FI79784B - STABILY PLACKFOERHINDRANDE TANDVAORDSMEDEL MED GOD SKUMBILDNING OCH FLUORIDSTABILITET. - Google Patents

Description

79784

This invention relates to a plaque-preventing dental treatment comprising a quaternary active ingredient and 1.5 to 2% by weight of a betaine-type surfactant such as coconut amidopropyl betaine, lauramidopropyl betaine ., which increases foaming and does not inactivate the antibacterial activity of the quaternary compound. Nonionic surfactants do not provide enough foam, and ionic surfactants inactivate the antibacterial activity of the quaternary agent. Carbowax 600 (polyethylene glycol) and / or sorbitol replace propylene glycol and glycerin as a wetting agent to keep the betaine-containing mixture stable. Preferably, carboxymethylcellulose is also avoided, as large organic molecules deactivate the quaternary compound. Nonionic gums such as hydroxyethylcellulose are used as a gelling / thickening agent for dental gel.

More specifically, this mixture does not contain anionic or nonionic surfactants and contains only a minimal amount of glycerin, 1-10% as a fluoride stabilizer (when using a fluoride compound) and preferably 5-7% by weight in a mixture containing only polyethylene glycol as a wetting agent.

It has been found that the addition of a betaine-type surfactant to an anti-plaque pancreatic formulation based on quaternary active ingredients improves its foaming properties without deactivating the quaternary antimicrobial. It has further been found that wetting agents other than glycerin are required in the betaine system to affect cosmetic stability, in particular polyethylene glycol and / or sorbitol. It is also necessary to limit the use of a gelling agent / thickener to nonionic gums such as hydroxyethylcellulose.

The ability of quaternary ammonium compounds to prevent dental plaque formation is well documented. However, these compounds 79784 pose a problem when added to a dental conditioner such that conventional anionic surfactants such as sodium lauryl sulfate reduce their activity. Stable, clinically effective dental formulations have been made from quaternary ammonium compounds and non-ionic surfactants, but these foam very poorly and result in poor quality products. Mixtures of anti-plaque quaternary ammonium compounds and nonionic surfactants are disclosed in U.S. Patents 4,080,441, 4,110,429, 4,118,472, 4,118,473, 4,118,475, 4,118,476, and GB in 1,573,356.

U.S. Patent 4,161,518 discloses a dentifrice composition containing 0.05-1% by weight of quaternary ammonium organosiloxane as an active antibacterial agent in a suitable vehicle containing suitable polishes, fluoride compounds, anionic surfactants and flavoring agents to prevent plaque formation. , thickeners such as carboxymethylcellulose, wetting agents such as glycerin, sorbitol and other polyhydric alcohols.

U.S. Patent 3,988,435 discloses pharmaceutical compositions comprising a dentifrice. It contains a quaternary ammonium dihydrocycalcone glucoside that is both antibacterial and sweet, abrasives, surfactants, non-chemical agents and "derivatives of betaine-structured fatty amines", swelling, gelling and thickening agents, especially hydroxyalkylcellulose, -glycols, polypropylene glycols, etc., wetting agents such as sorbitol, mannitol, glycerin, propylene glycol, colorants and flavors.

All of the above patents merely list conventional, useful additives for dental care compositions.

The use of a betaine compound as the sole surfactant in the manufacture of a highly foaming dental care agent has not been reported. It has also not been shown or understood that it is necessary to limit the wetting agent to polyethylene glycol and / or sorbitol and the thickener to nonionic gums such as hydroxyethylcellulose in order to obtain a cosmetically stable dental care system from the betaine and quaternary system.

U.S. Patent 4,363,795 and the corresponding International Patent Publication WO 80/00057 disclose a dentifrice having a quaternary ammonium compound, an ampholytic surfactant which may be imidazoline or betaine, and an aminocarboxylic type sequestering agent having a synergistic effect on therapeutic agents. All examples are for cleaning solutions. No mention is made of dental gels or the use of wetting or thickening agents.

