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WO2000023040A1 - Composition desodorisante seche pour administration buccale - Google Patents

Composition desodorisante seche pour administration buccale Download PDF

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Publication number
WO2000023040A1
WO2000023040A1 PCT/US1999/023811 US9923811W WO0023040A1 WO 2000023040 A1 WO2000023040 A1 WO 2000023040A1 US 9923811 W US9923811 W US 9923811W WO 0023040 A1 WO0023040 A1 WO 0023040A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition
deodorizing
group
mouth
dry
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US1999/023811
Other languages
English (en)
Inventor
Subraman R. Cherukuri
Tommy L. Chau
David M. Teale
Paul M. Croushorn
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Biovail Technologies Ltd
Original Assignee
Fuisz Technologies Ltd
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.)
Filing date
Publication date
Application filed by Fuisz Technologies Ltd filed Critical Fuisz Technologies Ltd
Priority to AU64280/99A priority Critical patent/AU6428099A/en
Publication of WO2000023040A1 publication Critical patent/WO2000023040A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • 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
    • A61K8/27—Zinc; Compounds thereof
    • 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/35—Ketones, e.g. benzophenone
    • 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • 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
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/58—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
    • 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A61K8/731—Cellulose; Quaternized cellulose derivatives
    • 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
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • 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
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/24—Thermal properties
    • A61K2800/244—Endothermic; Cooling; Cooling sensation
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/58—Metal complex; Coordination compounds

Definitions

  • the present invention relates to a deodorizing composition, and more particularly, to a dry, storage stable, orally-administered deodorizing composition which is highly effective as a mouthwash, mouth cleaner and breath freshener.
  • the composition provides a substantially alcohol-free (ethanol-free) microparticulate dispersion having oral antiseptic and microbial action.
  • the invention also relates to a method of neutralizing or masking malodor emanating from the mouth and digestive tract, which comprises administering the novel composition herein described.
  • a dry, deodorizing composition for oral administration which dissolves quickly in the mouth, has a palatable taste, and affords the user both instant and long-range breath and body odor protection, even after being rinsed from the mouth or swallowed.
  • the composition should furthermore provide bacteriostatic and antiseptic action, as well as impart a clean, cool or refreshing sensation to the mouth.
  • the formulation should be storage stable over extended periods, such that the individual components do not neutralize or react with one another while on the shelf.
  • Another desirable attribute of a deodorizing composition should include an ability to be tableted into lozenges which dissolve quickly under the action of saliva. In this way, the consumer is not left sucking on a candy mint for several minutes in social and business situations where such actions may not be acceptable.
  • a dry deodorizing composition in particulate form for oral administration which comprises at least one carrier material, at least one processing aid selected from the group consisting of oleaginous substances and at least one active ingredient which is selected from the group consisting of deodorizing substances and cleansers.
  • the formulation provides an antiseptic cleaning or bacteriostatic action, eliminating many of the common germs and bacteria found in the mouth, mucous membranes and between the teeth.
  • the composition herein described imparts a refreshing and cooling "vapor action" sensation to the oral and nasal passageways. Unlike most commercial liquid mouthwashes available today, the formulation of the invention is substantially alcohol-free (little or no ethanol).
  • Also provided as part of the invention is a method of effectively masking or neutralizing/eliminating odors emanating from the mouth, digestive tract and bodily pores which involves the oral administration of the formulation described above.
  • a method of effectively masking or neutralizing/eliminating odors emanating from the mouth, digestive tract and bodily pores which involves the oral administration of the formulation described above.
  • the invention provides a tableted, oral deodorizing composition and a method of making same.
  • the composition dissolves quite rapidly in the mouth, and has excellent oral cleansing attributes.
  • Figure 1 is a photo micrograph at 250X normal size of 0.8 grams of unprocessed mouth deodorizing and cleansing material.
  • Figure 2 is a photo micrograph at 250X normal size of 0.8 grams of the same material in Figure 1 after processing according to the procedures herein set forth.
  • Figures 3 - 7 are graphs of comparative test data for the composition of the invention in one embodiment versus one or more commercial brands of mouthwashes.
