Insecticide Solubility via c log P Mediator

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Solution Overview

Problem

2-fluoro-3-(N-methylbenzamide)-N-(2-bromo-6-trifluoromethyl-4-(heptafluoropropane-2-yl)phenyl)benzamide has poor solubility in common solvents, making it inconvenient to use in various dosage forms and reducing its effectiveness as an insecticide.

Innovation Solution

The use of a solubilizer with a calculated log P (c log P) within a specific range of 0.1 to 2.1, such as benzyl alcohol, N-methyl-2-pyrrolidone, and propylene glycol diacetate, to enhance the solubility of the insecticide in insecticide compositions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If 2-fluoro-3-(N-methylbenzamide)-N-(2-bromo-6-trifluoromethyl-4-(heptafluoropropane-2-yl)phenyl)benzamide is used as an insecticidal component, then high insecticidal effects and persistence against resistant pests are achieved, but poor solubility in common solvents makes it inconvenient to use in various dosage forms

Engineering Contradiction:
Improveinsecticidal effectsVSAvoidsolubility
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent introduces a specific solubilizer as an intermediary substance to bridge the incompatibility between the hydrophobic insecticidal component and the aqueous or polar solvent environment. The solubilizer has a c log P value within 0.1 to 2.1, which allows it to interact with both the insecticidal component and the solvent system, thereby enabling sufficient dissolution while maintaining the component's insecticidal activity.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent applies parameter changes by controlling the c log P value of the solubilizer within a specific range (0.1 to 2.1). This quantitative parameter control optimizes the balance between solubility enhancement and maintenance of insecticidal efficacy. By adjusting this critical parameter, the patent resolves the contradiction between solubility and effectiveness.

Inventive Principle:
Principle #35Parameter changes

2Device complexity

If the insecticidal component is used without adequate solubilization, then the formulation complexity is reduced, but the insecticidal effects are insufficient and the component is inconvenient to use in various dosage forms

Engineering Contradiction:
Improveformulation complexityVSAvoidinsecticidal effects
Core Design Contradiction:
Device complexityVSReliability

Solution Approach 1:

By specifying a narrow range for the c log P parameter (0.1 to 2.1), the patent simplifies the formulation development process. Instead of screening numerous solubilizers with varying properties, formulators can focus on compounds within this specific parameter range, thereby reducing formulation complexity while ensuring adequate solubility and insecticidal effects.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies local quality by focusing on the specific property of the solubilizer (c log P value) rather than requiring optimization of multiple formulation parameters. This localized approach to quality control enables effective solubilization with minimal formulation complexity.

Inventive Principle:
Principle #3Local quality

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

This approach allows for sufficient dissolution of the insecticide, resulting in high insecticidal effects and the ability to form stable formulations like aerosols and sprays, effectively targeting resistant pests.

Implementation Method 1

it is possible to dissolve 2-fluoro-3-(N-methylbenzamide)-N-(2-bromo-6-trifluoromethyl-4-(heptafluoropropane-2-yl)phenyl)benzamide in the composition sufficiently by using a solubilizer having a c log P within a specific range

Methodology Applied
Scientific EffectSolubility: Solvation

Data Source

PatentUS11382329B2Insecticide composition
Publication Date: 2022.07.12 MITSUI CHEM CROP & LIFE SOLUTIONS INC

AI summary

The present invention pertains to an insecticide composition containing 2-fluoro-3-(N-methylbenzamide)-N-(2-bromo-6-trifluoromethyl-4-(heptafluoropropane-2-yl)phenyl)benzamide and a solubilizer having a c log P of 0.1-2.1.