Title of Invention	"A COMPOSITION, FOR THE TREATMENT OF AN AFECTION OF THE ORAL CAVITY AND UPPER RESPIRATORY TRACT"
Abstract	The present invention is related to a composition, for the treatment of an affection of the oral cavity and upper respiratory tract, comprising: 1-200 mg anthocyanosides; 1-200 mg procyanidins; and 1-200 mg floroglucinols, wherein the anthocyanosides are derived from a Vaccinium myrtillus extract, the procyanidins are derived from a Vitis vinifera extract, a Camellia sinensis extract or from another edible plant containing the procyanidins, and the floroglucinols are derived from Hypericum spp., Mirtus spp. or Humulus lupulus extracts.

Title of Invention

"A COMPOSITION, FOR THE TREATMENT OF AN AFECTION OF THE ORAL CAVITY AND UPPER RESPIRATORY TRACT"

Abstract

The present invention is related to a composition, for the treatment of an affection of the oral cavity and upper respiratory tract, comprising: 1-200 mg anthocyanosides; 1-200 mg procyanidins; and 1-200 mg floroglucinols, wherein the anthocyanosides are derived from a Vaccinium myrtillus extract, the procyanidins are derived from a Vitis vinifera extract, a Camellia sinensis extract or from another edible plant containing the procyanidins, and the floroglucinols are derived from Hypericum spp., Mirtus spp. or Humulus lupulus extracts.

