Oral compositions for plaque, caries and calculus retardation with reduced staining tendencies

Claim 1

An oral composition effective in inhibiting the formation of plaque, caries and calculus, said composition comprising a carrier suitable for use in the oral cavity and from about 0.01% to about 2.5% by weight of a water-soluble bis-biguanide compound having the generic formula: ##STR8## wherein A and A' each are selected from the group consisting of (A) substituted and unsubstituted phenyl radicals wherein the substituents are selected from the group consisting of up to two groups selected from the group consisting of alkyl and alkoxy groups containing from 1 to about 4 carbon atoms, a nitro group, and a halogen atom; (B) an alkyl group containing from 1 to about 12 carbon atoms; and (C) alicyclic groups containing from 4 to about 12 carbon atoms; wherein X and X' each represent an alkylene radical containing from 1 to 3 carbon atoms; wherein z and z' each are selected from the group consisting of 0 and 1; wherein R and R' each are selected from the group consisting of hydrogen, an alkyl radical containing from 1 to about 12 carbon atoms, and on aralkyl radical containing from 7 to about 12 carbon atoms; wherein n is an integer from 2 to 12 inclusive; wherein the polymethylene chain (CH 2 ) n can be interrupted by up to 5 moieties selected from the group consisting of ether, thioether, phenyl, and naphthyl; wherein L is a number from about 1 to 4; and wherein Y is an anion which will form a pharmaceutically acceptable water-insoluble bis-biguanide compound, said anion being derived from a compound selected from the group consisting of bisulfites, polymaleates, phosphites, hypophosphites, perfluorooctanoates, silicates, sorbates, salicylates, maleates, tartrates, citrates, fumarates, ethylenediamine tetraacetates, iminodiacetates, cinnamates, thiocyanates, arginates, pyromellitates, tetracarboxybutyrates, benzoates, glutarates, perfluoropropionates and polyphosphonates selected from the group consisting of: ##STR9## wherein in both formulae R 1 and R 2 are selected from the group consisting of hydrogen and CH 2 OH; n is an integer of from 3 to 12; R 3 is selected from the group consisting of 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) and --CH 2 CH(PO 3 H 2 ) 2 ; and R 4 is selected from the group consisting of hydrogen, lower alkyl, amino, benzyl, halogen, hydroxyl, --CH 2 COOH, --CH 2 PO 3 H 2 , and -- CH 2 CH 2 PO 3 H 2 ; ##STR10## wherein R 5 , R 6 , R 7 , R 8 , R 9 , and R 10 are each selected from the group consisting of hydrogen and lower alkyl; ##STR11## wherein n is an integer from 3 to 9; ##STR12## carboxyphosphonates selected from the group consisting of ##STR13## ##STR14## wherein X and Y are each selected from the group consisting of hydrogen and hydroxy; and the condensation products of ammonia and phosphorous pentoxide, said condensation products consisting of the compounds ##STR15##