WO2006020190A1 - Composition dentifrice - Google Patents

Composition dentifrice Download PDF

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Publication number
WO2006020190A1
WO2006020190A1 PCT/US2005/025386 US2005025386W WO2006020190A1 WO 2006020190 A1 WO2006020190 A1 WO 2006020190A1 US 2005025386 W US2005025386 W US 2005025386W WO 2006020190 A1 WO2006020190 A1 WO 2006020190A1
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WO
WIPO (PCT)
Prior art keywords
oil
composition according
group
consisting essentially
composition
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Application number
PCT/US2005/025386
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English (en)
Inventor
Richard Plymale
Original Assignee
Richard Plymale
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
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Publication of WO2006020190A1 publication Critical patent/WO2006020190A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/26—Aluminium; Compounds thereof

Definitions

  • the present invention relates to a dentifrice composition. More specifically, the present invention relates to a dentifrice composition that is capable of being ingested.
  • Tooth powders later modified into toothpastes, have traditionally been available to counter dental caries, as well as gingivitis, the chronic inflammation of soft tissues surrounding the teeth.
  • the mechanism of treatment has been, and still is, the regular removal of the accumulations of deposits on the tooth surfaces. These deposits take several forms, starting with plaque that accumulates in a few hours after previous removal. If left for a longer period of time, the material builds up and becomes thicker, called tartar, which is more difficult to remove. Finally, if allowed to remain, the material is infiltrated with calcium and phosphate ions precipitating a hard, stony, brittle material that cannot be removed by brushing. This material is removed by currettage (scraping) done by a dental professional.
  • Drastic treatment and tooth removal are part of the treatment for this serious condition. Obviously prevention is the best treatment with this disease process: routine daily oral care and regular visits to a dental professional.
  • Regular daily home care includes brushing, flossing and using mouthwash to remove plaque, and in so doing removing the material that supports the presence of bacteria.
  • bacteria There are several species of bacteria associated with tooth decay. The mechanism is that the intake of foodstuffs, notably refined sugar, causes them to be nourished, and when they are, they provide acid as part of their normal metabolism.
  • An effective dentifrice composition should include compounds for the maintenance and preservation of tooth appearance through the removal of dental stains and the polishing of the teeth.
  • the composition should clean and remove exogenous debris as well, thereby aiding the prevention of tooth decay and promoting gingival health. Additionally, abrasives aid in the removal of the tightly adherent pellicle film to which dental stains are affixed.
  • Pellicle film usually comprises a thin acellular, glycoprotein-mucoprotein coating, which adheres to the enamel within minutes after teeth are cleaned. The presence of various food pigments lodged within the film accounts for most instances of teeth discoloration.
  • an abrasive should provide satisfactory cleaning by removal of the pellicle film with minimal abrasive damage to oral tissue, i.e. the dentin and enamel.
  • tooth appearance may be improved by imparting a polished character to the teeth, as the surface roughness, e.g., polish, affects light reflectance and scattering, which are integrally related to how teeth visibly appear.
  • the surface roughness also affects tooth feel, in other words, polished teeth have a clean, smooth and slick feel.
  • Toothpaste, brushing gel, and bleaching gel utilize a blended matrix material into which is provided a detergent, whiteners, plaque and/or tartar removers or inhibitors, flavorings, viscosity control agents, fluoridizers, and the like.
  • No particular toothpaste matrix material is utilized for a brushing gel or a bleaching gel.
  • water is a critical component of the blended matrix material. Toothpastes come in various viscosities and their flow characteristics fluctuate depending on whether the paste is thixotropic or not. There is a paucity of information about the relative viscosities of toothpastes, the film forming qualities of dentifrices (pastes and gels), and the importance of such to the utility of the product.
  • Fischer U.S. Patent No. 5,098,303, U.S. Patent No. 5,234,342, and U.S. Patent No. 5,376,006, teach that the viscosity characteristics of a bleaching gel should be different from the viscosity characteristics of a brushing gel and takes the position that bleaching gels must possess extremely high viscosities in order to stick to the teeth during a bleaching period.
  • Fischer describes excessively high viscosity (e.g., >500,000 centipoises) water-based gels using high carbomer gelling agent concentrations (3.5 weight percent or greater).
  • a dentifrice may bring to the gums and teeth certain ingredients that affect gums and teeth.
  • Such ingredients include fluorides, hydrogen peroxide, enzymes, and special gum treatment agents.
  • the utilities of such additives depend on the residence time in contact with the gums and tooth enamel. The longer such additives remain in contact with the gum and teeth, that is, the longer the residence time in contact with the gums and tooth enamel, one can assume that they better contribute their special qualities.
  • a dentifrice that disintegrates once it is brushed or otherwise exposed to the tooth and gum surfaces provides the minimum residence time.
