MXPA99001095A - Pesticidal composition and method of use - Google Patents

Pesticidal composition and method of use

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Publication number
MXPA99001095A
MXPA99001095A MXPA/A/1999/001095A MX9901095A MXPA99001095A MX PA99001095 A MXPA99001095 A MX PA99001095A MX 9901095 A MX9901095 A MX 9901095A MX PA99001095 A MXPA99001095 A MX PA99001095A
Authority
MX
Mexico
Prior art keywords
citronellil
composition
agent
pesticidal
parasiticidal
Prior art date
Application number
MXPA/A/1999/001095A
Other languages
Spanish (es)
Inventor
R Burklow Eddie
S Kiel Jeffrey
Original Assignee
Effcon Inc
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Filing date
Publication date
Application filed by Effcon Inc filed Critical Effcon Inc
Publication of MXPA99001095A publication Critical patent/MXPA99001095A/en

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Abstract

The present invention provides a pesticidal composition with an extraordinarily lethal effectiveness that can also be used to remove and repel parasite, such as lice. The pesticidal composition preferably contains a cleansing agent and a pesticidal agent such as citronellal, citronellol, citronellyl or a mixture thereof. The composition more preferably utilizes citronellyl acetate as the pesticidal agent. The compositions can be administered topically to humans, animals or any infested areas.

Description

PESTICIDE COMPOSITION AND METHOD FOR. ITS USE CROSS REFERENCE WITH A RELATED APPLICATION This application claims the priority of United States Provisional Patent Application No. 60 / 022,377, filed July 29, 1996.
FIELD OF THE INVENTION The present invention relates to parasiticides or pesticides. In particular, the invention relates to parasiticidal or pesticidal compositions for cleaning infested individuals and for repelling future parasites.
BACKGROUND OF THE INVENTION [0002] Parasiticides or pesticides and insect repellents have long been sought for use against harmful or annoying parasites. Pests or parasites such as lice and fleas are irritating and painful to their human and animal hosts and can also be vectors of other disease agents. However, parasiticides and repellents available from the prior art suffer from several deficiencies. Frequently, compositions provided as insect repellents are not P1109 / -. 9MX insecticides. In addition, many compositions are either toxic or generally unpleasant to the host. Others even require many separate active ingredients for efficient production and regulation. Many synthetic compositions of the prior art have been proposed as insect repellents but have subsequently been determined to be unsuitable for safe use in humans. A common active ingredient in the above commercial compositions is N, N-diethyl-m-toluamide (DEET). However, DEET has recently been associated with the provocation of various undesirable side effects, such as itching, damage to the mucous membranes and possibly attacks. In 1989, the Centers for Disease Control issued a precautionary statement regarding the use of DEET. Many other compounds of the prior art proposed to be used as repellents have been shown to be unsuitable for topical application in humans or other animals due to their toxic or harmful effect on the infested individual. Various crude oil extracts from certain plants, such as citronella oil obtained from Cymbopogon ci trata, or eucalyptus oil obtained from Eucalyptus citriodora, have been provided in the prior art, as parasite repellents. Without P1109 / 99 However, the same complex oil is greasy and may have an unpleasant odor, which makes its use undesirable. In addition, the consistent production of a safe and effective product is difficult, due to the variable amounts of the constituent compounds within the batches of these complex oils and the difficulty in monitoring a large number of components. Therefore, insect repellents containing citronella integral oil, for example, are undesirable due to their limited repellency, their unpleasant odor and consistency, and an unreliable composition of unnecessary and potentially harmful agents. Most insect repellents of the prior art have taught that they are effective only in specific synergistic compositions. In the art, a simple but effective parasiticidal or pesticidal composition that does not require the combination of an excess of multiple parasiticidal ingredients or pesticides has not been recognized. So far, no parasiticide or pesticide has been provided in a simple but effective composition that is acceptable for human use. What is needed in the art is an especially effective pesticidal composition with a lower number of active components that is easier to produce consistently as well as to monitor. The P1109 / 99MX composition should also be able to cleanse the individual who will be treated for infestation. Therefore, it is an object of the present invention to provide a pesticide that is deadly effective against parasites such as lice. It is an additional object to provide a composition that can be used as a shampoo, soap, cream, lotion or spray cleaner. These as well as other objects of the invention will be apparent to those skilled in the art.
SUMMARY OF THE INVENTION The present invention provides a parasiticidal or pesticidal composition with an extremely lethal effectiveness, which can also be used to eliminate and repel parasites, such as lice, from an individual host. The pesticidal composition preferably contains a cleaning agent and a parasiticidal or pesticidal agent such as citronellal, citronellol or citronellil. The pesticidal compositions more preferably comprise a citronellil salt and a cleansing agent. The compositions may be administered topically to humans, animals or any infested areas.
