BRPI1100016A2 - a pesticide controlled release composition system containing deltamethrin, propoxur and insect repellent - Google Patents

Abstract

A SYSTEM OF COMPOSITION OF RELEASE CONTROLLED BY PESTICIDES CONTAINING DELTAMETRINE, PROPOXUR AND INSECT REPELLENT. This Invention Patent concerns a Pesticide Controlled Release Composition System that contains Deltamethrin, Propoxur and Insect Repellent, for the control of fleas and ticks, repelling and controlling the phlebotomine vectors, controlling the leishmaniasis and mosquito vectors, heartworm vectors and act as pesticides in the system. The System can be produced as a solid polymer for the release of the active ingredient which comprises a vinyl polymer, a liquid plasticizer, an active ingredient for pest control. The present invention patent includes not only the combination of the new drug but also complete the release of the active ingredients.

Description

"A Release Control System Controlled by Pesticides Containing DELTAMETRINE, PROPOXUR AND INSECT REPELLENT".

1. INTRODUCTION

Refer to the disclosure report of the present invention "A Pesticide Controlled Release Composition System Containing Deltamethrin, Propoxur and Insect Repellent". This composition acts as an insecticide to control fleas and ticks, repel the control of sand flies, leishmaniasis vectors, mosquitoes, dirofllariose.

It was necessary to avoid the various drawbacks to obtain the controlled release system with the active ingredients that have the properties contained in the pesticides,

In the preparation of the composite composition parts of the active components of the polyvinyl chloride polymer, the preparation was injected and molded into the collars as a controlled release matrix for use in animals. This will eliminate the inconveniences that occur during mixing with a polymer plasticizer and the other active ingredients; These problems manifest with incomplete release of the active ingredients.

2. - STATE OF THE TECHNIQUE

A variety of active ingredients such as pesticide properties mixed and combined with the polymers can be found in US Patent documents and used in the manufacture of belts, animal collars or other controlled release items, for example, US Patent No. 3,318,769, 3,852,416. 4,150,109 and 6,413,532.

We also find other documents dealing with different lamellar plastic materials, such as patent application E92111619 which talks about insect pill carcasses, for example, W9303154EP which provides a collar as if it were a device type or a cattle brand. which can be placed in the ear, containing a fatty acid gel, silicone organic solvent and an active ingredient that protects against one or more arthropod pests E99305998.

All of these patents have the drawbacks mentioned and others like, polymer blends and active ingredients are released and not used for what you want; The problem occurs with the active ingredient when the mixture is not uniform and translate into a less effective use of the active ingredient. These systems utilize a vinyl polymer, such as polyvinyl chloride (PVC), which is highly miscible by adding a plasticizer and triphenyl phosphate (TPP) used as a carrier for the active ingredient.

3. - FIELD OF APPLICATION.

The scope of this Pesticide Controlled Release Composition System Containing Deltamethrin, Propoxur and Insect Repellent overcomes the above described drawbacks of the above patents. Surprisingly, we found that a mixture of triphenylphosphate cresyl diphenyl phosphate and significantly promotes a release of active ingredients. The application of the present invention relates to a controlled release system of a mixture of active parasite-fighting ingredients from a polymer matrix; They are most effective in releasing the active ingredients into the blends of the techniques listed above. In addition, the pesticides of the present invention have a uniform rate of active ingredient release which makes the use of the active ingredient more effective and efficient.

4. DETAILED DESCRIPTION OF THE INVENTION

A Pesticide Controlled Release Composition System Containing Deltamethrin, Propoxur and Insect Repellent is to repel flea and tick control, as well as the phlebotomine, leishmaniasis and mosquito vectors, the heartworm vectors and acts as a pesticide. in itself.

The system can be produced as a solid polymer active ingredient release system comprising a vinyl polymer, a synergistic blend of plasticizers and a combination of active pest control ingredients. The enhancement includes not only the combination of the new drug, the release of the active ingredients is complete, and more particularly the polymer matrix system, comprising as an ingredient of a vinyl polymer a polymer miscible liquid plasticizer, the plasticizer amounts are as large as possible so that the plasticizer and polymer mixture is always kept dry and fluid; a mixture of triphenyl phosphate and having cresyl diphenyl in quantity, are great for serving as a carrier for such active ingredients.