  • a dentifrice that does not readily disintegrate at the tooth and gum surfaces provides a higher residence time. The latter dentifrice can be expected to contribute more of the benefits to the teeth and gums of the additives in the dentifrice formulation.
  • Every dentifrice has some film forming qualities when applied to teeth and gums. The longer the dentifrice maintains a film while applied over the teeth and gums, the longer is the aforementioned residence time.
  • Dentifrices that are water based typically form fiims on the teeth and gum that quickly disintegrate once the film is exposed to water (water added by the user or saliva carried to the tooth and gum surface). Water is an excellent solvent for a water-based dentifrice. Consequently, water-based dentifrices have relatively short residence times.
  • dental cleansing compositions There are two basic fluid dental cleansing compositions marketed today. They are dental pastes (i.e., toothpastes) and dental gels (brushing gels and bleaching gels). Each is dispensed through a tubular orifice to the user's tooth brushing device or, in the case of some bleaching gels, to the user's dental tray (stint or mouthguard).
  • dental pastes i.e., toothpastes
  • dental gels brushing gels and bleaching gels
  • bleaching gels bleaching gels
  • An important quality of a dental cleansing composition is its flow characteristics as it issues from the tubular orifice. If the composition is runny as it issues to and from the orifice, it is difficult to control the amount of composition to be applied to the brushing device or dental tray. If the composition is too viscous, then it is difficult to expel to and from the orifice and consequentially, the amount of composition to be applied to the brushing device is difficult to control.
  • Dental gels are vehicles for dentifrices, bleaching aids, and fluoride compounds. Gels are colloids in which the dispersed phase has combined with the dispersion medium to produce a semisolid material, such as a jelly. Dental gels are used as a dental paste (toothpaste) substitute. The toothpaste substitute and the brushing gels are used with a toothbrush.
  • a dental paste is a dentifrice that is in the form of a soft, smooth, thick mixture containing a filler material, typically in an aqueous liquid vehicle, that gives the mixture flow characteristics.
  • a dental paste exhibits little of the chemical interactions tlpat take place in forming a dental gel.
  • Some of these dental gels are susceptible to viscosity increases and some to viscosity losses, without apparent scientific basis for either event occurring. Such a formulation may start out sticky and viscous, but with time, the formulation can significantly lose such properties.
  • Such gels are capable of levels of interbonding that when the products are squeezed from tubes and syringes, they leave a long stringy tacky residue emanating from the tube and syringe opening. Such residues deposit the gel in undesired places such as in a patient's mouth (as distinguished from the patient's teeth), on the users hands, on equipment such as a toothbrush handle, and the like.
  • a dentifrice composition including therein a sweetener, an absorbant deactivator, an anti- acid compound, and a carrier, which in combination form a substance that is particularly efficacious for use as a dentifrice agent.
  • the present invention provides an ingestible dentifrice. More specifically, the present invention provides a dentifrice that provides all of the benefits of the prior art dentifrice and is able to be swallowed by the user without the potential for side effects that can occur because of such digestion.
  • the present invention provides a composition that counters the destructive acid by the dual activity of two mechanisms, by supplying a sufficient quantity of a buffer (a substance that neutralizes acid), and supplying a sufficient quantity of a substance that interferes with acid production.
  • the specific dentifrice contains at least the following four ingredients: an antiacid compound, an absorbant deactivator, a carrier, and a sweetener.
  • Alternative components as are known to those of skill in the art, can be utilized without departing from the spirit of the present invention. Examples of such compounds include, but are not limited to, a humectant, an anti ⁇ inflammatory, an odor absorbing compound, an anti-microbial agent, and flavors.
  • the anti-acid agent of the present invention is any ingestible material that is capable of eliminating acid in the oral cavity.
  • Magaldrate U. S. P. Magaldrate is a double salt of aluminum and magnesium hydroxide. Both of these salts are commonly used as digestive aids by neutralizing stomach acid. Each alone has undesirable side effects. It was discovered that the combination did not have the same deleterious side effects and is marketed under the tradename Riopan®. This substance makes a desirable oral care product by providing a protection against the effect of high concentrations of acid in the mouth produced by bacteria such as S. mutans.
  • the absorbant deactivator of the present invention is any ingestible material that is capable of both absorbing and deactivating decay causing components in the dental cavity.
  • An example of such materials include soft, white clay particles is an ingredient not usually associated with an oral hygiene product.
  • Clay mineral is a naturally occurring siliceous mineral that is widely used as a digestive tract aid on the basis of the layer-like atomic structure. It has several desirable features. It is tasteless, white and smooth, non-nutritive and does not contain significant sodium.
