Fungicidal Salt Associate Particle Size Reduction
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Solution Overview
Problem
Existing fungicidal agents, such as fluconazole and the salt of 2.4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidene)amino-1,3-pyrimidine, have low solubility in aqueous and fatty media, limiting their effectiveness in medical, veterinary, and agricultural applications due to large particle size, which restricts their use in solutions for injections, inhalations, and treatments.
Innovation Solution
The synthesis of a salt associate, 5-[3,5-thiane-2-hydroxybenzylidene)amino]-4-hydrox-1H-pyrimidine-2-on with 1,2,3,4,5-pentahydroxy-6-methylaminohexane, resulting in particles with a length of less than 10 μm, significantly increasing solubility in water and oils, enabling more effective solution concentrations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If the fungicidal agent uses the salt of 2.4-dioxo-5-(2-hydroxy-3,5-dichlorobenzylidene)amino-1,3-pyrimidine, then it has pronounced antifungal activity with wide spectrum of effect, but it has very poor solubility in aqueous media and fats due to large particle size
Solution Approach 1:
The patent applies segmentation by mechanically breaking down the large crystal particles of the fungicidal agent into much smaller particles (reducing size by a factor of 3-4). This particle size reduction increases the surface area to volume ratio, thereby significantly improving solubility in both aqueous and fatty media while preserving the chemical structure and antifungal activity of the active substance.
Solution Approach 2:
The patent changes the physical parameter of particle size without altering the chemical composition of the fungicidal agent. By reducing particle dimensions, the substance achieves better dissolution properties in water and fats, enabling the preparation of solutions with higher concentrations of the active ingredient while maintaining its broad-spectrum antifungal efficacy.
2Stability of the object's composition
If the fungicidal agent has large particle size, then it maintains stable crystal structure, but it does not promote dissolution in aqueous or fatty media
Solution Approach 1:
The patent segments the large stable crystals into smaller particles through mechanical comminution. This process maintains the internal crystal structure and chemical stability of each particle while reducing overall particle size, thereby enabling better dissolution without compromising the stability of the active substance's composition.
Solution Approach 2:
The patent changes the physical parameter of particle size while preserving the chemical and structural integrity of the fungicidal agent. The reduced particle size enhances dissolution capability in aqueous and fatty media, making the substance easier to manufacture into effective solutions while maintaining compositional stability.
3Quantity of substance
If the solution concentration of the fungicidal agent is low, then it is easier to dissolve in aqueous media, but the solution is not sufficiently effective for treatment
Solution Approach 1:
The patent segments the fungicidal agent particles to reduce their size, which dramatically increases their solubility. This allows the preparation of solutions with much higher concentrations of the active substance (over 100-fold increase) while ensuring complete dissolution, thereby achieving both high solubility and sufficient treatment effectiveness.
Solution Approach 2:
The patent changes the particle size parameter to enable higher concentrations of the active substance to be dissolved in aqueous and fatty media. This parameter change allows the formulation of solutions with concentrations that are both achievable (due to improved solubility) and effective (due to higher active ingredient content).
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 new fungicidal agent achieves solubility up to 0.3-0.4% in water and 0.25-0.3% in oils, enhancing its therapeutic and preventative efficacy in treating fungal diseases and spoilage across various fields.
Implementation Method 1
A significant shift of the azomethine proton signal downfield (from 9.5 to 10 ppm) was registered, indicating the formation of a strong hydrogen bond.
Data Source
AI summary
The invention relates to a novel fungicidal agent in the form of a salt associate having the structural formula shown. The agent can be used for treating diseases caused by fungi, and also for preventing fungal damage to various materials and agricultural products. The present fungicidal agent is an associate of 5-[3,5-dichloro-2-hydroxy benzylidene)amino]-4-hydroxy-1H-pyrimidine-2-on with 1,2,3,4,5-pentahydroxy-6-methylaminohexane and has the formula (I).This fungicidal agent exhibits a broad range of activity and high solubility, which increases the effectiveness of the use thereof in the form of solutions. Compounds were obtained in a crystalline form, and the structure thereof was established by means of magnetic resonance spectra in dimethyl sulfoxide.