Indian Patents. 278152:ORAL LIQUID COMPOSITIONS OF RESVERATROL OR ITS PHARMACEUTICALLY , ACCEPTABLE SALT

Title of Invention	ORAL LIQUID COMPOSITIONS OF RESVERATROL OR ITS PHARMACEUTICALLY , ACCEPTABLE SALT
Abstract	A low-calorie liquid antioxidant compositions of stilbenoid, in particular resveratrol or its pharnnaceutically acceptable salts, solvates, enantiomers or derivatives thereof, the processes for preparing the same and methods of use and treatment of such compositions.

Full Text	Field of the invention: The present invention relates to low-calorie liquid antioxidant compositions of stilbenoid, in particular resveratrol or its pharmaceutically acceptable salts, solvates, enantiomers or derivatives thereof, the processes for preparing the same and methods of use and treatment of such compositions. Background of the invention: Resveratrol (Formula I) is a polyphenolic stilbenoid, chemically known as 5-[(1E)-2-(4-Hydroxyphenyl)ethenyl]-1,3,benzenediol. Stilbenoids such as resveratrol are considered to possess antitumor, antioxidant as well as a number of other positive health effects. Resveratrol has been shown to promote bone health, elicit a vasoprotective effect, counteract high fat diet and aid in weight loss. The activation of Sirtuin 1 (SIRT1) enzyme by resveratrol has been thought to be the key factor leading to the reported increase in life expectancy by resveratrol. (Formula I) Liquid formulations of resveratrol are commercially available. Vivix® Cellular Anti- aging tonic is a commercially available liquid dosage form of resveratrol. The tonic contains resveratrol in combination with a number of antioxidants. Resveratrol Life Tonic™, another liquid dosage form of resveratrol, from Life Time vitamins is available. Being tonics, these formulations deliver resveratrol in a highly concentrated form for elucidation of optimal effect. Liquid nutritional supplements such as tonics, owing to the high concentration of active present in the composition, suffer from potential patient non-compliance. These liquids are difficult to measure out precisely for the correct dose and also attract possibility of spillage which causes loss of active ingredients resulting in a deficient administered dose. Moreover, since the liquid supplements are usually loaded with ingredients (to deliver enough nutrients in one or two tablespoon dose), the taste of the such supplements usually, is unacceptable and is another major factor contributing to the unacceptability of such fortified liquid dosage forms by consumers. Functional liquids containing nutritional supplements are becoming mainstream due to ease of consumption and patient compliance. The functional beverages help individuals consume nutritional supplements in an easy and regular fashion. Moreover, being clear products just like water, consumers link them more closely with water's heritage, instead of a linkage to medicine and hence such products are more appealing to health conscious consumers. Resveratrol based dilute liquid drinks have been reported. EP1762234A1 exemplifies resveratrol formulations comprising fruit juice. The exemplified formulations are both non-carbonated as well as carbonated formulations. PCT publication WO 2009/003798A1 discloses a liquid composition of trans-resveratrol based on fruit juice comprising a liquid protein base. US 2008/0213433A1 reports a non-alcoholic and non-fermented beverage of resveratrol. The beverage comprises resveratrol solution buffered with a buffering agent such as sodium phosphate. The prior art dilute liquid formulations of resveratrol are either buffered solutions of resveratrol or have the drawback of being high on calorie content, due to the presence of fruit juice and artificial sugar in the formulations, which makes them unacceptable to health conscious consumers. None of the documents disclose buffer-free and low-calorie aqueous formulations of resveratrol, which are based majorly on natural ingredients. Thus, there are no known available liquid dosage forms of resveratrol as disclosed in the context of the present invention. Hence, the present invention fills a highly desirable gap in the technological field comprising economical and low-calorie functional beverages of resveratrol which do not comprise a buffer system. Summary of the invention: The aim of the present invention is to provide stable, aqueous compositions of resveratrol, wherein the resveratrol formulations do not contain