A composition comprising a disaccharide derived from the enzymatic conversion of methylxanthine and sucrose

Abstract

The present invention discloses a composition comprising a methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose. More specifically, the present invention discloses a composition comprising a methylxanthine and a disaccharide derived from the enzymatic conversion of sucrose selected from turanose, leucrose, trehalulose and isomaltulose or a combination thereof.

Description

Technical Field

[0001] The present invention relates to a composition comprising a methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose. More particularly, the present invention relates to a composition comprising a methylxanthine and a disaccharide derived from the enzymatic conversion of sucrose selected from or a combination of turanose, leucrose, trehalulose and isomaltulose.

Background Art

[0002] Methylated xanthines are components of foods, beverages and dietary supplements and are produced by a limited number of plant species including tea (Camellia sinensis L, C. assamica var. kucha (green tea)), coffee (e.g. Coffea arabica, C. liberica, C. dewevrei, C. abeokut), cocoa (Theobroma cacao L.), Cola (e.g. Cola nitida), Paullinia (e.g. Paullinia cupana) and Ilex (e.g. Ilex paraguariensis).

[0003] Natural products containing methylxanthines are frequently used in the food industry as dietary supplements, functional foods or nutraceuticals as a direct result of their function of improving long-term sustainability and increase of energy, mood and concentration, improving memory, cognitive improvement, mind-muscle connection, performance improvement, better vigilance and increasing fat burning power.

[0004] The pharmacological activity of methylxanthine at the cellular level is thought to be due to its functions of blocking the binding of the neurotransmitter adenosine to receptors in the brain, inhibiting phosphodiesterase enzymes, blocking dopamine transporter proteins, modulating GABA receptor action, and regulating intracellular calcium levels.

[0005] Methylxanthine is also known to act as a stimulant and a powerful bronchodilator, improving blood flow and preventing uric acid crystallization.

[0006] Although some dietary supplements containing methylxanthine are available, there is a need to develop a composition containing methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose, thereby providing an immediate, delayed, or sustained-release long-term energy booster that improves mood, concentration, memory, alertness, cognitive function, enhances the mind-muscle connection, improves performance, increases fat-burning power and information processing.

[0007] In addition to the above, it is also important to mask the bitter taste of methylxanthine by developing an appropriate formulation.

[0008] Therefore, it is an object of the present invention to provide a composition containing methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose, selected from turanose, leucrose, trehalulose, and isomaltulose or mixtures thereof, so as to mask the bitter taste of methylxanthine.

Summary of the Invention

Means for Solving the Problems

[0009] Accordingly, the present invention provides a composition comprising methylxanthine in an amount of 0.01% - 20% w / w and a disaccharide derived from the enzymatic conversion of sucrose in an amount of 10% - 90% w / w.

[0010] In one aspect, the methylxanthine is selected from caffeine, theacrine, and methylribelin, paraxanthine, theobromine, theophylline alone or in combination thereof in an amount of 0.01% to 20% w / w.

[0011] In another aspect, the disaccharide derived from the enzymatic conversion of sucrose is selected from the group consisting of turanose, leucrose, trehalulose, and isomaltulose alone or in combination thereof in an amount of 10% to 90% w / w.

[0012] In a further aspect, the present invention provides a composition comprising an individual methylxanthine selected from the group consisting of caffeine, theacrine, paraxanthine, theobromine, theophylline, and methylribelin in an amount of 0.01% to 20% w / w, in combination with a disaccharide derived from enzymatically treated sucrose selected from the group consisting of turanose, leucrose, trehalulose, and isomaltulose alone or in combination thereof in an amount of 10% to 90% w / w.

[0013] In another aspect, the composition of the present invention may comprise a functional food supplement such as a stilbenoid selected from resveratrol and pterostilbene present in an amount of 0% to 20% w / w.

[0014] In another aspect, the composition of the present invention may comprise a suitable carrier or additive or nutritional supplement in an amount of 0.01% to 20% w / w.

[0015] In another aspect, the composition of the present invention may comprise a functional additive in an amount of 5% to 90% w / w.

[0016] In yet another aspect, the present invention is a process for the preparation of a composition comprising methylxanthine alone or in combination thereof together with a disaccharide derived from enzymatically treated sucrose, i. adding methylxanthine individually or in combination in an amount of 0.01% to 20% w / w to an aqueous solution of sucrose treated with an enzyme in an amount of 90% to 10% w / w, ii. adding stilbenoids such as pterostilbene and resveratrol to the solution of step (i) in an amount of 0 to 20% w / w, iii. adding a functional additive to the solution of step (ii) in an amount of 5 to 90% w / w, and iv. stirring the solution of step (iii) at room temperature to avoid the thermally induced conversion of sucrose to obtain the desired composition A process is provided that includes the above steps.

