Chewable antiplaque confectionery dental composition

Tag : ammonium bisulfite


Abstract
A chewable confectionery dental composition delivering to the moutha unit dose of a plaque reducing enzyme the composition comprisingan enzyme and a non-cariogenic sweetener, the enzyme beingincorporated in the composition at a temperature less than about80.degree. C.
Description of the Invention
SUMMARY OF THE INVENTION

In accordance with the present invention, there is provided achewable confectionery composition such as a chewable tablet or gumcomprised of a small but effective amount of a plaque reducingenzyme, a non-cariogenic sweetener and optionally aplasticizing/softening agent.

Due to the inherent nature of the chewable tablet or gum product,prolonged contact with the tooth surfaces is achieved when theproduct is chewed, forming a paste with saliva containing theenzyme which coats the tooth surfaces. The delivery of the enzymein a chewable tablet or gum form insures that an adequate dosage ofthe antiplaque enzyme is deliverable when the product is chewed bythe user. The chewable confectionery composition of the presentinvention is portable and can be packaged and stored in a consumerspocket or purse for consumption anytime and anywhere.

When the chewable confectionery composition of the presentinvention is placed within the mouth and chewed, an effectiveantiplaque amount of the enzyme is released from the compositioninto the saliva where it can reach the surface of the teeth toprevent further plaque accumulation. The tablet or gum of thepresent invention is formed so as to release the enzyme over aperiod of 0.5 to 2 minutes. Consistent daily use of the chewabletablets or gums of the present invention will then obtain maximumplaque reduction from the teeth of the consumer.

The term "chewable confectionery composition" as usedherein includes within its meaning chewing gum, and chewable andorally soluble tablets, troches and lozenges.

DESCRIPTION OF THE PREFERRED EMBODIMENTS

The composition of the present invention as stated is a chewableproduct which reduces plaque and contains as the active ingredient,a protease enzyme. The product is preferably sugarless.

A representative chewable antiplaque tablet in accordance with thepractice of this invention contains about 0.1 to 3% by weight of anenzyme, 0.5 to 5% by weight of a combination plasticizing/softeningingredient and about 50 to about 90% by weight of a non-cariogenicsweetener. In addition to the ingredients discussed above fortablets, chewable gum compositions will contain 10 to 40% by weightof a gum base.

As water promotes the denaturization of the papain enzyme, thepresence of water in the chewable confectionery product of thepresent invention should be at relatively low concentrations inorder to impart maximum stability and shelf life to the chewable.For this purpose, it has been found essential to limit the totalamount of water present in the chewable product to no more than 5%by weight.

Enzymes

The enzymes useful in the practice of the present invention includecarbohydrases such as glucoamylase and enzymes extracted fromnatural fruit products such as proteases which breakdown orhydrolyze proteins.

Protease enzymes useful in the practice of the present inventioninclude those extracted from natural fruit products. Theproteolytic enzymes are obtained from natural sources or by theaction of microorganisms having a nitrogen source and a carbonsource. Examples of proteolylic enzymes useful in the practice ofthe present invention include the naturally occurring enzymespapain (from papaya), bromelain (from pineapple), as well as serineproteases such as chymotrypsin. Additional enzymes include ficinand alcalase. Papain is a protease enzyme preferred for use in thepractice of the present invention, the papain having an activity of150 to 939 MCU per milligram as determined by the Milk Clot AssayTest of the Biddle Sawyer Group (see J. Biol. Chem., vol. 121,pages 737-745). The protease enzymes are included in thecompositions of the present invention at a concentration of about0.1 to about 3% by weight and preferably about 0.2 to about 2% byweight.

Enzymes which may beneficially be used in combination with theproteolytic enzymes and glucoamylase enzymes include carbohydrasessuch as glucoamylase, alpha-amylase, beta-amylase, tannase andlipases such as plant lipase, gastric lipase and pancreatic lipase.

Glucoamylase is a saccharifying glucoamylase of Aspergiullus nigerorigin cultivated by fermentation. This enzyme can hydrolyze boththe alpha-D-1,6 glucosidic branch points and the alpha-1,4glucosidic bonds of glucosyl oligosaccharides. Additionalcarbohydrases useful in accordance with this invention are alphaand beta-amylase, dextranase and mutanase. Glucoamylase is apreferred enzyme and is incorporated in the oral composition of thepresent invention at a concentration of about 0.001 to 2% by weightand preferably about 0.01 to 0.55% by weight.

