Indian Patents. 253285:COMPOSITION COMPRISING AN ACTIVE CORE ENCAPSULATED BY MATRIX INCLUDING POLYMER AND SUCRALOSE AND METHOD OF PREPARATION THEREOF

Title of Invention	COMPOSITION COMPRISING AN ACTIVE CORE ENCAPSULATED BY MATRIX INCLUDING POLYMER AND SUCRALOSE AND METHOD OF PREPARATION THEREOF
Abstract	Some embodiments provide a composition including active region which includes an active such as sucralose and at least one coating layer contiguous with the active region. The coating layer includes a polymer and sucralose; wherein the coating layer either partially or completely surrounds and encapsulates the active region.

Full Text	FIELD Included are encapsulated compositions including a polymer and sucralose. The compositions include an encapsulant including a polymer in combination with sucralose. Methods of preparing the encapsulated compositions are also provided. BACKGROUND Encapsulated intense sweeteners have a particular advantage when included in gum compositions such as chewing gum and bubble gum compositions. The encapsulated sweeteners are not immediately released as sugar would be when included in a chewing gum. By contrast, an encapsulated sweetener composition provides extended sweetening on chewing because the sweetener is not released until the encapsulating material has been subjected to mastication. Intense sweeteners such as aspartame (APM) and acesulfame potassium (Ace-K) have been used in encapsulated compositions in combination with high molecular weight polymers which allow for their slow release upon chewing in a gum composition. Sucralose is another popular intense sweetener which is derived from sucrose in which one or more hydroxy groups are replaced by chlorine atoms. This compound is described in U.K. Patent No. 1,543,167, the disclosure of which is incorporated herein by reference. Sucralose may be referred to by different chemical names including: 4-chloro-4- deoxy-a-D-galactopyranosyl, l,6-dichlorol,6-dideoxy- P-D-fructofuranoside, and known as 4,r,6',-trichloro-4,r,6'-trideoxygalactosucrose. Sucralose is relatively stable and inert. This includes exhibiting stability in acid aqueous solutions, in marked contrast to peptide-based sweeteners such as aspartame. Under completely dry conditions, however, sucralose which is present in a crystalline form tends to discolor in response to elevated temperatures. For example, such discoloration can be exhibited after twenty minutes of exposure of pure dry sucralose to a temperature of 100°C, wherein the color changes to a pale brown. This degradation of sucralose results in a commercially unacceptable product. This high temperature instability of sucralose has made it commercially impractical to prepare an encapsulated sucralose with the extrusion techniques used to prepare the encapsulated APM and Ace-K compositions using high tensile strength / softening point polymers. Since sucralose is a desirable sweetener, and is preferred for compositions where APM stability is questionable, there is a need for an encapsulated sucralose composition which may be used in a variety of compositions including gum compositions. Ideally, the encapsulated composition would include an active such as another sweetener, medicament, vitamin or flavor. SUMMARY In some embodiments, there is a composition which includes an active and at least one coating layer. The coating layer includes polyvinyl acetate and sucralose and at least partially encapsulates the active. Also provided is a sucralose composition which includes a sucralose region and at least one encapsulating layer which includes a polymer such as polyvinyl acetate and sucralose. Some embodiments also provide a composition including a sucralose region and at least one coating layer contiguous with the sucralose region. The coating layer includes a polymer and sucralose; wherein the coating layer completely surrounds the sucralose region. Other embodiments provide a method of preparing a composition comprising which includes: (a) suspending, active particles in a fiuidizing air stream; (b) preparing a coating composition including a polymer, sucralose, and a solvent; and (c) spraying the coating composition onto the suspended active particles to provide an encapsulated composition. In other embodiments there is an encapsulated sweetener prepared by the following steps: (a) suspending sucralose particles in a fluidizing air stream; (b) preparing a coating composition including a polymer, sucralose, and a solvent; (c) spraying the coating composition onto the sucralose particles to provide an encapsulated sucralose composition; and (d) evaporating the solvent from the encapsulated sucralose composition. In some embodiments, there is a composition including a plurality of particles including comprising an active core encapsulated by a matrix including polymer and sucralose. DETAILED DESCRIPTION As used herein the transitional tenn "comprising," (also "comprises," etc.) which is synonymous with "including," "containing," or "characterized by," is inclusive or open-ended and does not exclude additional, unrecited elements or method steps, regardless of its use in the preamble or the body of a claim. As used herein, the terms "bubble gum" and "chewing gum" are used interchangeably and are both meant to include any gum compositions. As used herein, the term "active" refers to any composition which may be included in the encapsulated compositions of some embodiments, wherein the active provides some desirable property upon release from encapsulation. Examples of suitable actives include sweeteners, such as sucralose, flavors, medicaments, vitamins, and combinations thereof. For the encapsulated compositions of some embodiments, the coating composition includes a high-tensile strength polymer in addition to sucralose. The active may encapsulated by the coating composition either wholly or partly. The active may alternatively be part of a matrix formed by the polymer in combination with sucralose. In the encapsulated composition, the active may be present in any desired amount, such as from about 5% to about 50% by weight of the encapsulated composition. Any of a variety of active ingredients may be included in the present embodiments. These include sweeteners, flavors, breath-freshening agents, medicaments such as analgesics, anti-histamines, decongestants, and antacids, and vitamins. Suitable sweeteners may be selected from a wide range of materials including water- soluble sweeteners, water-soluble artificial sweeteners, water-soluble sweeteners derived from naturally occurring water-soluble sweeteners, dipeptide based sweeteners, and protein based sweeteners, including mixtures thereof. Without being limited to particular sweeteners, representative categories and examples include: (a) water-soluble sweetening agents such as dihydrochalcones, monellin, steviosides, glycyrrhizin, dihydioflavenol, and sugar alcohols such as sorbitol, mannitol, maltitol, and L- aminodicarboxylic acid aminoalkenoic acid ester amides, such as those disclosed in U.S. Pat. No. 4,619,834, which disclosure is incorporated herein by reference, and mixtures thereof; (b) water-soluble artificial sweeteners such as soluble saccharin salts, i.e., sodium or calcium saccharin salts, cyclamate salts, the sodium, ammonium or calcium salt of 3,4- dihydro-6-methyl-l,2,3-oxathiazine-4-one-2,2-dioxide, the potassium salt of 3,4-dihydro-6- methyl-l,2,3-oxathiazine-4-one-2,2-dioxide (Acesulfame-K), the free acid form of saccharin, and mixtures thereof; (c) dipeptide based sweeteners, such as L-aspartic acid derived sweeteners, such as L-aspartyl-L-phenylalanine methyl ester (Aspartame) and materials described in U.S. Pat. No. 3,492,131, L-alphaaspartyl-N-(2,2,4,4-tetramemyl-3-thietanyl)-D-alaninarnide hydrate (Alitame), methyl esters of L-aspartyl-L-phenylglycerine and L-aspartyl-L-2,5- dihydrophenyl-glycine, L-aspartyl-2,5-dihydro-L-phenylalanine; L-aspartyl-L-(l- cyclohexen)-alanine, and mixtures thereof; (d) water-soluble sweeteners derived from naturally occurring water-soluble sweeteners, such as chlorinated derivatives of ordinary sugar (sucrose), e.g., chlorodeoxysugar derivatives such as derivatives of chlorodeoxysucrose or chlorodeoxygalactosucrose, known, for example, under the product designation of Sucralose; examples of chlorodeoxysucrose and chlorodeoxygalactosucrose derivatives include but are not limited to: l-chloro-l'-deoxysucrose; 4-chloro-4-deoxy-alpha-D-galactopyranosyl-alpha- D-fructofuranoside, or 4-chloro-4-deoxygalactosucrose; 4-chloro-4-deoxy-alpha-D- galactopyranosyl-1-chloro-l-deoxy-beta-D-fructo-furanoside, or 4,1'-dichloro-4,1- dideoxygalactosucrose; 1,6'-dichloror,6'-dideoxysucrose;4-chloro-4-deoxy-alpha-D- galactopyranosyl-l,6-dichloro-l,6-dideoxy-beta-D- fructofuranoside, or 4,1,6,-trichloro- 4,r,6'-trideoxygalactosucrose;4,6-dichloro-4,6-dlideoxy-alpha-D-galactopyranosyl-6-chloro- 6~deoxy-beta-D- fructofuranoside, or 4,6,6'-trichloro4,6,6-trideoxygalactosucrose; 6,1',6'- trichloro-6,1,6'-trideoxysucarose,4,6-dichloro-4,6-dideoxy-alpha-D-galacto-pyranosyl-1,6- dichloro-l,6-dideox y-beta-D-fructoforanoside, or 4,6,r,6'-tetraachloro 4,6,1,6'- tetradeoxygalacto-sucrose; and 4,6,1,6'-tetradeoxy-sucrose, and mixtures thereof; and (e) protein based sweeteners such as thaumaoccous danielli (Thaumatin I and II). The intense sweetening agents may be used in many distinct physical forms well- known in the art to provide an initial burst of sweetness and/or a prolonged sensation of sweetness. Without being limited thereto, such physical forms include free forms, such as spray dried, powdered, beaded forms, encapsulated forms, and mixtures thereof. In some embodiments wherein the active is a sweetener, it may be a high intensity sweetener such as sucralose, saccharin salts, acesulfame potassium, aspartame, thaumatin, neotame, alitame, and combinations thereof. More specifically, sucralose may be used alone or in combination with another sweetener either as the active or in the coating layer. The flavoring agents which may be used include those flavors known to the skilled artisan, such as natural and artificial flavors. These flavorings may be chosen from synthetic flavor oils and flavoring aromatics and/or oils, oleoresins and extracts derived from plants, leaves, flowers, fruits, and so forth, and combinations thereof. Nonlimiting representative flavor oils include spearmint oil, cinnamon oil, oil of wintergreen (methyl salicylate), peppermint oil, clove oil, bay oil, anise oil, eucalyptus oil, thyme oil, cedar leaf oil, oil of nutmeg, allspice, oil of sage, mace, oil of bitter almonds, and cassia oil. Also useful flavorings are artificial, natural and synthetic fruit flavors such as vanilla, and citrus oils including lemon, orange, lime, grapefruit, and fruit essences including apple, pear, peach, grape, strawberry, raspberry, cherry, plum, pineapple, apricot and so forth. These flavoring agents may be used in liquid or solid form and may be used individually or in admixture. Commonly used flavors include rnints such as peppermint, menthol, spearmint, artificial vanilla, cinnamon derivatives, and various fruit flavors, whether employed individually or in admixture. Flavors may also provide breath freshening properties, particularly the mint flavors. Other useful flavorings include aldehydes and esters such as cinnamyl acetate, cinnamaldehyde, citral diethylacetal, dihydrocarvyl acetate, eugenyl formate, p- methylamisol, and so forth may be used. Generally any flavoring or food additive such as those described in Chemicals Used in Food Processing, publication 1274, pages 63-258, by the National Academy of Sciences, may be used. This publication is incorporated herein by reference. This may include natural as well as synthetic flavors. Further examples of aldehyde flavorings include but are not limited to acetaldehyde (apple), benzaldehyde (cherry, almond), anisic aldehyde (licorice, anise), cinnamic aldehyde (cinnamon), citral, i.e., alpha-citral (lemon, lime), neral, i.e., beta-citral (lemon, lime), decanal (orange, lemon), ethyl vanillin (vanilla, cream), heliotrope, i.e., piperonal (vanilla, cream), vanillin (vanilla, cream), alpha-amyl cinnamaldehyde (spicy fruity flavors), butyraldehyde (butter, cheese), valeraldehyde (butter, cheese), citronellal (modifies, many types), decanal (citrus fruits), aldehyde C-8 (citrus fruits), aldehyde C-9 (citrus fruits), aldehyde C-12 (citrus fruits), 2-ethyl butyraldehyde (berry fruits), hexenal, i.e., trans-2 (berry fruits), tolyl aldehyde (cherry, almond), veratraldehyde (vanilla), 2,6-dimethyl-5-heptenal, i.e., melonal (melon), 2,6-dimethyloctanal (green fruit), and 2-dodecenal (citrus, mandarin), cherry, grape, strawberry shortcake, and mixtures thereof. In some embodiments, a flavoring agent may be employed in either liquid form and/or dried form. When employed in the latter form, suitable drying means such as spray drying the oil may be used. Alternatively, the flavoring agent may be absorbed onto water soluble materials, such as cellulose, starch, sugar, maltodextrin, gum arabic and so forth or may be encapsulated. The actual techniques for preparing such dried forms are well-known. In some embodiments, the flavoring agents may be used in many distinct physical forms well-known in the art to provide an initial burst of flavor and/or a prolonged sensation of flavor. Without being limited thereto, such