FR3033700A1 - COMPOSITION FOR THE TREATMENT OR INHIBITION OF ORAL BRAIN IN THE FORM OF A SPRAY - Google Patents

Abstract

The present invention relates to a composition for the treatment or inhibition of bad breath orally in the form of a spray, a spray or a nebulization, containing, in weight percent by volume, between 0, 15 and 0.25% of an antimicrobial compound selected from chlorhexidine, a chlorhexidine salt, octenidine, a salt of octenidine or a mixture of such compounds, and between 1.50 and 2.50% a zinc salt or a mixture of such salts.

Description

The present invention relates to a composition for treating or inhibiting oral bad breath. Bad breath, or halitosis, or foul breath, is the phenomenon by which a bad smell emanates from the mouth of a subject. Halitosis is due to the production, by bacteria in the oral cavity, of malodorous compounds such as volatile sulfur compounds (CVS), for example hydrogen sulphide, methyl mercaptan, dimethyl sulphide and disulfide. dimethyl. Other malodorous compounds that can be produced are diamines and short chain fatty acids. The bacteria responsible for producing malodorous compounds are anaerobic bacteria, such as Porphyromonas gingivalis, Bacteroides forsythus or Treponema denticola. The phenomenon of halitosis appears, for example, in cases of periodontal disease. The extent of the phenomenon is generally proportional to the degree of progression of the disease. It also often occurs in some people in the morning when they wake up, in situations where food debris has not been removed from the mouth, for example in the absence of effective tooth brushing the night before. Another situation conducive to the occurrence of halitosis is the decline in saliva production. Indeed, salivary flow is useful for maintaining oral hygiene. Taking certain medications, for example, results in reduced saliva production. The consumption of tobacco or alcohol is also responsible for halitosis. The prevalent treatments for halitosis are, as a first step, good oral hygiene. Some specialists recommend, moreover, to exercise a tongue scraping with a brush.

The consumption of candies or chewing gum scented, often acclaimed after a meal, can ephemerally hide the bad breath. But this is not a treatment. Indeed, commercially available candies and chewing gums do not contain effective active ingredients in the removal of malodorous compounds or bacteria.

