BE730888A - - Google Patents

Description

  

   <Desc / Clms Page number 1>
 
 EMI1.1
 rxDI & "IV iF rG" 3IG: Orally applicable compositions for delaying the formation of caries and dental stones, and methods for the preparation and use of such compositions.

 <Desc / Clms Page number 2>

 The present invention relates to compositions for
 EMI2.1
 Oral or buccal cables (hereinafter sisaleaent referred to as "oral compositions"), comprising certain ssinophosphates or fluorine-ire-phosphate combinations, as well as processes for their preparation and use. More particularly,

   the present invention relates to oral compositions comprising
 EMI2.2
 an ammonium salt of a de-condensation product of annsoniac and phosphorus pentoxide which renders the composition more effective for hygiene and anticarious and anti-limescale therapy. The ex-
 EMI2.3
 'pressure' oral compositions' - as used in the present description should be understood as designating products which are not intentionally ingested during ordinary use or administration, but are used in the oral cavity in such a way that practically all of the dental surfaces are in contact with them.

     By - il - such products include, for example, toothpastes, toothpaste or mouthwash, solutions to be administered locally (or topically), and prophylactic pastes. In addition to said salts, such oral compositions also include a "vehicle or
 EMI2.4
 suitable support for use in cavity b, iccal ", a term to be understood as meaning non-toxic substances (such as cleaning or polishing agents, foaming or soap-like agents, humectants and the like) hereinafter specified as constituents of toothpastes and prophylactics), as well as water and other liquids serving as vehicles in toothpaste, mouthwash, and topically administered solutions.



   It has hitherto been proposed to combine a fluoride
 EMI2.5
 ; 1 1. mineral phosphate, soluble in water, in compounds-1teL, anticaries usable orally and such as these toothpaste preparations and pastes Se-en as the use of mineral phosphates, soluble in 1 " In oral compositions containing these fluorides either .EE: .ae '-. î: In the art (eg, Canada Patent No. 570,303), the soluble phosphate content of such compositions contributes relatively little to the effect. anticaries of fluorides at the low concentrations specified.



   The present invention is based on the discovery that particular types of soluble phosphates, namely
 EMI2.6
 ammonium salts of condensation products of ammonia and

 <Desc / Clms Page number 3>

 phosphorus pentoxide, possess surprising inherent anti-calc properties, and exhibit remarkably improved anticavity efficacy in the presence of fluoride ions, and preferably also in the presence of stannous ions.



   Dental research has undoubtedly proven that beyond the age of forty, tooth loss is mainly due to periodontal complications rather than dental caries. The single most important factor contributing to the
 EMI3.1
 Periocontic disease is the buildup of dental stones (eg, salivary tartar) on the teeth. These concrete
 EMI3.2
 Stony structures or deposits result in inf3a-ar.iation of the surrounding gum tissue and, this condition becoming more and more serious, damage to the jawbone. These reactions lead to the destruction of the structures which support the teeth, and consequently to the loss of mass of the latter.



   It was believed to be correct that the accumulation of dental stones could be inhibited through the use of new and more active cleaning and polishing agents. A more highly polished and cleaned tooth, and therefore a smoother tooth, is considered to be less likely to be the site of an accumulation of solid debris, such as stones, than a rough tooth surface. However, agents:
 EMI3.3
 Chemicals (such as cleaning and polishing agents) - as opposed to physical agents - have been widely used due to the safety concerns posed by such chemical agents.

   Consequently, the object of the present invention, according to the first of its aspects, is the use of
 EMI3.4
 compositions comprising ammonium salts of condensation products of ammonium ac and phosphorus pentoxide which exhibit surprising and unexpected efficacy as anti-calc agents (ie, agents which can be used to decrease the tendency. hard oral tissues to be the site of accumulation that Ciz C¯a.iS den ': 3ires) while being able to be used safely in the oral cavity.



   In accordance with the present invention, it has been found that oral compositions should contain from about 1% up to about 40% (and preferably from about
 EMI3.5
 5% up to about 15%) of amonium salts of condensation products of al., Oniac and phosphorus pentoxide, for example:

 <Desc / Clms Page number 4>

 
 EMI4.1
 and a vehicle for use in the oral cavity. XI agrees that
 EMI4.2
 the pH values of such oral compositions: o.i <# xÎ relatively low (between 4 and 5) when there is. i. ": - porous fluoride ions they are highly effective in lowering
 EMI4.3
 the solubility of tooth enamel.

   As many specialists know, dental caries is caused in part by the dissolution of enamel in intraoral acids.
 EMI4.4
 biologically produced, and the decrease in the solubility of tooth enamel in such acids considerably decreases the risk of dental caries. The ineffectiveness of antica- rants in decreasing the solubility of enamel in acids is a well known fact. which definitely indicates agent ineffectiveness.



   An essential aim 'of the present invention is therefore to produce novel and original compositions characterized
 EMI4.5
 by the incorporation of salts of a! Coniunt of condensation products of ammonia and phosphorus pentoxide.



  Another 1 # ut is 31; wentio is, the acidic oral compositions of the Genus cue - t4-or. ,, des 1: z>: fi :: our1-, ';? xni. # <* # tgn ;; : a;, i '..i.t nnti #, ri: # ùm ± -:,.:; rs ;. f.:::C01r't-; #: n. ;;: t # eb ;; te: ::: l,.; t:;:. we are; t 1: :: c :: f3 :: iser n #: # <; - e; ù. # ix prnc> 6d4J p: 9 = #. = à = tiànt de 1: xtler o =? # t = - # f. # s cirié = s den- 2z; ir.ez.



  ? t: .i has # abre goal of 1? inve =: tio? F * sù e3e rlisr new -ccKposiûicr .; usable p-cur di =! in's <? r les risc'5 <i''scc-j: # îsulaicn de * ': 3l-'j: Is r3entai = es zrr: .15 tissues o = a #.: #. i. ## s- 7 i- '== -.... # "ia # tzg - * = +' -ri '' * i; 1. # la r'.st in.T # ttl # J ' . " ;: ': 1 l 1' lcct; ## e -fJ8 flg '..i'r-itA-' tsm * s>; Ev # aate, y: iô.a #; a:. = ewj; L.35 b :! e; #feoe; #z,; o # i 1 # ni; atif #. l. <2 '; c- "osl'.is .Jral # -5 <2H questi -.- a. =. = -: # j = ren # erE = Cepuis' SKTiron 1% until>; noe.ir. J # 40S (àe prafer & rsc'x from n7iron 55 '& up to approx. 5;}. D! 3 ze + ls This products e con #

 <Desc / Clms Page number 5>

 densation of ammonia and phosphorus pentoxide such as, for example, those having the following formulas:
 EMI5.1
 'and a vehicle usable in the oral cavity.