Full Text	COMPOSITIONS FOR THE TREATMENT OF AFFECTIONS OF THE ORAL CAVITY AND UPPER RESPIRATORY TRACT The present invention relates to compositions containing anthocyanosides and/or procyanidins in combination with floroglucinols for the treatment of the affections of the oral cavity and upper respiratory tract. TECHNOLOGICAL BACKGROUND Throat redness and inflammation, with formation of plaques, usually accompany common influenza, coryza and other cold diseases. Common cold and influenza, which on the average affect up to three times a year both children and adults, are related to mild viral infections caused by rhinovirus (40%), coronavirus (10%) and, to a less extent, adenovirus and parainfluenza viruses. Although no specific treatments exist for these pathologies, antihistamines and decongestants are considered useful, as the edema reduction alleviates pain and makes the course of the disease shorter. DISCLOSURE OF THE INVENTION The present invention relates to compositions containing: a) anthocyanosides, and/or b) procyanidins, and c) floroglucinols, useful for the treatment of the affections of the oral cavity and upper respiratory tract. According to the present invention, the compositions contain 1 to 200 mg of anthocyanosides, and/or 1 to 200 mg of procyanidins, and 1 to 200 mg of floroglucinols. According to the present invention, "anthocyanosides" includes both real anthocyanosides and anthocyanidins, their aglycones. The anthocyanosides preferably are derived from Vaccinium myrtillus extracts. The extract of bilberry (Vaccinium myrtillus), as described in literature, has marked antiinflammatory activity, in particular topically, due to its action on capillary permeability and fragility. The preparation of bilberry extracts containing anthocyanosides is known to those skilled in the art. Bilberry anthocyanosides and procyanidins exert bacteriostatic action which prevents bacterial and fungal adhesion, for example at the dental and paradental level and on mucous membranes. •** According to the present invention, the procyanidins can preferably be derived from Vitis vinifera extracts, obtained as disclosed in GB 1,541,469, or from Camellia sinensis extracts, as disclosed in EP 0 814 823, or from other plants, preferably edible, containing them. Floroglucinols exert strong bacteriostatic action on a great number of bacteria and fungi strains. The minimum inhibitory concentration values of some floroglucinols on gram+ bacteria, gram- anaerobic bacteria and strains of Candida albicans range from 0.5 to 4 ug/ml. According to the present invention, floroglucinols can be derived from Hypericum spp. extracts, preferably Hypericum perforatum, or from Mirtus spp. extracts, preferably Mirtus communis, or from Humulus spp. fractions, preferably Humulus lupulus, enriched in a and (3 acids. According to the invention, the fraction of p-acids prepared from Humulus lupulus contains 20 to 80%, preferably 60%, of floroglucinols expressed as colupulone; the fraction of a-acids contains 20 to 80%, preferably 60%, of humulone. According to the present invention, among the Hypericum sp. extracts, particularly preferred is a Hypericum perforatum extract with a floroglucinols (adhyperforin/hyperforin) content ranging from 20 to 80%, preferably 60%. According to the present invention, the Mirtus communis extract is prepared from the leaves, by extraction with carbon dioxide under conditions of pressure ranging from 235 to 260 bars and temperatures ranging from 40 to 60°C, preferably 45°C. The resulting extract usually has a mirtocumolone content of 35%. The compositions of the invention are capable of preventing the formation of purulent plaques deriving from various saprophytic infections of the oral cavity, thus avoiding the use of antibiotics, while reducing the progress of the infection. In particular, the compositions of the invention proved to exert a synergistic effect mainly as regards the duration of the disease. Furthermore, the compositions of the invention exert favourable action on the cleanliness of the oral cavity and the removal of the dental plaque, thanks to the effect reducing bacterial adhesiveness, as already mentioned, exerted by bilberry extract and procyanidins, and to the high activity of floroglucinols on anaerobic bacterial strains. The pharmaceutical compositions will be preferably presented in the form of tablets for the slow dissolution in the oral cavity or chewing gums which provide the slow release of the active principles. These compositions are used in preventive and prophylactic treatments as well as for the hygiene of the oral cavity. According to a further preferred aspect, the compositions of the present invention will further contain essential oils, in particular mint oil. According to a further preferred aspect; .the compositions of the present invention will further contain a Glycyrrhiza extract, preferably having a content in glycyrrhizic acid of 10%. The present invention, therefore, relates to compositions for the treatment of the affections of the oral cavity and upper respiratory tract, containing the combinations described