The following specification particularly describes the invention and the manner in
which it is to be performed.
1
FORM 2
THE PATENTS ACT 1970
(39 of 1970)
&
THE PATENT RULES, 2003
COMPLETE SPECIFICATION
[See Section 10 and Rule 13]
Title of the invention: HERBICIDAL COMPOSITION
Name of the Applicant: UPL LIMITED
Nationality: Indian
Address: UPL R&D CENTRE, Plot Nos. B-20 & C, 12, Rd Number 16, Wagle Industrial Estate, Thane West, Thane, Maharashtra 400604, India
2
TECHNICAL FIELD
The present invention relates to a herbicidal composition. The present invention particularly relates to an emulsifiable concentrate (EC). 5
BACKGROUND AND PRIOR ART
While formulating agrochemicals, it is essential to dissolve or suspend the agrochemically active ingredient in a solvent and then dilute it in a larger volume of water or any other carrier to be broadcast in the form of a fine spray or for its application 10 on seed surfaces.
Some active ingredients, which are usually used as salts, can be dissolved and diluted in water, majority of agrochemically active ingredients are hydrophobic and are therefore water insoluble. For application by the end user, herbicide compounds may 15 be formulated in solid forms, such as wettable powders and granules, as well as in liquid forms, such as emulsifiable concentrates (EC’s) or suspension concentrates (SC’s). In case of active ingredients that are water insoluble, it is necessary to dissolve the active in a water-immiscible solvent followed by addition of one or more surfactants, so that the solution will form an oil-in-water emulsion, when added to 20 water.
However, like many active ingredients that are used as herbicides, saflufenacil is only sparingly soluble in water and in mixtures of water with water-miscible solvents such as C1-C4-alkanols or C2-C4-alkandiols and -triols. 25
Emulsifiable concentrate (EC) formulations generally counter problems of toxicity, phytotoxicity, and flammability, that are caused by organic solvents and synthetic
3
surface-active agents used in preparation of the EC formulation. Typical solvents used for preparing conventional EC formulations include aromatic hydrocarbons, for example, xylene or high solvency naphthalene-depleted C11 aromatic fluid. These solvents have exceptionally low solubilities in water and a high capability of dissolving a wide range of active ingredients, therefore not making them conducive for 5 agricultural applications.
One of the improvements is using water, instead of organic solvents, which results in an emulsion or microemulsion. The other method is solidifying the EC formulation, which results in an EG (emulsifiable granule) or EP (emulsifiable powder) formulation. 10 Another way is using safer organic solvents and emulsifiers in formulation recipes.
Therefore, there is a need in the art to provide a formulation comprising an environment-friendly solvent, which results in solubility of saflufenacil in the formulation. 15
SUMMARY OF THE INVENTION
The present disclosure provides a herbicide composition comprising protoporphyrinogen oxidase (PPO) inhibitor herbicides and synthetic auxin herbicides, having an improved solvent system and agrochemically acceptable excipients. 20
In an aspect, the present disclosure provides an emulsifiable concentrate (EC) comprising protoporphyrinogen oxidase (PPO) inhibitor herbicides and synthetic auxin herbicides, having an improved solvent system, an emulsifier, a pH stabilizer and agrochemically acceptable excipients. 25
In an aspect, the present disclosure provides an emulsifiable concentrate (EC) comprising;
4
(i)
at least one herbicide selected from the group comprising protoporphyrinogen oxidase (PPO) inhibitor herbicides,
(ii)
at least one herbicide selected from the group comprising synthetic auxins,
(iii)
at least one solvent(s) comprising an amide solvent,
(iv)
at least one co-solvent, and 5
(v)
agrochemically acceptable excipients.
In another aspect, the present disclosure provides an emulsifiable concentrate (EC) comprising;
(i)
at least one herbicide selected from the group comprising N-phenyl-imides, 10
(ii)
at least one herbicide selected from the group comprising pyridyloxy-carboxylates,
(iii)
at least one solvent(s) comprising an amide solvent,
(iv)
at least one co-solvent, and
(v)
agrochemically acceptable excipients. 15
In yet another aspect, the present disclosure provides an emulsifiable concentrate (EC) formulation comprising saflufenacil, triclopyr, solvent(s) comprising an amide solvent, a co-solvent, and at least one emulsifier, a pH stabilizer, and agrochemically acceptable excipients. 20
DETAILED DESCRIPTION OF THE INVENTION
The present disclosure now will be described hereinafter with reference to the accompanying examples, in which embodiments of the disclosure are shown. This description is not intended to be a detailed catalogue of all the different ways in which 25 the disclosure may be implemented, or all the features that may be added to the instant disclosure. For example, features illustrated with respect to one embodiment may be incorporated into other embodiments, and features illustrated with respect to a
5
particular embodiment may be deleted from that embodiment. Thus, the disclosure contemplates that in some embodiments of the disclosure, any feature or combination of features set forth herein can be excluded or omitted. In addition, numerous variations and additions to the various embodiments suggested herein will be apparent to those skilled in the art in light of the instant disclosure, which do not depart from the instant 5 disclosure. Hence, the following descriptions are intended to illustrate some particular embodiments of the disclosure, and not to exhaustively specify all permutations, combinations and variations thereof.