[0017] In one aspect, the composition of the present invention can be formulated into various forms of health supplements such as powders, tablets, capsules, gel formulations, water-soluble formulations, etc. containing caffeine, theacrine, and methylrebirn along with various isomers of enzymatically treated sucrose, and can be used as a central nervous system stimulant and a metabolic activator.

Mode for Carrying Out the Invention

[0018] The present invention will now be described in detail in its preferred and optional embodiments so that various aspects can be more clearly understood and correctly recognized.

[0019] Accordingly, the present invention discloses a composition comprising a methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose, wherein the amount of methylxanthine is 0.01% to 20% w / w and the amount of the disaccharide derived from the enzymatic conversion of sucrose is 10% to 90% w / w.

[0020] In yet another embodiment, the methylxanthines are in their pure form or are co-crystals or solvates, and the conformer / solvate is selected from the group including phenol, cinnamic acid, resveratrol, pterostilbene, alcohol, organic acids, etc.

[0021] According to the present invention, methylxanthine is selected from the group consisting of caffeine, theacrine and methylribelin, paraxanthine, theobromine, theophylline or combinations thereof in an amount of 0.01% to 20% w / w.

[0022] In another embodiment, the disaccharide derived from the enzymatic conversion of sucrose is selected from the group consisting of turanose, leucrose, trehalulose and isomaltulose or combinations thereof in an amount of 10% to 90% w / w.

[0023] In yet another embodiment, the present invention provides a composition comprising an individual methylxanthine selected from the group consisting of caffeine, theacrine, paraxanthine, theobromine, theophylline and methylribelin in an amount of 0.01 to 20% w / w, in combination with a disaccharide derived from enzymatically treated sucrose selected from the group consisting of turanose, leucrose, trehalulose and isomaltulose alone or in combination thereof in an amount of 10% to 90% w / w.

[0024] In another embodiment, the composition may comprise a functional food supplement such as a stilbenoid selected from resveratrol and pterostilbene in an amount of 0% to 20% w / w.

[0025] In yet another embodiment, the composition may comprise a suitable carrier or additive or dietary supplement in an amount of 0.01% to 20% w / w.

[0026] In another embodiment, the carrier or additive or dietary supplement is selected from the group consisting of, but not limited to, flavorants, colorants, viscosity modifiers, preservatives, chelating agents, antioxidants, surface modifiers and other dietary supplements alone or in combinations thereof.

[0027] In yet another embodiment, the composition may comprise a functional additive in an amount of 5 to 90% w / w.

[0028] In another embodiment, the functional additive is selected from the group comprising binders, diluents, lubricants, stabilizers, solubilizers, sustained-release polymers, colorants, flavor enhancers and the like.

[0029] In yet another embodiment, the composition optionally comprises a bitterness masking agent.

[0030] In another embodiment, the composition may be formulated to be an oral solid, liquid or suspension.

[0031] In another embodiment, the composition may be formulated for oral administration in various forms of dietary supplements such as powders, tablets, capsules, gel formulations or water-soluble formulations.

[0032] In another embodiment, the composition is provided as a water-soluble composition.

[0033] In another embodiment, the present invention is a process for the preparation of a composition comprising methylxanthine alone or in combination with a disaccharide derived from enzymatically treated sucrose, i. adding methylxanthine individually or in combination in an amount of 0.01% - 20% w / w to an aqueous solution of sucrose treated with an enzyme in an amount of 90 - 10% w / w, ii. adding a stilbenoid such as pterostilbene, resveratrol in an amount of 0 - 20% w / w to the solution of step (i), iii. adding a functional additive in an amount of 5 - 90% w / w to the solution of step (ii), and iv. stirring the solution of step (iii) at room temperature to avoid thermally induced conversion of sucrose to obtain the desired composition A process is provided which comprises.

[0034] In another embodiment, a process for the preparation of a composition comprising methylxanthine alone or in combination with a disaccharide derived from enzymatically treated sucrose, wherein the methylxanthine is selected from the group consisting of caffeine, theacrine, methylribeline, paraxanthine, theobromine and theophylline, the disaccharide is selected from the group consisting of turanose, leucrose, trehalulose and isomaltulose, the suitable carrier or additive or dietary supplement is selected from the group consisting of flavoring agents, coloring agents, viscosity modifiers, preservatives, chelating agents, antioxidants, surface modifiers and other dietary supplements, and the functional additives are selected from the group consisting of binders, diluents, lubricants, stabilizers, solubilizers, sustained-release polymers, coloring agents, taste enhancers and the like.

