Drug – bio-affecting and body treating compositions – Dentifrices
Patent
1992-09-28
1995-06-06
Griffin, Ronald W.
Drug, bio-affecting and body treating compositions
Dentifrices
A61K 716
Patent
active
054220980
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to dentifrices having an improved effect against the growth of plaque on teeth. The dentifrices may be in the form of powders, tooth pastes, chewing gum etc., but tooth pastes are normally preferred. An important constituent of the dentifrices of the invention is organopolysiloxanes.
From Britist Patent No. 686,429 it is known to incorporate organopolysiloxanes in dentifrices to prevent the adhesion of or facilitate the removal of tars, stains, tartar and the like from teeth.
British Patent No. 789,851 discloses oral hygiene compositions containing an organopolysiloxane and a higher aliphatic acyl amide of an amino carboxylic acid compound which is preferably a water-soluble carboxylate salt. British Patent No. 1,194,885 describes the addition of a quaternized tertiary cyclic amine in which a C.sub.8-22 aliphatic radical is attached to the quaternary nitrogen atom, to a dimethyl polysiloxane to improve the adherence of the silicone film to the teeth.
A similar solution is suggested in U.S. Pat. No. 4,161,518 where quaternary ammonium groups are incorporated in an organosiloxane molecule.
EP patent application, publication No. 0376363 discloses the use of aminoalkyl silicones and sarcosinate surfactants to prevent staining of teeth and in preventing caries, particularly in conjunction with antimicrobials which have a tendency to stain teeth.
Bacterial growth on teeth is a well known problem. The two major dental diseases, caries and periodontitis, are initiated and develop only in the presence of dental plaque. Dental plaque consists of dense aggregates of bacteria which attach to the tooth enamel, mainly in the interproximal area, or along the gingival margin. The enamel disintegrates when sucrose or other fermentable carbohydrates are consured; the plaque bacteria produce organic acids (mainly lactate) in this situation which cause dissolution of the hydroxyapatite of which enamel mainly consists. Dental plaque may also produce enzymes, toxins or antigens which may cause inflammation of the gingival tissue. A chronic inflammation under certain conditions lead to loss of the alveolar bone which supports the teeth, and subsequent toothloss.
Inhibition of adsorption of bacteria to dental enamel will thus have the potential to prevent both dental caries and periodonal disease. The mecanism by which the bacteria bind to enamel is not well understood. The inhibition of plaque formation obtained up to now has been caused by antibacterial agents with a longterm effect in the mouth. These substances interfere with bacterial growth rather than with the absorption of bacteria to enamel. Such substances have untoward side effects like staining of teeth and tongue, and unpleasant taste, and they cause a general decrease of the number of bacteria on the oral cavity. Substances which solely reduce the growth of plaque on the teeth by interference with their binding mechanisms have not yet been found.
As it will appear from the above it is previously known that silicone oil binds to the enamel surface of the teeth, and provides a hydrophobic surface thereon by forming a thin layer of oil which covers the surface for several hours after a single application. We have now surprisingly found that this layer of silicone oil can serve as a reservoir of certain antibacterial agents which are soluble in silicon oil directly, or indirectly, after an initial step where the antibacterial agent is dissolved in another organic solvent, and the resulting solution is then dissolved in silicon oil.
Thus, the invention provides a dentifrice which comprises silicone oil and a fat-soluble antibacterial agent dissolved therein, either directly or after dissolution of the anti-bacterial agent in an organic solvent.
Suitable silicone oils are e.g. the fluid organopolysiloxanes described in the above mentioned British Patent No. 789,851. A preferred class comprises the diphenyl or di(C.sub.1-4)alkyl polysiloxanes, in particular liquid dimethylpolysiloxane.
Suitable antibacterial agents are antiseptic phenols, in p
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Chemical Abstracts 81:20897y (1974).
Ellingsen Jan E.
Rolla Gunnar
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