Other elements of the present invention acting as external propoxur parasites are suitable for fleas, ticks and / or lice. The etiologic agents are flea sensitive, Ctenocephalides felis, Ctenocephalus canis, PuIex irritans, Tunga penetrans, Ticks, Riphicephalus sanguineus, Amblyomma maculatum, Fossum, Neumanni Amblyoma, Lice, Trichodectes canis, Linognathus subrusus spinus and Felognusus spinus.

Propoxur is a carbamate that binds to acetylcholinesterase and inactivates it. This inactivation therefore causes an increase in acetylcholine in the muscarinic and nicotinic receptors of the autonomic nervous system. At appropriate doses, the described effects are produced on acetylcholinesterase insects, which determine their death by paralysis.

There is evidence that percutaneous absorption and propoxur metabolism in a bi-behavioral organ culture model at non-toxic propoxur concentrations applied topically to the skin discs of pigs, rabbits and humans, where the permeability rates of The skin of humans and rabbits were comparable, while pigs were also twice as large, the permeable skin tissue of the three species has the ability to metabolize propoxur, propoxur hydrolysis produces 2 - isopropoxyphenol (PPI), followed by a face of reactions of conjugation II. The conjugation rate of IPP appears to be species specific. In tissue cultures of porcine origin, glucuronides and sulfates were detected in human skin, and were observed only with sulfate conjugation. In rabbit skin tissue, the main route of conjugation was instituted by glucuronation, followed by small amounts of sulfates and an unidentified metabolite.

The percentage of metabolised propoxur that was inserted into the rabbit's hair was not influenced by the dose in the range of 25-200 ml crograms / cm 2. In contrast, in human skin it was practically saturated at 100 metabolism, micrograms / cm 2.

Another active ingredient is ethyl butylacetylaminopropionate, which can be a very effective insect to arthropod repellent when stung. Mosquito (Anopheles gambiae and funestus), aedes aegypti and aedes albopictus, culex pipiens and culex quinquefasciatus). Phlebotomines (Lutzomyia longipalpis aragaoi, Lutzomyia cruzi, Lutzomyia intermedia, Lutzomyia migonei, Lutzomyia whitmani shanonni, Lutzomyia, Tejadai Lutzomyia, vexator Lutzomyia). Lice, horseflies, ticks, rubber, stable flies, wasps and bees.

Therefore, the system of the present invention is formed with the following components:

1- PVC resin;

2- Pyrethroids;

3-Propoxur;

Ethyl 4-butylacetylamino propionate;

5-Isoctyl phthalate;

6- Diphenyl cresyl phosphate;

7- Triphenyl Phosphate.

The object of the present patent is the controlled release system in most cases a dog cholera with ethyl propoxur, deltamethrin and butylacetylamino propionate and with the following drugs injected in proportions with percent values.

<table> table see original document page 5 </column> </row> <table> <table> table see original document page 6 </column> </row> <table>

The pyrethroid active ingredient may be selected from the following compounds: deltametry, acrinathrin, tralomethrin, permethrin, cypermethrin, alfamethrine, cyhalothrin, with pyrethroid being preferred.

Deltamethrin is one of the components used in insecticides worldwide, is a member of the family of safe insecticides, synthetic pyrethroids.

Deltamethrin is used in both agriculture, veterinary medicine and even insect control at home. Deltamethrin has been used to prevent the spread of mosquito and tick-borne diseases in dogs, rodents and other animals. It is effective in eliminating spiders, fleas, ticks, cockroaches, bed bugs, ants, mosquitoes and others.

Deltametry plays an important role in the control of disease vectors such as malaria and leishmania. It is used in the manufacture of long lasting insecticide nets. It is used to control different vectors including: Mosquito (Anopheles SSP, anopheles gambiae and funestus, aedes aegypti, aedes albopictus, celex pipiens, celex quinquefasciatus). Phlebotomines (lutzomyia longipalpis aragaoi, lutzomyia cruzi, lutzomyia intermedia, lutzomyia migonei, lutzomyia whitmani shanonni, tejadai lutzomyia, vexator lutzomyia). Lice, horseflies, ticks, rubber, booby flies, wasps, bees and flies. The most common is pyrethroid and can be used in conjunction with other insecticides.