[0035] In another embodiment, the composition of the present invention can be formulated into various forms of health supplements such as powders, tablets, capsules, gel formulations, water-soluble formulations, etc., containing caffeine, theacrine and methylribeline together with various isomers of enzymatically treated sucrose, which are useful as stimulants and metabolic activators of the central nervous system.

[0036] In yet another embodiment, the present invention provides a composition useful for substantially improving the long-term persistence and increase of energy, mood and concentration, improving memory and cognitive enhancement, increasing, maintaining and prolonging walking activity, performance improvement, attentiveness, increasing fat burning capacity, increasing endurance, reducing depressive states, providing beneficial hypoglycemic effects and alleviating sleep deprivation.

[0037] In another embodiment, the present invention provides a composition useful for substantially improving endurance, motor ability, reduction of hunger and body weight, reduction of inflammation and pain, preventive and therapeutic treatment of nervous system diseases, academic performance, mood improvement, attentiveness, reduction of uric acid and management.

[0038] In yet another embodiment, the composition provides a sustained-release or extended-release composition.

[0039] In another embodiment, the present invention is a method for substantially stimulating the central nervous system and metabolic stimulation in a subject, the method comprising providing to the subject a composition comprising a methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose in a nutraceutically effective amount.

[0040] In another embodiment, the present invention is a method for substantially improving endurance, exercise ability, reduction of hunger and body weight, and reduction of inflammation and pain, preventive and therapeutic treatment of nervous system diseases, academic performance, mood improvement, attentiveness, reduction of uric acid, and management in a subject, the method comprising providing to the subject a composition comprising a methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose in a nutraceutically effective amount.

[0041] In another embodiment, the present invention is a method for substantially improving long-term persistence and increase of energy, mood and concentration, improving memory and cognitive improvement, improving walking activity, performance improvement, increasing attentiveness, maintaining, extending, increasing fat burning power, increasing endurance, reducing depressive state, providing beneficial hypoglycemic effect, and alleviating sleep deprivation in a subject, the method comprising providing to the subject a composition comprising a methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose in a nutraceutically effective amount.

[0042] In one embodiment, the present invention provides a composition suitable for oral administration to mammalian subjects including but not limited to humans, the composition comprising caffeine, theacrine and methylribelin in solid or liquid dosage forms.

[0043] According to another embodiment, the total concentration of caffeine, theacrine and methylribelin in the composition ranges from 0.01% to 20% by weight based on the total weight of the composition, and the remaining weight mainly contains disaccharides derived from isomers of enzymatically treated sucrose alone or in combination, is provided in solid or liquid dosage forms, and suitable carriers or additives or nutritional supplements are used.

[0044] The total amount of methylxanthine was maintained between 0.01% and 20% in the sucrose solution treated with the enzyme.

[0045] To achieve stability, solubility, and taste, appropriate food-grade preservatives, viscosity modifiers, and optionally bitterness masking agents such as stilbenoids like resveratrol and pterostilbene were added to the formulation.

[0046] The compositions of the present invention provide endurance, exercise ability, reduction of hunger and body weight, and reduction of inflammation and pain, preventive and therapeutic treatment of nervous system diseases, academic performance, mood improvement, attentiveness, reduction of uric acid, and substantial improvement in management.

[0047] The compositions of the present invention also provide debittering of methylxanthine due to the function of methylxanthine that forms a complex with the glucose moiety of the disaccharide.

[0048] The composition further provides slow metabolism of caffeine and a low glycemic index due to a longer metabolic time required for the breakdown of the treated disaccharide compound compared to untreated sucrose or glucose, resulting in a long-lasting or sustained-release of a long-term energy booster.

[0049] The compositions and processes for their preparation are further illustrated by the following non-limiting examples that provide a preferred mode for carrying out the process of the present invention. It should be recognized that some modifications, variations, optimizations, and alternatives of the processes described herein are well within the scope of those skilled in the art, and such modifications, variations, optimizations, alternatives, etc. should be construed as being within the scope of the concept of the present invention as disclosed herein.

[0050] Illustrative formulations: The formulations listed below are described for illustrative purposes only and should not be used in any way to limit the proper interpretation of the claims. In the formulations, the percentage of functional additives varies from 5 to 90% w / w.

