FR2662352A1 - Gum-hygiene and health products based on elastin peptides - Google Patents

Gum-hygiene and health products based on elastin peptides Download PDF

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FR2662352A1
FR2662352A1 FR9006517A FR9006517A FR2662352A1 FR 2662352 A1 FR2662352 A1 FR 2662352A1 FR 9006517 A FR9006517 A FR 9006517A FR 9006517 A FR9006517 A FR 9006517A FR 2662352 A1 FR2662352 A1 FR 2662352A1
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hygiene
health products
peptides
elastin
gums according
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FR2662352B1 (en
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Jean Jacques Goupil
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Cosmetics (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Gum-hygiene and health products intended for limiting or even destroying the effects of elastase type proteases on connective tissue, which contain type C45 elastin peptides in a concentration of between 0.25 mg/ml and 20 mg/ml, and preferably of 2.5 mg/ml.

Description

PRODUITS D'HYGIENE ET DE SANTE POUR LES GENCIVES A BASE DE
PEPTIDES D'ELASTINE
La présente invention est relative à des produits d' hygi ène et de santé pour les gencives notamment pâte gingivale, bain de bouche, gel traitant ou autre, permettant de réaliser, corrélativement à une action de nettoyage ou de désinfection des gencives ou de la cavité buccale, une action efficace contre les élastases présentes au niveau de la gencive et qui conduisent généralement à une atrophie progressive et à un vieillissement du tissu conjonctif et, parfois à des manifestations inflammatoires souvent douloureuses.HYGIENE AND HEALTH PRODUCTS FOR GENDER-BASED
ELASTINE PEPTIDES
The present invention relates to hygiene and health products for the gums, in particular gingival paste, mouthwash, treating gel or the like, making it possible to carry out, correlatively to a cleaning or disinfecting action on the gums or the cavity. buccal, an effective action against the elastases present on the level of the gum and which generally lead to a progressive atrophy and to an aging of the connective tissue and, sometimes to inflammatory manifestations often painful.

On sait que les cellules musculaires lisses comme les cellules mésenchymateuses du genre des fibroblastes produisent naturellement des enzymes du genre. protéases et plus particulièrement du type élastases. La synthèse de ces enzymes augmente avec l'âge des individus et les conditions pathologiques éventuelles.On sait également que les élastases jouent un rôle important dans le déchaussement des dents de par leur action sur le tissu conjonctif qu' elles atrophient, cette action étant d'autant plus préjudiciable qu' à la production intrinsèque d' élastases par des cellules elles-memes, s' ajoutent souvent des infections locales, dues à des germes ou bactéries, capables également de produire de tels enzymes et d' attaquer les constituants des tissus conjonctifs. It is known that smooth muscle cells like mesenchymal cells of the fibroblast genus naturally produce enzymes of the genus. proteases and more particularly of the elastase type. The synthesis of these enzymes increases with the age of the individuals and the possible pathological conditions. We also know that elastases play an important role in the loosening of teeth by their action on the connective tissue that they atrophy, this action being d 'all the more harmful than the intrinsic production of elastases by cells themselves, are often added local infections, due to germs or bacteria, also capable of producing such enzymes and attacking the constituents of tissues conjunctives.

I1 s' avère donc particulièrement intéressant de pouvoir réaliser une inhibition efficace de 1' action de ces enzymes élastasiques et d'assurer ainsi un traitement amélioré des parodontopathies superficielles. It therefore turns out to be particularly advantageous to be able to effect effective inhibition of the action of these elastatic enzymes and thus to ensure an improved treatment of superficial periodontal diseases.

La présente invention a pour objet un produit d'hygiène et de santé gingivale qui répond à cet objectif de manière particulièrement intéressante, notamment quant à la permanence de son activité et à 1' efficacité des résultats obtenus contre 1' atrophie des gencives et les gingivites, et par suite sur les pertes dentaires qui en sont souvent la conséquence. The subject of the present invention is a gingival hygiene and health product which responds to this objective in a particularly advantageous manner, in particular as regards the permanence of its activity and the effectiveness of the results obtained against atrophy of the gums and gingivitis. , and consequently on the dental losses which are often the consequence.