Unless otherwise defined, all technical and scientific terms used herein have the same 10 meaning as commonly understood by one of ordinary skill in the art to which this disclosure belongs. Although methods and materials similar or equivalent to those described herein can be used in the practice or testing of the disclosure, suitable methods and materials are described herein.
15
“About” or “approximately” as used herein is inclusive of the stated value and means within an acceptable range of deviation for the particular value as determined by one of ordinary skill in the art, considering the measurement in question and the error associated with measurement of the particular quantity (i.e., the limitations of the measurement system). For example, “about” can mean within one or more standard 20 deviations, or within ± 10% or ± 5% of the stated value.
Recitation of ranges of values are merely intended to serve as a shorthand method of referring individually to each separate value falling within the range, unless otherwise indicated herein, and each separate value is incorporated into the specification as if it 25 were individually recited herein. The endpoints of all ranges are included within the range and independently combinable. As used herein, all numerical values or numerical ranges include integers within such ranges and fractions of the values or the integers within ranges unless the context clearly indicates otherwise. Thus, for example,
6
reference to a range of 90-100%, includes 91%, 92%, 93%, 94%, 95%, 95%, 97%, etc., as well as 91.1%, 91.2%, 91.3%, 91.4%, 91.5%, etc., 92.1%, 92.2%, 92.3%, 92.4%, 92.5%, etc., and so forth. All methods described herein can be performed in a suitable order unless otherwise indicated herein or otherwise clearly contradicted by context.
5
The use of the terms “a”, “an” and “the” and similar referents (especially in the context of the following claims) are to be construed to cover both the singular and the plural, unless otherwise indicated herein or clearly 5contradicted by context. The terms first, second etc., as used herein are not meant to denote any particular ordering, but simply for convenience to denote a plurality of, for example, layers. 10
The terms “comprising”, “having”, “including”, and “containing” are to be construed as open-ended terms (i.e., meaning “including, but not limited to”) unless otherwise noted.
15
The use of any and all examples, or exemplary language (e.g., “such as”), is intended merely to better illustrate the disclosure and does not pose a limitation on the scope of the disclosure unless otherwise claimed. No language in the specification should be construed as indicating any non-claimed element as essential to the practice of the disclosure as used herein. 20
While the disclosure has been described with reference to an exemplary embodiment, it will be understood by those skilled in the art that various changes may be made, and equivalents may be substituted for elements thereof without departing from the scope of the disclosure. In addition, many modifications may be made to adapt a particular 25 situation or material to the teachings of the disclosure without departing from the essential scope thereof. Therefore, it is intended that the disclosure is not limited to the particular embodiment disclosed as the best mode contemplated for carrying out this
7
disclosure, but that the disclosure will include all embodiments falling within the scope of the appended claims.
The expression of various quantities in terms of “%” or “% w/v” means the percentage by weight of the total solution or composition unless otherwise specified. 5
The term “herbicide” as used herein denotes a compound which controls or modifies the growth of undesired weeds/plants.
The term “herbicidally effective amount” indicates the quantity of such a compound or 10 combination of such compounds which is capable of controlling or modifying effect on the growth of harmful plants/undesired vegetation/weeds. Controlling effects include all deviation from natural development, for example: killing, retardation, leaf burn, albinism, dwarfism, etc.
15
The term “primary solvent” or “solvent” is a substance that dissolves a solute, resulting in a solution.
The term “co-solvent” is a substance added to a primary solvent or a solvent in small amounts to increase the solubility of a poorly soluble compound. The “co-solvent” is a 20 solvent that in conjunction with another solvent can dissolve a solute.
The term “green solvent” refers to solvents which are used in various applications and help to minimize their environmental footprint. These solvents are deliberately formulated to achieve two primary objectives: reducing toxicity and conserving energy 25 resources. Advantages of green solvent include – being eco-friendly; being non-toxic or have low toxicity; more sustainable; not contributing to greenhouse gas emissions; better for worker health and reducing chemical exposure; energy-efficient; driving
8
innovation and research in sustainable technologies; cost effective; and naturally reducing reliance on finite resources.
The term “plants” refer to all physical parts of a plant, including seeds, seedlings, saplings, roots, tubers, stems, stalks, foliage and fruits. The terms “plants” and 5 “vegetation” include, but are not limited to, germinant seeds, emerging seedlings, plants emerging from vegetative propagules, and established vegetation.
The term “crop” shall include a multitude of desired crop plants or an individual crop plant growing at a locus. 10
As used herein, the term “pre-emergence” refers to the time point before seedlings emerge from the ground. When any herbicide is applied at the pre-emergence stage, it prevents establishment of the germinated weed seedlings. As used herein, the term “post-emergence” refers to the time point after seedlings emerge from the ground. 15 When any herbicide is applied at post-emergence stage, it prevents growth of the germinated weed seedlings.
The terms “undesirable vegetation”, “harmful plants”, “unwanted plants”, “weeds” and “weed species”, as used herein, are synonyms. 20
The term “control” provides a weed, includes control of the weed, as well as protecting a plant, a portion of the plant, or a plant seed from attack or invasion by said weed.
The term “locus” as used herein shall denote the vicinity of a desired crop in which 25 weed control, typically selective weed control is desired. The locus includes the vicinity of desired crop plants wherein the weed infestation has either emerged or is yet to emerge.
