Adhesive Patch Antioxidant Stabilization
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Solution Overview
Problem
Conventional patches containing butorphanol and its pharmaceutically acceptable salts often generate butorphanol oxidants during manufacturing and storage, which are degradation products that must be controlled to ensure drug safety and efficacy, as per International Council for Harmonisation guidelines, necessitating a method to inhibit their generation effectively.
Innovation Solution
Incorporating an antioxidant with a sulfur atom, specifically 2-mercaptobenzimidazole, into the adhesive layer of the patch, along with a rubber-based or silicone-based adhesive base, to significantly reduce the formation of butorphanol oxidants and prevent crystal precipitation, thereby enhancing the stability and safety of the patch.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If butorphanol is used in a patch adhesive layer, then analgesic efficacy is achieved, but butorphanol oxidant degradation products are generated during manufacturing and storage
Solution Approach 1:
The patent introduces 2-mercaptobenzimidazole as an intermediary antioxidant substance in the adhesive layer that mediates between butorphanol and oxygen, preventing direct oxidation of butorphanol while maintaining drug efficacy. The sulfur-containing antioxidant acts as a sacrificial agent that reacts with oxidizing conditions rather than allowing butorphanol degradation
Solution Approach 2:
The patent changes the chemical composition parameters of the adhesive layer by incorporating specific antioxidants (2-mercaptobenzimidazole) and selecting appropriate adhesive bases (rubber-based or silicone-based) with specific properties. This parameter modification transforms the adhesive layer from an oxidizing environment to a protective, antioxidant environment that preserves butorphanol stability
2Object-affected harmful factors
If conventional antioxidants are used in the adhesive layer, then oxidation resistance is improved, but crystal precipitation of butorphanol may occur
Solution Approach 1:
The patent changes the chemical parameters by selecting 2-mercaptobenzimidazole with specific molecular properties (sulfur-containing structure, particular solubility characteristics) that differ from conventional antioxidants. This parameter change allows the antioxidant to function without inducing crystal precipitation, as the specific chemical structure maintains butorphanol in solution while providing antioxidant protection
Solution Approach 2:
The patent creates a composite adhesive layer system combining 2-mercaptobenzimidazole antioxidant with rubber-based or silicone-based adhesive bases. This composite formulation achieves synergistic effects where the adhesive base provides structural integrity and the antioxidant provides oxidation protection without causing precipitation, resolving the contradiction between oxidation resistance and compositional stability
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 use of 2-mercaptobenzimidazole in the adhesive layer effectively inhibits the generation of butorphanol oxidants and prevents crystal precipitation, resulting in a patch with improved long-term stability and safety, maintaining skin permeability and adhesive properties.
Implementation Method 1
the adhesive layer contains an antioxidant containing a sulfur atom in its molecule, wherein the antioxidant containing a sulfur atom in its molecule is 2-mercaptobenzimidazole... generates almost no butorphanol oxidant and also can remarkably inhibit the generation of the butorphanol oxidant even for a long-term storage
Implementation Method 2
the adhesive layer (in particular, the adhesive layer containing a rubber-based adhesive base) in such a patch is also sufficiently inhibited from precipitating crystals (crystal precipitation of free forms of butorphanol)
Data Source
AI summary
A patch comprises a backing layer and an adhesive layer, wherein the adhesive layer contains at least one selected from the group consisting of butorphanol and pharmaceutically acceptable salts thereof, and contains an adhesive base and an antioxidant containing a sulfur atom in its molecule.