WO2001012173A1 - Composition a faible teneur pour traiter des parasites et procede associe - Google Patents

Composition a faible teneur pour traiter des parasites et procede associe Download PDF

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Publication number
WO2001012173A1
WO2001012173A1 PCT/US2000/021417 US0021417W WO0112173A1 WO 2001012173 A1 WO2001012173 A1 WO 2001012173A1 US 0021417 W US0021417 W US 0021417W WO 0112173 A1 WO0112173 A1 WO 0112173A1
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WO
WIPO (PCT)
Prior art keywords
composition
ovicidal
citronellyl
pedicuucidal
component
Prior art date
Application number
PCT/US2000/021417
Other languages
English (en)
Inventor
Jeffrey H. Ping
Original Assignee
Effcon Laboratories, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Effcon Laboratories, Inc. filed Critical Effcon Laboratories, Inc.
Priority to AU66226/00A priority Critical patent/AU6622600A/en
Publication of WO2001012173A1 publication Critical patent/WO2001012173A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/02—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings containing insect repellants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/342—Alcohols having more than seven atoms in an unbroken chain
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids

Definitions

  • the present invention relates to agents and methods for the treatment of pest infestations.
  • the invention relates to compositions for cleansing infested individuals of parasites and their ova.
  • Pesticides and insects repellents have long been sought for use against harmful or annoying parasites. Pests such as lice and fleas are irritating and painful to their human and animal hosts, and can also be vectors for other agents of disease.
  • the pesticides and repellents available in the prior art suffer from various deficiencies. Often, compositions provided as insect repellents are not insecticidal. Furthermore, many compositions are either toxic or generally unpleasant to the host. Still others require too many separate active ingredients for efficient production and regulation. Many synthetic prior art compositions have been proposed as insect repellents, but have later been determined to be unsuitable for safe use by humans.
  • One common active ingredient in prior commercial compositions is N,N-Diethyl-m- toluamide (DEET).
  • DEET has recently been associated with causing various undesirable side-effects, such as stinging, damage to mucous membranes, and possibly seizures.
  • the Centers for Disease Control issued a cautionary statement regarding the use of DEET.
  • Many other prior art compounds proposed for use as a repellent have proven unsuitable for topical application to humans or other aiiirnals due to their toxic or noxious effect on the infested individual.
  • insect repellents containing the whole oil of citronella are undesirable due to their limited repellency, unpleasant odor and consistency, and unrehable composition of potentially harmful and unnecessary agents.
  • Most prior art insect treatments are taught to be effective only with specific synergistic combinations of multiple pesticides.
  • pedicuUcidal and ovicidal composition that is effective at low concentrations and which does not require a combination of excess multiple pesticidal ingredients.
  • pedicuUcidal and ovicidal composition with fewer active components and with a lower concentration of pedicuUcidal and ovicidal compositions.
  • the composition should also be able to cleanse an individual being treated for infestation.
  • the present invention provides a pediculicidal and ovicidal composition containing low concentrations of the active ingredient which demonstrates an extraordinarily lethal effectiveness against parasites, such as lice.
  • the pedicuUcidal and ovicidal composition of the present invention is effective in cleansing an individual, human or animal, of a pest infestation.
  • the composition of the present invention contains a purified derivative of an organic oil.
  • An example of an organic oil from which these compounds can be derived is citroneUa oil. These purified derivatives can be both pedicuUcidal and ovicidal. Examples of purified derivatives of citronella oil include citroneUal, citroneUol and citroneUyl compounds. Purified nerol and geraniol can also be derived from citronella oil.
  • the pedicuUcidal and ovicidal composition preferably contains a active agent such as citroneUal, citronellol or citroneUyl compound.
  • the citronellal, citronellol or citronellyl compound is present in a concentration of less than 8% w/w.
  • the pediculicidal and ovicidal composition more preferably comprises a citronellyl salt and an alcohol.
  • the composition also preferably contains an acid and an aqueous detergent.
  • the compositions can be administered topically to humans, animals or to any infested areas.