   These salts and a procedure for their preparation are described in the E.U.A. n 2,122,122. Such salts are sold commercially by the Stauffer Chemical Company under the trademark "Victamide" and are hereinafter referred to as that name. Such oral compositions preferably also include stannous and fluoride ions and have relatively low pH values (between 4 and 5).

   Among the vehicles which can be used in the oral cavity are, in the case of toothpastes and prophylactics, cleaning and polishing agents and the other constituents ordinarily incorporated in toothpastes and prophylactics. In the case of solutions and mouthwashes to be applied locally, among adequate vehicles include water and other liquids.



   Such compositions demonstrate remarkable effectiveness in reducing the risks of a buildup of dental stones on hard oral tissue. In addition, when they are used in combination with the stannous and / or fluorescent compounds, chalk compositions containing "Victamide" in the proportions specified above exhibit a level of anticavity activity which is substantially and surprisingly higher than that achievable with stannous ions and fluoride without "Victamide".



   Fluoride compounds which provide fluoride ions in aqueous solution and which are therefore usable in the oral compositions according to the present invention are, of course, well known to those skilled in the art. Typical examples of such fluorinated compounds are water-soluble flower-type salts such as SnF2, NaF, SnF4, KF, InF3, PbF2 and LiF, as well as more complex chemical species containing.

 <Desc / Clms Page number 6>

   is fluorine-free and soluble in water, for example florosi-
 EMI6.1
 licates such as Na25iF6 'fluoroxirconates such as SnZrF6' fluorostannites such as NaSnF 31 fluorotitanates such as TaTir ^ 5, fluorogermanates such as K2GeF6 'Zr (GeF),

   and mixed halides such as SnClF and Sn2ClF3. It is also possible to use mixtures of two suitable salts of the fluoride type. Preferably, stannous salts containing
 EMI6.2
 fluoride ions (-such as SnF2 and SnZrF.).



   Various compatible cleaning and polishing agents which can be used in the toothpaste which is the subject of the present invention.
 EMI6.3
 tion are known in the art, including insoluble calcium inetaphosphate, insoluble sodium metaphosphate, calcium pyronhosphate, calcium hydrogen phosphate dihydrate, anhydrous calcium hydrogen phosphate, and substantially water-impermeable, transversely crosslinked synthetic resins. , thermosetting, highly polymerized (for example:
 EMI6.4
 non-elamine-formaldehyde resins) as described in the E.U.A. n 3,070,510, and preferably zirconium silicate or mixtures of zirconium silicate with other cleaning and polishing agents (eg talc).

   Mixtures of at least two such polishing agents can also be used.



   It is possible that when using "Victamide" at higher concentrations, problems of enamel erosion (decalcification) are encountered; in the first place because
 EMI6.5
 the strength of "Victamide" coxse chelating agent and csuse its affinity for calcium ions. However, we have that the presence of divalent cations (such q: ie ca ", Kg 's Sn *' * \ analogues) makes the 'Vic> aoeié ='" acmpièt = ze # t inoif. == # sà.f. By csn # seq'.1ent, preferred compositions therefore contain at 1 :: ir1s about 0.1% of such cations or mixtures of at least two such cations.

   Preference is given to the stannous ion because of its beneficial activity in preventing these caries. Stannous chloride and more especially stannous fluoride and stannous fluorozirconate are more especially preferred sources of stannous ion.



   As has been pointed out above ;, compositions c-
 EMI6.6
 The lines forming the object of the present invention comprise about 1-1.0% and preferably about 5-15% of. "Siçtamide". Such compositions preferably comprise fluoride ion.

 <Desc / Clms Page number 7>

 from about 0.01 to 15%, depending on the particular end use for which the composition is intended. Further, such toothpaste and prophylactic compositions contain about 20-80% compatible cleaning and polishing agent, depending on the particular type of composition desired, as well known to those skilled in the art.



   Oral formulas for daily use in routine grooming such as dentifrices and the like typically include about 20-70% compatible cleaning and polishing agent as a suitable vehicle for their use in the oral cavity. The content of
 EMI7.1
 weight of "Victa, nest" is between approximately; and 40%, and preferably between 5 and 15%, based on the weight of the preparation.
 EMI7.2
 tion toothpaste. The optimum content of t'slictaide ^ varies depending on the desired pH and the polishing agent and the particular active agents used. Such compositions show remarkable efficacy as anti-calc agents.



   Preferably a minimal but effective and non-toxic proportion of a fluoride compound, a proportion within a range sufficient to provide from about 0.01 to about 2, OR (preferably about 0.1%) of fluoride ion, is also provided in the composition to make it anticavity. When SnF or SnZrF6 is used, such salts are preferably used in particular.
 EMI7.3
 bran about 0, and 0.3% respectively (because about 0.4% of SnF2 provides about 0.1% of fluoride ion, as does about 0.3% of .SnrF 83.



   Toothpaste preparations produced in accordance with the present invention and containing fluoride ion are preferably
 EMI7.4
 pil i3e '-. Ip.' .. S'e .., 's values in the range acids, er generally less than 5.0. The pH of such preparations is preferably between 4.0 and 5.0.



   The toothpaste compositions in question are prepared in a conventional basket, and are usually incorporated therein additional ingredients capable of rendering the composition in question.
 EMI7.5
 tion 31ü pleasant to con50at0urs.



  Dental pastes require a substance serving as a binder for their development of the desired textual properties. We bind to give them these desired texture properties. For this purpose, binders of the natural gum type can be used.
 EMI7.6
 such as tragacanth, karaya (or Basra) gum. gum arabic, etc., or substances obtained from algae such as

 <Desc / Clms Page number 8>

 Irish moss and alqinates, and cellulose derivatives
 EMI8.1
 soluble in water such as qi? 1.iyàrox'yétiayl-cellulose and sodium derivative of carlxp4a1--ce.?a.ase. It is advantageous to use those of these substances which are most compatible with the fluoride ion.

   Binders devoid of ionic groups, such
 EMI8.2
 that 1 hy droxyethyl cellulose, are more especially preferred.



  Texture improvements are also made by incorporating an additional substance such as colloidal magnesium silicate.
 EMI8.3
 sius and aluminiua.



   To form a satisfactory toothpaste, the thickening agents can be used in an amount of 0.5 to 5.0% by weight.



   Toothpastes conventionally contain soap-like foaming agents. Among such agents, one can
 EMI8.4
 , ter, without this enumeration being limiting, alkayl sul- fates soluble in water and comprising from 8 to is carbon atoms in the alkyl radical and such as sodium lauryl sulphate.
 EMI8.5
 dium; water-soluble salts of sulfonated Ktonoglycerides of fatty acids having from 10 to 18 carbon atoms in the alkyl radical, such as nor.o - LI;.: sodium ceride-su2onave derived from fatty acids coconut; acid salts
 EMI8.6
 taurine fatty amides such as the sodium salt of: i-Ifiei2jia.c; : oy? -tacrice; and salts of fatty acid esters of isr¯tlionic acid.



