Emamectin Benzoate Modification V Crystalline Stability
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing crystalline modifications of emamectin benzoate are prone to conversion during storage, aggregation, and recrystallization after dilution, making them unsuitable for commercial formulations.
Innovation Solution
A novel crystalline polymorph (modification V) of emamectin benzoate is developed, which is stable during prolonged storage and easier to comminute, with a lower tendency to aggregate and recrystallize, allowing for the preparation of stable formulations such as suspension concentrates and water-soluble granules.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing crystalline modifications of emamectin benzoate are used, then the pesticide can be formulated, but the formulations are unstable during storage and after dilution due to polymorph conversion, aggregation, and recrystallization
Solution Approach 1:
The patent applies parameter changes by discovering and utilizing a new crystalline polymorph (Modification V) of emamectin benzoate with different physical and chemical parameters compared to existing modifications. This new polymorph exhibits superior stability characteristics, lower aggregation tendency, and reduced recrystallization after dilution, directly resolving the formulation stability issues while maintaining pesticidal efficacy
Solution Approach 2:
The patent creates a composite formulation system by combining the novel crystalline Modification V with specific excipients and carriers. This composite approach enhances overall formulation stability, prevents polymorph conversion, and maintains consistent performance during storage and after application dilution
2Productivity
If existing crystalline modifications are used, then formulations can be prepared, but they form residues that block spraying filters after dilution
Solution Approach 1:
The novel crystalline Modification V possesses altered physical parameters including particle size distribution, surface area, and solubility characteristics that prevent residue formation. These parameter changes enable complete dissolution and suspension stability, eliminating filter blockage issues while maintaining high spraying efficiency and coverage
3Ease of manufacture
If existing crystalline modifications are used, then formulations can be prepared, but they are difficult to comminute and grind
Solution Approach 1:
The novel crystalline Modification V exhibits different mechanical properties including reduced crystal hardness and improved friability compared to existing modifications. These parameter changes facilitate easier comminution, grinding, and size reduction during manufacturing, reducing energy consumption and improving processing efficiency while maintaining formulation 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
The crystalline modification V of emamectin benzoate provides long-term stability to formulations, reducing residue formation and improving handling characteristics, making it more suitable for commercial agrochemical preparations.
Implementation Method 1
the crystalline polymorph of emamectin benzoate, termed crystalline modification V in the following, has a significant improvement in its stability. The crystalline modification V does not convert to other crystalline modifications even during prolonged storage.
Implementation Method 2
the crystalline modification V has a lower tendency to aggregate and recrystallize after dilution compared to the other crystalline modifications described in U.S. Pat. No. 6,486,195
Data Source
AI summary
A crystalline modification V of emamectin benzoate, exhibiting at least 3 of the following reflexes in an X-ray powder diffractogram recorded using Cu—Kα radiation at 25° C.:2θ=4.34±0.2 (1)2θ=10.58±0.2 (2)2θ=12.32±0.2 (3)2θ=15.19±0.2 (4)2θ=18.57±0.2 (5)2θ=20.41±0.2 (6)A process for the preparation of emamectin benzoate in the aforementioned form comprises i) preparing a solution of a solid form of emamectin benzoate in a solvent comprising ethyl acetate and n-hexane; ii) effecting crystallization of emamectin benzoate from the solution; and iii) isolating the emamectin benzoate formed. The crystalline modification V can be formulated to any suitable pesticidal formulations.