A cet effet, les produits considérés, destines à limiter, voire à annihiler les effets des protéases de type élastasiques sur les tissus conjonctifs, se caractérisent en ce qu'ils comportent, en proportions et concentrations déterminées, des peptides d' élastine. To this end, the products under consideration, intended to limit, or even annihilate the effects of proteases of the elastatic type on the connective tissues, are characterized in that they contain, in determined proportions and concentrations, elastin peptides.

De préférence, les peptides d' élastine mis en oeuvre dans les produits considérés sont des peptides de type C 45, la concentration en peptides étant comprise entre 0,25 mg/ml et 20 mg/ml, et de préférence approximativement voisine de 2,5 mg/ml. Preferably, the elastin peptides used in the products under consideration are type C 45 peptides, the concentration of peptides being between 0.25 mg / ml and 20 mg / ml, and preferably approximately around 2, 5 mg / ml.

Avantageusement, les peptides présentent un poids moléculaire compris entre 5.000 et 150.000, et de préférence voisin de 45. 000. De préférence également, ces peptides sont réalisés à partir d'une hydrolyse de fibres élastiques provenant d'un prélèvement de nuque de boeuf et d' activité inhibitrice mesurée sur un substrat synthétique de séquence Suc (Ala) 3 pNA. Advantageously, the peptides have a molecular weight of between 5,000 and 150,000, and preferably close to 45,000. Preferably also, these peptides are produced from a hydrolysis of elastic fibers originating from a sample from the nape of the ox and of inhibitory activity measured on a synthetic substrate of sequence Suc (Ala) 3 pNA.

Des expérimentations ont été conduites par le
Professeur Ladislas ROBERT. Le tableau ci-après fournit les résultats d'expérimentations effectuées sur des prélèvements ou biopsies de gencives de sujets atteints de parodontopathies diverses, notamment de gingivites correspondant notamment aux stades 2 ou 3 de l'indice de
LOE et SILNESS (1963), confirmées par des photographies endobuccales, sans atteinte significative de l'os alvéolaire, 1' état pathologique ainsi constaté n'étant pas dû à une cause hormonale ou médicamenteuse susceptible de fausser la mesure.Experiments have been conducted by the
Professor Ladislas ROBERT. The table below provides the results of experiments carried out on samples or biopsies of gum tissue from subjects suffering from various periodontopathies, in particular gingivitis corresponding in particular to stages 2 or 3 of the index of
LOE and SILNESS (1963), confirmed by intraoral photographs, without significant damage to the alveolar bone, the pathological condition thus observed not being due to a hormonal or medicinal cause liable to distort the measurement.

