa-based active ingredient, has an antiemetic activity which makes it possible to reduce the Advantageously, the present antiemetic composition contains powder and / or an extract of cocoa beans (Theobroma cacao), more particularly cocoa bean powder (Theobroma cacao) comprising at least 5% preferably from 5% to 60%, by weight of total polyphenols and / or cocoa bean extract (Theobroma cacao) produced by means of a polar solvent, said extract comprising at least 5%, preferably 5% by weight, % at 60% by weight of total polyphenols. Advantageously, the present antiemetic composition contains powder and / or a red fruit extract, more particularly red fruit powder comprising at least 5%, preferably from 5% to 30%, by weight of anthocyanins. and / or a red fruit extract made using a polar solvent, said extract comprising from 5% to 70% of anthocyanins.

Preferably, the active ingredient based on red fruits is Fragaria strawberry, preferably chosen from the Fragaria x ananassa, Fragaria virginiana, Fragaria vesca or Fragaria viridis varieties. Cocoa and strawberry are known to be interesting sources of flavonoids, polyphenols, vitamins, with antioxidant effects. Cocoa is particularly well described for its effects on the cardiovascular system and in particular the vascular endothelium. The strawberry is not described to have a particular effect. Nothing could suggest that these two fruits can have any effectiveness on the nausea of the pregnant woman.

Cocoa, derived from cocoa beans (Theobroma cacao), in powder form contains about 10% flavonoids, especially catechin and epicatechin, which gives it a high antioxidant capacity. In the form of an extract, the cocoa comprises about 40% of flavonoids. The strawberry, strawberry fruit (Fragaria) in the form of powder or extract is also a source of flavonoids, including anthocyanins, 150 to 600 mg / kg of dry matter, responsible for its antioxidant effect. Cocoa and strawberry may be provided in the form of powder or extract in said composition as mentioned above. The cocoa-based active ingredient is advantageously present in the composition in a weight ratio of between 5% and 85%, preferably between 30% and 85%, more preferably between 65% and 85%. The active ingredient based on red fruits is advantageously present in the composition in a weight ratio of between 2% and 65%, preferably between 10% and 65% and more preferably between 15% and 35%. This antiemetic composition is preferably incorporated into a dietary supplement, a dietary product or a fortified food. The various constituents of said composition may be provided individually or together in the final product according to the manufacturing and implementation facilities. The present invention also relates to a food supplement or a fortified food or a dietetic product comprising the abovementioned antiemetic composition, preferably in weight proportions of between 0.1% and 85%, preferably between 3% and 65%, preferably still between 20 and 60%. Food supplement means a foodstuff whose purpose is to supplement a normal diet and which constitutes a concentrated source of 35 nutrients or other substances having a nutritional or physiological effect, alone or in combination, marketed in the form of doses. By dose is meant all conventional forms: capsules, lozenges, tablets, ampoules, or sachets. When the food supplements are in the form of a soft capsule or capsule, the envelope of these soft capsules or capsules may contain in particular animal gelatin such as fish gelatin, glycerin, or a source material plant such as a cellulose or starch derivative, or a vegetable protein. When the food supplements are in capsule, tablet, or granule form, the mixture of active ingredients can be attached to a powdery carrier such as silica, cellulose or maltodextrin. By fortified foods is meant here products, such as yogurt or drinks, which have been added nutrients, in this case in which the antiemetic composition of the invention has dissolved. Dietary products intended for a particular diet are foodstuffs which, by reason of their particular composition or particular process of manufacture, are clearly distinguishable from foodstuffs for everyday consumption, are suitable for a stated nutritional purpose and are marketed in indicating that they meet this objective. These characteristics above give the dietary supplement, the dietary product, the fortified food according to the invention antiemetic properties to reduce nausea. This benefit is sought for many causes such as pregnancy, but also motion sickness, drug treatments and more broadly all that relates to nausea and vomiting. The dietary supplement, the dietary product, the fortified food may also comprise at least one active ingredient chosen from: vitamins, such as vitamins B6 or B9; carotenoids, such as beta-carotene or lutein; mineral trace elements, such as magnesium, calcium or iron; ginger, apricot, prune; polyphenols and / or additional anthocyanins. Other pharmaceutically and / or food acceptable agents may be added to the antiemetic composition, such as fillers, fluidizers, natural extracts, other vitamins, minerals, trace elements, amino acids, fatty acids, anti-caking agents, dyes, acidifiers, thickeners, preservatives, sweeteners, adjuvants, dyes, flavors.

