Oral composition comprising gymnema sylvestre liquid extract and the use thereof

Abstract

The subject matter of the invention is an oral composition comprising a Gymnema sylvestre liquid extract characterised in that the Drug Extract Ratio (DER, the ratio of the amount of plant material to the amount of the obtained extract) is from 1:3 to 1:5, wherein the composition is in the form of an aerosol and is sprayed with an atomizer. The invention also relates to the use of the composition according to the invention for the topical blocking of taste receptors.

Description

Description Title of Invention: Oral composition comprising Gymnema sylvestre liquid extract and the use thereof

[0001] The present invention relates to an oral composition comprising a Gymnema sylvestre liquid extract that blocks sweet taste receptors, and its use in blood sugar elimination and body weight control.Technical Field

[0002] Gymnema sylvestre is a woody climbing plant originating from India, Africa, and China, known for its potential anti-diabetic effects, and gymnemic acids are the main bioactive components of this plant species. Gymnemic acid is a dietary supplement sold worldwide, mainly in the form of capsules, soluble tablets or lozenges. Gymnemic acids selectively and temporarily suppress taste responses to sweet compounds without affecting the perception of other taste elements (salty, sour, bitter and umami) when applied directly to the oral cavity by blocking the taste buds responsible for sweet taste that are present on the tongue and palate. The sweet taste suppressing effect of gymnemic acids is transient and usually lasts from 30 to 60 minutes. However, the use of products comprising gymnemic acid in the form of capsules, soluble tablets or lozenges does not reduce the sweet taste perception at all or to an adequate extent.Background Art

[0003] In the state of the art, dietary supplements comprising gymnemic acid are known, which block the perception of sweet taste.

[0004] CN109745359A discloses a composition, the main ingredient of which is Gymnema sylvestre, which allows maintaining sugar balance in the blood, preventing diabetes mellitus and its complications.

[0005] EP4203897A1 discloses an oral care composition, which comprising, e.g., a source of zinc ions and an herbal extract including Gymnema sylvestre.

[0006] EP3154518A2 discloses a composition of gymnemic acid and at least one form of zinc. The composition is administered orally to block sweet taste receptors in the oral cavity.

[0007] W003061679A1 discloses a preparation that comprises herbs, minerals and vitamins to reduce insulin resistance and blood sugar level.

[0008] In addition, compositions masking other flavours, e.g. bitter, are known in the state of the art. PL / EP 2243473 discloses tablets comprising at least one bitter-tasting pharmaceutically active compound and at least one zinc salt.

[0009] However, in the state of the art, there is no oral composition comprising Gymnema sylvestre extract that provides a topical effect of a complete absence of perception of the sweet taste of consumed foods for a specific period.Technical Problem

[0010] The object of the present invention is to provide an oral composition comprising a Gymnema sylvestre liquid extract, which provides the effect of a complete absence of perception of the sweet taste as a result of local blocking of taste receptors by covering the relevant surface of the oral cavity, including the tongue, where the taste buds responsible for sweet taste are located.

[0011] Thus, the object of the invention is to reduce the perception of the sweet taste of consumed foods and to suppress appetite. A further object is to promote body weight control, maintain normal blood glucose level and limit the caloric value of food intake. As a result, the composition according to the invention allows, at the level of mental therapy, to facilitate the withdrawal of the consumption of sweet-tasting foods.

[0012] The above problems are solved by the present invention.Summary of Invention

[0013] The subject matter of the invention is an oral composition comprising a Gymnema sylvestre liquid extract characterised in that the Drug Extract Ratio (DER, the ratio of the amount of plant material to the amount of the obtained extract) is from 1:3 to 1:5, wherein the composition is in the form of an aerosol and is sprayed with an atomizer.

[0014] Preferably, the subject matter is a composition according to the invention characterised in that the atomizer sprays from 0.1 mL to 0.2 mL of the Gymnema sylvestre liquid extract at a time.

[0015] Preferably, the subject matter is a composition according to the invention characterised in that the atomizer has an aerosol-releasing aperture diameter ranging from 0.28 mm to 0.3 mm.

[0016] Preferably, the subject matter is a composition according to the invention characterised in that it further comprises lactisol.

[0017] Preferably, the subject matter is a composition according to the invention characterised in that it further comprises zinc ions in the form of a compound selected from the group including zinc acetate, zinc carbonate, zinc chloride, zinc citrate, zinc gluconate, zinc sulphate, zinc bisulphite, zinc oxide, zinc halide, zinc hydride, zinc carbide and combination thereof.

[0018] Preferably, the subject matter is a composition according to the invention characterised in that the DER is 1:5.

[0019] The subject matter is also a composition according to the invention for the use of local blocking of taste receptors, the administration being a topical administration into the oral cavity of an individual.