[0051] Exemplary formulations are described below: [Table 1] [Table 2]

[0052] General procedure for the preparation of a formulation of sucrose isomers and methylxanthines To an aqueous solution (90% - 10% w / w) of enzymatically treated sucrose isomers (trehalulose, leucrose, trehalulose and isomaltulose or combinations thereof), methylxanthines (caffeine, theacrine, methylribelin, paraxanthine, theobromine, theophylline or combinations thereof: 0.01% - 20% w / w) are added, and then functional additives (5 - 90% w / w) such as stilbenoids like resveratrol (0 - 20% w / w), pterostilbene (0 - 20% w / w) and binders, diluents, lubricants, stabilizers, solubilizers, sustained-release polymers, suitable colorants, flavor enhancers, etc. are added. The composition is stirred at room temperature for 1.0 - 2.0 hours to avoid thermally induced inversion of sucrose. The resulting solution / suspension is packed for use. [Examples]

[0053] Example 1: 12.5 g of trehalulose and 12.5 g of isomaltulose were added to 100 ml of purified water with stirring at room temperature. 150 mg of caffeine, 100 mg of theacrine and 50 mg of methylribelin were added slowly and stirred for 30 minutes, and then 5 g of calcium stearate was added. The resulting solution was stirred at room temperature for 2 - 3 hours.

[0054] Example 2: 12.5 g of turanose and 12.5 g of leucrose were added to 100 ml of purified water at room temperature with stirring. 150 mg of caffeine, 50 mg of theacrine, and 100 mg of methyl riberine were slowly added, and the mixture was stirred for 30 minutes. Then, 5 g of calcium stearate was added. The resulting solution was stirred at room temperature for 2 - 3 hours.

[0055] Example 3: 25 g of trehalulose was added to 100 ml of purified water at room temperature with stirring. 150 mg of caffeine, 100 mg of theacrine, and 50 mg of methyl riberine were slowly added, and the mixture was stirred for 30 minutes. Then, 500 mg of pterostilbene and 5 g of calcium stearate were added. The resulting solution was stirred at room temperature for 2 - 3 hours.

[0056] Example 4: 25 g of trehalulose was added to 100 ml of purified water at room temperature with stirring. 150 mg of caffeine, 100 mg of theacrine, and 50 mg of methyl riberine were slowly added, and the mixture was stirred for 30 minutes. Then, 300 mg of pterostilbene and 5 g of calcium stearate were added. The resulting solution was stirred at room temperature for 2 - 3 hours.

[0057] Example 5: 12.5 g of turanose and 12.5 g of leucrose were added to 100 ml of purified water at room temperature with stirring. 150 mg of caffeine, 50 mg of theacrine, and 100 mg of methyl riberine were slowly added, and the mixture was stirred for 30 minutes. Then, 500 mg of resveratrol and 5 g of calcium stearate were added. The resulting solution was stirred at room temperature for 2 - 3 hours.

[0058] Although the present invention has been described in detail above for illustrative purposes, it should be understood that such details are for illustrative purposes only and can be modified by those skilled in the art without departing from the spirit and scope of the invention except as limited by the claims.

Claims

1. A composition comprising a methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose, wherein the amount of the methylxanthine is 0.01% to 20% w / w and the amount of the disaccharide derived from the enzymatic conversion of sucrose is 10% to 90% w / w.

2. The composition according to claim 1, wherein the methylxanthine is in its pure form or a cocrystal or solvate compound.

3. The conformer / solvate compound is selected from the group comprising phenol, cinnamic acid, resveratrol, pterostilbene, alcohol, organic acid, etc., of the composition according to claim 2.

4. The methylxanthine is selected from the group comprising caffeine, theacrine, methylribine, paraxanthine, theobromine, theophylline alone or in combination thereof in an amount of 0.01% to 20% w / w, of the composition according to claims 1 and 2.

5. The disaccharide derived from the enzymatic conversion of sucrose is selected from the group comprising turanose, leucrose, trehalulose and isomaltulose alone or in combination thereof in an amount of 10% to 90% w / w, of the composition according to claim 1.

6. The composition according to claim 1 may contain a functional food selected from stilbenoids in an amount of 0% to 20% w / w.

7. The stilbenoid is selected from resveratrol and pterostilbene, of the composition according to claim 6.

8. The composition according to claim 1 contains a suitable carrier or additive or nutritional supplement in an amount of 0.01% to 20% w / w.