The World Health Organization (WHO) has identified an increase in leishmaniasis. The WHO report recommends that dogs wear a deltamethrin-impregnated collar to prevent infection and contact between sand flies and animals, reducing the risk of infection in humans and canines.

The repellent system according to the present invention is particularly applicable to the control of mites, for example ticks, fly tills, insects, lice, bed bugs and various types of biting insects. The system also applies to sandfly-biting insects involved in the transmission of canine leishmaniasis caused by an insect bite that they can transmit to humans; This disease is very common in countries located in tropical and subtropical areas. Another feature of the present invention is protection against insects, mosquitoes, lice and other insects carrying infections; the best are a nuisance and at worst the vectors of diseases like malaria and yellow fever. Arthropod territory is dangerous as the Asian Tiger Mosquito (Aedes albopictus) and can be counteracted with the bultilacetylamino propionate ethylic feature of the present invention with an extremely effective profile and safe toxicologicals.

Amount for 100 kg and calculated for 100% drug.

<table> table see original document page 7 </column> </row> <table>

To prepare the substance use a PVC helix mixer, when it starts to warm the mixer jacket reaches 80 ° C, add the isoctyl phthalate maintaining the temperature of 8 ° C, then add the triphenyl phosphate mixing until complete homogenization. Deltamethrin at 80 ° C5 is then added gradually, then add propoxur at 80 ° C and stir until complete homogenization.

The butylacetylamino propionate ingredient is a repellent used and aggregated into the mixer keeping the mixture up to continuous flow freely, the last step being to inject in the proper size.

To test the efficacy of the trial, a migration of deltamethrin, propoxur, butylacetylamino propionate, triphenyl phosphate, ethyl phosphate and cresyl diphenyl collar was performed in one sample and in the competition collar sample, the following comparative results are obtained.

Table of concentration of assets in collars.

<table> table see original document page 8 </column> </row> <table>

The procedure used for the measurement was as follows: a cotton swab for each of the different moments of the surface of each ring; The contents are then cleaned by mixing them with a HPLC-sized solvent using the standard of each substance.

In the judgment a measurement of the concentration of the assets on the surface of the collar was used. The concentration of the assets was always in the biggest collar; Concerning the competition collar, that is, in the case of the mixture of triphenyl phosphate and diphenyl cresyl phosphate, it was observed that the relationship between the two favored the release to maintain a high concentration of deltamethrin and propoxur on the surface. in the lap through its role in transporting the asset to the surface.

Competition table on a leash.

<table> table see original document page 9 </column> </row> <table>

Table of ingredients inserted into the collar.

<table> table see original document page 9 </column> </row> <table>

The collars prevent contact between dogs and sand flies; they are likely to reach universal use to prevent parasite circulation and disease in humans, where they could disappear as in the dog that is the parasite's largest reservoir. The following examples illustrate the present patent:

Method of preparation 2.

Another preferred embodiment of the present invention is added to "vinyl chloride", a mixture of dry or more highly plasticizable miscible resin such as dioctyl adipate. The amount of plasticizer used is the maximum amount allowed for the dry and smooth mixture to remain. Separately the active ingredients are mixed with a mixture consisting of triphenyl transport phosphate, diphenyl phosphate and crecyl in a predetermined ratio to form a car-IA mixture. This mixture is melted and homogenized into a complete mixture and cooled to give a solid foundation that is the ground for small particles.

Results were obtained on the following parameters:

<table> table see original document page 10 </column> </row> <table>

Examples of the results:

1 - Bead comparison is obtained by injecting 10% deltamethrin propoxur g, 3 and 4 g acetyl ethyl butyl aminopropionate 1 g% versus 4% g injected deltamethrin cholera applied to dogs experimentally infected with ctenocephalides felis.