U.S. Patent 4,130,637 discloses a specific group of betaines, or a mixture of said betaine and a 9: 1 quaternary ammonium salt of the corresponding carboxylic acid. These act as decolorizing, antimicrobial and anti-plaque agents in a dental care medium containing the above-mentioned conventional wetting and gelling agents as well as a nonionic surfactant. This patent fails to disclose the need to use only a betaine-type surfactant, a specific nonionic gelling agent, hydroxyethylcellulose, and a specific wetting agent for polyethylene glycol and / or sorbitol to provide a stable, high-foaming and pliable .

U.S. Patents 4,117,107 and 4,117,108 also disclose a specific class of betaine compounds and their salts as plaque inhibitors in a dental care medium containing conventional wetting and gelling agents as well as anionic / nonionic surfactants. The use of an antibacterial quaternary ammonium compound, and not exclusively a betaine-type surfactant, has been reported. The specificity of the wetting and gelling agent and the exclusion of anionic / nonionic surfactants from the quaternary and betaine system, which is necessary to obtain a stable, high-foaming and anti-plaque dental care agent, have also not been recognized.

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However, none of the aforementioned prior publications discloses a cosmetically stable anti-plaque treatment agent with improved foamability and fluoride stability, which contains essentially a plaque-preventing cationic polyamene would be compatible with a cationic anti-plaque agent, and as a non-ionic gelling agent hydroxyethylcellulose, all in an aqueous medium with a tooth abrasive. There is also no prior disclosure of the use of a sorbitol wetting agent as a long-term fluoride stability enhancer or the use of small amounts of glycerin in a polyethylene glycol wetting agent that would also improve long-term fluoride stability.

It has been found that hair paste formulations containing anti-plaque quaternary ammonium compounds can be stabilized and foam better when conventional anionic and nonionic surfactants are replaced with betaine-type surfactants. The conventional wetting agent glycerin must be replaced by agents such as polyethylene glycol and sorbitol, which would give the product better cosmetic stability. However, a small amount of glycerol can be used to stabilize the fluoride-containing compound if polyethylene glycol alone is used as the wetting agent. As a gelling agent, nonionic gums such as hydroxyethylcellulose replace anionic carboxymethylcellulose, which also has the ability to deactivate a quaternary compound.

Thus, it is a main object of the present invention to provide a better foaming, anti-plaque dental care agent based on quaternary active ingredients using a flotation. as a zwitterionic betaine type surfactant.

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Another object of the present invention is to provide a cosmetically stable, foaming and anti-plaque dentifrice which contains polyethylene glycol and / or sorbitol as a wetting agent and which is compatible with betaine-type and quaternary active ingredients.

It is a further object of this invention to provide a stable, foaming and anti-plaque dentifrice containing nonionic gum, hydroxyethylcellulose as a gelling agent to stabilize the betaine quaternary system and to prevent the anionic sites of the carboxymethylcellulose molecules from deactivating the anionic sites.

It is also an object of the present invention to provide a cosmetically (physically) and chemically stable, foaming and anti-plaque dental care composition comprising a fluoride-forming compound and sorbitol or minimal amounts of glycerin (1-10% by weight) as a stabilizing agent without adversely affecting the cosmetic stability of the dental care product. -lisuuteen.

Additional objects, advantages and novel features of the invention will be set forth in part in the description which follows, and in part will become apparent to those skilled in the art upon examination of the following description or learning of the practice of the invention.

In order to achieve the above and other objects described and extensively described herein in accordance with the present invention, the novel, stable, foaming and anti-plaque dental care agent contains 0.01 to 5% by weight of an anti-plaque quaternary ammonium compound as essential ingredients, at least 1.5% by weight. - up to 2% by weight of a betaine-type surfactant, 20-30% by weight of a wetting agent selected from the group consisting of polyethylene glycol, sorbitol and mixtures thereof, 0.5-5% by weight of a nonionic gelling agent and fluoride in an aqueous medium containing a tooth abrasive.