a buffer system. Further it is an objective of the present invention to provide antioxidant compositions of resveratrol, which are formulated majorly with natural ingredients and are extremely low on calorie content. Detailed description of the invention: The present invention relates to stable compositions which comprise a liquid antioxidant composition of a stilbenoid, particularly resveratrol. The resveratrol compositions as per the present invention are fonnulated with a calorie content of less than 1 calorie and do not contain a buffer system. As used herein, the term "resveratrol" refers collectively to trans-resveratrol, cis-resveratrol, mixtures thereof or their pharmaceutically acceptable salts, solvates, enantiomers or derivatives. In an embodiment, resveratrol salts such as resveratrol phosphate, resveratrol glycinate, resveratrol serinate, resveratrol alaninate etc were used as the source of the active ingredient resveratrol in the context of the present invention. The preferred concentration of resveratrol in the preparation according to the invention is from about 5 mg to about 300 mg per 100 ml of the formulation, in particular from about 50 mg to about 150 mg per 100 ml of the formulation, especially from about 75 mg to about 125 mg per 100 ml of the formulation. In an embodiment, stable antioxidant compositions as disclosed in the present invention are formulated as liquid formulations, in particular liquid oral formulations in a solvent. In another embodiment of the present invention, the preferable solvent is water. In yet another embodiment, the antioxidant compositions as disclosed in the context of the present invention comprise oral rehydration salts. Oral rehydration salts replenish the body's electrolyte levels following dehydration caused by exercise, diaphoresis, diarrhea, vomiting, intoxication or starvation. The oral rehydration salts which may be used are exemplified by but are not limited to sodium chloride, potassium chloride, trisodium citrate, anhydrous glucose, sodium monohydrogen carbonate and the like. Combinations of the electrolyte replenishers in various ratios and proportions as required are covered within the scope of the invention without limitation. In an embodiment, sodium chloride and potassium chloride were found useful in the context of the present invention. An electrolyte replenisher such as sodium chloride may optionally be present in a range of from about 50 mg to about 250 mg per 100 ml of the formulation. In an embodiment, sodium chloride was present in the range of from about 75 mg to about 125 mg per 100 ml of the formulation. Potassium chloride, as an electrolyte replenisher may optionally be present in a range of from about 0 mg to about 50 mg per 100 ml of the formulation. In an embodiment, potassium chloride was present in the range of from about 20 mg to about 40 mg per 100 ml of the formulation. The composition according to the invention may contain further pharmaceutically acceptable adjuncts and additives, for example preservatives, antioxidants, flavors, colors, emulsifiers, sweeteners and the like. Suitable preservatives, which may be added to the formulation, are benzoic acid or salts thereof, such as sodium, potassium or calcium salts, 4-hydroxybenzoic acid esters, such as methyl, ethyl or propyl 4-hydroxybenzoate (PHB esters) and the like may be added to the liquid formulation although other pharmaceutically acceptable preservatives can be substituted. In an embodiment, sodium benzoate was used as the preservative in the context of the present formulation. A preservative such as sodium benzoate can be optionally present in a range of from about 0.002 to about 0.5% w/v, preferably from about 0.038% to about 0.38% w/v, more particularly from about 0.25% to about 0.35% w/v. Antioxidants nnay be used in tlie present invention to protect the active(s) from oxidative degradation. Tlie antioxidants or free radical scavengers or combinations thereof used in various ratios are exemplified by but are not limited to glutathione, lycopene, pycnogenol, N-acetyl cysteine, allyl methyl trisulfide, BHT, BHA, diallyl sulfide, astanxanthin, sulphites, ascorbic acid, dithiolthiones, rosemary extracts, lutein, anthrocyanidins, uric acid, tocopherols, catechins, epicatechins, alpha- lipoic acid, carotenes, zeaxanthin, ubiquinols and the like. Combinations of more than one antioxidant in various ratios and proportions as well as their