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Title:
COMPOSITION COMPRISING DISTILLATE AND ESSENCE OF BERGAMOT
Document Type and Number:
WIPO Patent Application WO/2008/035391
Kind Code:
A3
Abstract:
The current object of the present study, regards a composition of distilled bergamot and bergamot essence. This distilled bergamot is obtained from the distillation of the central and external part of the bergamot after extractive process with antibacterial and antimicrobic activities. It also expresses a repellent action towards insects maintaining a pleasant fragrance. It can be used as active principle, as flavouring or preserving agent.

Inventors:
MINICUCI PANSERA MARIA (IT)
MINICUCI CLAUDIA (IT)
Application Number:
PCT/IT2007/000660
Publication Date:
May 08, 2008
Filing Date:
September 24, 2007
Export Citation:
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Assignee:
FARMACIA MINICUCI DELLA DOTT S
MINICUCI PANSERA MARIA (IT)
MINICUCI CLAUDIA (IT)
International Classes:
A61K36/752
Other References:
ALOI ET AL.: "Progetto di legge n.4866", CAMERA DEI DEPUTATI, PROPOSTE DI LEGGE (LAW PROPOSALS), 1998, Rome, XP002466987, Retrieved from the Internet [retrieved on 20080129]
ROMANO L ET AL: "In vitro activity of bergamot natural essence and furocoumarin-free and distilled extracts, and their associations with boric acid, against clinical yeast isolates", JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, vol. 55, no. 1, January 2005 (2005-01-01), pages 110 - 114, XP002466984, ISSN: 0305-7453
MAUDSLEY F ET AL: "Microbiological safety of essential oils used in complementary therapies and the activity of these compounds against bacterial and fungal pathogens", SUPPORTIVE CARE IN CANCER 1999 GERMANY, vol. 7, no. 2, 1999, pages 100 - 102, XP002466985, ISSN: 0941-4355
MANDALARI GIUSEPPINA ET AL: "Characterization of flavonoids and Pectins from bergamot (Citrus bergamia Risso) peel, a major byproduct of essential oil extraction", JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, vol. 54, no. 1, January 2006 (2006-01-01), pages 197 - 203, XP002467133, ISSN: 0021-8561
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; 25 October 1952 (1952-10-25), MEINERI P A: "[Disinfecting action of oil of bergamot with cream base.]", XP002467136, Database accession no. NLM13024973
MANDALARI GIUSEPPINA ET AL: "Enzymatic hydrolysis of flavonoids and pectic oligosaccharides from bergamot (Citrus bergamia Risso) Peel", JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, vol. 54, no. 21, October 2006 (2006-10-01), pages 8307 - 8313, XP002467134, ISSN: 0021-8561
MANDALARI G ET AL: "Antimicrobial activity of flavonoids extracted from bergamot (Citrus bergamia Risso) peel, a byproduct of the essential oil industry", JOURNAL OF APPLIED MICROBIOLOGY, vol. 103, no. 6, December 2007 (2007-12-01), pages 2056 - 2064, XP002466986, ISSN: 1364-5072
Attorney, Agent or Firm:
SCARFONE MARIA ADELAIDE (Viale Lucrezia della Valle 8, Catanzaro, IT)
Download PDF:
Claims:

CLAIM.

1. Composition utilized pure or in part for total characterized from the fact that include bergamot distillate and bergamot essence.

2. Composition utilized pure or in part for total, as claimed in claim 1 , characterized from the fact that this distillate is obtained from the distillation of the secondary products or discarded stuff of the extractive process of the bergamot essence.

3. Composition utilized pure or in part for total, as claimed in claim 1 , characterized from the fact that it includes other active principles in simple or complex formulation adding other excipients.

4. Composition utilized pure or in part for total, as claimed in claim 1 , it can have a topic use, it can be inhalated or other.

5. Composition utilized pure or in part for total, as claimed in claim 1 , characterized from the fact that it can be liquid with watery basis, oily or hydroalcoholic.