  • the designation "kaolin” is used as an all-encompassing designation for specific materials. Examples of such materials include, but are not limited to, attapulgite, smectite, montmorillonite, and bauxite. Also included in this category designation are materials that have been processed or refined as are commercially available.
  • the carrier of the present invention can be any compound capable., of functioning orally to carry the necessary compounds of the present invention.
  • a non-reacting expedient When forming a tablet, a non-reacting expedient must be used as a carrier.
  • a non-reacting expedient is widely used as an expedient in pharmaceutical products: a non-reacting expedient used widely for tableting. It is accepted as an inert filler that is ultimately excreted unchanged. An added benefit is that these materials control solid tablet disintegration rate.
  • the sweetener can be any sweetener that does not cause or increase the incident of dental damage.
  • suitable sweetening agents include sorbitol, sodium cyclamate, saccharine, commercial materials such as NutrasweetTM brand of aspartame and xylitol.
  • Xylitol is a naturally occurring pentose that has a sweet taste similar to sugar. It is non-carcinogenic (doesn't promote tooth decay) on the basis that it is chemically different from sugar and cannot be metabolized by oral bacteria responsible for tooth decay, and is appreciated for this activity.
  • Acesulfame-K is a sweetener now commonly used in Europe, but it is gaining acceptance in the United States to provide sweetening to products where sugar is not used.
  • Acesulfame's additional benefit is that it augments the sweet taste of xylitol, with a lingering pleasant after taste, important in a orally retained product.
  • compositions of the present invention can be flavored.
  • the flavors are formulated to be as pleasant.
  • examples of such flavors include, but rare not limited to, a good quality mint or a fruit flavoring such as apple or orange.
  • the flavoring preferably remains for a longer-than- expected time period thus enhancing the "its working" perception without negative medicinal connotations, which are found to reduce frequency of use and undermine the frequent cleansing advantage.
  • the feeling in the mouth is equally pleasant. A smooth, tingly "something's happening” feeling is perceived immediately upon application, followed by a clean, fresh, well lubricated mouth and tooth surface that persists much longer than mints, gums, breath fresheners and even mouth washes and toothpastes.
  • the high flavor levels which can be pleasantly incorporated into the present invention, whose frequent application is encouraged by the unique character of the invention, and which are retained in the mouth for long time periods also contribute to the plaque controlling properties of this invention.
  • natural and synthetic flavor and sweetener agents as diverse as menthol, xylitol and glycyrrhizin are known to be beneficial towards plaque control and are included in the compositions of the present invention (begai, J. Pharm. ScL, 74 pp. 79-81 (1985) and Makkinen, J. Am. Dent. Assoc. Ill, pp. 740-741).
  • the flavoring component is present as a denaturant in the non-toxic alcohol component capable of digestion.
  • the conventional flavoring components are exemplified by the following materials, menthol, anise oil, benzaldehyde, bitter almond oil, camphor, cedar leaf oil, cinnamic aldehyde, cinnamon oil, citronella oil, clove oil, eucalyptol, heliotropine, lavendar oil, mustard oil, peppermint oil, phenyl salicylate, pine oil, pine needle oil, rosemark oil, sassafras oil, spearmint oil, thyme oil, thymol, wintergreen oil, lemon and orange oils, vanillin, and other flavoring oils generally regarded a safe (GRAS) by health authorities.
  • GRAS a safe
  • compositions of the invention can also contain certain phosphate salts, such as sodium pyrophosphate, which have been shown to aid in the control of plaque and the calcified plaque called tartar.
  • certain phosphate salts such as sodium pyrophosphate, which have been shown to aid in the control of plaque and the calcified plaque called tartar.
  • preferred embodiments of the present invention include various viscosity control agents to impart certain viscosity characteristics to the products of the invention. Viscosity can play a role in achieving optimum mouth feel and flavor retention characteristics of the invention, therefore altering the viscosity can be beneficial.
  • Viscosity between about 30 and about 600 cps is preferred and between about 70 and 250 cps is particularly preferred.
  • Viscosity control agents are known in the prior art and can be selected from natural and synthetic gums such as gum tragacanth, methyl cellulose, polyvinyl pyrrolidone, and hydrophylic carboxyvinyl polymers such as those sold under the trademark Carbopoi 934. Generally, about 0.1 percent to about 5 percent of a solution of viscosity control agent is used. However, other amounts can be used for creating alternative viscosities.
  • the coloring agent is typically added in an amount of 0.01 percent to about 0.02 percent by weight.
  • Citric acid is often utilized as a flavor additive. All types of flavoring materials are generally used in amounts of about 0.01 to about 5.0 percent by weight, preferably about 0.05 percent to about 3.0 percent by weight.
  • a buffering ingredient can also be added to the compositions of the invention in order to prevent natural degradation of the flavoring components.
  • the pH of these compositions is adjusted to 3.5 to about 7, preferably from about 5 to about 6.
  • the buffering ingredients can be an alkali metal salt of a weak organic acid, for instance, sodium benzoate, sodium citrate, sodium phosphate, or potassium tartrate.
