Iontophoretic Patch Composition Low-Temperature Stability
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Solution Overview
Problem
Current iontophoretic transdermal delivery systems for triptan compounds, such as Sumatriptan, are unstable at low temperatures, leading to viscosity reduction and precipitation of lauric acid, which compromises the stability and efficacy of the drug delivery.
Innovation Solution
A modified composition comprising a salt of a triptan compound, a polyamine, a dicarboxylic acid, and water, with the removal of monocarboxylic acids and the use of a different polyamine like KOLLICOAT® SMARTSEAL, which maintains viscosity and conductivity, ensuring stability at low temperatures and preventing leakage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a conventional iontophoretic transdermal delivery system for triptan compounds is used, then transdermal delivery of the drug is achieved, but the composition becomes unstable at low temperatures leading to viscosity reduction and precipitation
Solution Approach 1:
The patent changes the chemical composition parameters by replacing monocarboxylic acids with dicarboxylic acids (specifically adipic acid) and using specific polyamines (EUDRAGIT® E 100). This chemical parameter change fundamentally alters the composition's behavior at low temperatures, preventing the viscosity reduction and precipitation that occur with conventional formulations. The new parameter combination creates a composition that remains stable across a wider temperature range.
2Productivity
If the composition is formulated for transdermal delivery, then drug delivery function is achieved, but leakage occurs at low temperatures due to viscosity loss
Solution Approach 1:
The patent applies prior cushioning by pre-formulating the composition with dicarboxylic acids and polyamines in specific proportions before any temperature exposure occurs. This preventive formulation approach ensures that when low temperatures are encountered, the composition already has the chemical structure necessary to maintain viscosity and prevent leakage, rather than attempting to correct the problem after viscosity loss occurs.
3Ease of operation
If standard iontophoretic composition is used, then basic transdermal delivery is achieved, but higher voltage is required due to lower conductivity
Solution Approach 1:
The patent changes the electrical conductivity parameter by selecting specific polyamine compounds (EUDRAGIT® E 100) and dicarboxylic acids that, when combined, create a composition with inherently higher conductivity. This parameter change reduces the voltage requirement for iontophoretic delivery, making the system easier to operate with lower energy input while maintaining effective drug delivery.
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 modified composition maintains viscosity and stability at temperatures below 15°C, preventing precipitation and ensuring effective transdermal delivery of Sumatriptan, with higher conductivity allowing lower voltage application and minimizing patch leakage.
Implementation Method 1
maintains viscosity and conductivity, ensuring stability at low temperatures
Implementation Method 2
iontophoresis is a delivery method which relies on the basic principle that application of electric current can provide external energy to enable or enhance the passage of drug ions across the skin
Implementation Method 3
When ions bearing a positive charge (e. g. cationic active agents) are placed into or under the anode of an iontophoretic system, these ions will then—upon application of current—be forced to move away from the anode and, following the direction of the electrical field, towards the cathode
Data Source
AI summary
The present invention relates to frigostable compositions suitable for iontophoretic transdermal delivery of a triptan compound. The inventive compositions include a salt of a triptan compound, preferably sumatriptan succinate, a polyamine, a dicarboxylic acid, and water or an aqueous solvent mixture, with the composition being free of monocarboxylic acids. The invention further relates to the use of the composition as an integral component of an iontophoretic patch, preferably as an anodic reservoir of the patch.