Classifications

• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N53/00—Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof

Definitions

• the present invention relates to stable and safe incense formulation product containing insecticidal active ingredient Renofluthrin.
• the invention relates to effective products containing Renofluthrin as active ingredient, preferably in incense and burning forms like coils and sticks, wherein the said composition exhibits significant mosquitoes and insect's repellent activity.
• Insecticides of various classes of chemical compounds such as pyrethroids, organophosphates, carbamates, etc. can be applied to control the ' pest species. These chemicals are included in the composition of the insecticidal products as active ingredients.
• the insectoacaricidal formulations are available in the form of containerized aerosols, ready to-use liquids in propellant free package, dustable powders, wettable powders, soluble powders, tablets and granules, emulsions and their concentrates (macro-, micro-, suspoemulsions, flowable and microencapsulated formulations), baits of all the kinds, bait stations, sticky traps, electric heaters with mosquito mats and liquid vaporizers, coils, spirals, incense, crayons, gels, creams, lotions, shampoos etc.
• Incense and burning forms such as coils, cylindrical, spirals, sticks, and other shapes.
• Insecticidal incesnse forms are popular and commonly used household items. All these product types use burning / glowing / smouldering / diffusion / smoke / fumes, to release the active ingredient substance into air. The release of the active ingredient repels or kills target flying insects in households.
• Some incense formulation types use water in the process of manufacture. Burning duration of various incense forms and shapes can range from few minutes to many hours.
• composition of insecticidal incense forms normally include, but not limited to, the following ingredients: a) Fillers: like Brown saw Dust, wood flour, coconut shell powder etc. Sometimes in case of black coil, charcoal is added, along with option of clay dust, calcite dust in the range of 65% to 92% w/w;
• Binders like Starch, Jigget, Guar gum, Tamarind seed powder, etc. in the range of 10% to 22% w/w;
• Burning agent / Smouldering agent like Pottasium nitrate in the range of 0.1% to 0.4% w/w;
• Preservative like Sodium Benzoate in the range of 0.1% to 1 .5% w/w;
• Insecticide active ingredient 0.005% to 3% w/w along with optional addition of emulsifiers / surfactants .
• Incense forms like Coils are placed on a stand before burning.
• Incense forms like incesnse sticks are suppoterd by a stick in the centre (the stick can be made from bamboo or other materials).
• Insecticide active ingredient is mixed with around equal or less quantity of surfactant (emulsifier like alcohol ethoxylates, or any similar Oil and water' surfactants) and stirred for 30 to 40 minutes.
• surfactant emulsifier like alcohol ethoxylates, or any similar Oil and water' surfactants
• smouldering agent like Pottasium nitrate
• Preservative like Sodium Benzoate
• Kneading In this process coil powder (mixture contains saw Dust, Coconut Shell Powder and Binders etc.) and water is added in the Kneader, ingredients are mixed, solution of potassium nitrate and sodium benzoate is added. Further the solution of insecticide active ingredient emulsion and perfume is added to the mixture. Kneading of the mixture to form evenly mixed dough.
• Extrusion, stamping and drying The dough is crushed, extruded and given desired shape of incense. Once incense of desired shape; size and weight is made, they are kept for drying. In case of incense stick, the incense is shaped around a centre stick. Drying can be done at room temperature, by sunlight, or by heating. In some cases, heating is carried out (sometimes with release of moisture) at temperatures of 50° to 85°C. In some cases the incense can also be dried naturally at room temperature indoors or outdoors.
• insecticide active ingredient is not added during the incense ingredients mixing and kneading process. Active ingredient is added by spraying, dosing or dipping after the incense is made and dried. Insecticidal active is added to the finished and shaped incense or to dried incense. Sometimes along with the active ingredient insecticide, perfume can also be added, dosed, sprayed or dipped.
• the weight of the mosquito coil insecticidal incense can be increased or decreased.
• the proportion of the different ingredients in the composition can be varied depending on the needs.
• Emulsifiers / surfactants and their quantity in proportion to the active ingredient can also be adjusted depending on needs. All these changes can vary the burning time, strength, hardness, properties of the incense.
• Insecticidal incense can be in any shape or form like stick, tube, cylindrical, or spiral (like mosquito coils) and others.
• Metofluthrin formulation is applicable to not only existing formulations and devices such as a mosquito coil and a liquid vaporizer, but also various other type products such as a fan vaporizer, a paper emanator and a resin emanator.
• Another Indian patent application No. 8431/DELNP/2011 discloses the mixture of insecticide active ingredient with emulsifiers /surfactants.
• This patent application discloses dilution of the insecticide active ingredient in solvents like D100 (Exxon), and the spraying / dosing of this on incense. It discloses active ingredient compound mixed with surfactants / emulsifiers, along with stabilizers / antioxidants like BHT (Butylated hydroxytoluene) and solvent. This mixture is then used in the preparation of incense.
