Transdermal Patch Formulation for Pain Relief
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Solution Overview
Problem
Current transdermal anaesthetic and analgesic formulations, particularly those using lidocaine, face challenges such as poor skin penetration, short duration of action, and limited potency, necessitating improved delivery systems for neuropathic and nociceptive pain management.
Innovation Solution
A transdermal patch formulation comprising ropivacaine or an opioid, a pharmaceutically acceptable adhesive, and additional excipients like penetration enhancers, hydrophilic materials, and carrier oils, which enhance skin permeation and solubility, resulting in a formulation with an in vitro human skin permeation rate greater than 1.8 µg/cm²/h.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional transdermal anaesthetic formulations (e.g., lidocaine) are used, then transdermal delivery is achieved, but skin penetration is poor and duration of action is short
Solution Approach 1:
The patent changes the chemical parameters of the formulation by incorporating specific penetration enhancers (e.g., azone, oleic ethers, terpenes, ethoxy ethanols) and carrier oils (e.g., sorbitan monooleate, triglycerides of caprylic/capric acid, propylene glycol dicaprylate/dicaprate) to modify the physical-chemical properties of the anaesthetic formulation, thereby improving skin penetration and extending duration of action
Solution Approach 2:
The patent creates a composite transdermal formulation by combining ropivacaine or opioid with multiple excipients including penetration enhancers, hydrophilic materials, and carrier oils in a synergistic formulation that enhances both penetration and duration of action simultaneously
2Quantity of substance
If conventional transdermal formulations are used, then pain relief is provided, but drug potency is limited
Solution Approach 1:
The patent optimizes the concentration and formulation parameters of the anaesthetic agent (ropivacaine or opioid) combined with penetration enhancers to achieve higher drug potency while maintaining reliable skin penetration through the enhanced formulation system
3Ease of operation
If transdermal delivery is implemented, then localized pain suppression is achieved, but plasma levels are reduced which may limit efficacy
Solution Approach 1:
The patent modifies the formulation parameters to optimize the balance between localized delivery and plasma level maintenance, using enhanced penetration agents to ensure sufficient drug reaches the target site while controlling systemic absorption to achieve therapeutic plasma levels
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 formulation achieves improved skin penetration and prolonged pain relief by increasing the permeation rate of ropivacaine or opioids, addressing the limitations of existing formulations with enhanced drug potency and duration of action.
Implementation Method 1
a penetration enhancer selected from sugar fatty acid esters and ethers, C8-C18 fatty alcohol, azone, oleic ethers, terpenes and ethoxy ethanols
Implementation Method 2
a hydrophilic material; and additionally a carrier oil selected from sorbitan monooleate, sorbitan trioleate, triglycerides of carprylic/capric acid, propylene glycol dicaprylate/dicaprate, ethoxy diglycol, propylene glycol monocaprylate, glycerol monooleate, lanolin, acetylated lanolin, polyethylene glycol lanolin, glycerol monocaprylate/caprate, propylene glycol laurate, and/or mono- or diglycerides of capric acid
Data Source
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AI summary
The present invention relates to a transdermal patch comprising a pharmaceutical formulation, the formulation comprising ropivacaine or an opioid, a pharmaceutically-acceptable adhesive and optionally one or more excipients selected from the group consisting of carrier oils, penetration enhancers and hydrophilic materials. The present invention also relates to methods of preparation of such a pharmaceutical formulation, as well as the use of such a transdermal patch in the treatment of pain (e.g. nociceptive and/or neuropathic pain).