  • the buffering agent is generally added in an amount of about 0.1 to about 1.0 percent by weight.
  • compositions of the invention can optionally contain at least one humectant selected from the group consisting of glycerine, xylitol, sorbitol and propylene glycol.
  • humectants are utilized in the proportion of about 3 percent to about 12 percent by weight based upon the total weight of the composition.
  • the humectant is utilized in an amount of about 3 to 4 percent by weight.
  • Various natural compounds can be added to the composition of the present invention. For example, ApplephenonTM (Asahi), a blend of polyphenols from apples and a unique blend of procyanidians flavonoids as primary constituents.
  • ApplephenonTM inhibits glucosyltransferase of S. mutans and other microorganism that have an activity of dental plaque formation as a small dose loading.
  • Another example is citrus bioflavonoids, fruit pulp fibrous material that contained a number of substances that have a beneficial effect in the mouth.
  • TeavigoTM a green tea extract, can be added.
  • orange oil or orange oil fractions such as limonene might be added for a persistent "fresh orange” effect.
  • certain citrus products have germicidal effects as pointed out earlier.
  • Magnesium Stearate, NF or stearic acid can also be added.
  • Magnesium Stearate is an excipient commonly used in tableting to provide a slipperiness to allow tablets to be ejected from tableting machine dies without crumbling or breaking. The point is to use the salt stearic acid (also which is widely used for the same purpose) to avoid any pH contributions that are not desired.
  • Oil of Melaleuka can also be added to the composition of the present invention.
  • Oil of Melaleuka is a naturally occurring essential oil from the tea tree indigenous to Australia, widely known for its obtundent and anti ⁇ inflammatory properties.
  • Cyclodextrans can also be added to the composition of the present invention. Cyclodextrans are naturally occurring organic compounds that have a circular configuration and have the unique ability to absorb small molecules, thereby eliminating odor. They are available in three sizes, alpha (six-amylose), beta (7-amylose), and gamma (8-amylose), and various configurations and are usually used as blends. All combinations are encompassed in the designation "cyclodextrans".
  • polyhydric glycols Another additional compound is polyhydric glycols.
  • Polyalcohols for example, are commonly used to convert dry powered materials into a paste. Representative examples include, but are not limited to, glycerine and propylene glycol.
  • Antimicrobial agents can also be added to the composition.
  • examples of such agents include, but are not limited to, Domiphen Bromine, U.S. P. and Cetylpyridium chloride.
  • Such compounds are widely accepted as antiseptics and wetting agents that are used in several major brands of mouthwash, such as "Scope” and “Greenmint”. They are available in powder form that is readily tableted. They are "mature" product and thus are widely available as a standard material.
  • Oxygenation agents can also be added to the composition. Such agents are typically peroxides, per oxygen compounds are known to provide an oxidative reaction by releasing oxygen. Representative examples include, but are not limited to, hydrogen peroxide and carbamide peroxide.
  • the dentifrice can be in the form of a tablet, or similar type formulation, or a paste or other similar formulation such as for example a gel, as disclosed in detail above.
  • a paste or other similar formulation such as for example a gel, as disclosed in detail above.
  • the primary difference between the prior art dentifrice pastes or gels is the compounds included in the composition.
  • Tablets can be readily carried in a small tube making them available whenever desired, such as right after eating, or before close face to face contact.
  • the composition of the present invention contains no harsh ingredients, can be readily swallowed, so toothpaste of this formula would be ideal for those whose health is compromised i.e. such as persons in nursing homes. Some people, stroke victims, or with dementia, do not frequently swallow so oral prevention is further maximized for increasing benefits.
  • One of the benefits of the dentifrice of the present invention is the ability of the composition to reside in the mouth for extended periods of time, since the composition does not need to be rinsed from the user's mouth. Since the dentifrice can reside in the mouth for longer periods of time, the dentifrice is capable of functioning more effectively as it has a longer period of time in which to work.
  • the benefits of present invention are numerous including the ability to provide a convenient, simple to use mouth-cleansing agent.
  • the composition is portable and does not require a flask like mouthwash or brush and toothpaste equipment. All of the ingredients can be swallowed where mouthwash and toothpaste should be spit out.
  • the invention is easy to produce, because tableting is easily accomplished as these materials are compressed. Additionally, the product is easily packaged, because rolls are commonly used, sold and distributed.
  • composition of the present invention is also efficacious against mouth odor and dryness by promoting mouth freshness, has buffering capacity that negates any rise in pH. Absorbing characteristics of the composition destabilizes plaque and selectively absorbs at sites that would otherwise absorb oral debris.
  • the composition also has sustained germicidal qualities achieved by the presence of several germicidal ingredients to inhibit oral micro-organisms.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