  • Another example of an organic oil from which a compound can be derived is teatree oU.
  • Compounds such as terpinen-4-ol can be derived from teatree oil.
  • the present invention also includes a method of using the pedicuUcidal and ovicidal compositions.
  • the method includes applying the composition to the infested area, aUowing the composition to remain in contact with the infested area for a period of time, rinsing the composition from the area and, in the case of an infestation of hair such as a Uce infestation, combing the infested area with a suitable nit comb.
  • the method also includes varying the period of time the composition is allowed to remain in contact with the infested area, caUed the residence time, so that lower concentrations of active ingredient can be used while pedicuUcidal and ovicidal effectiveness is maintained.
  • the residence time can be increased when a composition containing a lower concentration of the active ingredient is used in the treatment method.
  • composition that may be used as a cleansing shampoo, soap, cream, lotion, gel or spray.
  • Another object of the present invention is to provide a method of using a pedicuUcidal and ovicidal composition to cleanse an individual of a pest infestation.
  • Fig. 1 shows a Unear regression of percent mortality against concentration of active ingredient.
  • Fig. 2 shows exposure time against percent activity.
  • a “pest” is meant to include aU parasites, such as but not limited to arthropods, arachnids, triatomes, insects, bugs, flies, Uce, fleas, mites, gnats, nits, chiggers, mosquitoes, and ticks, for example.
  • the composition of the present invention is, therefore, intended to be used against aU parasites which succumb to the lethal properties thereof.
  • the present invention provides pedicuUcidal and ovicidal compositions comprising purified derivatives of organic oUs as active ingredients.
  • purified derivatives of citroneUa oil can be used as active ingredients in pedicuUcidal and ovicidal compositions.
  • derivatives purified from citroneUa oU include citroneUal, citroneUol and citronellyl compounds. Other examples include nerol and geraniol.
  • the present invention provides a pedicuUcidal and ovicidal composition
  • a pedicuUcidal and ovicidal composition comprising an alcohol, an acid, an aqueous detergent and an active agent comprising citroneUal, citroneUol or citronellyl in a concentration of less than 8% w/w.
  • CitroneUal, citroneUol and citroneUyl are currently avaUable in the trade as food and cosmetic additives.
  • a pharmaceutical grade of citroneUyl acetate may be available from Delmar Chemicals (Montreal, Canada).
  • the pesticidal agent utilized is citroneUyl.
  • the citroneUyl compound is selected from the group consisting of citroneUyl acetate, citronellyl butyrate, citronellyl formate, citroneUyl isobutyrate, citronellyl phenylacetate, citroneUyl proprionate and citronellyl valerate.
  • the citronellyl salt is acetate.
  • the invention preferably provides a pedicuUcidal and ovicidal composition wherein the pesticidal agent, for example citronellyl, is in a concentration of between about 0.01% and 8% w/w, more preferably between about 1% and 8% w/w, and most preferably between about 2.5% and 8% w/w.
  • the pesticidal agent for example citronellyl
  • Compositions are also provided which contain nerol or geraniol as their active agent. Varying percentages of these compounds can be used in compositions. These percentages can vary from 0.1 % w/w to 25 % w/w.
  • the composition of the present invention also includes an alcohol.
  • the alcohol is a short chain alcohol, such as ethanol, propanol or isopropanol.
  • the amount of alcohol in the present invention can range from 1 to 40 % w/w.
  • the concentration is between about 10 and 30 % w/w, more preferably between about 15 and 25 % w/w, and most preferably about 20 % w/w.
  • the alcohol is preferably isopropanol. It is believed that the presence of an alcohol in the composition increases the composition's pedicuUcidal and ovicidal effectiveness by permeabiUzing the outer membrane of the parasite ova thereby aUowing the pesticidal agent to penetrate the outer membrane of the ova. Functional substitutes that achieve the same result can be substituted for the alcohol without departing from the scope and spirit of the claims.
  • the composition also contains an acid in a concentration of between about 0.01 and 10 % w/w. More preferably, the invention contains between about 1 and 8 % w/w, and most preferably contains about 5 to 6 % w/w.
  • the acid is an ionic or organic acid.
  • the acid is hydrochloric acid or acetic acid. More preferably, the acid is glacial acetic acid. It is beUeved that the acetic acid makes the membranes more permeable as the chitinous bards may be weakened at low pH.
