CA1092512A - Dental thixotropic flucride-phosphate composition - Google Patents
Dental thixotropic flucride-phosphate compositionInfo
- Publication number
- CA1092512A CA1092512A CA255,446A CA255446A CA1092512A CA 1092512 A CA1092512 A CA 1092512A CA 255446 A CA255446 A CA 255446A CA 1092512 A CA1092512 A CA 1092512A
- Authority
- CA
- Canada
- Prior art keywords
- fluoride
- composition
- thixotropic
- phosphate
- gel
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K6/00—Preparations for dentistry
- A61K6/60—Preparations for dentistry comprising organic or organo-metallic additives
- A61K6/65—Dyes
- A61K6/66—Photochromic dyes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K6/00—Preparations for dentistry
- A61K6/60—Preparations for dentistry comprising organic or organo-metallic additives
- A61K6/69—Medicaments
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K6/00—Preparations for dentistry
- A61K6/70—Preparations for dentistry comprising inorganic additives
- A61K6/71—Fillers
- A61K6/76—Fillers comprising silicon-containing compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/20—Halogens; Compounds thereof
- A61K8/21—Fluorides; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/24—Phosphorous; Compounds thereof
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Inorganic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Birds (AREA)
- Cosmetics (AREA)
- Dental Preparations (AREA)
- Medicinal Preparation (AREA)
Abstract
DENTAL THIXOTROPIC FLUORIDE-PHOSPHATE COMPOSITION
Abstract of the Disclosure A fluoride-phosphate dental composition, for topical application to the teeth for the control and pre-vention of dental caries, which is comprised of active fluoride and phosphate ions in an acid solution with a thixotropic carrier which imparts gel-like properties to the resulting composition. The thixotropic properties of the carrier enable the composition to be handled like a liquid during filling and dispensing by simple agitation of the mixture whereas, when held stationary, the solution sets up very quickly into a gel-like material which enables it to be applied to and retained by a dental applicator tray when inserted in a patient's mouth. The fluoride-phosphate composition, besides its thixotropic gel-like characteristics, is heat- and acid-stable, deep-penetrating to the inter-proximal surfaces of the teeth and, following set up, will not drip, run or thin out in use, even when used in an inverted tray to treat the lower teeth. In a preferred embodiment the carrier comprises about 10% by weight of the total composition of complex colloidal magnesium aluminum silicate to provide thixotropic properties, and about 1% by weight silica dioxide powder used as an acid-stabilizing and thickening agent, either alone or with additional thickening agents provided, if desired, by carboxymethyl cellulose, hydroxyethyl cellulose or other cellulose gums. Sweeteners, flavoring and coloring agents are also included to improve the appearance, taste and acceptability of the fluoride "gel" composition.
Abstract of the Disclosure A fluoride-phosphate dental composition, for topical application to the teeth for the control and pre-vention of dental caries, which is comprised of active fluoride and phosphate ions in an acid solution with a thixotropic carrier which imparts gel-like properties to the resulting composition. The thixotropic properties of the carrier enable the composition to be handled like a liquid during filling and dispensing by simple agitation of the mixture whereas, when held stationary, the solution sets up very quickly into a gel-like material which enables it to be applied to and retained by a dental applicator tray when inserted in a patient's mouth. The fluoride-phosphate composition, besides its thixotropic gel-like characteristics, is heat- and acid-stable, deep-penetrating to the inter-proximal surfaces of the teeth and, following set up, will not drip, run or thin out in use, even when used in an inverted tray to treat the lower teeth. In a preferred embodiment the carrier comprises about 10% by weight of the total composition of complex colloidal magnesium aluminum silicate to provide thixotropic properties, and about 1% by weight silica dioxide powder used as an acid-stabilizing and thickening agent, either alone or with additional thickening agents provided, if desired, by carboxymethyl cellulose, hydroxyethyl cellulose or other cellulose gums. Sweeteners, flavoring and coloring agents are also included to improve the appearance, taste and acceptability of the fluoride "gel" composition.
Description
10925i~
THIXOTROPIC TOPICAL FLUORIDE-PHOSPHATE
"GEL" COMPOSITIONS USEFUL FOR THE
PREVENTION OF DENTAL CARIES
Background of the Invention - -~ . .
