WO2008068408A2

WO2008068408A2 - Oral hygiene composition and its use in the treatment of halitosis

Info

Publication number: WO2008068408A2
Application number: PCT/FR2007/001849
Authority: WO
Inventors: Jean-Claude Vezin; Gérard D'ARROS
Original assignee: Pierre Fabre Medicament
Priority date: 2006-11-13
Filing date: 2007-11-08
Publication date: 2008-06-12
Also published as: FR2908311A1; FR2908311B1; WO2008068408A3; WO2008068408A9

Abstract

The present invention relates to an oral hygiene composition comprising a parsley essential oil composition an a green tea extract, as well as its use in nutraceutic, cosmetic and/or therapeutic compositions for the preparation of a drug for the treatment of halitosis.

Description

ORAL HYGIENE COMPOSITION AND ITS USE IN THE TREATMENT OF HALITOSIS

The present invention relates to a composition based on parsley essential oil and a green tea extract as well as its use in nutraceutical, cosmetic and / or therapeutic preparations for the preparation of a medicament for preventing and / or treat halitosis.

The main origin of halitosis is oral in about 85% of cases, ENT problems, digestive are the cause of 10% of cases, halitosis can also be a consequence of diseases such as diabetes or certain cancers .

The main cause of the oral origin is bacterial. Certain bacteria such as Porphyromonas, Prevotella, Fusobacterium present on the dental surfaces, in the periodontal pockets, on the dorsal part of the tongue, in the presence of food debris of amino acids, and as a function of the pH release volatile compounds dragged towards the outside by the exhaled air.

These volatile compounds have a strong odor, very unpleasant at extremely low concentrations. These are essentially sulfur derivatives and amino derivatives. Among the sulfur derivatives are present essentially: hydrogen sulfide H ₂ S methylmercaptan CH ₃ SH - dimethylmercaptan (CH ₃ ) ₂ S

They are detectable by a "human nose" from the concentration of a few tens of ppb. The main cause of halitosis being well known, it may seem simple to fight it. One can imagine that strengthening hygiene is an effective remedy. The use of antiseptics known to be active in the oral field should make it possible to eradicate the responsible bacteria, but their location and their ability to colonize and grow oppose this purpose. The use of antiseptic solutions improves the disease state but does not completely eliminate the causes.

The use of menthol flavors transiently masks bad smells, but this action is fleeting and the extreme sensitivity of people makes this concept random. Another method may be useful and effective, it consists of using molecules or complex extracts reacting with the sulfur compounds mentioned above to make them less or nonvolatile. These are essentially zinc salts, especially chlorides or lactates, green tea extracts and some essential oils.

Therefore, it appears necessary to have a new anti-halitosis composition whose effectiveness would be enhanced compared to the compositions of the prior art.

To this end, the present invention relates to an oral hygiene composition comprising a combination of parsley essential oil and a green tea extract; and its use in nutraceutical, cosmetic and / or therapeutic preparations for the preparation of a medicament for preventing and / or treating oral diseases including halitosis. Advantageously, the oral hygiene composition according to the present invention comprising parsley essential oil and a green tea extract is characterized in that the amounts of essential oil of parsley and green tea extract are respectively between 0.01 and 5%; and between 0.005 and 1% by weight relative to the total weight of the composition.

For the purposes of the present invention, the term "parsley essential oil" is intended to mean the essential oil obtained from leaves and / or stalks of parsley.

For the purposes of the present invention, the amounts of green tea extract in the composition are expressed by weight of dry extract of green tea relative to the total weight of said composition.

Preferentially, the amount of parsley essential oil is between 0.02 and 2% and even more preferably between 0.1 and 1% by weight relative to the total weight of the composition.

Advantageously, the amount of green tea extract is between 0.008 and 0.5% and even more advantageously between 0.01 and 0.1% by weight relative to the total weight of the composition.

The Applicant has furthermore shown that the anti-halitosis composition according to the present invention is particularly effective when the mass ratio essential oil of parsley / green tea extract is between 5 and 30, preferentially between 10 and 20 and even more preferentially about equal. at 15. It has been remarked surprisingly and completely unexpectedly that said composition provides long-term protection.

Similarly, said composition has a pleasant taste accompanied by a feeling of freshness for the end user.

Nothing in the state of the art suggested this combination in these particular ranges in order to obtain a synergistic effect in the prevention and / or treatment of oral diseases and in particular of halitosis.