physical forms include free forms, such as spray dried, powdered, beaded forms, encapsulated forms, and mixtures thereof. The amount of flavoring agent employed herein may be a matter of preference subject to such factors as the type of final chewing gum composition, the individual flavor, the gum base employed, and the strength of flavor desired. Thus, the amount of flavoring may be varied in order to obtain the result desired in the final product and such variations are within the capabilities of those skilled in the art without the need for undue experimentation. In gum compositions, the flavoring agent is generally present in amounts from about 0.02% to about 5%, and more specifically from about 0.1% to about 2%, and even more specifically, from about 0.8% to about 1.8%, by weight of the chewing gum composition. A variety of drugs, including medications, herbs, and nutritional supplements may also be included as the active to be encapsulated. Examples of useful drugs include ace- inhibitors, antianginal drugs, anti-arrhythmias, anti-asthmatics, anti-cholesterolemics, analgesics, anesthetics, anti-convulsants, anti-depressants, anti-diabetic agents, anti-diarrhea preparations, antidotes, anti-histamines, anti-hypertensive drugs, anti-inflammatory agents, anti-lipid agents, anti-manics, anti-nauseants, anti-stroke agents, anti-thyroid preparations, anti-tumor drugs, anti-viral agents, acne drugs, alkaloids, amino acid preparations, anti- tussives, anti-uricemic drugs, anti-viral drugs, anabolic preparations, systemic and non- systemic anti-infective agents, anti-neoplasties, anti-parkinsonian agents, anti-rheumatic agents, appetite stimulants, biological response modifiers, blood modifiers, bone metabolism regulators, cardiovascular agents, central nervous system stimulates, cholinesterase inhibitors, contraceptives, decongestants, dietary supplements, dopamine receptor agonists, endometriosis management agents, enzymes, erectile dysfunction therapies such as sildenafil citrate, which is currently marketed as Viagra®, fertility agents, gastrointestinal agents, homeopathic remedies, hormones, hypercalcemia and hypocalcemia management agents, immunomodulators, immunosuppressives, migraine preparations, motion sickness treatments, muscle relaxants, obesity management agents, osteoporosis preparations, oxytocics, parasympatholytics, parasympathomimetics, prostaglandins, psychotherapeutic agents, respiratory agents, sedatives, smoking cessation aids such as bromocryptine or nicotine, sympatholytics, tremor preparations, urinary tract agents, vasodilators, laxatives, antacids, ion exchange resins, anti-pyretics, appetite suppressants, expectorants, anti-anxiety agents, anti- ulcer agents, anti-inflammatory substances, coronary dilators, cerebral dilators, peripheral vasodilators, psycho-tropics, stimulants, anti-hypertensive drugs, vasoconstrictors, migraine treatments, antibiotics, tranquilizers, anti-psychotics, anti-tumor drugs, anti-coagulants, anti- thrombotic drugs, hypnotics, anti-emetics, anti-nauseants, anti-convulsants, neuromuscular drugs, hyper- and hypo-glycemic agents, thyroid and anti-thyroid preparations, diuretics, anti- spasmodics, terine relaxants, anti-obesity drugs, erythropoietic drugs, anti-asthmatics, cough suppressants,, mucolytics, DNA and genetic modifying drugs, and combinations thereof. The coating layer which surrounds the active, may also include a solvent. In addition to the sucralose and polymer, the solvent should be capable of dissolving the polymer, The solvent may be any solvent known for this purpose. For example, if the polymer is polyvinyl acetate, suitable solvents include of ethyl acetate, diethyl ether, acetone, benzene, ethylene dichloride, methanol, methyl ethyl ketone, ethanol, toluene, xylene, amyl acetate, and combinations thereof. One or more coating layers may be present. In some embodiments wherein more than one coating layer is present, the first coating layer may include sucralose and a high tensile strength polymer, with the optional addition of another sweetener. A second coating may completely or partially encapsulate the active particles and may include either a single polymer, a combination of different polymers, or a combination of one or rnore polymers and a sweetener such as sucralose. Polymers which may be used in the coating layers include acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene, polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof. One or more different polymers may be used in each of the coating layers. For example, polyvinyl acetate may be included in a first coating with a combination of polyvinyl acetate and another polymer in a subsequent exterior coating. The encapsulated particles of some embodiments may be prepared by any suitable spray coating method as known in the art. One suitable process is the Wurster process. This process provides a method for encapsulating individual particulate materials. First the particles to be encapsulated are suspended in a fluidizing air stream which provides a generally cyclic flow in front of a spray nozzle. The spray nozzle sprays an atomized flow of the coating solution, which will include sucralose, a polymer and a suitable solvent. The atomized coating solution collides with the particles as they are carried away from the nozzle to provide a particle coating with the coating solution. The temperature of the fluidizing air stream, which also serves to suspend the particles to be coated, may be adjusted to evaporate the solvent shortly after the coating solution contacts the particles. This serves to solidify the coating on the particles, resulting in the desired encapsulated particle. This process may be repeated until the desired thickness of the coating is achieved. Alternatively, 1he process may be repeated with a different coating solution to provide different and distinct coating layers in the encapsulated particle composition. Following the coating process, the particles may then be formed to an appropriate size as desired, generally from an average particle size range of about 50 µm to about 800 µm. This may be accomplished by any suitable means such as chopping, pulverizing, milling or grinding the particles. The gum compositions of some embodiments may include a gum base as well as the encapsulated active composition. The gum base may include any component known in the chewing gum art. For example, the gum base may include elastomers, bulking agents, waxes, elastomer solvents, emulsifiers, plasticizers, fillers and mixtures thereof. The elastomers (rubbers) employed in the gum base will vary greatly depending upon various factors such as the type of gum base desired, the consistency of gum composition desired and the other components used in the composition to make the final chewing gum product. The elastomer may be any water-insoluble polymer known in the art, and includes those gum polymers utilized for chewing gums and bubble gums. Illustrative examples of suitable polymers in gum bases include both natural and synthetic elastomers. For example, those polymers which are suitable in gum base compositions include, without limitation, natural substances (of vegetable origin) such as chicle, natural rubber, crown gum, nispero, rosidinha, jelutong, perillo, niger gutta, tunu, balata, guttapercha, lechi capsi, sorva, gutta kay, and the like, and combinations thereof. Examples of synthetic elastomers include, without limitation, styrene-butadiene copolymers (SBR), polyisobutylene, isobutylene-isoprene copolymers, polyethylene, polyvinyl acetate and the like, and combinations thereof. Additional useful polymers include: crosslinked polyvinyl pyrrolidone, polymethylmethacrylate; copolymers of lactic acid, polyhydroxyalkanoates, plasticized ethylcellulose, polyvinyl acetatephthalate and combinations thereof. The amount of elastomer employed in the gum base may vary depending upon various factors such as the type of gum base used, the consistency of the gum composition desired and the other components used in the composition to make the final chewing gum product. In general, the elastomer will be present, in the gum base in an amount from about 10% to about 60% by weight of the gum region, desirably from about 35% to about 40% by weight In some embodiments, the gum base may include wax. It softens the polymeric elastomer mixture and improves the elasticity of the gum base. When present, the waxes employed will have a melting point below about 60°C, and preferably between about 45°C. and about 55°C. The low melting wax may be a paraffin wax. The wax may be present in the gum base in an amount from about 6% to about 10%, and preferably from about 7% to about 9.5%, by weight of the gum base. In addition to the low melting point waxes, waxes having a higher melting point may be used in the gum base in amounts up to about 5%, by weight of the gum base. Such high melting waxes include beeswax, vegetable wax, candelilla wax, carnuba wax, most petroleum waxes, and the like, and mixtures thereof. In addition to the components set out above, the gum base may include a variety of other ingredients, such as components selected from elastomer solvents, emulsifiers, plasticizers, fillers, and mixtures thereof. The gum base may contain elastomer solvents to aid in softening the elastomer component. Such elastomer solvents may include those elastomer solvents known in the art, for example, terpinene resins such as polymers of alpha-pinene or beta-pinene, methyl, glycerol and pentaerythritol esters of rosins and modified rosins and gums such as hydrogenated, dimerized and polymerized rosins, and mixtures thereof. Examples of elastomer solvents suitable for use herein may include the pentaerythritol ester of partially hydrogenated wood and gum rosin, the pentaerythritol ester of wood and gum rosin, the glycerol ester of wood rosin, the glycerol ester of partially dimerized wood and gum rosin, the glycerol ester of polymerized wood and gum rosin, the glycerol ester of tall oil rosin, the glycerol ester of wood and gum rosin and the partially hydrogenated wood and gum rosin and the partially hydrogenated methyl ester of wood and rosin, and the like, and mixtures thereof. The elastomer solvent may be employed in the gum base in amounts from about 2% to about 15%, and preferably from about 7% to about 11%, by weight of the gum base. The gum base may also include emulsifiers which aid in dispersing the immiscible components into a single stable system. The emulsifiers useful in this invention include glyceryl monostearate, lecithin, fatty acid monoglycerides, diglycerides, propylene glycol monostearate, and the like, and mixtures thereof. The emulsifier may be employed in amounts from about 2% to about 15%, and more specifically, from about 7% to about 11%, by weight of the gum base. The gum base may also include plasticizers or softeners to provide a variety of desirable textures and consistency properties. Because of the low molecular weight of these ingredients, the plasticizers and softeners are able to penetrate the fundamental structure of the gum base making it plastic and less viscous. Useful plasticizers and softeners include lanolin, palmitic acid, oleic acid, stearic acid, sodium stearate, potassium stearate, glyceryl triacetate, glyceryl lecithin, glyceryl monostearate, propylene glycol monostearate, acetylated monoglyceride, glycerine, and the like, and mixtures thereof. Waxes, for example, natural and synthetic waxes, hydrogenated vegetable oils, petroleum waxes such as polyurethane waxes, polyethylene waxes, paraffin waxes, microcrystalline waxes, fatty waxes, sorbitan monostearate, tallow, propylene glycol, mixtures thereof, and the like, may also be incorporated into the gum base. The plasticizers and softeners are generally employed in the gum base in amounts up to about 20% by weight of the gum base, and more specifically in amounts from about 9% to about 17%, by weight of the gum base. Plasticizers also include are the hydrogenated vegetable oils and include soybean oil and cottonseed oil which may be employed alone or in combination. These plasticizers provide the gum base with good texture and soft chew characteristics. These plasticizers and softeners are generally employed in amounts from about 5% to about 14%, and more specifically in amounts from about 5% to about 13.5%, by weight of the gum base. Anhydrous glycerin may also be employed as a softening agent, such as the commercially available United States Pharmacopeia (USP) grade. Glycerin is a syrupy liquid with a sweet warm taste and has a sweetness of about 60% of that of cane sugar. Because glycerin is hygroscopic, the anhydrous glycerin may be maintained under anhydrous conditions throughout the preparation of the chewing gum composition. In some embodiments, the gum base of this invention may also include effective amounts of bulking agents such as mineral adjuvants which may serve as fillers and textural agents. Useful mineral adjuvants include calcium carbonate, magnesium carbonate, alumina, aluminum hydroxide, aluminum silicate, talc, tricalcium phosphate, dicalcium phosphate, calcium sulfate and the like, and mixtures thereof. These fillers or adjuvants may be used in the gum base compositions in various amounts. The amount of filler, may be present in an amount from about zero to about 40%, and more specifically from about zero to about 