This invention relates to improvements in fluoride-phosphate compositions for topical application to the teeth -for the control and prevention of dental caries. More parti-cularly, the present invention is directed to an improved thixotropic solution having gel-like handling characteristics which has acid and heat stability, and other desirable properties for use in the formulation of a gel-like topical fluoride-phosphate dental composition. The thixotropic agents disclosed herein are solutions rather than true gels, but when immobilized for a short period of time they set up and assume a gel-like appearance which, however, is fully reversible as the composition can readily be returned to a fluid state by simple agitation. ;~-For convenience of reference, and because of the similarities in certain particulars, specifically their end application, the -therapeutic dental fluoride gel-like compositions of the present invention will be referred to hereinafter in abbreviated form as fluoride "gels".
In Elbreder U.S. patent 3,337,412 there is dis-closed various topical fluoride-phosphate gel compositions ;
useful in the control and prevention of dental caries which are comprised of a fluoride component, an acid phosphate component `- ~
and a gelling agent. The gelling agents disclosed by Elbreder ;~ - -as being useful in the composition of such fluoride gels, include those of the cellulose type, e.g. hydroxyethyl cellulose and carboxymethyI cellulose, and silica-based gelling agents such as magn~sium aluminum silicate and silica aerogel. The gelling agents indicated by Elbreder as being suitable are those which possess the
THIXOTROPIC TOPICAL FLUORIDE-PHOSPHATE
"GEL" COMPOSITIONS USEFUL FOR THE
PREVENTION OF DENTAL CARIES
Background of the Invention - -~ . .
This invention relates to improvements in fluoride-phosphate compositions for topical application to the teeth -for the control and prevention of dental caries. More parti-cularly, the present invention is directed to an improved thixotropic solution having gel-like handling characteristics which has acid and heat stability, and other desirable properties for use in the formulation of a gel-like topical fluoride-phosphate dental composition. The thixotropic agents disclosed herein are solutions rather than true gels, but when immobilized for a short period of time they set up and assume a gel-like appearance which, however, is fully reversible as the composition can readily be returned to a fluid state by simple agitation. ;~-For convenience of reference, and because of the similarities in certain particulars, specifically their end application, the -therapeutic dental fluoride gel-like compositions of the present invention will be referred to hereinafter in abbreviated form as fluoride "gels".
In Elbreder U.S. patent 3,337,412 there is dis-closed various topical fluoride-phosphate gel compositions ;
useful in the control and prevention of dental caries which are comprised of a fluoride component, an acid phosphate component `- ~
and a gelling agent. The gelling agents disclosed by Elbreder ;~ - -as being useful in the composition of such fluoride gels, include those of the cellulose type, e.g. hydroxyethyl cellulose and carboxymethyI cellulose, and silica-based gelling agents such as magn~sium aluminum silicate and silica aerogel. The gelling agents indicated by Elbreder as being suitable are those which possess the
- 2 -X '~ ' ``` 109~512 characteristics of being substantially acid-stable in a pH
range of approximately 1.8 to 4.5, compatible with fluoride under such acid conditions, and impart a viscosity to the resultant fluoride gel composition of between approximately 7000 and lO0,000 centipoises.
While fluoride gel compositions of the type dis-closed by Elbreder have been widely adopted for use in the treatment and control of dental caries, it has been found that there are certain practical and clinical disadvantages present in the Elbreder-type product resulting from inherent deficiencies in the gelling agent selected. Specifically, because of the relatively high viscosity of the Elbreder-type cellulose and silica-based gelling agents, it is difficult ;
for the user to conveniently, uniformly and completely dispense the product from the packaging container onto the individual applicator tray prior to its insertion into the mouth of the patient. The same high viscosity characteristlc of the gelling agent, which enahles the fluoride gel composi-tion to adhere well to the teeth and applicator tray and not thin out in the pres~;lce of saliva and run down into the throat, operates ~gainst the composition's having sufficient n flowability to -dequat41y penetrate and protect the inter-proximal surfaces of the teeth. Further, it has been found ~
that cellulose and silica-type gelling agents of the type ~ ~-disclosed by Elbreder tend to be unstable in the presence of the highly acid environment of the fluoride-phosphate gel composition and tend to thin out with the passage of time if l0~%si2 not refrigerated, thus reducing the useful shelf life of the product.