9
As used herein, the term “g/L” denotes the concentration of the respective active ingredient in “grams” present “per liter” of the composition. The terms “g ai/L”, “g a.i./L” and “g/L” may be used interchangeably.
The terms “g a.i./ha” as used herein denotes the concentration of the respective active 5 ingredient in “grams” applied “per hectare” of the crop field. The terms “g ai/ha”, “g a.i./ha”, “g a.i./h”, “g ai/h” and “g/ha” may be used interchangeably.
Each of the aspects described above may have one or more embodiments. Each of the embodiments described hereinafter may apply to one or all of the aspects described 10 hereinabove. These embodiments are intended to be read as being preferred features of one or all of the aspects described hereinabove. Each of the embodiments described hereinafter applies to each of the aspects described hereinabove individually.
The present disclosure provides a herbicide composition comprising a 15 protoporphyrinogen oxidase (PPO) inhibitor herbicide, a synthetic auxin herbicide, an improved solvent system, and agrochemically acceptable excipients. The improved solvent system of the present invention employs a green solvent to obtain dissolution of the PPO inhibitor herbicides with the aid of a co-solvent.
20
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) formulation comprising an improved solvent system and agrochemically acceptable excipients.
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) 25 comprising;
(i)
at least one herbicide selected from the group comprising protoporphyrinogen oxidase (PPO) inhibitor herbicides,
(ii)
at least one herbicide selected from the group comprising synthetic auxins,
10
(iii)
at least one solvent(s) comprising an amide solvent,
(iv)
at least one co-solvent, and
(v)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides a herbicidal composition 5 comprising:
(i)
at least one herbicide selected from the group comprising N-phenyl-imides;
(ii)
at least one herbicide selected from the group comprising pyridyloxy-carboxylates;
(iii)
at least one solvent comprising an amide solvent; 10
(iv)
at least one co-solvent; and
(v)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) comprising; 15
(i)
at least one herbicide selected from the group comprising N-phenyl-imides,
(ii)
at least one herbicide selected from the group comprising pyridyloxy-carboxylates,
(iii)
at least one solvent(s) comprising an amide solvent,
(iv)
at least one co-solvent, and 20
(v)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) comprising;
(i)
at least one herbicide selected from the group comprising protoporphyrinogen 25 oxidase (PPO) inhibitor herbicides,
(ii)
at least one herbicide selected from the group comprising synthetic auxins,
(iii)
at least one solvent(s) comprising an amide solvent,
(iv)
at least one co-solvent,
11
(v)
a pH stabilizer,
(vi)
an emulsifier, and
(vii)
agrochemically acceptable excipients.
5
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) formulation comprising;
(i)
at least one herbicide selected from the group comprising N-phenyl-imides,
(ii)
at least one herbicide selected from the group comprising pyridyloxy-carboxylates, 10
(iii)
at least one solvent(s) comprising an amide solvent,
(iv)
at least one co-solvent,
(v)
a pH stabilizer,
(vi)
an emulsifier, and
(vii)
an agrochemically acceptable excipients. 15
In an embodiment, the N-phenyl-imide herbicides comprises saflufenacil, butafenacil, epyrifenacil, tiafenacil, flumioxazin, pentoxazone, trifludimoxazin, flumiclorac-pentyl and cinidon-ethyl or salts thereof.
20
In a preferred embodiment, the N-phenyl-imide herbicides comprise saflufenacil or its salts.
In an embodiment, the pyridyloxy-carboxylate herbicides comprise triclopyr or fluroxypyr or salts or esters thereof. 25
In a preferred embodiment, the pyridyloxy-carboxylate herbicide comprises triclopyr or salts or esters thereof. In a preferred embodiment, the pyridyloxy-carboxylate herbicide comprises triclopyr butotyl ester.
12
In yet another aspect, the present disclosure provides an emulsifiable concentrate (EC) formulation comprising triclopyr, saflufenacil, solvent(s) comprising a primary solvent selected from at least one amide solvent, at least one co-solvent, an emulsifier, a pH stabilizer, and an agrochemically acceptable excipient. 5
In an embodiment, the solvent(s) comprising an amide solvent is a primary solvent.
In an embodiment, the solvent comprises dimethyl amide solvents comprising N,N-dimethyloctanamide, N,N-dimethyl decanamide, or combinations thereof. In a preferred embodiment, the solvent comprises N, N-dimethyl decanamide. 10
In an embodiment, the co-solvent comprises organic solvents comprising amide solvents, tert butyl alcohol, ethanol, n-propanol, n-butanol, isopropanol, ethyl acetate, acetone, methyl acetate, methanol, carbon tetrachloride, dimethylsulfoxide, chlorobutanol, cyclohexane, acetic acid, or combinations thereof. In a preferred 15 embodiment, the co-solvent comprises 2-hydroxy-N,N-dimethyl propanamide or Propanamide, 2-hydroxy-N,N-dimethyl.