derivatives, precursors and combinations thereof, as required are covered within the scope of the invention without limitation. Addition of synergists, such as citric acid, citraconic acid, phosphoric acid, tartaric acid and the like to potentiate the antioxidant effect is covered within the scope of the invention without limitation. In an embodiment, ascorbic acid was found to be useful as an antioxidant in the context of the present invention. An antioxidant such as ascorbic acid may be present in an amount of from about 0.01% to about 0.1% w/v, preferably in an amount of from about 0.03% to about 0.08% w/v. Flavors can be added in the formulation. Flavoring agents that may be used include, but are not limited to natural flavors, natural fruit flavors, artificial flavors, artificial fruit flavors, flavor enhancers or mixtures thereof. Natural flavors, artificial flavors or mixtures thereof include, but are not limited to mint (such as peppermint or spearmint), menthol, cinnamon, vanilla, artificial vanilla, chocolate, artificial chocolate, bubblegum and the like. Natural fruit flavors, artificial fruit flavors or mixtures thereof include, but are not limited to cherry, grape, orange, strawberry, lemon and the like. Flavor enhancers include, but are not limited to citric acid and the like. A flavoring agent such as orange flavor used in the present invention has a range of from about 5 mg to about 40 mg per 100 ml of the formulation, preferably from about 15 mg to about 30 mg per 100 ml of the formulation. A flavor enhancer such as citric acid may be added in the formulation in the range of from about 0% to about 2% w/v, preferably from about 0.10% to about 0.30% w/v. Coloring agents also can be incorporated to provide an appealing color to the liquid formulation. Suitable coloring agents include those that avoid chemical incompatibilities with other ingredients. Both natural and synthetic colors as known in the art may be used as coloring agents. Colors may also be added to match the flavor of the end product. Orange color was used as a coloring agent in an embodiment. In another embodiment, grape color was used. The coloring agent in the context of the present invention, for example, such as orange color may be present in a range of from about 5.0 mg to about 50.0 mg per 100 ml of the formulation, preferably from about 20.0 mg to about 35.0 mg per 100 ml of the fomnulation. In an embodiment, the liquid composition as disclosed in the present invention may include a sweetening agent. Sweeteners which can be used in the liquid composition include but are not limited to tagatose, stevia, sucralose, saccharin, aspartame, acesulfame- K, erythritol, fructose, trehalose, isomaltulose, xylitol, sorbitol, mannitol, naringin. neohesperidin, lactitol, cyclamates, maltitol and the like. Natural sweeteners, synthetic sweeteners or combinations thereof, in various ratios and proportions are covered within the scope of the present invention without limitation. The amount of sweetener used in the taste masking composition will vary depending on the degree of palatability desired for the liquid composition. In an embodiment, the liquid composition of the present invention comprises stevia as the sweetening agent. Generally the total amount of sweetener used in the context of the present invention has a range of about 50 to about 250 mg per 100 ml, preferably, the amount of sweetener used is present in a range of from about 100 mg to about 200 mg per 100 ml of the formulation, more preferably, the amount of sweetener used in the present invention is in a range of from about 125 mg to about 175 mg per 100 ml of the formulation. The liquid composition as disclosed in the present invention may optionally be carbonated. Carbonation of the composition may be done by carbonation techniques known in the art. In an embodiment, the liquid composition was purged with carbon dioxide to achieve carbonation of the composition. The pH of of the antioxidant compositions as disclosed in the context of the present invention may optionally range from about 2.0 to about 7.0. In an embodiment, the pH of the carbonated composition of resveratrol ranges from about 2.0 to about 3.5. Oral liquid formulations according to the invention may comprise other excipients commonly employed in oral formulations for peroral administration so as to provide the required stability. This may include any other excipients commonly used in the preparation of