BR102017006286A2 - repellent chemical formulation containing natural andiroba component - Google Patents

Abstract

Repellent chemical formulation containing natural andiroba component. The present invention relates to chemical insect repellent formulation containing as one of the active ingredients a natural component derived from andiroba (carapa guianensis or carapa procera). More specifically, the present invention relates to n, n-diethyl-3-methylbenzamide-repellent formulation, also called n, n-diethyl-meta-toluamide (deet), whose repellent effects have been surprisingly enhanced by the synergism established by the incorporation of natural component originating from andiroba.

Description

(54) Title: CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL ANDIROBA COMPONENT (51) Int. Cl .: A01N 37/18; A01N 65/26; A01N 25/04; A01P 7/04 (73) Holder (s): BERACA INGREDIENTES NATURAIS S.A.

(72) Inventor (s): DANIEL NOSÉ SABARÁ (85) Start date of the National Phase:

27/03/2017 (57) Abstract: CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL ANDIROBA COMPONENT. The present invention deals with an insect repellent chemical formulation containing, as one of the active ingredients, a natural component derived from andiroba (Carapa guianensis or Carapa procera). More specifically, the present invention deals with a repellent formulation based on N, N-diethyl-3-methylbenzamide, also called N, N-diethyl-metho-toluamide (DEET), whose repellent effects were surprisingly improved by the synergism established by the incorporation of natural component originating from andiroba.

1/7 “REPELLENT CHEMICAL FORMULATION CONTAINING ANDIROBA NATURAL COMPONENT”

Field of the Invention [0001] The present invention deals with an insect repellent chemical formulation containing, as one of the active ingredients, a natural component derived from andiroba (Carapa guianensis or Carapa procera).

[0002] More specifically, the present invention deals with a repellent formulation based on N, N-diethyl-3-methylbenzamide, also called N, Ndietyl-meta-toluamide (DEET), whose repellent effects were surprisingly improved by the synergism established by the incorporation natural component originating from andiroba.

Description of the State of the Art [0003] DEET is an active ingredient found in the formulas of many topical repellents. It is a virtually colorless liquid with a characteristic odor. It is manufactured to be applied directly to the skin or clothes, having as main function to protect against insect, tick and arthropod bites. In particular, DEET protects against tick bites (which transmit Lyme disease) and mosquito bites (which transmit dengue, malaria and yellow fever), among other insects, such as ants.

[0004] In Brazil, commercially available products, which are sold as repellents for topical use on the skin, DEET has its name of active ingredient indicated on packaging such as Diethyl Toluamide, in Portuguese, Dietiltoluamida, and its concentration generally varies between 5% and 15%. The use of DEET is strictly regulated and controlled by the Health Surveillance Agency (ANVISA-Brasil), with maximum concentrations established according to the type of product and the target age group.

[0005] In Brazil, according to data obtained from ANVISA, there are 122 commercial repellents available. Among them, those that contain DEET as

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2/7 active components are the most suitable for repelling mosquitoes of the Aedes genera. However, it should be noted that DEET is a synthetic asset that, despite having proven efficacy and safety, also presents restrictions of use and a high degree of irritability of human skin. The formulations currently on the market that have only the active component DEET in a concentration of 5% by weight / weight give, on average, a protection of only 90 minutes. In concentrations in the order of 15% by weight / weight, the time of action of the repellents based on DEET recommended for adults is about 6 hours and for children only two hours.

[0006] Thus, natural alternatives that can increase the performance of DEET-based repellents by 5% weight / weight, which are less irritating and toxic, are of great interest to the cosmetic market. In addition, stimulating the application of Brazilian biodiversity assets for actions with a high degree of national and international demand is of great interest for economic development through the sustainable use of plant raw materials.

[0007] Andiroba, also known as andirova, andiroba-suruba, angirova, carapace and purga-de-santo-inácio, is a tree of the Meliaceae family. Its use is officially recognized by the Ministry of Health of Brazil as a plant with phytotherapic properties.

[0008] Andiroba has a repellent action and its effectiveness has already been demonstrated in some scientific studies, where the repellent power was justified by the concentrations of limonoids present in its composition. In the Amazon region, where oil is widely used as a medicinal plant by residents, andiroba is recognized as having antibacterial, antifungal and antiviral action, in addition to its repellent action. Also, andiroba oil has a tonic effect on the hair and can also be used as a massage oil.

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3/7 [0009] The oil contained in the andiroba almond is light yellow and extremely bitter and, when subjected to a temperature below 25 ° C, it solidifies, becoming with a consistency similar to that of petroleum jelly. Andiroba oil is composed mainly of palmitic, oleic, linoleic and stearic acid, in addition to an unsaponifiable fraction (1 to 5%) formed mainly of terpenoids, especially limonoids, which are mainly responsible for the biological activity of the oil.