   Foaming agents can be used in compositions according to the invention in a proportion of between approximately
 EMI8.7
 ron 0.5 and about 5.0% by weight based on the weight of the total composition.



   It is also desirable to incorporate, in a dental paste
 EMI8.8
 ra $ an adequate proportion of a urling agent preventing this r.1tt2.: :: ', arC¯.'. â 4 .. '.' ::, ces; .i; = 1-erzs cs # :: ,:; 4%>. B.:é= used for this 40: Ifl, ## can cite:; ll '..: Ji: 1e7 sor. And other alcohols 30: e? 0.'ß'iüF'S Humectants can represent up to 35% of the toothpaste composition.



  It is also possible to incorporate, in the compositions in question, a.:;a.saâ V i3 of small proportions of essences of 'Ninter # green and of Peppermint, as well as sweetening agents such as saccharin, dextrose, levulose.



   Various preferred compositions of toothpaste according to
 EMI8.9
 present invention are given below in - * - 4-: re examples well

 <Desc / Clms Page number 9>

 understood without limitation.
Example I.-
 EMI9.1
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb>
 
 EMI9.2
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ (C 'lu.

   1
 EMI9.3
 
<tb>
<tb> <SEP> zirconium <SEP> silicate <SEP> 43.0
<tb> "Victamide" <SEP> 1.0
<tb> glycerin <SEP> 12.8
<tb> sorbitol <SEP> (70% aqueous <SEP> solution <SEP> <SEP>) <SEP> 14.8
<tb>
 
 EMI9.4
 coconut-rnar¯og3ycéridesulfonate sodium acids sodium lauryi-sulfae 1.0
 EMI9.5
 
<tb>
<tb> veegum <SEP> (silicate <SEP> of <SEP> magnesium <SEP> and <SEP> alu-
<tb> -minium) <SEP> 1.0
<tb> <SEP> sodium <SEP> salt <SEP> <SEP> carboxymethyl cellulose <SEP> 1.0
<tb> flavoring <SEP> agents <SEP> 0.1
<tb> <SEP> coloring agents <SEP> 1.0
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.1
<tb> <SEP> distilled water <SEP> @ <SEP> 23.2
<tb> 100.0
<tb>
 
 EMI9.6
 Exer:

  1D 1 e II.-
 EMI9.7
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb> (%)
<tb> <SEP> zirconium <SEP> silicate <SEP> 15.0
<tb> <SEP> calcium <SEP> pyrophosphate <SEP> 30.0
<tb> "Victamide" <SEP> 10.0
<tb>
 
 EMI9.8
 stannous fluorozirconate 0.3
 EMI9.9
 
<tb>
<tb> glycerin <SEP> 12.0
<tb> sorbitol <SEP> (70% aqueous <SEP> <SEP> <SEP> solution) <SEP> 15.0
<tb>
 
 EMI9.10
 coconut acids-nonog3yceriae-
 EMI9.11
 
<tb>
<tb> <SEP> sodium <SEP> sulfonate <SEP> 0.5
<tb>
 
 EMI9.12
 sodium lauryl sulfate 2,0 -eeß3s:

  c (magnesium aluminum silicate) 0.4 sodium salt of carboxymethyl-cellulose '1.0
 EMI9.13
 
<tb>
<tb> <SEP> coloring agents <SEP> 0.4
<tb> <SEP> flavoring agents <SEP> 0.8
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.2
<tb>
 
 EMI9.14
 distilled water ¯¯¯12,4¯¯¯¯
 EMI9.15
 
<tb>
<tb> 100.0
<tb>
 

 <Desc / Clms Page number 10>

 Example III.-
 EMI10.1
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb>
 
 EMI10.2
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯
 EMI10.3
 
<tb>
<tb> <SEP> calcium <SEP> pyrophosphate <SEP> 45.6
<tb>
 
 EMI10.4
 "Vi <tamide" 5.0
 EMI10.5
 
<tb>
<tb> stannous <SEP> fluoride <SEP> 0.4
<tb> glycerin <SEP> 12.0
<tb>
 
 EMI10.6
 sorbitol (70-, aqueous solution) 35L 'coconut acids-sodium monoglyceridesulfonate 0.5 lau, sodium rylsulfate 2,

  0
 EMI10.7
 
<tb>
<tb> veegum <SEP> (<SEP> magnesium <SEP> and <SEP> aluminum silicate <SEP>) <SEP> 0.4
<tb> <SEP> sodium <SEP> salt <SEP> <SEP> carboxymethyl cellulose <SEP> 1.0
<tb> <SEP> coloring agents <SEP> 0.5
<tb> flavoring <SEP> agents <SEP> 0.6
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.1
<tb> <SEP> distilled water <SEP> 16.9
<tb> 100.0
<tb>
 Example IV.-
 EMI10.8
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb>
 
 EMI10.9
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ (%) 24.0 hydrogen-phosphste calcium dihydrate of anhydrous calcium 24.0 "Victamide" 15.0
 EMI10.10
 
<tb>
<tb> stannous <SEP> chloride <SEP> 1.0
<tb> glycerin <SEP> 13.0
<tb> sorbitol <SEP> (70% aqueous <SEP> solution <SEP> <SEP>) <SEP> 15,

  0
<tb>
 
 EMI10.11
 coconut acids # monoglyceride # .. 'ul for'aie sodium O 1:.: .. 1. Sodium sulphate '1: rO vc -7 -, (silicate of sagnesiux! And aluminiunt) 1.0 sodium salt of ceboxyetyl-cellulo5e lC aramatizing agents, 2
 EMI10.12
 
<tb>
<tb> <SEP> coloring agents <SEP> 0.5
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.1
<tb> <SEP> distilled water <SEP> 3.2
<tb> 100.0
<tb>
 

 <Desc / Clms Page number 11>

 Example V, -
 EMI11.1
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb>
 
 EMI11.2
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ Ass
 EMI11.3
 
<tb>
<tb> silicate <SEP> of <SEP> zirconium <SEP> 14.0
<tb> talc <SEP> improved <SEP> * <SEP> 28.0
<tb> <SEP> calcium <SEP> chloride <SEP> 0.5
<tb> "Victamide" <SEP> 10.0
<tb> glycerin.

