WO2002024182A1 - Formulation contre les ectoparasites - Google Patents

Formulation contre les ectoparasites Download PDF

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Publication number
WO2002024182A1
WO2002024182A1 PCT/AU2001/001183 AU0101183W WO0224182A1 WO 2002024182 A1 WO2002024182 A1 WO 2002024182A1 AU 0101183 W AU0101183 W AU 0101183W WO 0224182 A1 WO0224182 A1 WO 0224182A1
Authority
WO
WIPO (PCT)
Prior art keywords
treatment formulation
formulation
polymers
agent
treatment
Prior art date
Application number
PCT/AU2001/001183
Other languages
English (en)
Inventor
William Victor Greig
Wendy Louise Free
Original Assignee
Hair Advisory Centre Pty Ltd T/A Queensland Cosmetic Laboratories
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 Hair Advisory Centre Pty Ltd T/A Queensland Cosmetic Laboratories filed Critical Hair Advisory Centre Pty Ltd T/A Queensland Cosmetic Laboratories
Priority to AU2001291485A priority Critical patent/AU2001291485A1/en
Publication of WO2002024182A1 publication Critical patent/WO2002024182A1/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
    • 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
    • A61K8/37—Esters of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/14—Ectoparasiticides, e.g. scabicides

Definitions

  • TITLE OF INVENTION ECTOPARASITE FORMULATION FIELD OF THE INVENTION relates to an ectoparasite formulation for treatment of headlice and other parasitic infections which may be utilised in susceptible human and animal species.
  • a primary active component of the formulation is a C,- ⁇ lower alkanol which may be selected from ethanol or isopropanol.
  • 95/255544 which refers to a gel composition for treatment of skin diseases and for disinfection of the skin which comprises more than 90% of ethanol based on the weight of the gel composition and less than 10% of water based on the weight of the gel composition. There is also provided between 0.1 and 10% by weight of a high molecular weight polymer gelling agent.
  • the gel composition utilised in this reference was of use in treatment of open wounds such as skin abrasions and also skin eruptions caused by viral infections, especially herpes infections.
  • the composition could be applied to the mucous membranes and could also be utilised for controlling parasitic organisms inclusive of ectoparasites such as scabies, chigger and headlice.
  • the active component in the abovementioned gel composition was the ethanol which disinfected the infected area and protected the infected area against reinfection via a "plaster effect" obtained by the dried gel, until the wound had healed.
  • the disinfectant action of the ethanol would only be obtained when used in a concentrated form i.e. more than 90% because the use of the ethanol in lower concentrations such as 60% provided a distinct pain reaction which made it inappropriate for use, especially in application to the mucous membranes.
  • the water could only be used in concentrations less than 10% because of the necessity of the gel composition to be hygroscopic.
  • Patent 5783202 was that they do not kill lice consistently when used in shampoos.
  • a surface wetting agent which is preferably sodium or calcium dioctyl sulphosuccinate
  • the object of the invention is to provide an ectoparasite treatment formulation which is non toxic and effective in use.
  • the treatment formulation of the invention comprises from 20-87% w/w of a lower alcohol having 1 -4 carbon atoms and 0.1 -20.0% of a thickening agent. Preferably there is also included 0.05-20.0% w/w of a conditioning or anti-static agent or emulsion binding and/or stabilising agent.
  • the lower alcohol used in the formulation of the invention to most preferably isopropanol although ethanol can be utilised if desired. Methanol or butanol may be used, although they are less preferred as they may be toxic in some circumstances.
  • the thickening agent used in the formulation of the invention may be any substance that increases the viscosity of the formulation and which is also alcohol compatible.
  • the viscosity of the formulation after inclusion of the thickening agent, may be from 100 to 100,000 centistokes.
  • the thickening agent may be used singly or a combination of thickening agents may be utilised.
  • the thickening agent may be a polymer which can be linear, branched or cross linked and may be naturally derived, or may be synthetic. Any of the gelling or thickening agents may be used that are described in WO 95/255544, which is totally incorporated herein by reference.
  • Such polymers are mostly cellulose derivatives, naturally derived polysaccharides and synthetic polymers inclusive of polyethylene glycols, polyethylene oxides, polyvinyl pyrrolidones and polyacrylic acid.
  • suitable thickening agents may be those described in "International Cosmetic Ingredient Dictionary and Handbook” published by The Cosmetic, Toiletry and Fragrance
  • Such thickening agents may be selected from viscosity increasing agents that thicken or have a gelling effect on the aqueous or alcoholic components of cosmetic or therapeutic products. Their ability to perform this function is related to their water and alcohol solubility or hydrophilic nature and includes acrylamide copolymers, cross polymers or copolymers having an acrylate component, alginic acid or alginates, carbomers, carboxymethyl polymers, betaines, tallowamides, stearamides, gums, cocamides, gelatins, kelp, polythylene glycols and polymers containing polyethylene glycol, clays including bentonite, hyaluronic acid, lauramides, oleamides, palmamides, kemelamides and the like.
