COMPLETE AFTER PROVISIONAL
LEFT ON 12/07/06

FORM 2
THE PATENTS ACT, 1970
(39 of 1970)
85
The Patent Rules, 2003
COMPLETE SPECIFICATION
' (See section 10 and rule 13)
TITLE OF THE INVENTION
"SWEETENER COMPOSITION WITH ENHANCED SWEETNESS"
We, ALKEM LABORATORIES LIMITED, of Devashish, Alkem House, Senapati Bapat Marg, Lower Parel, Mumbai - 400 013.
The following specification particularly describes the invention and the manner in which it is to be performed.

SWEETENER COMPOSITION WITH ENHANCED SWEETNESS
The present invention relates to a sweetener composition with enhanced sweetness profile. More particularly, the present invention relates to a sweetener composition comprising sucralose and a sweetener enhancing agent selected from one or more of fructo-oligosaccharide, stevia, neohesperidine and neotame, which displays sweetness enhancement to the order of 600 to 2500 over sucralose per se.
It is well established in the art that persons who wish to restrict their dietary intake of calories or who suffer from diabetes must preferably replace their intake of sugar with low calorie or no-calorie sweeteners. It is also known that the use of low-calorie or no-calorie sweeteners can be used in for weight reduction in the case of patients of obesity, or for medical reasons or for diabetics to reduce intake of carbohydrates and thereby limit the intake of sucrose, glucose and the like.
Several artificial sweetener compositions are known in the art. Predominantly, such compositions contain saccharin and its salts, aspartame, acesulafame -K, cyclamates, extracts of Stevia rebaudiana (stevioside), thaumatin extracted from Thaumatococcus danieli, sucralose, alitame, and the like. A problem associated with practically all sweetener compositions known in the art are that they leave a bitter or metallic after taste. Saccharin and its salts are characterized as having a bitter aftertaste. Sucralose is a well known artificial sweetener but also suffers from the disadvantage of a bitter after taste. Aspartame on the other hand is reported to have a cloying sweet aftertaste. Cyclamates and acesulfame-K are both known to have a slightly metallic aftertaste. As will be evident, the presence of an undesirable aftertaste reduces the effectiveness of these sweetener compositions.
Another problem associated with most sweetener compositions known in the art is that the ingredients are expensive. For example, aspartame, acesulfame-K, sucralose and alitame are significantly more expensive than saccharin or cyclamates. While the use of such ingredients to enhance sweetness intensity is known, there is a disincentive in view of their increased costs.
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Several methods have been propounded in the art to enhance the sweetness intensity. It is known to combine sucralose with other high intensity sweeteners such as saccharin, acesulfame-K, and stevioside. For example, GB Patent 2098848 and US Patent 4,495,170 both teach mixtures of sucralose and stevioside. GB Patent 2154850 teaches a mixture of sucralose and cyclamates. GB Patent 2153651 teaches a mixture of sucralose and aspartame. While these compositions evince a slight increase in sweetness intensity, there is no reduction in the metallic or bitter aftertaste present due to the use of such sweeteners.
Several attempts have also been made to reduce the bitter or metallic aftertaste of sweetening compositions. For example, US Patent 3,625,711 teaches a mixture of potassium bitartarate and a small amount of sugar to saccharin in order to reduce the aftertaste thereof. Similarly, US Patent 3,695,898 teaches the addition of small amounts of aspartame to mask the bitter aftertaste of saccharin. Canadian Patent 1,043,158 teaches the use of asparatame, saccharin and cyclamate to reduce the lingering or bitter aftertaste of the individual sweeteners.
To the applicants knowledge there is no disclosure in the art of any compositions where sweetness intensity is enhanced as well as aftertaste reduced in the case of sweetener compositions containing sucralose. Again, to the applicants' knowledge, there is no report in the art of any attempt to synergise the properties of sucralose and sucrose or any other ingredient.
The present invention resides in providing sweetener compositions with enhanced sweetness intensity as well as reduced undesirable aftertaste, comprising essentially of sucralose admixed with one or more of sweetness enhancing agents and bitterness reducing agents selected from the group comprising of fructooligosaccharides (FOS), neotame, stevia, neohesperidine and thaumatin. While the prior art teaches away from any synergy in combining natural sugars such as fructose, sucrose or glucoses with sucralose, it has now surprisingly been found that a combination of sucralose with fructooligosaccharides shows a tremendous
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improvement of sweetness intensity, thereby enabling a reduction in the amount of sweetener intake for a subject. The added advantages of use of fructooligosaccharides has been the surprising reduction in undesirable bitter or metallic aftertaste of other sweeteners as well as the reduction in cost due to the easy availability of FOS.
