Buprenorphine Patch Adhesive Composition for 7-Day Delivery
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Solution Overview
Problem
Existing transdermal therapeutic systems (TTS) for buprenorphine administration face issues with skin irritation and high drug amounts, leading to potential illicit use and waste, while maintaining a convenient once-weekly exchange mode is desirable.
Innovation Solution
A transdermal therapeutic system comprising a buprenorphine-containing self-adhesive layer with a buprenorphine-impermeable backing layer and a pressure-sensitive adhesive layer, incorporating carboxylic acids or levulinic acid to solubilize buprenorphine, providing a smaller area of release and effective pain relief for 7 days.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If a conventional TTS with large area of release is used to deliver sufficient buprenorphine for 7 days, then the duration of action is maintained, but the amount of drug required increases leading to potential illicit use and waste
Solution Approach 1:
The patent changes the chemical parameters of the adhesive system by introducing carboxylic acids (oleic, linoleic, linolenic, or levulinic acid) that can solubilize buprenorphine. This chemical parameter change enables the drug to be delivered from a smaller total amount while maintaining the 7-day duration of action, thereby reducing the quantity of buprenorphine required in the TTS.
2Loss of substance
If the amount of buprenorphine in the TTS is reduced to minimize waste and illicit use potential, then drug waste is reduced, but the area of release must be minimized which may affect delivery efficiency
Solution Approach 1:
By changing the chemical composition parameters of the adhesive layer to include carboxylic acids with solubilizing capabilities, the patent achieves efficient drug delivery from a smaller area of release. The carboxylic acids enhance the solubility and release characteristics of buprenorphine, allowing the TTS to maintain therapeutic effectiveness with reduced drug amounts and smaller application area.
3Quantity of substance
If a high potency formulation is used to reduce the amount of buprenorphine required, then the quantity of drug is reduced, but skin irritation may increase
Solution Approach 1:
The patent introduces carboxylic acids as intermediary substances that mediate between the buprenorphine and the skin. These acids solubilize the high potency buprenorphine formulation, creating a more compatible interface with skin tissue. The carboxylic acids act as buffers and solubilizing agents that reduce the direct irritant effect of concentrated buprenorphine while maintaining its therapeutic potency.
4Ease of operation
If the TTS is designed for once-weekly exchange to improve convenience, then ease of operation is improved, but the system must maintain stable drug release over 7 days which increases complexity
Solution Approach 1:
The patent merges the adhesive function and drug delivery function into a single integrated pressure-sensitive adhesive layer. The carboxylic acid-buprenorphine complex is incorporated directly into the pressure-sensitive adhesive matrix, eliminating the need for separate rate-controlling membranes or reservoirs. This merging simplifies the overall device structure while maintaining stable 7-day release characteristics and once-weekly exchange convenience.
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 system reduces skin irritation and drug waste, maintains a weekly exchange mode, and ensures effective pain relief with a smaller amount of buprenorphine, enhancing patient compliance and reducing illicit use potential.
Implementation Method 1
a carboxylic acid selected from the group consisting of oleic acid, linoleic acid, linolenic acid, levulinic acid and mixtures thereof, in an amount sufficient so that said analgesically effective amount of buprenorphine (e.g. buprenorphine base) is solubilized therein to form a mixture
Data Source
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AI summary
The invention relates to transdermal therapeutic system for the transdermal administration of buprenorphine, comprising a buprenorphine-containing self- adhesive layer structure comprising A) a buprenophihine-impermeable backing layer, and B) a buprenorphine-containing pressure-sensitive adhesive layer on said buprenorphine-impermeable backing layer, the adhesive layer comprising a) at least one polymer-based pressure-sensitive adhesive, b) an analgesically effective amount of buprenorphine base or a pharmaceutically acceptable salt thereof, and c) a carboxylic acid selected from the group consisting of oleic acid, linoleic acid and linolenic acid, levulinic acid and mixtures thereof, in an amount sufficient so that said analgesically effective amount of buprenorphine is solubilized therein to form a mixture, and the carboxylic acid buprenorphine mixture forms dispersed deposits in the said pressure-sensitive adhesive, wherein said buprenorphine-containing pressure-sensitive adhesive layer is the skin contact layer.