PEG Alkyl Ether Acylamide Carrier for Stable Topical Emulsions
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Solution Overview
Problem
Acylamides are difficult to incorporate and solubilize within emulsions, leading to instability and reduced trans-cutaneous absorption, which affects their biological activity and application in topical formulations.
Innovation Solution
A carrier composition comprising an acylamide and a polyethylene glycol alkyl ether dispersing agent, prepared by heating and cooling to form an amorphous mixture, facilitating dispersion and incorporation into emulsions without recrystallization.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If acylamides are solubilized within the fatty phase of an emulsion using very high temperatures (above 90°C), then the solubility of acylamides is improved, but the thermal stability of active substances and lipophilic excipients is compromised, leading to degradation
Solution Approach 1:
The invention changes the temperature parameter from very high temperatures (above 90°C) to moderate temperatures (60-80°C), and introduces a specific weight ratio parameter (1:3 to 1:10 of acylamide to fatty acid amide) to achieve solubilization under milder conditions that preserve thermal stability of other components
Solution Approach 2:
The invention introduces fatty acid amides as an intermediary substance that facilitates the solubilization of acylamides in the fatty phase. The fatty acid amide acts as a mediator that enables acylamide incorporation at lower temperatures, preventing direct thermal exposure of other heat-sensitive active substances and excipients
2Adaptability or versatility
If acylamides are incorporated into emulsions, then the topical application potential is improved, but recrystallization occurs after cooling, impairing physico-chemical stability
Solution Approach 1:
The invention optimizes the weight ratio parameter of acylamide to fatty acid amide (1:3 to 1:10), which prevents recrystallization by maintaining acylamides in a solubilized state within the fatty phase even after cooling, thus preserving emulsion stability
Solution Approach 2:
The invention creates a composite system combining acylamides with fatty acid amides in specific proportions, forming a stable mixed fatty phase that prevents phase separation and recrystallization, enhancing overall emulsion stability
3Adaptability or versatility
If acylamides are incorporated into emulsions, then topical application is enabled, but trans-cutaneous absorption is reduced due to partial recrystallization
Solution Approach 1:
The invention optimizes the concentration ratio of acylamide to fatty acid amide (1:3 to 1:10), ensuring complete solubilization that prevents recrystallization and maintains acylamides in an absorbable state for effective trans-cutaneous delivery
Solution Approach 2:
Fatty acid amides serve as a mediator that keeps acylamides in solution within the fatty phase, preventing crystallization that would block absorption pathways and enabling sustained trans-cutaneous penetration
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 carrier composition enhances the stability and biological activity of acylamides by promoting trans-cutaneous absorption and ease of use in topical formulations, improving their effectiveness in treating skin conditions.
Implementation Method 1
a dispersing agent consisting of a polyethylene glycol alkyl ether of formula II wherein R1 is a linear or branched, saturated alkyl, characterized by a number of carbon atoms comprised between C1 and C4, wherein one of the carbons may or may not be bonded to a hydroxyl, m is comprised between 16 and 18, n is comprised between 7 and 10, z is comprised between 9 and 14, the first solid active and the dispersing agent are in a weight ratio comprised between 1:1.5 and 1:23, so that the first solid active is dispersed in the dispersing agent
Implementation Method 2
heating the dispersing agent at a temperature ≥ 25°C
Data Source
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Figure 5~6
AI summary
The present patent application relates to a carrier composition comprising a first solid active consisting of an acylamide of formula I, a dispersing agent consisting of a polyethylene glycol alkyl ether of formula II, wherein: R1 is a linear or branched, saturated alkyl, characterized by a number of carbon atoms comprised between C1 and C4, wherein one of the carbons may or may not be bonded to a hydroxyl, m is comprised between 16 and 18, n is comprised between 7 and 10, z is comprised between 9 and 14, the first solid active and the dispersing agent are in a weight ratio comprised between 1:1.5 and 1:23, so that the first solid active is dispersed in the dispersing agent.