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
  • A61Q11/02—Preparations for deodorising, bleaching or disinfecting dentures
• • 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
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives 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
  • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
  • A61K8/66—Enzymes
• • 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
  • A61K2800/51—Chelating agents

Definitions

• This invention relates to denture • cleanser compositions and more particularly to an improved water-soluble denture cleanser composition containing enzymatic and chelating cleansing agents.
• Dentures may be cleansed either by immersion in a cleansing solution or by brushing with a cleansing agent in the manner of natural teeth.
• the former method is generally preferred, partly for convenience but primarily since brushing tends to mar the smooth surfaces of plastic dentures.
• Cleansing solutions may be made from preformed liquid solutions but for storage convenience are usually in solid form in which case the cleansing solution is prepared at the time of use by dissolving the solid form in tap water.
• the solid form cleanser may be in the form of loose powder or granules or may be in the form of tablets.
• denture cleanser tablets usually also contain one or more active oxygen compounds such as sodium perborate monohydrate, potassium peroxydisulfate, potassium monopersulfate, sodium carbonate peroxide, potassium peroxydiphosphate, diperisophthalic acid, monoperphthalic acid and the like, which cause the tablets to evolve micro-bubbles of active or nascent oxygen as they are dissolved in water and provide an oxidizing cleansing action including a bleaching effect on the denture stains.
• active oxygen compounds such as sodium perborate monohydrate, potassium peroxydisulfate, potassium monopersulfate, sodium carbonate peroxide, potassium peroxydiphosphate, diperisophthalic acid, monoperphthalic acid and the like, which cause the tablets to evolve micro-bubbles of active or nascent oxygen as they are dissolved in water and provide an oxidizing cleansing action including a bleaching effect on the denture stains.
• active oxygen compounds such as sodium perborate monohydrate, potassium peroxydisulfate, potassium mono
• denture cleanser tablets usually also contain various other relatively inactive ingredients such as fillers, extenders, binders, indicators or dyes, flavors and the like.
• Lubricant systems such as magnesium stearate or talc, to facilitate smooth and even flow of the dry granular materials of the formulations during tableting operations may also be added.
• Improvement in denture cleansers has been primarily carried out by manipulating the oxidizing system, e.g., perborate and persulfate, and pH in order to achieve improved food stain removal.
• Hypochlorite generating formulations are well known to achieve a high level of plaque removal and moderate level of food stain removal, but it is known that they are harmful to denture metals and generate an odor unacceptable to the consumer.
• Denture plaque is a complex glycoprotein which is believed responsible, in part, for denture odor. It is this substance which forms on the surface of the dentures initially. Upon its disintegration, there remains a residue composed of 5 hydroxyapetite and other components which contain calcium. It is this residue which hardens to form calculus which continues to obtain new layers of plaque if not removed. This layering sequence also aids in stain retention by preferential stain adsorption.
• 4,155,868 discloses a single layer tablet in which an enzyme, active oxygen compounds and an effervescence producing composition are allegedly incorporated in such a manner that they are retained in a stable form until the tablet is ready for use.
• the patentee states that by careful control of the particle sizes and the surface treatments of selective components, the enzyme is not detrimentally inactivated during storage.
• the patentee further states that they provide added stability while in the dry tablet, the enzyme may be granulated or coated.
• compositions of this invention overcome the prior art deficiencies by utilizing an effective amount of chelating agent along with an effective amount of enzyme to synergistically remove calculus/plaque deposits within a short period of time.
• compositions of the present invention provide for the addition of a bleaching component, which does not react with halides to produce an enzyme deactivating composition such as a hypohalide, to an effective amount of a chelating agent along with an effective amount of enzyme to synergistically remove calculus/plaque deposits within a short period of time.
• a bleaching component which does not react with halides to produce an enzyme deactivating composition such as a hypohalide
• an enzyme deactivating composition such as a hypohalide
• a water soluble denture cleanser composition may be prepared which comprises:
• a water soluble denture cleanser composition may be prepared which comprises:
• a water soluble denture cleanser composition which comprises:
• the invention also contemplates a method for cleansing dentures which method comprises placing the water-soluble denture cleanser composition and denture to be cleaned in an amount of water sufficient to dissolve the composition and to completely cover the denture for a sufficient time to effect the desired cleaning. Cleaning times of up to about 15 minutes and even up to about 5 minutes have been found suitable to clean dentures with the formulations of this invention even though such times are not considered essential to the invention.
