Urea–Surfactant Complexes for Rapid Active Dissolution
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Solution Overview
Problem
Existing methods for delivering poorly soluble agrochemical and pharmaceutical active ingredients face challenges in achieving rapid release and enhanced bioavailability, particularly in agricultural applications where formulations are sprayed on target plants or soil, leading to inconsistent results and insufficient solubilization.
Innovation Solution
Compositions comprising urea and non-ionic surfactants in specific ratios form a single-phase solution with active ingredients, allowing for rapid dissolution and formation of small, bioavailable particles upon contact with water, suitable for agricultural and pharmaceutical applications.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If active ingredients are milled to fine particles and suspended in water (suspension concentrate), then delivery to target is improved, but solubility remains insufficient for particularly insoluble actives
Solution Approach 1:
The patent changes the physical-chemical parameters of the active ingredient by forming amorphous solid dispersions, transforming crystalline materials into amorphous states with enhanced solubility and dissolution rates without requiring complex formulation additions
Solution Approach 2:
The patent creates composite materials by combining active ingredients with carriers or excipients in amorphous solid dispersion systems, producing a new material state that exhibits improved solubility properties while maintaining formulation simplicity
2Reliability
If crop oil concentrates are added to enhance delivery, then uptake is improved, but cost and complexity increase
Solution Approach 1:
The patent extracts and eliminates the need for separate oil adjuvants by incorporating solubility-enhancing carriers directly into the formulation, simplifying the application process while maintaining consistent delivery performance
Solution Approach 2:
The patent creates multi-functional formulations where the carrier serves both as a solubility enhancer and delivery vehicle, replacing the need for separate adjuvant products and simplifying the overall application system
3Speed
If amorphous solid dispersions are used in pharmaceuticals, then dissolution is accelerated, but recrystallization occurs during storage
Solution Approach 1:
The patent applies stabilizing agents and optimized formulation compositions before storage to prevent recrystallization, cushioning against the inherent instability of amorphous states during long-term storage while maintaining rapid dissolution when applied
Solution Approach 2:
The patent carefully controls physical-chemical parameters such as glass transition temperature, molecular mobility, and formulation composition to stabilize the amorphous state during storage while preserving the rapid dissolution characteristics when the formulation is activated
4Quantity of substance
If high loadings of active ingredients are achieved, then efficacy is improved, but solubility and bioavailability decrease
Solution Approach 1:
The patent changes the physical state and molecular environment of the active ingredient through amorphous solid dispersion, enabling high loadings to be achieved while maintaining enhanced solubility and bioavailability compared to crystalline forms
Solution Approach 2:
The patent develops composite material systems where the active ingredient is dispersed at molecular levels within carriers, allowing high concentrations to be achieved without the aggregation and solubility loss that typically occurs with simple mixing
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 urea complexes enable high loadings of active ingredients with improved bioavailability and efficacy, providing superior dissolution and dispersion properties, stabilizing actives against decomposition, and enhancing foliar uptake.
Implementation Method 1
compositions in solid form based on urea and comprising active ingredients with certain structural and physical properties and non-ionic surfactants in certain amounts and ratios, allow quick dissolution in water or aqueous diluents
Implementation Method 2
comprising (a) a total amount of at least about 5% by weight of one or more pesticidal or pharmaceutical active ingredients... (c) a total amount of at least about 1% by weight of one or more non-ionic surfactants
Data Source
AI summary
The present invention relates to the technical field of delivery systems for agrochemical active ingredients or pharmaceutical active ingredients. The present invention primarily relates to certain compositions in solid form comprising as constituent (a) at least one agrochemical or pharmaceutical active ingredients, as constituent (b) urea, and as constituent (c) at least one non-ionic surfactant. The present invention also relates to products obtainable or obtained by the processes defined in the context of the present invention. The present invention further relates to formulations comprising these compositions or products and application mixtures obtainable or obtained by dilution of these compositions or products with water or aqueous surfactant solutions. The present invention further relates to processes for preparing these compositions, products, formulations and application mixtures as well as to uses thereof and methods of using these compositions, products, formulations and application mixtures.