30%, by weight of the gum base. A variety of traditional ingredients may be optionally included in the gum compositions in effective amounts such as coloring agents, antioxidants, preservatives, flavoring agents, and the like. For example, titanium dioxide and other dyes suitable for food, drug and cosmetic applications, known as F. D. & C. dyes, may be utilized. An anti-oxidant such as butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), propyl gallate, and mixtures thereof, may also be included. Other conventional chewing gum additives known to one having ordinary skill in the chewing gum art may also be used in the gum base. The gum composition may include amounts of conventional additives selected from the group consisting of sweetening agents (sweeteners), plasticizers, softeners, emulsifiers, waxes, fillers, bulking agents (carriers, extenders, bulk sweeteners), mineral adjuvants, flavoring agents (flavors, flavorings), coloring agents (colorants, colorings), antioxidants, acidulants, thickeners, medicaments, and the like, and mixtures thereof. Some of these additives may serve more than one purpose. For example, in sugarless gum compositions, a sweetener, such as maltitol or other sugar alcohol, may also function as a bulking agent. The plasticizers, softening agents, mineral adjuvants, waxes and antioxidants discussed above, as being suitable for use in the gum base, may also be used in the chewing gum composition. Examples of other conventional additives which may be used include emulsifiers, such as lecithin and glyceryl monostearate, thickeners, used alone or in combination with other softeners, such as methyl cellulose, alginates, carrageenan, xanthan gum, gelatin, carob, tragacanth, locust bean gum, pectin, alginates, galactomannans such as guar gum, carob bean gum, glucomannan, gelatin, starch, starch derivatives, dextrins and cellulose derivatives such as carboxy methyl cellulose, acidulants such as malic acid, adipic acid, citric acid, tartaric acid, fumade acid, and mixtures thereof, and fillers, such as those discussed above under the category of mineral adjuvants. In some embodiments, the gum region may also contain a bulking agent. Suitable bulking agents may be water-soluble and include sweetening agents selected from, but not limited to, monosaccharides, disaccharides, polysaccharides, sugar alcohols, and mixtures thereof; randomly bonded glucose polymers such as those polymers distributed under the trade name POLYDEXTROSE by Pfizer, Inc., Groton, Conn.; isomalt (a racemic mixture of alpha-D-glucopyranosyl-l,6-mannitol and alpha-D-glucopyranosyl-L6-sorbitol manufactured under the trade name PALATINIT by Suddeutsche Zucker), maltodextrins; hydrogenated starch hydrolysates; hydrogenated hexoses; hydrogenated disaccharides; minerals, such as calcium carbonate, talc, titanium dioxide, dicalcium phosphate; celluloses; and mixtures thereof. Suitable sugar bulking agents include monosaccharides, disaccharides and polysaccharides such as xylose, ribulose, glucose (dextrose), mannose, galactose, fructose (levulose), sucrose (sugar), maltose, invert sugar, partially hydrolyzed starch and com syrup solids, and mixtures thereof. Suitable sugar alcohol bulking agents include sorbitol, xylitol, mannitol, galactitol maltitol, and mixtures thereof. Suitable hydrogenated starch hydrolysates include those disclosed in U.S. Pat. Nos. 25,959,3,356,811,4,279,931 and various hydrogenated glucose syrups and/or powders which contain sorbitol, hydrogenated disaccharides, hydrogenated higher polysaccharides, or mixtures thereof. Hydrogenated starch hydrolysates are primarily prepared by the controlled catalytic hydrogenation of corn syrups. The resulting hydrogenated starch hydrolysates are mixtures of monomelic, dimeric, and polymeric saccharides. The ratios of these different saccharides give different hydrogenated starch hydrolysates different properties. Mixtures of hydrogenated starch hydrolysates, such as LYCASIN, a commercially available product manufactured, by Roquette Freres of France, and HYSTAR, a commercially available product manufactured by Lonza, Inc., of Fairlawn, N.J., are also useful. Any sweetening agent or flavoring agent, as described above, may also be added as an optional component to the gum compositions. Coloring agents may be used in amounts effective to produce the desired color. The coloring agents may include pigments which may be incorporated in amounts up to about 6%, by weight of the gum composition. For example, titanium dioxide may be incorporated in amounts up to about 2%, and preferably less than about 1%, by weight of the gum composition. The colorants may also include natural food colors and dyes suitable for food, drug and cosmetic applications. These colorants are known as F.D.& C. dyes and lakes. The materials acceptable for the foregoing uses are preferably water-soluble. Illustrative nonlimiting examples include the indigoid dye known as F.D.& C. Blue No.2, which is the disodium salt of 5,5-indigotmdisulfonic acid. Similarly, the dye known as F.D.& C. Green No.l comprises a triphenylmethane dye and is the monosodium salt of 4-[4-(N-ethyl-p- sulfoniumbenzylamino)diphenylmemylene][l-(N-ethyl-N-p-sulfoniumbenzyl)-delta-2,5- cyclohexadieneimine]. A full recitation of all F.D.& C. colorants and their corresponding chemical structures may be found in the Kirk-Othmer Encyclopedia of Chemical Technology, 3rd Edition, in volume 5 at pages 857-884, which text is incorporated herein by reference. Suitable oils and fats usable in gum compositions include partially hydrogenated vegetable or animal fats, such as coconut oil, palm kernel oil, beef tallow, and lard, among others. These ingredients when used are generally present in amounts up to about 7%, and preferably up to about 3.5%, by weight of the gum composition. Some embodiments may include a method for preparing the improved chewing gum compositions for the gum region, including both chewing gum and bubble gum compositions. The chewing gum compositions may be prepared using standard techniques and equipment known to those skilled in the art. The apparatus useful in accordance with some embodiments comprises mixing and heating apparatus well known in the chewing gum manufacturing arts, and therefore the selection of the specific apparatus will be apparent to the artisan. While there have been described what are presently believed to be the preferred embodiments of the invention, those skilled in the art will realize that changes and modifications may be made thereto without departing from the spirit of the invention, and it is intended to include all such changes and modifications as fall within the true scope of the invention. WE CLAIM: 1. A composition comprising an active, selected from the group consisting of sweeteners, flavors, medicaments, vitamins, and combinations thereof, and at least one coating layer, such as herein described, wherein said coating layer either partially or completely encapsulate said active; and said coating layer comprises polyvinyl acetate and sucralose. 2. The composition as claimed in claim 1, wherein said coating layer contains a solvent, such as herein described. 3. The composition as claimed in claim 1, having additional coating layers. 4. The composition as claimed in claim 1, wherein said coating layer contains an additional sweetener other than sucralose. 5. The composition as claimed in claim 1, wherein said sweetener is a high intensity sweetener. 6. The composition as claimed in claim 1, having an additional coating layer, wherein (1) said additional coating layer comprises a polymer and (2) said additional coating layer completely surrounds said encapsulated composition. 7. The composition as claimed in claim 6, wherein said polymer of the additional coating layer is selected from the group consisting of acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene, polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof. 8. The composition as claimed in claim 4, wherein said additional sweetener comprises a high intensity sweetener. 9. The composition as claimed in claim 8, wherein Said additional sweetener is a member selected from the group consisting of saccharin salts, acesulfame potassium, aspartame, thaumatin, neotame, alitame, and combinations thereof. 10. The composition as claimed in claim 2, wherein said solvent is selected from the group consisting of ethyl acetate, diethyl ether, acetone, benzene, ethylene dichloride, methanol, methyl ethyl ketone, ethanol, toluene, xylene, amyl acetate, and combinations thereof. 11. The composition as claimed in claim 1, wherein said encapsulated composition comprises particles having an average particle size range of 50 urn to 800 µm. 12. A composition as claimed in claim 1, having a sucralose region and at least one coating layer contiguous with said sucralose region; said coating layer comprising a polymer and sucralose; wherein said coating layer completely surrounds said sucralose region. 13. The composition as claimed in claim 12, wherein said polymer is selected from the group consisting of acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene, polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof. 14. The composition as claimed in claim 13, wherein said polymer comprises polyvinyl acetate. 15. The composition as claimed in claim 12, wherein said coating layer contains a solvent, such as herein described. 16. The composition as claimed in claim 1, being a sucralose composition, which has a sucralose region and at least one encapsulating layer; said encapsulating layer comprising polyvinyl acetate and sucralose. 17. A method of preparing an encapsulated composition as claimed in claim 1, involving the steps of: (a) suspending active particles in a fluidizing air stream; (b) preparing a coating composition comprising a polymer, sucralose, and a solvent; and (c) spraying said coating composition onto said suspended active particles to provide an encapsulated composition. 18. The method as claimed in claim 17, wherein the polymer is selected from the group consisting of acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene, polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof. 19. The method as claimed in claim 17, wherein the polymer is polyvinyl acetate. 20. The method as claimed in claim 17, wherein said active is selected from the group consisting of high intensity sweeteners, flavors, medicaments, vitamins and combinations thereof. 21. The method as claimed in claim 17, involving the step of: (d) evaporating said solvent from said encapsulated composition. 22. The method as claimed in claim 21, involving the steps of: (e) suspending said encapsulated composition in a fluidizing air stream; (f) preparing a second coating composition comprising a polymer and a solvent; and (g) spraying said second coating composition onto said encapsulated composition. 23. The method as claimed in claim 17, wherein said coating composition has an additional sweetener other than sucralose. 24. The method as claimed in claim 22, wherein said polymer in step (f) is selected from the group consisting of acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene, polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof. 25. The method as claimed in claim 23, wherein said additional sweetener comprises a high intensity sweetener. 26. The method as claimed in claim 25, wherein said high intensity sweetener is a member selected from the group consisting of saccharin salts, acesulfame potassium, aspartame, thaumatin, neotame, alitame, and combinations thereof. 27. The method as claimed in claim 17, wherein said solvent is selected from the group consisting of ethyl acetate, diethyl ether, acetone, benzene, ethylene dichloride, methanol, methyl ethyl ketone, ethanol, toluene, xylene, amyl acetate, and combinations thereof. 28. The method as claimed in claim 19, wherein said encapsulated sucralose composition comprises particles having an average particle size in the range of 50 µm to 800 µm. 29. An encapsulated sweetener from a composition as claimed in claim 1, prepared by the following steps: (a) suspending sucralose particles in a fluidizing air stream; (b) preparing a coating composition having a polymer, sucralose, and a solvent; (c) spraying said coating composition onto said sucralose particles to provide an encapsulated sucralose composition; and (d) evaporating said solvent from said encapsulated sucralose composition. 30. A composition as claimed in claim 1, having a plurality of particulates comprising a sucralose core, encapsulated by a matrix comprising polymer and sucralose. 31. The composition as claimed in claim 30, wherein the polymer is selected from the group consisting of acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene, polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof. 32. The composition as claimed in claim 30, wherein the polymer is polyvinyl acetate. "COMPOSITION COMPRISING AN ACTIVE CORE ENCAPSULATED BY MATRIX INCLUDING POLYMER AND SUCRALOSE AND METHOD OF PREPARATION THEREOF" (57) Abstract: Some embodiments provide a composition including active region which includes an active such as sucralose and at least one coating layer contiguous with the active region. The coating layer includes a polymer and sucralose; wherein the coating layer either partially or completely surrounds and encapsulates the active region.