  • the novel dry deodorizing composition of the invention comprises a carrier material as one component.
  • This carrier material is utilized to provide support for, or "piggyback", the hereinafter described active deodorizing substance(s), especially during preparation of the composition.
  • Carrier materials are typically chosen from the listing of saccharide materials available in the food industry. These materials will include mono, di, tri- and polysaccharide material, either alone or in combination, and their related oligomers, as well as oligosaccharides.
  • invert sugar, sucrose, fructose, maltose, dextrose, polydextrose, polydextrin, glucose (corn syrup), maltodextrin, corn syrup solids, etc. are just some examples of suitable carrier material.
  • sugar alcohols are also included in the term saccharides.
  • a non-limiting list of sugar alcohols includes the following: sorbitol, mannitol, maltitol, pentatol, isomalt (Palatinit®), xylitol, et al.
  • Sugar derivatives include chemical and enzymatic derivatives and include, but are not limited to, chloro derivatives of sugar such as sucralose.
  • Especially preferred carrier materials for use in the novel dry deodorizing composition are those which may be referred to as "non- sucrose", and include polydextrose, maltodextrin, isomalt and combinations thereof.
  • the carrier component of the composition of the invention will typically constitute about 10 - 98% thereof, more particularly about 50 -95%, and even more desirably about 70-90% of the composition of the invention (unless otherwise stated, all percentages provided herein are weight percentages based on the total weight of the final composition).
  • active ingredients may be naturally or synthetically (man-made) derived and are chosen from those available in the industry with active deodorizing and/or cleansing prowess; they are capable of effectively masking or neutralizing/ eliminating body odor.
  • the compounds that neutralize odor do so by reacting with the sulfur and other chemical compounds contained in organic substances, particularly food substances, that are responsible for the malodor.
  • Preferred active ingredients include one or more metallic ions along with their equivalent salts, esters or other equivalent compounds thereof.
  • Metallic ions can include, for example, copper and zinc ions. In particular, zinc gluconate, copper gluconate and sodium copper chlorophyllin are desirable. Other metallic ions and inorganic compounds and substances available to the skilled artisan may also be utilized.
  • active ingredients includes members of the ionone/ketone terpene compounds utilized as odor neutralizers, particularly odor emanating from the mouth and digestive tract.
  • a compound known as alpha-ionone may be desirable.
  • This family of compounds is particularly desirable because its members are known to react with sulfur in, for example, garlic and onions, to effectively neutralize the disagreeable smells associated with the normal breakdown of these food substances.
  • active ingredients capable of oral administration may be used as active ingredients. These would include such compounds as menthol, menthone, thymol and eucalyptus. Any of the active ingredients may be available in their raw, unprocessed state, but can also be provided as a commercial preparation in dry powder or liquid form. Other examples of highly desirable active ingredients include the residue from cardamon seeds, such as cardamon oil, which is well-recognized by the skilled artisan for its deodorizing capabilities. Mushroom extract, ginseng, parsley seed extract and sunflower oil may also be desirable. Other naturally derived extracts are also highly suitable.
  • active ingredient(s) heretofore described will typically comprise from about 0.001 to 10% of the composition of the invention, and more preferably will usually be within the range of from about 0.01 to 5% thereof. In certain embodiments, it may even be desirable to utilize 0.1 to 3% of the actives as part of the final overall deodorizing formulation. The foregoing percentages may be decreased or increased by the person skilled in the art, depending upon how strong or weak of a final composition is ultimately desired.
  • the active ingredients heretofore described are preferably provided as part of an encapsulated matrix within the novel deodorizing composition set forth herein. In this way, the actives' deodorizing and/or cleansing prowess is preserved until the composition is taken orally and dissolved in the mouth by an end user.
  • one or more processing aids such as oleaginous material is utilized. It is believed that the oleaginous material surrounds and enrobes individual particles of the active ingredients, thereby creating a matrix of several thousand individually enrobed particles within each serving of the final composition.
  • Suitable oleaginous material includes various food-grade oils and fats available in the industry. Of these, those with emulsifying properties are often particularly desirable.
  • Edible vegetable and animal oils and fats may be utilized for this purpose.
