Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
1999-09-27
2001-01-30
Jarvis, William R. A. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C514S558000, C424S052000
Reexamination Certificate
active
06180599
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to a new use of medium-chain fatty acids as a prophylactic against dental caries and as a therapeutic treatment of the disease, and a pharmaceutical composition containing these medium-chain fatty acids as active ingredients.
Particularly, the present invention relates to the use of the salt form of specific medium-chain (C
9
-C
14
) fatty acids; nonanoic acid (C
9
) capric acid (C
10
), undecanoic acid (C
11
), lauric acid (C
12
), tridecanoic acid (C
13
) or myristic acids (C
14
), as a prophylactic against dental caries and therapeutic treatment of the same disease and periodontal disease. The pharmaceutical composition of these medium-chain fatty acids may include lectins and/or fluoride as well.
Dental caries, one of the most prevalent and significant forms of oral disease, can lead to loss of teeth in spite of development of therapeutics. Caused by dental plaque formed on the surface of teeth, dental caries results in tooth loss as a result of organic acids, the natural metabolite of plaque bacteria contained in dental plaque, which decalcify dental hard tissue locally and gradually.
The composition of dental plaque is approximately 80% (w/w) water, 10% plaque bacteria, 6% matrix protein and 2% extracellular polysaccharide. No method that prevents formation of dental plaque has been reported, in the presence of saliva, which always exists in the human oral cavity. When teeth are exposed to saliva, an acquired pellicle, which is a thin acellular protein film, originated from salivary glycoprotein is formed in a few minutes. This acquired pellicle always exists as long as teeth are exposed to saliva. The acquired pellicle's function is to protect teeth; however, it induces formation of dental plaque by acting as a matrix where oral bacteria attach. Bacteria adhere to the surface of teeth within several hours, and matrix protein is deposited as reversible adhesion of bacteria progresses. Extracellular polysaccharides, synthesized by plaque bacteria, are continuously deposited on the plaque matrix and this allows the dental plaque to grow.
Plaque bacteria decompose an oligosaccharide chain of glycoprotein which exist in saliva, and use this decomposition as an energy source regardless of food supply.
And a portion of the protein denatured by removing this oligosaccharide chain, incorporates into the plaque matrix. On the other hand, plaque bacteria synthesize extracellular polysaccharides by using sucrose as a major substrate when food is supplied. Extracellular polysaccharides, contained in the plaque matrix, act as an aggregating factor for some oral bacteria, and act as an energy source in case of an interruption in their regular food supply.
As mentioned above, dental plaque can be formed without food, and dental plaque progresses more when food is supplied. Dental plaque will be formed as long as saliva exists in the oral cavity. Consequently, it is important to remove dental plaque efficiently for prevention and treatment of dental caries.
The tooth, a calcified hard tissue, is not regenerated once affected by dental caries, making it very important to prevent dental caries as much as treating it. There are two ways to prevent dental caries; one is to strengthen the structure of teeth so that they may resist the attack of organic acid formed by plaque bacteria, and the other is to remove or inhibit formation of dental plaque (or, in practice, inhibit metabolism of acidogenic plaque bacteria).
Tooth brushing is the most obvious method of removing dental plaque and preventing longstanding accumulation on the surface of teeth. Unfortunately, this method does not remove enough dental plaque from the gingival margins, fissures, and contact points of teeth and cannot prevent dental caries in these regions. Thus, to resist acid attack, it is necessary to strengthen the structure of teeth in addition to tooth brushing. For this, the most prevalent method is converting hydroxyapatite [Ca
10
(PO
4
)
6
(OH)
2
], the smallest building unit of enamel apatite, into fluorapatite [Ca
10
(PO
4
)
6
F
2
] by ingesting fluoride of a suitable concentration. In some areas, the drinking water is naturally or artificially fluoridated. It is reported that the frequency of dental caries is reduced by 40
~
60% by water fluoridation, but it is not abolished. The structure of teeth is somewhat strengthened by fluoridation of the water supply, by topical application of fluoride and by using medicines containing fluoride. However, dental caries ultimately breaks out by continuous acid attack. Thus, it is necessary to provide an active method to inhibit or prevent organic acids which are metabolites of plaque bacteria. Although the need is great, a dental caries-inhibitor with the above-mentioned effect has not been developed yet.
Many kinds of medicine for prevention and treatment world-wide since 1970: Listerine®, which contains a phenol compound; Scope®, which contains a tertiary ammonium compound; and Peridex®, which contains chlorohexidine. However, these medicines are not effective as a dental caries-inhibitor because they mainly apply to periodontal pathogens. Listerine® and Scope® have few side effects, but their action of removing dental plaque and their antibacterial effect is not satisfying. On the other hand, Peridex® has a good effect as a medicine but has serious side effects. Ulcers of oral mucosa, exfoliating gingivitis and discoloration occur even when using a normal dose, xerostomia occurs with frequent use, and it has been reported that long term use of Peridex® may cause cancer in experimental animals. Thus, the development of a safe dental caries-inhibitor without side effects and which is usable for a long time, is an urgent matter.
The present inventor completed this invention through finding that medium-chain fatty acids have an excellent effect on inhibiting production of organic acids, growth of acidogenic plaque bacteria and synthesis of extracellular polysaccharide.
SUMMARY OF THE INVENTION
The object of the present invention is to provide use of medium-chain fatty acids as a prophylactic against dental caries and as a therapeutic treatment for the disease. A pharmaceutical composition containing medium-chain fatty acids as active ingredients of the present invention can be the best agent for prevention and treatment of dental caries.
The pharmaceutical composition containing medium-chain fatty acids as active ingredients of the present invention may include lectins and/or fluoride compound in addition to medium-chain fatty acids.
REFERENCES:
patent: 3952092 (1976-04-01), Bowen et al.
patent: 4217341 (1980-08-01), Suddick et al.
patent: 4353892 (1982-10-01), Caslavsky et al.
patent: 4533544 (1985-08-01), Groat et al.
patent: 4540576 (1985-09-01), Zahradnik
patent: 4619825 (1986-10-01), Eigen et al.
patent: 4737359 (1988-04-01), Eigen et al.
patent: 4942034 (1990-07-01), Hill et al.
patent: 4976954 (1990-12-01), Kleber et al.
patent: 4988499 (1991-01-01), Bristow et al.
patent: 5098711 (1992-03-01), Hill et al.
patent: 5240710 (1993-08-01), Bar-Shalom et al.
patent: 5284648 (1994-02-01), White et al.
patent: 5416075 (1995-05-01), Carson et al.
patent: 5679377 (1997-10-01), Bernstein et al.
patent: 5824292 (1998-10-01), Carr et al.
patent: 5840338 (1998-11-01), Roos et al.
patent: 5962428 (1999-10-01), Carrano et al.
patent: 0481701 (1992-04-01), None
Hayers et al., The effects of medium chain fatty acids and fluoride on . . . , Arch. Oral Biol., vol. 35/12, pp. 939-943, (1990).
Copy of chemical seach abstract from Registry.
Bachman & LaPointe P.C.
Jarvis William R. A.
Kim Vickie
LandOfFree
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