Pyripyropene Emulsifiable Formulation Stability via Heating

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Solution Overview

Problem

Liquid emulsifiable formulations of pyripyropene derivative I exhibit low physical stability upon storage, leading to crystalline material formation and dosage issues, and the use of certain adjuvants can further decrease stability, making it challenging to maintain stability regardless of the starting material used.

Innovation Solution

A method involving dissolving surfactants and pyripyropene derivative I in an aromatic hydrocarbon solvent, followed by heating the solution to at least 40°C to create a stable emulsifiable formulation that remains homogeneous and stable for prolonged storage periods, even at extreme temperatures.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If pyripyropene derivative I is solubilized in aromatic hydrocarbon solvent for emulsifiable formulation, then the formulation can be diluted with water to form emulsion, but crystalline material forms upon storage reducing physical stability

Engineering Contradiction:
Improveemulsion formation capabilityVSAvoidphysical stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent changes the physical state parameter by heating the formulation to 40°C or higher. This temperature parameter change prevents crystalline material formation and maintains physical stability while preserving emulsion formation capability. The heating step transforms the system from a potentially unstable state to a stable homogeneous solution.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite system combining pyripyropene derivative I, aromatic hydrocarbon solvent, and surfactant in specific proportions. This composite formulation maintains solubility and prevents crystallization through the synergistic interaction of components, particularly the surfactant which stabilizes the emulsion and prevents precipitation.

Inventive Principle:
Principle #40Composite materials

2Reliability

If surface active adjuvant is added to enhance insecticidal activity, then bioactivity is improved, but solubilization of pyripyropene derivative I is interfered with decreasing physical stability

Engineering Contradiction:
Improveinsecticidal activityVSAvoidphysical stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent applies temperature parameter change (heating to 40°C or higher) to overcome the solubilization interference caused by adjuvants. This thermal energy input disrupts the unfavorable interactions between adjuvant and pyripyropene derivative, restoring solubility and physical stability while maintaining the adjuvant's bioactivity enhancement function.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent performs preliminary heating treatment during formulation preparation to prevent crystalline material formation before storage. This advance action ensures that the interaction between adjuvant and active ingredient does not lead to precipitation during subsequent storage, maintaining both stability and activity.

Inventive Principle:
Principle #10Preliminary action

3Ease of manufacture

If conventional formulation method is used without heating, then manufacturing is simple, but crystalline material separates causing dosage problems and clogging

Engineering Contradiction:
Improveformulation simplicityVSAvoiddosage accuracy
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent introduces a temperature parameter change (heating to 40°C or higher) as a simple process modification. This single parameter change prevents crystalline material separation, ensuring accurate dosing and preventing clogging, while adding minimal complexity to the manufacturing process.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies preliminary heating during the formulation preparation stage to prevent crystallization issues before they occur. This advance treatment ensures that the final formulation remains stable during storage and application, eliminating dosage accuracy problems and clogging risks.

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 method produces stable liquid emulsifiable formulations that prevent crystalline material formation, ensuring consistent performance and ease of use without stability issues, even after prolonged storage and extreme temperature exposure.

Implementation Method 1

heating the solution to a temperature of at least 40°C

Methodology Applied
Scientific EffectThermal energy input: Heating

Data Source

PatentEP2945481B1Method for producing a liquid emulsifiable formulation comprising a pyripyropene pesticide
Publication Date: 2019.03.13 BASF SE
  • EP2945481B1 patent drawing
  • EP2945481B1 patent drawing
  • EP2945481B1 patent drawing

AI summary

The present invention relates to a method for producing a liquid non-aqueous emulsifiable formulation comprising a pyripyropene pesticide of the formula (I) as defined below which is dissolved in an aromatic hydrocarbon or hydrocarbon mixture containing surfactants, which stabilize the emulsion upon dilution with water, which method comprises the steps i) and ii) as described hereinafter: i) dissolving the at least one surfactant and the compound of formula (I) in the organic solvent or solvent mixture to obtain a clear solution of the at least one surfactant and the compound of the formula(I); ii) heating the solution to a temperature of at least 40°C.