"formulation with caffeine-like effects"

Abstract

The present patent application relates to a formulation capable of improving tolerance to stressful situations and the ability to concentrate and memory, while limiting or eliminating side effects such as anxiety, tachycardia, and sleep disorders.

Description

[0001] "Formulation with caffeine-like effects"

[0002] DESCRIPTION

[0003] Background art

[0004] In recent years, the market for products containing methylxanthines, especially energy drinks and dietary supplements, has worryingly increased. The currently published data underline that the consumption of methylxanthine, like caffeine, is related to risks associated with coronary heart disease, arterial hypertension, and an increase in the plasma concentration of cholesterol and homocysteine.

[0005] Caffeine is also a central nervous system stimulant and ranks among the most commonly used psychoactive substances worldwide. The physiological effect of caffeine and the lack of nutritional value arouse great interest in its impact on health, especially with reference to pregnancy and childhood. In fact, excessive consumption of caffeine can cause negative health consequences in adults such as psychomotor agitation, insomnia, headaches, gastrointestinal disorders. These side effects are maximized in children and adolescents, in whom caffeine negatively affects the central nervous system, and the duration and quality of sleep .

[0006] Therefore, there is a need to develop a product which can slowly be replaced or integrated in consumers' diets. The present disclosure aims to provide a healthy alternative to caf feine , increasing the beneficial ef fects thereof .

[0007] In fact , the formulation of the invention proves to be capable of improving tolerance to stress ful situations and the ability to concentrate and remember ( Fig . 1 ) , eliminating side effects such as anxiety, tachycardia, and sleep disorders .

[0008] By virtue of the careful process ing method, the solubility of the components which make the product more stable and expand the possible applications of the semi- finished product is improved . The product is also beneficial for the intestinal tract through the addition of elements which promote regulari zation .

[0009] Summary of the invention

[0010] The inventor of the present patent application has developed a new type of semi- finished product which can surprisingly represent an alternative to caf feine consumption . In fact , the product ensures beneficial aspects , limiting side ef fects . The semi- finished product has a powder-like appearance and can be applied to the production of products with high nutritional and functional value , with the aim of improving physical and cognitive performance , as well as health . The amount of active ingredient for the formulation of new beverages can vary based on the additive components , providing an almost unlimited range of products which can be generated from the semi-finished product . The invention introduces a product with optimized dosages for human consumption, using a production process different from the usual one. The stability of the product which provides tangible advantages is thus ensured, thereby enhancing the ergogenic effects of the invention.

[0011] Brief description of the drawings

[0012] Figure 1 shows a graph with the results of a study on the beneficial effects perceived by the 20 participants following the intake of the product of the invention.

[0013] Figure 2 shows the structure of inulin.

[0014] Figure 3 shows the structure of gum arable.

[0015] Object of the invention

[0016] In a first object, the present invention describes a composition of plant origin.

[0017] In a second object, a formulation comprising the composition of the invention is described.

[0018] In a third object, a process for preparing the formulation of the invention is described.

[0019] In a further object, the use of the composition or formulation of the invention is described, as a substitute for caffeine- based products.

[0020] In a still further object, the use of the composition or formulation of the invention for the health of the gastrointestinal tract is described. Detailed description of the invention

[0021] The present description discloses the semi-finished product and the production method thereof. More in particular, the invention describes a combination of different components processed according to a precise processing method, which generate a powdery product. Such a semi-finished product offers an alternative to caffeine which, although it does not have its typical side effects, offers similar benefits. The semi-finished product finds applicability in the field of production processes and in the production of products aimed at enhancing the physical and cognitive performance, as well as the health status of individuals. For this reason, the semi-finished product can generate a wide range of products, varying the composition of beverages and other compounds in which the active ingredient is inserted .

[0022] The present invention introduces a product with dosages optimized for human consumption. In fact, the use of a production process different from the canonical one ensures the stability of the semi-finished product. Specifically, the methodology adopted allows the development of a product which not only gives tangible benefits, but also demonstrates greater applicability and stability, thereby amplifying the ergogenic effects. Composition : In accordance with the first object, the present innovation describes a composition comprising:

[0023] 1. Withania somnifera (Ashwagandha) .

[0024] 2. Ginkgo biloba.

[0025] 3. Ocimum tenuiflorum (Tulsi or Holy Basil) .

[0026] 4. Avena sativa.

[0027] For the purposes of the present invention, Withania somnifera is employed as a root.