In terms of treatments using active ingredients, are proposed mouthwashes, based on antiseptics. The use of mouthwashes is perceived as restrictive by the majority of users, especially by the active people, exercising their profession in conditions that do not allow to easily rinse the mouth 3033700 2 after a meal or during A day of work. Access to a washroom, bathroom or at least a sink is necessary. The object of the present invention is to provide a composition for the treatment or inhibition of bad breath by the oral route, which is formulated on the basis of active principles capable of eliminating the bacteria responsible for the synthesis of malodorous compounds or these compounds. same, and that is easy to use, in any place and any circumstance, in a fast, discreet and ambulatory way. To this end, the invention relates to a composition for the treatment or inhibition of bad breath orally in the form of a spray, a spray or a nebulization, containing, as a percentage of weight per unit volume, between 0.15 and 0.25% of an antiseptic compound selected from chlorhexidine, a chlorhexidine salt, octenidine, a salt of octenidine or a mixture of such compounds, and between 1.5 and 2.5% of a zinc salt or a mixture of such salts. Chlorhexidine, of the chemical formula C22H30Cl2N10 (N, N "-1,6-Hexanediylbis [N '- (4-chlorophenyl) (imidodicarbonimidic diamide)]), is an antiseptic of the biguanide group. Bactericidal and bacteriostatic This compound is generally used in the form of a salt, in which it is most soluble in an aqueous medium Its mechanism of action is based on the alteration of the bacterial wall, mainly by the neutralization of the electronegative charges of the wall, leading to the leakage of cellular constituents.It can also attack the cytoplasmic membrane and coagulate compounds of the cytoplasm, leading to the death of the cell by apoptosis. , inactivate the volatile sulfur compounds by converting them to non-volatile sulfur compounds According to one embodiment of the invention, the antiseptic compound is chorhexidine digluconate, chorhex idine gluconate, chorhexidine diacetate or octenidine dihydrochloride, preferably chorhexidine digluconate. Advantageously, the zinc salt is zinc gluconate, zinc digluconate, zinc acetate, zinc citrate or zinc lactate, especially zinc gluconate. The formulation spray, spray or nebulization allows use anywhere and any time. It makes it possible to target the oral areas to be treated: mucous membranes 3033700 3 of the inside of the cheeks, gums, tongue, palate. It does not necessarily require rinsing. According to one embodiment of the invention, the composition comprises between 0.20 and 0.25%, preferentially 0.21% of said antiseptic compound or said mixture of antiseptic compounds. Advantageously, the composition comprises between 1.90 and 2.10%, preferably 2.00% of the zinc salt or of said mixture. Advantageously, the composition comprises one or more excipients chosen from alcohol, one or more surfactants, one or more moisturizing and / or softening agents, one or more pH-regulating agents, one or more flavors, one or more solvents. , one or more flavor enhancers, one or more preservatives, one or more flavors, one or more colorants, or a plurality of thickeners or viscosity control agents. The excipients chosen are those commonly used in the food, pharmaceutical or cosmetic industry. The presence of alcohol in the composition is advantageous because it makes it possible to increase the antibacterial effect, starting from a quantity of 10 g / 100 ml. Advantageously, the composition comprises at least one additional antimicrobial or antiseptic compound. This additional antimicrobial or antiseptic compound is different from and is complementary to those mentioned above. A composition according to the invention may also comprise at least one other active compound against bad breath, such as a plant extract, for example parsley, or an essential oil or an active compound capable of treating another disorder. of the oral cavity as a breath problem. According to a particular embodiment of the invention, the composition further comprises a green tea leaf extract, in particular such an extract containing at least 1% by weight of tannins. Green tea leaf extract is here used as an active ingredient on the treatment and prevention of halitosis. This particular embodiment is preferably intended for tobacco smokers. An extract of green tea leaf is defined in the French pharmacopoeia as obtained from green tea leaves, young, unfermented, and subjected to rapid hot drying. The leaves are from Camellia sinensis L. Kuntze and 3033700 4 of its cultivated varieties. For example, such a green tea extract is marketed by GREENTECH S.A. (France). Advantageously, the pH is between 3 and 5, in particular the pH is 4. A basic medium promotes the proliferation of anaerobic bacteria and therefore bad breath. Therefore, the composition has an acidic pH. According to a particular and preferred embodiment of the invention, the composition comprises, as antiseptic compound, chorhexidine digluconate and zinc salt as zinc gluconate. According to another particular and preferred embodiment of the invention, the composition comprises, as an antiseptic compound, chorhexidine digluconate, octenidine dihydrochloride, and zinc salt as zinc salt. The invention also relates to a composition as defined above for its use in the treatment or prevention of breath disorders, more particularly of oral halitosis, as well as a method of treatment or prevention, cosmetic or therapeutic , breath disorders, more particularly oral halitosis, comprising oral administration by spray, spray or nebulization, of a composition as described above. Advantageously, the composition is delivered in the form of a dose of 50 to 100 microliters (1.1L), preferably 60 to 80 microliters, more preferably microliters. In the present invention, all percentages are percentages of weight per volume, in grams per 100 milliliters. The following examples of formulations of a composition according to the invention.