liquid compositions for oral administration. The liquid compositions according to the said invention may comprise other agents which may enhance and/ or potentiate the effect of resveratrol. Such said compositions may further comprise other polyphenols including, but not limited to, quercetin, naringenin, catechin, epicatechin, piceatannol, kaempferol, fisetin, apigenin, morin and the like as well as/or other pharmaceutically acceptable excipients. The present invention describes making a composition for delivering liquid nutritional supplement in an easily consumable form which does not require dilution. The liquid nutritional supplement is dispensed in commonly available packages such as carton based packages or metal or plastic based containers. An embodiment of the present invention includes a composition for delivering a stable liquid drink which is low in calorie content. The liquid resveratrol composition according to the present invention can be used as a health beverage or a liquid nutritional supplement. The aqueous composition in the present invention may be prepared by processes Known to one skilled in the art but is not limited to the following process: a) Dissolving resveratrol along with other pharmaceutically acceptable excipients in a solvent, irrespective of the order of dissolution of the ingredients in the solvent, so as to achieve a clear solution. b) Optionally adjusting the pH to suitable values. c) Optionally subjecting the solution to filtration and subsequent carbonation. d) Packaging of the formulation Examples The following examples are included to illustrate certain aspects of the invention in greater detail but are not intended to limit the scope of the invention in any way. Various examples as well as alternate embodiments will be evident to a person skilled in the art upon reference to the description and are presumed to be within the scope of the invention. Example 1: Composition of Resveratrol solution Manufacturing procedure: Dissolve required amounts of Sodium chloride, Potassium chloride. Sodium benzoate, Stevia powder and Ascorbic acid in 90.00 ml of purified water, with stirring, until each of the previous ingredients dissolves completely prior to addition of the next ingredient. After a clear solution is obtained, add Resveratrol Phosphate and stir to dissolution. Add citric acid to the prepared resveratrol solution. Add required amounts of color and flavor and stir to dissolution. make up the volume and filter the solution through a 2 \|jm pore size filter. Purge the solution with a gas such as carbon dioxide and subsequently fill in aluminium cans. Example 2 : Composition of Resveratrol solution Manufacturing procedure: Dissolve required amounts of Sodium chloride, Potassium chloride, Sodium benzoate, Stevia powder and Ascorbic acid in 90.00 ml of purified water, with stirring, until each of the previous ingredients dissolves completely prior to addition of the next ingredient. After a clear solution is obtained, add Resveratrol Phosphate and stir to dissolution. Add citric acid to the prepared Resveratrol solution. Add required amounts of color and flavor and stir to dissolution. Make up the volume and filter the solution through a 2 \|jm pore size filter. Purge the solution with a gas such as carbon dioxide and subsequently fill in aluminum cans. We claim; 1. A low-calorie liquid antioxidant composition of stilbenoid. 2. A low-calorie liquid antioxidant composition as claimed in claim 1, wherein the stilbinoid is resveratrol or its pharmaceutically acceptable salts, solvates, enantiomers or derivatives thereof. 3. A process for preparing the low-calorie liquid antioxidant composition comprising the steps of; a. Dissolving resveratrol along with other pharmaceutically acceptable excipients in a solvent, irrespective of the order of dissolution of the ingredients in the solvent, so as to achieve a clear solution. b. Optionally adjusting the pH to suitable values. c. Optionally subjecting the solution to filtration and subsequent carbonation. d. Packaging of the formulation 4. The process as claimed in claim 3, wherein the pH of the antioxidant compositions is about 2.0 to about 7.0. 5. The process as claimed in claim 3 and 4, wherein the pH of the antioxidant compositions is maintained between 2.0 to 3.5. 6. The process as claimed in claim 3, wherein the carbonation is carried out by purging carbon dioxide to achieve carbonation of the composition.

