JPS59108717A - Antigingivitic oral product - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

[Detailed description of the invention]

BACKGROUND OF THE INVENTION The present invention provides an effective gingivitis inhibitor, 1-imidazoyl-1
-(p-chlorophenoxy)5-5-dimethyl 2-butanone (Crimhasol by Bayer). Hot-containing eye rinses or toothpastes can be applied topically to the cavity to promote oral cavity irritation and plaque buildup. The present invention relates to a composition for gingivitis and a gingivitis inhibitor. Periodontitis, or alveolar pyrorrhea, is caused by the tooth retaining tissues, including the gums7.
It is a disease that destroys the structure that connects the alveolus in which the tooth resides, as well as the bone surrounding the tooth. The disease may initially be associated with constant irritation from plaque9, food impact, slow tooth healing, traumatic bites, or chemical irritants.
It's ugly. Gums contain plaque, i.e. minerals and bacteria found in u9
Be severely harmed by the combination. Bacteria associated with dental plaque can stimulate the secretion of enzymes and endotoxins that can cause inflammatory gingivitis. As the gums become increasingly irritated by this process, they begin to bleed.
0 It does not lose its strength and elasticity, it separates from the tooth and leaves periodontal pockets. In it, there is dental residue secretion, more bacteria and A element, and more accumulators. It is also possible to store it in the diet (in the pocket of the human body), thereby providing nutritional conditions for increased idle growth and production of endotoxins and destructive enzymes. . In this process “formed”
Bacteria are commonly found to be present during the active phase of periodontitis. Such microorganisms are commonly present and found in membranous excreta as well as related tissues, and they (and lymph) are involved in the entire system through venous blood flow. Pyorrhoea
'l, to the meat (2 machina! Machining, inflammation t↑, 5 strain, and 1 first lo, 'Unaro. Therefore, effective suppression of gingivitis and direct weight σ)C's periodontal It is an essential element of flame prevention IL. It suppresses oral diseases such as dental plaque, cavities, and bad breath, as well as periodontitis such as gingivitis and alveolar leakage. A number of substances have traditionally been advocated for 21.
Nothing left Tekko completely satisfied. For example, swelling associated with gingivitis due to the accumulation of tartar formation and/or inhibition of oral calculus. Oral compositions containing anti-inflammatory agents that reduce bleeding and signs of inflammation are disclosed in U.S. Pat. No. 3,497,591:
Dichloro-2-guazininobenzimidazole disclosed in U.S. Pat. No. 6,523,154: U.S. Pat.
Carrageenan as disclosed in U.S. Pat. No. 4,272,512; tranexamic acid and folic acid as disclosed in U.S. Pat. U.S. Pat. No. 3,577,520 is also based on correcting the disorder of paradontotis. In the treatment of alveolar pyorrhea, U.S. Pat. 5.5'-diaryl-
2,4 ~ 411 toothpastes run by imidazolidine dione are open to the public. U.S. Pat. No. 3,911,155 discloses an antibacterial silicate gel that is effective against both Gram-positive and Gram-negative bacteria (7).

[7, Bis (Imitarso 1 Noum West Grade 1 story) Imidazole derivative physical strength, 1J father, tartar formation prevention 11P) or gingivitis prevention [Eσ] method and 17 years old 1- cleaning fluid, toothpaste, and dental gel σ〕1
Useful at t1. US J1￥d No. 4,246,670 is +11! Filamentous fungi, 1 inch of yeast. Mold, hiphase funji
i) Against i6 and gram 14 cocci (7 strong/, C
Antibacterial and antibacterial agents, toothpaste and mouthwash Jlf
It is useful as an additive to oral hygiene products such as 4-liquid σ) to prevent infections caused by mucous membranes σ], and it is useful as a pre-disease agent for infections. It has been disclosed that some Durum-negative microorganisms such as Bacteroides asa, C. There is a strong relationship between periodontitis and the presence of gingivitis in the gingivitis tissue. Effective inhibition of periodontitis can be achieved by removing the periodontitis from the body. Therefore, by removing the periodontitis from the body, periodontitis can be effectively inhibited.
ont. RC3, Ueno 65-75 (1979), metronidazole. (See I CH (JH 1'') was shown to cause the removal of the above-mentioned Durham-negative anaerobic bacteria from dental plaque, even if given systemically. ,(
'、1inical Perindnntology
6.197-209 (1979), as demonstrated in
Therein, metronidazole has been shown to be effective in reducing dental plaque and gingivitis scars in dogs, and by Lacier et al. in J. of C11nical P.
