DESC:RENOFLUTHRIN INDOOR SPACE SPRAY COMPOSITION

FIELD OF THE INVENTION
The present invention relates to a novel indoor space spray composition comprising pyrethroid
insecticide as an active ingredient. Particularly, the present invention relates to a novel and
5 effective insecticidal composition comprising Renofluthrin alone or in combination with at
least one another insecticide for delivery via aerosol or trigger spray or single push, wherein
the said composition exhibits significant flying and crawling insect control activity.
BACKGROUND OF THE INVENTION
Pest control in and around the home is a never-ending issue. Mosquitoes and other crawling
10 and flying insects need to be controlled to avoid the spread of vector-borne diseases. Flying
insects such as mosquitoes, flies and the like, and crawling insects such as cockroaches and red
ants are known to carry disease causing bacteria on their bodies. Flying insects cause great
human sufferings and is a global problem. Diseases like malaria, filariasis, chikungunya,
Dengue fever, yellow fever, Japanese encephalitis, Ross River virus, Burma forest virus,
15 Murray Valley encephalitis etc, are known to spread through mosquitoes. Crawling insects,
such as ants and cockroaches, are also responsible for health problems. Cockroaches may play
a role as carriers of intestinal diseases, such as diarrhoea, dysentery, typhoid fever and cholera.
In addition, control of dust mites cannot be neglected as they are the most common indoor
allergens. They are tiny organisms that can barely be seen by naked eye and feed on house dust
20 and moisture in the air. They are potentially capable of triggering asthma in humans.
Spray cans, oil sprays, mosquito coils, and slow-release vaporising systems including mats and
liquid vaporisers are the most commonly utilized techniques to control household insect
menace. Neem oil, Pyrethrin, Malathion, and carbaryl are all common household pesticides.
However, prolonged exposure to the odour or toxic chemical emissions from commonly
25 available commercial pesticide products may constitute a health risk. Negative health effects
from overexposure and an increase in vector resistance to these commonly used insecticides is
a matter of concern.
Pyrethrum is an insecticide of natural origin, and is endowed with very positive characteristics,
such as high insecticide activity and a very low toxicity for mammals. However, natural

3

pyrethrum is readily oxidized by air in the presence of light (photooxidation) and is easily
degraded, and therefore it is not suited for insecticidal applications.
Numerous compounds have been synthetized, which have a slightly modified structure of
natural pyrethrum, in order to preserve the insecticide action and cause low toxicity to
5 mammals.
Whilst some of these compounds (synthetic pyrethroids) possess the characteristics mentioned
above, conventionally used aerosol compositions may have high flammability, inhalational
toxicity and may cause damage to the environment due to the need of formulating at a
perpetually higher active concentration. The aerosols are designed to work even in closed
10 spaces hence the risk of being exposed to such high amount of insecticidal composition can be
perceived as a risk to health of the user. Thus, it is necessary to formulate a suitable composition
having improved efficacy along with protecting the molecules as much as possible from photo-
oxidation, ensuring a high persistence of the insecticide action at lower concentration of active.
Recently, the inventors of IN4121/MUM/2013 have developed an active ingredient
15 'Renofluthrin' which is found to be effective in-home insecticidal formulations. Renofluthrin is
found to be effective and practical for use in existing known formulation types and also has the
potential to adapt for developing new formulations and delivery systems. Active ingredient,
'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 (1R, 3S
20 and1S, 3R in native form and almost in equal amounts) ranging from 90% to 99.90% and total
cis isomers (1R, 3R and 1S, 3S in native form and almost in equal amounts) ranging from 0.1%
to 10%.
Hitherto, there is a need in the art to formulate an indoor space spray composition which is
safer to use and economically advantageous. These objectives can be achieved by providing an
25 insecticidal composition that can achieve improved knock down efficacy at lower amount of
active as compared to the conventionally used insecticides.
Moreover, there is a further need in the art for an insecticidal pyrethroid composition that has
both insecticidal as well acaricidal properties.
Therefore, the present invention aims to overcome the problems in the prior art and provide a
30 stable and effective indoor space spray composition comprising Renofluthrin alone or in
combination with other insecticides/acaricides known in the art.