[0028] Withania somnifera root, also known as Ashwagandha (or Indian ginseng) , contains withanolides, withaferins and whitanosides , which compounds have shown different beneficial effects in the cognitive sphere. Relevant in vitro, in vivo and clinical investigations have demonstrated potent bioactivity of W. somnifera extracts against stress, anxiety and fatigue. The cardioprotective and cardiotropic properties of root extracts are also known, in addition to those related to the improvement of sleep and brain functions.

[0029] For the purposes of the present invention, Avena sativa is used as seeds.

[0030] Avena sativa is an immature oat (harvested when still green) , containing avenacosides , avenacides, and avenanthramides . In particular, the benefits are linked to one of the most important functional components of oats, p-glucan, a soluble dietary fiber, which has physiological effects on improving cognitive functions, especially in terms of increasing memory, and improving mood.

[0031] For the purposes of the present invention, Ginko biloba is used as leaves. The Ginkgo biloba plant contains terpenes (such as ginkgolides and bilobalides ) , which have shown different beneficial effects on the cognitive sphere (improves blood circulation to the brain, reducing memory disorders, headaches, difficulty in concentration) .

[0032] For the purposes of the present invention, Ocimum tenuiflorum is used as leaves.

[0033] Lastly, Ocimum tenuiflorum (also known as Tulsi and / or holy basil) is a plant containing eugenol, essential oils, flavonoids, coumarins and phenolic acids which have demonstrated beneficial effects on the cognitive sphere and also possesses analgesic properties (reduces stress, improves mood, rich in antioxidants, has anti-aging actions, supports the inflammatory system) .

[0034] For the purposes of the present invention, the intermediate product consisting of the four plant components mentioned above will have a D:E ratio (Drug Extract ratio) ranging from 1:2.5 to 1:5.

[0035] The composition of the invention further comprises two components represented by: Lactobacillus acidophilus and

[0036] Lactobacillus rhamnosus . For the purposes of the present invention, both strains are thermally inactivated .

[0037] The Lactobacill us acidophil us strain is a strain of Grampositive lactic acid bacteria belonging to the genus Lactobacillus . It is commonly present in the human gastrointestinal tract , mainly in the small intestine and colon where it plays a fundamental role in the health of the gastrointestinal tract .

[0038] Lactobacill us rhamnosus is a strain of Gram-positive lactic acid bacteria belonging to the genus Lactobacillus .

[0039] To the interest of the present invention, both bacterial strains used are heat treated and inactivated, thus allowing the intrinsic beneficial features to be kept , obtaining however a stable product under all possible conditions present in the world of beverages and food ( such as pH, temperature and interactions with other substances ) .

[0040] For the purposes of the present invention, the lactic acid bacteria are employed in a quantity of about 1-20 billion CFU per dose for both Lactobacill us acidophil us and Lactobacill us rhamnosus .

[0041] The quantity of lactobacilli is constant and equal in each composition of the invention . The formulation of the present invention further comprises one or more of the further components selected from : inulin, arable gum, and silica dioxide .

[0042] Inulin is derived from p-D- fructose and it is a carbohydrate polymer with a lower molecular weight than starch, the monomers of which are linked by p-2 , 1 glycosidic bonds . It is usual ly present in Jerusalem artichoke tubers , chicory, salsi fy roots and agave plant roots . In the present invention, in addition to the binding properties , it also helps with the fluidity and stability of the preparation, and in combination with the bacterial strains , it allows of fering a product , which brings a complete benefit to the intestine . Moreover, since it is a water- soluble fiber, it plays a functional and physiological role , also providing benefits at the intestinal level .

[0043] The aggregating properties of inulin are given by the branched chemical structure ( Fig . 2 ) which make it insoluble in ethyl alcohol ( the solvent forming the tincture ) . For the purposes of the present invention, there is used inulin having a molecular weight of 1800-3000 g / mol

[0044] Regarding arabl e gum (molecular weight of arable gum is 600- l O O Oxl O3g / mol ) also known as acacia gum, char gum, char goond or meska, it is a natural gum obtained from the hardened resin of acacia trees . Aarabic gum is edible and has features similar to those of glue . It essentially consists of a long-chain branched polysaccharide ( consi sting of L-arabinose , D- galactose , L-rhamnose and D-glucuronic acid) and alkaline earth metal and alkali metal salts . Arabic gum is mainly used in the food industry, for example as a stabili zer, emulsi fier or thickener, and it is an important ingredient in the formulation of syrups for soft drinks and "hard" gummies . In the case of the aforesaid invention, arable gum mainly plays the role of binder and stabili zer . By virtue of these features , it is possible to improve the compactness and stability of the preparation at issue , thus obtaining a product which is less sensitive to moisture and with better and longer conservation . The properties of arable gum, due to the branched molecular structure , make it insoluble in ethyl alcohol and promote the aggregation of particles during the drying step . Moreover, the viscoelastic properties of this component allow the formation of a matrix , which adheres to the active product particles , improving its cohesion . At the same time , the ability of arable gum to absorb moisture prevents agglomeration, avoiding the destabili zation of the active ingredient during the storage period .