  • the conditioning or anti-static agents are primarily cationic or anionic surfactants, amines, betaines, protein derivatives, amino acids and quaternary ammonium compounds that alter the electrical properties of the formulation after application to skin or scalp by reducing their tendency to acquire an electrical charge. Examples of such conditioning agents or anti-static agents are described in the publication "International Cosmetic Ingredient Dictionary and Handbook" discussed above.
  • conditioning agents may include polyquaternium species, polyethylene glycol amides, polyethylene glycol amines, quaternium species, polyethylene glycol tallow amines, isostearamidopropyl compounds, steramidopropyl compounds and the like.
  • the formulation of the invention may also include an emulsion stabiliser that may assist in the formation and stabilisation of emulsions.
  • emulsion stabilisers may be used in lieu of the antistatic or conditioning agent or used in combination with the anti-static or conditioning agent.
  • the emulsion stabilisers may also be utilised as a thickening agent.
  • Emulsion stabilisers do not function as primary emulsifiers but prevent or reduce the coalescence of emulsified droplets by modifying the continuous or disperse phase of the emulsion.
  • the stabilisation may result from electrical repulsion from changes in viscosity or from film formation on the droplet surface.
  • emulsion stabilisers examples include aluminium salts of long chain fatty acids, C 9-11 alcohols, C 12 . 18 alcohols, C 20 _ 40 alcohols, C 1-5 alkyl galactomannan, C 18-38 alkyl hydroxystearoyl stearate, C 14-30 glycols, lanolin and the like.
  • the formulation of the invention may also include emollients or skin conditioning agents also described in the publication "International Cosmetic Ingredient Dictionary and Handbook” described above.
  • suitable emollients are canola sterols, avocado sterols, brain lipids, algae extract and the like.
  • the formulation of the invention may also include humectants which are skin conditioning agents that increase the water content of the top layers of the skin. Examples of humectants are described in the "International Cosmetic Ingredient Dictionary and Handbook" publication described above and include agarose, honey, lactose, sea salt, urea and the like.
  • the formulation of the invention may also include occlusive skin conditioning agents that retard the evaporation of water from the skin surface.
  • skin conditioning agents are described in the "International Cosmetic Ingredient Dictionary and Handbook" publication referred to above and are generally lipids that remain on the skin surface. Examples are kernel oils, castor oils, waxes, beeswax, methicone compounds and the like.
  • Preferred formulations of the invention include from 50- 70% lower alkanol, from 1 -5% of the thickening agent and 0.1 -5% of the conditioning and/or anti-static agent and/or emulsion stabilising agent with or without secondary active components.
  • the balance of the formulation is water.
  • An especially preferred formulation is 64% lower alkanol 0.2% conditioning agent and 1 .0% thickening agent.
  • humectants emollients and/or occlusive skin conditioning agents
  • these may be in a concentration of 0.1 -0.5%.
  • Colourants and/or fragrances may be used in a concentration of 0.05-0.2%.
  • the formulation of the invention may be applied to a suitable subject for a period of from 1 -10 minutes. More preferably this period is from 2-5 minutes.
  • a 12 year old female patient was diagnosed as having a severe headlice infection and live eggs and some nymphs were identified in the hair of the patient.
  • the formulation of the invention comprising 64.0% isopropanol, 0.2% quaternary ammonium salt in the form of Ceteareth-12 and 1 .0% gel in the form of Carbomer 940 was applied topically to the hair for 6 minutes and subsequently the hair was combed thoroughly. Thereafter about 100 dead nymphs were identified which were removed. The quantity of lice or nymphs were assessed by combing the hair about 2cm from the scalp to the hair tips and the eggs were allowed to remain. On a follow up visit within seven days, 50 eggs were identified and tested and found to be all dead i.e. they did not snap. Thus in a complete comb through the hair, zero nymphs and zero lice were found. It was also confirmed that no additional treatment had occurred in the interim period.
  • Example 1 A 1 2 year old female was diagnosed with five eggs and some nymphs. This headlice infection had been treated with four different products which were various combinations of Neem Oil, Tea Tree Oil, Permethrin and Maldison over the last 2-3 months.
  • the removal step was carried out by combining through within 2cm from the scalp to the hair tips allowing the eggs within 2cm of the scalp to remain. A follow up visit 7 days later ascertained that no lice were present.
  • a five year old female patient was diagnosed as having a headlice infection with live eggs and some nymphs.
  • the patient had been treated with four different headlice treatments involving active ingredients including pyrethrins, tea tree oil and Maldison over the past 2-3 weeks.
  • active ingredients including pyrethrins, tea tree oil and Maldison over the past 2-3 weeks.
  • After application of the formulation referred to in Example 1 for 5 minutes a subsequent comb through of the hair resulted in approximately 400 dead nymphs and lice being removed.
  • the removal step comprised combing the hair approximately 2cm from the scalp to the tips allowing the eggs within 2cm of the scalp to remain.