6. Composition utilized pure or in part for total, as claimed in claim 1 , characterized from the fact that it can be creamy, it can be an emulsion, gel, oil, spray or milk.

7. Use of the composition, as claimed in claim 1 , it can be used for the production of an antimicrobic and antibacterial activity on positive gram bacteria, negative gram and fungi.

Description:

COMPOSITION COMPRISING DISTILLATE OF BERGAMOT AND ESSENCE OF BERGAMOT. UTILIZED PURE OR IN PART FOR TOTAL.

TECHNICAL FIELD

5 The current, object of the present invention, regards a composition including distillate of bergamot and bergamot essence. This invention, in any formulation, expresses antimicrobic action on gram positive microbes, negative gram and fungi.

The union of these two compounds allows also the titration, the variation 10 of concentration or the 5-MOP elimination.

It also express a repellent action towards the insects but maintaining still the pleasant fragrance. It can be used as active principle, as a flavouring or preserving agent.

15 BACKGROUND ART

The bergamot (Citrus Bergamia Risso et Poiteau) is a typical citrus fruit cultivated in the province of Reggio Calabria.

The essence of petitgrain is extracted from the leaves and the tender branchs, while the essence of neroli comes from the flowers blossomed 20 prematurely in February or later in June which exclude the possibility of fructification.

The essence of bergamot obtained without using heat through mechanical extractive processes from the middle and external part of the fruit. It is mentioned in the official pharmacopoeia, where its -2-5-- quantitative -and -qua-Kta-tive--desel4ρtitm--usefu-l-rfoτ^rts -

found. The beneficial of the essence of bergamot are well known. This essence is appreciated and used throughout the world for its properties as fixative of the aromatic bouquet of the fragrances and as equilibrator of the other essences for which it is known in the international perfume industry. Besides being used for perfumes and cosmetics, the essence of bergamot is also used in the pharmaceutical where, however notwithstanding the antiseptic and antibacterial properties, it is mostly used as excipient and flavouring without being considered as active agent of the formulations. This use is possible thanks to the presence of Bergaptene (5 MOP) that represents the photosensitive part of the compound, which must be used with care.

In fact if exposed to the sun or UVA rays it can activate a reaction that can determines chemical burns on the skin.

To avoid this problem several techniques have been introduced to decrease and/or titrate this component. An example of this is the or the existence of compositions involving pure bergamot essence with distilled bergamot essence. The international patent PCT N°WO01/13783 regards a composition having a mixture of bergamot essence with the distilled part of the essence, without bergaptene, in order to titrate the extract percentage of 5 MOP that is in the solution and to allow a correct clinical use. These techniques, nevertheless, not only increase the price of the finished product, but are also of difficult use. Moreover all the phototoxic effects are still present imposing a moderate use.

A product containing distillate pure bergamot essence with the regi ster&d- trademark "B -eτgartta:P ~ exi-sts .

The use, in phytotherapy, of the bergamot juice as an alimentary integrator together with omega 3 , extracts from algae oil to lower the colesterol and tryglycerids in the blood or in association with red rice fibres to lower the sugar absorption, like the commercial product "Bergam 8" of the Spechiasol society is well known.

The essence of bergamot is widely used in aromatherapy because of the sunny scent that has the power to decrease emotional excesses, to encourage personal trust and to lift a person's vitality, helping to overcome apathy and morning laziness. In the food industry it is used as flavouring in liquors, sweets and drinks. In the past the dried rind was used to produce snuff-boxes and today it is used to create decoration flower in the artisan industry.

However, nor the status of the technical in use, or the patents with new methods can solve the critical aspects.

DISCLOSURE OF INVENTION

This invention wants to solve all the problems and the disadvantages existing now.

One of the principal aims is to solve the disadvantages mentioned above realizing a composition, having a distillate of bergamot and its essence, that reinforce the antiseptic and antibacterial properties of the distillate of pure bergamot and increase the antimicrobic activity proved on bacterial samples, without loosing the intensity of the fragrance of the bergamot essence.