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More particularly, this invention relates to a stable, anti-plaque dental care formulation having improved foamability and fluoride stability containing an effective amount of an antimicrobial quaternary ammonium compound, about 1.5-2% by weight betaine, about 20-30% by weight wetting agent, which is selected from the group consisting of polyethylene glycol, sorbitol, and mixtures thereof, about 0.5-2% hydroxyethylcellulose and about 0.05-2% by weight fluoride-producing compound, in an aqueous medium containing about 40-60% water-insoluble dentifrice . The sorbitol component, which stabilizes the betaine-quaternary system, also improves the long-term chemical fluoride stability of the dental care agent. A small amount of glycerin, up to 1%, can be used in a polyethylene glycol-containing wetting agent alone to improve long-term flucide stability without adversely affecting the cosmetic stability of the dental care agent.

Cationic antibacterial agents are well known in the art.

See, e.g., the section "Quaternary Ammonium and Related Compounds" in the article "Antiseptics and Disinfectants" in the Kirk-Othmer Encyclopedia of Chemical Technology, 2nd edition (Vol. 2, pages 632-635), here included as a reference.

Cationic agents with antibacterial activity (i.e., germicides) are used against bacteria and have been used against plaque formation by bacteria in the oral cavity.

The most common of these antibacterial anti-plaque quaternary ammonium compounds are benzethonium chloride, also known as Hyamiine 1622 or diisobutylphenoxyethoxyethyldimethylbenzylammonium chloride, and cetylpyridinium chloride. In the oral preparation, these materials are very effective in improving oral hygiene, reducing the formation of dental plaque and tartar, which usually results in a reduction in diseases of the tissues surrounding the tooth. Other cationic antibacterial agents of this type are mentioned, for example, in U.S. Patents 2,984,639, 3,325,402, 3,431,208 and 3,703,583, and in GB Patent 1,319,396.

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Other antibacterial and plaque quaternary compounds are those in which one or two of the quaternary nitrogen substituents have a carbon chain length (typically an alkyl group) of about 8-20, typically 10-18 carbon atoms, while the remaining substituents have a smaller number of carbon atoms (typically alkyl or benzyl group) such as 1 to 7 carbon atoms (typically methyl or ethyl groups). Dodecyltrimethylammonium bromide, benzyldimethylstearylammonium chloride, cetylpyridinium chloride and quaternized 5-amino-1,3-bis (2-ethylhexyl) -5-methylhexahydropyrimidine are typical antibacterial quaternary ammonium.

The dentifrice formulation of this invention contains an effective amount of an anti-plaque quaternary ammonium compound, preferably about 0.01-5% and more preferably 0.025-1% by weight of the mixture.

The ability of quaternary ammonium compounds to prevent the formation of dental plaque is well known. However, anionic surfactants such as sodium lauryl sulfate commonly used in dental care formulations reduce their activity. Replacing anionic surfactants with nonionics eliminates the problem of deactivation, but this results in poorly foaming products.

The incorporation of betaine-type surfactants into dental compositions based on anti-plaque quaternary active ingredients surprisingly improves the foamability of these compositions without reducing the activity of quaternary antibacterial agents.

The general formula of the betaine component of this dental care composition is: 8 79784? 2 R1-N + - R4 ~ COO ~ * 3 wherein R1 is an alkyl group of about 10-20 carbon atoms, preferably 12-16 carbon atoms, or an amido group:

0 H

M I

R-C-mCH, * £ 3 wherein R is an alkyl group of 10-20 carbon atoms and a is an integer from 1 to 3. R 2 and R 2 are each alkyl groups having 1 to 3, preferably 1 carbon atoms, R 2 is an alkylene or hydroxyalkylene group having 1 to 4 carbon atoms and optionally one hydroxyl group. Typical alkyldimethylbetaines include decyllibetaine or 2- (N-Decyl-N, N-dimethylammonio) acetate, coconut betaine or 2- (N-coconut-N, N-dimethylammonio) acetate, myristyl betaine, palmityl betaine, lauryl betaine, lauryl betaine, lauryl betaine .. Amidobetaines also include coconut amidoethyl betaine, coconut amidopropyl betaine, lauramidopropyl betaine, etc.

Betaines, which are zwitterionic materials, act as a blowing agent in dentifrice compositions containing quaternary substances. They act cationically over a wide pH range but do not reduce quaternary antimicrobial activity. This has been demonstrated in in vitro experiments with wool test pieces that simulate human skin and oral tissue and act as an absorbent material in the Red-80 stain test, cf.