The fillers are advantageously microcrystalline cellulose, maltodextrin potato or corn. The thickener preferably used is selected from: potato starch, hydroxypropyl methylcellulose, citrus pectin, guar gum, locust bean, agar-agar, konjac, hydrogenated oils, beeswax or a mixture thereof. The fluidizers may be magnesium silicate, magnesium stearate or colloidal silica. Anti-caking agents are those commonly used in the food industry, such as magnesium stearate or colloidal silica. The other vitamins can be chosen from, among others, vitamins B6, B1, B2, B3, B5, B8, C, D or E. As an acid, citric acid can also be used in the composition according to the present invention. The stabilizers used in the manufacture of the food supplement or fortified food or dietary product according to the present invention are those usually used in the food industry, derived from sugars and / or cereals, such as sorbitol. The sweeteners that can be used are, inter alia, inulin, xylitol, aspartame, glucose syrup, fructo-oligosaccharide syrup, maltitol powder or syrup, acesulfame potassium, fructooligosaccharide , sucralose, neohesperidin, steviosides and / or sodium cyclamate. Fatty acids may also be added to the composition, such as omega 3 and / or omega 6 fatty acids, galactolipids, but also amino acids, such as tryptophan, leucine, arginine and / or glycine. The presence of flavors is no longer necessary, the active ingredients being made from red fruits and cocoa which have organoleptic properties. Preservatives are useful so that said antiemetic composition or said dietary supplement or fortified food or dietary product is preserved over time. The preservatives used may be, for example, potassium sorbate, parabens, sodium benzoate, citric acid, benzoic acid, rosemary or ascorbyl palmitate (antioxidant). All these compounds are not limiting, pharmaceutically and / or food acceptable agents may be added to the antiemetic composition or said food supplement or fortified food or dietary product according to the present invention. The dietary supplement, the dietary product or the fortified food may be in the form of naked or coated tablets, multilayer tablets, effervescent tablets, coated tablets, capsules, capsules, powder, granules, sticks, lozenges, soft capsules, patch, solution or aqueous suspension in a glass, stick or beverage ampoule, dropper bottle, or spray. Advantageously, the dietary supplement, the dietary product or the fortified food is preferably administered to man, one to four times per day, per dose comprising from 10 mg to 4 g, preferably from 20 mg to 2 g and from even more advantageously from 100 mg to 1000 mg of said antiemetic composition according to the invention and this, for a period ranging from 1 day to 3 years.

The present invention also relates to the process for preparing the antiemetic composition as described above. The process for producing the antiemetic composition based on cocoa powder and strawberry comprises at least one of the following steps i) or ii): i) roasting and then grinding almonds of cocoa beans (Theobroma cacao), 20 the obtained cocoa powder containing at least 5% by weight of total polyphenols; ii) Extraction of cocoa beans (Theobroma cacao) with a polar solvent, such as water, alcohol or a hydro-alcoholic mixture, and concentration of the extract to obtain a cocoa extract containing at least 5% of total polyphenols, and in that it comprises at least one of the following steps iii) and iv) of: iii) crushing and pressing of the berries, liquid / solid separation and recovery of the juice, concentration juice obtained and dried to dryness to obtain a powder, the powder obtained containing at least 5% by weight of anthocyanins, iv) extraction of red fruits using a polar solvent, such as water, water, alcohol or a hydro-alcoholic mixture, then concentration of the extract so as to obtain a red fruit extract containing at least 5% by weight of total anthocyanins, the steps i) and / or ii) and iii) and / or iv) being followed by a step of mixing the cocoa powder and / or the cacao extract prepared according to at least one of the steps i) and / or ii) with the red fruit powder and / or the berry extract prepared according to at least one of the steps iii) and / or iv).