4

OBJECTS AND ADVANTAGES OF THE INVENTION:
It is the main object of the present invention to provide a novel and effective pesticidal
composition comprising Renofluthrin.
It is another main object of the present invention to provide a novel and effective indoor space
5 spray composition comprising Renofluthrin alone.
It is another main object of the present invention to provide a novel and effective insecticidal
indoor space spray composition comprising Renofluthrin in combination with at least one
another insecticide/acaricide.
It is another object of the present invention to provide a novel and effective composition that
10 can be used to control/kill mosquitoes, insects and mites.
It is another object of the present invention to provide a novel and effective composition that
provide broad spectrum pesticidal control in household application.
It is another object of the present invention to provide a novel and effective composition that
can exhibit both acaricidal as well as insecticidal properties.
15 It is another object of the present invention to provide a novel and effective composition that
can act as a ‘Crawling Insect Killer’ (CIK) and a ‘Flying Insect Killer’ (FIK)
It is another object of the present invention to provide a novel and effective composition that
is safe to use.
It is another object of the present invention to provide a novel and effective composition that
20 shows lower inhalational toxicity.
It is another object of the present invention to provide a novel and effective composition that
can be formulated easily.
It is another object of the present invention to provide a novel and effective composition that
is ‘Ready to Use’.
25 In is another object of the present invention to provide a novel effective composition that can
be formulated as an aerosol or trigger spray or single push spray.
It is another object of the present invention to provide a novel and effective composition that
is economically preferrable.

5

It is another object of the present invention to provide a novel and effective composition that
uses lower concentration of actives as compared to the conventional formulations.
It is another object of the present invention to provide a novel and effective insecticidal
composition that shows better knock down efficacy over conventionally known aerosol
5 compositions.
It is yet another object of the present invention to provide a novel and effective composition
that is stable upon storage at room temperature.
Some or all these and other objects of the invention can be achieved by way of the invention
described hereinafter.
10 SUMMARY OF THE INVENTION
Accordingly, the present invention relates to a novel and effective pesticidal indoor space spray
composition comprising:
a) Renofluthrin alone or in combination with at least one another insecticide selected from
Cypermethrin, Permethrin, Fipronil, Deltamethrin, Lambda Cyhalothrin and
15 Imiprothrin; and
b) One or more chemically acceptable excipients.
In one embodiment of the present invention, the novel pesticidal composition is an insecticidal/
acaricidal single push spray composition.
In one embodiment of the present invention, the novel pesticidal composition is an insecticidal/
20 acaricidal trigger spray composition.
In one embodiment of the present invention, the novel pesticidal composition is an insecticidal/
acaricidal aerosol composition.
In another preferred embodiment of the present invention, the novel pesticidal composition is
an insecticidal/ acaricidal aerosol composition.
25 In another preferred embodiment of the present invention, the pesticidal composition
comprises:
a) Renofluthrin present in an amount ranging from 0.02% to 2% by weight of the total
composition; and

6

b) One or more chemically acceptable excipients selected from a group comprising of
solvent, propellant, perfume, synergist, antioxidants, corrosion inhibitor sand pH
buffers.
In yet another preferred embodiment of the present invention, the pesticidal composition
5 comprises:
a) Renofluthrin present in an amount ranging from 0.02% to 2% by weight of the total
composition in combination with at least one another insecticide selected from
Cypermethrin, Permethrin, Fipronil, Deltamethrin, Lambda Cyhalothrin and
Imiprothrin, present in an amount ranging from 0.05% to 2% by weight of the total
10 composition; and
b) One or more chemically acceptable excipients selected from a group comprising of
solvent, propellant, perfume, synergist, corrosion inhibitors and pH buffers.
In another preferred embodiment of the present invention, the pesticidal composition
comprises:
15 a) Renofluthrin present in an amount ranging from 0.02% to 2% by weight of the total
composition in combination with Cypermethrin present in an amount ranging from
0.05% to 2% by weight of the total composition; and
b) One or more chemically acceptable excipients selected from a group comprising of
solvent, propellant, perfume, synergist, corrosion inhibitors and pH buffers.
20 In one embodiment of the present invention, the pesticidal composition comprises:
a) A synergistic combination of Renofluthrin and at least one another insecticide selected
from Cypermethrin, Permethrin, Fipronil, Deltamethrin, Lambda Cyhalothrin and
Imiprothrin; and
b) One or more chemically acceptable excipients selected from a group comprising of
25 solvent, propellant, perfume, synergist, corrosion inhibitors and pH buffers.
In yet another embodiment, the present invention provides a process of preparation of the
pesticidal composition comprising:
a) Renofluthrin alone or in combination with at least one another insecticide selected from
Cypermethrin, Permethrin, Fipronil, Deltamethrin, Lambda Cyhalothrin and
30 Imiprothrin; and