eriodontology. 8.29-44 (1981), in which it was demonstrated that metronidazole was effective in reducing the number of anaerobic B, Azatsuka A IJ tics in plaque removed from periodontal pockets, and associated It is considered as a decrease in pocket depth] 1.1 ℃ 1 cure) Force/resistance σ) 10
It has been shown that this happens in one field.し／＋）L、
Flagyl (1!”l agy l) σ) Trade name and publisher Otdeiro Metronidazole is carcinogenic and C yen +
ysic, 1an11, efference l1and
Book 176i1) cannot be used for sick and undifferentiated man 1]. Now here, another derivative of imidazole grabs the above,
It has been discovered that it is effective against negative anaerobic microorganisms, is non-mutagenic, non-carcinogenic, and can be applied locally into cavities for the treatment of gingivitis. . fi-, σ), i.e. 1-imidazoyl-1
-(090lofenyl)5-5-cymefl2-7-tanone. Imidazoylketones such as 1-imidazoyl-1-(4-chlorophenoxy)-ro,ro-dimethyl-2-butanone σ) are listed in US Pat. No. 5.817.142-'4
:T6 and 5.9Uro, 287th v Kodite, practice'
)Qtl, 'y'/Iz, rimIJ-m. Pharmaceutical composition containing aqueous T・9 and non-aqueous suspension w [Seni 1
6 and are disclosed as useful antifungal agents. disease 1
Its action against Durham-positive and -negative bacteria, such as Streptococcus t7+-protozoa, Staphylococcus aureus and Escherichia coli σ), is also described here. English 1 H] Patent No. 1,502,
No. 144 Sai6 and its equivalent German Patent No. 2,450,0
No. 59 is an imidazoyl ketone antifungal agent dispersed in a dermatologically acceptable carrier containing a detergent active compound.
meet Pityrosporum obei/L/ (Pi tyrosp
Discloses hair, hair and skin treatment compositions that are effective against hair, hair and skin. These compositions may be in cream, aerosol, powder and liquid form)
Ru. German Patent No. 2.60 [], 800, in dry form: b. Alternatively, plaster paint 1 can be applied either as a dispersion in water, as a water-in-oil or oil-in-water emulsion, or as a spray.
Disperse dye, wallpaper, tile surface 2 paint, v, bitumina, urine 3, leather. Clean shower curtains, textiles, carpets, wood and paper from a long list of pathogenic fungi, molds and Ii+III fungi (
protection against 1-imidazoyl-1-(1-imidazoyl-1-(
410 rophenoxy), 5. ro-dimethyl 2-butanone is disclosed. 1 to 1, Batateroides a. Regarding the anaerobic Gram I microorganisms by line, (iq V) is not mentioned. German Patent No. 2.700,
No. 806 is a mixture of an imidazo ylketone fungicide and an ammonium fungicide useful for protecting materials such as paints, glues, bianimens, cellulose, paper, textiles, leather, and paper. Missing disclosure and C color. Traditional technology has been developed to specifically treat imidazoyl ketones as antifungal agents, especially for hair and skin.