J. Soc. Cosmet. Chem. _31 ^, 271-278 (Sept., Oct. 1 980).

Due to the same isoelectronic and isoionic points, wool has the same type of absorbent properties as oral tissue.

Using the Red-80 color test, the following test shows that a betaine-type surfactant does not inactivate a quaternary substance. The Red-80 stain test was performed with coconut amidepropyl betaine solution alone, with benzethonium chloride alone, and with a mixture of coconut amidopropyl betaine and benzethonium chloride. The degree of staining of the specimens was almost the same when treated with benzethonium chloride alone and a mixture of benzethonium chloride and a beta-compound, and both stained darker than the specimen treated with coconut amidopropyl betaine. This indicates that benzethonium chloride is a "stronger" cationic compound than betaine, i.e. it has a greater attraction to wool than betaine, indicating that the betaine compound does not deactivate Bent-cetonium chloride.

However, wool test pieces treated with a mixture of benzethonium chloride and an anionic surfactant, sodium lauryl sulfate, do not stain (do not retain red color), indicating that benzethonium chloride is completely inactivated by the anionic surfactant.

When the wool specimens were treated with a mixture of benzethonium chloride and a nonionic surfactant, polyoxyethylene sorbitan diisostearate (20 moles of ethylene oxide), the degree of staining was essentially the same as when treated with benzethonium chloride alone. This indicates that the nonionic surfactant does not deactivate benzethonium chloride.

In addition to the fact that betaine compounds do not interfere with quaternary activity, laboratory experiments have shown that formulations containing both quaternary compound and betaine foam 2-3 times better than formulations of nonionic / quaternary compounds. Mixtures of nonionic / quaternary compounds have a foaming index of about 20, while mixtures of betaine and quaternary compounds have a foaming index of about 40-60. In the foamability test used, place 1 g of the toothpaste to be tested in 10 ml of water (175PPM) in a cylinder with a scale of 32 ° C, shake for 15 s and read the height of the foam.

The zwitterionic betaine compounds are fully compatible with quaternary antimicrobial plaque inhibitors and impart cleaning and foaming-enhancing properties to a dental care composition containing quaternary compounds without deactivating its antimicrobial activity. The amount of betaine that effectively improves foamability can be varied from 1.5 to 2% by weight of the total formulation. Increased betaine levels adversely affect the taste of the dental conditioner.

All dental care products containing zwitterionic substances have cosmetic stability problems such as slow flavor leakage. The flavor exudes and does not dissolve in the zwitterionic surfactant.

Therefore, a specific class of wetting agent, including polyethylene glycol, sorbitol, and mixtures thereof, must be used to affect the cosmetic stability of the betaine system. Glycerin and propylene glycol alone do not provide enough cosmetic stability for betaine systems. The wetting agent system comprises about 20-30% by weight, preferably 20-25% of the material, and is selected from the group consisting of polyethylene: glycol, sorbitol, and mixtures thereof.

Another essential part of this dental care agent is a gelling agent which is a non-ionic gum and which is present up to 5% by weight, preferably 0.5-2%. It has been found that large organic molecules such as carboxymethylcellulose have the ability to inactivate quaternary antibacterial activity. Thus, hydroxyethylcellulose, which is a small nonionic organic molecule, provides a stable slimy gel in the betaine-quaternary system of the present invention and is thus the best gelling agent. Other gel excipients such as hydroxymethylcellulose and the like may be used.

It has been found that only by using a certain combination of betaine, a polyethylene glycol and / or sorbitol wetting agent and a nonionic gelling agent can a stable anti-plaque dental care agent with improved foaming and based on quaternary antibacterial compounds be obtained.

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The characteristic fluoride-producing compounds that are the preferred additives for this dental care product are that they are capable of releasing fluoride ions in water and do not substantially react with other dental care product compounds. These materials include inorganic fluoride salts such as soluble alkali metal, alkaline earth metal and heavy metal salts, e.g. sodium fluoride, potassium fluoride, ammonium fluoride, lead fluoride, copper fluoride such as cuprofluoride, zinc fluoride, tin fluoride, stannous fluoride, stannous fluoride or stannous fluoride such as stannous fluoride. ammonium fluorosilicate, sodium fluorozirconate, sodium monofluorophosphate, aluminum mono- and difluorophosphate and fluorinated sodium calcium pyrophosphate. Alkali metal and tin fluorides such as sodium and stannofluorides, sodium monofluorophosphate and mixtures thereof are preferred.