The effectiveness of the composition according to the present invention in the treatment of halitosis was tested in vitro: the various mixtures were brought into contact with sulfur products such as dimethyl mercaptan and the evolution of the concentration of these products. was measured by gas chromatography. The protocol is as follows: In air-filled gas sampling bags equipped with a septum, parsley essential oil and green tea extract were dissolved in alcoholic or hydroalcoholic solution, then dimethyl mercaptan a been introduced. This contact plant extract / dimethyl mercaptan was carried out for a period of 2 minutes before analysis by gas chromatography of the dimethyl mercaptan concentration.

The analysis consists in measuring the height of the dimethylmercaptan peak obtained on the chromatogram.

Experimental conditions: Apolar capillary column Injection by valve

TCD detector in coupling with a FID detector Temperature: isothermal mode at 120 ^° C. The results obtained are shown in Table 1 below:

TABLE 1: Efficacy of different mixtures of parsley essential oil / green tea extract in the treatment of halitosis

The decrease in the height of the dimethylmercaptan peak is characteristic of the efficacy of the extracts in the treatment of halitosis.

The most effective mixtures are therefore those having quantities of parsley essential oil and green tea extract of approximately 0.6% and 0.04% respectively; a mass ratio essential oil of parsley / tea extract approximately equal to 15.

The composition according to the present invention may be in a form selected from the group consisting of a tablet or lozenge (simple or cooked sugar type), capsule, chewing gum, toothpaste, toothpaste gel, mouthwash, spray. The different excipients to be incorporated into the composition as a function of the dosage form chosen are known to those skilled in the art. The amounts of the active ingredients and excipients will be adjusted by those skilled in the art to obtain a preparation final having a satisfactory taste and texture for the user.

Preferably, the capsule form comprises an envelope which solubilizes very rapidly according to the teaching of the patent application WO03 / 045166.

Advantageously, the compressed form to be sucked is of the "cooked sugar" type conventionally known to a person skilled in the art or obtained according to the teaching of application WO02 / 085334. The pellets called cooked sugars are conventionally prepared from a syrup of diluent substance, sweetened or not, boiled, then baked at a higher temperature, typically from 100 ⁰ C to 160 ⁰ C. To this sweet base, are added auxiliary substances such as sweeteners, antioxidants, dyes, flavors and the active ingredient (s).

At the end of cooking, the active ingredient (s) are added to the mass in a mixer as well as auxiliary substances such as sweeteners, anti-oxidants, colorants, flavorings. The mass thus prepared is kneaded on a suitable cold surface, then rolled and spun, to then be pressed or cut into pellets to the desired shape.

In a particular embodiment of the invention, said composition further comprises at least one glycerol ester of a linear C6 to C12 saturated fatty acid.

The invention therefore also relates to an anti-halitosis composition comprising parsley essential oil and a green tea extract in previously described ranges; and at least one glycerol ester of a C6 to C12 linear saturated fatty acid.

Advantageously, said glycerol ester is chosen from the group consisting of glycerol esters of fatty acids saturated linear C8 and ClO, used alone or in mixture.

Advantageously, the composition according to the present invention is the following:

% by weight

COMPOUNDS compared to the total weight of the composition essential oil of parsley 0.1 - 1.0% green tea extract 0.01 - 0.1% glycerol esters of fatty acids C8 and ClO 50 - 80%

Gelatin 10%

Excipients qs.

Even more advantageously, the composition according to the present invention is as follows:

% by weight

COMPOUNDS compared to the total weight of the composition parsley essential oil about 0.6 green tea extract about 0.04 glycerol esters of fatty acids C8 and ClO 50 - 80%

Gelatin 10%

Excipients qs. EXAMPLES OF FORMULATION:

EXAMPLE 1 Instant Dissolving Capsule

Spherical capsules consist of a gelatin shell containing about 0.04% green tea extract; and a liquid core containing about 0.6% parsley essential oil and about 70% glycerol esters of C8 and C10 acids. The percentages shown are grams per 100 grams of final composition.

The capsules have a diameter of 4 to 8 mm and a weight of 60 to 160 mg. Conventional excipients used by a person skilled in the art can then be added.