Full Text

FIELD
Included are encapsulated compositions including a polymer and sucralose. The
compositions include an encapsulant including a polymer in combination with sucralose.
Methods of preparing the encapsulated compositions are also provided.
BACKGROUND
Encapsulated intense sweeteners have a particular advantage when included in gum
compositions such as chewing gum and bubble gum compositions. The encapsulated
sweeteners are not immediately released as sugar would be when included in a chewing gum.
By contrast, an encapsulated sweetener composition provides extended sweetening on
chewing because the sweetener is not released until the encapsulating material has been
subjected to mastication.
Intense sweeteners such as aspartame (APM) and acesulfame potassium (Ace-K) have
been used in encapsulated compositions in combination with high molecular weight polymers
which allow for their slow release upon chewing in a gum composition.
Sucralose is another popular intense sweetener which is derived from sucrose in
which one or more hydroxy groups are replaced by chlorine atoms. This compound is
described in U.K. Patent No. 1,543,167, the disclosure of which is incorporated herein by
reference. Sucralose may be referred to by different chemical names including: 4-chloro-4-
deoxy-a-D-galactopyranosyl, l,6-dichlorol,6-dideoxy- P-D-fructofuranoside, and known as
4,r,6',-trichloro-4,r,6'-trideoxygalactosucrose.
Sucralose is relatively stable and inert. This includes exhibiting stability in acid
aqueous solutions, in marked contrast to peptide-based sweeteners such as aspartame. Under
completely dry conditions, however, sucralose which is present in a crystalline form tends to
discolor in response to elevated temperatures. For example, such discoloration can be
exhibited after twenty minutes of exposure of pure dry sucralose to a temperature of 100°C,