Su~mary of the Invention The present invention is directed to an improved agent for use in the formulation of topical dental fluoride compositions which substitutes, for the cellulose and silica-type gels disclosed by Elbreder, a gel-like solution having thixo-tropic properties. By simple agitation of the thixotropic composition, such as by manually shaking the bottle or other bulk container in which it is stored, the viscosity of the composition is greatly reduced so that the material becomes readily flowable and liquid-like, thus enabling it to be readily and uniformly dispensed by the user into individual 15 applicator trays. From a preparation standpoint the thixo- ; ~-~
tropic properties imparted to the fluoride "gel" by the compo-sition of the present invention permit the speedy dispensing -;~
of the material into bulk containers and later into individual applicator trays, as a liquid-like material is being dealt 20 with in the filling and dispensing procedure rather than a ' `
highly viscous gel. This greatly facilitates the feasibility of factory pre-packaging of the composition in single-use individual applicator trays which are filled with "gel" and then sealed with a removable lid prior ~o shipment to the customer. Alternatively, the "gel" because of its thixotropic .. , ~
, . : . , . : ,.. .. - , .. .
~os2s~2 property can be conveniently dispensed as needed into individual trays from a bulk container at the dentist's office.
Once dispensed into the applicator tray, either in the factory or at the dentist's office, as the thixotropic material is allowed to remain at rest it sets up in a very short time span, on the order of a few seconds, into a highly viscous gel-like material so that, when the tray is inserted into the oral cavity, even in an inverted position against the teeth of the lower jaw, the fluoride "gel" composition remains in the tray, adhering to the teeth, including the inter-proximal surfaces not usually reached by conventional gels, and does not tend to thin out, drip or run down into the mo~th and throat. ~This non-drip, non-run property is a very important characteristic for a topical fluoride dental composition as it has been found that ingestion of the com-position by patients in many cases causes retching, regurgita-tion and peristaltic cramps.) In addition, the improved dental fluoride gel-like composition disclosed herein is highly heat and acid stable for substantial periods of time, thus materially lengthening its shelf life. Further, the thixotropic composition of the present invention has been .~ - , found, from empirical subjective observations, to greatly - enhance the flavor characteristics of the flavoring agent typically employed in fluoride gels to mask out the bitter taste of the acid constituent of the composition. This ~, ,.
::: - . . - - , . . - , . .
flavor-enhancement property permits a material reduction in the amount of flavoring agent required to achieve equivalent flavor masking effects.
A principal objective of the present invention is to provide a fluoride-phosphate dental composition, useful for topical application to the teeth for the control of dental caries, comprising a fluoride compound which is soluble in water to provide a source of fluoride ions under acid condi-tions, an acid phosphate compound which is soluble in water to provide a source of phosphate ions, a thixotropic consti-tuent which serves to impart thixotropic gel-lil;e properties to the resulting composition, said thixotropic constituent being compatible with fluoride ions under acid conditions and stable in a pH range of approximately 3.0 to 5.0 and being within the range of 3.5 to 12% by weight of said fluoride-phosphate composition, and water.
Detailed Description of the Invention The present invention èmploys as a preferred thixotropic agent, in the formulation of topical fluoride-phosphate "gel" compositions of the type described, a complex colloidal magnesium aluminum silicate gum, either alone or in mixtures with relatively small amounts of thickening and/or stabilizing agents. In a preferred embodiment the thixotropic agent, comprised of the mixture of complex colloidal magnesium aluminum silicate and a fumed silica dioxide powder in a ten to one ratio, comprises only about eleven percent by weight of the resultant fluoride "gel" composition.
Because of the apparent high viscosity imparted to the 30 resultant composition by the thixotropic gum constituent, ~ ;
.--: ,: ,. - : : . : : .
it has been found that a lesser quantity of this agent n~ed be employed to obtain the desired degree of set up of - the "~el" in the mouth, as compared to the conventional, non-thixotropic gelling agents disclosed by Elbreder. One gum found especially suitable as the thixotropic constituent for the "gel" mixture herein disclosed is the complex colloidal magnesium al~minum silicate product which is marketed under the trade mark "VEEGUM" by R.T. Vanderbilt Company, -.
Inc., of New York, New York. Among the cellulose gums found ~ -10 suitable for use as thickening agents in the mixture are -carboxymethyl cellulose and hydroxyethyl cellulose, one suitable form of the latter being that marketed under the `
trade mark "METHOC~L" by Dow Chemical Company, of Midland, Michigan. However, cellulose gum thicke~ers - -;
.