above. Said compositions will be prepared according to conventional methods well known in pharmaceutical technique, as those described in "Remington's Pharmaceutical Handbook", Mack Publishing Co., N.Y., USA, together with suitable excipients commonly used in the art. The present invention also relates to the use of a combination of anthocyanosides, and/or procyanidins, and floroglucinols, for the preparation of a medicament for the treatment of the affections of the oral cavity and upper respiratory tract. The examples reported hereinbelow further illustrate the invention. Example I - Tablets Each 500 mg tablet contains: Vaccinium myrtillus extract (25% in anthocyanidins) 60 mg Humidus lupulus extract (60% in floroglucinols) 10 mg Soy lecithin (30% phosphatidylcholine) 30 mg Glycyrrhiza extract (10% of glycyrrhizic acid) 20 mg Mint essential oil 10 mg Saccharose 200 mg Maltodextrin 150 mg Acacia gum 15 mg Magnesium stearate . 5 mg Example II - Tablets Each 500 mg tablet contains: Vitis vinifera extract (95% in procyanidins) 80 mg Humulus lupulus extract (60% in floroglucinols) lOmg Soy lecithin (30% phosphatidylcholine) 30 mg Glycyrrhiza extract (10% of glycyrrhizic acid) 20 mg Mint essential oil 10 mg Mannitol 320 mg Povidone 20 mg Silicium dioxide 5 mg Magnesium stearate 5 mg Example III - Tablets Each 500 mg tablet contains: Vitis vinifera extract (95% in procyanidins) 80 mg Mirtus communis lipophilic extract (35% in mirtocupulone) 10 mg Glycyrrhiza extract (10% of glycyrrhizic acid) 20 mg Mint essential oil 10 mg Maltodextrin 332 mg Sodium saccharin 3 mg Arabic gum 30 mg Talc lOmg Magnesium stearate 5 mg Example IV - Tablets Each 500 mg tablet contains: Vacciniwn myrtillus extract (25% in anthocyanidins) 60 mg Mirtus communis lipophilic extract (35% in mirtocupulone) lOmg Soy lecithin (30% phosphatidylcholine) 30 mg Glycyrrhiza extract (10% of glycyrrhizic acid) 20 mg Mint essential oil 10 mg Saccharose 330 mg Tragacanth gum 20 mg Silicium dioxide 5 mg Magnesium stearate 5 mg Example V - Tablets Each 500 mg tablet contains: Camellia sinensis extract (70% in procyanidole oligomers) 80 mg Humulus lupulus extract (60% in floroglucinols) 10 mg Soy lecithin (30% phosphatidylcholine) 30 mg Glycyrrhiza extract (10% of glycyrrhizic acid) 20 mg Mint essential oil 10 mg Mannitol 320 mg Povidone 20 mg Silicium dioxide 5 mg Magnesium stearate 5 mg Example VI - Tablets Each 500 mg tablet contains: Camellia sinensis extract (70% in procyanidole oligomers) 80 mg Hypericum perforatum extract (60% in floroglucinols) 10 mg Soy lecithin (30% phosphatidylcholine) 30 mg Glycyrrhiza extract (10% of glycyrrhizic acid) 20 mg Mint essential oil 10 mg Mannitol 320 mg Povidone 20 mg Silicium dioxide 5 mg Magnesium stearate 5 mg Example VII - Chewing Gum Each 2000 mg chewing gum contains: Vitis vinifera extract (95% in procyanidins) 80 mg Mirtus communis lipophilic extract (30% in mirtocupulone) 10 mg Glycyrrhiza extract (10% of glycyrrhizic acid) 20 mg Mint essential oil 10 mg Gum base 1598 mg Xylitol 250 mg Aspartame 2 mg Magnesium stearate 15 mg Talc 15 mg We Claim: 1. A composition, for the treatment of an affection of the oral cavity and upper respiratory tract, comprising: 1-200 mg anthocyanosides; 1-200 mg procyanidins; and 1-200 mg floroglucinols, wherein the anthocyanosides are derived from a Vaccinium myrtillus extract, the procyanidins are derived from a Vitis vinifera extract, a Camellia sinensis extract or from another edible plant containing the procyanidins, and the floroglucinols are derived from Hypericum spp., Mirtus spp. or Humulus lupulus extracts. 2. The composition as claimed in claim 1, wherein the floroglucinols are derived from Hypericum perforatum or Mirtus communis extracts, or from Humulus lupulus fractions enriched in a and ß acids. 3. The composition as claimed in claim 2, wherein 20 to 80% of floroglucinols from the ß acids of Humulus lupulus are colupulone, and the a acids contain 20 to 80% of humulone. 4. The composition as claimed in claim 3, wherein 60% of floroglucinols from the ß acids of Humulus lupulus are colupulone, and the a acids contain 60% of humulone. 5. The composition as claimed in claim 1, wherein the Hypericum sp. extract is a Hypericum perforatum extract with floroglucinols content ranging from 20 to 80%. 6. The composition as claimed in claim 5, wherein the floroglucinols content of the Hypericum perforatum extract is 60%. 7. The composition as claimed in claim 2, wherein the Mirtus communis extract is prepared from the leaves of Mirtus communis by extraction with carbon dioxide at a pressure ranging from 235 to 260 bars and a temperature ranging from 40 to 60°C. 8. The composition as claimed in claim 7, wherein the Mirtus communis extract has a mirtocumolone content of 35%. 9. The composition as claimed in claim 1, further containing at least one essential oil. 10. The composition as claimed in claim 9, wherein the essential oil is mint oil. 11. The composition as claimed in claim 1, whenever used for the preparation of a medicament for the treatment of the affections of the oral cavity and upper respiratory tract.