  • On a follow up visit 7 days later it was ascertained that no lice were present.
  • the aim of this example was to collect a single population of adult lice from an infestation and subject the lice to a number of different commercially available head lice treatment products.
  • subjects who have significant infestations were sought. None were found with more than 9 adult lice (no nymphs were present as the patients had been treated the previous week with the formulation of Example 1 and it was anticipated that the population selected was due to a re-infestation).
  • Permethrin has been regarded as an effective treatment for some time although resistant populations are known to exist.
  • Foams are considered to be the most effective at penetrating the insect (and eggs).
  • Example 1 The control, and Permethrin subjected lice were randomly subjected to either Example 1 Formulation or Tea Tree Lice Foam that resulted in immediate cessation of movement.
  • the Lice Blaster product was highly effective and the lice were almost certainly fatally dosed, responding only weakly when provoked.
  • the test confirms that the formulations of the invention immobilise lice on contact, and that such formulations compare favourably with popular commercially available products.
  • the test demonstrates that the formulation and presentation of the formulation of Example 1 is equally as effective as the Lice foam in totally immobilising lice.
  • the test also demonstrates that the immobilisation is irreversible over the time period measured.
  • the treatment regime was essentially unchanged for each person screened and real time written records prepared. Individuals contacted the office and initial discussions determined the willingness of the families to participate. Home visits were arranged at mutually convenient times and all family members (present) were screened used the "conditioner and comb" technique. Treatment was applied to the hair and scalp beginning at the fringe and working to the nape of the neck, saturating all hair and scalp. Assessment of the kill was made using a thorough comb through using a lice-meister (or like) comb. Counts and/or estimates of climbers and nymphs were recorded. For the purpose of evaluating nit kill, nits were (on most occasions) allowed to remain within 2cm of the scalp and were not removed using the comb.
  • the formulation of the invention can be used in conjunction with 0.01 -10% and more preferably 0.2-2.0% and most preferably 0.5-1.0% of other secondary active components to increase the knock down rate and thus improve the efficacy of the formulation in use.
  • Suitable secondary active components are essential oils, inclusive of tea tree oil and rosemary oil, natural and synthetic pyrethroids, organophosphates and the like.
  • the ectoparasitic formulation of the invention is effective in use and does not involve the use of toxic components.
  • the formulation of the invention may be used in treatment of acute and chronic external parasitic infections.
  • the therapeutic action of the isopropanol which is the preferred lower alkanol is a function of its intrinsic de-fatting solvency and its volatile nature that results in an azeotropic dehydration activity.
  • the action of alcoholic evaporation is exothermic, drawing heat from the body and thereby providing a cooling effect. Both the cooling effect and the dehydration reaction are prolonged by the adherence of the thickened formulation to the scalp.
  • the addition of the thickening agent has the following effect;
  • the addition of the anti-static and/or hair/skin conditioning agents minimises detrimental loss of "condition", through static build up and moisture loss, both of which could be expected to occur as a result of the de-fatting and dehydrating action of the alcohol.
  • the addition of the emulsion binding and/or stabilising agent is to facilitate shelf life and stability of the compounded alcohol formulation.
  • the pH of the ectoparasite formulation of the invention may be from 4.5-8.5 and more suitably about 5.5-7.5.
  • the dosage is dependant on hair length, but may range from 20-500mls of the formulation.
  • the formulation of the invention contains a lower C C 4 alcohol that the formulation will have a fluid base, which is preferably translucent and non-aqueous, while still being a mobile liquid or semi-solid gel that facilitates the distribution of both active and excipient or non-active components across the treatment area.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Birds (AREA)
  • Medicinal Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une formulation contre les ectoparasites qui est non toxique et efficace en utilisation, cette formulation comprenant entre 20 et 87 % en poids d'un alcanol inférieur renfermant entre 1 et 4 atomes de carbone et entre 0,1 et 2,0 % en poids d'un agent épaississant. Cette formulation peut également contenir entre 0,05 et 20,0 % en poids d'un agent de conditionnement ou d'un agent antistatique ou d'un agent de liaison ou de stabilisation d'émulsion. Une formulation préférée contient de 50 à 70 % d'isopropanol, de 1,0 à 5,0 % d'agent épaississant et de 0,1 à 5,0 % d'agent de conditionnement ou d'agent antistatique ou encore d'agent de liaison ou de stabilisation d'émulsion.
PCT/AU2001/001183 2000-09-21 2001-09-20 Formulation contre les ectoparasites WO2002024182A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001291485A AU2001291485A1 (en) 2000-09-21 2001-09-20 Ectoparasite formulation