7

b) One or more chemically acceptable excipients.
In another preferred embodiment of the present invention, the pesticidal composition comprises
Renofluthrin or 2,3,5,6-tetrafluoro-4- (methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2-
dimethylcyclopropane carboxylate , wherein total trans isomers (1R, 3S and1S, 3R in native
5 form and almost in equal amounts) ranging from 90% to 99.90% and total cis isomers (1R, 3R
and 1S, 3S in native form and almost in equal amounts) ranging from 0.1% to 10% as an active
ingredient.
In another preferred embodiment of the present invention, the pesticidal composition comprises
a combination Renofluthrin and/or Cypermethrin as active ingredients.
10 In another preferred embodiment of the present invention, the present pesticidal composition
comprises a synergistic combination of Renofluthrin and Cypermethrin.
In a further embodiment of the present invention, the pesticidal composition is used as a
repellent against mosquitoes, insects and mites.
In a further embodiment of the present invention, the indoor space spray composition is used
15 to effectively control/kill mosquitoes, insects and mites.
In a further embodiment of the present invention the aerosol composition can be sprayed by an
aerosol spray device comprising a pressurised container holding a liquid to be discharged from
the device by a liquified gas propellant along with the spray discharge assembly. The spray
discharge assembly mounted on the container comprises a valve stem, a spray outlet and a flow
20 conduit.
In still another embodiment of the present invention, the present aerosol composition is a Ready
to Use formulation for repelling/ controlling mosquitoes, insects and mites in the indoor space.
In a further embodiment of the present invention the trigger spray composition can be sprayed
by a spray device that does not contain propellant instead comprises an alcohol based suitable
25 solvent.
In still another embodiment of the present invention, the present trigger spray composition is a
Ready to Use formulation for repelling/ controlling mosquitoes, insects and mites in the indoor
space.

8

DETAILED DESCRIPTION OF THE INVENTION
Discussed below are some representative embodiments of the present invention. The invention
in its broader aspect is not limited to the specific details and representative methods. The
illustrative examples are described in this section in connection with the embodiments and
5 methods provided. The invention according to its various aspects is particularly pointed out
when read in view of this specification and appropriate equivalents.
All technical and scientific terms used herein have the same meanings as commonly understood
by someone ordinarily skilled in the art to which the present subject matter belongs. It is to be
noted that, as used in the specification, the singular forms "a", "an" and "the" include plural
10 referents unless the context clearly dictates otherwise. Thus, for example, reference to a
composition containing “a compound” may include a mixture of two or more compounds. It
should also be noted that the term “or” is generally employed in its sense including “and/or”
unless the context clearly dictates otherwise.
The expression of various quantities in terms of “% w/w” or “%” means the percentage by
15 weight, relative to the weight of the total formulation or composition unless otherwise
specified.
The term “indoor space spray” as used herein refers to compositions with or without propellants
including aerosol, trigger spray or single push spray formulations.
The term “insect” as used herein refers to flying and/or crawling insects and other insects in
20 the public hygiene area including but not limited to all the species of mosquito, housefly, sand
fly, stable and face fly, cockroaches, ants, mites, etc.
The term “control” as used herein refers to kill, knockdown and/or repel mosquitoes, other
insects and flies.
The term “active ingredient” (a.i.) or “active agent” used herein refers to that component of the
25 composition responsible for control and killing of mosquitoes, other insects and flies.
The term “formulation” and “composition” as used herein conveys the same meaning and can
be used interchangeably.
The term “knock-down” as used herein conveys knockdown in insects following application
of an insecticide which may be defined as the state of intoxication and partial paralysis which
30 usually precedes death.