   <SEP> 12.0
<tb> sorbitol <SEP> (70% aqueous <SEP> solution <SEP> <SEP>) <SEP> 14.0
<tb> <SEP> nuts <SEP> <SEP> .de <SEP> coco-monoglyceridesulfonate <SEP> <SEP> sodium <SEP> 0.5 acids
<tb> <SEP> sodium <SEP> lauryl sulfate <SEP> 2.0
<tb> veegum <SEP> (silicate <SEP> of <SEP> magnesium <SEP> and <SEP> aluminum) <SEP> 1.0
<tb> <SEP> sodium <SEP> salt <SEP> <SEP> carboxymethyl cellulose <SEP> 1.0
<tb> <SEP> coloring agents <SEP> 0.5
<tb> flavoring <SEP> agents <SEP> 0.5
<tb> derived <SEP> from <SEP> sodium <SEP> from <SEP> the <SEP> saccharin <SEP>, <SEP> 0.2
<tb> <SEP> distilled water <SEP> 15.8
<tb> 100.0
<tb>
 
 EMI11.4
 .

   Talc, M93si4010 (OH) 2 'containing at least a minimal proportion of tremolite, Ca "<g3 (SiC3), as impurities Example VI. -
 EMI11.5
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb>
 
 EMI11.6
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ 1 (%)
 EMI11.7
 
<tb>
<tb> <SEP> zirconium <SEP> silicate <SEP> 15.0
<tb> resin <SEP> 30.0
<tb>
 
 EMI11.8
 "Victa111ide" 5.0
 EMI11.9
 
<tb>
<tb> <SEP> sodium <SEP> fluoride <SEP> 0.2
<tb> glycerin <SEP> 13.0
<tb> sorbitol <SEP> (70% aqueous <SEP> <SEP> <SEP> solution) <SEP> 15.0
<tb>
 
 EMI11.10
 cocci-nonogiyceridesulfonBte ce sodium 1.0 31:

  Sodium yl-silicate 1.0 veegun (magnesium aluminum silicate) 1.0 sodium salt of carboxymethylcellulose 1.0
 EMI11.11
 
<tb>
<tb> flavoring <SEP> agents <SEP> 0.5
<tb> <SEP> coloring agents <SEP> 0.7
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.1
<tb> <SEP> distilled water <SEP> 16.5
<tb> 100.0
<tb>
 . covered by the E.U.A. n 3,070,510

 <Desc / Clms Page number 12>

 
Toothpaste preparations established according to the above-specified formulas are suitable for frequent application to the teeth (for example, as often as several times a day}.



  When used in this way, a new and interesting method is available to fight against cavities and / or dental stones.



   Among the oral compositions which are the subject of the present invention are, in addition to the toothpaste preparations specified above, compositions of the prophylactic pastes type because.
 EMI12.1
 all for less frequent applications (by: W ::: 3'g once or twice a year) either by a professional L, 'te--' '¯': 1: l dentist or a specialist in dental hygiene), or by the
 EMI12.2
 holds itself.

   Such a paste-like composition generally differs from a dentifrice composition in that the cleaning and polishing agent is much more abrasive (and hence cleans teeth better). Since such a prophylactic paste only applies once or twice a second, it is safe to incorporate a more abrasive cleaning and polishing agent that would be dangerous to use in a preparation. toothpaste, because in such a very frequently used preparation, such a strong cleaning and polishing agent has
 EMI12.3
 brasif could endowmTiaçer in a perrnan way '::

  flies hard oral tissue.
 EMI12.4
 The compatible substances specified above as suitable cleaning and polishing agents to be incorporated into toothpaste preparations can also be used as a constituent.
 EMI12.5
 $ "yY?" ï '.: i and polishing ï'a "ââ ë (5' â.iS, é.:. t3T J :;. # z-pe paste prophy- ¯., - 'r" <" ,: - utoi, ::: 't:;: 4 t: .n:' e a .- "t .: '" ;; ie ==, 1 =?:; tes the ii-ß>' w " -f's-; w H.sâ 7f, '"* o' / 'li -'''- 5'" T ''% 3r * "cj¯ =% p * mi" E == 1 => 5> àz ;, = t; oyJji = .al = <: e yalisx # = jé = un: # -r # n = ùicr = 4tri # oef) fly - == o =; Siji # = atia: m Ji.ipéri ± ci = -ile .àes>. = r # ic: islands .de ia substance "en., 3r'S: 'iâs ::: e'.,.;."., '; ?? 7ï ¯oU' '' '' - (J! .¯., :: ...-...... ':; ..... ¯5D By - "" ...: ....- e: t a silic " / te1 :? zirconium 6 .., including in view irp its use CC :: 12 ".



  3gen cleaner and polish in one composition; of the 9ropy} açtiJe paste type. and? find Ce-cr4 in. ',' 3â: '' "';? eT <.é'so .3257¯282 accorc-ê on 2l'j.; 5n lS> 66 at ef''1a; èersse.



  .-v- <': .d .. .'r = sc: - ,,, "".' "- p .. & -, .....". "" ,, and suitable polishes are listed .0 :; ' ± J of ro silicate * = of tin dioxide, of d3 ;; ier:.; pence of lava, silica, GtI, calcium carbonate, and the like.



     - We establish the composition formula of the type of paste

 <Desc / Clms Page number 13>

 phylactic according to the present invention with about -40% and preferably about 5-15% of "Victamide". The cleaning and polishing agent serves as a vehicle or carrier and is used in an amount of about 30 to 80% depending on the particular composition desired, as is well known to those skilled in the art.



   Such oral compositions are effective in decreasing the tendency of hard oral tissue to be the site of dental root accumulation.



   In addition to the essential ingredients specified above, the flammable ion is preferably used at an effective non-toxic level, usually between about 1% and about. based on the weight of the subject prophylactic paste composition. When SnF2 or SnZrF- is used, such salts are preferably used in an amount of approximately 8% and 30% respectively; about 8% SnF provides about 2% fluoride ion, while 30% SnZrF6 provides about 10% fluoride ion.



   Those of the prophylactic paste compositions produced in accordance with the present invention which contain fluoride ions exhibit pH values in the acidic range, generally less than 5.0. The pH values of such preparations are preferably between 4.0 and 5.0.



   Such prophylactic paste-type compositions are prepared by working in a conventional manner, and usually by incorporating therein ingredients which make the overall composition commercially acceptable. For example, such pastes typically contain conventional components such as bleaches, binders, humectants, flavorings and the like.



   Preferred prophylactic paste-like compositions produced in accordance with the present invention are specified hereinafter in Examples VII to IX, but it is understood that these examples too are given by way of illustration and are in no way limiting.

