Asenapine Transdermal Patch Sustained Release
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Solution Overview
Problem
Current asenapine administration methods, particularly sublingual tablets, are associated with unpleasant side effects, poor patient compliance due to frequent dosing, and difficulties in monitoring and administration, especially in institutionalized or incapable patients.
Innovation Solution
A transdermal therapeutic system (TTS) comprising a self-adhesive layer structure with a backing layer and an asenapine-containing matrix layer, which includes asenapine, a polymer such as acrylic polymers, and medium chain triglycerides, designed to provide improved skin adhesion and sustained release of asenapine for up to 7 days.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If sublingual tablets are used for asenapine administration, then bioavailability is improved by avoiding first-pass metabolism, but patient compliance deteriorates due to frequent dosing requirements
Solution Approach 1:
The transdermal therapeutic system provides continuous delivery of asenapine through the skin, maintaining steady plasma concentrations over extended periods (up to 7 days). This eliminates the fluctuating concentration profile associated with sublingual tablets and the need for frequent dosing, thereby improving patient compliance while maintaining reliable drug delivery.
2Speed
If sublingual administration is used, then rapid absorption is achieved with peak concentrations within 0.5-1.5 hours, but plasma concentration fluctuation increases leading to multiple daily doses
Solution Approach 1:
The transdermal system provides continuous, controlled release of asenapine through the skin, eliminating the rapid peak-and-trough concentration profile characteristic of sublingual administration. This results in stable plasma concentrations without the need for multiple daily doses.
Solution Approach 2:
The transdermal therapeutic system enables dosing at extended intervals (once weekly or less frequently), transforming the periodic dosing frequency from multiple times daily to once per week or longer, thereby improving compliance while maintaining therapeutic efficacy.
3Device complexity
If passive transdermal delivery is implemented, then TTS complexity is reduced compared to active transportation methods, but achieving sufficient permeation rate for therapeutic doses becomes challenging
Solution Approach 1:
The patent optimizes key formulation parameters including polymer composition, plasticizer ratios, and drug load to achieve the desired balance between adhesion and permeation. By carefully adjusting these parameters, the system attains sufficient asenapine permeation rates through passive diffusion while maintaining simple TTS structure and manufacturing.
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 improved skin adhesion and sustained release of asenapine, reducing plasma concentration fluctuations and enhancing patient compliance by allowing less frequent dosing, while also minimizing side effects compared to sublingual administration.
Implementation Method 1
Passive transport of active agents from a transdermal therapeutic system (TTS) through the skin makes use of the driving force based on the concentration gradient between the concentration of active agent in the transdermal system and on the outer surface of the skin and the concentration in the blood stream.
Implementation Method 2
The blood plasma concentration thus exhibits a certain degree of fluctuation with peaks about 1 hour post-dose, followed by a concentration decrease resulting in a low point just before the next dose, even in steady state. The relatively rapid concentration decrease also inevitably leads to multiple daily doses
Data Source
AI summary
The present invention relates to transdermal therapeutic systems (TTS) for the transdermal administration of asenapine comprising a self-adhesive layer structure containing a therapeutically effective amount of asenapine, such asenapine TTS for use in a method of treatment, processes of manufacture of such TTS as well as asenapine and transdermal therapeutic systems containing asenapine for use in a method of treatment and to a method of treating a human patient by transdermal administration of asenapine.