Biopsie Concentration en peptides at élastine C 45
0 0,025 0,25 1 2,5 10 20
1- 0,832 0,777(7%) 0,399(52%) 0,250(70%) 0,050(941) 0,010(99%) 0,005(99)
2- 0,271 0,262(3%) 0,144(47%) 0,088(68%) 0,038(86%) 0,021(92%) 0,002(99%)
3- 0,450 0,040(11%) 0,027(40%) 0,021(53%) 0,016(64%) 0,015(67%) 0,007(82%)
4- 0,444 0,431(3%) 0,209(53%) 0,115(74%) 0,021(958) 0,003(99%) 0,0-lOt98%)
5- 0,384 0,357(7%) 0,190(51%) 0,092(75%) 0,017(96%) 0,012(97%) 0,014(96)
6- 0,184 0,175(5%) 0,93(49%) 0,068(63%) 0,011(94%) 0,003(99%) 0,001(99%)
Les chiffres donnés dans ce tableau fournissent, pour une série d'échantillons successifs, des résultats mesurant le taux en % dtinhibition de l'activité élestasique en fonction de la concentration en peptides de C 45, utilisant comme substrat le Suc (Ala) 3 pNA.Biopsy Concentration of peptides at elastin C 45
0 0.025 0.25 1 2.5 10 20
1- 0.832 0.777 (7%) 0.399 (52%) 0.250 (70%) 0.050 (941) 0.010 (99%) 0.005 (99)
2- 0.271 0.262 (3%) 0.144 (47%) 0.088 (68%) 0.038 (86%) 0.021 (92%) 0.002 (99%)
3- 0.450 0.040 (11%) 0.027 (40%) 0.021 (53%) 0.016 (64%) 0.015 (67%) 0.007 (82%)
4- 0.444 0.431 (3%) 0.209 (53%) 0.115 (74%) 0.021 (958) 0.003 (99%) 0.0-10% 98)
5- 0.384 0.357 (7%) 0.190 (51%) 0.092 (75%) 0.017 (96%) 0.012 (97%) 0.014 (96)
6 - 0.184 0.175 (5%) 0.93 (49%) 0.068 (63%) 0.011 (94%) 0.003 (99%) 0.001 (99%)
The figures given in this table provide, for a series of successive samples, results measuring the rate in% of inhibition of the elestastic activity as a function of the concentration of C 45 peptides, using as substrate Suc (Ala) 3 pNA .

On constate ainsi que le taux dtinhibition , qui s' élève déjà à 50 % environ pour une concentration en peptides de 0,25 mg/ml, atteint ou dépasse pratiquement 90 % pour une concentration de 2,5 mg/ml et s' approche de 99 % pour une concentration allant de 10 à 20 mg/ml. It can thus be seen that the inhibition rate, which already amounts to approximately 50% for a peptide concentration of 0.25 mg / ml, reaches or exceeds practically 90% for a concentration of 2.5 mg / ml and is approaching 99% for a concentration ranging from 10 to 20 mg / ml.

Il résulte des diverses expérimentations cliniques in vivo ainsi que des expériences in vitro que les nouvelles préparations à base de peptides d'élastine selon 1' invention sont très efficaces dans le traitement des parodontes en ce qu' elles inhibent de façon très importante l'activité élastasique. It follows from various clinical experiments in vivo as well as from in vitro experiments that the new preparations based on elastin peptides according to the invention are very effective in the treatment of periodonts in that they very significantly inhibit the activity elastatic.

A partir de des constatations, on a considéré selon la présente invention que l'apport par voie locale de ces préparations à base de peptides d' élastine, au tissu gingival, entrainerait une réduction des phénomènes inflammatoires. From observations, it has been considered according to the present invention that the local supply of these preparations based on elastin peptides, to the gum tissue, would lead to a reduction in inflammatory phenomena.

Selon la présente invention et à titre d' exemples indicatifs mais non limitatifs, on donne ci-après diverses formulations de produits d'hygiène incorporant des peptides d'élastine solutilisés dans des excipients appropriés et dont 1' activité sur les protéases élastasiques se révèle particulièrement efficace dans les conditions de l'utilisation de ces produits. According to the present invention and by way of indicative but nonlimiting examples, various formulations of hygienic products are given below incorporating elastin peptides used in suitable excipients and the activity of which on elastatic proteases is particularly revealed effective under the conditions of use of these products.