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
AUPR0280 2000-09-21
AUPR0280A AUPR028000A0 (en) 2000-09-21 2000-09-21 Ectoparasite formulation

Publications (1)

Publication Number Publication Date
WO2002024182A1 true WO2002024182A1 (fr) 2002-03-28

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PCT/AU2001/001183 WO2002024182A1 (fr) 2000-09-21 2001-09-20 Formulation contre les ectoparasites

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AU (1) AUPR028000A0 (fr)
WO (1) WO2002024182A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006007630A1 (fr) * 2004-07-22 2006-01-26 Jurox Pty Ltd Formulation insecticide/parasiticide aqueuse
CN108245445A (zh) * 2018-02-07 2018-07-06 泉州微聚商贸有限公司 一种用于防治脱发、修复头皮、滋养生发、抗菌祛螨的植物配方洗发乳

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR7800991A (pt) * 1978-02-17 1978-07-18 I Repenning Alcool em pasta
GB2017491A (en) * 1978-03-31 1979-10-10 Landstingens Inkopscentral Ointments containing alcohols
GB2222774A (en) * 1988-09-15 1990-03-21 Euro Celtique Sa Lice control
WO1995025544A1 (fr) * 1994-03-21 1995-09-28 John Brown Thomsen Gel destine au traitement des maladies de la peau et a la desinfection de celle-ci

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR7800991A (pt) * 1978-02-17 1978-07-18 I Repenning Alcool em pasta
GB2017491A (en) * 1978-03-31 1979-10-10 Landstingens Inkopscentral Ointments containing alcohols
GB2222774A (en) * 1988-09-15 1990-03-21 Euro Celtique Sa Lice control
WO1995025544A1 (fr) * 1994-03-21 1995-09-28 John Brown Thomsen Gel destine au traitement des maladies de la peau et a la desinfection de celle-ci

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, vol. 90, no. 1979, Columbus, Ohio, US; abstract no. 76564, NETO RUY NOGUEIRA ET AL.: "Alcohol-containing paste" *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006007630A1 (fr) * 2004-07-22 2006-01-26 Jurox Pty Ltd Formulation insecticide/parasiticide aqueuse
CN108245445A (zh) * 2018-02-07 2018-07-06 泉州微聚商贸有限公司 一种用于防治脱发、修复头皮、滋养生发、抗菌祛螨的植物配方洗发乳

Also Published As

Publication number Publication date
AUPR028000A0 (en) 2000-10-12

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