[0045] A further advantage in the use o f arable gum is its power as a masking agent , since by virtue of its intrinsic properties , the invention is capable of of fering a product which has no bitter notes , and therefore its application is simpler and better defined within the beverage and food field, in fact a use of such components would not allow the product to have a balanced and pleasant taste due to the very strong and bitter tastes of the components forming the product.

[0046] Lastly, silica dioxide is an anti-caking agent, used to prevent particle aggregation due to moisture. Silica dioxide prevents particles which are exposed to moisture from sticking together due to bonds with water molecules.

[0047] The present invention describes the formulation of the invention for preparing a beverage, a tincture, a syrup, soft drinks, plant-based beverages.

[0048] The present invention discloses the formulation of the invention for preparing food selected from the group comprising:

[0049] - bread and bakery products: bread, cookies, breadsticks, crackers , etc . ;

[0050] - dairy products: cheeses, yogurts, puddings, chocolates, etc . ;

[0051] - desserts and sweets: candies, chewing gums, spreadable creams, "energy" bars (for recovery during sports activities or activities characterized by intense physical or mental effort) , snacks, ice creams, etc.;

[0052] - preserves: jams, jellies, etc.

[0053] Production process

[0054] In the third object, there is disclosed the processing process which leads to the creation of a stable product, applicable to different fields such as "food & beverage," nutraceuticals and food supplements, while being capable of benefiting the gastrointestinal well-being. Such a process has been carefully studied to make the product stable, to reduce the possibility of contamination and to improve the handling of intermediate products .

[0055] The production process comprises the following steps:

[0056] - Cold maceration: Cold maceration is a refined process, widely used for the extraction of desired compounds from plant material, including herbs, and other ingredients. This technique involves the use of low or ambient temperatures and is divided into several key steps, offering an effective overview of the operation thereof. It starts with a scrupulous selection of ingredients to macerate, which can encompass a wide range of elements, including herbaceous aromas, and other components rich in essential oils, fragrances, pigments, and other components. To maximize the extraction efficiency, the ingredients are prepared through a thorough cleaning, cutting and crushing, increasing the contact area between the plant material and the extractor liquid. The prepared ingredients are placed inside a suitable container, such as a glass jar or stainless steel container. The extractor liquid, consisting of ethanol and water, is poured over the ingredients. Cold maceration is characteri zed by the use of ambient or very low temperatures to preserve volatile and heatsensitive aromatic compounds , ensuring the maximum integrity of the aromas . The duration of the maceration process can vary widely according to the ingredients used and the speci fic targets , and can extend for weeks or even months .

[0057] During the maceration step, it is possible to stir or periodically mix the contents so as to ensure a uni form distribution of the extracted compounds . At the end of the maceration, the extracted liquid is subj ected to a filtration process so as to eliminate any solids or residues of the ingredients , obtaining an extracted liquid which contains the aromas , colors and above all the active ingredients of the selected plants .

[0058] The extracted liquid obtained can be used in various applications , including the preparation of products in the Food & Beverage field . Cold maceration stands as a versatile and sophisticated technique , which allows obtaining intense and natural aromas from fresh ingredients , contributing to confer a distinctive and refined note to the flavors of food and beverages .

[0059] - Spray-drying : The spray-drying process is a fundamental and widely adopted method of trans forming a liquid into a solid form, in the form of small particles or powder . This technique is employed in various industrial fields , such as food, pharmaceutical and chemical , to produce a wide range of products .

[0060] The basic process develops through several interconnected steps . Initially, there starts from a liquid to be dried, which can be a solution, in this case a tincture containing the active substances of the selected plants .

[0061] The liquid is then sent to a spraying device , where it is trans formed into small drops , through the use of high- pressure noz zles or rotating discs . The result of this step is a "nebula" of fine liquid droplets , ready for the next step .

[0062] The sprayed drops are introduced into a drying chamber, where they are hit by a stream of hot air, usually air . This hot air has the task of vaporizing the moisture contained in the drops , removing it and leaving only the solid . This occurs quickly and at relatively low temperatures , minimi zing the risk of damaging the heatsensitive substances present in the product .

