Whitening anti-plaque and anti-tartar low abrasivity tooth...

Drug – bio-affecting and body treating compositions – Dentifrices – Ferment containing

Reexamination Certificate

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C424S049000, C424S052000, C424S057000

Reexamination Certificate

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06432388

ABSTRACT:

FIELD OF THE INVENTION
This invention relates to some improvements made to the object of the Spanish patent application no. P9401832 relating to a whitening toothpaste which is anti-plaque and anti-tartar of low abrasion, optionally suitable for the treatment of sensitive teeth, consisting of the formulation of a whitening toothpaste which is anti-plaque and anti-tartar of low abrasion, which, contrary to the toothpaste described in said Spanish patent application, has a greater proteolytic enzyme content and lacks detergents.
BACKGROUND OF THE INVENTION
The Spanish patent application no. P9401832 describes a whitening toothpaste which is anti-plaque and anti-tartar of low abrasion, optionally suitable for the treatment of sensitive teeth, that comprises 5-10% of xylitol, 0.7-1.1% of sodium laurysarcosinate, 16-18% of silica, 3-7% of a proteolytic enzyme with low specificity, or alternatively, 0.3-3% carbamide peroxide, along with a buffer, water, humectants, re-mineralising agents, bining agents, opacifiers, colouring agents, aromatising agents, sweeteners and preservatives.
In the whitening toothpaste formulation, which is anti-plaque and anti-tartar, of low abrasion, the buffer used consists of a mixture of tetra-sodium pyrosulphate and di-sodium dihydrogenopyrophosphate, while in the whitening toothpaste formulation, which is anti-plaque and anti-tartar of low abrasion and desensitising, that is to say, suitable for the treatment of sensitive teeth, the buffer used consists of a mixture of tetra-potassium pyrophosphate and di-potassium dihydrogenopyrophosphate.
The production of the whitening toothpaste, which is anti-plaque and anti-tartar, of low abrasion, encounters problems with the solubility of the sodium salts that make up the working buffer.
The Spanish addition certificate application no. P9501732 solves the aforementioned problem by using a potassium buffer, consisting of a mixture of potassium salts, along with a reduction in the xylithol content and the use of a humectation system that comprises a mixture of glycerine and sorbitol, and provides a the whitening toothpaste, which is anti-plaque and anti-tartar of low abrasion and which is suitable for the treatment of sensitive teeth, that comprises 1-5% xylitol, 1.5-2% sodium laurylsarcosinate, 16-18% silica, a buffer consisting of 4-5% tetra-potassium pyrosulphate and 1-3% of potassium dihydrogenopyrophosphate, 3-7% of a proteolytic enzyme with low specificity, or alternatively, 0.3-3% of carbamide peroxide.
An occurrence in common between the toothpastes described in the Spanish patent application P9401832 and in the Spanish addition certificate application no. P9501732 is the presence of a detergent, such as sodium laurylsarcosinate in a quantity lying between 1.5 and 2% by weight. The usual toothpastes also include a detergent in their formulation, generally sodium laurylsulphate (SLS).
However, the use of such detergents can seriously damage gums and lead to a series of alterations to the mucous, such as desquamtation of the oral mucus, irritation and foreshortening (B. B. Herlosfoson and P. Barkvoll,
Acta Odontol. Scand.,
1993, 51: 39-43, “Desquamative effect of sodium lauryl sulfate on oral mucosa. A preliminary study”; B. B. Herlosfoson and P. Barkvoll,
Eur. J Oral Sci.,
1996, 104, 21-26, “Oral mucosal desquamation caused by two toothpaste detergents in an experimental model”; B. B. Herlosfoson and P. Barkvoll,
J Clin. Periodontol.,
1996, 24, 1-5, “Oral mucosal desquamation of pre- and post- menopausal women”). Similarly, SLS significantly increases the appearances of new ulcers in patients with recurrent ulcers or cankers (B. B. Herlosfoson and P. Barkvoll,
Acta Odontol. Scand.,
1994, 52:257-259, “Sodium lauryl sulfate and recurrent aphthous ulcers. A preliminary study”; B. B. Herlosfoson and P. Barkvoll,
Acta Odontol. Scand.,
