Tranexamic Acid Ester Sulfonate Salts for Stable Skin Dispersions
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing tranexamic acid ester salts have poor solubility in water and oil, leading to crystallization and aggregation in cosmetic compositions, resulting in product instability and poor texture and feel, and require multi-step processes or petrochemical-derived polymers for stabilization.
Innovation Solution
Development of tranexamic acid ester salts with sulfonic acid counter-ions, such as lauryl, myristyl, cetyl, and stearyl tranexamate mesylate, esylate, besylate, and tosylate, which form stable and homogeneous aqueous dispersions without additional processing steps or secondary materials.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional tranexamic acid ester salts (e.g., hydrochloride salts) are used in cosmetic compositions, then the compositions can provide anti-pigmentation effects, but the salts exhibit poor solubility in water and oil, leading to crystallization and aggregation
Solution Approach 1:
The patent changes the chemical parameter of the counter-ion from conventional hydrochloride to sulfonic acid derivatives (mesylate, esylate, besylate, tosylate). This parameter change fundamentally alters the solubility characteristics of the tranexamic acid ester salt, enabling it to form stable aqueous dispersions without crystallization or aggregation, thereby resolving the solubility-stability contradiction
Solution Approach 2:
The patent creates a composite salt structure by combining tranexamic acid ester with specific sulfonic acid counter-ions. This composite approach produces a new material class that inherently possesses both the desired anti-pigmentation activity and improved solubility/dispersibility properties, eliminating the need for additional stabilizers
2Reliability
If complex emulsions or multi-step processes are used to stabilize tranexamic acid ester salts, then product stability can be improved, but the manufacturing complexity and cost increase
Solution Approach 1:
The sulfonic acid ester salts of tranexamic acid esters are self-stabilizing in aqueous environments. The molecular structure inherently prevents crystallization and aggregation without requiring external stabilizers, amphiphilic substances, or complex emulsion systems. This self-service property dramatically simplifies the formulation process from multi-step complex procedures to simple mixing operations
Solution Approach 2:
The patent extracts and eliminates the need for secondary stabilizing materials and complex processing steps. By using the sulfonic acid ester salt form, the formulation no longer requires amphiphilic polymers, emulsifiers, or multi-step stabilization processes, thereby reducing manufacturing complexity and cost while maintaining stability
3Stability of the object's composition
If secondary materials such as petrochemical-derived polymers are used to stabilize tranexamic acid ester salts, then dispersion stability can be improved, but consumer acceptance decreases due to preference for natural and simple products
Solution Approach 1:
The sulfonic acid ester salts provide self-stabilization through their inherent molecular structure. The salts naturally form stable aqueous dispersions without requiring petrochemical-derived polymers or synthetic stabilizers. This eliminates the conflict between stability and natural product preference, as the stabilization comes from the salt itself rather than external synthetic additives
Solution Approach 2:
By changing the counter-ion parameter to sulfonic acid derivatives, the patent fundamentally alters the interaction between the active ingredient and water. This parameter change enables natural, simple aqueous dispersions that are both stable and consumer-friendly, eliminating the need for petrochemical polymers while maintaining dispersion stability
Data Source
AI summary
Various salts of tranexamic acid esters compounds are described, along with compositions including such compounds. Methods of use for treatment of external surfaces (e.g. skin) and processes of producing the compounds and compositions are also described.