Buprenorphine Transdermal Patch Sustained Release via Alpha-Hydroxy Acid

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Solution Overview

Problem

Current oral analgesics require frequent administration due to short duration of pain relief, leading to gastrointestinal irritation and drug metabolism issues, while transdermal delivery offers advantages but lacks sustained release options for buprenorphine.

Innovation Solution

Extended transdermal delivery devices combining buprenorphine with an α-hydroxy acid and a pressure-sensitive adhesive in a single matrix layer, providing a sustained release of buprenorphine for seven days or longer, maintaining 90% or greater of peak flux and delivering 75% or more of the drug over the extended period.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If oral analgesics are administered multiple times per day to maintain sustained amount, then pain relief duration is improved, but gastrointestinal irritation and drug metabolism issues worsen

Engineering Contradiction:

Improvepain relief durationVSAvoidgastrointestinal irritation

Core Design Contradiction:

Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent introduces the skin as an intermediary route for drug delivery, using transdermal patches as mediators to deliver buprenorphine systematically. This bypasses the gastrointestinal tract entirely, eliminating GI irritation while maintaining sustained pain relief through controlled transdermal absorption into the bloodstream

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the oral administration mechanical system (ingestion, digestion, absorption through GI tract) with a transdermal delivery system. The patch uses pressure-sensitive adhesive mechanics and controlled diffusion through skin layers to achieve sustained drug release without gastrointestinal contact

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Quantity of substance

If oral analgesics are administered multiple times per day, then sustained amount of drug is maintained, but administration frequency and complexity worsen

Engineering Contradiction:

Improvesustained amount of drugVSAvoidadministration frequency

Core Design Contradiction:

Quantity of substanceVSEase of operation

Solution Approach 1:

The transdermal patch provides continuous drug delivery over extended periods (3-7 days or longer) through sustained diffusion of buprenorphine from the pressure-sensitive adhesive matrix through the skin. This continuous action maintains therapeutic drug levels without requiring repeated administrations, simplifying the dosing regimen to a single application

Inventive Principle:

Principle #20Continuity of useful action

Solution Approach 2:

The patch is applied in advance and pre-loaded with sufficient buprenorphine to maintain therapeutic levels throughout the intended wear period. The drug is already positioned in the adhesive matrix ready for controlled release, eliminating the need for repeated dosing actions by the patient

Inventive Principle:

Principle #10Preliminary action

3Reliability

If transdermal delivery is used for buprenorphine, then avoidance of first pass metabolism and controlled delivery are achieved, but extended release duration is insufficient

Engineering Contradiction:

Improveavoidance of first pass metabolismVSAvoidrelease duration

Core Design Contradiction:

ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent modifies the formulation parameters of the transdermal patch by incorporating specific ratios of buprenorphine to penetration enhancers and using pressure-sensitive adhesive matrices with controlled drug loading. These parameter changes enable the system to maintain stable drug release over extended periods (3-7+ days) while preserving the advantages of transdermal delivery

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patch uses a composite pressure-sensitive adhesive matrix combining buprenorphine with penetration enhancers and adhesive polymers. This composite structure enables both the reliability of transdermal delivery (avoiding first-pass metabolism) and extended release duration through the synergistic properties of the composite material system

Inventive Principle:

Principle #40Composite materials

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 solution provides prolonged pain relief with reduced frequency of administration, minimizing gastrointestinal irritation and drug metabolism issues, while maintaining a consistent and high buprenorphine flux, ensuring effective and sustained analgesia.

Implementation Method 1

Transdermal delivery systems are patches that contain an active agent that are adhered to the skin to deliver the active agents by percutaneous absorption. After a transdermal patch is applied to the skin, the active agent contained in the patch passes through, or permeates the skin and can reach its site of action through a systemic blood flow.

Methodology Applied

Scientific EffectPercutaneous absorption: Permeation

Data Source

PatentUS11547676B2Extended buprenorphine transdermal delivery compositions and methods for using the same

Publication Date: 2023.01.10 TEIKOKU SEIYAKU CO LTD

AI summary

Aspects of the invention include extended transdermal delivery devices for delivering buprenorphine to a subject for an extended period of time, where the transdermal delivery devices include buprenorphine, an α-hydroxy acid and a pressure sensitive adhesive. In certain instances, buprenorphine, α-hydroxy acid and the pressure sensitive adhesive are provided as a single matrix layer formulation. Also provided are methods of using the subject extended transdermal delivery devices, as well as kits containing the extended transdermal delivery device.