FR3114005A3 - repellent composition - Google Patents

Abstract

The invention relates to a composition comprising: - an extract of turmeric, - an extract of squash, and - essential oils for its use in the prevention of infestation by blood-sucking mites of mammals. Figure for abstract: no figure

Description

repellent composition

The invention relates to a repellent composition in particular blood-sucking mites.

Ticks are hematophagous ectoparasites that feed on the blood mainly of mammals and birds.

Ticks are arachnids of the parasitiform mite subclass, the majority of which belong to the Ixodidae family. Three species are particularly common in the environment of humans and animals: Rhipicephalus sanguineus (also known as the "kennel tick" or "brown dog tick", Ixodes scapularis , also called the blacklegged tick, and Ixodes ricinus sheep tick and formerly also dog tick, whose population has increased significantly in the northern hemisphere and especially in western Europe.

Ticks are considered dangerous mites insofar as, in addition to the bite they inflict on their host to feed, they are vectors of many diseases, and in particular in humans Lyme disease caused by the transmission bacteria of the Borrelia genus.

In addition, the population of ticks in the world has continued to increase for several decades, thus making the risk of bites more frequent and therefore the risk of disease transmission.

Also, there is a need to try to limit either the tick population itself, or to limit bites.

To do this, many products have been proposed to kill ticks or repel them away from their hosts. Many "insecticides" have been used with varying degrees of success. International application WO2006026598 is also known, which describes methoprenes for limiting tick infestation. However, these are again chemical compounds whose long-term safety is not known.

Also, the need to provide a means of preventing tick infestation, and therefore the pathologies that they can transmit, remains.

The object of the invention is to remedy these shortcomings of the prior art.

One of the aims of the invention is to provide a new natural composition which makes it possible to fight effectively against the infestation of mites and in particular ticks, and in particular to act as a repellent for them, without however exerting a harmful effect on the 'environment.

Another object of the invention is to provide a means of preventing the occurrence of pathologies and parasitosis due to mite bites in a simple and almost natural way, always with respect for nature and the environment.

Thus, the invention relates to a composition comprising at least two of the following compounds:

- an extract of turmeric,

- a pumpkin extract,

- essential oil of thyme, and

- savory essential oil

for its use in the prevention of infestation by mites, in particular by blood-sucking mites, in particular by mammalian ticks.

Advantageously, the invention therefore relates to the use of a composition comprising at least two of the following compounds:

- an extract of turmeric,

- a pumpkin extract,

- essential oil of thyme, and

- savory essential oil

in particular for the manufacture of a medicament, intended to prevent infestation by mites, in particular by blood-sucking mites, in particular by mammalian ticks.

The invention is based on the unexpected observation made by the inventors that plant extracts and essential oils are capable, in combination, of exerting a repellent effect on mites, in particular hematophagous mites, in particular ticks, in particular after ingestion, and therefore limit the risks of contamination by the parasites carried by them.

In the invention, the term “composition comprising at least two of the following compounds” means compositions which comprise or consist of two, three or four of the aforementioned ingredients. In other words, the invention relates to the following compositions:

- a composition comprising a turmeric extract and a squash extract, for its use for the prevention of infestation by mites, in particular by hematophagous mites, in particular by mammalian ticks,

- a composition comprising an extract of turmeric and essential oil of thyme, for its use for the prevention of infestation by mites, in particular by hematophagous mites, in particular by mammalian ticks,

- a composition comprising an extract of turmeric and essential oil of savory, for its use for the prevention of infestation by mites, in particular by hematophagous mites, in particular by mammalian ticks,

- a composition comprising a squash extract and essential oil of thyme, for its use for the prevention of infestation by mites, in particular by hematophagous mites, in particular by mammalian ticks,

- a composition comprising a squash extract and savory essential oil, for its use for the prevention of infestation by mites, in particular by hematophagous mites, in particular by mammalian ticks,

- a composition comprising an extract of turmeric, an extract of squash and essential oil of thyme, for its use for the prevention of infestation by mites, in particular by hematophagous mites, in particular by mammalian ticks,

- a composition comprising a turmeric extract, a squash extract and essential oil of savory, for its use for the prevention of mites, in particular blood-sucking mites, in particular infestation by mammalian ticks,

- a composition comprising an extract of turmeric, essential oil of thyme and essential oil of savory, for its use for the prevention of infestation by mites, in particular by hematophagous mites, in particular by ticks mammals, and

- a composition comprising an extract of turmeric, an extract of squash, essential oil of thyme and essential oil of savory, for its use for the prevention of infestation by mites, in particular by blood-sucking mites, especially by mammalian ticks.