wherein the color changes to a pale brown. This degradation of sucralose results in a
commercially unacceptable product. This high temperature instability of sucralose has made
it commercially impractical to prepare an encapsulated sucralose with the extrusion
techniques used to prepare the encapsulated APM and Ace-K compositions using high tensile
strength / softening point polymers.
Since sucralose is a desirable sweetener, and is preferred for compositions where
APM stability is questionable, there is a need for an encapsulated sucralose composition
which may be used in a variety of compositions including gum compositions. Ideally, the
encapsulated composition would include an active such as another sweetener, medicament,
vitamin or flavor.
SUMMARY
In some embodiments, there is a composition which includes an active and at least
one coating layer. The coating layer includes polyvinyl acetate and sucralose and at least
partially encapsulates the active.
Also provided is a sucralose composition which includes a sucralose region and at
least one encapsulating layer which includes a polymer such as polyvinyl acetate and
sucralose.
Some embodiments also provide a composition including a sucralose region and at
least one coating layer contiguous with the sucralose region. The coating layer includes a
polymer and sucralose; wherein the coating layer completely surrounds the sucralose region.
Other embodiments provide a method of preparing a composition comprising which
includes:
(a) suspending, active particles in a fiuidizing air stream;
(b) preparing a coating composition including a polymer, sucralose, and a solvent;
and
(c) spraying the coating composition onto the suspended active particles to
provide an encapsulated composition.

In other embodiments there is an encapsulated sweetener prepared by the following
steps:
(a) suspending sucralose particles in a fluidizing air stream;
(b) preparing a coating composition including a polymer, sucralose, and a solvent;
(c) spraying the coating composition onto the sucralose particles to provide an
encapsulated sucralose composition; and
(d) evaporating the solvent from the encapsulated sucralose composition.
In some embodiments, there is a composition including a plurality of particles
including comprising an active core encapsulated by a matrix including polymer and
sucralose.
DETAILED DESCRIPTION
As used herein the transitional tenn "comprising," (also "comprises," etc.) which is
synonymous with "including," "containing," or "characterized by," is inclusive or open-ended
and does not exclude additional, unrecited elements or method steps, regardless of its use in
the preamble or the body of a claim.
As used herein, the terms "bubble gum" and "chewing gum" are used interchangeably
and are both meant to include any gum compositions.
As used herein, the term "active" refers to any composition which may be included in
the encapsulated compositions of some embodiments, wherein the active provides some
desirable property upon release from encapsulation. Examples of suitable actives include
sweeteners, such as sucralose, flavors, medicaments, vitamins, and combinations thereof.
For the encapsulated compositions of some embodiments, the coating composition
includes a high-tensile strength polymer in addition to sucralose. The active may
encapsulated by the coating composition either wholly or partly. The active may
alternatively be part of a matrix formed by the polymer in combination with sucralose. In the
encapsulated composition, the active may be present in any desired amount, such as from
about 5% to about 50% by weight of the encapsulated composition.

Any of a variety of active ingredients may be included in the present embodiments.
These include sweeteners, flavors, breath-freshening agents, medicaments such as analgesics,
anti-histamines, decongestants, and antacids, and vitamins.
Suitable sweeteners may be selected from a wide range of materials including water-
soluble sweeteners, water-soluble artificial sweeteners, water-soluble sweeteners derived
from naturally occurring water-soluble sweeteners, dipeptide based sweeteners, and protein
based sweeteners, including mixtures thereof. Without being limited to particular sweeteners,
representative categories and examples include:
(a) water-soluble sweetening agents such as dihydrochalcones, monellin, steviosides,
glycyrrhizin, dihydioflavenol, and sugar alcohols such as sorbitol, mannitol, maltitol, and L-
aminodicarboxylic acid aminoalkenoic acid ester amides, such as those disclosed in U.S. Pat.
No. 4,619,834, which disclosure is incorporated herein by reference, and mixtures thereof;
(b) water-soluble artificial sweeteners such as soluble saccharin salts, i.e., sodium or
calcium saccharin salts, cyclamate salts, the sodium, ammonium or calcium salt of 3,4-
dihydro-6-methyl-l,2,3-oxathiazine-4-one-2,2-dioxide, the potassium salt of 3,4-dihydro-6-
methyl-l,2,3-oxathiazine-4-one-2,2-dioxide (Acesulfame-K), the free acid form of saccharin,
and mixtures thereof;
(c) dipeptide based sweeteners, such as L-aspartic acid derived sweeteners, such as
L-aspartyl-L-phenylalanine methyl ester (Aspartame) and materials described in U.S. Pat.
No. 3,492,131, L-alphaaspartyl-N-(2,2,4,4-tetramemyl-3-thietanyl)-D-alaninarnide hydrate
(Alitame), methyl esters of L-aspartyl-L-phenylglycerine and L-aspartyl-L-2,5-
dihydrophenyl-glycine, L-aspartyl-2,5-dihydro-L-phenylalanine; L-aspartyl-L-(l-
cyclohexen)-alanine, and mixtures thereof;
(d) water-soluble sweeteners derived from naturally occurring water-soluble
sweeteners, such as chlorinated derivatives of ordinary sugar (sucrose), e.g.,
chlorodeoxysugar derivatives such as derivatives of chlorodeoxysucrose or
chlorodeoxygalactosucrose, known, for example, under the product designation of Sucralose;
examples of chlorodeoxysucrose and chlorodeoxygalactosucrose derivatives include but are
not limited to: l-chloro-l'-deoxysucrose; 4-chloro-4-deoxy-alpha-D-galactopyranosyl-alpha-
D-fructofuranoside, or 4-chloro-4-deoxygalactosucrose; 4-chloro-4-deoxy-alpha-D-
galactopyranosyl-1-chloro-l-deoxy-beta-D-fructo-furanoside, or 4,1'-dichloro-4,1-
dideoxygalactosucrose; 1,6'-dichloror,6'-dideoxysucrose;4-chloro-4-deoxy-alpha-D-
galactopyranosyl-l,6-dichloro-l,6-dideoxy-beta-D- fructofuranoside, or 4,1,6,-trichloro-

4,r,6'-trideoxygalactosucrose;4,6-dichloro-4,6-dlideoxy-alpha-D-galactopyranosyl-6-chloro-
6~deoxy-beta-D- fructofuranoside, or 4,6,6'-trichloro4,6,6-trideoxygalactosucrose; 6,1',6'-
trichloro-6,1,6'-trideoxysucarose,4,6-dichloro-4,6-dideoxy-alpha-D-galacto-pyranosyl-1,6-
dichloro-l,6-dideox y-beta-D-fructoforanoside, or 4,6,r,6'-tetraachloro 4,6,1,6'-
tetradeoxygalacto-sucrose; and 4,6,1,6'-tetradeoxy-sucrose, and mixtures thereof; and
(e) protein based sweeteners such as thaumaoccous danielli (Thaumatin I and II).
The intense sweetening agents may be used in many distinct physical forms well-
known in the art to provide an initial burst of sweetness and/or a prolonged sensation of
sweetness. Without being limited thereto, such physical forms include free forms, such as
spray dried, powdered, beaded forms, encapsulated forms, and mixtures thereof.
In some embodiments wherein the active is a sweetener, it may be a high intensity
sweetener such as sucralose, saccharin salts, acesulfame potassium, aspartame, thaumatin,
neotame, alitame, and combinations thereof. More specifically, sucralose may be used alone
or in combination with another sweetener either as the active or in the coating layer.
The flavoring agents which may be used include those flavors known to the skilled
artisan, such as natural and artificial flavors. These flavorings may be chosen from synthetic
flavor oils and flavoring aromatics and/or oils, oleoresins and extracts derived from plants,
leaves, flowers, fruits, and so forth, and combinations thereof. Nonlimiting representative
flavor oils include spearmint oil, cinnamon oil, oil of wintergreen (methyl salicylate),
peppermint oil, clove oil, bay oil, anise oil, eucalyptus oil, thyme oil, cedar leaf oil, oil of
nutmeg, allspice, oil of sage, mace, oil of bitter almonds, and cassia oil. Also useful
flavorings are artificial, natural and synthetic fruit flavors such as vanilla, and citrus oils
including lemon, orange, lime, grapefruit, and fruit essences including apple, pear, peach,
grape, strawberry, raspberry, cherry, plum, pineapple, apricot and so forth. These flavoring
agents may be used in liquid or solid form and may be used individually or in admixture.
Commonly used flavors include rnints such as peppermint, menthol, spearmint, artificial
vanilla, cinnamon derivatives, and various fruit flavors, whether employed individually or in
admixture. Flavors may also provide breath freshening properties, particularly the mint
flavors.