[0063] As the water evaporates from the drops , they turn into solid particles or powder . The particle si ze and shape can vary based on speci fic process settings and end product requirements . Lastly, the solid particles or the powdered product are collected in the lower part of the drying chamber. This is the finished form of the product, which can be further processed or packaged for use or sale.

[0064] The spray drying process is particularly appreciated for the ability to obtain dry products, finely divided and easy to be handled starting from liquids or suspensions. It is an ideal method for heat-sensitive products, as the drying occurs quickly and at low temperatures. Moreover, it allows an accurate control over particle size and ensures uniform distribution of solids in the finished product, making it an essential process in several manufacturing industries.

[0065] These existing processes havethen been customized to define a production process which enhanced the chemical-physical and organoleptic features of the product:

[0066] 1. Raw material quality check.

[0067] 2. Plant maceration.

[0068] 3. Pressing solid residues.

[0069] 4. Separating the solid component from the liquid one.

[0070] 5. Fluid bed spray-drying with the addition of technological adjuvants and lactobacilli.

[0071] 6. Drying and sedimentation of powder for collection.

[0072] 7. Sieving to avoid agglomerations with dimensions greater than 1 mm. Adding silica dioxide The production process starts with an accurate selection of the plants based on a first visual check to assess whether parameters such as color, si ze , leaf strength and plant age reflect the set standards . Once such parameters have been determined (which are of fundamental importance to understand the state of health of a plant ) , it is proceeded with the elimination of impurities and / or parts not necessary for producing a stock tincture . For the purposes of the product in hand, roots , leaves and seeds of Wi thania somnif ra, shells and fibrous parts of Avena sa ti va, woody parts of Ginkgo bil oba stems o f Ocimum tenuifl orum) are used .

[0073] The four plant components listed above are present in equal amounts ( 25% by weight each) . The aforementioned parts are then inserted into a maceration tank containing a hydroalcoholic solution with a degree varying from 50 ° to 80 ° . The choice to use a hydroalcoholic solution was decided after a careful study of the chemical properties of the active components ( ginkgolides , eugenol , avenacosides , avenacids , withanolides and whitanosides ) , which are not soluble in water . The alcohol was carefully selected after conducting production tests in small batches to understand the correct alcohol content to have an optimal extraction of all the ingredients . A 50% hydroalcoholic solution represents the lowest possible ideal percentage for high production ef ficiency .

[0074] The maceration process occurs cold . The heat , normally used to increase the solubility of the compounds , would modi fy the organoleptic and chemical-physical properties of the product of this invention . The plants and the solution are left to macerate for a time ranging from two to four weeks . Once the maceration period is over, the solid organic matrix is subj ected to a mechanical process known as pressing to complete the extraction of the active ingredients . The solid organic component can be subj ected to a double press ing, in which the matrix is , following the first pressing, inserted into the maceration tank again for a variable period . Following the second maceration period, which allows extracting further active substances , the second mechanical pressing process is carried out . The solution is then filtered to remove impurities and separate the processing waste from the product of interest . The two components thus obtained are the stock tincture

[0075] ( liquid part ) and the spent organic material ( solid part ) . Once the filtration is complete, a tincture based on

[0076] Withania somnifera (Ashwagandha or Indian ginseng) , Ginkgo biloba Avena sativa and Ocimum tenuiflorum (Tulsi or holy basil) is obtained. With a total Drug-Extract ratio (D:E) between 1:2 and 1:10, it is possible to ensure a very high degree of purity and concentration of the active ingredients. This range allows an excellent balance, avoiding problems of under-saturation or over-saturation which could affect the stability of the tincture and the subsequent production steps. The spent organic material will be added to the waste material resulting from cleaning the plants. The technological adjuvants inulin and arable gum (or acacia fiber) are inserted at the base of a fluid bed dryer with a ratio varying between 1:0.5 and 1:2. In the same step, the two bacterial strains Lactobacillus acidophilus and Lactobacillus rhamnosus are also inserted into the fluid bed chamber with the dosages mentioned above.

[0077] Once the supports are positioned inside the fluid bed, parameters such as temperature and air flow are meticulously adjusted. This allows ensuring precise control over the space in which the supports must be evenly and efficiently distributed. After identifying and setting the optimal parameters for the supports present, there proceeds with the preparation of the predetermined tincture dosage, which will be sprayed on arable gum and inulin with a tincture : support ratio ranging from 1:0.5 to 1:2.