  • Some embodiments of the present invention also include an aqueous detergent.
  • the aqueous detergent is capable of chelating debris or disrupting hydrophobic suspensions, for example, in order to assist in the removal of pests and their ova.
  • the concentration of the aqueous detergent within the present invention is preferably between about 7 and 21 % w/w and more preferably between about 14 and 18 % w/w.
  • Many weU known cleansing agents can be used.
  • the aqueous detergent is a surfactant, such as sodium laureth sulfate. Sodium laureth sulfate is available in commercial preparations such as
  • Steol® CS-230 which is available from Stepan (North Field, Illinois).
  • Steol® CS-230 is an aqueous preparation of sodium lauryl ether sulfate derived from fatty alcohols, ethoxylated to an average of two moles, and sulfated via a continuous S03 process.
  • Steol® CS-230 is about 25.5 % sodium laureth sulfate.
  • the concentration of Steol® CS-230 within the present invention is preferably between about 30 and 80 % w/w and more preferably between about 55 and 70 % w/w.
  • composition of the present invention may be suitably preserved. Any suitable preservative may be used so long as it does not interfere with the pest removing abitity of the composition.
  • methylparaben and propylparaben are included in the composition as preservatives. Methylparaben and propylparaben are preferred parabens, but others can be substituted.
  • composition of the present invention can contain other ingredients so long as the beneficial, pedicuUcidal and ovicidal nature of the invention is not adversely affected and so long as the effectiveness of the invention is not altered.
  • embodiments of the present invention can contain methylparaben and propylparaben which are antimicrobial agents.
  • embodiments of the present invention can contain viscosity modifiers such as sodium chloride or antipruritic agents such as camphor.
  • the composition of the present invention can be used in different forms, such as a Uquid body soap or a shampoo.
  • the present invention takes the form of a gel, an emulsion, a lotion, an aerosol spray, a mousse, or a cream.
  • the composition of the present invention is in the form of a shampoo.
  • the invention also provides a method of treating an individual having a parasite infestation comprising administering to the infestation an insecticide composition as described above.
  • the composition of the present invention is effective as an insecticide intended for killing and removing Uce from humans.
  • Varied treatment regimens are contemplated as being within the method of treatment provided by this invention. Treatment regimens can vary from a single administration to repeated administrations over long time periods. The various possible treatment regimens would be apparent to one skilled in the art based on the invention disclosed herein and are intended to be encompassed in the scope and spirit of the claims.
  • This method includes applying the composition to the infested area, such as the hair of an individual with a Uce infestation.
  • the composition is appUed to the hair.
  • the composition is left on the hair for a period of time referred to as the residence time.
  • the residence time can vary as needed to produce effective results.
  • the residence time can be as long as 12 hours and as short as one minute.
  • the residence time is between 5 and 60 minutes. More preferably, the residence time is between approximately 10 and 30 minutes.
  • the composition is rinsed from the area of infestation.
  • the time period between uses of the pest removing composition can vary as needed to remove the pest infestation from the individual.
  • the composition of the present invention is advantageous because it aUows for frequent use, whereas the use of compositions containing high doses of pesticides can be limited by their high toxicity. This ability to use the composition of the present invention increases the its effectiveness in cleansing individuals of pest infestations.
  • nit comb Before or after appUcation of the composition the hair may be combed with a suitable nit comb, however combing is not necessarily required.
  • Any suitable nit comb can be used in the described method of use of the composition of the present invention.
  • a suitable nit comb may be made of various materials such as metal and plastic.
  • Metal teeth are sturdier and stiffer than those composed of materials such as plastic. Nit combs with metal teeth therefore often last longer than nit combs without metal teeth.
  • the number of teeth and the diameters of the teeth can also vary.
  • the spacing between teeth can also vary; however, the teeth should be close enough to one another to remove nits.
  • the distance between teeth should be 0.3mm or less, the generally accepted width of nits attached to human hair.