Composition dentifrice incluant un édulcorant, un désactivant absorbant, un composé antiacide et un support, qui, une fois mélangés, forment une substance particulièrement efficace comme agent dentifrice.
PCT/US2005/025386 2004-07-16 2005-07-18 Composition dentifrice WO2006020190A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58881204P 2004-07-16 2004-07-16
US60/588,812 2004-07-16

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WO2006020190A1 true WO2006020190A1 (fr) 2006-02-23

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101244023B (zh) * 2008-03-28 2010-10-13 贾剑 凹凸棒绿茶牙粉
EP2407146A1 (fr) * 2010-07-15 2012-01-18 Nutrinova Nutrition Specialties & Food Ingredients GmbH Utilisation d'acésulfame K en tant que modulateur de saveur

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01117820A (ja) * 1987-10-29 1989-05-10 Noevir Co Ltd 頭髪用化粧料
JPH01308221A (ja) * 1988-06-03 1989-12-12 Tsumura & Co 浴剤組成物
FR2666227A1 (fr) * 1990-09-05 1992-03-06 Darcy Laboratoires Composition therapeutique notamment pour le traitement des affections de la cavite buccale.
US6319513B1 (en) * 1998-08-24 2001-11-20 The Procter & Gamble Company Oral liquid mucoadhesive compounds

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH01117820A (ja) * 1987-10-29 1989-05-10 Noevir Co Ltd 頭髪用化粧料
JPH01308221A (ja) * 1988-06-03 1989-12-12 Tsumura & Co 浴剤組成物
FR2666227A1 (fr) * 1990-09-05 1992-03-06 Darcy Laboratoires Composition therapeutique notamment pour le traitement des affections de la cavite buccale.
US6319513B1 (en) * 1998-08-24 2001-11-20 The Procter & Gamble Company Oral liquid mucoadhesive compounds

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DATABASE CAPLUS 10 May 1989 (1989-05-10), YOSHIMASA ET AL.: "Synergistic antidandruff hair preparations containing benzoic acid and hinokitiol and/or oil of Melaleuka alternifoia", XP002992720 *
DATABASE CAPLUS 12 December 1989 (1989-12-12), HASHIMOTO ET AL.: "Bath preparations containing Melaleuka alternifolia oils.", XP002992719 *
DATABASE WPI Week 199218, 6 March 1992 Derwent World Patents Index; AN 1992-143348, XP002992718, "Treatment of mouth and throat disorders - using tablets contg.clathrate or menthol in cyclodextrin." *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101244023B (zh) * 2008-03-28 2010-10-13 贾剑 凹凸棒绿茶牙粉
EP2407146A1 (fr) * 2010-07-15 2012-01-18 Nutrinova Nutrition Specialties & Food Ingredients GmbH Utilisation d'acésulfame K en tant que modulateur de saveur
WO2012007170A1 (fr) * 2010-07-15 2012-01-19 Nutrinova Nutrition Specialities And Food Ingredients Gmbh Utilisation de l'acésulfame k en tant que modulateur d'arôme

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