[0078] The temperature allows alcohol and water to evaporate, leaving only the active components of the product, thus ensuring drying and the pre-set parameters. By virtue of a careful selection of components, we are able to spray a virtually unlimited concentration of the tincture, using a main adjuvant insoluble in ethanol and solvents, but soluble in water.

[0079] This careful choice provides excellent flexibility to tailor the product based on specific customer requests, ensuring a precise and tailor-made response to different needs . When the desired amount sprayed on the supports is reached, the air flow and temperature are gradually reduced, and then turned off. This will allow the powder to settle at the base of the fluid bed and then be collected and divided into bags . The product is then sieved through a sieve with holes 1 mm in size to prevent any aggregates from exceeding such a maximum size. This step is of fundamental importance since it allows obtaining a more homogeneous powder product in terms of size .

[0080] 8 . After that , a percentage of silica dioxide will be introduced to the product to improve the stability and moisture resistance thereof .

[0081] The production process described of fers advantages in terms of stability and applications of use of products which otherwise could not be used except with large losses of active components , thus with a huge stability problem .

[0082] The formulation described of fers qualitative advantages by virtue of the extraction method of the active ingredients from the plants taken into consideration, to avoid under and / or overdosing, which in the first case would not benefit the customer, while in the second case would lead to generating side ef fects .

[0083] The raw material s used can be made using "bio" products , i . e . , obtained from agriculture which applies organic principles according to current regulations .

[0084] The production process described allows a better solubility in liquids with temperatures greater than or equal to 40 ° C .

[0085] The production process , designed to achieve greater ef ficiency, allows more active ingredient to be extracted from a smaller amount of raw material . The semi- finished product obtained is thus present at high concentrations , ensuring reduced dosages in di f ferent applications . Moreover, since the ranges of normal use of the compounds characteri zing the product are wide , based on the application and daily consumption, it is possible to vary the dosages based on the di f ferent final products .

[0086] The amount of formulation which can be taken daily is preferably between 250 and 1000 mg . By virtue of the use of ethanol- insoluble and water-soluble supports , the spray drying process allows spraying a virtually unlimited amount of tincture on the selected adj uvants , avoiding problems such as premature aggregation of the product .

[0087] The use of inulin, arable gum and silica dioxide allows improving the solubility, storage and moisture resistance of the components of the semi- finished product which are otherwise di f ficult to use in " Food & beverage" products .

[0088] In a further obj ect , the use of the composition or formulation of the invention is described, as a substitute for caf feine- based products .

[0089] In a still further obj ect, the use of the composition or formulation of the invention for positively modulating the health of the gastrointestinal tract by optimi zing digestive functions and promoting intestinal microbial balance is described . We would like to express our sincere gratitude to Mr. Carlo

[0090] Longari . His expertise contributed to the collection and analysis of data useful for the creation of the product.

Claims

1. A composition comprising:Withania somnifera- Ginkgo biloba- Ocimum tenuiflorum- Avena sativa- heat-treated Lactobacillus acidophilus- heat-treated Lactobacillus rhamnosus .

2. A formulation comprising the composition according to the preceding claim, further comprising one or more from: inulin, arable gum, silica dioxide.

3. A formulation according to the preceding claim for preparing a beverage, a tincture, a syrup, soft drinks, plantbased beverages.

4. A formulation according to claim 2 or 3 for preparing food selected from the group comprising:- bread and bakery products: bread, cookies, breadsticks, crackers , etc . ;- dairy products: cheeses, yogurts, puddings, chocolates, etc . ;- desserts and sweets: candies, chewing gums, spreadable creams, "energy" bars (for recovery during sports activities or activities characterized by intense physical or mental effort) , snacks, ice creams, etc.;- preserves: jams, jellies, etc.

5. A process for preparing the formulation according to any one of claims 2 to 4, comprising the steps of:cold-macerating the plant components: Withania somnifera, Ginkgo biloba, Ocimum tenuiflorum and Avena sativa,- pressing the solid residue,- separating the solid component from the liquid one,- spray-drying with added inulin and arable gum,- adding Lactobacillus acidophilus and Lactobacillus rhamnosus ,- sieving,- adding silica dioxide.

6. A process according to the preceding claim, wherein the spray-drying step is carried out on a fluid bed.

7. Use of a composition according to claim 1 or a formulation according to any one of claims 2 to 4, as a substitute for caffeine-based products.

8. Use of a composition according to claim 1 or a formulation according to any one of claims 2 to 4, for positively modulating the health of the gastrointestinal tract by optimizing digestive functions and promoting intestinal microbial balance.