Drug – bio-affecting and body treating compositions – Dentifrices – Ammonia – amine – or derivative thereof
Patent
1992-01-28
1993-11-30
Rose, Shep K.
Drug, bio-affecting and body treating compositions
Dentifrices
Ammonia, amine, or derivative thereof
424 49, A61K 716, A61K 722
Patent
active
052663060
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to a composition for the oral cavity. More particularly, it relates to an oral composition wherein adsorption of cetylpyridinium chloride as a bactericide to the surfaces of teeth is promoted.
BACKGROUND OF THE INVENTION
Dental plaque is formed by adsorption and propagation of intraoral bacteria such as Streptococcus mutans and the like on the surfaces of teeth. It is well known that dental plaque is the cause of dental caries and is also the cause of gingivitis or alveolar pyorrhea. Therefore, it is important to remove dental plaque and to prevent adhesion of it (plaque control) for oral sanitation.
Among the plaque control methods, the method which is performed most commonly is that for removing dental plaque mechanically by brushing, that is, by using a toothbrush. However, in order to remove dental plaque completely by brushing, high-level brushing technique is needed. In practice, almost all people are conducting insufficient brushing and, therefore, the rate of diseases such as dental caries, gingivitis and alveolar pyorrhea is not reduced despite brushing.
Accordingly, in order to compensate brushing, or to substitute for brushing, a chemical plaque control method has been studied. The pyridinium compounds having C.sub.8-18 straight or blanched chain alkyl group are known. Among them, the compound of which efficacy and safety are clinically acknowledged is cetylpyridinium chloride.
It is known that cetylpyridinium chloride is a compound represented by the formula: ##STR1## and it has a bactericidal action and is easily to adsorbed to oral mucosa or the surfaces of teeth. Thereby, it is considered that adsorption of intraoral bacteria to the surfaces of teeth is prevented and, further, formation of dental plaque is prevented. However, a study on promoting adsorption of such cetylpyridinium chloride to the surfaces of teeth or on improving it's effect has not been performed yet.
The present inventors have intensively studied to promote retention of cetylpyridinium chloride in the oral cavity, particularly adsorption of it to the surfaces of teeth and to enhance the effect of preventing formation of bacterial plaque. As a result, it has been found that, when cetylpyridinium chloride is used in combination with an N.sup..alpha. -longer acyl basic amino acid lower alkyl ester or a salt thereof, adsorption of cetylpyridinium chloride to the surfaces of teeth is greatly enhanced. Thus, the present invention has been completed.
DISCLOSURE OF THE INVENTION
According to the present invention, there is provided an oral composition comprising cetylpyridinium chloride and an N.sup..alpha. -longer acyl basic amino acid lower alkyl ester or a salt thereof. According to the present invention, an oral composition which promotes adsorption of cetylpyridinium chloride to the surfaces of teeth and has excellent effect for preventing formation of dental plaque and dental caries can be obtained.
Cetylpyridinium chloride is normally formulated into the composition in an amount of more than 0.002 % by weight, preferably more than 0.01 % by weight. In view of bactericidal effect, the upper limit of the amount of cetylpyridinium chloride is not specifically limited. Considering the fact that cetylpyridinium chloride has a bitter taste and is likely to color teeth when the amount is too large, or influence on oral mucosa and the like, it is normally preferred that the amount is less than 1 % by weight.
As the basic amino acid part of the N.sup..alpha. -longer acyl basic amino acid lower alkyl ester to be used, ornithine, lysine and arginine are particularly preferred and it may be either an optical isomer or racemate thereof. The acyl group thereof is a saturated or unsaturated natural or synthetic fatty acid residue having 8 to 22 carbon atoms, for example, it may be a natural system mixed fatty acid residue such as coconut oil fatty acid, tallow fatty acid residue and the like, in addition to a monofatty acid residue such as lauroyl, myristyl, stearoyl group and th
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Fujita Tomomi
Ohtsuki Hidehiko
Rose Shep K.
Sunstar Kabushiki Kaisha
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