9

The term “MUP” as used herein refers to any pesticide product other than an end use product.
The product may consist of the technical grade of active ingredient only or may contain inert
ingredients such as stabilizers or solvents.
The term “RTU” as used herein refers to Ready to Use Formulation.
5 The term “Peet-Grady Chamber test”, as used in the present invention means a standardized
procedure for the evaluation and testing of insect control compositions or products. In the case
of flying insects, the knock-down percentage is determined after subjecting the insects to the
composition for 60 minutes as recommended by the World Health Organisation’s guidelines
for evaluation of pesticides.
10 The term “Bio-efficacy”, as used in the present invention means efficacy of an insect control
composition or an insect control product to knockdown or kill a determined type of insect.
In line with the above objective, the invention provides a novel and effective pesticidal
composition comprising active ingredient 'Renofluthrin', wherein Renofluthrin is present alone
or in combination with at least one another insecticide. In another embodiment, the invention
15 provides cost effective, simple process for manufacturing the composition comprising
'Renofluthrin'.
Renofluthrin is an isomeric composition having CAS.RN-352271-52-4, The IUPAC name is
2,3,5,6-tetrafluoro-4- (methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropane
carboxylate , wherein total trans isomers (1R, 3S and1S, 3R in native form and almost in equal
20 amounts) ranging from 90% to 99.90% and total cis isomers (1R, 3R and 1S, 3S in native form
and almost in equal amounts) ranging from 0.1% to 10%.
Chemical structure of Renofluthrin is represented below:

Renofluthrin
25 Renofluthrin or RNF is a pyrethroid ester insecticide for controlling mosquitoes and other
insects in household spaces. In one embodiment of the present invention, the present
insecticidal composition is a ready-to-use aerosol/ trigger spray formulation product

10

comprising lower concentration of Renofluthrin, prepared from active ingredient, or technical
grade, or from its MUP formulation.
In another embodiment of the present invention, the present pesticidal composition comprises
Renofluthrin OR 2,3,5,6-tetrafluoro-4- (methoxymethyl)benzyl3-(2,2-dichlorovinyl)-2,2-
5 dimethylcyclopropane carboxylate ,wherein total trans isomers (1R,3Sand1S,3R in native form
and almost in equal amounts) ranging from 90% to 99.90% and total cis isomers (1R, 3R and
1S, 3S in native form and almost in equal amounts) ranging from 0.1% to 10%.
According to the main embodiment of the present invention, the pesticidal composition is an
indoor space spray composition comprising of Renofluthrin alone or in combination with at
10 least one another insecticide.
According to still another embodiment of the present invention, the indoor space spray
composition can be formulated as aerosol, trigger spray and single push spray formulation.
In yet another embodiment of the present invention, the present pesticidal composition is an
insecticidal aerosol composition comprising 'Renofluthrin' alone or in combination with at least
15 one another insecticide.
In still another embodiment of the present invention, Renofluthrin is diluted in solvent or mix
of solvents and /or along with emulsifiers/surfactants.
In yet another embodiment of the present invention, the present pesticidal composition is an
insecticidal trigger spray composition comprising Renofluthrin alone or in combination with
20 at least one another insecticide.
In yet another preferred embodiment of the present invention, the novel pesticidal composition
comprises Renofluthrin in an amount ranging from 0.02% to 2% by weight of the total
composition.
In yet another preferred embodiment of the present invention, the novel pesticidal composition
25 comprises a combination of Renofluthrin and at least one another insecticide selected from
Cypermethrin, Permethrin, Fipronil, Deltamethrin, Lambda Cyhalothrin and Imiprothrin. In
still another preferred embodiment the at least one another insecticide is Cypermethrin.
In still another preferred embodiment of the present invention, the novel aerosol composition
comprises of a combination of Renofluthrin and Cypermethrin along with one or more suitable
30 and chemically acceptable excipients.

11

In still another preferred embodiment of the present invention, the novel trigger spray
composition comprises of a combination of Renofluthrin and Cypermethrin along with one or
more suitable and chemically acceptable excipients.
In another embodiment of the present invention, the at least one another insecticide is present
5 in an amount ranging from 0.05% to 2% by weight of the total composition.
In another embodiment of the present invention, the chemically acceptable excipients include
one or more of, but are not limited to antioxidants, perfume, propellant, anti-foaming agent,
wetting agent, antimicrobial/anti-bacterial agent, adjuvants, synergists, fillers, preservatives,
buffering agent and solvent thereof.
10 In still another embodiment of the present invention, the solvent is selected from but not limited
to Isopropyl alcohol, Tri-propylene glycol, Mono-methyl ether, Ethylene glycol D-methyl
ether, Butyl cortisol, Hydroseal, Ketrul d-80, Deodorised kerosene, or combinations thereof.
In still another embodiment of the present invention the surface active agents are selected from
but not limited to fatty acid ester, sorbitan fatty acid ester (Lubricit™ SMO), alkyl alcohol
15 ethoxylate (Alkamuls® AL-CS 20, Alkamuls® AL-CS 25), or combinations thereof
In still another embodiment of the present invention, the propellant is selected from but not
limited to nitrogen, butane, isobutane, propane, hydrofluorocarbon, or combinations thereof.,
Liquified Petroleum gas, etc.
In still another embodiment of the present invention, the synergist is selected from but not
20 limited to piperonyl butoxide, N-octyl bicycloheptene dicarboximide, propargyl propyl phenyl
phosphonate, etc.
According to yet another embodiment, the present invention may comprise corrosion inhibitor
such as sodium benzoate.
According to yet another embodiment the present invention may comprise anti-oxidant such as
25 ethoxyquin or tertiary butylhydroquinone (TBHQ)
In another embodiment of the present invention, the pesticidal composition comprises perfume
present in an amount ranging from 0.1% to 1% by weight of the total composition.
In another embodiment of the present invention, the pesticidal composition comprises solvent
present in an amount ranging from 30% to 99% by weight of the total composition.