Exemple 1 - Pâte gingivale N 1
- Glycérine 5 %
- Sorbitol (70 %) 5 %
- Gel 1 %
- Conservateur 0,1 %
- Saccharinate de sodium 0,1
- Phosphate di cal ci que 37 %
- Laurylsulfate de sodium 1
- Diatami 15-40 microns 5 %
- Arôme 1 %
- Elastine 1 %
- Eau QSP 100 %
Exemple 2 - Pâte gingivale N 2
- Veegum 1 %
- Carboxyméthyl cellulose sodique 0, 5 %
- Glycérine 30 %
- Phosphate di cal cique 47 %
- Laurylsulfate de sodium 2 %
- Conservateur 0, 3 %
- Arôme 1 %
- Elastine 2
- Eau QSP 100 %
Exemple 3 - Gel gingival
- Hexamétaphosphate 0,20 %
- Phosphate disodique 0,10
- Saccharinate de sodium 0,02 %
- Carboxyméthyl cellulose sodique 0,55 %
- Silice liquide (Sident 22 S) 12,00 %
- Polyéthylène glycol (PEG 400) 3,50 %
- Sorbitol (70%) 68,00 %
- Conservateur 0,30 %
- Arôme 0,50 %
- Elastine 5,00 %
- Eau QSP 100 %
Exemple 4 - Bain de bouche
- Essence de menthe hydrosoluble 2,00 %
- Saccharinate de sodium 0, 50 %
- Huile de castor hydrogénéé
(Arlatone 975) 2,00 %
- Aromatisation menthe (Frescofor) 0, 50 %
- Conservateur (parahydroxybenzoate
de méthyle) 0,20 %
- Elastine 0, 50 %
- Eau QSP 100 % Example 1 - Gingival paste N 1
- Glycerin 5%
- Sorbitol (70%) 5%
- Gel 1%
- Preservative 0.1%
- Sodium saccharinate 0.1
- Phosphate di cal ci that 37%
- Sodium lauryl sulfate 1
- Diatami 15-40 microns 5%
- Aroma 1%
- Elastin 1%
- 100% QSP water
Example 2 - Gingival paste N 2
- Veegum 1%
- Carboxymethyl cellulose sodium 0.5%
- Glycerin 30%
- Calcium phosphate 47%
- Sodium lauryl sulfate 2%
- Preservative 0.3%
- Aroma 1%
- Elastin 2
- 100% QSP water
EXAMPLE 3 Gingival Gel
- Hexametaphosphate 0.20%
- Disodium phosphate 0.10
- 0.02% sodium saccharinate
- Carboxymethyl cellulose sodium 0.55%
- Liquid silica (Sident 22 S) 12.00%
- Polyethylene glycol (PEG 400) 3.50%
- Sorbitol (70%) 68.00%
- Preservative 0.30%
- Aroma 0.50%
- Elastin 5.00%
- 100% QSP water
Example 4 - Mouthwash
- Essence of water-soluble mint 2.00%
- Sodium saccharin 0.50%
- Hydrogenated beaver oil
(Arlatone 975) 2.00%
- Mint flavoring (Frescofor) 0, 50%
- Preservative (parahydroxybenzoate
methyl) 0.20%
- Elastin 0.50%
- 100% QSP water

Claims (9)