  • Stearine may be utilized as an encapsulating agent, while a fat product marketed under the name DurEm 117 is also efficacious.
  • Canola oil is preferred as well, while medium chain triglyceride (MCT) oils are also desirable.
  • Oleaginous material as encapsulating/processing aids will typically comprise about 0.1 to 10% of the deodorizing composition of the invention, and more desirably will make up from about 1 to 7% thereof.
  • encapsulation techniques may be utilized to provide the encapsulated actives matrix as part of the composition of the invention.
  • the flash-flow processing techniques set forth in U.S. Patent No. 5,380,473 can be utilized.
  • the techniques of the 473 patent may be further utilized in conjunction with a unique tower device in which material to be encapsulated is provided in free fall by a sprayer at the top of the tower, and an encapsulant material such as oleaginous substances is extruded in the form of droplets to coat and encapsulate the dry, particulate material exiting the tower.
  • Other methods available in the art such as, e.g. spray-drying, atomizing and simple and complex extrusion processes are also within the scope herein set forth.
  • Simple mixing methods with industrial scale mixing equipment Hobart and Sigma type mixers) may also be utilized to prepare encapsulations.
  • sweeteners are included to impart a palatable sweetness or savoriness to the final formulation.
  • Sweeteners can be chosen from the listing of saccharide material also available to the skilled artisan as the carrier component, or can be different materials from those comprising the carrier material, heretofore described.
  • Sweeteners can include mono-, di- and tri- and polysaccharide materials, either alone or in combination, and their related oligomers. Invert sugar, sucrose, fructose, maltose, dextrose, polydextrose, polydextrin, glucose (corn syrup), maltodextrin (corn syrup solids) etc. are just some examples of suitable sweeteners.
  • sweeteners include saccharin, aspartame, acesulfame, sucralose, sorbitol, mannitol, maltitol, xylitol as well as other commercially available sweeteners such as the dihydrochalcone compounds, glycyrrhizin, Stevia Rebaudiana (Stevioside), and the hydrogenated starch hydrolysates.
  • those sweeteners considered in the industry to be sugarless or non-sucrose are perhaps more preferred.
  • Other sweeteners contemplated by the skilled artisan which are typically utilized in the food or mouthwash industry may also be used.
  • the sweeteners are added in amounts equal to about 0 - 10% of the composition, and preferably within the range of about 0.01 - 5%. More preferably, the sweeteners will comprise about 0.1 - 1% of the final dry deodorizing formulation according to its various embodiments.
  • Flavoring agents may also be included as part of the deodorizing composition of the invention. These may or may not be recognized as true deodorizers in and of themselves, i.e. they may or may not neutralize or even mask odor, but are particularly preferred because they impart an agreeable taste and flavor to the composition in one or more of its various embodiments. Any number of flavoring agents may be utilized (in whatever form), and can be chosen from the listing of suitable natural and synthetic flavoring liquids and powders, etc. available in the industry. An illustrative list of such agents includes such oils as volatile oils and synthetic flavor oils, flavoring aromatics, liquids, powders, oleoresins and extracts derived from plants, leaves, flowers, fruits, stems, and bark, etc., as well as any combinations thereof.
  • the listing includes those flavoring agents which impart a cooling, refreshing or mint-tasting flavor to the final composition, as for example cinnamon, and those of "mint" origin such as peppermint, spearmint and wintergreen.
  • These flavoring agents can comprise from about 0 - 5% of the composition. Desirably, they will make up about 0.01 - 5% of the formulations herein set forth.
  • Coloring agents may also be included as part of the novel composition of the invention.
  • Naturally and synthetically-derived food dyes can make up from about 0 to 1%, more preferably about 0.0001 to 0.5% of the final composition.
  • An optional component of the novel deodorizing formulation herein described is an absorbent material.
  • the absorbent material assists in the absorption of malodorous substances from the mouth and gut.
  • This material should preferably possess bioadhesive properties and have an affinity for the mucous membranes of the mouth under the presence of saliva or other aqueous media, thereby assisting the body's absorption of the active ingredients.