  • a nit comb such as the ALB 006 is used, which is avaUable from Albyn Stonehaven Ltd. (Stonehaven, Scotland).
  • This comb has 62 metal pins arranged side by side which act as the teeth of the comb. These pins extend approximately 12.5mm from a plastic piece which acts as the handle of the nit comb.
  • the pins on either end have a diameter of 0.9mm and the 60 inner teeth have a diameter of 0.6mm.
  • the gap between the teeth is 0.3mm.
  • the pedicuUcidal and ovicidal composition comprises 1 to 8% w/w citroneUyl acetate.
  • This embodiment of the present invention further comprises about 1 to 40% w/w isopropyl alcohol, 0.01 to 5% w/w methylparaben, 0.01 to 5% w/w propylparaben, 0.01 to 10% w/w acetic acid, 30 to 60% w/w detergent and water q.s.p. 100 g.
  • the pedicuUcidal and ovicidal composition of the present invention more preferably comprises about 7.5% citronellyl acetate, about 20% w/w isopropyl alcohol, 0.2% w/w methylparaben, 0.1% w/w propylparaben, 5.0% w/w acetic acid, 55.5% w/w detergent and water q.s.p 100 %.
  • Embodiments of the pedicuUcidal and ovicidal composition of the present invention can further include a viscosity modifier, or an antipruritic agent, for example.
  • the pediculicidal and ovicidal composition further comprises camphor as an antipruritic agent, sodium chloride as a viscosity modifier, methylparaben and/or propylparaben as an antimicrobial agent, acetic acid as a pH modifier and cleansing agent, and water.
  • the pedicuUcidal and ovicidal composition further comprises about 0.01 to 5% w/w camphor and 1 to 10% w/w sodium chloride.
  • the pediculicidal and ovicidal composition can comprise about 0.75% w/w camphor, 4.87% w/w sodium chloride, 0.2% w/w methylparaben, 0.1% w/w propylparaben, 5.7% w/w acetic acid, 35.14% w/w detergent and water q.s.p 100 %.
  • the pedicuUcidal and ovicidal composition of the present invention can further be embodied in a two component system. In the two component system, two components are prepared and stored separately, and then mixed together at the point of use.
  • the "Active Ingredient Component" comprises an alcohol, a pedicuUcidal and ovicidal agent, an antimicrobial agent and a detergent.
  • the “DUuent Component” comprises a pH modifier and an antimicrobial agent.
  • the "Active Ingredient Component” further comprises isopropanol as an alcohol, citroneUyl acetate as an active ingredient, methylparaben as an antimicrobial agent, propylparaben as an antimicrobial agent and Steol CS-230 as a detergent and water
  • the "Diluent Component” further comprises glacial acetic acid as a pH modifier and as a cleansing agent, methylparaben as an antimicrobial agent, propylparaben as an antimicrobial agent and water as a diluent.
  • the "Active Ingredient Component” further comprises 8.5% w/w citroneUyl acetate, 22.64% w/w isopropanol, 0.2% w/w methylparaben, 0.1% w/w propylparaben, and 62.8% w/w Steol CS-230, and the "Diluent Component” further comprises 42.86% w/w glacial acetic acid, 0.2% w/w methylparaben, 0.1% w/w propylparaben, and water q.s.
  • the "DUuent Component” comprises about 11 2/3% of the combined final product.
  • the combined final product in this most preferred embodiment comprises 7.5% w/w citronellyl acetate, 20% w/w isopropanol, 0.2% w/w methylparaben, 0.1% w/w propylparaben, 55.5% w/w Steol CS-230, 5% w/w acetic acid and water q.s. 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 accordingly the ratio of their combination, to yield a functional pesticide composition.
  • citroneUal and citroneUol also possess a surprising degree of pedicuUcidal and ovicidal effectiveness at low concentrations. Therefore, the invention contemplates that either citronellal and citronellol may be substituted for citroneUyl, or added to the pesticidal agent of the composition.
  • CitroneUa oU is a complex mixture containing components which may ordinarily mask the potential effectiveness of the individual pesticidal agents citroneUyl, citroneUol, and citroneUal, as disclosed by the present invention. It also appears that a synergistically beneficial effect is achieved in the compositions of the present invention.
  • the presence of an alcohol in the compositions appears to aid the surprising pedicuUcidal and ovicidal effectiveness of the low concentration pesticide compositions described herein.
  • the presence of an acid and an aqueous detergent with the active pesticidal ingredient is believed to contribute to the surprising effectiveness of the present invention at killing pests and cleansing individuals of pest infestations.
  • the present invention is intended to be administered topicaUy to infested areas of an individual, such as the hair and scalp or pubic areas.
  • the composition is preferably provided in the form of a Uquid or soUd, such as shampoo, soap, cream, or lotion.
  • various other complimentary ingredients can be included, such as an antipruritic agent, a pH modifier, or as a general medium.