1- Produits d'hygiène et de santé pour les gencives destinés à limiter ou même anihiler les effets des protéases de type élastatiques sur les tissus conjonctifs, caractérisés en ce qu'ils comportent, en proportion et concentration déterminées, des peptides d' élastine. 1- Hygiene and health products for the gums intended to limit or even annihilate the effects of elastatic type proteases on the connective tissues, characterized in that they contain, in determined proportion and concentration, elastin peptides. REVENDICATIONS 2- Produits d' hygiène et de santé pour les gencives selon la revendication 1, caractérisés en que que la concentration en peptides d'élastine est comprise entre 0, 25 mg/ml et 20mg/ml et de préférence voisine de 2, 5 mg/ml. 2- hygiene and health products for the gums according to claim 1, characterized in that the concentration of elastin peptides is between 0.25 mg / ml and 20 mg / ml and preferably close to 2.5 mg / ml. 3- Produits d'hygiène et de santé pour les gencives selon 1' une des revendications 1 ou 2, caractérisés en ce que les peptides d'élast:.ne sont des peptides de type C 45. 3- Hygiene and health products for the gums according to one of claims 1 or 2, characterized in that the elast peptides: are not type C 45 peptides. 4- Produits d'hygiène et de santé pour les gencives selon 1' une quelconque des rev ndi cations 1 à 3, caractérisés en ce que les peptides sont obtenus par hydrolyse de fibres élastiques dont 1' activité inibitrice est mesurée sur un substrat de séquence Suc (Ala) 3 pNA. 4- Hygiene and health products for the gums according to any one of rev ndi cations 1 to 3, characterized in that the peptides are obtained by hydrolysis of elastic fibers, the inibitating activity of which is measured on a substrate of sequence Suc (Ala) 3 pNA. 5- Produits d'hygiène et de santé pour les gencives selon la revendication 4, caractérisés en que les fibres élastiques sont prélevés sur une nuque de boeuf. 5- hygiene and health products for the gums according to claim 4, characterized in that the elastic fibers are taken from a neck of beef. 6- Produits d'hygiène et de santé pour les gencives selon 1' une quelconque des revendications 1 à 5, caractérisés en ce que les peptides d'élastine sont obtenues par synthèse. 6. Hygiene and health products for the gums according to any one of claims 1 to 5, characterized in that the elastin peptides are obtained by synthesis. 7- Produits d'hygiène et de santé pour les gencives selon l'une quelconque des revendications 1 à 6, caractérisés en ce qu'ils constituent une pâte gingivale dans laquelle ltélastine entre pour une proportion de 1 à 2 % environ. 7- Hygiene and health products for the gums according to any one of claims 1 to 6, characterized in that they constitute a gingival paste in which ltélastine enters for a proportion of 1 to 2% approximately. 8- Produits d'hygiène et de santé pour les gencives selon 1' une quelconque de revendications 1 à 6, caractérisée en ce qu' ils constituent un gel gingival dans 1' élastine entre pour une proportion de 5 % environ.  8- Hygiene and health products for the gums according to any of claims 1 to 6, characterized in that they constitute a gingival gel in elastin between for a proportion of approximately 5%. 9- Produits d'hygiène et de santé pour les gencives selon l'une quelconque des revendication 1 à 6, caractérisés en ce qu'ils constituent un bain de bouche dans lequel l'élastine entre pour une proportion de 0,5 % environ.  9- Hygiene and health products for the gums according to any one of claims 1 to 6, characterized in that they constitute a mouthwash in which the elastin enters for a proportion of approximately 0.5%.
FR9006517A 1990-05-25 1990-05-25 HYGIENE AND HEALTH PRODUCTS FOR GENCIVES BASED ON ELASTINE PEPTIDES. Expired - Fee Related FR2662352B1 (en)

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2353282A1 (en) * 1976-06-02 1977-12-30 Invap Etablissement APPLICATION OF ELASTIN AND ITS DERIVATIVES IN COSMETICS
JPS6289609A (en) * 1985-10-16 1987-04-24 Shiseido Co Ltd Clear aqueous gel cosmetic
FR2618679A1 (en) * 1987-07-30 1989-02-03 Bonnaure Mallet Martine Use of elastin for the preparation of a pharmaceutical composition which is useful in the treatment of periodontal disorders
JPH01283213A (en) * 1988-05-09 1989-11-14 Tadao Shiraishi Toiletry product blended with enzyme

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2353282A1 (en) * 1976-06-02 1977-12-30 Invap Etablissement APPLICATION OF ELASTIN AND ITS DERIVATIVES IN COSMETICS
JPS6289609A (en) * 1985-10-16 1987-04-24 Shiseido Co Ltd Clear aqueous gel cosmetic
FR2618679A1 (en) * 1987-07-30 1989-02-03 Bonnaure Mallet Martine Use of elastin for the preparation of a pharmaceutical composition which is useful in the treatment of periodontal disorders
JPH01283213A (en) * 1988-05-09 1989-11-14 Tadao Shiraishi Toiletry product blended with enzyme

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
PATENT ABSTRACTS OF JAPAN, vol. 11, no. 297 (C-448)[2744], 25 septembre 1987; & JP-A-62 89 609 (SHISEIDO CO.) 24-04-1987 *
PATENT ABSTRACTS OF JAPAN, vol. 14, no. 57 (C-684)[4000], 2 février 1990; & JP-A-01 283 213 (TADAO SHIRAISHI) 14-11-1989 *

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