The powder and / or the cocoa extract and red fruits can be mixed simultaneously or not with other active ingredients, in order to obtain a homogeneous mixture. The polar solvent for the extraction is preferably a solvent having a dipole moment other than zero and in particular greater than 1.5. The polar solvent is advantageously a protic solvent. Alcohols such as methanol, ethanol, propanol, butanol and pentanol, water such as osmosis water, distilled water, permuted, as well as one of their mixtures are suitable as polar solvent according to the present invention. The solvent may furthermore comprise an additive such as an antioxidant agent, a preserving agent, one or more enzymes, in particular intended to degrade the plant walls, for example to facilitate the extraction, an anti-foaming agent, an acid or else a base, especially to modify the isoelectric point and promote precipitation. The extraction step may be by: decoction, maceration, infusion, digestion, percolation, leaching, hot water entrainment, such as distillation or hydrodistillation, microwave assisted solvent, and exchange column. ions. The decoction comprises the following steps: The boiling of cocoa or berries in a polar solvent as defined above; and maintaining this boiling for a particular time, especially from 1 minute to 2 hours, in particular about 20 minutes, and optionally a return to ambient temperature. By "maceration" is meant a method of cold soaking the cocoa beans or berries in the polar solvent for a particular period of time in order to extract the soluble compounds therefrom. In particular, the maceration step has a duration ranging from 1 hour to 15 days, and preferably 1 day. In particular, it is at room temperature, ie 10 to 25 ° C. The infusion is a process of pouring the polar solvent preferably at boiling temperature onto the cocoa beans or berries and then infusing for a period of one minute to two hours.

Digestion is a process of heating the cocoa beans or berries in the polar solvent at a temperature below the boiling point, for example in the case of water at 10 to 89 ° C, and in particular from 25 to 70 ° C.

By percolation or leaching is meant a process of passing the polar solvent through the cocoa beans or berries. The distillation can be carried out for example by VMHD (pulsed vacuum microwave hydrodistillation). During this extraction step, the polar solvent is brought to a pressure greater than atmospheric pressure. In particular when the solvent is water, it may be in the subcritical state, that is to say that the water is at a temperature between 100 and 374 ° C and at a pressure between 1 and 218 bars. Under these conditions, the water is in liquid form. At the end of the extraction step, the polar solvent is brought to a temperature ranging from ambient temperature (25 ° C.) to a temperature of 300 ° C. above the boiling point of the solvent used. and preferably at the boiling point of the solvent used. Thus, the polar solvent is at least partially reduced or completely eliminated, in particular by evaporation, by sublimation, and preferably under reduced pressure. The term "boiling point of the solvent" means the highest temperature that the solvent can reach before evaporating, in gaseous form, freely. This temperature is calculated at atmospheric pressure of 1 atmosphere (101.3 kPa). The extraction step of the process according to the invention may be continuous or discontinuous, and may comprise a step involving heating, in particular of a duration ranging from 1 second to 15 days, and in particular from 10 seconds to 8 hours.

In a further step, the extracts recovered after extraction can be sterilized, in particular by heating with or without pressure and / or by passage over a membrane. These extracts of cocoa beans and berries of red fruits can also be disinfected, in particular by heating with or without pressure or by means of a disinfecting agent. Finally, these extracts are usually dried. This drying can be carried out by lyophilization and / or by atomization. This polar solvent extraction process thus makes it possible to obtain extracts of cocoa beans comprising from 5% to 60%, in particular from 5% to 40% of total polyphenols and extracts of berries of red fruits comprising from 5% to 70% anthocyanins, and especially from 10% to 60% by weight. The antiemetic composition prepared by mixing said extracts and / or cocoa powders and red fruits can thus be incorporated into a dietary supplement, a dietary product or a fortified food. The various constituents of said composition may be provided individually or together in the final product according to the manufacturing facilities. Examples of non-limiting embodiments The following examples of food supplement or fortified food compositions are intended to illustrate the invention without in any way limiting its scope: The cocoa-based active agent used in these examples is an extract of Theobroma cacao L. beans, spray-dried and sieved. The extract has a particle size such that more than 95% of the particles pass through a 20 mesh screen (0.853 mm) and contain a content greater than 20% by weight of total polyphenols. The strawberry powder used in these examples, obtained from pulverized Fragaria virginiana pulp, has a particle size such that more than 95% of the particles are greater than 0.5 mm and comprise at least 5% of anthocyanins. As indicated above, the presence of flavors is not essential, the flavoring type ingredients are noted in parentheses in the examples below. EXAMPLE 1 A food supplement or a fortified food in powder form is prepared, then packaged in a bag (stick), by mixing the ingredients shown in Table 1: Ingredients Per stick in mg Cocoa extract 500,00 Strawberry powder 250,00 Fructo oligosaccharides 1200,00 (Aroma) (10,00) Sweetener 5,00 Table 1 This dietary supplement or fortified food can be diluted in a glass of water or can be ingested directly by humans. Example 2: The food supplement or the fortified food containing the ingredients shown in Table 2 is packaged in the form of a stopper capable of being screwed onto a 300 ml, 1 L or 1.5 L water bottle. Ingredients Per pot in mg Cocoa extract 250,00 Strawberry powder 500,00 Inulin 1820,00 (Aroma) (25,00) Sweetener 5,00 Colorant 10,00 Maltodextrine qsp Table 2 In order to use this supplement or this fortified food, it it is sufficient for the user to screw the stopper containing said composition onto a 300 ml, 1 L or 1.5 L bottle containing, for example, water. The recommended dose for the individual will then be 1 cork per day.