Full Text

COMPOSITIONS FOR THE TREATMENT OF AFFECTIONS OF THE ORAL CAVITY AND UPPER RESPIRATORY TRACT
The present invention relates to compositions containing anthocyanosides and/or procyanidins in combination with floroglucinols for the treatment of the affections of the oral cavity and upper respiratory tract.
TECHNOLOGICAL BACKGROUND
Throat redness and inflammation, with formation of plaques, usually accompany common influenza, coryza and other cold diseases. Common cold and influenza, which on the average affect up to three times a year both children and adults, are related to mild viral infections caused by rhinovirus (40%), coronavirus (10%) and, to a less extent, adenovirus and parainfluenza viruses. Although no specific treatments exist for these pathologies, antihistamines and decongestants are considered useful, as the edema reduction alleviates pain and makes the course of the disease shorter.
DISCLOSURE OF THE INVENTION
The present invention relates to compositions containing:
a) anthocyanosides, and/or
b) procyanidins, and
c) floroglucinols,
useful for the treatment of the affections of the oral cavity and upper respiratory tract.
According to the present invention, the compositions contain 1 to 200 mg of anthocyanosides, and/or 1 to 200 mg of procyanidins, and 1 to 200 mg of floroglucinols.
According to the present invention, "anthocyanosides" includes both real anthocyanosides and anthocyanidins, their aglycones. The anthocyanosides preferably are derived from Vaccinium myrtillus extracts.

The extract of bilberry (Vaccinium myrtillus), as described in literature, has marked antiinflammatory activity, in particular topically, due to its action on capillary permeability and fragility. The preparation of bilberry extracts containing anthocyanosides is known to those skilled in the art. Bilberry anthocyanosides and procyanidins exert bacteriostatic action which prevents bacterial and fungal adhesion, for example at the dental and paradental level and on mucous membranes. •**
According to the present invention, the procyanidins can preferably be derived from Vitis vinifera extracts, obtained as disclosed in GB 1,541,469, or from Camellia sinensis extracts, as disclosed in EP 0 814 823, or from other plants, preferably edible, containing them.
Floroglucinols exert strong bacteriostatic action on a great number of bacteria and fungi strains. The minimum inhibitory concentration values of some floroglucinols on gram+ bacteria, gram- anaerobic bacteria and strains of Candida albicans range from 0.5 to 4 ug/ml.
According to the present invention, floroglucinols can be derived from Hypericum spp. extracts, preferably Hypericum perforatum, or from Mirtus spp. extracts, preferably Mirtus communis, or from Humulus spp. fractions, preferably Humulus lupulus, enriched in a and (3 acids. According to the invention, the fraction of p-acids prepared from Humulus lupulus contains 20 to 80%, preferably 60%, of floroglucinols expressed as colupulone; the fraction of a-acids contains 20 to 80%, preferably 60%, of humulone.
According to the present invention, among the Hypericum sp. extracts, particularly preferred is a Hypericum perforatum extract with a floroglucinols (adhyperforin/hyperforin) content ranging from 20 to 80%, preferably 60%.
According to the present invention, the Mirtus communis extract is prepared from the leaves, by extraction with carbon dioxide under conditions

of pressure ranging from 235 to 260 bars and temperatures ranging from 40 to 60°C, preferably 45°C. The resulting extract usually has a mirtocumolone content of 35%.
The compositions of the invention are capable of preventing the formation of purulent plaques deriving from various saprophytic infections of the oral cavity, thus avoiding the use of antibiotics, while reducing the progress of the infection. In particular, the compositions of the invention proved to exert a synergistic effect mainly as regards the duration of the disease.
Furthermore, the compositions of the invention exert favourable action on the cleanliness of the oral cavity and the removal of the dental plaque, thanks to the effect reducing bacterial adhesiveness, as already mentioned, exerted by bilberry extract and procyanidins, and to the high activity of floroglucinols on anaerobic bacterial strains.
The pharmaceutical compositions will be preferably presented in the form of tablets for the slow dissolution in the oral cavity or chewing gums which provide the slow release of the active principles. These compositions are used in preventive and prophylactic treatments as well as for the hygiene of the oral cavity.
According to a further preferred aspect, the compositions of the present invention will further contain essential oils, in particular mint oil.
According to a further preferred aspect; .the compositions of the present invention will further contain a Glycyrrhiza extract, preferably having a content in glycyrrhizic acid of 10%.
The present invention, therefore, relates to compositions for the treatment of the affections of the oral cavity and upper respiratory tract, containing the combinations described above.
Said compositions will be prepared according to conventional methods