• Renofluthrin active ingredient 'Renofluthrin' (Application No.4121/MUM/2013) which is found to be effective in home insecticidal formulations. Renofluthrin is found to be effective and practical for use in existing known formulations types and also has potential to adapt for developing new formulations and delivery systems.
• Active ingredient, 'Renofluthrin' is isomeric composition of 2,3,5,6- tetrafluoro-4-(methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2- dimethylcyclopropanecarboxylate , wherein isomers (1R,3S) and (1 S,3R) are present in range of 90% to 99.90% and balance being isomers (1R,3R) and (1 S,3S).
• Renofluthrin is not soluble in solvent D100 (Exxon) and similar solvents. Hence the methods disclosed in the prior art are not suitable to prepare incense and other formulation product forms containing Renofluthrin as active ingredient.
• Other formulation types have their own limitations.
• the MUP manufactured use product
• EC Emsifiable Concentrate
• Other popular formulations used are, Soluble Concentrate (SL), Suspension Concentrate (SC).
• SL Soluble Concentrate
• SC Suspension Concentrate
• the EC / SC / SC formulations are not useful.
• use of EC / SC / SL etc may interfere with the working of the product formulation.
• Emulsifiers / surfactants can affect performance of the product. For example, in case of Aerosol spray forms, it can sometimes cause problem with the valves. In liquid evaporation systems that use a Wick with capillary action, some surfactants / emulsifiers can cause blocks, thereby causing changes in rate of evaporation release affecting performance of the product. The effect and efficacy of the insect repellent (RTU formulation) is reduced when there is block to the release of the active ingredient.
• use of EC / SC / SL has limitations and is not practical and usable for many product types and forms.
• MUP manufacture use product
• SOL01GE solvent used to prepare many different RTU (Ready To Use) product formulations.
• Renofluthrin MUP can contain between 2.5% to 18% w/w of Renofluthrin. For illustration purposes in these examples, Renofluthrin 5% w/w MUP has been mentioned)
• the invention provides a stable insecticidal incense composition containing active ingredient 'Renofluthrin'.
• the invention provides cost effective, simple process for manufacturing the incense composition comprising 'Renofluthrin'.
• Renofluthrin is an isomeric composition of 2,3,5,6-tetrafluoro-4- (methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropane carboxylate, wherein total trans isomers ranging from 90% to 99.90% and total cis isomers ranging from 0.1%) to 10% , having the below structure:
• Renofluthim is found to be effective, when used as insecticide in the manufacture of mosquito repellent and other household pest repellents.
• 'Renofluthrin' has total trans isomers ranging from 90% to 99.90% and rest being cis isomers.
• the invention provides ready-to-use products, solid formulations as insecticidal compositions comprising lower concentration of Renofluthrin, prepared from active ingredient, or technical grade, or from its MUP formulation, having better insecticidal activity.
• the invention provides insecticidal incense containing Renofluthrin, 2,3,5,6-tetrafluoro-4-(methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2- dimethylcyclopropane carboxylate, wherein isomers (1R,3S) and (1 S,3R) are present in range of 90% to 99.90% and the balance being isomers (1R,3R) and (1 S,3S).
• the insecticidal incense compositions comprise 'Renofluthrin' or its diluted forms, including manufacture use product (MUP) and other formulations.
• the Renofluthrin is diluted in solvent or mix of solvents and /or along with emulsifiers/surfactants.
• the insecticidal incense comprises Renofluthrin in the range of 0.005 % to 5% w/w.
• the invention provides insecticidal incense comprising Renofluthrin of various shapes and sizes including coils, spirals, sticks, fumigants, evaporators and other burning or heating forms and other shapes and forms.
• the insecticidal incense according to the invention will have burning duration time ranging from minutes to many hours, in all forms of burning / smouldering / incense etc. causing evaporation / diffusion /release of Renofluthrin in air.
• the insecticide incense composition according to invention comprises Renofluthrin along with fillers, binders, emulsifiers, surfactants, burning agent, preserving agent, color, perfume etc.
• the invention provides a process for preparation of incense containing Renofluthrin which comprises;
• step (b) Adding the ingredient mix of step (b) during kneading to the mix of step (a);
• Renofluthrin directly, or through its diluted formulations, or MUP formulations
• the surfactants / emulsifiers as used in the invention are selected from the group consisting of Nonyl or Octyl Phenol Ethylene and its oxides and condensates, Lauryl alcohol ethoxylates, Lauryl alcohol ethylene oxide condensates, Isotridecyl alcohol ,and its oxylates and condensates, etc.