  • glycerins, glycols, alcohols, lanoUns, aloe vera gel may be provided in the composition.
  • the preferred compositions are shampoos and soaps containing ingredients capable of assisting in cleansing individuals of the debris of dead parasites.
  • the composition may also be provided in sun screening, tanning or any other topically applicable products.
  • compositions can be provided as a pesticide and cleaning agent for fruits and vegetables.
  • the composition can additionally serve as a repellent for cats, dogs, birds, cattle, or sheep, for example.
  • the composition may also be used as a carpet powder, or as a detergent additive, rinse or spray for clothing, bedding or other fabrics.
  • the composition may also be used as an aerosol bomb or as a room spray.
  • Other such uses would be apparent to one skiUed in the art upon contemplating the invention disclosed herein and such uses are intended to be encompassed in the scope and spirit of the claims.
  • test were conducted as follows. Twenty-five (25) adult Uce were placed into a vial having a screen bottom.
  • the vial was placed in a container of the composition to be tested which was maintained at a temperature of 32°C.
  • a screened plunger was inserted into the top of the vial containing the Uce to ensure that the Uce did not float to the surface.
  • the Uce were thus submerged in the test composition for a set exposure time.
  • the Uce containing vial was then dipped in distilled water maintained at a temperature of 32°C and gently agitated for one minute.
  • the Uce were then gently washed by a stream of 32°C distiUed water. Excess water was removed by blotting with paper toweling.
  • Mortality percentages were corrected by Abbott's Formula. The percent of mortality in a control was subtracted from the percent mortality in the test and then divided by the percent mortality in the test.
  • each test was conducted as follows. Thirty human louse eggs attached to human hair cuttings were used for each test condition. The human hair cuttings were affixed to a wood applicator stick and then immersed in the composition to be tested for various exposure times. The test composition was maintained at 32°C. The eggs were then washed by vigorously moving the stick up and down in 32°C tap water for one minute. A wash bottle was then used to further wash the eggs with 32°C tap water for an additional minute.
  • the eggs were then incubated until aU eggs exposed to control conditions hatched (approximately 12 days). AU eggs were then observed for hatching. Eggs that faUed to hatch were recorded as mortalities.
  • Mortality percentages were corrected by Abbott's Formula. The percent of mortality in a control was subtracted from the percent mortality in the test and then divided by the percent mortality in the test.
  • the two component composition was produced and stored separately. The two components were mixed just prior to use. The first component was an 'Active Ingredient Component" and the second component was an "Diluent Component.” The two component composition was prepared in the following manner.
  • the isopropanol and the methyl and propylparabens were mixed in a vessel until the parabens were completely dissolved.
  • the Steol CS-230 was then added and mixed untU completely uniform.
  • citronellyl acetate was added and mixed until uniform. This step was skipped in the 0% formulation. Purified water was then used to dilute the mixture to its final weight and mixed until completely uniform.
  • a portion of the total purified water was added to a mixing vessel. Glacial acetic acid was added to the vessel and mixed untU completely uniform. The methyl and propylparabens were then added to the mixing vessel and mixed until completely dissolved. The resulting solution was then diluted to the final target weight with purified water.
  • the two components were mixed together at the point of use in 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.
  • the amount of citronellyl acetate contained in the "Active Ingredient Component" and consequently the concentration of citroneUyl acetate in the final product varied between formulations.
  • the final concentrations of citronellyl acetate in each of the formulations is shown below.
  • Formulations A-F were each tested for in vitro pedicuUcidal activity with a 10 minute exposure time in the test described in Example I.
  • Formulation A and B showed only 2.1 and 4.3% pedicuUcidal activity, respectively, whUe formulations C, D, E and F demonstrated 40.7, 100, 100 and 100% pedicuUcidal activity, respectively.