• a water-soluble denture composition comprising two essential components, a proteolytic enzyme and a sequestering agent.
• This formulation functions in cleansing the denture by removal of surface plaque by the enzyme and concurrent degradation of proteinaceous material along with the chelating effect to remove calcium and calculus deposits achieved by the sequestrant.
• the effervescence-producing and bleaching materials of the preferred composition aid in removing stains and debris from the object being cleaned as it is being reacted upon by the other components.
• the composition once prepared may be used as a powdered formulation or compressed into tablet form or other suitable format which is effective upon dissolution in water to remove denture plaque, calculus and food stains.
• the enzyme is incorporated in the compositions of the present invention in a granular encapsulated form.
• the denture cleanser compositions of the present invention may be in single layered or ulti-layered tablet form.
• the enzyme component of the denture composition herein is a proteolytic enzyme and most preferably a neutral or alkaline proteolytic enzyme which is capable of acting on food, food degradation products, mucin and plaque.
• the proteolytic enzyme is preferably employed in a granulated, encapsulated form.
• the enzymes may be of plant, animal or microbial origin and even synthetically produced. Many are available commercially under various tradenames which are useable in this invention.
• the enzyme particle size is not critical for the compositions of this invention but are preferably able to pass through a 10 to 20 mesh sieve (U.S. standard screen) when the composition is to be tabletted.
• the enzymes should be active within a pH range of about 7.0 to 12.0 and preferably 7 to 10.5.
• the proteolytic enzyme, used in the present invention can be of vegetable, animal or microorganism origin. Preferably it is of the latter origin, which includes yeasts, fungi, molds and bacteria. Particularly preferred are bacterial subtilisin type proteases, obtained from e.g. particular strains of B. subtilis and B. licheniformis. Examples of suitable commercially available proteases are Alcalase, Savinase, Esperase, all of NOVO Industri A/S; Maxatase and Maxacal of Gist-Brocades; Kuzusase of Showa Denko; BPN and BPN' proteases and so on.
• the activity of the proteolytic enzyme included in the composition typically ranges from about 0.1-150 AU/g or its equivalent. Naturally, mixtures of different proteolytic enzymes may be used. There are standard measures of enzyme activity such as the Anson Unit (AU) and the Novo Protease Unit (NPU) and the Glycine Unit (GU) . These measurers of activity are well known and defined as follows:
• Anson Unit the amount of enzyme* which digests hemoglobin at an initial rate such that there is liberated per minute an amount of TCA-soluble product which gives the same color with phenol reagent as one milliequivalent of tyrosine
• 1 Novo Protease Unit the amount of enzyme* which hydrolyzes casein at such a rate that the initial rate of formation of peptides/minute corresponds to 1 micromole of glycine/minute
• a GU is a glycine unit, which is the amount of proteolytic enzyme which under standard incubation conditions produces an amount of terminal NH memo-groups equivalent to 1 microgramme/ml of glycine.
• the enzymes When utilized in the denture cleanser composition of this invention the enzymes should be used in amounts of about 0.5% to about 15% by weight of the total formulation and preferably 1% to about 7% by weight. Amounts below these amounts are not effective in removing sufficient plaque to be economical whereas higher amounts do not achieve any added benefit other than speed of cleaning. Typically, the enzymes useful in the present invention will have an activity of about about 2AU or its equivalent when expressed in other units.
• the chelating or sequestering agents useful in the present invention are to be used in amounts of about 8% up to about 99.9% by weight of the total composition.
• Sequestering agents useful in the present invention are carboxylic acid derivatives and phosphonic acid and its derivatives.
• carboxylic acid derivatives useful as chelating or sequestering agents include the hydroxycarboxylic acids and salts thereof, as well as amino carboxylates.
• the hydroxycarboxylic acid compounds include gluconic acid and citric acid, among others known in the art.
• the amino carboxylates include nitriloacetic acid, ethylenediaminetetraacetic acid (EDTA) and isoserine diacetate and their salts.
• EDTA ethylenediaminetetraacetic acid
• phosphonic acid derivatives are the salts of ethane-1- hydroxy-1, 1-diphosphonic acid.
• aminotriomethylene phosphonic acid aminotriomethylene phosphonic acid
• 1-hydroxyethylidene- 1, 1-diphosphonic acid ethylenediamine tetra(methylene phosphonic acid)
• ethylenediaminetetra(methylene phosphonic acid) ethylenediaminetetra(methylene phosphonic acid)
• hexamethylenediaminetetra(methylene-phosphonic acid) diethylene triamine penta(methylene-phosphonic acid), among others.