P1109 / 99MX DETAILED DESCRIPTION OF THE INVENTION A "pest", according to the term "parasiticide or pesticide", is intended to include all parasites, such as, for example, arthropods, arachnids, triatomines, insects, bedbugs, flies, lice, fleas, mites, gnat, nits, chagas or trypanosomes, mosquitoes and ticks. Therefore, it is intended that the composition of the present invention be used against all parasites that succumb to the lethal properties thereof. The present invention provides a pesticidal composition comprising a cleaning agent and a parasiticidal or pesticidal agent comprising citronellal, citronellol or citronellil in a concentration of at least about 8% by volume. Citronellal, citronellol and citronellil are available from Élan (Newark, NJ). In the preferred embodiments, the pesticidal agent used is citronellil. In the most preferred embodiments, citronellil is a salt selected from the group consisting of acetate, butyrate, formate, isobutyrate, phenylacetate, propionate and valerate. In a more preferred embodiment, the citronellil salt is acetate. The pesticidal compositions of the invention that P1109 / 99 X contain concentrations of citronellal, citronellol or citronellil greater than 0.75% by volume or v / v, show parasiticidal or pesticidal activity. As the concentration of the pesticidal agent increases, the deadly or lethal effectiveness of the composition also increases, as determined by the parasiticidal and ovicidal data. The unexpected and increasingly lethal effectiveness of the invention is demonstrated at concentrations of 5%, 7.5%, 8%, 8.5%, 9%, 9.5%, 10%, 10.5%, 11%, 11.5%, 12%, 12.5%, 13%, 13.5%, 14%, 14.5% and 15% v / v. The invention preferably provides a pesticidal composition, wherein the parasiticidal or pesticidal agent, for example, citronellil, is in a concentration of between about 8% and 25% v / v, more preferably, between about 8% and 15% v / vy, with the greatest preference, of approximately 12.5% v / v. The invention stipulates that the composition contains a cleaning agent to aid in the elimination of undesirable parasites and residues. By cleansing agent, reference is made to a composition capable of sequestering or chelating the waste or of breaking the hydrophobic suspensions, for example, in order to help the elimination of parasites and eggs. Many well-known cleaning agents can be used. The cleaning agent can be a detergent. The detergent P1109 / 99MX can be an aqueous detergent such as Steol CS-230 (also known as Sodium Laureth Sulfate) that can be obtained from Stepan (Northfield, IL) or non-aqueous detergent Cedepal HC (also known as Sodium Lauryl Sulfate) which can also be obtained from Stepan (Northfield, IL). The pesticidal composition of the invention may further comprise an alcohol. Preferred alcohols include isopropanol and ethanol but can be substituted by others. It is considered that the presence of an alcohol in the composition increases the parasiticidal effectiveness of the composition by making it permeable to the outer membrane of the parasite eggs, thereby allowing the pesticidal agent to penetrate the outer membrane of the eggs. Functional substitutes that achieve the same result can substitute alcohol without deviating from the scope and spirit of the claims. The pesticide composition can, for example, additionally include a transport agent or excipient, an antimicrobial agent or a pH modifier. In a preferred embodiment, the pesticidal composition comprises a paraben as an antimicrobial agent, an acid as a pH modifier and as a cleaning agent and water. Preferred parabens are methyl paraben and propyl paraben but can be substituted by others. The acid P1109 / 99MX d Acetic is the preferred acid but can be replaced by others. In the preferred embodiment, the pesticidal composition further comprises from about 1 to 40% w / v of isopropyl alcohol, from 0.01 to 5% w / v w / v methyl paraben, from 0.01 to 5% w / v of propil paraben, from 0.01 to 10% w / v of acetic acid, from 30 to 60% v / v of detergent and water when enough for 100 g. The pesticidal composition more preferably comprises about 20% w / v isopropyl alcohol, 0.2% w / v methyl paraben, 0.1% w / v propyl paraben, 5.0% w / v acetic acid, 55.5% v / v detergent and water enough for 100 g. The pesticidal composition may further include a viscosity modifier or an antipruritic agent, for example, in a preferred embodiment, the parasiticidal or pesticidal composition further comprises camphor as an antipruritic agent, sodium chloride as a viscosity modifier, methyl paraben and / or propyl. paraben as an antimicrobial agent, acetic acid as a pH modifier and as a cleaning agent and water. In a preferred embodiment, the pesticidal composition further comprises about 0.01 to 5% w / v of camphor and 1 to 10% w / v of sodium chloride. The pesticidal composition may comprise about 0.75% w / v of camphor, 4.87% w / v of sodium chloride, 0.2% w / v of methyl paraben, 0.1% w / v of propyl P1109 / 99 X paraben, 5.7% w / v acetic acid, 35.14% v / v detergent and water as long as it is sufficient for 100 g. The pesticidal composition may additionally take the form of a non-aqueous composition. In one embodiment, the pesticidal composition comprises a pesticidal agent, an alcohol, a pH modifier, a detergent, an antimicrobial agent, a non-aqueous solvent and a detergent. In a preferred embodiment, the pesticidal composition further comprises citronellil as a pesticidal agent, isopropanol as an alcohol, acetic acid as a pH modifier and cleaning agent, methyl paraben as an antimicrobial agent, propyl paraben as an antimicrobial agent, propylene glycol as a solvent, glycerin as a