15- have been found to be not altogether satisfactory in certain formulations and applications as the low pH of~the resultant ~ -fluoride "gel" composition, on the order of 3.0 to 5.0, causes l~ -the gum to hydrolyze, thus rendering the mixture unstable in ; time and reducing its effective shelf life. To overcome 20 this problem encountered with cellulose-type thickeners it `~
has been found that better results are obtained by including in the "gelling" mixture, either together with or as a substitute for the cellulose gum, about 1% by weight of -fumed silica dioxide microni~ed particulate which acts as a 25 stabilizer to retain moisture and prevent separation of the - ¦`
"gel" composition in its high acid medium. The silica particulate is also slightly thixotropic in its own right and thus its presence improves this desired property in the resultant "gel" composition. One form o~ fumed silica dioxide found suitable for this specialized application is a 1, ~7 ~ -7' ' ~ ~
lO9Z512 pharmaceutical grade 5, 0.3 micron mesh powder marketed under tlle trade mar~ "CABOSIL" by Cabot Corporation, of Boston, Massachusetts.
It has been found that the useful range for the thixotropic constituent of the mixture is 3.5 to 12% by weight of the total fluoride"gel" composition. Below about
range of approximately 1.8 to 4.5, compatible with fluoride under such acid conditions, and impart a viscosity to the resultant fluoride gel composition of between approximately 7000 and lO0,000 centipoises.
While fluoride gel compositions of the type dis-closed by Elbreder have been widely adopted for use in the treatment and control of dental caries, it has been found that there are certain practical and clinical disadvantages present in the Elbreder-type product resulting from inherent deficiencies in the gelling agent selected. Specifically, because of the relatively high viscosity of the Elbreder-type cellulose and silica-based gelling agents, it is difficult ;
for the user to conveniently, uniformly and completely dispense the product from the packaging container onto the individual applicator tray prior to its insertion into the mouth of the patient. The same high viscosity characteristlc of the gelling agent, which enahles the fluoride gel composi-tion to adhere well to the teeth and applicator tray and not thin out in the pres~;lce of saliva and run down into the throat, operates ~gainst the composition's having sufficient n flowability to -dequat41y penetrate and protect the inter-proximal surfaces of the teeth. Further, it has been found ~
that cellulose and silica-type gelling agents of the type ~ ~-disclosed by Elbreder tend to be unstable in the presence of the highly acid environment of the fluoride-phosphate gel composition and tend to thin out with the passage of time if l0~%si2 not refrigerated, thus reducing the useful shelf life of the product.
Su~mary of the Invention The present invention is directed to an improved agent for use in the formulation of topical dental fluoride compositions which substitutes, for the cellulose and silica-type gels disclosed by Elbreder, a gel-like solution having thixo-tropic properties. By simple agitation of the thixotropic composition, such as by manually shaking the bottle or other bulk container in which it is stored, the viscosity of the composition is greatly reduced so that the material becomes readily flowable and liquid-like, thus enabling it to be readily and uniformly dispensed by the user into individual 15 applicator trays. From a preparation standpoint the thixo- ; ~-~
tropic properties imparted to the fluoride "gel" by the compo-sition of the present invention permit the speedy dispensing -;~
of the material into bulk containers and later into individual applicator trays, as a liquid-like material is being dealt 20 with in the filling and dispensing procedure rather than a ' `
highly viscous gel. This greatly facilitates the feasibility of factory pre-packaging of the composition in single-use individual applicator trays which are filled with "gel" and then sealed with a removable lid prior ~o shipment to the customer. Alternatively, the "gel" because of its thixotropic .. , ~
, . : . , . : ,.. .. - , .. .
~os2s~2 property can be conveniently dispensed as needed into individual trays from a bulk container at the dentist's office.
Once dispensed into the applicator tray, either in the factory or at the dentist's office, as the thixotropic material is allowed to remain at rest it sets up in a very short time span, on the order of a few seconds, into a highly viscous gel-like material so that, when the tray is inserted into the oral cavity, even in an inverted position against the teeth of the lower jaw, the fluoride "gel" composition remains in the tray, adhering to the teeth, including the inter-proximal surfaces not usually reached by conventional gels, and does not tend to thin out, drip or run down into the mo~th and throat. ~This non-drip, non-run property is a very important characteristic for a topical fluoride dental composition as it has been found that ingestion of the com-position by patients in many cases causes retching, regurgita-tion and peristaltic cramps.) In addition, the improved dental fluoride gel-like composition disclosed herein is highly heat and acid stable for substantial periods of time, thus materially lengthening its shelf life. Further, the thixotropic composition of the present invention has been .~ - , found, from empirical subjective observations, to greatly - enhance the flavor characteristics of the flavoring agent typically employed in fluoride gels to mask out the bitter taste of the acid constituent of the composition. This ~, ,.
