Avermectin Emulsion Viscosity Control via Cooling Plateau
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Solution Overview
Problem
Existing emulsions containing avermectins, such as ivermectin, experience significant viscosity increases due to the swelling of lamellar structures formed by non-ionic surfactants and fatty alcohols, leading to instability and affecting product quality, which necessitates a holding period before release, impacting manufacturing economics.
Innovation Solution
A controlled cooling process is implemented for the emulsion after introducing the avermectin active phase, where the emulsion is emulsified at 60-75°C, cooled to 48-55°C, and then cooled to 30-40°C at a controlled rate of 0.5-1.5°C/min or maintained at a plateau temperature before reaching the target temperature, stabilizing the viscosity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If the emulsion is prepared using conventional cooling methods, then the emulsion is formed, but the viscosity increases significantly (30-150%) during the week following manufacture
Solution Approach 1:
The patent applies parameter changes by controlling the cooling rate from 0.5-1.5°C per 5 minutes and maintaining a plateau temperature of 42-47°C for 10-20 minutes before final cooling to 30-40°C. This controlled temperature profile prevents the swelling of lamellar structures that causes viscosity increase, thereby maintaining viscosity stability without requiring extended holding time.
Solution Approach 2:
The patent implements preliminary action by controlling the cooling process and maintaining a temperature plateau before final cooling to prevent viscosity increase in advance. This proactive approach stabilizes the emulsion structure before it can undergo the swelling phenomenon, eliminating the need for post-manufacturing holding periods.
2Productivity
If the emulsion is cooled rapidly to save time, then productivity increases, but the viscosity becomes unstable and increases significantly
Solution Approach 1:
The patent optimizes the cooling parameters by implementing a controlled cooling rate of 0.5-1.5°C per 5 minutes with a plateau phase, rather than rapid cooling. This optimized parameter set maintains both manufacturing efficiency and viscosity stability, resolving the contradiction between productivity and composition stability.
3Reliability
If the emulsion is held for extended periods to ensure quality, then product quality is maintained, but manufacturing economics are negatively impacted
Solution Approach 1:
The patent applies preliminary action by implementing controlled cooling and temperature plateau maintenance during the manufacturing process itself to ensure product quality. This prevents quality issues before they occur, eliminating the need for extended holding periods and thereby maintaining both high reliability and manufacturing efficiency.
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 process maintains a stable viscosity within 10% variation over 7 days post-manufacturing, ensuring physical and chemical stability of the emulsion, preventing recrystallization of avermectin, and allowing for consistent product quality without the need for extended maturation periods.
Implementation Method 1
cooling said emulsion to a target temperature of from 30 to 40°C, wherein in said cooling step, said emulsion is subjected to a controlled cooling to said target temperature
Implementation Method 2
it is assumed that this increase in viscosity is due to the swelling in water of lamellar structure formed by the non-ionic surfactants and fatty alcohols initially present in the oily phase
Data Source
Figure 1A~1B
Figure 2~3
Figure 4A~4B
AI summary
The present invention pertains to a process for preparing a stable emulsion comprising at least one avermectin. It is also directed to the emulsion thus obtained, especially for use in the treatment of dermatological disorders such as rosacea.