In an embodiment, both the solvent and co-solvent comprise a dimethyl amide solvent. In another embodiment, one of the two dimethyl amide solvents comprise a co-solvent. 20
In an embodiment, the emulsifier(s) can be non-ionic emulsifier(s) such as alkoxylated castor oil, alkoxylated polyarylphenols, alkoxylated alkylarylphenols, or alkoxylated fatty alcohols, or mixtures thereof; or anionic emulsifier(s) such as calcium-dodecylbenzene sulfonate, di-octyl sulfosuccinate, sulfated or phosphated alkoxylated 25 fatty alcohols, or sulfated or phosphated alkoxylated alkylaryl phenols, or mixtures thereof; or a mixture of non-ionic emulsifier(s) and anionic emulsifier(s). In a preferred embodiment, the emulsifier comprises calcium dodecyl benzene sulphonate, polyaryl phenol ethoxylate, or combinations thereof.
13
In an embodiment, the pH stabilizer is selected from the group comprising amines such as primary, secondary or tertiary amine. It can be a straight chain, branched or cyclic aliphatic amine or an aromatic amine. In an embodiment, the pH stabilizer comprises diethyl amine. 5
In an embodiment, the present disclosure provides agrochemically acceptable excipients selected from the group comprising pH stabilizer(s), emulsifier(s), surfactant(s), binder(s), antifoam agent(s), diluent(s), filler(s), colorant(s), anticaking agent(s), preservative(s), biocide(s), other formulation aid(s), or combinations thereof. 10
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) comprising;
(i)
saflufenacil or its salts,
(ii)
triclopyr or salts or esters thereof, 15
(iii)
at least one solvent(s) comprising an amide solvent,
(iv)
at least one co-solvent, and
(v)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) 20 comprising;
(i)
epyrifenacil or its salts,
(ii)
triclopyr or salts or esters thereof,
(iii)
at least one solvent(s) comprising an amide solvent,
(iv)
at least one co-solvent, and 25
(v)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) comprising;
14
(i)
tiafenacil or its salts,
(ii)
triclopyr or salts or esters thereof,
(iii)
at least one solvent(s) comprising an amide solvent,
(iv)
at least one co-solvent, and
(v)
agrochemically acceptable excipients. 5
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) comprising;
(i)
saflufenacil or its salts,
(ii)
triclopyr or salts or esters thereof, 10
(iii)
at least one solvent(s) comprising a dimethyl amide solvent,
(iv)
at least one co-solvent, and
(v)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) 15 comprising;
(i)
saflufenacil or its salts,
(ii)
triclopyr or salts or esters thereof,
(iii)
at least one solvent(s) comprising N,N-dimethyloctanamide, N,N-dimethyldecanamide or mixtures thereof, 20
(iv)
at least one co-solvent comprising 2-hydroxy-N,N-dimethyl propanamide, and
(v)
agrochemically acceptable excipients.
In an embodiment, the concentration of the pyridyloxy-carboxylate herbicide ranges from about 10 g/L to about 800 g/L, preferably from about 100 g/L to about 750 g/L, 25 preferably from about 200 g/L to about 700 g/L, and more preferably from about 400 g/L to about 690 g/L. In a preferred embodiment, the concentration of the pyridyloxy-carboxylate herbicide is about 480 g/L. In a preferred embodiment, the concentration of the pyridyloxy-carboxylate herbicide is about 680 g/L.
15
In a preferred embodiment, the concentration of triclopyr is about 480 g/L. In a preferred embodiment, the concentration of triclopyr is about 680 g/L.
In an embodiment, the concentration of the N-phenyl-imide herbicide ranges from 5 about 1 g/L to about 100 g/L, preferably from about 10 g/L to about 80 g/L, preferably from about 15 g/L to about 60 g/L, and more preferably from about 20 g/L to about 50 g/L. In a preferred embodiment, the concentration of the N-phenyl-imide herbicide is about 28 g/L.
10
In a preferred embodiment, the concentration of saflufenacil is about 28 g/L.
In another embodiment, the concentration of the N-phenyl-imide herbicide ranges from about 10 g/L to about 80 g/L and the concentration of the pyridyloxy-carboxylate herbicide ranges from about 200 g/L to about 700 g/L. 15
In another embodiment, the synthetic auxin (or pyridyloxy-carboxylate herbicide) is present in an amount ranging from about 40% to about 80% w/w of the composition. In an embodiment, the synthetic auxin (or pyridyloxy-carboxylate herbicide) is present in an amount ranging from about 50% to about 70% w/w of the composition. 20
In an embodiment, triclopyr is present in an amount ranging from about 40% to about 80% w/w of the composition. In an embodiment, triclopyr is present in an amount ranging from about 50% to about 70% w/w of the composition. In a preferred embodiment, triclopyr butotyl ester is present in an amount ranging from about 55% to 25 about 65% w/w of the composition.
In an embodiment, the PPO inhibitor herbicide (or N-phenyl-imide herbicide) is present in an amount ranging from about 0.1% to about 10% w/w of the composition.
16
In an embodiment, the PPO inhibitor herbicide (or N-phenyl-imide herbicide) is present in an amount ranging from about 1% to about 5% w/w of the composition.
In an embodiment, saflufenacil is present in an amount ranging from about 0.1% to about 10% w/w of the composition. In an embodiment, saflufenacil is present in an 5 amount ranging from about 1% to about 5% w/w of the composition. In a preferred embodiment, saflufenacil is present in an amount ranging from about 2% to about 3% w/w of the composition.