solvent and Cedepal HC as non-aqueous detergent. In a more preferred embodiment, the pesticidal composition further comprises about 12.55 citronellil acetate, 20% isopropanol, 5% acetic acid, 0.2% methyl paraben, 0.1% propyl paraben, 20% propylene glycol, 15% Cedepal HC and the sufficient amount of glycerin. The pesticidal composition can furthermore take the form of a two component system. In the two-component system, the two components are prepared and stored separately and then mixed at the point of use. The "Active Ingredient Component" P1109 / 99MX comprises an alcohol, a pesticidal agent, an antimicrobial agent and a detergent. The "Diluent Component" comprises a pH modifier and an antimicrobial agent. In the preferred embodiment, the "Active Ingredient Component" further comprises isopropanol as alcohol, citronellil acetate as a pesticidal agent, methyl paraben as an antimicrobial agent, propyl paraben as an antimicrobial agent and Steol CS-230 as a detergent, and the "Diluent Component" comprises in addition glacial acetic acid as a pH modifier and as a cleaning agent, methyl paraben as an antimicrobial agent, propyl paraben as an antimicrobial agent and water as a diluent. In the preferred embodiment, the "Active Ingredient Component" further comprises 14.15% w / v citronellil acetate, 22.64% w / v isopropanol, 0.2% w / v methyl paraben, 0.1% w / v propyl paraben, and 62.83 % w / v of Steol CS-230, and the "Diluent Component" further comprises 42.86% w / v of glacial acetic acid, 0.2% w / v of methyl paraben, 0.1% w / v of propyl paraben and the necessary amount of Water. In this preferred embodiment, the "diluent component comprises approximately 11 2/3% of the combined final product.The final product combined in this most preferred embodiment comprises 12.5% w / v citronellyl acetate, 20% w / v isopropanol, 0.2 % w / v of methyl paraben, 0.1% w / v of propyl paraben, 55.5% w / v of Steol CS-230, 5% w / v of acetic acid P1109 / 99MX and the required amount of water. Therefore, the "Active Ingredient Component" and the "Diluent Component" are combined in a ratio of about 7.5 to 1. One skilled in the art can routinely modify the relative concentrations of these components and, in accordance with the above , its combination ratio to produce a functional pesticidal composition. According to the inventor's knowledge, previously there has been no recognition of the parasiticidal or pesticidal effectiveness of a citronellil as demonstrated herein. The invention stipulates that citronellal and citronellol also possess a surprising degree of pesticidal effectiveness. Therefore, the invention contemplates that any of citronellal and citronellol may be the substituents of citronellil or, added to the pesticidal agent of the composition. Without being limited by theory, it is believed that the composition of the present invention is surprisingly effective due to the purification of the individual components. Citronella oil is a complex mixture containing components that ordinarily can mask the potential effectiveness of the individual pesticidal agents citronellil, citronellol and citronellal, as disclosed by the present invention. It also turns out that in the P-.109 / 99MX compositions of the present invention achieve a beneficial synergistic effect. The invention also provides a method for treating an individual that is infested with parasites and which comprises administering to the infested an insecticidal composition as described above. In particular, the composition of the present invention is effective as an insecticide that is intended to kill and eliminate lice from humans. Various treatment regimens that are within the treatment method provided by this invention are contemplated. Treatment regimens can vary from a single administration to repeated administrations over long periods of time. The various possible treatment regimens would be apparent to one skilled in the art, based on the invention disclosed herein and intended to be encompassed or included in the scope and spirit of the claims. It is intended that the present invention be administered topically to the infested areas of an individual, such as hair and scalp or pubic areas. The composition is preferably provided in liquid or solid form, such as a shampoo, a soap, a cream or a lotion. The invention contemplates that various other P1109 / 99MX supplemental ingredients, such as, may be, an antipruritic agent, a pH modifier or as a general medium. For example, glycerins, glycols, alcohols, lanolins, aloe vera gel can be supplied in the composition. The preferred compositions are shampoos and soaps containing ingredients that have the ability to help cleanse individuals of the remains of dead parasites. The composition can also be supplied in sunscreens, bronzers or in any other topically applicable products. Other uses of the composition are contemplated, such as a pesticide spray or a pesticide nebulizer to apply directly to pests or parasites or potentially infested areas. For example, the composition can be provided as a pesticidal agent and cleaner for fruits and vegetables. The composition can additionally serve as a repellent for cats, dogs, birds, cattle or sheep, for example. The composition can also be used as a powder for carpets or as an additive for detergents, rinses or rubbers for garments, bedding or other goods. The composition can also be used as an aerosol pump or as a spray for rooms. Other uses will be apparent to someone experienced in the art after P1109 / 99MX to contemplate the invention disclosed herein and it is intended that said uses be included in the scope and spirit of the claims.
