Imidacloprid Crystalline Polymorphs for Reduced Non-Target Exposure
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Solution Overview
Problem
The extensive use of imidacloprid, a leading insecticide, in agriculture has led to decreased insect biomass and worrying declines in bee colonies, necessitating strategies to enhance its contact activity while reducing exposure to non-target organisms.
Innovation Solution
The development of novel crystalline forms of imidacloprid, such as Forms IX, VIII, VII, VI, V, IV, and III, which are produced through specific melting and cooling processes, including seeding and nanoconfinement, to enhance contact activity and stability, allowing for reduced application amounts and minimized exposure to non-target organisms.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If imidacloprid is extensively used in agriculture to control pests, then pest control effectiveness is improved, but exposure to non-target organisms increases causing bee colony decline
Solution Approach 1:
The patent applies parameter changes by discovering and utilizing different crystalline forms (polymorphs) of imidacloprid with distinct physical properties. Specifically, Form IX and other novel forms exhibit different solubility, stability, and contact activity characteristics compared to conventional Form I. By changing the crystalline form parameter, the invention achieves enhanced contact activity and faster knockdown times while potentially reducing the total amount of active ingredient needed, thus addressing both pest control effectiveness and non-target organism exposure
Solution Approach 2:
The patent applies local quality by creating formulations where the active ingredient is distributed in specific physical forms (microcrystals of particular polymorphs) that enhance local contact activity at the point of insect interaction. The novel crystalline forms provide improved surface properties and contact efficiency at the application site, allowing for reduced overall application rates while maintaining or improving pest control performance
2Reliability
If imidacloprid application amount is increased to enhance pest control, then lethality against pests is improved, but harm to non-target organisms increases
Solution Approach 1:
The patent changes the physical state parameter of imidacloprid by utilizing novel crystalline forms (Forms III, IV, V, VI, VII, VIII, and IX) with enhanced contact activity. These forms demonstrate up to nine times faster knockdown times compared to conventional Form I, achieving improved lethality at lower application rates. This parameter change in crystalline structure directly addresses the contradiction by reducing the quantity of substance needed while maintaining or enhancing pest control effectiveness
Solution Approach 2:
The patent creates composite formulations incorporating novel crystalline forms of imidacloprid with specific physical characteristics. These composite materials combine the active ingredient in optimized crystalline forms with formulation excipients that enhance contact activity and stability, achieving superior pest control at reduced application rates and minimizing harm to non-target organisms through improved specificity and efficiency
3Ease of operation
If conventional imidacloprid formulation is used to simplify application, then ease of operation is improved, but contact activity and lethality are insufficient
Solution Approach 1:
The patent applies parameter changes by transforming the crystalline form parameter of imidacloprid from conventional Form I to novel forms (particularly Form IX and others), which exhibit enhanced contact activity and faster insect knockdown times. Despite these physical parameter changes, the formulations remain practical for field application, maintaining ease of operation while dramatically improving contact activity and lethality through the superior properties of the novel polymorphs
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
These crystalline forms demonstrate improved lethality against mosquito vectors and other pests, offering up to nine times faster action compared to commercial imidacloprid, effectively controlling disease vectors like Aedes, Anopheles, and Culex mosquitoes while minimizing harm to non-target organisms.
Implementation Method 1
produced through specific melting and cooling processes
Implementation Method 2
growing crystals of imidacloprid Form IX from the molten imidacloprid
Implementation Method 3
seeding the molten imidacloprid with Form VII crystals and growing crystals of imidacloprid Form VII
Implementation Method 4
diffusing the molten imidacloprid into a porous medium, cooling imidacloprid Form I to about 25° C., and growing crystals of imidacloprid Form VII within the porous media
Data Source
AI summary
The present invention relates to crystalline polymorphs of imidacloprid for effective pest management strategies at lower dosages. The present invention further relates to processes of preparing the crystalline polymorphs, and to methods of controlling pests using the novel crystalline polymorphs.