In an embodiment, the composition comprises from about 40% to about 80% w/w 10 pyridyloxy-carboxylate herbicide and from about 0.1% to about 10% w/w N-phenyl-imide herbicide of total weight of the composition.
In an embodiment, the (primary) solvent(s) is present in an amount ranging from about 1% to about 40% w/w of the composition. In an embodiment, the (primary) solvent(s) 15 is present in an amount ranging from about 10% to about 20% w/w of the composition.
In an embodiment, the dimethyl amide solvent(s) is present in an amount ranging from about 1% to about 40% w/w of the composition. In an embodiment, the dimethyl amide solvent(s) is present in an amount ranging from about 10% to about 20% w/w of the 20 composition.
In an embodiment, N,N-dimethyl decanamide is present in an amount ranging from about 1% to about 40% w/w of the composition. In an embodiment, N,N-dimethyl decanamide is present in an amount ranging from about 10% to about 20% w/w of the 25 composition.
17
In an embodiment, the co-solvent is present in an amount ranging from about 0.1% to about 20% w/w of the composition. In an embodiment, the co-solvent is present in an amount ranging from about 1% to about 10% w/w of the composition.
In an embodiment, 2-hydroxy-N,N-dimethyl propanamide is present in an amount 5 ranging from about 0.1% to about 20% w/w of the composition. In an embodiment, 2-hydroxy-N,N-dimethyl propanamide or Propanamide, 2-hydroxy-N,N-dimethyl is present in an amount ranging from about 1% to about 10% w/w of the composition.
In an embodiment, the composition comprises from about 1% to about 40% w/w 10 solvent and from about 0.1% to about 20% w/w co-solvent of total weight of the composition.
In an embodiment, the (primary) solvent and the co-solvent are present in a ratio ranging from about 1:1 to about 1:20. 15
In an embodiment, the emulsifier(s) is present in an amount ranging from about 1% to about 20% w/w of the composition. In a preferred embodiment, calcium dodecyl benzene sulphonate is present in an amount ranging from about 4% to about 8% w/w of the composition. In a preferred embodiment, polyaryl phenol ethoxylate is present 20 in an amount ranging from about 8% to about 12% w/w of the composition.
In an embodiment, the pH stabilizer is present in an amount ranging from about 1% to about 2% w/w of the composition. In an embodiment, the pH stabilizer is present in an amount ranging from about 0.1% to about 0.5% w/w of the composition. 25
In an embodiment, diethyl amine is present in an amount ranging from about 1% to about 2% w/w of the composition. In an embodiment, diethyl amine is present in an amount ranging from about 0.1% to about 0.5% w/w of the composition.
18
In an embodiment, the composition comprises from about 1% to about 20% w/w emulsifier and from about 1% to about 2% w/w pH stabilizer of total weight of the composition.
5
In an embodiment, the composition is in a form of an emulsifiable concentrate (EC).
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) composition comprising:
(i)
saflufenacil; 10
(ii)
triclopyr;
(iii)
at least one solvent comprising a dimethyl amide solvent;
(iv)
at least one co-solvent, and
(v)
agrochemically acceptable excipients.
15
In an embodiment, the solvent comprises N,N-dimethyloctanamide, N,N-dimethyldecanamide or mixtures thereof; and the co-solvent comprises 2-hydroxy-N,N-dimethyl propanamide.
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) 20 comprising;
(i)
saflufenacil or its salts in an amount ranging from about 40% to about 80% w/w of the composition,
(ii)
triclopyr or salts or esters thereof in an amount ranging from about 0.1% to about 10% w/w of the composition, 25
(iii)
at least one solvent(s) comprising an amide solvent in an amount ranging from about 1% to about 40% w/w of the composition,
(iv)
at least one co-solvent in an amount ranging from about 0.1% to about 20% w/w of the composition, and
19
(v)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) comprising;
(i)
saflufenacil or its salts in an amount ranging from about 40% to about 80% 5 w/w of the composition,
(ii)
triclopyr or salts or esters thereof in an amount ranging from about 0.1% to about 10% w/w of the composition,
(iii)
at least one solvent(s) comprising a dimethyl amide solvent in an amount ranging from about 1% to about 40% w/w of the composition, 10
(vi)
at least one co-solvent in an amount ranging from about 0.1% to about 20% w/w of the composition, and
(vii)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides an emulsifiable concentrate (EC) 15 comprising;
(i)
saflufenacil or its salts in an amount ranging from about 40% to about 80% w/w of the composition,
(ii)
triclopyr or salts or esters thereof in an amount ranging from about 0.1% to about 10% w/w of the composition, 20
(iii)
at least one solvent(s) comprising N,N-dimethyloctanamide, N,N-dimethyldecanamide or mixtures thereof in an amount ranging from about 1% to about 40% w/w of the composition,
(iv)
at least one co-solvent comprising 2-hydroxy-N,N-dimethyl propanamide in an amountranging from about 0.1% to about 20% w/w of the composition, and 25
(v)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides use of a herbicidal composition for controlling weeds, the composition comprising:
20
(i)
at least one herbicide selected from the group comprising N-phenyl-imides;
(ii)
at least one herbicide selected from the group comprising pyridyloxy-carboxylates;
(iii)
at least one solvent comprising an amide solvent;
(iv)
at least one co-solvent; and 5
(v)
agrochemically acceptable excipients.