  • a clinical study was designed and performed to evaluate the efficacy and safety of treating human patients with infestations of human head Uce with a two component pedicuUcidal and ovicidal composition. Twenty patients diagnosed with a head Uce infestation were treated on Day 1 with the pedicuUcidal and ovicidal composition described in Example HI containing a 7.5% concentration of citroneUyl acetate. After wetting the hair, the pedicuUcidal and ovicidal composition was appUed and allowed to sit for a residence time of 10 minutes before it was rinsed out.
  • the rinse water was strained to collect Uce that were removed from the hair after treatment.
  • the Uce were placed in a petri dish, examined for viabiUty, and incubated for 24 +/- 2 hours under appropriate conditions.
  • the pedicuUcidal and ovicidal composition with 7.5% citronellyl acetate effectively reduced or eliminated head Uce infestations. Additionally, the composition was 100% pediculicidal, and the composition was well tolerated.
  • Example VI the primary efficacy outcome criterion was clinical outcome evaluated 14 days after the final apphcation. Outcome was classified as cured, re-infestation, or failure based on the number of lice and nits found in the hair.
  • Secondary efficacy criteria included a viabiUty assessment of Uce collected before and after treatment.
  • the viabiUty of the Uce collected was assessed 1 hour after coUection and 24 hours after collection. After 1 hour, 74.4, 78.7 and 86.1 % of the Uce collected after treatment with the 2.5 %, 5.0 % and 7.5 % pediculicidal and ovicidal compositions, respectively, were dead. After 24 hours, 99.1, 99.6 and 100 % of the Uce collected after treatment with the 2.5 %, 5.0 % and 7.5 % pediculicidal and ovicidal compositions, respectively, were dead.
  • citroneUyl acetate 5.0 and 7.5 % citroneUyl acetate was effective in treating Uce infestations and was weU tolerated. AdditionaUy, each pediculicidal and ovicidal composition showed a very high degree of pediculicidal activity.
  • compositions with citronellyl acetate concentrations of 2.5% and 7.5%, as weU as pedicuUcidal and ovicidal compositions with citroneUyl acetate concentrations of 7.5% and 12.5% that were dUuted 50/50 with tap water were prepared according to the method described in Example TV. Each composition was tested on nits collected from lice infested humans.
  • the pedicuUcidal and ovicidal composition with a citronellyl acetate concentraion of 2.5% showed 97.3% ovicidal activity, whUe the 7.5% composition showed 100% ovicidal activity.
  • the 7.5% and 12.5% compositions diluted 50/50 with tap water demonstrated 99.9% and 99.4% ovicidal activity, respectively.
  • Example VIII Production of a Two Component Compositions
  • Each component of the composition is produced and stored separately.
  • the two components are mixed just prior to use.
  • the first component is an "Active Ingredient Component” and the second component is an “Diluent Component.”
  • the two component composition are prepared in the foUowing manner.
  • the foUowing ingredients are combined in approximate relative amounts to make the "Active Ingredient Component.”
  • the isopropanol and the methylparabens and propylparabens are mixed in a vessel until the parabens are completely dissolved.
  • the Steol CS-230 is then added and mixed until completely uniform.
  • citroneUyl acetate is added and mixed until uniform.
  • Purified water is then used to dilute the mixture to its final weight and mixed until completely uniform.
  • the foUowing ingredients are combined in approximate relative amounts to produce the "Diluent Component.”
  • a portion of the total purified water is added to a mixing vessel. Glacial acetic acid is added to the vessel and mixed until completely uniform. The methylparabns and propylparabens are then added to the mixing vessel and mixed until completely dissolved. The resulting solution is then diluted to the final target weight with purified water. The two components are mixed together at the point of use in relative amounts such that the "Diluent Component" comprised approximately 11 2/3 % of the final combined product. The final product contains the foUowing ingredients in the approximate relative amounts listed below.
  • Each component of the composition is produced and stored separately.
  • the two components are mixed just prior to use.
  • the first component is an "Active Ingredient Component” and the second component is an “Diluent Component.”
  • the two component composition are prepared in the foUowing manner.
  • the foUowing ingredients are combined in approximate relative amounts to make the "Active Ingredient Component.”
  • the isopropanol and the methylparabens and propylparabens are mixed in a vessel untU the parabens are completely dissolved.
  • the Steol CS-230 is then added and mixed until completely uniform.
  • geraniol is added and mixed until uniform.
  • Purified water is then used to dUute the mixture to its final weight and mixed until completely uniform.
  • the foUowing ingredients are combined in approximate relative amounts to produce the "Diluent Component.”