Other useful flavorings include aldehydes and esters such as cinnamyl acetate,
cinnamaldehyde, citral diethylacetal, dihydrocarvyl acetate, eugenyl formate, p-
methylamisol, and so forth may be used. Generally any flavoring or food additive such as
those described in Chemicals Used in Food Processing, publication 1274, pages 63-258, by
the National Academy of Sciences, may be used. This publication is incorporated herein by
reference. This may include natural as well as synthetic flavors.
Further examples of aldehyde flavorings include but are not limited to acetaldehyde
(apple), benzaldehyde (cherry, almond), anisic aldehyde (licorice, anise), cinnamic aldehyde
(cinnamon), citral, i.e., alpha-citral (lemon, lime), neral, i.e., beta-citral (lemon, lime),
decanal (orange, lemon), ethyl vanillin (vanilla, cream), heliotrope, i.e., piperonal (vanilla,
cream), vanillin (vanilla, cream), alpha-amyl cinnamaldehyde (spicy fruity flavors),
butyraldehyde (butter, cheese), valeraldehyde (butter, cheese), citronellal (modifies, many
types), decanal (citrus fruits), aldehyde C-8 (citrus fruits), aldehyde C-9 (citrus fruits),
aldehyde C-12 (citrus fruits), 2-ethyl butyraldehyde (berry fruits), hexenal, i.e., trans-2 (berry
fruits), tolyl aldehyde (cherry, almond), veratraldehyde (vanilla), 2,6-dimethyl-5-heptenal,
i.e., melonal (melon), 2,6-dimethyloctanal (green fruit), and 2-dodecenal (citrus, mandarin),
cherry, grape, strawberry shortcake, and mixtures thereof.
In some embodiments, a flavoring agent may be employed in either liquid form and/or
dried form. When employed in the latter form, suitable drying means such as spray drying the
oil may be used. Alternatively, the flavoring agent may be absorbed onto water soluble
materials, such as cellulose, starch, sugar, maltodextrin, gum arabic and so forth or may be
encapsulated. The actual techniques for preparing such dried forms are well-known.
In some embodiments, the flavoring agents may be used in many distinct physical
forms well-known in the art to provide an initial burst of flavor and/or a prolonged sensation
of flavor. Without being limited thereto, such physical forms include free forms, such as
spray dried, powdered, beaded forms, encapsulated forms, and mixtures thereof.
The amount of flavoring agent employed herein may be a matter of preference subject
to such factors as the type of final chewing gum composition, the individual flavor, the gum
base employed, and the strength of flavor desired. Thus, the amount of flavoring may be
varied in order to obtain the result desired in the final product and such variations are within

the capabilities of those skilled in the art without the need for undue experimentation. In gum
compositions, the flavoring agent is generally present in amounts from about 0.02% to about
5%, and more specifically from about 0.1% to about 2%, and even more specifically, from
about 0.8% to about 1.8%, by weight of the chewing gum composition.
A variety of drugs, including medications, herbs, and nutritional supplements may
also be included as the active to be encapsulated. Examples of useful drugs include ace-
inhibitors, antianginal drugs, anti-arrhythmias, anti-asthmatics, anti-cholesterolemics,
analgesics, anesthetics, anti-convulsants, anti-depressants, anti-diabetic agents, anti-diarrhea
preparations, antidotes, anti-histamines, anti-hypertensive drugs, anti-inflammatory agents,
anti-lipid agents, anti-manics, anti-nauseants, anti-stroke agents, anti-thyroid preparations,
anti-tumor drugs, anti-viral agents, acne drugs, alkaloids, amino acid preparations, anti-
tussives, anti-uricemic drugs, anti-viral drugs, anabolic preparations, systemic and non-
systemic anti-infective agents, anti-neoplasties, anti-parkinsonian agents, anti-rheumatic
agents, appetite stimulants, biological response modifiers, blood modifiers, bone metabolism
regulators, cardiovascular agents, central nervous system stimulates, cholinesterase inhibitors,
contraceptives, decongestants, dietary supplements, dopamine receptor agonists,
endometriosis management agents, enzymes, erectile dysfunction therapies such as sildenafil
citrate, which is currently marketed as Viagra®, fertility agents, gastrointestinal agents,
homeopathic remedies, hormones, hypercalcemia and hypocalcemia management agents,
immunomodulators, immunosuppressives, migraine preparations, motion sickness treatments,
muscle relaxants, obesity management agents, osteoporosis preparations, oxytocics,
parasympatholytics, parasympathomimetics, prostaglandins, psychotherapeutic agents,
respiratory agents, sedatives, smoking cessation aids such as bromocryptine or nicotine,
sympatholytics, tremor preparations, urinary tract agents, vasodilators, laxatives, antacids, ion
exchange resins, anti-pyretics, appetite suppressants, expectorants, anti-anxiety agents, anti-
ulcer agents, anti-inflammatory substances, coronary dilators, cerebral dilators, peripheral
vasodilators, psycho-tropics, stimulants, anti-hypertensive drugs, vasoconstrictors, migraine
treatments, antibiotics, tranquilizers, anti-psychotics, anti-tumor drugs, anti-coagulants, anti-
thrombotic drugs, hypnotics, anti-emetics, anti-nauseants, anti-convulsants, neuromuscular
drugs, hyper- and hypo-glycemic agents, thyroid and anti-thyroid preparations, diuretics, anti-
spasmodics, terine relaxants, anti-obesity drugs, erythropoietic drugs, anti-asthmatics, cough
suppressants,, mucolytics, DNA and genetic modifying drugs, and combinations thereof.

The coating layer which surrounds the active, may also include a solvent. In addition
to the sucralose and polymer, the solvent should be capable of dissolving the polymer, The
solvent may be any solvent known for this purpose. For example, if the polymer is polyvinyl
acetate, suitable solvents include of ethyl acetate, diethyl ether, acetone, benzene, ethylene
dichloride, methanol, methyl ethyl ketone, ethanol, toluene, xylene, amyl acetate, and
combinations thereof.
One or more coating layers may be present. In some embodiments wherein more than
one coating layer is present, the first coating layer may include sucralose and a high tensile
strength polymer, with the optional addition of another sweetener. A second coating may
completely or partially encapsulate the active particles and may include either a single
polymer, a combination of different polymers, or a combination of one or rnore polymers and
a sweetener such as sucralose.
Polymers which may be used in the coating layers include acrylic polymers and
copolymers, carboxyvinyl polymer, polyamides, polystyrene, polyvinyl acetate, polyvinyl
acetate phthalate, polyvinylpyrrolidone, and combinations thereof. One or more different
polymers may be used in each of the coating layers. For example, polyvinyl acetate may be
included in a first coating with a combination of polyvinyl acetate and another polymer in a
subsequent exterior coating.
The encapsulated particles of some embodiments may be prepared by any suitable
spray coating method as known in the art. One suitable process is the Wurster process. This
process provides a method for encapsulating individual particulate materials. First the
particles to be encapsulated are suspended in a fluidizing air stream which provides a
generally cyclic flow in front of a spray nozzle. The spray nozzle sprays an atomized flow of
the coating solution, which will include sucralose, a polymer and a suitable solvent.
The atomized coating solution collides with the particles as they are carried away
from the nozzle to provide a particle coating with the coating solution. The temperature of
the fluidizing air stream, which also serves to suspend the particles to be coated, may be
adjusted to evaporate the solvent shortly after the coating solution contacts the particles. This
serves to solidify the coating on the particles, resulting in the desired encapsulated particle.