1i' for use in dental formulations or their effectiveness against certain Durham-negative anaerobic organisms associated with gingivitis and periodontitis. There is no disclosure of J. Description of the invention Water-insoluble imidazoyl ketone, 1-(mitazoyl-1-
(p-rialophenoxy)ro-ro-dimethyl-2-butanone, is selectively effective against certain anaerobic gram-negative microorganisms associated with gingivitis when applied topically to diseased gums. Actually, it was discovered here and now. It is therefore a principal object of the present invention to provide an oral formulation containing the water-insoluble imidazoyl ketone described above as a gingivitis inhibitor solubilized in an oral vehicle. One object of the present invention is to provide a daily rinse or toothpaste that is effective in controlling and treating dental plaque, gingivitis and periodontitis. Yet another object of the present invention is to provide a gingival composition comprising the above-described gingivitis inhibitor solubilized in an aqueous vehicle comprising a nonionic compound. Another object of the present invention is to provide oral compositions containing antimicrobial agents that are useful in the prevention and treatment of gingivitis in animals. Yet another object of the present invention is to provide a method for improving oral cavity hygiene by topically applying to the oral cavity an antibacterial agent-containing composition comprising the aforementioned o1-solubilized imidazoyl ketone. Other objects of the present invention, (1 [points, and
The following will be apparent to those skilled in the art upon consideration or will be understood by practice of the present invention. The objects and advantages of the invention may be realized and obtained by means of the instrumentalities and combinations particularly pointed out in the appended claims. To achieve these and other objects in accordance with the present invention as embodied and broadly described herein, the present invention provides an oral vehicle; 1. Hydrophobic group of sufficient length to dissolve, Yt 10% to 80
% of polyoxyethylene hydrophilic (1')
The ratio between hydrophobic group and parent, water group is 8:10)%. Anti-gingivitis, which is solubilized in non-ionic compounds such as 1-imidazo(tu-1-(p-chlorophenoxy)ro-rosimethyl-butanone), an effective water-insoluble gingivitis inhibitor. σ) For oral use I] It is related to the composition. More specifically, the present invention provides hydrophobic groups containing 1 to 20 carbon 7-containing fatty acid groups, polyoxypropylene, hexitane mono-multiplex fatty acid esters, and fatty acid amides: and a parent aqueous group polyoxyethylene of sufficient length to effect solubilization; about 0.1 to 5 parts by weight of the above solubilized in an aqueous oral vehicle consisting of a non-ionic compound including; The present invention relates to an oral composition comprising a gingivitis inhibitor. Oral vehicles may be liquids such as mouthwashes or rinses, solids such as chewing cams, or reams such as tooth powders, toothpastes or dental creams. These oral compositions are non-toxic and have a p 1i of about 5 to 5. Mouthwashes with about 5 to 7.5 OpH are hydroalcoholic vehicles containing block polymers of ethylene oxide, mixed polymers of propylene oxide and ethylene oxide, 10-80 E-oles of ethylene oxide per mole. Polyoxyethylene, hexitane mono-quaternary fatty acid tn ester, and fatty acid mono- and diethanolamide esters, mixtures thereof, are selected from nonionic surfactants. Contains approximately 1-5% of market weight. Typical surfactants contain at least 11 J-80% hydrophilic units of polyoxyethylene to hydrophobic groups such as polyoxypropylene. The preferred ratio of hydrophilic groups to one hydrolyzable group is ε3:1 and about 3250 θ molecules, as in the case of brobylene oxide, ethylene oxide, and sigma polymers. The ratio of n1 bathing agent to imidazoyl compound is about 1:1 to 25=1;
Preferably about 5=1 to 25:1. At ratios exceeding 25:1. Gelation occurs. Toothpaste is also about 5-Z5 l)t]Y<
') with a dentally acceptable polish: water and approx.
400 commercial quantities of a nonionic humectant, including at least one humectant selected from the group consisting of polyethylene glycol and polypropylene glycol; glycerin, sorbitol or mannitol. Suppression of gingivitis in L? ill may be solubilized and placed in a part of the moisturizing agent. The gingivitis agent 10 used in the present invention has the structural formula: 1-imidazoyl-(p-chlorophenoxy)3
-6-dimethyl 2-butanone, which is incorporated by reference in U.S. Pat.
, 903,287. 1-Bromo-1-(4-chlorophenoxy)-,'S,
It is made by reacting 3-dimethyl-2-butanone with 7.1 imidazole, dissolved in acetonitrile. This imidazoyl ketone has a melting point of 94.5-
K) is a water-insoluble crystalline powder at 97.8°C and can be obtained manually as Climbazole from Bayer. Since this imidazole compound is water immobile, it must first be solubilized in a non-ionic compound prior to separation of the ionic substance in an aqueous medium. It's ugly. This antibacterial compound, when added to oral vehicles, is highly effective against certain anaerobic microorganisms associated with periodontitis.
．． Not only is it effective, but it also reduces the number of bacteria associated with periodontitis when applied once or twice. It was discovered that Walker et al.'s method (Antimicrnb
ial and Chcmoth''erapy, Vol. 16a, pp. 452-457, 1979) Ilzttt Measurement 1.-T. Ichino!l (MIC) is "J') 7C Z8 is also between 61.2 micrograms. 13. The MIC of one gingivalis is 25 micrograms/rue. 13. IViI C for G. gracilis and other spindle-shaped bacteria
For each / - 5U greater than 9 Nigerum positive imitators, M I of Actinomyces viscosus NichiC.
