WO2006109344A2

WO2006109344A2 - Composition to be used for the treatment of parodontal pathologies

Info

Publication number: WO2006109344A2
Application number: PCT/IT2006/000249
Authority: WO
Inventors: Andrea Monti
Original assignee: Gasparini, Gianluigi
Priority date: 2005-04-13
Filing date: 2006-04-13
Publication date: 2006-10-19
Also published as: ITRM20050179A1; WO2006109344A3

Abstract

A composition to be used for the treatment and the prevention of parodontal pathologies which is prepared by micro-encapsulation of slow release capsules.

Description

Composition to be used for the treatment of parodontal pathologies

The present invention relates to pharmaceutical products, particularly those for dentistry. A composition is disclosed which is able to prepare products for use both in dentist's surgery and at home for the treatment and prevention of parodontal diseases .

Periodontium is the apparatus supporting a tooth and consists of gum, parodontal ligament, alveolar bone, and cement. Parodontal diseases or parodontal pathologies affect then the tooth supporting system and can cause a loosening and even the loss of the tooth as they progress.

The sparking factors are different: an insufficient dental cleaning with the consequence of bacterial dental plague and tartar deposit which causes processes of inflammation and mechanical irritations due to residual food deposit, dental traumas, anomalous tooth alignment, tooth filling or dental prosthesis. Further pathologies such as malnutrition, diabetes mellitus or blood pathologies or the prolonged use of some drugs can help the onset of diseases of the periodontium too.

Therefore, the need for the preparation of pharmaceutical products that can be used for the treatment and prevention of parodontal diseases makes itself particularly felt.

The inventors of the present invention have set up a combination of natural extracts comprising propolis, ϋncaria Tomentosa, Aloe Vera Barbadensis, Calendula, Vitamin K, Coenzyme QlO, vitamin ed extract of grapefruit seeds, the single functions of which are listed below.

The effectiveness of propolis in the treatment of disease of the gum system is known at the state of art

(Monti A., Gasparini G., Zegarelli P. T., Battaglia G.

Attual. Odontostomatol. , XVIII, 3, 2002). Propolis is really effective as natural antibiotic.

Uncaria Tomentosa has antibacterial, antimycotic, decongestant, cicatrizant properties (Taylor L., Herbal Secrets of the Rainforest, 2nd ed. , Sage press, Inc. , 2002) .

Aloe Vera Barbadensis is a natural substance with antibacterial activity particularly to Stafilococco Aureo, Streptococcus Viridans, Streptococcus Mutans, Corynebacterium xerosis, antiviral, fungicidal activity (Candida Albicans), virucide activity (Herpes simplex and Herpes zoster) , anti-inflammatory activity, stabilizes and help the recovery of hurts and burns because of its easy penetration of the deepest epithelial layers. Clinical studies comparing the anti-inflammatory effectiveness of Aloe Vera with prednisolone and indomethacin have found similar effects (Sims R. M., Zimmermann E. R., report of effect of Aloe Vera on growth of certain micro-organisms. Ava Inc. Archivies, 1:230-233, 1969).

Calendula is a vegetal antioxidant and a natural antiinflammatory. Vitamin Kl is a specific anti-hemorrhagic agent. Coenzyme QlO is a natural bearer of folic acid. Vitamin C is astringent and antioxidant. GSE, extract of grapefruit seeds, has a natural marked antibiotic action over a wide germ spectrum such as: Staphylococcus, Streptococcus, Salmonella, Escherichia CoIi, Pseudomonas, Lactobacillus, Klebsiella , Shigella , Legionella pneumophila , Chlamidia, Helicobacter pylori, Herpes, Candida albicans, Aspergillus, Trocophyton and other fungus and ferments. Its action affects the cytoplasmic membrane of the micro-organisms where its proximate principles upset the structure thereof, thus preventing amino acids from being absorbed and inducing portions with low molecular weight to come out of the cells ("Grapefruit Seed Extract", Alt. Med. Dig. USA, 7, 1994) . Said proximate principles are not known in the form allowing them to be used in dentistry.

Typically, propolis is used as hydroalcoholic extract of propolis which is liquid and allows only a short- time application which is non-effective to develop the antibiotic, anti-inflammatory action at the gum groove.

Also Uncaria Tomentosa is typically used in the form of fluid extract which can stay in situ, i.e. the gum groove, only for a short time. Conversely, the composition which is the object of the present invention allows the single components to be available and active at the periodontium and at the same time their combination allows the therapeutic effectiveness to be increased synergistically . According to another advantageous feature, the preparation of said composition by micro-encapsulation in non-phospholipidic vesicles allows a slower transdermic release of the active components and a greater stability of the latter.