Full Text

Field of the invention:

The present invention relates to low-calorie liquid antioxidant compositions of stilbenoid, in particular resveratrol or its pharmaceutically acceptable salts, solvates, enantiomers or derivatives thereof, the processes for preparing the same and methods of use and treatment of such compositions.

Background of the invention:

Resveratrol (Formula I) is a polyphenolic stilbenoid, chemically known as 5-[(1E)-2-(4-Hydroxyphenyl)ethenyl]-1,3,benzenediol. Stilbenoids such as resveratrol are considered to possess antitumor, antioxidant as well as a number of other positive health effects. Resveratrol has been shown to promote bone health, elicit a vasoprotective effect, counteract high fat diet and aid in weight loss. The activation of Sirtuin 1 (SIRT1) enzyme by resveratrol has been thought to be the key factor leading to the reported increase in life expectancy by resveratrol.

(Formula I)

Liquid formulations of resveratrol are commercially available. Vivix® Cellular Anti- aging tonic is a commercially available liquid dosage form of resveratrol. The tonic contains resveratrol in combination with a number of antioxidants. Resveratrol Life Tonic™, another liquid dosage form of resveratrol, from Life Time vitamins is available. Being tonics, these formulations deliver resveratrol in a highly concentrated form for elucidation of optimal effect.

Liquid nutritional supplements such as tonics, owing to the high concentration of active present in the composition, suffer from potential patient non-compliance. These liquids are difficult to measure out precisely for the correct dose and also attract possibility of spillage which causes loss of active ingredients resulting in a deficient administered dose. Moreover, since the liquid supplements are usually loaded with ingredients (to deliver enough nutrients in one or two tablespoon dose), the taste of the such supplements usually, is unacceptable and is another major factor contributing to the unacceptability of such fortified liquid dosage forms by consumers.

Functional liquids containing nutritional supplements are becoming mainstream due to ease of consumption and patient compliance. The functional beverages help individuals consume nutritional supplements in an easy and regular fashion. Moreover, being clear products just like water, consumers link them more closely with water's heritage, instead of a linkage to medicine and hence such products are more appealing to health conscious consumers.

Resveratrol based dilute liquid drinks have been reported. EP1762234A1 exemplifies resveratrol formulations comprising fruit juice. The exemplified formulations are both non-carbonated as well as carbonated formulations. PCT publication WO 2009/003798A1 discloses a liquid composition of trans-resveratrol based on fruit juice comprising a liquid protein base. US 2008/0213433A1 reports a non-alcoholic and non-fermented beverage of resveratrol. The beverage comprises resveratrol solution buffered with a buffering agent such as sodium phosphate. The prior art dilute liquid formulations of resveratrol are either buffered solutions of resveratrol or have the drawback of being high on calorie content, due to the presence of fruit juice and artificial sugar in the formulations, which makes them unacceptable to health conscious consumers.

None of the documents disclose buffer-free and low-calorie aqueous formulations of resveratrol, which are based majorly on natural ingredients. Thus, there are no known available liquid dosage forms of resveratrol as disclosed in the context of the present invention. Hence, the present invention fills a highly desirable gap in the technological field comprising economical and low-calorie functional beverages of resveratrol which do not comprise a buffer system.

Summary of the invention:

The aim of the present invention is to provide stable, aqueous compositions of resveratrol, wherein the resveratrol formulations do not contain a buffer system.

Further it is an objective of the present invention to provide antioxidant compositions of resveratrol, which are formulated majorly with natural ingredients and are extremely low on calorie content.

Detailed description of the invention:

The present invention relates to stable compositions which comprise a liquid antioxidant composition of a stilbenoid, particularly resveratrol. The resveratrol compositions as per the present invention are fonnulated with a calorie content of less than 1 calorie and do not contain a buffer system.

As used herein, the term "resveratrol" refers collectively to trans-resveratrol, cis-resveratrol, mixtures thereof or their pharmaceutically acceptable salts, solvates, enantiomers or derivatives. In an embodiment, resveratrol salts such as resveratrol phosphate, resveratrol glycinate, resveratrol serinate, resveratrol alaninate etc were used as the source of the active ingredient resveratrol in the context of the present invention.

