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 a composition comprising a carrier suitable for use in the oral cavity, and 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:
• ##EQU4## 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 to 1;
• wherein R and R' each represent either hydrogen, an alkyl radical containing from 1 to about 12 carbon atoms 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, the amount of said composition being sufficient to provide at least 0.001 grams of the said bis-biguanide compound;
• 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, in excess of the molar amount which will react with the amount of bis-biguanide compound of Step A, of an amino carboxylate compound which in said concentration range effectively reduces said bis-biguanide tooth stain without precipitating said tooth-staining bis-biguanide and which is selected from the group consisting of nitrilo triacetic acid and its pharmaceutically acceptable water-soluble salts;
• said composition having a pH of from about 4.5 to about 8.0.

A process of inhibiting dental plaque and caries comprising the step of contacting the oral cavity with 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 use, and having the generic formula:
• ##EQU5## 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 to 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 0.01% to about 1.25% by weight, in excess of the molar amount which will react with the tooth-staining bis-biguanide compounds of an amino carboxylate compound which in said concentration range effectively reduces said bis-biguanide tooth stain without precipitating said tooth-staining bis-biguanide and which is selected from the group consisting of nitrilo triacetic acid and its pharmaceutically acceptable water-soluble salts;
• said composition having a pH of from about 4.5 to about 8.0.