Pramipexole Transdermal Patch Using Ionic Liquid Solvent System
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Solution Overview
Problem
Current transdermal patches for dopamine receptor agonists like pramipexole face challenges in solubility and stability due to the poorly soluble nature of pramipexole hydrochloride, leading to issues such as precipitation and adverse reactions, and there is a need for a long-lasting, non-irritating formulation that enhances percutaneous absorption.
Innovation Solution
A nonaqueous transdermal patch is developed using a C14-C18 fatty acid-based ionic liquid and a divalent alcohol, combined with a fatty acid ester, which improves solubility and stability of pramipexole, and includes a filler to enhance drug release and absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If pramipexole hydrochloride is used as the active ingredient in a transdermal patch, then the therapeutic effect for Parkinson's disease and restless legs syndrome is achieved, but the poor solubility of pramipexole hydrochloride causes precipitation and stability issues
Solution Approach 1:
The patent introduces a specific solvent system comprising propylene glycol (10-40 wt%), diethyl sebacate (5-30 wt%), and isopropyl myristate (5-30 wt%) as intermediary substances to mediate the solubility of pramipexole hydrochloride. This solvent mixture acts as a bridge between the poorly soluble active ingredient and the transdermal patch matrix, preventing precipitation while maintaining stability during storage and application.
2Reliability
If conventional transdermal patches are used for dopamine receptor agonists, then drug delivery is achieved, but adverse reactions and skin irritation occur
Solution Approach 1:
The patent modifies the chemical parameters of the transdermal patch formulation by selecting specific solvents and co-solvents with appropriate polarity, viscosity, and skin penetration properties. The propylene glycol/diethyl sebacate/isopropyl myristate system creates optimal parameters for drug solubility and controlled release, reducing skin irritation while maintaining therapeutic efficacy.
3Ease of operation
If pramipexole is formulated for transdermal delivery, then percutaneous absorption is needed, but the poorly soluble nature of the drug hinders effective absorption
Solution Approach 1:
The patent creates a composite solvent system combining three different chemical agents (propylene glycol, diethyl sebacate, and isopropyl myristate) with complementary properties. This composite material approach leverages the hydrophilic nature of propylene glycol, the lipophilic characteristics of diethyl sebacate and isopropyl myristate, and their synergistic interaction to achieve both solubility and enhanced percutaneous absorption of pramipexole hydrochloride.
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 patch provides a stable and effective transdermal delivery of pramipexole with improved percutaneous absorption and reduced precipitation, maintaining stability and efficacy over time without significant yellowing or adverse reactions.
Implementation Method 1
A nonaqueous transdermal patch is developed using a C14-C18 fatty acid-based ionic liquid and a divalent alcohol, combined with a fatty acid ester, which improves solubility and stability of pramipexole
Implementation Method 2
The patch provides a stable and effective transdermal delivery of pramipexole with improved percutaneous absorption
Implementation Method 3
includes a filler to enhance drug release and absorption
Data Source
AI summary
The purpose of the present invention is to provide a nonaqueous tape that is stable and has high percutaneous absorption performance, and that contains pramipexole hydrochloride, which is slightly soluble in organic solvents and has high crystallinity. The present invention could produce a nonaqueous tape that is stable and has high percutaneous absorption performance by dissolving pramipexole, using a combination of a fatty acid ionic liquid and a divalent alcohol and a fatty acid ester. As a result, it has become possible to provide a transdermal patch (tape) containing pramipexole for the treatment of Parkinson's disease with which the problems associated with a conventional water-containing poultice of discoloration of the preparation and stability of the pramipexole can be solved.