The preferred concentration of resveratrol in the preparation according to the invention is from about 5 mg to about 300 mg per 100 ml of the formulation, in particular from about 50 mg to about 150 mg per 100 ml of the formulation, especially from about 75 mg to about 125 mg per 100 ml of the formulation.

In an embodiment, stable antioxidant compositions as disclosed in the present invention are formulated as liquid formulations, in particular liquid oral formulations in a solvent. In another embodiment of the present invention, the preferable solvent is water.

In yet another embodiment, the antioxidant compositions as disclosed in the context of the present invention comprise oral rehydration salts.

Oral rehydration salts replenish the body's electrolyte levels following dehydration caused by exercise, diaphoresis, diarrhea, vomiting, intoxication or starvation. The oral rehydration salts which may be used are exemplified by but are not limited to sodium chloride, potassium chloride, trisodium citrate, anhydrous glucose, sodium monohydrogen carbonate and the like. Combinations of the electrolyte replenishers in various ratios and proportions as required are covered within the scope of the invention without limitation. In an embodiment, sodium chloride and potassium chloride were found useful in the context of the present invention. An electrolyte replenisher such as sodium chloride may optionally be present in a range of from about 50 mg to about 250 mg per 100 ml of the formulation. In an embodiment, sodium chloride was present in the range of from about 75 mg to about 125 mg per 100 ml of the formulation. Potassium chloride, as an electrolyte replenisher may optionally be present in a range of from about 0 mg to about 50 mg per 100 ml of the formulation. In an embodiment, potassium chloride was present in the range of from about 20 mg to about 40 mg per 100 ml of the formulation.

The composition according to the invention may contain further pharmaceutically acceptable adjuncts and additives, for example preservatives, antioxidants, flavors, colors, emulsifiers, sweeteners and the like.

Suitable preservatives, which may be added to the formulation, are benzoic acid or salts thereof, such as sodium, potassium or calcium salts, 4-hydroxybenzoic acid esters, such as methyl, ethyl or propyl 4-hydroxybenzoate (PHB esters) and the like may be added to the liquid formulation although other pharmaceutically acceptable preservatives can be substituted. In an embodiment, sodium benzoate was used as the preservative in the context of the present formulation. A preservative such as sodium benzoate can be optionally present in a range of from about 0.002 to about 0.5% w/v, preferably from about 0.038% to about 0.38% w/v, more particularly from about 0.25% to about 0.35% w/v.

Antioxidants nnay be used in tlie present invention to protect the active(s) from oxidative degradation. Tlie antioxidants or free radical scavengers or combinations thereof used in various ratios are exemplified by but are not limited to glutathione, lycopene, pycnogenol, N-acetyl cysteine, allyl methyl trisulfide, BHT, BHA, diallyl sulfide, astanxanthin, sulphites, ascorbic acid, dithiolthiones, rosemary extracts, lutein, anthrocyanidins, uric acid, tocopherols, catechins, epicatechins, alpha- lipoic acid, carotenes, zeaxanthin, ubiquinols and the like. Combinations of more than one antioxidant in various ratios and proportions as well as their derivatives, precursors and combinations thereof, as required are covered within the scope of the invention without limitation. Addition of synergists, such as citric acid, citraconic acid, phosphoric acid, tartaric acid and the like to potentiate the antioxidant effect is covered within the scope of the invention without limitation. In an embodiment, ascorbic acid was found to be useful as an antioxidant in the context of the present invention. An antioxidant such as ascorbic acid may be present in an amount of from about 0.01% to about 0.1% w/v, preferably in an amount of from about 0.03% to about 0.08% w/v.

