Acrylic Adhesive Transdermal Patch for Silodosin Solubility
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Solution Overview
Problem
Current transdermal absorption preparations for α1-blockers like silodosin and tamsulosin face challenges in maintaining high drug solubility and skin permeability, leading to reduced efficacy and increased side effects due to low drug concentrations and insufficient adhesion.
Innovation Solution
A transdermal absorption preparation using an acrylic pressure-sensitive adhesive copolymer with a carboxyl group and a transdermal absorption promoting agent like lauromacrogol, which maintains high drug solubility and skin permeability for extended periods, allowing for higher drug concentrations and improved adhesion.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If the drug concentration in the pressure-sensitive adhesive is increased to improve transdermal absorption efficacy, then the drug solubility requirement increases, but the drug crystallizes in the adhesive layer leading to reduced drug release
Solution Approach 1:
The patent changes the chemical composition parameters of the pressure-sensitive adhesive by incorporating specific solubilizing agents (polyethylene glycol, propylene glycol, ethyl oleate) and adjusting the adhesive polymer structure. This enables the adhesive to maintain drug solubility at higher drug concentrations (silodosin 1-10 wt%, tamsulosin 0.1-5 wt%) without crystallization, resolving the contradiction between increasing drug concentration and maintaining drug solubility.
Solution Approach 2:
The patent creates a composite pressure-sensitive adhesive system combining multiple components: adhesive polymer (acrylic or silicone), solubilizing agents (polyethylene glycol, propylene glycol, ethyl oleate), and transdermal absorption promoters (oleyl alcohol, isopropyl myristate). This composite material achieves both high drug loading capacity and sustained drug release by leveraging the synergistic effects of its components.
2Ease of operation
If oral administration is used to achieve sufficient drug dose, then the drug can be administered easily, but the drug undergoes first-pass metabolism leading to increased side effects and reduced efficacy
Solution Approach 1:
The patent replaces the oral administration route (which involves digestive tract and liver metabolism) with a transdermal delivery system. The pressure-sensitive adhesive patch delivers the drug directly through the skin into systemic circulation, bypassing the first-pass metabolic effect in the liver. This substitution eliminates the harmful first-pass metabolism while maintaining ease of administration through the simple patch application method.
3Duration of action of moving object
If transdermal absorption preparation is used to reduce number of administrations and improve compliance, then the drug efficacy is sustained longer, but the drug solubility and skin permeability must be significantly increased
Solution Approach 1:
The patent introduces transdermal absorption promoters (oleyl alcohol, isopropyl myristate) as intermediary substances that facilitate drug penetration through the skin barrier. These promoters enhance skin permeability by interacting with skin lipids and creating pathways for drug transport. Simultaneously, the solubilizing agents (polyethylene glycol, propylene glycol, ethyl oleate) act as intermediaries to maintain drug solubility in the adhesive matrix, enabling sustained release over extended periods (24 hours or more).
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 preparation effectively maintains silodosin or tamsulosin in a dissolved state for 24 hours or longer, enhancing skin absorption and reducing side effects by achieving higher blood levels and sustained drug release.
Implementation Method 1
the drug having a concentration as high as possible be dissolved in the pressure-sensitive adhesive (the drug solubility)
Implementation Method 2
that said drug be sustainably released from the pressure-sensitive adhesive and be shifted to the skin (the release characteristics of a drug or the skin permeability of a drug)
Data Source
AI summary
Provided is a novel transdermal absorption preparation containing silodosin or tamsulosin, or salt thereof as an active ingredient, wherein the transdermal absorption preparation is capable of keeping a dissolved state for a long time, as well as has a high permeability to a skin, and can effectively and sustainably exert the transdermal absorbability. A transdermal absorption preparation containing the transdermal absorption preparation comprises an acrylic pressure-sensitive adhesive that comprises a copolymer of at least one (meth)acrylic acid monomer and at least one vinyl monomer and that contains a carboxyl group, and at least one transdermal absorption promoting agent selected from the group consisting of oleyl alcohol, lauryl alcohol, and lauromacrogol.