 <Desc / Clms Page number 14>

 Example VII.-
 EMI14.1
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb>
 
 EMI14.2
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ (%) zirconium silicate 5530 'Victamidep po, such .uaroirconate stannous 1570 glycerin 5, ex sorbitol (70% aqueous solution) 70 veegum (magnesium aluminum silicate) 0.7 sodium carbohydrate salt;

  > * methyl-ce11u'ose i, E '
 EMI14.3
 
<tb>
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.2
<tb> <SEP> sodium <SEP> cyclamate <SEP> 0.4
<tb> <SEP> flavoring agent <SEP> 2.0
<tb> agent <SEP> coloring <SEP> 0.5
<tb>
 
 EMI14.4
 distilled water ¯¯¯¯¯3¯¯¯¯
 EMI14.5
 
<tb>
<tb> 100.0
<tb>
 Example VIII.-
 EMI14.6
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb>
 
 EMI14.7
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯) ¯¯ ###
 EMI14.8
 
<tb>
<tb> <SEP> zirconium <SEP> silicate <SEP> 45.0
<tb> tin dioxide <SEP> <SEP> '<SEP> 5.0
<tb> stannous <SEP> fluoride <SEP> 9.0
<tb> "Victamide" <SEP> 15.0
<tb> glycerin <SEP> 5.0
<tb> sorbitol <SEP> (70% aqueous <SEP> solution <SEP> <SEP>) <SEP> 7.0
<tb> veegum <SEP> (silicate <SEP> of <SEP> magnesium <SEP> and <SEP> aluminum) <SEP> 0,

  7
<tb> <SEP> sodium <SEP> salt <SEP> <SEP> carboxymethyl cellulose <SEP> 1.0
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.2
<tb>
 
 EMI14.9
 ycissas e sodium O, 4
 EMI14.10
 
<tb>
<tb> agent <SEP> aromatisa ;; <SEP> 2.0
<tb> agent <SEP> coloring <SEP> 0.5
<tb>
 
 EMI14.11
 distilled water .- # JJ! ¯¯¯
 EMI14.12
 
<tb>
<tb> 100.0
<tb>
 

 <Desc / Clms Page number 15>

 Example IX, -
 EMI15.1
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb> (%)
<tb> pumice <SEP> of <SEP> lava <SEP> 48.0
<tb> "Victamide" <SEP> 5.0
<tb> glycerin <SEP> 9.0
<tb> sorbitol <SEP> (70% aqueous <SEP> solution <SEP> <SEP>) <SEP> 11.1
<tb> veegum <SEP> (silicate <SEP> de-magnesium <SEP> and <SEP> aluminum) <SEP> 0.7
<tb>
 
 EMI15.2
 sodium salt of carboxymethyl-cellulose 1,

  0
 EMI15.3
 
<tb>
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.2
<tb> <SEP> sodium <SEP> cyclamate <SEP> 0.4
<tb> <SEP> flavoring agent <SEP> 2.0
<tb> agent <SEP> coloring <SEP> 0.5
<tb> <SEP> distilled water <SEP> 22.1
<tb> 100.0
<tb>
 
A composition of the prophylactic paste type according to the present invention finds useful applications as an agent applicable semi-annually by a dentist or by a specialist in dental hygiene. Such a composition can also be advantageously used by the patient himself to clean his teeth under the supervision of a competent professional, at similar semi-annual intervals.



   When compositions of the prophylactic paste type whose formulas are specified above are suitably used (either by a specialist professional or by the patient himself), a new and interesting method results. to fight against caries and / or dental stones.



   In addition to toothpastes and prophylactics, "Victamide" is found to be of interest when used in other oral compositions (such as for example those of the type of toothpaste and mouthwashes which can be administered in local applications) comprising stannous ions. and fluoride as shown by the following non-limiting examples.



   Example X.- Locally administrable solution.
 EMI15.4
 
<tb>
<tb>



  Component <SEP> Parts <SEP> in <SEP> weight
<tb> (%)
<tb> "Victamide" <SEP>. <SEP> 5.0
<tb> <SEP> flavoring agent <SEP> 1.5
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.1
<tb> <SEP> distilled water <SEP> 93.4
<tb> 100.0
<tb>
 

 <Desc / Clms Page number 16>

 
 EMI16.1
 Exennium XI.- Locally aduinistrable solution.
 EMI16.2
 
<tb>
<tb>



  Component <SEP> Parts <SEP> in <SEP> weight
<tb> (%)
<tb> stannous <SEP> fluoride <SEP> 2.0
<tb> "Victamide" <SEP> lottery
<tb> <SEP> flavoring agent <SEP> 2.0
<tb> sodium <SEP> derivative <SEP> <SEP> saccharin <SEP> 0.2
<tb> <SEP> distilled water <SEP> - <SEP> 85.8
<tb> .100.0
<tb>
 Example XII - Toothpaste or mouthwash.

   
 EMI16.3
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb>
 
 EMI16.4
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ () .Victamideft 5.0
 EMI16.5
 
<tb>
<tb> sorbitol <SEP> (70% aqueous <SEP> solution <SEP> <SEP>) <SEP> 10.0
<tb> ethanol <SEP> (95% aqueous <SEP> <SEP> <SEP> <SEP> solution) <SEP> 20.6
<tb>
 
 EMI16.6
 polyoxyethylene sorbitan monostearate bone 6
 EMI16.7
 
<tb>
<tb> bactericidal <SEP> agent <SEP> 0.1
<tb> agent <SEP> coloring <SEP> 0.4
<tb> <SEP> flavoring agent <SEP> 0.2
<tb> derivative <SEP> of <SEP> sodium <SEP> of <SEP> the <SEP> saccharin <SEP> 0.2
<tb> <SEP> sodium <SEP> 0.2 cyclamate <SEP>
<tb> <SEP> distilled water <SEP> 62.7
<tb> 100.0
<tb>
 
 EMI16.8
 Compensation X 1 II. - Toothpaste or mouthwash.

   
 EMI16.9
 
<tb>
<tb> Constituent <SEP> Parts <SEP> in <SEP> weight
<tb>
 
 EMI16.10
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ (Â) Vctamiàe '10'O sorbitol (solution 70% aqueous) 10.0 ethanol (9% aqueous solution) 20.6 molyo monostearate> -, ethylene-sorl-14-4 - anne 0.6
 EMI16.11
 
<tb>
<tb> bactericidal <SEP> agent <SEP> 0.1
<tb> agent <SEP> coloring <SEP> 0.4
<tb> <SEP> flavoring agent <SEP> 0.2
<tb>
 
 EMI16.12
 socius derivative of saccharin O, 2 vG S. &. F.Sf34c of sodi-um 0.2 water distillcG z?
 EMI16.13
 
<tb>
<tb> 100,

  0
<tb>
 
 EMI16.14
 The effectiveness of an acet as an inhibitor of the -¯eorr-ation of dental stones is unreachable by carrying out the procedure described below * Tooth enamel specimens of approximately square shape are cut from

 <Desc / Clms Page number 17>

 the incisor half of the crowns of the central incisors of the maxilla of cattle, using diamond discs. Sections are embedded in preformed clear acrylic resin blocks, using pink dental acrylic adhesive as an adhesive so that only the labial surfaces are exposed.