Ci direct is 125 for aerobic methods and 250 for anaerobic methods. This is utilized herein as a gingivitis inhibitor! 2 clearly demonstrates the selectivity of the antibacterial activity of the positive imidazole compounds. Evaluation of an oral composition against gingivitis using a mouth rinse containing 0.5% climbazolone in a 10-week study on 50 Pegle dogs clearly demonstrated its immediate effectiveness against gingivitis. It shows. The method used involves completely removing hard and soft dental deposits and then keeping the dog on a soft diet for 6 weeks to allow gingivitis to develop. The dentition is then dipped in the test solution on both sides of the mouth. Treat for approximately 15 seconds twice a day, 5 days a week. These animals are examined and the degree of gingival inflammation is recorded according to a scale of 0 to 5. 0 - No inflammation. 1- Mild local edema and redness around the gums; bleeding does not occur with gentle finger pressure. 2- Moderate edema and redness around the gums with bleeding during gentle acupressure. 5 = Severe edema and perigingival margins and sticking
ed) Gingival ulcers, and bleeding even with gentle finger pressure. Gaseous rinses and 0.5% metronidazole rinses were carefully used as control standards for Gesei and 1E. The data are shown in Table 1. Summary 1. Gas, Vy 4-4-Grilling liquid 958 filtration 8-
-56931 - -52872--ru 11 initial gingival u old ts gas i
) Medication, both metronidazole and clinobazol rinses reduced the gingivitis i.p.
The expression of ``ingival units'' was significantly decreased. , /Is +, , less amount (Q,
5%) Crimunoxol is more effective against gingivitis! It shows the same efficacy as metronidazole (0.5%). However, as per the well-documented prior art, metronidazole, while effective against certain Durum-negative microorganisms associated with periodontitis when used systemically, does not work well when applied topically. The cause of this poor result is due to the absence of suitable hydrophobic groups in its structural formula, which are necessary for penetration into the gingival tissue. (p-chlorophenoxy)ro-3-dimethyl-2-butanone, which provides good penetration into the tissues where the destructive process of periodontitis is occurring and is associated with this disease. This allows the antimicrobial agent to maintain effective concentrations without reducing the bacterial population of Durham-negative anaerobic microorganisms.Furthermore, metronidazole is mutagenic in all of its nitro groups; Crimsol is non-inducible in mutagenesis tests because it does not have a nitro group as shown by the following structural formula. The oral composition of the present invention can be used as a mouthwash or eye rinse The vehicle may be a liquid (such as a liquid). In such formulations, the vehicle is typically a water-alcohol 71:1 mixture. Generally, the water to alcohol ratio is about 1 by weight. =
1 to about 20:1. Preferably it is in the range of 5:1 to 20:1. The alcohol content is approximately 20-4% of the vehicle.
It is preferable to configure a zero-tier system. The total density of the water-alcohol mixture in this type of formulation typically ranges from about 70 to about 98 parts by weight of the formulation. The p l-1 of such liquid and other formulations of the invention generally ranges from about 5 to about 7'5. The key ingredient of the liquid oral preparation is about 1-5% of hydrophobic polyoxypropylene or a non-ionic surfactant containing 10-80% polyoxyethylene units 2 to higher fatty acids, fatty acid esters or fatty acid amides. The amount is %. The preferred percentage ratio of hydrophilic to hydrophobic groups is 8:1 for water-insoluble climbazol solubilized in a dehydrating alcohol vehicle. Suitable nonionic surfactants are block polymers of ethylene oxide, mixed polymers of propylene oxide-ethylene oxide,
-20 carbon atoms and preferably 4-100 per mole &
-110-80 moles of ethylene oxide and polyoxyethylene hexitane mono-higher fatty acid ester. Preferably. Hexitane is sorbitane, and mannitane and other hexitanes are also often useful, and higher fatty acyls have 10-16 or 20 carbon atoms,
Preferably there are 12-16 or 18, with about 12 being most preferred and the number of ethoxides being 15.