::: - . . - - , . . - , . .
flavor-enhancement property permits a material reduction in the amount of flavoring agent required to achieve equivalent flavor masking effects.
A principal objective of the present invention is to provide a fluoride-phosphate dental composition, useful for topical application to the teeth for the control of dental caries, comprising a fluoride compound which is soluble in water to provide a source of fluoride ions under acid condi-tions, an acid phosphate compound which is soluble in water to provide a source of phosphate ions, a thixotropic consti-tuent which serves to impart thixotropic gel-lil;e properties to the resulting composition, said thixotropic constituent being compatible with fluoride ions under acid conditions and stable in a pH range of approximately 3.0 to 5.0 and being within the range of 3.5 to 12% by weight of said fluoride-phosphate composition, and water.
Detailed Description of the Invention The present invention èmploys as a preferred thixotropic agent, in the formulation of topical fluoride-phosphate "gel" compositions of the type described, a complex colloidal magnesium aluminum silicate gum, either alone or in mixtures with relatively small amounts of thickening and/or stabilizing agents. In a preferred embodiment the thixotropic agent, comprised of the mixture of complex colloidal magnesium aluminum silicate and a fumed silica dioxide powder in a ten to one ratio, comprises only about eleven percent by weight of the resultant fluoride "gel" composition.
Because of the apparent high viscosity imparted to the 30 resultant composition by the thixotropic gum constituent, ~ ;
.--: ,: ,. - : : . : : .
it has been found that a lesser quantity of this agent n~ed be employed to obtain the desired degree of set up of - the "~el" in the mouth, as compared to the conventional, non-thixotropic gelling agents disclosed by Elbreder. One gum found especially suitable as the thixotropic constituent for the "gel" mixture herein disclosed is the complex colloidal magnesium al~minum silicate product which is marketed under the trade mark "VEEGUM" by R.T. Vanderbilt Company, -.
Inc., of New York, New York. Among the cellulose gums found ~ -10 suitable for use as thickening agents in the mixture are -carboxymethyl cellulose and hydroxyethyl cellulose, one suitable form of the latter being that marketed under the `
trade mark "METHOC~L" by Dow Chemical Company, of Midland, Michigan. However, cellulose gum thicke~ers - -;
.
15- have been found to be not altogether satisfactory in certain formulations and applications as the low pH of~the resultant ~ -fluoride "gel" composition, on the order of 3.0 to 5.0, causes l~ -the gum to hydrolyze, thus rendering the mixture unstable in ; time and reducing its effective shelf life. To overcome 20 this problem encountered with cellulose-type thickeners it `~
has been found that better results are obtained by including in the "gelling" mixture, either together with or as a substitute for the cellulose gum, about 1% by weight of -fumed silica dioxide microni~ed particulate which acts as a 25 stabilizer to retain moisture and prevent separation of the - ¦`
"gel" composition in its high acid medium. The silica particulate is also slightly thixotropic in its own right and thus its presence improves this desired property in the resultant "gel" composition. One form o~ fumed silica dioxide found suitable for this specialized application is a 1, ~7 ~ -7' ' ~ ~
lO9Z512 pharmaceutical grade 5, 0.3 micron mesh powder marketed under tlle trade mar~ "CABOSIL" by Cabot Corporation, of Boston, Massachusetts.
It has been found that the useful range for the thixotropic constituent of the mixture is 3.5 to 12% by weight of the total fluoride"gel" composition. Below about
3.5% the amount of this constituent is sufficiently small that it does no~ impart any substantial thixotropic property to the overall composition; on the other hand, amounts of 10 this constituent above the indicated upp~r range causes the ~ -~
resultant fluoride "gel" composition to become pasty and :
highly viscous, with a constituency similar to toothpaste, so that the composition does not break up and exhibit the deslred fluid characteristics when agitated.~
: 15 . The preferred formulation for the thixotropic fluoride "gel" composition, in accordance w1~h the;teachings of tne present inventioD, comprises the follow;ing~percentage~
by weight constituents: ~ :
Component Percentage by Weight 20 Actives: : . ~ ;
1.24 Fluoride Ions Sodium fluoride USP powder ~ 2.6 Hydrofluoric acid AR 48% 0.2 Excipients:
25. VEEGUM HS c~omplex colloidal ` magnesium aluminum silicate . 10.0 ~ CABOSIL micronized superfine ::~ fumed silica dioxide powder, ~:
. . pharmaceutical grade M5 1.0 .Phosphoric acid 75~, food grade 1.3 Sodium saccharin NF (sweetener) 0.2 30 . . -Trace amounts of coloring and flavoring agents --:Distilled Wat-er 84.7 100.0 , . .:. ., . . . ... . ... , Q
` -lO9Z5~2 The thixotropic agent and resulting gel-like material are formulated according to the following procedure:
The VEEGUM and CABOSIL constituents are hydrated in hot distilled water. Sodium fluoride powder is added, together with a solution of coloring agent and sodium saccharin sweetener, and flavoring is then added. The -~
solution is blended well and next the phosphoric and hydro-fluoric acids are added with sufficient distilled water to ~ -dilute the solution to volume. Then the solution is thoroughly mixed until homogeneous, the pH level checked and, if necessary, sufficient phosphoric acid added to adjust the pH to lie within the range of 3.0 to 4Ø
.