Advantageously, the invention relates to a composition comprising

- an extract of turmeric,

- a pumpkin extract,

- essential oil of thyme, and

- savory essential oil

for its use in the prevention of infestation by mites, in particular by blood-sucking mites, in particular by mammalian ticks.

Advantageously, the invention relates to the use of a composition comprising

- an extract of turmeric,

- a pumpkin extract,

- essential oil of thyme, and

- savory essential oil

in particular for the manufacture of a medicament, for the prevention of infestation by mites, in particular by blood-sucking mites, in particular by mammalian ticks.

The aforementioned composition according to the invention is advantageously a solid composition, in particular in the form of a powder, encapsulated or not, or of a tablet comprising the active ingredients as listed above.

It is not particularly advantageous for the composition according to the invention to comprise other ingredients which do not participate in the anti-tick effect. However, other inert ingredients may be present, or ingredients that allow the stability or longevity of the ingredients.

Turmeric, by its scientific name Curcuma longa , is a perennial rhizomatous herbaceous plant of the genus Curcuma of the Zingiberaceae family native to South or Southeast Asia. Turmeric is known as an aromatic or spice, and for its medicinal properties such as beneficial effects against gastrointestinal disorders, anti-inflammatory properties and possible action in the prevention of cancer.

Squash, by its scientific name Cucurbita pepo , is a species of the Cucurbitaceae family of which there are many subspecies and varieties.

Thyme, from its scientific name Thymus, is a plant of the Lamiaceae family, very rich in essential oils and therefore part of the aromatic plants. There are several types of essential oils extracted from different species of teyps, essential oils classified according to their content of aromatic compounds: thymol essential oil (comprising about 40% thymol), thujanol essential oil (comprising 20 45% thujanol), geraniol essential oil (comprising 11-26% geranol and 14-40% geranyl acetate), linalool essential oil (comprising 65-85% linalool ) and borneol essential oil (comprising about 30% borneol). One of the advantageous essential oils of thyme in the invention is an essential oil containing linalool by steam distillation of the flowering tops of Thymus zygis L.

Savory, scientifically named Satureja , is a genus of aromatic flowering plants in the family Lamiaceae . The leaves and flowering tops are digestive, stimulating, antiseptic and antiputrid. They would also have deworming properties. Mountain savory, scientifically named Satureja montana L., is particularly beneficial. An advantageous essential oil of savory according to the invention is an essential oil of mountain savory, and in particular an essential oil obtained by steam distillation of the flowering stems of Satureia montana L.

The composition according to the invention is particularly suitable in the context of the repulsion, and therefore the limitation of the infestation, of mites such as lice or chiggers, or even hematophagous mites such as argacids (soft-bodied ticks) or the so-called "common" ticks, in particular Ixodes ricinus .

Advantageously, the invention relates to the composition described above for its use as defined above, where the turmeric extract is an extract of turmeric rhizome.

Turmeric rhizomes have been known for a very long time to contain many compounds used as spices, preservatives, dyes, cosmetic or therapeutic agents.

The turmeric rhizomes contain in particular curcuminoids, which give the yellow color and which are the main active ingredients such as curcumin, methoxycurcumin, bidesmethoxycurcumin, dihydrocurcumin. The rhizomes further contain quinoids, sesquiterpenes (e.g. bisacumol, and bisacurone, steroids, monoterpenes, phenylpropanoids and many other compounds.

The turmeric rhizome extract of the invention is for example derived from extraction with ethyl acetate after powder reduction of the root. A particularly advantageous extract is in particular in powder form and contains in particular 95% by mass relative to the mass of the curcuminoid extract. More particularly, the extract contains 70 to 80% curcumin, 13 to 20% desmethoxycurcumin and 1 to 5% bisdesmethoxycurcumin, the percentages being expressed by mass relative to the total mass of the extract. This extract is usually in the form of red-orange granules. An example of a rhizome extract used according to the invention is marketed by the company Natural extract under the reference CUR95DC001.

Advantageously, the invention relates to the composition described above for its use as defined above, where the squash extract is a squash seed extract.

Rich in phytosterols, pumpkin seed is mainly used in the prior art to fight against prostate disorders and generally promote urinary comfort in both men and women. This edible seed is also a vermifuge against intestinal parasites. Its trace elements also help combat fatigue and menopausal disorders.

Pumpkin seed extracts are advantageously obtained by water extraction from Curcubita pepo seed, and spray-drying, so as to obtain a light brown powder. An example of pumpkin seed extract used according to the invention is marketed by the company Natural extract under the reference COUR4_1001.

The invention advantageously relates to the composition described above for its use as defined above, said composition being such that it comprises:

- 53 to 93% turmeric extract

- 3 to 30% thyme essential oil, and

- 3 to 16% savory essential oil

the percentages being expressed by mass relative to the total mass of turmeric extract and thyme essential oil and savory essential oil.

In the invention, the term “from 53 to 93% turmeric extract” means 53%, 54%, 55%, 56%, 57%, 58%, 59%, 60%, 61%, 62%, 63%, 64%, 65%, 66%, 67%, 68%, 69%, 70%, 71%, 72%, 73%, 74%, 75%, 76%, 77%, 78%, 79% , 80%, 81%, 82%, 83%, 84%, 85%, 86%, 87%, 88%, 89%, 90%, 91%, 92% or 93% turmeric extract, the percentages being expressed in mass as mentioned above.

The term “from 3 to 30% of essential oil of thyme” is understood to mean 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14 %, 15%, 16%, 17%, 18%, 19%, 20%, 21%, 22%, 23%, 24%, 25%, 26%, 27%, 28%, 29% or 30% d essential oil of thyme, the percentages being expressed by mass as mentioned above.

“From 3 to 16% savory essential oil” also means 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15% or 16%, the percentages being expressed by weight as mentioned above.

According to regulatory data, the daily dose of turmeric extract should not exceed 210 mg, and those of thyme and savory essential oils should not exceed 120 mg and 65 mg, respectively. Also, knowing that there is no limit in the daily quantity of pumpkin seed extract, the person skilled in the art will be able to adapt the doses of the various components so as not to exceed the applicable regulatory limits.

In the context of a composition that would include the maximum authorized for each of the ingredients, the turmeric extract would represent 53%, the essential oil of thyme would represent 30% and the essential oil of savory would represent 16%, the percentages being expressed by mass relative to the mass of the three components, i.e. the turmeric extract, and the two essential oils.

Advantageously, the invention relates to the composition described above for its use as defined above, said composition being in a form suitable for oral administration.

While ticks are ectoparasites which attack the skin of their host, the composition according to the invention is surprising because it exerts its repellent activity against these mites when it is ingested by a man or an animal likely to be stung. Also, unlike known repellent compositions which are sprayed or applied in the environment where ticks are likely to be present, or directly on the animal, the composition according to the invention is ingested and therefore has no harmful effect for the environment, nor for the host since he can ingest it.

Also, advantageously, the composition according to the invention is in a form capable of being administered per os, in particular in the form of tablets, capsules, capsules, lozenges or powders, or in a drinkable form such as syrups, oral suspensions, or even solutions.

Advantageously, the invention relates to the composition described above for its use as defined above, said composition further comprising a carrier.

It is particularly advantageous for the composition according to the invention to additionally comprise at least one support allowing the adsorption of the essential oils of thyme and savory. Indeed, these oils being hydrophobic and not very miscible in water, the adsorption on a support makes it possible to promote the mixing of the different ingredients. In particular, when the squash and turmeric extracts are in powder form, the mixing of the ingredients is facilitated if the essential oils are adsorbed on a powdery support.

The supports can generally be inert compounds, such as silicas or derivatives thereof, polysaccharides, or other supports known to the state of the art.

These carriers do not participate directly in the therapeutic effect of the composition according to the invention, but can act as agents allowing controlled, delayed release, or even have a gastro-resistant effect.

Advantageously, said support represents from 51 to 84% by mass relative to the total mass of the composition.

Advantageously, the invention relates to the composition described above for its use as defined above, said composition comprising

- from 10 to 25% by mass of a turmeric extract,

- from 5 to 20% by mass of a pumpkin extract,

- from 0.5 to 2% by mass of thyme essential oil, and

- from 0.5 to 2% by mass of savory essential oil,

the percentages being expressed by mass relative to the total mass of the composition.

Also, even more advantageously, the invention relates to a composition comprising, or consisting of:

- from 51 to 84% by mass of a support or at least one support,

- from 10 to 25% by mass of a turmeric extract,

- from 5 to 20% by mass of a pumpkin extract,

- from 0.5 to 2% by mass of thyme essential oil, and

- from 0.5 to 2% by mass of savory essential oil,

the percentages being expressed by mass relative to the total mass of the composition.

Other compounds may be present in the composition according to the invention, in particular dietary fibers. For example rice fibers are advantageous.

In the invention, the term "from 0.5 to 2% by mass of essential oil" means 0.5, 0.6, 0.7, 0, 8, 0.9, 1, 1.1, 1, 2, 1.3, 1.4, 1.5, 1.6, 1.7, 1.8, 1.9 or 2% essential oil.

In the invention, the term “from 0.5 to 2% by mass of a turmeric extract” is understood to mean 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18% , 19%, 20%, 21%, 22%, 23%, 24% or 25% by mass of a turmeric extract.

The term “from 5 to 20% by mass of a squash extract” is understood to mean 5%, 6%, 7%, 8%, 9%, 10%, 11%, 12%, 13%, 14%, 15% , 16%, 17%, 18%, 19%, or 20% by mass of a pumpkin extract.

“51 to 84% of a support or at least one support” also means 51, 52, 53%, 54%, 55%, 56%, 57%, 58%, 59%, 60%, 61% , 62%, 63%, 64%, 65%, 66%, 67%, 68%, 69%, 70%, 71%, 72%, 73%, 74%, 75%, 76%, 77%, 78 %, 79%, 80%, 81%, 82%, 83% or 84% by mass of a support or at least one support.

The invention further relates to the aforementioned composition, for its use for the prevention of a disease induced by tick bites, in particular Lyme disease, but also tick-borne encephalitis, human granulocytic anaplasmosis, tularemia, Q fever, TIBOLA and LAR rickettsioses, pyroplasmosis, ehrlichiosis, and feline hemobartonellosis.

Ticks are vectors of more or less serious diseases in humans and animals. According to an estimate by the National Institute of Agronomic Research in France, ticks are the vectors of 30 to 40 bacteria or parasites and some viruses capable of infecting humans or animals.

Although it is the most well-known disease caused by tick bites, Lyme disease is not the only infection that ticks can transmit to humans. Six other pathologies have been identified in France by the administrations responsible for health vigilance: tick-borne encephalitis, human granulocytic anaplasmosis, tularemia, Q fever and two rickettsioses: TIBOLA (tick-borne lymphadenopathy) and LAR (lymphangitis -associated rickettsiosis).

Lyme disease is caused by infection with bacteria of the genus Borelia . On average thirty days after the tick bite, an erythema migrans is observed from the bite point. The lesion of the skin can be accompanied by muscle and joint pain, or fever. In the absence of treatment in the first stage, an evolution towards a secondary phase, not systematic, can worsen the prognosis. The infection can become chronic and spread from the skin to the whole body. Serious complications affecting several organs (joints, brain, heart, etc.) are then observable. In more serious forms, later serious tertiary manifestations can also be observed, in particular articular, cutaneous, neurological, muscular, or cardiac.

Tick-borne encephalitis is a disease of viral origin transmitted to humans by tick bites. It affects the central nervous system and can cause severe brain damage. The first symptoms are banal (fever, headache, sometimes nausea and vomiting). In 30% of cases, these symptoms are followed by high fever and signs of central nervous system involvement. In its second phase, encephalitis can lead to paralysis and, in less than 1% of cases, lead to the death of the infected person.

Human granulocytic anaplasmosis is also a viral infection transmitted by the bite of a tick. The symptoms are similar to those of the flu: chills, fever, headache, myalgia... Anaplasmosis can also be accompanied by forms of conjunctivitis, pharyngitis or cough.

Tularemia is a rare disease caused by the bacterium Francisella tularensis transmitted to humans through the bite. The tick is not the only vector of this disease which can be transmitted by rodents (rabbits, rats…), but also mosquitoes or flies. The symptoms are like the previous pathologies the appearance of fever, headaches and are accompanied by muscle pain and great fatigue.

Q fever is caused by the bacterium Coxiella burnetti , transmitted by ticks, although its primary mode of transmission is through the air, inhalation of contaminated airborne particles, and skin contact or mucosa with the fluids of infected animals. Q fever is most often manifested by a flu-like state, a rash in the chest, armpits and thighs.

LAR and TIBOLA rickettsioses are two infections caused by ticks. Both infections cause an inoculation eschar which is surrounded by a red halo‚ most often on the scalp.

In dogs, there are also potentially serious diseases such as babesiosis or pyroplasmosis, which induces anemia in infected animals by hemolysis, ehrlichiosis, Lyme disease.

In cats, in addition to Lyme disease and ehrlichiosis, tick bites can transmit a parasite causing feline hemobartonellosis, which attacks red blood cells and can be fatal.

Also disclosed is a method of preventing tick infestation, and preventing disease induced by tick bites, said method comprising administering to an animal or human an effective dose of a composition as defined above.

The invention will be better understood in the light of the following examples.

Examples

EXAMPLE 1 - formulation according to the invention

A composition according to the invention as used in the examples below is composed of:

- 17% turmeric rhizome extract comprising 95% curcuminoids,

- 8.5% pumpkin seed extract,

- 0.68% linalool thyme essential oil,

- 0.68% mountain savory essential oil, and

- 54.24% sorbitol as carrier,

the percentages being expressed by mass relative to the total mass of the composition.

For the per os formulation, the composition is prepared in the form of mini tablets, in particular mini tablets of 80 mg each.

Essential oils are infused onto the sorbitol, and the sorbitol is mixed with squash extract and turmeric powder. The mixture of powders is then compressed to obtain powdery tablets, then sieved in order to eliminate uncompressed powder residues. After checking the mass of the tablets, they are packaged for storage and marketing.

The tablets obtained being friable, they can easily be crushed (for example with a pestle) to be mixed with food or with drinking water. The tablets can be taken daily at once, or spread out over the day (morning and evening, morning noon and evening, etc.). Each tablet includes 13.6 mg of turmeric extract and 0.68 mg of each essential oil.

The prescribed daily dose for men is 15 tablets, which represents a quantity of turmeric extract below the regulatory limit of 210 mg.

The prescribed dose in animals is 1 tablet of 80 mg per 4 kg of animal.

EXAMPLE 2 - application in humans

A breeder of beef cows and poultry was a daily victim of tick bites.

As part of taking food supplements, this breeder began in February 2020 to consume the composition according to the invention at the rate of 15 mini tablets per day.

After a few days of using the composition according to the invention, the breeder and his wife initially noticed that he no longer had ticks on his skin or on his clothes.

In April 2020, the breeder stopped consuming the composition according to the invention, and very quickly the ticks gradually returned.

The infestation on his skin and clothes very quickly disappeared as soon as the composition according to the invention was taken up again.

At the same time, the breeder's wife gave the same treatment to her 5-year-old daughter, very regularly affected by tick bites. After a few days of treatment, the result was just as effective as that observed on his father.

These results show that the consumption of the composition according to the invention has positive effects in humans, and that its consumption prevents infestation (and therefore tick bites) both in adults and also in children.

EXAMPLE 3 - application in animals

A game warden in the region of Tours in France, owner of a dog who very often walks in the undergrowth or in the tall grass, favorable ground for ticks during the summer period (June, July, August), saw his dog prone to numerous tick bites.

On June ¹ , 2020, the game warden integrated the composition according to the invention into the daily mash of his bitch at the rate of 3 mini tablets per day (1 tablet for 4 kilos of weight).

After a few days of treatment, the results observed are just as obvious as those obtained in humans or children, namely the disappearance of ticks on the animal. Without having changed her behavior and her walks in the grass, the dog, still under treatment, has had no bites or presence of ticks since the beginning of this cure.

These results show that the consumption of the composition according to the invention is both effective in humans and animals.

Claims (10)

Composition comprising
- an extract of turmeric,
- a pumpkin extract,
- thyme essential oil, and
- savory essential oil
for its use in the prevention of infestation by blood-sucking mites of mammals. A composition for its use according to claim 1, wherein said mites are ticks. A composition for use according to claim 1 or claim 2, wherein the turmeric extract is a turmeric rhizome extract. Composition for its use according to any one of Claims 1 to 3, in which the pumpkin extract is a pumpkin seed extract. Composition for its use according to any one of Claims 1 to 4, the said composition being such that it comprises:
- 54 to 90% turmeric extract
- 5 to 30% thyme essential oil, and
- 5 to 16% savory essential oil
the percentages being expressed by mass relative to the total mass of turmeric extract and of the essential oil of thyme and of the essential oil of savory. Composition for its use according to any one of Claims 1 to 5, the said composition being in a form capable of being administered per os. A composition for use according to any one of claims 1 to 6, said composition further comprising a carrier. Composition according to Claim 7, in which the said support represents from 51 to 84% by mass relative to the total mass of the composition. Composition for its use according to any one of claims 1 to 8, said composition comprising
- from 10 to 25% by mass of a turmeric extract,
- from 5 to 20% by mass of a pumpkin extract,
- from 0.5 to 2% by mass of thyme essential oil, and
- from 0.5 to 2% by mass of savory essential oil,
the percentages being expressed by mass relative to the total mass of the composition. Composition as defined in any one of Claims 1 to 9, for its use in the prevention of a disease induced by tick bites, in particular Lyme disease