- 80 pieces, often preferably about 20 pieces (
- Yes. Particularly preferred is the product sold under the trade name Tween 20, also known as polyoxyethylene (20) sorbitan monolaurate [polysorbate 20]. Products that are also useful are sold under the same name, such as Tween 40, 60, 65 and 80. Alternatively, polyoxyethylene sorbitan is a nonionic surfactant that is oleoyl and has a mole of 1 mole of ethylene sorbitan. Monolaurates are usually preferred. Polyoxyethylene (80) sorbitan monolaurate may be used in place of polysorbate (20) above. Other suitable nonionic surfactants are cocomonoethanolamide, Cocojetanolamide. Mono- and di-mono- and di-codyl fatty acids having about 10-18 carbon atoms in the acyl group, such as lauryl myristyljetanolamide, lauryl monoethanolamide, combinations of cocojetanolamide, etc. Contains ethanolamide. Honsahemei's Oral Use 41' Parabolic Toothpaste Puco may be burnut-like in character, such as a dental cream. Such a paste Vehicles for oral preparations include polishing agents. Examples of youthful agents are water-insoluble sodium metaphosphate, potassium metaphosphate, tricalcium phosphate, calcium pyrophosphate, magnesium orthophosphate, trimagnesium phosphate, calcium carbonate, alumina. , alumina, aluminum silicates. Zirconium silicate, silica, bentonite, crystalline silica with particle size up to 5 microns, silica gel, complex amorphous alkali metal aluminosilicates. Dicalcium phosphate, and mixtures thereof. When using gelke that is transparent to the naked eye, colloidal silica such as thyroid 72 and thyroid 74 and 1-
Those sold under the trade name Santocel, such as 7.1 Mo or Zantocel 100, and alkali metal aluminosilicate composites, sold under the trade name Thyroid, are! Useful for samurai. This is because they have a refractive index close to that of the gelling agent-liquid (water and/or gel-containing moisturizer) used in tube 7+l'l in toothpaste. Polishing agents are generally present in oral formulations at concentrations ranging from about 10 to 99 degrees. Preferably. In men's toothpaste, about 10% to about 75% of the teeth are present vertically. In toothpastes, the liquid vehicle typically consists of 1 part water and a humectant, ranging from about 10 parts to about 90 parts part of the formulation.Essentials of toothpastes and dental creams. The ingredients are solubilized in a water-insoluble climbazole-dehydrated Vt vehicle, with the addition of a non-ionic humectant containing at least one humectant selected from the group consisting of polyethylene glycol and polypropylene glycol. 40%. Glycerin, sorbitol, or mannitol can be added to at least 1 portion of the imidazole compound as long as it is solubilized in the oxyethylene or polyoxypropylene glycol.
It may be directly replaced with a portion of the moisture-retaining cutting material containing 0-80%, preferably 80:10%, of polyoxyethylene groups or polypropylene groups. Natural rubber is synthetic rubber and rubber-like substances are typically red algae, sodium carboxymethylcellulose, methylcellulose, hydroxyethylcellulose, gum tragacanth, polyvinylpyrrolidone, starch, and hydroxylpropylmethylcellulose. The gelling agent is usually used in an amount of about 1 weight, preferably about 0.
．． It exists in the range of 5 parts to about 5 parts. In a toothpaste or gel, the liquid and solid have a ratio of 7 J [1] to form a creamy or gel-like mass extruded from a container or from a collapsible, e.g., aluminum or lead tube. The oral compositions of the present invention generally include a concentrated IW, non-soap, water-soluble, synthetic organic anionic or nonionic surfactant in the range of about 1-5% by weight to provide wetting, May promote cleansing and foaming properties. U.S. Patent No. 4.041
, 149 contains suitable anionic surfactants of this kind in column 4, lines 1-68, and suitable nonionic surfactants of this kind in column 8, lines 50-68 and column 9, lines 1-12. Each section of the Activator Disclosure (~deori. Kosai II-) is cited in this book. The antibacterial agent-containing oral composition of the present invention includes inorganic fluoride salts such as soluble alkali metal salts, alkaline earth metal salts, and heavy metal salts: for example, fluorinated salts, potassium fluoride, ammonium fluoride, Calcium fluoride, cuprous fluoride 5
copper fluoride, zinc fluoride, stannic fluoride, stannous chlorofluoride, barium fluoride, sodium silifluoride, ammonium silicofluoride, fluorozirconate sodium,
Sodium monofluorophosphate, mono- and difluorophosphate
