Transdermal Patch Composition for Acidic Drugs
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Solution Overview
Problem
Existing transdermal absorption preparations fail to provide stable and superior transdermal absorbability for drugs due to volatility of solvents and limited skin permeation, often showing enhanced effects only for specific drugs or not achieving broad utility.
Innovation Solution
A composition comprising a polyvalent alcohol with 3-8 carbon atoms, a higher alcohol with 12-20 carbon atoms, and an organic amine with 2-9 carbon atoms, where the polyvalent alcohol constitutes 90-97% of the total weight, is used to enhance transdermal absorption, particularly for acidic drugs, in patch preparations.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional solvents (lower alcohols, fatty acid ionic liquids) are used to improve transdermal absorbability, then transdermal absorption is enhanced, but the composition becomes unstable due to solvent volatilization
Solution Approach 1:
The patent changes the key parameter from using conventional lower alcohols (1-3 carbon atoms) to higher alcohols (12-20 carbon atoms) with much lower volatility. This parameter change maintains the transdermal absorption enhancement while eliminating the stability problem caused by solvent volatilization. The higher alcohols provide a stable composition base that doesn't evaporate readily.
Solution Approach 2:
The patent creates a composite solvent system combining higher alcohol (12-20 carbon atoms) with polyvalent alcohol (3-8 carbon atoms) and organic amine (2-9 carbon atoms) in specific proportions. This composite material leverages the low volatility of higher alcohol while incorporating the skin permeation enhancement properties of polyvalent alcohols and organic amines, achieving both stability and enhanced absorption.
2Quantity of substance
If existing composition formulations are used, then some transdermal absorption enhancement is achieved, but skin permeation amount of drug cannot be sufficiently increased
Solution Approach 1:
The patent optimizes the carbon atom count parameters of the solvent components: higher alcohol (12-20 carbons) provides stability, while polyvalent alcohol (3-8 carbons) and organic amine (2-9 carbons) provide permeation enhancement. The specific proportion ranges (higher alcohol: 1-99 wt%, polyvalent alcohol: 1-50 wt%, organic amine: 1-50 wt%) are carefully determined to achieve sufficient drug permeation and reliable pharmacological effects.
3Quantity of substance
If conventional transdermal absorption enhancing compositions are used, then absorption enhancement is achieved for particular drugs, but broad utility is not obtained
Solution Approach 1:
The patent creates a universal solvent composition system that can enhance transdermal absorption of various acidic drugs with different molecular structures and properties. The combination of higher alcohol, polyvalent alcohol, and organic amine provides a versatile platform that works across multiple drug types, achieving broad utility while maintaining absorption enhancement effectiveness.
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 composition significantly improves the transdermal absorption of acidic drugs, achieving high skin permeability and broad utility, allowing for effective and stable delivery of drugs through transdermal patches.
Implementation Method 1
A composition for enhancing transdermal absorption of an acidic drug, comprising a polyvalent alcohol having 3 - 8 carbon atoms, a higher alcohol having 12 - 20 carbon atoms and an organic amine having 2 - 9 carbon atoms
Data Source
AI summary
The problem of the present invention is to provide a composition for enhancing transdermal absorption of a drug, which shows a sufficiently high enhancing effect on transdermal absorption of an acidic drug. A composition for enhancing transdermal absorption of an acidic drug, comprising a polyvalent alcohol having 3 - 8 carbon atoms, a higher alcohol having 12 - 20 carbon atoms and an organic amine having 2 - 9 carbon atoms.