[0010] Due to the well-known fact of the repellent effect of andiroba, some patent documents of the state of the art generally cite its uses in repellent compositions, but without any specificity, examples of achievements and tests to prove effectiveness. Among them, the US patent application US20090069407, filed by Phero Tech International Inc., dealing with hematophagous arthropod repellent compositions containing one or more allyl sulfide, allyl disulfide and / or allyl polysulfide. This document mentions compositions containing DEET and natural insect repellent substances, but none of the aforementioned DEET associations refers specifically to andiroba (see [0011] and [0012]). This document has the Brazilian correspondent PI08094160, filed as published by the National Institute of Industrial Property - INPI, on March 29, 2016. Another US patent application, US20150064124, filed by Segetis Inc., deals with personal care formulations containing alkyl ketal esters with a specifically defined chemical structure. Vegetable oils, including andiroba (see [0097]), and other insecticides, such as DEET (see [0265]), are mentioned as possible additional ingredients in these formulations. However, these ingredients do not appear in the same formulation. Although this document US20150064124 generally cites andiroba and DEET as possibilities of presence in an insect repellent composition, it does not even present at least one example of a composition containing these two active principles, that is, it does not reveal or deal with the combination of andiroba with DEET. This document has the Brazilian correspondents BR1120120287176 and BR1120120287206.

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4/7 [0011] Against this backdrop, the Depositor sought natural repellency alternatives that are of great interest to the cosmetic market, but at the same time presents the potential for results only achieved with an increase in the concentration of the chemical component DEET, which is not advisable, nor allowed by governmental bodies regulating public health, imposing restrictions on use due to its high irritability and possible toxicity.

[0012] Furthermore, promoting the use of natural components and sustainable economic development favors the promotion of new markets and social growth of the steakholders involved.

[0013] Thus, the association of andiroba oil provides a degree of naturalness for repellent formulations, notably for DEET-based formulations that are used against Aedes mosquitoes.

[0014] This natural alternative provided by the present invention was achieved by incorporating andiroba oil, obtained according to the Depositor's own methodology, in DEET-based formulations that typically do not exceed concentrations in the order of 5% weight / weight, resulting in a formulation high efficiency in insect repellency, notably those that cause diseases such as dengue, zika, chikungunya, malaria and yellow fever, among others.

Brief Description of the Invention [0015] The present invention aims to provide an insect repellent formulation that presents a greater performance in its effectiveness even using conventional amounts of the chemical component DEET as low as 5% by weight of the formulation.

[0016] Another objective of the present invention is to provide an insect repellent formulation based on DEET (5% by weight / weight) that by the association of the natural component of andiroba oil (5% by weight / weight) increases its

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5/7 performance in the effectiveness time of the current about 90 minutes to about 6 hours, both in adult and child use.

[0017] Yet another objective of the present invention is to provide an insect repellent formulation based on DEET and andiroba oil that does not present irritability on human skin, even in continuous applications.

[0018] The present invention provides an insect repellent formulation with a low concentration of DEET and, at the same time, has a long time of effectiveness, both in adult and child use.

Detailed Description of the Invention [0019] The formulation object of the present invention comprises, in weight / weight percentage, 5% of Ν, Ν-diethyl-meta-toluamide (DEET), 5% of andiroba, 5% of the commercial product Hostacerin SAF, 1.5% of the commercial product Nipaguard SCP, and deionized water (100% qsp).

[0020] Hostacerin SAF is a registered trademark rheology modifying product of the company Clariant SA, which comprises mineral oil, isopropyl palmitate, Trilaureth-4 phosphate, rapeseed oil sobol ester, ammonium dimethyl acetate and vinylpyrrolidone copolymer . Nipaguard is a preservative product, also from Clariant S.A., which comprises sorbitan caprylate and phenoxyethanol.

[0021] The formulation according to the present invention is produced in the form of a cream emulsion for topical application. In general, the formulation object of the present invention is prepared by conventional method of mixing the components. Thus, a first phase is prepared by mixing and homogenizing the components DEET, Hostacerin SAF, andiroba oil and Nipaguard SCP, followed by the addition of a second phase of deionized water and mixing until reaching a final homogenized phase.

Repellent Efficiency Tests [0022] The repellent formulation according to the present invention has been subjected to efficiency tests by a specialized laboratory of the Department

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6/7 Entomology of Laboratories Ecolyzer Ltda. (accredited by Cgcre under number CRL 640), against the species of mosquitoes Aedes aegypti. These tests are described below in a synthetic form and were performed in accordance with OPPTS 810.3700: Insect Repellents for Human Skin and Outdoor Premises Product Performance Test Guidelines - EPA Environmental Protection Agency 712-C-10-001 July 7, 201. They were also following the regulations of Resolution 466, of 12/12/2012 - Regulatory Guidelines and Norms for Research Involving Human Beings - National Health Council - Brazil.