• the alkali metal salts and analoges of the above phosphonates are also useful. Mixtures of any or all of the chelating or sequestering agents is also contemplated.
• the preferred chelating or sequestering agent used in this invention is EDTA, most preferred is the tetra sodium salt of ethylenediamine tetraacetic acid, dihydrate.
• Another preferred sequestering agent is isoserine diacetate trisodium salt.
• This component is essential for use in the denture cleanser compositions of this invention and is employed in an amount of about 8% up to about 99.5% by weight of the total composition. A preferred amount is about 15% to about 80% and a most preferred amount is 15 to 50% by weight of the total composition.
• the sequestering agent is believed to function in the inventive compositions by reacting with the calcium present in the calculus rendering the underlying proteinous material susceptible to attack by the proteolytic enzyme.
• the enzyme in turn attacks plaque thereby exposing more calculus to attack by the sequestering agent.
• This combination reaction results in the synergistic removal of the plaque and calculus along with adsorbed stain beyond that which can be achieved by using these materials separately.
• Bleaching or active oxygen components useful in the present invention are those which do not inactivate proteolytic enzymes directly and which do not interact with halides to produce an enzyme deactivating composition.
• suitable bleaching components include alkali metal and alkaline earth metal perborates and percarbonates. Perborates are the preferred bleaching component and sodium perborate monohydrate is the most preferred.
• the bleaching component when utilized in the denture cleanser composition is present in amounts up to about 55% preferably from about 12% to about 55% and most preferably from about 25% to about 55% by weight of the total denture cleanser composition.
• the term "bleaching component” shall include those compounds known in the art as "active oxygen” compounds. These compounds reduce stain and remove calculus and plaque.
• the effervescence-producing composition may be selected from a wide range of materials which aid in cleaning the denture surfaces by causing the active components to be rapidly dissolved.
• the effervescence-producing composition may be comprised of an acid selected from the group consisting of citric acid, tartaric acid, gluconic acid and malic acid and an alkali metal carbonate selected from ' the group consisting of sodium bicarbonate, potassium bicarbonate, sodium carbonate and potassium carbonate.
• an acid selected from the group consisting of citric acid, tartaric acid, gluconic acid and malic acid and an alkali metal carbonate selected from ' the group consisting of sodium bicarbonate, potassium bicarbonate, sodium carbonate and potassium carbonate.
• the effervescence-producing composition may be anhydrous sodium perborate.
• This particular component is the preferred effervescence-producing composition when the enzyme employed has a higher pH activity range, namely an alkaline proteolytic enzyme. This material exhibits a pH value around 9.5 to 10.5 when employed in the compositions of this invention.
• the effervescence-producing composition should be employed in amounts up to about 75% by weight of the total composition and preferably in amounts of about 15% to about 25% by weight. Amounts above 75% do not enable sufficient active components to be present to remove adequate levels of plaque and calculus whereas levels below about 15% do not adequately disperse the components in solution.
• the bleaching agent is sodium perborate monohydrate and the effervescence-producing agent is anhydrous sodium perborate.
• the weight ratio of sodium perborate monohydrate and anhydrous sodium perborate in a preferred embodiment is from about 5:3 to about 3:5.
• the present compositions may contain a variety of additional ingredients selected on the basis of desired end use.
• the compositions may include detergent compounds, such as organic and inorganic detergents, including non-ionic detergents such as the various polyoxyethylene esters of aromatic and alaphatic alcohols, as well as the polyoxyethylene esters of hydrophobic propylene oxide polymers. These compounds assist in maintaining a foaming action, in the instance where the cleansing compositions are placed in aqueous solution.
• compositions may contain other adjuvant materials, that may be inorganic or organic in structure.
• adjuvant materials such as alkali and alkaline earth metal carbonates, hydroxides, and mixtures may be added.
• the present compositions may optionally contain additional sequestrants for the purpose of maintaining solution clarity, in the instance where the compositions are placed in solution.
• additional sequestrants may also assist in the inhibition of corrosion and tarnish of articles soaked in solution containing the present compositions.
• Useful ' sequestrants include polyfunctional organic acids, such as citric acid, maleic acid and their corresponding salts.
