Buccal Paracetamol Hydroalcoholic Solution for Rapid Absorption
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Solution Overview
Problem
Current oral administration of paracetamol results in significant losses and metabolism during the digestive and hepatic pass effects, leading to reduced bioavailability and delayed therapeutic action due to its lipophilic nature and short half-life, necessitating higher doses and longer latency periods for effectiveness.
Innovation Solution
A galenical form in the form of a stable, completely dissolved hydroalcoholic solution with at least 10% alcohol by mass, allowing rapid absorption through mucous membranes in the buccal cavity and oropharynx, facilitating immediate systemic absorption without digestive or hepatic passage, using a hydroalcoholic solution with a variable alcohol content between 10° and 70° to promote accelerated permucosal absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If paracetamol is administered orally, then it can be easily taken by the patient, but the bioavailability is reduced due to first digestive pass and first hepatic pass effects
Solution Approach 1:
The patent uses the buccal cavity mucous membrane as an intermediary pathway for drug absorption, bypassing the digestive and hepatic systems. The paracetamol is formulated in a hydroalcoholic solution that facilitates rapid permeation through the buccal mucosa directly into the systemic circulation, eliminating the first-pass metabolic effects while maintaining ease of administration.
2Quantity of substance
If paracetamol is administered orally at standard doses, then adequate dosage can be given, but the latency period before therapeutic effectiveness is long due to digestive absorption and tissue diffusion
Solution Approach 1:
The patent extracts the paracetamol from the traditional oral digestive pathway and delivers it directly to the systemic circulation through buccal mucosal absorption. This extraction of the drug from the slow digestive-absorptive pathway and placement into a rapid transmucosal pathway eliminates the latency period while maintaining adequate dosing.
3Quantity of substance
If paracetamol is administered orally, then it can be distributed throughout the organism, but the short half-life results in dilution and reduced effectiveness at central receptors
Solution Approach 1:
The patent implements preliminary action by achieving rapid peak concentrations at the central receptors through direct buccal absorption. By delivering the drug immediately to the systemic circulation and specifically targeting rapid CNS penetration, the therapy achieves effective concentrations at the site of action before significant distribution dilution occurs, thereby extending the effective duration of action.
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
Enables immediate and effective analgesic and antipyretic action by ensuring nearly instantaneous absorption and distribution of paracetamol to the central circulation, overcoming the limitations of traditional oral administration, with reduced dose requirements and rapid onset of action, similar to intravenous delivery but without the need for antimicrobial preservatives and with simpler production and stability.
Implementation Method 1
allow fast absorption of said active ingredient through the mucous membranes of the buccal cavity and/or the oropharynx
Implementation Method 2
the alcohol, present at at least 10% by mass, does not play only the role of solvent, but also that of promoter of an accelerated permucosal absorption
Data Source
AI summary
A galenical form for the transmucous administration of at least one active ingredient, characterized in that the active ingredient is paracetamol in a stable and complete dissolved state in a hydroalcoholic solution that includes at least 10% by mass of alcohol so as to allow fast absorption of the active ingredient through the mucous membranes of the buccal cavity and/or the oropharynx. A process for production and the uses of the galenical form are also disclosed.