Flavors can be added in the formulation. Flavoring agents that may be used include, but are not limited to natural flavors, natural fruit flavors, artificial flavors, artificial fruit flavors, flavor enhancers or mixtures thereof. Natural flavors, artificial flavors or mixtures thereof include, but are not limited to mint (such as peppermint or spearmint), menthol, cinnamon, vanilla, artificial vanilla, chocolate, artificial chocolate, bubblegum and the like. Natural fruit flavors, artificial fruit flavors or mixtures thereof include, but are not limited to cherry, grape, orange, strawberry, lemon and the like. Flavor enhancers include, but are not limited to citric acid and the like. A flavoring agent such as orange flavor used in the present invention has a range of from about 5 mg to about 40 mg per 100 ml of the formulation, preferably from about 15 mg to about 30 mg per 100 ml of the formulation. A flavor enhancer such as citric acid may be added in the formulation in the range of from about 0% to about 2% w/v, preferably from about 0.10% to about 0.30% w/v.

Coloring agents also can be incorporated to provide an appealing color to the liquid formulation. Suitable coloring agents include those that avoid chemical incompatibilities with other ingredients. Both natural and synthetic colors as known in the art may be used as coloring agents. Colors may also be added to match the flavor of the end product. Orange color was used as a coloring agent in an embodiment. In another embodiment, grape color was used. The coloring agent in the context of the present invention, for example, such as orange color may be present in a range of from about 5.0 mg to about 50.0 mg per 100 ml of the formulation, preferably from about 20.0 mg to about 35.0 mg per 100 ml of the fomnulation.

In an embodiment, the liquid composition as disclosed in the present invention may include a sweetening agent. Sweeteners which can be used in the liquid composition include but are not limited to tagatose, stevia, sucralose, saccharin, aspartame, acesulfame- K, erythritol, fructose, trehalose, isomaltulose, xylitol, sorbitol, mannitol, naringin.

neohesperidin, lactitol, cyclamates, maltitol and the like. Natural sweeteners, synthetic sweeteners or combinations thereof, in various ratios and proportions are covered within the scope of the present invention without limitation. The amount of sweetener used in the taste masking composition will vary depending on the degree of palatability desired for the liquid composition. In an embodiment, the liquid composition of the present invention comprises stevia as the sweetening agent. Generally the total amount of sweetener used in the context of the present invention has a range of about 50 to about 250 mg per 100 ml, preferably, the amount of sweetener used is present in a range of from about 100 mg to about 200 mg per 100 ml of the formulation, more preferably, the amount of sweetener used in the present invention is in a range of from about 125 mg to about 175 mg per 100 ml of the formulation.
The liquid composition as disclosed in the present invention may optionally be carbonated. Carbonation of the composition may be done by carbonation techniques known in the art. In an embodiment, the liquid composition was purged with carbon dioxide to achieve carbonation of the composition.

The pH of of the antioxidant compositions as disclosed in the context of the present invention may optionally range from about 2.0 to about 7.0. In an embodiment, the pH of the carbonated composition of resveratrol ranges from about 2.0 to about 3.5.
Oral liquid formulations according to the invention may comprise other excipients commonly employed in oral formulations for peroral administration so as to provide the required stability. This may include any other excipients commonly used in the preparation of liquid compositions for oral administration.

The liquid compositions according to the said invention may comprise other agents which may enhance and/ or potentiate the effect of resveratrol. Such said compositions may further comprise other polyphenols including, but not limited to, quercetin, naringenin, catechin, epicatechin, piceatannol, kaempferol, fisetin, apigenin, morin and the like as well as/or other pharmaceutically acceptable excipients.

The present invention describes making a composition for delivering liquid nutritional supplement in an easily consumable form which does not require dilution. The liquid nutritional supplement is dispensed in commonly available packages such as carton based packages or metal or plastic based containers.
An embodiment of the present invention includes a composition for delivering a stable liquid drink which is low in calorie content. The liquid resveratrol composition according to the present invention can be used as a health beverage or a liquid nutritional supplement.