• flavorings may include varieties of mint, oil of • clove, artificial vanilla flavoring and others. These materials may be included and blended in various combinations within the scope of the present invention. The choice of the required amounts is likewise within the skill of the art.
• colorants useful herein are those known as F.D.& C. & D.& C. dyes and lakes. These materials are certified by the Federal Food and Drug Administration as acceptable for use in food, drug and cosmetic applications, and drug and cosmetic colorings.
• the materials acceptable for the foregoing spectrum of use are preferably water-soluble, and include indigoid dye, known as F.D.& C. Blue No. 2, or its Lake which is the disodium salt of 5,5-indigo-tindisulfonic acid.
• the dye known as F.D.& C. Green No. comprises a triphenylmethane dye or F.D. & c. Green #3 and is the monosodiu salt of 4-[4-N-ethyl- p-sulfobenzylami o)diphenylmethylene]-[1-(N-ethyl-N-p- sulfoniumbenzyl)2,5-cyclohexadienimine] or F.D.
• the foregoing colorants may be blended with each other in a variety of combinations. It is particularly desirable that the colorants be chosen so that the composition when initially dissolved will present a deep hue. This is important in the instance where the composition serves as a denture cleanser, as the fading phenonmenon embodied in denture cleansers can be more easily observed by the end user.
• F.D. & C. Blue #1 Lake is particularly important in that the tablet color is blue without adversely affecting the color of the solution.
• inventive • denture cleanser compositions of the present invention include a peroxygen or active oxygen component.
• These materials are compounds which form hydrogen peroxide or active oxygen when placed in solution.
• Typical active oxygen compounds include sodium perborate monohydrate and tetrahydrate, potassium monopersulfate, sodium carbonate peroxide, diperisophthalic acid, monoperphthalic acid, potassium peroxydiphosphate, sodium aluminum amino- hydroperoxide and the like.
• the peroxygen or active oxygen component is preferably employed in a granular form and in an amount of from about 10 to about 40% weight, preferably from about 15 to about 25% based on the total composition.
• a further feature of the invention comprises the preparation of a compacted granulated mixture containing the anhydrous perborate salt in combination with a monohydrate perborate salt and optional addition of a polymeric fluorocarbon.
• Such mixtures are recited in Reissue Patent 32,771 and 4,405,486 which is incorporated herein by reference.
• such formulations comprise a combination of anhydrous perborate and monohydrate perborate in the amount of about 50% to about 70% by weight of the total cleansing compositions, wherein the combination includes at least 20% by weight of the total cleansing composition of anhydrous perborate, said combination having a portion present in a compacted, granulated mixture with up to about 0.70% by weight of said combination of a polymeric fluorocarbon.
• compositions and tablets described herein are superior in efficacy to the prior art in removal of stains, plaque and calculus.
• the efficacy of these compositions is of course a function of time, temperature and water volume used and as such comparisons must be based on an amount of cleansing per a specific set of values for these factors.
• the effervescent, denture cleanser compositions prepared as described are employed to clean dentures by placing them in water with the denture to be cleaned for a time sufficient to effect the desired cleaning.
• the tablets When the cleanser is in tablet form, the tablets may be from about 2 to about 3.2 grams in total weight, and are usually employed with warm water, preferably about 120ml initially about 40 to about 50°C in an amount sufficient to completely cover the denture. Tablet weight is not critical. When so employed, effective and desired cleaning may be achieved in about 5 to about 15 minutes but in more highly stained dentures, longer periods may be desirable.
• the tablets when thus employed are found to effectively remove mucin, plaque, calculus, and stains which are not as readily removed by tablets not containing enzymes and sequesterants utilized herein. Moreover, this is accomplished without brushing and usually without the overnight soaking necessary with the generally available tablets.
• compositions of the invention are prepared by mixing the components together until a homogenous mixture is obtained.
• the composition may then be stored or compressed into tablets.
• the optional ingredients Prior to packaging or compression, the optional ingredients may be added and blended to obtain a uniform mixture.
• the components Prior to packaging or compression, the components may be dried prior to blending so that they are substantially moisture free. Drying procedures are well known in the art and do not constitute a novel aspect of this invention.
• Example A represents a preferred composition of the instant invention.
• Example I represents the prior art composition whereby the amount of EDTA is low (3.83%), it contains no enzymes and the solution pH is 8.4.
• Example II represents a typical composition of the prior art using enzymes in a potassium monopersulfate formula.
• Example III represents the prior art whereby the amount of EDTA is high (39.2%), it contains no enzymes and the solution pH is 10.3.