The amount of fluoride-forming substance depends to some extent on the type of substance, its solubility and the dentifrice, but it must be non-toxic. In a solid oral preparation such as a toothpaste or gel, an amount that does not release more than 1% by weight of the preparation is considered satisfactory. Any minimum amount of such a compound can be used, but it is recommended to use enough of the compound to release 0.005-1%, preferably about 0.1% fluoride ions. In the case of alkali metal fluorides and stannofluorides, this component is typically present up to 2% by weight, based on the weight of the preparation, and preferably in the range of 0.05-1%. In the case of sodium monofluorophosphate, the compound may be present up to 7.6% by weight, more typically 0.76%.

It has further been found that the long-term chemical stability of fluoride in a sorbitol-based wetting agent or surfactant system with polyethylene glycol and at least 5% sorbitol is significantly improved compared to a polyethylene glycol-based wetting agent in which its fluoride stability is marginal but acceptable. However, small amounts of glycerin, about 1-10% and preferably 79784 1-10% by weight in the polyethylene glycol-based wetting agent significantly improved long-term fluoride stability without adversely affecting the cosmetic stability of the dental care formulation in question. The glycerin component involved herein functions and is used as a chemical stabilizer for the fluoride moiety only when polyethylene glycol is used as the sole wetting agent.

Based on the results of a three-week aging test at 49 ° C, 5% glycerin improves fluoride stability by 25% without adversely affecting cosmetic stability. The mechanistic reason why a small amount of glycerin improves fluoride stability is unclear. Fluoride stability data after 12 weeks at 38 ° C further confirm that the use of small amounts of glycerin in a dental conditioner provides a significant improvement. Table I clearly shows improved fluoride stability in the polyethylene glycol wetting agent system.

Table I Soluble fluoride

Glycerin: 3 weeks 6 weeks 9 weeks 12 weeks

Polyethylene is oo glycol at the beginning 38 c 38 c 38 c 38 c 0:20 0.093 0.077 0.068 0.063 0.057 1:19 0.088 0.081 0.074 0.066 0.066 3:17 0.093 0.082 0.074 0.069 0.067 5:15 0.093 0.081 0.077 0.071 0.070 10:10 0.094 0.086 0.083 0.080 0.077

It has also been found that increasing the glycerin content leads to a decrease in pH, see Table II.

Table II

Glycerin: pH

polyethylene- 9 weeks

glycol 49 C

0:20 9.8 1:19 9.7 3:17 9.4 5:15 9.4 10:10 8.9 13 79784 The dentifrice of the present invention, which is a toothpaste or gel, contains conventional water-insoluble polishing agents. and abrasives up to about 20-75%, preferably in amounts of about 40-60% by weight of the total manufacturing formula. Suitable examples of the teeth grinding and polishing materials include sodium metaphosphate, potassium metaphosphate, tricalcium phosphate, dihydrated calcium phosphate, anhydrous dicalcium phosphate, calcium pyrophosphate, magnesium, trimagnesiumfosfaatti, calcium carbonate, carbonate, alumina, hydrated alumina, alumi-niumsilikaatti, zirconium silicate, silica, bentonite and mixtures thereof.

The dentifrice of this invention may also contain conventional additives such as colorants and bleaches, preservatives, flavors and sweeteners, and ammonia materials such as monoammonium glycyrrhizinate. These additives may each be added to the dentifrice in small amounts up to 5% by weight, provided that they do not interfere with the foamability, stability and anti-plaque properties of the finished product.

The dentifrice of the present invention is prepared by the methods of conventional toothpastes and / or gels. More specifically, toothpaste can be prepared by forming a gel from hydroxyethylcellulose and water, adding to it by mixing powder materials, e.g. a fluoride compound and a wetting agent, further adding to it a mixing polish, then betaine and a sweetener, and sealing the final mixture in tubes.