Another aim is to create a composition that when is applied present very low risks in connection to the presence of the bergaptene 5-MOP in the bergamot essence.

Another aim is to realize a composition to be used directly in any kind of application without pre-treatments.

Considering the above mentioned aims and according to the invention, it's furnished a composition having a distillate of bergamot and its essence, this distillate is obtained from the distillation of the secondary products of the productive process of the essential oil, more precisely from the distillation of the external and middle part, after the extraction of the bergamot essence.

The union of these two substances, in any form of percentage, used pure or in part for total, allows to be used for all the useful reasons and in any application field. So in this way the antimicrobic, the antimicotic and antiseptic activity of the bergamot distillate is increased, maintaining the organoleptic characteristics of the bergamot essence like the citrus fragrance and the persistence of the fragrance.

It expresses a repellent action towards the insects maintaining the pleasant fragrance. It can be used as active agent, flavouring or preserver.

This composition can be used for any possible preparation, without excluding the presence of active principles, in simple or complex formulations adding excipients in order to improve the use.

The composition, according to the invention, can be in a liquid solution, in an oily one, hydroalcoholic, creamy, in emulsion, gel, oil, spray, milk or other forms, depending on the need.

This solution is used in dermacosmetics, as active agent or scent fixer, weather for the people or for the environment.

It is used in the medical surgery, in chemistry, in the traditional medicine and in the alternative one like aromatherapy and phytotherapy. It can be used in the food industry and in the chemical one. The distillate of bergamot comes from the secondary products during the working process of the essential oil, that is of the middle and external part of the fruit (epicarpo and mesocarpo), after the extraction of the bergamot essence.

The composition, according to the invention, is able to increase and strengthen the antimicrobic and antibacterial activity of the distilled bergamot against some bacterial samples without loosing the persistence and the intensity of the fragrance of the bergamot essence.

We'll describe the advantages of the invention:

1 -Increase of the antimicrobic and antibacterial, connected to the distillate of bergamot, on gram positive and negative bacteria and fungi. 2-Persistence and intensity of the aroma connected to the bergamot essence.

3-Elimination and/or the titration of the 5-MOP through the different percentage of the two components.

4-Direct use in chemistry, in dermacosmetics, in the medical areas, in ~ - ftrστKτrdustry 5 ; in rrhy to therapy and-aroma therapy.-

5- Use of the secondary products of the extractive process of the bergamot essence if not used.

The following examples want just to show the invention and not to limit it, as shown in the vindications.

BEST MODE FOR CARRYING OUT THE INVENTION

The following compositions are just an example and they don't have to be considered as limitations for the invention.

We'll call the substance x, the external part of the bergamot after the extractive process of the bergamot essence and we'll call the substance y, the bergamot essence.

Five different samples have been created pouring in five different bottles the two substances x and y with the following percentages: bottle A Y 100% X 0% bottle B Y 95% X 5% bottle C Y 5% X 95% bottle D Y 50% X 50% bottle E Y 0% X 100%

The five different compositions have been exposed to gascromatographic analysis and to a valuation of the antimicrobic and antibacterial activity.

The chemical composition defined with gascromatography, of X bergamot distilled, is described in detail in the E sample table and from the results show that the composition is without bergapteni.

From the tests carried out in vitro, the sample C and E show a high antimicrobic activity; there is a potential synergy between the two substances X and Y, on same bacterial parts, the sample C as shown in the table, determinates an increase of antimicrobic activity which is dominant in these samples in respect to the bergamot essence(sampleA).

Although the E sample has the same scent, it lacks the organoleptic characteristics of the essence because the persistence and intensity of the fragrance in respect to the bergamot essence is weak. This is the main characteristic of the essence that has made the bergamot essence famous throughout the world.

The results of the inhibition halos are showen in the table below.

From the table we can notice a certain antimicrobic activity in the bergamot essence (sampleA), this is more evident in E and became stronger in C aspecially on the bacterial strains Bacillus Subtilis, Streptococcus Mutans e Helicobacter Pilori.