In dogs, the efficacy of two pesticides was compared; were used in 30 animals of both sexes, crossbred and of different ages, which were infested with 50 fleas (ctenocephalides delis) for fasting adults. At the first extoparasite count performed the combing technique was used in the first 24 hours; the canines were randomly divided into three groups of 10 animals: group "a" was treated with a 10% propoxur g, deltamethrin and 4 g acetyl ethyl butyl aminipropionate injected plastic collar; group "b" with a plastic rope injected with 4% deltamethrin and in group "c" a non-insecticidal plastic collar (control) was placed. The animals were kept in individual kennels, being fed with balanced feed and water ad libitum. In the treated groups there were no contacts with others at any time of the study. The first observation was made between 24 and 48 hours after application of the product. Each animal was re-infested with 25 fleas (Ctenocephalides felis) in adults and in seven days, 14,21,35,60,90,120,150,180 and 210.

After re-infestation, 24 and 48 hours, the efficacy observed during the first 48 hours after treatment application exceeded 95% in group "a" and did not reach 80%; in group "b". In group "a", the efficacy observed between days 15 and 121 was between 95% and 98%, and at 152 days a value considered low was found.

It was concluded that the plastic matrix of the deltamethrin impregnated collar, 10% propoxur g, and 4 g acetyl-et-butyl g aminopropionate, determines:

1- That flea infestation and re-infestation was controlled with (ctenocephalides felis), achieved higher efficacy rates for a long time with the 4 g% deltamethrin-containing period.

2- That the comparison of beads injected with 10% deltamethrin propoxur g, and 4 g of 1 g% aminopropionate acetyl-ethyl butyl versus cholera with deltamethrin, injecting 4% g and applied to experimentally infected rhipicephalus dogs in the bloodstream .

In dogs experimentally infected with ticks (blood rhipicephalus) the efficacy of the two ectoparasiticide-injected plastic collars was evaluated. One product contained 10% propuxur g, deltamethrin and 4 g acetyl ethyl butyl g aminopropionate 1 product "a" and the other 4 g deltramethrin in product "b". They were used in 30 animals of both sexes, crossbred and of different ages. Dogs had moderate sedation and were infected in experiments with about 50 adult ticks and malnourished compared to male or female, after 15 minutes, it was found that at least 50% of the parasites were fixed on the animal.

The canines were randomly divided into three groups of 10 animals each, in 48 hours were assigned the following treatments:

Group "a": were treated with a plastic collar injected with 10% propoxur g, and 4g% deltamethrin, Ig% ethyl acetyl butyl aminopropionate.

Group "b": were treated with a plastic collar injected with 4% deltamethrin.

Group "c": were treated with a plastic necklace

no insecticide (control).

The animals were kept in individual kennels, being fed with balanced feed and water. The treated groups did not maintain contact with others at any time during the study. The first evaluation was performed within 48 hours after product application. Each animal was re-infested with 50 adult and malnourished ticks in relation to male and female (1: 1) on days 7,15,30,60,90,120,180,195 and 210, the effect of acaricide was measured as a percentage of efficiency. and calculated at 9 days, 17,32,62,92,122,152,182,197 and 212. The efficacy observed within 48 hours after application exceeded 90% in group "a" and did not reach 65% in group "b"; in group "a", efficacy was observed between 17 and 182 and remained between 90% and 94% at 197 days, efficacy was 86%.

In the plastic collar was impregnated with 10% propoxur g, 4 g of acetyl ethyl butyl deltramethrin, infestation and re-infestation aminopropionate Ig in tick controls (Rhipicephalus blood); Efficacy rates were achieved over a period of time containing 4 g of deltamethrin.

3- The effect of anti-feeding and mortality of the collar with 10% injected propaxur g, deltamethrin 4 g, acetyl ethyl butyl g, aminopropionate and against leishmanniosis phlebotomines in dogs exposed under laboratory conditions.

The aim of the experimental test was to evaluate the effect of anti-pitting, anti-feeding and mortality of a 10% insecticide-injected collar, deltamethrin propuxur g, and 4 g acetyl ethyl butyl, 1 g aminopropionate against the sandflies for 36 weeks. They were used in 20 dogs of both sexes, mongrel and of different ages. In ten (10) cholera the insecticide was applied by injecting 10% propuxuron deltammetry, and 4 g acetyl ethyl butyl, 1 g aminopropionate. In the other animals were equipped with a collar without any active ingredient. The animals were exposed in individual nests of 1.8 meters and 1.2 square meters with gauze and cotton made at the bottom of the sides.

