Insecticidal Formulation Using Glycol Ether Solvents

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Solution Overview

Problem

Current agrochemical formulations struggle with achieving stable combinations of dissolved and suspended active ingredients, particularly insecticides, that maintain bioavailability and penetration capacity across a wide temperature range, while also ensuring storage stability.

Innovation Solution

The development of insecticidal compositions comprising a combination of an active ingredient in solid form, a soluble active ingredient, an ammonium salt, an alkyl polypropylene glycol-polyethylene glycol dispersant, and a glycol ether solvent, which are essentially water-free to enhance penetration and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If active ingredients are formulated as suspension concentrates (SC) or oil-based suspension concentrates (OD) with solid particulate form, then storage stability is improved, but biological activity and penetration capacity are reduced due to limited dissolution and bioavailability

Engineering Contradiction:
Improvestorage stabilityVSAvoidbiological activity
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The formulation separates active ingredients into two distinct phases: a dissolved active ingredient providing immediate bioavailability and penetration, and a suspended active ingredient providing long-term storage stability. This segmentation allows each component to fulfill its specific function without compromising the other.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite formulation system combining EC (emulsion concentrate) and SC (suspension concentrate) characteristics into a single product. This composite approach integrates the advantages of both formulation types: the dissolved phase provides EC-like penetration while the suspended phase provides SC-like storage stability.

Inventive Principle:
Principle #40Composite materials

2Ease of manufacture

If active ingredients with low melting point are used, then ease of manufacture is improved, but storage stability deteriorates at high temperatures due to softening or melting

Engineering Contradiction:
ImproveformulabilityVSAvoidstorage stability
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The formulation uses glycol ether solvents with specific physical and chemical parameters (low melting point, high boiling point, appropriate polarity) to dissolve active ingredients that would otherwise be difficult to formulate. This parameter selection allows low-melting-point active ingredients to remain stable in dissolved form across a wide temperature range.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

Glycol ether solvents act as intermediary substances between the active ingredient and the aqueous environment. These solvents mediate the interaction by providing a compatible medium that maintains active ingredient stability and solubility while preventing premature crystallization or degradation at temperature extremes.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Quantity of substance

If active ingredients are dissolved in aqueous solution or formulated as emulsion concentrate (EC) or soluble liquid (SL), then penetration and bioavailability are improved, but storage stability deteriorates due to dissolution equilibrium limitations

Engineering Contradiction:
Improvebiological activityVSAvoidstorage stability
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The formulation separates active ingredients into two distinct phases: a dissolved active ingredient providing immediate bioavailability and penetration, and a suspended active ingredient providing long-term storage stability. This segmentation allows each component to fulfill its specific function without compromising the other.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The dissolved active ingredient is prepared in advance at optimal concentration to ensure immediate penetration efficacy upon application. This preliminary dissolution ensures that the active ingredient is ready for rapid uptake by the target organism without waiting for dissolution equilibrium during application.

Inventive Principle:
Principle #10Preliminary action

4Ease of operation

If water is added to enhance solubility, then ease of operation is improved, but penetration capacity deteriorates due to reduced lipophilicity

Engineering Contradiction:
ImprovesolubilityVSAvoidpenetration capacity
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

The formulation uses glycol ether solvents with specific physical and chemical parameters (low melting point, high boiling point, appropriate polarity) to dissolve active ingredients that would otherwise be difficult to formulate. This parameter selection allows low-melting-point active ingredients to remain stable in dissolved form across a wide temperature range.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

Glycol ether solvents act as intermediary substances between the active ingredient and the aqueous environment. These solvents mediate the interaction by providing a compatible medium that maintains active ingredient stability and solubility while preventing premature crystallization or degradation at temperature extremes.

Inventive Principle:
Principle #24Intermediary (Mediator)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compositions demonstrate improved penetration and stability for both active ingredients, maintaining bioavailability and storage stability at high and low temperatures, effectively addressing the limitations of existing formulations.

Implementation Method 1

The invention relates to insecticidal active ingredient formulations comprising at least one dissolved active ingredient... at least one water-insoluble active ingredient... and at least one solvent selected from the group of the glycol ethers

Methodology Applied
Scientific EffectDissolution: Solvation

Implementation Method 2

biological activity can optionally be increased further by adding suitable adjuvants/penetrants

Methodology Applied
Scientific EffectPenetration enhancement:

Implementation Method 3

at least one dispersant from the class of the alkyl propoxylated ethoxylates

Methodology Applied
Scientific EffectDispersion: Dispersion (of waves)

Implementation Method 4

stable suspension concentrates that they are both physically and chemically storage-stable over a prolonged period (12-24 months) and over a wide temperature range (0 to 54°C)

Methodology Applied
Scientific EffectThermal stability:

Data Source

PatentEP4275493A1Formulation of insecticidal mixtures comprising glycol ether solvents
Publication Date: 2023.11.15 BAYER AG
  • EP4275493A1 patent drawingFigure 1
  • EP4275493A1 patent drawingFigure 2
  • EP4275493A1 patent drawing

AI summary

The invention relates to insecticidal active ingredient formulations comprising at least one dissolved active ingredient and one active ingredient in solid form having good storage stability at high and low temperatures and high active ingredient penetration, to a process for production thereof and to the use thereof for application of the active ingredients present.