The aqueous composition in the present invention may be prepared by processes Known to one skilled in the art but is not limited to the following process:

a) Dissolving resveratrol along with other pharmaceutically acceptable excipients in a solvent, irrespective of the order of dissolution of the ingredients in the solvent, so as to achieve a clear solution.

b) Optionally adjusting the pH to suitable values.

c) Optionally subjecting the solution to filtration and subsequent carbonation.

d) Packaging of the formulation

Examples

The following examples are included to illustrate certain aspects of the invention in greater detail but are not intended to limit the scope of the invention in any way. Various examples as well as alternate embodiments will be evident to a person skilled in the art upon reference to the description and are presumed to be within the scope of the invention.

Example 1: Composition of Resveratrol solution

Manufacturing procedure:

Dissolve required amounts of Sodium chloride, Potassium chloride. Sodium benzoate, Stevia powder and Ascorbic acid in 90.00 ml of purified water, with stirring, until each of the previous ingredients dissolves completely prior to addition of the next ingredient. After a clear solution is obtained, add Resveratrol Phosphate and stir to dissolution. Add citric acid to the prepared resveratrol solution. Add required amounts of color and flavor and stir to dissolution. make up the volume and filter the solution through a 2 |jm pore size filter. Purge the solution with a gas such as carbon dioxide and subsequently fill in aluminium cans.

Example 2 : Composition of Resveratrol solution
Manufacturing procedure:
Dissolve required amounts of Sodium chloride, Potassium chloride, Sodium benzoate, Stevia powder and Ascorbic acid in 90.00 ml of purified water, with stirring, until each of the previous ingredients dissolves completely prior to addition of the next ingredient. After a clear solution is obtained, add Resveratrol Phosphate and stir to dissolution. Add citric acid to the prepared Resveratrol solution. Add required amounts of color and flavor and stir to dissolution. Make up the volume and filter the solution through a 2 |jm pore size filter. Purge the solution with a gas such as carbon dioxide and subsequently fill in aluminum cans.

We claim;

1. A low-calorie liquid antioxidant composition of stilbenoid.

2. A low-calorie liquid antioxidant composition as claimed in claim 1, wherein the stilbinoid is resveratrol or its
pharmaceutically acceptable salts, solvates, enantiomers or derivatives thereof.

3. A process for preparing the low-calorie liquid antioxidant composition comprising the steps of;

a. Dissolving resveratrol along with other pharmaceutically acceptable excipients in a solvent, irrespective of the order of dissolution of the ingredients in the solvent, so as to achieve a clear solution.

b. Optionally adjusting the pH to suitable values.

c. Optionally subjecting the solution to filtration and subsequent carbonation.

d. Packaging of the formulation

4. The process as claimed in claim 3, wherein the pH of the antioxidant compositions is about 2.0 to about 7.0.

5. The process as claimed in claim 3 and 4, wherein the pH of the antioxidant compositions is maintained between 2.0 to 3.5.

6. The process as claimed in claim 3, wherein the carbonation is carried out by purging carbon dioxide to achieve carbonation of the composition.

Documents:

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Patent Number

278152

Indian Patent Application Number

1377/CHE/2009

PG Journal Number

52/2016

Publication Date

16-Dec-2016

Grant Date

15-Dec-2016

Date of Filing

11-Jun-2009

Name of Patentee

LAURUS LABS PVT LTD

Applicant Address

2ND FLOOR SERENE CHAMBERS ROAD #7 BANJARA HILLS HYDERABAD 500034

Inventors:

#	Inventor's Name	Inventor's Address
1	KAVURI NARENDRA KUMAR	2ND FLOOR, SERENE CHAMBERS, ROAD NO.7, BANJARA HILLS, HYDERABAD - 500034
2	KACHHWAHA JOHARILAL SANDEEP	2ND FLOOR, SERENE CHAMBERS, ROAD NO.7, BANJARA HILLS, HYDERABAD - 500034

PCT International Classification Number

A61K31/00

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA