IT201600102856A1 - Composition with repellent activity for ticks, fleas and mosquitoes. - Google Patents

Description

Field of the invention

The present invention refers to a composition with repellent activity for ticks, fleas and mosquitoes.

In particular, the present invention refers to a synergistic composition, with repellent activity for ticks, fleas and mosquitoes, comprising as active ingredients neem oil in combination with tea tree oil, lemongrass oil and lavender oil.

Description of the figures

Figure 1 shows an example of the rabbit (or other animal) hair base, obtained with the preparation procedure described in the experimental section.

Known technique

Neem oil is a vegetable oil obtained by cold pressing the seeds of the Azadirachta Indica plant, belonging to the Meliaceous family. This oil has antiviral, antibacterial, antiparasitic, antiseptic and antifungal properties that make its use suitable not only for the care of human health, but also for the protection of plants and animals from attacks by insects and parasites.

Malaleuca oil, also known as "tea tree" essential oil, is extracted from the leaves of the Melaleuca alternifolia tree, a plant species native to Australia. It has significant antifungal and antibacterial activity, in particular against streptococci, fungi and candida. Furthermore, it is effective in many skin diseases such as acne, eczema, psoriasis and in many genitourinary infections such as chronic cystitis and vaginitis. Thanks to its healing and disinfectant properties, it is used both in natural cosmetics and in household cleaning.

Lemongrass essential oil is obtained from Cymbopogon nardus, a plant of the Poaceae family. It is known for its stimulating activity on the nervous system and plays a positive action useful in case of headaches due to nervous tension, stress, psychophysical fatigue and on states of deconcentration. This oil is best known for its repellent properties against mosquitoes and other insects, and for its antiviral, antispamodic and deodorant activity.

Lavender oil is obtained from Lavandula angustifolia, a plant of the Labiate family. It exerts a rebalancing action on the central nervous system, being at the same time tonic and sedative. It is useful in cases of insomnia, menstrual pain and cystitis, and is also known as an antiseptic and antibiotic, antispasmodic, anti-inflammatory, analgesic and healing agent.

Compounds useful for killing or preventing the hatching of flea, tick and / or mosquito eggs are already known in the art.

The oldest known pesticides in the art are pyrethroids (derivatives of "pyrethrins"), these compounds inactivate the insect's nerve cells by blocking their sodium or chlorine channels. After exposure to pyrethrins, the flow of sodium in the insect's nerve cells is altered and repeated damage at the cellular level causes the insect to die.

The most used synergist compound with pyrethrins is “piperonyl butoxide”, it increases its penetration capacity into the insect.

Pyrethroids are a class of synthetic insecticides and acaricides synthetic analogues of pyrethrins.

Pyrethrins are natural constituents of Tanacetum cinerariifolium flowers.

Thanks to the similarity with pyrethrins of natural origin, synthetic pyrethroids act in the same way as pyrethrins, however overcoming the main limit of the latter, their photoleability.

The first synthetic pyrethroid was fenvalerate, launched on the market in 1978 and today this class is composed of about 42 active ingredients.

To date pyrethroids are present in almost all outdoor diffusers designed to fight mosquitoes and insects and to this class belong deltamethrin, cypermethrin, phenothrin, lambda-cyhalothrin, permethrin and transflutrin.

Organophosphates and organocarbamates are new generation pesticides used in pet collars for the killing of ticks and fleas.

These compounds inhibit acetylcholinesterase, an enzyme necessary for normal nerve function.

Organophosphates should not be used on cats, although they are present in many commercial pet collars for these animals and this group includes chlorpyrifos, dichlorvos, fosmet, naled, tetrachlorvinfos, diazinone and malathion.

These compounds are the active ingredients in dozens of pet products.

Chlorpyrifos is contained in a flea and tick collar for dogs.

Dichlorvos, naled, tetrachlorvinfos and diazinone are used in flea and tick collars for both dogs and cats.

The "Frontline" on sale today in many pet shops is based on Fipronil (arylheterocycles).

The United States patent US 2,219,569 describes a germicidal collar provided with a leather pocket in which the germicide is inserted.

US patent 3,978,820 describes a germicidal collar provided with an insecticide impregnated strip.

US patent US 4,091,766 discloses a collar with a tubular and flexible configuration, in which an insecticide strip is applicable.

Numerous further US patents relate to collars to be refilled or not, with substances having insecticidal activity.

The expert in the sector knows that despite the numerous patents and products on sale, the need is still very much felt in the art for new products not endowed with the toxicity of the compounds in use and mentioned above.

DESCRIPTION OF THE INVENTION

It has now been found that a composition comprising as active ingredients neem oil in combination with tea tree oil, lemongrass oil and lavender oil, and optionally one or more pharmaceutically acceptable excipients and / or diluents, shows an unexpected synergism in explicating a repellent activity on ticks, fleas and mosquitoes.

The object of the present invention is therefore a composition in solid, semi-solid, liquid or spray form, comprising as active ingredients neem oil in combination with tea tree oil, lemongrass oil and lavender oil, and optionally one or more excipients and / or diluents pharmaceutically acceptable.

A further object of the present invention is a composition in solid, semi-solid, liquid or spray form; comprising as active ingredients neem oil in combination with tea tree oil, lemongrass oil and lavender oil, and optionally one or more pharmaceutically acceptable excipients and / or diluents,

in which:

neem oil is present at a dose of 40-80%, preferably at a dose of 50-70%; most preferably at a dose of 60%,

Malaleuca oil is present at a dose of about 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%;

lemongrass oil is present at a dose of about 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%;

and lavender oil is present at a dose of about 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%.

A further object of the present invention is a composition in solid, semi-solid, liquid or spray form; comprising as active ingredients neem oil in combination with tea tree oil, lemongrass oil and lavender oil, and optionally one or more pharmaceutically acceptable excipients and / or diluents,

in which:

neem oil at a dose of 60%

tea tree oil at a dose of 13.3%

lemongrass oil at a dose of 13.3%

lavender oil at a dose of 13.3%.

A further object of the present invention is a composition, slow-release by volatilization, comprising as active ingredients neem oil in combination with tea tree oil, lemongrass oil and lavender oil, and optionally one or more pharmaceutically acceptable excipients and / or diluents. ;

in which:

- said active principles are loaded on a base composed of heated and pressed rabbit hair;

- said base is characterized by the fact that it favors the slow release by volatilization of the active ingredients;

- neem oil is present at a dose of 40-80%, preferably at a dose of 50-70%; most preferably at a dose of 60%,

Malaleuca oil is present at a dose of about 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%;

lemongrass oil is present at a dose of about 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%;

and lavender oil is present at a dose of about 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%;

for use for:

- prevent tick, flea and mosquito bites on animals and / or humans;

- prevent the presence of ticks and fleas on animals and / or humans;

- prevent the presence of ticks, fleas and / or mosquitoes in the environments where animals and / or humans live.

A further object of the present invention is a composition, slow-release by volatilization, comprising as active ingredients neem oil in combination with tea tree oil, lemongrass oil and lavender oil, and optionally one or more pharmaceutically acceptable excipients and / or diluents. ;

in which:

- said active principles are loaded on a suitable base composed of heated and pressed rabbit hair;

- said base is characterized by the fact that it favors the slow release by volatilization of the active ingredients;

- in which:

neem oil at a dose of 60%

tea tree oil at a dose of 13.3%

lemongrass oil at a dose of 13.3%

lavender oil at a dose of 13.3%;

for use for:

- prevent tick, flea and mosquito bites on animals and / or humans;

- prevent the presence of ticks and fleas on animals and / or humans;

- prevent the presence of ticks, fleas and / or mosquitoes in the environments where animals and / or humans live.

A further object of the present invention is the use of neem oil in combination with tea tree oil, lemongrass oil and lavender oil, and optionally one or more pharmaceutically acceptable excipients and / or diluents for the preparation of a pharmaceutical composition for use in the veterinary or human field, in the form of lotion, ointment, semi-fluid cream, fluid cream, gel or spray, in which said composition is directly applicable on the fur of animals; or on suitable supports applicable to animal collars or leashes; or in the form of more or less decorative objects to be placed in domestic environments or where animals are sheltered, such as homes, vehicles, stables, shelters or kennels.

By suitable base according to the present invention it is meant a soft, semi-soft or rigid base; of synthetic or natural origin, characterized by the fact that said base:

- possesses the ability to retain solid, liquid or semi-liquid substances such as oils, gels or creams in its structure;

-it is suitable for slow release by volatilization of the active ingredients.

An example of said base is supports of synthetic origin are sponges, rubber or fabrics having the characteristics described above, in the form of more or less decorative objects or labels applicable on leashes and / or collars of animals, preferably pets, or in environments in which which human beings and / or animals live.

An example of said base of natural origin is composed of compressed rabbit hair.

The composition according to the present invention was conceived in response to the need to prevent the bite of ticks, fleas and mosquitoes on animals and / or humans and in response to the need to favor the removal from domestic animals and from the environments where the animals live. people of ticks fleas and mosquitoes.

The following examples illustrate the invention without limiting it.

DETAILED DESCRIPTION OF THE INVENTION

EXAMPLE 1

Ability of neem oil alone or in combination with tea tree oil, lemongrass oil and / or lavender oil, to reduce the number of fleas and / or ticks on small and medium-sized pet dogs.

The test was carried out on 60 dogs, divided into groups of 10 each, in which said dogs were regularly taken to outdoor spaces dedicated to them and / or to public gardens.

The animals were divided into homogeneous groups based on the size and the period of enrollment.

On the collar or on a strap (external part) of each animal was applied a base (the same for all, 0,8cmx5cm) made of pressed rabbit fur.

The base was refilled with 5 drops of the tested compound once a week.

The enrollment of the animals began on May 1st and ended at the end of May.

All the animals were treated 15 days before the start of the test with the same product, known in the art, with anti-tick and flea activity.

All animals at time 0 did not show fleas and / or ticks (veterinary visit / expert in the field).

The observation was carried out for 3 months in the period May-July.

The recharging of the base and the control of the presence or absence of ticks and / or fleas (on animals) was carried out weekly by two experts in the sector.

On the date of finding the presence of the parasite, the animal was excluded from the test, washed appropriately and treated with one or more known products on the market as suggested by experts in the field.

The groups formed were the following:

- Group 1 complete composition according to the invention;

-Group 2 neem oil malaleuca oil;

-Group 3 Neem Oil Lemongrass Oil

-Group 4 neem oil lavender oil

-Group 5 Neem Oil Malaleuca Oil Lemongrass Oil

-Group 5 Neem Oil Lemongrass Oil Lavender Oil

-Group 6 neem oil malaleuca oil lavender oil

The different combinations contained the respective active agents at the following concentrations:

neem oil at a dose of 60% and / or

tea tree oil at a dose of 13.3% and / or

lemongrass oil at a dose of 13.3% and / or

lavender oil at a dose of 13.3%.

The results obtained are shown in the following table 1.

TABLE 1

Number of fleas and / or ticks on dogs, small and medium sized pets, treated with neem oil alone or in combination with tea tree oil, lemongrass oil and / or lavender oil.

ANIMAL GROUPS

N ° DAY IN WHICH THE PRESENCE WAS DETECTED

"-" = ABSENCE; PRESENCE OF TICKS (Z) or FLEAS (P)

1 2 3 4 5 6

1 - - - - - -2 42 (Z) 35 (PZ) 35 (P) 42 (PZ) 35 (Z) 42 (Z)

3 35 (P) 28 (Z) 42 (PZ) 35 (Z) 35 (PZ) 35 (P)

4 35 (Z) 35 (Z) 28 (PZ) 35 (Z) 49 (P) 35 (Z)

5 28 (Z) 42 (PZ) 35 (Z) 49 (P) 35 (Z) 42 (PZ)

6 42 (PZ) 35 (Z) 42 (Z) 35 (Z) 35 (P) 49 (PZ)

7 42 (Z) 35 (Z) 28 (Z) 42 (Z) 42 (PZ) 35 (P)

8 28 (Z) 28 (PZ) 42 (P) 35 (Z) 35 (Z) 42 (Z)

9 35 (Z) 42 (P) 35 (Z) 49 (PZ) 35 (Z) 42 (PZ)

10 42 (P) 35 (Z) 35 (PZ) 35 (P) 42 (Z) 35 (Z)

EXAMPLE 2

Ability to reduce the number of mosquitoes present in domestic environments in the May-September period of neem oil alone or in combination with tea tree oil, lemongrass oil and / or lavender oil; placed / administered on two labels of 0.8cm x 10cm composed of pressed rabbit fur, in which said labels were placed in two different places in the same environment.

The labels were refilled with 10 drops of compound once a week.

The environments treated were 10.

Observation period July-August.

The observation was made by the owner of the house.

When the mosquitoes persisted for more than a week in the treated environment, the treatment was stopped.

The results obtained are reported in the following Table 2.

TABLE 2

Presence or absence of mosquitoes in environments treated with neem oil alone or in combination with tea tree oil, lemongrass oil and / or lavender oil. GROUPS environment

PRESENCE OF MOSQUITOES: B = LOW (1-2); M: AVERAGE (> 2);

A = HIGH (> 5 MOSQUITOES); “0” = ABSENCE OF MOSQUITOES.

1 2 3 4 5 6

1 0 0 0 0 0 0

2 M M M A B M

3 A A M M B M

4 A M M M M B

5 M A A B M A

6 M M A B B M

7 A M M M M B

8 M B B B A M

9 M A M M B B

10 B M A B M M

The complete composition according to the invention shows an unexpected synergistic effect in preventing the colonization of dogs by ticks and fleas and in preventing the presence and bites of mosquitoes in homes compared to the use of individual components or minimal combinations between them.

In addition, the individuals treated with the composition according to the invention reported that they did not perceive olfactory disturbances and did not notice discomfort in the treated animals during the entire treatment period.

EXAMPLE 3

Method of preparing a rabbit hair base.

Rabbit hair was stratified in a hot air oven on suitable metal molds.

The amount of pile for each layer was chosen according to the desired thickness after pressing.

The shape of the mold determined the geometric appearance of the obtained base (square, rectangular, cord or other shape).

The heating temperature (about 90 ° C) selected was the maximum that did not cause obvious damage to the hair after 30 minutes of heating. The temperature to be used is easily determined by the expert in the field based on the type of animal hair desired / used.

At the end of the 30-minute treatment at the desired temperature, the molds were placed under a press and subjected to a pressure corresponding to that of about 80 atmospheres, obtaining a base of the type shown in Figure 1.

EXAMPLE 4

Comparative tests of slow release due to volatilization of the active ingredients

The following Table 3 shows the results obtained on slow release comparative tests by volatilization of the active ingredients placed on different bases of the same size and obtained with the same preparation method described in example 3; 5 drops per base; 5 bases per group; in which it is clear that only the rabbit hair allows a slow release that lasts for more than 7 days.

TABLE 3

BASIC DAY IN WHICH IT STARTS TO DECREASE IN ONE

SIGNIFICANT WAY THE SMELL OF THE COMPOUND FROM THE FUR OF COMPOUND ACCORDING TO THE INVENTION PLACED ON THE BASE

RABBIT 9

DOG 2

CAT 4

CATTLE (TAIL) 2

EQUINE (TAIL) 2

The base according to the present invention obtained with rabbit hair has not only an excellent ability to retain / remain impregnated with the composition according to the invention, but also to allow the slow release (slow volatilization) of the composition itself with respect to hair is other animals. In fact, slow release tests (base width 0.8cm x length 5cm x height / thickness 2 mm; 5 drops) with the composition according to the invention at the concentrations described in Example 1 showed that after one week the base still released, in external environment, an active quantity of “deterrent / repellent aroma” for ticks, fleas and mosquitoes.

The above data show that rabbit hair compared to other easy-to-find non-wild animal hair shows the best slow release.

Neem oil, tea tree oil, lemongrass oil and lavender oil are compounds known in the art for use in humans and animals, extensively tested and easily available on the market.

Although the dose will depend, according to the judgment of the veterinarian on the basis of the weight, age and general condition of the animal, it is generally advisable to refill the base with 5 drops of the composition according to the present invention once a week.

Non-limiting examples of compositions according to the present invention are reported below.

COMPOSITION 1 (preferred)

neem oil at a dose of 60%

tea tree oil at a dose of 13.3%

lemongrass oil at a dose of 13.3% lavender oil at a dose of 13.3%; optionally excipients and / or diluents.

COMPOSITION 2

neem oil at a dose of 50% malaleuca oil at a dose of 20% citronella oil at a dose of 20% lavender oil at a dose of 10%; optionally excipients and / or diluents.

COMPOSITION 5

neem oil at a dose of 40-80%

tea tree oil at a dose of 5-20%

lemongrass oil at a dose of 5-20%

and lavender oil is present at a dose of 5-20%; optionally excipients and / or diluents.

Claims (7)

CLAIMS 1. Composition comprising as active ingredients neem oil in combination with tea tree oil, lemongrass oil and lavender oil, and optionally one or more pharmaceutically acceptable excipients and / or diluents, in which: - neem oil is present at a dose of 40-80%, preferably at a dose of 50-70%; most preferably at a dose of 60%, Malaleuca oil is present at a dose of 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%; lemongrass oil is present at a dose of 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%; And lavender oil is present at a dose of about 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%. 2. Composition of claim 1, comprising: neem oil at a dose of 60% tea tree oil at a dose of 13.3% lemongrass oil at a dose of 13.3% lavender oil at a dose of 13.3% and optionally one or more pharmaceutically acceptable excipients and / or diluents. 3. Slow release composition by volatilization, comprising as active ingredients neem oil in combination with tea tree oil, lemongrass oil and lavender oil, and optionally one or more pharmaceutically acceptable excipients and / or diluents; in which: - said active principles are loaded on a base composed of heated and pressed rabbit hair; - said base is characterized by the fact that it favors the slow release by volatilization of the active ingredients; - neem oil is present at a dose of 40-80%, preferably at a dose of 50-70%; most preferably at a dose of 60%, - Malaleuca oil is present at a dose of 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%; - lemongrass oil is present at a dose of 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%; And - lavender oil is present at a dose of about 5-20%, preferred is a dose of about 7-15%, much preferred is a dose of 13.3%; for use for: - prevent tick, flea and mosquito bites on animals and / or humans; - prevent the presence of ticks and fleas on animals and / or humans; - prevent the presence of ticks, fleas and / or mosquitoes in environments where animals and / or humans live. 4. Composition according to claim 3, wherein said base: - has a width of 0.2-2 cm; preferred are 0.8 cm; a length of 1-10cm, preferred are 5-10cm; and a thickness of 0.1-5 mm, preferred are 0.2-0.4 mm, particularly preferred are 2 mm; - can be loaded with 1-20 drops of the composition of claim 1 or 3, preferred are 5-10 drops; - it has the ability to retain the active ingredient with which it is loaded; - it has the ability to promote a slow release by volatilization of the active ingredient and in which said slow release lasts more than 7 days. 5. Composition of claim 3 or 4, wherein said base is obtained by layering the rabbit fur on a mold, in which said mold is placed in a hot air oven for 1-60 minutes, preferably 30 minutes, at a temperature comprised between 50 and 130 ° C, and after heating the mold containing the rabbit hair is placed under a press at a pressure of 10-100 atmospheres to obtain a base with characteristics to the touch similar to those of a fabric of natural or synthetic origin having the shape of the mold and the thickness based on the height of the layer of hair used. 6. The composition of claim 5, wherein said base is applied to a collar or leash of an animal, or is placed in a room of a dwelling. 7. The composition of claim 6, wherein said base has any shape or size useful for the purpose.