  • An especially preferred absorbent material is hydroxypropylmethylcellulose (HPMC), as well as polyvinylacetate, and combinations thereof, but the absorbent material can also comprise one or more other substances known in the art with sulfur absorbing prowess.
  • cellulosic materials selected from the group consisting of alkyl celluloses, hydroxyalkyl celluloses and hydroxyalkylalkyl celluloses are contemplated.
  • other polyesters and polyalkyl- and polyalkylene esters, especially polyvinylesters are contemplated.
  • the absorbent material will comprise about 0 to 15% of the composition of the invention, and more desirably be within the range of about 0.1 to 5% thereof.
  • flash-flow processing provides a simple and effective method of preparing such compositions.
  • flash-flow has become recognized as referring to the conditions of temperature and force required to transform a solid feedstock having a certain morphological and/or chemical structure into a different morphological and/or chemical form without subjecting the materials to the excess heat or other requirements inherent in other forms of processing.
  • the resultant structure has now been referred to as a "shearform matrix.”
  • the concepts of flash-flow and shearform matrix are further described, for example, in co-owned U. S. Patent 5,236,734 issued August 17, 1993, and U. S. Patent 5,238,696 issued August 24, 1993, as well as in U. S. Patents 5,518,730, 5,387,431, 5,429,836 and 5,582,855.
  • flash-flow processing involves subjecting a feedstock to conditions of temperature and force which induce a solid feedstock to rapidly undergo such physical and/or chemical transformation.
  • the time during which the feedstock material is subjected to temperatures is extremely short.
  • Flash-flow processing can be accomplished either by the more preferred flash heat method or via a flash shear method, as both are described further herein.
  • a shearform matrix can be formed by spinning a feedstock in a "cotton candy" type fabricating type machine.
  • a spinning machine developed by Fuisz Technologies Ltd. of Chantilly, VA and patented under U.S. Patent No. 5,427,811 and especially under U.S. 5,458,823 may be preferred for the flash- heat process.
  • This patent describes a spinning machine which has a series of elongated heating elements arranged in between a base and a cover.
  • the heating elements, base and cover together define a chamber into which a non-solubilized feedstock material is inserted which is capable of intraparticle flow upon application of heat and force.
  • Means are provided for individually heating each of the elongated heating elements, and restriction means in the form of a cylindrical shell or annular plate which circumscribes the heating elements permits restrictive flow of the processed feedstock which is expelled from the chamber.
  • flash heat will be understood to mean a process which includes subjecting a feedstock to the combination of temperature, thermogradients, flow, flow rates, and mechanical forces of the type produced in a candy machine or the above-referenced U. S. Patent 5,427,811, as well as other apparatus having a spinning head, such as that described in U.S. Patent No.s 5,445,769, 5,447,423 and 5,458,823 and recently allowed U.S.S.N. 08/854,344.
  • the apparatus is operated at the temperature and speed which permits flash heat of the feedstock without deterioration of any of its ingredients, and these parameters can easily be optimized by those skilled in the art.
  • the feedstock material is heated sufficiently to create an internal flow condition, i.e., intra-particle flow, which permits part of the feedstock to move at a subparticle level with respect to the rest of the mass and exit openings provided in the perimeter of the spinning heat.
  • the centrifugal force created in the spinning head flings the flowing feedstock material outwardly from the heat so that it reforms with a changed structure.
  • the force required to discharge flowable feedstock is provided by the forces which result from the spinning head.
  • the flash heat process has been used in many cases to produce an amorphous matrix from a crystalline material, as disclosed in the aforementioned Fuisz patents.
  • the feedstock includes the heretofore described components constituting the orally administered deodorizing composition.
  • flash-flow flash heat or flash shear
  • a shearform matrix is formed by raising the temperature of the feedstock material, which includes a non-solubilized carrier, to a point where the carrier undergoes intra-particle flow.
  • the carrier component is preferably a saccharide-based material.
  • the feedstock is advanced and ejected from an extruder or similar type of machinery while the carrier is undergoing intra-particle flow and is then subjected to disruptive fluid shear forces to form multiple parts or masses.
  • the flash shear process can be carried out in an apparatus which has means for increasing the temperature of a non-solubilized feedstock and means for simultaneously advancing it for ejection.