well known in pharmaceutical technique, as those described in "Remington's Pharmaceutical Handbook", Mack Publishing Co., N.Y., USA, together with suitable excipients commonly used in the art.
The present invention also relates to the use of a combination of anthocyanosides, and/or procyanidins, and floroglucinols, for the preparation of a medicament for the treatment of the affections of the oral cavity and upper respiratory tract.
The examples reported hereinbelow further illustrate the invention.
Example I - Tablets
Each 500 mg tablet contains:
Vaccinium myrtillus extract
(25% in anthocyanidins) 60 mg
Humidus lupulus extract
(60% in floroglucinols) 10 mg
Soy lecithin (30% phosphatidylcholine) 30 mg
Glycyrrhiza extract
(10% of glycyrrhizic acid) 20 mg
Mint essential oil 10 mg
Saccharose 200 mg
Maltodextrin 150 mg
Acacia gum 15 mg
Magnesium stearate . 5 mg
Example II - Tablets
Each 500 mg tablet contains:
Vitis vinifera extract (95% in procyanidins) 80 mg
Humulus lupulus extract
(60% in floroglucinols) lOmg
Soy lecithin (30% phosphatidylcholine) 30 mg

Glycyrrhiza extract
(10% of glycyrrhizic acid) 20 mg
Mint essential oil 10 mg
Mannitol 320 mg
Povidone 20 mg
Silicium dioxide 5 mg
Magnesium stearate 5 mg
Example III - Tablets
Each 500 mg tablet contains:
Vitis vinifera extract (95% in procyanidins) 80 mg
Mirtus communis lipophilic extract
(35% in mirtocupulone) 10 mg
Glycyrrhiza extract
(10% of glycyrrhizic acid) 20 mg
Mint essential oil 10 mg
Maltodextrin 332 mg
Sodium saccharin 3 mg
Arabic gum 30 mg
Talc lOmg
Magnesium stearate 5 mg
Example IV - Tablets
Each 500 mg tablet contains:
Vacciniwn myrtillus extract
(25% in anthocyanidins) 60 mg
Mirtus communis lipophilic extract
(35% in mirtocupulone) lOmg
Soy lecithin (30% phosphatidylcholine) 30 mg
Glycyrrhiza extract

(10% of glycyrrhizic acid) 20 mg
Mint essential oil 10 mg
Saccharose 330 mg
Tragacanth gum 20 mg
Silicium dioxide 5 mg
Magnesium stearate 5 mg
Example V - Tablets
Each 500 mg tablet contains:
Camellia sinensis extract
(70% in procyanidole oligomers) 80 mg
Humulus lupulus extract
(60% in floroglucinols) 10 mg
Soy lecithin (30% phosphatidylcholine) 30 mg
Glycyrrhiza extract
(10% of glycyrrhizic acid) 20 mg
Mint essential oil 10 mg
Mannitol 320 mg
Povidone 20 mg
Silicium dioxide 5 mg
Magnesium stearate 5 mg
Example VI - Tablets
Each 500 mg tablet contains:
Camellia sinensis extract
(70% in procyanidole oligomers) 80 mg
Hypericum perforatum extract
(60% in floroglucinols) 10 mg
Soy lecithin (30% phosphatidylcholine) 30 mg
Glycyrrhiza extract

(10% of glycyrrhizic acid) 20 mg
Mint essential oil 10 mg
Mannitol 320 mg
Povidone 20 mg
Silicium dioxide 5 mg
Magnesium stearate 5 mg
Example VII - Chewing Gum
Each 2000 mg chewing gum contains:
Vitis vinifera extract (95% in procyanidins) 80 mg
Mirtus communis lipophilic extract
(30% in mirtocupulone) 10 mg
Glycyrrhiza extract
(10% of glycyrrhizic acid) 20 mg
Mint essential oil 10 mg
Gum base 1598 mg
Xylitol 250 mg
Aspartame 2 mg
Magnesium stearate 15 mg
Talc 15 mg