Aluminum uno-, 'J6 Yo Hihi r+ Phosphate fluoride sodium uno calcilyl: may optionally contain a fluorine-donating compound. Sodium fluoride and stannous fluoride. Alkali metal and tin fluorides such as sodium monofluorophosphate and mixtures thereof are preferred. The amount of fluorine-providing compounds varies depending on the type of compound,
Depending on its solubility and the type of oral formulation, it should be in a non-toxic amount. In solid oral preparations such as toothpaste and chewing gum, the sensitivity of this divine compound, which releases up to about 1% of the formulation, is considered satisfactory. Any suitable minimum solution of this type of compound may be used, but approximately 0.005%
It is preferred to use an amount sufficient to release fluoride ions from 1% to 1%, preferably about 1%. Typically, in the case of alkali metal fluorides and stannous fluoride, this component will be up to about double vertical, based on the weight of the formulation. Preferably, it is present at a concentration ranging from about 0.05 cl to 1 part. In the case of sodium monofluorophosphate, this compound contains up to 16 Lyh, more typically about 0.76 Lyh
May exist in the ridges. Various other substances which do not impair the properties of the composition, such as sweeteners (e.g. saccharin, sucrose, lactose, maltose, sorbitol, etc.), flavorings, oils (e.g. orchid root, sucrose, koji, sassafras, etc.);
Clove, sage, eucalyptus, majorana. cinnamon, lemon, orange, suet oil), colorants or whitening agents (e.g. titanium dioxide). Preservatives (eg, benzoic acid), etc. may be incorporated into the oral formulations of the present invention. By overlapping these substances, up to a total of about 5%, preferably l, < is 0, [] 1 part 1 % J] Slightly broken χ Added to this oral composition 7JI1
1. It's okay. The f-[1] composition for the cavity of the present invention can be easily prepared by a pure f4J mixing method from chain components that can be easily obtained by hand. L = (7) The imidazoyl compound typically contains water [1] It is important to first mix it with the nonionic component before adding it to the vehicle. For example, 1" rinse solution or The mouthwash may be made by first solubilizing the imidazole compound by emulsifying it in a nonionic surfactant before adding it to an aqueous (aqueous to alcoholic) vehicle. Other chain components such as additives, sweeteners, etc. may be added to the aqueous vehicle either before or after the solubilized imidazole is added to the aqueous vehicle. Good. Toothpaste should be non-ionic in nature, since imidazole is soluble in it, and 5) moisturizers and imidazole compounds should not be used.
, @L, then carboxymethylcellulose
(addition of thickener) may be made by adding thickening agent, water, and other ingredients in JD and JX. The order of addition of each keyaki ingredient is. As long as the imidazole compound is first solubilized in the nonionic humectant before addition to the water component.
You can change it. In the practice of the invention, 1-imidazoyl-1-(p
- Chlorophenoxy) 5-Rhodimethyl 2-butanone Gingival moxibustion inhibitor The oral composition according to the present invention is a mouthwash or toothpaste containing ash effective for promoting kerosene hygiene. [Regularly applied to tooth enamel] 2 times a day, preferably about 1 to about 5 times a day, about 5 to 6 times a day, about 7 times a day. Apply at a pH of 5. DETAILED DESCRIPTION OF THE INVENTION The following specific examples further illustrate the nature of the invention. The present invention is not limited thereto. The scope of the claims and all the terms and percentages mentioned here! Unless otherwise specified, it depends on the number of vehicles. Example 1 -r Serul = 25 Limvazole 2 05% Flavored Agent (K-91-586
3) = [ko22*)n, o = tsuk1
' l Q13 = 3.0 glycerin
:25 Sodium saccharin -0.03% water
Set it to 100%. * HAS t”ry also available from Iondot Co., Ltd. Molecule fJ!: 5250. Block polymer of 8=1% of polyoxyethylene and polyoxypropylene. Up to glycerin, flavoring agents and sodium sukka'
7JO is added to the hydroalcoholic vehicle containing J7'Y before γ loading. The products are effective in the control of gingivitis and the treatment of periodontitis and provide a simple means of improving oral health when used in a regular application regimen of one to several times per day per oral cavity. The unexpectedly excellent anti-gingivitis activity of this product is shown in Table 1, in which Example 10 was used as a rinse solution or test solution. The product also has antibacterial properties against Bacteroides azaccarolyticus and B. gingivalis. H, U ro1.3