  • a multiple heating zone twin extruder can be used for increasing the temperature and advancing material feedstock.
  • the apparatus includes a means for ejecting the feedstock in a condition for shearing it to provide the shearform matrix.
  • the means for ejecting is in fluid communication with the means for increasing the temperature and is arranged at the point to receive the feedstock while it is in the internal flow condition.
  • the means for ejecting the feedstock is preferably a nozzle which provides sufficient frictional gas force applied to the ejected feedstock stream to disrupt the stream and form shearform masses.
  • the means for shearing is arranged proximally to the ejector and is disposed to effect the shear of the feedstock while it is in the internal flow condition.
  • the means for shearing is the means for delivering fluid such as at sufficient velocity and at elevated temperature against the feedstock stream as it exists a nozzle.
  • Such a device can be an external atomizing nozzle.
  • the means for shearing can also be a chamber in which the environment can be maintained to induce shear upon the collision of a high velocity of a stream of feedstock directed against a preselected and maintained environment.
  • the individual components of the novel composition herein described may thus be subjected to flash shear processing as well. Those skilled in the art may find that flash-shear methodology and parameters can be further adjusted to their particular needs.
  • the time during which the feedstock material is subjected to elevated temperature is very short.
  • the feedstock is subjected to elevated temperature usually for only tenths of a second, and in the flash-shear method the feedstock is subjected to elevated temperatures for a time on the order of seconds. This has specific benefits in situations when materials might be degraded or otherwise detrimentally affected by excessive exposure to heat.
  • Flash-flow processing results in increased surface area and increased solubility of the ingredients subjected thereto, and contributes to actual mixing of the ingredients with each other without degradation and undesirable chemical reactions.
  • shearform matrix attributes as they are often referred to, are highly desirable in a final product.
  • the deodorizing product of the invention is produced in dry, particulate form as a result of being processed according to the unique procedures herein described as flash-flow.
  • the composition may also be described as having what can be referred to as "microparticulate dispersion" qualities. Minute particles of the individual components constituting the shearform matrix, and hence the formulation itself, are evenly mixed and dispersed throughout the entire matrix.
  • Figure 2 is a photo micrograph of the composition of the invention. The amorphous, random structure of the material shown in Figure 2 is a characteristic of the final composition's microparticulate dispersion.
  • microparticulate dispersion refers to the final single matrix containing integrally dispersed and combined amounts of dissimilar ingredients.
  • the disparate material is bound up in the matrix, which in this particular embodiment is a "flake".
  • Many of the microparticulates can be seen as small circles or spheres throughout the matrix.
  • Figure 2 is to be contrasted with Figure 1 , which shows material prior to being processed in the manner herein described.
  • the Figure 1 material does not possess the attributes of the material shown in Figure 2. Instead, there are relatively large crystalline chunks of material without any sort of matrix structure. Small granules, flakes, spicules, powders, particles, fibers and floss, etc.
  • the flash flow methods herein described impart another significant and unique advantage to the product of the invention.
  • the dry material is substantially free of moisture, to a significantly greater extent than had the individual components been combined using standard mixing apparatus.
  • the overall effect can not be understated. Excess moisture which is eliminated during the flash flow process can not then be present as a medium within which the components of the composition can react, and thereby render the composition unpalatable during storage.
  • the composition appears to be almost moisture-resistant as a result of flash-flow processing, until it is dissolved in the mouth or in water sufficient to yield a serving thereof.
  • many so-called breath deodorizing or mouthwash formulations commercially available today are in liquid form.
  • compositions require large, cumbersome and bulky packaging, i.e. plastic bottles in order to be marketed. In many instances, it is simply not possible to have these compositions in dry form, because they are not storage stable. The consumer is then left with the option of toting around bottles of mouthwash, whether small or large, which often break open in compartments such as purses and pockets.
  • the novel composition of the invention is storage stable in its dry form for a substantially long time period, and therefore may be housed in easy to use, tear-open foil-type packages.
