Tranexamate Salt Fine Particle Dispersion in External Compositions
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Solution Overview
Problem
Tranexamate is sparingly soluble in water or oil, making it difficult to formulate stable mixtures for external use, and existing methods result in sticky or oily formulations with limited choices for product forms.
Innovation Solution
Dispersing tranexamate salt in the form of fine particles, combined with a water-soluble polymer, to stabilize the active ingredient and prevent crystal growth, allowing for a broader range of formulation options and improved skin-whitening activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If a tranexamate is dissolved in a large amount of oil component to improve solubility, then the solubility is enhanced, but the formulation becomes sticky and oily with limited product form choices
Solution Approach 1:
The patent changes the physical state of tranexamate from dissolved to dispersed fine particles (0.1-100 μm), fundamentally altering how the substance exists in the formulation. This particle size reduction and state change allows adequate solubility without requiring excessive oil components, thereby eliminating the sticky and oily feeling while maintaining stability.
Solution Approach 2:
The patent creates a composite system combining tranexamate fine particles with specific cosmetic ingredients (emulsifiers, surfactants, thickeners) to achieve stable dispersion. This composite approach allows the tranexamate to be effectively delivered without relying on large amounts of oil, thus avoiding the harmful sticky and oily characteristics while maintaining solubility and stability.
2Object-generated harmful factors
If a tranexamate is dispersed as fine particles to eliminate sticky and oily feeling, then the sense of use is improved, but stable dispersion and prevention of crystal growth become challenging
Solution Approach 1:
The patent introduces intermediary substances (emulsifiers, surfactants, and thickeners) that mediate between the tranexamate fine particles and the aqueous base. These intermediaries prevent crystal growth by stabilizing the particle surfaces and maintain uniform dispersion, solving the stability challenge without requiring the particles to be dissolved.
Solution Approach 2:
The patent carefully controls particle size parameters (0.1-100 μm) and uses specific concentrations of stabilizing agents to optimize both the sensory properties and stability. By precisely controlling these parameters, the formulation achieves non-sticky, non-oily feel while maintaining long-term stability against crystal growth and aggregation.
3Stability of the object's composition
If tranexamate is used in dissolved form to ensure uniform distribution, then the formulation is homogeneous, but the formulation form is limited to cream or milky lotion
Solution Approach 1:
The patent changes the distribution state from molecular dissolution to fine particle suspension (0.1-100 μm), which fundamentally expands formulation versatility. This particle-based approach allows the active ingredient to be uniformly distributed while enabling diverse product forms including lotions, creams, gels, and washes, unlike dissolved forms that are limited to specific vehicle types.
Solution Approach 2:
The patent creates a universal delivery system using fine particles that can be adapted to multiple formulation types and application methods. The particle-based approach serves multiple functions: maintaining uniform distribution, enabling various product forms, providing stable dispersion, and eliminating oily feel, making the system universally applicable across different cosmetic and pharmaceutical products.
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 provides a stable, non-sticky, and non-oily composition that maintains skin-whitening activity over time, offering a comfortable application feel and versatile product forms.
Implementation Method 1
adding at least one salting-out agent into the obtained solution to precipitate the salt as crystals in the state of fine particles having an average particle size of 0.01 μm to 100 μm
Implementation Method 2
the salt of the tranexamate can be dispersed more stably by combining the salt with a water-soluble polymer selected from nonionic polymers and cationic polymers in the composition
Data Source
AI summary
A composition for external use containing a physiologically acceptable salt of a tranexamate as an active ingredient, which is dispersed in the composition in the state of fine particles, is provided. Thereby, a physiologically acceptable salt of the tranexamate is dissolved in a solvent to prepare a solution, to which a salting-out agent is added to precipitate the salt. Such salt is so dispersed in a composition for external use in the state of fine particles that the tranexamate salt can be mixed without using a large amount of an oil component to obtain a composition for external use affording excellent feel of use and stability.