   Holes, placed several millimeters away from the dental enamel cuts, are then drilled through the acrylic blocks to receive metal orthodontic fixation wires.



   After having received certain treatments described below, the enamel blocks are attached to a calculus forming machine designed to perform alternately an immersion of the enamel blocks in a liquid mass of human saline and an exposure of these blocks air over successive time periods of 30 seconds each.



   During the experimental evaluation, a total of 13 enamel blocks are used which are divided into two groups. The blocks of group 1 (the control group) receive a "prophylactic type" treatment by using a paste based on fine pumice powder for 3 minutes, then rotating in a liquid mass of human saliva for 24 hours. of each of the 28 days of the trial period. The blocks of group II receive a "prophylactic type" treatment by using a paste of fine powder of pumice stone for 3 minutes. After this treatment, the enamel blocks are attached to the stone forming machine and allowed to spin in a liquid mass of saliva for 23 hours.

   The saliva is then removed from the reservoir which contained it and, after having rinsed the blocks with distilled water, the reservoir is filled with a 5.0% aqueous solution of "Victamide". The blocks are then left to rotate through this solution. After one hour of such exposure to "Victaide", the "Victamide" solution is removed, the blocks are rinsed again with distilled water, then the reservoir is filled with fresh saliva. this procedure is repeated daily throughout the test period.



   At the end of the 28-day test period, the 13 enamel blocks are removed from the stone forming machine 4, and the stone weight deposited per developed area of tooth enamel (which is expressed in calculated weight by

 <Desc / Clms Page number 18>

 developed area). In addition, the blocks are examined using a system of visual scoring indices ranging from 0.0 (no stone-like deposits visible) to 5.0 (stone deposits which are visually seen to overlap. to-
 EMI18.1
 baleraeiat enamel cuts}.



  Table I summarizes the results of the above-specified stone formation inhibition tests. The data in Table 1 demonstrate very substantial cystinutions in the formation of stones observable by the use of the aqueous solution of this iTica - 3de according to the present invention.

   Table 1
 EMI18.2
 înowd3re de Agent pro Anti-Agent Notation Decrease Weight phylaceous sections visual calculations mean
 EMI18.3
 
<tb>
<tb> -.email <SEP> that <SEP> the <SEP> mo- <SEP> of
<tb> yenne <SEP> calculations
<tb> by <SEP> surface <SEP> de-
<tb>
 
 EMI18.4
 ¯¯¯¯¯¯¯¯ ¯¯¯¯¯¯¯¯¯¯¯ ¯¯¯¯¯¯¯¯¯¯ ¯¯¯¯¯¯¯ Veloooée
 EMI18.5
 
<tb>
<tb> powder <SEP> fine <SEP> none:

   <SEP> 2.1 <SEP> @ <SEP> 0.0280 <SEP> @
<tb> from <SEP> pierre
<tb> pumice
<tb> 7 <SEP> powder <SEP> fine <SEP> solution, <SEP> a- <SEP> 0.7 <SEP> 66.7 <SEP> 0.0117 <SEP> 58.2
<tb> from <SEP> pierre <SEP> Gueuse <SEP> to
<tb>
 
 EMI18.6
 pumice 5% of -1-Tic-
 EMI18.7
 
<tb>
<tb> tamide "
<tb>
 
From these results, it is therefore evident that the present invention provides means making it possible to reduce the
 EMI18.8
 rate of dental stone accumulation on the surface of these teeth *
The effectiveness of these oral compositions in question in reducing the frequency of dental caries is proven by
 EMI18.9
 The following experimental eir-aaations.

   Of effect these various com- 7-) or - ons with regard to the decrease in the so- .¯ Ii-ce of -, - 'tooth enamel in an acid constitute an indication. safe and 'valid anti-cavity efficacy. The characteristics of dental compositions with regard to the solution
 EMI18.10
 bility of the enamel is determinable. by various tests well known to specialists. The particular test for determining the solubility of dental enamel described here essentially comprises a comparison: of the solubility, in an acid, of a dental enamel before and after treatment with a composition to be tested
 EMI18.11
 given.

   This comparison is expressed in DSE, that is to say reduction in the solubility of the enamel.

 <Desc / Clms Page number 19>

 



   The SSD of rat teeth is determined in vivo as follows:
The teeth of a suitably selected group of test rats are subjected to a number of brushings with various toothpaste preparations over a suitable period of time. The animals are then sacrificed. Each hemi-maxilla is removed and the clinical crowns of each of these parts are decalcified in 0.2N sodium acetate buffer (pH 4) for 20 minutes, then the decalcification solutions are analyzed to determine the phosphorus therein by a colorimetric method (according to Fisk and Subbarow: "The Colorimetric Determination of Phosphorus" - the colorimetric determination of phosphorus -, Journal of Biological Chemistry, 66, 375, 1925).

   The release of phosphorus from teeth brushed with a toothpaste with a fluoride-"Victamide" mixture is compared with that observed on teeth similarly brushed with a control toothpaste containing neither stannous tin, nor fluoride, nor "Victamide": we note the result of such a comparison as the percent decrease in enamel solubility (i.e., DSE).



   The data relating to the DSE are determined as described above for several zirconium silicate toothpastes whose formulas are of the type specified in Example I, but with the proportions of stannous fluoride and "Vicatmide" indicated. in Table II. These data concerning DES, which appear in Table II, reveal that the presence of "Victamide" considerably improves the anticarious activity of the oral compositions evaluated.

 <Desc / Clms Page number 20>

 



  Table II
 EMI20.1
 
<tb>
<tb> Constituents <SEP> of <SEP> toothpaste <SEP> <SEP> data relating <SEP> to <SEP> the <SEP> DSE
<tb>
 
 EMI20.2
 ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ (mean decrease per cent) Abrasive Fluoride "Victamide" stannous ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ ¯% ¯¯¯¯¯¯¯
 EMI20.3
 
<tb>
<tb> ZrSiO4 <SEP> 0.0 <SEP> 0.0 <SEP> -----
<tb>
 
 EMI20.4
 ZrSi04 0.4 1.0 28.0
 EMI20.5
 
<tb>
<tb> ZrSiO <SEP> 0.4 <SEP> 2.5 <SEP> 70.8
<tb> ZrSiO4 <SEP> 0.4 <SEP> 5.0 <SEP> 69.9
<tb> ZrSiO <SEP> 0.4 <SEP> 7.5 <SEP> 71.3
<tb> ZrSiO <SEP> 4 <SEP> 0.4 <SEP> 10.0 <SEP> 77.9
<tb>
 
 EMI20.6
 ZrSi04 0.4 12.5 72.8
 EMI20.7
 
<tb>
<tb> ZrSiO4 <SEP> 0.4 <SEP> 15.0 <SEP> 77.3
<tb> ZrSiO4 <SEP> 0.4 <SEP> 22.0 <SEP> 80.5
<tb>
 
Another indication of the potential effectiveness of an anticavity adjuvant system is the proportion of tin and fluoride ions available in aqueous solution.