In accordance with the oral hygiene practice of this invention, the dentifrice is applied evenly over the enamel by brushing the teeth for 30-90 s at least once a day.

The following examples further illustrate the nature of the present invention, but it is to be understood that the invention is not limited thereto. Mixtures are prepared in the usual manner and all amounts and ratios referred to herein and in the appended claims are given by weight 14,79784 unless otherwise indicated. Example 1

Ingredients%

Hydroxyethylcellulose 1.0

Carbowax 600 ^ 20.0

Na-saccharin 0.2 MFP2 0.76 CAB3 (35% A.I.) 3.5

Dicalcium phosphate 49.0 BZCl 4 0.5 D.I. H 2 O 24.04 flavor 1, 0

Polyethylene glycol 2 sodium monofluorophosphate Cocosamidopropyl betaine 4 benzethonium chloride

Hydroxyethylcellulose and water are premixed for 10 minutes to form a gel. Powdered materials MFP, BZCl and saccharin as well as Carbowax wetting agent are added to the gel and mixed for 10-20 minutes. The gelled mixture is added to the dicalcium phosphate and stirred for 20 minutes at 8 ross. The resulting cosmetically pleasing tooth gel is sealed in a tube.

Aging tests for this product were performed in labeled tubes at room temperature, 4 ° C and 38 ° C for 9 weeks, and not in labeled tubes at 49 ° C for 9 weeks and show excellent cosmetic stability.

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Example 2

Ingredients%

Hydroxyethylcellulose 1.1

Carbowax 600 20.0

Na-saccharin 0.2 MFP 0.76 CAB (35% A.I.) 5.7 dicalcium phosphate 46.8 BZCL 0.5 H 2 O 24.04 flavor 1.0 This dental gel was prepared according to the method of Example 1. This product has a pH of 6.7 and a foaming height of 55, but does not taste good.

Example 3

Ingredients%

Hi Sweet Peppermint 1.0 (sweet peppermint) MAG1 0.1 BZCl 0.5 MFP 0.76

Na-saccharin 0.2 H 2 O 23.44

Peg 6002 20.0

Natrosol ^ 1.0 dicalcium phosphate 49.0 CAB (30% Al) 4.0 ^ monoammonium glycyrrhizinate 2 polyethylene glycol, molecular weight 600 hydroxyethylcellulose 3 16 79784 This dental gel is prepared according to the method of Example 1 except that the pH is adjusted to 8.5 with dilute NaOH: for hydration after addition of polyethylene glycol to the gelled premix.

The resulting gel looks good, has a foaming height of 38-40 and has excellent stability in aging tests over 12 weeks at 38 ° C and in labeled tubes at 60 ° for 3 weeks.

Example 4

Example 3 is repeated except that glycerin replaces polyethylene glycol as a wetting agent. This product gives a foaming height of 46, but shows the separation of the marks after 3 days at 60 ° C and the wettability and separation in the neck of the tube after 3 weeks at 49 ° C. This product is cosmetically unstable.

Example 5

Ingredients% H 2 O 21.14

Natrosol 1.3 propylene glycol 20.0

Na-saccharin 0.2 BZCl 0.5 MAG 0.1 MFP 0.76 dicalcium phosphate 50.0 CAB (30% Al) 5.0 Flavor 1.0 This dental gel is prepared according to the method of Example 1 except that the propylene glycol wetting agent is mixed with a premixed with the gel for only 10 minutes. The resulting product looks good and foams to a height of 44. However, it is clearly unstable due to separation, wetting of the edge and bleeding of the skin within 3 weeks at -13 ° C and at 4 ° C slight yellowing within 3 weeks at 43 ° C: and 49 ° C.

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Example 6

Ingredients% H 2 O 19.68

Natrosol 1 f 1

Carbowax 600 20.0

Na-saccharin 0.2 BZCl 0.5 MAG 0.1 MFP 0.76 dicalcium phosphate 50.0 CAB (30% A.I.) 6.66 flavor 1.0 This dental gel was prepared according to the method of Example 1.

The resulting product is a bit thick but has good foamability and stability.

