Co-crystal Insecticide Formulation for Controlled Release

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Solution Overview

Problem

Existing insecticides with high water solubility face challenges in maintaining long-term efficacy while minimizing phytotoxicity and elution rates, which affect their effectiveness and safety for plants and animals.

Innovation Solution

A co-crystal formed by combining a diamide-based insecticidal-active ingredient, such as cyantraniliprole, chlorantraniliprole, or cyclaniliprole, with a neonicotinoid-based ingredient like acetamiprid, where the molar ratio is controlled between 0.3 to 3, is produced through methods involving suspension in a solvent and heating, reducing the water solubility of the neonicotinoid and enhancing the insecticidal effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If neonicotinoid-based insecticides with high water solubility are used, then insecticidal efficacy is improved, but elution rate increases causing phytotoxicity and reduced long-term effectiveness

Engineering Contradiction:
Improveinsecticidal efficacyVSAvoidphytotoxicity and elution rate
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent creates a co-crystal composite material combining neonicotinoid-based insecticide (acetamiprid) with diamide-based insecticide (cyantraniliprole, chlorantraniliprole, or cyclaniliprole). This composite structure modifies the solubility and release characteristics of the neonicotinoid component, reducing its elution rate while maintaining insecticidal efficacy. The co-crystal form allows the high-solubility neonicotinoid to be delivered at controlled rates, preventing phytotoxicity while ensuring long-term effectiveness.

Inventive Principle:
Principle #40Composite materials

2Reliability

If water solubility of insecticidal ingredients is increased, then initial insecticidal effect is improved, but long-term maintenance of effect deteriorates due to rapid elution

Engineering Contradiction:
Improveinitial insecticidal effectVSAvoidlong-term effectiveness
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent changes the physical and chemical parameters of the neonicotinoid insecticide by forming a co-crystal structure. This transformation alters the solubility profile and release kinetics of the active ingredient. The co-crystal form maintains adequate water solubility for initial efficacy while providing controlled release characteristics that extend the duration of action, thereby solving the contradiction between initial effect and long-term maintenance.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If concentration of insecticidal application is increased, then immediate pest control is improved, but phytotoxicity to useful plants increases

Engineering Contradiction:
Improvepest control effectivenessVSAvoidphytotoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by pre-formulating the neonicotinoid insecticide in a co-crystal structure before application. This pre-modification of the chemical form ensures controlled release characteristics are built into the product itself, allowing effective pest control at lower application concentrations without risking phytotoxicity. The co-crystal structure acts as a built-in release control mechanism that prevents excessive concentration buildup in plants.

Inventive Principle:
Principle #10Preliminary action

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 co-crystal formulation achieves controlled elution of the insecticidal ingredients, maintaining excellent insecticidal effects over a long period without causing phytotoxicity to useful plants, as demonstrated by differential scanning calorimetry and X-ray diffraction results.

Implementation Method 1

acetamiprid and a diamide-based insecticidal-active ingredient, selected from cyantraniliprole, chlorantraniliprole and cyclaniliprole, form a co-crystal

Methodology Applied
Scientific EffectCo-crystal formation: Crystallisation

Implementation Method 2

suspending the diamide-based insecticidal-active ingredient and the neonicotinoid-based insecticidal-active ingredient in a solvent to obtain a suspension, and heating and stirring the suspension

Methodology Applied
Scientific EffectHeating: Heating

Implementation Method 3

heating and stirring the suspension

Methodology Applied
Scientific EffectStirring: Stirring

Data Source

PatentEP3069610B1Co-crystal and method for producing same
Publication Date: 2019.01.02 NIPPON SODA CO LTD
  • EP3069610B1 patent drawingFigure 1
  • EP3069610B1 patent drawingFigure 2
  • EP3069610B1 patent drawingFigure 3

AI summary

A co-crystal composed of a diamide-based insecticidal-active ingredient and a neonicotinoid-based insecticidal-active ingredient is provided as a co-crystal which exhibits excellent insecticidal effects over a long period of time while reducing the occurrence of chemical damage on useful plants. The co-crystal is obtained by a method including heating and stirring of a suspension obtained by suspending the diamide-based insecticidal-active ingredient and the neonicotinoid-based insecticidal-active ingredient in a solvent such as water.