12

In another embodiment of the present invention, the pesticidal composition comprises
propellant present in an amount ranging from 0% to 70% by weight of the total composition.
In another embodiment of the present invention, the pesticidal composition comprises synergist
present in an amount ranging from 0% to 2% by weight of the total composition.
5 In yet another embodiment of the present invention, the indoor space spray composition may
or may not comprise a propellant.
In another embodiment of the present invention, the indoor space spray composition controls
household mosquitoes, flies, insects, cockroaches, ants and mites.
In another embodiment, the process of manufacturing the aerosol composition of the present
10 invention is disclosed which comprises:
Manufacturing Process Flow Chart

A) Method of Manufacturing Renofluthrin Aerosol Formulation:

B) Method of Manufacturing Renofluthrin + Additional Insecticide Aerosol
Formulation:

13

Aerosol Manufacturing Process
1. Charge Weighed quantity of Solvent in premix preparation Tank.
2. Charge required weighed quantity of RNF MUP alone or in combination with at least
5 one another insecticide under stirring.
3. Charge required weighed quantity of Perfume under stirring.
4. Stir the mixture for 2 Hrs for uniform solution.
5. Check the Solution sample for Appearance, Active Ingredient content & density.
6. If it is Ok, then fill the Cans with premix known Quantity in gm.
10 7. Fix the Valve and fill known quantity of LPG.
8. Check the weight of the can for final Packing.
Toxicity Profile of Renofluthrin
In an insecticide / pesticide compound, toxicity and efficacy play a vital role. New insecticide
compounds are based on their effect on target pests and their Toxicology profile.
15 Acute Inhalation Toxicity:
In mosquito repellent and flying insect repellent products, Inhalation Toxicity is very
important. Most flying insect repellent products are based on evaporation and vapours of the
active ingredient. Household insecticide product forms like coils, mats, aerosol sprays, trigger
sprays, liquid evaporators, other forms of burning and vaporising formulations are based on
20 evaporation of the active ingredient. Concentration in air of the insecticide and its evaporation
are the most important aspects in flying insect repellent product.

14

Inhalation toxicity is measured in 'Lethal concentration' LC50 values. LC50 (lethal
concentration) is expressed as weight of test substance per standard volume of air (i.e. mg / L).
Higher the mg/L value of LC50, lower the inhalation toxicity and safer the product.
Known insecticide compounds with similar mode of action have the following reported LC50
5 values:
• Insecticide 'Prallethrin' LC50 is 0.658 mg/L (reported in literature in unit of measurement 658
mg/m3 which in mg/L is 0.658)
• Insecticide 'Transfluthrin' LC50 is 0.513 mg/L (reported in literature in unit of measurement
513 mg/m3 which in mg/L is 0.513)
10 • Insecticide 'Metofluthrin' LC50 is reported as > 1.08 and < 1.96 mg/L
These results are published and reported for the respective insecticides.
Acute Inhalation Toxicity Study of Renofluthrin was performed in Rats as per OECD guideline
No. 403. In Globally Harmonized System of Classifications and Labelling of Chemicals
(GHS), for Dust & mists (mg/1), the insecticide 'Renofluthrin' of the present invention falls in
15 category 4 which is > 1.0 and < 5 mg/L.
The insecticide 'Renofluthrin' of the present invention has LC50 greater than 3.81 mg/L. which
shows that Renofluthrin has the lowest Inhalation toxicity amongst all the compounds
commonly used as active ingredient in household insecticide products.
Bio-efficacy and activity of pesticidal aerosol composition comprising Renofluthrin and
20 its Combination.
The comparative, bio-ef?cacy of Reno?uthrin aerosol composition, on target pests has been
established vis-a-vis commonly marketed aerosol composition containing d-Trans Allethrin
and Transfluthrin”. Mosquito species ‘Aedes aegypti’ is a major vector of dengue fever,
chikungunya and yellow fever viruses, and other viral diseases. The effectiveness and ef?cacy
25 of the present aerosol composition was tested using a Peet Grady chamber.
The effectiveness / ef?cacy 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
30 on study conditions, mosquito species, and protocols.