The lipase enzyme is derived from a select strain of Aspergillusniger, exhibiting random cleaving of the 1,3 positions of fats andoils. The enzyme has maximum lipolytic activity at pH 5.0 to 7.0when assayed with olive oil. The enzyme has a measured activity of120,000 lipase units per gram. The lipase may be included in thedentifrice composition at a concentration of about 0.010 to about5.0% by weight and preferably about 0.02 to about 0.10% by weight.

The presence of tannase enzyme can be further beneficial infacilitating the breakdown of extrinsic stain. Tannase enzymes havebeen purified from Aspergillus niger and Aspergillus allianceus andare useful in the hydrolysis of tannins, known to discolor thetooth surface.

Other suitable enzymes which can comprise the present inventioninclude lysozyme, derived from egg white, which contains a singlepolypeptide chain crosslinked by four disulfide bonds having amolecular weight of 14,600 daltons. The enzyme can exhibitantibacterial properties by facilitating the hydrolysis ofbacterial cell walls cleaving the glycosidic bond between carbonnumber 1 of N-acetylmuramic acid and carbon number 4 ofN-acetyl-D-glucosamine, which in vivo, these two corbohydrates arepolymerized to form the cell wall polysaccharide. Additionally,pectinase, an enzyme that is present in most plants facilitates thehydrolysis of the polysaccharide pectin into sugars andgalacturonic acid. Finally, glucanase, which may be utilized tocatalyze the breakdown of complex carbohydrates to glucans and thehydrolysis of beta glucan to glucose.

Enzyme Stabilizing Agents

Enzyme stabilizing agents which protect the enzyme frominactivation by chelating metal impurities present in the chewableconfectionery composition of the present invention may beincorporated in the composition include ethylene diaminetetraacetic acid (EDTA) and sodium gluconate at concentrationsbetween 0.01 and 1% by weight, preferably between 0.1 and 0.5% byweight. Agents stabilizing the enzyme against oxidation includereducing agents such as sodium bisulfite, metal gallates, potassiumstannate, sodium stannate, ammonium sulfate,3,5,-di-tert-butyl-4-hydroxytoluene (BHT), Vitamin E (.alpha.,.beta.,.gamma., forms)/Vitamin E acetate and ascorbic acid.Potassium stannate is an enzyme stabilizing agent preferred for usein the practice of the present invention. The reducing agent ispresent in the oral composition of the present invention at aconcentration between about 0.05 to about 1.5% by weight,preferably between about 0.1 and about 0.75% by weight.

Tablets

Plasticizing/Softening Agents

Plasticizing/softening agents suitable for use in the preparationof tablets in accordance with the practice of this invention,include propylene glycol, glycerol, acetylated monoglyceride,glyceryl triacetate, glyceryl diacetate, lecithin, glycerin, andmixtures thereof. In a preferred embodiment of this invention, acombination of lecithin and glycerin is used, generally in amountsof about 0.5% to about 3.0% by weight, 0.1% to about 1.0% lecithinand about 1.0% to about 1.0% by weight glycerin by weight, based onthe weight of the total chewable tablet composition.

Sweeteners

The sweetening agent ingredient used in the practice of the presentinvention include bulk sweeteners such as the polyols of 5 to 12carbon atoms substituted with 5 to 9 hydroxyl groups such as sugaralcohols including xylitol, sorbitol, mannitol. Sugar alcoholsprovide bulk or texture to the chewable compositions of the presentinvention and are utilized in amounts of about 25% to about 90% byweight preferably about 40% to about 85% by weight Artificialsweeteners include as sodium or calcium saccharin salts, cyclamatesalts, such as the sodium salt and the like, and the free acid formof saccharin; dipeptide based sweetening agents such asL-aspartyl-L-phenyl-alanine methyl ester, dihydrochalcone;glycyrrhizin; and the synthetic sweetener 3,6-dihydro-6-methyl-1,1,2,3-oxathiazin-4-one-2,2-dioxide, particularly the potassium(Acesulfame-K), sodium and calcium salts. Artificial sweeteners arepresent in the chewable confectionery compositions of the presentinvention at a concentration of about 0.1 to about 1% by weight.