EXAMPLE 3 After mixing the ingredients of Table 3 and placing in an ampoule, after autoclaving and according to techniques known to those skilled in the art, a complex composed of cocoa extracts and strawberry powder is obtained. . Ingredients Per ampoule in mg Cocoa extract 400.00 Strawberry powder 200.00 (Aroma) (50.00) Sweetener 10.00 Water qs Table 3 The recommended dose of administration is one ampoule per day to be diluted in one glass of water. EXAMPLE 4 After mixing the ingredients collected in Table 4 and extruding the mixture, according to techniques known to those skilled in the art, a food supplement or fortified food in the form of extruded granules is obtained. Ingredients Per jar in mg Cocoa extract 18000,00 Strawberry powder 14000,00 Inulin 128 000,00 Table 4 The recommended daily dose is 2.6 g of granules, for example, dosed with a teaspoon and diluted in one glass of water. Example 5: Preparation of capsules. Ingredients Per capsule in mg Cocoa extract 95.00 Strawberry powder 65.00 Excipients: 1.00 Colloidal silica QS 1.00 Magnesium stearate QS Table 5 The recommended daily dose is 1 capsule per day. Example 6: Preparation of tablets.20 Ingredients Per tablet in mg Cocoa extract 400.00 Strawberry powder 300.00 Excipients: 95.00 Microcrystalline cellulose 5.00 Colloidal silica 14.00 Magnesium stearate Table 6 The recommended daily dose is 1 tablet a day.

Example 7 Ingredients Per vial in mg Cocoa extract 7500.00 Strawberry powder 4000.00 (Flavor) (4000.00) Sweetener 500.00 Citric acid pH <4.5 500.00 Potassium sorbate 500.00 Benzoate sodium 500.00 Table 7 The dietary supplement, dietetic product or fortified food according to this example is, after homogeneous mixing of the ingredients of Table 7, packaged in a bottle with measuring cup. The recommended daily dose is 25 mL (dosed with the measuring cup) and diluted in a glass of water. Example 8: Tests in the pregnant woman: The effect of the composition was evaluated in pregnant women and having nausea. Seven pregnant women who reported experiencing nausea received one tablet daily for 4 days of the composition as described in Example 6 (400 mg cocoa extract, 300 mg strawberry extract). Subjects reported the severity of their nausea using a visual analogue scale as well as the number of vomiting within 24 hours before treatment and within 4 days of treatment. The results show a reduction of nausea from the second day and a decrease in vomiting compared to the beginning of the study. The results of this preliminary study make it possible to demonstrate the effectiveness of the composition for reducing the nausea and vomiting of the pregnant woman. Although the invention has been described in connection with a particular embodiment, it is obvious that it is not limited thereto and that it comprises all the technical equivalents of the means described and their combinations if they fall within the scope of the invention.