  • a portion of the total purified water is added to a mixing vessel. Glacial acetic acid is added to the vessel and mixed until completely uniform. The methylparabns and propylparabens are then added to the mixing vessel and mixed until completely dissolved. The resulting solution is then diluted to the final target weight with purified water.
  • the two components are mixed together at the point of use in relative amounts such that the "Diluent Component" comprised approximately 11 2/3 % of the final combined product.
  • the final product contains the foUowing ingredients in the approximate relative amounts listed below.
  • composition is then tested for in vitro pedicuUcidal activity with a 10 minute exposure time in the test described in Example I.
  • Each component of the composition is produced and stored separately.
  • the two components are mixed just prior to use.
  • the first component is an "Active Ingredient Component” and the second component is an “Diluent Component.”
  • the two component composition are prepared in the foUowing manner.
  • the foUowing ingredients are combined in approximate relative amounts to make the "Active Ingredient Component.”
  • the isopropanol and the methylparabens and propylparabens are mixed in a vessel until the parabens are completely dissolved.
  • the Steol CS-230 is then added and mixed until completely uniform.
  • nerol is added and mixed until uniform.
  • Purified water is then used to dUute the mixture to its final weight and mixed until completely uniform.
  • the foUowing ingredients are combined in approximate relative amounts to produce the "Diluent Component.”
  • a portion of the total purified water is added to a mixing vessel. Glacial acetic acid is added to the vessel and mixed until completely uniform. The methylparabns and propylparabens are then added to the mixing vessel and mixed untU completely dissolved. The resulting solution is then diluted to the final target weight with purified water.
  • the two components are mixed together at the point of use in relative amounts such that the "Diluent Component" comprised approximately 11 2/3 % of the final combined product.
  • the final product contains the foUowing ingredients in the approximate relative amounts listed below.
  • Example XI Production of a Two Component Compositions Containing
  • Each component of the composition is produced and stored separately.
  • the two components are mixed just prior to use.
  • the first component is an "Active Ingredient Component” and the second component is an “Diluent Component.”
  • the two component composition are prepared in the foUowing manner.
  • the foUowing ingredients are combined in approximate relative amounts to make the "Active Ingredient Component.”
  • the isopropanol and the methylparabens and propylparabens are mixed in a vessel until the parabens are completely dissolved.
  • the Steol CS-230 is then added and mixed untU completely uniform.
  • terpinen-4-ol is added and mixed until uniform.
  • Purified water is then used to dUute the mixture to its final weight and mixed untU completely uniform.
  • a portion of the total purified water is added to a mixing vessel. Glacial acetic acid is added to the vessel and mixed until completely uniform. The methylparabns and propylparabens are then added to the mixing vessel and mixed until completely dissolved. The resulting solution is then diluted to the final target weight with purified water.
  • the two components are mixed together at the point of use in relative amounts such that the "Diluent Component" comprised approximately 11 2/3 % of the final combined product.
  • the final product contains the following ingredients in the approximate relative amounts listed below.
  • composition is then tested for in vitro pedicuUcidal activity with a 10 minute exposure time in the test described in Example I.
  • compositions containing 0.1, 0.75, 1.75 and 2.5 % w/w citronellyl acetate are prepared according to Example VTfl. These compositions are then tested for pedicuUcidal activity according to the method set forth in Example I, except that the amount of time the composition is left in contact with the test Uce, the residence time, is varied. Each concentration is tested for pediculicidal activity with a residence time of 20 minutes and 30 minutes. The results of the exposure time testing are summarized in Fig. 2. Graphical representation of the data clearly shows that increasing the exposure time from 10 minutes to 30 minutes has Uttle significant effect on the in vitro pedicuUcidal activity of the compositions. However, it did increase the 1.75% effectiveness considerably (from 1.7% to 50.8% and 21.7%) which collaborates the findings of the dose escalation study which showed that citroneUyl acetate concentrations above 0.75% possess statistically significant activity.

