Transdermal Drug Composite Particles for Crystallization Suppression
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Solution Overview
Problem
Transdermal absorbable preparations with drugs of poor solubility in a base face challenges in maintaining stability and preventing crystallization, leading to inadequate skin permeability and prolonged time to drug efficacy.
Innovation Solution
The use of composite particles composed of a silicate compound, such as silicic anhydride, and an organic acid, like acetic acid, in a transdermal absorbable preparation, which are complexed with the drug, enhances crystallization suppression and skin absorbability, improving stability and reducing the time to drug efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a drug with poor solubility in a base is blended in high concentration to improve transdermal absorbability, then transdermal absorbability is improved, but the drug is apt to crystallize and stability deteriorates
Solution Approach 1:
The patent introduces silicic anhydride particles as an intermediary substance between the drug and the base. These particles serve as a mediator that prevents direct interaction between the poorly soluble drug and the base, thereby suppressing crystallization while maintaining high drug concentration for improved transdermal absorbability. The silicic anhydride acts as a protective intermediary that stabilizes the drug in the base without compromising its therapeutic efficacy.
2Stability of the object's composition
If silicic anhydride is used to suppress crystallization of the drug, then crystallization is suppressed initially, but the suppression effect deteriorates over time due to temperature and humidity changes
Solution Approach 1:
The patent creates a composite material system consisting of silicic anhydride particles combined with specific polymers (polyethylene glycol and polyisobutylene) in defined ratios. This composite structure provides enhanced stability over time by combining the crystallization-suppressing properties of silicic anhydride with the stabilizing effects of the polymer matrix, which together resist the deteriorating effects of temperature and humidity changes throughout the product's shelf life.
3Reliability
If polyhydric alcohol is blended in much amount to enhance transdermal absorption, then transdermal absorbability is improved, but the aggregation force of the pressure-sensitive adhesive matrix is lowered
Solution Approach 1:
The patent optimizes the concentration parameters of multiple components simultaneously: it specifies precise ranges for polyhydric alcohol (5-30 parts by weight), silicic anhydride (5-30 parts by weight), and polymer content (70-50 parts by weight). By carefully adjusting these parameters within defined ranges, the formulation achieves both high transdermal absorbability through sufficient polyhydric alcohol content and maintains adequate aggregation force through balanced polymer content and silicic anhydride reinforcement.
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
This approach results in a stable transdermal absorbable preparation with improved skin permeability, allowing for rapid drug efficacy and maintaining homogeneity and manufacturing aptness, even with high concentrations of poorly soluble drugs.
Implementation Method 1
crystallization of the drug is more surely suppressed, and as a result of further research, also found that, by blending composite particles of the silicate compound and the organic acid in a transdermally absorbable preparation comprising the drug and a base
Implementation Method 2
transdermally absorbable preparation comprising a drug blended with a silicate compound and an organic acid
Data Source
AI summary
A transdermally absorbable preparation that even when a drug with poor solubility in a base is added in high concentration, is stable over time and can suppress crystallization of the drug, excelling in transdermal absorbability. There is provided a transdermally absorbable preparation, comprising a base and, added thereto, at least composite particles which are composed of a silicate compound and an organic acid and a drug.