Solid Anesthetic Lozenge for Rapid Transmucosal Delivery
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Solution Overview
Problem
Current dental anesthesia methods, including creams, gels, and patches, suffer from slow induction times, superficial anesthesia, and low active substance load rates, making them inadequate for rapid and deep anesthesia, especially for procedures involving enamel, dentin, or channels, and pose challenges with needle phobia and waste management.
Innovation Solution
A pharmaceutical product comprising a polymer phase of poly(vinyl) pyrrolidone (PVP) and carboxymethylcellulose (CMC) that allows for a high load rate of anesthetics (>40% by mass) and rapid dissolution on contact with water, providing flexible, hygroscopic, and adhesive properties for efficient transdermal or transmucosal delivery without leaving residues.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If cream, gel or wet patch type products based on anesthetic formulations are used, then the anesthesia induction time is slow (typically 1 hour), but the resulting anesthesia is a light surface anesthesia that is rarely sufficient for routine care procedures
Solution Approach 1:
The patent changes the physical state parameter of the anesthetic formulation from semi-solid (cream/gel) to solid (lozenge/patch), and modifies the polymer matrix composition to achieve rapid dissolution. This parameter change enables both fast induction (within minutes) and deep anesthesia while maintaining high active substance load rates up to 65% by mass
Solution Approach 2:
The patent uses a composite polymer system combining poly(vinyl) pyrrolidone (PVP) and carboxymethylcellulose (CMC) in specific ratios (PVP: 25-53%, CMC: 5-30%). This composite material provides both rapid dissolution kinetics and high anesthetic loading capacity, resolving the contradiction between induction speed and substance load rate
2Speed
If needle-based devices are used to inject anesthetics, then rapid and deep anesthesia can be achieved, but sharp biological waste must be disposed of through specialized channels and needle phobia affects a significant portion of the population
Solution Approach 1:
The patent replaces the mechanical needle injection system with a non-invasive solid formulation (lozenge or patch) that delivers anesthetic through dissolution and passive diffusion. This substitution eliminates needles entirely, removing the source of patient anxiety and sharp waste while maintaining effective anesthetic delivery through the polymer matrix dissolution mechanism
3Quantity of substance
If the pharmaceutical product comprises high content of active substance (>40% by mass), then rapid and deep anesthesia is achieved, but the formulation complexity increases
Solution Approach 1:
The patent optimizes the polymer-to-anesthetic ratio and selects specific polymer types (PVP and CMC) with known dissolution properties to achieve high anesthetic loading (40-65%) while maintaining simple processing. The formulation complexity is managed by controlling dissolution rate parameters rather than adding complex delivery mechanisms
Solution Approach 2:
The patent uses a binary polymer system (PVP + CMC) that is simple in composition but effective in function. This composite approach allows high anesthetic loading while maintaining ease of manufacture through straightforward mixing and molding processes, avoiding the need for complex encapsulation or multi-layer structures
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 product achieves rapid and deep anesthesia with high active substance release in less than an hour, addressing the limitations of existing formulations by ensuring effective pain management without the drawbacks of needle-based administration and residue generation.
Implementation Method 1
the polymeric phase used in the pharmaceutical product according to the invention consists of poly(vinyl) pyrrolidone (PVP) and carboxymethylcellulose (CMC) or one of its salts
Implementation Method 2
capable of swelling with water or the aqueous solution and then dissolving completely, i.e. without generating residues, thus releasing the anesthetic it contains
Implementation Method 3
local anesthesia temporarily and reversibly stops the excitability of sensory nerve fibers... passive diffusion of active substances at the topical, transdermal, transgingival and/or transmucosal level
Data Source
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AI summary
The present invention relates to a pharmaceutical product comprising between 40% and 65% by mass of at least one active substance; between 25% and 53% by mass of poly(vinyl pyrrolidone) (PVP); and between 5% and 30% by mass of carboxymethylcellulose (CMC) or a salt thereof; the % by mass being expressed relative to the total dry mass of said product. The present invention also relates to a packaging in which this product is stored, to a method for preparing this product and to the medical use thereof, in particular as an anaesthetic or for promoting or improving healing.