EXAMPLES EXAMPLE I Method for Testing the Pediculicidal Activity of a Composition To determine the pediculicidal activity of various compositions of the invention, "The Standard Test Method for Effectiveness of Liquid, Gel, or Cream Insecticides Against Adult Human Lice" was used. Normal to Determine the Effectiveness of Liquid, Gel or Cream Insecticides Against Lice in * Human Adults "). The protocol of the test has been published by the American Society for Testing and Materials according to the designation E938-83 (which was approved again in 1988) and which is incorporated herein by reference. Briefly, the test is conducted as follows. Twenty-five (25) adult lice were placed in a vial that has a mesh bottom. The vial was placed in the container of the composition to be tested, which was maintained at a temperature of 32 ° C. In the upper part of the vial containing the lice a plunger with mesh was inserted to ensure that the lice were not P1109 / 99MX float to the surface. The lice were then submerged in the test composition for a set of several minutes (1, 4 or 10). The vial containing the lice was then immersed in distilled water maintained at a temperature of 32 ° C and stirred gently for one minute. The lice were washed gently by means of a stream of distilled water at 32 ° C. The excess water was removed by drying with blotting paper. The lice were then placed in a dark patch and incubated at 31.7 ° C and 60% RH. At one and twenty-four hours after the treatment, the lice were tested to determine if they moved toward a 37 ° C patch. The undead, morbid or dying lice will move towards the 37 ° C patch. By the term "morbid" reference is made to a louse which is unable to move towards heat after one hour of treatment. The louse is sick but not necessarily agonizing. A "morbid" louse can recover 24 hours after treatment. By the term "moribund" reference is made to a louse unable to move towards heat twenty-four hours after treatment; the louse is dead or dying. Those lice that died or were dying within twenty-four hours were counted as casualties or deaths. The mortality percentages were corrected P1109 / 99 X by the Abbott Formula. The percentage of mortality of a control was subtracted from the percent mortality of the test and then divided by the percentage of test mortality.
EXAMPLE II Method for Testing the Ovicide Activity of a Composition To determine the ovicidal activity of various compositions of the invention, the "Standard Test Method for Determining the Effectiveness of Liquid, Gel, Cream, or Shampoo Insecticides Against Human Louse OVA" was used. Normal Test Method to Determine the Effectiveness of Liquid, Gel, Cream or Shampoo Insecticides Against Human Louse Eggs "). This protocol was published by the American Society for Testing and Materials under the designation E5117-93 and is incorporated herein by reference. Briefly, each test was conducted as follows. Thirty human louse eggs attached to cuts of human hair were used for each test condition. The human hair clippings were fixed to a wooden applicator bar and then immersed in the composition to be tested for ten minutes. The test composition was maintained at 32 ° C. The eggs were washed then vigorously moving the bar towards P1109 / 99MX up and down in tap water at 32 ° C for one minute. A wash bottle was then used to further wash the eggs with tap water at 32 ° C during an additional minute. The eggs were then incubated until all eggs exposed to control conditions developed (approximately 12 days). Then the development of all the eggs was observed. Eggs that could not be incubated were recorded as deaths. The mortality percentages were corrected by the Abbott Formula. The percentage of mortality of a control was subtracted from the percentage of mortality of the test and then divided by the percentage of mortality of the test.
EXAMPLE III Production of Pesticide Compositions Utilizing Citronelal, Citronellol and Citronellil The following components were combined in approximate relative amounts to prepare Formulas A-C. citronellyl acetate Formula A 0.75% v / v Formula B 0.0% v / v Formula C 0.0% v / v P1109 / 99MX citronelal Formula A 0.0% v / v Formula B 0.75% v / v Formula C 0.0% v / v citronellol Formula A 0.0% v / v Formula B 0.0% v / v Formula C 0.75% v / v synthetic camphor 0.75 % w / v sodium chloride 4.87% w / v methyl paraben 0.2% w / v propyl paraben 0.1% w / v acetic acid 5.7% v / v Steol CS-230 36.55% v / v purified water enough for all the steps of mixing described here were performed with a mixer - air driven and explosion-proof. The acetic acid was transferred to a mixing vessel. Citronellyl acetate and camphor were added separately, each was mixed until completely uniform. The Steol CS-230 detergent was transferred to a second mixing vessel. While mixing, the acetic acid phase was added to the detergent and mixed thoroughly. In a third vessel, the sodium chloride dissolved in water Purified P1109 / 99MX. This solution was then transferred to the second mixing vessel and mixed thoroughly. The methyl paraben and the propyl paraben were then added while mixing. The final product was emptied through a polished filter. The compositions produced by Formulas A-C demonstrated only a slight ovicidal activity when the ovicidal activity was tested as described in Example II. The compositions produced by Formulas A-C exhibited 0.3%, 3.4% and 1.2% ovicidal activity, respectively.