Since, as is generally known, thixotropic composi-tions exhibit non-Newtonian flow patterns, see for example the pamphlet entitled "VEEGUM," Bulletin No. 32, published by R.T. Vanderbilt Company, Inc., it is not possible to conveniently measure or describe in quantitative terms the viscosity characteristics of such compositions, as their viscosity is relative to the method of measurement employed and other measurement variables. Accordingly, it is not meaningful to set forth any specifications as to the viscosity characteristics exhibited by the improved thixotropic fluoride "gel" compositions of the present invention.
The above-formulated fluoride "gel" composition, as previously mentioned, sets up very quickly, on the order of only a few seconds, so that immediately after the composition -is dispensed into an applicator tray the tray can be turned upside down and no dripping or running of "gel" can be ~; -observed, even after five minutes or longer duration.
When the formulation of the thixotropic or other ~-::: -: . : - .
- -:: ~ . .: . . . ~ ,: . -iO925~Z
"gelling" constituents is substantially varied from that set out above it has been found that certain deterioration in desired properties for the "gel" composition result. Speci-fically, if the percentage of VEEGUM complex colloidal mag-nesium aluminum silicate is matsrially reduced from thepreferred level of 10%, then the resultant "gel" does not exhibit the desired thixotropic property and does not set up quickly when dispensed for use. On the other hand, as pre-viously mentioned, too much of the thixotropic constituent, above about 12%, produces a pasty, too viscous mixture.
The presence of a stabilizer such as the CABOSIL
silica dioxide powder is also important as, when a cellulose gum thickener is used alone, the resulting "gel" is somewhat acid-unstable and will tend to break up and separate in time.
It will be understood that thixotropic gums other than the complex colloidal magnesium aluminum silicate referred to herein may be suitably used as the thixotropic component of the fluoride "gel" composition. Also, "gel"
thickeners and stabilizers other than the cellulose gums and silica dioxide powder disclosed herein may be suitably used in dental compositions formulated in accordance with the teachings of the present invention.
As various changes could be made in the thixotropic topical fluoride-phosphate "gel" compositions disclosed herein without departing from the scope of the present invention, it is intended that all matter contained in the above description shall be interpreted as illustrative and not in a limiting sense.
The terms and expressions which have been employed in the foregoing abstract and specification are used therein as terms of description and not of limitation, and there is ~10 ~,: ~ . ... . .
, , .~. .
10925~Z
no intention, in the use of such terms and expressions, of excluding equivalents of the features shown and described or portions thereof, it being recognized that the scope of the invention is defined and limited only by the claims ~.
5 which follow. ~ ;
11 ~
resultant fluoride "gel" composition to become pasty and :
highly viscous, with a constituency similar to toothpaste, so that the composition does not break up and exhibit the deslred fluid characteristics when agitated.~
: 15 . The preferred formulation for the thixotropic fluoride "gel" composition, in accordance w1~h the;teachings of tne present inventioD, comprises the follow;ing~percentage~
by weight constituents: ~ :
Component Percentage by Weight 20 Actives: : . ~ ;
1.24 Fluoride Ions Sodium fluoride USP powder ~ 2.6 Hydrofluoric acid AR 48% 0.2 Excipients:
25. VEEGUM HS c~omplex colloidal ` magnesium aluminum silicate . 10.0 ~ CABOSIL micronized superfine ::~ fumed silica dioxide powder, ~:
. . pharmaceutical grade M5 1.0 .Phosphoric acid 75~, food grade 1.3 Sodium saccharin NF (sweetener) 0.2 30 . . -Trace amounts of coloring and flavoring agents --:Distilled Wat-er 84.7 100.0 , . .:. ., . . . ... . ... , Q
` -lO9Z5~2 The thixotropic agent and resulting gel-like material are formulated according to the following procedure:
The VEEGUM and CABOSIL constituents are hydrated in hot distilled water. Sodium fluoride powder is added, together with a solution of coloring agent and sodium saccharin sweetener, and flavoring is then added. The -~
solution is blended well and next the phosphoric and hydro-fluoric acids are added with sufficient distilled water to ~ -dilute the solution to volume. Then the solution is thoroughly mixed until homogeneous, the pH level checked and, if necessary, sufficient phosphoric acid added to adjust the pH to lie within the range of 3.0 to 4Ø
.