EXAMPLE 2: lozenge to suck

The process for producing pellets according to the invention comprises the following steps: a dissolution / boiling step: in a PAGES ^® type dissolver, a mixture of purified water and isomalt is heated to boiling. (mass ratio isomalt / water is approximately equal to 5) a cooking step: said mixture is transferred to a cooker type PAGES ^® . The mass is cooked until reaching a temperature of about 150 ^° C. a mixing step: the mass thus recovered is introduced into a previously lubricated type blender RUFFINATI ^® where are then added the active ingredients (about 0.6% parsley essential oil and about 0.04% green tea extract ,% by weight of the total weight of the composition) a final step of hot manufacture of the pellets: the preparation obtained above is kneaded in a kneader equipped with an internal cooling system type RUFFINATTI. Then the mass is rolled, spun and finally shaped square by pressing. The pellets obtained have a weight of 2.5 g.

The pellets are prepared by first making a paste with a portion of sucrose. This dough is heated until slightly boiling. The rest of the sucrose, the active ingredient (s) and the auxiliary substances are then added. After homogenization, the mass thus prepared is dropped dropwise on a cold plate or is injected into a suitable mold.

The manufacture of these pellets is carried out hot.

The indication "without sugar" will be used in the case where the composition will not contain sucrose.

EXAMPLE 3 mucoadhesive fluid gel

The mucoadhesive fluid gel is composed of an anhydrous base formulated from a vegetable oil and a suspension of hydrophilic polymers. The mixture of active ingredients as described in Example 1 is incorporated in this base. The polymer particles in contact with the saliva hydrate and cause bioadhesion to the mucosa, teeth and tongue, depositing the active ingredients. EVALUATION IN VIVO:

The composition according to Example 1 was tested in vivo. Measurements of concentrations of derivatives in exhaled air are carried out using a halimeter: an instrument that measures the concentration of sulphide molecules in the breath or saliva. The concentration of volatile sulfur compounds is expressed in ppb (part per billion).

The literature indicates the ranges of values corresponding to the perception of halitosis by the environment.

The apparatus was therefore calibrated using a permeation calibrator PPA200M for hydrogen sulfide.

Five measurement ranges from 1 to 5 were defined for the concentration of sulfur derivatives:

Concentration of sulfur derivatives (ppb) index

<150 ppb 1

From 150 to 300 ppb 2

From 300 to 450 ppb 3

From 450 to 600 ppb 4

> 600 ppb 5

The use of the halimeter is very simple: the halimeter is energized for preheating for 6 minutes. The device is then ready to perform the measurements. The user must inhale when the "inhale" signal appears, then the "exhale" signal must blow into the cell containing the detector. A value between 1 and 5 will be displayed on the screen. Twelve volunteers agreed to eat garlic-flavored dishes at lunch and not to brush their teeth afterwards. Two hours later, these people tested their breath using the halimeter described above (measure TO).

Then a composition according to the present invention was administered. Two new measurements were taken respectively 15 minutes after taking (measurement at TO + 15 minutes) and 1 hour after (measurement at TO + 1 hour)

The results obtained are shown in Table 2 below:

TABLE 2 ^{• In} Vivo Evaluation of a Composition According to Example 1 in the Treatment of Halitosis

The results obtained show a significant decrease in the values of halitosis after use of the described composition.

Claims

1. Use of an oral hygiene composition comprising parsley essential oil and a green tea extract characterized in that the amounts of parsley essential oil and green tea extract are respectively between 0, 01 and 5%; and between 0.005 and 1% by weight relative to the total weight of the composition, in nutraceutical, cosmetic and / or therapeutic preparations for the preparation of a medicament for preventing and / or treating halitosis.

2. Use according to claim 1 characterized in that the mass ratio essential oil of parsley / green tea extract is between 5 and 30.

3. Use according to claim 1 or 2 characterized in that the mass ratio essential oil of parsley / green tea extract is equal to 15.

4. Use according to any one of the preceding claims characterized in that the amount of parsley essential oil is equal to 0.6% by weight relative to the total weight of the composition.

5. Use according to any one of the preceding claims characterized in that the amount of green tea extract is equal to 0.04% by weight relative to the total weight of the composition.

6. Use according to any one of the preceding claims characterized in that it further contains at least one glycerol ester of a linear saturated fatty acid C6 to C12.

7. Use according to any one of the preceding claims characterized in that said ester of glycerol is selected from the group consisting of glycerol esters of linear saturated fatty acids in

C8 and ClO, used alone or in mixtures.

8. Use according to any one of the preceding claims, characterized in that it comprises

0.1 to 1.0% parsley essential oil; from 0.01 to

0.1% green tea extract; from 50 to 80% of glycerol esters of C8 and ClO fatty acids; about 10% gelatin and sufficient excipients; the percentages being indicated by weight relative to the total weight of the composition.