EXAMPLE IV Production of Pesticide Compositions Containing Citronellal The following components were combined in the approximate relative amounts to prepare Formulas A-F. Citronelal Formula A 0.75% v / v Formula B 2.5% v / v Formula C 5.0% v / v Formula D 7.5% v / v Formula E 10.0% v / v Formula F 12.5% v / v P1109 / 99MX Synthetic Camphor 0.75% w / v Sodium Chloride 4.87% w / v Meth paraben 0.2% w / v Propil paraben 0.1% w / v Acetic Acid 3.65% v / v Steol CS-230 36.55% v / v Purified Water how much is enough for all the mixing steps described here were done with an explosion-proof air-driven mixer. The acetic acid was transferred to a mixing vessel. Citronellal and camphor were added separately, each was mixed until completely uniform. The Steol CS-230 detergent was transferred to a second mixing vessel. While mixing, the acetic acid phase was added to the detergent and mixed thoroughly. In a third vessel, the sodium chloride was dissolved in purified water. This solution was then transferred to the second mixing vessel and mixed thoroughly. The methyl paraben and the propyl paraben were then added while mixing. The final product was emptied through a polished filter. To the compositions produced by the Formulas E and F were tested for ovicidal activity as described in Example II. The composition produced by P1109 / 99MX Formula E showed 3.5% ovicidal activity and the composition produced by Formula F showed 0.0% ovicidal activity. In the compositions produced by the Formulas A-E their pediculicidal activity was tested as described in Example I. They demonstrated pediculicidal activities of 1.5%, 15.7%, 10.9%, 17% and 100%, respectively.
EXAMPLE V Production of Pesticide Compositions Containing Citronellil The following components were combined in the approximate relative amounts to prepare Formulas A-C. Citronellil Acetate Formula A 8.9% v / v Formula B 10.0% v / v Formula C 12.5% v / v Synthetic Camphor 0.75% w / v Sodium Chloride 4.87% w / v Meth paraben 0.2% w / v Propil paraben 0.1% w / v Acetic Acid Formula A 3.65% v / v - Formula B 3.65% v / v P1109 / 99MX Formula C 5.0% v / v Steol CS-230 36.55% v / v Purified Water as Sufficient for All the mixing steps described here were performed with an explosion-proof air-driven mixer. The acetic acid was transferred to a mixing vessel. Citronellil and camphor were added separately, each was mixed until completely uniform. The Steol CS-230 detergent was transferred to a second mixing vessel. While mixing, the acetic acid phase was added to the detergent and mixed thoroughly. In a third vessel, the sodium chloride was dissolved in purified water. This solution was then transferred to the second mixing vessel and mixed thoroughly. The methyl paraben and the propyl paraben were then added while mixing. The final product was emptied through a polished filter. The compositions produced by Formulas B and C were tested for their ovicidal activity as described in Example II. The compositions produced by both Formulas showed 0.0% ovicidal activity. The compositions produced by the Formulas A-C were tested for their pediculicidal activity as described in Example I. These demonstrated pediculicidal activities of the P1109 / 99MX 97. 0%, 100 0% and 100 0%, respectively.
EXAMPLE VI Production of Pesticide Compositions Containing an Alcohol The following components were combined in the approximate relative amounts to produce a pesticidal composition containing an alcohol. Citronellil Acetate 12.5% v / v Synthetic Camphor 0.75% w / v Acetic Acid 6.0% v / v Alcohol Isopropanol Formula A 0.0% v / v Formula B 0.0% v / v Formula C 20.0% v / v Formula D 30.0% v / v Ethanol Formula A 20.0% v / v Formula B 30.0% v / v Formula C 0.0% v / v Formula D 0.0% v / v Steol CS-230 46.0% v / v Methyl paraben 0.2% w / v Propil paraben 0.1 % w / v P1109 / 99MX Purified Water how much is enough for The alcohol was transferred to a mixing vessel. The camphor was added to this vessel and mixed until completely dissolved. The methyl paraben and the propyl paraben were then added and mixed until completely dissolved. The citronellil acetate was added and mixed until completely uniform. Acetic acid was added to the container and mixed until completely uniform. Steol CS-230 was added and mixed until completely uniform. Sufficient water was then added to bring the composition to its target weight. The compositions produced by Formulas A-D demonstrated high levels of ovicidal activity when tested in accordance with the protocol described in Example II. The compositions produced by Formulas A-C showed 100.0% ovicidal activity and the composition produced by Formula D showed 99.3% ovicidal activity.