Since, as is generally known, thixotropic composi-tions exhibit non-Newtonian flow patterns, see for example the pamphlet entitled "VEEGUM," Bulletin No. 32, published by R.T. Vanderbilt Company, Inc., it is not possible to conveniently measure or describe in quantitative terms the viscosity characteristics of such compositions, as their viscosity is relative to the method of measurement employed and other measurement variables. Accordingly, it is not meaningful to set forth any specifications as to the viscosity characteristics exhibited by the improved thixotropic fluoride "gel" compositions of the present invention.
The above-formulated fluoride "gel" composition, as previously mentioned, sets up very quickly, on the order of only a few seconds, so that immediately after the composition -is dispensed into an applicator tray the tray can be turned upside down and no dripping or running of "gel" can be ~; -observed, even after five minutes or longer duration.
When the formulation of the thixotropic or other ~-::: -: . : - .
- -:: ~ . .: . . . ~ ,: . -iO925~Z
"gelling" constituents is substantially varied from that set out above it has been found that certain deterioration in desired properties for the "gel" composition result. Speci-fically, if the percentage of VEEGUM complex colloidal mag-nesium aluminum silicate is matsrially reduced from thepreferred level of 10%, then the resultant "gel" does not exhibit the desired thixotropic property and does not set up quickly when dispensed for use. On the other hand, as pre-viously mentioned, too much of the thixotropic constituent, above about 12%, produces a pasty, too viscous mixture.
The presence of a stabilizer such as the CABOSIL
silica dioxide powder is also important as, when a cellulose gum thickener is used alone, the resulting "gel" is somewhat acid-unstable and will tend to break up and separate in time.
It will be understood that thixotropic gums other than the complex colloidal magnesium aluminum silicate referred to herein may be suitably used as the thixotropic component of the fluoride "gel" composition. Also, "gel"
thickeners and stabilizers other than the cellulose gums and silica dioxide powder disclosed herein may be suitably used in dental compositions formulated in accordance with the teachings of the present invention.
As various changes could be made in the thixotropic topical fluoride-phosphate "gel" compositions disclosed herein without departing from the scope of the present invention, it is intended that all matter contained in the above description shall be interpreted as illustrative and not in a limiting sense.
The terms and expressions which have been employed in the foregoing abstract and specification are used therein as terms of description and not of limitation, and there is ~10 ~,: ~ . ... . .
, , .~. .
10925~Z
no intention, in the use of such terms and expressions, of excluding equivalents of the features shown and described or portions thereof, it being recognized that the scope of the invention is defined and limited only by the claims ~.
5 which follow. ~ ;
11 ~
Claims (6)
1. A fluoride-phosphate dental composition useful for topical application to the teeth for the control of dental caries, comprising a fluoride compound which is soluble in water to provide a source of fluoride ions under acid con-ditions, an acid phosphate compound which is soluble in water to provide a source of phosphate ions, a thixotropic constituent, and water, said thixotropic constituent serving to impart thixotropic gel-like properties to the resulting fluoride-phosphate composition so that it possesses a viscosity between approximately 7,000 and 100,000 centipoises, said composition exhibiting fluid properties when agitated so as to facilitate its dispensation from a bulk container into a dental applicator tray but, when immobilized, sets up on the tray in a few seconds into a gel-like substance which, when followed by inversion and insertion of the tray in the mouth cavity over the lower teeth, will not trip, run or thin out in the presence of saliva for a sustained period of time of at least five minutes duration, and said thixotropic constituent being compatible with fluoride ions under acid conditions and stable in pH range of approximately 3.0 to 4.5 and being within the range of 3.5 to 12% by weight of said fluoride-phosphate composition.
2 The fluoride-phosphate dental composition of claim 1 wherein said thixotropic constituent is comprised of about 10% by weight of complex colloidal magnesium aluminum silicate.