1996, 54:150-153, “The effect of two toothpaste detergents on the frequency of recurrent aphthous ulcers”) and provokes rapid vasodilation with an increased blood flow when applied to the lips (B. B. Herlofson, P. Brodin and H Aars,
J Clin. Periodontol.,
1996, 23(11), “Increased human gingival blood flow induced by sodium lauryl sulfate”).
It seems that these adverse effects of SLS are due to the surfactant nature of SLS, to its affinity for glycoproteins and to his ability to fix calcium ions. SLS can even lead to the disintegration of the mucin layer, denaturing of the proteins of the epithelial cells and the dissolving of the structural lipids of the cells, provoking finally the penetration of SLS into the deepest layers of the mucus where the functioning of the live tissue can be compromised.
On the other hand, the toothpaste formulations described in the Spanish patent application P9401832 and in its addition certificate no P9501732 have a relatively high content of proteolytic enzyme with low specificity (papain), lying between 3 and 7% by weight, which could influence the cost of the product and lead to irritations of the mouth.
The invention provides a solution to the aforementioned problems which consists of some improvements introduced in the formulation of the toothpaste that comprise eliminating SLS and reducing the quantity of papain.
DETAILED DESCRIPTION OF THE INVENTION
The invention provides some improvements introduced into the object of the Spanish patent application P9401832 relating to a whitening toothpaste which is anti-plaque and anti-tartar of low abrasion, consisting of the development of a whitening toothpaste which is anti-plaque and anti-tartar of low abrasion and which is suitable for treating sensitive teeth, that is characterised by the lack of detergents and whose formulation comprises:
Component
% by weight with respect to total
Papain
0.1-1  
Xylitol
 5-10
abrasive system based on silica
16-18
a buffer consisting of:
i)
tetra-potassium pyrophosphate
4-5
ii)
potassium dihydrogen phosphate
1-3
additives/excipients
s.q.
[s.q.: sufficient quantity to make up 100%]
Papain is a proteolytic enzyme with low specificity, suitable for cleaning the salivary protein plaque that has a whitening effect on the tooth surfaces. A valued enzymatic extract can be used, whose proteolytic activity has been adjusted to a constant value, from a latex obtained from unripe fruits of the
Carica papaya
(papaya). Papain hydrolysed proteins, amides and amino acid esters, and its activity is associated with the presence of free sulphyl (—SH) groups in its active center. To produce the toothpaste of this invention, an enzymatic extract is preferably used that contains papain with a proteolytic activity of, approximately, 6,000 U-USP/mg [Units of United States Pharmacopea]. The optimum working temperature for this enzyme lies between 40 and 65° C. Due to the low substrate specificity, papain can act on multiple protein products, in over pH range of from 3 to 9. Outside these values the enzyme is inactive. In general, the toothpaste that contains papain conveniently has a pH near to neutral, that is to say, approximately 7, with a view to guaranteeing the activity of the enzyme without de-mineralising the enamel. Papain has a cleaning action on the bacterial plaque and tartar by breaking the glycoprotein and lipoprotein chains from the saliva fluid as well as acting on the bacterial excretory activity of mucylaginose substances (capsule) that attach themselves to the enamel allowing colonisation by bucal flora (bacterial plaque) and the fixing of calcium salts to these structures that act as supports (tartar). Therefore, by attacking these structures, the processes associated with plaque and tartar excess are improved such as tooth decay and periodontal disease.
The xylitol is active in several ways as, on the one hand, it acts as a humectant and refresher. while on the other, it has voluminous anti-tooth decay sweetening activity and inhibits capture and metabolism of glucose by certain bacteria, preventing the formation of organic acids, that attack the hydroxyapatite of the enamel dissolving it and provoking the appearance o

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