The employee is accounted for the Lutzonia longipalpis mosquito. The frequency of observation was 24.48,72 and 96 hours, and at 4 weeks, 8,12,16,20,24,30 and 36, thirty minutes before each observation, 130 to 150 females were placed in each nest. 30 males from 7 to 20 days old. He then introduced a sedated dog to each nest and kept it for two hours. After this time, the dogs were removed from the nest and brushed to collect dead insects in the mantle. Dead insects found on the nest floor were collected with a brush and placed in a suitable container, identified by the animal number.

Living insects were collected by aspiration and kept in a suitable container, identified by the animal number. At 2 and 20 hours from the beginning of each test, live and dead females were counted and classified, males and females were not fed. The Anti-feeding effect was obtained and compared with the results between dogs treated by dividing the mean difference and between the insects fed on control animals and those treated by the average number of insects that fed on the animals.

In animals treated for a period of 36 weeks, only 30% of female Lutzomia longpalpis had been fed in the nest. The anti-feeding were 97%. Mortality at four weeks reached 95% and at week 65% to 36%.

4- The effect of anti-pitting-benchmarking and mortality of the insecticide collar injected with 10% deltamethrin propoxur g, and 4 g acetyl ethyl butyl g% aminopropionate 1 versus injected deltamethrin insecticide collar, 4 phlebotomine ventors of leshmaniosis in dogs exposed under laboratory conditions.

The purpose of the experimental test was to evaluate the anti-sting, anti-feed effect, mortality of a propoxur insecticide on the injected collar with 10%, 4% deltametry g, and acetyl ethyl butyl g, aminopropionate 1 and the other injected ones. with 4 g% deltamethrin against phlebotomine leishmaniasis ventilators in dogs exposed under laboratory conditions for 36 weeks.

Thirty crossbreed dogs of both sexes of different ages were used, each group constituting 10 animals for treatment. Treatment "A": 10% collar injected with insecitated deltamethrin propuxor g, and 4 g of acetyl ethyl butyl aminopropionate 1 g; Treatment "B": 4 g% injected deltamethrin insecticide on the collar and Treatment "C": a necklace with no active ingredient. The animals were exposed in individual nests of 1.8 meters and 1.2 square meters with gauze and cotton made at the bottom and sides. The Lutzonia longipalpis mosquito was counted, the observation frequency was 24.48,72 and 96 hours, and at 4 weeks, 8,12,16,20,24,30 and 36, thirty minutes before each observation was placed in each nest 130-15 females and 30 males from 7 to 20 days old then he introduced a sedated dog to each nest and remained for two hours after this time the dogs were removed from the nest and were brushed to order to collect a dead insect in the cloak. The dead insects were found on the nest floor and was collected with a brush placed them in a suitable container, identified by the animal number.

Living insects were collected by aspiration and kept in a suitable container, identified by the animal number. At 2 and 20 hours from the beginning of each test, the fed and live and dead females were counted and classified. The anti-feeding effect was obtained by comparing the results between controls and dogs treated by dividing the mean difference between insects fed on control animals and those treated by the average number of insects that feed on control animals. In Treatment "A": Over a 36-week period, only 2.0% of female Lutzomia longipalpis recovered in fed nests.

Anti-feeding was 98%, mortality at four weeks reached 97% and at 68 weeks 36%. In Treatment "B": Over a 36-week period, 9.0% female longipalpis lutzomia recovered in the nest, they had been fed. Anti-feeding was 91%, mortality at 4 weeks 92% and 42 weeks at 36%.

5- The anti-sting effect and anti-feeding of collar mortality were injected with 10% propoxur g insecticide, deltamethrin, 4 g acetyl ethyl butyl and aminopropionate 1 versus 4 g deltamethrin insecticide, clulex pipiens the mosquito canine heartworm transmitters in 8 (eight) months.

The objective of the experimental test was to evaluate the effect of anti-capping and anti-feeding the mortality of two collars with insecticides against the mosquito culex pipiens and the transmission of canine heartworm.

Treatment is a cholera with 10% injected insecticide propoxur g, deltamethrin, 4 g acetyl-ethyl-buitl aminipropionate, 1 g, in the collar for the treatment of insecticide deltamethrin B containing 4 g are the animals that are part of the treatment. "C", where a plastic collar was placed without repellent or insecticides, were used in 30 dogs of both sexes, crossbred of different ages, 10 (three) animals were treated with anti-capping and anti-feeding. mortality rates were measured from 24 to 48 hours per week, in a week of 2,4,8,12,16,20,24,28 and 32.