  • compositions according to the various embodiments herein described are that as a result of flash-flow processing, the formulation may be tabletted into standard, bite size lozenges and single-serving tablets. Standard tablet presses known to the skilled artisan may be utilized for this purpose. It has now been further found that the material to be tabletted can be in the form of granules, particulates, flakes and spicules, etc. prior to entering the tablet press. Typically, shearform matrix material has been in the form of fiber or floss prior to being tabletted into dosage forms for pharmaceutical applications. Floss requires chopping, however, in order to enhance the flowability of the material. The composition of the invention, therefore, represents a further advance in the state of the art of processing shearform matrix material.
  • the tabletted lozenges of the invention dissolve rapidly in the mouth, preferably in under about 30 seconds or even less time. There is no need for the end user to be left sucking on a standard breath mint in social and business situations where this would not be desirable. The consumer can quickly deodorize his/her breath by dissolving the tabletted formulation rapidly and completely in the mouth.
  • the composition of the invention is available in dry form, individuals do not need to tote around bottles of mouthwash which are bulky and which tend to spill their contents. Yet the composition herein set forth compares favorably with all commercial brands of mouthwashes sold over-the-counter in liquid form. It is therefore considered to be a further advance in the art to formulate a mouthwash in dry, non-liquid form which can replace many of the liquid products available today.
  • composition herein described is substantially ethanol-free.
  • the product herein described will freshen breath and clean and deodorize the mouth without this carrier.
  • the user may first dissolve a pre-set amount in an excess of suitable liquid such as a half glass of water. More preferably, the composition may simply be placed in the mouth as is (e.g., dry flakes or dry tablet form), and allowed to dissolve with the action of saliva or other aqueous media. The composition is then swished around the mouth to provide rinsing action and a cooling, refreshing vapor action sensation. Movement inside the mouth aids in contacting the mucous membranes and in reaching between the teeth to neutralize chemical odors and kill the living organisms which cause bad breath. The composition may then be expunged from the mouth. Alternatively, the composition is swallowed to allow the active ingredients to act on the sources of malodor, e.g.
  • a suitable serving size can vary according to the particular desires of the skilled artisan, but is usually within the range of about 0.1 to 50 grams, preferably about 0.3 to 20 grams. Volume-based serving sizes, e.g. one or two teaspoons or tablespoons, are also within the scope of the invention.
  • composition herein described may be further utilized as part of a larger confectionery formulation in that it can comprise one ingredient in a candy, mint, chewing gum or other edible delivery system.
  • the composition may be easily blended therein by traditional mixing methods.
  • a dry, deodorizing formulation for oral administration was prepared with components as set forth in TABLE 1 below:
  • a dry, deodorizing formulation for oral administration was prepared with components as set forth in TABLE 1 above, with the exception that additional menthol (up to about 7%) was utilized to provide an even more cooling, vapor action sensation. A corresponding amount of polysaccharide material was reduced.
  • Each tester was then instructed to assign the sample a hedonic score of between 1 and 10 for each of the following criteria: flavor, mouthfeel, vapor action, cooling sensation, bitterness, burning sensation, sweetness and melt characteristics. The higher the rating, the more positively the product's attribute was judged by the tester.
  • the scores for the attributes were then totaled for each product. The mean total score for the four products was 47.54, with all total scores within approximately 1.5 points of the mean. This indicated that all products had comparable subjective sensory ratings. This further indicates that a dry mouthwash formulation can provide the same sensory qualities as well-established commercial liquid brands, as well as cough drops.
  • the product of the invention was compared with LISTERTNE brand mouth wash by an independent testing firm, Woelfel Research, Inc. of Vienna, Virginia. Following the protocol set forth in Example 3, twelve testers chosen from the public were asked to rate the product of the invention (embodiment according to TABLE 1) with LISTERTNE mint-flavored mouthwash on a hedonic scale of 1 to 10 according to the following criteria: flavor, texture, vapor action, cooling, breath freshening and overall. The results are graphed in Figure 3. The results again indicate that the dry mouthwash product of the invention has comparable or even better sensory qualities than does the commercial brand, and is available in dry, particulate form with no alcohol.
  • Figures 4 - 7 are graphs of the results obtained from the twelve panelists who then rated the effects of the respective products for up to 15 minutes after rinsing or swallowing, respectively, for the following criteria: breath freshening intensity, flavor intensity, intensity of coolness in the throat, and intensity of coolness in the nasal cavity.