This process may be repeated until the desired thickness of the coating is achieved.
Alternatively, 1he process may be repeated with a different coating solution to provide
different and distinct coating layers in the encapsulated particle composition.
Following the coating process, the particles may then be formed to an appropriate size
as desired, generally from an average particle size range of about 50 µm to about 800 µm.
This may be accomplished by any suitable means such as chopping, pulverizing, milling or
grinding the particles.
The gum compositions of some embodiments may include a gum base as well as the
encapsulated active composition. The gum base may include any component known in the
chewing gum art. For example, the gum base may include elastomers, bulking agents, waxes,
elastomer solvents, emulsifiers, plasticizers, fillers and mixtures thereof.
The elastomers (rubbers) employed in the gum base will vary greatly depending upon
various factors such as the type of gum base desired, the consistency of gum composition
desired and the other components used in the composition to make the final chewing gum
product. The elastomer may be any water-insoluble polymer known in the art, and includes
those gum polymers utilized for chewing gums and bubble gums. Illustrative examples of
suitable polymers in gum bases include both natural and synthetic elastomers. For example,
those polymers which are suitable in gum base compositions include, without limitation,
natural substances (of vegetable origin) such as chicle, natural rubber, crown gum, nispero,
rosidinha, jelutong, perillo, niger gutta, tunu, balata, guttapercha, lechi capsi, sorva, gutta kay,
and the like, and combinations thereof. Examples of synthetic elastomers include, without
limitation, styrene-butadiene copolymers (SBR), polyisobutylene, isobutylene-isoprene
copolymers, polyethylene, polyvinyl acetate and the like, and combinations thereof.
Additional useful polymers include: crosslinked polyvinyl pyrrolidone,
polymethylmethacrylate; copolymers of lactic acid, polyhydroxyalkanoates, plasticized
ethylcellulose, polyvinyl acetatephthalate and combinations thereof.
The amount of elastomer employed in the gum base may vary depending upon
various factors such as the type of gum base used, the consistency of the gum composition
desired and the other components used in the composition to make the final chewing gum

product. In general, the elastomer will be present, in the gum base in an amount from about
10% to about 60% by weight of the gum region, desirably from about 35% to about 40% by
weight
In some embodiments, the gum base may include wax. It softens the polymeric
elastomer mixture and improves the elasticity of the gum base. When present, the waxes
employed will have a melting point below about 60°C, and preferably between about 45°C.
and about 55°C. The low melting wax may be a paraffin wax. The wax may be present in the
gum base in an amount from about 6% to about 10%, and preferably from about 7% to about
9.5%, by weight of the gum base.
In addition to the low melting point waxes, waxes having a higher melting point may
be used in the gum base in amounts up to about 5%, by weight of the gum base. Such high
melting waxes include beeswax, vegetable wax, candelilla wax, carnuba wax, most petroleum
waxes, and the like, and mixtures thereof.
In addition to the components set out above, the gum base may include a variety of
other ingredients, such as components selected from elastomer solvents, emulsifiers,
plasticizers, fillers, and mixtures thereof.
The gum base may contain elastomer solvents to aid in softening the elastomer
component. Such elastomer solvents may include those elastomer solvents known in the art,
for example, terpinene resins such as polymers of alpha-pinene or beta-pinene, methyl,
glycerol and pentaerythritol esters of rosins and modified rosins and gums such as
hydrogenated, dimerized and polymerized rosins, and mixtures thereof. Examples of
elastomer solvents suitable for use herein may include the pentaerythritol ester of partially
hydrogenated wood and gum rosin, the pentaerythritol ester of wood and gum rosin, the
glycerol ester of wood rosin, the glycerol ester of partially dimerized wood and gum rosin,
the glycerol ester of polymerized wood and gum rosin, the glycerol ester of tall oil rosin, the
glycerol ester of wood and gum rosin and the partially hydrogenated wood and gum rosin and
the partially hydrogenated methyl ester of wood and rosin, and the like, and mixtures thereof.
The elastomer solvent may be employed in the gum base in amounts from about 2% to about
15%, and preferably from about 7% to about 11%, by weight of the gum base.

The gum base may also include emulsifiers which aid in dispersing the immiscible
components into a single stable system. The emulsifiers useful in this invention include
glyceryl monostearate, lecithin, fatty acid monoglycerides, diglycerides, propylene glycol
monostearate, and the like, and mixtures thereof. The emulsifier may be employed in
amounts from about 2% to about 15%, and more specifically, from about 7% to about 11%,
by weight of the gum base.
The gum base may also include plasticizers or softeners to provide a variety of
desirable textures and consistency properties. Because of the low molecular weight of these
ingredients, the plasticizers and softeners are able to penetrate the fundamental structure of
the gum base making it plastic and less viscous. Useful plasticizers and softeners include
lanolin, palmitic acid, oleic acid, stearic acid, sodium stearate, potassium stearate, glyceryl
triacetate, glyceryl lecithin, glyceryl monostearate, propylene glycol monostearate, acetylated
monoglyceride, glycerine, and the like, and mixtures thereof. Waxes, for example, natural
and synthetic waxes, hydrogenated vegetable oils, petroleum waxes such as polyurethane
waxes, polyethylene waxes, paraffin waxes, microcrystalline waxes, fatty waxes, sorbitan
monostearate, tallow, propylene glycol, mixtures thereof, and the like, may also be
incorporated into the gum base. The plasticizers and softeners are generally employed in the
gum base in amounts up to about 20% by weight of the gum base, and more specifically in
amounts from about 9% to about 17%, by weight of the gum base.
Plasticizers also include are the hydrogenated vegetable oils and include soybean oil
and cottonseed oil which may be employed alone or in combination. These plasticizers
provide the gum base with good texture and soft chew characteristics. These plasticizers and
softeners are generally employed in amounts from about 5% to about 14%, and more
specifically in amounts from about 5% to about 13.5%, by weight of the gum base.
Anhydrous glycerin may also be employed as a softening agent, such as the
commercially available United States Pharmacopeia (USP) grade. Glycerin is a syrupy liquid
with a sweet warm taste and has a sweetness of about 60% of that of cane sugar. Because
glycerin is hygroscopic, the anhydrous glycerin may be maintained under anhydrous
conditions throughout the preparation of the chewing gum composition.

In some embodiments, the gum base of this invention may also include effective
amounts of bulking agents such as mineral adjuvants which may serve as fillers and textural
agents. Useful mineral adjuvants include calcium carbonate, magnesium carbonate, alumina,
aluminum hydroxide, aluminum silicate, talc, tricalcium phosphate, dicalcium phosphate,
calcium sulfate and the like, and mixtures thereof. These fillers or adjuvants may be used in
the gum base compositions in various amounts. The amount of filler, may be present in an
amount from about zero to about 40%, and more specifically from about zero to about 30%,
by weight of the gum base.
A variety of traditional ingredients may be optionally included in the gum
compositions in effective amounts such as coloring agents, antioxidants, preservatives,
flavoring agents, and the like. For example, titanium dioxide and other dyes suitable for food,
drug and cosmetic applications, known as F. D. & C. dyes, may be utilized. An anti-oxidant
such as butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), propyl gallate,
and mixtures thereof, may also be included. Other conventional chewing gum additives
known to one having ordinary skill in the chewing gum art may also be used in the gum base.
The gum composition may include amounts of conventional additives selected from
the group consisting of sweetening agents (sweeteners), plasticizers, softeners, emulsifiers,
waxes, fillers, bulking agents (carriers, extenders, bulk sweeteners), mineral adjuvants,
flavoring agents (flavors, flavorings), coloring agents (colorants, colorings), antioxidants,
acidulants, thickeners, medicaments, and the like, and mixtures thereof. Some of these
additives may serve more than one purpose. For example, in sugarless gum compositions, a
sweetener, such as maltitol or other sugar alcohol, may also function as a bulking agent.
The plasticizers, softening agents, mineral adjuvants, waxes and antioxidants
discussed above, as being suitable for use in the gum base, may also be used in the chewing
gum composition. Examples of other conventional additives which may be used include
emulsifiers, such as lecithin and glyceryl monostearate, thickeners, used alone or in
combination with other softeners, such as methyl cellulose, alginates, carrageenan, xanthan
gum, gelatin, carob, tragacanth, locust bean gum, pectin, alginates, galactomannans such as
guar gum, carob bean gum, glucomannan, gelatin, starch, starch derivatives, dextrins and
cellulose derivatives such as carboxy methyl cellulose, acidulants such as malic acid, adipic

acid, citric acid, tartaric acid, fumade acid, and mixtures thereof, and fillers, such as those
discussed above under the category of mineral adjuvants.
In some embodiments, the gum region may also contain a bulking agent. Suitable
bulking agents may be water-soluble and include sweetening agents selected from, but not
limited to, monosaccharides, disaccharides, polysaccharides, sugar alcohols, and mixtures
thereof; randomly bonded glucose polymers such as those polymers distributed under the
trade name POLYDEXTROSE by Pfizer, Inc., Groton, Conn.; isomalt (a racemic mixture of
alpha-D-glucopyranosyl-l,6-mannitol and alpha-D-glucopyranosyl-L6-sorbitol manufactured
under the trade name PALATINIT by Suddeutsche Zucker), maltodextrins; hydrogenated
starch hydrolysates; hydrogenated hexoses; hydrogenated disaccharides; minerals, such as
calcium carbonate, talc, titanium dioxide, dicalcium phosphate; celluloses; and mixtures
thereof.
Suitable sugar bulking agents include monosaccharides, disaccharides and
polysaccharides such as xylose, ribulose, glucose (dextrose), mannose, galactose, fructose
(levulose), sucrose (sugar), maltose, invert sugar, partially hydrolyzed starch and com syrup
solids, and mixtures thereof.
Suitable sugar alcohol bulking agents include sorbitol, xylitol, mannitol, galactitol
maltitol, and mixtures thereof.
Suitable hydrogenated starch hydrolysates include those disclosed in U.S. Pat. Nos.
25,959,3,356,811,4,279,931 and various hydrogenated glucose syrups and/or powders
which contain sorbitol, hydrogenated disaccharides, hydrogenated higher polysaccharides, or
mixtures thereof. Hydrogenated starch hydrolysates are primarily prepared by the controlled
catalytic hydrogenation of corn syrups. The resulting hydrogenated starch hydrolysates are
mixtures of monomelic, dimeric, and polymeric saccharides. The ratios of these different
saccharides give different hydrogenated starch hydrolysates different properties. Mixtures of
hydrogenated starch hydrolysates, such as LYCASIN, a commercially available product
manufactured, by Roquette Freres of France, and HYSTAR, a commercially available product
manufactured by Lonza, Inc., of Fairlawn, N.J., are also useful.