Example 7

Ingredients% H 2 O 21.34

Natrosol 1, 1

Carbowax 600 20.0

Na-saccharin 0.2 BZCl 0.5 MAG 0.1 MFP 0.76

Ca 2 P 2 O 71 50.0 CAB (30% A.I.) 5.0 Flavor 1.0 ^ Calcium Pyrophosphate 18 79784 This dental gel was prepared according to the method of Example 1.

The resulting gel is thick and granular, which may be due to the roughness of the tooth abrasive, calcium pyrophosphate.

Example 8

Ingredients% H 2 O 17.68

Natrosol 1, 1

Carbowax 600 20.0

Na-saccharin 0.2 BZCl 0.5 MAG 0.1 MFP 0.76 dicalcium phosphate dihydrate 42.0 anhydrous dicalcium phosphate 10.0 CAB (30% A.I.) 6.66 flavor 1, 0

Example 9

Ingredients%

Carbowax 600 20.0

Natrosol 1.1

Na-saccharin 0.2 MAG 0.1 BZCl 0.5 H 2 O 17.68 MFP ° '76 hydrated alumina 42.0 calcined alumina 10.0 6 66 coconut amidopropyl betaine (30% A.I.) ',. 1 f0 flavor pH 8.3

II

This product is completely stable after 9 weeks of aging at room temperature, 4 ° C, 38 ° C and 49 ° C.

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Examples 10 and 11

Ingredients Example 10 Example 11 __% _% _ PEG 600 20.0 20.0

Natrosol 1.1 1.3

Na-saccharin 0.3 0.3 hydrated alumina 42.0 42.0 calcined alumina 10.0 10.0 CAB (30% Al) 5.0 5.0 MFP 0.76 0.76 flavor 1.0 l, 0 H20 DI 19.27 18.64 BZCl 0.5 0.5

Red 40 (1% solution) 0.07 0.07

Example 12

Ingredients% __ _

Sorbitol 70% 28.0

Natrosol 1, 1

Na-saccharin 0.3 BZCl 0.5 MFP 0.76 alumina 42.0 calcined alumina 10.0 CAB (30% A.I.) 5.0 flavor 1.0 H 2 O 11.34

Initial pH 7.4 3 weeks pH 7.5 6 weeks pH 7.6 This product is completely stable at -13 ° C and 4 ° C for 9 weeks but slightly wets the stopper at 43 ° C and 49 ° C after 3-9 weeks. In addition to good physical stability, the content of the active ingredient (ionic fluoride and benzethonium chloride) in this product remains stable, as indicated by the constant pH.

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Example 13

Ingredients% H 2 O 21.14

Natrosol 1, 3 sorbitol 20.0

Na-saccharin 0.2 BZCl 0.5 MAG 0.1 MFP 0.76 dicalcium phosphate dihydrate 50.0 CAB (30% A.I.) 5.0 flavor 1, 0

The resulting gel has a foaming viscosity of 42 and no taste

Q

no release of the substance has occurred after 9 weeks at 49 ° C.

This product is completely stable at -13 ° C and 4 ° C for a period of 9 weeks, but has wet marks on the cap after 3-9 weeks at 43 ° C and 49 ° C.

Example 14

Ingredients%

Natrosol 1.1

Na-saccharin 0.3 BZCl 0.5 MFP 0.76

Carbowax 600 10.0 Sorbitol (70%) 10.0 H 2 O Deionized 19.34 Hydrated Alumina 10.0 Calcined Alumina 42.0 Flavor ** '® CAB (30% A.I.) 5.0 Li

Example 15

Ingredients% 21,79784

Natrosol 1.1

Na-saccharin 0.3 MFP 0.76 BZCl 0.5

Carbowax 600 15.0 Sorbitol (70%) 5.0 H 2 O 19.34 Hydrated alumina 42, Calcined alumina 10.00 Flavor 1, 0 CAB (30% Al) 5.0 With this product containing 5% sorbitol, soluble fluoride the recovery in 12 weeks is 84% compared to 61% (acceptable level) with a wetting system containing polyethylene glycol alone under the same conditions, cf. Examples 1 and 11. This shows that the presence of sorbitol in amounts as low as 5% (70% A.I.) gives excellent fluoride stability.