We Claim:
1. A composition, for the treatment of an affection of the oral cavity and upper respiratory
tract, comprising:
1-200 mg anthocyanosides;
1-200 mg procyanidins; and
1-200 mg floroglucinols,
wherein the anthocyanosides are derived from a Vaccinium myrtillus extract, the
procyanidins are derived from a Vitis vinifera extract, a Camellia sinensis extract or from
another edible plant containing the procyanidins, and the floroglucinols are derived from
Hypericum spp., Mirtus spp. or Humulus lupulus extracts.
2. The composition as claimed in claim 1, wherein the floroglucinols are derived from Hypericum perforatum or Mirtus communis extracts, or from Humulus lupulus fractions enriched in a and ß acids.
3. The composition as claimed in claim 2, wherein 20 to 80% of floroglucinols from the ß acids of Humulus lupulus are colupulone, and the a acids contain 20 to 80% of humulone.
4. The composition as claimed in claim 3, wherein 60% of floroglucinols from the ß acids of Humulus lupulus are colupulone, and the a acids contain 60% of humulone.
5. The composition as claimed in claim 1, wherein the Hypericum sp. extract is a Hypericum perforatum extract with floroglucinols content ranging from 20 to 80%.
6. The composition as claimed in claim 5, wherein the floroglucinols content of the Hypericum perforatum extract is 60%.
7. The composition as claimed in claim 2, wherein the Mirtus communis extract is prepared from the leaves of Mirtus communis by extraction with carbon dioxide at a pressure ranging from 235 to 260 bars and a temperature ranging from 40 to 60°C.
8. The composition as claimed in claim 7, wherein the Mirtus communis extract has a
mirtocumolone content of 35%.
9. The composition as claimed in claim 1, further containing at least one essential oil.
10. The composition as claimed in claim 9, wherein the essential oil is mint oil.
11. The composition as claimed in claim 1, whenever used for the preparation of a medicament for the treatment of the affections of the oral cavity and upper respiratory tract.

Documents:

2888-DELNP-2006-Abstract-(11-01-2012).pdf

2888-DELNP-2006-Abstract-(19-04-2012).pdf

2888-delnp-2006-abstract.pdf

2888-DELNP-2006-Claims-(11-01-2012).pdf

2888-DELNP-2006-Claims-(19-04-2012).pdf

2888-delnp-2006-claims.pdf

2888-delnp-2006-Correspodence Others-(22-07-2011).pdf

2888-DELNP-2006-Correspondence Others-(11-01-2012).pdf

2888-DELNP-2006-Correspondence Others-(19-04-2012).pdf

2888-delnp-2006-correspondence-others 1.pdf

2888-DELNP-2006-Correspondence-Others-(14-01-2011).pdf

2888-delnp-2006-description (complete).pdf

2888-DELNP-2006-Form-1-(19-04-2012).pdf

2888-delnp-2006-form-1.pdf

2888-delnp-2006-form-18.pdf

2888-DELNP-2006-Form-2-(19-04-2012).pdf

2888-delnp-2006-form-2.pdf

2888-DELNP-2006-Form-3-(11-01-2012).pdf

2888-delnp-2006-Form-3-(22-07-2011).pdf

2888-delnp-2006-form-3.pdf

2888-delnp-2006-form-5.pdf

2888-DELNP-2006-GPA-(14-01-2011).pdf

2888-delnp-2006-pct-304.pdf

2888-delnp-2006-pct-401.pdf

2888-delnp-2006-pct-409.pdf

2888-delnp-2006-pct-416.pdf

2888-delnp-2006-pct-request form.pdf

2888-delnp-2006-pct-search report.pdf

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Patent Number

253024

Indian Patent Application Number

2888/DELNP/2006

PG Journal Number

25/2012

Publication Date

22-Jun-2012

Grant Date

15-Jun-2012

Date of Filing

22-May-2006

Name of Patentee

INDENA S.P.A.

Applicant Address

VIALE ORTLES, 12,I-20139 MILANO ITALY.

Inventors:

#	Inventor's Name	Inventor's Address
1	EZIO, BOMBARDELLI	VIA GABETTA, 13, 27027 GROPPELLO CAIROLI (PAVIA), ITALY.

PCT International Classification Number

A61K 31/35

PCT International Application Number

PCT/EP2004/012472

PCT International Filing date

2004-11-04

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1	MI2003A002287	2003-11-24	Italy