  • breath freshening intensity a parameter that specifies the amount of breath freshening intensity of the dry breath-freshening and deodorizing formulation of the invention in just one of its embodiments is highly competitive with the best-selling commercial liquid brand of mouthwash.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)

Abstract

Cette invention se rapporte à une composition désodorisante sèche pour administration buccale, qui contient au moins une substance véhicule, au moins un auxiliaire de transformation et au moins un ingrédient actif qui est choisi dans le groupe constitué par des substances désodorisantes. La formule de cette composition est très stable au stockage et assure durablement une protection rafraîchissante de l'haleine. Cette composition produit une sensation froide rafraîchissante dans la cavité buccale de l'utilisateur et possède des propriétés antiseptiques et bactériostatiques.
PCT/US1999/023811 1998-10-16 1999-10-14 Composition desodorisante seche pour administration buccale Ceased WO2000023040A1 (fr)

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US09/173,998 1998-10-16

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WO2002041862A1 (fr) * 2000-11-21 2002-05-30 Orix As Preparation pour hygiene bucco-dentaire contre l'halitose
WO2002058469A1 (fr) * 2001-01-23 2002-08-01 Van Beek, Ron Composes et compositions pesticides
FR2821552A1 (fr) * 2001-03-01 2002-09-06 Cll Pharma Procede pour rendre hydrosoluble un principe actif naturellement peu ou pas soluble dans l'eau et ses utilisations
WO2007016644A1 (fr) * 2005-08-02 2007-02-08 Wm. Wrigley Jr. Company Procede de criblage pour l'identification de composes convenant au traitement des mauvaises odeurs de la cavite buccale associees a la consommation d'ail
WO2008016855A1 (fr) * 2006-08-02 2008-02-07 Wm. Wrigley Jr. Company Compositions orales efficaces pour le traitement de la mauvaise haleine de la cavité buccale associée à la consommation de composés donnant une odeur
EP2070528A1 (fr) * 2007-12-13 2009-06-17 Gudrun Pieper Procédé destiné à l'élimination d'odeurs
US20110293668A1 (en) * 2010-06-01 2011-12-01 Donald Conover Oral odor control method and product
CN105030579A (zh) * 2015-06-26 2015-11-11 江苏奇力康皮肤药业有限公司 一种芳香止吐漱口水及其制备方法
CN106727359A (zh) * 2017-02-08 2017-05-31 成都通德药业有限公司 一种提高叶绿素铜钠稳定性的制备方法

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EP0449782A1 (fr) * 1990-03-30 1991-10-02 Warner-Lambert Company Arôme encapsulé à caractère bioadhésif en comprimés à la menthe et confiserie
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WO1996003894A1 (fr) * 1994-08-05 1996-02-15 Fuisz Technologies Ltd. Produits alimentaires comprenant un systeme stabilise d'une composante tres aromatisante
EP0711547A1 (fr) * 1994-11-04 1996-05-15 Fuisz Technologies Ltd. Administration d'un système à libération contrÔlée avec matrice "shearform"
WO1998042316A1 (fr) * 1997-03-25 1998-10-01 R.P. Scherer Corporation Gelules comestibles a enrobages aromatises
WO1999008658A1 (fr) * 1997-08-20 1999-02-25 Fuisz Technologies Ltd. Unites de prise comestibles se dissolvant rapidement, formees dans des conditions de vitesse elevee/pression elevee
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US4814163A (en) * 1986-03-10 1989-03-21 Colgate-Palmolive Company Solid antitartar mouth deodorant
GB2233228A (en) * 1989-06-26 1991-01-09 Warner Lambert Co Taste-masked oral zinc compositions.