15

A comparative study for bio-efficacy evaluation of the aerosol composition of the present
invention versus other aerosol compositions known in the art was conducted against ‘Aedes
aegypti’ species of mosquitoes and German cockroach; and the results obtained are presented
in the tables below:
1) Bioefficacy comparison of d-Trans Allethrin 0.25% Aerosol and Renofluthrin 0.03%
Aerosol against Aedes aeygypti in Peet Grandy chamber
5 Method: Experiments were conducted with 2 replicates for each aerosol against mosquitoes,
Aedes aegypti. The aerosol was primed in fume hood/out of the test area for 2-3 times before
testing. After priming, pre weight of the aerosol can was recorded. 0.65 ± 0.10g discharge of
the formulated product was sprayed in a single application towards the centre of the chamber
through a port provided at one of the side walls of the chamber. The knock down observations
10 were recorded at 1 minute interval up to 10 mins followed by 2 mins interval till 20 mins and
thereafter 5 mins interval till 60 minutes.
Table 1: Bioefficacy comparison of d-Trans Allethrin 0.25% Aerosol and Renofluthrin
0.03% Aerosol against Aedes aeygypti in Peet Grandy chamber
Sr. No. Product Information Parameter Knock Down Time
in Mins.
1. d-Trans Allethrin 0.25% Aerosol KT50 7.20
KT90 10.71
2. Renofluthrin 0.03% Aerosol KT50 6.41
KT90 10.66

15 Result: From the table above, it is evident that Renofluthrin aerosol formulation showed better
effect as compared to d-trans allethrin aerosol formulation. The knock down time for both 50%
and 90% of mosquitoes was lesser in Renofluthrin as compared to d-Trans allethrin at an active
concentration of 0.03% as against 0.25%.
Thus, Renofluthrin 0.03% Aerosol demonstrates excellent efficacy at a lower concentration of
20 active.
2) Initial and Residual Bioefficacy testing of Aerosols against Free Flying, Aedes aegypti
mosquitoes in Peet Grandy chamber.

16

Method: mosquitoes were released in the Peet Grady chamber and post acclimatisation period
the aerosol product were sprayed @ 0.65 grams ± 0.1 grams and knockdown readings were
recorded up to 60 minutes and the data was plotted to calculate the KT50 and KT 90 values
using SPSS software. The product was sprayed once and the readings were recorded after 0
5 (Fresh), after 4 hours, after 8 hours and after 10 hours from start of spray and the residual
efficacy was evaluated.
Table 2: Initial and Residual Bioefficacy testing of RNF 0.05% Aerosol, RNF 0.03% +
CYPERMETHRIN 0.1% Aerosol & Transfluthrin (TFT) 0.08% Aerosol against Free
Flying, Aedes aegypti mosquitoes in Peet Grandy chamber
Time
Points
(Hours)

Test Parameters RNF
0.05%
Aerosol

RNF 0.03% +
CYPERMETHRIN
0.1% Aerosol

TFT 0.08%
Aerosol
0 KT 50 in Minutes 6.17 6.78 7.08
KT 90 in Minutes 9.06 9.31 11.23
% Mortality After
24 Hrs

100.00 100.00 100.00
4 KT 50 in Minutes 20.67 22.29 20.28
KT 90 in Minutes 33.96 37.97 37.35
% Mortality After
24 Hrs

100.00 100.0 100.00
8 KT 50 in Minutes 27.01 33.22 35.46
KT 90 in Minutes 47.90 51.52 61.96
% Mortality After
24 Hrs

100.00 100.00 98.00
10 KT 50 in Minutes 28.98 39.91 41.15
KT 90 in Minutes 50.05 67.68 74.58
% Mortality After
24 Hrs

100.00 97.00 92.00

Result:
10 TFT 0.08% Aerosol shows residual protection up to 4 hours.
RNF 0.03% + CYPERMETHRIN 0.1% Aerosol shows residual protection up to 8 hours.
Residual efficacy is the highest for RNF 0.05% Aerosol formulation i.e. until 8 to 10 hours.