Example 1: Spray composition against halitosis: 3033700 5 FUNCTION NAME NOMENCLATURE INCI PERCENTAGE (g / 100m1) Solvent Water AQUA 70,9033 Solvent Alcohol ALCOHOL 22,5228 (ethanol) Humectant Hydrolyzate HYDROGENATED 3,5000 STARCH Starch HYDROLYSATE Hydrogenated corn Active ZINC GLUCONATE Gluconate 2.0880 zinc Surfactant no Castor oil PEG-40 HYDROGENATED 0.3000 hydrogenated ionic and CASTOR OIL ethoxylated emulsifier AROMA Flavors Purple Purple 0.2500 Active CHLORHEXIDINE Digluconate 0.2100 Antibacterial chlorhexidine DIGLUCONATE Antiseptic Regulator pH Lactic acid LACTIC ACID 0,1680 Taste enhancer Preservative Aroma Menthol MENTHOL 0,0480 pH regulator Hydroxide of SODIUM HYDROXIDE 0,0099 sodium Total 100,0000 Of which allergens: EUGENOL (flavoring) 0,0030 3033700 6 The composition is presented under a liquid form that is delivered in the form of a spray distributing a dose of 701.it in the oral cavity. Example 2: Halitosis spray composition for smokers: FUNCTION NAME NOMENCLATURE INCI PERCENTAGE (g / 100m1) Solvent Water AQUA 70,82785 Solvent Alcohol ALCOHOL 22,5228 (Ethanol) Humectant Starch HYDROGENATED Hydrolyzate 3,5000 Starch HYDROLYSATE Hydrogenated corn Active ZINC GLUCONATE Gluconate 2.0880 zinc Surfactant no Castor oil PEG-40 HYDROGENATED 0.3000 hydrogenated ion and ethoxylated CASTOR OIL Flavors AROMA 0.3000 Active CHLORHEXIDINE digluconate 0.2100 Antibacterial chlorhexidine DIGLUCONATE Antiseptic pH regulator Lactic acid LACTIC ACID 0,1680 Taste enhancer Preservative Aroma Menthol MENTHOL 0.0480 Humectant Glycerin GLYCERIN 0.02300 pH regulator SODIUM hydroxide HYDROXIDE 0.00990 sodium 3033700 7 Active CAMELLIA SINENSIS extract 0.00100 LEAF EXTRACT tea leaf green Acid pH regulator citric CITRIC ACID 0.00100 Preservative SODIUM BENZOATE 0.00030 Preservative POTASSIUM SORBATE 0.00015 Total 100.0000 Of which allergenic s: EUGENOL (flavor) 0.0030 LIMONENE (fragrance) 0.00105 The liquid form composition is delivered as a spray dispensing a dose of 700 mg into the oral cavity. The compositions of Examples 1 and 2 have been shown to be effective in the treatment and inhibition of halitosis for more than one hour after administration. Rinsing is not necessary. No dental staining is observed. The mouth taste after spraying is now acceptable.

Claims (10)

1) Composition for the treatment or inhibition of bad breath orally in the form of a spray, a spray or a nebulization, containing, in weight percent by volume, between 0.15 and 0 , 25% of an antimicrobial compound selected from chlorhexidine, a chlorhexidine salt, octenidine, a salt of octenidine or a mixture of such compounds, and between 1.50 and 2.50% of a zinc salt or a mixture of such salts. 2) Composition according to claim 1, characterized in that said antimicrobial compound is chorhexidine digluconate, chorhexidine gluconate, chorhexidine diacetate or octenidine dihydrochloride, preferably chorhexidine digluconate. 3) Composition according to claim 1 or 2, characterized in that said zinc salt is zinc gluconate, zinc digluconate, zinc acetate or zinc lactate, in particular zinc gluconate. 4) Composition according to one of the preceding claims, characterized in that it comprises between 0.20 and 0.25%, preferably 0.20% of said antimicrobial compound or said mixture. 5) Composition according to one of the preceding claims, characterized in that it comprises between 1.90 and 2.10%, preferably 2.00% of the zinc salt or said mixture. 6) Composition according to one of the preceding claim, characterized in that it comprises one or more excipients selected from alcohol, one or more surfactants, one or more moisturizing agents and / or softeners, one or more agents regulating pH, one or more flavors, one or more solvents, one or more flavor enhancers, one or more preservatives, one or more fragrances, one or more colorants, or multiple thickeners or viscosity control agents. 3033700 9 7) Composition according to one of the preceding claims, characterized in that it comprises at least one additional antiseptic compound, in particular eugenol. 5 8) Composition according to one of the preceding claims, characterized in that it further comprises a green tea leaf extract, in particular such an extract containing at least 1% by weight of tannins. 9) Composition according to one of the preceding claims, characterized in that the pH is between 3 and 5, preferably 4. 10) Composition as defined in one of claims 1 to 9 for use in the treatment or prevention of breath disorders, more particularly oral halitosis.