In an embodiment, the present disclosure provides a method for controlling weeds by applying an effective amount of a herbicidal composition to a plant or a locus thereof, the composition comprising: 10
(i)
at least one herbicide selected from the group comprising N-phenyl-imides;
(ii)
at least one herbicide selected from the group comprising pyridyloxy-carboxylates;
(iii)
at least one solvent comprising an amide solvent;
(iv)
at least one co-solvent; and 15
(v)
agrochemically acceptable excipients.
In an embodiment, the pyridyloxy-carboxylate herbicide is applied at an application rate ranging from about 10 g a.i./ha to about 800 g a.i./ha, preferably from about 50 g a.i./ha to about 750 g a.i./ha, preferably from about 100 g a.i./ha to about 600 g a.i./ha, 20 and more preferably from about 200 g a.i./ha to about 500 g a.i./ha.
In a preferred embodiment, the pyridyloxy-carboxylate herbicide is applied at an application rate of about 240 g a.i./ha. In a preferred embodiment, the pyridyloxy-carboxylate herbicide is applied at an application rate of about 480 g a.i./ha. 25
21
In a preferred embodiment, triclopyr is applied at an application rate of about 240 g a.i./ha. In a preferred embodiment, triclopyr is applied at an application rate of about 480 g a.i./ha.
In an embodiment, the N-phenyl-imide herbicide is applied at an application rate 5 ranging from about 0.5 g a.i./ha to about 100 g a.i./ha, preferably from about 1 g a.i./ha to about 75 g a.i./ha, preferably from about 1.2 g a.i./ha to about 50 g a.i./ha, and more preferably from about 1.5 g a.i./ha to about 40 g a.i./ha.
In a preferred embodiment, the N-phenyl-imide herbicide is applied at an application 10 rate of about 1.75 g a.i./ha. In a preferred embodiment, the N-phenyl-imide herbicide is applied at an application rate of about 3.5 g a.i./ha. In a preferred embodiment, the N-phenyl-imide herbicide is applied at an application rate of about 7 g a.i./ha. In a preferred embodiment, the N-phenyl-imide herbicide is applied at an application rate of about 28 g a.i./ha. 15
In a preferred embodiment, saflufenacil is applied at an application rate of about 1.75 g a.i./ha. In a preferred embodiment, saflufenacil is applied at an application rate of about 3.5 g a.i./ha. In a preferred embodiment, saflufenacil is applied at an application rate of about 7 g a.i./ha. In a preferred embodiment, saflufenacil is applied at an 20 application rate of about 28 g a.i./ha.
In an embodiment, the herbicidal composition is applied to a plant or a locus thereof to control from about 50% to about 100% of the weeds.
25
In an embodiment, the present invention provides at least one herbicide selected from the group comprising N-phenyl-imides and at least one herbicide selected from the group comprising pyridyloxy-carboxylates, wherein the composition controls from about 50% to about 100% of the weeds.
22
In another embodiment, the herbicidal composition is applied to weeds selected from the group comprising Amaranthus hybridus, Amaranthus albus, Amaranthus blitoides, Amaranthus blitum, Amaranthus caudatus, Amaranthus deflexus, Amaranthus graecizans, Amaranthus retroflexus, Amaranthus viridis, Bidens subalternans, Bidens 5 aurea, Bidens bipinnata, Bidens frondose, Bidens Pilosa, Bidens tripartite, Conyza spp., Conyza abyssinica, Conyza adenocarpa, Conyza ageratoides, Conyza agnewii, Conyza agrostophylla, or combinations thereof.
In a preferred embodiment, the weeds are selected from the group comprising 10 Amaranthus hybridus, Bidens subalternans, Conyza spp., or combinations thereof.
In an embodiment, the present disclosure provides preferred combinations, compositions and methods thereof. The methods of the invention include a method of controlling weeds at a locus by applying to the locus the combination or the 15 composition, or a method of increasing yield in a crop by application of the combination or composition, or a method of improving the plant health by application at the locus of the plant the combination or the composition. The embodiments described herein describe the preferred embodiments of all these possible combinations, compositions and methods of the invention. 20
In an embodiment, the herbicidal composition comprising at least one N-phenyl-imide herbicide, at least one pyridyloxy-carboxylate herbicide and at least one solvent and co-solvent may provide synergistic control for weeds at pre-emergent and/or at post-emergent stage. In another embodiment, the herbicidal composition is synergistic and 25 effective in improving yield of desired crop by controlling weeds. The herbicidal combination also provides increase in crop yield and crop quality.
23
In view of the above, it will be seen that the several advantages of the disclosure are achieved, and other advantageous results are attained. Although the present disclosure has been disclosed in full, it will be understood that numerous additional modifications and variations could be made thereto without departing from the scope of the disclosure. The embodiments may be combined together for better understanding of 5 the disclosure, without departing from the scope of the disclosure.
In another embodiment, alternative or multiple embodiments of the disclosure disclosed herein are not to be construed as limitations. Each embodiment can be referred to and claimed individually or in any combination with other embodiments of 10 the disclosure. One or more embodiments of the disclosure can be combined together to exhibit the teaching of the invention, without departing from the scope of the disclosure.