   Percent availability refers to a comparison of an ionic concentration level for a reference solution of the adjuvant without the carrier vehicle (eg, an aqueous solution of the adjuvant.
 EMI20.8
 juvant not maintained at a reference ionic concentration level, such as 1000 p.p.m. of fluoride).

   A percentage ratio of the ionic concentration level for the solution of the combination compared to that of the reference solution is expressed as a percentage of availability (for example, a solution of the combination of carrier vehicle in fluoride
 EMI20.9
 $ ïâz, z $ "^ yt? Ld :. t ci.] s '... 6s>, ..;: i ..'. hâ ^ aT titrated 9CO p, p, m, of fluoride compara->" 6 a 'salmis d = r; 5: f5rer: - = i !!' -du ": l1 -;" =. u: = i :; stsnneux and he i 'S. as.x: .Cn xs69 to' 1 ('' ') 9.;:. n. fJr..5 $ ;; rt n4? .d: isp4. = - = ;. li: é i s .. with regard to the area Fpriuà> e 3 90zr # ir of fluoride ions).



  The more we determine the following are the percent availability figures for starry tin ions and an aqueous suspension of the composition which
 EMI20.10
 one '6a, 4iiw'. ro'é is stirred m4caniçJ = xenr for a lapse of tcxps d '; # o.'. . = '= il equ <1o (psr example about 15 minutes), THEN we C! ;;'.:.; ::.; . ' '' - the i. '.> 43ioa', ïE'i: ï1'X what we get a phJJe on ;;;;; j =, wi = .:, .ta? ice <On SMi-yce such aliquots dis ph <1:. '> c ut': '' 1C, H "" ¯ ', "Ji;) t: liG ..

   Ati3a6 - .. TLi S ,, fa p.H.ti. 5 dS-tinct aliquots of the liquid to assay them. .fluoride ions and. 7LG1i1aiL4J1? . po; this le- dosage of 1 "ion: -: fluÓ: iure, we have recourse to the.-method with thorium nitrate and distillation of perchloric acid.

 <Desc / Clms Page number 21>

 for the determination of stannous ions, the potentiometric titration with potassium periodate is used. The experimental values are then compared with those obtained from an aqueous reference solution containing the same proportion of stannous ions and fluoride to arrive at a figure of percent availability.



   Percent availability data is determined by waxing as follows for various toothpaste systems containing 0.4% stannous fluoride and several different concentrations of "Victamide" ranging from 1.0 to 10.0%. Three different abrasive systems are used, namely: a 1: 3 mixture by weight of zirconium silicate: melamine-formaldehyde resin produced according to the indications of Cooley et al. in U.S. Patents n s 3,070,510 and 3,251,800; a mixture of 1: 3 by weight calcium zirconium spyrophosphate silicate produced according to the indications of the U.S. patent. n 3,112,247; and a mixture of 1: 3 by weight zirconium silicate:

   "improved talc '* (i.e. talc Mg3Si4O10 (OH) 2 containing at least a minimal amount of tremolite CaMg3 (SiO3) 4 as an impurity). The compositions of these toothpastes are the same, except for variations in the proportions of the abrasive systems and of “Victamide.” The data relating to the percentage of availability are shown in Table 3. These data clearly demonstrate the anticavity effectiveness of the compositions which are the subject of the present invention. In particular, although the incorporation of "Victamide" into such dentifrice compositions improves the availability of fluoride ions, the effect of "Victamide" is even more pronounced in the case of stannous ions.

   Accordingly, in its preferred form, the scope of the present invention encompasses the incorporation of "Victamiden into oral compositions comprising anticavity adjuvants containing stannous and fluoride ions.

 <Desc / Clms Page number 22>

 



    TABLE III
 EMI22.1
 Gcntiunr, c7u dr: nti.t.co nimn # SysQn (t1bradf Sr1! '2 (%) "Victamide" (%) Sn ++ (%) fi' "(%)" "'P" 1'1t \ W \' I .IfiI'I. <I. "" 'M' IU, "¯iII I¯l -, I, '' 'I81' Ir" lt t> -............



  : 1..c of Kicconiums ü, ii. 10 loti 6 ggt3 talc 1I1 (Hior.Q o, 4 7.5;> 3, 9678 (in4-1.nge 1: 3 an weight) 0 4 5 o ci 95.6 O, 4 4, s7.7 90 , 3
 EMI22.2
 
<tb> 0.4 <SEP> 2.5 <SEP> 70.3 <SEP> 90.3
<tb> 0.4 <SEP> 1.0 <SEP> 37.9 <SEP> 75.5
<tb> <SEP> zirconium silicate <SEP>: <SEP> 0.4 <SEP> 10 <SEP> 92.8 <SEP> 91.1
<tb>
 
 EMI22.3
 cal pyrophoophake, bzz 7.5 eat3 8413 ciuin Il 0, 5 o 8 5, 81el (mixture 1: 3 by weight) O4 4eo 65 79.5
 EMI22.4
 
<tb> 0.4 <SEP> 2.5 <SEP> 73.7 <SEP> 63.2
<tb>
 
 EMI22.5
 Oe4 leo 44.3 zou zi carr3.uma silicate 0.10 3, 87.6 resin *. e: n ci.i) Ot4 7.5 90.7 f5.3 (loélanç6 1:

  3 by weight) U 4 9 8oye2 69e4 '' an '76t7 7310
 EMI22.6
 
<tb> 0.4 <SEP> 2.5 <SEP> 66.4 <SEP> 69,
<tb> 0.4 <SEP> 1.0 <SEP> 50.5 <SEP> 70 <SEP> 2
<tb>
 
 EMI22.7
 a .U.A patent. n8 3,112,247 .. E.U.A. patent n 3,070,510

 <Desc / Clms Page number 23>

 
DSE data for zirconium silicate: talc (mixture 1: 3 by weight) toothpastes containing either stannous fluoride or stannous fluorozirconate as anticavity adjuvant, and either "Victamide" or
NaH2PO4, or KG2PO4. Except that, these compositions comprise the same conventional constituents of dentifrices.

