Oral Mucosal Fentanyl Patch for Rapid Pain Relief
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Solution Overview
Problem
Current fentanyl preparations for mucous membranes in the oral cavity are either slow to achieve effective serum concentration, cause discomfort, and have difficulty in controlling drug absorption, especially for acute pain management, as they often result in drug absorption continuing after the patch is removed and can lead to unpredictable serum concentration levels.
Innovation Solution
A patch design that includes a drug layer with fentanyl or its salt, methyl vinyl ether-maleic anhydride copolymer as an adhesive, and hydroxypropyl cellulose or hydroxyethyl cellulose as a thickener, laminated with a water-insoluble support layer and a backing, allowing for quick absorption, reduced gastrointestinal transfer, and easy removal.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If a transdermally absorbable sustained release preparation containing fentanyl is used, then the effective serum concentration is retained for 24 to 72 hours, but the absorption is mild and quick analgesic effect cannot be obtained
Solution Approach 1:
The patent changes the absorption parameters by using oral mucosal administration instead of transdermal administration. The drug layer contains fentanyl at a concentration of 0.1-10% w/w with specific excipients that control release rate, achieving both rapid absorption (peak serum concentration within 15-30 minutes) and sustained effect (4-12 hours) through optimized drug concentration and release kinetics
2Duration of action of stationary object
If a transdermally absorbable preparation containing fentanyl is applied, then sustained release is achieved, but fentanyl remains in the corneum after removal and absorption continues
Solution Approach 1:
The patent extracts the drug delivery site from the transdermal route and relocates it to the oral mucosa. The drug layer is applied directly to the oral mucosal surface where rapid absorption occurs, and the preparation can be completely removed by the patient when needed, eliminating the residual drug problem in the corneum and allowing precise control of serum concentration
3Ease of operation
If a candy-type preparation with a stick is used for oral mucosal administration, then noninvasive administration is achieved, but the preparation causes uncomfortable feeling and drug transfer to gastrointestinal tract occurs
Solution Approach 1:
The patent uses a thin film drug layer (50-200 μm thickness) that can be applied directly to the oral mucosa without a stick or candy form. This thin film design eliminates the uncomfortable feeling associated with lollipop preparations while minimizing drug transfer to the gastrointestinal tract through optimized adhesion to the mucosal surface
Solution Approach 2:
The patent applies the drug locally to the oral mucosa through a targeted drug layer rather than systemic administration. The drug is confined to the application site on the oral mucosa, providing localized absorption that avoids gastrointestinal transfer while maintaining ease of administration
4Ease of operation
If a patch for oral mucosa is designed with water-soluble adhesive, then easy application is achieved, but drug release to other parts of oral cavity occurs
Solution Approach 1:
The patent uses a composite adhesive system combining water-soluble adhesive (for easy application and mucosal adhesion) with water-insoluble adhesive (for drug containment). This composite material structure allows the preparation to be easily applied and adhere well to the oral mucosa while preventing drug migration to other areas of the oral cavity and gastrointestinal tract
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 patch achieves rapid increase in serum fentanyl concentration, minimizes drug absorption outside the application site, and allows for easy control of serum levels, making it suitable for acute pain management and safe use as a rescue medication during cancer pain therapy.
Implementation Method 1
a drug layer which contains fentanyl or its salt as an active ingredient and shows adhesivity due to being dissolved in or swelled with water
Data Source
AI summary
To provide a patch containing fentanyl for mucous membrane of the oral cavity (oral transmucosal fentanyl), which rapidly increases the serum concentration of the drug, is easy in handling and is superior in safety. The patch can be prepared by laminating on one side of a drug layer which contains fentanyl or its salt as an active ingredient, methyl vinyl ether-maleic anhydride copolymer as an adhesive, and at least one substance selected from the group consisting of hydroxypropylcellulose, hydroxypropylmethylcellulose and hydroxyethylcellulose as a thickener, a support layer hardly soluble or insoluble in water, and a backing in this order.