• the Renofluthrin can be added into the incense composition after the incense composition is made, i.e. after kneading and shaping OR after kneading, shaping and drying.
• Renofluthrin or Renofluthin MUP can be added by spraying or dosing on the incense composition, or by dipping in liquid solution containing Renofluthrin prior to drying.
• the use of emulsifier or surfactant is not required.
• perfume or aroma ingredients can also be dosed or sprayed on incense along with Renofluthrin or Renofluthrin MUP.
• the invention provides insecticidal incense containing Renofluthrin for use in mosquito and other insect control applications.
• the invention provides method of controlling/repelling the mosquitoes and other insects from an area which method comprises treating the area with an incense composition comprising Renofluthrin.
• the invention provides an insect repellent/insect control formulation of Renofluthrin with better efficacy.
• the active ingredient, Renofluthrin, or its MUP (manufacture use product) are used to make various formulations, including insecticidal incense.
• Renofluthrin 5% MUP (containing active ingredient 5% w/w based on purity) or other % w/w dilutions can be used in the preparation of RTU (Ready to Use) formulations and insecticidal incense.
• the invention provides Renofluthrin, the active ingredient or Renofluthrin MUP in the manufacture of different forms of RTU (Ready To Use) formulations and products, including but not limited to, incense, sprays, liquid evaporation systems, and other burning, glowing, smouldering, evaporation products, etc.
• Renofluthrin MUP is a practical and suitable route to prepare various types of RTU formulations.
• 'Renofluthrin' is known to be effective against mosquitoes and other flying insects.
• the instant insecticidal incense formulations of Renofluthrin according to the present invention are selected from the group consisting of mosquito coils, spirals, stick, cylindrical shapes, agarbatti, incense stick, tube shapes, other shapes, fumigants, evaporators and other burning or heating forms and like thereof.
• the products and compositions presented herein are also referred to as insecticidal incense, incense, incense stick (commonly known as 'agarbatti'), incense coil, spirals, mosquito coils, mosquito sticks, etc.
• Renofluthrin used in the insecticidal incense formulations exhibits limited scope of solubility. It is almost insoluble in water and soluble in some hydrocarbon aromatic solvents. However, the aromatic solvents have strong smell and cannot be used in evaporation based insecticides for use in home applications. Even in combinations with other solvents, the smell of aromatic solvent is still dominant, hence cannot be used on regular basis within households. Therefore, Renofluthrin or its MUP formulation has been used to manufacture insecticidal incense compositions. Also, Renofluthrin diluted forms like manufacturing use products (MUP) are ideal for making various types of end use RTU (Ready to use) formulation products for consumer use, including insecticidal incense.
• MUP manufacturing use products
• Renofluthrin MUP liquid composition with active ingredient content between 2.5% to 18% is provided as intermediate or manufacturing use product (MUP) in the preparations of lower concentration insecticidal compositions and formulations.
• 'Renofluthrin' content in the final insecticidal incense composition provided in accordance with the invention can range from 0.005 % to 5% w/w.
• the invention provides a process for preparation of different compositions of insecticidal incense containing Renofluthrin that result in better efficacy. Accordingly, in one embodiment, the invention provides process for preparation of spiral incense or incense coils (commonly known as mosquito coils). In another embodiment, the invention provides process for preparation of incense sticks (commonly known as Agarbatti).
• the process for preparation of insectidal incense containing Renofluthrin comprises of mixing ingredients in desired ratio or percentage (%) weight/weight (w/w) followed by kneading them to form dough. Then the dough is converted into desired shapes such as Spirals / Coils / Stick or other forms. In case of incense sticks, the incense is supported by stick in the centre wherein the stick can be made from bamboo or other materials. Renofluthrin can be added into the composition in various ways. At the stage of kneading to form dough, Renofluthrin can be added directly or can be added through Renofluthrin MUP formulation.
• Preferred forms of addition at kneading stage include mixing Renofluthrin directly, or optionally along with surfactants or emulsifiers, or mixing its MUP formulation directly or optionally along with surfactants or emulsifiers; diluting this mix in water and adding the same to kneader mix.
• Surfactants / Emulsifiers can be chosen from any of the following types including but not limited to Nonyl or Octyl Phenol Ethylene and its oxides and condensates, Lauryl alcohol ethoxylates, Lauryl alcohol ethylene oxide condensates, Isotridecyl alcohol ,and its oxylates and condensates, etc. Many of these are commonly used in the manufacture of insecticidal incense.
• Renofluthrin can be added in incense composition after the incense composition is made, i.e. after kneading and shaping OR after kneading, shaping and drying.
• the emulsifier or surfactant may not be required.
• Renofluthrin or Renofluthin MUP, or diluted Renofluthrin can be sprayed or dosed on the incense composition.