Examples 16-20

Ingredients eg 16 eg 17 eg 18 eg 19 eg 20%%%%%

Polyethylene glycol 15 17 19 10 20 (Carbovax 600) glycerin 5 3 1 10 0 hydroxyethylcellulose 1.10 1.10 1.10 1.10 1.10 sodium monofluorophosphate 0.76 0.76 0 .76 0.76 0.76

Na-saccharin 0.30 0.30 0.30 0.30 0.30 benzethonium chloride 0.50 0.50 0.50 0.50 0.50 Hydrated alumina 42 42 42 42 42 Calcined alumina 10 10 10 10 10 22 79784

Ingredients e.g. 16 e.g. 17 e.g. 18 e.g. 19 e.g. 20%%%%% CAB (30% Al) 5 5 5 5 5 flavor 11 11 1 water 19.34 19.34 19.34 19.34 19 , 34

Fl concentration '*' 0.07 0.07 0.07 0.07 0.07

Chemical stability of the above assemblies after accelerated aging at 12 ° for 12 weeks, determined as a percentage of the F1 content.

All of the above guidelines are effective against plaque-related bacteria and at the same time have better foamability as well as cosmetic and chemical stability. The presence of a small amount of glycerin, up to 1% by weight, increases the chemical stability of fluoride in a dentifrice containing polyethylene glycol as a wetting agent beyond the inherently acceptable fluoride stability achieved in the absence of glycerin.

The above compositions can be modified. Thus, the coconut amidopropyl betaine used in the examples can be replaced by other betaines such as lauramidopropyl betaine, coconut betaine, etc. Similarly, the specific abrasives of the examples can be replaced by other abrasives.

Similarly, the sodium monofluorophosphate used in the specified examples may be replaced by other fluoride-containing compounds such as sodium fluoride, potassium fluoride, etc.

Claims (15)

23 79784 Stable anti-plaque toothpaste with good foamability and fluoride stability, characterized in that it contains, as essential ingredients, 0.01 to 5% by weight of anti-plaque quaternary ammonium compounds, at least 1.5% by weight to 2% by weight up to betaine-type surfactant, 20-30% by weight of a wetting agent selected from the group consisting of polyethylene glycol, sorbitol and mixtures thereof, 0.5-5% by weight of a nonionic gelling agent and a fluoride-producing compound, in an aqueous vehicle with a tooth abrasive. Toothpaste according to claim 1, characterized in that the nonionic gelling agent is hydroxyethylcellulose present in an amount of about 0.5 to 2% by weight. Toothpaste according to Claim 2, characterized in that it contains about 20 to 30% by weight of polyethylene glycol having a molecular weight of 600. Toothpaste according to Claim 2, characterized in that it contains about 20 to 30% by weight of sorbitol. Toothpaste according to Claim 1, characterized in that it contains about 40 to 60% by weight of a water-insoluble tooth abrasive. Toothpaste according to Claim 5, characterized in that the tooth abrasive is dicalcium phosphate. Toothpaste according to claim 2, characterized in that the anti-plaque agent is benzethonium chloride present in an amount of about 0.01 to 5% by weight. 24 7 9 7 3 4 Toothpaste according to claim 1, characterized in that the fluoride-producing substance constitutes about 0.05 to 2% by weight of the toothpaste. Toothpaste according to Claim 8, characterized in that the fluoride-producing substance is monofluorophosphate. Toothpaste according to Claim 8, characterized in that the humectant is a mixture of about 20 to 30% by weight of polyethylene glycol and at least 5% of sorbitol. Toothpaste according to Claim 8, characterized in that it also contains 1 to 10% by weight of glycerol as a fluoride stabilizer in a wetting agent which is polyethylene glycol. Toothpaste according to Claim 1, characterized in that the betaine compound is coconut amidopropyl libetin. Toothpaste according to Claim 1, characterized in that it does not contain nonionic or arionic surfactants. Toothpaste according to Claim 5, characterized in that the abrasive is alumina. Toothpaste according to Claim 14, characterized in that the abrasive is a mixture of hydrated alumina and calcined alumina. 25 7 9 7 8 4