In each dog sedated for 90 minutes, they were exposed to 50 laboratory-fed culex pipiens females without food and in a custom net, after which time the animal was removed from the net and they were brushed to collect dead insects on the mantle. . Dead insects found on the nest floor were taken and placed in a suitable container and identified by the animal number, live insects were collected by aspiration and kept in an appropriate container and identified by the number of animals fed with water and honey.

The effect of anti-feeding was observed between 24 and 48 hours, were counted and classified fed, live and dead females, not fed, alive and dead females. The anti-feeding effect was obtained by calculating the ratio of the difference between the anti-feeding rate in the treated animals and divided by the difference between the anti-feeding rate in the animals. Mortality was obtained by calculating from the ratio of the difference in the mortality rate in treated dogs and the mortality rate in the control animals, was the anti-feeding effect.

Treatment "A": 98 and 100% over 32 weeks; Treatment "B": 92 and 97% for the first 28 weeks and 89% to 32 weeks, Treatment A: 85 and 96% for 28 weeks, 92% for 32 weeks, Treatment "B": 63 and 85% for 28 weeks, 70% to 32 weeks.

The guarantees provided for both anti-feed and anti-bite mortality of the canine heartworm transmitter culex pipiens mosquito were obtained through the use of a 10% g insecticide collar injected with propoxur, deltamethrin, 4% ethyl, butyl and 1 % aminopropionate, from those found in the deltamethrin insecticide and injected with 4 g% during the 32 weeks of the trial.

Thus one of the possibilities leading to the embodiment of the invention and its operation has been summarized, all of which complements the synthesis of the invention contained in the appending clauses.

5.- CONCLUSION

From all that has been described and illustrated, this is a Pesticide Controlled Release Composition System containing Deltamethrin, Propoxur and Insect Repellent, which fills an important gap in the market and fits within the standards. governing the Invention Patent, deserving for the foregoing and as a consequence, the respective privilege.

Claims (13)

1. A PESTICIDES CONTROLLED RELEASE COMPOSITION SYSTEM CONTAINING DELTAMETRINE, PROPOXUR AND INSECT REPELLENT ". (1) characterized in that it is composed of triphenyl phosphate deltamethrin, propuxur, butylacetylamino propylate in phosphatyl and a phenyl defenyl ratio This composition acts as an insecticide to repel and control fleas and ticks, as well as phlebotomine vectors, leishmaniasis and heartworm mosquito vectors. 2. A pesticide controlled composition system wherein the composition contains PVC5 ethyl butylacetylamino propionate resin, deltamethrin, propoxur, flalate isoctyl, cresyl diphenyl phosphate, triphenyl phosphate. A system according to claim (1) wherein the polyvinyl chloride polymer matrix is injected into cholera and other devices of similar use. A system according to claim (1) wherein the polyvinyl chloride in a concentration of 40 - 50%. A system according to claim (1) wherein Propoxur is in a concentration of 5 to 20%. A system according to claim (1) wherein the Pyrethroid is at a concentration of 1 to 10%. A system according to claim (1) comprising the pyrethroid and deltamethrin. A system according to claim (1) wherein the repellent is in a concentration of 0.1 to 5%. A system according to claim (1) wherein the repellent is ethyl butylacetylamino propionate. 10 A system according to claim (1) wherein isoctyl phthalate is at a concentration of 5 to 15%. -11. A system according to claim (1) wherein the triphenyl phosphate is in a concentration of 5 to 30%. -12. A system according to claim (1) wherein the diphenyl cresyl phosphate is in a concentration of 5 to 30%. -13. A pesticide controlled release composition system comprising deltamethrin, propoxur, butylacetamino triphenyl phosphate propionate, ethyl phosphate and cresyl diphenyl in a suitable ratio. This composition acts as an insecticide to control and repel fleas, ticks, vectors of sand flies, leishmaniasis and mosquitoes, as well as heartworm. The quantities of diphenyl and cresyl trefenyl phosphates are sufficient to serve as a vehicle for the active substances.