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

The process of inhibiting bis-biguanide tooth-staining and dental plaque and caries, comprising the steps of:

• A. contacting the oral cavity with an effective amount of a composition comprising a carrier suitable for use in the oral cavity, and from about 0.01% to about 2.5% by weight of a tooth-staining bis-biguanide compound, otherwise tending to produce a rather offensive brown tooth stain upon continuous oral use, and having a generic formula:
• ##STR4## wherein A and A' each represent either (1) a phenyl radical which can contain as substituents up to two alkyl or alkoxy groups containing from 1 to about 4 carbon atoms, a nitro group, or a halogen atom;
• (2) an alkyl group containing from 1 to about 12 carbon atoms;
• or (3) 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 can be either 0 or 1;
• wherein R and R' each represent either hydrogen, an alkyl radical containing from 1 to about 12 carbon atoms, or an aralkyl radical containing from 7 to about 12 carbon atoms;
• wherein n is an integer from 2 to 12 inclusive;
• and wherein the polymethylene chain (CH.sub.2).sub.n can be interrupted by up to 5 ether, thioether, phenyl, or naphthyl moieties;
• or the pharmaceutically acceptable salts thereof;
• and
• B. contacting said oral cavity with a second composition comprising a carrier suitable for use in the oral cavity and from about 0.10% to about 1.25% by weight of the combined compositions of a chelator in excess of the amount of chelator which will react with the bis-biguanide compounds of Step A, and which in said concentration range effectively reduces said bis-biguanide tooth stain without precipitating said tooth-staining bis-biguanide, said chelator being an amino carboxylate compound selected from the group consisting of:
• Ethylenediaminediacetic acid, and the water-soluble pharmaceutically acceptable salts thereof,
• said compositions having a pH of from about 4.5 to about 9.5.

A process of inhibiting bis-biguanide tooth-staining and dental plaque and caries comprising the step of contacting the oral cavity with an effective amount of a composition comprising a carrier suitable for use in the oral cavity;

• and
• A. from about 0.01% to about 2.5% by weight of a tooth-staining bis-biguanide compound, otherwise tending to produce a rather offensive brown tooth stain upon continuous oral use, and having the generic formula:
• ##STR5## wherein A and A' each represent either (1) a phenyl radical which can contain as substituents up to two alkyl or alkoxy groups containing from 1 [t-] to about 4 carbon atoms, a nitro group, or a halogen atom;
• (2) an alkyl group containing from 1 to about 12 carbon atoms;
• or (3) 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 can be either 0 or 1;
• wherein R and R' each represent either hydrogen, an alkyl radical containing from 1 to about 12 carbon atoms, or an aralkyl radical containing from 7 to about 12 carbon atoms;
• wherein n is an integer from 2 to 12 inclusive;
• and wherein the polymethylene chain (CH.sub.2).sub.n can be interrupted by up to 5 ether, thioether, phenyl, or naphthyl moieties, or the pharmaceutically acceptable salts thereof;
• and
• B. from about 0.10% to about 1.25% by weight of the composition of a chelator in excess of the amount of chelator which will react with the bis-biguanide compounds, and which in said concentration range effectively reduces said bis-biguanide tooth stain without precipitating said tooth-staining bis-biguanide, said chelator being an amino carboxylate compound selected from the group consisting of:
• Ethylene-diaminediacetic acid, and the water-soluble pharmaceutically acceptable water-soluble salts thereof,
• said composition having a pH of from about 4.5 to about 9.5.

An oral composition effective in inhibiting bis-biguanide tooth staining and the formation of plaque, caries and calculus comprising a carrier suitable for use in the oral cavity and

• A. from about 0.01% to about 2.5% by weight of a tooth staining bis-biguanide compound, otherwise tending to produce a rather offensive brown tooth stain upon continuous oral use and having the generic formula:
• ##STR6## wherein A and A' each represent either (1) a phenyl radical which can contain as substituents up to two alkyl or alkoxy groups containing from 1 to about 4 carbon atoms, a nitro group, or a halogen atom;
• (2) an alkyl group containing from 1 to about 12 carbon atoms;
• or (3) 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 can be either 0 or 1;
• wherein R and R' each represent either hydrogen, an alkyl radical containing from 1 to about 12 carbon atoms, or an aralkyl radical containing from 7 to about 12 carbon atoms;
• wherein n is an integer from 2 to 12 inclusive;
• and wherein the polymethylene chain (CH.sub.2).sub.n can be interrupted by up to 5 ether, thioether, phenyl, or naphthyl moieties;
• or the pharmaceutically acceptable salts thereof;
• and
• B. from about 0.5% to about 6.0% by weight of the composition of a chelator which in said concentration range is present in excess of the amount of chelator which will react with the bis-biguanide and which effectively reduces said bis-biguanide tooth stain without precipitating said tooth-staining bis-biguanide, said chelator being an amino carboxylate compound selected from the group consisting of:
• Ethylene-diaminediacetic acid and the water-soluble pharmaceutically acceptable salts thereof,
• said composition having a pH of from about 4.5 to about 9.5.