Claims (15)

REVENDICATIONS1. An antiemetic composition containing as active the mixture of at least one active ingredient based on red fruits and at least one cocoa-based active ingredient, said active ingredients being in the form of extract and / or powder. 2. An antiemetic composition according to claim 1, characterized in that the active red fruits is derived from strawberries, raspberries, currants, blueberries, cranberries, blackberries, currants, cherries, lingonberries or a mixture of these fruits . 3. antiemetic composition according to claim 1 or 2, characterized in that it contains cocoa bean powder (Theobroma cacao) comprising at least 5%, preferably from 5% to 60%, by weight of total polyphenols . 4. antiemetic composition according to claim 1 or 2, characterized in that it contains an extract of cocoa beans (Theobroma cacao) made using a polar solvent, said extract comprising at least 5%, preferably 5 % to 60%, by weight of total polyphenols. 5. An antiemetic composition according to claim 1 or 2, characterized in that it contains red fruit powder comprising at least 5%, preferably from 5% to 30%, by weight of anthocyanins. 25 6. antiemetic composition according to claim 1 or 2, characterized in that it contains a red fruit extract made using a polar solvent, said extract comprising from 5% to 70% of anthocyanins. 30 7. An antiemetic composition according to any one of the preceding claims, characterized in that the active red fruits is strawberry (Fragaria, preferably selected from the varieties Fragaria x ananassa, Fragaria virginiana, Fragaria vesca or Fragaria viridis). 35 8. An antiemetic composition according to any one of the preceding claims, used to prevent and / or treat nausea in pregnant women. 9. Antiemetic composition according to any one of the preceding claims, characterized in that the cocoa-based active ingredient is present in the composition in a proportion by weight of between 5% and 85%, preferably between 30% and 85%, More preferably between 65% and 85%. 10. Antiemetic composition according to any one of the preceding claims, characterized in that the active ingredient based on red fruits is present in the composition in a proportion by weight of between 2% and 65%, preferably between 10% and 10%. %, more preferably between 15% and 35%. 11. Food supplement or fortified food or dietary product comprising the antiemetic composition according to any one of the preceding claims in weight proportions of between 0.1% and 85%, preferably between 15% and 65%, more preferably between 20 and 60%. 12. Food supplement or fortified food or dietary product according to claim 11, characterized in that it further comprises at least one active ingredient chosen from: vitamins, such as vitamins B6 or B9; carotenoids, such as beta-carotene or lutein; mineral trace elements, such as magnesium, calcium or iron; ginger, apricot, prune; polyphenols and / or additional anthocyanins. 13. Food supplement or fortified food or dietary product according to claim 11 or 12, characterized in that it is in the form of naked or coated tablets, multilayer tablets, effervescent tablets, dragees, capsules, capsules , powder, granules, sticks, lozenges, soft capsules, patch, aqueous solution or suspension in a glass, stick or beverage ampoule, in a dropper bottle, or spray. 30 14. Process for the preparation of the antiemetic composition according to any one of claims 1 to 10, characterized in that it comprises at least one of the following steps i) or ii) of: i) roasting and grinding of almonds cocoa beans (Theobroma cacao), the cocoa powder obtained containing at least 5% by weight of total polyphenols, and ii) extraction of cocoa beans (Theobroma cacao) using a polar solvent, such as water , the alcohol or a hydro-alcoholic mixture, then concentration of the extract so as to obtain a cocoa extract containing at least 5% of total polyphenols, and in that it comprises at least one of the steps iii) and iv) following: iii) crushing and pressing of the berries, liquid / solid separation and recovery of the juice, concentration of the juice obtained and drying to dryness to obtain a powder, the resulting powder containing at least 5% by weight of anthocyanins, iv) extraction of red fruits by means of a polar solvent, such as water, alcohol or a hydroalcoholic mixture, then concentration of the extract so as to obtain a red fruit extract containing at least 5% by weight of total anthocyanins, the steps i and / or ii) and iii) and / or iv) being followed by a step of mixing the cocoa powder and / or cocoa extract prepared according to at least one of steps i) and / or ii) with the red fruit powder and / or the red fruit extract prepared according to at least one of the steps iii) and / or iv). 15 15. Process for the preparation of the antiemetic composition according to claim 14, characterized in that it comprises the step of mixing the cocoa powder and / or the cocoa extract with the red fruit powder and / or the red fruit extract in the following respective weight proportions: from 5% to 85%, preferably from 30% to 85%, more preferably from 65% to 85% by weight, and and / or cocoa extract and from 2% to 65%, preferably from 10% to 65%, more preferably from 15% to 35% of powder and / or fruit extract. red, to obtain said antiemetic composition. 25