Abstract

L'invention concerne une composition pédiculicide et ovicide présentant une efficacité létale extraordinaire et pouvant être utilisée pour éliminer des parasites tels que les poux. Ladite composition contient, de préférence, un alcool et un agent pesticide tel que citronellal, citronellyle ou un mélange de ceux-ci. On préfère en outre utiliser, comme agent pesticide, l'acétate de citronellyle. Les compositions peuvent être administrées localement à l'homme, aux animaux ou à toute zone attaquée.
PCT/US2000/021417 1999-08-13 2000-08-04 Composition a faible teneur pour traiter des parasites et procede associe WO2001012173A1 (fr)

Priority Applications (1)

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AU66226/00A AU6622600A (en) 1999-08-13 2000-08-04 Low concentration pest treatment composition and method

Applications Claiming Priority (2)

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US14887799P 1999-08-13 1999-08-13
US60/148,877 1999-08-13

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6664292B2 (en) * 2001-06-04 2003-12-16 Mark H. Bogart Methods for the treatment of nail fungus and other microbial and mycotic conditions and compositions useful therefor
US6663876B2 (en) 2002-04-29 2003-12-16 Piedmont Pharmaceuticals, Llc Methods and compositions for treating ectoparasite infestation

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000005964A1 (fr) * 1998-07-28 2000-02-10 Ecosmart Technologies, Inc. Compositions pesticides a action synergique et residuelle renfermant des huiles essentielles vegetales
JP2000128720A (ja) * 1998-10-20 2000-05-09 Huajian Medical Science & Technol Co Ltd 虫除け用組成物およびそれを用いた虫除けパッチ

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000005964A1 (fr) * 1998-07-28 2000-02-10 Ecosmart Technologies, Inc. Compositions pesticides a action synergique et residuelle renfermant des huiles essentielles vegetales
JP2000128720A (ja) * 1998-10-20 2000-05-09 Huajian Medical Science & Technol Co Ltd 虫除け用組成物およびそれを用いた虫除けパッチ

Non-Patent Citations (3)

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Title
DATABASE CAPLUS ON ACS BESSETTE ET AL.: "Synergistic and residual insecticidal compositions containing essential oils", XP002934424 *
DATABASE CAPLUS ON ACS CHODNEKAR ET AL.: "Pesticidal terpenoid and polyunsaturated acid and alcohol derivatives", XP002934422 *
DATABASE CAPLUS ON ACS LAI ET AL.: "Insect-repellent compositions containing essential oils, patch having the compostion and its manufacture", XP002934423 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6664292B2 (en) * 2001-06-04 2003-12-16 Mark H. Bogart Methods for the treatment of nail fungus and other microbial and mycotic conditions and compositions useful therefor
EP1401421A1 (fr) * 2001-06-04 2004-03-31 Mark H. Bogart Methodes et compositions pour le traitement de l'onychomycose et autres pathologies microbiennes et mycosiques
EP1401421A4 (fr) * 2001-06-04 2004-09-15 Mark H Bogart Methodes et compositions pour le traitement de l'onychomycose et autres pathologies microbiennes et mycosiques
US6663876B2 (en) 2002-04-29 2003-12-16 Piedmont Pharmaceuticals, Llc Methods and compositions for treating ectoparasite infestation
US8178116B2 (en) 2002-04-29 2012-05-15 Piedmont Pharmaceuticals, Llc Methods and compositions for treating ectoparasite infestation
US8815270B2 (en) 2002-04-29 2014-08-26 Piedmont Pharmaceuticals, Llc Methods and compositions for treating ectoparasite infestation

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