9. The carrier or additive or nutritional supplement is selected from the group including, but not limited to, flavors, colorants, viscosity modifiers, preservatives, chelating agents, antioxidants, surface modifiers and other nutritional supplements alone or in combination thereof, of the composition according to claim 8.

10. The composition according to claim 1 may contain a functional additive in an amount of 5% to 90% w / w.

11. The functional additive is selected from the group comprising binders, diluents, lubricants, stabilizers, solubilizers, sustained-release polymers, colorants, flavor enhancers and other similar ones, of the composition according to claim 10.

12. The composition according to claim 1, comprising an individual methylxanthine selected from the group consisting of caffeine, theacrine, paraxanthine, theobromine, theophylline, and methylribelin in an amount of 0.01% to 20% w / w, in combination with a disaccharide derived from enzymatically treated sucrose selected from the group consisting of turanose, leucrose, trehalulose, and isomaltulose, alone or in combination, in an amount of 10% to 90% w / w.

13. The composition according to claim 1, optionally comprising a bitterness masking agent.

14. The composition according to any one of claims 1 to 13, which may be formulated to be an oral solid, liquid, or suspension.

15. The composition according to any one of claims 1 to 13, which may be formulated for oral administration in various forms of health supplements such as powders, tablets, capsules, gel formulations, or water-soluble formulations.

16. The composition according to claims 1 to 13, which is provided as a water-soluble composition.

17. A process for the preparation of a composition comprising methylxanthine alone or in combination with a disaccharide derived from enzymatically treated sucrose, comprising: i. adding methylxanthine individually or in combination in an amount of 0.01% to 20% w / w to an aqueous solution of sucrose treated with an enzyme in an amount of 90 to 10% w / w; ii. adding stilbenoid in an amount of 0 to 20% w / w to the solution of step (i); iii. adding a functional additive in an amount of 5 to 90% w / w to the solution of step (ii); and iv. stirring the solution of step (iii) at room temperature to avoid thermally induced conversion of sucrose to obtain the desired composition A process comprising.

18. The methylxanthine is selected from the group consisting of caffeine, theacrine, methylribelin, paraxanthine, theobromine and theophylline, the disaccharide is selected from the group consisting of turanose, leucrose, trehalulose and isomaltulose, the preferred carrier or additive or dietary supplement is selected from the group consisting of flavoring agents, coloring agents, viscosity modifiers, preservatives, chelating agents, antioxidants, surface modifiers and other dietary supplements, and the functional additive is selected from the group consisting of binders, diluents, lubricants, stabilizers, solubilizing agents, sustained-release polymers, coloring agents, flavor enhancers and the like. The process according to claim 17.

19. The composition according to any one of claims 1 to 18, which is useful as a central nervous system stimulant and a metabolic activator.

20. Improving long-term persistence and increase of energy, mood and concentration, improving memory and cognitive ability, increasing, maintaining and prolonging walking activity and performance, increasing vigilance, increasing fat burning power, increasing endurance, reducing depressive state, providing beneficial hypoglycemic effect and relieving sleep deprivation. The composition according to any one of claims 1 to 18.

21. Useful for reducing endurance, exercise ability, hunger and body weight, as well as reducing inflammation and pain, for the prophylactic and therapeutic treatment of nervous system diseases, for improving academic performance, mood, vigilance, reducing uric acid and improving management. The composition according to any one of claims 1 to 18.

22. The composition according to any one of claims 1 to 21, wherein the composition provides a sustained-release or slow-release composition.

23. A method for stimulating the central nervous system and metabolic stimulation in a subject, the method comprising providing to the subject a composition comprising methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose according to any one of claims 1 to 22 in an amount effective for nutritional enhancement.

24. A method for improving endurance, exercise ability, reducing hunger and body weight, as well as reducing inflammation and pain, for the prophylactic and therapeutic treatment of nervous system diseases, for improving academic performance, mood, vigilance, reducing uric acid and improving management in a subject, the method comprising providing to the subject a composition comprising methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose according to any one of claims 1 to 23 in an amount effective for nutritional enhancement.

25. A method for improving long-term maintenance and increase of energy, mood and concentration, improving memory and cognition, improving walking activity, performance, increasing attentiveness, maintaining, prolonging, increasing fat burning ability, increasing endurance, reducing depressive states, providing beneficial hypoglycemic effects and alleviating sleep deprivation in a subject, said method comprising providing to the subject a composition comprising methylxanthine in combination with a disaccharide derived from the enzymatic conversion of sucrose according to any one of claims 1 to 24 in an amount effective for nutritional enhancement.

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