EXAMPLES 15
Example 1: Triclopyr (680 g/L) and saflufenacil (28 g/L) EC Formulation
Table 1
Sr. No.
Ingredients
Concentration % (w/w)
1.
Triclopyr Butotyl ester
55 to 65
2.
Saflufenacil
2 to 3
3.
Diethyl Amine
0.1 to 0.5
4.
Calcium dodecyl benzene sulphonate
4 to 8
5.
Polyaryl phenol ethoxylate
8 to 12
6.
N, N dimethyl decanamide
10 to 20
7.
Propanamide, 2-hydroxy-N,N-dimethyl
1 to 10
24
8.
Total
100
Process:
In a vessel the solvent, the co-solvent and saflufenacil were combined and stirred together to dissolve completely. To the vessel triclopyr butotyl ester and diethyl amine were added and stirring was continued. Further, both the emulsifiers were added to the 5 vessel followed by stirring for two hours. The mixture was filtered to obtain the required formulation.
Example 2: Solubility screening studies
The solubility of saflufenacil is determined with different solvents. 10
Table 2
Treatment no.
Active
Concentrations
(% w/w)
Solubility
Saflufenacil
1.5
1.5
1.5
1.5
1.5
1.5
NA
Solvent system
1.
N,N dimethyl decanamide
10
Soluble
2.
Propanamide, 2-hydroxy-N,N-dimethyl
10
Soluble
3.
C9 Aromatic Hydrocarbons Solvents
10
Slightly soluble
4.
Mix xylene
10
No
25
5.
Naphthalene-depleted C10 aromatic fluid
10
No
6.
C10 aromatic fluid
10
No
The solubility of saflufenacil was best identified with amide-based solvents as observed from the Table in Treatments 1 and 2. The solvents used in treatment nos. 3, 4, 5 and 6 did not show any solubility.
5
Example 3: Stability studies
The stability of the formulation prepared according to Example 1 is provided in Table 3 below.
Table 3
Sr. No
Parameters
Results
0 Day
Ambient
AHS - 14 days
1
Appearance
Pale yellow stable clear liquid free from extraneous matter
2
Active Content
i) Triclopyr (g/L)
681.8
680.8
680
ii) Saflufenacil (g/L)
30.5
30.5
30
3
1% PH of emulsion
5.77
5.59
5.54
4
Persistence foam (mL)
34
30
36
5
Water Content by KF
0.43
0.46
0.44
6
Specific Gravity@ 0 ± 2°C
1.152
1.152
1.153
7
Emulsion stability
0.5 hr
Nil
Nil
Nil
2 hr
Nil
Nil
Nil
26
24 hr
Nil
Nil
Nil
24.5 hr
Nil
Nil
Nil
The formulation is physically and chemically stable in accelerated heat stability conditions (AHS). The said AHS conditions are for 14 days at 54°C.
Example 4: Triclopyr (480 g/L) and saflufenacil (28 g/L) EC Formulation 5
Table 4
Sr. No.
Ingredients
Concentration % (w/w)
1.
Triclopyr Butotyl ester
40 to 65
2.
Saflufenacil
2 to 3
3.
Diethyl Amine
0.1 to 0.5
4.
Calcium dodecyl benzene sulphonate
4 to 8
5.
Polyaryl phenol ethoxylate
8 to 12
6.
N, N dimethyl decanamide
10 to 20
7.
Propanamide, 2-hydroxy-N,N-dimethyl
1 to 10
8.
Total
100
Example 5: Efficacy of Triclopyr and Saflufenacil on Amaranthus hybridus
The herbicidal composition comprising triclopyr and saflufenacil was evaluated to assess the efficacy of the composition for percentage control of Amaranthus hybridus 10 on 7, 14, 21 and 28 days after application (DAA). No phytotoxicity was observed on the crops. The results have been tabulated in Table 5.
Table 5
Component
Weed Control (%)
27
Application Rate
(g a.i./ha)
7 DAA
14 DAA
21 DAA
28 DAA
Triclopyr
240
38
67
67
78
Triclopyr
480
41
74
78
86
Saflufenacil
1.75
43
36
35
22
Saflufenacil
3.5
44
36
36
24
Saflufenacil
7
60
41
39
26
Saflufenacil
28
94
78
68
49
Triclopyr +
Saflufenacil
240 +
1.75
72
82
87
87
Triclopyr +
Saflufenacil
240 +
3.5
84
85
94
94
Triclopyr +
Saflufenacil
240 +
7
90
91
92
94
Triclopyr +
Saflufenacil
480 +
28
99
99
100
100
It was observed that the herbicidal composition comprising triclopyr and saflufenacil showed significant control for Amaranthus hybridus.
Example 6: Efficacy of Triclopyr and Saflufenacil on Bidens subalternans 5
The herbicidal composition comprising triclopyr and saflufenacil was evaluated to assess the efficacy of the composition for percentage control of Bidens subalternans on 7, 14 and 21 days after application (DAA). No phytotoxicity was observed on the crops. The results have been tabulated in Table 6.