[0020] Preferably, the composition is administered for a period of no more than 1 min before meal consumption.

[0021] Preferably, a single dose of the composition comprises 0.2 to 0.4 mL of a Gymnema sylvestre liquid extract with the DER of 1:5.

[0022] Preferably, the composition is administered at least three times a day, for a period of at least one month, with a monthly dose of the Gymnema sylvestre liquid extract with the DER of 1:5 of at least 27 mL.

[0023] Preferably, the composition is administered for the prevention or treatment of a condition or disorder selected from the group including appetite suppression, promotion of body weight control, maintenance of normal blood glucose level or limitation of the caloric value of food intake.Advantageous Effects of Invention

[0024] The composition according to the invention makes it possible to eliminate sugar from the diet and to reduce body weight level on a systemic and psychological level. Systemic action should be understood as reducing and maintaining a constant level of blood glucose. The psychological action consists of reducing the consumption of sugar by reducing the snacking of products comprising it, in particular sweets. After using the composition according to the invention, the individual associates sugar-comprising products as a tasteless, non-tasty product.

[0025] Furthermore, the composition according to the invention makes it possible to suppress appetite, promote body weight control, maintain normal blood glucose level and limit the caloric value of food intake.Description of Embodiments

[0026] The oral composition according to the invention comprises a liquid extract from the leaves of Gymnema sylvestre (Gymnema sylvestre Folium). The gymnemic acids comprised in Gymnema sylvestre are the active substances of the composition according to the invention. The gymnemic acids comprised in Gymnema sylvestre will be referred to interchangeably hereafter as "gymnemic acid" or "gymnemic acids".

[0027] The ratio of the amount of plant raw material to the amount of the resulting plant preparation (DER, Drug Extract Ratio) ranging from 1:3 to 1:5, preferably 1:5. By plant raw material is meant the leaves of Gymnema sylvestre (Gymnema sylvestre Folium) and the plant preparation is the aqueous-glycol extract of Gymnema sylvestre leaves comprising gymnemic acids. The aqueous-glycol extract is produced in a multi- step process, subjected to a temperature regime by macerating the freshly obtainedraw material several times, centrifuging and decanting. This ratio of the composition according to the invention provides its appropriate effect at the point, local blocking of the sweet taste during the foods consumption distinguished by a sweet taste.

[0028] As used herein, the term "foods distinguished by their sweet taste" "sweet- tasting foods" or "sweet foods" means any food that is intended for consumption and is consumed orally by an individual, e.g. foods, foodstuff, meals, drinks and all other analogous and synonymous terms related thereto and characterised by a sweet taste perceived by the individual. Typically, sweet food is characterised by a high content of sugars.

[0029] As used herein, the term "individual" refers to individuals in the animal kingdom (according to taxonomy). Preferably, an individual is a human.

[0030] The oral composition according to the invention is in the form of an aerosol and is sprayed using an atomizer, which ensures adequate contact of gymnemic acid with the taste buds not provided by other forms of administration such as capsules, soluble tablets or lozenges. The atomizer sprays from 0.1 mL to 0.2 mL of liquid Gymnema sylvestre extract at a time, preferably 0.15 mL. This form and scope of application ensures coverage of the relevant surface of the tongue, where the taste buds responsible for the perception of sweet taste are located. The atomizer, which sprays the composition according to the invention, has an aerosol-releasing aperture diameter ranging from 0.28 mm to 0.3 mm.

[0031] The composition of another embodiment of the invention further comprises lactisol. Lactisol is the sodium salt and commonly supplied form of 2-(4- methoxyphenoxy)propionic acid, a natural carboxylic acid found in roasted coffee beans. 5 mM lactisol is added to the composition according to the invention.

[0032] The composition of another embodiment of the invention comprises 5 mM lactisol and 27 mL Gymnema sylvestre liquid extract with the DER of 1:5. Lactisol in combination with gymnemic acid causes a synergistic sweet taste inhibiting effect.

[0033] In another embodiment, the composition according to the invention further comprises zinc ions in the form of a compound selected from the group including zinc acetate, zinc carbonate, zinc chloride, zinc citrate, zinc gluconate, zinc sulphate, zinc bisulphite, zinc oxide, zinc halide, zinc hydride, zinc carbide and combinations thereof. A preferred source of zinc is zinc chloride. 0.64 g of a zinc source, preferably zinc chloride, is added to the composition according to the invention in the form of an aqueous solution.

[0034] The composition of another embodiment of the invention comprises 0.64 g of zinc chloride in the form of an aqueous solution (5 mL) and 25 mL of a Gymnema sylvestre liquid extract with the DER of 1:5. The zinc ions block the bitter taste of gymnema acid, improving the palatability of the composition according to the invention.

