Topical Vitamin D3 Composition for Stability in High-Water Formulas
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Solution Overview
Problem
Vitamin D3 stability decreases upon dissolution in water, particularly when the water content increases, posing a challenge in topical compositions containing both vitamin D3 and glucocorticoids.
Innovation Solution
A topical composition comprising vitamin D3, a glucocorticoid, a polyoxyalkylene hydrogenated castor oil as nonionic surfactant A, and another nonionic surfactant B, such as polyoxyalkylene alkyl ethers or polyoxyalkylene glycols, with specific HLB values and content ranges, along with an ester oil and water, to enhance stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If water content is increased in the topical composition, then the composition becomes more suitable for topical application and patient comfort, but the stability of vitamin D3 decreases
Solution Approach 1:
The patent introduces a specific nonionic surfactant system (polyoxyalkylene hydrogenated castor oil combined with another nonionic surfactant having HLB value of 6 or more) as an intermediary between water and vitamin D3. This surfactant system forms micellar structures that solubilize vitamin D3 in the aqueous environment while protecting it from degradation, enabling high water content formulations to maintain vitamin D3 stability.
Solution Approach 2:
The patent changes the physical-chemical parameters of the water-vitamin D3 system by introducing surfactants that alter the microenvironment. The specific combination of nonionic surfactants modifies the solubility characteristics and stability parameters, allowing vitamin D3 to remain stable in high-water-content formulations through controlled micellar encapsulation and interfacial protection.
2Stability of the object's composition
If vitamin D3 is dissolved in water for topical composition, then the composition achieves homogeneous distribution and ease of application, but vitamin D3 stability decreases significantly
Solution Approach 1:
The patent creates a composite surfactant system combining polyoxyalkylene hydrogenated castor oil with another nonionic surfactant (such as polyoxyalkylene alkyl ethers, polyoxyalkylene glycols, polyoxyalkylene fatty acid esters, polyoxyalkylene sorbitol fatty acid esters, or polyglycerol fatty acid esters). This composite surfactant system provides synergistic protection to vitamin D3, maintaining both homogeneity and stability through combined micellar and emulsifying actions.
Solution Approach 2:
The dual nonionic surfactant system acts as an intermediary phase that accommodates vitamin D3 within micellar structures, allowing homogeneous distribution throughout the aqueous formulation while shielding the vitamin from water-induced degradation pathways.
3Ease of operation
If high water content is used in the topical composition, then the composition is more comfortable for skin application, but the therapeutic efficacy may be compromised due to vitamin D3 degradation
Solution Approach 1:
The nonionic surfactant system serves as a protective intermediary that enables high water content formulations to maintain both patient comfort and therapeutic efficacy. The surfactants encapsulate vitamin D3 in stable micellar structures that prevent degradation while allowing the formulation to remain water-based for comfortable topical application.
Solution Approach 2:
The patent modifies the formulation parameters by introducing specific nonionic surfactants that change the microenvironmental conditions for vitamin D3. This allows the macroscopic formulation to have high water content for comfort while the microscopic micellar environment protects vitamin D3 stability and maintains therapeutic efficacy.
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 composition maintains improved stability of vitamin D3 even with increased water content, ensuring effective therapeutic efficacy.
Implementation Method 1
a nonionic surfactant A, which is a polyoxyalkylene hydrogenated castor oil, and a nonionic surfactant B, which is a nonionic surfactant other than polyoxyalkylene hydrogenated castor oils
Data Source
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AI summary
The present invention provides a technique for further improving the stability of vitamin D3 in a topical composition comprising vitamin D3 and a glucocorticoid, even when the amount of water present in the topical composition is increased. Provided is a topical composition comprising vitamin D3, a glucocorticoid, a nonionic surfactant A, which is a polyoxyalkylene hydrogenated castor oil, and a nonionic surfactant B, which is a nonionic surfactant other than polyoxyalkylene hydrogenated castor oils.