EXAMPLE VII Production of Pesticide Compositions Containing Citronellol The following components were combined in the approximate relative amounts in accordance with the P1109 / 99MX Formulas A and B for producing pesticidal compositions containing citronellol. Citronelol 12.5% v / v Alcohol Isopropanol Formula A 0.0% v / v Formula B 20.0% v / v Ethanol Formula A 20.0% v / v Formula B 0.0% v / v Synthetic Camphor 0.75% w / v Meth paraben 0.2% w / v Propil paraben 0.1% w / v Acetic Acid 6.0% v / v Steol CS-230 46.0% v / v Purified Water as long as enough for The alcohol was transferred to a mixing vessel. The camphor was added to this vessel and mixed until completely dissolved. The methyl paraben and the propyl paraben were then added and mixed until completely dissolved. Citronellol was added and mixed until complete uniformity. The acetic acid was added to the vessel and mixed until completely uniform. The Steol CS-230 was added and mixed until it was P1109 / 99MX completely uniform. Sufficient water was then added to bring the composition to its target weight. The compositions produced by Formulas A and B showed 100.0% ovicidal activity.
EXAMPLE VI I Production of Non-Aqueous Pesticide Compositions The following ingredients were combined in the approximate relative amounts to produce a non-aqueous pesticidal composition. Citronellil acetate 12.5% v / v Isopropanol 20.0% v / v Acetic acid 5.0% v / v Propylene glycol 20.0% v / v Methyl paraben 0.2% w / v Propil paraben 0.1% w / v Cedepal HC 15.0% v / v Glycerin how much Sufficient for the methyl paraben and the propyl paraben were dissolved in the isopropanol in a mixing vessel. The citronellil acetate was added to this vessel and mixed until completely uniform. The acetic acid was then added and mixed until completely uniform. Next, the Cedepal HC was added to the container and mixed until it was completely P1109 / 99MX uniform. The propylene glycol was then added and mixed until completely uniform. Finally, the glycerin was added to bring the mixture to its target weight. This composition demonstrated 13.0% ovicidal activity when tested according to the procedure of Example II.
EXAMPLE IX Production of a Non-Aqueous Pesticide Composition with a Conditioning Base The following ingredients were combined in the approximate relative amounts to produce a non-aqueous cream rinse formulation. Citronellil acetate 12.5% v / v Isopropanol 20.0% v / v Acetic acid 5.0% v / v Methyl paraben 0.2% w / v Propil paraben 0.1% w / v Amidox L-5 4.0% v / v Ammonyx 4002 8.4% v / v Cedepal HC enough for Ammonyx 4002, a conditioner obtainable from Stepan (Northfield, IL) and the methyl paraben and propyl paraben were completely dissolved in the isopropanol in a mixing vessel. The acetate P1109 / 99MX citronellil was added to the vessel and mixed until completely uniform. Next, the Amidox L-5, a foaming agent obtained from Stepan (Northfield, IL), was dissolved in the mixture. Finally, Cedepal HC was added to bring the mixture to its target weight and mixed until uniform. This pesticidal composition exhibited an ovicidal activity of 12.0% when tested according to the procedure of Example II.
EXAMPLE X Production of a Two-Component Pesticide Composition The compositions that were aqueous and contained higher levels of acetic acid (approximately 5%) exhibited a high ovicidal activity. However, citronellil acetate degraded over time in the compositions containing acetic acid and water. Therefore, two-component pesticidal compositions were developed. Each component of the compositions was produced and stored separately. The two components were mixed at the point of use. The first component was a "Active Ingredient Component" and the second component was a "Diluent Component". One of these two component pesticidal compositions was prepared in the following manner.
P1109 / 99MX The following ingredients were combined in the approximate relative amounts to prepare the "Active Ingredient Component". Citronellil acetate 14.15% v / v Isopropanol 22.64% v / v Methyl paraben 0.2% w / v Propil paraben 0.1% w / v Steol CS-230 62.91% v / v Isopropanol, methyl paraben and propyl paraben were mixed in a mixing vessel until the parabens completely dissolved. The resulting isopropanol / paraben solution was transferred to a second mixing vessel. Steol CS-230 was added to the second mixing vessel and mixed until completely uniform. Citronellil acetate was added to this vessel and mixed until uniform. The resulting solution was diluted to its final target weight by the addition of Steol CS-230. The following ingredients were combined in the approximate relative amounts to produce the "Component. Diluent". One of these two component pesticidal compositions was prepared in the following manner. The following ingredients were combined in the approximate relative amounts to prepare the P1109 / 99MX component "Active Ingredient". Citronellil acetate 14.15% v / v Isopropanol 22.64% v / v Methyl paraben 0.2% w / v Propil paraben 0.1% w / v Steol CS-230 62.91% v / v Isopropanol, methyl paraben and propyl paraben were mixed in a mixing vessel until the parabens completely dissolved. The resulting isopropanol / paraben solution was transferred to a second mixing vessel. Steol CS-230 was added to the second mixing vessel and mixed until completely uniform. Citronellil acetate was added to this vessel and mixed until uniform. The resulting solution was diluted to its final target weight by the addition of Steol CS-230. The following ingredients were combined in the approximate relative amounts to produce the "Diluent Component" Glacial Acetic Acid 42.86% v / v Methyl paraben 0.2% w / v Propyl paraben 0.1% w / v Purified Water as long as it is sufficient for the specified amount of purified water was added to a mixing vessel. Acid was added P1109 / 99MX glacial acetic acid to the mixing vessel and mixed until completely uniform. The methyl paraben and the propyl paraben were added to the mixing vessel and mixed until completely dissolved. The resulting solution was diluted to the final objective weight with purified water. The two components were mixed at the point of use in the relative amounts such that the "Diluent Component" comprised approximately 11 2/3% of the final combined product. The final product contained the following ingredients in the approximate relative amounts listed below. Citronellil acetate 12.5% v / v Isopropanol 20.0% v / v Methyl paraben 0.2% w / v Propil paraben 0.1% w / v Steol CS-230 55.5% v / v Glacial acetic acid 5.0% v / v Purified Water as long as it is enough to The final combined product of this two-component pesticidal composition showed 100.0% ovicidal activity when tested according to the conditions described in Example II.