[0035] In another embodiment, the composition according to the invention simultaneously comprises 25 mL of Gymnema sylvestre liquid extract with the DER of 1:5, 5 mM lactisol and 0.64 g of zinc chloride in the form of an aqueous solution (5 mL).

[0036] The composition according to the invention is administered topically into the oral cavity of an individual for a period of no more than 1 min before the consumption of a sweet-tasting meal.

[0037] A single dose of the composition according to the invention is from 0.2 to 0.4 mL, preferably 0.3 mL. The dose is provided by pressing the atomizer twice. Thus, the desired effect is achieved, a local blocking of the taste buds responsible for the sweet taste for a period of time of about 30-40 minutes. Thanks to this period of action, taste receptors are blocked during the period of so-called hypoglycaemia, when the individual has an urge to consume sweet foods, e.g. sweets. Hypoglycaemia refers to a state in which the amount of glucose in the blood falls below 70 mg per decilitre and manifests itself, inter alia, by increased hunger, especially associated with sweet foods.

[0038] The composition according to the invention is administered from once a day to 5 times a day, preferably three times a day, for a period of at least one week to four weeks, preferably four weeks.

[0039] In another embodiment, the daily dose of Gymnema sylvestre liquid extract with the DER of 1:5 is 0.9 mL, and the monthly dose is 27 mL.

[0040] All technical and scientific terms used herein have a meaning as commonly understood by a person skilled in the art.

[0041] A person skilled in the art will understand that the elements included in this description constitute non-limiting variant embodiments of the present invention, the scope of which is defined by the claims. The features described concerning one embodiment may be combined with those of other embodiments to the extent that such features are compatible and not alternative. The scope of the present invention includes such modifications and variations.

[0042] Example embodiments of the invention are discussed below to outline the principles of composition and use disclosed herein. References used in the description correspond to the references shown in the examples.Examples

[0043] Example 1

[0044] The oral composition according to the invention comprises a Gymnema sylvestre liquid extract from leaves (Gymnema sylvestre Folium).

[0045] The extract is obtained from the plant raw material, which is the leaves of Gymnema sylvestre (Gymnema sylvestre Folium). The solvents used for extraction are water and glycol (e.g. propylene glycol). The water-glycol extract is produced in a multi-stage process subjected to a temperature regime by macerating the freshly obtained raw material several times, centrifuging and decanting. The extract is a so-called plant processor, where the DER is 1:5 (raw material to processor ratio).

[0046] The resulting extract comprises gymnemic acids as active substances.

[0047] Example 2

[0048] The technical effect of the compositions according to the invention is confirmed by a comparative study of the composition according to the invention with an Apetiblock lozenge comprising 50 mg of Gymnema Sylvestre extract. Both compositions comprise gymnemic acid. The study is carried out concerning the effect related to local sweet taste blocking.

[0049] The study involves 16 individuals who are divided into 2 groups of 8 individuals each.

[0050] The first group is administered the composition according to the invention resulted in Example 1, which comprises a Gymnema sylvestre liquid extract in a quantitative Drug Extract Ratio (DER, the ratio of the amount of plant material to the amount of the obtained extract) of 1:5.

[0051] The composition administered according to the invention has the following parameters:

[0052] a) is in the form of an aerosol applied topically by spraying the composition twice into the oral cavity of the individual,

[0053] b) a single atomization of the composition with the atomizer generates a dose of 0.15 mL, which means that the single dose resulting from two atomizations occurring one after the other is a total of 0.3 mL of the composition according to the invention,

[0054] c) the atomizer used to spray the composition has an aerosol-releasing aperture diameter ranging from 0.28 mm to 0.3 mm.

[0055] The Apetiblock lozenge administered has the following composition:

[0056] a) Gymnema sylvestre extract 50 mg,

[0057] b) Garcinia cambogia extract 50 mg including 30 mg hydroxycitric acid,

[0058] c) chromium 40 pg.

[0059] The composition and the Apetiblock lozenge are administered to both groups of individuals 1 min before the consumption of a meal showing a sweet taste, e.g. comprising sugars. The meal is sugar (commercially available White Crystal Sugar, Diamant) at 5 g (teaspoon).

[0060] After this, the individuals take the said meal and, after completion of consumption, they assess the extent of their sweet taste perception through a questionnaire.

[0061] The assessment takes place immediately after the meal and 30 minutes after consumption.

[0062] The results obtained are shown in Table 1, with individuals from 1 to 8 being administered the composition according to the invention and individuals from 9 to 16 being administered the Apetiblock tablet. The effect was evaluated using a rating scale of 0-10, where 0 means no sweet taste perception at all and 10 means full sweet taste perception (i.e. no effect of the substance administered).

