Drug – bio-affecting and body treating compositions – Dentifrices
Patent
1994-09-14
1998-11-03
Shaver, Paul F.
Drug, bio-affecting and body treating compositions
Dentifrices
424 55, A61K 716
Patent
active
058304371
DESCRIPTION:
BRIEF SUMMARY
The present invention concerns compositions for oral use for avoiding stain formation on teeth and adhesion of exogenous substances. The invention also relates to an oral hygiene method using such compositions.
The formation of stains on teeth poses an aesthetic problem for many individuals, in particular those susceptible to staining from tar and tartar or to stains caused by ingested food, smokers and tea or coffee drinkers.
Adsorption and retention of food substances contributes greatly to stain formation on both natural and artificial teeth, partly caused by the adhesion of exogenous substances. Tea, coffee, wine, red fruits and tobacco are the main causes of stain formation.
Antibacterial antiplaque agents can also cause stain formation: biguanidohexanes such as chlorhexidine and alexidine and quaternary ammonium salts such as benzethonium chloride and cetylpyridinium chloride can cause stains to form.
Patents U.S. Pat. No. 4,224,309, U.S. Pat. No. 4,118,474 and U.S. Pat. No. 4,118,473 describe the use of additives such as 2-phosphonobutane-1,2,4-tricarboxylic acid, phosphono- acetic acid and iminodiacetic N-methylenephosphonic acid to reduce stain formation on teeth which is caused by continual use of antibacterial agents.
Document EP-A-373 688 describes the use of organopolysiloxanes to prevent tar, stains, tartar and food particles from adhering to the teeth.
Finally, some synthetic linear anionic polymers, polycarboxylates, have been described for oral application, particularly in association with a source of fluoride ions to encourage the action of some antitartar agents based on alkaline polyphosphates by impeding their enzymatic hydrolysis by saliva. Examples of these polymers include crosslinked carboxyvinyl compounds, sold by BF GOODRICH under the trade name "CARBOPOL" (CARBOPOL 934, CARBOPOL 940, CARBOPOL 941), copolymers of maleic anhydride and methylvinylether with an average molecular weight of 30 000 to 1 000 000, preferably 30 000 to 500 000, sold by GAF CORPORATION under the trade name "GANTREZ", in particular "GANTREZ S-97 PHARMACEUTICAL GRADE" (average molecular weight 70 000), and copolymers of vinyl acetate and crotonic acid, such as those sold by HOECHST under the trade name "ARISTOFLEX A".
We have now developed, surprisingly, linear or crosslinked synthetic hydrocarbon polymers which contain carboxylate and hydroxymethyl groups which effectively prevent stain formation on teeth. The anti-staining action has been demonstrated in vitro by colorimetric measurement of hydroxyapatite (HAP) powder pellets treated with a solution of the polymer compared with untreated pellets of HAP powder. In addition, compositions for oral use containing these polymers not only prevent stain formation as described above, i.e. due to retention and/or adsorption of food substances, but also prevent darkening of natural or artificial teeth caused by the presence of known antibacterial antiplaque agents. The compositions also readily prevent adhesion of exogenous substances to the teeth and are active in preventing the appearance of dental plaque and tartar. They also contribute generally to oral hygiene.
The present invention thus concerns a composition for oral use, characterized in that it comprises at least one linear or crosslinked hydrocarbon polymer which is principally constituted by units with the following formula: ##STR1## where:
R represents H or CH.sub.2 OH,
A represents an alkali metal or an ammonium, amine or alkanolamine salt, the average frequency of the units corresponding to a carboxylate/hydroxymethyl ratio greater than 0.5 in the polymer, and
a physiologically acceptable vehicle.
The units with formula (Ia) and (Ib) can be disposed in any order and the average frequency of the units in the polymer preferably corresponds to a carboxylate/hydroxymethyl ratio of between 1.1 and 16, better still between 2 and 9. The average degree of polymerization is 3 to 1 000, preferably 50 to 600.
"Oral use" means the products are not ingested, but can be retained in the mouth for a sufficient period
REFERENCES:
patent: 4992258 (1991-02-01), Mason
patent: 5093170 (1992-03-01), Degenhardt et al.
patent: 5120460 (1992-06-01), Asai et al.
patent: 5292501 (1994-03-01), Degenhardt et al.
Ascione Jean Marc
Forestier Serge
"L'Oreal"
Shaver Paul F.
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