Frigostable Iontophoretic Patch Formulation for Triptan Delivery
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Solution Overview
Problem
Existing triptan compositions, such as Sumatriptan, are unstable at low temperatures, leading to irreversible liquefaction and precipitation of lauric acid, which compromises their viscosity and effectiveness in transdermal iontophoretic delivery systems.
Innovation Solution
Increasing the amount of polyamine, specifically EUDRAGIT® E 100, and dicarboxylic acids like adipic acid in the formulation to enhance frigostability, conductivity, and viscosity, allowing for stable delivery at temperatures below 15°C without leakage or precipitation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If the composition is stored at low temperatures (below 15°C), then the delivery system provides stable transdermal iontophoretic delivery, but the composition undergoes irreversible liquefaction and precipitation of lauric acid, compromising viscosity and effectiveness
Solution Approach 1:
The patent modifies the chemical composition parameters by increasing polyamine content to 10-30% and dicarboxylic acid content to 1-10%, which changes the physical-chemical properties of the formulation to prevent phase separation and precipitation at low temperatures while maintaining delivery stability
Solution Approach 2:
The patent creates a composite formulation system combining triptan compound, polyamine, dicarboxylic acid, and other excipients in specific ratios, where the interaction between components synergistically prevents precipitation and maintains viscosity stability across temperature ranges
2Stability of the object's composition
If the amount of polyamine and dicarboxylic acid is increased to enhance frigostability, then the composition maintains viscosity and prevents precipitation at low temperatures, but the formulation complexity and manufacturing precision requirements increase
Solution Approach 1:
The patent establishes specific parameter ranges (polyamine: 10-30%, dicarboxylic acid: 1-10%) that provide a robust formulation window, allowing manufacturing flexibility while ensuring frigostability is achieved without requiring extreme precision
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 or increases viscosity, ensuring stable delivery and preventing precipitation, thus improving the frigostability and effectiveness of triptan compounds like Sumatriptan in iontophoretic transdermal systems.
Implementation Method 1
Increasing the amount of polyamine, specifically EUDRAGIT® E 100, and dicarboxylic acids like adipic acid in the formulation to enhance frigostability, conductivity, and viscosity
Implementation Method 2
The process of iontophoresis was originally described by LeDuc in 1908... 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 that includes: a salt of a triptan compound, preferably sumatriptan succinate, a polyamine, one or more dicarboxylic acids, 0.5 to 10.0 wt.-% (based on the total weight of the composition) of one or more monocarboxylic acids, and water or an aqueous solvent mixture. 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.