3. The fluoride-phosphate dental composition of claim 2 wherein said thixotropic constituent further comprises an acid-stabilizing and thickening agent serving to promote longer shelf life and to prevent separation in said resulting gel-like composition.
4. The fluoride-phosphate dental composition of claim 3 wherein said stabilizing and thickening agent comprises about 1% by weight of fumed silica dioxide micronized particulate.
5. The fluoride-phosphate dental composition of claim 1 wherein said thixotropic constituent is comprised of about 10% by weight of complex colloidal magnesium aluminum silicate and about 1% by weight of fumed silica dioxide micronized particulate.
6. The fluoride-phosphate dental composition of claim 1 wherein said dental composition further includes sweetening, coloring and flavoring agents to improve the appearance, taste and acceptability of said composition to patient users.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US62606875A | 1975-10-28 | 1975-10-28 | |
| US626,068 | 1975-10-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1092512A true CA1092512A (en) | 1980-12-30 |
Family
ID=24508818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA255,446A Expired CA1092512A (en) | 1975-10-28 | 1976-06-22 | Dental thixotropic flucride-phosphate composition |
Country Status (4)
| Country | Link |
|---|---|
| AU (1) | AU502755B2 (en) |
| CA (1) | CA1092512A (en) |
| GB (1) | GB1551388A (en) |
| MX (1) | MX4362E (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ204974A (en) * | 1982-08-02 | 1985-10-11 | Johnson & Johnson Dental Prod | Thickened aqueous sodium fluoride compositions for dental care |
| US4419346A (en) * | 1982-08-13 | 1983-12-06 | Nabisco Brands, Inc. | Method and composition to inhibit the growth of Streptococcus mutans by the use of saccharin/fluoride combination |
| EP0106442B1 (en) * | 1982-08-24 | 1988-10-05 | National Research Development Corporation | Fluoride-containing compositions |
| NL8801087A (en) * | 1988-04-26 | 1989-11-16 | Explore | ANTI-MICROBIAL PREPARATION WITH LONG-TERM EFFICACY. |
-
1976
- 1976-06-22 CA CA255,446A patent/CA1092512A/en not_active Expired
- 1976-06-30 MX MX76910U patent/MX4362E/en unknown
- 1976-07-08 GB GB28408/76A patent/GB1551388A/en not_active Expired
- 1976-08-18 AU AU16953/76A patent/AU502755B2/en not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| AU1695376A (en) | 1978-02-23 |
| MX4362E (en) | 1982-04-19 |
| AU502755B2 (en) | 1979-08-09 |
| GB1551388A (en) | 1979-08-30 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US4267167A (en) | Thixotropic topical fluoride-phosphate gel compositions useful for the prevention of dental caries | |
| US5928628A (en) | Two-component dental bleaching system and method | |
| US4980154A (en) | Tooth and gum dentifrice composition and method of making same | |
| US3004897A (en) | Dental preparation | |
| US5372802A (en) | Stabilized peroxide gels containing fluoride | |
| US5073363A (en) | Foamable fluoride gels and method | |
| US5208010A (en) | Tooth whitening dentifrice | |
| US6447757B1 (en) | Teeth whitening composition with increased bleaching efficiency and storage stability | |
| JP5121800B2 (en) | Anti-caries chewing gum, candy, gel, toothpaste and dentifrice | |
| US4897258A (en) | Periodontal composition and method | |
| US6511654B2 (en) | Starch thickened non-aqueous dentifrices | |
| US8574555B2 (en) | Stable one-part aqueous tooth whitening composition | |
| JPS6330881B2 (en) | ||
| US5071637A (en) | Foamable fluoride compositions and method | |
| JP5714202B2 (en) | Stabilized oxygen release composition | |
| JPH04257511A (en) | Antibacterial oral composition free from pollution | |
| US5690912A (en) | SnF2 gel of improved stand-up and efficacy in the treatment of dentine hypersensitivity | |
| IE55409B1 (en) | Neutral topical sodium fluoride gel | |
| CA1092512A (en) | Dental thixotropic flucride-phosphate composition | |
| US4415550A (en) | Treatment-and-prophylactic tooth paste possessing anticarious effect | |
| US4540576A (en) | Neutral topical sodium fluoride gel | |
| JP3479823B2 (en) | Toothpaste composition | |
| US20200085864A1 (en) | Stannous Fluoride Sugar Alcohol Solid Solutions | |
| JPS6043322B2 (en) | Oral composition | |
| JP4703904B2 (en) | Oral composition |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKEX | Expiry |