Table 6 10
Component
Weed Control (%)
28
Application Rate
(g a.i./ha)
7 DAA
14 DAA
21 DAA
Triclopyr
240
45
67
91
Saflufenacil
1.75
41
33
33
Saflufenacil
3.5
41
37
33
Saflufenacil
7
64
51
40
Triclopyr +
Saflufenacil
240 +
1.75
84
95
99
Triclopyr +
Saflufenacil
240 +
3.5
82
93
97
Triclopyr +
Saflufenacil
240 +
7
87
96
97
It was observed that the herbicidal composition comprising triclopyr and saflufenacil showed significant control for Bidens subalternans.
Example 7: Efficacy of Triclopyr and Saflufenacil on Conyza spp. 5
The herbicidal composition comprising triclopyr and saflufenacil was evaluated to assess the efficacy of the composition for percentage control of Conyza spp. on 7, 14, 21 and 28 days after application (DAA). No phytotoxicity was observed on the crops. The results have been tabulated in Table 7.
Table 7 10
Component
Application Rate
(g a.i./ha)
Weed Control (%)
7 DAA
14 DAA
21 DAA
28 DAA
Triclopyr
240
38
38
40
45
Saflufenacil
1.75
20
10
10
10
29
Saflufenacil
3.5
29
15
15
15
Triclopyr +
Saflufenacil
240 +
1.75
65
66
59
56
Triclopyr +
Saflufenacil
240 +
3.5
65
65
50
58
It was observed that the herbicidal composition comprising triclopyr and saflufenacil showed significant control for Conyza spp.
30
We Claim:
1.
A herbicidal composition comprising:
(i)
at least one herbicide selected from the group comprising N-phenyl-imides;
(ii)
at least one herbicide selected from the group comprising pyridyloxy-carboxylates; 5
(iii)
at least one solvent comprising an amide solvent;
(iv)
at least one co-solvent; and
(v)
agrochemically acceptable excipients.
2.
The composition as claimed in claim 1, wherein the N-phenyl-imide herbicide 10 comprises saflufenacil, butafenacil, epyrifenacil, tiafenacil, flumioxazin, pentoxazone, trifludimoxazin, flumiclorac-pentyl and cinidon-ethyl or salts thereof.
3.
The composition as claimed in claim 1, wherein the pyridyloxy-carboxylate 15 herbicide comprises triclopyr or fluroxypyr or salts or esters thereof.
4.
The composition as claimed in claim 1, the concentration of the N-phenyl-imide herbicide ranges from about 10 g/L to about 80 g/L and the concentration of the pyridyloxy-carboxylate herbicide ranges from about 200 g/L to about 700 g/L. 20
5.
The composition as claimed in claim 1, wherein the solvent comprises dimethyl amide solvents comprising N,N-dimethyloctanamide, N,N-dimethyldecanamide or combinations thereof.
25
6.
The composition as claimed in claim 1, wherein the co-solvent comprises organic solvents comprising amide solvents, tert butyl alcohol, ethanol, n-propanol, n-butanol, isopropanol, ethyl acetate, acetone, methyl acetate, methanol, carbon
31
tetrachloride, dimethylsulfoxide, chlorobutanol, cyclohexane, acetic acid
, or combinations thereof.
7.
The composition as claimed in claim 1, wherein the composition further comprises a pH stabilizer and an emulsifier. 5
8.
The composition as claimed in claim 1, wherein the composition comprises from about 40% to about 80% w/w pyridyloxy-carboxylate herbicide and from about 0.1% to about 10% w/w N-phenyl-imide herbicide of total weight of the composition. 10
9.
The composition as claimed in claim 1, the composition comprises from about 1% to about 40% w/w solvent and from about 0.1% to about 20% w/w co-solvent of total weight of the composition.
15
10.
The composition as claimed in claim 1, wherein the solvent and the co-solvent are present in a ratio ranging from about 1:1 to about 1:20.
11.
The composition as claimed in claim 7, wherein the composition comprises from about 1% to about 20% w/w emulsifier and from about 1% to about 2% w/w pH 20 stabilizer of total weight of the composition.
12.
The composition as claimed in claim 1, wherein the composition is in a form of an emulsifiable concentrate.
25
13.
An emulsifiable concentrate composition comprising:
(i)
saflufenacil;
(ii)
triclopyr;
32
(iii)
at least one solvent comprising a dimethyl amide solvent;
(iv)
at least one co-solvent; and
(v)
agrochemically acceptable excipients.
14.
The composition as claimed in claim 13, wherein the solvent comprises N,N-5 dimethyloctanamide, N,N-dimethyldecanamide or mixtures thereof; and the co-solvent comprises 2-hydroxy-N,N-dimethyl propanamide.
15.
Use of a herbicidal composition for controlling weeds, the composition comprising: 10
(i)
at least one herbicide selected from the group comprising N-phenyl-imides;
(ii)
at least one herbicide selected from the group comprising pyridyloxy-carboxylates;
(iii)
at least one solvent comprising an amide solvent;
(iv)
at least one co-solvent; and 15
(v)
agrochemically acceptable excipients.
16.
A method for controlling weeds by applying an effective amount of a herbicidal composition to a plant or a locus thereof, the composition comprising:
(i)
at least one herbicide selected from the group comprising N-phenyl-imides; 20
(ii)
at least one herbicide selected from the group comprising pyridyloxy-carboxylates;
(iii)
at least one solvent comprising an amide solvent;
(iv)
at least one co-solvent; and
(v)
agrochemically acceptable excipients.