It has been found that a combination of sucralose with saccharides such as fructose, glucose, maltose and other gluco-ologosaccharides, mixtures thereof with invert sugar, high fructose com syrups, starch derived glucose syrups and sugar alcohols, particularly monosaccharide sugar alcohols such as xyliton, sorbital and mannitol, as well as FOS obtained from sucrose and stevia as well other sweetener agents such as neohesperidine and neotame result in a sweetener composition with a significant enhancement of sweetness intensity as well as reduced or absent undesirable aftertastes.
Fructo-oligosaccharides (FOS), also known as neosugars, are short-chain oligosaccharides comprised of D-fructose and D-glucose, containing from three to five monosaccharide units. FOS are produced on a commercial scale from sucrose using a fungal fructosyltransferase enzyme. FOS are resistant to digestion in the upper gastrointestinal tract and s re known to stimulate the growth of Bifidobacterium species in the large intestine. FOS are marketed in the United States in combination with probiotic bacteria and in some functional food products.
Fructooligosaccharides (FOS) are one of the best-documented natural nutrients for promoting the growth the lactobacilli and bifidobacteria that are the linchpin of sound health. FOS has also been clinically studied for its ability to increase magnesium and calcium absorption, lower blood glucose, cholesterol, and LDL levels, and to inhibit production of the reductase enzymes that can contribute to cancer. Because FOS may increase magnesium absorption, it may also lead to lowered blood pressure and better cardiovascular health. In addition, FOS also has another benefit: It has a naturally sweet taste
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Stevia is a perennial shrub that grows up to 1 m tall and has leaves 2-3 cm long. It belongs to the Aster family, which is indigenous to the northern regions of South America. Stevia is still found growing wild in the highlands of the Amambay and Iguacu districts (a border area between Brazil and Paraguay). It is grown commercially in many parts of Brazil, Paraguay, Uruguay, Central America, Israel, Thailand, and China. The use of stevia as a sweetener is well known in tribal and herbal medicine in Brazil and Paraguay. The shrub is known locally as kaa jhee by the Guarani Indians of Paraguay who use it to sweeten their yerba mate tea. It is also known to be used for sweetening other teas and foods and medicinally as a cardiotonic, for obesity, hypertension, and heartburn, and to help lower uric acid levels.
In addition to being a sweetener, stevia is considered in Brazilian herbal medicine to be hypoglycemic, hypotensive, diuretic, cardiotonic, and tonic. The leaf is used for diabetes, obesity, cavities, hypertension, fatigue, depression, sweet cravings, and infections. The leaf is employed in traditional medical systems in Paraguay for the same purposes as in Brazil. In the United States, herbalists use the leaf for diabetes, high blood pressure, infections, and as a sweetening agent. In Japan and Brazil, stevia is approved as a food additive and sugar substitute.
Over 100 phytochomicals have been discovered in stevia. It is rich in terpenes
and flavonoids. The constituents responsible for stevia's sweetness were documented
in 1931, when eight novel plant chemicals called glycosides were discovered and
named. Of these eight glycosides, one called stevioside is considered the sweetest -
and has been tested to be approximately 300 times sweeter than sugar. Stevioside,
comprising 6-18% of the stevia leaf, is also the most prevalent glycoside in the leaf.
Other sweet constituents include steviolbioside, rebausiosides A-E, and dulcoside A.
The main plant chemicals: in stevia include: apigenin, austroinulin, avicularin, beta-
sitosterol, caffeic acid, campesterol, caryophyllene, centaureidin, chlorogenic acid,
chlorophyll, cosmosiin, cynaroside, daucosterol, diterpene glycosides, dulcosides A-B,
foeniculin, formic acid, gibberellic acid, gibberellin, indole-3-acetonitrile, isoquercitrin,
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isosteviol, jhanol, kaempferol, kaurene, lupeol, luteolin, polystachoside, quercetin, quercitrin, rebaudioside A-F, scopoletin, sterebin A-H, steviol, steviolbioside, steviolmonoside, steviouide, stevioside a-3, stigmasterol, umbelliferone, and xanthophylls.
The main sweet chemical, stevioside, has been found to be nontoxic in acute toxicity studies with rats, rabbits, guinea pigs, and birds. It also has been shown not to cause cellular changes (mutagenic) or to have any effect on fertility. The natural stevia leaf also has been found 1;o be nontoxic and has no mutagenic activity. Studies conflict as to the effect of stevia leaf on fertility. While the majority of clinical studies show stevia leaf to have no effect on fertility in both males and females, one study reveals that the water extract of the leaf reduces testosterone levels and sperm count in male rats.