P1109 / 99MX EXAMPLE XI Assay for Citronellyl Acetate In order to test the stability of citronellil acetate in various pesticidal compositions, the following assay was used. This assay used an inverted phase high resolution liquid chromatography (HPLC) method. Two standard solutions were prepared by dissolving 141.5 mg of citronellil acetate in about 20 ml of a 25% water / 75% acetonitrile solution. The column was calibrated using these patterns. A concordance between the two standards within 3% was considered acceptable. The pattern was then injected into the column five times. The average and the relative percentage of standard deviation (% RSD) of the peak were calculated. A% RSD of 3% or less was considered acceptable. One gram of the test composition was then placed in a 100 ml volumetric flask and adjusted to volume with the 25% water / 75% acetonitrile solution. An aliquot of the resulting solution was then filtered through a 0.45 PP filter and injected into the HPLC column. Each sample preparation was tested twice and the pattern was run in the column after every two test injections. The acetate concentration was calculated P1109 / 99MX citronellil for each test composition by dividing the peak response of the sample between the peak response of the standard and by multiplying the result by the weight factor of the sample and the standard test concentration in% declared on the label. The following ingredients were combined in the approximate relative amounts to produce pesticidal compositions with Formula A-K and were tested with this assay. The compositions were produced using the same procedures and basic ingredients as the compositions described in the preceding examples. The key ingredients were the following. Formulas A-J contained 12.5% citronellil acetate and Formula K contained 12.5% citronellol. All Formulas contained 20.0% isopropanol. Formulas A-F and Formulas J and K contained 55.0% Steol CS-230 and water. Formulas G-I did not contain water and Formulas H and I contained 4.0% Ammonyx. Formula I also contained 6.0% Stepanol WA100 and 1.8% Amidox. Formula J was titrated at a pH of 3.5 with IN HCl. Formula A did not contain acid. Formulas B-I and Formula K contained varying amounts of acetic acid as listed below.
P1109 / 99MX Formula Acetic acid concentration B 0.1% C 1.0% D 2.0% E 3.0% F 5.0% G 5.0% H 5.0% I 5.% K 5.% The initial concentration of citronellil acetate for each composition tested was determined using the assay described above. The compositions produced from Formulas A, B and F were stored at room temperature, 40 ° C (accelerated standard temperature) and 60 ° C. The compositions stored at 60 ° C were tested for active citronellyl acetate after two weeks. The compositions stored at room temperature and at 40 ° C were tested by active citronellyl acetate at one and two months. The compositions produced in accordance with Formulas C, D, E, G, H, J and K were stored for two weeks at 60 ° C and active citronellyl acetate was tested. The results of these assays are presented in the following table.
P1109 / 99MX No results available for Formula I It is intended that the above examples be demonstrative but not exhaustive of the embodiments contemplated by the present invention. It is intended that other obvious deviations for those skilled in the art from the above-described invention are included in the scope and spirit of the claims.
P1109 / 99MX

Claims (27)

  1. NOVELTY OF THE INVENTION Having described the present invention, it is considered as a novelty and, therefore, the content of the following CLAIMS is claimed as property: 1. A parasiticidal or pesticidal and ovicidal composition comprising an aqueous detergent, a selected alcohol of the group consisting of ethanol and isopropanol, and a pesticide and ovicidal agent selected from the group consisting of citronellal, citronellol, citronellil and combinations thereof, wherein the parasiticidal or pesticidal agent and ovicide is at a concentration of at least about 8% v / vy, where the composition is not harmful to humans and has more than 13% parasiticidal or pesticidal and ovicidal activity as determined by ASTM standards E938-83 and E5117-93, respectively.
