Oral composition for calculus retardation

Abstract

Oral compositions, such as toothpaste, mouthwash, and the like, containing certain polyphosphonic acids and their salts which retard dental calculus formation without damaging tooth structure.

What is claimed is: 
     
       1. .[.An oral.]. .Iadd.A dentifrice .Iaddend.composition effective in inhibiting the formation of dental calculus without adversely affecting tooth structure, comprising (1) from about .01% to about 10% by weight of a polyphosphonate selected from the group consisting of those of the formulae: ##STR3##wherein R 1  and R 2  are each hydrogen or CH 2  OH; n is an integer of from 3 to 10; R 3  is hydrogen, alkyl containing from 1 to about 20 carbon atoms, alkenyl containing from 2 to about 20 carbon atoms, phenyl, naphthyl, phenylethyl, benzyl, halogen, amino, dimethylamino, diethylamino, N-hydroxy-N-ethylamino, acetylamino, --CH 2  COOH --CH 2  PO 3  H 2 , --CH(PO 3  H 2 )(OH) or --CH 2  CH(PO 3  H 2 ) 2  R 4  is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl --CH 2  COOH, CH 2  PO 3  H 2 , or --CH 2  CH 2  PO 3  H 2  ; or a pharmaceutically acceptable salt thereof, and (2) .[.a carrier suitable for use in the oral cavity,.]. .Iadd.from about 0.5% to 95% by weight of an abrasive material, .Iaddend.the pH of the compositon being within the range from about 5.0 to 11.0, .Iadd.said composition being free of calcium abrasives which would yield enough soluble calcium to significantly impair the anticalculus activity of said polyphosphonate. .Iaddend.   
     
     
       2. The composition of claim 1 in which the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       3. The composition of claim 1 in which the polyphosphonate is methanediphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       4. The composition of claim 1 in which the polyphosphonate is methanedichlorodiphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       5. The composition of claim 1 in which the polyphosphonate is ethane-1-hydroxy-1,1,2-triphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       6. The composition of claim 1 in which the polyphosphonate is methanehydroxydiphosphonic acid or a pharamaceutically acceptable salt thereof. 
     
     
       7. The composition of claim 1 in which the polyphosphonate is propane-1,1,3,3-tetraphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       8. The composition of claim 1 in which the polyphosphonate is ethane-2-carboxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       9. The composition of claim 1 in which the polyphosphonate is ethane-1,1,2-triphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       10. The composition of claim 1 in which the polyphosphonate is ethane-1-amino-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       11. The composition of claim 1 in which the polyphosphonate is ethanedichlorodiphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       12. The composition of claim 1 in which the polyphosphonate is nonane-5,5-diphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       13. The composition of claim 1 in which the polyphosphonate is n-pentane-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       14. The composition of claim 1 in which the polyphosphonate is methanedibromodiphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       15. The composition of claim 1 in which the polyphosphonate is propane-1-hydroxy-1,1,3-triphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       16. The composition of claim 1 in which the polyphosphonate is propane-1,2,3-triphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       17. The composition of claim 1 in which the polyphosphonate is butane-1,2,3,4-tetraphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       18. The composition of claim 1 in which the polyphosphonate is hexane-1,2,3,4,5,6-hexaphosphonic acid or a pharmaceutically acceptable salt thereof. 
     
     
       19. A toothpaste composition comprising (1) from about 0.1% to about 5.0% by weight of a polyphosphonate selected from the group consisting of those of the formulae: ##STR4##wherein R 1  and R 2  are each hydrogen or CH 2  OH; n is an integer of from 3 to 10; R 3  is hydrogen, alkyl containing from 1 to about 20 carbon atoms, alkenyl containing from 2 to about 20 carbon atoms, phenyl, naphthyl, phenylethenyl, benzyl, halogen, amino, dimethylamino, diethylamino, N-hydroxy-N-ethylamino, acetylamino, --CH 2  COOH --CH 2  PO 3  H 2 , --CH(PO 3  H 2 )(OH) or --CH 2  CH(PO 3  H 2 ) 2  R 4  is hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH 2  COOH, --CH 2  PO 3  H 2 , or --CH 2  CH 2  PO 3  H 2  ; or a pharmaceutically acceptable salt thereof, and (2) from about 20% to about 60% by weight of an abrasive material, the pH of said composition being within the range from about 7 to about 10, .Iadd.said composition being free of calcium abrasives which would yield enough soluble calcium to significantly impair the anticalculus activity of said polyphosphonate. .Iaddend. 
     
     
       20. The composition of claim 19 in which the polyphosphonate is ethane-1-hydroxy-1,1-diphosphonic acid or a pharmaceutically acceptable salt thereof. .Iadd.21. The composition of claim 19 wherein the abrasive material is selected from the group consisting of β-phase calcium pyrophosphate, thermosetting polymerized resins, alumina and insoluble non-calcium metaphosphates. .Iaddend.