• Example IV represents the use of only one enzyme (Milezyme APUG-330) in solution.
• Example A which represents the composition of the instant invention contains a large amount of the chelating agent, ethylene diamine tetraacetic acid tetra sodium salt dihydrate (EDTA), and an effective amount of Enzyme (Milezyme APUG-330) at a pH of 10.3 and contains an equivalent amount of titratable oxygen initially to the prior art levels in I, II, and III.
• EDTA ethylene diamine tetraacetic acid tetra sodium salt dihydrate
• Milezyme APUG-330 an effective amount of Enzyme
• Example A The preferred composition of the instant invention Example A was prepared according to the Reissue Patent #32,771 as follows. Initially, a quantity of anhydrous sodium perborate, in the form of a fluffy powder, tetra sodium EDTA dihydrate and sodium perborate monohydrate was combined in a container with a quantity of polytetrafluorothylene powder identified as Grade F5A by Allied Chemical Corp. The polytetrafluoroethylene was added in the amounts based upon the weight of the perborate, as indicated with respect to each of the examples. Blending was performed for about 3 minutes, after which the mixture was predried for 1 hour at 90°C. The dried materials which represent almost 94% of the formula were added to the other excipients and the enzyme.
• Example III the prior art composition was also not heat cured.
• Reissue Patent #32,771 is incorporated herein by re erence. Cleaning Process
• the denture (food stained plaque/calculus matrix) tiles were immersed in 125 ml. of water at 45°C, and one of the compositions indicated in Table I were added. At the end of 15 minutes, the tiles were dunked in a 200ml volume of tap water 20 times the water replaced with a fresh 200ml volume and the dunking process repeated another 20 times and allowed to air dry at (20°C) room temperature. The tiles were visually inspected. The extent of the calculus and plaque removal was further determined both by a reflectance method and the SEM method.
• Tables II and III represent the analysis of the tiles to determine the percent plaque/tartar removal using the (SEM) Scaning Electron Microscope method and the
• Table II represents the percent Ca, P, O, N, and Ti remaining on the surface of the plaque/tartar coated tiles after treatment with the test compositions I, II, III, A and IV. Both the virgin tiles and the untreated tartar/plaque coated tiles were also examined to determine the baseline. As evidenced, as the Ca, P and 0 increases the higher the calculus coating on the surface of the tile. In Table II, the results of using composition A as the plaque/tartar tiles gives the lowest Ca, P and O values indicating that (A is the most efficient in removing the surface coating of tartar/plaque.
• the Reflectance Method determines the plaque/tartar remaining on the surface after treatment with the test compositions I, II, III, A and IV. Again the use of composition A gives the highest % plaque/tartar removal.
• the amount used for the cleaning test all had the equivalent of 100 mg of Enzyme (alcalase)/Treatment. * The detergent is athanol LAL Powder which contains 30% NaCl TABLE II
• Examples A represents the preferred composition of the instant invention which contains both the EDTA (a chelating agent) and the said enzyme (Milezyme APUG-330) and III represents a composition without an enzyme.
• the objective is to demonstrate that 0 the Example A synergistically removes plague from tiles which have very little calculus accumulations as evidenced by an SCM analysis. See Table V where the calcium level is only 0.03.
• the stability of the preferred composition A is further evidenced when tablets are subjected to aging at room temperature and accelerated aging by maintaining the temperature at 45°C for 4 months. At the end of this period, the tablets were tested for % plaque removal to determine the stability of the enzymes. The 4 month aged tablets were compared to freshly prepared tablets and the results on Table IV indicate an equal amount of plaque removal. In addition thereto, Table IV results indicate that when the tablets are dissolved, the preferred composition (Example A) continues to remove plaque, that is, 61.9% after 30 minutes of soaking and 74.3% plaque removal after 16 hours of soaking. The comparative formulation (Example III) does not remove more plaque with increased soaking time and stops cleaning after removing around 25% plaque * in about 15 minutes.

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• 1991
  • 1991-11-01 JP JP50185292A patent/JPH05503947A/ja active Pending
  • 1991-11-01 CA CA 2075287 patent/CA2075287A1/en not_active Abandoned
  • 1991-11-01 WO PCT/US1991/008107 patent/WO1992010165A1/en not_active Application Discontinuation
  • 1991-11-01 EP EP19920900958 patent/EP0514520A1/de not_active Withdrawn

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