156.5 Sodium benzoate 0.5
2.5Na-Saccharin 0.2
1.0 Bo! JEchit/7ri! J:ff-#600'
25.0 125 Climbazole
1.0 5. tJ carboxymethyl cellulose 1.5 7.5+Iloit-
24423,015,0 Zeo-49335,0175 Sodium lauryl sulfate 15 Z
5 Seasoning is agent i, o
5.1)]: H(su(II2C■12), (
Jtl, n is the number of V of 10-14, preferably 1
2.5 to 14 k). It has 2 molecular lengths of 570-650. 2: Colloidal silica 3: Sodium aluminosilicate (silica with 1% bound alumina) (from Huber). Climbazole is premixed with polyethylene glycol prior to the addition of carboxymethyl cellulose to form a gel. Stir the thyroid into this gel for 17 min. Add Zeo, Lauryl Itt, m-sodium, flavoring agent, water, benzoate, and →J-tucarin. The benzoic acid salt and saccharin may be dissolved in water before mixing with the remaining ingredients. Similarly, the gel, flavoring agent, and lauryl alcohol may be premixed prior to addition to the gel. This product also has good antibacterial and anti-gingivitis properties. Other conventional ingredients may be substituted or added as described above. For example, water-containing alumina or water-insoluble metaphosphates or dicalcium phosphates may be substituted in whole or in part by other rejuvenating agents such as gelkyl metal aluminum/silicates (Zeo) or colloidal silica (Syloid). Similarly, other nonionic surfactants may be substituted for block polymers of ethylene oxide (Pluronics), such as polyoxyethylene hexitane mono-shangwei fatty acid esters. It is understood that the foregoing detailed description is given for illustrative purposes only and that various modifications may be made without departing from the spirit of the invention. Patent Applicant: Colgate Vermolive Company
- 7 Way Kroger Lane, New Chassis, USA

Claims (1)

[Scope of Claims] 1.] The cavity vehicle, the nonionic compound, and the gingivitis inhibitor are in a heavy ratio of 1 to 25:1. Solubilized in nonionic compounds. Effective number of water-insoluble gingivitis inhibitor 1-imidazoyl-1-(p-chlorophenyl) 5-,! , -dimethyl 2-7-1 nont: 1] Cavity composition for the treatment of gingivitis and periodontitis. 2. The above-mentioned gingivitis inhibitor of about 0.1-5% has a hydrophobic group length of about 1%, which is long enough to cause solubilization.
An aqueous compound consisting of a nonionic compound containing 0-80% polyoxyethylene hydrophilic units with a solubility ratio n in a cavity vehicle. % The oral composition according to claim 1. 6. The water-insoluble gingivitis inhibitor is solubilized in a non-ionic compound containing a mixture of hydrophilic and hydrophobic groups of sufficient length to effect solubilization in an aqueous vehicle; The weight ratio of hydrophobic group to hydrophilic group in the ionic compound is F,
+8:1. An oral composition according to claim 1. 4. pH is about 5 to 15; K. ethylene oxide block polymer, mixed polymer of propylene oxide and ethylene oxide. Polyoxyethylene hexitane mono-higher fatty acid esters containing 10-80 moles of ethylene oxite per mole and N fatty acid mono- and di-ethanolamides and mixtures thereof. The mouthwash has a hydroalcoholic vehicle containing about 1 to 5 nonionic surfactants selected from the group consisting of: The oral composition according to claim 5. 5. pH of about 5-15; containing a dentally acceptable polishing agent and at least one humectant selected from the group consisting of water and polyethylene glycol and polypropylene glycol; a toothpaste. A masticatory proboscis according to claim 1. 6. Glycerin, sorbitol or mannitol, -F, as long as the gingivitis inhibitor is solubilized. 1 line πI that may be replaced with a part of the moisturizing agent-containing 1 rat: described in item 5 of the i+i+1 box σ) For oral cavity use 1↑compound I. Z. 1. A method for improving oral hygiene, which comprises applying the silk composition for oral cavity according to claim 1 locally to oral cavity every day. 8. To the diseased gums 1- as set forth in claim 4
]-1 Consists of daily application of rinsing liquid. Gingivitis treatment method. ? , [sigma] described in claim 5] consists of washing the mountain every day with toothpaste. Gingivitis inhibitor method. 10. The oral composition according to claim 2 is applied topically to the cavity. A method for reducing the number of harmful anaerobic Durum-negative microorganisms found in periodontal pockets in diseased gingival areas.