  2. 2. The composition according to claim 1, wherein the parasiticidal or pesticidal agent is citronellil.
  3. 3. The composition according to claim 2, wherein citronellil is a salt selected from the group consisting of acetate, butyrate, formate, isobutyrate, phenylacetate, propionate and valerate.
  4. 4. The composition according to claim 3, wherein the citronellil salt is acetate. P1109 / 99 X 5. The composition according to claim 2, wherein the citronellil is in a concentration between about 8% and 25% v / v. 6. The composition according to claim 5, wherein the citronellil is in a concentration of between 10% to 20% v / v. The composition according to claim 1, wherein the composition further comprises a pH modifier, an antimicrobial agent or a viscosity modifier. The composition according to claim 1, wherein the composition further comprises an antipruritic agent. 9. A kit comprising: a first component of aqueous detergent, an alcohol selected from the group consisting of ethanol and isopropanol, and a parasiticidal or pesticidal and ovicidal agent selected from the group consisting of citronellal, citronellol, citronellil and combinations thereof , wherein the parasiticidal or pesticidal and ovicidal agent is in a concentration of at least about 8% v / v, respectively; and a second component containing acid and water, wherein at least one component further comprises a cleaning agent, wherein when the components are mixed P1109 / 99MX first and second, the resulting composition is not harmful to humans and has more than 13% parasiticidal or pesticidal and ovicidal activity as determined by ASTM E938-83 and E5117-93 standards. 10. The kit according to claim 9, wherein the parasiticidal or pesticidal agent is citronellil. The kit according to claim 10, wherein the citronellil is a salt selected from the group consisting of acetate, butyrate, formate, isobutyrate, phenylacetate, propionate and valerate. 12. The kit according to claim 12, wherein the citronellil salt is acetate. 13. The kit according to claim 10, wherein the citronellil is in a concentration between about 8% and 25% v / v. The kit according to claim 13, wherein the citronellil is in a concentration of between 10% to 20% v / v. 15. The kit according to claim 9, wherein at least one component further comprises an antipruritic agent. The kit according to claim 9, wherein at least one component further comprises a pH modifier, an antimicrobial agent or a viscosity modifier. P1109 / 99MX 17. The kit according to claim 16, wherein the first component further comprises about 8% to 25% v / v of citronellil acetate, from 0.01% to 40% w / v isopropanol, of 0.01% a 5% w / v of methyl paraben, from 0.01% to 5% w / v of propyl paraben and a sufficient amount of aqueous detergent and, wherein, the second component further comprises about 0.1% to 45% w / v of acid acetic, from 0.01% to 5% w / v of methyl paraben, from 0.01% to 5% of propyl paraben and a sufficient amount of water. 18. The case according to claim 17, wherein the first component further comprises between about 10% to 20% v / v citronellil acetate, 15% to 30% w / v isopropanol, 0.1% to 1% w / v paraben and 40% at 80% w / v aqueous detergent, wherein the second one comprises in addition to approximately 20% to 60% w / v acetic acid, from 0.1% to 1% w / v paraben and the sufficient amount of water and, in wherein, the volume ratio between the first component and the second component during use is from about 7.5 to 1. 19. A method for treating a parasite infestation comprising topically administering to the infestation a composition comprising an aqueous detergent. , an alcohol selected from the group consisting of ethanol and isopropanol, and a parasiticidal agent or pesticide and ovicide selected from the group consisting of citronellal, P1109 / 99MX citronellol, citronellil and combinations thereof, wherein the parasiticidal or pesticidal agent and ovicide is at a concentration of at least about 8% v / vy, wherein the composition is not harmful to humans and has more than 13% parasiticidal or pesticidal and ovicidal activity as determined by ASTM standards E938-83 and E5117-93, respectively. The method according to claim 19, wherein the parasiticidal or pesticidal agent is citronellil. The method according to claim 20, wherein citronellil is a salt selected from the group consisting of acetate, butyrate, formate, isobutyrate, phenylacetate, propionate and valerate. 22. The method according to claim 21, wherein the citronellil salt is acetate. 23. The method according to claim 20, wherein the citronellil is in a concentration of between about 8% and 25% v / v. The method according to claim 25, wherein the citronellil is in a concentration of about 10% to 20% v / v. 25. The method according to claim 19, wherein the composition further comprises an antipruritic agent. 26. The method according to claim 19, in P1109 / 99MX wherein the composition further comprises a pH modifier, an antimicrobial agent or a viscosity modifier. 27. The method according to claim 19, wherein the infestation is found in a mammal. P1109 / 99MX
MXPA/A/1999/001095A 1996-07-29 1999-01-29 Pesticidal composition and method of use MXPA99001095A (en)

Applications Claiming Priority (2)

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US022377 1996-07-29
US08901216 1997-07-28

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MXPA99001095A true MXPA99001095A (en) 2000-06-05

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