Oral hygiene composition

Drug – bio-affecting and body treating compositions – Dentifrices

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424 54, 424 57, A61K 716, A61K 722

Patent

active

056957459

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to an oral hygiene composition having antimicrobial action. The invention relates in particular to a stabilised composition comprising both a cationic antimicrobial agent and an anionic anticalculus and/or antistaining agent, and to methods for use of such a composition.
The term `oral hygiene composition` as used herein includes inter alia dentifrices, mouthwashes, toothpowders, chewing gums and lozenges and denture cleansing formulations. Mouthwashes are particularly preferred.
Oral hygiene compositions containing cationic antimicrobial agents are well-known in the art. Such antimicrobial agents are known to be effective to reduce levels of plaque in the mouth.
Separate oral hygiene compositions comprising anionic anticalculus agents are also known. For example, U.S. Pat. No. 4,515,772 (Parran) describes an oral hygiene composition in the form of a mouthwash, liquid dentifrice or toothpaste which comprises an anionic anticalculus agent in the form of a water-soluble alkali-metal pyrophosphate.
However, many prior art compositions comprising both cationic antimicrobial agents (antimicrobials) and anionic anticalculus agents, especially polyphosphates, have been found to be unstable in use, especially at the pHs normally required in an oral hygiene composition. Accordingly, it has not so far normally been possible to combine the excellent antiplaque action of cationic antimicrobials with the excellent anticalculus action of anionic species such as polyphosphates. Rather, it has been necessary either to use cationic anticalculus agents such as zinc ions, as described in U.S. Pat. No. 4,022,880 (Vinson et al) or non-cationic antimicrobials such as biphenolics and halogenated salicylanilides, as described in GB-A-2230187 (Colgate Palmolive).
This problem is reflected in GB-A-2230187 where it is stated at page 2, lines 11/18 that:
"Hitherto, the cationic antibacterial materials such as chlorhexidine, benzethonium chloride and cetyl pyridinium chloride have been the subject of greatest investigation as antibacterial antiplaque agents. However, in spite of their being used in conjunction with zinc anticalculus agent, they are not effective when used with anionic materials such as polyphosphate anticalculus agent".
U.S. Pat. No. 3,934,002 (Procter and Gamble) discloses an oral composition comprising a bis-biguanide antimicrobial agent and an anionic anti-calculus agent which inhibits the tendency of the bis-biguanide compound to produce a stain on oral surfaces. A surfactant, such as polyoxyethylene (20) sorbitan monoisostearate, may be included in the composition. However, it appears that the composition is not fully stabilised, since it is stated that where the bis-biguanide compound is not a water-insoluble compound having a solubility in water less than the corresponding salt of the bis-biguanide with the anti-calculus agent, then an excess of the anti-calculus agent must be used to neutralise the bis-biguanide compound, otherwise the two will react leaving insufficient free anti-calculus agent.
U.S. Pat. No. 4,323,551 (Procter and Gamble) discloses a mouthwash composition exhibiting plaque control/reduced staining tendencies comprising a quaternary annonium compound and a pyrophosphate salt and having a pH of from 7.0 to 9.5.
European Patent Publication No. 480812 (Colgate-Palmolive) discloses an oral composition comprising both a cationic antibacterial agent (such as chlorhexidine digluconate) and an anionic active agent (such as certain polyphosphates and polyphosphonates). The composition is stabilised by use of an effective amount of a betaine-type surfactant. The document states that "only the ampholyte betaine offers the window of opportunity wherein both precipitation inhibition and activity prevail". It is further stated that the betaine must be present in a quantity at least sufficient to prevent the precipitation of the bis-biguanide anionic agent salt.
It has now surprisingly been found that the amount of the betaine-type surfactant can be substantially reduced by inc

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