17

100% mortality is seen up to 10 hours for RNF 0.05% aerosol under test condition, however,
for RNF 0.03% + CYPERMETHRIN 0.1% Aerosol it is up to 8 hours, similarly for TFT 0.08%
Aerosol formulation it is up to 4 hours only.
Thus, RNF 0.05% Aerosol shows enhanced residual protection against mosquitoes tested.
3) Bioefficacy of Aerosols RNF 0.05%, RNF 0.03% + CYPERMETHRIN 0.1% and
Deltamethrin 0.02% + Allethrin 0.13% Samples against German Cockroach on Cement
surface
Method: The product was sprayed on cement panel and after drying 10 cockroaches were
exposed on the panels with two replicates and the mortality was checked after 30 minutes of
exposure and after 4 hours and 24 hours while in holding condition.

Table 3: Bioefficacy of Aerosol Samples against German Cockroach on Cement surface
KNOCK DOWN AND MORTALITY PERCENTAGE ON CEMENT SURFACE AGAINST
CRAWLING INSECTS *
Species RNF 0.05% Aerosol

RNF 0.03% +
CYPERMETHRIN 0.1%
Aerosol

Deltamethrin 0.02% +
Allethrin 0.13% Aerosol

Treatment/Control Treatment Untreated

control Treatment

Untreated
control Treatment

Untreated
control
% KD at 30Minutes 10.00 0.00 10.00 0.00 0.00 0.00
% KD at 4 Hours 15.00 0.00 30.00 0.00 10.00 0.00
% Mortality at 24
Hrs. 30.00 0.00 80.00 0.00 55.00 0.00
Mean Weight Loss
(g.) 0.72 0.70 0.72
Note: Mean of Two Replicate
5
Result:
RNF 0.05% Aerosol formulation showed 30% mortality at 24 hrs.
However, RNF 0.03% + CYPERMETHRIN 0.1% Aerosol formulation showed enhanced
efficacy with 80% mortality as compared to Deltamethrin 0.02% + Allethrin 0.13% Aerosol
(55% mortality at 24 hrs.) already known in the art.
10 Thus, Renofluthrin 0.03% + CYPERMETHRIN 0.1% Aerosol formulation demonstrates
excellent control of crawling insects even at low doses of actives.

18

4) Bioefficacy of Aerosols RNF 0.05%, RNF 0.03% + Cypermethrin 0.1% and
Deltamethrin 0.02% + Allethrin 0.13% Samples against German Cockroach using
direct spray knockdown method

5 Method: Five Cockroaches were contained in a SS mesh bullet of 6 inches having two sides
SS Mesh and were placed in the chamber at a predetermined distance and the aerosol products
were sprayed on the bullet. 100% Mortality was observed and recorded in seconds; and 24
hours revival data if any, was recorded.
Sr.
No.

Treatment Details Parameters
Weight loss
(g)

100% KD
time in sec.

% 24 Hours
Mortality
1. RNF 0.05% Aerosol 0.68 232 100
2. RNF 0.03% +
CYPERMETHRIN 0.1%
Aerosol

0.66 161 100

3. Deltamethrin 0.02% +
Allethrin 0.13% Aerosol

0.68 167 100

4. Untreated control NA > 5 Min. NA

10 Result: 100% mortality was at par for all the 3 Treatments. However, 100% KD was observed
in 161 seconds for RNF 0.03% + Cypermethrin 0.1%. Thus, RNF 0.03% + Cypermethrin 0.1%
demonstrated excellent control in least time.
Examples
A) Composition of 0.04 % Renofluthrin Aerosol Formulation from Technical:
Sr.No. Ingredients % in Aerosol w/w
1 Renofluthrin Technical 0.04
2 Perfume 0.30
3 Ketrul d-80 (solvent) 39.65
4 LPG Q.S
15
B) Composition of 0.04 % Renofluthrin Aerosol Formulation from 5% MUP:
Sr.No. Ingredients % in Aerosol w/w
1 Renofluthrin 5% MUP 0.80