Preferred bulk sweeteners include Lycasin, a commercially availablemixture of sorbitol, malitol and high molecular weight dextransdisclosed in Re 26,969 and Isomalt, a sugar alcohol of adisaccharide such as alpha-D-glucopyranosyl-1, 6-mannitol, itsisomer, alpha, D-glucopyranosyl-1, 6-sorbitol or a mixture thereofwhich is obtained by the hydrogenation of palatinose which isconverted from sucrose as a raw material with glycosyltransferase.A preferred artificial sweetener is aspartame.

In a preferred embodiment of this invention, the sweetening agentused is a combination of an artificial sweetener such as aspartameand acesulfame and the bulk sweeteners such as Lycasin and Isomalt,the artificial sweetener being present generally in amounts ofabout 0.05% to about 0.3% by weight and preferably about 0.18% toabout 0.22% by weight and about 40% to about 60% by weight,preferably about 45% to about 55% by weight Lycasin and about 15%to about 35% by weight preferably about 20% to about 30% by weightIsomalt.

Flavoring Agents

One or more flavoring agents in liquid powder or encapsulated formare used in the chewable composition of this invention. A varietyof flavors known in the art may be used, including essential oils,such as cinnamon, spearmint, peppermint, menthol, birch, anisewintergreen oil and eucalyptus oil. Natural fruit flavors derivedfrom the essence of fruits, such as apple, pear, peach, strawberry,cherry, apricot, orange, watermelon, banana and the like; beanderived flavors such as coffee, cocoa and the like; wine derivedcuracao zin and the like, and pungent materials, such as affinin,pepper, mustard and the like. Flavoring agents are incorporated inthe chewable confectionery compositions at a concentration of about0.5 to about 5% by weight and preferably about 1.0 to about 3.0% byweight.

Other Ingredients

Calcium salts may be incorporated in the chewable compositions ofthe resent invention as fillers and anticavity agents. Examples ofthe calcium salts to be used in the present invention as theanticaries agent are, for example, calcium chloride, calciumnitrate, calcium sulfate, dicalcium phosphate dihydrate, calciumcarbonate, calcium citrate, calcium hydrogen pyrophosphate, calciumgluconate, calcium glycerophosphate, calcium hydroxide, calciumoxide, calcium silicate and the like, but not limited thereto. Thecalcium salt is present in the tablet or gum at a concentration ofabout 5 to about 20% by weight and preferably 7 to 10% by weight.Alkaline agents such as sodium bicarbonate may be incorporated inthe chewable confectionery composition of the present invention toprovide additional cleaning and breath freshening properties to thecomposition.

Chewing Gum

The chewing gum of the present invention is preferably a sugarlesschewing gum containing the enzyme, as sugarless gums do not promotetooth decay. Chewing gum formulations in which the enzymes of thepresent invention may be incorporated are well known in the art andtypically contain, in addition to, a chewing gum base, one or moreplasticizing agents; at least one sweetening agent and at least oneflavoring agent.

Gum base materials suitable for use in the practice of thisinvention are well known in the art and include natural orsynthetic gum bases or mixtures thereof. Representative naturalgums or elastomers include chicle, natural rubber, jelutong,balata, guttapercha, lechi caspi, sorva, guttakay, crown gum,perillo, or mixtures thereof. Representative synthetic gums orelastomers include butadiene-styrene copolymers, polyisobutyleneand isobutylene-isoprene copolymers.

The gum base is incorporated in the chewing gum product at aconcentration of about 10 to about 40% by weight and preferablyabout 20 to about 35% by weight.

Plasticizing/softening agents commonly used in chewing gumcompositions are suitable for use in this invention, includinggelatin, waxes and mixtures thereof in amounts of 0.1 to 5% byweight.

The sweetening agent ingredient used in the practice of thisinvention may be selected from a wide range of materials. Bulksweeteners include the same sweeteners used for the preparation ofchewable tablets as are artificial sweeteners. The bulk sweeteneris present in the chewing gum composition of the present inventionin amounts of about 40 to about 80% by weight and preferably about50 to about 75% by weight. The artificial sweetener is present inthe chewing gum composition of the present invention in amounts ofabout 0.1 to about 2% by weight and preferably about 0.3 to 1% byweight.