[0063] [Table 1]

[0064] The data obtained show that the composition according to the invention exhibits an effect related to the effective blocking of taste buds responsible for sweet taste, and located on the tongue. 5 out of 8 individuals from the group taking the composition according to the invention stated that they did not completely feel the sweet taste 1 minute after administration of the invention. The average score was 0.5. This effect persisted for at least 30 min after meal consumption (i.e. about 31 min afterapplication of the composition according to the invention). In comparison, none of the individuals in the group taking the Apetiblock tablet rated the taste blocking as 0, i.e. each individual perceived a sweet taste to a high degree. The average score was 8.75. This means that the composition according to the invention blocks the perception of sweet taste significantly more than the Apetiblock tablet.

[0065] The characteristics of the developed composition according to the invention make it possible to realize the indicated effect, as it makes it possible to cover the relevant surface of the oral cavity, including the tongue, where the taste buds responsible for the sweet taste are located. The composition makes it possible to block the taste buds for a period of time of at least 30 minutes. Thanks to this duration of action, taste receptors are blocked during the period of so-called hypoglycaemia, when the individual perceives the greatest need associated with the consumption of sweet foods (e.g. sweets, sweet drinks, etc.). Such a blockade of the taste buds thus offers the possibility of using the composition according to the invention for the prevention or treatment of a condition or disorder selected from the group comprising appetite suppression, promotion of body weight control, maintenance of normal blood glucose level or limitation of the caloric value of food intake.

[0066] In contrast to the composition according to the invention, the Apetiblock tablet does not effectively block the perception of sweet taste. It is alleged that this is because the form of the lozenge does not provide the free form of gymnemic acid in a suitable concentration and environment, and does not effectively cover the part of the tongue where the taste buds for sweet taste are located, and ultimately the taste buds themselves.

[0067] Example 3

[0068] The composition according to the invention and the Apetiblock tablet are administered at least three times a day (before meal consumption) for a period of 1 month. The monthly dose of the Gymnema sylvestre liquid extract with DER 1:5 comprised in the composition according to the invention is at least 27 mL. The monthly dose of gymnemic acid in the Apetiblock tablet is 4500 mg. Individuals are instructed not to change their dietary and lifestyle habits during the study.

[0069] After a period of 1 month, individuals in the group taking the composition according to the invention showed an average body weight loss of 2.1 kg (compared to their prestudy body weight). In contrast, no body weight loss was observed among individuals in the group taking the Apetiblock tablet (the difference was statistically omitted).

[0070] An additional effect in the group taking the composition according to the invention was the effect of remembering the unpleasant taste (taste deprived of the sweet taste) of sugar-comprising products, mainly sweets, chocolate or cola and other sugar- comprising carbonated drinks, which resulted in a partial or complete withdrawal ofthese products from their diet. This effect was described by trial participants as a break in their addiction to sugar and sugar-comprising products.

[0071] The above effect was not observed in the group taking the Apetiblock lozenge.

Claims

Claims

1. An oral composition comprising a Gymnema sylvestre liquid extract, characterised in that the Drug Extract Ratio (DER) is from 1:3 to 1:5, wherein the composition is in the form of an aerosol and is sprayed with an atomizer.

2. The composition according to claim 1, characterized in that the atomizer sprays from 0.1 mL to 0.2 mL of the Gymnema sylvestre liquid extract at a time.

3. The composition according to claim 1, characterised in that the atomizer has an aerosol-releasing aperture diameter ranging from 0.28 mm to 0.3 mm.

4. The composition according to claim 1, characterised in that it further comprises lactisol.

5. The composition according to claims 1 or 4, characterised in that it further comprises zinc ions in the form of a compound selected from the group of zinc acetate, zinc carbonate, zinc chloride, zinc citrate, zinc gluconate, zinc sulphate, zinc bisulphite, zinc oxide, zinc halide, zinc hydride, zinc carbide and combination thereof.

6. The composition according to claim 1, characterised in that theDER is 1:5.

7. The composition according to claims 1 to 6, for the use of local blocking of taste receptors, the administration being a topical administration into the oral cavity of an individual.

8. The composition for the use according to claim 7, wherein the composition is administered for a period of no more than 1 min before meal consumption.

9. The composition for the use according to claims 7 or 8, wherein a single dose of the composition comprises 0.2 to 0.4 mL of a Gymnema sylvestre liquid extract with the DER of 1:5.

10. The composition for the use according to claims 7 to 9, wherein the composition is administered at least three times a day, for a period of at least one month, with a monthly dose of the Gymnema sylvestre liquid extract with a DER of 1:5 of at least 27 mL.

11. The composition for the use according to claims 7 to 10, wherein the composition is administered for the prevention or treatment ofa condition or disorder selected from the group including appetite suppression, promotion of body weight control, maintenance of normal blood glucose level or limitation of the caloric value of food intake.

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