   The data from DSE prove that in each case a considerably improved anti-cancer activity is observed by "Victamide" compared with the mineral phosphates used at the same content.



   Dentifrices prepared by the preferred embodiment of the present invention have been shown to be effective in decreasing the frequency of dental caries by clinical studies in humans. In such a study, a total of 250 children aged 10 to 13 years residing in a fluoride-free region underwent a comprehensive clinical examination for dental caries using x-rays taken with a mount comprising seven x-ray films held between the jaws, according to previously described techniques (Muhler, JADA, 64, 216, 1962). The subjects are then divided into five equal groups according to their dental age and according to the observation of dental caries in the past.

   Everyone is given a toothbrush and a supply of the respective toothpaste packaged in tubes marked with a code system, without clear indications. Three of these five groups receive toothpastes containing "Victamide". New supplies of toothpaste and new toothbrushes are provided each month during a one-year study period, after which subjects are again given a full clinical examination with radiographic examination for cavities. , to determine the number of decayed, missing and filled teeth (DCMO) and decayed, missing and filled surfaces (SCMO), well-known indices of anticavity efficacy.

   The results of this study are summarized in Table V: they prove the efficacy of the compositions based on fluoride and "Victamide" according to the present invention in reducing the frequency of dental caries, and also prove the marked superiority of " Victamide "on mineral phosphates to improve anticavity activity.

 <Desc / Clms Page number 24>

 
 EMI24.1
 



  TABLEAII iV
 EMI24.2
 ¯¯¯¯¯¯¯ Know itu nn t ciu ctentifrice .¯¯¯¯¯¯¯ PhohntG¯s¯.¯¯¯¯¯ ponnoit do Diz Abrasive nF snz rf 6 nViclamid "Natt0 Kki 2PO fold mean decrease. ¯¯ ¯¯¯¯¯¯¯¯¯¯ .. ¯ '¯ 9. ¯ J¯ ¯¯¯¯3LJ .--.



  Ca 2 P 2 0 7 * -Cul ---- wwr, ow - ar.w wmv 500 wqwww v ç; â3.l7svKlIiC, p 0.41 30 zizi. '57e9 Zr $ io4: talc bzz O41 30 4,; a "20.1 4xi.C: lc, 3; ex, 41 30 4t5 24, 4:" il c -41t 510 0.28 30 bzz 63.2 4 talc -39 "0.28 30 4.5 28.3 KrSiO: talc -39% 0.28 30 4.5 1512
 EMI24.3
 Control, mixture 1: 3 by weight.

 <Desc / Clms Page number 25>

 



    TABLE V
 EMI25.1
 Constituents toothpaste '' augmenta- U m nu- augmenta- '"d imin #### Group Abrasive fluoride tion mo- tion mo- tison inooupe ras uoride (in weight yenne of enne% yenne of yenne eg DCNO of ÎÉ21 des. ##### ################ ¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯¯ w- 11 -....... ..---- ..., ......... 1
 EMI25.2
 
<tb> 1 <SEP> pyropliosphate <SEP> of
<tb> calcium <SEP> ------ <SEP> 0 <SEP> 4.90 <SEP> ----- <SEP> 6.64 <SEP> -------
<tb> 2 <SEP> pyrophosphate <SEP> from
<tb> calcium <SEP> SnF2 <SEP> 0 <SEP> 2.47 <SEP> 49.5 <SEP> 3.75 <SEP> 43.6
<tb> 3 <SEP> silicate <SEP> from <SEP> zir-
<tb>
 
 EMI25.3
 conium: talc améZrOGer6 5 1.88 61.8 2.00 '69.9
 EMI25.4
 
<tb> 4 <SEP> zirconium <SEP> silicate <SEP>: talc <SEP> am-
<tb>
 
 EMI25.5
 improved Zr (Ger 6 le23 74.5 2e26 $ 6.9
 EMI25.6
 
<tb> 5 <SEP> <SEP> zirconium <SEP> silicate:

  talc <SEP> am-
<tb>
 
 EMI25.7
 improved SnF2 10 1.35 72ts lesq lt, 5 'U.S. Patent n s 2.876.166 and 2.876.168 .. 1: 3 mixture by weight

 <Desc / Clms Page number 26>

 
Although the present invention has been described above with reference to certain embodiments chosen by way of examples, it should not be lost sight of the fact that the specialist can easily imagine and still use this very many other variations, modifications. and alternatives both of the substances and of the preparation procedures, without thereby departing from the spirit or the scope of said invention.

 

Claims (1)

EMI27.1 R E V E N D 1 C¯A¯T 1 0 N S 1. Oral composition characterized by the presence of a carrier veal which can be used in the buctal cavity and a. salt EMI27.2 :: the ammonium of a condensation product of actrsoniac (NH3} and:> phosphorus entoxide CP 4 "10). Composition according to Claim 1, characterized in = e raw said ammonium salt is EMI27.3 3. Composition according to claim 1 or 2, characterized in that said ammonium salt is present in an amount of approximately L to 40%, and preferably 5 to 15%, by weight, based on the weight of the composition. . Composition according to claim 1, 2 or 3, characterized in that the vehicle is a dental cleaning and polishing agent. 8. The composition of claim 1, 2, 3 or 4, characterized in that the composition comprises an antica- ie component containing fluoride. 6. Composition according to claim 5, characterized in: that the pH of the composition is between approximately 4.0 and 5.0. Composition according to Claim 5, characterized in: that stannous ions are present in the composition. EMI27.4 l. A method for preparing an oral body according to claim 1 for reducing the tendency of hard tissues to accumulate dental stones, characterized by EMI27.5 : e that it consists essentially in ıncormarer z an adequate vehicle an a! xnonium salt of a condensation product of anstoniac IXIIT3) and of phosphorus penroxide CP 1; 1.0). Process according to Claim 8, characterized in that the edit ammonium salt is <Desc / Clms Page number 28> EMI28.1 10. Process according to claim 8 or 9, characterized in that said ammonium salt is incorporated in the course of the reaction at a rate of approximately 1 to 40%, and preferably 5 to 15%, @@@ peid. . He. A method according to claim 8 or 9, wherein a dental cleaning and smoothing agent is used as the vehicle. 12. The method of claim 8, 9 or 10, character. in that one incorporates into the composition a constituent anie containing fluoride. 13. The method of claim 12, characterized in that the pH of the composition is adjusted to a value between approximately 4.0 and 5.0. 14. The method of claim 12, characterized in c is incorporated into the composition a substance which provides stannous ions. 15. A method for reducing the tendency of hard oral tissues to be the site of an accumulation of dental stones, the site of caries, characterized in that or * it consists essentially in applying to said tissues, or in treating them, an oral composition according to any one of claims 1 to 7.