Therefore, the present invention provides a sweetener composition comprising sucralose and a sweetening agent selected from the group consisting of fructooligosaccharides, stevia, sugar alcohols, saccharides selected in turn from glucose, maltose, fructose:, neotame, neohesperidine and thaumatin, or any mixture thereof. The present invention also provides a method for the preparation of such compositions comprising combining sucralose with one or more of sweetening agents selected from the group consisting of fructooligosaccharides, stevia, sugar alcohols, saccharides selected in turn from glucose, maltose, fructose, neotame, neohesperidine and thaumatin, or any mixture thereof, and adding if desired one or more of conventional additives such as bulking agents, diluents, coloring agents and the like. The composition of the invention may be in oral powder or syrup form, and can be used as a food additive. Examples of foods where such compositions can be used include beverages such as carbonated soft drinks, chocolates, cereals, energy drinks, bakery products, diet foods and supplements, and the like. The compositions of the invention can also be used as such as a table top sweetener such as for coffee or tea.
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It has been observed that the increased sweetening power is to the scale of 650 to 2500, when the sweetness index is taken as 1 based on the sweetness of sucrose. The synergy is observed per unit weight obtained for the composition as a percentage of the expected degree of sweetening power (sum total of the sweetening powers of the theoretical sweetening powers of each ingredient). It has been observed that the saving in amounts is to extent of at least 25% for fructose and at least 18% with invert sugar.
In the invention, all sweeteners were prepared with tap water and served at room temperature. All concentrations are expressed as percentages of weight by volume. Concentrations of sucralose, fructose, invert sugar, glucose, high fructose corn syrup, glucose syrup, xylitol, mannitol, sorbitol and sucrose were equisweet with standard sucrose solution and were measured by taste panels using constant stimulus paired comparison method. A series of five or more concentrations of increasing intensity were prepared for each sweetener such that the mid-concentration was approximately the same sweetness as the sucrose control.
It was observed that while the sugar intensity of FOS is approximately 1, and that of sucralose is approximately 600, a mixture thereof revealed a sweetness intensity in the range of over 700. In the testing followed to validate the invention, the following samples were prepared:
1. 8 mg of sucralose in 100 ml water is equivalent to 4.8 g of Sugar in 100 ml water.
Sweetness of both the solutions is same and identical. Hence, Sucralose is required
600 times lesser as compared to Sugar
2. Levels of Sucralose drop by more than 1000 times compared to Sugar requirement
when blended with Fructo Oligosaccharide. Various trials undertaken with 10:90,
20:80, 30:70, 40:60, 50:50, 60:40, 70:30, 80:20, 90:10, 100:0
The combinations prepared above were tested and it was noted that there was a drastic increase in sweetness intensity. The parameters of the study comprised preparation of the solutions of the above concentration in 100 ml water and taste-test
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subjected at 30°C (Room Temperature). The standard solution prepared from Sugar (5 g in 100 ml water) and all the above concentrations were evaluated for sweetness profile.
It has also been observed in the invention that the use of Neohesperidine
further enhances the sweetness intensity of the combination thereby resulting in
lowering the quantity of Sucralose required by 1500 times compared to Sugar quantity. Thus, in place of 5 g sugar just less than 4 mg sucralose would be required in the sweetener combination. (3.5 mg).
An alternative anc more useful measure of synergy is the percentage saving, that is to say the difference between the amount actually needed to obtain a certain degree of sweetness and the theoretical amount needed expressed as a percentage of the theoretical amount needed. The combination would result in cost savings as far as formulation cost is concerned. With the reduced levels of Sucralose (which is expensive) & cost of Fructo oligosaccharide is reasonably lower. Combination would yield substantial (at least 30%) cost savings.
The present invention provides several advantages over the prior art. The FOS acts as not only sweetening agents but also binders enabling formation of the composition into different dosage forms. In addition, the combination of sucralose with FOS, (and with or without stevia or neohesperidine) shows drastic enhancement in sweetness intensity. The compositions of the invention also show reduced lingering effect with respect to sweetness as well as a balanced sweetness profile without leaving any bitter or metal ic aftertastes. The other advantages associated with the invention include improved sensory profile, mouth feel, aroma of various foods formulations such as Beverages, Dessert mixes, Sweets, Confectionary, Protein -Fiber Diskettes & Biscuits, Cookies, Confectionery, Chocolates,
FOS helps to activate taste buds with specific reference to sweetness. This
effect is not reported in any literature to the best of the knowledge of the applicants.