Any sweetening agent or flavoring agent, as described above, may also be added as an
optional component to the gum compositions.
Coloring agents may be used in amounts effective to produce the desired color. The
coloring agents may include pigments which may be incorporated in amounts up to about
6%, by weight of the gum composition. For example, titanium dioxide may be incorporated
in amounts up to about 2%, and preferably less than about 1%, by weight of the gum
composition. The colorants may also include natural food colors and dyes suitable for food,
drug and cosmetic applications. These colorants are known as F.D.& C. dyes and lakes. The
materials acceptable for the foregoing uses are preferably water-soluble. Illustrative
nonlimiting examples include the indigoid dye known as F.D.& C. Blue No.2, which is the
disodium salt of 5,5-indigotmdisulfonic acid. Similarly, the dye known as F.D.& C. Green
No.l comprises a triphenylmethane dye and is the monosodium salt of 4-[4-(N-ethyl-p-
sulfoniumbenzylamino)diphenylmemylene][l-(N-ethyl-N-p-sulfoniumbenzyl)-delta-2,5-
cyclohexadieneimine]. A full recitation of all F.D.& C. colorants and their corresponding
chemical structures may be found in the Kirk-Othmer Encyclopedia of Chemical Technology,
3rd Edition, in volume 5 at pages 857-884, which text is incorporated herein by reference.
Suitable oils and fats usable in gum compositions include partially hydrogenated
vegetable or animal fats, such as coconut oil, palm kernel oil, beef tallow, and lard, among
others. These ingredients when used are generally present in amounts up to about 7%, and
preferably up to about 3.5%, by weight of the gum composition.
Some embodiments may include a method for preparing the improved chewing gum
compositions for the gum region, including both chewing gum and bubble gum compositions.
The chewing gum compositions may be prepared using standard techniques and equipment
known to those skilled in the art. The apparatus useful in accordance with some embodiments
comprises mixing and heating apparatus well known in the chewing gum manufacturing arts,
and therefore the selection of the specific apparatus will be apparent to the artisan.
While there have been described what are presently believed to be the preferred
embodiments of the invention, those skilled in the art will realize that changes and
modifications may be made thereto without departing from the spirit of the invention, and it
is intended to include all such changes and modifications as fall within the true scope of the

invention.

WE CLAIM:
1. A composition comprising an active, selected from the group consisting of sweeteners, flavors,
medicaments, vitamins, and combinations thereof, and at least one coating layer, such as herein
described, wherein said coating layer either partially or completely encapsulate said active; and said
coating layer comprises polyvinyl acetate and sucralose.
2. The composition as claimed in claim 1, wherein said coating layer contains a solvent, such as
herein described.
3. The composition as claimed in claim 1, having additional coating layers.
4. The composition as claimed in claim 1, wherein said coating layer contains an additional
sweetener other than sucralose.
5. The composition as claimed in claim 1, wherein said sweetener is a high intensity sweetener.
6. The composition as claimed in claim 1, having an additional coating layer, wherein (1) said
additional coating layer comprises a polymer and (2) said additional coating layer completely
surrounds said encapsulated composition.
7. The composition as claimed in claim 6, wherein said polymer of the additional coating layer is
selected from the group consisting of acrylic polymers and copolymers, carboxyvinyl polymer,
polyamides, polystyrene, polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and
combinations thereof.
8. The composition as claimed in claim 4, wherein said additional sweetener comprises a high
intensity sweetener.
9. The composition as claimed in claim 8, wherein Said additional sweetener is a member selected
from the group consisting of saccharin salts, acesulfame potassium, aspartame, thaumatin, neotame,
alitame, and combinations thereof.

10. The composition as claimed in claim 2, wherein said solvent is selected from the group
consisting of ethyl acetate, diethyl ether, acetone, benzene, ethylene dichloride, methanol, methyl ethyl
ketone, ethanol, toluene, xylene, amyl acetate, and combinations thereof.
11. The composition as claimed in claim 1, wherein said encapsulated composition comprises
particles having an average particle size range of 50 urn to 800 µm.
12. A composition as claimed in claim 1, having a sucralose region and at least one coating layer
contiguous with said sucralose region; said coating layer comprising a polymer and sucralose; wherein
said coating layer completely surrounds said sucralose region.
13. The composition as claimed in claim 12, wherein said polymer is selected from the group
consisting of acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene,
polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof.
14. The composition as claimed in claim 13, wherein said polymer comprises polyvinyl acetate.
15. The composition as claimed in claim 12, wherein said coating layer contains a solvent, such as
herein described.
16. The composition as claimed in claim 1, being a sucralose composition, which has a sucralose
region and at least one encapsulating layer; said encapsulating layer comprising polyvinyl acetate and
sucralose.
17. A method of preparing an encapsulated composition as claimed in claim 1, involving the steps
of:

(a) suspending active particles in a fluidizing air stream;
(b) preparing a coating composition comprising a polymer, sucralose, and a solvent; and
(c) spraying said coating composition onto said suspended active particles to
provide an encapsulated composition.

18. The method as claimed in claim 17, wherein the polymer is selected from the group consisting
of acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene, polyvinyl
acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof.
19. The method as claimed in claim 17, wherein the polymer is polyvinyl acetate.
20. The method as claimed in claim 17, wherein said active is selected from the group consisting of
high intensity sweeteners, flavors, medicaments, vitamins and combinations thereof.
21. The method as claimed in claim 17, involving the step of:
(d) evaporating said solvent from said encapsulated composition.
22. The method as claimed in claim 21, involving the steps of:
(e) suspending said encapsulated composition in a fluidizing air stream;
(f) preparing a second coating composition comprising a polymer and a solvent;
and
(g) spraying said second coating composition onto said encapsulated composition.

23. The method as claimed in claim 17, wherein said coating composition has an additional
sweetener other than sucralose.
24. The method as claimed in claim 22, wherein said polymer in step (f) is selected from the group
consisting of acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene,
polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof.
25. The method as claimed in claim 23, wherein said additional sweetener comprises a high
intensity sweetener.
26. The method as claimed in claim 25, wherein said high intensity sweetener is a member selected
from the group consisting of saccharin salts, acesulfame potassium, aspartame, thaumatin, neotame,
alitame, and combinations thereof.

27. The method as claimed in claim 17, wherein said solvent is selected from the group consisting
of ethyl acetate, diethyl ether, acetone, benzene, ethylene dichloride, methanol, methyl ethyl ketone,
ethanol, toluene, xylene, amyl acetate, and combinations thereof.
28. The method as claimed in claim 19, wherein said encapsulated sucralose composition comprises
particles having an average particle size in the range of 50 µm to 800 µm.
29. An encapsulated sweetener from a composition as claimed in claim 1, prepared by the following
steps:

(a) suspending sucralose particles in a fluidizing air stream;
(b) preparing a coating composition having a polymer, sucralose, and a solvent;
(c) spraying said coating composition onto said sucralose particles to provide an
encapsulated sucralose composition; and
(d) evaporating said solvent from said encapsulated sucralose composition.

30. A composition as claimed in claim 1, having a plurality of particulates comprising a sucralose
core, encapsulated by a matrix comprising polymer and sucralose.
31. The composition as claimed in claim 30, wherein the polymer is selected from the group
consisting of acrylic polymers and copolymers, carboxyvinyl polymer, polyamides, polystyrene,
polyvinyl acetate, polyvinyl acetate phthalate, polyvinylpyrrolidone, and combinations thereof.
32. The composition as claimed in claim 30, wherein the polymer is polyvinyl acetate.

"COMPOSITION COMPRISING AN ACTIVE CORE ENCAPSULATED BY MATRIX
INCLUDING POLYMER AND SUCRALOSE AND METHOD OF PREPARATION THEREOF"
(57) Abstract: Some embodiments provide a composition including active region which includes an active such as sucralose and
at least one coating layer contiguous with the active region. The coating layer includes a polymer and sucralose; wherein the coating
layer either partially or completely surrounds and encapsulates the active region.

COMPOSITION COMPRISING AN ACTIVE CORE ENCAPSULATED BY MATRIX INCLUDING POLYMER AND SUCRALOSE AND METHOD OF PREPARATION THEREOF

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