Memantine Transdermal Patch Sustained Release
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Solution Overview
Problem
Current transdermal therapeutic systems for treating central nervous system diseases, such as Alzheimer's, have limitations in maintaining pharmacologically effective plasma concentrations for an extended period, requiring frequent administration and high care efforts, and existing dosage forms are not suitable for achieving systemic concentrations effectively.
Innovation Solution
A transdermal therapeutic system (TTS) administering memantine in the form of its free base or physiologically compatible salt/prodrug, with a backing impermeable to the active ingredient, an active-ingredient-containing layer, and a release liner, designed to maintain effective plasma concentrations for at least 12 hours and up to several days, reducing the need for frequent administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral dosage forms (tablets, drops) are used for memantine administration, then the medication can be effectively absorbed systemically, but the administration requires frequent dosing multiple times per day and strict supervision
Solution Approach 1:
The transdermal therapeutic system enables continuous drug delivery through the skin over extended periods (up to 72 hours), eliminating the need for multiple daily dosing administrations. The controlled release mechanism maintains steady plasma concentrations continuously, reducing administration frequency from multiple times daily to once or twice daily, thereby improving ease of operation while maintaining pharmacological effectiveness.
Solution Approach 2:
The transdermal patch acts as an intermediary delivery system between the drug and the bloodstream. Through the skin (an intermediary barrier), the system transports memantine from the patch into the systemic circulation, providing controlled and sustained release. This intermediary approach bypasses the need for direct oral administration, reducing the burden of frequent dosing and supervision while maintaining reliable pharmacological effect.
2Reliability
If oral dosage forms are used, then the medication can be administered, but the strict therapy schedule and need for supervision result in high therapy costs and care effort
Solution Approach 1:
The transdermal system provides continuous drug delivery over extended periods (up to 72 hours), replacing the need for strict multiple-times-daily scheduling. This continuous action reduces the complexity of therapy management and care requirements while maintaining reliable therapeutic effect through sustained plasma concentrations.
Solution Approach 2:
The transdermal patch is designed for self-administration by the patient or caregiver, eliminating the need for complex supervision and monitoring of dosing schedules. The patch is applied once or twice daily and automatically delivers the medication through controlled release, reducing the complexity of care requirements and therapy management while ensuring consistent therapeutic effect.
3Ease of operation
If existing transdermal systems are used, then transdermal delivery is achieved, but they cannot maintain pharmacologically effective plasma concentrations for extended periods
Solution Approach 1:
The transdermal patch is designed with a predetermined drug reservoir and controlled release mechanism that is prepared in advance. The patch contains sufficient memantine to maintain effective plasma concentrations for extended periods (up to 72 hours) from the moment of application, eliminating the need for frequent reapplication and ensuring prolonged duration of action while maintaining ease of transdermal delivery.
Solution Approach 2:
The system modifies the release parameters of the drug by controlling the diffusion and permeation rates through the skin. By adjusting the patch design, drug concentration, and release mechanism, the system achieves extended duration of action (up to 72 hours) while maintaining effective plasma concentrations, overcoming the limitation of existing transdermal systems that cannot sustain delivery for such extended periods.
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 TTS achieves sustained pharmacologically effective plasma concentrations of memantine for extended periods, minimizing the frequency of administration and care requirements, while maintaining a low interindividual variability and controlled release rates, thus enhancing therapeutic efficacy and safety.
Implementation Method 1
Transdermal administration of memantine... a transdermal therapeutic system (TTS) for administering the active ingredient memantine... achieves, in the blood plasma of the individual requiring treatment, the following active ingredient concentrations
Data Source
AI summary
The invention relates to transdermal therapeutic systems (TTS) which include, as active ingredient, the NMDA receptor antagonist memantine or one of its physiologically compatible salts. The TTSs can be produced and used for treating diseases of the central nervous system.