In addition to the ingredients listed above, the gum compositionsmay also include conventional additives such as colorants,flavoring agents and the like. For example, titanium dioxide may beutilized as a colorant. A variety of flavors known in the art maybe used, including essential oils, such as cinnamon, spearmint,peppermint, menthol, birch, anise and the like; natural fruitflavors derived from the essence of fruits, such as apple, pear,peach, strawberry, cherry, apricot, orange, watermelon, banana andthe like; bean-derived flavors, such as coffee, cocoa and the like.Flavoring agents are incorporated in the chewing gum formulation ata concentration of about 0.5 to about 5% by weight and preferably 1to 3% by weight.

Method of Manufacture

The challenge in incorporating enzymes into the confectionarycomposition is maintaining enzymatic stability and activity duringstorage. Enzymes are quaternary proteins whose structure, function,and stability are sensitive to chemical environment and processingparameters. Enzymes denature in harsh chemical environment and athigh temperatures. Formulation and processing procedures areoptimized at low moisture and low temperature for both the enzymechewable tablet and the enzyme gum to preserve enzymatic activityand in vivo efficacy.

The chewable composition of the present invention is made by anysuitable process where the protease enzyme is incorporated into thesolid base material such that no water or a limited amount ofingredients that absorb water are used that would result inundesirable amounts of water being introduced into the compositionduring processing or storage. Further, at the time the enzyme isintroduced into ingredients used to prepare the chewablecomposition that the temperature at the time of addition is lessthen about 80.degree. C. Therefore, it is critical to the practiceof the present invention that the composition contain less than 5%by weight water and preferably less than 3% by weight water andthat the temperature at which processing of the enzyme occurs beless than about 80.degree. C. The presence in the composition ofwater in amounts greater than 5% by weight or the use oftemperatures in excess of 80.degree. C. will act to denature theprotease enzyme thereby substantially reducing the efficacy of theenzyme in effecting plaque reduction on teeth.

One method for manufacturing the composition of the inventioncomprises first heating the base material to a temperaturesufficient to drive off any water in the composition. The basematerial is then cooled to a temperature at which the enzyme andother temperature sensitive ingredients such as plasticizers, othersweeteners are incorporated and mixed into the base material.

Formulations, equipment and processing techniques have been welldeveloped in the art for preparing and packaging chewing gum andchewable tablets and lozenges. As the enzyme is subject todeterioration and inactivation under conditions such as high shearand elevated temperatures, processing conditions are controlledduring the time period that the enzymes are admixed with the otheringredients of the formulation and converted into finished productsso that the temperature at the time of admixture does not exceedabout 80.degree. C. for any extended period of time.

The tablets of the confectionary composition of the presentinvention are conventionally made by grinding the ingredients oncemixed and then compressing or molding the ingredients to form asuitable means for the delivery of the enzyme. In order to producetablets it is necessary to have a free flowing material which hasgood self binding properties and which will not stick to themolding or compression equipment.

An illustrative procedure for formulating the chewing gumcomposition is as follows: the gum base is first melted in a heatedkettle at 55'-65.degree. C. One or more of the sweeteners are thenadded to the gum base followed by one or more flavors, plasticizer.All ingredients are then mixed for a sufficient period of time toensure adequate dispersion. The mixture is then allowed to cool andthe enzyme is added and is cut into suitable serving sizes.

In order to enhance shelf stability, in addition to the admixtureused in the preparation of the chewable product being substantiallyfree of water, the finished product should be packaged in a mannerso as to minimize exposure to air and moisture.

Claim 1 of 28 Claims
1. A chewable confectionery composition comprising: a) an enzymecomprising a protease which has been extracted from a fruit andwherein said enzyme is incorporated into a gum base; b) anon-cariogenic sweetener; and c) an enzyme stabilizing agent whichis a metal chelating agent or an antioxidation agent; wherein thecomposition contains less than 5% by weight water the enzyme isincorporated into the composition at a temperature of less than80.degree. C.; and the enzyme maintains its initial activity overat least a 4 week period when stored at 23.degree. C.
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