Oral compositions containing trifluoromethyl phenyl bis-biguanides as antiplaque agents

Claim 2

A bis-biguanide compound having the generic formula: ##STR3## wherein n is from 2 to 4 inclusive; wherein X and X' each represent an alkylene radical containing from 1 to 3 carbon atoms; wherein z and z' are selected from the group consisting of 0 to 1; wherein R and R' are each selected from the group consisting of hydrogen, alkyl radicals containing from 1 to about 12 carbon atoms and aralkyl radicals containing from 7 to about 12 carbon atoms; and wherein R 2 and R 2 ' are each selected from the group consisting of hydrogen and alkyl radicals of 1 to 2 carbon atoms; and the pharmaceutically acceptable salts thereof.

Claim 3

The compound of claim 1 wherein said salt is a water-soluble salt.

Claim 4

The compound of claim 2 wherein the salt is selected from the group consisting of the dihydrochloride, diacetate and digluconate salts.

Claim 5

The compound of claim 1 wherein n equals 2, z and z' are each O and R, R', R 2 and R 2 ' are each hydrogen.

Claim 6

The compound of claim 4 wherein the trifluoromethyl groups are in the meta position.

Claim 7

The compound of claim 4 wherein said compound is a pharmaceutically acceptable, water-soluble salt.

Claim 8

The compound of claim 5 wherein said compound is a pharmaceutically acceptable, water-soluble salt.

Claim 9

The compound of claim 7 wherein said salt is selected from the group consisting of the dihydrochloride diacetate and digluconate salts.

Claim 10

An oral composition comprising a carrier suitable for use in the oral cavity and from about 0.01% to about 2.5% of an antiplaque agent having the formula: ##STR4## wherein n is from 2 to 4 inclusive; 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 to 1; wherein R and R' are selected from the group consisting of hydrogen, alkyl radicals containing from 1 to about 12 carbon atoms and aralkyl radicals containing from 7 to about 12 carbon atoms and wherein R 2 and R 2 ' each are selected from the group consisting of hydrogen and alkyl radicals of 1 to 2 carbon atoms, and the pharmaceutically acceptable salts thereof.

Claim 11

An oral composition comprising a carrier suitable for use in the oral cavity and from about 0.01% to about 2.5% of an antiplaque agent having the formula: ##STR4## wherein n is from 2 to 4 inclusive; 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 to 1; wherein R and R' are selected from the group consisting of hydrogen, alkyl radicals containing from 1 to about 12 carbon atoms and aralkyl radicals containing from 7 to about 12 carbon atoms and wherein R 2 and R 2 ' each are selected from the group consisting of hydrogen and alkyl radicals of 1 to 2 carbon atoms, and the pharmaceutically acceptable salts thereof.

Claim 12

The composition of claim 9 wherein said antiplaque agent is in the form of a water-soluble, pharmaceutically acceptable salt.

Claim 13

The composition of claim 10, wherein said salt is selected from the group consisting of the dihydrochloride, diacetate and digluconate salts.

Claim 14

The composition of claim 9 wherein n equals 2, z and z' are each O and R, R', R 2 and R 2 ' are each hydrogen.

Claim 15

The composition of claim 12 wherein the trifluoromethyl groups in the antiplaque agent are in the meta position.

Claim 16

The composition of claim 12 wherein said antiplaque agent is a pharmaceutically acceptable water-soluble salt.

Claim 17

The composition of claim 13 wherein said antiplaque agent is in the form of a pharmaceutically acceptable water-soluble salt.

Claim 18

The composition of claim 15 wherein said salt is selected from the group consisting of the dihydrochloride, diacetate and digluconate salts.

Claim 19

The compositions of claim 16 wherein the amount of antiplaque agent in said composition is from about 0.05% to about 1.2%.

Claim 20

The composition of claim 16 in the form of a dentifrice wherein said antiplaque agent is present at a level of from about 0.1% to about 2.0% and wherein said composition contains as an additional ingredient from about 0.5% to about 95% of an abrasive.

Claim 21

The composition of claim 16 in the form of a mouthwash wherein said antiplaque agent is present at a level of from about 0.5% to about 1.5% and wherein said composition contains as additional components: A. from about 5% to about 40% ethyl alcohol; B. from 0% to about 20% humectant; C. from 0% to about 2% sudsing agent; D. from 0% to about 0.5% sweetening agent; E. from about 0.05% to about 0.3% flavoring agent; and F. the balance water.

Claim 22

A composition in accordance with claim 9 which additionally contains from about 0.01% 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 compound, said chelator being selected from the group consisting of nitrilotriacetic acid, ethylenediamine diacetic acid, kojic acid, maltol, ethyl maltol, calcium dihydrogen ethylenediamine tetraacetate, di-N-substituted ethylene diamine diacetic acids wherein the substituents are selected from the group consisting of ethyl and 2-hydroxyethyl and the pharmaceutically acceptable water-soluble salts of said chelators.