EP0449782A1 (fr) * 1990-03-30 1991-10-02 Warner-Lambert Company Arôme encapsulé à caractère bioadhésif en comprimés à la menthe et confiserie
WO1993008699A1 (fr) * 1991-11-04 1993-05-13 Fuisz Technologies Ltd. Systemes d'apport solubles dans l'eau pour liquides hydrophobes
WO1996003894A1 (fr) * 1994-08-05 1996-02-15 Fuisz Technologies Ltd. Produits alimentaires comprenant un systeme stabilise d'une composante tres aromatisante
EP0711547A1 (fr) * 1994-11-04 1996-05-15 Fuisz Technologies Ltd. Administration d'un système à libération contrÔlée avec matrice "shearform"
WO1998042316A1 (fr) * 1997-03-25 1998-10-01 R.P. Scherer Corporation Gelules comestibles a enrobages aromatises
WO1999008658A1 (fr) * 1997-08-20 1999-02-25 Fuisz Technologies Ltd. Unites de prise comestibles se dissolvant rapidement, formees dans des conditions de vitesse elevee/pression elevee
WO1999051211A1 (fr) * 1998-04-03 1999-10-14 Biovail Technologies Ltd. Formulations en sachet

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WO2002041862A1 (fr) * 2000-11-21 2002-05-30 Orix As Preparation pour hygiene bucco-dentaire contre l'halitose
WO2002058469A1 (fr) * 2001-01-23 2002-08-01 Van Beek, Ron Composes et compositions pesticides
US6844369B2 (en) 2001-01-23 2005-01-18 Van Beek Global, Llc Pesticidal compounds and compositions
RU2279219C2 (ru) * 2001-01-23 2006-07-10 Ван Бик Глобал, ЛЛС. Пестицидные композиции и способ борьбы с паразитами
US7208519B2 (en) 2001-01-23 2007-04-24 Van Beek Natural Science, Llc Pesticidal compounds and compositions
FR2821552A1 (fr) * 2001-03-01 2002-09-06 Cll Pharma Procede pour rendre hydrosoluble un principe actif naturellement peu ou pas soluble dans l'eau et ses utilisations
WO2002069931A1 (fr) * 2001-03-01 2002-09-12 Cll Pharma Procede pour rendre hydrosoluble un antiseptique naturellement peu ou pas soluble dans l'eau et ses utilisations
US7666685B2 (en) 2005-08-02 2010-02-23 Wm. Wrigley Jr. Company Screening method for identification of compounds suitable for treatment of oral cavity malodor associated with consumption of garlic
WO2007016644A1 (fr) * 2005-08-02 2007-02-08 Wm. Wrigley Jr. Company Procede de criblage pour l'identification de composes convenant au traitement des mauvaises odeurs de la cavite buccale associees a la consommation d'ail
AU2006275373B2 (en) * 2005-08-02 2010-06-03 Wm. Wrigley Jr. Company Screening method for identification of compounds suitable for treatment of oral cavity malodor associated with consumption of garlic
WO2008016855A1 (fr) * 2006-08-02 2008-02-07 Wm. Wrigley Jr. Company Compositions orales efficaces pour le traitement de la mauvaise haleine de la cavité buccale associée à la consommation de composés donnant une odeur
WO2009074320A1 (fr) * 2007-12-13 2009-06-18 Gudrun Pieper Procédé de suppression d'odeurs
EP2070528A1 (fr) * 2007-12-13 2009-06-17 Gudrun Pieper Procédé destiné à l'élimination d'odeurs
US20110293668A1 (en) * 2010-06-01 2011-12-01 Donald Conover Oral odor control method and product
CN102985053A (zh) * 2010-06-01 2013-03-20 百利-亚尔香芬公司 口腔异味控制方法和产品
EP2575740A4 (fr) * 2010-06-01 2015-09-30 Belle Aire Fragrances Inc Méthode et produit permettant de lutter contre les odeurs orales
US9408810B2 (en) 2010-06-01 2016-08-09 Belle-Aire Frangrances, Inc. Oral odor control method and product
CN107638312A (zh) * 2010-06-01 2018-01-30 百利-亚尔香芬公司 口腔异味控制方法和产品
CN105030579A (zh) * 2015-06-26 2015-11-11 江苏奇力康皮肤药业有限公司 一种芳香止吐漱口水及其制备方法
CN106727359A (zh) * 2017-02-08 2017-05-31 成都通德药业有限公司 一种提高叶绿素铜钠稳定性的制备方法

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