19

2 Perfume 0.30
3 Solvent 38.90
4 LPG Q.S

C) Composition of 0.10 % Renofluthrin Aerosol Formulation from Technical:
Sr.No. Ingredients % in Aerosol w/w
1 Renofluthrin Technical 0.10
2 Perfume 0.30
3 Solvent 39.60
4 LPG Q.S

5 D) Composition of 0.04 % Renofluthrin + 0.10 % Cypermethrin Aerosol Formulation:
Sr.No. Ingredients % in Premix w/w % in Aerosol w/w
1 Renofluthrin 0.10 0.04
2 Cypermethrin 0.25 0.10
2 Perfume 0.75 0.30
3 Solvent 98.90 39.56
4 LPG - Q.S

E) Composition of 0.04% Renofluthrin + 0.10% Cypermethrin Trigger Spray
Formulation:
Sr. No. Ingredients % in Trigger Spray
w/w
1 Renofluthrin 0.04
2 Cypermethrin 0.10
3 Perfume 0.30
4 Synergist 1
5 Solvent Q.S

10 From the foregoing it will be observed that numerous modifications and variations can be
effectuated without departing from the true spirit and scope of the novel concepts of the present
invention. It is to be understood that no limitations with respect to the specific embodiments
illustrated is intended or should be inferred. It should be understood that all such modifications
and improvements are properly covered within the scope this application.
15

20

Dated this 20th day of March 2024

Anshu Agrawal
IN-PA-4170
Patent Agent for the Applicant

To
The Controller of Patents
The Patent Office
At New Delhi
,CLAIMS:WE CLAIM:

Claim 1: A pesticidal indoor space spray composition comprising A) Renofluthrin alone or in
combination with at least one another insecticide; and B) one or more chemically acceptable
excipients.
Claim 2: The pesticidal composition as claimed in claim 1, wherein the at least one another
insecticide is selected from the group consisting of Cypermethrin, Permethrin, Fipronil,
Deltamethrin, Lambda Cyhalothrin and Imiprothrin.
Claim 3: The pesticidal composition as claimed in Claim 1, wherein Renofluthrin is present in
an amount ranging from 0.02% to 2% by weight of the total composition.
Claim 4: The pesticidal composition as claimed in claim 1, wherein the at least one another
insecticide is present in an amount ranging from 0.05% to 2% by weight of the total
composition.
Claim 5: The pesticidal composition as claimed in claim 1, wherein the at least one another
insecticide is Cypermethrin.
Claim 6: The pesticidal composition as claimed in claim 1, wherein one or more chemically
acceptable excipients are selected from a group comprising of solvent, propellant, perfume,
synergist, corrosion inhibitors and pH buffers.
Claim 7: The pesticidal composition as claimed in claim 1 and claim 6, wherein the solvent is
selected from Isopropyl alcohol, Tri-propylene glycol, Mono-methyl ether, Ethylene glycol D-
methyl ether, Butyl cortisol, Hydroseal, Ketrul d-80, Deodorised kerosene, or combinations
thereof and present in an amount ranging from 30% to 99 % by weight of the total composition.
Claim 8: The pesticidal composition as claimed in claim 1 and claim 6, wherein the propellant
is selected from liquified petroleum gas, nitrogen, butane, isobutane, propane,
hydrofluorocarbon, or combinations thereof and present in an amount ranging from 0% to 70%
by weight of the total composition.
Claim 9: The pesticidal composition as claimed in claim 1 and claim 6, wherein the perfume
is present in an amount of ranging from 0.2% to 1% by weight of the total composition.
Claim 10: The pesticidal composition as claimed in claim 1 and claim 6, wherein the synergist
is selected from piperonyl butoxide, N-octyl bicycloheptene dicarboximide, propargyl propyl
phenyl phosphonate, or combinations thereof and present in an amount ranging from 0% to 2%
by weight of the total composition.
Claim 11: The pesticidal composition as claimed in claim 1 and claim 6, wherein corrosion
inhibitors and pH buffers are optionally present.

23

Claim 12: The pesticidal composition as claimed in claim 1, wherein Renofluthrin is used
alone or in combination with at least one another insecticide for delivery via aerosol or trigger
spray or single push.
Claim 13: The pesticidal composition as claimed in claim 1 is an insecticidal/acaricidal
composition.
Claim 14: The pesticidal composition as claimed in claim 1, wherein the said composition
exhibits significant flying and crawling insect and mite control activity.