[0023] The tests were conducted with twelve volunteer people, duly identified by their personal characteristics, such as sex, age, color, height and weight. These two people were used as negative controls. Mosquitoes, raised in the laboratory, were also characterized by their respective stages, age and sex, having been previously prepared by blood feeding and / or fasting before studies, carried out in rooms that are properly environmentalized. Sample doses of 2g / 600m3 were applied to the volunteers' forearms, with exposure to mosquitoes for a period of five minutes for each period evaluated.

[0024] The tests are considered satisfactory if after a period of one hour from the application of the sample, 100% repellent efficacy is proven, that is, no bite observed in all volunteers.

[0025] The results of mosquito activities in untreated volunteers are illustrated in Table 1 below:

TABLE 1

Time Volunteer without treatment (1) Volunteer without treatment (2) No. of landings No. of bites No. of landings No. of bites 1 hour 7 1 14 2 2 hours 8 0 10 2 3 hours 11 0 13 0 4 hours 13 2 11 1 5 hours 7 1 10 2 6 hours 5 1 16 3 1 hour 9 0 12 1

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1Π [0026] The results of stings in the volunteers treated with the sample (R1 to R10) are illustrated in Table 2 below:

TABLE 2

Time R1 Number of stings R10 R2 R3 R4 R5 R6 R7 R8 R9 1 hour 0 0 0 0 0 0 0 0 0 0 2 hours 0 0 0 0 0 0 0 0 0 0 3 hours 0 0 0 0 0 0 0 0 0 0 4 hours 0 0 0 0 0 0 0 0 0 0 5 hours 0 0 0 0 0 0 0 0 0 0 6 hours 0 0 0 0 0 0 0 0 0 0 7 hours 0 1 0 0 2 1 3 0 0 1

[0027] The above results demonstrate that the repellent sample formulated in accordance with this one behaved in a fully satisfactory and efficient manner for at least 6 hours in duration, without any bite from the Aedes egypti mosquito. This behavior demonstrates the synergism specifically developed with the association of only 5% by weight / weight of andiroba in a formulation containing as low amounts of DEET as 5% by weight / weight, reaching an efficacy of about 6 hours of action against just 90 minutes obtained with state of the art formulations.

[0028] The present invention extends to any other equivalent formulations, where DEET is used as an active component in association with andiroba, in order to prolong its effectiveness, especially against insects, preferably the Aedes egypti mosquito.

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Claims (7)

Claims 1. CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL COMPONENT ANDIROBA, characterized by comprising, in weight / weight percentage, 5% of Ν, Ν-diethyl-meta-toluamide (DEET), 5% of andiroba, 5% of the commercial product Hostacerin SAF, 1 , 5% of the commercial product Nipaguard SCP, and deionized water (100% qsp). 2. CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL COMPONENT ANDIROBA, according to claim 1, characterized by the fact that Hostacerim SAF is a product comprising mineral oil, isopropyl palmitate, Trilaureth-4 phosphate, rapeseed oil ester, dimethyl acetate ammonia and vinylpyrrolidone copolymer. 3. CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL ANDIROBA COMPONENT, according to claim 1, characterized by the fact that Nipaguard is comprised of sorbitan caprylate and phenoxyethanol. 4. CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL ANDIROBA COMPONENT, according to claim 1, characterized by the fact that it has an effectiveness of about 6 hours of action, both in adult and child use. 4. CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL ANDIROBA COMPONENT, according to claim 1, characterized by the fact that its use is against insects such as ticks and ants and mosquito bites. 5. CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL ANDIROBA COMPONENT, according to claim 4, characterized by the fact that the mosquito is Aedes egypti. Petition 870170020218, of March 27, 2017, p. 12/15 2/2 6. CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL COMPONENT ANDIROBA, according to claim 1, characterized by the fact that it is produced in the form of a cream emulsion for topical application. 6. CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL ANDIROBA COMPONENT, according to claim 1, characterized by the fact that it is produced in the form of a cream emulsion for topical application. 7. CHEMICAL FORMULATION REPELLENT CONTAINING NATURAL COMPONENT ANDIROBA, according to claim 6, characterized by the fact that a method of mixing the components is produced, a first stage being prepared by mixing and homogenizing the components DEET, Hoscerin SAF, andiroba oil and Nipaguard SCP, followed by the addition of a second phase of deionized water and mixing until reaching a final homogenized phase. Petition 870170020218, of March 27, 2017, p. 13/15 1/1