• the insecticidal incense can also be dipped in liquid solution containing Renofluthrin and then dried. Additionally or as an option, perfume or aroma ingredient can also be dosed or sprayed on incense along with Renofluthrin or Renofluthrin MUP.
• the final insectidal incense composition should preferably contain 0.005 % to 5% w/w of Renofluthrin.
• These incense composition may be provided in various shapes like coils, spirals, sticks and other shapes.
• the burning time duration of thse insecticidal incense may vary from a few minutes to many hours, depending on the size, weight and shape of the incense composition.
• the invention provides insecticidal incense containing Renofluthrin for use in mosquito and other insect control applications.
• the invention provides method of controlling/repelling mosquitoes and other insects from an area which method comprises treating the area with an incense composition comprising Renofluthrin.
• Renofluthrin 5% MUP added in incense mixture at kneading stage, to make incense containing 0.025% w/w Renofluthrin.
• Renofluthrin 5% MUP added in incense mixture at kneading stage, to make incense containing 0.05% w/w Renofluthrin.
• Quantity 1% w/w of Renofluthrin 5% MUP, (i.e. 1% of total incense weight) along with equal quantity of surfactant/emulsifier was mixed. This mix was further diluted in equal quantity of water , and added in the incense mixture dough during kneading. This composition after kneading, extruding, shape and drying, gives insecticidal incense containing Renofluthrin 0.05% w/w.
• perfume or aroma ingredient can also be mixed with the MUP and sprayed on incense
• Renofluthrin diluted solution added in stick shape incense, to make incense containing 1% w/w Renofluthrin
• Renofluthrin added in stick shape incense, to make incense containing 0.5 % w/w Renofluthrin
• Incense stick is prepared.
• perfume or aroma ingredient(s) is added in these sticks (agarbatti), by diluting the perfume in solvents or phthalate esters (like dibutyl phthalate or diethyl phthalate).
• the said addition is done either by dipping the sticks in diluted perfume solution or by spraying diluted perfume solution on the sticks, and then drying the same.
• Renofluthrin is directly added in diluted perfume solution and stirred well to make it clear solution.
• the incense sticks are then dipped in this diluted solution. Sticks are removed and dried.
• Increase in weight of the incense sticks can be used to estimate % w/w of Renofluthrin content in incense stick. For example, in the diluted perfume solution if Renofluthrin 3% w/w is added, and incense stick weighing 1.50 grams is dipped in this liquid solution. If weight of incense sticks increases to 1.80 grams, this gives insecticidal incense stick containing Renofluthrin 0.5 % w/w. Similar dosing can also be carried out by spraying on the incense sticks.
• An incense composition containing 0.1% w/w d-trans allethrin was prepared.
• Another incense of same total weight, containing 0.025%) w/w Renofluthrin was prepared. Content of Renofluthrin is 4 times lower than d-trans allethrin in the incense composition.
• Lower insecticide active content makes the incense safer, and also gives economic advantage.
• the effectiveness / efficacy of mosquito repellent formulation is normally measured in "Knock-down time" (KT) in minutes of percentage of the test population of mosquitoes i.e. KT50 values, referring to knock down time of 50% of the test insects quantity. Lower the time in minutes required for KT50, higher the effectiveness of the insecticide. Results can vary based on study conditions, mosquito species, and protocols. Both the incense compositions prepared are tested on two species of mosquitoes in 'Peet Grady Chamber' and the KT50 measured are presented in the below table 1 .
• the incense compositions containing Renofluthrin at much lower concentration shows much better and faster effect on both species of mosquitoes, compared to incense containing d-trans allethrin.
• Faster knock down action is important for protection of people from mosquito bites.
• the content of 'Renofluthrin' in incense is 4 times lower than content of 'd-trans allethrin' in incense. Even at four times lower content, Renofluthrin exhibits higher effect on mosquitoes than the most common and widely available 'd-trans allethrin' incense mosquito coil in India.

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• Life Sciences & Earth Sciences (AREA)
• Agronomy & Crop Science (AREA)
• Pest Control & Pesticides (AREA)
• Plant Pathology (AREA)
• Health & Medical Sciences (AREA)
• Engineering & Computer Science (AREA)
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• General Health & Medical Sciences (AREA)
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Cited By (2)

• 2015
  • 2015-11-26 IN IN3405MU2015 patent/IN2015MU03405A/en unknown
  • 2015-11-26 MX MX2018001743A patent/MX391341B/es unknown
  • 2015-11-26 MY MYPI2017704194A patent/MY184807A/en unknown
  • 2015-11-26 WO PCT/IN2015/000437 patent/WO2017037726A1/en not_active Ceased
• 2018
  • 2018-03-01 ZA ZA2018/01435A patent/ZA201801435B/en unknown

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