FOS replaces Lactose from the formulation, which is used mainly as a binder in tablets
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compression, thus enabling tablet form for use as a table top sweetener without lactose. This is of special interest for subjects suffering from lactose intolerance. It has also been observed that the compositions are heat resistant thereby enabling their use in bakery products and processed food products.
Examples
1. Combinations of sucralose and neotame in various proportions such as 50:50, 40:60; 60:40; 70:30: 80:20; 90:10 and 100:0 were prepared and their sweetness profile tested by taste tests by an independent panel of experts. It was observed that combinations of sucralose with neotame worked very well without reduction in sweetness intensity. It was particularly observed that for specific food applications, specific combinations work better in terms of taste profile and sweetness synergy. For example a 70:30 ratio worked best for fruit juices and 80:20 for carbonated beverages.
2. Combinations of sucralose and fructooligosaccharide in various ratios of 10:90; 20:80; 30:70; 40:60; 50:50; 60:40; 70:30; 80:20 and 90:10 were prepared and their sweetness intensity tested by means of blind tests. It was observed that the formulations showed the same levels of sweetness as those of pure sucralose formulations but without or reduction in metallic after taste or lingering sweetness.
Details are given in Figure 1.
3. Solutions of the concentrations listed in (2) above were prepared in 100 ml water and taste tests carried out at 30°C (room temperature). The standard solution was prepared from sugar (5g in 100 ml water). The sweetness profile of all concentrations was evaluated using standard methodology.
4. To the formulations of (3) above, neohesperidine was added in an amount of up to 0.1 to 2 % by weight. It was observed that this further resulted in enhancement of sweetness intensity when tested according to standard methodology. The quantity of sucralose required was reduced by over 1000-15000 times
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Various bulking agents such as maltodextrin, oligosaccharides can also be used in order to enhance the bulk of the sweetener without enhancing the calorie levels of the sweetener composition.
The above examples are illustrative and departures are possible therefrom without departing from the spirit and scope of the invention in any manner.
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We claim:
1. A sweetener composition comprising sucralose and a sweetness enhancing agent selected from the group consisting of fructooligosaccharide, neotame, stevia, neohesperidine, saccharides and thaumatin, wherein the inter se ratios of the sucralose to the sweetness enhancing agent is in the range of 10:90 to 90:10 by weight, the balance if any comprising one of more conventional adjuvants such as bulking agents, diluents, viscosity modifiers, coloring agents.
2. A sweetener composition as claimed in claim 1 wherein the saccharides are selected from the group consisting of glucose, fructose and maltose.
3. A sweetener compositon as claimed in claim 1 or 2 wherein the ratio of the sucralose to the sweetness enhancing agent is selected from 80:20; 70:30; 60:40; 50:50; 40:60; 30:70; 20: B0.
4. A composition as claimed in any preceding claim wherein the sweetness enhancing agent is neotame.
5. A process for the preparation of a sweetener composition comprising mixing in any known manner sucralose and a sweetness enhancing agent selected from the group consisting of fructooligosaccharide, neotame, stevia, neohesperidine, saccharides and thaumatin, wherein the inter se ratios of the sucralose to the sweetness enhancing agent is in the range of 10:90 to 90:10 by weight, the balance if any comprising one of more conventional adjuvants such as bulking agents, diluents, viscosity modifiers, coloring agents.
6. A process as claimed in claim 5 wherein saccharides are selected from the group consisting of glucose, fructose and maltose.
7. A process as claimed in claim 5 or 6 wherein wherein the ratio of the sucralose to the sweetness enhancing agent is selected from 80:20; 70:30; 60:40; 50:50; 40:60; 30:70; 20:80.
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8. A composition as claimed in any preceding claim 5 to 7 wherein the sweetness enhancing agent is neotame.
9. A sweetener composition substantially as described hereinbefore and with reference to the foregoing examples and accompanying drawings.
10. A process substantially as described hereinbefore and with reference to the foregoing examples and accompanying drawings.
Dated this the 11th day of July 2005.

ABSTRACT
SWEETENER COMPOSITION WITH ENHANCED SWEETNESS
The present invention relates to a sweetener composition comprising sucralose and a sweetness enhancing agent selected from the group consisting of fructooligosaccharide, neotame, stevia, neohesperidine, saccharides and thaumatin, wherein the inter se ratios of the sucralose to the sweetness enhancing agent is in the range of 10:90 to 90:10 by weight, the balance if any comprising one of more conventional adjuvants such as bulking agents, diluents, viscosity modifiers, coloring agents and to a method of preparation thereof and use thereof in food products.

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12 JUL 2006