Self-gelling liquid composition for topical application in the oral cavity

Claim 2

A fluoride-containing, self-gelling aqueous composition for topical application on tooth surfaces in the oral cavity for the prevention of dental caries, which composition comprises in combination: (a) a low-viscosity, liquid, aqueous solution of a monomer or prepolymer ethyl orthosilicate in an amount to provide for the conversion of the liquid to a gel state; (b) a water-soluble fluoride compound in an amount to inhibit or prevent dental caries on topical application of the composition; and (c) a gelation agent in an amount to provide in situ self-gelation of the composition from a low-viscosity liquid composition to a gel state, on topical application of the liquid composition onto the surface of the teeth in a patient, the gelation from a liquid to a gel state occurring in a time period of about 1 hour or less after mixing by hydrolysis of the silicate.

Claim 3

The composition of claim 1 wherein the amount of the ethyl orthosilicate in the composition ranges from about 5% to 30% by weight.

Claim 4

The composition of claim 1 wherein the water-soluble fluoride is selected from the group consisting of sodium fluoride, potassium fluoride, ammonium fluoride and combinations thereof.

Claim 5

The composition of claim 1 wherein the water-soluble fluoride is present in an amount of from about 0.01 M to 1.5 M.

Claim 6

The composition of claim 1 wherein the gelation agent comprises from about 0.01% to 2% by weight of a surface-active agent.

Claim 7

The composition of claim 5 wherein the surface-active agent is selected from the group consisting of a sodium lauryl sulfate, a cetyl pyridinium halide, a nonionic polyoxyethylene derivative of fatty-acid partial esters of sorbitol anhydrides and combinations thereof.

Claim 8

The combination of claim 1 wherein the composition includes a buffering agent in an amount to provide for buffering of the pH of the solution from about 4.0 to 7.5.

Claim 9

The composition of claim 1 wherein the time from in situ gelation from a liquid to a gel state is about 10 minutes or less after admixing.

Claim 10

The composition of claim 1 which includes the addition of a viscosity-increasing agent in an amount of from about 0.01% to 1% by weight.

Claim 11

The composition of claim 1 wherein the monomer ethyl orthosilicate has been prepolymerized in an amount of up to 50%.

Claim 12

A self-gelling, fluoride-containing aqueous liquid composition for topical application and use on tooth surfaces in the oral cavity, which composition comprises: (a) a solution of an ethyl orthosilicate, which solution contains from about 5% to 30% by weight of the ethyl orthosilicate; (b) a water-soluble fluoride compound in an amount of from about 0.05 M to about 1.5 M; (c) a surface-active gelling agent in an amount of from about 0.01% to 2% of the composition; and (d) the composition characterized by being a low-viscosity aqueous liquid solution having a pH of from about 3 to 8.5 which, after mixing and on topical application of the liquid onto the surface of the teeth in the oral cavity of a patient, gels in situ to a gel state in a time period of from about 1 hour or less, thereby providing a solution which more readily will enter into the narrow spaces between the teeth and into conformity with the teeth surface and forming a gel state, to provide for the sustained release of the fluoride into the enamel of the teeth.

Claim 13

A self-gelling, fluoride-containing aqueous liquid composition for topical application and use on tooth surfaces in the oral cavity, which composition comprises: (a) a solution of an ethyl orthosilicate, which solution contains from about 5% to 30% by weight of the ethyl orthosilicate; (b) a water-soluble fluoride compound in an amount of from about 0.05 M to about 1.5 M; (c) a surface-active gelling agent in an amount of from about 0.01% to 2% of the composition; and (d) the composition characterized by being a low-viscosity aqueous liquid solution having a pH of from about 3 to 8.5 which, after mixing and on topical application of the liquid onto the surface of the teeth in the oral cavity of a patient, gels in situ to a gel state in a time period of from about 1 hour or less, thereby providing a solution which more readily will enter into the narrow spaces between the teeth and into conformity with the teeth surface and forming a gel state, to provide for the sustained release of the fluoride into the enamel of the teeth.

Claim 14

The composition of claim 11 wherein the water-soluble fluoride is selected from the group consisting of sodium fluoride, potassium fluoride, ammonium fluoride and combinations thereof.

Claim 17

The method of claim 13 wherein the ethyl orthosilicate comprises a tetraethyl orthosilicate monomer or prepolymer.

Claim 18

The method of claim 13 which includes vigorously admixing an aqueous solution containing the ethyl silicate and the water-soluble fluoride with a solution of the gelling agent.

Claim 19

The method of claim 13 wherein the gelling agent is selected from the group consisting of fluoride ions, ammonium ions, surface-active agents and combinations thereof in a sufficient amount, to provide, after mixing of the ingredients, the in situ conversion of the aqueous composition from a liquid to a substantially gel state in a time period of about 1 hour or less by hydrolysis of the silicate.

Claim 20

The method of claim 13 which includes employing in the self-gelling composition an aqueous neutral solution of a water-soluble fluoride.

Claim 21

The method of claim 13 wherein the self-gelling composition has a pH of from about 3 to 8.5.

Claim 22

A self-gelling aqueous composition for topical application in the oral cavity as a low-viscosity liquid and for sustained release of an active ingredient from a gel formed in situ in the oral cavity after application of the liquid, which aqueous composition comprises the following ingredients in combination: (a) a monomer or prepolymer hydrolyzable, alkyl orthosilicate in an amount to provide for the conversion of the liquid to a gel state; (b) an active ingredient comprising a water-soluble fluoride compound in an amount to inhibit dental caries; and (c) a gelling agent selected from the group consisting of fluoride ions, ammonium ions, surface-active agents and combinations thereof in a sufficient amount, to provide, after mixing of the ingredients, the in situ conversion of the aqueous composition from a liquid to a substantially gel state in a time period of about 1 hour or less by hydrolysis of the silicate.

Claim 23

A self-gelling aqueous composition for topical application in the oral cavity as a low-viscosity liquid and for sustained release of an active ingredient from a gel formed in situ in the oral cavity after application of the liquid, which aqueous composition comprises the following ingredients in combination: (a) a monomer or prepolymer hydrolyzable, alkyl orthosilicate in an amount to provide for the conversion of the liquid to a gel state; (b) an active ingredient comprising a water-soluble fluoride compound in an amount to inhibit dental caries; and (c) a gelling agent selected from the group consisting of fluoride ions, ammonium ions, surface-active agents and combinations thereof in a sufficient amount, to provide, after mixing of the ingredients, the in situ conversion of the aqueous composition from a liquid to a substantially gel state in a time period of about 1 hour or less by hydrolysis of the silicate.

Claim 24

The composition of claim 19 having a pH range of from about 3 to 8.5.

Claim 25

The composition of claim 19 wherein the silicate is selected from the group consisting of a tetraethyl orthosilicate, an aminopropyl triethyl orthosilicate and combinations thereof.

Claim 26

The composition of claim 19 wherein the water-soluble fluoride compound comprises ammonium fluoride.

Claim 27

The composition of claim 19 wherein the surface-active agent is selected from the group consisting of cetyl pyridinium halide, sodium lauryl sulfate, a nonionic polyoxyethylene derivative of fatty-acid partial esters of sorbitol anhydrides and combinations thereof.

Claim 28

The composition of claim 19 wherein the composition has a gel time of about 10 minutes or less.

Claim 29

The composition of claim 19 which includes ammonium phosphate.