A further embodiment of the invention consists of different formulations that can be used according to the parodontal disease to be faced. In particular there is provided:

- a preparation provided for use in dentist' s surgery and to be used after parodontal treatments (tartar ablation, courettage above and under gums, parodontal interventions) ; - a preparation for use at home in prolonged treatments;

- a preparation to carry on the therapy through the daily dental care in the form of toothpaste or mouthwash. Therefore, an object of the present invention is a composition that can be used for the preparation of a medicine for the treatment and prevention of parodontal pathologies having the following composition referred to 1000 g of product: Propolis 15-30 g

Uncaria Tomentosa 5-10 g

Calendula 15-30 g

Aloe Vera 10-20 g

Vitamin C 1-5 g Vitamin Kl 5-10 g

Dry extract of GSE 15-30 g optionally added with coenzyme QlO 10-20 g. The composition also provides the addition of suitable excipients selected from the group consisting of: fructose, hydroxymethyl cellulose, glycerol, mint extract, and water. The single formulations for use both in dentist's surgery and at home are listed below as embodiments of the invention, all referred to 1000 g of product.

1. Formulation for use in dentist's surgery:

Propolis 30 g Uncaria Tomentosa 10 g

Calendula 30 g

Aloe Vera 20 g

Vitamin C 5 g

Coenzyme QlO 20 g Vitamin Kl 10 g

Dry extract of GSE 30 g

Fructose 20 g

Hydroxymethyl cellulose 18 g

Glycerol 80 g Mint extract 1 g

Water 726 g

2. Formulation for use at home in prolongjeΘdQ. tI Lrieead.tLmlLLecnt:

Propolis 15 g

Uncaria Tomentosa 5 g Calendula 15 g

Aloe Vera 10. g

Vitamin C 5 g

Vitamin Kl 10 g

Dry extract of GSE 15 g Fructose 10 g

Hydroxymethyl cellulose 18 g

Glycerol 80 g

Mint extract o, 5 g

Water 816, 5 g 3. Formulation for dental care in tthhee ffoorrmm of toothpaste :

Propolis 20 g Uncaria Tomentosa 10 g

Calendula 20 g

Aloe Vera 10 g

Vitamin C 5 g Coenzyme QlO 10 ^' g

Vitamin Kl 10 g

Dry extract of GSE 20 g

Fructose 10 g

Hydroxymethyl cellulose 18 g Glycerol 80 g

Mint extract o, 5 g

Water 786, 5 g

4. Formulation for dental care in tthhee ffoorrmm of mouthpaste : Propolis 20 g

Uncaria Tomentosa 10 g

Calendula 20 g

Aloe Vera 10 g

Vitamin C 5 g Coenzyme QlO 10 g

Vitamin Kl 10 g

Dry extract of GSE 20 g

Fructose 10 g

Mint extract 0, 5 g Water 884, 5 g

Claims

1. A composition to be used to prepare a medicine for the treatment and the prevention of parodontal pathologies comprising in 1000 g of product:

Propolis 15-30 g Uncaria Tomentosa 5-10 g

Calendula 15-30 g

Aloe Vera 10-20 g

Vitamin C 1-5 g

Vitamin Kl 5-10 g Dry extract of GSE 15-30 g and suitable pharmacologically acceptable excipients .

2. The composition according to claim 1, further comprising 10 to 20 g coenzyme QlO.

3. The composition according to claim 1 for professional service in dentist's surgery having the following composition in 1000 g of product: Propolis 30 g

Uncaria Tomentosa 10 g

Calendula 30 g

Aloe Vera 20 g

Vitamin C 5 g Coenzyme QlO 2O g

Vitamin Kl 1O g

Dry extract of GSE 30 g

Fructose 20 g

Hydroxymethyl cellulose 18 g Glycerol 8O g

Mint extract 1 g

Water 726 g

4. The composition according to claim 1 for use at home in prolonged treatments having the following composition in 1000 g of product:

Propolis ^■ 15 g

Uncaria Tomentosa 5 g Calendula 15 g

Aloe Vera 10 g

Vitamin C 5 g

Vitamin Kl 1O g

Dry extract of GSE 15 g Fructose 10 g

Hydroxymethyl cellulose 18 g

Glycerol 80 g

Mint extract 0,5 g

Water 816,5 g

5. The composition according to claim 1 for dental care in the form of toothpaste having the following composition:

Propolis 20 g ϋncaria Tomentosa 10 g

Calendula ^" 20 g

Aloe Vera 10 g

Vitamin C 5 g

Coenzyme QlO 10 g Vitamin Kl 10 g

Dry extract of GSE 20 g

Fructose 10 g Hydroxymethyl cellulose 18 g

Glycerol 80 g

Mint extract 0,5 g

Water 786,5 g

6. The composition according to claim 1 for dental care in the form of mouthwash having the following composition:

Propolis 20 g Uncaria Tomentosa 10 g

Calendula 20 g

Aloe Vera 10 g

Vitamin C 5 g

Coenzyme QlO 10 g Vitamin Kl 10 g

Dry extract of GSE 20 g

Fructose 10 g

Mint extract 0,5 g

Water 884,5 g

7. The composition according to any preceding claim, characterized in that it is able to be prepared by micro-encapsulation in non-phospholipidic vesicles, thus providing a slower transdermic release of the active components and a greater stability of the latter.