Stabilized stannous compositions

Patent metadata

Field	Value
Publication number	US-10912722-B2
Application number	US-201415105748-A
Country	US
Kind code	B2
Filing date	Dec 24, 2014
Priority date	Dec 24, 2013
Publication date	Feb 9, 2021
Grant date	Feb 9, 2021

Abstract

The present invention relates to improved complexes of amorphous calcium phosphate and/or amorphous calcium fluoride phosphate stabilised by phosphopeptides/phosphoproteins by addition of stannous ions. These complexes have anticariogenic properties useful to protect tooth structures as they remineralize (repair) early stages of dental caries and have other dental/medical applications (including anti-calculus, anti-erosion/corrosion and anti-dentinal hypersensitivity). Methods of making the complexes of the invention and of treatment or prevention of various dental conditions including dental caries, dental calculus, dental erosion/corrosion and dental hypersensitivity are also provided.

First claim

The invention claimed is:

1. A stannous-associated phosphopeptide-stabilized amorphous calcium phosphate (ACP) and/or amorphous calcium fluoride phosphate (ACFP) complex having a stannous ion content of at least 1 mole of stannous per mole of phosphopeptide.

2. A stannous-associated phosphopeptide-stabilized amorphous calcium phosphate (ACP) and/or amorphous calcium fluoride phosphate (ACFP) complex according to claim 1 , wherein the complex has a stannous ion content of at least 5 moles of stannous per mole of phosphopeptide.

3. A stannous-associated phosphopeptide-stabilized amorphous calcium phosphate (ACP) and/or amorphous calcium fluoride phosphate (ACFP) complex according to claim 1 , wherein the complex has a stannous ion content of about 7 moles of stannous per mole of phosphopeptide.

4. A stannous-associated phosphopeptide-stabilized amorphous calcium phosphate (ACP) and/or amorphous calcium fluoride phosphate (ACFP) complex according to claim 1 , wherein the stannous is provided by a compound selected from the group consisting of stannous fluoride, stannous chloride, potassium stannous fluoride, sodium stannous fluorozirconate, stannous chloride fluoride, stannous acetate, sodium stannous fluoride, stannous hexafluorozirconate, stannous sulfate, stannous tartrate, stannous gluconate, and disodium monostannous citrate.

5. A stannous-associated phosphopeptide-stabilized amorphous calcium phosphate (ACP) and/or amorphous calcium fluoride phosphate (ACFP) complex according to claim 4 , wherein the compound is stannous fluoride.

6. A method of producing a stannous-associated phosphopeptide-stabilized amorphous calcium phosphate (ACP) or stannous-associated phosphopeptide-stabilized amorphous calcium fluoride phosphate (ACFP) complex according to claim 1 , comprising admixing CPP-ACP or CPP-ACFP, respectively, and a stannous compound in an aqueous solution, while maintaining the pH at about 6.5 or below, wherein the complex has a stannous ion content of at least 1 mole of stannous per mole of phosphopeptide.

7. An oral care formulation comprising a stannous-associated phosphopeptide-stabilized amorphous calcium phosphate (ACP) and/or amorphous calcium fluoride phosphate (ACFP) complex according to claim 1 .

8. An oral care formulation according to claim 7 , wherein the composition is in the form applicable to the mouth selected from the group consisting of dentifrice including toothpaste, toothpowder and liquid dentifrice, mouthwash, mouthrinse, mouth spray, varnish, dental cement, troche, chewing gum, dental paste, gingival massage cream, gargle tablet, dairy product and other foodstuffs.

9. An oral care formulation according to claim 8 , formulated as a dentifrice.

10. An oral formulation according to claim 9 , wherein the dentifrice is a toothpaste.

11. A method of mineralizing a dental surface or sub-surface, comprising contacting the dental surface or subsurface with a stannous-associated phosphopeptide-stabilized ACP or ACFP according to claim 1 .

12. A method according to claim 11 , wherein the dental surface is a lesion in the enamel caused by caries, dental erosion or fluorosis.

13. A method according to claim 11 , wherein the dental surface is exposed dentine causing dentinal hypersensitivity.

14. A method of forming a protective layer bonded to the surface of the tooth, wherein the layer comprises calcium and phosphate, the method comprising contacting the dental surface or subsurface with a stannous-associated phosphopeptide-stabilized ACP or ACFP according to claim 1 .

15. A method according to claim 14 , wherein the layer has a calcium:phosphate ratio equivalent to normal apatite.

16. A method according to claim 14 , wherein the layer contains peptides from casein phosphopeptides that stabilize the ACP or ACFP.

17. A method according to claim 14 , wherein the layer contains carbon, oxygen, fluoride, phosphate, calcium and stannous.

18. A method according to claim 17 , wherein the layer contains 20 to 30 wt % carbon, 35 to 45 wt % oxygen, 0.1 to 1 wt % fluoride, 8 to 12 wt % phosphate, 16 to 24 wt % calcium and 0.5 to 2 wt % stannous.

19. A stannous-associated phosphopeptide-stabilized amorphous calcium phosphate (ACP) and/or amorphous calcium fluoride phosphate (ACFP) complex according to claim 1 , wherein the phosphopeptide is casein phosphopeptide.

20. A stannous-associated phosphopeptide-stabilized amorphous calcium phosphate (ACP) and/or amorphous calcium fluoride phosphate (ACFP) complex according to claim 1 , wherein the ACP or ACFP in the complex is predominantly in a basic form.

Assignees

• Univ Melbourne

Inventors

• Reynolds Eric Charles

Classifications

• A61K33/24

  Heavy metals; Compounds thereof · CPC title

• A61K8/24

  Phosphorous; Compounds thereof · CPC title

• A61K6/74

  comprising phosphorus-containing compounds · CPC title

• A61K9/006

  Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays · CPC title

• A61Q11/00

  Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses · CPC title